3-hetero-substituted-n-benzyl-indoles and prevention of leucotriene
申请人:Merck Frosst Canada, Inc.
公开号:US05081138A1
公开(公告)日:1992-01-14
Compounds having the formula: ##STR1## are inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents. They are also useful in treating diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion, dysmenorrhea, and migraine.
Tetrahydrocarbazole 1-alkanoic acids, pharmaceutical compositions and use
申请人:Merck & Co., Inc.
公开号:US04808608A1
公开(公告)日:1989-02-28
Tetrahydrocarbazole 1-alkanoic acids are disclosed. The compounds act as prostaglandin and thromboxane antagonists and are useful in treating asthma, diarrhea, hypertension, angina, platlet aggregation, cerebral spasm, premature labor, spontaneous abortion and dysmenorrhea and as cytoprotective agents.
Tetrahydrocarbazole esters, pharmaceutical compositions and use
申请人:Merck Frosst Canada, Inc.
公开号:US04940719A1
公开(公告)日:1990-07-10
Tetrahydrocarbazole esters are disclosed. The compounds act as prostaglandin and thromboxane antagonists and are useful in treating asthma, diarrhea, hypertension, angina, platelet aggregation, cerebral spasm, premature labor, spontaneous abortion and dysmenorrhea and nephrotoxicity caused by cyclosporin A and as cytoprotective agents.
Tetrahydrocarbazoles for the improvement of cyclosporin therapy
申请人:MERCK FROSST CANADA INC.
公开号:EP0307077A1
公开(公告)日:1989-03-15
Tetrahydrocarbazoles, especially Tetrahydrocarbazole-1-alkanoic acids are disclosed. The compounds are useful for improving cyclosporine therapy. In particular, the compounds are useful for limiting cyclosporine induced nephrotoxicity which comprises the adjunct administration in a mammal of an effective amount of cyclosporine and an effective amount of the tetrahydrocarbazole 1-alkanoic acids.
Asymmetric Synthesis of a Prostaglandin D<sub>2</sub> Receptor Antagonist
作者:Kevin R. Campos、Michel Journet、Sandra Lee、Edward J. J. Grabowski、Richard D. Tillyer
DOI:10.1021/jo048305+
日期:2005.1.1
An asymmetric synthesis was developed for the production of a prostaglandinD2 receptor antagonist for the treatment of allergic rhinitis. The stereogenic center was set using asymmetric allylic alkylation chemistry, and the core of the structure was constructed via Pd-catalyzed N-cyclization/Heck methodology. The synthesis relies on a late stage indoline oxidation which does not racemize the product