Certain 1,1-diaryl-propenyl-3-(1-pyrrolidino-2-carboxylic acids,

Details Certain 1,1-diaryl-propenyl-3-(1-pyrrolidino-2-carboxylic acids, Certain 1,1-diaryl-propenyl-3-(1-pyrrolidino-2-carboxylic acids,

1984-07-27

1986-09-09

Rotman, Alan L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

514317, 514318, 514423, 546194, 546281, 548532, C07D40106, A61K 3144

Patent

active

046109951

ABSTRACT:
The invention provides a compound of the formula (I): ##STR1## or a salt, ester or amide thereof; wherein R.sub.1 is hydrogen or C.sub.1-4 alkyl and R.sub.2 is C.sub.1-4 alkyl substituted by a group R.sub.3 CO.sub.2 H or R.sub.1 and R.sub.2 taken together with the nitrogen comprise a nitrogen-containing heterocyclic ring having four to six ring members substituted by a group R.sub.3 CO.sub.2 H, wherein R.sub.3 is a C.sub.1-7 aliphatic hydrocarbon group or a single bond;
R.sub.4 is hydrogen, halogen, hydroxy, cyano, C.sub.1-4 acyloxy, C.sub.1-4 alkoxy or C.sub.1-4 alkyl optionally substituted by one to three halogen atoms;
X is --N.dbd. or --CH.dbd.; and
A and B each represent hydrogen atoms or --CA--CB-- represents --C.dbd.C--.
The invention also provides a method for the preparation of compounds of the formula (I), novel chemical intermediates in their preparation and pharmaceutical formulations. Compounds of the formula (I) have antihistaminic activity.

REFERENCES:
patent: 2567245 (1951-09-01), Sperber et al.
patent: 4562258 (1985-12-01), Findlay et al.
patent: 4584382 (1986-04-01), Findlay et al.
Carren et al., Chemical Abstracts 77:88328m.

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