초록

In particular, the present invention relates to compounds having the structure: [ STR 1 ] and the tautomers, acceptable salts, and biohydrolyzable amides, esters, and imides thereof, wherein A, Q, n, P, L.sub.1, L.sub.2, L.sub.3, L.sub.4, Z, X, B.sub.1, and B.sub.2 are defined herein.

대표청구항 ▼

[ What is claimed is:] [1.] A compound having the structure: [ STR 57 ] and the tautomers, acceptable salts, and biohydrolyzable amides, ester, and imides thereof, wherein:(a) B.sub.1 is selected from the group consisting of hydrogen, methyl, ethyl, propyl;(b) B.sub.2 is selected from the group cons

[ What is claimed is:] [1.] A compound having the structure: [ STR 57 ] and the tautomers, acceptable salts, and biohydrolyzable amides, ester, and imides thereof, wherein:(a) B.sub.1 is selected from the group consisting of hydrogen, methyl, ethyl, propyl;(b) B.sub.2 is selected from the group consisting of hydrogen, methyl, ethyl, propyl;(c) X is selected from the group consisting of nil, --CH.sub.2 --, and --NH--;(d) Z is an aromatic, substituted or unsubstituted, monocyclic or polycyclic, carbocyclic ring;(e) L.sub.1, L.sub.2, and L.sub.3 are each, independently, selected from the group consisting of nil, --NH--, --O--, --S--, --C(O)--, --CF.sub.2 --, alkylene, alkenylene, cycloalkylene, arylene, arylalkylene, arylalkenylene, --C(O)NH--, --NHSO.sub.2 R.sup.1 --, --C(O)R.sup.2 --, --C(O)R.sup.3 --O--, --C(O)R.sup.4 --S--, --C(O)R.sup.5 --NH--, --NH--R.sup.6 --, --OR.sup.7 --, --C(O)O--R.sup.8 --, --C(O)NH--R.sup.9 --, --NHC(O)--R.sup.10 --, --OC(O)R.sup.11 -- and --C(O)--CH(R.sup.12)--N(R.sup.13)--Y--, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, and R.sup.11 are, independently selected from the group consisting of alkyl, alkenyl, cycloalkyl, aryl, arylalkyl, arylalkenyl, alkylamino, protected alkylamino, arylamino, protected arylamino, arylalkylamino, protected arylalkylamino, wherein R.sup.2 is selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, aryl, arylalkyl, arylalkenyl, alkylamino, protected alkylamino, arylamino, protected arylamino, arylalkylamino, protected arylalkylamino, and --AA wherein --AA is an amino acid side chain, and R.sup.13 is hydrogen, and wherein Y is nil or --C(O)--CH(R.sup.14)--N(R.sup.15)-- wherein R.sup.14 is selected from the group consisting of hydrogen, alkyl, alkenyl, cycloalkyl, aryl, arylalkyl, arylalkenyl, alkylamino, protected alkylamino, arylamino, protected arylamino, arylalkylamino, protected arylalkylamino, and --AA wherein --AA is an amino acid side chain, and R.sup.15 is hydrogen;(f) L.sub.4 is nil or --C(O)--;(g) P is a poly(alkylene oxide) polymer selected from the group consisting of a linear poly(alkylene oxide), a branched chain poly(alkylene oxide), and a star poly(alkylene oxide);(h) n is an integer from 1 to about 100;(i) Q is nil or --O--; and(j) A is selected from the group consisting of alkyl alkenyl, cycloalkyl, aryl, arylalkyl, arylalkenyl, Z', wherein Z' is an aromatic, substituted or unsubstituted, monocyclic or polycyclic, carbocyclic ring; --C(O)--Z', and --C(O)--R.sup.15 --CF.sub.3, wherein R.sup.15 is nil or alkyl, and [ STR 58 ] wherein L.sub.1 ', L.sub.2 ', L.sub.3 ', Z', X', B.sub.1 ', and B.sub.2 ' are defined as for, respectively L.sub.1, L.sub.2, L.sub.3, Z, X, B.sub.1, and B.sub.2 ;wherein the compound is not (I) wherein (I) has the structure: [ STR 59 ] wherein m is an integer from about 5 to about 500.