Merck + Co., Inc.

Shuet-Hing Lee Chiu

Josephine R Carlin

Richard L Tolman

Donald W Graham

Rae Taub

Su-er Wu Huskey

This invention is concerned with mammalian metabolites of the compound 2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-(4-fluoro)-phenyl-4-(3-(5-oxo-1H,4H-1,2,4-triazolo)methylmorpholine which is a tachykinin receptor antagonist that is useful in the prevention and treatment of certain disorders, including emesis and psychiatric disorders such as depression and anxiety.

Mammalian metabolites of a tachykinin receptor antagonist

7-substituted 4-aza cholanic acid derivatives and their use

Compounds of the Formula I ##STR1## wherein: the dotted line indicates that a double bond may be present or absent; R.sup.1 is H, methyl or ethyl; R.sup.2 is .alpha.- or .beta.-C.sub.1-10 straight or branched alkyl; R.sup.3 is CO.sub.2 H, CN, CO.sub.2 R.sup.4, COHNR.sup.4, or CON(R.sup.4).sub.2 ; R.sup.4 is H, C.sub.1-10 straight or branched alkyl, aryl, heteroaryl, or aralkyl; Aryl is phenyl, substituted phenyl, naphthyl, or biphenyl; Heteroaryl is pyridyl, pyrrolyl, thienyl, furanyl or quinolinyl; and Aralkyl is C.sub.1-10 alkyl substituted with one to three phenyl or substituted phenyl moieties; and their pharmaceutically acceptable salts are described. These compounds are 5.alpha.-reductase type 1 inhibitors. They may be used for treating conditions associated with an excess of DHT, either alone or in combination with other 5.alpha.-reductase inhibitors.

There are disclosed novel ivermectin compounds and a process for preparing them, the novel ivermectin compounds containing straight chain or branched fatty acid residues of from about C.sub.2 to about C.sub.20 and having the formula: ##STR1##

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Westfield, NJ, United States of America

Shuet-Hing Lee Chiu