Process for the preparation of substituted...

C - Chemistry – Metallurgy – 07 – D

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260/251, 260/266

C07D 271/04 (2006.01) C07D 295/28 (2006.01) C07D 413/00 (2006.01)

Patent

CA 1127642

ABSTRACT OF THE DISCLOSURE Substituted 3-amino-sydnone-imines having the general formula: Image (I) and pharmacologically acceptable acid addition salts thereof, wherein R1 denotes hydrogen or halogen, R2 denotes hydrogen, -NO or a -COR3 or -SO2R4 group, R3 denotes hydrogen, an aliphatic radical, a cycloaliphatic radical, an aryl radical, an araliphatic radical, an alkoxy radical, an aryloxy radical, a five-membered or six-membered hetero-aromatic radical or an alkoxycarbonyl radical, A denotes the group Image , in which m is 0, 1 or 2, or the group Image , R4 and R5 independently of one another denote an aliphatic radical, an aryl radical, or a dialkylamino group, are prepared by optionally cyclising a compound of the general formula II Image (II) to give a compound of the general formula Ia, which can also be present in the form of an acid addition salt, Image (Ia) and optionally, a.) acylating the resulting compound Ia or its acid addition salt with acylating agents introducing the radical -COR3 or -SO2R4 or nitrosating the resulting compound Ia or its acid addition salt, and/or optionally b.) halogenating the resulting compound Ia or its acid addition salt with halogen or halogenating agents whereby the optional steps a.) and b.) are carried out in any order, and the compound thus obtained is optionally converted to the acid addition salt. The novel compounds and their salts have beneficial and improved effects on the cardio-vascular system, for example, by lowering blood pressure, the pulmonary artery pressure and the left vertricular enddiastolic pressure, thus reducing the cardiac work in the sense of an anti-anginal action without provoking refluxtachycardia.

357074

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