Hoffmann-La Roche Inc.

Roche Palo Alto LLC

Biocryst Pharmaceuticals, Inc.

Thomas Cleary

Thimma R Rawalpally

Yaohui Ji

Olaf Grassmann

Roland Meier

Pingsheng Zhang

Jason Yang

Shan-Ming Kuang

Franziska E Rohrer

Miall Cedilote

Doreen Miller

Regina Moog

Alexander Glomme

Hans Iding

Keshab Sarma

Gary R Lee

Gary Bartley

John Lang

John F Lang

The present disclosure provides novel hemi- and mono-salts of 7-[(3R,4R)-3-Hydroxy-4-hydroxymethyl-pyrrolidin-1-ylmethyl]-3,5-dihydro-pyrrolo[3,2-]pyrimidin-4-one (Compound 1) with various organic and inorganic acids. In one embodiment, the organic acid is a C4 organic diacids. The present disclosure further provides novel methods for preparing these salts. The novel monohydrates hemisalts of the C4 organic diacids are isostructural and can be prepared with different properties. Multiple acids can be used simultaneously and the proportion of acids can be varied offering the opportunity to select hemi-salts of compound 1 with desired properties.

Useful pharmaceutical salts of 7-[(3R, 4R)-3-Hydroxy-4-hydroxymethyl-pyrrolidin-1-ylmethyl]-3, 5-dihydro-pyrrolo [3, 2-D] pyrimidin-4-one

The present invention provides novel methods for preparing 5-(trifluoromethoxy)-1H-3-indazolecarboxylic acid (3), which is a useful precursor for the preparation of bicyclic-5-trifluoromethoxy-1H-indazole-3-carboxylic acid amides of Formula (1). Compounds of Formula (1) are active as agonists and partial agonists of the nicotinic &#x3b1;-7 receptor and are being studied for their use in the treatment of disease conditions associated with defective or malfunctioning nicotinic acetylcholine receptors, especially of the brain, such as for the treatment of Alzheimer's disease and schizophrenia, as well as other psychiatric and neurological disorders. The present methods are useful for preparing compound (3) on scale up levels.

Diazonium-free method to make an indazole intermediate in the synthesis of bicyclic 5-(trifluormethoxy)-1H-3-indazolecarboxylic acid amides

The present invention relates to mono-sulfate and hemi-sulfate salts of 2-Chloro-4-[1-(4-fluoro-phenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]-pyridine, to crystalline and amorphous forms thereof and to their use in pharmaceutical formulations.

Solid forms of 2-chloro-4-[1-(4-fluoro-phenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]-pyridine

The present invention relates to the mono-sulfate salt, crystalline forms A and B of the mono-sulfate salt, an amorphous form of the mono-sulfate salt, hemi-sulfate salts, and a crystalline form A of the hemi-sulfate salt of the compound 2-chloro-4-[1-(4-fluoro-phenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]-pyridine.

Solid forms of 2-Chloro-4-[1-(4-fluoro-phenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]-pyridine

The present invention provides novel methods for preparing a key intermediate, 3,5-di-O-acyl-2-fluoro-2-C-methyl-D-ribono-&#x3b3;-lactone (2), for the preparation of 1-(2-deoxy-2-fluoro-2-C-methyl-&#x3b2;-D-ribofuranosyl)cytosine (1), which is a potent and selective anti-hepatitis C virus agent.

Process for the preparation of 3,5-di-O-acyl-2-fluoro-2-C-methyl-D-ribono-gamma-lactone

The present invention provides a novel method for preparing a key intermediate, 3-amino-pentan-1,5-diol (2), which is useful for the preparation of 6-(2,4-difluorophenoxy)-2-[3-hydroxy-1-(2-hydroxyethyl)-propylamino]-8-methyl-8H-pyrido[2,3-d]pyrimidine-7-one (1) a MAP-kinase inhibitor useful in the treatment of rheumatoid arthritis.

Process for the preparation of 3-amino-pentan-1,5-diol

A method of nitrating a compound selected from the group consisting of is provided.

Mono-nitration of aromatic compounds via nitrate salts

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Florence, SC, United States of America

Thomas Cleary