发明名称 Interheteroaryl 7-oxabicyclic [2.2.1]heptane oxazoles as prostaglandin F2alpha antagonists
摘要 The present invention provides novel compounds represented by the general formula I.whereinm 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 P(O)(OH)2, 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 heteroatom-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; andX is selected from the group consisting of H, R6, hydroxy,N(R6)2, CON(R6)2, SR6, sulfoxy, sulfone, halogen, COOR6, NO2, CN and OR6, wherein R6 is C1-C6 alkyl; Y is O or S; Z is N or CH and pharmaceutically acceptable salts thereof. The novel compounds are PGF2alpha antagonists, useful in pharmaceutical compositions for treating PGF2alpha-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.
申请公布号 US6369089(B1) 申请公布日期 2002.04.09
申请号 US20010840675 申请日期 2001.04.23
申请人 ALLERGAN SALES, INC. 发明人 BURK ROBERT M.;DONDE YARIV
分类号 A61K31/422;A61P1/04;A61P7/02;A61P9/04;A61P11/06;A61P15/00;A61P17/06;A61P19/02;A61P19/10;A61P29/00;A61P43/00;C07D493/08;(IPC1-7):A61K31/422;C07D413/14 主分类号 A61K31/422
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