Patent ID: 6534037
Filing Date: 2003-03-18
Classification: A61K

Abstract:
A compound of the formula (I) R4 is selected from H, â€”OH, halide and C1-C3alkyl; R5 is selected from H, â€”OH, halide and C1-C3alkyl; R6 is selected from H, â€”OH, â€”SH, halide, C1-C3alkyl, C(&boxH;O)CH3, thio and oxo; C1 and C2 are joined together by a single bond, where C1 and C2 are independently substituted with H, halogen, or C1-C3alkyl; â€ƒrepresents a number â€œnâ€  of methylene (CH2) or fluoromethylene (CFH or CF2) groups, where n is independently selected at each occurrence from 0, 1 and 2; B1 and B2 each has a structure independently selected from R10 at each occurrence is independently selected from R11 at each occurrence is independently selected from H and protecting groups for the A9 moiety, where A9 and R11 may together form â€”N(CH2â€”COOH)2; R12 is selected from hydrogen and pro-drug substituents selected from the group consisting of C1-C3alkyl, â€”C(&boxH;O)(H, C1-C3alkyl or Ar); â€”C(&boxH;O)â€”(C1-C3alkylene)-N(independently H or C1-C3alkyl)2, â€”C(&boxH;O)Oâ€”(H, C1-C3alkyl or Ar), â€”C(&boxH;O)CH(NH2)(H, C1-C3alkyl or Ar), â€”(C1-C3alkylene)-C(&boxH;O)Oâ€”(H, C1-C3alkyl or Ar), â€”(C1-C3alkylene)-OC(&boxH;O)â€”(H, C1-C3alkyl or Ar), â€”(C1-C3alkylene)-N(independently H or C1-C3alkyl)2, â€”(C1-C3alkylene)-NHC(&boxH;O)â€”Ar, â€”(C1-C3alkylene)-CN, â€”(C1-C3alkylene)-NO2, and R13 and R14 are independently selected from H, R15, CN, NO, NO2, â€”C(OC1-C3alkyl)&boxH;NH, â€”N&boxH;C&boxH;O, â€”N&boxH;C&boxH;S, and â€”C(&boxH;O)OR15 such that when R10 is bonded to E then R13 is a direct bond to E; R15 is C1-C6hydrocarbyl; A9 is an electron-donating moiety independently selected at each occurrence from O, S, C(&boxH;O)NH and N(R12); A10 is independently selected from O and S; and E is an extender arm having a structure which provides a stable chain of 2-60 atoms selected from carbon, oxygen, nitrogen and sulfur.