Theravance, Inc.

Kezar Life Sciences

Theravance Biopharma R&d Ip, LLC

Applied Molecular Transport Inc.

Btg International Limited

Onyx Pharmaceuticals, Inc.

Global Blood Therapeutics, Inc.

Onyx Therapeutics, Inc.

Tobira Therapeutics, Inc.

Thornhill Therapeutics, Inc.

Sean Dalziel

Miroslav Rapta

Leticia Maria Preza

Pierre-Jean Colson

Dustin L McMinn

Henry Johnson

Kirsten M Phizackerley

Evan Lewis

Daniel D Long

Andrew S Thompson

Alexander James Bridges

Randall J Mrsny

John Joseph Koleng, Jr

Tahir Mahmood

Derek Maclean

Sally Rhiannon Postlethwaite

Marvin R Garovoy

James Robert Zeller

Weijun Feng

James Alan Kerschen

Rajendra Tandale

Hyojin Kim

Bittoo Kanwar

Kevin Yin

Robert Murray McKinnell

Lan Jiang

John R Jacobsen

Daisuke Roland Saito

Timothy J Church

Priscilla M Van Dyke

Ioanna Stergiades

Mark Michael Menning

Olivier Dapremont

James Andrew Whitney

Naveen Bejugam

Khushdeep Mangat

Thomas Elliott Jacks

Mouhannad Jumaa

Milind D Choubal

Peter Shwonek

DeMei Leung

Ali Komeyli

Nazila Habibizad

Hyunjung Kim

Dustin Mcminn

John Koleng

Elizabeth Bhatt

Marvin Garovoy

Charles Olson

Sally Postlethwaite

Amir Porat

Leticia Preza

Daniel Long

Disclosed herein are methods for preparing [(2S,3R)—N—[(2S)-3-(cyclopent-1-en-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[(2S)-2-[2-(morpholin-4-yl)acetamido]propanamido]propanamide (compound “G”): and precursors thereof.

Process of preparing a peptide epoxyketone immunoproteasome inhibitor, and precursors thereof

Provided herein is a peptide epoxyketone immunoproteasome inhibitor, crystal forms, salts, and processes for making the same, and formulations thereof.

Crystalline salts of peptide epoxyketone immunoproteasome inhibitor

Disclosed herein are methods for preparing [(2S,3R)-N-[(2S)-3-(cyclopent-1-en-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[(2S)-2-[2-(morpholin-4-yl)acetamido]propanamido]propanamide (compound 'G'): and precursors thereof.

Described herein are cholix-IL-10 fusion proteins, and methods of use thereof, which can be characterized by a distinct response in an individual when administered. This distinct response can comprise changes in levels of one or more markers in the individual and/or co-localization of IL-10 in the lamina propria of the individual. Further described herein, in some embodiments, are oral formulations of the cholix-IL-10 fusion proteins. Described herein are methods for the purification of an IL-10 delivery construct, including methods for refolding and enrichment, which can result in maintenance of a high percentage of the IL-10 delivery constructs in the biologically active dimer form. Described herein are oral formulations configured for site-specific release of a therapeutic protein in the small intestines or colon. In some cases, the therapeutic protein is in the form of a dimer, such as an IL-10 delivery construct capable of crossing the gut epithelium.

Compositions, formulations and interleukin production and purification

Provided herein is a peptide epoxyketone immunoproteasome inhibitor having a structure: Formula (I) wherein X&#x2014; is a counterion, crystal forms, salts, and processes for making the same, and formulations thereof. 

Disclosed herein are methods for preparing [(2S,3R)&#x2014;N-[(2S)-3-(cyclopent-1-en-1-yl)-1-[(2R)-2-methyloxiran-2-yl]-1-oxopropan-2-yl]-3-hydroxy-3-(4-methoxyphenyl)-2-[(2S)-2-[2-(morpholin-4-yl)acetamido]propanamido]propanamide (compound 'G'): and precursors thereof. 

Provided herein are high strength/high drug load tablets comprising 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde ('Compound 1'), dispersible tablets comprising Compound 1, processes of manufacturing such tablets, and methods for treating patients with the tablets. Compound 1 is useful for treating hematological disorders such as sickle cell disease, pulmonary disease such as idiopathic pulmonary fibrosis, and hypoxia and hypoxemia conditions.

Tablets comprising 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde

The invention provides a crystalline sulfate salt of 3-endo-(8-{2-[cyclohexylmethyl-((S)-2,3-dihydroxy-propionyl)amino]ethyl}-8-aza-bicyclo[3.2.1]oct-3-yl)benzamide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline salt forms.

Crystalline forms of an 8-azabicyclo[3.2.1]octane compound

This disclosure provides methods for formulating compositions comprising one or more peptide proteasome inhibitors and a cyclodextrin, particularly a substituted cyclodextrin. As well as cyclodextrin complexation methods of formulating a peptide proteasome inhibitor (e.g., a compound of formula (1)-(5) or a pharmaceutically acceptable salt thereof) with one or more cyclodextrins. Such methods substantially increase the solubility and stability of these proteasome inhibitors and facilitate both their manufacture and administration. For example, homogenous solutions of a compound of formula (5) (carfilzomib) can be obtained at a pharmaceutically useful pH (e.g., about 3.5) and at higher concentrations (e.g., about 5 mg/mL) than could be obtained without one or more cyclodextrins and the processes of complexation between the compound and one or more cyclodextrins provided herein. 

Cyclodextrin complexation methods for formulating peptide proteasome inhibitors

The present disclosure relates to novel crystalline salt forms of lamivudine, methods for the preparation thereof, pharmaceutical compositions thereof, and their use in the treatment of viruses such as Human Immunodeficiency Virus (HIV) infection.

Lamivudine salts

A new method for the synthesis of L-Glutamyl-&#x3b3;-D-Glutamic acid and its use in the synthesis of (2R)-((4S)-carboxy-4-(4,N-(((6S)-2-(hydroxymethyl)-4-oxo-3,4,7,8-tetrahydro-3H-cyclopenta[g]quinazolin-6-yl)-N-(prop-2-ynyl)amino)benzamido)butanamido)pentanedioic acid, 1 are provided. Also provided is an efficient method for the isolation and purification of the trisodium salt of the abovementioned acid, 2, in a form suitable for long term storage and use in a parenteral dosing form.

Efficient peptide couplings and their use in the synthesis and isolation of a cyclopenta (G) quinazoline trisodium salt

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San Francisco, CA, United States of America

Sean Dalziel