Bicyclic carboxamides as 5-ht1a antagonists

C - Chemistry – Metallurgy – 07 – D

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C07D 451/02 (2006.01) A61K 31/495 (2006.01) A61K 31/55 (2006.01) C07D 209/44 (2006.01) C07D 209/52 (2006.01) C07D 221/22 (2006.01) C07D 223/14 (2006.01) C07D 295/185 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 471/08 (2006.01) C07D 487/08 (2006.01)

Patent

CA 2200443

Bicyclic carboxamides of formula (I) and the pharmaceutically acceptable acid addition salts are 5-HT1A binding agents, particularly 5-HT1A antagonists, and may be used, for example, as anxiolytics. In the formula, X represents -CR2 = CR2- or -(CR2)q-; m represents 0, 1 or 2; n represents 0, 1 or 2; p represents 0, 1, 2 or 3, and q represents 0, 1, 2 or 3; A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups; R is a mono or bicyclic aryl or heteroaryl radical; R1 is an aryl or aryl(lower)alkyl radical; and each R2 is independently hydrogen or lower alkyl.

Ces carboxamides bicycliques de la formule (I), ainsi que leurs sels d'addition d'acide, acceptables sur le plan pharmacologique, sont des agents de liaison de 5-HT¿1A?, notamment des antagonistes de 5-HT¿1A?, et peuvent être utilisés, par exemple, en tant anxiolytiques. Dans cette formule, X représente -CR?2¿=CR?2¿- ou -(CR?2¿)¿q?-: m représente 0, 1 ou 2; n représente 0, 1 ou 2; p représente 0, 1, 2 ou 3 et q représente 0, 1, 2 ou 3; A représente une chaîne alkylène possédant 1 ou 2 atome(s) de carbone éventuellement substitué(s) par un ou plusieurs groupe(s) alkyle(s) inférieur(s); R représente un radical aryle ou hétéroaryle, mono ou bicyclique; R?1¿ représente un radical aryle ou aryle-alkyle(inférieur); et chaque R?2¿ représente indépendamment hydrogène ou alkyle inférieur.

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