Bristol-Myers Squibb Compnay

E. R. Squibb Sons, Inc.

Rutgers, the State University of New Jersey

St. Jude Children's Research Hospital

Mmv Medicines for Malaria Venture

Venenum Biodesign, LLC

Philip D Stein

Steven E Hall

Yan Shi

Saleem Ahmad

Natesan Murugesan

Joel C Barrish

David M Floyd

Stephen P O'Connor

Philip Michael Sher

Raj N Misra

Karnail S Atwal

John T Hunt

Chi Li

John E Lloyd

William N Washburn

Khehyong Ngu

Francis N Ferrara

Michael R Lawrence

Jagabandhu Das

Jeffrey A Robl

Chunhong He

Michael A Poss

Dean A Wacker

Sharon N Bisaha

David L Green

Gregory S Bisacchi

George C Rovnyak

Steven P Seitz

Wen-Ching Han

Brian F McGuinness

Guohua Zhao

Jay A Markwalder

Charles Z Ding

Gary J Grover

Jeffrey John Letourneau

David J Carini

Chia-Yu Huang

Dongchuan Shi

Andrew G Cole

Steven G Kultgen

Rodney Kiplin Guy

Spencer Knapp

Jeffrey G Varnes

Fangyi Zhu

James R Beasley

Lawrnce G Hamann

Thomas J Caulfield

Wendyam Armand Guiguemde

Steve Castro

Chet Kwon

The present invention relates to sulfonamide compounds of formula (I) and formula (II), or a pharmaceutically acceptable salt thereof. The present sulfonamide compounds are useful non-systemic TGR5 agonists that can be used to treat diabetic diseases in human. The present invention provides a pharmaceutical composition containing sulfonamide compounds of formula (I) and formula (II) and a method of making as well as a method of using same in treating patients inflicted with metabolic disorders by administering same. The compounds of the present invention may be used in combination with additional anti-diabetic drugs. 

Non-systemic TGR5 agonists

In one aspect, the invention relates to novel substituted 2-alkyl-1-oxo-N-phenyl-3-heteroaryl -1,2,3,4-tetrahydroisoquinoline-4-carboxamides; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating and/or preventing malaria. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Substituted 2-alkyl-1-OXO-N-phenyl-3-heteroaryl-1,2,3,4-tetrahydroisoquinoline-4-carboxamides for antimalarial therapies

The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R, R, R, R, and Rare defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.

Substituted pyrazinone melanin concentrating hormone receptor-1 antagonists and methods

The present invention provides modulators of serotonin receptors, pharmaceutical compositions containing such modulators and methods for treating various diseases, conditions and disorders associated with modulation of serotonin receptors such as, for example: metabolic diseases, which includes but is not limited to obesity, diabetes, diabetic complications, atherosclerosis, impaired glucose tolerance and dyslipidemia; central nervous system diseases which includes but is not limited to, anxiety, depression, obsessive compulsive disorder, panic disorder, psychosis, schizophrenia, sleep disorder, sexual disorder and social phobias; cephalic pain; migraine; and gastrointestinal disorders using such compounds and compositions.

Modulators of serotonin receptors

Compounds are provided of the following structure are HMG CoA reductase inhibitors and thus are active in inhibiting cholesterol biosynthesis, modulating blood serum lipids, for example, lowering LDL cholesterol and/or increasing HDL cholesterol, and treating hyperlipidemia and dyslipidemia, hypercholesterolemia, hypertriglyceridemia and atherosclerosis wherein variables A and B are defined herein.

HMG-CoA reductase inhibitors

Sulfonamide lactams of the following formula wherein X, R, R, R, R, R, R, R, R, R, Rand Rare as described herein, are provided which inhibitors of Factor Xa and are useful as anticoagulants in the treatment of cardiovascular diseases associated with thromboses.

Sulfonamide lactam inhibitors of FXa and method

Compounds having the formula (I), and pharmaceutically acceptable salts thereof,are useful for modulating mitochondrial FFATPase activity and treating ischemic conditions including myocardial infarction, congestive heart failure, and cardiac arrhythmias.

(1-phenyl-2-heteoaryl)ethyl-guanidine compounds as inhibitors of mitochondrial F1F0 ATP hydrolase

Phenyl sulfonamide endothelin antagonists

Benzoic acid derivatives and related compounds as antiarrhythmic agents

Lactam inhibitors of factor Xa and method

Lactam inhibitors of FXa and method

Caprolactam inhibitors are provided which have the structure

Tetralone derivatives of the formula ##STR1## where R.sup.1 is halo, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, (aryl)alkenyl, (aryl)alkynyl, alkoxy, O-alkenyl, O-aryl, O-alkyl(heterocyclo), COO-alkyl,alkanoyl, CO-amino, CO-substituted amino, alkyl-CO-amino, alkyl-CO-substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-alkyl(heterocyclo), N(alkyl)CO-alkyl, N(alkyl)CO-aryl, N(alkyl)CO-heterocyclo, N(alkyl)CO-alkyl(heterocyclo);

Tetralone derivatives as antiarrhythmic agents

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Pennington, NJ, United States of America

Philip D Stein