Arqule, Inc.

University of Massachusetts

Craig G Bates

David P Reed

Jianmin Mao

Dhandapani Venkataraman

Jian-Xie Chen

Pranorm Saejueng

Jean-Marc Lapierre

Manish Tandon

Kiyoshi Nakayama

Yusuke Ota

Yoshihiro Shibata

Hiroaki Inagaki

Sudharshan Eathiraj

Takayuki Momose

Masahiro Ota

Tomoyuki Tsunemi

Takashi Odagiri

Erika Volckova

Rattan K Gujadhur

The present application relates to methods of preparing Compound A: or a salt thereof, and a polymorph of Compound A dihydrochloride salt: 

Methods for preparing substituted 5,6-dihydro-6-phenylbenzo[f]isoquinolin-2-amine

The application relates to a compound of Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, or tautomer thereof, which modulates the activity of BTK, a pharmaceutical composition comprising a compound of Formula (I), and a method of treating or preventing a disease in which BTK plays a role.

Amino-pyrrolopyrimidinone compounds and methods of use thereof

The present application provides solid forms of (2-chloro-4-phenoxyphenyl)(4-(((3R,6S)-6-(hydroxymethyl)tetrahydro-2H-pyran-3-yl)amino)-7H-pyrrolo[2,3-d]pyrimidin-5-yl)methanone free base, and methods of preparing and using the same.

Solid forms of tetrahydropyranyl amino-pyrrolopyrimidinone compounds

The present application provides solid forms of (R)-6-(2-fluorophenyl)-N-(3-(2-(2-methoxyethylamino)ethyl)phenyl)-5,6-dihydrobenzo[h]quinazolin-2-amine dihydrochloride, and methods of preparing and using same.

Solid forms of substituted 5,6-dihydro-6-phenylbenzo[F]isoquinolin-2-amine compounds

Methods for preparing substituted 5,6-dihydro-6-phenylbenzo[F]isoquinolin-2-amine

The present invention is directed to a processes for the synthesis of 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine: 

Process of preparing 3-(3-(4-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-B]pyridin-2-YL)pyridin-2-amine

Process of preparing 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-B]pyridin-2-yl)pyridin-2-amine

The present application relates to salts of Compound A, 3-(3-(4-(1-aminocyclobutyl) phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine, solid state forms of Compound A free base or of salts of Compound A, amorphous forms of Compound A free base or of salts of Compound A, crystalline forms of Compound A free base or of salts of Compound A, polymorphs of Compound A free base or of salts of Compound A, and mesomorphs of Compound A free base or of salts of Compound A. The present application also relates to pharmaceutical compositions comprising these salts, solid state forms, amorphous forms, crystalline forms, polymorphs, or mesomorphs of Compound A free base or of salts of Compound A. The present application provides methods for preparing these salts, solid state forms, amorphous forms, crystalline forms, polymorphs, or mesomorphs of Compound A free base or of salts of Compound A.

Salts and polymorphs of a substituted imidazopyridinyl-aminopyridine compound

A copper(I)-catalyzed procedure for the synthesis of benzo[b]heterocycles. This protocol can be used to synthesize a variety of 2-arylbenzo[b]furans and indoles in good to excellent yields. This method can tolerate a variety of functional groups, does not require the use of expensive additives and is palladium-free.

Methods and systems for preparing fused heterocyclic compounds using copper(I) catalysts

A copper(I) bi-dentate ligand complex-catalyzed procedure for synthesis of 1,3-enynes. The methods and/or systems of this invention afford a variety of enynes, tolerate a variety of sensitive functional groups, and can be employed without resort to expensive palladium reagents.

Methods of 1,3-enyne preparation using copper (I) catalysts

A mild, palladium-free synthetic protocol for the cross-coupling reaction of vinyl or aryl iodides and thiols or selenols using, in certain embodiments, 10 mol % CuI and 10 mol % neocuproine, with NaOt-Bu as the base, in toluene at 110 &#xb0; C. A variety of vinyl/aryl sulfides and vinyl/aryl selenides can be synthesized in excellent yields from readily available iodides and thiols or selenols.

Growing community of inventors

South Hadley, MA, United States of America

Craig G Bates