Patent ID: 6559137
Filing Date: 2003-05-06
Classification: A61P,C07C,C07D,C07F,C07H

Abstract:
A compound of formula I: wherein:A is selected from Ht; â€”Râ€²â€”Ht; each Râ€² is independently selected from â€”C(O)â€”, â€”S(O)2â€”, â€”C(O)â€”C(O)â€”, â€”Oâ€”C(O)â€”, â€”Oâ€”S(O)2, â€”N(R2)â€”S(O)2â€”, â€”N(R2)â€”(O)â€” or â€”N(R2)â€”C(O)â€”C(O)â€”; each Ht is independently selected from C3-C7 cycloalkyl; C5-C7 cycloalkenyl; C6-C10 aryl; or a 5-7 membered saturated or unsaturated heterocycle, containing one or more heteroatoms selected from N, N(R2), O, S and S(O)n; wherein said aryl or said heterocycle is optionally fused to Q; and wherein any member of said Ht is optionally substituted with one or more substituents independently selected from oxo, â€”OR2, SR2, â€”R2, â€”N(R2)2, â€”(C1-C4)-alkyl substituted with OH and optionally substituted with Q, â€”CN, â€”C(O)Oâ€”R2, â€”C(O)â€”N(R2)2, â€”S(O)2â€”N(R2)2, â€”N(R2)â€”C(O)â€”R2, â€”C(O)â€”R2, â€”S(O)nâ€”R2, â€”OCF3, â€”S(O)nâ€”Q, methylenedioxy, â€”N(R2)â€”S(O)2â€”R2, halo, â€”CF3, â€”NO2, Q, â€”OQ, â€”OR7, â€”SR7, â€”R7, â€”N(R2)(R7) or â€”N(R7)2; each R2 is independently selected from H, or (C1-C4)-alkyl optionally substituted with Q; B, when present, is â€”N(R2)â€”C(R3)2â€”C(O)â€”; each x is independently 0 or 1; each R3 is independently selected from H, Ht, (C1-C6)-alkyl, (C2-C6)-alkenyl, (C3-C6)-cycloalkyl or (C5-C6)-cycloalkenyl; wherein any member of said R3, except H, is optionally substituted with one or more substituents selected from â€”OR2, â€”C(O)â€”NHâ€”R2, â€”S(O)nâ€”N(R2)2, Ht, â€”CN, â€”SR2, â€”CO2R2, N(R2)â€”C(O)â€”R2; each n is independently 1 or 2; G, when present, is selected from H, R7 or (C1-C4)-alkyl; D and Dâ€² are independently selected from Q; (C1-C6)-alkyl, which is optionally substituted with one or more groups selected from (C3-C6)-cycloalkyl, â€”OR2, â€”R3, â€”Oâ€”Q or Q; (C2-C4)-alkenyl, which is optionally substituted with one or more groups selected from (C3-C6)-cycloalkyl, â€”OR2, â€”R3, â€”Oâ€”Q or Q; (C3-C6)-cycloalkyl, which is optionally substituted with or fused to Q; or (C5-C6)-cycloalkenyl, which is optionally substituted with or fused to Q; each Q is independently selected from a 3-7 membered saturated, partially saturated or unsaturated carbocyclic ring system; or a 5-7 membered saturated, partially saturated or unsaturated heterocyclic ring containing one or more heteroatoms selected from O, N, S, S(O)n or N(R2); wherein any ring in Q is optionally substituted with one or more groups selected from oxo, â€”OR2, â€”R2, â€”N(R2)2, â€”N(R2)â€”C(O)â€”R2, â€”(C1-C4)-alkyl substituted with OH and optionally substituted with Q, â€”CN, â€”C(O)OR2, â€”C(O)â€”N(R2)2, halo or â€”CF3; E is selected from Ht; Oâ€”Ht; Htâ€”Ht; (C3-C6)-saturated carbocycle, which is optionally substituted with one or more groups selected from R4 or Ht; or (C5-C6)-unsaturated carbocycle, which is optionally substituted with one or more groups selected from R4 or Ht; each R4 is independently selected from â€”OR2, â€”SR2, â€”C(O)â€”NHR2, â€”S(O)2â€”NHR2, halo, â€”N(R2)â€”C(O)â€”R2, â€”N(R2)2 or â€”CN; each R7 is independently selected from wherein each M is independently selected from H, Li, Na, K, Mg, Ca, Ba, N(R2)4, (C1-C12)-alkyl, (C2-C12)-alkenyl, or â€”R6; wherein 1 to 4 â€”CH2 radicals of the alkyl or alkenyl group, other than the â€”CH2 that is bound to Z, is optionally replaced by a heteroatom group selected from O, S, S(O), S(O)2, or N(R2); and wherein any hydrogen in said alkyl, alkenyl or R6 is optionally replaced with a substituent selected from oxo, â€”OR2, â€”R2, N(R2)2, N(R2)3, R2OH, â€”CN, â€”C(O)OR2, â€”C(O)â€”N(R2)2, S(O)2â€”N(R2)2, N(R2)â€”C(O)â€”R2, C(O)R2, â€”S(O)nâ€”R2, OCF3, â€”S(O)nâ€”R6, N(R2)â€”S(O)2â€”R2, halo, â€”CF3, or â€”NO2; Mâ€² is H, (C1-C12)-alkyl, (C2-C12)-alkenyl, or â€”R6; wherein 1 to 4 â€”CH2 radicals of the alkyl or alkenyl group is optionally replaced by a heteroatom group selected from O, S, S(O), S(O)2, or N(R2); and wherein any hydrogen in said alkyl, alkenyl or R6 is optionally replaced with a substituent selected from oxo, â€”OR2, â€”R2, â€”N(R2)2, N(R2)3, â€”R2OH, â€”CN, â€”CO2R2, â€”C(O)â€”N(R2)2, â€”S(O)2â€”N(R2)2, â€”N(R2)â€”C(O)â€”R2, â€”C(O)R2, â€”S(O)nâ€”R2, â€”OCF3, â€”S(O)nâ€”R6, â€”N(R2)â€”S(O)2â€”R2, halo, â€”CF3, or â€”NO2; Z is â€”CH2â€”, O, S, â€”N(R2)â€”, or, when M is not present, H, CH3, or â€”N(R2)2; Y is P or S; X is O or S; R9 is C(R2)2, O or N(R2); and wherein when Y is S, Z is not S; and R6 is a 5-6 membered saturated, partially saturated or unsaturated carbocyclic or heterocyclic ring system, or an 8-10 membered saturated, partially saturated or unsaturated bicyclic ring system; wherein any of said heterocyclic ring systems contains one or more heteroatoms selected from O, N, S, S(O)n or N(R2); and wherein any of said ring systems optionally contains 1 to 4 substituents independently selected from OH, C1-C4 alkyl, Oâ€”(C1-C4)-alkyl or Oâ€”C(O)â€”(C1-C4)-alkyl.