N-substituted derivatives of 3R,4R-ethyl-[(1-methyl-1H-imidazol-

Details N-substituted derivatives of 3R,4R-ethyl-[(1-methyl-1H-imidazol- N-substituted derivatives of 3R,4R-ethyl-[(1-methyl-1H-imidazol-

1994-06-24

1995-09-26

Haley, Jacqueline

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

5483147, A61K 31415, C07D40514

Patent

active

054534348

ABSTRACT:
The present invention relates to new carbonyl 3R, 4R-ethyl-[(1-methyl-1H-imidzaol-5-yl)methyl]-2-pyrrolidinone derivatives carrying a carboxyester-type lipophilic moiety on the pyrrolidinone nitrogenand are valuable antiglaucoma agents and targeted for use in the treatment of so-called dry eye.
More particularly, the present invention concerns new N-substituted carbonyl-3R, 4R-ethyl-[(1-methyl-1H-imidazol-5-7)methyl]-2-pyrrolidinone derivatives of the formula (I): ##STR1## wherein R is selected from the group consisting of ##STR2## wherein R.sup.1 is a halo radical, e.g. a chloro radical, or a lower alkyl radical, e.g. a methyl or ethyl radical, with the proviso that when m is 1, R.sup.1 is not methyl or t-butyl, m is an integer of 1 or 2, n is 0 or an integer of 1 or 2 and X is O or S, and pharmaceutically-acceptable acid addition salts thereof.

REFERENCES:
patent: 3470197 (1969-09-01), VanDyke
patent: 5264449 (1993-11-01), Albaugh
Noller, Textbook of Organic Chemistry, 2nd Ed., W. B. Saunders Co., Philadelphia, p. 185, (1962).

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