Patent ID: 6118011
Filing Date: 2000-09-12
Classification: A61K,A61P,B82Y,C07D,C07F

Abstract:
A lipid carrier comprising:(a) a headgroup-modified lipid;(b) a bioactive agent: and,(c) a taxane having the formula: ##STR12## wherein: A.sup.1 is H or a group having the formula Q--C(O)NHCH(C.sub.6 H.sub.5)CH(OR)C(O)--;Q is C.sub.6 H.sub.5 --, (CH.sub.3).sub.3 C--O-- or (CH.sub.3)CH.dbd.C(CH.sub.3)--;A.sup.2 is H or CH.sub.3 C(O)--;R is H, or a group having the formula Y.sup.1, Z.sup.1 X.sup.1, or Z.sup.1 D.sup.1 ;R.sup.1 is H, or a group having the formula Y.sup.2, Z.sup.2 X.sup.2, or Z.sup.2 D.sup.2 ;wherein each of X.sup.1 and X.sup.2 is independently a group having the formula: ##STR13## wherein G.sup.1 is --OP(O).sub.2 OCH.sub.2 CH.sub.2 N(CH.sub.3).sub.3, --OP(O).sub.2 OCH.sub.2 CH.sub.2 NH.sub.2' --OP(O).sub.2 OCH.sub.2 CH(OH)CH.sub.2 OH, or --OP(O).sub.2 OCH.sub.2 H(NH.sub.2)CO.sub.2 H;wherein each of D.sup.1 and D.sup.2 is independently a group having the formula: ##STR14## wherein: each of Y.sup.1 and Y.sup.2 is independently a group having the formula C(O)(CH.sub.2).sub.a (CH.dbd.CH).sub.b (CH.sub.2).sub.c (CH.dbd.CH).sub.d (CH.sub.2).sub.e (CH.dbd.CH).sub.f (CH.sub.2).sub.g (CH.dbd.CH).sub.h (CH.sub.2).sub.i CH.sub.3,the sum of a+2b+c+2d+e+2f+g+2h+i is equal to an integer of from 7 to 22,a is zero or an integer from 1 to 22,each of b, d, f and h is independently zero or 1,c is zero or an integer from 1 to 20,e is zero or an integer from 1 to 17,g is zero or an integer from 1 to 14,i is zero or an integer from 1 to 11,a to i can be the same or different at each occurrence;wherein:each of Z.sup.1 and Z.sup.2 is independently a linker of the formula: --C(O)(CH.sub.2).sub.j (CH.dbd.CH).sub.k (CH.sub.2).sub.l (CH.dbd.CH).sub.m (CH.sub.2).sub.n (CH.dbd.CH).sub.o CH.sub.2).sub.p (CH.dbd.CH).sub.g (CH.sub.2).sub.r C(O)--,the sum of i+2k+l+2m+n+2o+p+2q+r is equal to an integer from 2to 22,each of k, m, o and q is independently zero or 1,j is zero or an integer from 2 to 22,l is zero or an integer from 1 to 20,n is zero or an integer from 1 to 17,p is zero or an integer from 1 to 14,r is zero or an integer from 1 to 11,each of j to r can be the same or different at each occurrence,wherein when R.sup.1 is H, A.sup.1 is a group having the formula Q--C(O)NHCH(C.sub.6 H.sub.5)CH(OR)C(O)-- and R is not H;wherein when A.sup.1 is H or when A.sup.1 is a group having the formula Q--C(O)NHCH(C.sub.6 H.sub.5)CH(OR)C(O)-- and R is H, R.sup.1 is not H; andwherein at least one of R and R.sup.1 is not H.