Global patent index - EP 0968190 A1

EP 0968190 A1 2000-01-05 - SUBSTITUTED ISOQUINOLINE DERIVATIVES AND THEIR USE AS ANTICONVULSANTS

Title (en)

SUBSTITUTED ISOQUINOLINE DERIVATIVES AND THEIR USE AS ANTICONVULSANTS

Title (de)

SUBSTITUIERTE ISOCHINOLINE DERIVATE UND IHRE VERWENDUNG ALS ANTICONVULSIVA

Title (fr)

DERIVES D'ISOQUINOLINE SUBSTITUEE ET LEUR UTILISATION EN TANT QU'ANTICONVULSIVANTS

Publication

EP 0968190 A1 (EN)

Application

EP 98909647 A

Priority

  • GB 9800782 W
  • GB 9705619 A
  • GB 9726695 A

Abstract (en)

[origin: WO9841508A1] Compounds of formula (I) and pharmaceutically acceptable salts thereof; where Q is a monocyclic or bicyclic aryl or heteroaryl ring, R<1> is hydrogen, C1-6alkyl (optionally substituted by hydroxy or C1-4alkoxy), C1-6alkenyl, C1-6alkynyl, C1-6alkylCO-, formyl, CF3CO- or C1-6alkylSO2-, R<2> is hydrogen or up to three substituents selected from halogen, NO2, CN, N3, CF3O-, CF3S-, CF3CO-, trifluoromethyldiazirinyl, C1-6alkyl, C1-6alkenyl, C1-6alkynyl, C1-6perfluoroalkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl-, C1-6alkylO-, C1-6alkylCO-, C3-6cycloalkylO-, C3-6cycloalkylCO-, C3-6cycloalkyl-C1-4alkylO-, C3-6cycloalkyl-C1-4alkylCO-, phenyl, phenoxy, benzyloxy, benzoyl, phenyl-C1-4alkyl-, C1-6alkylS-, C1-6alkylSO2-, (C1-4alkyl)2NSO2-, (C1-4alkyl)NHSO2-, (C1-4alkyl)2NCO-, (C1-4alkyl)NHCO- or CONH2; or -NR<3>R<4> where R<3> is hydroven or C1-4alkyl, and R<4> is hydrogen, C1-4alkyl, formyl, -CO2C1-4alkyl or -COC1-4alkyl; or two R<2> groups together form a carbocyclic ring that is saturated or unsaturated and unsubstituted or substituted by -OH or =O; and X is hydrogen, halogen, C1-6alkoxy, C1-6alkyl, amino or trifluoroacetylamino, but when X is hydrogen excluding compounds in which R<2> is 2-alkoxy and when X is hydrogen excluding the compounds N-(7-iodo-2-methyl-1,2,3,4-tetrahydroisoquinolin-5-yl) -5-benzoyl-2-methoxybenzamide, N-(7-iodo-1,2,3,4-tetrahydroisoquinolin-5-yl) -5-benzoyl-2-methoxybenzamide, N-(5-iodo-1,2,3,4-tetrahydroisoquinolin-7-yl) -5-benzoyl-2-methoxybenzamide, N-(5-iodo-1,2,3,4-tetrahydroisoquinolin-7-yl) -2-methoxy-4-trifluoromethyldiazirinylbenzamide, N-(5-iodo-1,2,3,4-tetrahydroisoquinolin-7-yl) -2-methoxy-5-trifluoromethyldiazirinylbenzamide, N-(7-iodo-1,2,3,4,-tetrahydroisoquinolin-5-yl) -2-methoxy-5-trifluoromethyldiazirinylbenzamide et N-(8-fluoro-2-methyl-1,2,3,4-tetrahydroisoquinolin-5-yl) -4-t-butyl-2-methoxybenzamide, are useful inter alia in the treatment and prophylaxis of epilepsy.

IPC 1-7 (main, further and additional classification)

C07D 217/04; A61K 31/47; C07D 217/02; C07D 217/06; C07D 401/12; C07D 405/12; C07D 409/12; C07D 413/12; C07D 417/12

IPC 8 full level (invention and additional information)

A61P 25/04 (2006.01); A61K 31/472 (2006.01); A61K 31/4725 (2006.01); A61P 3/10 (2006.01); A61P 21/00 (2006.01); A61P 21/02 (2006.01); A61P 25/06 (2006.01); A61P 25/08 (2006.01); A61P 25/16 (2006.01); A61P 25/18 (2006.01); A61P 25/20 (2006.01); A61P 25/22 (2006.01); A61P 25/24 (2006.01); A61P 25/28 (2006.01); A61P 25/30 (2006.01); C07D 217/02 (2006.01); C07D 217/04 (2006.01); C07D 217/06 (2006.01); C07D 401/12 (2006.01); C07D 405/12 (2006.01); C07D 409/12 (2006.01); C07D 413/12 (2006.01); C07D 417/12 (2006.01)

CPC (invention and additional information)

C07D 401/12 (2013.01); C07D 217/02 (2013.01); C07D 217/04 (2013.01); C07D 217/06 (2013.01); C07D 405/12 (2013.01); C07D 409/12 (2013.01); C07D 413/12 (2013.01); C07D 417/12 (2013.01)

Citation (search report)

See references of WO 9841508A1

Designated contracting state (EPC)

AT BE CH DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE

EPO simple patent family

WO 9841508 A1 19980924; AR 012092 A1 20000927; AU 6412898 A 19981012; AU 737955 B2 20010906; BR 9809047 A 20000801; CA 2284218 A1 19980924; CN 1183116 C 20050105; CN 1255124 A 20000531; CO 4950553 A1 20000901; EP 0968190 A1 20000105; IL 131756 D0 20010319; JP 2001515504 A 20010918; JP 3690423 B2 20050831; NO 314081 B1 20030127; NO 994510 A 19990917; NO 994510 D0 19990917; NZ 337424 A 20010831; PL 192116 B1 20060831; PL 335676 A1 20000508; TR 9902283 T2 19991221; TW 555694 B 20031001

INPADOC legal status

2008-03-26 [18D] DEEMED TO BE WITHDRAWN

- Effective date: 20071002

2007-11-02 [REG HK WD] APPLICATIONS WITHDRAWN, DEEMED TO BE WITHDRAWN, OR REFUSED AFTER PUBLICATION IN HONG KONG

- Ref Country Code: HK

- Ref Legal Event Code: WD

- Ref Document Number: 1024697

- Country of Ref Document: HK

2002-09-04 [RAP1] TRANSFER OF RIGHTS OF AN EP APPLICATION

- Owner name: SMITHKLINE BEECHAM PLC

2002-03-06 [17Q] FIRST EXAMINATION REPORT

- Effective date: 20020122

2000-01-05 [17P] REQUEST FOR EXAMINATION FILED

- Effective date: 19990824

2000-01-05 [AK] DESIGNATED CONTRACTING STATES:

- Kind Code of Ref Document: A1

- Designated State(s): AT BE CH DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE

2000-01-05 [AX] REQUEST FOR EXTENSION OF THE EUROPEAN PATENT TO

- Free Format Text: SI PAYMENT 19990824