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1. (WO2003000253) SUBSTITUTED INDOLE ACID DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR-1 (PAI-1)
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2003/000253    International Application No.:    PCT/US2002/019344
Publication Date: 03.01.2003 International Filing Date: 18.06.2002
Chapter 2 Demand Filed:    12.12.2002    
IPC:
C07D 209/12 (2006.01)
Applicants: WYETH [US/US]; Five Giralda Farms, Madison, NJ 07940-0874 (US)
Inventors: ELOKDAH, Hassan, Mahmoud; (US).
MCFARLANE, Geraldine, Ruth; (US).
LI, David, Zenan; (US).
JENNINGS, Lee, Dalton; (US).
CRANDALL, David, Leroy; (US)
Agent: NAGY, Michael, R.; Wyeth, Patent Law Department, Five Giralda Farms, Madison, NJ 07940-0874 (US).
WILEMAN, David Françis, CONNELLY Michael John MANNION, Sally Kim; and TALBOTT, Dawn Jacqueline; c/o WyETH Pharmaceuticals, Huntercombe Lane South, Taplow, Maidenhead, Berkshire SL6 OPH, United Kingdom (GB)
Priority Data:
60/299,657 20.06.2001 US
Title (EN) SUBSTITUTED INDOLE ACID DERIVATIVES AS INHIBITORS OF PLASMINOGEN ACTIVATOR INHIBITOR-1 (PAI-1)
(FR) DERIVES D'ACIDE INDOLE SUBSTITUE UTILISES EN TANT QU'INHIBITEURS DE L'INHIBITEUR-1 (PAI-1) DE L'ACTIVATEUR PLASMINOGENE
Abstract: front page image
(EN)This invention provides compounds of the formula : (I) wherein: X is a chemical bond, -CH2- or -C(O)-; R1 is alkyl, cycloalkyl, -CH2-cycloalkyl, pyridinyl, -CH2-pyridinyl, phenyl or benzyl; R2 is H, alkyl, cycloalkyl, -CH2-cycloalkyl, or perfluoroalkyl; R3 is H, halo, alkyl, perfluoroalkyl, alkoxy, cycloalkyl, -CH2-cycloalkyl, -NH2, or -NO2; R4 is optionally substituted phenyl, benzyl, benzyloxy, pyridinyl, or -CH2-pyridinyl, or the salt or ester forms thereof, as well as methods for using the compounds as inhibitors of plasminogen activator inhibitor-1 (PAI-1) and as therapeutic compositions for treating conditions resulting from fibrinolytic disorders such as deep vein thrombosis and coronary heart disease, and pulmonary fibrosis, and processes for their preparation.
(FR)L'invention concerne des composés représentés par la formule (I) dans laquelle X est une liaison chimique, -CH2- ou -C(O)-; R1 est alkyle, cykloalkyle, -CH2-cycloalkyl, pyridinyl, -CH2-pyridinyl, phényl or benzyl; R2 est H, alkyle, cycloalkyle, -CH2-cycloalkyle, ou perfluoroalkyle; R3 est H, halo, alkyle, perfluoroalkyl, alkoxy, cycloalkyle, -CH2-cycloalkyle, -NH2, ou -NO2; R4 est phényle, benzyl, benzyloxy, pyridinyle facultativement substitués , ou-CH2-pyridinyl, ou les formes de sel ou d'ester de ces composés, ainsi que des procédés d'utilisation de ces composés en tant qu'inhibiteurs de l'inhibiteur-1 (PAI-1) et des compositions pharmaceutiques utilisées dans le traitement des conditions liées à des troubles fibrinolytiques tels que les thromboses veineuses profondes, les maladies coronariennes, les fibroses pulmonaires, et des procédés de préparation correspondant.
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NO, NZ, OM, PH, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TN, TR, TT, TZ, UA, UG, UZ, VN, YU, ZA, ZM, ZW.
African Regional Intellectual Property Organization (GH, GM, KE, LS, MW, MZ, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)