Hoffmann-La Roche Inc.

Glaxo Group Limited

Basilea Pharmaceutica Ag

Werner Bollag

Gottlieb Ryser

Rudolf Ruegg

Michael J Klaus

Francesco Sinigaglia

Paola Panina-Bordignon

Pierre-Charles Wyss

Fritz Ott

Peter Mohr

Marcel Muller

Michael Rosenberger

Ulrich Schwieter

Hans Johann Mayer

Paul Zeller

Norbert Rigassi

Ado Kaiser

Joseph Francis Grippo

Hugo Gutmann

Albert Langemann

Arthur Levin

Kurt Reber

Balthasar Hegedus

9-cis retinoic acid and pharmaceutically acceptable salts and pharmaceutically acceptable hydrolyzable esters thereof, 9-cis retinal and pharmaceutically acceptable acetals thereof, and 9-cis retinol and pharmaceutically acceptable hydrolyzable esters thereof as well as metabolites of 9-cis retinoic acid have been found to be efficacious in treating T-helper cell type 1 mediated immune diseases in well tolerated doses. Preferably, the active ingredient is formulated as a medicament for oral or topical administration.

Treatment of cell-mediated immune diseases

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

The invention is related to a method of treating chronic hand eczema in a human patient in need of treatment, using oral administration of 9-cis retinoic acid and pharmaceutically acceptable salts and pharmaceutically acceptable hydrolysable esters thereof, in an effective amount of from 0.05 to 1.5 milligrams per kilogram body weight per day.

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

Retinoid antagonists and use thereof

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

The compound 9-cis-retinoic acid, its pharmaceutically acceptable salts or its pharmaceutically acceptable esters can be used in the treatment of precancerous or premalignant epithelial lesions as well as in the treatment of malignant tumors of an epithelial nature.

Prevention and treatment of premalignant epithelial lesions and

1,2,3,4-Tetrahydro-1,1,4,4-tetramethyl-6-(.alpha.-methylstyryl)naphthalene possesses antihyperplastic, antimetaplastic, antineoplastic tumor-preventative and tumor-therapeutic properties and can accordingly be used in the treatment of precancerous or premalignant lesions as well as in the treatment of malignant tumors of epithelial and mesenchymal nature.

Treatment of premalignant lesions and certain malignant tumors

1,2,3,4-Tetrahydro-1,1,4,4-tetramethyl-6-(alpha-methylstyryl)naphthalene possesses antikeratinizing, antiinflammatory and immunomodulatory properties and can be used in the treatment or prevention of dermatoses which are accompanied by a pathological cornification as well as inflammatory, autoimmune, rheumatic and allergic illnesses.

Treatment of diseases which cause pathological cornification of the

Treatment of dermatoses and illnesses producing inflammation

Novel 9-phenyl 5,6-dimethyl-nona-2,4,6,8-tetraenoic acid,- tetraenal or tetraenol derivatives useful as anti-tumor agents.

Substituted triarylphosphonium derivatives

The novel retinoids of the formula ##STR1## wherein R represents a residue of a sugar attached ester-wise or a residue of an amino-sugar attached amide-wise or of derivatives of such sugars and n is 1 or 2, can be used as medicaments, e.g. for the treatment of neoplasms, acne and psoriasis. These compounds are obtained by reacting a sugar or an aminosugar or a derivative thereof with a reactive derivative of 9-(4-methoxy-2,3,6-trimethylphenyl)-3,7-dimethyl-2,4,6,8-nonatetraenoic acid, optionally followed by the modification of reactive groups present in the reaction product.

Retinoid carbohydrates

Novel 9-phenyl 5,6-dimethyl-nona-2,4,6,8-tetraenoic acid,-tetraenal or tetraenol derivatives useful as anti-tumor agents.

Substituted triaryl phosphonium derivatives

Methods for the prophylaxis of certain premalignant conditions and epithelial carcinomas comprising systemically administrating 13-cis vitamin A acid and a suitable pharmaceutical carrier material are described and compositions containing 13-cis Vitamin A acid suitable for systemic administration are disclosed.

Compositions and methods for using 13-cis vitamin A acid compounds

Novel 9-phenyl 5,6-dimethyl-nona-2,4,6,8-tetraenoic acid, tetraenal or tetraenol derivatives useful as anti-tumor agents.

Certain 6-(3'-methoxyphenyl) derivatives of 2,4-hexadienal

The invention relates to novel sugar esters and glycosides especially derivatives of D-glucopyranoside and D-glucopyranaronate suitable for the treatment of neoplasms, acne, psoriasis and dermatoses.

Growing community of inventors

Basel, Switzerland

Werner Bollag