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US 5,177,072 AGranted
Treatment of autoimmune inflammatory, and psoriatic diseases with heterocyclic aminoalkyl esters of mycophenolic acid and derivatives
AssigneeSyntex (U.S.A.) Inc.
InventorsPeter H. Nelson, Chee-Liang L. Gu, Anthony C. Allison, Elsie M. Eugui, William A. Lee
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Abstract
Heterocyclic aminoalkyl esters of mycophenolic acid, and the derivatives and pharmaceutically acceptable salts thereof, are useful as immunosuppressive agents, anti-inflammatory agents, anti-tumor agents, anti-viral agents, and anti-psoriatic agents.
Claims9
A method of treating a mammal for a disease state selected from the group consisting of:
- autoimmune disease, inflammatory disease, and psoriatic disease, which comprises administering a therapeutically effective amount of a compound represented by the formula:
- ##STR16## wherein:
- m is an integer from two to four;
- Z is selected from formulae (a), (b), (c), or (d), as follows:
- (a) ##STR17## in which:
- R.sup.1 is hydrogen, alkyl or cycloalkyl having seven or more carbon atoms, or --NR.sup.2 R.sup.3, in which;
- R.sup.2 is hydrogen or lower alkyl, and
- R.sup.3 is hydrogen, lower alkyl, -phenyl--CO.sub.2 R.sup.2, or a pharmaceutically acceptable cation;
- (b) ##STR18## in which:
- R.sup.4 is hydrogen, alkyl, aryl, or --NR.sup.2 R.sup.3 ;
- (c) ##STR19## in which:
- n is an integer from zero to six, and R.sup.5 is hydrogen, lower alkyl, or a pharmaceutically acceptable cation;
- (d) ##STR20## in which:
- R.sup.6 and R.sup.7 are independently hydrogen or --CO.sub.2 R.sup.5 ;
- and
- Y is lower alkylene of four to six carbon atoms, or lower alkylene of three to five carbon atoms plus one member that is --O--, --S--, or --N(R.sup.8)-- where R.sup.8 is hydrogen or alkyl of one to five carbon atoms;
- or a pharmaceutically acceptable salt thereof.
14 more elements
Dependencies are inferred from the claim text.