Genentech, Inc.

Agouron Pharmaceuticals, Inc.

Sumitomo Chemical Company, Limited

F. Hoffmann-La Roche Ag

Qingping Tian

Srinivasan Babu

Francis Gosselin

Zhigang Cheng

Haiming Zhang

Sushant Malhotra

Mark E Reynolds

Stephan Bachmann

Ngiap-Kie Lim

Alec Fettes

Herbert Yajima

Theresa Cravillion

Alexander Gmehling

Danial Beaudry

Steven Lee Bender

Scott J Savage

Michael J Melnick

Terence J Moran

Travis Paul Remarchuk

Raymond Dagnino, Jr

Junhua Tao

Naresh Nayyar

Lennert J Mitchell, Jr

Reinhard Reents

Ursula Hoffmann

Pirmin Hidber

Takashi Miki

Jayaram Kasturi Srirangam

Mark Bryan Mitchell

Theresa Humphries

James Edward Saenz

Yasuharu Shimasaki

Brigitte Leigh Ewanicki

Erik Jon Flahive

Annie Judith Kasparian

Michael David Perry

Shu Yu

Stacy Ann O'Neill-Slawecki

Nebojsa Slobodan Stankovic

Bing Shi

Neal William Sach

Methods for preparing the Bruton's Tyrosine Kinase ('BTK') inhibitor compound 2-{3'-hydroxymethyl-1-methyl-5-[5-((S)-2-methyl-4-oxetan-3-yl-piperazin-1-yl)-pyridin-2-ylamino]-6-oxo-1,6-dihydro-[3,4&#x2032;]bipyridinyl-2&#x2032;-yl}-7,7-dimethyl-3,4,7,8-tetrahydro-2H,6H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1-one are provided. Methods for preparing tricyclic lactam compounds are also provided.

Process for preparing BTK inhibitors

Process methods for making the dual mTOR/PI3K inhibitor GDC-0980, named as (S)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one, having the structure:  and stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof.

Process for making thienopyrimidine compounds

The present invention relates to a method for manufacturing a boronic acid ester compound, characterized by reacting an aryl halide compound and a diboron ester compound in the presence of a nitrogen-containing organic base, a nickel catalyst, a phosphine compound and a solvent. According to the manufacturing method of the present invention, even if a nickel catalyst is used as the catalyst, a desired boronic acid ester compound can be obtained in a sufficiently high yield. Furthermore, even if aryl chloride or aryl bromide having relatively low price and low reactivity, was used as the aryl halide compound, a desired boronic acid ester compound can be obtained in a sufficiently high yield.

Method for manufacturing a boronic acid ester compound

The invention provides processes of preparing, separating, and purifying PI3K inhibitor, Formula I and II compounds, and novel intermediates for preparing Formula I and II compounds.  

The invention provides processes of preparing, separating, and purifying PI3K inhibitor, Formula (I) and (II) compounds, and novel intermediates for preparing Formula (I) and (II) compounds. 

The present invention relates to methods for preparing indazole compounds of formula I, which are useful as modulators and/or inhibitors of protein kinases. The present invention also relates to intermediate compounds useful in the preparation of compounds of formula I.

Methods of preparing indazole compounds

Efficient synthetic routes for the preparation of rhinovirus protease inhibitors of formula I, as well as key intermediates useful in those synthetic routes. These compounds of formula I, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.

Efficient synthetic routes for the preparation of rhinovirus protease inhibitors and key intermediates

Efficient synthetic routes for the preparation of rhinovirus protease inhibitors of formula I, as well as key intermediates useful in those synthetic routes. These compounds of formula I, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses

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Qingping Tian