Hoffmann-la Roche Inc.

Syntex (u.s.a.) Inc.

Other

Roche Palo Alto LLC

Givaudan Corporation

Michael J Klaus

Peter Mohr

Ekkehard Weiss

Peter Loeliger

Jean-Marc Lapierre

Albert E Fischli

Hans Johann Mayer

Paula Nanette Belloni

Alexander E Wick

Beverly A Pawson

Harald Weiser

Michael Rosenberger

Werner Bollag

Francesco Sinigaglia

Paola Panina-Bordignon

Allen John Lovey

Synese Jolidon

Denis John Kertesz

Daniel Helmlinger

Mario Pesaro

The current invention provide novel heterocyclic retinoid compounds, methods of treating or preventing chronic obstructive pulmonary disease, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of these disorders and methods for delivering formulations of these retinoids to a mammal having these disorders.

Heterocyclic retinoid compounds

The current invention provide novel compounds, methods of treating or preventing emphysema, cancer and dermatological disorders, pharmaceutical compositions suitable for the treatment or prevention of emphysema, cancer and dermatological disorders and methods for delivering formulations into the lung of a mammal suffering from emphysema, cancer and dermatological disorders.

Alkyl urea retinoid agonists

Substituted urea retinoid agonists

Selective retinoid agonists

Aromatic carboxylic acid derivatives

Retinoids with retinoid receptor antagonistic activity, pharmaceutically acceptable salts and pharmaceutically acceptable hydrolyzable esters thereof, have been found efficacious in treating T-helper cell type 2 (Th2)-mediated immune diseases, such as immunoglobulin E (IgE)-mediated allergic diseases.

Treatment of T-helper cell type 2-mediated immune diseases by retinoid antagonists

New compounds containing bicyclic fused rings, one of which being a phenyl moiety connected by an aliphatic chain to a cycloalkyl or aryl moiety, and pharmaceutically active salts thereof are useful as RAR selective retinoid agonists. Furthermore, such retinoic acid receptor agonists, particularly retinoic acid receptor &ggr; (RAR&ggr;) selective agonists, are useful for the treatment of emphysema and associated pulmonary diseases, as well as for the therapy and prophylaxis of dermatological disorders, for the therapy and prophylaxis of malignant and premalignant epithelial lesions, tumors and precancerous changes of the mucous membrane in the mouth, tongue, larynx, esophagus, bladder, cervix and colon.

RAR selective retinoid agonists

This invention relates to new retinoic acid receptor selective retinoid agonists, to pharmaceutical compositions containing such compounds, and to the use of such retinoic acid receptor agonists, particularly retinoic acid receptor &ggr; (RAR&ggr;) selective agonists, for the treatment of emphysema and related pulmonary diseases.

Thiophene derivatives

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

Retinoid antagonists and use thereof

This invention provides methods of treating emphysema and other diseases associated with alveolar damage by treatment with an RAR&ggr; selective agonist. In another aspect, this invention provides methods of promoting tropoelastin gene expression and alveolar matrix repair by contacting the pulmonary intestitial fibroblast with an RAR agonist, preferably an RAR&ggr; selective agonist.

Treatment of emphysema using RARy selective retinoid agonists

Treatment of T-helper cell type 2-mediated immune disease by retinoid

Compounds of the formula: ##STR1## wherein R.sup.2 and X are as described, are disclosed. The compounds are useful for treating dermatological disorders which are accompanied by epithelial lesions, e.g., acne and psoriasis, as well as malignant and premalignant epithelial lesions, tumours and precancerous changes of the mucous membrane in the mouth, tongue, larynx, oesophagus, bladder, cervix and colon.

Retinoids

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

Growing community of inventors

Weil am Rhein, Germany

Michael J Klaus