Quinoline derivatives which are 5-hydroxytryptamine antagonists

Details Quinoline derivatives which are 5-hydroxytryptamine antagonists Quinoline derivatives which are 5-hydroxytryptamine antagonists

1982-05-26

1984-03-06

Daus, Donald G.

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

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

546157, 546167, 546173, 546180, A61K 3147, C07D21536

Patent

active

044354053

ABSTRACT:
Compounds of the formula: ##STR1## wherein A stands for the radical --(CH.sub.2).sub.2 -- which may bear one or two defined substituents; R.sup.1 stands for a (3-4C) alkyl or cyclopropyl radical, or a phenyl radical which may optionally bear one or two defined substituents, or a heteroaryl radical of five or six ring atoms which may optionally bear a (1-3C)alkyl substituent; R.sup.2 and R.sup.3 stand for hydrogen or a (1-2C)alkyl radical, or R.sup.2 stands for a (2-4C)alkylene radical which is linked to one of the carbon atoms forming the two-carbon-atom-backbone of A so as to form, together with the adjacent nitrogen atom, a pyrrolidinyl or piperidyl radical; and one of R.sup.4 and R.sup.5 stands for hydrogen, and the other stands for hydrogen, a halogen atom or a (1-3C)alkyl or (1-3C)alkoxy radical; and acid-addition salts thereof. Processes for the manufacture of said compounds. Pharmaceutical compositions comprising one of said compounds and a pharmaceutical diluent or carrier. The compounds are 5-hydroxytryptamine antagonists.

REFERENCES:
patent: Re16394 (1926-07-01), Callsen
patent: 1572768 (1926-02-01), Callsen
patent: 1860286 (1932-05-01), Hartmann et al.
patent: 4343805 (1982-08-01), Crossley et al.
Zayed et al., Chemical Abstracts, vol. 89, 215199v (1978).
Gilman et al., J. Am. Chem. Soc., vol. 71, pp. 3667-3668 (1949).
Westland et al., J. Med. Chem., vol. 16(4), pp. 328-331 (1973).
Zayed et al., Pharmazie, 33, No. 9, pp. 572-575 (1978).

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