Rexahn Pharmaceuticals, Inc.

Colucid Pharmaceuticals, Inc.

Summit (oxford) Limited

Jean-Francois Carniaux

Jonathan Cummins

Deog Joong Kim

Yi Wang

Petra Dieterich

Eliezer Falb

Vikram Chandrakant Purohit

Leigh Andre Pearcey

Haifeng Yin

Laura Trespidi

Francis X Wilson

Peter Timmins

Vikrain Chandrakant Purohit

The present invention relates to solid tablet oral dosage forms of 2,2'-di(pyridin-4-yl)-1H,1′H-5,5′-bibenzo[d]imidazole (which may also be known as 2,2′-di-4-pyridinyl-6,6′-bi-1H-benzimidazole; 5,5′-bis[2-(4-pyridinyl)-1H-benzimidazole]; 2,2′-bis(4-pyridyl)-3H,3′H-5,5′-bibenzimidazole; or 2-pyridin-4-yl-6-(2-pyridin-4-yl-3H-benzimidazol-5-yl)-1H-benzimidazole), referenced herein by the INN name ridinilazole, and pharmaceutically acceptable derivatives, salts, hydrates, solvates, complexes, bioisosteres, metabolites or prodrugs thereof.

Solid tablet dosage form of ridinilazole

Processes for the preparation of 4-amino-1-((1S,4R,5S)-2-fluoro-4,5-dihydroxy-3 -hydroxymethyl-cyclopent-2-enyl)-1H-pyrimidin-2-one(13, RX-3117) and its intermediates are described. 

Process for the preparation of 4-amino 1-((1S,4R,5S)-2-fluoro-4,5-dihydroxy-3-hydroxymethyl-cyclopent-2-enyl)-1H-pyrimidin-2-one

Processes for the preparation of 4-amino-1-((1S,4R,5S)-2-fluoro-4,5-dihydroxy-3-hydroxymethyl-cyclopent-2-enyl)-1H-pyrimidin-2-one (13, RX-3117) and its intermediates are described. 

Process or the preparation of 4-amino 1-((1S,4R,5S)-2-fluoro-4,5-dihydroxy-3-hydroxymethyl-cyclopent-2-Enyl)-1H-pyrimidin-2-one

Process for the preparation of 4-amino-1-((1S,4R,5S)-2-fluoro-4,5-dihydroxy-3-hydroxymethyl-cyclopent-2-enyl)-1H-pyrimidin-2-one

The present invention provides a novel polymorph of the hemisuccinate salt of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide (Form A) characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure. This polymorph is useful in pharmaceutical compositions, for example, for the treatment and prevention of migraine. The invention also provides a process for the synthesis of pyridinoylpiperidine compounds of Formula I in high yield and high purity. In particular, the provides a process for the preparation of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide, its hemisuccinate salt and polymorph (Form A).

Compositions and methods of synthesis of pyridinolypiperidine 5-HT1F agonists

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Abingdon, United Kingdom

Jean-Francois Carniaux