Corticotropin-releasing factor antagonism compounds
AssigneeNova Pharmaceutical Corporation
InventorsMary E. Abreu, Waclaw Rzeszotarski, Donald J. Kyle, Roger N. Hiner, Richard L. Elliott
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Abstract
The present invention relates to a method of producing corticotropin-releasing factor (CRF) antagonist activity and thus provides a method of treating a wide range of stress-related disorders, including affective illnesses, such as depression and anxiety, as well as irritable bowel syndrome, anorexia nervosa, cardiovascular abnormalities and stress-induced immune suppression. The invention also relates to compounds (4-substituted thio-5-oxo-3-pyrazolines) and to pharmaceutical compositions suitable for use in such a method.
Claims8
A corticotropoin-releasing factor antagonist represented by the Formula I:
- ##STR2## wherein:
- R.sub.1 is hydrogen;
- phenyl;
- phenyl singly or multiply substituted with halogen, nitro, amino, alkylamino, dialkylamino, dialkylaminomethyl, C.sub.1-8 alkyl (straight chain, branched, saturated or unsaturated), hydroxy, alkoxy, cyano, trifluoromethyl, alkylthio, alkylsulfonyl, or methylenedioxy;
- naphthyl;
- indanyl;
- indenyl;
- C.sub.1-4 alkyl (straight chain, branched, saturated or unsaturated);
- or aralkyl (where the aryl group is selected from phenyl or naphthyl and the alkyl group is C.sub.1-3);
- R.sub.2 is C.sub.1-4 alkyl (straight chain, branched, saturated or unsaturated);
- phenyl;
- or aralkyl (where the aryl group is selected from those set forth in the definition of R.sub.1 and the alkyl is C.sub.1-3);
- R.sub.3 is C.sub.1-8 alkyl (straight chain, branched, saturated or unsaturated);
- C.sub.1-8 straight chain alkyl substituted with at least one carboxylic acid, amino or carboxymethoxy group;
- phenyl;
- or phenyl singly or multiply substituted with acetimido, amino, nitro, alkylamino, dialkylaminomethyl, hydroxy, alkoxy, alkylsulfonyl, methylenedioxy, halogen or trifluoromethyl;
- R.sub.4 is SCO-C.sub.1-4 alkyl, or pharmaceutically acceptable salt thereof.
The compound 2,3-dimethyl-5-oxo-1-phenyl-3-pyrazolin-4-yl thioacetate, or pharmaceutically acceptable salt thereof.
A pharmaceutical composition in dosage unit form suitable for use in producing a corticotropin releasing factor antagonistic effect in an animal comprising, as an active ingredient, an amount of 2,3-dimethyl-5-oxo-1-phenyl-3-pyrazolin-4-yl thioacetate, or pharmaceutically acceptable salt thereof, sufficient to exert said effect, together with a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.