Patent ID: 6670324
Filing Date: 2003-12-30
Classification: A61K,A61P,C07K

Abstract:
A compound of formula I wherein:R is independently at each occurrence hydrogen, hydroxy, or Oâ€”Pg; R1 is hydrogen, methyl, CH2C(O)NH2, CH2C(O)NHâ€”Pg; R2 and R3 are independently hydrogen or methyl; R4 is a moiety of the formula R5 is a moiety of the formula A is independently at each occurrence phen-di-yl, pyridin-di-yl, pyridazin-di-yl, pyrimidin-di-yl, pyrazin-di-yl, furan-di-yl, or thiophen-di-yl rings; X is independently at each occurrence a bond or Câ‰¡C; R6 is hydrogen, C1-C12 alkyl, C2-C12 alkynyl, C1-C12 alkoxy, C1-C12 alkylthio, halo, or â€”Oâ€”(CH2)mâ€”[Oâ€”(CH2)n]pâ€”Oâ€”(C1-C12 alkyl), or â€”Oâ€”(CH2)qâ€”Zâ€”R8; R7 is independently at each occurrence hydrogen, hydroxy, amino, azido, OR5, Oâ€”Pg, or NHpâ€”Pg; R7â€² is CHR7CH2R7, CHR7CH2OR9, ethyl, CHR7CO2H, CHR7CH2Oâ€”Pg, or CHR7C(O)â€”Pg; R7â€³ is hydrogen, CH2R7, CH2OR9, methyl, CO2H, CH2Oâ€”Pg, CH2NHpâ€”Pg or C(O)â€”Pg; m, n, and q are independently 2, 3 or 4; p is 0 or 1; Z is pyrrolidin-di-yl, piperidin-di-yl, or piperazin-di-yl; R8 is hydrogen, C1-C12 alkyl, benzyl, or substituted C3-C12 cycloalkylmethyl; R9 is SO3H or a moiety of the formula R10 is hydroxy, C1-C6 alkyl, C1-C6 alkoxy, phenyl, phenoxy, p-halophenyl, p-halophenoxy, p-nitrophenyl, p-nitrophenoxy, benzyl, benzyloxy, p-halobenzyl, p-halobenzyloxy, p-nitrobenzyl, or p-nitrobenzyloxy; and Pg is a hydroxy, amino, amido or carboxy protecting group; with the proviso that the total number of R7 substituents that are OR5 groups does not exceed two; or a pharmaceutical salt or solvate thereof.