Syntex (u.s.a.) Inc.

Syntex LLC

Cortech, Inc.

Zenith Cosmetic Technologies LLC

John M Young

Gordon H Jones

Michael C Venuti

D V Murthy

Joseph M Muchowski

Robert J Greenhouse

Lyle W Spruce

Albert Charles Gyorkos

Alexander Krantz

John C Cheronis

Val S Goodfellow

James Ivan Gerrity

Axel H Leimer

The invention relates to a process for making compounds having fatty acid moieties by reacting a fatty acid with a (hydroxyalkyl)amino alkane acid or a (hydroxyalkyl)amine and an aqueous base followed by heating the reaction mixture. The process is particularly useful for the formation of di-fatty acid esters from BES, and tri-fatty acid esters from TES. The reaction parameters can be adjusted to produce useful additional products of the TES-trioleate, including fatty acid amides of mono-, di- and tri-oleoyl-TES.

Process for the manufacture of compounds containing a fatty acid moiety

The present invention relates to cysteine protease inhibitors of the general formula (I): ##STR1## wherein Z is a cysteine protease binding moiety; X and Y are S, O or optionally substituted N; and R.sub.1 is optionally substituted alkyl or aryl.

Cysteine protease inhibitors

Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 is lower alkoxy or optionally substituted phenoxy;

Naphthalene lipoxygenase-inhibiting agents

Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 is lower alkoxy or optionally substituted phenoxy,

Method for treating disease states in mammals with naphthalene

Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 is alkoxy, alkylthio, optionally substituted phenoxy or optionally substituted phenylthio;

Naphthalene anti-psoriatic agents

Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are the same and are lower alkoxy or optionally substituted phenoxy,

3-[.omega.-(3,5-Di-t-butyl-4-hydroxyphenyl)alkanoyl]-pyrroles and their de-oxy analogs, for example, 3-(3,5-di-t-butyl-4-hydroxybenzyl)pyrrole, 2-chloro-4-(3,5-di-t-butyl-4-hydroxybenzoyl)pyrrole, 3-(3,5-di-t-butyl-4-hydroxybenzoyl)pyrrole and 3-[2-(3,5-di-t-butyl-4-hydroxyphenyl)-1-oxoethyl]pyrrole, have high pharmacological potency as anti-inflammatory, analgesic and antipyretic agents.

3-[.omega.-(3,5-Di-t-butyl-4-hydroxyphenyl)alkyl]pyrroles, and

Novel alkoxycarbonylamino benzoates and related copounds (carbamoyl benzoates) are disclosed for treatment of auto-immune disease states, such as arthritis.

Novel use for carbamoyl benzoates

Naphthalenes of the formula: ##STR1## wherein: m is 1 or 2;

3-(.omega.-(3,5,-di-t-butyl-4-hydroxyphenyl)-alkanoyl)pyrroles, and

Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are the same and are lower alkoxy, lower alkylthio, optionally substituted phenoxy or optionally substituted phenylthio,

Psoriasis in mammals is relieved by topically administering naphthoquinones of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are lower alkoxy; and

Naphthoquinone anti-psoriatic agents

Psoriasis in mammals is relieved by topically administering substituted naphthoquinone of the formula: ##STR1## wherein: R.sup.3 is halo, linear or branched alkoxy of one to eighteen carbon atoms or --S(O).sub.n R wherein:

The 2,3-diesters of 6-substituted-2,3-dihydroxy-1,4-naphthoquinones exhibit useful anti-psoriatic activity in mammals.

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Redwood City, CA, United States of America

John M Young