Hoffmann-la Roche Inc.

Michael Rosenberger

Gabriel G Saucy

Allen John Lovey

Noal Cohen

Edward R Aig

John W Coffey

Peter Mohr

Michael J Klaus

Werner Bollag

Stanley S Shapiro

Thomas I Doran

Francesco Sinigaglia

Paola Panina-Bordignon

The present invention relates to novel retinoid antagonists of the formula I

Retinoid antagonists and use thereof

Novel nonatetraenoic acid derivatives which selectively bind to retinoic acid X-receptors (RXR) and which have anti-acne acitvity and which potentiate the activity of retinoids having RAR.alpha. activity are disclosed.

RXR selective ligands

Retinoic acid X-receptor ligands

A compound of the formula ##STR1## its pharmaceutically acceptable salts, and its pharmaceutically acceptable hydrolyzable esters for reducing sebum secretion and combatting acne as well as oral and topical compositions for use thereof.

Nonatetraenoic acid derivative for use in treating acne

The compounds 9-phenyl-3,7-dimethyl-2,4,6,8 nonatetraenoic acids wherein the phenyl group is substituted with an alkyl, aminoalkyl, hydroxyalkyl, alkoxy, hydroxyalkylamino, and a hydroxy alkoxy group, and derivatives thereof which are used as disease modifying anti-rheumatic agents and as immunosuppressants.

Phenyl substituted-2,4,6,8-nonatetraenoic acid

The compounds 9-phenyl-3,7-dimethyl-2,4,6,8-nonatetraenoic acids wherein the phenyl group is substituted with an alkyl, aminoalkyl, hydroxyalkyl, alkoxy, hydroxyalkylamino, and a hydroxy alkoxy group, and derivatives thereof which are used as disease modifying anti-rheumatic agents and as immunosuppressants.

A chemical synthesis of an SRS-A active compound from the reaction product of 1-halo-2-octyne and the ether of 2-penten-4-yn-1-ol including intermediates in the synthesis, some of which being antagonists of SRS-A useful for treating allergic reactions.

Synthesis of SRS-active compounds

A total synthesis of canthaxanthin or dinor-canthaxanthin, known food coloring agents, from pentols.

Acetylenic diols and monoethers thereof

9-Furyl substituted retinoic acid derivatives which are useful as antitumor agents and in the treatment of acne as well as a method for their manufacture are disclosed.

Growing community of inventors

Caldwell, NJ, United States of America

Michael Rosenberger