Bristol-myers Squibb Compnay

Karo Bio Ab

Other

Yolanda V Caringal

Minsheng Zhang

Jon J Hangeland

Denis E Ryono

Johan Malm

Todd J Friends

Pratik Devasthale

Arthur M P Doweyko

Tamara Dejneka

Konrad Koehler

Neeraj Garg

Chris Litten

Yi-Lin Li

Ye Liu

Ana Maria Garcia Collazo

Andrei Sanin

Roger Astbury Smith

Hanno Wild

Jill E Wood

John E Lyons

Robert B Dally

Wendy Lee

Michael B Katz

Daniel Harry Rogers

Cheri Lynn Blum

A method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a Tregulated gene, wherein a compound as described in the general formula I below is administered in a therapeutically effective amount: 

Thyroid receptor ligands

Thyroid receptor ligands are provided which have the general formula I wherein:   In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolism dysfunction or which are dependent upon the expression of a Tregulated gene, wherein a compound as described above is administered in a therapeutically effective amount.

New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; Ris halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; Rand Rare the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at least one of Rand Rbeing other than hydrogen; Ris a carboxylic acid amide (CONR'R&#x2033;) or an acylsulphonamide (CONHSOR&#x2032;) derivative, or a pharmaceutically acceptable salt thereof, and all stereolsom thereof; or when n is equal to or greater than one, Rmay be heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR&#x2032;R&#x2033;). Ris hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R&#x2014;H). In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependant upon the expression of a Tregulated gene, wherein a compound as described above is administered in a therapeutically effective amount. Examples of such diseases associated with metabolism dysfunction or are dependent upon the expression of a Tregulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders. 

Thyroid receptor ligands and method II

New thyroid receptor ligands are provided which have general formula (I) in which: n is an integer from 0 to 4; Ris halogen, trifluoromethyl, or alkyl of 1 to 6 carbons or cycloalkyl of 3 to 7 carbons; Rand Rare the same or different and are hydrogen, halogen, alkyl of 1 to 4 carbons or cycloalkyl of 3 to 5 carbons, at least one of Rand Rbeing other than hydrogen; Ris a carboxylic acid amide (CONR'R&#x2033;) or an acylsulphonamide (CONHSO2R&#x2032;) derivative, or a pharmaceutically acceptable salt thereof, and all stereoisomers thereof; or when n is equal to or greater than one, Rmay be a heteroaromatic moiety which may be substituted or unsubstituted, or an amine (NR&#x2032;R&#x2033;). Ris hydrogen or an acyl (such as acetyl or benzoyl) or other group capable of bioconversion to generate the free phenol structure (wherein R=H). In addition, a method is provided for preventing, inhibiting or treating a disease associated with metabolism dysfunction or which is dependent upon the expression of a Tregulated gene, wherein a compound as described above is administered in a therapeutically effective amount. Examples of such diseases associated with metabolism dysfunction or are dependent upon the expression of a Tregulated gene include obesity, hypercholesterolemia, atherosclerosis, cardiac arrhythmias, depression, osteoporosis, hypothyroidism, goiter, thyroid cancer as well as glaucoma, congestive heart failure and skin disorders.

Pyridine-based thyroid receptor ligands

Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.

Inhibition of raf kinase activity using aryl ureas

Growing community of inventors

Lawrenceville, NJ, United States of America

Yolanda V Caringal