La Jolla Cancer Research Foundation

Incyte San Diego Inc.

Ortho-Mcneil Pharmaceutical Corp.

The Burnham Institute

Galderma Research & Development Snc

Sri International

Ligand Pharmaceuticals, Inc.

Other

Maxia Pharmaceuticals, Inc.

Magnus Pfahl

Catherine Tachdjian

Hussien A Al-Shamma

Lyle W Spruce

Xiao-kun Zhang

Andrea Fanjul

David P M Pleynet

James F Cameron

Ling Jong

Peter D Hobbs

Michael Karin

Marcia I Dawson

Darryl Rideout

Xian-Ping Lu

Hongyue Zhang

Jurgen M Lehmann

Torsten R Wiemann

James Zapf

Jianhua Guo

Karine Jakubowicz-Jaillardon

Mohamed Boudjelal

Andrea Fanjul Giachino

Richard Masten Fine

Marcia L Dawson

David Pm Pleynet

Jason B Ibarra

Maty Tzukerman

J Urgen Lehmann

The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymphoma, Hodgkin's Disease, leukemia, breast cancer, prostate cancer or cancers in general; and inflammation, such as osteoarthritis, rheumatoid arthritis, Crohn's Disease or Inflammatory Bowel Disease 

Substituted heterocycles for the treatment of diabetes and other diseases

The invention relates to certain bicyclic heterocycles havng the structure shown below which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, and atherosclerosis. 

Bicyclic heterocycles for the treatment of diabetes and other diseases

The invention relates to certain heterocyclic compounds useful for the treatment of cancer and other diseases, having the Formula (I): wherein:

Heterocyclic derivatives for the treatment of cancer and other proliferative diseases

The present invention relates to certain substituted heterocycles of Formula (200), wherein B, H, I, J and K together with the Arform a ring containing at least one amide residue, and W, X, Y and Z together form a 2,4-thiazolidinedione, 2-thioxo-thiazolidine-4-one, 2,4-imidazolidinedione or 2-thioxo-imidazolidine-4-one residue; or a pharmaceutically acceptable salt thereof. The compounds are useful in the treatment of diseases such as type 2 diabetes, and related disorders of lipid and carbohydrate metabolism, including atherosclerosis. The compounds are also useful for treating diseases of uncontrolled proliferation, such as cancers in general, including breast cancer.

Heterocyclic amide derivatives for the treatment of diabetes and other diseases

This invention provides a purified heterodimer comprising an RXR and a hormone receptor. The invention also provides a method of screening ligands for their effect on the activity of an RXR-containing hormone receptor heterodimer comprising combining the heterodimer with the ligand and determining the effect on activity. Also provided is a method of amplifying the activity of a hormone receptor comprising forming a heterodimer with another hormone receptor.

Heterodimers of retinoid X receptors (RXRS) and other steroid hormone receptors

The present invention relates to certain compounds of Formula (I) which can be useful in the treatment of diseases, such as, cancer, metabolic disorders, Type 2 Diabetes, dyslipidemia and/or hyperchloesterolemia: 

N-substituted heterocycles for the treatment of hypercholesteremia, dyslipidemia and other metabolic disorders; cancer, and other diseases

The present invention relates to certain substituted heterocycles of Formula (I) which are useful in the treatment of diseases related to lipid and carbohydrate metabolism, such as type 2 diabetes, adipocyte differentiation, uncontrolled proliferation, such as lymphoma, Hodgkin's Disease, leukemia, breast cancer, prostate cancer or cancers in general; and inflammation, such as osteoarthritis, rheumatoid arthritis, Crohn's Disease or Inflammatory Bowel Disease.

Imidazolidinedione derivatives for the treatment of diabetes and other diseases

The invention relates to the discovery that specific adamantyl or adamantyl group derivatives containing retinoid-related compounds induce apoptosis of cancer cells and therefore may be used for the treatment of cancer, including advanced cancer. Also, the present invention relates to novel adamantyl or adamantyl group derivatives containing retinoid compounds and their usage for treatment and/or prevention of cancer, keratinization disorders, dermatological conditions, and other therapies More specifically, it has been shown that such adamantyl compounds, e.g., 6-&lsqb;3-(1-adamantyl)-4-methoxyphenyl&rsqb;-2-naphthoicacid, 2-&lsqb;3-(1-adamantyl)-4-methoxyphenyl&rsqb;-5-benzimidazole carboxylic acid, and 6-&lsqb;3-(1-adamantyl)-4,5-methylenedioxyphenyl&rsqb;-2-naphthoic acid, can be used to treat or prevent cervical cancers and precancers such as cervical dysplasias, including high grade and low grade dysplasias.

Apoptosis inducing adamantyl derivatives and their usage as anti-cancer agents, especially for cervical cancers and dysplasias

Thiazolidinedione derivatives for the treatment of diabetes and other diseases

This invention provides a method of inhibiting the transcription of a gene, which is activated by AP-1 or an AP-1 component, comprising binding AP-1 or the component with a nuclear receptor so as to prevent the binding of AP-1 to the gene. The nuclear receptor can be the retinoic acid receptor, glucocorticoid receptor, vitamin D3 receptor, thyroid receptor, or estrogen receptor. Also provided is a composition of matter comprising AP-1 or an AP-1 component bound to a nuclear receptor. These methods and compositions can be used to treat arthritis and cancer.

Method of inhibiting transcription utilizing nuclear receptors

Heterocyclic derivatives for the treatment of diabetes and other diseases

The invention relates to the discovery that specific adamantyl or adamantyl group derivatives containing retinoid-related compounds induce apoptosis of cancer cells and therefore may be used for the treatment of cancer, including advanced cancer. Also, the present invention relates to novel adamantyl or adamantyl group derivatives containing retinoid compounds and their usage for treatment and/or prevention of cancer, keratinization disorders, dermatological conditions, and other therapies More specifically, it has been shown that such adamantyl compounds, e.g., 6-&lsqb;3-(1-adamantyl)-4-methoxyphenyl&rsqb;-2-naphthoic acid, 2-&lsqb;3-(1-adamantyl)-4-methoxyphenyl&rsqb;-5-benzimidazole carboxylic acid, and 6-&lsqb;3-(1-adamantyl)-4,5-methylenedioxyphenyl&rsqb;-2-naphthoic acid, can be used to treat or prevent cervical cancers and precancers such as cervical dysplasias, including high grade and low grade dysplasias.

This invention relates to substantially purified Retinoic Acid Receptor &egr; (RAR&egr;), having the amino acid sequence given in FIG. and to the isolated nucleic acid encoding RAR&egr;. In addition, polypeptides comprising, and nucleic acids encoding, the DNA-binding and hormone-binding domain of the receptor are provided. Further, methods of detecting RAR&egr; and nucleic acids encoding RAR&egr; and its domains are provided.

Retinoic acid receptor &egr;(rar&egr;)

Apoptosis inducing adamantyl derivatives and their usage as anti-cancer

Growing community of inventors

Solana Beach, CA, United States of America

Magnus Pfahl