Patent ID: 6071895
Filing Date: 2000-06-06
Classification: A61K,C07C,C07D,C07F,C07K

Abstract:
A compound according to formula (I) or a pharmaceutically acceptable salt of prodrug thereof:W--(A).sub.n --B--A(A*).sub.m --V (I)wherein n and m are both 1,B is ##STR783## wherein R.sub.14* is hydrogen and M is OR.sub.15 wherein R.sub.15 is a group Px;Px is a solubilising group which is labile in vivo;V is a group ##STR784## wherein R.sub.2* is selected from the group consisting of optionally substituted (C.sub.1 -C.sub.18)acyl and C(O)OR.sub.21, wherein R.sub.21 is selected from hydrogen and R.sub.20, and wherein R.sub.20 is selected from the group consisting ofoptionally substituted (C.sub.1 -C.sub.12)alkyl,optionally substituted (C.sub.2 -C.sub.12)alkenyl,optionally substituted (C.sub.2 -C.sub.12)alkynyl,optionally substituted (C.sub.3 -C.sub.12)cycloalkyl,optionally substituted (C.sub.3 -C.sub.12)cycloalkyl(C.sub.1 -C.sub.6)alkyl,optionally substituted (C.sub.3 -C.sub.18)cycloalkyl(C.sub.2 -C.sub.18)alkenyl,optionally substituted (C.sub.3 -C.sub.18)cycloalkyl(C.sub.2 -C.sub.18)alkynyl,optionally substituted (C.sub.6 -C.sub.12)aryl,optionally substituted (C.sub.6 -C.sub.12)aryl(C.sub.1 -C.sub.6)alkyl,optionally substituted (C.sub.1 -C.sub.12)acyl, andoptionally substituted heterocyclic;R.sub.50 and R.sub.51 and the nitrogen atoms to which they are bound together form a cyclic diazaalkane of the formula: ##STR785## where p is 1 to 3, each R is independently selected from the group consisting of hydrogen, --R'H, --R'C(O)OR"", where R"" and R'"" are (C.sub.1 -C.sub.12)alkyl, (C.sub.3 -C.sub.12)-cycloalkyl, (C.sub.3 -C.sub.12)cycloalkyl(C.sub.1 -C.sub.6)alkyl, (C.sub.6 -C.sub.12)aryl, (C.sub.7 -C.sub.16)aralkyl, (C.sub.2 -C.sub.12)-alkenyl, (C.sub.8 -C.sub.16 C)aralkenyl,(C.sub.2 -C.sub.12)alkynyl, (C.sub.8 -C.sub.16)aralkynyl, or heterocyclic; and R' is an optionally substituted divalent radical derived from (C.sub.1 -C.sub.12)alkyl, (C.sub.3 -C.sub.12)-cycloalkyl, (C.sub.3 -C.sub.12)cycloalkyl(C.sub.1 -C.sub.6 alkyl, (C.sub.6 -C.sub.12)aryl, (C.sub.7 -C.sub.16)aralkyl, (C.sub.2u -C.sub.12)-alkenyl, (C.sub.8 -C.sub.16)aralkenyl,(C.sub.2 -C.sub.12)alkynyl (C.sub.8 -C.sub.16)aralkynyl, or heterocyclic; and wherein any two R substituents, not necessarily vicinal, taken together are optionally substituted (C.sub.2 -C8)alkylidene; andR.sup.8 is R, --NH.sub.2, --NHR, --NR.sub.2, --COOH, --COOR, --CHO, --C(O)R, --CN, halo, --CF.sub.3, --OR, --SR, --S(O)R, --CONH.sub.2, --CONHR, --CONR.sub.2, --NHON, --NHOR, --NO.sub.2, .dbd.O, .dbd.S OR --NHNH.sub.2,wherein each R is independently as defined above;A and A* are each ##STR786## wherein L is a bond, R.sub.13 is hydrogen and each R.sub.12 independently is selected from the group consisting of hydrogen and R.sub.20 as previously defined; andW is R.sub.1* X*, wherein R.sub.1* is a group represented by the formula R.sub.401 NHCH(R.sub.400)C(O)--wherein R.sub.400 is the side chain of a naturally occurring amino acid, and R.sub.401 is quinoline-2-carbonyl; and X* is NR.sub.10, wherein R.sub.10 is selected from the group consisting of hydrogen and R.sub.20 as previously defined.