Array Biopharma Inc.

Genentech, Inc.

Arena Pharmaceuticals, Inc.

Astrazeneca Ab

Astrazeneca Sb

Sagar Raj Shakya

Anthony C Blackburn

Jaimie Karyn Rueter

Keith Lee Spencer

Antonio Garrido Montalban

John A DeMattei

Marlon Carlos

Lee Alani Selvey

Peter J Stengel

You-An Ma

James Gair Ford

Mark Allen Hadd

Ryan O Castro

Bruno P Hache

John Leonard

Matthew Charles Evans

Anthony D Piscopio

Chong Han

Travis Remarchuk

Koen Peeters

Simon Mark Pointon

Jonathan W Lane

Timothy John Lilley

C Gregory Sowell

David Askin

Paul Nichols

Michelangelo Scalone

Francis Gosselin

Weidong Liu

Zackary D Crane

Keena Green

Bradley R Barnett

Paul J Nichols

John Demattei

James Gair Astrazeneca Ab Ford

Matthew Charles Astrazeneca Ab Evans

John Astrazeneca Ab Leonard

Timothy John Astrazeneca Ab Lilley

Matthew Charles Pdlsw2 PR&D Office Um2 Astrazeneca Evans

Simon Mark Astrazeneca Ab Pointon

The present invention relates to, inter alia, a novel crystalline free-plate habit or morphology, processes for preparing the crystalline free-plate habit, and uses of the crystalline free-plate habit of the L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta[b]indol-3-yl)acetic acid (Compound 1) in the treatment of S1Preceptor-associated disorders, for example, diseases and disorders mediated by lymphocytes, transplant rejection, autoimmune diseases and disorders, inflammatory diseases and disorders (e.g., acute and chronic inflammatory conditions), cancer, and conditions characterized by an underlying defect in the vascular integrity or that are associated with angiogenesis such as may be pathologic (e.g., as may occur in inflammation, tumor development, and atherosclerosis).

Crystalline l-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(compound1) for use in SIPI receptor-associated disorders

Crystalline L-arginine salt of ()-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(Compound1) for use in S1Preceptor-associated disorders

Crystalline L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3, 4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(compound1) for use in S1Preceptor-associated disorders

Crystalline L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(Compound 1) for use in SIPI receptor-associated disorders

The invention provides processes of preparation thereof useful in the preparation of compounds that can be used as CHK1 inhibitors.

Process for preparing a compound

Crystalline L-arginine salt of (R)-2-(7-(4-cyclopentyl-3-(trifluoromethyl)benzyloxy)-1,2,3,4-tetrahydrocyclo-penta [b]indol-3-yl)acetic acid(Compund1) for use in SIPI receptor-associated disorders

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 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 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.

Provided are processes for the preparation of benzimidazole structures having Formula VIIIb-1: and salts and solvates thereof, wherein Z, X, R, Rand Rare as defined herein. Compounds of Formula VIIIb-1 are useful for the preparation of benzimidazole derivatives.

Processes for preparing benzimidazole compounds

Provided are compounds having Formula VIIIa-1: wherein Z, X, R, Rand Rare as defined herein. Compounds of Formula VIIIa-1 can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.

Benzimidazole compounds

Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ib-1: wherein Z, X, X, X, Rand Rare as defined herein. Compounds of Formula Ib-1 can be used to prepare heterocyclic derivatives such as benzimidazole derivatives.

Process for preparing benzimidazole compounds

Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-2 and their synthetic intermediates: wherein X, X, X, R, Rand Rare as defined herein. Compounds of Formula Ia-2 and their synthetic intermediates can be used to prepare heterocyclic derivatives such as benzimidazole derivatives. 

SNAR process for preparing benzimidazole compounds

Provided are methods for the synthesis of heterocyclic compounds such as benzimidazole carboxylic acid core structures having Formula Ia-1 and their synthetic intermediates: wherein Z, X, X, X, Rand Rare as defined herein. Compounds of Formula Ia-1 and their synthetic intermediates can be used to prepare heterocyclic derivatives such as benzimidazole derivatives. 

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San Diego, CA, United States of America

Sagar Raj Shakya