Syntex (u.s.a.) Inc.

Arlindo L Castelhano

Alexander Krantz

Diana H Pliura

Michael C Venuti

Lawrence M DeYoung

This invention is directed to compounds of the formula: ##STR1## or an optical isomer thereof, or a pharmaceutically acceptable salt thereof, wherein: n is 0, 1 or 2; p and q are independently 0, 1 or 2 and the sum of (p+q) is less than or equal to 3; X is selected from the group consisting of: halo; --OR.sup.2, --SR.sup.2, --S(O)R.sup.2, --S(O).sub.2 R.sup.2, and --S(O).sub.2 NHR.sup.2, wherein R.sup.2 is lower alkyl, mono-, di- or tri-fluoro alkyl of 2 or 3 carbon atoms, optionally substituted aryl; R is H or an N-protecting group; R.sup.1 is alkylthio, arylthio, amino, alkylamino, optionally substituted arylamino, or optionally substituted aralkylamino; and when the sum of n+p+q is greater than or equal to one, R.sup.1 is also hydroxy, alkoxy, or aralkoxy; and each (aa) is independently an .alpha.-amino acid residue with an optionally protected amino acid side chain.

Transglutaminase inhibitors

The present invention is directed to certain 3,5 substituted, 4,5-dihydroisoxazoles, and methods for their use. These compounds are transglutaminase inhibitors, and are particularly effective in the inhibition of epidermal transglutaminase and the treatment of acne.

The present invention is directed to certain 3,5 substituted, 4,5-dihydroisoxazoles, and methods for their use. These compounds are transgulatminase inhibitors, and are particularly effective in the inhibition of epidermal transglutaminase and the treatment of acne.

3,5-substituted 4,5-dihydroisoxazoles as transglutaminase inhibitors

This invention is for .gamma.-allenyl-.gamma.-aminobutyric acid derivatives which are .gamma.-aminobutyric acid transaminase inhibitors.

.gamma.-allenyl-.gamma.-aminobutyric acids

Novel .alpha.-allenic-.alpha.-amino acids which are enzyme inhibitors of the suicide or k.sub.cat type are disclosed herein.

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Mississauga, Canada

Arlindo L Castelhano