| 摘要 |
PCT No. PCT/EP97/05709 Sec. 371 Date Apr. 7, 1999 Sec. 102(e) Date Apr. 7, 1999 PCT Filed Oct. 10, 1997 PCT Pub. No. WO98/17639 PCT Pub. Date Apr. 30, 1998Mercapto amino acid derivatives of formula (I), wherein R is hydrogen, a salt-forming cation of a in vivo hydrolysable ester-forming group; R1 is selected from (a) and (b) in which A is a monocyclic aryl or heteroaryl ring and B is a monocyclic aryl, alicyclic or heterocyclic ring, C and D are independently -Zp-(CR8CR9)q- or -(CR8CR9)q-Zp- where p is 0 or 1, q is 0 to 3 provided that p+q in C is not 0, R8 and R9 are independently hydrogen or (C1-6)alkyl or together represent oxo and Z is O, NR10 or S(O)x where R10 is hydrogen, (C1-6)alkyl or aryl(C1-6)alkyl and x is 0-2, and wherein C and D are linked ortho to one another on each of the rings A and B in formula (b); R2 is hydrogen, (C1-6)alkyl or aryl(C1-6)alkyl; R3 is hydrogen, (C1-6)alkyl optionally substituted by up to three halogen atoms, (C3-7)cycloalkyl, fused aryl(C3-7)cycloalkyl, (C3-7)cycloalkyl(C2-6)alkyl, (C2-6)alkenyl, (C2-6)alkynyl, aryl, aryl-(CH2)m-X-(CH2)n, heterocyclyl or heterocyclyl-(CH2)m-X-(CH2)n, where m is 0 to 3, n is 1 to 3 and X is O or S(O)x where x is 0-2 or a bond; R4 is hydrogen or an in vivo hydrolysable acyl group; and R5 and R6 are independently hydrogen and (C1-6)alkyl or together represent (CH2)r, where r is 2 to 5; for use in treatment of bacterial infections in humans or animals by administration in combination with a beta -lactam antiobiotic. |
