Merck + Co., Inc.

Merck Sharp + Dohme Corp.

Msd K.k.

Yaling Wang

Nobuyoshi Yasuda

Shinji Kato

Kenneth M Wells

Robert Wenslow

Hisaki Kojima

Makoto Ishikawa

Masashi Kawasaki

Nobuaki Nonoyama

David M Tellers

Zhiguo Jake Song

Artis Klapars

Toshihiro Wada

Yi Xiao

Steven A Weissman

Kevin Campos

Yuji Haga

Chunhua Yang

Wei Xu

Lisa F Frey

Nelo R Rivera

Fuyuki Yamamoto

Taketo Ikeno

Mark S Jensen

Laura Marie Artino

David R Lieberman

Aaron J Moment

Russell R Ferlita

Jennifer R Foley

Cheng-Yi Chen

J Christopher McWilliams

Michael Palucki

Andrey V Peresypkin

Sachin Lohani

Alex Minhua Chen

Nobuya Satake

C Scott Shultz

Paolo Avalle

Robert M Wenslow

Shuntaro Furukawa

Wataru Minagawa

Naotaka Sawada

Debra J Wallace

Kazuki Shigemori

Keisuke Kamei

Peter Yehl

Peter Mullens

The present invention relates to synthetic processes useful in the preparation of macrocyclic compounds of Formula (I) that are useful as inhibitors of the hepatitis C virus NS3 protease and have application in the treatment of conditions caused by the hepatitis C virus. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation. 

Processes for preparing protease inhibitors of hepatitis C virus

The present invention relates to a process for producing a hydrate of 3-(2,6-dichlorophenyl)-4-imino-7-[(2'-methyl-2&#x2032;,3&#x2032;-dihydro-1&#x2032;H-spiro[cyclopropane-1,4&#x2032;-isoquinolin]-7&#x2032;-yl)amino]-3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one (Compound A) or of a pharmaceutically acceptable salt of Compound A and a crystalline form of Compound A or of a pharmaceutically acceptable salt of Compound A, which are useful in the field of treatment of various cancers as a kinase inhibitor, especially as a Weel kinase inhibitor.

Process for producing bicycloaniline derivatives

This invention relates to salt forms of the compound N-[(2R)-1,4-dioxan-2-ylmethyl]-N-methyl-N'-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]sulfamide, an inhibitor of tyrosine kinases, in particular the receptor tyrosine kinase MET, that are useful in the treatment of cellular proliferative diseases, for example cancer, hyperplasias, restenosis, cardiac hypertrophy, immune disorders and inflammation. In particular, the invention relates to the sodium salt of N-[(2R)-1,4-dioxan-2-ylmethyl]-N-methyl-N&#x2032;-[3-(1-methyl-1H-pyrazol-4-yl)-5-oxo-5H-benzo[4,5]cyclohepta[1,2-b]pyridin-7-yl]sulfamide.

Tyrosine kinase inhibitors

The present invention relates to a process for producing crystalline trans-N-[1-(2-fluorophenyl)-S-pyrazoly]-3-ox-ospiro[6-azaisobenzofuran-1(3H),1'-cyclohexane]-4&#x2032;-carboxamide and novel salts, hydrates and polymorphs thereof.

Synthesis and crystalline forms of NPY5 antagonist

The present invention is directed to a practical process for the preparation of an enamide (II) by palladium catalyzed coupling of a primary amide (IV) with a compound of structural formula (III), as shown below: As well as to crystalline forms of a compound produced by this process, in particular, an anhydrous crystal form, Form B, and crystalline solvates falling into three patterns, Type 1, Type 2, and Type 3, and crystalline intermediate compounds produced in the process. Still further, the present invention relates to the stereoselective reduction of the tetrasubstituted enamide (II) to the corresponding amide (I).

Formation of tetra-substituted enamides and stereoselective reduction thereof

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

The present invention relates to novel crystalline forms of the integrin &agr;v&bgr;3 antagonist 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.

Crystalline forms 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

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Westfield, NJ, United States of America

Yaling Wang