N-arylphenylacetamide derivatives and pharmaceutical...

C - Chemistry – Metallurgy – 07 – C

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C07C 235/38 (2006.01) A61K 31/167 (2006.01) A61K 31/341 (2006.01) A61K 31/343 (2006.01) A61K 31/357 (2006.01) A61K 31/36 (2006.01) A61K 31/381 (2006.01) A61K 31/385 (2006.01) A61K 31/40 (2006.01) A61K 31/404 (2006.01) A61K 31/4164 (2006.01) A61K 31/426 (2006.01) A61K 31/4402 (2006.01) A61K 31/4406 (2006.01) A61K 31/4409 (2006.01) A61K 31/445 (2006.01) A61K 31/4453 (2006.01) A61K 31/451 (2006.01) A61K 31/47 (2006.01) A61K 31/505 (2006.01) A61K 31/5375 (2006.01) A61K 31/55 (2006.01) A61P 11/00 (2006.01) A61P

Patent

CA 2448764

N-Arylphenylacetamide derivatives represented by the following general formula (I): (I) wherein R1 represents C1-6 alkoxy, etc.; R2 represents hydrogen, - (CH2)m-N(R6)(R7) (wherein m is an integer of from 1 to 4; R6 represents hydrogen, C1-4 alkyl, etc.; and R7 represents hydrogen, etc.); R3 represents hydrogen, halogeno, etc.; R4 represents C6-10 alkyl, -Y-R8 (wherein Y represents a single bond, C1-6 alkylene, C2-6 alkenylene, C2-6 alkynylene, etc.; and R8 represents aryl, C3-8 cycloalkyl, C6-15 polyccyloalkyl, etc.), etc.; R5 represents hydrogen, etc.; and X1 represents hydrogen; or physiologically acceptable salts thereof or hydrates or solvates of the same; and medicinal compositions containing the same. These compounds are useful as preventives and/or remedies which give no pain at the early stage of administration, are efficacious in oral administration and have potent analgesic and antiinflammtory effects, etc.

L'invention concerne des dérivés de N-arlyphénylacétamide représentés par la formule générale (I) ou leurs sels physiologiquement acceptables ou leurs hydrates ou leur solvates. Dans cette formule R?1¿ représente alcoxy C¿1-6?, etc. ; R?2¿ représente hydrogène, - (CH¿2?)¿m?-N(R?6¿)(R?7¿), où m représente un entier de 1 à 4 ; R?6¿ représente hydrogène, alkyle C¿1-4?, etc. ; et R?7¿ représente hydrogène, etc.) ; R?3¿ représente hydrogène, halogéno, etc. ; R?4¿ représente alkyle C¿6-10?, -Y-R?8¿, (où Y représente une liaison simple, alkylène C¿1-6?, alcénylène C¿2-6?, alkynylène C¿2-6?, etc. ; et R?8¿ représente aryle, cycloalkyle C¿3-8?, polycycloalkyle C¿6-15?, etc.), etc. ; R?5¿ représente hydrogène, etc. ; et X?1¿ représente hydrogène. L'invention concerne également des compositions médicinales contenant lesdits dérivés. Les composés selon l'invention conviennent comme prophylactiques et/ou comme remèdes qui ne sont pas accompagnés de douleurs à un stade précoce d'administration. En outre, ces composés sont efficacement administrés par voie orale et ils ont de puissants effets analgésiques et anti-inflammatoires, etc.

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