Patent ID: 6753410
Filing Date: 2004-06-22
Classification: A61K,C07K

Abstract:
A compound of formula I or a salt thereof: wherein:R1 is benzoylphenyl or benzoylphenylC1-6alkyl wherein the benzoylphenyl moiety is optionally substituted by from one to nine bromine atoms and the alkyl moiety is optionally substituted by C1-6alkylsulfonylamino; or C1-6alkoxy; R2 and R3 are independently chosen from C1-10alkyl, C1-10alkoxy, C2-10alkenyl, C2-10alkenyloxy, C2-10alkynyl or C2-10alkynyloxy; phenyl; naphthyl; a five-membered heteroaromatic ring containing 1, 2, 3 or 4 heteroatoms independently chosen from O, N and S, at most one of the heteroatoms being O or S; a six-membered heteroaromatic ring containing 1,2 or 3 nitrogen atoms; and a group (CH2)pQ1 wherein Q1 is phenyl, naphthyl, a five-membered heteroaromatic ring containing 1, 2, 3 or 4 heteroatoms independently chosen from O, N and S, at most one of the heteroatoms being O or S, and a six-membered heteroaromatic ring containing 1, 2 or 3 nitrogen atoms; and wherein each of R2 and R3 is independently optionally substituted by one to three groups independently chosen from: (a) halogen, cyano and nitro, (b) hydroxy, (c) C1-3alkyl, C2-3 alkenyl and C2-3alkynyl, (d) C1-3alkoxy, (e) NR6R7 wherein R6 and R7 are independently chosen from hydrogen, C1-5alkyl and C1-5alkoxyC1-5alkyl, (f) CO2R8 wherein R8 is hydrogen or C1-4alkyl, (g) CONR6R7 or OCONR6R7 wherein R6 and R7 are independently as defined above, (h) SO2NR6R7 wherein R6 and R7 are independently as defined above, (i) CH2NR6R7 wherein R6 and R7 are independently as defined above, (j) N(R8)COR8â€² wherein R8 is independently as defined above and R8â€² is independently as defined for R8, (k) NR8SO2R8â€² where R8 and R8â€² are independently as defined above; alternatively R3 may be hydrogen; R4 and R5 are independently chosen from hydrogen, C1-6alkyl optionally substituted by halogen, hydroxy, thiol, amino, C1-4alkoxy, C1-4 alkylthio, carboxy, C1-4 alkoxycarbonyl and (CH2)qQ2 wherein Q2 is a five-membered unsaturated heterocycle containing 1, 2, 3 or 4 heteroatoms optionally chosen from O, N, and S providing that not more than one heteroatom is O or S, a six-membered unsaturated heterocycle containing 1, 2 or 3 N atoms and phenyl and naphthyl, or a fused ring which is indolyl, each of the foregoing rings being optionally substituted with one to three groups independently chosen from hydroxy, C1-4alkyl, C1-4alkoxy, thiol, C1-4alkylthio, halogen, amino, carboxy, amido, CO2H and â€”NHC(NH2)2 and wherein each of the foregoing rings is optionally fused to a benzene ring; alternatively R5 may be benzoylbenzyl which is optionally substituted by from one to nine bromine atoms; B is C&boxH;O or CHOH in the R configuration; L is a bond or [(CH2)mNHCO]n in which one of the methylene groups may be replaced by a disulphide group; Z is (CH2)kamino, benzoxy or biotin, or when L is a bond then Z is hydrogen, or biotin providing that when Z is hydrogen then either R1 is not C1-6alkoxy or R5 is benzoxybenzyl; k is an integer of from one to ten; each m is independently an integer of from one to ten; n is an integer of from one to ten; p is zero, one, two or three; and q is zero, one, two or three; with the proviso that no carbon atom is substituted by more than one hydroxy group.