Patent ID: 6177473
Filing Date: 2001-01-23
Classification: A61P,C07D

Abstract:
A compound of the following formula: ##STR6##wherein:Z.sup.1 and Z.sup.2 are independently --O--, --N(R.sup.9)--, --S--, --S(O)--, --S(O).sub.2 --, or --OCH.sub.2 --;R.sup.1 and R.sup.4 are each independently hydrogen, halo, alkyl, nitro, --OR.sup.9, --C(O)OR.sup.9, --C(O)N(R.sup.9)R.sup.10, --N(R.sup.9)R.sup.10, --N(R.sup.9)C(O)R.sup.9, or --N(H)S(O).sub.2 R.sup.12 ;R.sup.2 is --C(NH)NH.sub.2, --C(NH)N(H)OR.sup.9, --C(NH)N(H)C(O)OR.sup.2, --C(NH)N(H)C(O)R.sup.9, --C(NH)N(H)S(O).sub.2 R.sup.12, or --C(NH)N(H)C(O)N(H)R.sup.9 ;R.sup.3 is hydrogen, halo, alkyl, haloalkyl, nitro, ureido, guanidino, --OR.sup.9, --C(NH)NH.sub.2, --C(NH)N(H)OR.sup.9, --C(O)N(R.sup.9)R.sup.10, --R.sup.10, --C(O)N(R.sup.9)R.sup.10, --CH(OH)C(O)N(R.sup.9)R.sup.10, --N(R.sup.9)R.sup.10, --R.sup.11 --N(R.sup.9)R.sup.10, --C(O)OR.sup.9, --R.sup.11 --C(O)OR.sup.9, --N(R.sup.9)C(O)R.sup.9, (1,2)-tetrahydropyrimidinyl (optionally substituted by alkyl), (1,2)-imidazolyl (optionally substituted by alkyl), or (1,2)-imidazolinyl (optionally substituted by alkyl);R.sup.5 and R.sup.6 are independently hydrogen, halo, alkyl, haloalkyl, nitro, --N(R.sup.9)R.sup.10, --C(O)OR.sup.9, --C(O)N(R.sup.9)R.sup.10, --C(O)N(R.sup.9)CH.sub.2 C(O)N(R.sup.9)R.sup.10, --N(R.sup.9)C(O)N(R.sup.9)R.sup.10, --N(R.sup.9)C(O)R.sup.10, or --N(R.sup.9)S(O).sub.2 R.sup.12 ;R.sup.7 is --N(R.sup.9)--(C(R.sup.9)(R.sup.10)).sub.n --R.sup.13 (where n is 0 to 4), --O--(C(R.sup.9)(R.sup.10)).sub.n --R.sup.13 (where n is 0 to 4), or --N(R.sup.14)R.sup.15 ;R.sub.8 is hydrogen, alkyl or halo;each R.sup.9 and R.sup.10 is independently hydrogen, alkyl, aryl (optionally substituted by halo, alkyl, hydroxy, alkoxy, aralkoxy, amino, dialkylamino, monoalkylamino, nitro, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl, or dialkylaminocarbonyl), or aralkyl (optionally substituted by halo, alkyl, aryl, hydroxy, alkoxy, aralkyl, amino, dialkylamino, monoalkylamino, nitro, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl, or dialkylaminocarbonyl);R.sup.11 is a straight or branched alkylene chain;R.sup.12 is alkyl, aryl (optionally substituted by halo, alkyl, hydroxy, alkoxy, aralkoxy, amino, dialkylamino, monoalkylamino, nitro, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl, or dialkylaminocarbonyl), or aralkyl (optionally substituted by halo, alkyl, aryl, hydroxy, alkoxy, aralkyl, amino, dialkylamino, monoalkylamino, nitro, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl, or dialkylaminocarbonyl);R.sup.13 is a mono-, bi- or tricyclic carbocyclic ring system containing from 3 to 15 carbon atoms which may be partially or fully saturated or aromatic, wherein the carbon atoms may be optionally oxidized and wherein the carbocyclic ring system is substituted by --(C(R.sup.9)(R.sup.10)).sub.m --R.sup.16 (where m is 0 to 4), and is optionally substituted by alkyl, aryl, aralkyl, alkoxy, aryloxy, aralkoxy, halo, haloalkyl, haloalkoxy, hydroxy, --N(R.sup.9)R.sup.10, --C(O)OR.sup.9, or --C(O)N(R.sup.9)R.sup.10 ;or R.sup.13 is a mono-, bi- or tri-cyclic heterocyclic ring system containing from 3 to 15 ring members including carbon and 1 to 4 hetero atoms selected from nitrogen, oxygen and sulfur atoms, wherein the carbon, nitrogen and sulfur atoms may be optionally oxidized and wherein the heterocyclic ring system may be partially or fully saturated or aromatic and is substituted by --C(R.sup.9)(R.sup.10)).sub.m --R.sup.16 (where m is 0 to 4), and is optionally substituted by alkyl, aryl, aralkyl, alkoxy, aryloxy, aralkoxy, halo, haloalkyl, haloalkoxy, hydroxy, --N(R.sup.9)R.sup.10, --C(O)OR.sup.9, or --C(O)N(R.sup.9)R.sup.10 ;R.sup.14 and R.sup.15, together with the nitrogen atom, form a mono-, bi- or tricyclic heterocyclic ring system containing from 3 to 15 ring members including carbon and 1 to 3 additional hetero atoms selected from nitrogen, oxygen and sulfur atoms, wherein the carbon, nitrogen, or sulfur atoms may be optionally oxidized and wherein the heterocyclic ring system may be partially or fully saturated or aromatic and is substituted by --(C(R.sup.9)(R.sup.10)).sub.n --R.sup.16 (where m is 0 to 4), and is optionally substituted by alkyl, aryl, aralkyl, alkoxy, aryloxy, aralkoxy, halo, haloalkyl, haloalkoxy, hydroxy, --N(R.sup.9)R.sup.10, --C(O)OR.sup.9, or --C(O)N(R.sup.9)R.sup.10 ; andR.sup.16 is --C(O)OR.sup.9 or --C(O)N(R.sup.9)R.sup.10 ;provided that when R.sup.7 is --N(R.sup.9)--(C(R.sup.9)(R.sup.10),--R.sup.13 (where n is 0), R.sup.13 can not be phenyl, naphthyl or piperidinyl substituted by --C(O)OR.sup.9 ; when R.sup.7 is --O--(C(R.sup.9)(R.sup.10)).sub.n --R.sup.13 (where n is 0), R.sup.13 can not be phenyl, naphthyl, piperidinyl or pyrrolidinyl substituted by --C(O)OR.sup.9 ; and when R.sup.7 is --N(R.sup.4)R.sup.15, R.sup.14 and R.sup.15, together with the nitrogen atom, can not be piperazinyl or piperidinyl substituted by --C(O)OR.sup.9 ;as a single stereoisomer or a mixture thereof; or a pharmaceutically acceptable salt thereof.