Patent ID: 6211186
Filing Date: 2001-04-03
Classification: A61K,A61P,A61Q,C07C,C08G,Y10S

Abstract:
A compound having the structure: ##STR58##and the tautomers, acceptable salts, and biohydrolyzable amides, ester, and imides thereof, wherein:(a) B.sub.1 is selected from the group consisting of a methylene group connected to B.sub.2 through a single bond such that B.sub.1 and B.sub.2 form a five-membered ring, and a methylene group connected to B.sub.2 through another methylene group such that B.sub.1 and B.sub.2 form a six membered ring;(b) B.sub.2 is selected from the group consisting of a methylene group connected to B.sub.1 through a single bond such that B.sub.1 and B.sub.2 form a five-membered ring, and a methylene group connected to B.sub.2 through another methylene group such that B.sub.1 and B.sub.2 form a six membered ring;(c) X is selected from the group consisting of nil, --CH.sub.2 --, and --NH--;(d) Z is a heterocyclic 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.12 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, or R.sup.12 and R.sup.13 together form a monocyclic of polycyclic heterocyclic ring including the nitrogen to which R.sup.13 is bonded, 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, or R.sup.14 and R.sup.15 together form a second monocyclic or polycyclic heterocyclic ring including the nitrogen to which R.sup.15 is bonded;(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 ##STR59##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.