Patent ID: 6737420
Filing Date: 2004-05-18
Classification: A61K,A61P,C07B,C07C,C07D,C07K

Abstract:
A compound of the formula: or a pharmaceutically acceptable salt thereof whereinR1 is: (I) C1-C6 alkyl, unsubstituted or substituted with one, two or three C1-C3 alkyl, â€”F, â€”Cl, â€”Br, â€”I, â€”OH, â€”NH2, â€”Câ‰¡N, â€”CF3, or â€”N3, (II) â€”(CH2)1-2â€”Sâ€”CH3, (III) â€”CH2â€”CH2â€”Sâ€”CH3, (IV) â€”CH2â€”(C2-C6 alkenyl) unsubstituted or substituted by one â€”F, (V) â€”(CH2)0-3â€”(R1-aryl) where R1-aryl is phenyl, 1-naphthyl, 2-naphthyl, indanyl, indenyl, dihydronaphthyl, tetralinyl unsubstituted or independently substituted on the aryl ring with one or two of C1-C3 alkyl, â€”CF3, â€”F, Cl, â€”Br, â€”I, C1-C3 alkoxy, â€”Oâ€”CF3, â€”NH2, â€”OH, or â€”Câ‰¡N; R2 is: (I) â€”H, (II) C1-C6 alkyl, or (III) â€”(CH2)0-4â€”R2-1 where R2-1 is (C3-C6)cycloalkyl, R1-aryl where R1-aryl is optionally substituted with R100, where R100 is (1) C1-C6 alkyl, (2) â€”F, â€”Cl, â€”Br, or â€”I, (3) â€”OH, (4) â€”NO2, (5) â€”COâ€”OH, (6) â€”Câ‰¡N, (7) â€”COâ€”NRN-2RN-3 where RN-2 and RN-3 are the same or different and are: (a) â€”H, (b) â€”C1-C6 alkyl unsubstituted or substituted with one â€”OH or â€”NH2, (c) â€”C1-C6 alkyl unsubstituted or substituted with one to three â€”F, â€”Cl, â€”Br, or â€”I, (d) â€”C3-C7 cycloalkyl, (e) â€”(C1-C2 alkyl)â€”(C3-C7 cycloalkyl), (f) â€”(C1-C6 alkyl)â€”Oâ€”(C1-C3 alkyl), (g) â€”C1-C6 alkenyl with one or two double bonds, (h) â€”C1-C6 alkynyl with one or two triple bonds, (i) â€”C1-C6 alkyl chain with one double bond and one triple bond, (8) â€”COâ€”(C3-C12 alkyl), (9) â€”COâ€”(C3-C6 cycloalkyl), (11) â€”COâ€”R1-heterocycle where R1-heterocycle is morpholinyl, thiomorpholinyl, thiomorpholinyl S-oxide, thiomorpholinyl S, S-dioxide, piperazinyl, homopiperazinyl, pyrrolidinyl, pyrrolinyl. tetrahydropyranyl, piperidinyl, tetrahydrofuranyl, or tetrahydrothiophenyl, where the R1-heterocycle group is bonded by any atom of the parent R1-heterocycle group substituted by hydrogen such that the new bond to the R1-heterocycle group replaces the hydrogen atom and its bond, where heterocycle is unsubstituted or substituted with one or two &boxH;O, Cl-C3 alkyl, â€”CF3, â€”F, Cl, â€”Br, â€”I, C1-C3 alkoxy, â€”OCF3, â€”NH2, â€”OH, or â€”Câ‰¡N, (12) â€”COâ€”RNN-4 where RN-4 is morpholinyl, thiomorpholinyl, piperazinyl, piperidinyl or pyrrolidinyl where each group is unsubstituted or substituted with one or two C1-C3 alkyl, (13) â€”COâ€”Oâ€”RN-4 where RN-5 is: (a) C1-C6 alkyl, or (b) â€”(CH2)0-2â€”(R1-aryl) where Raryl is as defined above, (14) â€”SO2â€”NRN-2RN-3 where RN-2 and RN-3 are as defined above, (15) â€”SOâ€”(C1-C8 alkyl), (16) â€”SO2â€”(C3-C12 alkyl), (17) â€”NHâ€”COâ€”Oâ€”RN-5 where RN-5 is as defined above, (18) â€”NHâ€”COâ€”N(C1-C3 alkyl)2, (19) â€”Nâ€”CSâ€”N(C1-C3 alkyl)2, (20) â€”N(C1-C3 alkyl)â€”COâ€”RN-5 where RN-5 is as defined above, (21) â€”NRN-2RN-3 where RN-2 and RN-3 can be the same or different and are as defined above, (22) â€”RN-4 where RN-4 is as defined above, (23) â€”Oâ€”COâ€”(C1-C6 alkyl), (24) â€”Oâ€”COâ€”N(C1-C3 alkyl)2, (25) â€”Oâ€”CSâ€”N(C1-C3 alkyl)2, (26) â€”Oâ€”(C1-C6 alkyl), (27) â€”Oâ€”(C2-C5 alkyl)â€”COOH, (28) â€”Sâ€”(C1-C6 alkyl), (29) C1-C6 alkyl unsubstituted or substituted with 1, 2, 3, 4, or 5 â€”F, or (30) â€”Oâ€”(C1-C6 alkyl unsubstituted or substituted with 1, 2, 3, 4, or 5 â€”F, or (31) â€”O-&phgr;; RN-1 is phenyl that is independently substituted with one, two, three or four of R100; Ra is hydrogen or C1-C6 alkyl; Rc is: â€”(C1-C10)alkyl-K1-3 in which: (A) the alkyl chain is unsubstituted or substituted with one â€”OH, (B) the alkyl chain is unsubstituted or substituted with one C1-C6 alkoxy unsubstituted or substituted with 1-5 â€”F, (D) the alkyl chain is unsubstituted or substituted with 1-5 â€”F, (F) each K is: (1) H, (2) C1-C3 alkyl, (3) C1-C3 alkoxy, (4) C1-C3 alkylthioxy, (5) C1-C6 alkylacylamino, (6) C1-C6 alkylacyloxy, (7) amino (8) C1-C6 alkylamino (9) phenylamino, (10) carbamyl (11) carboxyl (12) carboxy(C2-C5)alkoxy, (13) carboxy(C2-C5)alkylthioxy, (16) amino unsubstituted or substituted with C1-C6 alkyl, (17) hydroxyl, or (18) carboxyl methyl ester.