Patent ID: 6720427
Filing Date: 2004-04-13
Classification: A61P,C07D

Abstract:
A compound of the formula wherein R1 is a straight chain or branched (C2-C8)alkyl, a straight chain or branched (C2-C8)alkenyl, a straight chain or branched (C2-C8)alkynyl, (C3-C8)cycloalkyl, (C4-C8)cycloalkenyl, (3-8 membered) heterocycloalkyl, (C5-C11)bicycloalkyl, (C7-C11)bicycloalkenyl, (5-11 membered) heterobicycloalkyl, (C6-C14) aryl, (5-14 membered) heteroaryl, or ABN-; and wherein R1 is optionally substituted with from one to six substituents R5 independently selected from F, Cl, Br, I, nitro, cyano, â€”CF3, â€”NR7R8, â€”NR7C(&boxH;O)R8, â€”NR7C(&boxH;O)OR8, â€”NR7C(&boxH;O)NR8R9, â€”NR7S(&boxH;O)2R8, â€”NR7S(&boxH;O)2NR8R9, â€”OR7, â€”OC(&boxH;O)R7, â€”OC(&boxH;O)OR7, â€”C(&boxH;O)OR7, â€”C(&boxH;O)R7, â€”C(&boxH;O)NR7R8, â€”OC(&boxH;O)NR7R8, â€”OC(&boxH;O)SR7, â€”SR7, â€”S(&boxH;O)R7, â€”S(&boxH;O)2R7, â€”S(&boxH;O)2NR7R8, and R7;A and B are each independently selected from straight or branched (C1-C8)alkyl, straight chain or branched (C2-C8)alkenyl, straight chain or branched (C2-C8)alkynyl, (C3-C6)cycloalkyl, (C4-C8)cycloalkenyl, (3-8 membered) heterocycloalkyl, (C5-C11)bicycloalkyl, (C7-C11)bicycloalkenyl, and (5-11 membered) heterocycloalkyl; or A and B may be connected to form a 3-8 membered heterocyclic ring optionally containing one or two double bonds and optionally containing one or two further hetero atoms selected independently from O, S, and N; and A and B, or the heterocyclic ring formed thereby, can be optionally independently substituted with from one to six substituents R5 independently selected from F, Cl, Br, I, nitro, cyano, â€”CF3, â€”NR7R8, â€”NR7C(&boxH;O)R8, â€”NR7C(&boxH;O)OR8, â€”NR7C(&boxH;O)NR8R9, â€”NR7S(&boxH;O)2R8, â€”NR7S(&boxH;O)2NR8R9, â€”OR7, â€”OC(&boxH;O)R7, â€”OC(&boxH;O)OR7, â€”C(&boxH;O)OR7, â€”C(&boxH;O)R7, â€”C(&boxH;O)NR7R8, â€”OC(&boxH;O)NR7R8, â€”OC(&boxH;O)SR7, â€”SR7, â€”S(&boxH;O)R7, â€”S(&boxH;O)2R7, â€”S(&boxH;O)2NR7R8, and R7; R3 is â€”C(&boxH;O)NR9â€”, â€”C(&boxH;O)Oâ€”, â€”C(&boxH;O)(CR10R11)nâ€”, or â€”(CR10R11)nâ€”; R4 is a straight chain or a branched (C1-C8)alkyl, a straight chain or a branched (C2-C8)alkenyl, a straight chain or branched (C2-C8 alkynyl), (C3-C8)cycloalkyl, (C4-C8)cycloalkenyl, (3-8 membered) heterocycloalkyl, (C5-C11)bicycloalkyl, (C7-C11)bicycloalkenyl, (5-11 membered) heterobicycloalkyl, (C6-C14)aryl, or (5-14 membered) heteroaryl; and wherein R4 is optionally substituted with from one to three substituents R6 independently selected from F, Cl, Br, I, nitro, cyano, â€”CF3, â€”NR7R8, â€”NR7C(&boxH;O)R8, â€”NR7C(&boxH;O)OR8, â€”NR7C(&boxH;O)NR8R9, â€”NR7S(&boxH;O)2R8,â€”NR7S(&boxH;O)2NR8R9, â€”OR7, â€”OC(&boxH;O)R7, â€”OC(&boxH;O)OR7, â€”C(&boxH;O)OR7, â€”C(&boxH;O)R7, â€”C(&boxH;O)NR7R8, â€”OC(&boxH;O)NR7R8, â€”OC(&boxH;O)SR7, â€”SR7, â€”S(&boxH;O)R7, â€”S(&boxH;O)2R7, â€”S(&boxH;O)2NR7R8, or R7; each R7, R8, and R9 is independently selected from H, straight chain or branched (C1-C8)alkyl, straight chain or branched (C2-C8)alkenyl, straight chain or branched (C2-C8 alkynyl), (C3-C8)cycloalkyl, (C4-C8)cycloalkenyl, (3-8 membered) heterocycloalkyl, (C5-C11)bicycloalkyl, (C7-C11)bicycloalkenyl, (5-11 membered) heterobicycloalkyl, (C6-C14)aryl, and (5-14 membered) heteroaryl, wherein R7, R8, and R9 are each independently optionally substituted with from one to six substituents independently selected from F, Cl, Br, I, NO2, â€”CN, â€”CF3, â€”NR10R11, â€”NR10C(&boxH;O)R11, â€”NR10C(&boxH;O)OR11, â€”NR10C(&boxH;O)NR11R12, â€”NR10S(&boxH;O)2R11, â€”NR10S(&boxH;O)2NR11R12, â€”OR10, OC(&boxH;O)R10, â€”OC(&boxH;O)OR10, â€”OC(&boxH;O)NR10R11, â€”OC(&boxH;O)SR10, â€”SR10, â€”S(&boxH;O)R10, â€”S(&boxH;O)2R10, â€”S(&boxH;O)2NR10R11, â€”C(&boxH;O)R10, â€”C(&boxH;O)OR10, â€”C(&boxH;O)NR10R11, and R10; or, when R7 and R8 are as in NR7R8, they may instead optionally be connected to form with the nitrogen of NR7R8 to which they are attached a heterocycloalkyl moiety of from three to seven ring members, said heterocycloalkyl moiety optionally comprising one or two further heteroatoms independently selected from N, O, and S; each R10, R11, and R12 is independently selected from H, straight chain or branched (C1-C8)alkyl, straight chain or branched (C2-C8)alkenyl, straight chain or branched (C2-C8 alkynyl), (C3-C8)cycloalkyl, (C4-C8)cycloalkenyl, (3-8 membered) heterocycloalkyl, (C5-C11)bicycloalkyl, (C7-C11)bicycloalkenyl, (5-11 membered) heterobicycloalkyl, (C6-C14)aryl, and (5-14 membered) heteroaryl, wherein R10, R11, and R12 are each independently optionally substituted with from one to six substituents independently selected from F, Cl, Br, I, NO2, â€”CN, â€”CF3, â€”NR13R14, â€”NR13C(&boxH;O)R14, â€”NR13C(&boxH;O)OR14, â€”NR13C(&boxH;O)NR14R15, â€”NR13S(&boxH;O)2R14, â€”NR13S(&boxH;O)2NR14R15, â€”OR13, â€”OC(&boxH;O)R13, â€”OC(&boxH;O)OR13, â€”OC(&boxH;O)NR13R14, â€”OC(&boxH;O)SR13, â€”SR13, â€”S(&boxH;O)R13, â€”S(&boxH;O)2R13, â€”S(&boxH;O)2NR13R14, â€”C(&boxH;O)R13, â€”C(&boxH;O)OR13, â€”C(&boxH;O)NR13R14, and R13; each R13, R14, and R15 is independently selected from H, straight chain or branched (C1-C8)alkyl, straight chain or branched (C2-C8)alkenyl, straight chain or branched (C2-C8 alkynyl), (C3-C8)cycloalkyl, (C4-C8)cycloalkenyl, (3-8 membered) heterocycloalkyl, (C5-C11)bicycloalkyl, (C7-C11)bicycloalkenyl, (5-11 membered) heterobicycloalkyl, (C6-C14)aryl, and (5-14 membered) heteroaryl, wherein R13, R14, and R15 are each independently optionally substituted with from one to six substituents independently selected from F, Cl, Br, I, NO2, â€”CN, â€”CF3, â€”NR16R17, â€”NR16C(&boxH;O)R17, â€”NR16C(&boxH;O)OR17, â€”NR16C(&boxH;O)NR17R18, â€”NR16S(&boxH;O)2R17, â€”NR16S(&boxH;O)2NR17R18, â€”OR16, â€”OC(&boxH;O)R16, â€”OC(&boxH;O)OR16, â€”OC(&boxH;O)NR16R17, â€”OC(&boxH;O)SR16, â€”SR16, â€”S(&boxH;O)R16, â€”S(&boxH;O)2R16, â€”S(&boxH;O)2NR16R17, â€”C(&boxH;O)R16, â€”C(&boxH;O)OR16, â€”C(&boxH;O)NR16R17, and R16; each R16, R17, and R18 is independently selected from H, straight chain or branched (C1-C8)alkyl, straight chain or branched (C2-C8)alkenyl, straight chain or branched (C2-C8 alkynyl), (C3-C8)cycloalkyl, (C4-C8)cycloalkenyl, (3-8 membered) heterocycloalkyl, (C5-C11)bicycloalkyl, (C7-C11)bicycloalkenyl, (5-11 membered) heterobicycloalkyl, (C6-C14)aryl, and (5-14 membered) heteroaryl; n is 0, 1, 2, or 3; wherein R10 and R11 in â€”C(&boxH;O)(CR10R11)nâ€” and â€”(CR10R11)nâ€” are for each iteration of n defined independently as recited above; or a pharmaceutically acceptable salt thereof.