Interphenylene 7-oxabicyclic [2.2.1] heptane oxazoles as prostaglandin F2a antagonists
AssigneeAllergan Sales, Inc.
InventorsRobert M. Burk, Yariv Donde, Michael E. Garst
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Abstract
The present invention provides novel compounds represented by the general formula I. 1 and pharmaceutically acceptable salts thereof wherein m, n, X, R, R1 and R2 are as defined in the specification. The novel compounds are PGF2α antagonists, useful in pharmaceutical compositions for treating PGF2α-mediated disease responses such as inflammatory reactions relating to rheumatoid arthritis and psoriasis, reproductive disorders, bronchoconstrictive disorders (asthma), excessive bone breakdown (osteoporosis), peptic ulcers, heart disease, platelet aggregation and thrombosis.
Claims17
A compound represented by the general formula I
- 9
- wherein m is an integer of from 1 to 3;
- n is 0 or an integer of from 1 to 4;
- R is selected from the group consisting of CO2H, CO2 R6, CH2OH, CH2O R6
- 10
- and CONR3R4;
- R1 and R2 are independently selected from the group consisting of H, R6, C1-C6 alkenyl, C1-C6 alkynyl, C3-C7 cycloalkyl, C4-C12 alkylcycloalkyl, C6-C10 aryl, C7-C12 alkyl aryl radicals and hetero atom-substituted derivatives thereof, wherein one or more of the hydrogen or carbon atoms in said radicals is replaced with a halogen, nitrogen or sulfur-containing radical;
- R3 and R4 are selected from the group consisting of H and R6;
- and X is selected from the group consisting of R6, hydroxy,
- N(R6)2, CON(R6)2, SR6, COOR6, NO2, CN and OR6, wherein R6 is C1-C6 alkyl, and pharmaceutically acceptable salts thereof.
Dependencies are inferred from the claim text.