Benzamide compounds and pharmaceutical use thereof

Details Benzamide compounds and pharmaceutical use thereof Benzamide compounds and pharmaceutical use thereof

C - Chemistry, Metallurgy

07

D

C07D 471/04 (2006.01) A61K 31/395 (2006.01) C07D 213/75 (2006.01) C07D 213/82 (2006.01) C07D 215/42 (2006.01) C07D 239/28 (2006.01) C07D 239/42 (2006.01) C07D 239/48 (2006.01) C07D 401/12 (2006.01) C07D 413/12 (2006.01) C07D 417/12 (2006.01) C07D 473/34 (2006.01) C07D 487/04 (2006.01) C07D 491/048 (2006.01) C07D 495/04 (2006.01) C07D 498/04 (2006.01) C07D 513/04 (2006.01)

Patent

CA 2188164

Benzamide compounds of the formula (see formula I)~ wherein each symbol is as defined in the specification, isomers thereof and pharmaceutically acceptable acid addition salts thereof. Pharmaceutical compositions comprising a therapeutically effective amount of this compound and a pharmaceutically acceptable additive, and therapeutic agents for hypertension, therapeutic agents for angina pectoris, therapeutic agent for asthma, therapeutic agents for renal and peripheral circulatory disturbances and inhibitor of cerebral vasospasm, which comprise this compound. The compound of the present invention has strong smooth muscle relaxing action, and shows hypotensive action and cerebral .cndot. coronary vasodilating action like conventional calcium antagonists, as well as long-lasting renal and peripheral circulation improving action. Unlike calcium antagonists, it permits oral administration to suppress vascular contraction caused by various agonists, and is useful as a strong and long-acting agent for prophylaxis and treatment of circulatory diseases in coronary, cerebral, renal and peripheral arteries, as a therapeutic agent for hypertension, angina pectoris, and renal and peripheral circulation disorder, an inhibitor of cerebral vasospasm and the like. Moreover, the compound of the present invention is useful as a therapeutic agent for asthma.

Composé benzamide de formule générale (I) (dans laquelle chaque symbole est tel que défini dans la demande), isomère ou sel d'addition acide pharmaceutiquement acceptable, composition médicale comprenant une dose thérapeutiquement efficace du composé et des excipients pharmaceutiquement acceptables, et remèdes pour l'hypertension, l'angine de poitrine, l'asthme, et des troubles de la circulation périphérique et rénale, ainsi que suppresseur des spasmes vasculaires cérébraux, contenant tous ledit composé. Ce composé a un puissant effet relaxant des muscles lisses et, à l'instar des antagonistes traditionnels du calcium, un effet hypotenseur et un effet vasodilatateur coronaire et cérébral. De plus, il présente un effet améliorant de manière persistante la circulation périphérique et rénale et, au contraire des antagonistes du calcium, un effet inhibiteur de la vasoconstriction causée par divers agonistes. Il est en outre administrable par voie orale. Il est par conséquent utile pour prévenir ou soigner des maladies des organes de la circulation, dont les artères coronaires, cérébrales, rénales et périphériques, par exemple, pour soigner l'hypertension, l'angine de poitrine et les troubles de la circulation périphérique et rénale et il est également un suppresseur des spasmes vasculaires cérébraux. Il est en outre utile comme remède contre l'asthme.

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