Denali Therapeutics Inc.

Genentech, Inc.

Array Biopharma Inc.

Genetech, Inc.

Green Tech Corporation

F. Hoffmann-la Roche Ag

Travis Remarchuk

Anantha R Sudhakar

Keith Lee Spencer

Peter J Stengel

Sagar Raj Shakya

Jonathan W Lane

C Gregory Sowell

Chong Han

David Askin

Zachary Kevin Sweeney

Anthony A Estrada

Javier De Vicente Fidalgo

Jianwen A Feng

Brian M Fox

Maksim Osipov

Jeffrey Stults

Robert A Craig, Ii

Katrina W Lexa

Christopher R H Hale

Frederic St-Jean

Francis Gosselin

Sushant Malhotra

Srinivasan Babu

Scott J Savage

Herbert Yajima

Remy Angelaud

Danial Beaudry

Yingqing Ran

Danial R Beaudry

Diane E Carrera

Fredric St-Jean

Diane Carrera

The present disclosure relates to methods of making LRRK2-inhibiting, pyrimidinyl-4-aminopyrazole compounds and intermediates of formulae I and IV: The compounds are useful as LRRK2 inhibitors in the treatment of LRRK2 mediated diseases, and as intermediates for their manufacture.

Process for the preparation of pyrimidinyl-4-aminopyrazole compounds

The present disclosure relates generally to eukaryotic initiation factor 2B modulators, or a pharmaceutically acceptable salt, stereoisomer, mixture of stereoisomers or prodrug thereof, and methods of making and using thereof.

Modulators of eukaryotic initiation factor 2B, compositions and methods

The present disclosure relates to crystalline polymorph and amorphous forms of 2-methyl-2-(3-methyl-4-(4-(methylamino)-5-(trifluoromethyl)pyrimidin-2-ylamino)-1H-pyrazol-1-yl)propanenitrile or solvates, tautomers, and pharmaceutically acceptable salts or cocrystals thereof, and processes for their preparation.

Polymorphs and solid forms of a pyrimidinylamino-pyrazole compound, and methods of production

The invention provides processes for preparing a compound of formula I and salts thereof, wherein Ris defined herein, and compounds and intermediates of said formula.

Process for making hydroxylated cyclopentylpyrimidine compounds

The present invention relates to crystalline polymorphs of (2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide (GDC-0032, taselisib), methods of use, and processes of preparing thereof.

Polymorphs of 2-(4-(2-(1-(isopropyl-3-methyl-1H-1,2,4,triazol-5-yl)-5,6-dihydrobenzo[f] imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide, methods of production, and pharmaceutical uses thereof

The invention provides processes for preparing a compound of formula I and salts thereof, wherein Ris defined herein, and compounds and intermediates of said formula. 

The invention provides new processes for making and purifying salts of hydroxylated cyclopentapyrimidine compounds, which are useful as AKT inhibitors used in the treatment of diseases such as cancer, including the monohydrochloride salt of (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one.

Process of making hydroxylated cyclopentapyrimidine compounds and salts thereof

The invention provides new processes for making and purifying hydroxylated cyclopenta[d]pyrimidine compounds, which are useful for the treatment of diseases such as cancer as AKT protein kinase inhibitors, including the compound (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one.

Processes are described for the preparation of PI3K inhibitor, GDC-0032, Formula I, having the structure: 

Process for making benzoxazepin compounds

The invention provides new processes for making and purifying amino acid compounds, which are useful in the preparation of AKT inhibitors used in the treatment of diseases such as cancer, including the compound (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one.

Process for making amino acid compounds

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South San Francisco, CA, United States of America

Travis Remarchuk