Ortho Pharmaceutical Corporation

Janssen Pharmaceutica Nv

Ronald K Russell

Zhihua Sui

Shawn T Branum

Christopher A Teleha

Kenneth M Wells

Mark J Macielag

Scott L Dax

Mark Andrew Youngman

Jeffery B Press

James J McNally

Donald William Ludovici

Christopher M Flores

Jay M Matthews

Ning Qin

Michele C Jetter

Raymond W Colburn

Yi Liu

Scott C Youells

Joseph J Salata

Laura M Reaney

William V Murray

Sumihiro Nomura

Xun Li

Nagy E Fawzy

Fu-An Kang

Richard Anthony Rampulla

Derek A Beauchamp

Yosuke Matsumura

Michael Reuman

Laura M Andraka

James J Mcnally

Laura M Reany

The present invention is directed to a novel process for the preparation of compounds having inhibitory activity against sodium-dependent glucose transporter (SGLT) being present in the intestine or kidney.

Process for the preparation of compounds useful as inhibitors of SGLT-2

Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R, R, R, and Rare defined herein.

Sulfonamides as TRPM8 modulators

The present invention comprises processes for preparing compounds of Formula (I). wherein: R, R, R, R, R, R, and A are as defined in the specification.

Fused cyclopentyl antagonists of CCR2

This invention relates to aminoethylthiophene derivatives and more particularly 2- and 3-aminoethylthiophene derivatives which are useful as antiarrhythmic agents, their methods of use as antiarrhythmic agents, and novel intermediate compounds useful for preparation of the aminoethylthiophene derivatives of the invention.

Aminoethylthiophene derivatives

This invention relates to thieno tetrahydropyridine and isoquinoline derivative compounds which are useful as antiarrhythmic agents, pharmaceutical compositions comprising such compounds, novel intermediates for their preparation and their methods of use. More particularly these thieno tetrahydropyridine and isoquinoline derivative compounds have been demonstrated to increase the effective refractory period (ERP) of isolated perfused cardiac tissue in vitro.

Thieno tetrahydropyridines useful as class III antiarrhythmic agents

A process for producing a compound of formula I: ##STR1## comprising reacting 5-(2-fluorophenyl)-1H-tetrazole with a Grignard reagent to produce the desired product is disclosed. Novel compounds produced by this process for use as intermediates in making certain angiotension II antagonists are also disclosed.

Process for the preparation of certain substituted biphenyl tetrazoles

This invention relates to aminoethylthiophene derivatives and more particularly 2-and 3-aminoethylthiophene derivatives which are useful as antiarrhythmic agents, their methods of use as antiarrhythmic agents, and novel intermediate compounds useful for preparation of the aminoethylthiophene derivatives of the invention.

The synthesis of novel ethanesulfonamide compounds is described. The novel ethanesulfonamide compounds have antisecretory activity and are used in the treatment of peptic ulcer disease. The intermediates used to prepare the ethanesulfonamides are useful in the treatment of osteoporosis and other bone wasting diseases.

Ethanesulfonamide derivatives

The synthesis of ring-fused thienopyrimidinedione derivatives is described. The novel ring-fused thienopyrimidinedione derivatives are generally vasodilating agents and antihypertensive agents and as such are useful as cardiovascular agents.

Ring-fused thienopyrimidinedione derivatives

The synthesis of novel ethanesulfonamide compounds is described. The novel ethanesulfonamide compounds have antisecretory activity and are used in the treatment of peptic ulcer disease.

Novel thienopyrimidine-2,4-dione piperidine derivatives and novel furo[3,4-d]pyrimidine-2,4-dione piperidine derivatives are described. The novel piperidine derivatives are selective serotonin antagonists and alpha adrenergic blocking agents with cardiovascular, gastrointestinal and central nervous system activites.

Thieno- and furopyrimidine-2,4-dione piperidine derivatives as serotonin

The synthesis of thienopyrimidine-2,4-dione derivatives and their urea intermediates is described. The novel urea intermediates and thienopyrimidine-2,4-dione derivatives are general vasodilating agents and anti-hypertensive agents. The compounds are useful as cardiovascular agents.

N-(substituted thienyl)-N'-(substituted piperazinyl)-ureas

The synthesis of thienopyrimidine-2,4-dione derivatives and their urea intermediates is described. The novel urea intermediates and thienopyrimidine-2,4-dione derivatives are generally vasodilating agents and anti-hypertensive agents. The compounds are useful as cardiovascular agents.

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Titusville, NJ, United States of America

Ronald K Russell