Syntex (u.s.a.) Inc.

Other

Byk Gulden Lomberg Chemische Fabrik Gmbh

Michael C Venuti

Gordon H Jones

John M Young

John J Bruno

Diana H Pliura

Robert Alvarez

Arlindo L Castelhano

John H Fried

Alexander Krantz

D V Murthy

Lawrence M DeYoung

Richard T Dean

John Lister-James

Joseph M Muchowski

Jurg R Pfister

Bradley J Benson

David D Lesikar

Steven Shak

Todd C Somers

John T Stults

Kathleen A Shiffer

Cynthia P Quan

John H Frenz

Young, John M

The invention provides compounds comprising glycoprotein IIb/IIIa receptor-binding benzodiazepine derivatives covalently linked to metal ion chelators. The compounds of the invention may be labeled with a radionuclide such as,Tc and used to image thrombi.

Benzodiazepine derivatives for imaging thrombi

Stable lung surfactant compositions are provided, as well as methods for their preparation, modification, formulation, assay, and therapeutic use.

Surfactant compositions and methods

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:

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

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,

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

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

Pharmaceutical compositions comprising, or compositions consisting essentially of, compounds according to the formula ##STR1## or an optical isomer thereof are disclosed, wherein the substituents A, Z and R.sup.1 are defined herein. The invention is also directed to certain compounds of the above class. The compounds of Formula I are cyclic AMP phosphodiesterase inhibitors useful as antithrombotic and inotropic agents and the like in mammals.

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San Francisco, CA, United States of America

Michael C Venuti