Patent ID: 6127427
Filing Date: 2000-10-03
Classification: A61P,C07C,C07D

Abstract:
A compound of general formula (I) ##STR50## wherein: X is a --CONHOH group;R.sub.1 is a cycloalkyl or a cycloalkenyl;R.sub.2 is a C.sub.1 -C.sub.12 alkyl, C.sub.2 -C.sub.12 alkenyl, C.sub.2 -C.sub.12 alkynyl, phenyl(C.sub.1 -C.sub.6, alkyl)-, cycloalkyl(C.sub.1 -C.sub.6 alkyl)-, cycloalkenyl(C.sub.1 -C.sub.6 alkyl)-, phenoxy(C.sub.1 -C.sub.6 alkyl)-, phenyl(C.sub.1 -C.sub.6 alkyl)O(C.sub.1 -C.sub.6 alkyl)-, phenyl(C.sub.1 -C.sub.6 alkyl)S(C.sub.1 -C.sub.6 alkyl)-, or any one of which may be optionally substituted by C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, halo, cyano (--CN), phenyl, a substituted phenyl;R.sub.3 is the characterising group of a natural or non-natural .alpha. amino acid in which any functional groups may be protected,R.sub.4 is(a) an optionally substituted cycloalkyl or cycloalkenyl ring or(b) a group --CHR.sup.x R.sup.y wherein R.sup.x and R.sup.y each independently represents an optionally substituted phenyl ring which may be linked covalently to each other by a bond or by a C.sub.1 -C.sub.4 alkylene or C.sub.2 -C.sub.4 alkenylene bridge, or(c) a group of formula --(Z--O).sub.n --Z wherein Z is straight or branched C.sub.1 -C.sub.6 alkyl optionally interrupted by one or more non-adjacent S and/or N atoms, n is an integer >1, and no continuous linear sequence of atoms in the group R.sub.4 is >12, or(d) a straight or branched C.sub.1 -C.sub.6 alkyl group, optionally interrupted by one or more non-adjacent S and/or N atoms, which is substituted by at least two substituents of formula --(Z).sub.p --(OZ).sub.q wherein Z is straight or branched C.sub.1 -C.sub.6 alkyl optionally interrupted by one or more non-adjacent S and/or N atoms, p is 0 or 1, q is 1 or 2, and no continuous linear sequence of atoms in the group R.sub.4 is >12, or(e) hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.4 perfluoroalkyl, or a group D-(C.sub.1 -C.sub.6 alkyl)- wherein D is hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, acylamino, optionally substituted phenyl, NH.sub.2, or mono- or di-(C.sub.1 -C.sub.6 alkyl)amino;or R.sub.3 and R.sub.4 taken together represent a divalent chain of formula --C(R.sup.a) (R.sup.b)--A--Alk--, wherein R.sup.a and R.sup.b are independently hydrogen or C.sub.1 -C.sub.6 alkyl, A is a bond, --O--, --S--, --S--S--, --NH-- or --NR.sup.a -- wherein R.sup.a is C.sub.1 -C.sub.6 alkyl, and Alk is C.sub.1 -C.sub.6 alkylene;R.sub.5 is hydrogen or a C.sub.1 -C.sub.6 alkyl group;or a salt, hydrate or solvate thereof.