Patent ID: 6221889
Filing Date: 2001-04-24
Classification: A61P,C07D

Abstract:
A compound of the formula: ##STR20##whereinR is --NH--C(X)--NH--(CR.sub.13 R.sub.14).sub.v --Z;Z is W, HET, ##STR21##optionally substituted C.sub.1-10 alkyl, optionally substituted C.sub.2-10 alkenyl, or optionally substituted C.sub.2-10 alkynyl;X is O, or 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, (CR.sub.8 R.sub.8)qC(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)q NR.sub.4 C(NR.sub.5)R.sub.11, (CR.sub.8 R.sub.8)q NHS(O).sub.2 R.sub.17, and (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 rings may be optionally substituted;n is an integer having a value of 1 to 3;m is an integer having a value of 1 to 5;p 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;HET is an optionally substituted heteroaryl ring;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, 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 and 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, hydroxy C.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)q NR.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.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)q NR.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)q NR.sub.4 C(NR.sub.5)R.sub.11, (CR.sub.8 R.sub.8)qNHS(O).sub.2 R.sub.a, and (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 rings may 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 and 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 heteroaryl C.sub.1-4 alkyl, optionally substituted heterocyclic, or optionally substituted heterocyclic C.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 an 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, heteroaryl C.sub.1-4 alkyl, heterocyclic, or heterocyclic C.sub.1-4 alkyl, wherein the aryl, heteroaryl and heterocyclic containing rings may all be optionally substituted;R.sub.a is NR.sub.6 R.sub.7, C.sub.1-4 alkyl, aryl C.sub.1-4 alkyl, aryl C.sub.2-4 alkenyl, heteroaryl, heteroaryl-C.sub.1-4 alkyl, heteroarylC.sub.2-4 alkenyl, heterocyclic, or heterocyclic C.sub.1-4 alkyl, wherein the aryl, heteroaryl and heterocyclic containing rings may all be optionally substituted;W is ##STR22##the E containing ring is optionally selected from ##STR23##the asterix * denoting point of attachment of the ring;or a pharmaceutically acceptable salt thereof.