5-AMINOINDENO(1,2-C)PYRAZOL-4-ONES AS ANTI-CANCER AND ANTI-PROLIFERATIVE AGENTS

Abstract: The present invention relates to the synthesis of a new class of indeno [1,2-c]pyrazol-4-ones of formula (I), that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits known as cyclines A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.

Description: 5-AMINOINDENO(l,2~C)PYRAZOL-4-ONES AS ANTI-CANCER AND ANTI-PROLIFERATTVE AGENTS FIELD OF THE INVENTION This invention relates generally to novel 5- substituted-indeno [1, 2-c] pyrazol-4-ones which are useful as cyclin dependent kinase (cdk) inhibitors, pharmaceutical compositions comprising the same, methods for using the same for treating proliferative diseases, and intermediates and processes for making the same. BACKGROUND OF THE INVENTION One of the most important and fundamental processes in biology is the division of cells mediated by the cell cycle. This process ensures the controlled production of subsequent generations of cells with defined biological function. It is a highly regulated phenomenon and responds to a diverse set of cellular signals both within the cell and from external sources. A complex network of tumor promoting and suppressing gene products are key components of this cellular signaling process. Over expression of the tumor promoting components or the subsequent loss of the tumor suppressing products will lead to unregulated cellular proliferation and the generation of tumors (Pardee, Science 246:603-608, 1989) . Cyclin dependent kinases (cdks) play a key role in regulating the cell cycle machinery. These complexes consist of two components: a catalytic subunit (the kinase) and a regulatory subunit (the cyclin) . To date, six kinase subunits (cdk 1-7) have been identified along with several regulatory subunits (cyclins A-H) . Each kinase associates with a specific regulatory partner and together make up the active catalytic moiety. Each transition of the cell cycle is regulated by a particular cdk complex: Gl/S by cdk2/cyclin E, cdk4/cyclin Dl and cdk6/cyclinD2 ; S/G2 by cdk2/cyclin A and cdkl/cyclin A; G2/M by cdkl/B. The coordinated activity of these kinases guides the individual cells through the replication process and ensures the vitality of each subsequent generation (Sherr, Cell 73:1059- 1065, 1993; Draetta, Trends Biochem . Sci . 15:378-382, 1990) An increasing body of evidence has shown a link between tumor development and cdk related malfunctions. Over expression of the cyclin regulatory proteins and subsequent kinase hyperactivity have been linked to several types of cancers (Jiang, Proc . Natl . Acad. Sci . USA 90:9026-9030, 1993; Wang, Nature 343:555-557, 1990). More recently, endogenous, highly specific protein inhibitors of cdks were found to have a major affect on cellular proliferation (Kamb et al, Science 264:436-440, 1994; Beach, Nature 336:701-704, 1993) . These inhibitors include pl6 IΝK4 (an inhibitor of cdk4/Dl) , p21 CIP1 (a general cdk inhibitor) , and p27 KIP1 (a specific cdk2/E inhibitor) . A recent crystal structure of p27 bound to cdk2/A revealed how these proteins effectively inhibit the kinase activity through multiple interactions with the cdk complex (Pavletich, Nature 382:325-331, 1996). These proteins help to regulate the cell cycle through specific interactions with their corresponding cdk complexes. Cells deficient in these inhibitors are prone to unregulated growth and tumor formation. This body of evidence has led to an intense search for small molecule inhibitors of the cdk family as an approach to cancer chemotherapy. There are no known examples of molecules related to the current invention which describe 5- subs ti tu ed-indeno [1,2-c] pyrazoles as cdk inhibitors. There is one case describing indeno [1 , 2-c] yrazoles having anticancer activity. There are two other examples which describe indeno [1 , 2-c] pyrazoles having unrelated utilities and structures. A series of indeno [1 , 2-c] pyrazoles having anticancer activity are described in JP 60130521 and JP 62099361 with the following generic structure: No substitution is claimed on the indenophenyl portion of the molecule and the molecules are not indicated to be cdk inhibitors. In addition, we discovered that substitution at the 5-position was critical for cdk inhibitory activity. A series of indeno [1 , 2-c] pyrazoles having herbicidal activity are described in GB 2223946 with the following generic structure: O The above compounds differ from the presently claimed invention in X n is defined as halo, alkyl, haloalkyl, and haloalkoxy; n = 0-2. In addition, Ri is defined as acyl and R2 is defined as alkyl or cycloalkyl. A series of 1- (6 ' -substituted-4 ' -methylquinol-2 ' -yl) -3- methylindeno [1, 2-c] pyrazoles having CNS activity are described by Quraishi, Farmaco 44:753-8, 1989 with the following generic structure: Compounds of this series are not considered to be part of the presently claimed invention. SUMMARY OF THE INVENTION The present invention describes a novel class of indeno [1 , 2-c] pyrazol -4 -ones or pharmaceutically acceptable salt forms thereof that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk 1-7 and their regulatory subunits know as cyclins A-H. It is another object of this invention to provide a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. It is another object of this invention to provide a novel method of treating cancer or other proliferative diseases, which comprises administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti- proliferative agents. These and other objectives have been achieved by the inventors' discovery that compounds of formula (I) : (I) wherein Ri , R2 and X are defined below or pharmaceutically acceptable salts thereof are cyclin dependent kinase inhibitors . DETAILED DESCRIPTION OF PREFERRED EMBODIMENTS The invention pertains to novel cyclin dependent kinase inhibitors (cdks) and specifically, but not exclusively, as inhibitors of cdk/cyclin complexes. The inhibitors of this invention are indeno [1 , 2-c] pyrazol-4 -one analogs. Certain analogs were selective for their activity against cdks and their cyclin bound complexes and were less active against other known serine/threonine kinases such as Protein Kinase A (PKA) and Protein Kinase C (PKC) . In addition, these inhibitors were less active against tyrosine kinases such as c-Abl. As described herein, the inhibitors of this invention are capable of inhibiting the cell -cycle machinery and consequently would be useful in modulating cell -cycle progression, which would ultimately control cell growth and differentiation. Such compounds would be useful for treating subjects having disorders associated with excessive cell proliferation, such as the treatment of cancer, psoriasis, immunological disorders involving unwanted leukocyte proliferation, in the treatment of restinosis and other smooth muscle cell disorders, and the like. The present invention, in a first embodiment, describes a novel compound of formula (I) : (I) or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein: X is selected from the group: 0, S, and NR; R is selected from the group: H, Cι_4 alkyl, and NR 5 R 5a ; R 1 is selected from the group: H, Ci-io alkyl substituted with 0-3 R C , C2-10 alkenyl substituted with 0-3 R C , c 2 - 10 alkynyl substituted with 0-3 R c , -NHR 4 , C3-10 carbocycle substituted with 0-5 R , and 3-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S and substituted with 0-5 R ; R is independently at each occurrence selected from the group: halo, -CN , N 3 , NO2 , C1-4 alkyl, C1- 4 haloalkyl, NR 3 R 3a , =0, OR 3 , COR 3 , CO2R 3 , CONR 3 R 3 , NHC(0)NR 3 R 3a , NHC(S)NR 3 R 3a , NR 3 C (0) OR 3 , NR 3 C (0) R 3 , Sθ2NR 3 R 3a , Sθ2R 3b , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from 0, N, and S; alternatively, when two R a ' s are present on adjacent carbon atoms they combine to form -OCH2O- or -OCH2CH2O-; R is independently at each occurrence selected from the group: halo, -CN, NO2 , C1-4 alkyl, Cι_4 haloalkyl, NR 3 R 3a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , NHC(0)NR 3 R 3a , NHC (S) NR 3 R 3a , Sθ2NR 3 R 3a , and Sθ2R 3b ; R is independently at each occurrence selected from the group: halo, -CN, NO2 , Cl-4 alkyl, Cχ-4 haloalkyl, NR 3 R 3a , NR 5 NR 5 R 5a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , =0, OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , NHC(0)NR 3 R 3a , NHC (S) NR 3 R 3a , S02NR 3 R 3a , S02R 3b , C3-10 carbocycle substituted with 0-5 R a , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from 0, N, and S, substituted 3 with 0-3 R ; R2 is selected from the group: H, Cι_ιo alkyl substituted with 0-3 R C , C2-10 alkenyl substituted with 0-3 R C , C2-10 alkynyl substituted with 0-3 R C , -(CF2) m CF3, C3-10 carbocycle substituted with 0-5 R , and 3-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S and substituted with 0-5 R ; 3 R is selected from the group: H, halo, -CN, NO2 , C1- 4 haloalkyl, NR 5 R 5a , NR 5 NR 5 R 5a , NR 5 C(0)OR 5 , NR 5 C(0)R 5 , =0, OR 5 , COR 5 , CO2R 5 , CONR 5 R 5a , NHC (O) NR 5 R 5a , NHC(S)NR 5 R 5a , Sθ2NR 5 R 5a , Sθ2R 5b , Cι_ 4 alkyl, phenyl, and benzyl ; R a is selected from the group: H, C1-4 alkyl, phenyl, and benzyl ; alternatively, R 3 and R 3a , together with the nitrogen atom to which they are attached, form a heterocycle having 4-8 atoms in the ring containing an additional 0-1 N, S, or O atom and substituted with 0-3 R 3c ; R is selected from the group: H, C1-4 alkyl, phenyl, and benzyl ; R 3c is independently at each occurrence selected from the group: halo, -CN , N 3 , NO2 , C1-4 alkyl, C1-4 haloalkyl, NR 3 R 3b , =0, OR 3 , COR 3 , CO2 3 , CONR 3 R 3b , NHC(0)NR 3 R 3b , NHC(S)NR 3 R 3b , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , Sθ2NR 3 R 3 , Sθ2R 3b , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from 0, N, and S; R 4 is independently at each occurrence selected from the group: H, -CN, C1-4 alkyl, C3 . -4 haloalkyl, NR 3 R 3a , NR 3 C(0)OR 3 , NR C(0)R 3 , OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , NHC(0)NR 3 R 3a , NHC(S)NR 3 R 3a , Sθ2NR 3 R 3a , Sθ2R 3b , C3-10 carbocycle substituted with 0-5 R a , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected 3 from 0, N, and S, substituted with 0-3 R ; R 5 is independently selected from the group: H, C1- 4 alkyl, phenyl and benzyl; R 5a is independently selected from the group: H, C1- 4 alkyl , phenyl and benzyl ; R 5 is independently selected from the group: H, C1-4 alkyl , phenyl and benzyl ; and m is selected from 0, 1, 2, and 3. In a preferred embodiment, the present invention provides a novel compound of formula (I) , wherein: X is selected from the group: 0, S, and NR; R is selected from the group: H, C1-4 alkyl, and NR 5 R 5a ; R 1 is selected from the group: H, C1-5 alkyl substituted with 0-3 R C , C2-5 alkenyl substituted with 0-3 R C , C2-5 alkynyl substituted with 0-3 R c , -NHR 4 , C3-g carbocycle substituted with 0-5 R , and 3-6 membered heterocycle containing from 1-4 heteroatoms selected from 0, N, and S and substituted with 0-5 R ; R is independently at each occurrence selected from the group: halo, -CN, N 3 , NO2 , C1-4 alkyl, C1-4 haloalkyl, NR 3 R 3a , NR 3 C(0)OR 3 , NR 3 C (0) R 3 , =0, OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , NHC(0)NR 3 R 3a , NHC (S) NR 3 R 3a , Sθ2NR 3 R 3a , Sθ2R 3b , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S ; alternatively, when two R a ' s are present on adjacent carbon atoms they combine to form -OCH2O- or -OCH2CH2O- ; R is independently at each occurrence selected from the group: halo, -CN, NO2 , C1-4 alkyl, C1-4 haloalkyl, NR 3 R 3a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , NHC(0)NR 3 R 3a , NHC (S) NR 3 R 3a , Sθ2NR 3 R 3a , and Sθ2R 3b ; R c is independently at each occurrence selected from the group: halo, -CN, NO2 , Cι_4 alkyl, C1-4 haloalkyl, NR 3 R 3a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , NR 5 NR 5 R 5a , =0, OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , NHC(0)NR 3 R 3a , NHC (S) NR 3 R 3a , Sθ2NR 3 R 3a , Sθ2R 3b , C3-10 carbocycle substituted with 0-5 R a , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from 0, N, and S, substituted 3 with 0-3 R ; R 2 is selected from the group: H, C1-5 alkyl substituted with 0-3 Rc , C2-5 alkenyl substituted with 0-3 Rc , C2-5 alkynyl substituted with 0-3 R C , -(CF2)mCF3, C3-6 carbocycle substituted with 0-5 R , and 3-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S and substituted with 0-5 R ; 3 R is selected from the group: H, halo, -CN, NO2 , C1-4 haloalkyl, NR 5 R 5a , NR 5 NR 5 R 5a , NR 5 C(0)OR 5 , NR 5 C(0)R 5 , =0, OR 5 , COR 5 , CO2R 5 , CONR 5 R 5a , NHC (0) NR 5 R 5a , NHC(S)NR 5 R 5a , S02NR 5 R 5a , Sθ2R 5b , Cι_ 4 alkyl, phenyl, and benzyl ; R a is selected from the group: H, C1-4 alkyl, phenyl, and benzyl ; alternatively, R 3 and R 3a , together with the nitrogen atom to which they are attached, form a heterocycle having 4-8 atoms in the ring containing an additional 0-1 N, S, or 0 atom and substituted with 0-3 R 3c ; R is selected from the group: H, C1-4 alkyl, phenyl, and benzyl ; R 3c is independently at each occurrence selected from the group: halo, -CN , N 3 , NO2 , C1-4 alkyl, C1-4 haloalkyl, NR 3 R 3b , =0, OR 3 , COR 3 , CO2R 3 , CONR 3 R 3b , 10 NHC (0) NR 3 R 3 b , NHC ( S ) NR 3 R 3 b , NR 3 C (0) OR 3 , NR 3 C ( 0 ) R 3 , Sθ2NR 3 R 3 , Sθ2 3b , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S; R 4 is independently at each occurrence selected from the group: H, -CN, C1-4 alkyl, C1- 4 haloalkyl, NR R a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , NHC(0)NR 3 R 3a , NHC(S)NR 3 R 3a , Sθ2NR 3 R 3a , Sθ2R 3b , C3-10 carbocycle substituted with 0-5 R a , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected 3 from 0, N, and S, substituted with 0-3 R ; R 5 is independently selected from the group: H, C1-4 alkyl, phenyl , and benzyl ; R 5a is independently selected from the group: H, Cι_ 4 alkyl , phenyl and benzyl ; R 5b is independently selected from the group: H, C1- 4 alkyl, phenyl, and benzyl; and m is selected from 0, 1, 2, and 3. In a more preferred embodiment, the present invention provides a novel compound of formula (I) , wherein: X is selected from the group: 0 and S; R 1 is selected from the group: H, C1-5 alkyl substituted with 0-3 R c , C2-5 alkenyl substituted with 0-3 R c , -NHR 4 , C3-6 carbocycle substituted with 0-5 R , and 3-6 11 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S and substituted with 0-5 R ; R is independently at each occurrence selected from the group: halo, -CN, N 3 , C1-4 alkyl, C1-4 haloalkyl, NR 3 R 3a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , NHC(0)NR 3 R 3a , Sθ2NR 3 R 3a , Sθ2R 3b , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S; alternatively, when two R a ' s are present on adjacent carbon atoms they combine to form -OCH2O- or -OCH2CH 2 O- ; • . R is independently at each occurrence selected from the group: halo, -CN, C1-4 alkyl, C 1 -4 haloalkyl, NR 3R3a, NR 3 C(0)OR 3 , NR 3 C(0)R 3 , OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , NHC(0)NR 3 R 3a , Sθ2NR 3 R 3a , and Sθ2R 3b R is independently at each occurrence selected from the 3 3a group: halo, -CN, C 1 - 4 alkyl, C1- 4 haloalkyl, NR R , NR 5 NR 5 R 5a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , =0, OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , NHC(0)NR 3 R 3a , Sθ2NR 3 R 3a , Sθ2 3b , C3_ιo carbocycle substituted with 0-5 R a , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from 0, N, and S, substituted with 0-3 R ; R 2 is selected from the group: H, C1-.5 alkyl substituted with 0-3 R C , C2-5 alkenyl substituted with 0-3 R , -(CF2)mCF3, C3-6 carbocycle substituted with 0-5 R , and 3-6 membered heterocycle containing from 1-4 12 heteroatoms selected from O, N, and S and substituted with 0-5 R b ; 3 R is selected from the group: H, halo, -CN, O2 , C1-4 haloalkyl, NR 5 R 5a , NR 5 NR 5 R 5a , NR 5 C(0)OR 5 , NR 5 C(0)R 5 , =0, OR 5 , COR 5 , CO2R 5 , C0NR 5 R 5a , NHC (0) NR 5 R 5a , NHC(S)NR 5 R 5a , Sθ2NR 5 R 5a , Sθ2R 5b , C1- 4 alkyl, phenyl, and benzyl ; R 3a is selected from the group: H, C1- 4 alkyl, phenyl, and benzyl; alternatively, R 3 and R 3a , together with the nitrogen atom to which they are attached, form a heterocycle having 5-6 atoms in the ring containing an additional 0-1 N, S, or 0 atom and substituted with 0-3 R 3c ; " V*\ R is selected from the group: H, C1-4 alkyl, phenyl, and benzyl ; R 3c is independently at each occurrence selected from the group: halo, -CN , N 3 , NO2 , C1-4 alkyl, C1- 4 haloalkyl, NR 3 R 3b , =0, OR 3 , COR 3 , CO2R 3 , CONR 3 R 3b , NHC(0)NR 3 R 3b , NHC(S)NR 3 R 3b , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , Sθ2NR 3 R 3 , Sθ2R 3b , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from 0, N, and S; R 4 is independently at each occurrence selected from the group: H, -CN, C1-4 alkyl, C1-4 haloalkyl, NR 3 R 3a , NR 3 C(0)0R 3 , NR 3 C(0)R 3 , OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , 13 NHC(0)NR 3 R 3a , NHC (S) NR 3 R 3a , S0 2 NR 3 R 3a , Sθ R 3b , C3-10 carbocycle substituted with 0-5 R a , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected 3 from 0, N, and S, substituted with 0-3 R ; R 5 is independently selected from the group: H, C 1 -. 4 alkyl, phenyl , and benzyl ; R 5a is independently selected from the group: H, C1-4 alkyl , phenyl and benzyl ; R 5b is independently selected from the group: H, C1-4 alkyl , phenyl , and benzyl ; and m is selected from 0, 1, 2, and 3. In a even more preferred embodiment, the present invention provides a novel compound of formula (I) , wherein: X is selected from the group: O and S ; R 1 is selected from the group: H, C 1 -5 alkyl substituted with 0-2 R C , -NHR 4 , C3-6 carbocycle substituted with 0-5 R , and 5-6 membered heterocycle containing from 1-4 heteroatoms selected from 0, N, and S and substituted with 0-5 R ; R a is independently at each occurrence selected from the group: halo, -CN, N 3 , Cχ-4 alkyl, C1-4 haloalkyl, NR 3 R 3a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , NHC(0)NR 3 R 3a , Sθ2NR 3 R 3a , Sθ2R 3b , and 5-6 14 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S; alternatively, when two R a ' s are present on adjacent carbon atoms they combine to form -OCH2O- or -OCH2CH2O- ; R is independently at each occurrence selected from the group: halo, C1-.4 alkyl, C1- 4 haloalkyl, NR 3R3a, NR 3 C(0)OR 3 , NR 3 C(0)R 3 , OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , NHC(0)NR 3 R 3a , Sθ2NR 3 R 3a , and Sθ2R 3b ; R c is independently at each occurrence selected from the group: halo, C 1 -4 alkyl, C1- 4 haloalkyl, NR R , NR 5 NR 5 R 5a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , OR 3 , COR 3 , C0 2 R 3 , CONR 3 R 3a , NHC(0)NR 3 R 3a , Sθ2NR 3 R 3a , Sθ2R 3b , C3-10 carbocycle substituted with 0-5 R a , and 5-6 membered heterocycle containing from 1-4 heteroatoms selected 3 from O, N, and S, substituted with 0-3 R ; R 2 is selected from the group: C1-5 alkyl substituted with 0-3 R , -(CF2)mCF3, C3-6 carbocycle substituted with 0-5 R , and 5-6 membered heterocycle containing from 1-4 heteroatoms selected from 0, N, and S and substituted with 0-3 R ; 3 R is selected from the group: H, halo, -CN, NO2 , C1-4 haloalkyl, NR 5 R 5a , NR 5 NR 5 R 5a , NR 5 C(0)OR 5 , NR 5 C(0)R 5 , =0, OR 5 , COR 5 , CO2R 5 , C0NR 5 R 5a , NHC (0) NR 5 R 5a , NHC(S)NR 5 R 5a , Sθ2NR 5 R 5a , S02R 5b , C1-4 alkyl, phenyl, and benzyl ; 15 R is selected from the group: H, Cχ- 4 alkyl, phenyl, and benzyl ; alternatively, R 3 and R 3a , together with the nitrogen atom to which they are attached, form a heterocycle having 5-6 atoms in the ring containing an additional 0-1 N, S, or 0 atom and substituted with 0-3 R 3c ; R is selected from the group: H, C1- 4 alkyl, phenyl, and benzyl ; R 3c is independently at each occurrence selected from the group: halo, -CN , N 3 , NO2 , C1- 4 alkyl, C1-.4 haloalkyl, NR 3 R 3b , =0, OR 3 , COR 3 , CO2R 3 , CONR 3 R 3b , NHC(0)NR 3 R 3b , NHC(S)NR 3 R 3b , NR 3 C (O) OR 3 , NR 3 C (0) R 3 , Sθ2NR 3 R 3 , Sθ2R 3b , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from 0, N, and S; R 4 is independently at each occurrence selected from the group: H, -CN, C1- 4 alkyl, C 1 - 4 haloalkyl, NR 3 R 3a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , NHC(0)NR 3 R 3a , NHC(S)NR 3 R 3a , Sθ2NR 3 R 3a , Sθ2R 3b , C3-10 carbocycle substituted with 0-5 R a , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from 0, N, and S, substituted with 0-3 R ; R 5 is independently selected from the group: H and C1- 4 alkyl ; R 5a is independently selected from the group: H, C1-4 alkyl , phenyl and benzyl ; 16 R 5b is independently selected from the group: H and C1- 4 alkyl ; and m is selected from 0, 1, 2, and 3. In a most preferred embodiment, the compounds of formula (I) are selected from: 3- (4-methoxyphenyl) -5- (acetamido) indeno [1 , 2 -c] pyrazol -4 -one; 3- (phenyl) -5- (acetamido) indeno [1 , 2-c] pyrazol -4 -one; 3- (4-methylthiophenyl) -5- (acetamido) indeno [1 , 2-c] pyrazol -4- one ; 3- (4 -methylsulfonylphenyl) -5- (acetamido) indeno [1,2- c] pyrazol -4 -one ; 3- (4-N,N-dimethylphenyl) -5- (acetamido) indeno [1, 2-c] pyrazol- 4 -one ; 3- (3 -pyridyl) -5- (acetamido) indeno [1, 2-c] pyrazol -4 -one; 3 - (4-methoxyphenyl) -5- (formamido) indeno [1 , 2-c] pyrazol -4 -one ; 3- (4-hydroxyphenyl) -5- (acetamido) indeno [1, 2-c] pyrazol -4 -one; 3- (4- (1-piperidinyl) phenyl) -5- (acetamido) indeno [1,2- c] pyrazol-4 -one; 3- (4-morpholinyl) phenyl) -5- (acetamido) indeno [1 , 2-c] yrazol- 4 -one ; 3- (4-ethoxyphenyl) -5- (acetamido) indeno [1 , 2-c] pyrazol -4 -one; 3- (4-butylphenyl) -5- (acetamido) indeno [1, 2-c] pyrazol -4 -one; 17 - (4-ethylphenyl) -5- (acetamido) indeno [1, 2-c] pyrazol-4-one; - (4-n-propylphenyl) -5- (acetamido) indeno [1 , 2-c] yrazol-4- one; 3- (4-methoxyphenyl) -5- ( (4-aminophenyl) acetamido) indeno [1,2- c] pyrazol -4 -one; 3- (4-pyridyl) -5- (formamido) indeno [1, 2-c] pyrazol -4 -one; 3- (4-pyridyl) -5- (acetamido) indeno [1, 2-c] pyrazol -4 -one; 3- (4-methoxyphenyl) -5- ( (4-aminophenyl) acetamido) indeno [1,2- c] pyrazol-4-one ; 3- (4~methoxyphenyl) -5- ( (4-azidophenyl) acetamido) indeno [1,2- c] pyrazol -4 -one; 3- (4-methoxyphenyl) -5- ( (4-methoxycarbonylaminophenyl) acetamido) indeno [1 , 2-c] pyrazol-4 -one; 3- (4-methoxyphenyl) -5- ( (4-aminomethylcarbonylaminophenyl) acetamido) indeno [1 , 2-c] pyrazol-4 -one; 3- (4-methoxyphenyl) -5- ( (4-dimethylaminomethylcarbonyl aminophenyl) acetamido) indeno [1 , 2-c] pyrazol-4 -one; 3- (4-methoxyphenyl) -5- ( (4-acetamidophenyl) acetamido) indeno [1, 2-c] pyrazol-4 -one; 3- (4-methoxyphenyl) -5- (pyrrolidinylacetamido) indeno [1,2- c] pyrazol -4 -one; 3- (4-methoxyphenyl) -5- (morpholinylacetamido) indeno [1,2- c] pyrazol -4-one; 18 3 - (4-methoxyphenyl) -5- (thiomorpholinylacetamido) indeno [1,2- c] pyrazol-4 -one; 3 - (4-methoxyphenyl) -5- (ethylaminoacetamido) indeno [1,2- c] pyrazol -4 -one; 3- (4-methoxyphenyl) -5- (piperidinylacetamido) indeno [1,2- c] pyrazol -4 -one; 3- (4-methoxyphenyl) -5- (4-aminomethylpiperidinylacetamido) indeno [1 , 2-c] yrazol-4-one; 3- (4-methoxyphenyl) -5- (piperazinylacetamido) indeno [1,2- c] pyrazol-4 -one; 3- (4-methoxyphenyl) -5- (4-methylpiperazinylacetamido) indeno [1 , 2-c] pyrazol -4 -one; 3- (4-methoxyphenyl) -5- (4- (2- hydroxyethyl) piperazinylacetamido) indeno [1, 2-c] pyrazol - 4 -one; 3- (4-methoxyphenyl) -5- (N,N-dimethylaminoacetamido) indeno [1 , 2-c] pyrazol -4 -one; 3- (4-methoxyphenyl) -5- ( (2 -hydroxyethyl) aminoacetamido) indeno [1 , 2-c] pyrazol -4 -one; 3- (4-methoxyphenyl) -5- (aminoacetamido) indeno [1 , 2-c] pyrazol- 4-one ; 3- (4-methoxyphenyl) -5- ( (2-chlorophenyl) acetamido) indeno [1,2- c] pyrazol-4-one; 3- (4-methoxyphenyl) -5- ((2,4- dichlorophenyl) acetamido) indeno [1, 2 -c] pyrazol -4 -one; 19 3- (4-methoxyphenyl) -5- ( (3 , 4-dichlorophenyl) acetamido) indeno [1, 2-c] yrazol -4 -one; 3- (4-methoxyphenyl) -5- ( (2 -methoxyphenyl) acetamido) indeno [1, 2-c] pyrazol -4 -one; 3- (4-dimethoxyphenyl) -5- ( (3-thiophene) acetamido) indeno [1,2- c] pyrazol-4 -one ; 3- (4 -methoxyphenyl) -5- ( (3 , 4-ethylenedioxyphenyl) acetamido) indeno [1, 2-c] pyrazol -4 -one; 3- (3 , 4-dimethoxyphenyl) -5- (acetamido) indeno [1 , 2-c] pyrazol -4- one; 3- (2 -methoxyphenyl) -5- (acetamido) indeno [1, 2-c] pyrazol -4 -one; 3- (4 -methoxyphenyl) -5- ( (2 , 5-dimethoxyphenyl) acetamido) indeno [1 , 2-c] pyrazol-4 -one; 3- (4 -methoxyphenyl) -5- ( (3 , 4-dimethoxyphenyl) acetamido) indeno [1, 2-c] pyrazol -4 -one; 3- (4 -methoxyphenyl) -5- ( (4 -methoxyphenyl) acetamido) indeno [1, 2 -c] pyrazol -4 -one; 3- (4 -methoxyphenyl) -5- ( (3- methoxyphenyl ) acetamido) indeno [1, 2-c] pyrazol -4 -one; 3- (4 -methoxyphenyl) -5- ( (4 -chlorophenyl) acetamido) indeno [1,2- c] pyrazol-4-one; 3- (4 -methoxyphenyl) -5- (butylcarbamoyl) aminoindeno [1, 2- c] pyrazol -4-one ; 3- (4 -methoxyphenyl) -5- (4-aminobenzylcarbamoyl) aminoindeno [1, 2-c] yrazol -4-one; 20 3- (4 -methoxyphenyl) -5- (4-pyridylcarbamoyl) aminoindeno [1,2- c] pyrazol -4 -one; 3- (4 -methoxyphenyl) -5- (phenylcarbamoyl) aminoindeno [1 , 2- c] pyrazol -4 -one ; 3- (4 -methoxyphenyl) -5- (eyelobutylamido) indeno [1 , 2-c] pyrazol - 4 -one ; 3 - (4 -methoxyphenyl) -5- (cyclopentylamido) indeno [1,2- c] pyrazol -4 -one; 3- (4 -methoxyphenyl) -5- (propylamido) indeno [1 , 2-c] pyrazol -4 - one; 3- (4 -methoxyphenyl) -5- (ethylamido) indeno [1 , 2-c] pyrazol -4- one; 3- (4 -methoxyphenyl) -5- (benzylamido) indeno [1, 2-c] pyrazol -4- one; 3- (4 -methoxyphenyl) -5- (isopropylamido) indeno [1 , 2-c] pyrazol - 4 -one ; 3- (4 -methoxyphenyl) -5- (cyclopropylamido) indeno [1,2- c] yrazol -4 -one; 3- (4 -methoxyphenyl) -5- (chloroacetamido) indeno [1, 2 -c] pyrazol- 4-one; 3- (4 -methoxyphenyl) -5- (4-pyridinylaminomethylacetamido) indeno [1 , 2-c] pyrazol -4 -one; 3- (4-N,N-dimethylaminophenyl) -5- (morpholinylacetamido) indeno [1 , 2-c] pyrazol -4 -one; 3- (4-N,N-dimethylaminophenyl) -5- (dimethylaminoacetamido) indeno [1, 2-c] pyrazol-4 -one; 21 3- (4- (trifluoromethyl) phenyl) -5- (acetamido) indeno [1,2- c] pyrazol -4 -one; 3- (4- (dimethylamino) phenyl) -5- ( (4-methyl-l- piperazinyl) acetamido) indeno [1 , 2-c] pyrazol-4 -one; 3- (4- (dimethylamino) phenyl) -5- ( (4-aminomethyl-l- piperidinyl) acetamido) indeno [1 , 2-c] pyrazol -4 -one; 3- (4- (dimethylamino) phenyl) -5- ( (4-hydroxy-l- piperidinyl) acetamido) indeno [1 , 2-c] pyrazol -4 -one; 3- (4- (4 -morpholinyl) phenyl) -5- ( (4- morpholinyl) acetamido) indeno [1 , 2-c] pyrazol -4 -one; 3 - (4 - (4 -morpholinyl) phenyl) -5- ( (4 -methyl- 1 - piperazinyl) acetamido) indeno [1 , 2-c] pyrazol-4 -one; 3- (4- (4-morpholinyl) phenyl) -5- ( (4 -hydroxy- 1- piperidinyl) acetamido) indeno [1 , 2-c] pyrazol-4 -one ; 3- (4- (4-morpholinyl) phenyl) -5- ( (4-aminomethyl-l- piperidinyl) acetamido) indeno [1 , 2-c] pyrazol -4 -one; 3- (4- (1-piperazinyl) phenyl) -5- ( (4- morpholinyl) acetamido) indeno [1 , 2-c] pyrazol-4 -one; 3- (4- (1-piperazinyl) phenyl) -5- ( (dimethylamino) acetamido) indeno [1, 2-c] pyrazol-4 -one; 3- (4- (1-piperazinyl) phenyl) -5- ( (4-methyl-l- piperazinyl) acetamido) indeno [1 , 2-c] pyrazol -4-one; 3- (4- (1-piperazinyl) phenyl) -5- ( (4-aminomethyl-l- piperidinyl) acetamido) indeno [1, 2-c] yrazol -4 -one; 22 3- (4- (1 -piperazinyl) phenyl) -5- ( (aminocarbonyl) amino) indeno [1, 2-c] pyrazol -4 -one; 3- (4- (1-piperazinyl) phenyl) -5- ( (hydrazinocarbonyl) amino) indeno [1 , 2-c] pyrazol -4 -one; 3- (4- (1 -piperazinyl) phenyl) -5- ( ( (4- morpholinylamino) carbonyl) amino) indeno [1 , 2-c] pyrazol-4- one; 3- (4- (4 -methyl -1-piperazinyl) phenyl) -5- ( ( (4- morpholinylamino) carbonyl) amino) indeno [1 , 2-c] pyrazol-4- one; 3- (4- (4-ethyl-l-piperazinyl) phenyl) -5- ( ( (4- morpholinylamino) carbonyl) amino) indeno [1, 2-c] pyrazol-4- one; 3- (4- (4 -isopropyl-1-piperazinyl) phenyl) -5- ( ( (4- morpholinylamino) carbonyl) amino) indeno [1, 2-c] pyrazol -4- one ; 3- (4- (4- t-butoxycarbonyl-1-piperazinyl) phenyl) -5- ( ( (4- morpholinylamino) carbonyl) amino) indeno [1, 2-c] pyrazol -4- one; 3- (4- (dimethylamino) phenyl) -5- ( ( ( (4-methyl-l- piperazinyl) amino) carbonyl) amino) indeno [1, 2-c] pyrazol- 4-one; 3- (i-propyl) -5- (acetamido) indeno [1, 2-c] pyrazol -4 -one; 3- (c-propyl) -5- (acetamido) indeno [1, 2-c] pyrazol-4 -one; 3- (t-butyl) -5- (acetamido) indeno [1, 2-c] pyrazol -4 -one ; 3- (2-thienyl) -5- (acetamido) indeno [1 , 2-c] pyrazol-4 -one; 23 3- (3-methyl-2-thienyl) -5- (acetamido) indeno [1, 2-c] pyrazol -4- one; 3 - (ethyl) -5- (carbamoyl) aminoindeno [1 , 2-c] pyrazol-4-one; 3- (n-propyl) -5- (carbamoyl) aminoindeno [1 , 2-c] pyrazol -4-one; 3- (i-propyl) -5- (carbamoyl) aminoindeno [1, 2-c] pyrazol -4 -one; 3- (c-propyl) -5- (carbamoyl) aminoindeno [1, 2-c] pyrazol -4 -one; 3- (c-hexyl) -5- (carbamoyl) aminoindeno [1 , 2-c] pyrazol -4 -one; 3- (2-thιenyl) -5- (carbamoyl) aminoindeno [1 , 2-c] pyrazol -4 -one; 3- (3-methyl-2-thienyl) -5- (carbamoyl) aminoindeno [1,2- c] pyrazol -4-one; 3- (5-methyl-2-thienyl) -5- (carbamoyl) aminoindeno [1,2- c] pyrazol -4-one; 3- (5-ethylcarboxyl-2-thienyl) -5- (carbamoyl) aminoindeno [1,2- c] pyrazol-4-one; 3- (3-thienyl) -5- (carbamoyl) aminoindeno [1, 2-c] pyrazol -4 -one; 3- (1-methyl-3 -pyrrolyl) -5- (carbamoyl) aminoindeno [1,2- c] pyrazol -4 -one; 3- (2, 5-dimethyl-3 -thienyl) -5- (carbamoyl) aminoindeno [1,2- c] pyrazol -4-one; 3- (2-furanyl) -5- (carbamoyl) aminoindeno [1, 2-c] yrazol -4 -one; 3- (i -propyl) -5- (N,N-dimethylaminocarbamoyl) aminoindeno [1,2- c] pyrazol-4 -one; 24 3- (c-propyl) -5- (N,N-dimethylaminocarbamoyl) aminoindeno [1,2- c] yrazol-4 -one; 3- (c-hexyl) -5- (N, N-dimethylaminocarbamoyl) aminoindeno [1 , 2- c] pyrazol -4 -one; 3- (2-thienyl) -5- (N,N-dimethylaminocarbamoyl) aminoindeno [1, 2- c] pyrazol -4-one ; 3- (5-methoxy-2-thienyl) -5- (N,N- dimethylaminocarbamoyl) aminoindeno [1, 2-c] pyrazol-4 -one; 3- (5-methyl-2-thienyl) -5- (N,N- dimethylaminocarbamoyl) aminoindeno [1 , 2-c] pyrazol -4 -one; 3- (5 -ethylcarboxyl -2 -thienyl) -5- (N,N- dimethylaminocarbamoyl) aminoindeno [1 , 2-c] pyrazol-4 -one; 3 - (3 -thienyl) -5- (N,N-dimethylaminocarbamoyl) aminoindeno [1,2- c] pyrazol -4 -one; 3- (5-chloro-3-thienyl) -5- (N,N- dimethylaminocarbamoyl) aminoindeno [1 , 2-c] pyrazol -4 -one; 3- (2,5-dimethyl-3-thienyl) -5- (N,N- dimethylaminocarbamoyl) aminoindeno [1 , 2-c] pyrazol-4 -one; 3- (2-furanyl) -5- (N,N-dimethylaminocarbamoyl) aminoindeno [1,2- c] pyrazol-4-one; 3 - (i -propyl) -5- (4-carbamoylpiperidinylacetamido) indeno [1,2- c] pyrazol-4 -one; 3- (c-hexyl) -5- (4-carbamoylpiperidinylacetamido) indeno [1,2- c] pyrazol-4-one ; 3 - (ethyl ) - 5 - (4 -aminomethylpiperidinylacetamido) indeno [1 , 2 - c] pyrazol -4 -one ; 25 3- (i-propyl) -5- (4-aminomethylpiperidinylacetamido) indeno [1, 2-c] pyrazol-4 -one; 3- (c-propyl) -5- (4-aminomethylpiperidinylacetamido) indeno [1 , 2-c] pyrazol-4 -one; 3- (c-hexyl) -5- (4 -aminomethylpiperidinylacetamido) indeno [1,2- c] pyrazol -4-one; 3- (i-propyl) -5- (4-methylpiperazinylcarbamoyl) aminoindeno [1, 2 -c] pyrazol -4 -one; 3- (5-ethylcarboxyl-2-thienyl) -5- (4- methylpiperazinylcarbamoyl) aminoindeno [1, 2-c] pyrazol -4- one ; 3- (5-carboxyl-2 -thienyl) -5- (4- methylpiperazinylcarbamoyl) aminoindeno [1 , 2 -c] pyrazol -4- one; 3- (2, 5-dimethyl-3-thienyl) -5- (4- methylpiperazinylcarbamoyl) aminoindeno [1 , 2-c] pyrazol -4- one; 3- (i-propyl) -5- (morpholinylcarbamoyl) aminoindeno [1 , 2- c] pyrazol-4 -one; 3- (N-methylcarbamoyl-4-piperidinyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4 -one; 3- (5 -methyl -2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1 , 2-c] pyrazol -4-one; 3- (5-chloro-3-thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one; 26 3- (2, 5 -dimethyl-3 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4 -one; 3- (5-ethylcarboxyl-2-thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol -4 -one; 3- (5-carboxyl -2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol -4 -one; 3- (5-benzylcarboxamido-2-thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1 , 2-c] pyrazol -4 -one; 3- (5- (4-methylpiperazinyl) carboxamido-2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol -4 -one; 3- (5- (2- (1-methylpyrrolidinyl) ethyl) carboxamido-2-thienyl) - 5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4- one; 3 - (5- (N, N-dimethylamino) carboxamido-2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1 , 2-c] pyrazol-4 -one; 3- (5- (2- (N,N-dimethylamino) ethyl) carboxamido-2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1 , 2-c] pyrazol -4 -one; 3-(5-(2- (pyrrolidinyl) ethyl) carboxamido-2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1 , 2-c] pyrazol-4 -one; 3- (5- (2- (morpholinyl) ethyl) carboxamido-2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol -4 -one; 3- (5-morpholinylcarboxamido-2-thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol -4 -one; 3- (5- (3- ( yrrolidonyl) propyl) carboxamido-2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol -4 -one; 27 3- (5- (3- (imidazolyl) propyl) carboxamido-2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1 , 2-c] pyrazol -4 -one; 3- (5- (2- (2-pyridyl) ethyl) carboxamido-2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1 , 2-c] pyrazol-4 -one; 3- (5- ( (2 -pyridyl) methyl) carboxamido-2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1 , 2-c] pyrazol-4 -one; and 3 - (5- (2- (piperidinyl) ethyl) carboxamido-2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1 , 2-c] pyrazol -4 -one; or pharmaceutically acceptable salt form thereof. Another embodiment of the present invention is a pharmaceutical composition comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of formula (I) . Another embodiment of the present invention is a method of treating cancer and proliferative diseases comprising: administering to a host in need of such treatment a therapeutically effective amount of a compound of formula (I), or a pharmaceutically effective salt form thereof. DEFINITIONS As used herein, the following terms and expressions have the indicated meanings. The compounds of the present invention may contain an asymmetrically substituted carbon atom, and may be isolated in optically active or racemic forms. It is well known in the art how to prepare optically active forms, such as by resolution of racemic forms or by synthesis from optically active starting materials. All chiral, diastereomeric, racemic forms and all geometric isomeric forms of a structure are intended, unless the 28 specific stereochemistry or isomer form is specifically indicated. The term "alkyl" is intended to include both branched and straight-chain saturated aliphatic hydrocarbon groups having the specified number of carbon atoms. Examples of alkyl include, but are not limited to, methyl, ethyl, n- propyl , i-propyl, n-butyl , s-butyl, t-butyl, n-pentyl, and s-pentyl. In addition, the term is intended to include both unsubstituted and substituted alkyl groups, the latter referring to alkyl moieties having one or more hydrogen substituents replaced by, but not limited to halogen, hydroxyl, carbonyl, alkoxy, ester, ether, cyano, phosphoryl , amino, imino, amido, sulfhydryl, alkythio, thioester, sulfonyl, nitro, heterocyclo, aryl or heteroaryl. It will also be understood by those skilled in the art that the substituted moieties themselves can be substituted as well when appropriate . The terms "halo" or "halogen" as used herein refer to fluoro, chloro, bromo and iodo. The term "aryl" is intended to mean an aromatic moiety containing the specified number of carbon atoms, such as, but not limited to phenyl, indanyl or naphthyl. The terms "cycloalkyl" and "bicycloalkyl" are intended to mean any stable ring system, which may be saturated or partially unsaturated. Examples of such include, but are not limited to, cyclopropyl, cyclopentyl, cyclohexyl, norbornyl, bicyclo [2.2.2] nonane, adamantly, or tetrahydronaphthyl (tetralin) . As used herein, "carbocycle" or "carbocyclic residue" is intended to mean any stable 3- to 7 -membered monocyclic or bicyclic or 7- to 13-membered bicyclic or tricyclic, any of which may be saturated, partially unsaturated, or aromatic. Examples of such carbocycles include, but are not limited to, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, adamantyl , cyclooctyl,; [3.3.0] bicyclooctane, [4.3.0] bicyclononane, [4.4.0]bicyclodecane (decalin) , [2.2.2] bicyclooctane, fluorenyl , phenyl , naphthyl , indanyl , adamantyl , or tetrahydronaphthyl (tetralin) . 29 As used herein, the term "heterocycle" or "heterocyclic system" is intended to mean a stable 5- to 7- membered monocyclic or bicyclic or 7- to 10-membered bicyclic heterocyclic ring which is saturated partially unsaturated or unsaturated (aromatic) , and which consists of carbon atoms and from 1 to 4 heteroatoms independently selected from the group consisting of N, 0 and S and including any bicyclic group in which any of the above-defined heterocyclic rings is fused to a benzene ring. The nitrogen and sulfur heteroatoms may optionally be oxidized. The heterocyclic ring may be attached to its pendant group at any heteroatom or carbon atom which results in a stable structure. The heterocyclic rings described herein may be substituted on carbon or on a nitrogen atom if the resulting compound is stable. If specifically noted, a nitrogen in the heterocycle may optionally be quaternized. It is preferred that when the total number of S and 0 atoms in the heterocycle exceeds 1, then these heteroatoms are not adjacent to one another. It is preferred that the total number of S and 0 atoms in the heterocycle is not more than 1. As used herein, the term "aromatic heterocyclic system" is intended to mean a stable 5- to 7- membered monocyclic or bicyclic or 7- to 10-membered bicyclic heterocyclic aromatic ring which consists of carbon atoms and from 1 to 4 heterotams independently selected from the group consisting of N, 0 and S. It is preferred that the total number of S and 0 atoms in the aromatic heterocycle is not more than 1. Examples of heterocycles include, but are not limited to, lH-indazole, 2-pyrrolidonyl , 2H, 6H-1 , 5 , 2-dithiazinyl , 2H-pyrrolyl, 3H-indolyl, 4-piperidonyl , 4aH-carbazole, 4H- quinolizinyl, 6H-1 , 2 , 5-thiadiazinyl , acridinyl, azocinyl, benzimidazolyl , benzofuranyl , benzothiofuranyl , benzothiophenyl , benzoxazolyl , benzthiazolyl , benztriazolyl , benztetrazolyl, benzisoxazolyl , benzisothiazolyl , benzimidazalonyl, carbazolyl , 4aH-carbazolyl , b-carbolinyl, chromanyl, chromenyl , cinnolinyl, decahydroquinolinyl , IE, 6H-1, 5, 2-dithiazinyl, dihydrofuro [2, 3-Jb] tetrahydrofuran, 30 furanyl , furazanyl, imidazolidinyl , imidazolinyl , imidazolyl, lH-indazolyl, indolenyl, indolinyl, indolizinyl, indolyl, isobenzofuranyl , isochromanyl , isoindazolyl , isoindolinyl, isoindolyl, isoquinolinyl, isothiazolyl , isoxazolyl, morpholinyl, naphthyridinyl , octahydroisoquinolinyl, oxadiazolyl, 1, 2 , 3-oxadiazolyl , 1, 2 , 4-oxadiazolyl, 1, 2 , 5-oxadiazolyl , 1, 3 , 4-oxadiazolyl , oxazolidinyl . , oxazolyl, oxazolidinylperimidinyl , phenanthridinyl, phenanthrolinyl , phenarsazinyl , phenazinyl, phenothiazinyl , phenoxathiinyl , phenoxazinyl , phthalazinyl , piperazinyl, piperidinyl , pteridinyl, piperidonyl , 4-piperidonyl, pteridinyl, purinyl , pyranyl , pyrazinyl, pyrazolidinyl, pyrazolinyl, pyrazolyl, pyridazinyl, pyridooxazole, pyridoimidazole, pyridothiazole, pyridinyl, pyridyl, pyrimidinyl , pyrrolidinyl , pyrrolinyl, pyrrolyl , quinazolinyl , quinolinyl, 4H-quinolizinyl, quinoxalinyl , quinuclidinyl, carbolinyl, tetrahydrofuranyl , tetrahydroisoquinolinyl, tetrahydroquinolinyl , 6H- 1,2,5 - thiadiazinyl , 1 , 2 , 3-thiadiazolyl , 1 , 2 , 4-thiadiazolyl , 1,2,5- thiadiazolyl, 1 , 3 , 4-thiadiazolyl , thianthrenyl , thiazolyl, thienyl, thienothiazolyl , thienooxazolyl , thienoimidazolyl , thiophenyl, triazinyl, 1 , 2 , 3 -triazolyl , 1, 2 , 4 -triazolyl , 1, 2 , 5-triazolyl , 1 , 3 , 4-triazolyl , xanthenyl . Preferred heterocycles include, but are not limited to, pyridinyl, furanyl , thienyl , pyrrolyl , pyrazolyl , imidazolyl , indolyl , benzimidazolyl, lH-indazolyl , oxazolidinyl , benzotriazolyl, benzisoxazolyl, oxindolyl , benzoxazolinyl , or isatinoyl . Also included are fused ring and spiro compounds containing, for example, the above heterocycles. As used herein, "pharmaceutically acceptable salts" refer to derivatives of the disclosed compounds wherein the parent compound is modified by making acid or base salts thereof. Examples of pharmaceutically acceptable salts include, but are not limited to, mineral or organic acid salts of basic residues such as amines; alkali or organic salts of acidic residues such as carboxylic acids; and the like. The pharmaceutically acceptable salts include the 31 conventional non-toxic salts or the quaternary ammonium salts of the parent compound formed, for example, from nontoxic inorganic or organic acids. For example, such conventional non-toxic salts include those derived from inorganic acids such as hydrochloric, hydrobromic, sulfuric, sulfamic, phosphoric, nitric and the like; and the salts prepared from organic acids such as acetic, propionic, succinic, glycolic, stearic, lactic, malic, tartaric, citric, ascorbic, pamoic, maleic, hydroxymaleic, phenylacetic, glutamic, benzoic, salicylic, sulfanilic, 2- acetoxybenzoic, fumaric, toluenesulfonic, methanesulfonic, ethane disulfonic, oxalic, isethionic, and the like. The pharmaceutically acceptable salts of the present invention can be synthesized from the parent compound which contains a basic or acidic moiety by conventional chemical methods. Generally, such salts can be prepared by reacting the free acid or base forms of these compounds with a stoichiometric amount of the appropriate base or acid in water or in an organic solvent, or in a mixture of the two; generally, nonaqueous media like ether, ethyl acetate, ethanol, isopropanol, or acetonitrile are preferred. Lists of suitable salts are found in Remington ' s Pharmaceutical Sciences, 18th ed. , Mack Publishing Company, Easton, PA, 1990, p. 1445, the disclosure of which is hereby incorporated by reference. The phrase "pharmaceutically acceptable" is employed herein to refer to those compounds, materials, compositions, and/or dosage forms which are, within the scope of sound medical judgment, suitable for use in contact with the tissues of human beings and animals without excessive toxicity, irritation, allergic response, or other problem or complication commensurate with a reasonable benefit/risk ratio. "Prodrugs", as the term is used herein, are intended to include any covalently bonded carriers which release an active parent drug of the present invention in vivo when such prodrug is administered to a mammalian 32 vivo when such prodrug is administered to a mammalian subject. Since prodrugs are known to enhance numerous desirable qualities of pharmaceuticals (i.e., solubility, bioavailability, manufacturing, etc.) the compounds of the present invention may be delivered in prodrug form. Thus, the present invention is intended to cover prodrugs of the presently claimed compounds, methods of delivering the same, and compositions containing the same. Prodrugs of the present invention are prepared by modifying functional groups present in the compound in such a way that the modifications are cleaved, either in routine manipulation or in vivo, to the parent compound. Prodrugs include compounds of the present invention wherein a hydroxy, amino, or sulfhydryl group is bonded to any group that, when the prodrug of the present invention is administered to a mammalian subject, it cleaves to form a free hydroxyl, free amino, or free sulfydryl group, respectively. Examples of prodrugs include, but are not limited to, acetate, formate, and benzoate derivatives of alcohol and amine functional groups in the compounds of the present invention. "Substituted" is intended to indicate that one or more hydrogens on the atom indicated in the expression using "substituted" is replaced with a selection from the indicated group (s), provided that the indicated atom's normal valency is not exceeded, and that the substitution results in a stable compound. When a substituent is keto (i.e., =0) group, then 2 hydrogens on the atom are replaced. As used herein, the term "anti cancer" or "anti- proliferative" agent includes, but is not limited to, altretamine, busulfan, chlorambucil , cyclophosphamide, ifosfamide, mechlorethamine, melphalan, thiotepa, cladribine, fluorouracil , floxuridine, gemcitabine, thioguanine, pentostatin, methotrexate, 6-mercaptopurine, cytarabine, carmustine, lomustine, streptozotocin, carboplatin, cisplatin, oxaliplatin, iproplatin, tetraplatin, lobaplatin, JM216, JM335, fludarabine, aminoglutethimide, flutamide, goserelin, leuprolide, 33 diethylstilbestrol, prednisone, bleomycin, dactinomycin, daunorubicin, doxirubicin, idarubicin, mitoxantrone, losoxantrone, mitomycin-c, plicamycin, paclitaxel, docetaxel , topotecan, irinotecan, 9-amino camptothecan, nitro camptothecan, GS-211, etoposide, teniposide, vinblastine, vincristine, vinorelbine, procarbazine, asparaginase, pegaspargase, octreotide, estramustine, hydroxyurea . SYNTHESIS The compounds of the present invention can be synthesized using the methods described below, together with synthetic methods known in the art of synthetic organic chemistry, or variations thereon as appreciated by those skilled in the art. Preferred methods include, but are not limited to, those methods described below. Each of the references cited below are hereby incorporated herein by reference . SCHEME 1 C0 2 Me i . H 2 , Pd/C C0 2 e AC 2 O, pyr . C0 2 Me C0 2 Me base 1 . H 2 NNH 2 A, 2 . acid An approach to preparing indeno [1 , 2-c] pyrazol -4 -ones is presented in Scheme 1 and can be used to prepare compounds of the present invention. The nitro group of dimethyl 3- nitrophthalate was reduced to the amine using catalytic hydrogenation. The aniline was acylated using acetic anhydride and pyridine as a base. A mixture of the resulting acetamide 2 and an acetophenone were treated with a strong 34 base in an appropriate solvent at elevated temperature to give the desired triketone 3. Additional means of preparing triketones are known to one skilled in the art as described in Kilgore et al , Industrial and Engineering Chemistry 34:494-497, 1946, the contents of which are hereby incorporated herein by reference. The triketone was treated with hydrazine at elevated temperature in an appropriate solvent to give the indeno [1 , 2-c] pyrazol-4 -one ring system. Additional means of preparing indeno [1 , 2-c] pyrazol -4 -ones are known to one skilled in the art as described in Lemke et al., J " . Heterocyclic Chem. 19:1335-1340, 1982; Mosher and Soeder, J " . Heterocyclic Chem. 8:855-59, 1971; Hrnciar and Svanygova Collect . Czech . Chem . Commun . 59:2734-40, 1994 the contents of which are hereby incorporated herein by reference. The amide was deacylated by heating with a strong acid in an appropriate solvent to give aniline 4. This aniline was acylated under standard conditions using an acid chloride in an appropriate solvent to give the desired product 5. SCHEME 2 1 . acid Λ CI H 2 NNH 2 An alternative method for making compounds of the present invention is shown in Scheme 2. The intermediate triketone 3 can be deacylated with strong acid and reacylated with an appropriate acid chloride using methods 35 known to those skilled in the art. Subsequently, triketone 6 can the be converted to the indeno [1 , 2-c] pyrazol -4 -one ring system using the same conditions described previously in Scheme 1. SCHEME 3 RC0 2 Et, NaOEt, EtOH R A CH 3 (R = CH 3 or CF 3 ) . (R = alkyl, aryl, 6 a or heteroaryl) AcOH , Et3 reduction 6 b 6 c A X H∑NNH 2 6 6 e Another method for preparing the triketones 6 of Scheme 2 employs the condensation of a 1,3-diketone 6a with 3- nitrophthalic anhydride as described in Rotberg and Oshkaya, Zh . Organ . Khim . 8:84-87, 1972; Zh . Organ . Khim . 9:2548- 2550, 1973, the contents of which are hereby incorporated herein by reference. The 1, 3-diketones, when not commercially available can be readily prepared by one skilled in the art by the acetylation or trifluoroacetylation of the requisite methyl ketone, R 1 COCH 3 . 36 Reduction of the nitro derivative 6b to the aniline 6c can be accomplished in a variety of ways including catalyic hydrogenation, treatment with zinc or iron under acidic conditions, or treatment with other reducing agents such as sodium dithionite or stannous chloride. Subsequently the aniline 6c can be converted to the indeno [1 , 2-c] pyrazol -4- ones of this invention by acylation followed by treatment with hydrazine as described previously in Scheme 2. SCHEME 4 I 2 Me Me 2 H 2 ^o base H j H ; 1 . acid 2 . RCOC1 Another method for making the indeno [1 , 2-c] pyrazol -4- one ring system is shown in Scheme 4. Dimethyl hydrazine was reacted with 3-acetylpyridine with no solvent to give the hydrazone 7. This was treated in a similar fashion as described in Scheme 1 to give the desired intermediate 8. Additional means of preparing similar intermediates are known to one skilled in the art as described in Rappoport , J " . Org. Chem. 49:2948-2953, 1984, the contents of which are hereby incorporated herein by reference. This intermediate 37 was carried through the sequence in a similar fashion as described in Scheme 1. Other features of the invention will become apparent during the following descriptions of exemplary embodiments which are given for illustration of the invention and are not intended to be limiting thereof. Examples Abbreviations used in the Examples are defined as follows: "°C" for degrees Celsius, "CIMS" for chemical ionization mass spectroscopy, "eq" for equivalent or equivalents, "g" for gram or grams, "h" for hour or hours, "mg" for milligram or milligrams, "mL" for milliliter or milliliters, "mmol" for millimolar, "M" for molar, "min" for minute or minutes, "p-TsOH" for para-toluenesulphonic acid, "DMF" for dimethylformamide, and "TFA" for trifluoroacetic acid. Example I Preparation of 3- (4-methoxyphenyl) -5- (acetamido) indeno [1,2' c] pyrazol -4 -one N0 2 C0 2 e 1 . H 2 , Pd/C C0 2 Me 2 . Ac 2 0, OMβ 12 Step 1. Synthesis of 2 from dimethyl 3-nitrophthalate . A solution of dimethyl 3-nitrophthalate (25 g, 105 mmol) in methanol (100 mL) was treated with 5% Pd/C (2.5 g) 38 and hydrogenated on a Parr Shaker at 50 psi for 2 h. The solution was filtered (Celite) , the filtrate collected and the solvent removed at reduced pressure. The residue was dissolved in acetic anhydride (20 mL) treated with pyridine (0.05mL) and heated to 80 °C for 1 min. The reaction was cooled and stirred at 25°C for 2 h. The solvent was removed at reduced pressure and the residue recrystallized from ethanol to give the product as a white solid (21 g, 79%) . mp 104-105 °C; CIMS m/e calc'd for C12H14NO5 : 252.0872, found 252.0888; Analysis calc'd for C12H13NO5 : C, 57.37; H, 5.22; N, 5.58; found: C, 57.67; H, 5.29; N, 5.77. Step 2. Synthesis of triketone 11 from 2. A solution of 2 (1 g, 4.0 mmol) in dry DMF (2 mL) was treated with sodium hydride (0.15 g, 60% suspension in oil, 0.4 mmol) in one portion. After 1 h, 4- methoxyacetophenone (0.6 g, 4.0 mmol) was added in one portion and the reaction heated to 90 °C. A second portion of sodium hydride (0.15 g, 60% suspension in oil, 0.4 mmol) was added and the exothermic reaction turns deep red. After 20 min, the reaction was cooled to 25 °C, diluted with water (20 mL) , extracted with EtOAc (10 mL) and the aqueous phase separated. The aqueous phase was acidified with 2 N HCl to pH 2 and the crude product collected. Recrystalization with ethanol gave the desired product as a yellow solid (0.4 g, 30%) . mp 174-175 °C; CIMS m/e calc'd for C19H3 . 6NO5: 338.1028, found 338.1022; Analysis calc'd for C19H15NO5 : C, 67.65; H, 4.48; N, 4.15; found: C, 67.87; H, 4.29; N, 3.99. Step 3. Synthesis of 12 from 11. A solution of 11 (0.2 g, 0.6 mmol) in EtOH (5 mL) was treated with hydrazine hydrate (0.1 mL, 1.8 mmol) and p-TsOH (3 mg) . The reaction was heated to reflux and stirred for 2 h. The reaction was cooled to 25 °C and the product 39 collected as a yellow solid (0.1 g, 50%) . mp 268 °C; CIMS m/e calc'd for C19H16N3O3 : 334.1192, found: 334.1168; Analysis calc'd for C19H15N3O3 : C, 68.46; H, 4.54; N, 12.61; found: C, 68.81; H, 4.39; N, 12.45. Example II Preparation of 3- (4 -methoxyphenyl) -5- (chloroacetamido) indeno [1, 2-c] pyrazol -4 -one OMβ cone. HCl MeOH, reflux 13 12 OMe chloroacetyl chloride, NaHC0 3 , dioxane Step 1. Synthesis of 13 from 12. A suspension of 12 (1.0 g, 3.0 mmol) in MeOH (10 mL) was treated with cone. HCl (1 mL) and heated to reflux. After 2 h, the reaction was cooled and the product was collected as a greenish solid (0.7 g, 81%). mp 273 °C; CIMS m/e calc'd for C17H14N3O2 : 292.1086, found: 292.1080; Analysis calc'd for C17H13N3O2 : C, 69.85; H, 4.83; N, 14.37; found: C, 69.99; H, 4.59; N, 14.44. Step 2. Synthesis of 14 from 13. A suspension of 13 (20 mg, 0.07 mmol) in dioxane (2 mL) was treated with aqueous sat. NaHC03 (1 mL) and chloroacetyl chloride (30 mL, 0.21 mmol) . The reaction was heated to 50 °C and stirred for 2 h. The reaction was cooled, poured into 40 water (2 mL) , extracted with EtOAc (10 mL) , the organic layer separated, dried (MgSθ4) and the solvent removed at reduced pressure. The solid residue was recrystallized from EtOH to give the product as a yellow solid (9 mg, 35%) . mp 274 °C; CIMS m/e calc'd for C3 . 9H15N3O3CI : 368.0802, found: 368.0818. Example III Preparation of 3- (4-methoxyphenyl) -5- (cyclopropylamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example II using cyclopropylacetyl chloride as the starting material, mp 289 °C; CIMS /e calc'd for C21H18N3O3: 360.1348, found: 360.1330. Example IV Preparation of 3- ( -methoxyphenyl) -5- (isopropylamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example II using isopropylacetyl chloride as the starting material, mp 288 °C; CIMS m/e calc'd for C21H20N3O3: 362.1505, found: 362.1535. Example V Preparation of 3- (4 -methoxyphenyl) -5- (ethylamido) indeno [1, 2- c]pyrazol-4-one Prepared in a similar fashion as described for example II using propionyl chloride as the starting material, mp 287 °C; CIMS m/e calc'd for C20H18N3O3 : 348.1348, found: 348.1313. Example VI 41 Preparation of 3 - (4 -methoxyphenyl) -5- (cyclopentylamido) indeno [1 2-c] pyrazol -4 -one Prepared in a similar fashion as described for example II using cyclopentylacetyl chloride as the starting material, mp 267 °C; CIMS m/e calc'd for C23H22 N 3θ3 = 388.1661, found: 388.1626. Example VII Preparation of 3- (4 -methoxyphenyl) -5- (cyclobutylamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example II using cyclobutylacetyl chloride as the starting material, mp 297 °C; CIMS m/e calc'd for C22H20N3O3: 374.1505, found: 374.1530. Example VIII Preparation of 3- (4 -methoxyphenyl) -5- (phenylacetamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example II using phenylacetyl chloride as the starting material, mp 280 °C; CIMS m/e calc'd for C25H20N3O3: 410.1505, found: 410.1533. Example IX Preparation of 3- (4 -methoxyphenyl) -5- (butylamido) indeno [1, 2- c] yrazol-4 -one Prepared in a similar fashion as described for example II using butyryl chloride as the starting material, mp 282 °C; CIMS m/e calc'd for C21H20N3O3: 362.1505, found: 362.1500. 42 Example X Preparation of 3- (4-methoxyphenyl) -5- ( (4- chlorophenyl) acetamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example II using 4-chlorophenylacetyl chloride as the starting material, mp 238 °C; CIMS /e calc'd for C25H19N3O3CI : 444.1115, found: 444.1110. Example XI Preparation of 3- (4 -methoxyphenyl) -5- ( (3- methoxyphenyl) acetamido) indeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for example II using 3-methoxyphenylacetyl chloride as the starting material, mp >300 °C; CIMS m/e calc'd for C26 H 22N3θ 4 : 440.1610, found: 440.1620. Example XII Preparation of 3- (4-methoxyphenyl) -5- ( (4- methoxyphenyl) acetamido) indeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for example II using 4 -methoxyphenylacetyl chloride as the starting material, mp 280 °C; CIMS m/e calc'd for C26H22N3O4: 440.1610, found: 440.1630. Example XIII Preparation of 3- (4-methoxyphenyl) -5- ( (3, 4- dimethoxyphenyl) acetamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example II using 3 , 4-dimethoxyphenylacetyl chloride as the starting material, mp >300 °C; CIMS m/e calc'd for C27H24N3O5: 470.1716, found: 470.1731. 43 Example XIV Preparation of 3- (4 -methoxyphenyl) -5- ( (2, 5- dimethoxyphenyl) acetamido) indeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for example II using 2 , 5-dimethoxyphenylacetyl chloride as the starting material, mp 226 °C; CIMS m/e calc'd for C27H24N3O5: 470.1716, found: 470.1739. Example XV Preparation of 3 - (2 -methoxyphenyl) -5- (acetamido) indeno [1, 2- c] pyrazol-4-one Prepared in a similar fashion as described for example I using 2 -methoxyacetophenone as the starting material, mp 276 °C; CIMS m/e calc'd for C19H16N3O3 : 334.1192, found: 334.1169. Example XVI Preparation of 3- (3, 4-dimethoxyphenyl) -5- (acetamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example I using 3 , 4-dimethoxyacetophenone as the starting material. mp >300 °C; CIMS m/e calc'd for C20 H lδN3θ4: 364.1297, found: 364.1288. Example XVII Preparation of 3- (4 -methoxyphenyl) -5- ( (3, 4- ethylenedioxyphenyl) acetamido) indeno [1, 2-c]pyrazol-4-one 44 OMe 1 . e NaHcCC ,u acetone. 2 . H 2 NNH 2 , EtOH, reflux Step 1. Synthesis of 15 from 11. A suspension of 11 (5 g, 14.8 mmol) in MeOH (50 mL) was treated with cone. HCl (3 mL) and heated to reflux. After stirring for 2 h, the reaction was cooled to 0 °C and the product collected as a yellow solid (4.2 g, 96%). mp 173 °C; CIMS m/e calc'd for C17H14NO4 : 296.0923, Found: 296.0901. Step 2. Synthesis of 16 from 15. A suspension of 15 (20 mg, 0.07 mmol) in acetone (2 mL) was treated with NaHC03 (10 mg) and the acid chloride of (3 , 4-methylenedioxyphenyl) acetic acid (prepared by heating the acid in a benzene : thionyl chloride 4:1 mixture at 50 °C for 2 h, removing the volatile components at reduced pressure, and using the crude acid chloride without further purification) . The reaction was heated to 50 °C and stirred for 2 h. The reaction was cooled, poured into water (4 mL) , extracted with EtOAc (10 mL) , dried (MgS04) , filtered and concentrated. The crude triketone was suspended in EtOH (2 mL) , treated with hydrazine hydrate (0.05 mL) and p-TsOH (1 mg) and heated to reflux for 2 h. The reaction was cooled to 0 °C and the product filtered to give a yellow solid (6.5 mg, 20%). mp 297 °C; CIMS m/e calc'd for C26H20N3O5: 454.1403, Found: 454.1398. 45 Example XVIII Preparation of 3- (4-dimethoxyphenyl) -5- ( (3- thiophene) acetamido) indeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for example XVII using the acid chloride of 3-thiopheneacetic acid as the starting material, mp 293 °C; CIMS m/e calc'd for C23H18N3O3S: 416.1069, found: 416.1088. Example XIX Preparation of 3- (4-methoxyphenyl) -5- ( (2- methoxyphenyl) acetamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example XVII using the acid chloride of 2-methoxyphenylacetic acid as the starting material, mp 255 °C; CIMS m/e calc'd for C26H2 2 N3O 4 : 440.1610, found: 440.1622. Example XX Preparation of 3- (4-methoxyphenyl) -5- ( (3 , 4- dichlorophenyl) acetamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example XVII using the acid chloride of 3 , 4-dichlorophenylacetic acid as the starting material, mp 299 °C; CIMS m/e calc'd for C25H18 3O3CI2 : 478.0725, found: 478.0744. Example XXI Preparation of 3- (4-methoxyphenyl) -5- ( (2, 4- dichlorophenyl) acetamido) indeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for example XVII using the acid chloride of 2 , 4-dichlorophenylacetic 46 acid as the starting material, mp 286 °C; CIMS /e calc'd for C25H18N3O3CI2 : 478.0725, found: 478.0734. Example XXII Preparation of 3- (4-methoxyphenyl) -5- ( (2- chlorophenyl) acetamido) indeno [1, 2 -c] pyrazol-4-one Prepared in a similar fashion as described for example XVII using the acid chloride of 2-chlorophenylacetic acid as the starting material, mp 300 °C; CIMS /e calc'd for C25H19N3O3CI: 444.1115, found: 444.1111. Example XXIII Preparation of 3- (4-methoxyphenyl) -5- (aminoacetamido) indeno [1, 2-c] pyrazol-4 -one cone. NH ,OH, EtOH sealed tube A suspension of 14 (15 mg, 0.04 mmol) in EtOH (1 mL) was treated with cone. NH4OH (1 mL) , placed in a sealed tube and heated to 80 °C for 3 h. The reaction was cooled and the solvent removed at reduced pressure. The residue was recrystallized from EtOH to give the product as a yellow solid (9 mg, 62%) . mp >300 °C; CIMS /e calc'd for C20H19N4O3: 363.1457, Found: 363.1431. Example XXIV Preparation of 3- (4-methoxyphenyl) -5- ( (2- hydroxyethyl) aminoacetamido) indeno [1,2-c] pyrazol-4-one 47 Prepared in a similar fashion as described for example XXIII using hydroxylamine as the starting material, mp 243 °C; CIMS m/e calc'd for C21H21N4O4: 393.1563, found: 393.1539. Example XXV Preparation of 3- (4 -methoxyphenyl) -5- (N,N- dimethylaminoacetamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example XXIII using dimethylamine as the starting material, mp 279 °C; CIMS m/e calc'd for C21H21N4O3: 377.1614, found: 377.1640. Example XXVI Preparation of 3- (4 -methoxyphenyl) -5- (piperazinylacetamido) indeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for example XXIII using piperazine as the starting material, mp 277 °C; CIMS m/e calc'd for C23H24N5O3 : 418.1879, found: 418.1899. Example XXVII Preparation of 3- (4 -methoxyphenyl) -5- (4- methylpiperazinylacetamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example XXIII using 4-methylpiperizine as the starting material, mp >300 °C; CIMS m/e calc'd for C24H26N5O3 = 432.2036, found: 432.2030. Example XXVIII Preparation of 3- (4 -methoxyphenyl) -5- (4- (2- hydroxyethyl) piperazinylacetamido) indeno [1, 2-c] pyrazol -4 -one 48 Prepared in a similar ' fashion as described for example XXIII using 4-hydroxyethylpiperizine as the starting material, mp >300 °C; CIMS m/e calc'd for C25H28 5O4: 462.2141, found: 462.2128. Example XXIX Preparation of 3- (4-methoxyphenyl) -5- (piperidinylacetamido) indeno [1, 2 -c] pyrazol-4-one Prepared in a similar fashion as described for example XXIII using piperidine as the starting material, mp 291 °C; CIMS m/e calc'd for C24H25N4O3 : 417.1927, found: 417.1955. Example XXX Preparation of 3- (4-methoxyphenyl) -5- (4- aminomethylpiperidinylacetamido) indeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for example XXIII using 4-aminomethylpiperidine as the starting material, mp >300 °C; CIMS m/e calc'd for C25H28N5O3: 446.2192, found: 446.2166. Example XXXI Preparation of 3- (4-methoxyphenyl) -5- (ethylaminoacetamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example XXIII using ethylamine as the starting material, mp 250 °C; CIMS m/e calc'd for C21H21N4O3: 377.1614, found: 377.1644. Example XXXII Preparation of 3- (4-methoxyphenyl) -5- (thiomorpholinylacetamido) indeno [1, 2-c] yrazol-4-one 49 Prepared in a similar fashion as described for example XXIII using thiomorpholine as the starting material, mp 298 °C; CIMS m/e calc'd for C23H23N4O3S: 435.1491, found: 435.1477. Example XXXIII Preparation of 3- (4 -methoxyphenyl) -5- ( orpholinylacetamido) indeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for example XXIII using morpholine as the starting material, mp 295 °C; CIMS m/e calc'd for C23H23N4O4: 419.1719, found: 419.1744. Example XXXIV Preparation of 3- (4 -methoxyphenyl) -5- (pyrrolidinylacetamido) indeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for example XXIII using pyyrolidine as the starting material, mp 279 °C; CIMS m/e calc'd for C23H23N4O3: 403.1770, found: 403.1761. Example XXXV Preparation of 3- (4 -methoxyphenyl) -5- (4- pyridinylaminomethylacetamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example XXIII using 4-aminomethylpyridine as the starting material, mp >300 °C; CIMS m/e calc'd for C25H22N5O3 : 440.1723, found: 440.1762. Example XXXVI Preparation of 3- (4 -methoxyphenyl) -5- ( (4- acetamidophenyl) acetamido) indeno [1,2-c] pyrazol-4-one 50 H 2 N XX . ,OMe acetyl chloride, NaHCO 3 acetone A suspension of 18 (10 mg, 0.02 mmol) in dioxane (1 mL) was treated with aqueous sat. NaHC03 (0.5 mL) and acetyl chloride (0.01 mL) and heated at 50 °C for 1 h. The reaction was cooled, poured into water (5 mL) , extracted with EtOAc (10 mL) , the organic layer separated, dried (MgSθ4) and the solvent removed at reduced pressure. The residue was recrystallized from EtOH to give the product as a yellow solid (5.6 mg, 61%). mp 268 °C; CIMS m/e calc'd for C27H23N4O 4 : 467.1719, Found: 467.1730. Example XXXVII Preparation of 3- (4 -methoxyphenyl) -5- ( (4- methoxycarbonylaminophenyl) acetamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example XXXII using methylchloroformate as the starting material, mp 257 °C; CIMS m/e calc'd for C27H23N4O5: 483.1668, found: 483.1633. Example XXXVIII Preparation of 3- (4 -methoxyphenyl) -5- ( (4- aminomethylcarbonylaminophenyl) acetamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example XXIII and XXXII using chloroacetyl chloride and cone. NH4OH as the starting materias. mp 228 °C; CIMS m/e calc'd for C27H24N5O4: 482.1828, found: 482.1844. 51 Example XXXIX Preparation of 3- (4 -methoxyphenyl) -5- ( (4 -N,N- dimethylaminomethylcarbonylaminophenyl) acetamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example XXIII and XXXII using chloroacetyl chloride and dimethyl amine as the starting materias. mp >300 °C; CIMS m/e calc'd for C29H28N5O 4 : 510.2141, found: 510.2121. Example XL Preparation of 3- (4-methoxyphenyl) -5- ( (4- azidophenyl) acetamido) indeno [1, 2-c] pyrazol-4-one A solution of example XXXVI (20 mg, 0.04 mmol) in DMF (2 mL) was treated with 5% palladium on carbon (5 mg) and hydrogentaed at atmospheric pressure using a hydrogen baloon. After 2 h, the solution was filtered (Celite) , and the solvent removed at reduced pressure. The residue was recrystallized from EtOH to give the product as a yellow solid (15 mg, 78%). mp >300 °C; CIMS m/e calc'd for C 2 5H19N6O3: 451.1519, found: 451.1544. Example XLI Preparation of 3- (4-methoxyphenyl) -5- ( (4- aminophenyl) acetamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example XXVII using the acid chloride of 4-azidophenylacetic acid as the starting material, mp 283 °C; CIMS m/e calc'd for C25H21N4O3: 425.1614, found: 425.1643. 52 O 99/54308 Example XLII Preparation of 3- (4-methoxyphenyl)-5- (phenylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4 -one OMe aniline, DMAP, DMSO, 80°C 21 Step 1. Synthesis of 20 from 15. A suspension of 15 (0.5 g, 1.7 mmol) in acetone (10 mL) was treated with NaHC03 (0.5 g) and phenyl ehloroformate . The mixture was heated to 50 °C for 2 h. The reaction was cooled, poured into water (20 mL) , extracted with EtOAc (40 mL) , the organic layer separated, dried (MgS04) and the solvent removed at reduced pressure. The residue was suspended in EtOH (10 mL) and treated with hydrazine hydrate (0.16 mL, 5.1 mmol) and p-TsOH (10 mg) . The mixture was heated to reflux and stirred for 3 h. The reaction was cooled to 0 °C and the product collected as a yellow solid (0.25 g, 36%). mp 195 °C; CIMS m/e calc'd for C24H18N3O4: 412.1297, Found: 412.1308. Step 2. Synthesis of 21 from 20. 53 A solution of 20 (20 mg, 0.05 mmol) in DMSO (2 mL) was treated with aniline (20 mL, mmol) and dimethylaminopyridine (1 mg) . The mixture was heated to 80 °C for 2 h. The reaction was cooled, poured into water (4 mL) , extracted with EtOAc (15 mL) , the organic layer separated, dried (MgSθ4) an< the solvent removed at reduced pressure. The residue was recrystallized from EtOH to give the product as a yellow solid (9 mg, 44%) . mp >300 °C; CIMS m/e calc'd for C24H19N4O3: 411.1457, Found: 411.1432. Example XLIII Preparation of 3 - (4-methoxyphenyl) -5- (butylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example XLII using butyl amine as the starting material, mp 252 °C; CIMS m/e calc'd for C21H21N4O3: 377.1614, found: 377.1633. Example XLIV Preparation of 3- (4 -methoxyphenyl) -5- (4- aminobenzylcarbamoyl) aminoindeno [1, 2-c] pyrazol -4 -one Prepared in a similar fashion as described for example XLII using 4-aminobenzyl amine as the starting material, mp >300 °C; CIMS m/e calc'd for C25H22N5O3 : 440.1723, found: 440.1700. Example XLV Preparation of 3- (4 -methoxyphenyl) -5- (4- pyridylcarbamoyl) aminoindeno [1, 2-c] pyrazol -4 -one Prepared in a similar fashion as described for example XLII using 4-aminomethylpyridine as the starting material, mp >300 °C; CIMS m/e calc'd for C24H20N5O3: 426.1566, found: 426.1533. 54 Example XLVI Preparation of 3- (4-hydroxyphenyl) -5- (acetamido) indeno [1, 2- c] pyrazol-4-one OMe BBr, CH 2 C1 2 A suspension of 12 (20 mg, 0.07 mmol) in CH2CI 2 (2 mL) was treated with excess BBr3 (1.0 mL, 1.0 M in CH2CI 2 ) and stirred for 20 h. The reaction was slowly poured into aqueous sat. NaHCθ3 (5 mL) , extracted with EtOAc (10 mL) , dried (MgS04) and concentrated. The residue was recrystallized from EtOH to give the desired product as a yellow solid (7.5 mg, 33%). mp >300 °C; CIMS m/e calc'd for C18H1 4 N3O3: 320.1035, Found: 320.1050. Example XLVII Preparation of 3- (4 -methoxyphenyl) -5- (formamido) indeno [1, 2- c] pyrazol-4-one OMe OMe formic acid A suspension of 13 (20 mg, 0.06 mmol) in formic acid (2 mL) was heated to 100 °C for 2 h. The reaction mixture was cooled and the solvent removed at reduced pressure. The residue was recrystallized from EtOH to give the desired 55 product as a yellow solid (12 mg, 63%) . mp 280 °C; CIMS m/e calc'd for C18H14N3O3 : 320.1035, Found: 320.1040. Example XLVIII Preparation of 3- (3 -pyridyl) -5- (acetamido) indeno [1 , 2 -c] pyrazol -4 -one A 1 . 2 . NaN cmpd . H 2 NNH 2 Step 1. Synthesis of 24 from 3-acetylpyridine . A solution of 3-acetylpyridine (1.0 g, 8.3 mmol) in benzene (3 mL) was treated with 1 , 1-dimethylhydrazine (0.62 mL, 8.3 mmol) and p-TsOH (5 mg) . The mixture was heated to 85 °C and stirred for 3 h. The reaction was cooled and the solvent removed at reduced pressure. This crude hydrazone was treated with 1.0 M NaN(TMS)2 in THF (16.6 mL, 16.6 mmol) at 25 °C over 5 min. After 30 min dimethyl 3-acetamidophthalate (2.1 g, 8.3 mmol) was added in one portion and the reaction heated to reflux. Stirring was continued for 6 h. The reaction was cooled and quenched by the slow addition of TFA. The solvent was removed at reduced pressure and the residue chromatographed (silica, 2.5-5 % MeOH/CH2Cl2) to give the product as a yellow solid (0.35 g, 14%) . mp 265 °C; CIMS m/e calc'd for C17H13N2O4 : 309.0875, Found: 309.0888. Step 2. Synthesis of 25 from 24. 56 A suspension of 24 (30 mg, 0.09 mmol) in EtOH (2 mL) was treated with hydrazine hydrate (0.05 mL) and p-TsOH (1 mg) and heated to reflux. After stirring for 2 h. the reaction was cooled and the product filtered to give a yellow solid (12 mg, 44%) . mp >300 °C; CIMS m/e calc'd for C17H13N4O2: 305.1039, Found: 305.1048. Example XLIX Preparation of 3- (4 -pyridyl) -5- (acetamido) indeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for example XLVIII using 4 -acetylpyridine as the starting material, mp >300 °C; CIMS m/e calc'd for C17H13N4O2 : 305.1039, found: 305.1046. Example L Preparation of 3- (4 -pyridyl) -5- (formamido) indeno [1, 2-c] pyrazol -4 -one Prepared in a similar fashion as described for example XLVII using 4-acetylpyridine as the starting material, mp >300 °C; CIMS m/e calc'd for C16H11N4O2 : 291.0882, found: 291.0882. Example LI Preparation of 3 -phenyl- 5- (acetamido) indeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for example I using acetophenone as the starting material, mp >300 °C; CIMS m/e calc'd for C18H13N3O2 : 304.1065, found: 304.1086. 57 Example LII Preparation of 3- (4-methylthiophenyl) -5- (acetamido) indeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for example I using 4 ' -methylthioacetophenone as the starting material, mp 283 °C; CIMS m/e calc'd for C19H15N3O2S: 350.0956, found: 350.0963. Example LIII Preparation of 3- (4-methylsulphonylphenyl) -5- (acetamido) indeno [1, 2-c] pyrazol-4-one Prepared by oxidation of the product of example LII. mp >300 °C; CIMS /e calc'd for C 1 9H15N3O4S: 382.0860, found: 382.0862. Example LIV Preparation of 3- (4-N,N-dimethylaminophenyl) -5- (acetamido) indeno [1, 2 -c] pyrazol-4-one Prepared in a similar fashion as described for example I using 4 ' -N,N, -dimethylaminoacetophenone as the starting material, mp >300 °C; CIMS m/e calc'd for C20 H 18N4θ2= 347.1496, found: 347.1508. Example LV Preparation of 3- (4-N,N-dimethylaminophenyl) -5- (morpholinylacetamido) indeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for examples II and XXIII employing the product of example LIV and morpholine as the starting materials, mp >300 °C; CIMS m/e calc'd for C24H26N5O3: 432.2036, found: 432.2020. 58 Example LVI Preparation of 3- (4-N,N-dimethylaminophenyl) -5- (dimethylaminoacetamido) indeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for examples II and XXIII employing the product of example LIV and dimethylamine as the starting materials, mp >300 °C; CIMS m/e calc'd for C22H24N5O2 : 390.1930, found: 390.1948. Example LVII Preparation of 3- (4- (1-piperidinyl) phenyl) -5- (acetamido) indeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for example I using 4 '- (1-piperidinyl) acetophenone as the starting material, mp 291 °C; CIMS m/e calc'd for C23H22N4O2 : 387.1801, found: 387.1821. Example LVIII Preparation of 3- (4-morpholinyl) phenyl) -5- (acetamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example I using 4 ' -morpholinylacetophenone as the starting material. mp >300 °C; CIMS m/e calc'd for C22H20N4O3: 388.1528, found: 388.1535. Example LIX Preparation of 3- (4-ethoxyphenyl) -5- (acetamido) indeno [1, 2- c] pyrazol-4-one Prepared in a similar fashion as described for example I using 4 ' -et 59 288 °C; CIMS m/e calc'd for C20H17N3O3: 348.1325, found: 348.1348. Example LX Preparation of 3- (4 -butylphenyl) -5- (acetamido) indeno [1, 2- c] pyrazol-4-one Prepared in a similar fashion as described for example I using 4 ' -butylacetophenone as the starting material . mp 259 °C; CIMS m/e calc'd for C22H21N3O2 : 360.1701, found: 360.1712. Example LXI Preparation of 3 - (4 -ethylphenyl) -5- (acetamido) indeno [1, 2- c] pyrazol -4 -one Prepared in a similar fashion as described for example I using 4 ' -ethylacetophenone as the starting material . mp 294 °C; CIMS m/e calc'd for C20 H 17 N 3θ2= 331.1310, found: 331.1321. Example LXII Preparation of 3 - (4-n-propylphenyl) -5- (acetamido) indeno [1, 2 • c] pyrazol-4-one Prepared in a similar fashion as described for example I using 4 ' -n-propylacetophenone as the starting material, mp 269 °C; CIMS m/e calc'd for C21H19N3O2: 346.1555, found: 346.1554. Example LXIII Preparation of 3- (4 -methoxyphenyl) -5- carbamoylaminoindeno [1, 2-c] pyrazol-4 -one 60 Prepared in a similar fashion as described for example XLII using concentrated ammonium hydroxide as the starting material, mp >300 °C; CIMS m/e calc'd for C18H15N4O3 : 335.1144, found: 335.1113. Example LXIV Preparation of 3- (4 -methoxyphenyl) -5- (dimethylaminocarbamoyl) aminoindeno [1, 2-c] pyrazol -4 -one Prepared in a similar fashion as described for example XLII using dimethylamino hydrazine as the starting material, mp >300 °C; CIMS m/e calc'd for C20H20N5O3: 378.1566, found: 378.1555. Example LXV Preparation of 3- (4 -methoxyphenyl) -5- (methylcarbamoyl) aminoindeno [1, 2 -c] pyrazol-4-one Prepared in a similar fashion as described for example XLII using methylamine as the starting material, mp >300 °C; CIMS /e calc'd for C19H17N4O3 : 349.1300, found: 349.1311. Example LXVI Preparation of 3- (4 -methoxyphenyl) -5- (morpholinocarbamoyl) aminoindeno [1, 2-c] yrazol-4-one Prepared in a similar fashion as described for example XLII using N-aminomorpholine as the starting material, mp >300 °C; CIMS m/e calc'd for C22H22N5O4 : 420.1671, found: 420.1655. Example LXVII Preparation of 3- (4 -methoxyphenyl) -5- (cis-2 - aminocyclohexanylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one 61 Prepared in a similar fashion as described for example XLII using cis-1 , 2-diaminocyclohexane as the starting material, mp >300 °C; CIMS m/e calc'd for C24H26N5O3: 432.2035, found: 432.2020. Example LXVIII Preparation of 3- (4 -methoxyphenyl) -5- (4- ethylpiperazinylcarbamoyl) aminoindeno [1, 2-c] pyrazol -4 -one Prepared in a similar fashion as described for example XLII using (4-amino) methylpiperazine as the starting material, mp >300 °C; CIMS m/e calc'd for C23H25 6O3: 433.1987, found: 433.1999. Example LXIX Preparation of 3- (4 -methoxyphenyl) -5- (4- uridomethylpiperadinylacetamido) indeno [1, 2 -c] pyrazol-4-one Prepared in a similar fashion as described for example XXIII using example XXX as the starting material, mp >300 °C; CIMS m/e calc'd for C26 H 29N6θ4: 489.2250, found: 489.2209. Example LXX Preparation of 3- (4 -methoxyphenyl) -5- (4- (2- pyridyl) piperazinylacetamido) indeno [1, 2-c] pyrazol -4 -one Prepared in a similar fashion as described for example XXIII using 4- (2-pyridyl) piperazine as the starting material, mp >300 °C; CIMS m/e calc'd for C28H27N6O3: 495.2144, found: 495.2111. Example LXXI 62 Preparation of 3- (4 -methoxyphenyl) -5- (4- (aminoethyl) piperazinylacetamido) indeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for example XXIII using 4- (aminoethyl) piperazine as the starting material, mp >300 °C; CIMS m/e calc'd for C25H29N6O3: 461.2300, found: 461.2333. Example LXXII Preparation of 3- (4 -methoxyphenyl) -5- (4- amidopiperadinylacetamido) indeno [1, 2-c] pyrazol -4 -one Prepared in a similar fashion as described for example XXIII using isonipecotamide as the starting material, mp >300 °C; CIMS m/e calc'd for C25H26N5O4: 460.1984, found: 460.1998. Example LXXIII Preparation of 3 - (4 -methoxyphenyl) -5- (4- hydroxypiperadinylacetamido) indeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for example XXIII using 4-hydroxypiperadine as the starting material, mp >300 °C; CIMS /e calc'd for C24H25N4O4: 433.1875, found: 433.1844. Example LXXIV Preparation of 3- (4 -methoxyphenyl) -5- (4- hydroxmethylypiperadinylacetamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example XXIII using 4-hydroxmethylypiperadine as the starting 63 material, mp >300 °C; CIMS m/e calc'd for C25H27N4O4: 447.2032, found:447.2002. Example LXXV Preparation of 3- (4 -methoxyphenyl) -5- (4- amidopiperazinylacetamido) indeno [1, 2-c] pyrazol -4 -one Prepared in a similar fashion as described for example XXIII using 4-amidopiperazine as the starting material, mp >300 °C; CIMS m/e calc'd for C24H25N6O6: 493.1835, found:493.1802. Example LXXVI Preparation of 3 - (4 -methoxyphenyl) -5- (4- di ethylaminopiperadinylacetamido) indeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for example XXIII using 4-dimethylaminopiperadine as the starting material, mp >300 °C; CIMS m/e calc'd for C26 H 30 N 5°5 : 492.2246, found : 492.2220. Example LXXVII Preparation of 3 - (4 -methoxyphenyl) -5- (4- aminopiperadinylacetamido) indeno [1, 2-c] pyrazol -4 -one Prepared in a similar fashion as described for example XXIII using 4-aminopiperadine as the starting material, mp >300 °C; CIMS m/e calc'd for C24H26N5O5: 464.1933, found:464.1975. Example LXXVIII Preparation of 3- (4- (dimethylamino) phenyl) -5- ( (4-methyl-l- piperazinyl) acetamido) indeno [1, 2-c] pyrazol-4-one 64 Prepared in a similar fashion as described for examples II and XXIII employing the product of example LIV and 1- methylpiperazine as the starting materials, mp >300 °C; ESI- MS m/e calc'd for C25H29N6O2 : 445.2352, found: 445.2359. Example LXXIX Preparation of 3- (4- (dimethylamino) phenyl) -5- ( (4- aminomethyl-1-piperidinyl) acetamido) indeno [1, 2-c] pyrazol-4- one Prepared in a similar fashion as described for examples II and XXIII employing the product of example LIV and 4- (aminomethyl) piperidine as the starting materials. ESI -MS m/e calc'd for C26H31N6O2: 459.2508, found: 459.2508. Example LXXX Preparation of 3- (4- (dimethylamino) phenyl) -5- ( (4-hydroxy-l- piperidinyl) acetamido) indeno [1, 2-c] yrazol-4-one Prepared in a similar fashion as described for examples II and XXIII employing the product of example LIV and 4- hydroxypiperidine as the starting materials, mp 267 °C; ESI- MS m/e calc'd for C25H28N5O3 : 446.2192, found: 446.2206. Example LXXXI Preparation of 3- (4- (4 - orpholinyl) henyl) -5- (4- orpholinyl) acetamido) indeno [1, 2 -c] yrazol-4-one Prepared in a similar fashion as described for examples II and XXIII employing the product of example LVI II and morpholine as the starting materials, mp 258 °C; ESI -MS m/e calc'd for C26H28 5O4: 474.2141, found: 474.2151. Example LXXXII 65 Preparation of 3 - (4- (4-morpholinyl) phenyl) -5- ( (4-methyl-l- piperazinyl) acetamido) indeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for examples II and XXIII employing the product of example LVIII and 1- methylpiperazine as the starting materials, mp 258 °C; ESI- MS m/e calc'd for C27H31N6O3 : 487.2457, found: 487.2447. Example LXXXIII Preparation of 3- (4- (4-morpholinyl) phenyl) -5- ( (4-hydroxy-l- piperidinyl) acetamido) indeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for examples II and XXIII employing the product of example LVIII and 4- hydroxypiperidine as the starting materials, mp 245 °C; ESI- MS m/e calc'd for C2 7 H30N5O4: 488.2298, found: 488.2290. Example LXXXIV Preparation of 3- (4- (4-morpholinyl)phenyl) -5- ( (4- aminomethyl-1-piperidinyl) acetamido) indeno [1, 2-c] pyrazol-4- one Prepared in a similar fashion as described for examples II and XXIII employing the product of example LVIII and 4- (aminomethyl) piperidine as the starting materials, mp 240 °C; ESI-MS m/e calc'd for C28H33N6O3 : 501.2614, found: 501.2619. Example LXXXV Preparation of 3- (4- (dimethylamino) phenyl) -5- ((( (4 -methyl- 1- piperazinyl) amino) carbonyl) amino) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for examples I, XXVII, and XLII employing the 4- (dimethylamino) acetophenone and l-amino-4 -methylpiperazine as the starting 66 materials, mp >300 °C; ESI-MS m/e calc'd for C24H28 7O2 446.2304, found: 446.2310. Example LXXXVI Preparation of 3- (i-propyl) -5- (acetamido) indeno [1, 2-c] pyrazol-4 -one AcCI H2NNH2 29 -NH Step 1. Synthesis of 26 from 3 -nitrophthalic anhydride. A solution of 3 -nitrophthalic anhydride (9.7 g, 50 mmol) and 1 , 1, 1-trifluoro-5-methyl-2 , 4-hexanedione (9.1 g, 50 mmol) in acetic anhydride (28.3 mL, 300 mmol) was treated with triethylamine (13.95 mL, 100 mmol) and stirred at 25 °C for 4 h. The solution was diluted with 1 N HCl (200 mL) and the precipate collected and washed with water (200 mL) and hexane (400 mL) to give the product as a yellow solid (11.1 g, 85%). mp 127-129 °C; CIMS (M+H) calc'd for C13H12NO5 : 262.0715, found: 262.0694. Step 2. Synthesis of triketone 27 from 26 67 A solution of 26 (11 g, 42 mmol) in EtOH (224 mL) and water (56 mL) was treated with zinc (90 g, 1.4 mol) and calcium chloride (3 g, 27 mmol) and heated to reflux for 16 h. The reaction was filtered (Celite) and the filtrate was concentrated at reduced pressure to give an aqueous residue which was extracted with EtOAc (100 mL) . The organic layer was separated and washed with sat. EDTA (100 ml) and brine (100 mL) , dried (MgS04) , filtered, and concentrated at reduced pressure to give a yellow solid. Trituration with hexane gave the product as a yellow solid (7.1 g, 73%) . mp 241-243 °C; CIMS (M+H) calc'd for C13H14NO3 : 232.0974, found: 232.0962. Step 3. Synthesis of 28 from 27 A solution of 27 (500 mg, 2.16 mmol) in CH2C12 (5 mL) was treated with Et3N (0.36 mL, 2.59 mmol) and stirred at 25 °C for 15 min. The reaction mixture was treated with acetyl chloride (0.18 mL, 2.38 mmol) and stirred at 25 °C for 1 h. The reaction mixture was quenched with 1 N HCl (20 mL) and extracted with EtOAc (20 mL) . The organic layer was separated, dried (MgS04) , filtered, and concentrated at reduced pressure to give a brown residue. Trituration with hexane gave the product as a tan solid (484 mg, 82%) . mp 241-243 °C; CIMS (M+H) calc'd for C15H16NO4 : 274.1079, found: 274.1093. Step 4. Synthesis of 29 from 28. A solution of 28 (240 mg, 0.88 mmol) in BuOH (5 mL) was treated with hydrazine hydrate (0.055 mL, 1.76 mmol) and p- TsOH (8.4 mg, 0.044 mmol). The reaction was heated to reflux and stirred for 4 h. The reaction was cooled to 25 °C and the solvent removed at reduced pressure. Recrystalization with i-propyl alcohol gave the product collected as an off- 68 white solid (173 mg, 73%). mp >250 °C; ESIMS (M+H) calc'd for C15H16 3O2: 270.1242, found: 270.1258. Example LXXXVII Preparation of 3- (c-propyl) -5- (acetamido) indeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for example LXXXVI using the c-propyl analog of 26 as the starting material, mp 220-221 °C; CIMS (M+H) calc'd for C15H14N3O2 : 268.1086, found: 268.1078. Example LXXXVIII Preparation of 3~ (t-butyl) -5- (acetamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using the t-butyl analog of 26 as the starting material, mp >250 °C; CIMS (M+H) calc'd for C16H18N3O2 : 284.1399, found: 284.1395. Example LXXXIX Preparation of 3- (2-thienyl) -5- (acetamido) indeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for example LXXXVI using the 2-thienyl analog of 26 as the starting material, mp 269 °C; CIMS (M+H) calc'd for C16H12 3O2S: 310.0650, found: 310.0635. Example XC Preparation of 3- (3 -methyl-2- thienyl) -5- (acetamido) indeno [1, 2-c] yrazol -4 -one 69 Prepared in a similar fashion as described for example LXXXVI using the 3 -methyl -2 -thienyl analog of 26 as the starting material, mp 275 °C; ESIMS (M+H) calc'd for C17H14N3O2S: 324.0811, found: 324.0807. Example XCI Preparation of 3- (ethyl) -5- (carbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using ammonia and the ethyl analog of 15 as the starting materials, mp >250 °C; CIMS (M+H) calc'd for C13H13N4O2: 257.1039, found: 257.1033. Example XCII Preparation of 3- (n-propyl) -5- (carbamoyl) aminoindeno [1, 2-c] pyrazol -4 -one Prepared in a similar fashion as described for example LXXXVI using ammonia and the n-propyl analog of 15 as the starting materials, mp 187-189 °C; CIMS (M+H) calc'd for C14H15N4O2: 271.1195, found: 271.1187. Example XCIII Preparation of 3- (i-propyl) -5- (carbamoyl) aminoindeno [1, 2-c] pyrazol -4 -one Prepared in a similar fashion as described for example LXXXVI using ammonia and the i-propyl analog of 15 as the starting materials, mp >250 °C; CIMS (M+H) calc'd for C14H15N4O2: 271.1195, found: 271.1196. Example XCIV 70 Preparation of 3- (c-propyl) -5- (carbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using ammonia and the c-propyl analog of 15 as the starting materials, mp 252-253 °C; ESIMS (M-H) calc'd for C14H11N 4 O2: 267.0881, found: 267.0884. Example XCV Preparation of 3- (c-hexyl) -5- (carbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using ammonia and the c-hexyl analog of 15 as the starting materials, mp 178-179 °C; ESIMS (M+H) calc'd for C17H19N 4 O2: 311.1507, found: 311.1500. Example XCVI Preparation of 3- (2-thienyl) -5- (carbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using ammonia and the 2 -thienyl analog of 15 as the starting materials, mp 214 °C; CIMS m+ calc'd for C15H10N 4 O2S: 310.0517, found: 310.0524. Example XCVII Preparation of 3- (3 -methyl-2 -thienyl) -5- (carbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using ammonia and the 3 -methyl-2 -thienyl analog of 15 71 as the starting materials, mp 270 °C; ESIMS (M+H) calc'd for C16H13N4O2S: 325.0759, found: 325.0744. Example XCVIII Preparation of 3- ( 5 -methyl-2 -thienyl) -5- (carbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using ammonia and the 5 -methyl -2 -thienyl analog of 15 as the starting materials, mp >280 °C; ESIMS (M+H) calc'd for C16H13N4O2S: 325.0759, found: 325.0761. Example XC X Preparation of 3- (5-ethylcarboxyl-2- thienyl) -5- (carbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using ammonia and the 5-ethylcarboxyl-2-thienyl analog of 15 as the starting materials, mp >280 °C; ESIMS (M+H) calc'd for C18H15N4O4S: 383.0813, found: 383.0788. Example C Preparation of 3- (3 -thienyl) -5- (carbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using ammonia and the 3 -thienyl analog of 15 as the starting materials, mp >280 °C; ESIMS (M+H) calc'd for C15H11N4O2S: 311.0603, found: 311.0594. Example CI Preparation of 3- (5-chloro-3-thienyl) -5- (carbamoyl) aminoindeno [1, 2-c] pyrazol-4-one 72 Prepared in a similar fashion as described for example LXXXVI using ammonia and the 5-chloro-3 -thienyl analog of 15 as the starting materials, mp >300 °C; ESIMS (M+H) calc'd for C15H10N4O2SCI: 345.0209, found: 345.0213. Example CII Preparation of 3- (2, 5 -dimethyl-3- thienyl) -5- (carbamoyl) aminoindeno [1/ 2-c] pyrazol -4 -one Prepared in a similar fashion as described for example LXXXVI using ammonia and the 2 , 5-dimethyl-3 -thienyl analog of 15 as the starting materials, mp >280 °C; ESIMS (M+H) calc'd for C17H15N4O2S: 339.0916, found: 339.0905. Example CIII Preparation of 3- (2-furanyl) -5- (carbamoyl) aminoindeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for example LXXXVI using ammonia and the 2-furanyl analog of 15 as the starting materials, mp 278 °C; ESIMS (M+H) calc'd for C15H11N4O3: 295.0831, found: 295.0838. Example CIV Preparation of 3- (i-propyl) - 5- (N,N-dimethylaminocarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using 1 , 1-dimethylhydrazine and the i-propyl analog of 15 as the starting materials, mp 231-233 °C; ESIMS (M+H) calc'd for C16H20N5O2: 314.1616, found: 314.1599. 73 Example CV Preparation of 3- (c-propyl) -5- (N,N-dimethylaminocarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using 1 , 1-dimethylhydrazine and the c-propyl analog of 15 as the starting materials, mp XXX °C; ESIMS (M+H) calc'd for C16H18N5O2 : 312.1460, found: 312.1487. Example CVI Preparation of 3- (c-hexyl) -5- (N,N-dimethylaminocarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using 1 , 1-dimethylhydrazine and the c-hexyl analog of 15 as the starting materials, mp 229-231 °C; ESIMS (M+H) calc'd for C19H24N5O2 : 354.1929, found: 354.1932. Example CVII Preparation of 3- (2-thienyl) -5- (N,N-dimethylaminocarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using 1, 1-dimethylhydrazine and the 2-thienyl analog of 15 as the starting materials, mp 279 °C; ESIMS (M+H) calc'd for C17H16N5O2S: 354.1024, found: 354.1025. Example CVIII Preparation of 3- (5-methoxy-2 -thienyl) -5- 74 (N,N-dimethylaminocarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using 1 , 1-dimethylhydrazine and the 5-methoxy-2- thienyl analog of 15 as the starting materials, mp 280 °C; ESIMS (M+H) calc'd for C18H18N5O3S: 384.1130, found: 384.1119. Example CIX Preparation of 3- (5 -methyl-2-thienyl) -5- (N,N-dimethylaminocarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using 1 , 1-dimethylhydrazine and the 5-methyl-2- thienyl analog of 15 as the starting materials, mp >280 °C; ESIMS (M+H) calc'd for C18H18N5O2S: 368.1181, found: 368.1171. Example CX Preparation of 3- (5-ethylcarboxyl-2-thienyl) -5- (N,N-dimethylaminocarbamoyl) aminoindeno [1, 2 -c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using 1 , 1-dimethylhydrazine and the 5-ethylcarboxyl - 2 -thienyl analog of 15 as the starting materials, mp 252 °C; ESIMS (M+H) calc'd for C20H20N5O4S: 426.1236, found: 426.1251. Example CXI Preparation of 3- (3-thienyl) -5- 75 (N,N-dimethylaminocarbamoyl) aminoindeno [1,2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using 1 , 1-dimethylhydrazine and the 3-thienyl analog of 15 as the starting materials, mp 202 °C; ESIMS (M+H) calc'd for C17H16N5O2S: 354.1025, found: 354.1031. Example CXII Preparation of 3- (1-methyl-3 -pyrrolyl) -5- (carbamoyl) aminoindeno [1,2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using ammonia and the 1-methyl-3 -pyrrolyl analog of 15 as the starting materials, mp >300 °C; ESIMS (M+H) calc'd for C16H 14 N5O2: 308.1147, found: 308.1166. Example CXIII Preparation of 3- (2, 5-dimethyl-3 -thienyl) -5- (N,N-dimethylaminocarbamoyl) aminoindeno [1, 2-c]pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using 1 , 1-dimethylhydrazine and the 2 , 5-dimethyl-3- thienyl analog of 15 as the starting materials, mp 252 °C; ESIMS (M+H) calc'd for C19H20N5O2S: 382.1338, found: 382.1357. Example CXIV Preparation of 3- (2 -furanyl) -5- (N,N-dimethylaminocarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one 76 Prepared in a similar fashion as described for example LXXXVI using 1 , 1-dimethylhydrazine and the 2-furanyl analog of 15 as the starting materials, mp 202 °C; ESIMS (M+H) calc'd for C17H16N5O3 : 338.1253, found: 338.1248. Example CXV Preparation of 3- (i-propyl) -5- (4-carbamoylpiperidinylacetamido) indeno [1,2-c] pyrazol-4-one Prepared in a similar fashion as described for example XXIII using isonipecotamide and the i-propyl analog of 14 as the starting materials, mp 224-225 °C; ESIMS (M+H) calc'd for C21H26N5O3: 396.2035, found: 396.2036. Example CXVI Preparation of 3- (c-hexyl) -5- (4-carbamoylpiperidinylacetamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example XXIII using isonipecotamide and the c-hexyl analog of 14 as the starting materials, mp 228-229 °C; ESIMS (M+H) calc'd for C 24 H30N5O3: 436.2348, found: 436.2345. Example CXVII Preparation of 3- (ethyl) -5- (4-aminomethylpiperidinylacetamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example XXIII using 4- (aminomethyl) piperidine and the ethyl analog of 14 as the starting materials, mp 174-176 °C; ESIMS (M+H) calc'd for C20H26 5O2: 368.2086, found: 368.2078. 77 Example CXVIII Preparation of 3- (i-propyl) -5- (4-aminomethylpiperidinylacetamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example XXIII using 4- (aminomethyl) piperidine and the i-propyl analog of 14 as the starting materials, mp 218-220 °C; ESIMS (M+H) calc'd for C21H28 5O2: 382.2242, found: 382.2227. Example CXIX Preparation of 3- (c-propyl) -5- (4-aminomethylpiperidinylacetamido) indeno [1,2-c] pyrazol-4-one Prepared in a similar fashion as described for example XXIII using 4- (aminomethyl) piperidine and the c-propyl analog of 14 as the starting materials, mp 138-140 °C; ESIMS (M+H) calc'd for C21H26N5O2: 380.2086, found: 380.2079. Example CXX Preparation of 3- (c-hexyl) -5- (4-aminomethylpiperidinylacetamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example XXIII using 4- (aminomethyl) piperidine and the c-hexyl analog of 14 as the starting materials, mp 196-198 °C; ESIMS (M+H) calc'd for C24H32 5O2: 422.2555, found: 422.2540. Example CXXI Preparation of 3- (i-propyl) -5- (4-methylpiperazinylcarbamoyl) aminoindeno 78 [1, 2-c]pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using l-amino-4-methylpiperazine and the i-propyl analog of 15 as the starting materials, mp 231-233 °C; ESIMS (M+H) calc'd for C19H25N6O2: 369.2038, found: 369.2039. Example CXXII Preparation of 3- (5-ethylcarboxyl-2-thienyl) -5- (4-methylpiperazinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using 1-amino-4 -methylpiperazine and the 5- ethylcarboxyl-2 -thienyl analog of 15 as the starting materials, mp 249 °C; ESIMS (M+H) calc'd for C23H25N6O 4 S: 481.1657, found: 481.1642. Example CXXIII Preparation of 3- (5-carboxyl-2-thienyl) -5- (4-methylpiperazinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one A solution of CXXII (30 mg, 0.05 mmol) in 3:1 THF/water (2 mL) was treated with LiOH (23 mg, 0.5 mmol) and the reaction was stirred at 25 °C for 12 h and then heated to reflux for 1 h. The organic solvent was removed at reduced pressure and the residue was partioned between EtOAc (5 mL) and water (5 mL) . The organic layer was separated and the aqueous phase was adjusted to pH = 2 with 1 M HCl and re- extracted with EtOAc (5 mL) . The combined organic layers were dried (Na2S04) , filtered and concentrated at reduced pressure to give a crude residue. Purification by reverse phase HPLC gave the product as a yellow solid (10.4 mg, 79 46%). mp 270 °C; ESIMS (M+H) calc'd for C21H21N6O4S: 453.1344, found: 453.1353. Example CXXIV Preparation of 3- (2, 5 -dimethyl- 3 -thienyl) -5- (4-methylpiperazinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for example LXXXVI using l-amino-4 -methylpiperazine and the 2,5- dimethyl -3 -thienyl analog of 15 as the starting materials. mp 250 °C; ESIMS (M+H) calc'd for C22H25N6O2S: 437.1760, found: 437.1771. Example CXXV Preparation of 3- (i-propyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4 -one Prepared in a similar fashion as described for example LXXXVI using 4-aminomorpholine and the i-propyl analog of 15 as the starting materials, mp 256-258 °C; ESIMS (M-H) calc'd for C18H20N5O3 : 354.1566, found: 354.1543. Example CXXVI Preparation of 3- (N-methylcarbamoyl-4-piperidinyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2 -c] pyrazol-4 -one Prepared in a similar fashion as described for example LXXXVI using 4-aminomorpholine and the N-methylcarbamoyl-4- piperidinyl analog of 15 as the starting materials, mp 216- 218 °C; ESIMS (M+H) calc'd for C22H27N6O5: 455.2042, found: 455.2036. 80 Example CXXVII Preparation of 3- (5-methyl-2-thienyl) -5- (morpholinylcarbamoyl) aminoindeno tl,2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using 4-aminomorpholine and the 5-methyl -2 -thienyl analog of 15 as the starting materials, mp 261 °C; ESIMS (M+H) calc'd for C20H20N5O3S: 410.1287, found: 410.1308. Example CXXVIII Preparation of 3- (5-chloro-3-thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using 4-aminomorpholine and the 5-chloro-3-thienyl analog of 15 as the starting materials, mp 259 °C; ESIMS (M+H) calc'd for C19H17N5O3SCI : 430.0741, found: 430.0757. Example CXXIX Preparation of 3- (2 , 5-dimethyl-3 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using 4-aminomorpholine and the 2 , 5-dimethyl-3 - thienyl analog of 15 as the starting materials, mp >280 °C; ESIMS (M+H) calc'd for C21H22N5O3S: 424.1443, found: 424.1431. Example CXXX Preparation of 3- (5-ethylcarboxyl-2-thienyl) -5- 81 (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI using 4-aminomorpholine and the 5-ethylcarboxyl-2- thienyl analog of 15 as the starting materials, mp 258 °C; ESIMS (M+H) calc'd for C22H22N5O5S: 468.1341, found: 468.1331. Example CXXXI Preparation of 3- (5-carboxyl-2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI (HYDROLYSIS OF PREVIOUS ESTER) . mp 273 °C; ESIMS (M+H) calc'd for C20H18N5O5S: 440.1028, found: 440.1026. Example CXXX I Preparation of 3- (5-benzylcarboxamido-2-thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one A solution of benzylamine (0.01 mL, 0.09 mmol) in DMF (1 mL) was treated with acid CXXXI (40 mg, 0.09 mmol) and stirred at 25 °C. The reaction was treated with TBTU (29 mg, 0.09 mmol) and stirred at 25 °C for 30 min. Triethylamine (0.01 mL, 0.09 mmol) was added and the reaction stirred at 25 °C for 12 h. After adding more TBTU (15 mg, 0.045 mmol) and triethylamine (0.01 mL, 0.09 mmol) the reaction was stirred at 25 °C for an additional 4 h. The reaction was diluted with EtOAc (10 mL) and water (10 mL) and the aqueous layer was extracted with EtOAc (5 x 10 mL) . The combined organic layers were dried (Na2S04) , filtered, and the solvent removed at reduced pressure. Purification of the 82 residue using reverse phase HPLC gave the product as a yellow solid (21 mg, 42%) . mp 275 °C; ESIMS (M+H) calc'd for C27H25N5O4S: 529.1659, found: 529.1682. Example CXXXIII Preparation of 3- (5- (4-methylpiperazinyl) carboxamido-2 - thienyl) - 5 - (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol -4 -one Prepared in a similar fashion as described for example CXXXII using l-amino-4 -methylpiperazine as the starting material, mp 190 °C; ESIMS (M+H) calc'd for C25H29N8O4S: 537.2032, found: 537.2055. Example CXXXIV Preparation of 3- (5- (2- (1-methylpyrrolidinyl) ethyl) carboxamido- 2 - thienyl ) - 5 - (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol -4 -one Prepared in a similar fashion as described for example CXXXII using 2- (2-aminoethyl) -1-methylpyrrolidine as the starting material, mp 235 °C; ESIMS (M+H) calc'd for C27H32N7O4S: 550.2236, found: 550.2229. Example CXXXV Preparation of 3- (5- (N,N-dimethylamino) carboxamido- 2 - thienyl) - 5 - (morpholinylcarbamoyl) aminoindeno [l,2-c]pyrazol-4-one Prepared in a similar fashion as described for example CXXXII using 1, 1-dimethylhydrazine as the starting material 83 mp 201 °C; ESIMS (M+H) calc'd for C22H24N7O 4 S: 482.1610, found: 482.1588. Example CXXXVI Preparation of 3- (5- (2- (N,N-dimethylamino) ethyl) carboxamido-2-thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] yrazol-4-one Prepared in a similar fashion as described for example CXXXII using N,N-dimethylethylenediamine as the starting material, mp 190 °C; ESIMS (M+H) calc'd for C24H28N7O 4 S: 510.1923, found: 510.1922. Example CXXXVII Preparation of 3- (5- (2- (pyrrolidinyl) ethyl) carboxamido-2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example CXXXII using 1- (2-aminoethyl) pyrrolidine as the starting material, mp 224 °C; ESIMS (M+H) calc'd for C26H30N7O4S: 536.2080, found: 536.2091. Example CXXXVIII Preparation of 3 - (5- (2 - (morpnolinyl) ethyl) carboxamido- 2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1 , 2 -c] yrazol -4 -one Prepared in a similar fashion as described for example CXXXII using 4- (2 -aminoethyl) morpholine as the starting 84 material, mp 241 °C; ESIMS (M+H) calc'd for C26H30N 7 O5S: 552.2029, found: 552.2043. Example CXXXIX Preparation of 3- (5-morpholinylcarboxamido-2-thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example CXXXII using 4-aminomorpholine as the starting material, mp 271 °C; ESIMS (M+H) calc'd for C 24 H26N 7 O5S: 524.1716, found: 524.1719. Example CXL Preparation of 3- (5- (3- (pyrrolidonyl)propyl) carboxamido-2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example CXXXII using 1- (3-aminopropyl) -2 -pyrrolidinone as the starting material, mp 260 °C; ESIMS (M+H) calc'd for C27H30N7O5S: 564.2029, found: 564.2031. Example CXLI Preparation of 3- (5- (2- (3-pyridyl) ethyl) carboxamido-2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example CXXXII using 3- (2 -aminoethyl) pyridine as the starting material, mp 203 °C; ESIMS (M+H) calc'd for C27H26N7O4S: 544.1766, found: 544.1760. Example CXLII Preparation of 3- (5- (3- (imidazolyl) propyl) 85 carboxamido-2-thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example CXXXII using 1- (3 -aminopropyl) imidazole as the starting material, mp 263 °C; ESIMS (M+H) calc'd for C26H27N8O 4 S: 547.1875, found: 547.1872. Example CXLIII Preparation of 3- (5- (2- (2-pyridyl) ethyl) carboxamido-2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example CXXXII using 2- (2 -aminoethyl) pyridine as the starting material, mp >280 °C; ESIMS (M+H) calc'd for C27H26N7O4S: 544.1767, found: 544.1778. Example CXLIV Preparation of 3- (5- ( (2-pyridyl)methyl) carboxamido-2-thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example CXXXII using 2- (aminomethyl) yridine as the starting material, mp 239 °C; ESIMS (M+H) calc'd for C26H24N 7 O4S: 530.1610, found: 530.1603. Example CXLV Preparation of 3 - (5- (2 - (piperidinyl) ethyl) carboxamido-2-thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one 86 Prepared in a similar fashion as described for example CXXXII using 1- (2 -aminoethyl) piperidine as the starting material, mp 228 °C; ESIMS (M+H) calc'd for C27H32N7O4S: 550.2236, found: 550.2236. Example CXLVI Preparation of 3- (4- (trifluoromethyl) phenyl) -5- (acetamido) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for example LXXXVI employing 1- (4- (trifluoromethyl) phenyl) -4 , 4 , 4- trifluoro-1 , 3-butanedione as the starting material, mp >300 °C; ESl " -MS m/e calc'd for C19H11 3O2 : 370.0804, found: 370.0809. Example CXLVII Preparation of 3- (4- (4-t-butoxycarbonyl-l- piperazinyl) phenyl) -5- ( ( (4- morpholinylamino) carbonyl) amino) indeno [1, 2-c] pyrazol-4-one (BocfeO 3 0 Ex . 87 Step 1. Synthesis of 30. A solution of 4-piperazinoacetophenone (24.8 g, 121 mmol) and di- ert-butyl dicarbonate (27.8 g, 128 mmol) in 480 mL of tetrahydrofuran was refluxed for 16 h. After cooling to room temperature the solution was concentrated under vacuum. The resulting solids were washed with hexane and dried under vacuum to afford 29.4 g (80%) of the product as an off-white solid. NMR (CDC1 3 ) δ 7.89 (d, 2 H, J = 9 Hz), 6.87 (d, 2 H, J = 9 Hz), 3.59 (m, 4 H) , 3.33 (m, 4 H) , 2.53 (s, 3 H) , 1.49 (s, 9 H) . Step 2. Synthesis of 31 from 30. To a solution of 30 (11.35 g, 37 mmol) and ethyl trifluoroacetate (5.40 mL, 45 mmol) in 50 mL of tetrahydrofuran at 25 °C was added dropwise over 15 min. 21% sodium ethoxide in ethanol (16.8 mL, 45 mmol) , and the resulting solution then was stirred at 25 °C for 14 h. The reaction mixyure was diluted with water, adjusted to pH 5 with cone, hydrochloric acid, and extracted with ethyl acetate. The combined extracts was washed with water and brine, dried over anhydrous sodium sulfate, filtered, and concentrated under vacuum. The resulting solid was washed with diethyl ether and dried to furnish 12.1 g (81%) of the product as an orange solid. NMR (CDC1 3 ) δ 7.87 (d, 2 H, J = 9 Hz), 6.87 (d, 2 H, J = 9 Hz), 6.45 (s, 1 H) , 3.60 (m, 4 H) , 3.41 (m, 4 H) , 1.48 (s, 9 H) . Step 3. Synthesis of CXLVII from 31. Prepared in a similar fashion as described for examples LXXVI and XLII employing 31 and 4-aminomorpholine as starting materials, mp 242 °C; ESI -MS m/e calc'd for C30H36 7O5574.2778, found: 574.2762. 88 Example CXLVIII Preparation of 3- (4- (1-piperazinyl) phenyl) -5- ( ( (4- morpholinylamino) carbonyl) amino) indeno [1, 2-c] pyrazol-4-one A solution of CXLVII (0.58 g, 1.0 mmol) in 20 mL of trifluoroacetic acid was stirred at 25 °C for 2 h. The reaction mixture was concentrated under vacuum, and the residue was recrystallized from ethanol to provide 0.53 g (89%) of the yellow product as its TFA-salt. mp 263 °C; ESIMS m/e calc'd for C25H28N7O3 : 474.2254, found: 474.2280. Example CXLIX Preparation of 3- (4- (1-piperazinyl) phenyl) -5- ( (aminocarbonyl) amino) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for examples XLII and CXLVIII employing 2- (4- (4- t-butoxycarbonyl-l- piperazinyl) benzoyl) -4-amino-l, 3 -indanedione obtained in example CXLVII and ammonia as the starting materials, mp 257 °C; ESI-MS m/e calc'd for C21H21N6O2 : 389.1726, found: 389.1724. Example CL Preparation of 3- (4- (1-piperazinyl) phenyl) -5- ( (hydrazinocarbonyl) amino) indeno [1, 2-c] pyrazol-4-one Prepared in a similar fashion as described for examples XLII and CXLVIII employing 2- (4- (4- -butoxycarbonyl-l- piperazinyl) benzoyl) -4 -amino- 1 , 3-indanedione obtained in example CXLVII and hydrazine as the starting materials, mp 257 °C; ESI-MS m/e calc'd for C21H22 7O2: 404.1835, found: 404.1834. 89 Example CLI Preparation of 3- (4- (1-piperazinyl) phenyl) -5- ( (dimethylamino) acetamido) indeno [1, 2-c]pyrazol-4-one Prepared employing 2- (4- (4- t-butoxycarbonyl-1- piperazinyl) benzoyl) -4-amino-1, 3-indanedione obtained in example CXLVII as the starting material. Chloroacetylation and treatment with dimethylamine in a similar fashion as described for examples II and XXIII, followed by treatment with hydrazine and removal of the t-butoxycarbonyl group in a similar fashion as described for examples I and CXLVIII, afforded the example compound, mp 243 °C; ESI-MS m/e calc'd for C2 4 H2 7 N6O2 : 431.2196, found: 431.2198. Example CLII Preparation of 3- (4- (1-piperazinyl) phenyl) -5- ( (4- morpholinyl) acetamido) indeno [1, 2-c] pyrazol-4-one Prepared employing 2- (4- (4- t-butoxycarbonyl-l- piperazinyl) benzoyl) -4 -amino-1, 3 -indanedione obtained in example CXLVII as the starting material. Chloroacetylation and treatment with morpholine in a similar fashion as described for examples II and XXIII, followed by treatment with hydrazine and removal of the t-butoxycarbonyl group in a similar fashion as described for examples I and CXLVIII, afforded the example compound, mp 259 °C; ESI-MS m/e calc'd for C26H29N6O3 : 473.2301, found: 473.2302. Example CLIII Preparation of 3- (4- (1-piperazinyl) phenyl) -5- ( (4-methyl-1- piperazinyl) acetamido) indeno [1, 2-c]pyrazol-4-one Prepared employing 2- (4- (4- t-butoxycarbonyl-l- piperazinyl) benzoyl) -4 -amino-1, 3 -indanedione obtained in example CXLVII as the starting material. Chloroacetylation 90 and treatment with 1-methylpiperazine in a similar fashion as described for examples II and XXIII, followed by treatment with hydrazine and removal of the t-butoxycarbonyl group in a similar fashion as described for examples I and CXLVIII, afforded the example compound. ESI-MS m/e calc'd for C27H32N7O2: 486.2618, found: 486.2608. Example CLIV Preparation of 3- (4- (1-piperazinyl) phenyl) -5- ( (4- aminomethyl-1-piperidinyl) acetamido) indeno [1, 2-c] pyrazol-4- one Prepared employing 2 - (4- (4- -butoxycarbonyl-l- piperazinyl) benzoyl) -4 -amino- 1 , 3 -indanedione obtained in example CXLVII as the starting material. Chloroacetylation and treatment with 4- (aminomethyl) piperidine in a similar fashion as described for examples II and XXIII, followed by treatment with hydrazine and removal of the t-butoxycarbonyl group in a similar fashion as described for examples I and CXLVIII, afforded the example compound, mp 239 °C; ESI-MS m/e calc'd for C28H34N7O2 : 500.2774, found: 500.2772. Example CLV Preparation of 3- (4- (4-methyl-l-piperazinyl)phenyl) -5- ( ( (4- morpholinylamino) carbonyl) amino) indeno [1, 2-c] pyrazol-4-one Ex. Ex. CLV To a solution of CXLVIII (0.17 g, 0.29 mmol) in 10 mL of methanol and 2 mL of water at 25 °C was added sequentially 37% aqueous formaldehyde (0.45 g, 5.8 mmol), 91 sodium cyanoborohydride (0.18 g, 2.9 mmol), and 4 drops of acetic acid. The resulting solution was stirred at 25 °C for 16 h. The mixture was diluted with water. It then was made acidic (~pH 1) with cone, hydrochloric acid and stirred for 10 mm. The solution next was made basic (~pH 13) with 50% aqueous sodium hydroxide and finally adjusted to pH 10 with 1 N hydrochloric acid. The mixture was extracted with 4:1 chloroform/isopropanol . The combined extracts were washed with water and brine, dried over anhydrous sodium sulfate, and filtered. To the filtrate was added excess trifluoroacetic acid, and the solution was concentrated under vacuum. The residue was recrystallized from isopropanol to furnish 0.16 g (92%) of the yellow product as its TFA-salt. mp 245 °C; ESI-MS m/e calc'd for C26H30N7O3: 488.2410, found: 488.2420. Example CLVI Preparation of 3- (4- (4-ethyl-l-piperazinyl) phenyl) -5- ( ( (4- morpholinylami.no) carbonyl) amino) indeno [1, 2-c] pyrazol-4-one Prepared m a similar fashion as described for example CLV employing CXLVIII and acetaldehyde as the starting materials, mp 245 °C; ESI-MS m/e calc'd for C27H32N7O3 : 502.2567, found: 502.2555. Example CLVII Preparation of 3- (4- (4-isopropyl-l-piperazinyl)phenyl) -5- ( ( (4-morpholinylamino) carbonyl) amino) indeno [1, 2-c] pyrazol-4- one Prepared in a similar fashion as described for example CLV employing CXLVIII and acetone as the starting materials, mp 253 °C; ESI-MS m/e calc'd for C28H34N7O3 : 516.2723, found: 516.2726. 92 UTILITY Inhibition of Kinase/C clin Complex Enzymatic Activity Several of the compounds disclosed in this invention were assayed for their inhibitory activity against cdk4/Dl and cdk2/E kinase complexes. Briefly, the in vi tro assays employ cell lysates from insect cells expressing either of the kinases and subsequently their corresponding regulatory units. The cdk2/cyclinE is purified from insect cells expressing His-tagged cdk2 and cyclin E. The cdk/cyclin lysate is combined in a microtitre-type plate along with a kinase compatible buffer, 32 P-labeled ATP at a concentration of 50 mM, a GST-Rb fusion protein and the test compound at varying concentrations. The kinase reaction is allowed to proceeded with the radiolabled ATP, then effectively stopped by the addition of a large excess of EDTA and unlabeled ATP. The GST-Rb labeled protein is sequestered on a GSH-Sepharose bead suspension, washed, resuspended in scintillant, and the 32 P activity detected in a scintillation counter. The compound concentration which inhibits 50% of the kinase activity was calculated for each compound. A compound was considered active if its IC50 was found to be less than 1 μM. Inhibition of HCT 116 Cancer Cell Proliferation To test the cellular activity of several compounds disclosed in this invention, we examined the effect of these compounds on cultured HCT116 cells and determined their effect on cell-cycle progression by the colorimetric cytotoxcity test using sulforhodamine B (Skehan et al . J. Natl . Cancer Inst . 82:1107-12, 1990). Briefly, HCT116 cells are cultured in the presence of test compounds at increasing concentrations. At selected time points, groups of cells are fixed with trichloroacetic acid and stained with sulforhodamine B (SRB) . Unbound dye was removed by washing and protein-bound dye was extracted for determination of optical density. A compound was considered active if its IC50 was found to be less than 10 μM. 93 Table 1 Example R 1 R 2 mass mp # (M + H) CO I Methyl 4-MeOC6H4 334 268 II C1CH2 4-MeOC6H4 382 274 III cyclopropyl 4-MeOC6H4 360 289 IV isopropyl 4- eOC6H4 362 288 V ethyl 4-MeOCgH4 348 287 VI cyclopentyl 4- eOC6H4 388 267 VII cyclobutyl 4-MeOC6H4 374 297 VIII benzyl 4-MeOC6H4 410 280 IX n-propyl 4-MeOC6H4 362 282 X 4-CIC6H4CH2 4-MeOC6H4 444 238 XI 3-MeOC6H 4 CH2 4-MeOCδH4 440 >300 XII 4-MeOC6H 4 CH2 4-MeOC6H4 440 280 XIII 3,4-diMeOC6H 4 CH2 4-MeOC6H4 470 >300 XIV 2,5-diMeOC6H4CH2 4-MeOC6H4 470 226 XV Methyl 2-MeOCδH4 334 276 XVI Methyl 3,4-diMeOC6H4 364 >300 XVII 3,4-(OCH2θ)C 6 H 4 CH2 4-MeOCeH4 454 297 XVIII 3 -thiophenylCH2 4-MeOC6H4 416 293 XIX 2-MeOC6H4CH2 4-MeOCδH4 440 255 XX 3,4-diClOC6H4CH2 4-MeOC6H4 479 299 XXI 2,4-diClOC6H4CH2 4-MeOC6H4 479 286 XXII 2-CIC6H4CH2 4-MeOC6H4 444 300 94 XXIII H2NCH2 4-MeOCδH4 349 >300 XXIV HOCH2CH2NHCH2 4-MeOC6H4 393 243 XXV Me2NCH2 4-MeOC6H4 377 279 XXVI piperazinylCH2 4-MeOCδH4 418 277 XXVII 4-Me-piperazinylCH2 4-MeOCδH4 432 >300 XXVIII 4-MeOCδH4 4-HOCH 2 CH 2 - 462 >300 piperazinylCH2 XXIX piperidinylCH2 4-MeOCδH4 417 291 XXX 4-MeOC6H4 446 >300 4-NH 2 CH 2 - piperidinylCH2 XXXI CH3CH2NHCH2 4-MeOC6H4 377 250 XXXII thiomorpholinylCH2 -MeOC6H4 435 298 XXXIII morpholinylCH2 -MeOCδH4 419 295 XXXIV pyrrolidinylCH2 4- eOC6H4 403 279 XXXV 4 -pyridylCH 2 NHCH 2 4-MeOC6H4 440 >300 XXXVI 4-CH3CONHC6H4CH2 4-MeOC6H4 467 268 XXXVII 4 -CH3OCONHC6H4CH2 4-MeOC6H4 483 257 XXXVIII 4-NH2CH2CONHC6H4CH2 4-MeOC6H4 482 228 XXXIX 4-Me2NCH2CONHC6H4CH2 4-MeOC6H4 510 >300 XL 4-N3C6H4CH2 4-MeOC6H4 451 >300 XLI 4-NH2C6H4CH2 4-MeOC6H4 425 283 XLII C6H5NH 4-MeOC6H4 411 >300 XLIII CH3CH2CH2NH 4-MeOCδH4 377 252 XLIV Λ _ rT _ n -T τj _ τou 4-MeOC6H4 440 >300 XLV 4-pyridylCH 2 NH 4-MeOC6H4 426 >300 XLVI Methyl 4-HOC6H4 320 >300 XLVII H 4-MeOCδH 4 320 280 XLVIII Methyl 3 -pyridyl 305 >300 XLIX Methyl 4 -pyridyl 305 >300 L H 4 -pyridyl 291 >300 LI Methyl C6H5 305 >300 95 LII Methyl 4- eSCδH4 351 283 LIII Methyl 4-MeSθ2C6H4 383 >300 LVI Methyl 4-Me2NCδH4 348 >300 LV morpholinylCH 2 4-Me2NC6H4 432 >300 LVI Me 2 NCH 2 4-MΘ2NC6H4 390 >300 LVII Methyl 4- (piperdinyl) CgH4 388 291 LVI11 Methyl 4- 389 >300 (morpholinyl) CgH4 LIX Methyl 4-CH3CH2OC6H4 349 288 LX Methyl 4-CH3CH2CH2CH2C6H4 361 259 LXI Methyl 4-CH3CH2C6H4 332 294 LXII Methyl 4-CH3CH2CH2C6H4 347 269 LXI11 NH 2 4-MeOCδH4 335 >300 LXIV Me2NNH 4-MeOC6H4 378 >300 LXV MeNH 4-MeOC6H4 349 >300 LXVI morpholinylNH 4-MeOCδH4 420 >300 LXVII cis-1 , 2- 4-MeOC6H4 432 >300 diaminocyclohexanyl LXVIII 4- 4-MeOC6H4 433 >300 methylpiperazinylNH LXVIX 4- 4-MeOC6H4 489 >300 uridomethylpiperadin ylCH 2 LXX 4-(2- 4-MeOC6H 4 495 >300 pyridyl) piperazinyl CH 2 LXXI 4- 4-MeOCδH4 461 >300 (aminoethyl) piperazi nyl CH 2 LXXII 4-amidopiperidinylCH 2 4-MeOCδH4 460 >300 LXXIII 4- 4-MeOC6H4 433 >300 hydroxypiperidinylCH 2 96 LXXIV 4-MeOC6H4 447 >300 hydroxymethylpiperid inylCH 2 LXXV 4 -amidopiperazinylCH 2 4-MeOC6H4 493 >300 LXXVI 4- 4-MeOC6H4 492 >300 dimethylaminopiperad inylCH 2 LXXVII 4 -aminopiperadinylCH 2 4-MeOCδH4 464 >300 LXXVIII 4 -Me-piperazinylCH2 4-Me2NCδH 4 445 >300 LXXIX 4-NH 2 CH 2 - 4-Me2NCδH4 459 NA piperidinylCH2 LXXX 4 -OH-piperidinylCH2 4-MΘ2NC6H4 446 267 LXXXI morpholinylCH 2 4- 474 258 (morpholinyl) CβH 4 LXXXII 4 -Me-piperazinylCH2 4- 487 258 (morpholinyl) C6H 4 LXXXIII 4 -OH-piperidinylCH2 4- 488 245 (morpholinyl) C6H4 LXXXIV 4-NH 2 CH 2 - 4- 501 240 (morpholinyl) C6H4 piperidinylCH2 LXXXV 4-Me-piperazinylNH 4-Me2NCδH 4 446 >300 LXXXVI Methyl i-propyl 270 >250 LXXXVII Methyl c-propyl 268 220 LXXXVIII Methyl t-butyl 284 >250 LXXXIX Methyl 2 -thienyl 310 269 XC Methyl 3 -Me-2 -thienyl 324 275 XCI NH 2 Ethyl 257 >250 XCII NH 2 n-propyl 271 187 XCIII NH 2 i-propyl 271 >250 XCIV NH 2 c-propyl 267 252 (M-H) xcv NH 2 c-hexyl 311 178 XCVI NH 2 2 -thienyl 310 214 (M+) 97 XCVII NH 2 3 -Me-2 -thienyl 325 270 XCVIII NH 2 5-Me-2-thienyl 325 >280 XCIX NH 2 5-C02Et-2 -thienyl 383 >280 c NH 2 3 -thienyl 311 >280 CI H 2 5-Cl-3-thienyl 345 >300 CII NH 2 2, 5-diMe-3-thienyl 339 >280 cm NH 2 2 -furanyl 295 278 CIV Me2NNH i-propyl 314 231 cv Me2 NH c-propyl 312 CVI Me2NNH c-hexyl 354 229 CVII Me2NNH 2 -thienyl 354 279 CVI11 Me2NNH 5-MeO-2-thienyl 384 280 CIX Me2NNH 5-Me-2-thienyl 368 >280 ex Me2NNH 5-Cθ2Et-2-thienyl 426 252 CXI Me2 NH 3 -thienyl 354 202 CXII NH 2 l-methyl-3- 308 >300 pyrrolyl CXI11 Me2NNH 2 , 5-diMe-3-thienyl 382 252 CXIV Me2NNH 2 - furanyl 338 202 cxv 4-NH2CO- i-propyl 396 224 piperidinylCH2 CXVI 4-NH2CO- c-hexyl 436 228 piperidinylCH2 CXVII 4-NH2CH2- ethyl 368 174 piperidinylCH2 CXVIII 4-NH2CH2- i-propyl 382 218 piperidinylCH2 CXVIX 4-NH2CH2- c-propyl 380 138 piperidinylCH2 CXX 4-NH2CH2- c-hexyl 422 196 piperidinylCH2 CXXI 4 -CH3 -piperazinylNH i-propyl 369 231 CXXII 4 -CH3 -piperazinylNH 5 -CO2Et-2 -thienyl 481 249 CXXIII 4 -CH3 -piperazinylNH 5-CO2H-2 -thienyl 453 270 98 CXXIV 4 -CH3 -piperazinylNH 2 , 5-diMe-3-thienyl 437 250 CXXV morpholinylNH i-propyl 354 256 (M-H) CXXVI morpholinylNH 4-Cθ2Me- 455 216 piperidinyl CXXVII morpholinylNH 5-Me-2-thienyl 410 261 CXXVIII morpholinylNH 5-Cl-3-thienyl 430 259 CXXIX morpholinylNH 2 , 5-diMe-3 -thienyl 424 >280 cxxx morpholinylNH 5-Cθ2Et-2 -thienyl 468 258 CXXXI morpholinylNH 5-C02H-2-thienyl 440 273 CXXXII morpho1iny1NH 5-CONHBn-2-thienyl 529 275 CXXXI II morpholinylNH 5-CONH(4-Me- 537 190 piperazinyl) -2- thienyl CXXXIV morpholinylNH 5-CONHCH2CH2 (1-Me- 550 235 2-pyrrolidinyl) -2- thienyl CXXXV morpholinylNH 5-CONHNMe2-2- 482 201 thienyl CXXXVI morpholinylNH 5 -CONHCH2CH2NMe2 - 510 190 2 -thienyl CXXXVII morpholinylNH 5-CONHCH2CH2 (1- 536 224 pyrrolidinyl) -2- thienyl CXXXVI II morpholinylNH 5-CONHCH2CH2 (1- 552 241 morpholinyl) -2- thienyl CXXXIX morpholinylNH 5 -CONHmorpholinyl - 524 271 2 -thienyl CXL morpholinylNH 5-CONHCH2CH2CH2 (1- 564 260 pyrrolidonyl) -2- thienyl CXLI morpholinylNH 5-CONHCH2CH2 (3- 544 203 pyridyl) -2 -thienyl 99 CXL11 morpho1iny1NH 5-CONHCH2CH2CH2 (1- 547 263 imidazolyl) -2- thienyl CXLIII morpholinylNH 5-CONHCH2CH2 (2- 544 >280 pyridyl) -2 -thienyl CXLIV morpholinylNH 5-CONHCH2 (3- 530 239 pyridyl) -2 -thienyl CXLV morpholinylNH 5-CONHCH2CH2 (1- 550 228 piperidinyl) -2- thienyl CXLVI Methyl 4-CF3C6H4 370 >300 (M-H) " CXLVII morpho1iny1NH 4- (4-Boc- 574 242 piperazinyl) C6H4 CXLVIII morpholinylNH 4- 474 263 (piperazinyl) C6H4 CXLIX NH 2 4- 389 257 (piperazinyl) C6H4 CL NH2NH 4- 404 257 (piperazinyl) C6H4 CLI e2NCH2 4- 431 243 (piperazinyl) C6H4 CLII morpholinylCH 2 4- 473 259 (piperazinyl) C6H4 CLIII 4-Me-piperazinylCH2 4- 486 NA (piperazinyl) C6H4 CLIV 4-NH 2 CH 2 - 4- 500 239 (piperazinyl) C6H4 piperidinylCH2 CLV morpholinylNH 4- (4-Me- 488 245 piperazinyl) C6H4 CLVI morpholinylNH 4- (4-Et- 502 245 piperazinyl) C6H4 CLVII morpholinylNH 4- (4-i-Pr- 516 253 piperazinyl) C6H4 100 Table 2 Example R ^ R " Number 100 2 -pyridylmethyl 4-MeOCgH 4 101 2 -pyridylmethyl 3-MeOC6H 4 102 2 -pyridylmethyl 4-NH 2 C 6 H 4 103 2-pyridylmethyl 3-NH 2 C 6 H 4 104 2 -pyridylmethyl 2- H2C6H 4 105 2 -pyridylmethyl 4-Me2NC6H 4 106 2 -pyridylmethyl 3-Me2NCβH 4 107 2-pyridylmethyl 2-Me2NC6H 4 108 2 -pyridylmethyl 4-pyridyl 109 2 -pyridylmethyl 3 -pyridyl 110 2 -pyridylmethyl 2-pyridyl 111 2 -pyridylmethyl 2-thiazolyl 112 2 -pyridylmethyl 2 -pyrazolyl 113 2 -pyridylmethyl 5-isoquinolyl 114 2 -pyridylmethyl 3,4- methylenedioxyCgH3 115 2 -pyridylmethyl 3,4- ethylenedioxyC6H3 116 2 -pyridylmethyl 2 -imidazolyl 117 2 -pyridylmethyl 2-oxazolyl 118 2 -pyridylmethyl 4-isoxazolyl 119 2 -pyridylmethyl 4-HOC6H4 120 2 -pyridylmethyl 3-HOC6H4 121 2 -pyridylmethyl 3,4-diHOC6H 4 101 122 2 -pyridylmethyl 4-NH 2 CH 2 C 6 H4 123 2 -pyridylmethyl 3-NH2CH 2 C 6 H4 124 3 -pyridylmethyl 4-MeOC6H4 125 3 -pyridylmethyl 3-MeOCδH 4 126 3 -pyridylmethyl 4-NH2C6H4 127 3 -pyridylmethyl 3-NH 2 C 6 H 4 128 3 -pyridylmethyl 2-NH2C6H4 129 3 -pyridylmethyl 4-Me2NCeH 4 130 3 -pyridylmethyl 3-Me2NC δ H4 131 3 -pyridylmethyl 2-Me2NC6H 4 132 3 -pyridylmethyl 4 -pyridyl 133 3 -pyridylmethyl 3 -pyridyl 134 3 -pyridylmethyl 2 -pyridyl 135 3 -pyridylmethyl 2-thiazolyl 136 3 -pyridylmethyl 2 -pyrazolyl 137 3 -pyridylmethyl 5-isoquinolyl 138 3 -pyridylmethyl 3,4- methylenedioxyCgH3 139 3 -pyridylmethyl 3,4- ethylenedioxyCgH 3 140 3 -pyridylmethyl 2 -imidazolyl 141 3 -pyridylmethyl 2-oxazolyl 142 3 -pyridylmethyl 4-isoxazolyl 143 3 -pyridylmethyl 4-HOC6H4 144 3 -pyridylmethyl 3-HOC6H 4 145 3 -pyridylmethyl 3,4-diHOC6H 4 146 3 -pyridylmethyl 4-NH2CH2C6H 4 147 3 -pyridylmethyl 3-NH2CH2C6H 4 148 4-pyridylmethyl 4-MeOC6H4 149 4 -pyridylmethyl 3-MeOC6H4 150 4 -pyridylmethyl 4-NH2C6H4 151 4 -pyridylmethyl 3-NH 2 C 6 H 4 152 4 -pyridylmethyl 2- H2C6H4 153 4 -pyridylmethyl 4-Me2NC6H4 154 4 -pyridylmethyl 3-Me2NC6H4 102 O 99/54308 FC /US99/U801I 155 4 -pyridylmethyl 2-Me 2 NCβH 4 156 4-pyridylmethyl 4 -pyridyl 157 4 -pyridylmethyl 3 -pyridyl 158 4 -pyridylmethyl 2 -pyridyl 159 4-pyridylmethyl 2-thiazolyl 160 4 -pyridylmethyl 2 -pyrazolyl 161 4 -pyridylmethyl 5-isoquinolyl 162 4 -pyridylmethyl 3,4- methylenedioxyCgH3 163 4 -pyridylmethyl 3,4- ethylenedioxyCgH3 164 4-pyridylmethyl 2 -imidazolyl 165 4 -pyridylmethyl 2-oxazolyl 166 4 -pyridylmethyl 4-isoxazolyl 167 4 -pyridylmethyl 4-HOC6H 4 168 4-pyridylmethyl 3-HOC6H 4 169 4 -pyridylmethyl 3,4-diHOC6H 4 170 4 -pyridylmethyl 4-NH2CH2C6H 4 171 4 -pyridylmethyl 3-NH2CH2C6H 4 172 2-NH2C6H4CH2 4-MeOC6H4 173 2- H2C6H4CH2 3-MeOC6H4 174 2-NH2C6H4CH2 4-NH2C6H4 175 2-NH2C6H4CH2 3-NH 2 C 6 H 4 176 2-NH2C6H4CH2 2-NH2C6H 4 177 2-NH2C6H4CH2 4-Me2NC6H4 178 2-NH2C6H4CH2 3-Me2NCδH4 179 2-NH2C6H4CH2 2-Me2NC6H4 180 2-NH2C6H4CH2 4-pyridyl 181 2- H2C6H4CH2 3 -pyridyl 182 2-NH2C6H4CH2 2 -pyridyl 183 2-NH2C6H4CH2 2-thiazolyl 184 2-NH2C6H4CH2 2 -pyrazolyl 185 2-NH2C6H4CH2 5-isoquinolyl 186 2-NH2C6H4CH2 3,4- methylenedioxyC6H3 103 187 2-NH2C6H4CH2 3 , 4 - ethylenedioxyC6H3 188 2-NH2C6H4CH2 2 -imidazolyl 189 2-NH2C6H4CH2 2-oxazolyl 190 2-NH2C6H4CH2 4-isoxazolyl 191 2-NH2C6H4CH2 4-HOC6H4 192 2-NH2C6H4CH2 3-HOC6H4 193 2-NH 2 C 6 H 4 CH2 3,4-diHOC6H 4 194 2-NH2C6H4CH2 4-NH2CH2C6H4 195 2-NH2C6H4CH2 3-NH2CH2C6H4 196 3-NH2C6H4CH2 3-MeOCgH4 197 3-NH2C6H4CH2 4-NH 2 C 6 H 4 198 3-NH2C6H4CH2 3-NH 2 C 6 H 4 199 3-NH 2 C 6 H 4 CH2 2-NH2C6H 4 200 3-NH2C6H4CH2 4-Me2NC6H4 201 3-NH2C6H4CH2 3-Me2NC6H4 202 3-NH2C6H4CH2 2-Me2NCβH4 203 3-NH2C6H4CH2 4 -pyridyl 204 3-NH2C6H4CH2 3 -pyridyl 205 3-NH2C6H4CH2 2 -pyridyl 206 3-NH2C6H4CH2 2 -thiazolyl 207 3-NH2C6H4CH2 2 -pyrazolyl 208 3-NH 2 C 6 H 4 CH2 5-isoquinolyl 209 3-NH2C6H4CH2 3,4- methylenedioxyC6H3 210 3-NH2C6H4CH2 3,4- ethylenedioxyCgH3 211 3-NH2C6H4CH2 2 -imidazolyl 212 3-NH2C6H4CH2 2-oxazolyl 213 3-NH 2 C 6 H 4 CH2 4-isoxazolyl 214 3-NH2C6H4CH2 4-HOC6H4 215 3-NH2C6H4CH2 3-HOC6H4 216 3-NH2C6H4CH2 3,4-diHOC6H4 217 3-NH2C6H4CH2 4-NH2CH2C6H 4 104 218 3-NH2C 6 H 4 CH 2 3-NH 2 CH 2 C 6 H 4 219 4-NH 2 C6H CH 2 3-MeOC6H4 220 4-NH2C6H4CH2 4-NH 2 C 6 H 4 221 4-NH2C6H4CH2 3-NH 2 C 6 H 4 222 4-NH2C6H4CH2 2-NH2C6H4 223 4-NH2C6H4CH2 4-Me2NCδH4 224 4-NH2C6H4CH2 3-Me2NC6H 4 225 4-NH2C6H4CH2 2-Me2NC δ H 4 226 4-NH2C6H4CH2 4 -pyridyl 227 4-NH2C6H4CH2 3 -pyridyl 228 4-NH2C6H4CH2 2 -pyridyl 229 4-NH 2 C 6 H 4 CH2 2-thiazolyl 230 4-NH2C6H4CH2 2 -pyrazolyl 231 4-NH2C6H4CH2 5-isoquinolyl 232 4-NH2C6H4CH2 3,4- methylenedioxyCgH3 233 4-NH2C6H4CH2 3,4- ethylenedioxyCgH3 234 4-NH2C6H4CH2 2 -imidazolyl 235 4-NH2C6H4CH2 2-oxazolyl 236 4-NH2C6H4CH2 4-isoxazolyl 237 4-NH2C6H4CH2 4-HOC6H 4 238 4-NH2C6H4CH2 3-HOC6H 4 239 4-NH2C6H4CH2 3,4-diHOC6H4 240 4-NH2C6H4CH2 4-NH2CH2C6H4 241 4-NH2C6H4CH2 3-NH2CH2C6H4 242 2-MeOC6H4CH2 3-MeOCeH4 243 2-MeOC6H 4 CH2 4-NH 2 C 6 H 4 244 2-MeOCeH4CH2 3-NH 2 C 6 H4 245 2-MeOC6H4CH2 2-NH2C6H4 246 2-MeOCgH4CH2 4-Me2NC6H4 247 2-MeOC6H4CH2 3-Me2NCδH 4 248 2-MeOC6H 4 CH2 2-Me2NC6H4 249 2-MeOC6H4CH2 4-pyridyl 105 250 2-MeOC6H4CH2 3 -pyridyl 251 2-MeOC6H4CH2 2 -pyridyl 252 2-MeOC6H4CH2 2 -thiazolyl 253 2-MeOC6H4CH2 2 -pyrazolyl 254 2-MeOC6H4CH2 5-isoquinoly1 255 2-MeOC6H4CH2 3,4- methylenedioxyCgH3 256 2-MeOC6H4CH2 3,4- ethylenedioxyCgH3 257 2-MeOC6H4CH2 2 -imidazolyl 258 2-MeOC6H 4 CH2 2-oxazolyl 259 2-MeOC6H4CH2 4-isoxazolyl 260 2-MeOC6H4CH2 4-HOCgH4 261 2-MeOC6H4CH2 3-HOCgH4 262 2-MeOC6H4CH2 3,4-diHOCgH 4 263 2-MeOC6H4CH2 4-NH 2 CH 2 CgH 4 264 2-MeOC6H4CH2 3-NH 2 CH 2 CgH 4 265 3-MeOC6H4CH2 3-MeOCgH 4 266 3-MeOCδH4CH2 4-NH 2 CgH 4 267 3-MeOCeH4CH2 3-NH CgH 4 268 3-MeOCδH4CH2 2-NH2CgH4 269 3-MeOC6H4CH2 4-Me2NCgH 4 270 3-MeOC6H4CH2 3-Me2NCgH4 271 3-MeOC6H4CH2 2-Me2NCgH4 272 3-MeOC6H4CH2 4-pyridyl 273 3-MeOC6H4CH2 3 -pyridyl 274 3-MeOCgH 4 CH2 2 -pyridyl 275 3-MeOC6H4CH2 2-thiazolyl 276 3-MeOC6H4CH2 2 -pyrazolyl 277 3-MeOC6H4CH2 5-isoquinolyl 278 3-MeOC6H4CH2 3,4- methylenedioxyCgH3 279 3-MeOC6H4CH2 3,4- ethylenedioxyCgH3 106 280 3-MeOCgH 4 CH2 2 -imidazolyl 281 3-MeOCgH4CH2 2-oxazolyl 282 3-MeOCgH 4 CH2 4-isoxazolyl 283 3-MeOCgH4CH2 4-HOCgH4 284 3-MeOCgH4CH2 3-HOCgH4 285 3-MeOCgH4CH2 3,4-diHOCgH4 286 3-MeOCgH4CH2 4-NH 2 CH 2 CgH4 287 3-MeOCgH4CH2 3-NH 2 CH 2 CgH4 288 4-MeOCgH4CH2 3-MeOC6H4 289 4-MeOCgH4CH2 4-NH 2 CgH 4 290 4-MeOCgH4CH2 3-NH 2 CgH 4 291 4-MeOCgH4CH2 2-NH2CgH 4 292 4-MeOCgH4CH2 4-Me2NC H4 293 4-MeOCgH4CH2 3-Me2 C H4 294 4-MeOCgH4CH2 2-Me2NC H4 295 4-MeOCgH4CH2 4 -pyridyl 296 4-MeOCgH4CH2 3 -pyridyl 297 4-MeOCgH4CH2 2 -pyridyl 298 4-MeOCgH4CH2 2-thiazolyl 299 4-MeOCgH4CH2 2 -pyrazolyl 300 4-MeOCgH4CH2 5-isoquinolyl 301 4-MeOCgH 4 CH2 3,4- methylenedioxyCgH3 302 4-MeOCgH4CH2 3,4- ethylenedioxyCgH3 303 4-MeOCgH4CH2 2 -imidazolyl 304 4-MeOCgH4CH2 2-oxazolyl 305 4-MeOCgH 4 CH2 4-isoxazolyl 306 4-MeOCgH4CH2 4-HOCgH4 307 4-MeOCgH4CH2 3-HOCgH4 308 4-MeOCgH4CH2 3,4-diHOCgH4 309 4-MeOCgH4CH2 4-NH 2 CH 2 CgH 4 310 4-MeOCgH4CH2 3-NH 2 CH 2 CgH 4 311 2-HOCgH4CH2 4-MeOCgH4 107 312 2-HOCgH4CH2 3-MeOCgH 4 313 2-HOCgH4CH2 4-NH 2 CgH 4 314 2-HOCgH4CH2 3-NH 2 CgH 4 315 2-HOCgH4CH2 2-NH2CgH4 316 2-HOCgH4CH2 4-Me2NC H4 317 2-HOCgH4CH2 3-Me2NC H 4 318 2-HOCgH4CH2 2-Me2NCgH4 319 2-HOCgH4CH 2 4 -pyridyl 320 2-HOCgH4CH2 3 -pyridyl 321 2-HOCgH4CH2 2 -pyridyl 322 2-HOCgH4CH2 2-thiazolyl 323 2-HOCgH4CH2 2 -pyrazolyl 324 2-HOCgH4CH2 5-isoquinolyl 325 2-HOC6H4CH2 3,4- methylenedioxyCgH3 326 2-HOCgH4CH2 3,4- ethylenedioxyCgH3 327 2-HOCgH4CH2 2 -imidazolyl 328 2-HOCgH4CH2 2-oxazolyl 329 2-HOCgH4CH2 4-isoxazolyl 330 2-HOCgH4CH2 4-HOCgH 4 331 2-HOCgH4CH2 3-HOCgH4 332 2-HOCgH4CH2 3,4-diHOCgH 4 333 2-HOCgH4CH2 4-NH 2 CH 2 CgH 4 334 2-HOCgH4CH2 3-NH 2 CH 2 CgH 4 335 3-HOCgH4CH2 4-MeOCgH 4 336 3-HOCgH4CH2 3-MeOCgH 4 337 3-HOCgH4CH2 4-NH2C H4 338 3-HOCgH4CH2 3-NH 2 CgH 4 339 3-HOC6H4CH2 2-NH2C H4 340 3-HOCgH4CH2 4-Me2NCgH4 341 3-HOCgH4CH2 3-Me2NCgH4 342 3-HOCgH4CH2 2-Me2NCgH4 343 3-HOCgH4CH2 4 -pyridyl 108 344 3-HOCgH4CH2 3 -pyridyl 345 3-HOCgH4CH2 2 -pyridyl 346 3-HOCgH4CH2 2 -thiazolyl 347 3-HOCgH4CH2 2 -pyrazolyl 348 3-HOC H4CH2 5-isoquinolyl 349 3-HOCgH4CH2 3,4- methylenedioxyCgH3 350 3-HOCgH4CH2 3,4- ethylenedioxyCgH3 351 3-HOCgH4CH2 2 -imidazolyl 352 3-HOCgH4CH2 2-oxazolyl 353 3-HOCgH4CH2 4-isoxazolyl 354 3-HOCgH4CH2 4-HOCgH 4 355 3-HOCgH4CH2 3-HOCgH 4 356 3-HOC H4CH2 3,4-diHOCgH4 357 3-HOCgH4CH2 4-NH 2 CH 2 CgH 4 358 3-HOCgH4CH2 3-NH 2 CH 2 CgH 4 359 4-HOCgH4CH2 4-MeOCgH 4 360 4-HOCgH4CH2 3-MeOCgH4 361 4-HOCgH 4 CH2 4-NH 2 CgH 4 362 4-HOCgH 4 CH2 3-NH 2 CgH 4 363 4-HOCgH4CH2 2-NH2CgH4 364 4-HOCgH4CH2 4-Me2NC H4 365 4-HOCgH4CH2 3-Me2NCgH4 366 4-HOCgH4CH2 2-Me2NC H4 367 4-HOCgH 4 CH2 4 -pyridyl 368 4-HOCgH4CH2 3 -pyridyl 369 4-HOCgH4CH2 2 -pyridyl 370 4-HOCgH4CH2 2-thiazolyl 371 4-HOCgH4CH2 2 -pyrazolyl 372 4-HOCgH4CH2 5-isoquinolyl 373 4-HOCgH4CH2 3,4- methylenedioxyCgH3 109 374 4-HOCgH 4 CH2 3,4- ethylenedioxyCgH3 375 4-HOCgH 4 CH2 2 -imidazolyl 376 4-HOCgH 4 CH2 2 -oxazolyl 377 4-HOCgH4CH2 4-isoxazolyl 378 4-HOCgH4CH2 4-HOC6H4 379 4-HOCgH 4 CH2 3-HOCgH4 380 4-HOCgH4CH2 3,4-diHOCgH4 381 4-HOCgH4CH2 4-NH 2 CH 2 CgH 4 382 4-HOCgH4CH2 3-NH 2 CH 2 CgH 4 383 4-ClCgH4CH2 3-MeOCgH4 384 4-ClCgH 4 CH2 4-NH 2 CgH 4 385 4-ClCgH4CH 2 3-NH 2 CgH 4 386 4-ClCgH4CH2 2- H2C H4 387 4-ClCgH4CH2 4-Me2NC H4 388 4-ClCgH4CH2 3-Me2NCgH4 389 4-ClCgH4CH2 2-Me2NCgH4 390 4-CIC6H4CH2 4 -pyridyl 391 4-ClCgH4CH2 3 -pyridyl 392 4-ClCgH4CH2 2 -pyridyl 393 4-ClCgH4CH2 2-thiazolyl 394 4-ClCgH 4 CH2 2 -pyrazolyl 395 4-ClCgH 4 CH2 5 - isoquinolyl 396 4-ClCgH4CH2 3,4- methylenedioxyCgH3 397 4-ClCgH4CH2 3,4- ethylenedioxyCgH3 398 4-ClCgH4CH2 2 -imidazolyl 399 4-ClCgH4CH2 2 -oxazolyl 400 4-ClCgH4CH2 4-isoxazolyl 401 4-ClCgH4CH2 4-HOCgH4 402 4-ClCgH 4 CH2 3-HOCgH4 403 4-ClCgH4CH2 3,4-diHOCgH4 404 4-ClCgH4CH2 4-NH 2 CH 2 CgH 4 110 405 4-ClCgH4CH2 3-NH 2 CH 2 CgH4 406 2-NH2CH 2 CgH 4 CH2 4-MeOCgH4 407 2-NH 2 CH 2 CgH4CH 2 3-MeOCgH4 408 2-NH2CH2C H4CH2 4-NH 2 CgH 4 409 2-NH2CH2CgH4CH2 3-NH 2 CgH 4 410 2-NH2CH2C H4CH2 2- H2CgH4 411 2-NH2CH2CgH4CH2 4-Me2NCgH4 412 2-NH2CH2C H4CH 2 3-Me2NC H4 413 2- H2CH2CgH4CH2 2-Me2NCgH4 414 2-NH2CH2C H4CH2 4 -pyridyl 415 2-NH2CH2CgH4CH2 3 -pyridyl 416 2-NH2CH 2 CgH 4 CH2 2 -pyridyl 417 2-NH2CH 2 CgH 4 CH2 2 -thiazolyl 418 2-NH2CH 2 CgH 4 CH2 2 -pyrazolyl 419 2- H2CH2CgH4CH2 5 - isoquinolyl 420 2-NH2CH2CgH4CH2 3,4- methylenedioxyCgH3 421 2-NH2CH2CgH4CH2 3,4- ethylenedioxyCgH3 422 2-NH2CH2C H4CH2 2 -imidazolyl 423 2- H2CH2C H 4 CH2 2 -oxazolyl 424 2-NH2CH 2 CgH4CH2 4-isoxazolyl 425 2-NH 2 CH2CgH 4 CH2 4-HOCgH4 426 2-NH2CH2CgH4CH2 3-HOCgH4 427 2-NH2CH2CgH4CH2 3,4-diHOCgH 4 428 2- H2CH2CgH4CH2 4-NH 2 CH 2 CgH 4 429 2-NH2CH2CgH4CH2 3-NH 2 CH 2 CgH 4 430 3-NH 2 CH2CgH 4 CH2 4-MeOCgH4 431 3-NH2CH2C H4CH2 3-MeOCgH4 432 3-NH 2 CH 2 CgH4CH 2 4-NH 2 CgH 4 433 3-NH 2 CH2CgH 4 CH2 3-NH 2 CgH 4 434 3-NH 2 CH 2 CgH4CH 2 2-NH2CgH4 435 3-NH2CH 2 CgH 4 CH2 4-Me2NCgH4 436 3-NH 2 CH 2 CgH4CH2 3-Me2NC H4 111 437 3-NH 2 CH 2 CgH4CH2 2-Me2NC H4 438 3-NH 2 CH 2 CgH4CH2 4 -pyridyl 439 3-NH2CH 2 CgH 4 CH2 3 -pyridyl 440 3-NH2CH2CgH4CH2 2 -pyridyl 441 3-NH2CH2CgH4CH2 2 -thiazolyl 442 3-NH2CH2CgH4CH2 2 -pyrazolyl 443 3-NH2CH2C H4CH2 5 - isoquinolyl 444 3-NH2CH2C6H4CH2 3,4- methylenedioxyCgH3 445 3-NH2CH2C H4CH2 3,4- ethylenedioxyCgH3 446 3-NH2CH2C H4CH2 2 -imidazolyl 447 3-NH2CH2C H4CH2 2 -oxazolyl 448 3-NH2CH2CgH4CH2 4-isoxazolyl 449 3-NH2CH2C H4CH2 4-HOCgH4 450 3-NH2CH2CgH4CH2 3-HOCgH 4 451 3-NH 2 CH2CgH 4 CH2 3,4-diHOCgH4 452 3-NH 2 CH2CgH 4 CH2 4-NH2CH2CgH4 453 3-NH2CH2C H4CH2 3-NH 2 CH 2 CgH 4 454 4-NH 2 CH 2 CgH4CH 2 4-MeOCgH4 455 4-NH 2 CH 2 CgH 4 CH2 3-MeOCgH4 456 4-NH 2 CH 2 CgH 4 CH2 4-NH 2 CgH 4 457 4-NH 2 CH2CgH 4 CH2 3-NH 2 CgH 4 458 4-NH 2 CH 2 CgH4CH 2 2-NH 2 CgH 4 459 4-NH2CH 2 CgH 4 CH2 4-Me2NC H4 460 4-NH 2 CH 2 CgH4CH 2 3-Me2NCgH4 461 4-NH 2 CH2CgH 4 CH2 2-Me2NC H4 462 4-NH 2 CH 2 CgH4CH 2 4 -pyridyl 463 4-NH2CH 2 CgH 4 CH2 3 -pyridyl 464 4-NH 2 CH2CgH 4 CH2 2 -pyridyl 465 4-NH2CH 2 CgH 4 CH2 2 -thiazolyl 466 4-NH2CH 2 CgH 4 CH2 2 -pyrazolyl 467 4-NH2CH 2 CgH 4 CH2 5-isoquinolyl 112 468 4-NH2CH 2 CgH 4 CH2 3,4- methylenedioxyCgH3 469 4-NH2CH 2 CgH 4 CH2 3,4- ethylenedioxyCgH3 470 4-NH2CH 2 CgH 4 CH2 2 -imidazolyl 471 4-NH2CH 2 CgH 4 CH2 2 -oxazolyl 472 4-NH2CH 2 CgH 4 CH 2 4-isoxazolyl 473 4-NH2CH2C6H4CH2 4-HOCgH4 474 4-NH2CH 2 CgH 4 CH 2 3-HOCgH4 475 4-NH2CH 2 CgH 4 CH2 3,4-diHOCgH4 476 4-NH2CH2C H4CH2 4-NH2CH2CgH4 477 4-NH2CH 2 CgH 4 CH2 3-NH 2 CH 2 CgH 4 478 2-Me2NCH2CgH4CH2 4-MeOCgH4 479 2-Me2NCH2C H 4 CH2 3-MeOCgH4 480 2-Me2NCH2C H 4 CH2 4-NH 2 CgH 4 481 2-Me2NCH 2 CgH4CH2 3-NH 2 CgH 4 482 2-Mβ2NCH2CgH4CH2 2-NH2C H4 483 2-Mβ2NCH2CgH4CH2 4-Me2NC H4 484 2-Me2NCH2CgH4CH2 3-Mθ2 C H4 485 2-Me2NCH2CgH4CH2 2-Me2NCgH4 486 2-Me2NCH 2 CgH4CH2 4 -pyridyl 487 2-Mβ2NCH2C H4CH2 3 -pyridyl 488 2-Me2NCH2C H 4 CH2 2 -pyridyl 489 2-Me2NCH2C H4CH2 2-thiazolyl 490 2-Me2NCH2CgH4CH2 2 -pyrazolyl 491 2 -Me2NCH2CgH4CH2 5 - isoquinolyl 492 2 -Me2NCH2CgH4CH2 3,4- methylenedioxyCgH3 493 2-Me2NCH2C H4CH2 3,4- ethylenedioxyCgH3 494 2-Me 2 NCH2CgH4CH 2 2 -imidazolyl 495 2-Me2NCH2CgH4CH2 2 -oxazolyl 496 2-Me2NCH2C H4CH2 4-isoxazolyl 497 2-Me2NCH2C H4CH2 4-HOC6H4 113 498 2-Me2 CH2CgH4CH 2 3-HOCgH4 499 2-Me2NCH2C H4CH2 3,4-diHOCgH4 500 2-Me2NCH2C H4CH2 4-NH 2 CH 2 CgH 4 501 2- e2 CH2CgH4CH2 3-NH2CH2C H4 502 3-Me2NCH2CgH4CH2 4-MeOCgH4 503 3-Me2NCH2CgH4CH 2 3-MeOCgH4 504 3-Me2NCH2CgH4CH2 4-NH 2 CgH 4 505 3-Me2 CH2C H4CH2 3-NH 2 CgH 4 506 3-Me2NCH2CgH4CH2 2-NH 2 CgH 507 3-Me2NCH2C H 4 CH2 4-Me2NC H4 508 3-Me2NCH2CgH4CH2 3-Me2NCgH4 509 3-Me2NCH2CgH4CH2 2- e2NCgH4 510 3-Me2 CH2C H4CH2 4 -pyridyl 511 3-Me2NCH2CgH 4 CH 2 3 -pyridyl 512 3-Me2NCH2CgH4CH2 2 -pyridyl 513 3-Me2 CH2CgH4CH2 2-thiazolyl 514 3-Me2NCH2CgH 4 CH2 2 -pyrazolyl 515 3- e2NCH2CgH 4 CH2 5-isoquinolyl 516 3-Me2NCH2CgH4CH2 3,4- methylenedioxyCgH3 517 3-Me2NCH2CgH4CH2 3,4- ethylenedioxyCgH3 518 3-Me2NCH2CgH4CH2 2 -imidazolyl 519 3-Me2NCH2CgH 4 CH2 2 -oxazolyl 520 3-Me2NCH2CgH4CH2 4-isoxazolyl 521 3-Me2NCH2C H 4 CH2 4-HOCgH4 522 3-Me2NCH2CgH4CH2 3-HOCgH4 523 3-Me2NCH2CgH4CH2 3,4-diHOCgH4 524 3- e2NCH2CgH4CH2 4-NH 2 CH 2 CgH 4 525 3-Me2NCH2CgH4CH2 3-NH 2 CH 2 CgH 4 526 4-Mβ2NCH2CgH4CH2 4-MeOCgH4 527 4-Mβ2NCH2CgH4CH2 3-MeOCgH4 528 4-Me2NCH2C H4CH2 4-NH2C H4 529 4-Me2NCH2CgH4CH2 3-NH 2 CgH 4 114 530 4-Me2NCH2CgH4CH2 2-NH2CgH 4 531 4-Me2NCH2C H4CH2 4-Me2NCgH4 532 4-Me2NCH2CgH 4 CH2 3-Me2NCgH4 533 4-Me2NCH2CgH 4 CH2 2-Me2NCgH4 534 4-Me2NCH2C H4CH2 4 -pyridyl 535 4-Me2NCH2CgH4CH2 3 -pyridyl 536 4-Me2NCH2CgH4CH2 2 -pyridyl 537 4-Me2NCH2C H4CH2 2-thiazolyl 538 4-Me2NCH2CgH4CH2 2 -pyrazolyl 539 4-Me2NCH2CgH4CH2 5 - isoquinolyl 540 4-Me2NCH2C H4CH2 3,4- methylenedioxyCgH3 541 4-Me2NCH2CgH4CH2 3,4- ethylenedioxyCgH3 542 4-Me2NCH2CgH4CH2 2 -imidazolyl 543 4-Me2NCH2CgH4CH2 2 -oxazolyl 545 4-Me2NCH2C H4CH2 4-isoxazolyl 546 4-Me2NCH2C H4CH2 4-HOCgH4 547 4-Me2NCH2CgH4CH2 3-HOCgH4 548 4-Me2NCH2CgH4CH2 3,4-diHOCgH 4 549 4-Me2NCH2CgH4CH2 4-NH 2 CH2CgH 4 550 4-Me2NCH2C H4CH2 3-NH 2 CH 2 CgH 4 551 H 3-MeOCgH4 552 H 4-NH 2 CgH 4 553 H 3-NH 2 CgH 4 554 H 2-NH2CgH4 555 H 4-Me2NCgH4 556 H 3-Me2NCgH4 557 H 2-Me NCgH4 558 H 3 -pyridyl 559 H 2 -pyridyl 560 H 2 -thiazolyl 561 H 2 -pyrazolyl 562 H 5 -isoquinolyl 115 563 H 3,4- methylenedioxyCgH3 564 H 3,4- ethylenedioxyCgH3 565 H 2 -imidazolyl 566 H 2 -oxazolyl 567 H 4-isoxazolyl 568 H 4-HOCgH4 569 H 3-HOCgH4 570 H 3,4-diHOCgH 4 571 H 4-NH 2 CH 2 CgH 4 572 H 3-NH 2 CH 2 CgH 4 573 Me 3-MeOCgH4 574 Me 4-NH 2 CgH 4 575 Me 3-NH 2 CgH 4 576 Me 2-NH2CgH4 577 Me 4-Me2NCgH4 578 Me 3-Me2NCgH4 579 Me 2-Me2NCgH4 580 Me 3 -pyridyl 581 Me 2 -pyridyl 582 Me 2-thiazolyl 583 Me 2 -pyrazolyl 584 Me 5 -isoquinolyl 585 Me 3,4- ethylenedioxyCgH3 586 Me 2 -imidazolyl 587 Me 2 -oxazolyl 588 Me 4-isoxazolyl 589 Me 3-HOCgH4 590 Me 3,4-diHOCgH4 591 Me 4-NH 2 CH 2 CgH 4 592 Me 3-NH 2 CH 2 CgH 4 593 Et 3-MeOCgH4 594 Et 4-NH 2 CgH 4 116 595 Et 3-NH 2 CgH 4 596 Et 2- H2C H4 597 Et 4-Me2NCgH4 598 Et 3-Me2NCgH 4 599 Et 2-Me2NC H4 660000 EEtt 4-pyridyl 601 Et 3 -pyridyl 601 Et 2 -pyridyl 603 Et 2 -thiazolyl 604 Et 2 -pyrazolyl 660055 EEtt 5-isoquinolyl 606 Et 3,4- methylenedioxyCgH3 607 Et 3,4- ethylenedioxyC6H3 6 60088 E Ett 2-imidazolyl 609 Et 2 -oxazolyl 610 Et 4-isoxazolyl 611 Et 4-HOCgH4 612 Et 3-HOCgH4 6 61133 E Ett 3,4-diHOC6H 4 614 Et 4-NH 2 CH 2 CgH 4 615 Et 3-NH 2 CH 2 CgH4 616 Me2NCH 2 3-MeOCgH 4 617 Me2NCH2 4-NH 2 CgH 4 6 61188 M Mee22 CCHH22 3-NH 2 CgH4 619 Me2NCH2 2-NH 2 CgH 4 620 Me2NCH2 4-Me2NC H4 621 Me2NCH2 3-Me NCgH 4 622 Me2NCH2 2-Me2NCgH4 6 62233 M Mee22NNCCHH22 4 -pyridyl 624 Me2NCH2 3 -pyridyl 625 Me2 CH2 2 -pyridyl 626 Me 2 CH2 2-thiazolyl 627 Me2NCH2 2 -pyrazolyl 117 628 Me2NCH2 5-isoquinolyl 629 Me2NCH2 3,4- methylenedioxyCgH3 630 Me2NCH2 3,4- ethylenedioxyCgH3 631 Me2NCH2 2 -imidazolyl 632 Me2NCH2 2 -oxazolyl 633 Me2NCH2 4-isoxazolyl 634 Me2NCH2 4-HOC6H4 635 Me2NCH2 3-HOCgH4 636 Me2NCH2 3,4-diHOCgH 4 637 Me2NCH2 4-NH 2 CH 2 CgH 4 638 Me2NCH2 3-NH2CH CgH 4 639 EtNHCH2 3-MeOCgH4 640 EtNHCH2 4-NH 2 CgH 641 EtNHCH2 3-NH 2 CgH 4 642 EtNHCH2 2-NH2CgH 4 643 EtNHCH2 4-Me2NC H 4 644 EtNHCH2 3-Me2NCgH 4 645 EtNHCH2 2-Me2NC H 4 646 EtNHCH2 4-pyridyl 647 EtNHCH2 3 -pyridyl 648 EtNHCH2 2 -pyridyl 649 EtNHCH2 2-thiazolyl 650 EtNHCH2 2 -pyrazolyl 651 EtNHCH2 5-isoquinolyl 652 EtNHCH2 3,4- methylenedioxyCgH3 653 EtNHCH2 3,4- ethylenedioxyCgH3 654 EtNHCH2 2 -imidazolyl 655 EtNHCH2 2 -oxazolyl 656 EtNHCH2 4-isoxazolyl 657 EtNHCH2 4-HOCgH4 118 658 EtNHCH2 3-HOCgH4 659 EtNHCH2 3,4-diHOCgH4 660 EtNHCH2 4-NH 2 CH 2 CgH 4 661 EtNHCH2 3-NH 2 CH 2 CgH4 662 HOCH2CH2NHCH2 3-MeOCgH4 663 HOCH2CH2NHCH2 4-NH 2 CgH 4 664 HOCH2CH2NHCH2 3-NH 2 CgH 4 665 HOCH2CH2NHCH2 2-NH2C H4 666 HOCH2CH2NHCH2 4-Me2NCgH 4 667 HOCH2CH2NHCH2 3-Me2NCgH4 668 HOCH2CH2NHCH2 2- e2NC H4 669 HOCH2CH2NHCH2 4 -pyridyl 670 HOCH2CH2NHCH2 3 -pyridyl 671 HOCH2CH2NHCH2 2 -pyridyl 672 HOCH2CH2NHCH2 2 -thiazolyl 673 HOCH2CH2NHCH2 2 -pyrazolyl 674 HOCH2CH2NHCH2 5 - isoquinolyl 675 HOCH2CH2NHCH2 3,4- methylenedioxyCgH3 676 HOCH2CH2NHCH2 3,4- ethylenedioxyCgH3 677 HOCH2CH2NHCH2 2 -imidazolyl 678 HOCH2CH2NHCH2 2 -oxazolyl 679 HOCH2CH2NHCH2 4-isoxazolyl 680 HOCH2CH2NHCH2 4-HOC6H4 681 HOCH2CH2NHCH2 3-HOCgH4 682 HOCH2CH2NHCH2 3,4-diHOCgH 4 683 HOCH2CH2NHCH2 4-NH2CH2C H4 684 HOCH2CH2NHCH2 3-NH 2 CH 2 CgH 4 685 H2NCH2CH2NHCH2 4-MeOCgH4 686 H2NCH2CH2NHCH2 3-MeOCgH 4 687 H2NCH2CH2NHCH2 4-NH 2 CgH 4 688 H2NCH2CH2NHCH2 3-NH 2 CgH 4 689 H2NCH2CH2NHCH2 2-NH2CgH 4 119 690 H2NCH2CH2NHCH2 4-Me2NCgH4 691 H2NCH2CH2NHCH2 3-Me2NC H4 692 H2NCH2CH2NHCH2 2-Me2NCgH4 693 H2NCH2CH2NHCH2 4 -pyridyl 694 H2NCH2CH2NHCH2 3 -pyridyl 695 H2NCH2CH2NHCH2 2 -pyridyl 696 H2NCH2CH2NHCH2 2 -thiazolyl 697 H2NCH2CH2NHCH2 2 -pyrazolyl 698 H2NCH2CH2NHCH2 5 -isoquinolyl 699 H2NCH2CH2NHCH2 3,4- methylenedioxyCgH3 700 H2NCH2CH2NHCH2 3,4- ethylenedioxyCgH3 701 H2NCH2CH2NHCH2 2 -imidazolyl 702 H2NCH2CH2NHCH2 2 -oxazolyl 703 H2NCH2CH2NHCH2 4-isoxazolyl 704 H2NCH2CH2NHCH2 4-HOCgH4 705 H2NCH2CH2NHCH2 3-HOCgH4 706 H2NCH2CH2NHCH2 3,4-diHOCgH 4 707 H2NCH2CH2NHCH2 4-NH 2 CH 2 CgH4 708 H2NCH2CH2NHCH2 3-NH 2 CH 2 CgH4 709 Me2NCH2CH2NHCH2 4-MeOCgH4 710 Me2NCH2CH2NHCH2 3-MeOCgH4 711 Me2NCH2CH2NHCH2 4-NH 2 CgH 4 712 Me2NCH2CH2NHCH2 3-NH2C H4 713 Me2NCH2CH2NHCH2 2-NH2CgH4 714 Me2NCH2CH2NHCH2 4-Me2NCgH4 715 Me2NCH2CH2NHCH2 3-Me2NCgH4 716 Me2NCH2CH2NHCH2 2-Me2NCgH4 717 Me2NCH2CH2NHCH2 4 -pyridyl 718 Me2NCH2CH2NHCH2 3 -pyridyl 719 Me2NCH2CH2NHCH2 2 -pyridyl 720 Me2NCH2CH2NHCH2 2-thiazolyl 721 Me2NCH2CH2NHCH2 2 -pyrazolyl 120 722 Me2NCH2CH2NHCH2 5 -isoquinolyl 723 Me2NCH2CH2 HCH2 3,4- methylenedioxyCgH3 724 Me2NCH2CH 2 NHCH2 3,4- ethylenedioxyCgH3 725 Me2NCH2CH2NHCH2 2 -imidazolyl 726 Me2NCH2CH2NHCH2 2 -oxazolyl 727 Me2NCH2CH2NHCH2 4-isoxazolyl 728 Me2NCH2CH NHCH2 4-H0CgH4 729 Me2NCH2CH2NHCH2 3-H0CgH4 730 Me2NCH2CH 2 NHCH2 3,4-diHOCgH4 731 Me2 CH2CH2NHCH2 4-NH 2 CH 2 CgH 4 732 Me2NCH2CH2NHCH2 3-NH 2 CH 2 CgH 4 733 1 -morpholinylmethyl 3-MeOCgH4 734 1 -morpholinylmethyl 4-NH 2 CgH 4 735 1 -morpholinylmethyl 3-NH 2 CgH 4 736 1 -morpholinylmethyl 2-NH2C H4 737 1 -morpholinylmethyl 4-Me2NCgH4 738 1-morpholinylmethyl 3-Me2NCgH4 739 1-morpholinylmethyl 2-Me2NCgH4 740 1 -morpholinylmethyl 4 -pyridyl 741 1-morpholinylmethyl 3 -pyridyl 742 1 -morpholinylmethyl 2 -pyridyl 743 1-morpholinylmethyl 2 -thiazolyl 744 1 -morpholinylmethyl 2 -pyrazolyl 745 1 -morpholinylmethyl 5 - isoquinolyl 746 1 -morpholinylmethyl 3,4- methylenedioxyCgH3 747 1 -morpholinylmethyl 3,4- ethylenedioxyCgH3 748 1 -morpholinylmethyl 2 -imidazolyl 749 1-morpholinylmethyl 2 -oxazolyl 750 1 -morpholinylmethyl 4-isoxazolyl 751 1 -morpholinylmethyl 4-HOCgH4 752 1 -morpholinylmethyl 3-HOC H4 121 753 1 -morpholinylmethyl 3,4-diHOCgH4 754 1 -morpholinylmethyl 4-NH 2 CH 2 CgH 4 755 1 -morpholinylmethyl 3-NH 2 CH 2 CgH4 756 1-thiomorpholinylmethyl 3-MeOCgH4 757 1 -thiomorpholinylmethyl 4-NH 2 CgH 4 758 1 -thiomorpholinylmethyl 3-NH 2 CgH 4 759 1-thiomorpholinylmethyl 2-NH2C H4 760 1 -thiomorpholinylmethyl 4-Me2NCgH4 761 1-thiomorpholinylmethyl 3-Me2NCgH4 762 1 -thiomorpholinylmethyl 2-Me2NCgH 4 763 1 -thiomorpholinylmethyl 4 -pyridyl 764 1-thiomorpholinylmethyl 3 -pyridyl 765 1- thiomorpholinylmethyl 2 -pyridyl 766 1-thiomorpholinylmethyl 2-thiazolyl 767 1-thiomorpholinylmethyl 2 -pyrazolyl 768 1-thiomorpholinylmethyl 5 -isoquinolyl 769 1-thiomorpholinylmethyl 3,4- methylenedioxyCgH3 770 1-thiomorpholinylmethyl 3,4- ethylenedioxyCgH3 771 1-thiomorpholinylmethyl 2 -imidazolyl 772 1-thiomorpholinylmethyl 2 -oxazolyl 773 1-thiomorpholinylmethyl 4-isoxazolyl 774 1-thiomorpholinylmethyl 4-HOCgH4 775 1-thiomorpholinylmethyl 3-HOCgH4 776 1-thiomorpholinylmethyl 3,4-diHOC6H4 777 1 - hiomorpholinylmethyl 4-NH 2 CH 2 CgH4 778 1-thiomorpholinylmethyl 3-NH 2 CH 2 CgH4 779 1-piperazinylmethyl 3-MeOCgH4 780 1-piperazinylmethyl 4-NH 2 CgH4 781 1-piperazinylmethyl 3-NH 2 CgH 4 782 1-piperazinylmethyl 2-NH2C H4 783 1-piperazinylmethyl 4-Me2NCδH4 784 1 -piperazinylmethyl 3-Me 2 NCgH4 785 1 -piperazinylmethyl 2-Me2NCgH4 122 786 1 -piperazinylmethyl 4 -pyridyl 787 1 -piperazinylmethyl 3 -pyridyl 788 1 -piperazinylmethyl 2 -pyridyl 789 1-piperazinylmethyl 2-thiazolyl 790 1 -piperazinylmethyl 2 -pyrazolyl 791 1 -piperazinylmethyl 5 - isoquinolyl 792 1 -piperazinylmethyl 3,4- methylenedioxyCgH3 793 1 -piperazinylmethyl 3,4- ethylenedioxyCgH3 794 1 -piperazinylmethyl 2 -imidazolyl 795 1 -piperazinylmethyl 2 -oxazolyl 796 1-piperazinylmethyl 4-isoxazolyl 797 1 -piperazinylmethyl 4-HOCgH4 798 1 -piperazinylmethyl 3-HOCgH4 799 1 -piperazinylmethyl 3,4-diHOCgH4 800 1 -piperazinylmethyl 4-NH 2 CH 2 CgH4 801 1 -piperazinylmethyl 3-NH 2 CH 2 CgH 4 Table 3 Example R x R Number 802 2 -pyridylmethyl 4-MeOCgH4 803 2 -pyridylmethyl 3-MeOCgH4 804 2 -pyridylmethyl 4-NH 2 CgH 4 805 2 -pyridylmethyl 3-NH 2 CgH 4 806 2 -pyridylmethyl 2-NH 2 CgH 4 123 807 2 -pyridylmethyl 4- e2NCgH4 808 2 -pyridylmethyl 3-Me2NCgH 4 809 2 -pyridylmethyl 2-Me2NCgH4 810 2 -pyridylmethyl 4 -pyridyl 811 2 -pyridylmethyl 3 -pyridyl 812 2 -pyridylmethyl 2 -pyridyl 813 2 -pyridylmethyl 2 -thiazolyl 814 2 -pyridylmethyl 2 -pyrazolyl 815 2 -pyridylmethyl 5 -isoquinolyl 816 2 -pyridylmethyl 3,4- methylenedioxyCgH3 817 2 -pyridylmethyl 3,4- ethylenedioxyCgH3 818 2 -pyridylmethyl 2 -imidazolyl 819 2 -pyridylmethyl 2 -oxazolyl 820 2 -pyridylmethyl 4-isoxazolyl 821 2 -pyridylmethyl 4-HOC6H4 822 2 -pyridylmethyl 3-HOCgH4 823 2 -pyridylmethyl 3,4-diHOCgH4 824 2 -pyridylmethyl 4-NH 2 CH 2 CgH 4 825 2 -pyridylmethyl 3-NH2CH2C H4 826 3 -pyridylmethyl 4-MeOCgH4 827 3 -pyridylmethyl 3-MeOCgH4 828 3 -pyridylmethyl 4-NH 2 CgH 4 829 3 -pyridylmethyl 3-NH 2 CgH 4 830 3 -pyridylmethyl 2-NH2CgH4 831 3 -pyridylmethyl 4-Me2 CgH4 832 3 -pyridylmethyl 3-Me2NC H4 833 3 -pyridylmethyl 2-Me2NC H4 834 3 -pyridylmethyl 4 -pyridyl 835 3 -pyridylmethyl 3 -pyridyl 836 3 -pyridylmethyl 2 -pyridyl 837 3 -pyridylmethyl 2 -thiazolyl 838 3 -pyridylmethyl 2 -pyrazolyl 839 3 -pyridylmethyl 5 -isoquinolyl 124 840 3 -pyridylmethyl 3,4- methylenedioxyCgH3 841 3 -pyridylmethyl 3,4- ethylenedioxyCgH3 842 3 -pyridylmethyl 2 -imidazolyl 843 3 -pyridylmethyl 2 -oxazolyl 844 3 -pyridylmethyl 4-isoxazolyl 845 3 -pyridylmethyl 4-HOCgH4 846 3 -pyridylmethyl 3-HOCgH4 847 3 -pyridylmethyl 3,4-diHOCgH4 848 3 -pyridylmethyl 4-NH 2 CH 2 CgH 4 849 3 -pyridylmethyl 3-NH2CH2CgH4 850 4 -pyridylmethyl 4-MeOCgH4 851 4 -pyridylmethyl 3-MeOCgH4 852 4 -pyridylmethyl 4-NH 2 CgH 4 853 4 -pyridylmethyl 3-NH2CgH4 854 4 -pyridylmethyl 2-NH 2 CgH 4 855 4 -pyridylmethyl 4- e2NCgH4 856 4 -pyridylmethyl 3-Me2NCgH4 857 4 -pyridylmethyl 2-Me2NCgH4 858 4 -pyridylmethyl 4 -pyridyl 859 4 -pyridylmethyl 3 -pyridyl 860 4 -pyridylmethyl 2 -pyridyl 861 4 -pyridylmethyl 2-thiazolyl 862 4 -pyridylmethyl 2 -pyrazolyl 863 4 -pyridylmethyl 5-isoquinolyl 864 4 -pyridylmethyl 3,4- methylenedioxyCgH3 865 4 -pyridylmethyl 3,4- ethylenedioxyCgH3 866 4 -pyridylmethyl 2 -imidazolyl 867 4 -pyridylmethyl 2 -oxazolyl 868 4 -pyridylmethyl 4-isoxazolyl 869 4 -pyridylmethyl 4-HOCgH4 870 4 -pyridylmethyl 3-HOCgH4 871 4 -pyridylmethyl 3,4-diHOCgH 4 125 872 4 -pyridylmethyl 4-NH 2 CH 2 CgH4 873 4 -pyridylmethyl 3-NH 2 CH 2 CgH 4 874 2-NH2CgH4 4-MeOCgH 4 875 2-NH2CgH4 3-MeOCgH4 876 2-NH2CgH4 4-NH 2 CgH 4 877 2-NH 2 CgH 4 3-NH 2 CgH 4 878 2-NH 2 CgH 4 2-NH2CgH4 879 2-NH2CgH4 4- e2 C H4 880 2-NH2CgH4 3-Me2NCgH4 881 2-NH2CgH4 2-Me2NCgH4 882 2-NH2CgH4 4 -pyridyl 883 2-NH2CgH 4 3 -pyridyl 884 2-NH2CgH4 2 -pyridyl 885 2-NH2CgH4 2 -thiazolyl 886 2-NH2CgH4 2 -pyrazolyl 887 2-NH 2 CgH 4 5 -isoquinolyl 888 2-NH CgH4 3,4- methylenedioxyCgH3 889 2-NH 2 CgH 4 3,4- ethylenedioxyCgH3 890 2-NH 2 C 6 H 4 2 -imidazolyl 891 2-NH2CgH4 2-oxazolyl 892 2-NH2CgH4 4-isoxazolyl 893 2-NH 2 C 6 H 4 4-HOCgH4 894 2-NH2CgH4 3-HOCgH 4 895 2-NH2C H4 3,4-diHOCgH4 896 2-NH2CgH4 4-NH 2 CH 2 CgH4 897 2-NH2CgH4 3-NH 2 CH 2 CgH4 898 3-NH 2 CgH 4 4-MeOCgH4 899 3-NH 2 CgH 4 3-MeOCgH4 900 3-NH 2 CgH 4 4-NH 2 CgH 4 901 3-NH 2 C 6 H 4 3-NH 2 CgH 4 902 3-NH 2 CgH 4 2-NH2CgH4 903 3-NH 2 CgH 4 4-Me2NCgH4 126 904 3-NH 2 CgH 4 3-Me2NC H4 905 3-NH 2 CgH 4 2-Me2NCgH4 906 3-NH 2 CgH 4 4 -pyridyl 907 3- H2CgH4 3 -pyridyl 908 3-NH 2 CgH 4 2 -pyridyl 909 3-NH 2 CgH 4 2-thiazolyl 910 3-NH 2 CgH 4 2 -pyrazolyl 911 3-NH 2 CgH 4 5-isoquinolyl 912 3-NH2CgH4 3,4- methylenedioxyCgH3 913 3-NH 2 C 6 H 4 3,4- ethylenedioxyCgH3 914 3-NH 2 CgH 4 2 -imidazolyl 915 3-NH 2 CgH 4 2 -oxazolyl 916 3-NH 2 CgH 4 4-isoxazolyl 917 3-NH 2 CgH 4 4-HOCgH 4 918 3-NH 2 CgH 4 3-HOCgH 4 919 3-NH 2 CgH 4 3,4-diHOCgH4 920 3-NH 2 CgH 4 4-NH 2 CH 2 CgH 4 921 3-NH 2 CgH 4 3-NH 2 CH 2 CgH4 922 4-NH 2 CgH 4 4-MeOCgH4 923 4-NH 2 CgH 4 3-MeOCgH4 924 4-NH 2 CgH 4 4-NH 2 CgH 4 925 4-NH CgH 4 3-NH 2 CgH 4 926 4-NH 2 CgH 4 2-NH 2 CgH 4 927 4-NH 2 CgH 4 4-Me2NCgH4 928 4-NH 2 CgH 4 3-Me2NCgH4 930 4-NH 2 CgH 4 2-Me2NCgH 4 931 4-NH 2 CgH 4 4 -pyridyl 932 4-NH 2 CgH 3 -pyridyl 933 4-NH 2 CgH 4 2 -pyridyl 934 4-NH 2 C 6 H 4 2-thiazolyl 935 4-NH 2 CgH 4 2 -pyrazolyl 936 4-NH 2 CgH 4 5-isoquinolyl 127 937 4-NH 2 CgH 4 3 , 4 - methylenedioxyCgH3 938 4-NH 2 CgH 4 3,4- ethylenedioxyCgH3 939 4-NH 2 CgH 4 2 -imidazolyl 940 4-NH 2 CgH 4 2 -oxazolyl 941 4-NH 2 CgH 4 4-isoxazolyl 942 4-NH 2 CgH 4 4-HOCgH 4 943 4-NH 2 CgH 4 3-HOCgH4 944 4-NH 2 CgH 4 3,4-diH0CgH 4 945 4-NH 2 CgH 4 4-NH 2 CH 2 CgH 4 946 4-NH 2 CgH 4 3-NH 2 CH 2 CgH 4 947 2-MeOCgH4 4-MeOCgH4 948 2-MeOCgH4 3-MeOCgH4 949 2-MeOCgH4 4-NH2CgH4 950 2-MeOCgH4 3-NH 2 CgH 4 951 2-MeOCgH4 2- H2C H 4 952 2-MeOCgH4 4-Me2NCgH 4 953 2-MeOCgH4 3-Me2NCgH 4 954 2-MeOCgH4 2-Me2NCgH 4 955 2-MeOCgH4 4 -pyridyl 956 2-MeOCgH4 3 -pyridyl 957 2-MeOCgH4 2 -pyridyl 958 2-MeOCgH4 2-thiazolyl 959 2-MeOCgH4 2 -pyrazolyl 960 2-MeOCgH4 5-isoquinolyl 961 2-MeOCgH4 3,4- methylenedioxyCgH3 962 2-MeOCgH4 3,4- ethylenedioxyCgH3 963 2-MeOCgH4 2 -imidazolyl 964 2-MeOCgH4 2-oxazolyl 965 2-MeOC6H4 4-isoxazolyl 966 2-MeOCgH4 4-HOCgH4 128 967 2-MeOCgH4 3 -HOCgH 4 968 2-MeOCgH4 3,4-diHOCgH4 969 2-MeOCgH4 4-NH 2 CH 2 C 6 H 4 970 2-MeOCgH4 3-NH 2 CH 2 CgH 4 971 3-MeOCgH4 4-MeOCgH4 972 3-MeOCgH4 3-MeOCgH 4 973 3-MeOCgH4 4-NH 2 CgH 4 974 3-MeOCgH 4 3-NH 2 CgH 4 975 3-MeOCgH4 2-NH2CgH 4 976 3-MeOCgH4 4-Me2 C H4 977 3-MeOCgH4 3-Me2NCgH4 978 3-MeOCgH4 2-Me2NCgH4 979 3-MeOCgH4 4 -pyridyl 980 3-MeOCgH4 3 -pyridyl 981 3-MeOCgH4 2 -pyridyl 982 3-MeOCgH4 2-thiazolyl 983 3-MeOCgH4 2 -pyrazolyl 984 3-MeOCgH4 5-isoquinolyl 985 3-MeOCgH4 3,4- methylenedioxyCgH3 986 3-MeOCgH4 3,4- ethylenedioxyCgH3 987 3-MeOCgH4 2 -imidazolyl 988 3-MeOCgH4 2 -oxazolyl 989 3-MeOCgH4 4-isoxazolyl 990 3-MeOC6H4 4-HOCgH4 991 3-MeOCgH4 3-HOCgH4 992 3-MeOCgH4 3,4-diHOCgH4 993 3-MeOCgH4 4-NH 2 CH2CgH 4 994 3-MeOCgH4 3-NH 2 CH 2 CgH4 995 4-MeOCgH4 4-MeOCgH4 996 4-MeOCgH4 3-MeOCgH4 997 4-MeOCgH4 4-NH2CgH4 998 4-MeOCgH4 3-NH 2 CgH 4 129 999 4- eOC6H4 2- H2C H4 1000 4-MeOCgH4 4-Me2NCgH 4 1001 4-MeOCgH4 3-Me2NCgH4 1002 4-MeOCgH4 2-Me2NC H4 1003 4-MeOCgH4 4 -pyridyl 1004 4-MeOCgH4 3 -pyridyl 1005 4-MeOCgH4 2 -pyridyl 1006 4-MeOCgH 4 2 -thiazolyl 1007 4-MeOCgH4 2 -pyrazolyl 1008 4-MeOCgH4 5-isoquinolyl 1009 4-MeOCgH4 3,4- methylenedioxyCgH3 1010 4-MeOCgH 4 3,4- ethylenedioxyCgH3 1011 4-MeOCgH4 2 -imidazolyl 1012 4-MeOCgH4 2 -oxazolyl 1013 4-MeOCgH4 4-isoxazolyl 1014 4-MeOCgH 4 4-HOCgH 4 1015 4-MeOCgH4 3-HOCgH 4 1016 4-MeOCgH4 3,4-diH0CgH 4 1017 4-MeOCgH4 4-NH 2 CH 2 CgH4 1018 4-MeOCgH4 3-NH 2 CH 2 CgH 4 1019 2-HOCgH4 4-MeOCgH4 1020 2-HOCgH4 3-MeOCgH4 1021 2-HOCgH4 4-NH2CgH 4 1022 2-HOCgH4 3-NH CgH 4 1023 2-HOCgH4 2-NH2CgH4 1024 2-HOCgH4 4-Me2NC H4 1025 2-HOCgH4 3-Me2NC H4 1026 2-HOC H4 2-Me2NC H4 1027 2-HOCgH4 4 -pyridyl 1028 2-HOCgH4 3 -pyridyl 1029 2-HOCgH4 2-pyridyl 1030 2-HOC H4 2-thiazolyl 130 1031 2-HOCgH4 2 -pyrazolyl 1032 2-HOCgH4 5 -isoquinolyl 1033 2-HOCgH4 3,4- methylenedioxyCgH3 1034 2-HOCgH4 3,4- ethylenedioxyCgH3 1035 2-HOCgH4 2 -imidazolyl 1036 2-HOCgH4 2 -oxazolyl 1037 2-H0CgH4 4-isoxazolyl 1038 2-HOCgH4 4-H0CgH4 1039 2-HOCgH4 3-HOCgH4 1040 2-HOCgH4 3,4-diHOCgH4 1041 2-HOCgH4 4-NH 2 CH 2 CgH4 1042 2-HOCgH4 3-NH 2 CH 2 CgH4 1043 3-HOCgH4 4-MeOCgH4 1044 3-HOCgH4 3-MeOCgH4 1045 3-HOCgH 4 4-NH 2 CgH 4 1046 3-HOCgH4 3-NH 2 CgH 4 1047 3-HOCgH4 2-NH2C H4 1048 3-HOCgH4 4-Me2NCgH 4 1049 3-HOCgH4 3-Me2NC H4 1050 3-HOCgH4 2-Me2NC6H 4 1051 3-HOCgH4 4 -pyridyl 1052 3-HOCgH4 3 -pyridyl 1053 3-HOCgH4 2 -pyridyl 1054 3-HOCgH4 2 -thiazolyl 1055 3-HOCgH4 2 -pyrazolyl 1056 3-HOCgH4 5 - isoquinolyl 1057 3-HOCgH4 3,4- methylenedioxyCgH3 1058 3-HOCgH4 3,4- ethylenedioxyCgH3 1059 3-HOCgH4 2 -imidazolyl 1060 3-HOCgH4 2 -oxazolyl 131 1061 3-HOCgH4 4-isoxazolyl 1062 3-HOCgH4 4-H0CgH4 1063 3-HOCgH4 3-HOCgH4 1064 3-HOCgH 4 3,4-diHOCgH4 1065 3-HOCgH4 4-NH 2 CH 2 CgH 4 1066 3-HOCgH4 3-NH 2 CH 2 CgH4 1067 4-H0CgH4 4-MeOCgH 4 1068 4-HOCgH4 3-MeOCgH4 1069 4-HOCgH4 4-NH 2 CgH 4 1070 4-HOCgH4 3-NH 2 CgH 1071 4-HOCgH4 2-NH2CgH 4 1072 4-HOCgH4 4-Me2 CgH4 1073 4-HOCgH4 3-Me2 C H4 1074 4-HOCgH4 2-Me2NCgH 4 1075 4-HOCgH4 4 -pyridyl 1076 4-HOCgH4 3 -pyridyl 1077 4-HOCgH4 2 -pyridyl 1078 4-HOCgH4 2-thiazolyl 1079 4-HOCgH4 2 -pyrazolyl 1080 4-HOCgH4 5 -isoquinolyl 1081 4-HOCgH 4 3,4- methylenedioxyCgH3 1082 4-HOCgH4 3,4- ethylenedioxyCgH3 1083 4-HOCgH4 2 -imidazolyl 1084 4-HOCgH4 2 -oxazolyl 1085 4-HOCgH4 4-isoxazolyl 1086 4-HOCgH4 4-HOCgH 4 1087 4-HOCgH4 3-HOCgH4 1088 4-HOCgH4 3,4-diHOCgH4 1089 4-HOCgH4 4-NH2CH2CgH4 1090 4-HOC H4 3-NH2CH2CgH4 1091 4-ClCgH4 4-MeOCgH4 1092 4-ClCgH4 3-MeOCgH4 132 1093 4-ClCgH4 4-NH 2 CgH 4 1094 4-ClCgH4 3-NH 2 CgH 4 1095 4-ClCgH4 2-NH2CgH 4 1096 4-ClCgH4 4-Me2NCgH4 1097 4-ClCgH4 3-Me2NC H4 1098 4-ClCgH4 2-Me2NCgH4 1099 4-ClCgH4 4 -pyridyl 1100 4-ClCgH4 3 -pyridyl 1101 4-ClCgH4 2 -pyridyl 1102 4-ClCgH4 2-thiazolyl 1103 4-ClCgH4 2 -pyrazolyl 1104 4-ClCgH4 5 -isoquinolyl 1105 4-ClCgH 4 3,4- methylenedioxyCgH3 1106 4-ClCgH 4 3,4- ethylenedioxyCgH3 1107 4-ClCgH 4 2 -imidazolyl 1108 4-ClCgH 4 2 -oxazolyl 1109 4-ClCgH 4 4-isoxazolyl 1110 4-ClCgH4 4-HOCgH4 1111 4-ClCgH4 3-HOCgH4 1112 4-ClCgH 4 3,4-diHOCgH 4 1113 4-ClCgH 4 4-NH 2 CH 2 CgH 4 1114 4-ClCgH4 3-NH 2 CH 2 CgH 4 1115 2-NH2CH2CgH4 4-MeOCgH4 1116 2-NH2CH 2 CgH4 3-MeOCgH4 1117 2-NH2CH2CgH4 4- H2C6H4 1118 2-NH2CH2CgH4 3-NH 2 CgH 4 1119 2-NH2CH2C H4 2-NH2C H4 1120 2-NH2CH 2 CgH 4 4-Me2 CgH4 1121 2-NH2CH2C H4 3-Me2NCgH4 1122 2-NH2CH2CgH4 2-Me2NCgH4 1123 2-NH2CH2CgH4 4 -pyridyl 1124 2-NH 2 CH 2 CgH 4 3 -pyridyl 133 1125 2-NH 2 CH 2 CgH4 2 -pyridyl 1126 2-NH2CH2C H4 2-thiazolyl 1127 2-NH 2 CH 2 CgH 4 2 -pyrazolyl 1128 2-NH2CH2CgH4 5-isoquinolyl 1129 2-NH2CH2CgH4 3,4- methylenedioxyCgH3 1130 2-NH 2 CH 2 CgH 4 3,4- ethylenedioxyCgH3 1131 2-NH 2 CH 2 CgH 4 2 -imidazolyl 1132 2-NH2CH2CgH4 2 -oxazolyl 1133 2-NH2CH2CgH4 4-isoxazolyl 1134 2-NH2CH2C H4 4-HOCgH4 1135 2-NH2CH2CgH 4 3-HOCgH4 1136 2-NH 2 CH 2 CgH4 3,4-diHOCgH 4 1137 2-NH2CH2CgH 4 4-NH 2 CH 2 CgH 4 1138 2-NH2CH2CgH 4 3-NH 2 CH2CgH4 1139 3-NH 2 CH 2 CgH 4 4-MeOCgH 4 1140 3-NH 2 CH2CgH 4 3-MeOCgH 4 1141 3-NH2CH 2 CgH 4 4-NH 2 CgH 4 1142 3-NH 2 CH 2 CgH4 3- H2CgH 4 1143 3-NH 2 CH 2 CgH 4 2-NH2CgH 4 1144 3-NH 2 CH 2 CgH4 4-Me2NCgH 4 1145 3-NH 2 CH 2 CgH 4 3-Me2NC H4 1146 3-NH 2 CH 2 CgH4 2-Me NCgH 4 1147 3-NH 2 CH 2 CgH4 4 -pyridyl 1148 3-NH 2 CH 2 CgH 4 3 -pyridyl 1149 3-NH 2 CH 2 CgH 4 2 -pyridyl 1150 3-NH 2 CH 2 CgH 4 2 -thiazolyl 1151 3-NH2CH 2 CgH 4 2 -pyrazolyl 1152 3-NH 2 CH 2 CgH 4 5-isoquinolyl 1153 3-NH 2 CH 2 CgH4 3,4- methylenedioxyCgH3 1154 3-NH 2 CH 2 CgH 4 3,4- ethylenedioxyCgH3 134 1155 3-NH 2 CH 2 CgH 4 2 -imidazolyl 1156 3-NH 2 CH 2 CgH 4 2 -oxazolyl 1157 3-NH 2 CH 2 CgH4 4-isoxazolyl 1158 3-NH 2 CH 2 CgH 4 4-HOC H 4 1159 3-NH 2 CH 2 CgH4 3-HOCgH4 1160 3-NH 2 CH 2 CgH 4 3,4-diHOCgH 4 1161 3-NH 2 CH 2 CgH 4 4-NH 2 CH 2 CgH 4 1162 3-NH 2 CH 2 CgH4 3-NH 2 CH 2 CgH 4 1163 4-NH 2 CH 2 CgH 4 4-MeOCgH4 1164 4-NH 2 CH 2 CgH 4 3-MeOCgH 4 1165 4-NH 2 CH 2 CgH 4 4-NH 2 CgH 4 1166 4-NH 2 CH 2 CgH 4 3-NH 2 CgH 4 1167 4-NH 2 CH 2 CgH 4 2-NH2CgH 4 1168 4-NH 2 CH 2 CgH4 4-Me2NCgH 4 1169 4-NH 2 CH 2 CgH 4 3-Me2NCgH 4 1170 4-NH 2 CH 2 CgH4 2-Me2NC H4 1171 4-NH 2 CH 2 CgH 4 4-pyridyl 1172 4-NH 2 CH 2 CgH 4 3 -pyridyl 1173 4-NH 2 CH 2 CgH4 2 -pyridyl 1174 4-NH 2 CH 2 CgH 4 2-thiazolyl 1175 4-NH 2 CH 2 CgH 4 2 -pyrazolyl 1176 4-NH 2 CH 2 CgH 4 5 -isoquinolyl 1177 4-NH 2 CH 2 CgH 4 3,4- methylenedioxyCgH3 1178 4-NH CH 2 CgH4 3,4- ethylenedioxyCgH3 1179 4-NH 2 CH 2 CgH4 2-imidazolyl 1180 4-NH 2 CH 2 CgH 4 2 -oxazolyl 1181 4-NH 2 CH 2 CgH 4 4-isoxazolyl 1182 4-NH 2 CH 2 CgH 4 4-HOCgH4 1183 4-NH 2 CH 2 CgH4 3-HOCgH4 1184 4-NH2CH2C H4 3,4-diHOCgH 4 1185 4-NH 2 CH 2 CgH4 4-NH 2 CH 2 CgH4 1186 4-NH 2 CH 2 CgH4 3-NH 2 CH2CgH 4 135 1187 2-Me2NCH2CgH4 4-MeOCgH4 1188 2-Me2NCH2CgH4 3-MeOCgH4 1189 2-Me 2 NCH2CgH4 4-NH 2 CgH 4 1190 2-Me2NCH2CgH4 3-NH 2 CgH 4 1191 2-Me2 CH2C H4 2-NH2CgH4 1192 2-Me2NCH2CgH4 4-Me2NCgH 4 1193 2-Me2NCH2CgH4 3-Me2NCgH4 1194 2-Me2NCH2CgH4 2-Me2NCgH 4 1195 2-Me2NCH2CgH4 4 -pyridyl 1196 2-Me2NCH2CgH 4 3 -pyridyl 1197 2-Me2NCH2CgH4 2 -pyridyl 1198 2-Me2NCH2CgH4 2-thiazolyl 1199 2-Me2NCH2C H4 2 -pyrazolyl 1200 2-Me2NCH2C H4 5-isoquinolyl 1201 2-Me2NCH2C H4 3,4- methylenedioxyCgH 1202 2-Me2NCH2C H4 3,4- ethylenedioxyCgH3 1203 2-Me2NCH2CgH4 2 -imidazolyl 1204 2-Me2NCH2CgH4 2 -oxazolyl 1205 2-Me2NCH2CgH4 4-isoxazolyl 1206 2-Me2NCH2CgH4 4-HOCgH4 1207 2-Me2NCH2C H4 3-HOCgH4 1208 2-Me2NCH2C H4 3,4-diHOCgH 4 1209 2-Me2NCH2C H4 4-NH 2 CH 2 CgH 4 1210 2-Me2NCH2CgH4 3-NH CH 2 CgH 4 1211 3-Me2NCH2C H4 4-MeOCgH4 1212 3-Me2NCH2C H4 3-MeOCgH4 1213 3-Me2NCH2CgH4 4-NH 2 CgH 4 1214 3-Me2NCH2C H4 3-NH 2 CgH 4 1215 3- e2NCH2C H4 2-NH2CgH 4 1216 3-Me2NCH2C H4 4- e2NCgH4 1217 3-Me2NCH2C H4 3-Me2NCgH4 1218 3-Me2NCH2CgH4 2-Me2NC H4 136 1219 3-Me2NCH2CgH4 4 -pyridyl 1220 3-Me2NCH2C H4 3 -pyridyl 1221 3-Me2NCH2CgH4 2 -pyridyl 1222 3-Me2NCH2CgH4 2-thiazolyl 1223 3-Me2NCH2CgH4 2 -pyrazolyl 1224 3-Me2NCH2CgH4 5 -isoquinolyl 1225 3-Me2NCH 2 CgH4 3,4- methylenedioxyCgH3 1226 3-Me2NCH 2 CgH4 3,4- ethylenedioxyCgH3 1227 3-Me2NCH2CgH4 2 -imidazolyl 1228 3-Me2NCH2CgH4 2 -oxazolyl 1229 3-Me2NCH2CgH4 4-isoxazolyl 1230 3-Me2NCH 2 CgH 4 4-HOCgH4 1231 3-Me2NCH CgH 4 3-HOCgH4 1232 3-Me2NCH2C H4 3,4-diHOCgH4 1233 3-Me2 CH2C H4 4-NH 2 CH 2 CgH 4 1234 3-Me2NCH2CgH4 3-NH 2 CH 2 CgH 4 1235 4-Me2NCH2C H4 4-MeOCgH4 1236 4-Me2NCH2C H4 3-MeOCgH4 1237 4-Me2NCH2C H4 4-NH 2 CgH 4 1238 4-Me2NCH2CgH4 3-NH 2 CgH 4 1239 4-Me2NCH2CgH4 2-NH2CgH 4 1240 4- e2NCH2C H4 4-Me2NCgH4 1241 4- e2NCH2C H4 3-Me2NCgH4 1242 4-Me2NCH2C H4 2-Me2NC H4 1243 4-Me2NCH2CgH4 4 -pyridyl 1244 4-Me2NCH2C H4 3 -pyridyl 1245 4-Me2NCH2CgH4 2 -pyridyl 1246 4-Me2NCH 2 C H4 2-thiazolyl 1247 4-Me2NCH2CgH4 2 -pyrazolyl 1248 4-Me2NCH2CgH4 5 -isoquinolyl 1249 4-Me2NCH2CgH4 3,4- methylenedioxyCgH3 137 1250 4-Me2NCH2CgH4 3,4- ethylenedioxyCgH3 1251 4-Me2NCH2C H4 2 -imidazolyl 1252 4-Me2NCH2CgH4 2 -oxazolyl 1253 4-Me2NCH2CgH4 4-isoxazolyl 1254 4-Me2NCH2CgH4 4-HOCgH4 1255 4-Me2 CH2CgH4 3-HOCgH4 1256 4-Me2NCH2CgH4 3,4-diHOCgH 4 1257 4-Me2NCH2C H4 4-NH 2 CH 2 C 6 H4 1258 4-Me2NCH2CgH4 3-NH2CH2C H4 1259 H 4-MeOCgH4 1260 H 3-MeOCgH4 1261 H 4-NH 2 CgH 4 1262 H 3-NH 2 CgH 4 1263 H 2-NH2CgH4 1264 H 4-Me2NC H4 1265 H 3-Me2NCgH4 1266 H 2-Me2NC H4 1267 H 4 -pyridyl 1268 H 3 -pyridyl 1269 H 2 -pyridyl 1270 H 2-thiazolyl 1271 H 2 -pyrazolyl 1272 H 5 -isoquinolyl 1273 H 3,4- methylenedioxyCgH3 1274 H 3,4- ethylenedioxyCgH3 1275 H 2 -imidazolyl 1276 H 2 -oxazolyl 1277 H 4-isoxazolyl 1278 H 4-HOC6H4 1279 H 3-HOCgH4 1280 H 3,4-diHOCgH4 1281 H 4-NH 2 CH2CgH 4 138 1282 H 3- H 2 CH2CgH4 1283 Me 4-MeOCgH4 1284 Me 3-MeOCgH 4 1285 Me 4-NH 2 CgH 4 1286 Me 3-NH2CgH4 1287 Me 2- H2CgH 4 1288 Me 4-Me2NCgH4 1289 Me 3-Me2NCgH4 1290 Me 2-Me2NCgH4 1291 Me 4 -pyridyl 1292 Me 3 -pyridyl 1293 Me 2 -pyridyl 1294 Me 2-thiazolyl 1295 Me 2 -pyrazolyl 1296 Me 5 -isoquinolyl 1297 Me 3,4- methylenedioxyCgH3 1298 Me 3,4- ethylenedioxyCgH3 1299 Me 2 -imidazolyl 1300 Me 2 -oxazolyl 1301 Me 4-isoxazolyl 1302 Me 4-HOCgH 4 1303 Me 3-HOCgH4 1304 Me 3,4-diHOCgH4 1305 Me 4-NH 2 CH 2 CgH 4 1306 Me 3-NH 2 CH 2 CgH 4 1307 Et 4-MeOCgH4 1308 Et 3-MeOCgH4 1309 Et 4-NH 2 CgH 4 1310 Et 3-NH 2 CgH 4 1311 Et 2-NH2CgH4 1312 Et 4-Me2 C H4 1313 Et 3-Me2 C6H4 1314 Et 2-Me2NCgH4 139 1315 Et 4-pyridyl 1316 Et 3 -pyridyl 1317 Et 2 -pyridyl 1318 Et 2-thiazolyl 1319 Et 2 -pyrazolyl 11332200 EEtt 5-isoquinolyl 1321 Et 3,4- methylenedioxyCgH3 1322 Et 3,4- ethylenedioxyCgH3 1 1332233 E Ett 2-imidazolyl 1324 Et 2 -oxazolyl 1325 Et 4-isoxazolyl 1326 Et 4-HOCgH4 1327 Et 3-HOCgH 4 1 1332288 E Ett 3,4-diHOCgH 4 1329 Et 4-NH 2 CH 2 C6H 4 1330 Et 3-NH 2 CH2CgH 4 1331 2-NH2CgH4CH2 4-MeOC6H 4 1332 2-NH2CgH4CH2 3-MeOCgH4 1 1333333 2 2--NNHH22CCggHH44CCHH22 4-NH2CgH 4 1334 2-NH2CgH 4 CH2 3-NH 2 CgH 4 1335 2-NH2CgH4CH2 2-NH2C H4 1336 2-NH2CgH4CH2 4-Me2NC H4 1337 2-NH2CgH4CH2 3-Me2NCgH4 1 1333388 2 2--NNHH22CC HH44CCHH22 2-Me2 C H4 1339 2-NH2CgH4CH2 4 -pyridyl 1340 2-NH2C H4CH2 3 -pyridyl 1341 2-NH2CgH4CH2 2 -pyridyl 1342 2-NH2C H4CH2 2-thiazolyl 1 1334433 2 2-- HH22CC HH44CCHH22 2 -pyrazolyl 1344 2-NH2C H4CH2 5-isoquinolyl 1345 2-NH2CgH4CH2 3,4- methylenedioxyCgH3 140 1346 2-NH 2 CgH 4 CH2 3 , 4 - ethylenedioxyCgH3 1347 2-NH 2 CgH4CH2 2 -imidazolyl 1348 2-NH2CgH4CH2 2 -oxazolyl 1349 2-NH2CgH4CH2 4-isoxazolyl 1350 2- H2CgH4CH2 4-HOCgH4 1351 2-NH2CgH 4 CH2 3-HOCgH4 1352 2-NH2C H4CH2 3,4-diHOCgH4 1353 2- H2C H4CH2 4-NH 2 CH 2 CgH 4 1354 2-NH2CgH4CH2 3-NH 2 CH 2 C 6 H 4 1355 3-NH 2 CgH 4 CH 2 4-MeOCgH4 1356 3-NH 2 CgH 4 CH 2 3-MeOCgH4 1357 3-NH 2 CgH 4 CH 2 4-NH 2 CgH 4 1358 3-NH 2 CgH 4 CH 2 3-NH 2 CgH 4 1359 3-NH 2 CgH 4 CH 2 2-NH 2 CgH 4 1360 3-NH 2 CgH 4 CH 2 4-Me2NCgH4 1361 3-NH 2 CgH 4 CH 2 3-Me2NCgH 4 1362 3-NH 2 CgH 4 CH2 2-Me2NCgH 4 1363 3-NH 2 CgH 4 CH 2 4 -pyridyl 1364 3-NH 2 CgH 4 CH 2 3 -pyridyl 1365 3-NH 2 CgH 4 CH2 2 -pyridyl 1366 3-NH 2 CgH 4 CH 2 2-thiazolyl 1367 3-NH 2 CgH 4 CH 2 2 -pyrazolyl 1367 3-NH 2 CgH 4 CH 2 5-isoquinolyl 1369 3-NH 2 CgH 4 CH2 3,4- methylenedioxyCgH3 1370 3-NH 2 CgH 4 CH 2 3,4- ethylenedioxyCgH3 1371 3-NH 2 CgH 4 CH 2 2-imidazolyl 1372 3-NH 2 CgH 4 CH 2 2 -oxazolyl 1373 3-NH 2 CgH 4 CH2 4-isoxazolyl 1374 3-NH 2 CgH 4 CH2 4-HOCgH4 1375 3-NH 2 CgH 4 CH 2 3-HOC6H4 1376 3-NH 2 CgH 4 CH 2 3,4-diHOC6H4 141 1377 3-NH 2 CgH 4 CH 2 4-NH 2 CH 2 CgH4 1378 3-NH2CgH4CH2 3-NH 2 CH 2 CgH 4 1379 4-NH 2 CgH 4 CH 2 4-MeOCgH4 1380 4-NH 2 CgH 4 CH2 3-MeOCgH4 1381 4-NH 2 CgH 4 CH2 4-NH 2 CgH 4 1382 4-NH 2 CgH 4 CH 2 3-NH 2 CgH 4 1383 4-NH 2 CgH 4 CH2 2-NH2CgH 4 1384 4-NH 2 CgH 4 CH 2 4-Me2NCgH4 1385 4-NH 2 CgH 4 CH2 3-Me2NCgH 4 1386 4-NH 2 CgH 4 CH2 2-Me2NCgH4 1387 4-NH 2 CgH 4 CH 2 4 -pyridyl 1388 4-NH 2 CgH 4 CH 2 3 -pyridyl 1389 4-NH 2 CgH 4 CH2 2 -pyridyl 1390 4-NH2CgH 4 CH 2 2-thiazolyl 1391 4-NH 2 CgH 4 CH 2 2 -pyrazolyl 1392 4-NH 2 CgH 4 CH2 5-isoquinolyl 1393 4-NH 2 CgH 4 CH 2 3,4- methylenedioxyCgH3 1394 4-NH 2 CgH 4 CH 2 3,4- ethylenedioxyCgH3 1395 4-NH 2 CgH 4 CH 2 2 -imidazolyl 1396 4-NH 2 CgH 4 CH2 2 -oxazolyl 1397 4-NH 2 CgH 4 CH 2 4-isoxazolyl 1398 4-NH 2 CgH 4 CH 2 4-HOCgH4 1399 4-NH 2 CgH 4 CH 2 3-HOCgH 4 1400 4-NH 2 CgH 4 CH2 3,4-diHOCgH4 1401 4-NH 2 CgH 4 CH 2 4-NH 2 CH 2 CgH 4 1402 4-NH2CgH 4 CH 2 3-NH 2 CH 2 CgH 4 1403 2-MeOCgH4CH2 4-MeOCgH4 1404 2-MeOCgH4CH2 3-MeOCgH4 1405 2-MeOCgH4CH2 4-NH2C H4 1406 2-MeOCgH4CH2 3-NH 2 CgH 4 1407 2-MeOCgH4CH2 2-NH2CgH4 1408 2-MeOCgH4CH2 4-Me2NCgH4 142 1409 2-MeOCgH4CH2 3-Me2NCgH 4 1410 2-MeOCgH4CH2 2-Me2NCgH4 1411 2-MeOCgH4CH2 4 -pyridyl 1412 2-MeOCgH4CH2 3 -pyridyl 1413 2-MeOCgH4CH2 2 -pyridyl 1414 2-MeOCgH4CH2 2-thiazolyl 1415 2-MeOCgH4CH2 2 -pyrazolyl 1416 2-MeOCgH4CH2 5-isoquinolyl 1417 2-MeOCgH4CH2 3,4- methylenedioxyCgH3 1418 2-MeOCgH4CH2 3,4- ethylenedioxyCgH3 1419 2-MeOCgH4CH2 2 -imidazolyl 1420 2-MeOCgH4CH2 2 -oxazolyl 1421 2-MeOCgH4CH2 4-isoxazolyl 1422 2-MeOCgH4CH2 4-HOCgH 4 1423 2-MeOCgH4CH2 3-HOCgH 4 1424 2-MeOCgH4CH2 3,4-diHOCgH 4 1425 2-MeOCgH4CH2 4-NH 2 CH 2 CgH 4 1426 2-MeOCgH4CH2 3-NH 2 CH 2 CgH 4 1427 3-MeOCgH4CH2 4-MeOCgH4 1428 3-MeOCgH 4 CH2 3-MeOCgH 4 1429 3-MeOCgH4CH2 4-NH 2 CgH 4 1430 3-MeOCgH4CH2 3-NH 2 CgH 4 1431 3-MeOCgH4CH2 2-NH2CgH4 1432 3-MeOCgH 4 CH2 4-Me2NCgH4 1433 3-MeOCgH 4 CH2 3-Me2NCgH 4 1434 3-MeOCgH4CH2 2-Me2NCgH 4 1435 3-MeOCgH4CH2 4 -pyridyl 1436 3-MeOCgH 4 CH2 3 -pyridyl 1437 3-MeOCgH 4 CH2 2 -pyridyl 1438 3-MeOCgH 4 CH2 2-thiazolyl 1439 3-MeOCgH4CH2 2 -pyrazolyl 1440 3-MeOCgH 4 CH2 5-isoquinolyl 143 1441 3-MeOCgH4CH2 3 , 4 - methylenedioxyCgH3 1442 3-MeOCgH4CH2 3,4- ethylenedioxyCgH3 1443 3-MeOC6H4CH2 2 -imidazolyl 1444 3-MeOCgH4CH 2 2 -oxazolyl 1445 3-MeOCgH4CH 2 4-isoxazolyl 1446 3-MeOCgH4CH 4-HOCgH4 1447 3-MeOCgH4CH2 3-HOCgH4 1448 3-MeOCgH4CH 2 3,4-diHOCgH 4 1449 3-MeOCgH4CH2 4-NH 2 CH 2 CgH 4 1450 3-MeOCgH4CH 2 3-NH 2 CH 2 CgH 4 1451 4-MeOCgH4CH 2 4-MeOCgH4 1452 4-MeOCgH4CH2 3-MeOCgH 4 1453 4-MeOCgH4CH2 4-NH 2 CgH 4 1454 4-MeOCgH4CH2 3-NH 2 CgH 4 1455 4-MeOCgH4CH2 2-NH2C H 4 1456 4-MeOCgH4CH2 4-Me2NCgH4 1457 4-MeOCgH4CH2 3-Me2NCgH 4 1458 4-MeOCgH4CH2 2-Me2NC H 4 1459 4-MeOCgH4CH2 4 -pyridyl 1460 4-MeOCgH4CH2 3 -pyridyl 1461 4-MeOCgH4CH2 2 -pyridyl 1462 4-MeOCgH4CH2 2-thiazolyl 1463 4-MeOCgH4CH2 2 -pyrazolyl 1464 4-MeOCgH4CH2 5-isoquinolyl 1465 4-MeOCgH4CH2 3,4- methylenedioxyCgH3 1466 4-MeOCgH4CH2 3,4- ethylenedioxyCgH3 1467 4-MeOCgH4CH2 2 -imidazolyl 1468 4-MeOCgH4CH2 2 -oxazolyl 1469 4-MeOCgH4CH2 4-isoxazolyl 1470 4-MeOCgH4CH2 4-H0CgH4 144 1471 4-MeOCgH4CH2 3 -HOCgH4 1472 4-MeOCgH4CH2 3,4-diHOCgH4 1473 4-MeOCgH4CH2 4-NH 2 CH 2 CgH 4 1474 4-MeOCgH4CH2 3-NH 2 CH 2 CgH 4 1475 2-HOCgH4CH2 4-MeOCgH 4 1476 2-HOCgH4CH2 3-MeOCgH4 1477 2-HOCgH4CH2 4-NH 2 CgH 4 1478 2-HOCgH4CH2 3-NH 2 CgH 4 1479 2-HOCgH4CH2 2-NH2CgH 4 1480 2-HOCgH4CH2 4-Me2NC H4 1481 2-HOCgH4CH2 3-Me2NCgH 4 1482 2-HOCgH4CH2 2-Me2NC H4 1483 2-HOCgH4CH2 4 -pyridyl 1484 2-HOCgH 4 CH2 3 -pyridyl 1485 2-HOCgH4CH2 2 -pyridyl 1486 2-HOCgH4CH2 2 -thiazolyl 1487 2-HOCgH4CH2 2-pyrazolyl 1488 2-HOC H 4 CH2 5-isoquinolyl 1489 2-HOCgH4CH2 3,4- methylenedioxyCgH3 1490 2-HOCgH4CH2 3,4- ethylenedioxyCgH3 1491 2-HOCgH4CH2 2 -imidazolyl 1492 2-HOC H4CH2 2 -oxazolyl 1493 2-HOCgH4CH2 4-isoxazolyl 1494 2-HOCgH4CH2 4-HOCgH4 1495 2-HOCgH4CH2 3-HOCgH4 1496 2-HOCgH4CH2 3,4-diHOCgH 4 1497 2-HOCgH4CH2 4-NH2CH2C6H4 1498 2-HOCgH4CH2 3-NH 2 CH 2 CgH4 1499 3-HOCgH4CH2 4-MeOC6H4 1500 3-HOCgH4CH2 3-MeOCgH4 1501 3-HOC6H4CH2 4-NH 2 CgH 4 1502 3-HOC H4CH2 3-NH 2 CgH 4 145 1503 3-HOCgH 4 CH2 2-NH 2 CgH 4 1504 3-HOC H4CH2 4-Me2NCgH4 1505 3-HOCgH4CH2 3-Me2 CgH4 1506 3-HOCgH4CH2 2-Me2NCgH4 1507 3-HOCgH4CH2 4 -pyridyl 1508 3-HOCgH4CH2 3 -pyridyl 1509 3-HOCgH4CH2 2 -pyridyl 1510 3-HOCgH4CH2 2-thiazolyl 1511 3-HOCgH4CH2 2 -pyrazolyl 1512 3-HOCgH4CH2 5-isoquinolyl 1513 3-HOCgH 4 CH2 3,4- methylenedioxyCgH3 1514 3-HOCgH4CH2 3,4- ethylenedioxyCgH3 1514 3-HOCgH 4 CH2 2 -imidazolyl 1516 3-HOCgH4CH2 2 -oxazolyl 1517 3-HOCgH4CH2 4-isoxazolyl 1518 3-HOCgH4CH2 4-HOCgH4 1519 3-HOCgH4CH2 3-HOCgH4 1520 3-HOCgH4CH2 3,4-diHOCgH 4 1521 3-HOCgH4CH2 4-NH 2 CH 2 CgH4 1522 3-HOCgH 4 CH2 3-NH 2 CH 2 CgH 4 1523 4-HOCgH4CH2 4-MeOCgH4 1524 4-HOCgH4CH2 3-MeOCgH4 1525 4-HOCgH4CH2 4-NH 2 CgH 4 1526 4-HOCgH4CH2 3-NH 2 CgH 4 1527 4-HOCgH 4 CH2 2-NH2CgH 4 1528 4-HOCgH4CH2 4-Me2NC H4 1529 4-HOCgH4CH2 3-Me2NC H4 1530 4-HOCgH4CH2 2-Me2NCgH4 1531 4-HOCgH4CH2 4 -pyridyl 1532 4-HOCgH4CH2 3 -pyridyl 1533 4-HOCgH4CH2 2 -pyridyl 1534 4-HOCgH4CH2 2 -thiazolyl 146 1535 4-HOCgH4CH2 2 -pyrazolyl 1536 4-HOCgH4CH2 5- isoquinolyl 1537 4-HOCgH4CH2 3,4- methylenedioxyCgH3 1538 4-HOCgH4CH 2 3,4- ethylenedioxyCgH3 1539 4-HOCgH4CH2 2 -imidazolyl 1540 4-HOCgH 4 CH2 2 -oxazolyl 1541 4-HOCgH4CH2 4-isoxazolyl 1542 4-HOCgH 4 CH2 4-H0CgH4 1543 4-HOCgH4CH2 3-HOCgH4 1544 4-HOC6H4CH2 3,4-diHOCgH4 1545 4-HOCgH4CH2 4-NH 2 CH 2 CgH 4 1546 4-HOCgH 4 CH2 3-NH2CH2C H 4 1547 4-ClCgH 4 CH2 4-MeOCgH 4 1548 4-ClCgH4CH2 3-MeOC6H4 1549 4-ClCgH4CH2 4-NH 2 CgH 4 1550 4-ClCgH4CH2 3-NH 2 CgH 4 1551 4-ClCgH4CH2 2-NH 2 CgH 4 1552 4-ClCgH4CH2 4- e2NCgH4 1553 4-ClCgH4CH2 3-Me2NCgH4 1554 4-ClCgH 4 CH2 2-Me2NCgH4 1555 4-ClCgH4CH2 4 -pyridyl 1556 4-ClCgH4CH2 3 -pyridyl 1557 4-ClCgH 4 CH2 2 -pyridyl 1558 4-ClCgH4CH2 2-thiazolyl 1559 4-ClCgH4CH2 2 -pyrazolyl 1560 4-ClCgH4CH2 5- isoquinolyl 1561 4-ClCgH4CH2 3,4- methylenedioxyCgH3 1562 4-ClCgH 4 CH2 3,4- ethylenedioxyCgH3 1563 4-ClCgH4CH2 2 -imidazolyl 1564 4-ClCgH4CH 2 2 -oxazolyl 147 O 99/54308 F i/usywυβoi 1565 4-ClCgH4CH 2 4-isoxazolyl 1566 4-ClCgH 4 CH2 4-HOCgH4 1567 4-ClCgH4CH2 3-HOCgH4 1568 4-ClCgH4CH2 3,4-diHOCgH4 1569 4-ClCgH 4 CH2 4-NH 2 CH 2 CgH 4 1570 4-ClCgH4CH2 3-NH 2 CH 2 CgH 4 1571 2-NH2CH2CgH 4 CH 2 4-MeOCgH4 1572 2-NH2CH2CgH4CH2 3-MeOCgH4 1573 2-NH2CH2CgH4CH2 4-NH 2 CgH 4 1574 2-NH2CH2CgH4CH2 3-NH 2 CgH 4 1575 2-NH2CH 2 CgH 4 CH 2 2-NH2CgH4 1576 2-NH2CH2CgH4CH2 4-Me2 CgH4 1577 2-NH2CH2CgH4CH 2 3-Me2NCgH4 1578 2-NH2CH2CgH4CH 2 2-Me2NCgH4 1579 2-NH2CH CgH4CH 4 -pyridyl 1580 2-NH2CH2CgH4CH2 3 -pyridyl 1581 2-NH2CH2CgH4CH2 2 -pyridyl 1582 2-NH 2 CH 2 CgH4CH 2 2 -thiazolyl 1583 2-NH2CH 2 CgH 4 CH2 2 -pyrazolyl 1584 2-NH 2 CH 2 CgH4CH2 5 -isoquinolyl 1585 2-NH 2 CH 2 CgH4CH2 3,4- methylenedioxyCgH3 1586 2-NH 2 CH 2 CgH4CH 2 3,4- ethylenedioxyCgH3 1587 2-NH 2 CH 2 CgH4CH2 2 -imidazolyl 1588 2-NH 2 CH 2 CgH4CH2 2 -oxazolyl 1589 2- H2CH2C H4CH2 4-isoxazolyl 1590 2-NH 2 CH 2 CgH4CH 2 4-HOCgH4 1591 2-NH 2 CH 2 CgH4CH 2 3-HOCgH4 1592 2-NH2CH 2 CgH 4 CH2 3,4-diHOCgH4 1593 2-NH 2 CH 2 CgH4CH 2 4-NH 2 CH 2 CgH4 1594 2-NH 2 CH 2 CgH4CH2 3-NH 2 CH 2 CgH 4 1595 3-NH 2 CH2CgH 4 CH2 4-MeOCgH4 1596 3-NH 2 CH 2 CgH4CH 2 3-MeOCgH4 148 1597 3-NH2CH2CgH4CH2 4-NH 2 CgH 4 1598 3-NH 2 CH 2 CgH4CH 2 3-NH 2 CgH 4 1599 3-NH 2 CH2CgH 4 CH2 2-NH2CgH4 1600 3-NH2CH2CgH4CH2 4-Me2 CgH4 1601 3-NH 2 CH2CgH 4 CH2 3-Me2NCgH4 1602 3-NH2CH2CgH4CH2 2-Me2NCgH4 1603 3-NH 2 CH2CgH 4 CH2 4 -pyridyl 1604 3-NH 2 CH 2 CgH4CH 2 3 -pyridyl 1605 3-NH 2 CH 2 CgH4CH2 2 -pyridyl 1606 3- H2CH2C H4CH2 2 -thiazolyl 1607 3-NH2CH 2 CgH 4 CH2 2 -pyrazolyl 1608 3-NH 2 CH 2 CgH4CH2 5 -isoquinolyl 1609 3-NH2CH 2 CgH 4 CH2 3,4- methylenedioxyCgH3 1610 3-NH2CH2CgH4CH2 3,4- ethylenedioxyCgH3 1611 3-NH2CH2CgH4CH2 2 -imidazolyl 1612 3-NH2CH2CgH 4 CH2 2 -oxazolyl 1613 3-NH2CH2CgH4CH2 4-isoxazolyl 1614 3-NH2CH2C H4CH2 4-HOC6H4 1615 3-NH2CH2CgH4CH2 3-HOCgH 4 1616 3-NH 2 CH 2 CgH 4 CH2 3,4-diHOCgH 4 1617 3-NH2CH2C H4CH2 4-NH2CH2CgH4 1618 3-NH 2 CH 2 CgH4CH 2 3-NH 2 CH 2 CgH 4 1619 4-NH 2 CH 2 CgH 4 CH2 4-MeOCgH4 1620 4-NH 2 CH2CgH 4 CH2 3-MeOCgH4 1621 4-NH 2 CH 2 CgH4CH2 4-NH 2 CgH 4 1622 4-NH 2 CH2CgH 4 CH2 3-NH 2 CgH 4 1623 4-NH 2 CH 2 CgH 4 CH2 2-NH 2 CgH 4 1624 4-NH2CH2CgH 4 CH 2 4-Me2NCgH4 1625 4-NH 2 CH2CgH 4 CH2 3-Me 2 NCgH 4 1626 4-NH2CH2C H4CH2 2- e2NC H4 1627 4-NH 2 CH 2 CgH 4 CH2 4 -pyridyl 1628 4-NH 2 CH2CgH 4 CH2 3 -pyridyl 149 1629 4-NH 2 CH2CgH 4 CH2 2 -pyridyl 1630 4-NH 2 CH2CgH 4 CH2 2 -thiazolyl 1631 4-NH 2 CH 2 CgH 4 CH2 2 -pyrazolyl 1632 4-NH 2 CH 2 CgH4CH 2 5 -isoquinolyl 1633 4-NH2CH 2 CgH 4 CH2 3,4- methylenedioxyCgH3 1634 4-NH2CH2CgH4CH2 3,4- ethylenedioxyCgH3 1635 4-NH 2 CH2CgH 4 CH2 2 -imidazolyl 1636 4-NH 2 CH 2 CgH4CH 2 2 -oxazolyl 1637 4-NH2CH2CgH4CH2 4-isoxazolyl 1638 4-NH2CH2C H4CH2 4-HOCgH4 1639 4-NH 2 CH 2 CgH4CH 2 3-HOCgH4 1640 4-NH 2 CH 2 CgH4CH2 3,4-diHOCgH4 1641 4-NH2CH 2 CgH 4 CH2 4-NH 2 CH 2 CgH 4 1642 4-NH 2 CH2CgH 4 CH2 3-NH2CH 2 C 6 H4 1643 2-Me2NCH2CgH4CH2 4-MeOC6H4 1644 2-Me2NCH2CgH4CH2 3-MeOCgH4 1645 2-Me2NCH2CgH4CH2 4-NH 2 CgH 4 1646 2-Me2NCH2CgH4CH2 3-NH 2 CgH 4 1647 2-Me2NCH2CgH4CH2 2-NH2CgH4 1648 2-Me2NCH2C H4CH2 4-Me2NCgH4 1649 2-Me2NCH2C H4CH2 3-Me2NCgH4 1650 2-Me2NCH2CgH4CH2 2-Me2NCgH 4 1651 2-Me2NCH2CgH4CH2 4 -pyridyl 1652 2-Me2NCH2C H4CH2 3 -pyridyl 1653 2-Me2NCH2CgH4CH2 2 -pyridyl 1654 2-Me2NCH2CgH4CH2 2-thiazolyl 1655 2-Me2NCH2CgH4CH2 2 -pyrazolyl 1656 2-Me 2 NCH2C H4CH2 5 -isoquinolyl 1657 2-Me2NCH2CgH4CH2 3,4- methylenedioxyCgH3 1658 2-Me 2 NCH2CgH4CH2 3,4- ethylenedioxyCgH3 150 1659 2-Me2 CH 2 CgH4CH2 2 -imidazolyl 1660 2-Me2NCH2CgH4CH2 2 -oxazolyl 1661 2-Me2NCH2CgH4CH2 4-isoxazolyl 1662 2-Me2NCH2CgH4CH2 4-H0CgH4 1663 2-Me2NCH2CgH4CH 2 3-HOCgH4 1664 2-Me2NCH2CgH4CH2 3,4-diHOCgH4 1665 2-Me2NCH 2 CgH4CH2 4-NH 2 CH 2 CgH 4 1666 2 -Me2NCH2C H4CH2 3-NH 2 CH CgH4 1667 3-Me2NCH 2 CgH4CH 4-MeOCgH4 1668 3-Me 2 NCH 2 CgH4CH2 3-MeOCgH4 1669 3 -Me2NCH2CgH4CH2 4-NH 2 CgH 4 1670 3-Me2NCH2C H4CH2 3-NH CgH4 1671 3-Me2NCH2C H4CH2 2-NH 2 CgH4 1672 3-Me2NCH2CgH4CH2 4-Me NCgH4 1673 3-Me2NCH2CgH4CH2 3-Me 2 NCgH4 1674 3-Me2NCH2CgH4CH2 2-Me 2 NCgH4 1675 3-Me2NCH2CgH4CH2 4 -pyridyl 1676 3-Me2NCH2CgH4CH2 3 -pyridyl 1677 3-Me2NCH CgH4CH 2 2 -pyridyl 1678 3-Me2NCH2CgH4CH2 2-thiazolyl 1679 3-Me2NCH2CgH4CH2 2 -pyrazolyl 1680 3-Me2NCH2CgH4CH 5 - isoquinolyl 1681 3-Me2NCH2CgH4CH2 3,4- methylenedioxyCgH3 1682 3-Me2NCH2C H4CH2 3,4- ethylenedioxyCgH3 1683 3-Me2NCH2CgH4CH2 2 -imidazolyl 1684 3-Me2NCH2C H4CH2 2 -oxazolyl 1685 3-Me2NCH2CgH4CH2 4-isoxazolyl 1686 3-Me2NCH2C H4CH2 4-HOCgH4 1687 3-Me2NCH2CgH4CH2 3-HOCgH4 1688 3-Me2NCH2CgH4CH2 3,4-diHOCgH4 1689 3-Me2NCH2CgH4CH2 4-NH 2 CH 2 CgH 4 1690 3-Me2NCH2CgH4CH2 3-NH 2 CH 2 CgH4 151 WO 99/54308 PCT/US99/UJM 1691 4-Me2NCH2CgH 4 CH2 4-MeOCgH4 1692 4-Me2NCH2CgH4CH2 3-MeOCgH4 1693 4-Me2 CH2CgH4CH2 4-NH2CgH 1694 4-Me2NCH2C H4CH2 3-NH 2 CgH 4 1695 4-Me2NCH2C H4CH2 2-NH2CgH4 1696 4-Me2 CH 2 CgH4CH2 4-Me2NCgH4 1697 4-Me2NCH2CgH4CH2 3-Me2NC H4 1698 4- e2NCH2CgH 4 CH2 2-Me2NCgH4 1699 4-Me2NCH2CgH4CH2 4 -pyridyl 1700 4-Me 2 NCH 2 CgH4CH 2 3 -pyridyl 1701 4-Me2NCH2CgH4CH2 2 -pyridyl 1702 4-Me 2 NCH 2 CgH4CH 2 2-thiazolyl 1703 4-M NCH2CgH4CH2 2 -pyrazolyl 1704 4-Me2NCH2CgH4CH2 5 -isoquinolyl 1705 4-Me2 CH2CgH4CH2 3,4- methylenedioxyCgH3 1706 4-Me2NCH2CgH4CH2 3,4- ethylenedioxyCgH3 1707 4-Me2NCH2CgH4CH2 2 -imidazolyl 1708 4-Me2NCH2C H CH2 2 -oxazolyl 1709 4-Me2 CH2C H4CH2 4-isoxazolyl 1710 4-Me2NCH2CgH4CH2 4-HOCgH 4 1711 4-Me2NCH2C H4CH2 3-HOCgH 4 1712 4-Me2 CH2CgH4CH2 3,4-diHOCgH4 1713 4-Me2NCH2CgH 4 CH2 4-NH 2 CH 2 CgH 4 1714 4-Me2NCH2C H 4 CH2 3-NH 2 CH 2 CgH4 152 Table 4 Example R 1 R 2 Number 1715 Methyl 4-MeOCgH4 1716 C1CH2 4-MeOCgH4 1717 cyclopropyl 4-MeOCgH4 1718 isopropyl 4-MeOCgH4 1719 ethyl 4-MeOCgH4 1720 cyclopentyl 4-MeOCgH4 1721 cyclobutyl 4-MeOCgH4 1722 benzyl 4-MeOCgH4 1723 n-propyl 4-MeOCgH4 1724 4-ClCgH 4 CH2 4-MeOCgH4 1725 3-MeOCgH4CH2 4-MeOCgH4 1726 4-MeOCgH4CH2 4-MeOCgH4 1727 3,4-diMeOCgH 4 CH2 4-MeOCgH4 1728 2,5-diMeOCgH4CH2 4-MeOCgH4 1729 Methyl 2-MeOCgH4 1730 Methyl 3,4-diMeOCgH4 1731 3,4- (OCH 2 0)CgH 4 CH2 4-MeOCgH4 1732 3-thiophenylCH2 4-MeOCgH4 1733 2-MeOCgH4CH2 4-MeOCgH4 1734 3,4-diClOCgH4CH2 4-MeOCgH4 1735 2,4-diClOCgH4CH2 4-MeOCgH4 1736 2-ClCgH4CH2 4-MeOCgH4 153 1737 H2NCH2 4-MeOCgH4 1738 HOCH 2 NHCH CH 2 4-MeOCgH4 1739 Me 2 NCH 2 4-MeOCgH4 1740 piperazinylCH 2 4-MeOCgH4 1741 4-Me-piperazinylCH 2 4-MeOCgH4 1742 4-HOCH 2 CH 2 - 4-MeOCgH4 piperazinylCH 1743 piperidinylCH 2 4-MeOCgH4 1744 4-NH 2 CH 2 - 4-MeOCgH4 piperidinylCH2 1745 CH3CH2NHCH2 4-MeOCgH4 1746 thiomorpholinylCH2 4-MeOCgH4 1747 morpholinylCH2 4-MeOCgH4 1748 pyyrolidinylCH2 4-MeOCgH4 1749 4 -pyridylCH 2 NHCH 2 4-MeOCgH4 1750 4-CH3CONHCgH4CH2 4-MeOCgH4 1751 4-CH3θCONHCgH4CH2 4-MeOCgH4 1752 4-NH2CH2C0NHC H4CH2 4-MeOCgH4 1753 4-Me2NCH2CONHCgH 4 CH2 4-MeOCgH4 1754 4-N 3 CgH 4 CH2 4-MeOCgH4 1755 4-NH 2 CgH 4 CH 2 4-MeOCgH4 1756 CgHsNH 4-MeOCgH4 1757 CH3CH2CH2NH 4-MeOCgH4 1758 4-NH 2 C 6 H 4 CH 2 NH 4-MeOC6H4 1759 4-MeOCgH4 4-pyridyCH 2 NH 1760 Methyl 4-HOCgH4 1761 H 4-MeOCgH4 1762 Methyl 3 -pyridyl 1763 Methyl 4 -pyridyl 1764 H 4-pyridyl 1765 Methyl CgH 5 154 1766 Methyl 4-MeSCgH4 1767 Methyl 4-MeS02CgH4 1768 Methyl 4-Me2NCgH4 1769 morpholinylCH 4-Me2NCgH4 1770 Me 2 NCH 2 4-Mθ2NCgH4 1771 Me 2 NCH 2 4- (piperdinyl) CgH_; 1772 Me 2 NCH 2 4- (morpholinyl) C H4 1773 Me 2 NCH 2 4-CH3CH2θCgH4 1774 Me 2 NCH 2 4 -CH3CH2CH2CH2CgH- 1775 Me 2 NCH 2 4-CH3CH2C H4 1776 Me 2 NCH 2 4-CH3CH2CH2CgH4 155

Claims: CLAIMS What is claimed is 1. A compound according to formula (I] X or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein: X is selected from the group: O, S, and NR; R is selected from the group: H, C 1 - 4 alkyl, and NR 5 R 5a ; R 1 is selected from the group: H, Cχ-io alkyl substituted with 0-3 Rc , C2-10 alkenyl substituted with 0-3 Rc , C2-10 alkynyl substituted with 0-3 R c , -NHR 4 , C3-10 carbocycle substituted with 0-5 R , and 3-10 membered heterocycle containing from 1-4 heteroatoms selected from 0, N, and S and substituted with 0-5 R ; R is independently at each occurrence selected from the group: halo, -CN , N 3 , NO2 , C1-4 alkyl, C1- 4 haloalkyl, NR 3 R 3a , =0, OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , NHC(0)NR 3 R 3a , NHC(S)NR 3 R 3a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , S02NR 3 R 3a , S02R 3b , and 5-10 membered heterocycle 156 containing from 1-4 heteroatoms selected from 0, N, and S; alternatively, when two R a ' s are present on adjacent carbon atoms they combine to form -OCH2O- or -OCH2CH2O-; R is independently at each occurrence selected from the group: halo, -CN, NO2 , C1-4 alkyl, C1-4 haloalkyl, NR 3 R 3a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , OR 3 , COR 3 , CO2 3 , CONR 3 R 3a , NHC(0)NR 3 R 3a , NHC (S) NR 3 R 3a , Sθ2NR 3 R 3a , and Sθ2R 3b ; R is independently at each occurrence selected from the group: halo, -CN, NO2 , C1-4 alkyl, C1-4 haloalkyl, NR 3 R 3a , NR 5 NR 5 R 5a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , =0, OR 3 , COR 3 , C02 3 , CONR 3 R 3a , NHC (O) NR 3 R 3a , NHC (S) NR 3 R 3 a SO2N R 3a , Sθ2R 3b , C3-10 carbocycle substituted with 0-5 R a , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S, substituted with ,3 0-3 R " R 2 is selected from the group: H, Ci-io alkyl substituted with 0-3 R C , C2-10 alkenyl substituted with 0-3 R C , C2-10 alkynyl substituted with 0-3 R C , -(CF2)trCF3, C3-10 carbocycle substituted with 0-5 R , and 3-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S and substituted with 0-5 R ; 3 R is selected from the group: H, halo, -CN, N0 2 , C 1 _ haloalkyl, NR 5 R 5a , NR 5 NR 5 R 5a , NR 5 C(0)OR 5 , NR 5 C(0)R 5 , =0, 157 OR 5 , COR 5 , C0 2 R 5 , CONR 5 R 5a , NHC (0) NR 5 R 5a , NHC (S) NR 5 R 5a , S0 2 NR R a , S0 2 R , Ci-4 alkyl, phenyl, and benzyl; R is selected from the group: H, Cχ_4 alkyl, phenyl, and benzyl ; alternatively, R 3 and R a , together with the nitrogen atom to which they are attached, form a heterocycle having 4-8 atoms in the ring and containing an additional 0-1 N, S, or 0 atom and substituted with 0-3 R 3c ; "3 V-ι R is selected from the group: H, C1-. 4 alkyl, phenyl, and benzyl ; R 3c is independently at each occurrence selected from the group: halo, -CN , N 3 , NO2 , C 1 - 4 alkyl, C1- 4 haloalkyl, NR 3 R 3b , =0, OR 3 , COR 3 , CO2R 3 , CONR 3 R 3b , NHC(0)NR 3 R3 b , NHC (S) NR 3 R3 b , NR 3 C(0)OR 3 , NR 3 C (O) R 3 , Sθ2NR 3 R 3 , Sθ2 3b , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S; R 4 is independently at each occurrence selected from the group: H, -CN, C1-.4 alkyl, C1-.4 haloalkyl, NR 3 R 3a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , NHC(0)NR 3 R 3a , NHC (S) NR 3 R 3a , Sθ2NR 3 R 3a , Sθ2R 3b , C3-10 carbocycle substituted with 0-5 R a , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected 3 from O, N, and S, substituted with 0-3 R ; 158 R 5 is independently selected from the group: H, C3 . -4 alkyl, phenyl and benzyl ; R^a is independently selected from the group: H, C1-4 alkyl , phenyl and benzyl ; R5£ > is independently selected from the group: H, Cχ_4 alkyl , phenyl and benzyl ; and m is selected from 0, 1, 2, and 3. 2. A compound according to claim 1, wherein: X is selected from the group: 0, S, and NR; R is selected from the group: H, C1-4 alkyl, and NR^R 5 ; R 1 is selected from the group: H, C 1 -.5 alkyl substituted with 0-3 Rc , C 2 -5 alkenyl substituted with 0-3 Rc , C 2 -5 alkynyl substituted with 0-3 R , -NHR 4 , C3_g carbocycle substituted with 0-5 R , and 3-6 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S and substituted with 0-5 R ; R is independently at each occurrence selected from the group: halo, -CN, N 3 , NO2 , C1-4 alkyl, C1-4 haloalkyl, NR 3 R 3a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , =0, OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , NHC(0)NR 3 R 3a , NHC (S) R R 3a , Sθ2NR3R3a 7 Sθ2R 3b , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from 0, N, and S ; 159 alternatively, when two R a ' s are present on adjacent carbon atoms they combine to form -OCH2O- or -OCH2CH2O- ; R is independently at each occurrence selected from the group: halo, -CN, NO2 , C1- 4 alkyl, Cχ_4 haloalkyl, NR 3 R 3a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , NHC(0)NR 3 R3a NHC (S) NR 3 R 3a , Sθ2NR 3 R 3a , and Sθ2R 3b ; R is independently at each occurrence selected from the group: halo, -CN, NO2 , C1- 4 alkyl, C3 . - 4 haloalkyl, NR 3 R 3a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , NR 5 NR 5 R 5a , =0, OR 3 , COR 3 , Cθ2R 3 , CONR 3 R 3 , NHC(0)NR 3 R 3a , NHC (S) NR 3 R 3a , SO 2 NR R 3a , Sθ2R 3b , C3-10 carbocycle substituted with 0-5 R a , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S, substituted with 0-3 R 3 ; R 2 is selected from the group: H, C1-5 alkyl substituted with 0-3 R C , C2-5 alkenyl substituted with 0-3 R C , C 2 -5 alkynyl substituted with 0-3 R C , -(CF2)mCF3, C3- carbocycle substituted with 0-5 R , and 3-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S and substituted with 0-5 R ; 3 R is selected from the group: H, halo, -CN, N0 2 , ^. 4 haloalkyl, NR 5 R 5a , NR 5 NR 5 R 5& , NR 5 C(0)OR 5 , NR 5 C(0)R 5 , =0, OR 5 , COR 5 , C0 2 R 5 , C0NR 5 R 5S , NHC (0) NR 5 R 5a , NHC (S) R 5 R 5a , S0 2 NR R , S0 2 R , Cχ-4 alkyl, phenyl, and benzyl; 160 3a R is selected from the group: H, C 1 - 4 alkyl, phenyl, and benzyl ; alternatively, R 3 and R 3a , together with the nitrogen atom to which they are attached, form a heterocycle having 4-8 atoms in the ring and containing an additional 0-1 N, S, or O atom and substituted with 0-3 R 3c ; "2 V\ R is selected from the group: H, C1-4 alkyl, phenyl, and benzyl; R 3c is independently at each occurrence selected from the group: halo, -CN , N 3 , NO2 , C1- 4 alkyl, C1- 4 haloalkyl, NR 3 R 3b , =0, OR 3 , COR 3 , CO2R 3 , CONR 3 R 3b , NHC(0)NR 3 R 3t> , NHC (S) NR 3 R 3b , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , S02NR 3 R , S02R 3b , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from 0, N, and S; R 4 is independently at each occurrence selected from the group: H, -CN, C 1 - 4 alkyl, C1-4 haloalkyl, NR 3 R 3a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , NHC(0)NR 3 R 3a , NHC(S)NR 3 R 3a , Sθ2NR 3 R3a / sθ2R 3b , C3-10 carbocycle substituted with 0-5 R a , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from 0, N, and S, substituted with 0-3 R ; R 5 is independently selected from the group: H, C1-4 alkyl, phenyl , and benzyl ; 161 R 5a is independently selected from the group: H, C1- 4 alkyl , phenyl and benzyl ; R 5b is independently selected from the group: H, C1-4 alkyl , phenyl , and benzyl ; and m is selected from 0, 1, 2, and 3. 3. A compound according to claim 2, wherein: X is selected from the group: 0 and S ; R 1 is selected from the group: H, C1-5 alkyl substituted with 0-3 Rc , C2-5 alkenyl substituted with 0-3 Rc , -NHR 4 , C3_ carbocycle substituted with 0-5 R a , and 3-6 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S and substituted with 0-5 R ; R is independently at each occurrence selected from the group: halo, -CN, N 3 , C1- 4 alkyl, C1- 4 haloalkyl, NR 3 R 3a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , NHC(0)NR 3 R 3a , Sθ2NR 3 R3a ; sθ2R 3b , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S; alternatively, when two R a ' s are present on adjacent carbon atoms they combine to form -OCH2O- or -OCH2CH2O- ; R is independently at each occurrence selected from the group: halo, -CN, C1-4 alkyl, C1-4 haloalkyl, NR 3 R 3a , 162 NR 3 C(0)OR 3 , NR 3 C(0)R 3 , OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , NHC(0)NR 3 R 3a , Sθ2NR 3 R 3a , and Sθ2R 3b ; R is independently at each occurrence selected from the group: halo, -CN, C1-.4 alkyl, C1-4 haloalkyl, NR R , NR 5 NR 5 R 5a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , =0, OR 3 , COR 3 , C02R 3 , C0NR 3 R 3a , NHC(0)NR 3 R 3a , Sθ2NR 3 R 3a , S02R 3b , C3-10 carbocycle substituted with 0-5 R a , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected 3 from 0, N, and S, substituted with 0-3 R R 2 is selected from the group: H, C1-5 alkyl substituted with 0-3 R , C2-5 alkenyl substituted with 0-3 R , -(CF2)mCF3, C3_ carbocycle substituted with 0-5 R , and 3-6 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S and substituted with 0-5 R b ; 3 R is selected from the group: H, halo, -CN, N0 , C 1 _ 4 haloalkyl, NR 5 R 5a , NR 5 NR 5 R 5& , NR 5 C(0)OR 5 , NR 5 C(0)R 5 , =0, OR 5 , COR 5 , C0 2 R 5 , CONR 5 R 5a , NHC (0) R 5 R 5a , NHC (S) NR 5 R 5& , S0 2 NR R , S0 R , C1-4 alkyl, phenyl, and benzyl; R a is selected from the group: H, C1- 4 alkyl, phenyl, and benzyl ; alternatively, R 3 and R 3a , together with the nitrogen atom to which they are attached, form a heterocycle having 163 5-6 atoms in the ring and containing an additional 0-1 N, S, or 0 atom and substituted with 0-3 R 3c R is selected from the group: H, Cχ- 4 alkyl, phenyl, and benzyl ; R 3c is independently at each occurrence selected from the group: halo, -CN , N 3 , NO2 , C1-4 alkyl, C1-4 haloalkyl, NR 3 R 3b , =0, OR 3 , COR 3 , CO2R 3 , CONR 3 R3 b , NHC(0)NR 3 R3 b , NHC (S) NR 3 R3 b ; NR 3 C (0) OR 3 , NR 3 C (0) R 3 , Sθ2NR 3 R 3 , Sθ 2 R 3b , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S; R 4 is independently at each occurrence selected from the group: H, -CN, C1- 4 alkyl, C1-4 haloalkyl, NR 3 R 3a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , NHC(0)NR 3 R 3a , NHC(S)NR 3 R3a ? Sθ2NR 3 R 3a , Sθ2R 3b , C3-10 carbocycle substituted with 0-5 R , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S, substituted with 0-3 R ; R 5 is independently selected from the group: H, C1- 4 alkyl, phenyl , and benzyl ; R 5a is independently selected from the group: H, C1-4 alkyl , phenyl and benzyl ; R^b i s independently selected from the group: H, C1-4 alkyl, phenyl, and benzyl; and m is selected from 0, 1, 2, and 3 164 4. A compound according to claim 3, wherein: X is selected from the group: O and S; R 1 is selected from the group: H, Cχ-5 alkyl substituted with 0-2 R , -NHR 4 , C3_g carbocycle substituted with 0-5 R , and 5-6 membered heterocycle containing from 1-4 heteroatoms selected from 0, N, and S and substituted with 0-5 R ; R is independently at each occurrence selected from the group: halo, -CN, N 3 , Cχ- 4 alkyl, Cχ-4 haloalkyl, NR 3 R 3a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , OR 3 , COR 3 , CO2R 3 , CONR 3 R 3a , NHC(0)NR 3 R3a S02 R 3 R 3a , sθ2R 3b / and 5 _ 6 membered heterocycle containing from 1-4 heteroatoms selected from 0, N, and S; alternatively, when two R a ' s are present on adjacent carbon atoms they combine to form -OCH2O- or -OCH2CH 2 0- ; R is independently at each occurrence selected from the group: halo, C1-4 alkyl, C1- 4 haloalkyl, NR R , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , OR 3 , COR 3 , C0 R 3 , CONR R 3a , NHC(0)NR 3 R3a ; S0 2 NR 3 R 3 a and S02R 3b ; R is independently at each occurrence selected from the group: halo, C1-4 alkyl, Cχ_4 haloalkyl, NR 3R3a , NR 5 NR 5 R 5a , NR 3 C(0)0R 3 , NR 3 C(0)R 3 , OR 3 , COR 3 , C02R 3 , CONR 3 R 3a , NHC (0) NR 3 R 3a , Sθ2NR 3 R 3a , S02R 3b , C3-10 165 carbocycle substituted with 0-5 R , and 5-6 membered heterocycle containing from 1-4 heteroatoms selected 3 from 0, N, and S, substituted with 0-3 R ; R 2 is selected from the group: C1-5 alkyl substituted with 0-3 R , -(CF2)m CF 3 C3-6 carbocycle substituted with 0-5 R , and 5-6 membered heterocycle containing from 1-4 heteroatoms selected from O, N, and S and substituted with 0-3 R ; 3 R is selected from the group: H, halo, -CN, N0 2 , C ] __ 4 haloalkyl, NR 5 R 5a , NR 5 NR 5 R 5a , NR 5 C(0)OR 5 , NR 5 C(0)R 5 , =0, OR 5 , COR 5 , C0 2 R 5 , CONR 5 R 5a , NHC (0) NR 5 R 5& , NHC (S) NR 5 R 5a , 5 5a 5b S0 NR R , S0 2 R , C 1 -4 alkyl, phenyl, and benzyl; R is selected from the group: H, C1- 4 alkyl, phenyl, and benzyl ; alternatively, R 3 and R 3a , together with the nitrogen atom to which they are attached, form a heterocycle having 5-6 atoms m the ring and containing an additional 0-1 N, S, or O atom and substituted with 0-3 R3c; * 3 V\ R is selected from the group: H, Cχ_4 alkyl, phenyl, and benzyl ; R 3c is independently at each occurrence selected from the group: halo, -CN , N 3 , NO2, C1-4 alkyl, C1-4 haloalkyl, NR 3 R 3b , =0, OR 3 , COR 3 , CO2R 3 , CONR 3 R 3b , NHC(0)NR 3 R 3b , NHC(S)NR 3 R 3b , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , 166 Sθ2NR 3 R 3 , Sθ2R 3b , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected from 0, N, and S; R 4 is independently at each occurrence selected from the group: H, -CN, Cχ-4 alkyl, Cχ- 4 haloalkyl, NR 3 R 3a , NR 3 C(0)OR 3 , NR 3 C(0)R 3 , OR 3 , COR 3 , CO2R 3 , CONR 3 R 3 a f NHC(0)NR 3 R3a / NHC (S) NR 3 R 3a , S02NR 3 R3a / sθ2R 3b , C3-10 carbocycle substituted with 0-5 R a , and 5-10 membered heterocycle containing from 1-4 heteroatoms selected 3 from O, N, and S, substituted with 0-3 R ; R 5 is independently selected from the group: H and C1-4 alkyl ; R 5a is independently selected from the group: H, C1-4 alkyl , phenyl and benzyl ; R 5 is independently selected from the group: H and C1-. 4 alkyl ; and m is selected from 0, 1, 2, and 3 5. A compound according to claim 1, wherein the compound is selected from: (a) 3- (4-methoxyphenyl) -5- (acetamido) indeno [1 , 2-c] pyrazol- 4 -one; (b) 3- (phenyl) -5- (acetamido) indeno [1, 2-c] pyrazol -4 -one; (c) 3- (4 -methylthiophenyl) -5- (acetamido) indeno [1,2- c] pyrazol-4-one; 167 (d) 3- (4 -methylsulfonylphenyl) -5- (acetamido) indeno [1, 2- c] pyrazol -4 -one; (e) 3- (4-N,N-dimethylphenyl) -5- (acetamido) indeno [1,2- c] pyrazol -4 -one; (f ) 3- (3 -pyridyl) -5- (acetamido) indeno [1 , 2-c] pyrazol -4 -one; (g) 3- (4 -methoxyphenyl) -5- (formamido) indeno [1 , 2-c] pyrazol - 4 -one; (h) 3- (4 -hydroxypheny1) -5- (acetamido) indeno [1, 2 -c] pyrazol - 4 -one; (i) 3- (4- (1-piperidinyl) phenyl) -5- (acetamido) indeno [1,2- c] pyrazol -4 -one; (j ) 3- (4 -morpholinyl) phenyl) -5- (acetamido) indeno [1,2- c] pyrazol -4 -one; (k) 3- (4-ethoxyphenyl) -5- (acetamido) indeno [1, 2-c] pyrazol -4 - one; (1) 3- (4-butylphenyl) -5- (acetamido) indeno [1, 2-c] pyrazol -4- one ; (m) 3- (4-ethylphenyl) -5- (acetamido) indeno [1, 2-c] pyrazol-4- one; (n) 3- (4-n-propylphenyl) -5- (acetamido) indeno [1, 2-c] pyrazol- 4 -one ; (o) 3- (4 -methoxyphenyl) -5- ( (4- aminophenyl) acetamido) indeno [1, 2-c] pyrazol -4 -one; (p) 3- (4-pyridyl) -5- (formamido) indeno [1, 2-c] pyrazol -4 -one; 168 (q) 3- (4-pyridyl) -5- (acetamido) indeno [1, 2-c] pyrazol-4 -one; (r) 3- (4-methoxyphenyl) -5- ( (4- aminophenyl) acetamido) indeno [1, 2-c] pyrazol-4 -one; (s) 3- (4-methoxyphenyl) -5- ( (4- azidophenyl) acetamido) indeno [1, 2-c] pyrazol -4-one ; (t) 3- (4 -methoxyphenyl) -5- ( (4- methoxycarbonylaminophenyl) acetamido) indeno [1,2- c] pyrazol -4-one ; (u) 3- (4 -methoxyphenyl) -5- ( (4 - aminomethylcarbonylaminophenyl) acetamido) indeno [1 , 2-c] pyrazol-4 -one; (v) 3- (4 -methoxyphenyl) -5- ( (4-dimethylaminomethylcarbonyl aminophenyl) acetamido) indeno [1, 2-c] pyrazol -4 -one; (w) 3- (4 -methoxyphenyl) -5- ( (4- acetamidophenyl) cetamido) indeno [1 , 2-c] pyrazol -4 -one; (x) 3- (4 -methoxyphenyl) -5- (pyrrolidinylacetamido) indeno [1 , 2-c] pyrazol -4 -one; (y) 3- (4 -methoxyphenyl) -5- (morpholinylacetamido) indeno [1, 2- c] pyrazol -4 -one ; (z) 3- (4 -methoxyphenyl) -5- (thiomorpholinylacetamido) indeno [1 , 2-c] pyrazol-4-one; (aa) 3- (4 -methoxyphenyl) -5- (ethylaminoacetamido) indeno [1,2- c] pyrazol -4 -one ; (bb) 3- (4 -methoxyphenyl) -5- (piperidinylacetamido) indeno [1,2- c] pyrazol-4-one; (cc) 3- (4 -methoxyphenyl) -5- (4-aminomethylpiperidinyl 169 acetamido) indeno [1, 2-c] pyrazol-4 -one; (dd) 3- (4 -methoxyphenyl) -5- (piperazinylacetamido) indeno [1,2- c] pyrazol -4-one; (ee) 3- (4 -methoxyphenyl) -5- (4 -methylpiperazinylacetamido) indeno [1, 2-c] pyrazol-4 -one,• (ff) 3- (4 -methoxyphenyl) -5- (4- (2 -hydroxyethyl) piperazinyl acetamido) indeno [1, 2-c] pyrazol-4 -one; (gg) 3- (4 -methoxyphenyl) -5- (N,N- dimethylaminoacetamido) indeno [1 , 2-c] pyrazol -4 -one ; (hh) 3- (4 -methoxyphenyl) -5- ( (2 -hydroxyethyl) aminoacetamido) indeno [1, 2-c] pyrazol-4 -one; (ii) 3 - (4 -methoxyphenyl) -5- (aminoacetamido) indeno [1,2- c] pyrazol-4 -one; (jj) 3- (4 -methoxyphenyl) -5- ( (2- chlorophenyl) acetamido) indeno [1 , 2-c] pyrazol -4 -one ; (kk) 3- (4 -methoxyphenyl) -5- ( (2,4- dichlorophenyl) acetamido) indeno [1 , 2-c] pyrazol -4 -one ; (11) 3- (4 -methoxyphenyl) -5- ( (3,4- dichlorophenyl) acetamido) indeno [1 , 2-c] pyrazol-4 -one; (mm) 3- (4 -methoxyphenyl) -5- ( (2- methoxyphenyl) acetamido) indeno [1 , 2-c] pyrazol-4 -one; (nn) 3- (4-dimethoxyphenyl) -5- ( (3- thiophene) acetamido) indeno [1 , 2-c] pyrazol-4-one; (oo) 3- (4 -methoxyphenyl) -5- ( (3 ,4- ethylenedioxyphenyl) acetamido) indeno [1, 2-c] yrazol -4 -one; 170 (pp) 3- (3 , 4-dimethoxyphenyl) -5- (acetamido) indeno [1, 2- c] pyrazol-4 -one; (qq) 3- (2 -methoxyphenyl) -5- (acetamido) indeno [1, 2-c] pyrazol- 4 -one; (rr) 3- (4-methoxyphenyl) -5- ( (2 , 5- dimethoxyphenyl ) acetamido) indeno [1 , 2 -c] pyrazol -4-one ; (ss) 3- (4 -methoxyphenyl) -5- ( (3 ,4- dimethoxyphenyl ) acetamido) indeno [1 , 2-c] pyrazol -4 -one; (tt) 3- (4 -methoxyphenyl) -5- ( (4 - methoxyphenyl) acetamido) indeno [1 , 2-c] pyrazol -4-one; (uu) 3- (4 -methoxyphenyl) -5- ( (3- methoxyphenyl) acetamido) indeno [1 , 2-c] pyrazol -4 -one; (w) 3- (4 -methoxyphenyl) -5- ( (4- chlorophenyl) acetamido) indeno [1 , 2-c] pyrazol -4 -one ; (ww) 3- (4 -methoxyphenyl) -5- (butylcarbamoyl) aminoindeno [1, 2- c] pyrazol-4 -one; (xx) 3- (4 -methoxyphenyl) -5- (4-aminobenzylcarbamoyl) aminoindeno [1 , 2-c] pyrazol-4 -one; (yy) 3 - (4 -methoxyphenyl) -5- (4 - pyridylcarbamoyl) aminoindeno [1 , 2-c] pyrazol -4 -one ; (zz) 3- (4 -methoxyphenyl) -5- (phenylcarbamoyl) aminoindeno [1 , 2- c] pyrazol-4 -one ; (aaa) 3- (4 -methoxyphenyl) -5- (cyclobutylamido) indeno [1,2- c] pyrazol -4 -one; 171 (bbb) 3- (4 -methoxyphenyl) -5- (cyclopentylamido) indeno [1, 2-c] pyrazol-4 -one; (ccc) 3- (4 -methoxyphenyl) -5- (propylamido) indeno [1,2- c] pyrazol -4 -one; (ddd) 3- (4 -methoxyphenyl) -5- (ethylamido) indeno [1,2- c] pyrazol-4 -one; (eee) 3- (4-methoxyphenyl) -5- (benzylamido) indeno [1 , 2- c] pyrazol -4 -one, • (fff) 3- (4 -methoxyphenyl) -5- (isopropylamido) indeno [1,2- c] pyrazol -4 -one; (ggg) 3 - (4-methoxyphenyl) -5- ( (cyclopropylamido) indeno [1, 2-c] pyrazol -4 -one,• (hhh) 3- (4 -methoxyphenyl) -5- (chloroacetamido) indeno [1,2- c] pyrazol -4-one; (iii) 3- (4 -methoxyphenyl) -5- (4-pyridinylaminomethyl acetamido) indeno [1 , 2-c] pyrazol-4-one; (jjj) 3 - (4-N,N-dimethylaminophenyl) -5- (morpholinylacetamido) indeno [1 , 2-c] pyrazol -4 -one ; (kkk) 3- (4-N,N-dimethylaminophenyl) -5- dimethylaminoacetamido) indeno [1, 2-c] pyrazol-4-one; (111) 3- (4- (trifluoromethyl) phenyl) -5- (acetamido) indeno [1 , 2-c] pyrazol-4 -one; (mmm) 3- (4- (dimethylamino) phenyl) -5- ( (4 -methyl- 1- piperazinyl) acetamido) indeno [1, 2-c] pyrazol -4 -one; 172 (nnn) 3- (4- (dimethylamino) phenyl) -5- ( (4 -aminomethyl- 1- piperidinyl) acetamido) indeno [1, 2-c] pyrazol-4 -one; (ooo) 3- (4- (dimethylamino) phenyl) -5- ( (4 -hydroxy-1- piperidinyl) acetamido) indeno [1, 2-c] pyrazol -4 -one; (ppp) 3- (4- (4 -morpholinyl) phenyl) -5- ( (4- morpholinyl) acetamido) indeno [1, 2-c] pyrazol-4 -one; (qqq) 3- (4- (4-morpholinyl) phenyl) -5- ( (4-methyl-l- piperazinyl) acetamido) indeno [1 , 2-c] pyrazol-4-one ; (rrr) 3- (4- (4 -morpholinyl) phenyl) -5- ( (4 -hydroxy-1- piperidinyl) acetamido) indeno [1, 2-c] pyrazol -4 -one; (sss) 3- (4- (4-morpholinyl) phenyl) -5- ( (4-aminomethyl-l- piperidinyl) acetamido) indeno [1, 2-c] pyrazol-4 -one ; (ttt) 3- (4- (1-piperazinyl) phenyl) -5- ( (4- morpholinyl) acetamido) indeno [1, 2-c] pyrazol-4-one; (uuu) 3- (4- (1-piperazinyl) phenyl) -5- ( (dimethylamino) acetamido) indeno [1, 2-c] pyrazol -4 -one; (vw) 3- (4- (1-piperazinyl) phenyl) -5- ( (4-methyl-l- piperazinyl) acetamido) indeno [1, 2-c] pyrazol-4 -one; (www) 3- (4- (1-piperazinyl) phenyl) -5- ( (4-aminomethyl-l- piperidinyl) acetamido) indeno [1, 2-c] pyrazol-4 -one; (xxx) 3- (4- (1-piperazinyl) phenyl) -5- ( (aminocarbonyl) amino) indeno [1 , 2-c] pyrazol-4-one; (yyy) 3- (4- (l-piperazinyl) phenyl) -5- ( (hydrazinocarbonyl) amino) indeno [1, 2-c] pyrazol-4-one; 173 (zzz) 3- (4- (1-piperazinyl) phenyl) -5- ( ( (4- morpholinylamino) carbonyl) amino) indeno [1 , 2-c] pyrazol-4- one; (A) 3- (4- (4-methyl-1-piperazinyl) phenyl) -5- ( ( (4- morpholinylamino) carbonyl) amino) indeno [1 , 2-c] pyrazol-4- one; (B) 3- (4- (4 -ethyl -1 -piperazinyl) phenyl) -5- ( ( (4- morpholinylamino) carbonyl) amino) indeno [1 , 2-c] pyrazol -4- one ; (C) 3- (4- (4 - isopropyl -1 -piperazinyl) phenyl) -5- ( ( (4- morpholinylamino) carbonyl) amino) indeno [1 , 2-c] pyrazol -4- one; (D) 3- (4- (4- -butoxycarbonyl-l-piperazinyl) phenyl) -5- ( ( (4- morpholinylamino) carbonyl) amino) indeno [1, 2-c] pyrazol -4- one; (E) 3- (4- (dimethylamino) henyl) -5- ((( (4 -methyl- 1- piperazinyl) amino) carbonyl) amino) indeno [1, 2-c] pyrazol - 4 -one; (F) 3- (i-propyl) -5- (acetamido) indeno [1, 2-c] pyrazol -4 -one; (G) 3- (c-propyl) -5- (acetamido) indeno [1, 2-c] pyrazol -4 -one; (H) 3- (t-butyl) -5- (acetamido) indeno [1, 2-c] pyrazol -4 -one; (I) 3- (2 -thienyl) -5- (acetamido) indeno [1, 2-c] pyrazol -4 -one; (J) 3- (3 -methyl-2 -thienyl) -5- (acetamido) indeno [1,2- c] pyrazol -4 -one; (K) 3- (ethyl) -5- (carbamoyl) aminoindeno [1, 2-c] yrazol -4 -one; 174 (L) 3- (n-propyl) -5- (carbamoyl) aminoindeno [1 , 2-c] pyrazol-4- one; (M) 3- (i-propyl) -5- (carbamoyl) aminoindeno [1, 2-c] pyrazol -4- one; (N) 3- (c-propyl) -5- (carbamoyl) aminoindeno [1 , 2-c] pyrazol-4- one; (O) 3- (c-hexyl) -5- (carbamoyl) aminoindeno [1 , 2-c] pyrazol-4- one; (P) 3- (2 -thienyl) -5- (carbamoyl) aminoindeno [1, 2-c] pyrazol-4- one; (Q) 3- (3 -methyl -2 -thienyl) -5- (carbamoyl) aminoindeno [1, 2- c] pyrazol -4-one; (R) 3- (5 -methyl-2 -thienyl) -5- (carbamoyl) aminoindeno [1,2- c] pyrazol-4 -one; (S) 3- (5-ethylcarboxyl-2-thienyl) -5- (carbamoyl ) aminoindeno [1 , 2 -c] pyrazol-4 -one ; (T) 3- (3-thienyl) -5- (carbamoyl) aminoindeno [1, 2-c] pyrazol-4- one ; (U) 3- (1-methyl-3 -pyrrolyl) -5- (carbamoyl) aminoindeno [1,2- c] pyrazol-4-one ; (V) 3- (2,5-dimethyl-3-thienyl) -5- (carbamoyl) aminoindeno [1, 2-c] pyrazol-4 -one; (W) 3- (2-furanyl) -5- (carbamoyl) aminoindeno [1, 2-c] pyrazol-4- one; (X) 3- (i-propyl) -5- (N,N- dimethylaminocarbamoyl) aminoindeno [1, 2-c] pyrazol-4 -one; 175 (Y) 3- (c-propyl) -5- (N,N- dimethylaminocarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one; (Z) 3- (c-hexyl) -5- (N,N- dimethylaminocarbamoyl) aminoindeno [1 , 2-c] pyrazol -4 -one; (AA) 3- (2-thienyl) -5- (N,N- dimethylaminocarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one; (BB) 3- (5-methoxy-2 -thienyl) -5- (N,N- dimethylaminocarbamoyl) aminoindeno [1, 2-c] pyrazol-4 -one; (CC) 3- (5-methyl -2 -thienyl) -5- (N,N- dimethylaminocarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one; (DD) 3- (5-ethylcarboxyl-2-thienyl) -5- (N,N- dimethylaminocarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one; (EE) 3- (3-thienyl) -5- (N,N- dimethylaminocarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one; (FF) 3- (5-chloro-3-thienyl) -5- (N,N- dimethylaminocarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one; (GG) 3- (2,5-dimethyl-3-thienyl) -5- (N,N- dimethylaminocarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one; (HH) 3- (2-furanyl) -5- (N,N- dimethylaminocarbamoyl) aminoindeno [1, 2-c] pyrazol-4 -one; (II) 3- (i-propyl) -5- (4-carbamoylpiperidinylacetamido) indeno [1, 2 -c] pyrazol -4 -one; (JJ) 3- (c-hexyl) -5- (4-carbamoylpiperidinylacetamido) indeno [1, 2-c] yrazol -4 -one; 176 (KK) 3- (ethyl) -5- (4-aminomethylpiperidinylacetamido) indeno [1, 2-c] pyrazol-4-one; (LL) 3- (i-propyl) -5- (4-aminomethylpiperidinylacetamido) indeno [1, 2-c] pyrazol-4-one ; (MM) 3- (c-propyl) -5- (4-aminomethylpiperidinylacetamido) indeno [1, 2-c] pyrazol-4 -one; (NN) 3- (c-hexyl) -5- (4-aminomethylpiperidinylacetamido) indeno [1, 2-c] pyrazol -4 -one; (00) 3- (i-propyl) -5- (4 -methylpiperazinylcarbamoyl) amino indeno [1 , 2-c] pyrazol-4 -one; (PP) 3- (5-ethylcarboxyl-2-thienyl) -5- (4- methylpiperazinylcarbamoyl) aminoindeno [1, 2-c] pyrazol -4- one; (QQ) 3- (5-carboxyl-2 -thienyl) -5- (4- methylpiperazinylcarbamoyl) aminoindeno [1 , 2-c] pyrazol-4- one; (RR) 3- (2,5-dimethyl-3-thienyl) -5- (4- methylpiperazinylcarbamoyl) aminoindeno [1 , 2-c] pyrazol -4- one ; (SS) 3- (i-propyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2- c] pyrazol -4-one; (TT) 3- (N-methylcarbamoyl-4-piperidinyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4 -one; (UU) 3- (5 -methyl -2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol-4-one; (W) 3- (5-chloro-3-thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol -4-one; 177 (WW) 3- (2, 5-dimethyl-3 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1 , 2-c] pyrazol-4 -one; (XX) 3- (5-ethylcarboxyl-2-thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1 , 2-c] pyrazol -4 -one; (YY) 3- (5-carboxyl -2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1 , 2-c] pyrazol-4 -one; (ZZ) 3- (5-benzylcarboxamido-2-thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1 , 2-c] pyrazol -4 -one; (AAA) 3- (5- (4-methylpiperazinyl) carboxamido-2-thienyl) - 5- (morpholinylcarbamoyl) aminoindeno [1 , 2-c] pyrazol-4- one ; (BBB) 3- (5- (2- (1-methylpyrrolidinyl) ethyl) carboxamido-2- thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1 , 2- c] pyrazol-4 -one; (CCC) 3- (5- (N,N-dimethylamino) carboxamido-2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1 , 2-c] pyrazol-4 -one; (DDD) 3- (5- (2- (N,N-dimethylamino) ethyl) carboxamido-2- thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1 , 2- c] pyrazol-4-one ; (EEE) 3- (5- (2- (pyrrolidinyl) ethyl) carboxamido-2- thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1,2- c] pyrazol-4-one; (FFF) 3- (5- (2- (morpholinyl) ethyl) carboxamido-2 -thienyl) - 5- (morpholinylcarbamoyl) aminoindeno [1 , 2-c] pyrazol-4- one; (GGG) 3- (5-morpholinylcarboxamido-2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol -4-one; 178 (HHH) 3- (5- (3- (pyrrolidonyl) propyl) carboxamido-2- thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1,2- c] pyrazol-4 -one ; (III) 3- (5- (2- (3 -pyridyl) ethyl) carboxamido-2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol -4 -one; (JJJ) 3- (5- (3- (imidazolyl) propyl) carboxamido-2 -thienyl) - 5- (morpholinylcarbamoyl) aminoindeno [1 , 2-c] pyrazol-4- one ; (KKK) 3- (5- (2- (2-pyridyl) ethyl) carboxamido-2-thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1, 2-c] pyrazol -4 -one; (LLL) 3- (5- ( (2 -pyridyl) methyl) carboxamido-2 -thienyl) -5- (morpholinylcarbamoyl) aminoindeno [1 , 2-c] pyrazol -4 -one; and (MMM) 3- (5- (2- (piperidinyl) ethyl) carboxamido-2 -thienyl) • 5- (morpholinylcarbamoyl) aminoindeno [1 , 2-c] pyrazol -4- one; or pharmaceutically acceptable salt thereof. 6. A pharmaceutical composition, comprising: a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of claim 1. 7. A method of treating cancer and proliferative diseases comprising: administering to a host in need of such treatment a therapeutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt or prodrug form thereof. 179

Inventors: CARINI DAVID J, DIMEO SUSAN V, NUGIEL DAVID A, YUE EDDY W, CARINI, DAVID, J., DIMEO, SUSAN, V., NUGIEL, DAVID, A., YUE, EDDY, W.
Applicants: DU PONT PHARM CO, DU PONT PHARMACEUTICALS COMPANY
Application year: 1999
Main classification: C07D231
IPC codes: A61K31, A61P35, A61P43, C07D231, C07D401, C07D403, C07D405, C07D409, C07D413, C07D417