Patent ID: 6166088
Filing Date: 2000-12-26
Classification: A61P,C07D

Abstract:
A compound of Formula (I): ##STR8## wherein: A is --C(R.sup.8).dbd.;Z.sup.1 and Z.sup.2 are independently --O--, --N(R.sup.13)--, --S--, or --OCH.sub.2 --;R.sup.1 and R.sup.4 are each independently hydrogen, halo, alkyl, nitro, --OR.sup.13, --C(O)OR.sup.13, --C(O)N(R.sup.13)R.sup.14, --N(R.sup.13)R.sup.14, --N(R.sup.13)C(O)R.sup.13, or --N(H)S(O).sub.2 R.sup.16 ;R.sup.2 is --C(NH)NH.sub.2, --C(NH)N(H)OR.sup.13, --C(NH)N(H)C(O)OR.sup.16, --C(NH)N(H)C(O)R.sup.13, --C(NH)N(H)S(O).sub.2 R.sup.16, or --C(NH)N(H)C(O)N(H)R.sup.13 ;R.sup.3 is halo, alkyl, haloalkyl, nitro, amino, ureido, guanidino, --OR.sup.13, --C(NH)NH.sub.2, --C(NH)N(H)OR.sup.13, --C(O)N(R.sup.13)R.sup.14, --R.sup.15 --C(O)N(R.sup.13)R.sup.14, --CH(OH)C(O)N(R.sup.13)R.sup.14, --N(R.sup.13)R.sup.14, --R.sup.15 --N(R.sup.13)R.sup.14, --C(O)R.sup.13, --R.sup.15 --C(O)OR.sup.13, --N(R.sup.13)C(O)R.sup.13, (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.13)R.sup.14, --C(O)OR.sup.13, --C(O)N(R.sup.13)R.sup.14, --C(O)N(R.sup.13)CH.sub.2 C(O)N(R.sup.13)R.sup.14, --N(R.sup.13)C(O)N(R.sup.13)R.sup.14, --N(R.sup.13)C(O)R.sup.14, --N(R.sup.13)S(O).sub.2 R.sup.16, or N(R.sup.13)C(O)N(R.sup.13)--CH.sub.2 C(O)N(R.sup.13) R.sup.14 ;R.sup.7 is --N(R.sup.9)--(C(R.sup.10)(R.sup.11)).sub.n --R.sup.12 (where n is 1to 4) or --O--(C(R.sup.10)(R.sup.11)).sub.n --R.sup.12 (where n is 1 to 6;R.sup.8 is hydrogen, alkyl or halo;R.sup.9 is hydrogen, alkyl, aryl, aralkyl, --R.sup.15 --C(O)OR.sup.13, --R.sup.15 --C(O)N(R.sup.13)R.sup.14, --R.sup.15 --N(R.sup.13)R.sup.14, R.sup.15 --CH(N(R.sup.13)R.sup.14)C(O)OR.sup.13, or --R.sup.15 --S(O).sub.2 R.sup.16 ;each R.sup.10 is independently alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, cycloalkyl, cycloalkylalkyl, --C(O)OR.sup.13 --R.sup.15 C(O)OR.sup.13, R.sup.15 --C(O)N(R.sup.13)R.sup.14, --C(O)--R.sup.15 --N(R.sup.13)R.sup.14, --R.sup.15 --C(O)R.sup.13, --R.sup.15 --C(O)N(R.sup.13)N(R.sup.13)R.sup.14, --R.sup.15 --C(R.sup.13)(OR.sup.13)--R.sup.15 --N(R.sup.13)(R.sup.14), --C(R.sup.13)(OR.sup.13)C(O)OR.sup.14, --R.sup.15 --C(R.sup.13)(C(O)OR.sup.13).sub.2, --C(R.sup.13)(N(R.sup.13)R.sup.14)C(O)OR.sup.13, R.sup.15 --C(R.sup.13)(N(R.sup.13)R.sup.14)C(O)OR.sup.13, --C(R.sup.13)(OR.sup.13)R.sup.14, --R.sup.15 --N(R.sup.13)R.sup.14, --R.sup.15 --N(R.sup.13)C(O)OR.sup.16, --R.sup.15 --N(R.sup.13)C(O)R.sup.14, --R.sup.15 --N(R.sup.13)C(NR.sup.13)R.sup.16, --R.sup.15 --N(R.sup.13)S(O).sub.2 R.sup.16, --R.sup.15 --N(R.sup.13)C(O)N(R.sup.13)R.sup.14, --R.sup.15 --N(R.sup.13)C(NR.sup.13)N(R.sup.13)R.sup.14, --R.sup.15 --N(R.sup.13)C(NR.sup.13)N(R.sup.13)N(R.sup.13)R.sup.14, R.sup.15 --N(R.sup.13)--R.sup.15 --C(R.sup.13)(N(R.sup.13)R.sup.14)C(O)OR.sup.13, --R.sup.15 --N(R.sup.13)S(O)R.sup.14, --R.sup.15 OR.sup.13, R.sup.15 --ON(R.sup.13)C(NR.sup.13)N(R.sup.13)R.sup.14, --R.sup.15 --OS(O).sub.2 OR.sup.13, --R.sup.15 --P(O)(OR.sup.13)R.sup.14, --R.sup.15 --OP(O)(OR.sup.13).sub.2, --R.sup.15 --P(O)(OR.sup.13).sub.2, --R.sup.15 --SR.sup.13, --R.sup.15 --S--R.sup.15 --C(O)OR.sup.13, --R.sup.15 --S--R.sup.15 --N(R.sup.13)R.sup.14, --R.sup.15 --S--R.sup.15 --C(R.sup.13)(N(R.sup.13)R.sup.14)C(O)OR.sup.13, --R.sup.15 --S--R.sup.15 --N(R.sup.13)C(O)OR.sup.13, --R.sup.15 --S--R.sup.15 --N(R.sup.13)C(O)R.sup.13, --R.sup.15 --S--S--R.sup.15 --C(R.sup.13)(N(R.sup.13)R.sup.14)C(O)OR.sup.13, --R.sup.15 SC(O)N(R.sup.13)R.sup.14, --R.sup.15 --SC(S)N(R.sup.13)R.sup.14, --R.sup.15 --S(O)R.sup.13, --R.sup.15 --S(O).sub.2 R.sup.16, --R.sup.15 --S(O)OR.sup.13, --R.sup.15 --S(O).sub.2 OR.sup.13, --R.sup.15 --S(O).sub.2 N(R.sup.13)R.sup.14, --R.sup.15 --S(O)(NR.sup.13)R.sup.14,or each R.sup.10 is aryl (optionally substituted by one or more substituents selected from the group consisting of alkyl, halo, haloalkyl, haloalkoxy, nitro, --OR.sup.--,--SR.sup.13, --N(R.sup.13)R.sup.14, --C(O)OR.sup.13, --C(O)N(R.sup.13) R.sup.14, --S(O).sub.2 OR.sup.13 and OP(O)(OR.sup.13).sub.2),or each R.sup.10 is aralkyl (optionally substituted by one or more substituents selected from the group consisting of alkyl, halo, haloalkyl, haloalkoxy, cyano, nitro, --OR.sup.13, --SR.sup.13, --N(R.sup.13)R.sup.14,--C(O)OR.sup.13, --C(O)N(R.sup.13)R.sup.14, --S(O).sub.2 OR.sup.13 and --OP(O)(R.sup.13).sub.2),or each R.sup.10 is heterocyclyl (optionally substituted by one or more substituents selected from the group consisting of alkyl, halo, haloalkyl, haloalkoxy, aralkyl, --OR.sup.13, --C(O)OR.sup.13, --N(R.sup.13)R.sup.14, --C(O)N(R.sup.13)R.sup.14,--S(O).sub.2 OR.sup.13 and --OP(O)(OR.sup.13).sub.2),or each R.sup.10 is heterocyclylalkyl (where the heterocyclyl radical is optionally substituted by one or more substituents selected from the group consisting of alkyl, halo, haloalkyl, haloalkoxy, aralkyl, --OR.sup.13, --SR.sup.13, --C(O)OR.sup.13, --N(R.sup.13)R.sup.14, --C(O)N(R.sup.13)R.sup.14), --S(O).sub.2 OR.sup.13 and --OP(O)(OR.sup.13).sub.2),or each R.sup.10 is adamantyl (optionally substituted by alkyl, halo, haloalkyl, haloalkoxy, --OR.sup.13, --SR.sup.13.sub.1, --C(O)OR.sup.13, --N(R.sup.13)R.sup.14, --C(O)N(R.sup.13)R.sup.14, --S(O).sub.2 OR.sup.13 and --OP(O)(OR.sup.13).sub.2),or each R.sup.10 is adamantylalkyl (where the adamantyl radical is optionally substituted by alkyl, halo, haloalkyl, haloalkoxy, --C(O)N(R.sup.13)R.sup.14, --S(O).sub.2 OR.sup.13 and --OP(O)(OR.sup.13).sub.2);each R.sup.11 is independently hydrogen, alkyl, cycloalkyl, or aryl;R.sup.12 is --C(O)OR.sup.13 or --C(O)N(R.sup.13)R.sup.14 ;each R.sup.13 and R.sup.14 is independently hydrogen, alkyl, aryl (optionally substituted by halo, alkyl, hydroxy, alkoxy, aralkoxy, amino, dialkylamino, monoalkylamino, nitro, cyano, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl, or dialkylaminocarbonyl), or aralkyl (optionally substituted by halo, alkyl, aryl, hydroxy, alkoxy, aralkyl, amino, dialkylamino, monoalkylamino, nitro, cyano, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl, or dialkylaminocarbonyl);R.sup.15 is a straight or branched alkylene chain; andR.sup.16 is alkyl, aryl (optionally substituted by halo, alkyl, hydroxy, alkoxy, aralkoxy, amino, dialkylamino, monoalkylamino, nitro, cyano, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl, or dialkylaminocarbonyl), or aralkyl (optionally substituted by halo, alkyl, aryl, hydroxy, alkoxy, aralkyl, amino, dialkylamino, monoalkylamino, nitro, cyano, carboxy, alkoxycarbonyl, aminocarbonyl, monoalkylaminocarbonyl, or dialkylaminocarbonyl);as a single stereoisomer or a mixture thereof; or a pharmaceutically acceptable salt thereof.