Johnson Matthey Public Limited Company

Inflazyme Pharmaceuticals Ltd.

Nektar Therapeutics

Rgenix, Inc.

Nicholas D Paschalides

Mahmoud Mirmehrabi

David L Burgoyne

Yaping Shen

Yuanlin Zhou

Eugene W Kelleher

Kishore Ramachandran

Gueijun Ji

Patricia Andres

Eduardo J Martinez

Aniruddh Singh

Padmini Kavuru

Andreas G Grill

Yogesh Datar

Ramakrishna Gadiraju

Bruce Andrew Kowalczyk

Gabriel Christian Kuklis

Stephen A Wald

The present invention relates to new pharmaceutical salts of &#x3b2;-GPA which exhibit improved physical properties. In particular, the invention relates to salts of &#x3b2;-GPA with improved flow properties (e.g., improved Carr's index and/or Hausner ratio) such as fumarate salts, succinate salts, and oxalate salts. The invention also relates to pharmaceutical compositions including a pharmaceutically effective amount of one or more salts of &#x3b2;-GPA, as well as methods of treating cancer including administration of a formulation including a &#x3b2;-GPA salt of the invention to a subject in need thereof.

Pharmaceutically acceptable salts of B-guanidinopropionic acid with improved properties and uses thereof

Solid forms of certain opioid agonists are provided herein. Methods of preparing the solid forms, methods of using the solid forms, and pharmaceutical compositions comprising the solid forms are also provided herein.

[object Object]

The present disclosure is directed to crystalline forms of morphine sulfate and pharmaceutical compositions comprising any of the crystalline forms of morphine sulfate. Also provided are processes for the preparation of crystalline forms of morphine sulfate.

Crystalline forms of morphine sulfate

Steroids containing a cyclohexene moiety are efficiently oxidized to the corresponding &#x3b1;,&#x3b2;-unsaturated ketone using copper iodide and t-butyl hydroperoxide. A steroid compound containing the &#x3b1;,&#x3b2;-unsaturated ketone structure is efficiently converted to the corresponding vicinal diol using a hydroborating reagent followed by oxidative workup, e.g., borane followed by sodium perborate. Benzoyl and substituted benzoyls are superior protecting groups for hydroxyl groups present in the compounds.

Process improvements in steroid chemistry

Steroids containing a cyclohexene moiety are efficiently oxidized to the corresponding &agr;,&bgr;-unsaturated ketone using copper iodide and t-butyl hydroperoxide. A steroid compound containing the &agr;,&bgr;-unsaturated ketone structure is efficiently converted to the corresponding vicinal diol using a hydroborating reagent followed by oxidative workup, e.g., borane followed by sodium perborate. Benzoyl and substituted benzoyls are superior protecting groups for hydroxyl groups present in the compounds.

Process for the production of 6,7-diols of steroidal compounds

Growing community of inventors

Marlborough, MA, United States of America

Nicholas D Paschalides