Patent ID: 6518291
Filing Date: 2003-02-11
Classification: A61K,A61P,C07D,Y02A

Abstract:
A compound of the formula: wherein:R1 and R2 are independently selected from halogen, CN, NO2, CF3, OCF3, OH, R3, OR3, 1,2-methylenedioxy, 1,2-ethylenedioxy, SR3, S(O)R3, SO2R3, NH2, NHR3, N(R3)2, NR3R9, COOH, or COOR3; each R3 is independently (C1-C4)-straight or branched alkyl, or (C2-C4)-straight or branched alkenyl or alkynyl; each R4 is independently (C1-C6)-straight or branched alkyl, or (C2-C6)-straight or branched alkenyl or alkynyl; and each R4 optionally comprises up to 2 substituents, wherein: the first of said substituents, if present, is R1, R5 or R8, and the second of said substituents, if present, is R1; each R5 is independently selected from OR6, OC(O)R7, OC(O)R6, OC(O)OR7, OC(O)OR6, OC(O)N(R7)2, OP(O)(OR7)2, SR7, SR6, S(O)R7, S(O)R6, SO2R7, SO2R6, SO2N(R7)2, SO2NR6R7, SO3R7, C(O)R6, C(O)OR6, C(O)R7, C(O)OR7, NC(O)C(O)R7, NC(O)C(O)R6, NC(O)C(O)OR7, NC(O)C(O)N(R7)2, C(O)N(R7)2, C(O)N(OR7)R7, C(O)N(OR7)R6, C(NOR7)R7, C(NOR7)R6, N(R7)2, NR7C(O)R6, NR7C(O)R7, NR6C(O)R6, NR7C(O)OR7, NR7C(O)OR6, NR7C(O)N(R7)2, NR7C(O)NR6R7, NR7SO2R7, NR7SO2R6, NR7SO2N(R7)2, NR7SO2NR6R7, N(OR7)R7, N(OR7)R6, P(O)(OR7)N(R7)2, and P(O)(OR7)2; R6 is a monocyclic or a bicyclic ring system consisting of 5 to 6 members per ring, wherein said ring system optionally comprises up to 4 heteroatoms selected from N, O, and S, and wherein a CH2 adjacent to any of said N, O, or S heteroatoms is optionally substituted with C(O); and each R6 optionally comprises up to 3 substituents, each substituent independently selected from R1; each R7 is independently H, (C1-C4)-straight or branched alkyl, or (C2-C4) straight or branched alkenyl; and each R7 optionally comprises a substituent that is R8; R8 is a monocyclic or a bicyclic ring system consisting of 5 to 6 members per ring, wherein said ring system optionally comprises up to 4 heteroatoms selected from N, O, and S, and wherein a CH2 adjacent to said N, O or S maybe substituted with C(O); and each R8 optionally comprises up to 2 substituents independently chosen from H, (C1-C4)-straight or branched alkyl, (C2-C4) straight or branched alkenyl, 1,2-methylenedioxy, 1,2-ethylenedioxy and (CH2)nâ€”Z; wherein n is 0, 1 or 2; R9 is an amino protecting group; and wherein any carbon atom in any R3, R4 or R7 is optionally replaced by O, S, SO, SO2, NH, or N(C1-C4)-alkyl, each R10, R11, R12, and R13 is independently selected from hydrogen, R1, and R2, X is selected from CH2, CHR3, CHR4, O, S, NH, NR3, and NR4, and Y is selected from CH, CR3, CR4, and N, and wherein: when Y is N and R10-13 are H, either R1 or R2 is CN, and when Y is N and X is NH, no more than one of R1, R2, R10, R11, R12, and R13 may be Cl, Br, or CF3.