Apotex Inc.

Avedis Karadeolian

Fabio E S Souza

Allan W Rey

Prabhudas Bodhuri

Alexander J Stirk

Gamini Weeratunga

Boris Gorin

Stuart P Green

Alfredo Paul Ceccarelli

Melanie R A Green

Michael R Emmett

Eduardo Gustavo Cammisa

Fan Wang

Cameron L McPhail

Dineshkumar Patel

Provided is a cabozantinib acesulfamate salt and a crystalline form thereof. Also provided are pharmaceutical compositions including the salt and crystalline form thereof, and methods of treatment of progressive, metastatic medullary thyroid cancer (MTC) or advanced renal cell carcinoma (RCC) that has been treated previously with anti-angiogenic therapy using the cabozantinib acesulfamate salt.

Salt of cabozantinib

The present invention provides novel crystalline forms of tenofovir alafenamide comprising tenofovir alafenamide and two different pharmaceutically acceptable acids, compositions and processes for the preparation thereof, and their use in the treatment of a human immunodeficiency virus (HIV) infection or a hepatitis B virus (HBV) infection.

Crystalline forms of Tenofovir alafenamide

The present invention provides continuous flow processes for the preparation of the compound of Formula (2-A), an intermediate used in the preparation of zuclomiphene or a salt thereof. 

Processes for the preparation of zuclomiphene intermediates

The present invention provides novel crystalline forms of niraparib tosylate. Specific crystalline forms provided by the present invention include niraparib tosylate Form APO-I, a co-crystal of niraparib tosylate and urea, and niraparib tosylate Form APO-II, a co-crystal of niraparib tosylate and oxalic acid. Also provided are pharmaceutical compositions including the niraparib tosylate crystalline forms, and the use of these forms in treatment or prevention of conditions which can be ameliorated by the inhibition of poly(ADP-ribose) polymerase (PARP), in particular certain forms of cancer.

Crystalline forms of niraparib tosylate

The present invention provides processes for the preparation of zuclomiphene, as well as intermediates useful in the preparation thereof. In particular, processes are provided for the carbometallation of diphenylacetylene with a compound of Formula (3) to afford either zuclomiphene or an intermediate which is converted to zuclomiphene. 

Processes for the preparation of zuclomiphene and intermediates thereof

The present invention provides processes for the preparation of Apalutamide (1), as well as intermediates useful in the preparation thereof. In particular, the process of the invention utilizes the intermediate compound of Formula (2), wherein G is OH or a leaving group, which provides improvements over the known processes for the preparation of Apalutamide (1). 

Processes for the preparation of apalutamide and intermediates thereof

The present invention provides processes for the preparation of Lesinurad (1), as well as intermediates useful in the preparation thereof. In particular, the processes of the invention utilize novel intermediate compounds of Formulas (3) and (11), which provide improvements over the known processes for the preparation of Lesinurad (1). 

Processes for the preparation of lesinurad and intermediates thereof

The present invention provides processes for the preparation of Edoxaban (1) and salts thereof, as well as intermediates thereof. In particular, intermediate compounds and/or salts of the Formulae (3), (4), (6-A), (7-A), (8-A), (9-A) and (10-AS) are provided.

Processes for the preparation of edoxaban and intermediates thereof

Solid and crystalline forms of tofacitinib hydrochloride and tofacitinib hydrobromide, processes for the preparation thereof and processes for the use thereof in preparing tofacitinib citrate are provided.

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Cambridge, Canada

Avedis Karadeolian