Janssen Pharmaceutica Nv

Les Laboratoires Servier

Theravance Biopharma R&d IP, LLC

Noramco Gmbh

Vit Lellek

Neelakandha S Mani

Daniel J Pippel

Susanne Lochner

Lana K Young

Adrian Maurer

Diego Fernando Domenico Broggini

Matteo Conza

Diego Broggini

Christoph Strassler

Roger Fassler

Xiaojun Huang

Hartmut B Zinser

Dimitar Filipov

Stephen Roseblade

Christian Pater

Bjorn Gielen

Anja Huste

Norbert Kraut

Hartmut Zinser

Adrian Mauer

Roger Fässler

Christoph Strässler

The present disclosure provides processes for preparing a crystalline form of 3-((1R,3s,5S)-3-((7-((5-methyl-1H-pyrazol-3-yl)amino)-1,6-naphthyridin-5-yl)amino)-8-azabicyclo[3.2.1]octan-8-yl)propanenitrile and related intermediate compounds.

Processes for preparing a pan-JAK inhibitor and related intermediate compounds

The present invention is directed to novel processes for the preparation of histamine H3 receptor modulators, in the treatment of for example, cognitive disorders, sleep disorders and/or psychiatric disorders.

Process for the preparation of histamine H3 receptor modulators

The present invention is directed to a process for the preparation of opioid compounds such as buprenorphine, naltrexone, naloxone, nalbuphone, nalbuphine, and the like.

Process for the preparation of opioid compounds

The present invention is directed to novel processes for the preparation of histamine H3 receptor modulators, in the treatment of for example, cognitive disorders, sleep disorders and/or psychiatric disorders. 

Disclosed are two new crystalline forms, &#x3b4; and &#x3b5;, of perindopril erbumine. Those forms are suitable as therapeutic active substances for medicaments for the treatment of cardiovascular diseases, especially high blood pressure and heart failure. The &#x3b5; crystalline form is obtained in the crystallization of perindopril erbumine at from 30 to 45&#xb0; C., preferably from 34 to 45&#xb0; C., from MTBE containing from 1.5 to 2.5% (v/v) water; the crystallization is advantageously carried out with stirring. If the water is then removed, advantageously by azeotropic distillation, preferably at from 35 to 37&#xb0; C., and stirring is then continued for at least 15 h at from 30 to 45&#xb0; C., preferably from 35 to 37&#xb0; C., the &#x3b5; crystalline form is converted to the &#x3b4; crystalline form. The &#x3b4; crystalline form can also be obtained by stirring the &#x3b1; or &#x3b2; crystalline form at from 33 to 38&#xb0; C. in tert.-butyl methyl ether containing from 0.9 to 1.4% (v/v) water with seeding with the &#x3b4; crystalline form. The &#x3b5; crystalline form can also be obtained by stirring the &#x3b1; or &#x3b2; crystalline form at from 28 to 35&#xb0; C. in tert.-butyl methyl ether containing from 0.9 to 1.4% (v/v) water with seeding with the &#x3b5; crystalline form; or by stirring the &#x3b1; or &#x3b2; crystalline form at from 35 to 38&#xb0; C. in tert.-butyl methyl ether containing from 1.5 to 2.0% (v/v) water.

Crystalline forms of perindopril erbumine

Disclosed are two new crystalline forms, &#x3b4; and &#x3b5;, of perindopril erbumine. Those forms are suitable as therapeutic active substances for medicaments for the treatment of cardio-vascular diseases, especially high blood pressure and heart failure. The &#x3b5; crystalline form is obtained in the crystallization of perindopril erbumine at from 30 to 45&#xb0; C., preferably from 34 to 45&#xb0; C., from MTBE containing from 1.5 to 2.5% (v/v) water; the crystallization is advantageously carried out with stirring. If the water is then removed, advantageously by azeotropic distillation, preferably at from 35 to 37&#xb0; C., and stirring is then continued for at least 15 h at from 30 to 45&#xb0; C., preferably from 35 to 37&#xb0; C., the &#x3b5; crystalline form is converted to the &#x3b4; crystalline form. The &#x3b4; crystalline form can also be obtained by stirring the &#x3b1; or &#x3b2; crystalline form at from 33 to 38&#xb0; C. in tert.-butyl methyl ether containing from 0.9 to 1.4% (v/v) water with seeding with the &#x3b4; crystalline form. The &#x3b5; crystalline form can also be obtained by stirring the &#x3b1; or &#x3b2; crystalline form at from 28 to 35&#xb0; C. in tert.-butyl methyl ether containing from 0.9 to 1.4% (v/v) water with seeding with the &#x3b5; crystalline form; or by stirring the &#x3b1; or &#x3b2; crystalline form at from 35 to 38&#xb0; C. in tert.-butyl methyl ether containing from 1.5 to 2.0% (v/v) water.

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