C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 233/84 (2006.01) A61K 31/41 (2006.01) A61K 31/44 (2006.01) A61K 31/495 (2006.01) A61K 31/535 (2006.01) C07C 209/42 (2006.01) C07C 211/42 (2006.01) C07C 213/02 (2006.01) C07C 215/64 (2006.01) C07C 217/74 (2006.01) C07D 233/28 (2006.01) C07D 233/32 (2006.01) C07D 233/36 (2006.01) C07D 233/42 (2006.01) C07D 233/88 (2006.01) C07D 249/12 (2006.01) C07D 401/02 (2006.01) C07D 403/02 (2006.01) C07D 403/04 (2006.01) C07D 403/10 (2006.01) C07D 405/02 (2006.01) C07D 405/12 (2006.01) C07D 409/02 (2006.01) C07D 413
Patent
CA 2188748
The present invention relates to novel benzocycloalkylazolethione compounds of formula (I) in which n is 0, 1 or 2; t is 0, 1, 2 or 3; R1 is independently halo, hydroxy or (C1-4)alkyloxy; and R2 is attached to the .alpha., .beta. or .gamma.-position and is a group selected from formulae (a), (b) and (c) which are dopamine .beta.-hydroxylase inhibitors in which the benzocycloalkyl portion of the compound is selected from indanyl, 1,2,3,4- tetrahydronaphthalenyl and 6,7,8,9-tetrahydro-5H-benzocycloheptenyl (in which the benzo is optionally substituted with one to three substituents) and the azolethione portion of the compound is selected from 2-thioxo-2,3-dihydro-1H- imidazol-3-yl, 5-thioxo-4,5-dihydro-1H-[1,2,4]triazol-4-yl and 5-thioxo-4,5- dihydro-1H-[1,2,4]triazol-1-yl (each optionally substituted with one to three substituents); and the prodrugs, pharmaceutically acceptable salts, individual isomers and mixtures of isomers and the methods of using and preparing such benzocycloalkylazolethione compounds.
1a présente invention concerne de nouveaux composés des benzocycloalkylazoléthiones de formule (I) dans laquelle n vaut 0, 1 ou 2; t vaut 0, 1, 2, ou 3; R?1¿ représente, de manière indépendante, halo, hydroxy ou alkyloxy C¿1-4?; et R?2¿ est lié en position .alpha., .beta. ou .gamma. et représente un groupe choisi parmi les formules (a), (b), (c), qui sont des inhibiteurs de la dopamine .beta.-hydroxylase dans lesquels la partie benzocycloalkyle du composé est choisie parmi l'indanyle, le 1,2,3,4,-tétrahydronaphtyalényle et le 6,7,8,9-tétrahydro-5H-benzocycloheptényle (dans lequel le benzo est éventuellement substitué par un à trois substituants), et la partie azoléthione du composé est choisie parmi le 2-thioxo-2,3-dihydro-1H-imidazole-3-yle, le 5-thioxo-4,5-dihydro-1H-[1,2,4]triazole-4-yle et le 5-thioxo-4,5-dihydro-1H-[1,2,4]triazole-1-yle (chacun étant éventuellement substitué par un à trois substituants). L'invention concerne également les précurseurs de médicaments, les sels pharmaceutiquement acceptables, les isomères isolés ou en mélange, et les procédés d'utilisation et de préparation de tels composés des benzocycloalkylazoléthiones.
Bansal Rekha P.
Gooding Owen W.
Martinez Gregory R.
Muehldorf Alexander V.
O'yang Counde
Dennison Associates
Syntex (u.s.a.) Inc.
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