This invention provides substituted indole compounds of the general formula:
1
and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A
2
enzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.
Production method for optically active N-aryl-beta-amino acid compounds
申请人:Ajinomoto Co., Inc.
公开号:EP1471050A1
公开(公告)日:2004-10-27
In a method suitable for industrial application, an optically active N-aryl-β-amino acid compound is produced by the reaction of an aromatic amine and an optically active sulfonylated β-hydroxycarboxylic acid compound. The latter can be easily derived from a β-keto carboxylic acid compound.
Methods for the use of inhibitors of cytosolic phospholipase A2 in the treatment of thrombosis
申请人:Clerin Valerie
公开号:US20080009485A1
公开(公告)日:2008-01-10
This invention provides methods for the use of substituted indole compounds of the general formula:
and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds in the treating or preventing thrombosis in a mammal, or preventing progression of symptoms of thrombosis.
Isoxazole-sulfonamide endothelin antagonists of formula (I) below having good affinity for endothelin receptors and selectivity for ET
A
over ET
B
are described herein.
1
Such compounds are useful in the treatment of conditions mediated by endothelin, in particular, conditions mediated by endothelin ET
A
.
[EN] THIENYL-, FURYL-, PYRROLYL- AND BIPHENYLSULFONAMIDES AND DERIVATIVES THEREOF THAT MODULATE THE ACTIVITY OF ENDOTHELIN<br/>[FR] THIENYL-, FURYL-, PYRROLYL- ET BIPHENYL SULFONAMIDES ET LEURS DERIVES MODULANT L'ACTIVITE DE L'ENDOTHELINE
申请人:TEXAS BIOTECHNOLOGY CORPORATION
公开号:WO1996031492A1
公开(公告)日:1996-10-10
(EN) Thienyl-, furyl- and pyrrolyl-sulfonamides and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)-furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit or increase the activity of endothelin are also provided.(FR) Thiényl-, furyl- et pyrrolyl-sulfonamides et procédés de modulation ou d'altération de l'activité de la famille endothéline des peptides. L'invention porte en particulier sur des N-(isoxazolyl)thiényl sulfonamides, N-(isoxazolyl)-furyl sulfonamides et N-(isoxazolyl)pyrrolyl sulfonamides et sur des procédés mettant en oeuvre de tels sulfonamides pour inhiber la liaison d'un peptide d'entholéline à un récepteur d'endothéline en soumettant ce récepteur au contact du sulfonamide. L'invention porte également sur des méthodes de traitement des affections à médiation par l'endothéline par administration de quantités efficaces d'un ou plusieurs de ces sulfonamides ou de promédicaments issus de ces sulfonamides inhibant ou accroissant l'activité de l'endothéline.