[EN] SACCHARIN DERIVATIVES AS ORALLY ACTIVE ELASTASE INHIBITORS<br/>[FR] DERIVES DE SACCHARINE SERVANT D'INHIBITEURS D'ELASTASE ORALEMENT ACTIFS
申请人:SANOFI SYNTHELABO
公开号:WO2001044245A1
公开(公告)日:2001-06-21
Orally active compounds of general formula (I) wherein R1 is methyl, ethyl or 2-morpholino-ethyl group, R2 is piperidino, morpholino or 4-methyl-piperazinyl group, n is 2 or 3 and their salts, solvates and hydrates.
[EN] NOVEL ADENOSINE DERIVATIVES, PREPARATION METHODS THEREFOR, AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME<br/>[FR] NOUVEAUX DERIVES DE L'ADENOSINE, LEURS PROCEDES DE PREPARATION, COMPOSITIONS PHARMACEUTIQUES LES CONTENANT
申请人:LABORATOIRES UPSA
公开号:WO1995018817A1
公开(公告)日:1995-07-13
(EN) Derivatives of formula (I), addition salts thereof, and the therapeutical use thereof as pain killers, antihypertensive agents and drugs having antiproliferative properties, are disclosed.(FR) La présente invention concerne les dérivés de formule (I), ainsi que leurs sels d'addition et leur utilisation en thérapeutique comme antalgique, comme antihypertenseur et comme médicaments à propriétés antiprolifératives.
SACCHARIN DERIVATIVES AS ORALLY ACTIVE ELASTASE INHIBITORS
申请人:——
公开号:US20030114449A1
公开(公告)日:2003-06-19
Orally active compounds of general formula (I) wherein R
1
is methyl, ethyl or 2-morpholino-ethyl group, R
2
is piperidino, morpholino or 4-methyl-piperazinyl group, n is 2 or 3 and their salts, solvates and hydrates.
Human leukocyte elastase (HLE) is a serine proteinase, capable of degrading a variety of structural matrix proteins. SSR69071 2[(4-isoprop);1-6-methoxy-1,1-dioxido-3-oxo-1,2-benzisothiazol-2(3H)-yl)methoxy]-9-(2-piperidin-1-ylethoxy)-4H-pyrido[1,2-a]pyri- midin-4-one was selected as a novel orally active HLE inhibitor for treatment of chronic obstructive pulmonary diseases, asthma, emphysema, cystic fibrosis and several inflammatory diseases (WO 01/44245 Al) (J. Pharm. Exp. Ther., submitted for publication). (C) 2003 Editions scientifiques et medicales Elsevier SAS. All rights reserved.