Patent ID: 6211224
Filing Date: 2001-04-03
Classification: C07D

Abstract:
A compound of the formula ##STR28##whereinR.sub.0 is hydrogen, C.sub.1 -C.sub.6 alkyl, substituted C.sub.1 -C.sub.6 alkyl, wherein the substituents are as defined below; aryl, substituted aryl, aralkyl or substituted aralkyl, wherein the substituents are as defined for R.sub.3, R.sub.4 and R.sub.5;R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, substituted C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, substituted C.sub.3 -C.sub.7 cycloalkyl, a beterocyclic ring or bicyclic heterocyclic ring with from 1 to 4 heteroatoms selected from N, O or S which can be optionally substituted by R.sub.3, R.sub.4 and R.sub.5, C.sub.1 -C.sub.6 -alkyl substituted by a heterocyclic ring or bicyclic heterocyclic ring with from 1 to 4 heteroatoms selected from N, O or S which can be optionally substituted by R.sub.3, R.sub.4 and R.sub.5, C.sub.3 -C.sub.6 alkenyl, substituted C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, substituted C.sub.3 -C.sub.6 alkynyl, C.sub.0 -C.sub.5 -alkyl-S(O).sub.n --C.sub.0 -C.sub.5 alkyl, C.sub.2 -C.sub.6 alkyl(NR.sub.11 R.sub.12), C.sub.2 -C.sub.6 alkyl(OR.sub.11), or C.sub.1 -C.sub.6 alkyl (CONR.sub.11 R.sub.12); with the proviso that R.sub.11 and R.sub.12 independently or taken together are not aryl, substituted aryl, aralkyl, or substituted aralkyl; orR.sub.1 and R.sub.2 taken together form a non-heteroaromatic ring of 3-8 atoms containing 0,1 or 2 additional heteroatoms selected from S, O or N;R.sub.3, R.sub.4 and R.sub.5 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, substituted C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl, substituted C.sub.2 -C.sub.6 alkenyl, CN, nitro, C.sub.1 -C.sub.3 perfluoroalkyl, C.sub.1 -C.sub.3 perfluoroalkoxy, R.sub.11 O (CH.sub.2).sub.p -, R.sub.11 C(O)O(CH.sub.2).sub.p -, R.sub.11 OC(O)(CH.sub.2).sub.p -, --(CH.sub.2).sub.p S(O).sub.n R.sub.17, --(CH.sub.2).sub.p C(O)NR.sub.11 R.sub.12 or halogen; wherein R.sub.17 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.3 perfluoroalkyl;R.sub.3 and R.sub.4 taken together form a carbocyclic ring of 3-7 carbon atoms or a heterocyclic ring containing 1-3 beteroatoms selected from N, O and S;R.sub.6 is hydrogen, C.sub.1 -C.sub.6 alkyl, substituted C.sub.1 -C.sub.6 alkyl, aryl, substituted aryl, C.sub.1 -C.sub.3 perfluoroalkyl, CN, NO.sub.2, halogen, R.sub.11 O(CH.sub.2).sub.p -, NR.sub.12 C(O)R.sub.11, NR.sub.12 C(O)NR.sub.11 R.sub.12 or SO.sub.n R.sub.11 ;R.sub.7 is hydrogen, C.sub.1 -C.sub.6 alkyl, or substituted C.sub.1 -C.sub.6 alkyl, unless X is hydrogen or halogen, then R.sub.7 is absent;R.sub.8 is hydrogen, C(O)OR.sub.9, C(O)NR.sub.20 R.sub.21, N R.sub.20 R.sub.21, C(O)R.sub.11, NR.sub.20 C(O)R.sub.11, NR.sub.20 C(O)N R.sub.20 R.sub.21, NR.sub.20 S(O).sub.2 R.sub.11, NR.sub.20 S(O).sub.2 NR.sub.20 R.sub.21, OC(O)R.sub.11, OC(O)NR.sub.20 R.sub.21, OR.sub.11, SO.sub.n R.sub.11, S(O).sub.n NR.sub.20 R.sub.21, C.sub.1 -C.sub.6 alkyl or substituted C.sub.1 -C.sub.6 alkyl, unless X is hydrogen or halogen, then R.sub.8 is absent; orR.sub.7 and R.sub.8 taken together form a carbocyclic ring of 3-7 atoms;R.sub.9 and R.sub.9a are independently hydrogen, C.sub.1 -C.sub.6 alkyl, substituted C.sub.1 -C.sub.6 alkyl; aryl or substituted aryl, aralkyl or substituted aralkyl when m.noteq.0; orR.sub.9 and R.sub.9a taken together form a carbocyclic ring of 3-7 atoms or ##STR29##when m,.noteq.0;R.sub.10 and R.sub.10a are independently hydrogen, C.sub.1 -C.sub.6 alkyl, substituted C.sub.1 -C.sub.6 alkyl, aryl, substituted aryl, aralkyl or substituted aralkyl; orR.sub.10 and R.sub.10a taken together form a carbocyclic ring of 3-7 atoms or ##STR30##R.sub.9 and R.sub.10 taken together form a carbocyclic ring of 3-7 carbon atoms or a heterocyclic ring containing one or more heteroatoms when m.noteq.0; orR.sub.9 and R.sub.2 taken together form a heterocyclic ring containing 3-7 carbon atoms and one or more heteroatoms when m.noteq.0; orR.sub.10 and R.sub.2 taken together form a heterocyclic ring containing 3-7 carbon atoms and one or more heteroatoms;R.sub.11 and R.sub.12 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, substituted C.sub.1 -C.sub.6 alkyl, aryl, substituted aryl, aralkyl, substituted aralkyl, a carbocyclic ring of 3-7 atoms or a substituted carbocyclic ring containing 3-7 atoms;R.sub.11 and R.sub.12 taken together can form an optionally substituted ring of 3-7 atoms;R.sub.20 and R.sub.21 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, substituted C.sub.1 -C.sub.6 alkyl, aryl, substituted aryl, aralkyl, substituted aralkyl, a carbocyclic ring of 3-7 atoms or a substituted carbocyclic ring containing 3-7 atoms;X is hydrogen, halogen, N, O, S(O).sub.n, C(O), (CR.sub.11 R.sub.12).sub.p ; C.sub.2 -C.sub.6 alkenyl, substituted C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, or substituted C.sub.2 -C.sub.6 alkynyl; when X is hydrogen or halogen, R.sub.7 and R.sub.8 are absent; when X is O, S(O)n, C(O), or CR.sub.11 R.sub.12 only R.sub.7 or R.sub.8 is possible;Z is O, S, or NR.sub.11 ;m is 0-3;n is 0-2;p is 0-4; and the alkyl, alkenyl and alkynyl substituents are selected from C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, hydroxy, oxo, cyano, C.sub.1 -C.sub.6 alkoxy, fluoro, C(O)OR.sub.11, and the aryl substituents are as defined for R.sub.3, R.sub.4 and R.sub.5 ;or a pharmaceutically acceptable addition salt and/or hydrate thereof, or where applicable, a geometric or optical isomer or racemic mixture thereof.