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US 5,686,424 AGranted
2-oxoethyl derivatives as immunosuppressants
AssigneeMiles Inc.
InventorsRichard D. Connell, David G. Osterman, Michael E. Katz
Life of this patent
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Abstract
A class of compounds that suppress human T-lymphocyte proliferation is disclosed. The active compounds essentially contain at least the following structure: ##STR1##
Claims10
A compound having T-lymphocyte inhibitory activity and the generalized structure ##STR7## wherein n is 2 or 3;
- one of R.sup.2 and R.sup.3 is H, and the other is H or CH.sub.3 ;
- p is 0 or 1;
- and
- when p is 0, R.sup.4 is
- a) cyclohexyl optionally substituted by alkyl of 4-5 carbon atoms, or by phenyl, or by substituted phenyl wherein the substituent is halogen or methyl;
- b) bicycloheptyl optionally substituted up to three-fold by methyl;
- c) tricycloalkyl of 10 carbon atoms;
- d) 1,2,3,4-tetrahydronaphthyl;
- or
- e) methyl substituted by tricycloalkyl of 10 carbon atoms, which is in turn optionally substituted by methyl;
- when p is 1, R.sup.4 is
- f) butenyl substituted at least once by phenyl or by a diene of 11 carbon atoms;
- g) alpha-substituted benzyl wherein the alpha substituent is an alkyl group of 2-3 carbon atoms or cyclohexyl;
- or
- h) tricycloalkyl of 10 carbon atoms, substituted once by methyl;
- one of R.sup.11 and R.sup.12 is H, and the other is
- i) phenyl;
- or
- j) alkyl of 1-4 carbon atoms, optionally substituted by phenyl, or by benzyloxy, or by cyclohexyl;
- and
- R.sup.13 is unsubstituted benzyl, or benzyl substituted by methyl, or benzyl wherein the phenyl moiety is substituted by methoxy.
18 more elements
Dependencies are inferred from the claim text.