4(5)-substituted imidazole derivatives as .alpha..sub.2 -adrener

Details 4(5)-substituted imidazole derivatives as .alpha..sub.2 -adrener 4(5)-substituted imidazole derivatives as .alpha..sub.2 -adrener

1987-05-14

1990-06-12

Schwartz, Richard A.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514400, 548342, 548346, A61K 31415, C07D23364, C07D23358

Patent

active

049333593

ABSTRACT:
The invention provides 4(5)-substituted imidazole derivatives of formula ##STR1## and their acid addition salts, in which either X is --CH.sub.2 -- and R.sub.1 is --CN, --COOH, COO(lower alkyl), --CHO, --CO(lower alkyl), lower alkyl or 3 or 5 carbon atoms, lower alkenyl, or lower (hydroxy alkyl) or X is ##STR2## --C(:CH--R)-- or --CH(CH.sub.2 R)--, where R is hydrogen or lower alkyl, and R.sub.1 is lower alkyl, and R.sub.3 and R.sub.4 are each hydrogen, methyl, ethyl, methoxy, or halogen, and novel intermediates and processes for their preparation. These compounds, in particular when R.sub.1 is lower alkyl, lower alkenyl, or lower (hydroxy alkyl), possess valuable pharmacological properties and are useful especially as selective .alpha..sub.2 -receptor antagonists.

REFERENCES:
patent: 4464358 (1984-08-01), Cox
patent: 4689339 (1987-08-01), Karjalainen et al.
Chemical Abstracts, 105:218736c (1986) [Scheinin, H. et al., Eur. J. Pharmacol. 1986, 129 (1-2), 113-21].
Chemical Abstracts, 72: 21195u (1970) [D. Gracey, et al., J. Chem. Soc. B 1969, (9), 1207-9].

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