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1. (WO2005030199) 4-(1-BENZOFURAN-3-YL-METHYLIDENEAMINOXY.PROPOXY))-BENZOIC ACID DERIVATIVES AND RELATED COMPOUNDS AS PAI-1 INHIBITORS FOR THE TREATMENT OF IMPAIRMENT OF THE FIBRINOLYTIC SYSTEM AND OF THROMBOSIS
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2005/030199    International Application No.:    PCT/US2004/031361
Publication Date: 07.04.2005 International Filing Date: 24.09.2004
IPC:
C07D 307/81 (2006.01)
Applicants: WYETH [US/US]; Five Giralda Farms, Madison, NJ 07940 (US) (For All Designated States Except US).
HAVRAN, Lisa, Marie [US/US]; (US) (For US Only).
BUTERA, John, Anthony [US/US]; (US) (For US Only).
ELOKDAH, Hassan, Mahmoud [US/US]; (US) (For US Only).
JENKINS, Douglas, John [US/US]; (US) (For US Only).
GUNDERSEN, Eric, Gould [US/US]; (US) (For US Only)
Inventors: HAVRAN, Lisa, Marie; (US).
BUTERA, John, Anthony; (US).
ELOKDAH, Hassan, Mahmoud; (US).
JENKINS, Douglas, John; (US).
GUNDERSEN, Eric, Gould; (US)
Agent: LUCCI, Joseph; Woodcock Washburn LLP, One Liberty Place, 46th Floor, Philadelphia, PA 19103 (US)
Priority Data:
60/505,801 25.09.2003 US
10/947,930 23.09.2004 US
Title (EN) 4-(1-BENZOFURAN-3-YL-METHYLIDENEAMINOXY.PROPOXY))-BENZOIC ACID DERIVATIVES AND RELATED COMPOUNDS AS PAI-1 INHIBITORS FOR THE TREATMENT OF IMPAIRMENT OF THE FIBRINOLYTIC SYSTEM AND OF THROMBOSIS
(FR) DERIVES DE L'ACIDE 4-(1-BENZOFURAN-3-YL-METHYLIDENEAMINOXY-PROPOXY))-BENZOIQUE ET COMPOSES APPARENTES UTILISES COMME INHIBITEURS DE PAI-1 POUR LE TRAITEMENT D'UNE DEFICIENCE DU SYSTEME FIBRINOLYTIQUE ET DE LA THROMBOSE
Abstract: front page image
(EN)The present invention relates to benzofuryl-oximes of formula (I) or a pharmaceutically acceptable salt or ester form thereof wherein R1 is a direct bond to A, C1-C4 alkylene, or -O-C1-C4 alkylene; R2 and R3 are, independently hydrogen, halogen, C1-C4 alkyl, C1-C3 perfluoroalkyl, -O-C1-C3 perfluoroalkyl, C1-C3 alkoxy, -OH, -NH2, -NO2, -O(CH2)p-aryl, -O(CH2)P-heteroaryl, aryl, heteroaryl, -NH(CH2)P-aryl, -NH(CH2)P-heteroaryl, -NH(CO)-aryl, NH(CO)-heteroaryl, -O(CO)-aryl, O(CO)-heteroaryl, -NH(CO)-CH=CH-aryl, or -NH(CO)-CH=CH-heteroaryl; p is an integer from 0-6; R4 is hydrogen, C1-C8 alkyl, or C3-C6 cycloalkyl; A is -COOH or an acid mimic; X is C1-C8 alkylène, C3-C6 cycloalkylene, -(CH2)mO-, or -(CH2)mNH-; m is an integer from 1-6; and R5 is hydrogen, C1-C8 alkyl, C3-C6 alkyl, C3-C6 cycloalkyl, -CH2-C3-C6 cycloalkyl, heteroaryl, -CH2-heteroaryl, aryl or benzyl; R6 and R7 are independently, hydrogen, halogen, C1-C6 alkyl, C1-C6 perfluoroalkyl, -O-C1-C6 perfluoroalkyl, C1-C6 alkoxy, _OH, -NH2, -NO2, -O(CH2)n-aryl, -O(CH2)n-heteroaryl, aryl, or heteroaryl; and n is an integer from 0-6, wherein the alkyl, cycloalkyl, aryl and heteroaryl groups are each optionally substituted by one or more substituents. The present compounds are PAI-1 inhibitors for the treatment e.g of impairment of the fibrinolytic system, thrombosis or cardiovascular diseases.
(FR)La présente invention concerne des benzofuryl-oximes de formule (I) ou un sel pharmaceutiquement acceptable ou une forme estérique desdits composés. Dans ladite formule, R1 est directement lié à A, alkylène C1-C4 ou alkylène -O-C1-C4; R2 et R3 sont, indépendamment, hydrogène, halogène, alkyle C1-C4, perfluoroalkyle C1-C3 perfluoroalkyle, perfluoroalkyle -O-C1-C3, alcoxy C1-C3, OH, -NH2, -NO2, -O(CH2)p-aryle, -O(CH2)P-hétéroaryle, aryle, hétéroaryle, -NH(CH2)P-aryle, -NH(CH2)P-hétéroaryle, -NH(CO)-aryle, NH(CO)-hétéroaryle, -O(CO)-aryle, O(CO)-hétéroaryle, -NH(CO)-CH=CH-aryle ou -NH(CO)-CH=CH-hétéroaryle; p est un entier compris entre 0 et 6; R4 est hydrogène, alkyle C1-C8 ou cycloalkyle C3-C6; A est -COOH ou un analogue de l'acide; X est alkylène C1-C8, cycloalkylène C3-C6, -(CH2)mO- ou -CH2)mNH-; m est un entier compris entre 0 et 6; et R5 est hydrogène, alkyle C1-C8, alkyle C3-C6, cycloalkyle C3-C6, cycloalkyle -CH2-C3-C6, hétéroaryle, -CH2-hétéroaryle, aryle ou benzyle; R6 et R7 sont, indépendamment, hydrogène, halogène, alkyle C1-C6, perfluoroalkyle C1-C6, perfluoroalkyle -O-C1-C6, alcoxy C1-C6, -OH, -NH2, -NO2, -O(CH2)n-aryle, -O(CH2)n-hétéroaryle, aryle ou hétéroaryle; et n est un entier compris entre 0 et 6; les groupes alkyle, cycloalkyle, aryle et hétéroaryle étant chacun éventuellement susbstitués par un ou plusieurs susbstituants. Les composés de l'invention sont des inhibiteurs de PAI-1 destinés au traitement, par exemple, d'une déficience du système fibrinolytique, de la thrombose ou de maladies cardiovasculaire.
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, 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, NA, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IT, LU, MC, NL, PL, PT, RO, SE, SI, SK, 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)