4-[4(or 3)-acylaminophenyl]pyridines, their preparation and...

C - Chemistry – Metallurgy – 07 – D

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C07D 213/40 (2006.01)

Patent

CA 1161440

ABSTRACT OF THE DISCLOSURE Disclosed and claimed are a cardiac composition and a method for increasing cardiac contractility using an effective amount of a cardiotonic 4-[4-(or 3)-AcNH-phenyl]- 2-R2-3-R3-5-R5-6-R6-pyridine (I) or pharmaceutieally-accept- able salt thereof, where R2 is hydrogen, methyl, ethyl or hydroxyl, R6 is hydrogen, methyl or ethyl, R3 and R5 are each hydrogen or methyl, and Ac is hydrogen, hydroxyacetyl, acetoxyacetyl, .alpha.-hydroxypropionyl, .alpha.-acetoxypropionyl, methyoxyacetyl, 2-butenoyl or carbamyl or when NHAc is attached to the 4-position of the phenyl ring Ac also is formyl, n-propanoyl, 2,2-dimethyl-n-propanoyl or 3-car- boxypropanoyl or when NHAc is attached to the 3-position of the phenyl ring Ac also is acetyl. Novel compounds shown and claimed are 4-[4-(or 3)-Ac'NH-phenyl]-2-R2-3-R3-5-R5-6- R6-pyridines (II) or pharmaceutically-acceptable acid- addition salts thereof, where R2, R3, R5 and R6 are defined as above for I and Ac' is hydroxyacetyl, acetoxyacetyl, .alpha.- hydroxypropanoyl, .alpha.-acetoxypropionyl, methoxyaeetyl, 2- butenoyl or carbamyl or where Ac'NH is attached to the 4- position of the phenyl ring Ac' also is formyl, n-propanoyl, 2,2-dimethyl-n-propanoyl or 3-carboxypropanoyl. Also disclosed and claimed is the process for preparing said novel compounds (II).

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