Patent ID: 6495684
Filing Date: 2002-12-17
Classification: A61P,C07D

Abstract:
A compound selected from the group consisting of the following formulae: wherein:Z1 is â€”N(R9)â€”or â€”CH2â€”Oâ€”; Z2 is â€”N(R9)â€”or â€”Oâ€”CH2â€”; R1 and R4 are each independently hydrogen, halo, alkyl, nitro, â€”OR9, â€”C(O)OR9, â€”C(O)N(R9)R10, â€”N(R9)R10, â€”N(R9)C(O)R9, or â€”N(H)S(O)2R11; R2 is â€”C(NH)NH2, â€”C(NH)N(H)OR9, â€”C(NH)N(H)C(O)OR11, â€”C(NH)N(H)C(O)R9, â€”C(NH)N(H)S(O)2R11, or â€”C(NH)N(H)C(O)N(H)R9; R3 is hydrogen, halo, alkyl, haloalkyl, nitro, ureido, guanidino, â€”OR9, â€”C(NH)NH2, â€”C(NH)N(H)OR9, â€”C(O)N(R9)R10, â€”R12â€”C(O)N(R9)R10, â€”CH(OH)C(O)N(R9)R10, â€”N(R9)R10, â€”R12â€”N(R9)R10, â€”C(O)OR9, â€”R12â€”C(O)OR9, â€”N(R9)C(O)R9, (1,2)-tetrahydropyrimidinyl (optionally substituted by alkyl), (1,2)-imidazolyl (optionally substituted by alkyl), or (1,2)-imidazolinyl (optionally substituted by alkyl); R7 is â€”Xâ€”CH2â€”[C(R13)H]pâ€”C(R13)H2 or â€”Xâ€”C([C(R13)H]pâ€”C(R13)H2)2H where: p is 0 to 5; X is â€”Oâ€”, â€”S(O)nâ€” (where n is 0 to 2), orâ€”N(R9)â€”; and each R13 is independently â€”[C(OR9)H]mâ€”CH2â€”OR9 (where m is 1 to 4), â€”[CH2]nâ€”OR9, â€”[CH2]nâ€”SR9, â€”[CH2]nâ€”N(R9)R10, â€”[CH2]nâ€”OC(O)R9, â€”[CH2]nâ€”SC(O)R9, â€”[CH2]nâ€”N(R9)C(O)R9, â€”[CH2]nâ€”OC(O)OR11, â€”[CH2]nâ€”N(R9)C(O)OR11, â€”[CH2]nâ€”OC(O)N(R9)R10, or â€”[CH2]nâ€”N(R9)C(O)N(R9)R10 (where each n is independently 0 to 2); or R7 is selected from the group consisting of the following formulae: whereq is 0 to 4; p is 0 to 5; each R13 is independently â€”[C(OR9)H]mâ€”CH2â€”OR9 (where m is 1 to 4), â€”[CH2]nâ€”OR9, â€”[CH2]nâ€”SR9, â€”[CH2]nâ€”N(R9)R10, â€”(CH2)nâ€”OC(O)R9, â€”[CH2]nâ€”SC(O)R9, â€”[CH2]nâ€”N(R9)C(O)R9, â€”[CH2]nâ€”OC(O)OR11, â€”[CH2]nâ€”N(R9)C(O)OR11, â€”[CH2]nâ€”OC(O)N(R9)R10, or â€”[CH2]nâ€”N(R9)C(O)N(R9)R10 (where each n is independently 0 to 2); and each R14 is â€”Xâ€”[CH2]râ€” or â€”Xâ€”CH2â€”[C(R13)H]râ€”, where: each r is independently 0 to 5, and each X is â€”Oâ€”, â€”S(O)nâ€” (where n is 0 to 2), or â€”N(R9)â€”; and each R13 is independently â€”[CH(OR9)]mâ€”CH2â€”OR9 (where m is 1 to 4), â€”[CH2]nâ€”OR9, â€”[CH2]nâ€”SR9, â€”[CH2]nâ€”N(R9)R10, â€”[CH2]nâ€”OC(O)R9, â€”[CH2]nâ€”SC(O)R9, â€”[CH2]nâ€”N(R9)C(O)R9, â€”[CH2]nâ€”OC(O)OR11, â€”[CH2]nâ€”N(R9)C(O)OR11, â€”[CH2]nâ€”OC(O)N(R9)R10, or â€”[CH2]nâ€”N(R9)C(O)N(R9)R10 (where each n is independently 0 to 2); each R9 and R10 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); each R11 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); and each R12 is independently an alkylene or alkylidene chain; as a single stereoisomer or a mixture thereof; or a pharmaceutically acceptable salt thereof.