[EN] NOVEL INDOL CARBOXYLIC ACID BISPYRIDYL CARBOXAMIDE DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD AND COMPOSITION CONTAINING THE SAME AS AN ACTIVE INGREDIENT [FR] NOUVEAUX DÉRIVÉS DE BISPYRIDYL CARBOXAMIDE D'ACIDE INDOLE CARBOXYLIQUE, LEURS SELS PHARMACEUTIQUEMENT ACCEPTABLES, PROCÉDÉ DE PRÉPARATION ET COMPOSITION LES CONTENANT EN TANT D'INGRÉDIENT ACTIF
NOVEL INDOL CARBOXYLIC ACID BISPYRIDYL CARBOXAMIDE DERIVATIVES, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD AND COMPOSITION CONTAINING THE SAME AS AN ACTIVE INGREDIENT
Pyrrolopyrrolone derivatives as inhibitors of neutrophil elastase
申请人:Glaxo Wellcome Inc.
公开号:US05994344A1
公开(公告)日:1999-11-30
There are described according to the invention compounds of formula (I) (relative stereochemistry indicated), wherein R.sub.1, R.sub.2, R.sub.3 and X are as defined in the specification, together with processes for preparing them, compositions containing them and their use as pharmaceuticals. Compounds of formula (I) are indicated inter alia for the treatment of chronic bronchitis.
申请人:KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
公开号:EP2108649B1
公开(公告)日:2013-04-24
Synthesis and structure–activity relationship of 1H-indole-3-carboxylic acid pyridine-3-ylamides: A novel series of 5-HT2C receptor antagonists
作者:Chul Min Park、So Young Kim、Woo Kyu Park、No Sang Park、Churl Min Seong
DOI:10.1016/j.bmcl.2008.06.064
日期:2008.7
A novel series of 1H-indole-3-carboxylic acid pyridine-3-ylamides were synthesized and identified to show high affinity and selectivity for 5-HT2C receptor. Among them, 1H-indole-3-carboxylic acid[6-(2chloro-pyridin-3-yloxy)-pyridin-3-yl]-amide (15k) exhibits the highest affinity (IC50 = 0.5 nM) with an excellent selectivity (>2000 times) over other serotonin (5-HT1A, 5-HT2A, and 5-HT6) and dopamine (D-2-D-4) receptors. (C) 2008 Elsevier Ltd. All rights reserved.
PYRROLOPYRROLONE DERIVATIVES AS INHIBITORS OF NEUTROPHIL ELASTASE