E. R. Squibb Sons, Inc.

Bristol-myers Squibb Compnay

Karo Bio Ab

Denis E Ryono

Edward W Petrillo, Jr

Minsheng Zhang

Yan Shi

Harold N Weller, Iii

Peter T W Cheng

Johan Malm

Miguel A Ondetti

Wei Meng

Jon J Hangeland

Todd J Friends

Yolanda V Caringal

Neeraj Garg

Joseph Anthony Tino

Sean Chen

Scott A Bolton

Ying Wang

Eric M Gordon

Richard B Sulsky

William N Washburn

Pratik Devasthale

Arthur M P Doweyko

Tamara Dejneka

Konrad Koehler

Chris Litten

Yi-Lin Li

Ana Maria Garcia Collazo

Andrei Sanin

Ye Liu

Jeffrey A Robl

Donald S Karanewsky

Ashvinikumar V Gavai

John E Lloyd

Joel C Barrish

Philip Michael Sher

Gregory S Bisacchi

Bruce A Ellsworth

Sesha I Natarajan

Peter T Cheng

Kathleen M Poss

Chong-qing Sun

Chong-Oing Sun

Thomas Ericsson

Mahmoud Rahimi Ghadim

Thomas Anders Wilson Ericsson

Lars Johan Malm

Mahmoud Rahimi-Ghadim

Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure is a heteroaryl ring; A method for treating diabetes and related diseases employing the above compounds is also provided.

Substituted pyrazolylamides useful as glucokinase activators

Compounds are provided which are activators of the enzyme glucokinase and thus are useful in treating diabetes and related diseases, which compounds have the structure where Q is and R, R, R, R, R, R, Rand Rare as defined hereinor a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.

Glucokinase activators and methods of using same

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

Compounds are provided which are phosphonate and phosphinate activators and thus are useful in treating diabetes and related diseases and have the structure wherein is a heteroaryl ring;

Substituted pyrazolylamide compounds useful as glucokinase activators

Pyrazoloamides are provided which are phosphonate and phosphinate glucokinase activators that are useful in treating diabetes and related diseases and have the structure wherein is a pyrazoyl ring;

Phosphonate and phosphinate pyrazolylamide glucokinase activators

Compounds are provided which are activators of the enzyme glucokinase and thus are useful in treating diabetes and related diseases, which compounds have the structure where Q is and R, R, R, R, R, R, Rand Rare as defined herein or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.

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.

Novel thyroid receptor ligands are provided having the general formula I wherein In addition, a method is provided for preventing, inhibiting or treating diseases or disorders associated with metabolic 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.

Substituted anilide ligands for the thyroid receptor

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

This invention relates to novel compounds, which are thyroid receptor ligands, and to methods of preparing such compounds. 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 T3 regulated gene, wherein a compound as described herein is administered in a therapeutically effective amount.

Benzamide derivatives as thyroid receptor ligands

New thyroid receptor ligands are provided which have the general formula in which: 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.

Aniline-derived ligands for the thyroid receptor

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.

Benzamide ligands for the thyroid receptor

Compounds of the formula ##STR1## wherein X, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, A, B, D and E are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.

Biphenyl-substituted quinoline derivatives

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Princeton, NJ, United States of America

Denis E Ryono