Patent ID: 6300325
Filing Date: 2001-10-09
Classification: A61P,C07D,C07F

Abstract:
A compound of the formula: ##STR21##whereinR is --NH--C(X.sub.2)--NH--(CR.sub.13 R.sub.14).sub.v --Z;Z is W, HET, ##STR22##an optionally substituted C.sub.1-10 alkyl, an optionally substituted C.sub.2-10 alkenyl, or an optionally substituted C.sub.2-10 alkynyl;X is C(X.sub.1).sub.2, C(O), C(S), S(O).sub.2, PO(OR.sub.4), or C.dbd.N--R.sub.19 ;X.sub.1 is independently hydrogen, halogen, C.sub.1-10 alkyl, NR.sub.4 R.sub.5, C.sub.1-10 alkyl-NR.sub.4 R.sub.5, C(O)NR.sub.4 R.sub.5, optionally substituted C.sub.1-10 alkyl, C.sub.1-10 alkoxy, halosubstituted C.sub.1-10 alkoxy, hydroxy, aryl, aryl C.sub.1-4 alkyl, aryloxy, aryl C.sub.1-4 alkyloxy, heteroaryl, heteroarylalkyl, heterocyclic, heterocyclic C.sub.1-4 alkyl, or heteroaryl C.sub.1-4 alkyloxy;X.sub.2 is .dbd.O, or .dbd.S;R.sub.1 is independently selected from hydrogen; halogen; nitro; cyano; halosubstituted C.sub.1-10 alkyl; C.sub.1-10 alkyl; C.sub.2-10 alkenyl; C.sub.1-10 alkoxy; halosubstituted C.sub.1-10 alkoxy; azide; (CR.sub.8 R.sub.8)qS(O).sub.t R.sub.4, hydroxy; hydroxy C.sub.1-4 alkyl; aryl; aryl C.sub.1-4 alkyl; aryloxy; aryl C.sub.1-4 alkyloxy; heteroaryl; heteroarylalkyl; heterocyclic; heterocyclic C.sub.1-4 alkyl; heteroaryl C.sub.1-4 alkyloxy; aryl C.sub.2-10 alkenyl; heteroaryl C.sub.2-10 alkenyl; heterocyclic C.sub.2-10 alkenyl; (CR.sub.8 R.sub.8)qNR.sub.4 R.sub.5 ; C.sub.2-10 alkenyl C(O)NR.sub.4 R.sub.5 ; (CR.sub.8 R.sub.8)qC(O)NR.sub.4 R.sub.5 ; (CR.sub.8 R.sub.8)qC(O)NR.sub.4 R.sub.10 ; S(O).sub.3 R.sub.8 ; (CR.sub.8 R.sub.8)qC(O)R.sub.11 ; C.sub.2-10 alkenyl C(O)R.sub.11 ; C.sub.2-10 alkenyl C(O)OR.sub.11 ; C(O)R.sub.11 ; (CR.sub.8 R.sub.8)qC(O)OR.sub.12 ; (CR.sub.8 R.sub.8)qOC(O)R.sub.11 ; (CR.sub.8 R.sub.8)qC(NR.sub.4)NR.sub.4 R.sub.5 ; (CR.sub.8 R.sub.8)qNR.sub.4 C(NR.sub.5)R.sub.11 ; (CR.sub.8 R.sub.8)q NR.sub.4 C(O)R.sub.11 ; (CR.sub.8 R.sub.8)qNHS(O).sub.2 R.sub.17 ; (CR.sub.8 R.sub.8)qS(O).sub.2 NR.sub.4 R.sub.5 ; or two R.sub.1 moieties together may form O--(CH.sub.2).sub.s O or a 5 to 6 membered saturated or unsaturated ring; and wherein the aryl, heteroaryl, and heterocyclic containing moieties may all be optionally substituted;n is an integer having a value of 1 to 3;m is an integer having a value of 1 to 3;q is 0, or an integer having a value of 1 to 10;s is an integer having a value of 1 to 3;t is 0, or an integer having a value of 1 or 2;v is 0, or an integer having a value of 1 to 4;p is an integer having a value of 1 to 3;HET is an optionally substituted heteroaryl;R.sub.4 and R.sub.5 are independently hydrogen, optionally substituted C.sub.1-4 alkyl, optionally substituted aryl, optionally substituted aryl C.sub.1-4 alkyl, optionally substituted heteroaryl, optionally substituted heteroaryl C.sub.1-4 alkyl, heterocyclic, or heterocyclic C.sub.1-4 alkyl, or R.sub.4 and R.sub.5 together with the nitrogen to which they are attached form a 5 to 7 member ring which may optionally comprise an additional heteroatom selected from O/N/S;Y is independently selected from hydrogen; halogen; nitro; cyano; halosubstituted C.sub.1-10 alkyl; C.sub.1-10 alkyl; C.sub.2-10 alkenyl; C.sub.1-10 alkoxy; halosubstituted C.sub.1-10 alkoxy; azide; (CR.sub.8 R.sub.8)qS(O).sub.t R.sub.4 ; hydroxy; hydroxyC.sub.1-4 alkyl; aryl; aryl C.sub.1-4 alkyl; aryloxy; arylC.sub.1-4 alkyloxy; heteroaryl; heteroarylalkyl; heteroaryl C.sub.1-4 alkyloxy; heterocyclic, heterocyclic C.sub.1-4 alkyl; aryl C.sub.2-10 alkenyl; heteroaryl C.sub.2-10 alkenyl; heterocyclic C.sub.2-10 alkenyl; (CR.sub.8 R.sub.8)qNR.sub.4 R.sub.5 ; C.sub.2-10 alkenyl C(O)NR.sub.4 R.sub.5 ; (CR.sub.8 R.sub.8)qC(O)NR.sub.4 R.sub.5 ; (CR.sub.8 R.sub.8)qC(O)NR.sub.4 R.sub.10 ; S(O).sub.3 R.sub.8 ; (CR.sub.8 R.sub.8)qC(O)R.sub.11 ; C.sub.2-10 alkenyl C(O)R.sub.11 ; C.sub.2-10 alkenyl C(O)OR.sub.11 ; (CR.sub.8 R.sub.8)qC(O)OR.sub.12 ; (CR.sub.8 R.sub.8)qOC(O)R.sub.11 ; (CR.sub.8 R.sub.8)qNR.sub.4 C(O)R.sub.11 ; (CR.sub.8 R.sub.8)qC(NR.sub.4)NR.sub.4 R.sub.5 ; (CR.sub.8 R.sub.8)qNR.sub.4 C(NR.sub.5)R.sub.11 ; (CR.sub.8 R.sub.8)qNHS(O).sub.2 R.sub.a ; (CR.sub.8 R.sub.8)qS(O).sub.2 NR.sub.4 R.sub.5 ; or two Y moieties together may form O--(CH.sub.2).sub.s O or a 5 to 6 membered saturated or unsaturated ring; and wherein the aryl, heteroaryl, and heterocyclic containing moieties may all be optionally substituted;R.sub.6 and R.sub.7 are independently hydrogen or a C.sub.1-4 alkyl group, or R.sub.6 and R.sub.7 together with the nitrogen to which they are attached form a 5 to 7 member ring which ring may optionally contain an additional heteroatom which heteroatom is selected from oxygen, nitrogen or sulfur;R.sub.8 is independently hydrogen or C.sub.1-4 alkyl;R.sub.10 is C.sub.1-10 alkyl C(O).sub.2 R.sub.8 ;R.sub.11 is hydrogen, C.sub.1-4 alkyl, optionally substituted aryl, optionally substituted aryl C.sub.1-4 alkyl, optionally substituted heteroaryl, optionally substituted heteroarylC.sub.1-4 alkyl, optionally substituted heterocyclic, or optionally substituted heterocyclicC.sub.1-4 alkyl;R.sub.12 is hydrogen, C.sub.1-10 alkyl, optionally substituted aryl or optionally substituted arylalkyl;R.sub.13 and R.sub.14 are independently hydrogen, optionally substituted C.sub.1-4 alkyl, or one of R.sub.13 and R.sub.14 may be optionally substituted aryl;R.sub.15 and R.sub.16 are independently hydrogen, or an optionally substituted C.sub.1-4 alkyl;R.sub.17 is C.sub.1-4 alkyl, aryl, arylalkyl, heteroaryl, heteroarylC.sub.1-4 alkyl, heterocyclic, or heterocyclicC.sub.1-4 alkyl, wherein the aryl, heteroaryl and heterocyclic moieties may all be optionally substituted;R.sub.18 is hydrogen, optionally substituted C.sub.1-10 alkyl, C.sub.1-10 alkoxy, halosubstituted C.sub.1-10 alkoxy, hydroxy, arylC.sub.1-4 alkyl, arylC.sub.2-4 alkenyl, heteroaryl, heteroaryl-C.sub.1-4 alkyl, heteroarylC.sub.2-4 alkenyl, heterocyclic, or heterocyclicC.sub.1-4 alkyl, wherein all the aryl, heteroaryl and heterocyclic containing moieites may all be optionally substituted;R.sub.19 is cyano, nitro, S(O).sub.2 NR.sub.4 R.sub.5, S(O).sub.2 R.sub.17, alkyl, arylC.sub.1-4 alkyl, arylC.sub.2-4 alkenyl, heteroaryl, heteroaryl-C.sub.1-4 alkyl, heteroarylC.sub.2-4 alkenyl, heterocyclic, or heterocyclicC.sub.1-4 alkyl, wherein the alkyl, aryl, heteroaryl and heterocyclic containing moieites may all be optionally substituted;R.sub.a is NR.sub.6 R.sub.7, alkyl, arylC.sub.1-4 alkyl, arylC.sub.2-4 alkenyl, heteroaryl, heteroaryl-C.sub.1-4 alkyl, heteroarylC.sub.2-4 alkenyl, heterocyclic, or heterocyclicC.sub.1-4 alkyl, wherein the aryl, heteroaryl and heterocyclic containing moieites may all be optionally substituted;W is ##STR23##the E containing ring is optionally selected from ##STR24##the asterix*denoting point of attachment of the ring;or a pharmaceutically acceptable salt thereof.