Apotex Inc.

Alphora Research Inc.

Sandoz Ag

Fabio E S Souza

Allan W Rey

Boris Gorin

Bahareh Khalili

Ming Pan

Annyt Bhattacharyya

Avedis Karadeolian

Alexander J Stirk

Ricardo Orprecio

Jason A Bexrud

Alena Rudolph

Katherine A Rantanen

Huzaifa Rangwala

Yajun Zhao

Dino Alberico

Mohammed Abdul Raheem

Stuart P Green

Minh T N Nguyen

Jenny L Gerster

Michael R Emmett

Siva Ramarao Kakani

Teng Ko Ngooi

Gamini Weeratunga

Prabhudas Bodhuri

Alfredo Paul Ceccarelli

Kangying Li

Jason Edward Field

Wancheng Guo

Robert Jordan

Navindra Jainarine Ramjit

Fatemeh Mohammadpourmir

Dineshkumar Patel

Jingda Zhang

Tharsika Tharmanathan

Kun Cheng

Tracey Jende-Tindall

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 novel crystalline forms of zuclomiphene citrate. Specific crystalline forms provided by the present invention include zuclomiphene citrate Forms APO-I, APO-II, APO-III, and APO-IV. Also provided are pharmaceutical compositions including the zuclomiphene citrate crystalline forms, processes for the preparation thereof and the use of these forms in the treatment of a disorder selected from the group including osteoporosis, bone fractures, loss of bone mineral density (BMD) and hot flashes in a subject suffering therefrom.

Crystalline forms of zuclomiphene citrate

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 zuclomiphene salts, zuclomiphene binaphthyl hydrogen phosphate salt (1-A)&#xb7;(BPA) and zuclomiphene oxalate salt (1-A)&#xb7;(OXL), crystalline forms thereof and processes for the preparation thereof.

Zuclomiphene salts and crystalline forms thereof

The present invention provides a novel crystalline form of remdesivir, remdesivir Form APO-I, including remdesivir and dimethyl sulfoxide, compositions and processes for the preparation thereof, the use of this crystalline form in the treatment of a viral infection, and methods of treating viral infections using the same, and in particular, a viral infection caused by Severe Acute Respiratory Syndrome coronavirus 2 (SARS-CoV-2).

Crystalline form of Remdesivir

The present invention provides crystalline forms of Acalabrutinib, Specific crystalline forms provided by the present invention include Acalabrutinib Form APO-I, a co-crystal of Acalabrutinib and urea; APO-II, a co-crystal of Acalabrutinib and nicotinamide; APO-III, a co-crystal of Acalabrutinib and L-sorbitol; APO-IV, a crystalline form of Acalabrutinib; and APO-V, a co-crystal of Acalabrutinib and urea.

Crystalline forms of Acalabrutinib

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 novel crystalline forms of Ponatinib hydrochloride. Specific crystalline forms provided by the present invention include Ponatinib hydrochloride Form APO-I, APO-III and APO-IV, each of which is obtained from acetonitrile/formic acid solutions. Additionally, Form APO-V is provided, which is obtained from concentrated hydrochloric acid.

Crystalline forms of Ponatinib hydrochloride

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 a novel crystalline form of Lumacaftor, specifically Lumacaftor Form APO-I, a co-crystal of Lumacaftor and nicotinamide, compositions including this crystalline form, and processes for the preparation of this crystalline form.

Crystalline form of lumacaftor

The present invention provides a novel crystalline form of Eluxadoline, Eluxadoline Form APO-I, a co-crystal of Eluxadoline and methyl nicotinate, compositions and processes for the preparation thereof, and the use of this crystalline form in the treatment of opioid-modulated disorders, and in particular, gastrointestinal disorders, including irritable bowel syndrome with diarrhea (IBS-D).

Crystalline form of Eluxadoline

The present invention provides a novel crystalline form of Olaparib comprising Olaparib and benzyl alcohol, compositions thereof, and the use of this crystalline form in the treatment of cancers, such as germline BRCA-mutated (gBRCAm) advanced ovarian cancer.

Crystalline form of Olaparib

The present invention provides crystalline forms of Deutetrabenazine. Specific crystalline forms provided by the present invention include Deutetrabenazine Form APO-I, a co-crystal of Deutetrabenazine and quercetin, and Deutetrabenazine Form APO-II, a co-crystal of Deutetrabenazine and luteolin. Also provided are pharmaceutical compositions including the Deutetrabenazine crystalline forms, and the use of these forms in the treatment of tardive dyskinesia and chorea associated with Huntington's disease.

Crystalline forms of benzoquinoline inhibitors of vesicular monoamine transporter 2

The present invention provides a novel crystalline form of Ribociclib succinate, Ribociclib succinate Form APO-I, including Ribociclib succinate, benzyl alcohol and water, compositions thereof, processes for the preparation thereof, and the use of this crystalline form in the treatment of conditions associated with increased CDK4/6 kinase activity, and in particular, cancers, including certain forms of breast cancer.

Growing community of inventors

Mississauga, Canada

Fabio E S Souza