Alphora Research Inc.

Apotex Inc.

Akebia Therapeutics, Inc.

Sandoz Ag

Aerpio Therapeutics, Inc.

Ripple Therapeutics Corporation

Eon Labs, Inc.

Sandoz Gmbh

Boris Gorin

Jan Oudenes

Fabio E S Souza

Craig Edward Dixon

Dino Alberico

Christopher M Lanthier

Ricardo Orprecio

John M Janusz

James Densmore Copp

Joshua Clayton

Ming Pan

Jason A Bexrud

Gamini Weeratunga

Prabhudas Bodhuri

Alan Quigbo Lu

Alena Rudolph

Bahareh Khalili

Melanie R A Green

Huzaifa Rangwala

Allan W Rey

Avedis Karadeolian

Annyt Bhattacharyya

Elena Bejan

Teng Ko Ngooi

Robert Jordan

Ian Charles Parrag

Matthew Alexander John Statham

James Denmore Copp

Alfredo Paul Ceccarelli

Jenny L Gerster

Katherine A Rantanen

Michael R Emmett

Fabio Eduardo Silva E Souza

Jason Edward Field

Navindra Jainarine Ramjit

Bruce Goodbrand

Anne Buu Chau Luong

Javier Gonzalez

Alan O'Connor

Elizabeth Poloz

Sascha Jautze

Erich Kraus

Judith Anne Williams

Emma-Louise Elizabeth Moore

Kaarina K Milnes

Alan Qingbo Lu

Emma-Louise Moore

Varghese Rexon

Ryan Beharrilall

Graham McGowan

Fabio Souza

Walter Giust

Fabio Es Souza

Joshua A Clayton

Fabio ES Souza

The disclosure features polymorphs of a prodrug dimer of dexamethasone linked at the 21-C and 21'-C carbons via a carbonate-triethylene glycol-carbonate linker. Also disclosed are pharmaceutical compositions and articles comprising said polymorphs, and the use thereof in the treatment of a disease or condition, e.g. via the extended or controlled release of dexamethasone from said articles.

Crystalline forms of dexamethasone dimers and uses thereof

Disclosed herein are methods and processes of preparing vadadustat and pharmaceutically acceptable salts thereof, and intermediates of formula (I) and their salts useful for the synthesis of vadadustat.

Process for preparing 2-[[5-(3-chlorophenyl)-3-hydroxypyridine-2-carbonyl] amino] acetic acid

Disclosed are processes for preparing [(3-hydroxypyridine-2-carbonyl)amino]-alkanoic acids, derivatives, inter alia, 5-aryl substituted and 5-heteroaryl substituted [(3-hydroxypyridine-2-carbonyl]amino}acetic acids. Further disclosed are methods for making prodrugs of [(3-hydroxypyridine-2-carbonyl)-amino]acetic acids, for example, [(3-hydroxypyridine-2-carbonyl]amino}acetic acid esters and {[3-hydroxypyridine-2-carbonyl]amino}acetic acid amides. The disclosed compounds are useful as prolyl hydroxylase inhibitors or for treating conditions wherein prolyl hydroxylase inhibition is desired.

Process for preparing [(3-hydroxypyridine-2-carbonyl)amino]alkanoic acids, esters and amides

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 Acalabrutinib (1), as well as intermediates useful in the preparation thereof. In particular, processes are provided for coupling of a compound of Formula (5) and 2-butynoic acid in the presence of Carbodiimide (8) to afford Acalabrutinib (1). 

Process for the preparation of acalabrutinib

Process for preparing [(3-hydroxypyridine-2-carbonyl)amino] alkanoic acids, esters and amides

The present invention provides processes for the preparation of Veliparib (1), as well as intermediates useful in the preparation thereof. In particular, processes are provided for the production of the compound of Formula (3), or a salt thereof, and cyclization to afford Veliparib (1). 

Processes for the preparation of Veliparib 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 crystalline forms of Ibrutinib. Specific crystalline forms provided by the present invention include Ibrutinib Form APO-I, an anhydrous form; APO-II, a methyl benzoate solvate of Ibrutinib; and APO-IV, a methyl salicylate solvate of Ibrutinib.

Crystalline forms of ibrutinib

Disclosed is a compound of formula 1, or a pharmaceutically acceptable salt thereof, where R, R, R, R, R, R, R, R, R, R, R, R, Rand Rare as disclosed herein. Also, disclosed is a process for the preparation of the compound of formula 1, or a pharmaceutically acceptable salt thereof, and intermediates used therein. The compound of formula 1 can be used in the preparation of halichondrin analogs, such as Eribulin; and a process for its preparation from the compound of formula 1 is also disclosed. 

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Disclosed are processes for preparing [(3-hydroxypyridine-2-carbonyl)amino]-alkanoic acids, derivatives, inter alia, 5-aryl substituted and 5-heteroaryl substituted [(3-hydroxypyridine-2-carbonyl]amino}acetic acids. Further disclosed are methods for making prodrugs of [(3-hydroxypyridine-2-carbonyl)-amino]acetic acids, for example, {[(3-hydroxypyridine-2-carbonyl]amino}acetic acid esters and {[3-hydroxypyridine-2-carbonyl]amino}acetic acid amides. The disclosed compounds are useful as prolyl hydroxylase inhibittors or for treating conditions wherein prolyl hydroxylase inhibition is desired.

Disclosed is a continuous process for the preparation of ingenol-3-mebutate by reaction, in solution, of ingenol or ingenol anion and angelic anhydride or an equivalent angelylating agent. The continuous flow process is preferably performed in the presence of a base such as lithium hexamethyl disilazane (LiHMDS) and/or an activating agent such as dicyclohexylcarbodiimide (DCC). Also disclosed is a process for recycling the other reaction products obtained in the continuous process for preparation of ingenol-3-mebutate for formation of ingenol, which can then be recycled to form ingenol-3-mebutate. 

Continuous flow process for the preparation of Ingenol-3-mebutate

Synthetic process for preparation of macrocyclic C1-keto analogs of halichondrin B and intermediates useful therein

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Oakville, Canada

Boris Gorin