C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 211/26 (2006.01) A61K 31/40 (2006.01) A61K 31/445 (2006.01) C07D 207/09 (2006.01)
Patent
CA 2273364
Compounds of formula (I) and pharmaceutically acceptable salts thereof, where G is a methylene or ethylene linkage; R1 is hydrogen, C1-6alkylO-; R2 is hydrogen, halogen, CN, N3, trifluoromethyldiazirinyl, CF3, CF3O-, CF3S-, CF3CO- , C1-6alkyl, C3-6cycloalkyl, C3-6cycloalkyl-C1-4alkyl-, C1-6alkylO-, C1- 6alkylCO-, C3-6cycloalkylCO-, C3-6cycloalkyl-C1-4-alkylCO-, phenyl, phenoxy, benzyloxy, benzoyl and substituted benzoyl, phenyl-C1-4alkyl-, C1-6alkylSO2-, (C1-4alkyl)2NSO2- or (C1-4alkyl)NHSO2-; R3 is hydrogen, halogen, CN, N3, trifluoromethyldiazirinyl, C1-6alkylO-, C1-6alkylS-, C1-6alkyl, C3- 6cycloalkyl, C3-6cycloalkyl-C1-4alkyl-, C1-6alkenyl, C1-6alkynyl, CF3CO-, C1- 6alkylCO-, C3-6cycloalkylCO-, C3-6cycloalkyl-C1-4alkylCO-, phenyl, phenoxy, benzyloxy, benzoyl, phenyl-C1-4alkyl-, or -NR5R6 where R5 is hydrogen or C1- 4alkyl; and R6 is hydrogen, C1-4alkyl, -CHO, -CO2C1-4alkyl or -COC1-4alkyl; R4 is hydrogen, C1-6alkyl, C1-6alkenyl, or C1-6alkynyl, are useful in the prevention and treatment of anxiety, mania, depression disorders associated with a subarachnoid haemorrhage or neural shock, the effects associated with withdrawal from substances of abuse such as cocaine, nicotine, alcohol and benzodiazepines, disorders treatable and/or preventable with anti-convulsive agents, such as epilepsy including post-traumatic epilepsy, Parkinson's disease, psychosis, migraine, etc.
L'invention concerne de nouveaux composés de la formule (I) et des sels pharmaceutiquement acceptables desdits composés. Dans ladite formule, G est une liaison méthylène ou éthylène; R?1¿ est hydrogène, C¿1-6?alkyleO-; R?2¿ est hydrogène, halogène, CN, N¿3?, trifluorométhyldiazirinyle, CF¿3?, CF¿3?O-, CF¿3?S-, CF¿3?CO-, C¿1-6?alkyle, C¿3-6?cycloalkyle, C¿3-6?cycloalkyle-C¿1-4?alkyle-, C¿1-6?alkyleO-, C¿1-6?alkyleCO-, C¿3-6?cycloalkyleCO-, C¿3-6?cycloalkyle-C¿1-4?-alkyleCO-, phényle, phénoxy, benzyloxy, benzoyle et benzoyle substitué, phényle-C¿1-4?alkyle-, C¿1-6?alkyleSO¿2?-, (C¿1-4?alkyle)¿2?NSO¿2?- ou (C¿1-4?alkyle)NHSO¿2?-; R?3¿ est hydrogène, halogène, CN, N¿3?, trifluorométhyldiazirinyle, C¿1-6?alkyleO-, C¿1-6?alkyleS-, C¿1-6?alkyle, C¿3-6?cycloalkyle, C¿3-6?cycloalkyle-C¿1-4?alkyle-, C¿1-6?alcényle, C¿1-6?alkynyle, CF¿3?CO-, C¿1-6?alkyleCO-, C¿3-6?cycloalkyleCO-, C¿3-6?cycloalkyle-C¿1-4?alkyleCO-, phényle, phénoxy, benzyloxy, benzoyle, phényle-C¿1-4?alkyle- ou -NR?5¿R?6¿, R?5¿ étant hydrogène ou C¿1-4?alkyle et R?6¿ étant hydrogène, C¿1-4?alkyle, -CHO, -CO¿2?C¿1-4?alkyle ou -COC¿1-4?alkyle; R?4¿ est hydrogène, C¿1-6?alkyle, C¿1-6?alcényle ou C¿1-6?alkynyle. Lesdits composés sont utiles pour la prévention et le traitement d'affections telles que: anxiété, manie, affections dépressives liées à une hémorragie sous-arachnoïdienne ou choc nerveux, effets produits par le sevrage vis-à-vis de substances donnant lieu à des abus (cocaïne, nicotine, alcool ou benzodiazépines), maladies pouvant être traitées et/ou évitées à l'aide d'agents anti-convulsion, à savoir, par exemple, épilepsie (y compris l'épilepsie post-traumatique), maladie de Parkinson, psychose, migraine, etc.
Thompson Mervyn
Vong Antonio Kuok Keong
Ward Robert William
Gowling Lafleur Henderson Llp
Smithkline Beecham P.l.c.
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