Phenylaminoalkylcarboxylic acid derivatives and medicinal...

C - Chemistry – Metallurgy – 07 – C

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C07C 229/18 (2006.01) A61K 31/165 (2006.01) A61K 31/197 (2006.01) A61K 31/22 (2006.01) A61K 31/5375 (2006.01) A61P 1/00 (2006.01) A61P 3/00 (2006.01) A61P 13/00 (2006.01) A61P 25/24 (2006.01) C07C 237/06 (2006.01) C07D 295/185 (2006.01)

Patent

CA 2315235

The present invention provides novel phenylaminoalkyl--carboxylic acid derivatives represented by the general formula: (see formula I) wherein R1 represents a hydroxy group, a lower alkoxy group, an aralkoxy group, an amino group, an alicyclic amino group or a mono or di(lower alkyl)amino group which may have a hydroxy group or a lower alkoxy group as a substituent; R2 represents a hydroxy group or a lower alkyl group; R3 represents a hydrogen atom or a halogen atom; R4 and R5 are the same or different and each represents a hydrogen atom, a halogen atom or a lower alkyl group; A represents a lower alkylene group; the carbon atom marked with (R) represents a carbon atom in (R) configuration; and the carbon atom marked with (S) represents a carbon atom in (S) configuration; and pharmaceutically acceptable salts thereof, which have excellent .beta.3-adrenoceptor stimulating effects and are useful as agents for the prevention or treatment of obesity, hyperglycemia, the diseases caused by intestinal hypermotility, pollakiuria, urinary incontinence, depression, or the diseases caused by biliary calculi or hypermotility of biliary tract.

L'invention concerne de nouveaux dérivés d'acide phénylaminoalkylcarboxylique représentés par la formule générale (I) et leurs sels acceptables du point de vue pharmacologique, ces dérivés étant dotés d'un effet excellent comme stimulants du récepteur beta 3-adrénergique et s'utilisant comme agents préventifs ou médicaments contre l'obésité, l'hyperglycémie, les affections dues à des mouvements intestinaux accélérés, la pollakiurie ou l'incontinence urinaire, la dépression, la cholélithiase, les affections dues à des mouvements biliaires accélérés, etc. Dans la formule (I) selon l'invention, R<1> représente un hydroxy, un alkyle inférieur, un aralcoxy, un amino, un amino alicyclique éventuellement substitué par un hydroxy ou un alkyle inférieur, un mono- ou di-(alkyle inférieur)amino; R<2> représente un hydroxy ou un alkyle inférieur; R<3> représente un hydrogène ou un halogéno; R<4> et R<5> représentent chacun un hydrogène, un halogéno ou un alkyle inférieur; A représente un alkylène inférieur; l'atome de carbone portant la marque (R) est un atome de carbone présentant la configuration (R); et l'atome de carbone portant la marque (S) est un atome de carbone présentant la configuration (S).

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