Merck + Co., Inc.

Janssen Pharmaceutica Nv

Mitsubishi Tanabe Pharma Corporation

Kenneth M Wells

Ralph P Volante

Scott L Dax

Nobuyoshi Yasuda

Mark Andrew Youngman

Kai Rossen

Paul J Reider

David Askin

Richard John Varsolona

Ronald K Russell

Michele C Jetter

Shawn T Branum

Mark J Macielag

James J McNally

Donald William Ludovici

Joseph E Lynch

Christopher M Flores

Christopher A Teleha

Jay M Matthews

Ning Qin

Chunhua Yang

Raymond W Colburn

Mark S Jensen

Yao-Jun Shi

Yi Liu

Scott C Youells

Derek A Beauchamp

Sumihiro Nomura

Yi Xiao

Yaling Wang

Laura M Reaney

William H Parsons

Mark R Player

Jian Liu

Ahmed F Abdel-Magid

John Y Chung

Nelo R Rivera

Raul R Calvo

Steven Mehrman

Wenxi Pan

Xun Li

Wing S Cheung

Sharmila Patel

Michael Palucki

Lorraine Scott

Yu-Kai Lee

Michael Richard Brandt

Mitsuya Hongu

Fan Zhang-Plasket

Johnnie L Leazer, Jr

Yosuke Matsumura

Yuichi Koga

Maureen Chislom

Laura M Andraka

Michael Brandt

Raul L Calvo

Laura M Reany

James J Mcnally

Maureen Chisholm

Mark A Youngman

Michael R Brandt

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

Process for the preparation of compounds useful as inhibitors of SGLT

The present invention relates to a crystalline hydrochloride salt of (1-(4-fluorophenyl)-1H-indol-5-yl)(3-(4-(thiazole-2-carbonyl)piperazin-1-yl)azetidin-1-yl)methanone, methods of making said salt, pharmaceutical compositions containing said salt, and the use of said salt in the treatment of pain and diseases that cause such pain, and metabolic disorders such as, obesity, hyperphagia, and diabetes.

Crystalline hydrochloride salt of (1-(4-fluorophenyl)-1H-indol-5-yl)-(3-(4-(thiazole-2-carbonyl)piperazin-1-yl)azetidin-1-yl)methanone

The invention is directed to compounds of Formula (I): to pharmaceutical compositions containing such compounds and to methods of treatment using them.

Benzimidazole modulators of VR1

Amine salts of 3-{2-oxo-3-[3-(5,6,7,8-tetrahydro[1,8]naphthyridin-2-yl)-propyl]imidazolidin-1-yl}-3-(6-methoxy-pyridin-3-yl)propionic acid are potent antagonists of the integrin &#x3b1;v&#x3b2;3 receptor and are useful for the prevention and/or treatment of osteoporosis and vascular restenosis, as well as conditions associated with excessive angiogenesis, such as macular degeneration, diabetic retinopathy, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth. The invention also relates to a process for the preparation of the novel salts as well as pharmaceutical compositions containing the salts and methods of using the salts.

Amine salts of an integrin receptor antagonist

A novel process is provided for the preparation of imidazolidinone &agr;v&bgr;3/&agr;v&bgr;5 integrin antagonists, and the useful intermediates obtained therein. These compounds are antagonists of &agr;v&bgr;3/&agr;v&bgr;5 integrin receptors and thus useful for inhibiting bone resorption and treating and preventing osteoporosis. Also disclosed is 3-&lcub;2-oxo-3-&lsqb;3-(5,6,7,8-tetrahydro-&lsqb;1,8&rsqb;naphthyridin-2-yl)-propyl&rsqb;imidazolidin-1-yl&rcub;-3(S)-(6-methoxy-pyridin-3-yl)-propionic acid in the form of a hemihydrate.

Process and intermediates for the preparation of imidazolidinone &agr;v integrin antagonists

Crystalline 2-hydroxymethyl carbapenem intermediate compounds and process for synthesis thereof

Process for synthesizing carbapenem intermediates

The present invention is directed to an improved process for preparing the phenylacetic acid side chain of the compound of the formula ##STR1## This compound exhibits utility as a Class III antiarrhythmic agent.

Side chains synthesis for an anthiarrhythmic compound

The invention encompasses a novel process for the formation of enantiomerically enriched mixtures of compounds of Formula I, which are useful precursors in the synthesis of phosphodiestersae IV inhibitors.

Process for phosphodiesterase IV inhibitors

Intermediates of structural formula ##STR1## can be made by reacting a primary or secondary amine with glycosidol or an activated derivative thereof. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.

Process for making HIV protese inhibitors

The invention provides a process for regioselective substitution of trifluorobenzoate/trifluorobenzonitrile to afford the difluorobenzoate/difluorobenzonitrile in good yields. The resulting difluorobenzoate/difluorobenzonitrile can again be regioselectively substituted with a second nucleophile to give monofluorobenzoate/monofluorobenzonitrile also in good yields. This process is particularly useful for forming key intermediates in the synthesis of oxytocin antagonist compounds.

Process for regioselective substitution of trifluorobenzoate or

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Doylestown, PA, United States of America

Kenneth M Wells