4-[4(or 3)-Acylaminophenyl]pyridines and their use as cardiotoni

Details 4-[4(or 3)-Acylaminophenyl]pyridines and their use as cardiotoni 4-[4(or 3)-Acylaminophenyl]pyridines and their use as cardiotoni

1980-05-27

1982-03-02

Rotman, Alan L.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Bacterium or component thereof or substance produced by said...

546291, 546336, C07D21364, A61K 3144

Patent

active

043178278

ABSTRACT:
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-R.sub.2 -3-R.sub.3 -5-R.sub.5 -6-R.sub.6 -pyridine (I) or pharmaceutically-acceptable salt thereof, where R.sub.2 is hydrogen, methyl, ethyl or hydroxyl, R.sub.6 is hydrogen, methyl or ethyl, R.sub.3 and R.sub.5 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-carboxypropanoyl 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-R.sub.2 -3-R.sub.3 -5-R.sub.5 -6-R.sub.6 -pyridines (II) or pharmaceutically-acceptable acid-addition salts thereof, where R.sub.2, R.sub.3, R.sub.5 and R.sub.6 are defined as above for I and Ac' is hydroxyacetyl, acetoxyacetyl, .alpha.-hydroxypropanoyl, .alpha.-acetoxypropionyl, methoxyacetyl, 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).

REFERENCES:
patent: 3753993 (1973-08-01), Lesher et al.
patent: 3822278 (1974-07-01), Dufour
patent: 3907798 (1975-09-01), Lesher
patent: 4118557 (1978-10-01), Lesher
Heilbron et al., Journal of the Chemical Society, London, pp. 1279-1284, (1940).

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