Neurocrine Biosciences, Inc.

Agouron Pharmaceuticals, Inc.

Scott E Zook

Andrew Carr

Thierry Bonnaud

Kevin McGee

Steven Lee Bender

Michael E Deason

Michael J Melnick

Donald Nicholas Hettinger

Bin-Feng Li

Raymond Dagnino, Jr

Bennett C Borer

Juliette K Busse

Henry R DuBois, Iii

Henry R Dubois

Provided herein are salts of (S)-2-amino-3-methyl-butyric acid (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-yl ester in amorphous and crystalline forms, and processes of preparation, and pharmaceutical compositions thereof. Also provided are methods of their use for treating, preventing, or ameliorating one or more symptoms of neurological disorders and diseases including hyperkinetic movement disorders or diseases.

Valbenazine salts and polymorphs thereof

Provided herein are salts of (S)-2-amino-3-methyl-butyric acid (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]-isoquinolin-2-yl ester in amorphous and crystalline forms, and processes of preparation, and pharmaceutical compositions thereof. Also provided are methods of their use for treating, preventing, or ameliorating one or more symptoms of neurological disorders and diseases including hyperkinetic movement disorders or diseases.

Provided herein are salts of (S)-2-amino-3-methyl-butyric acid (2R,3R,11bR)-3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,l-a]isoquinolin-2-yl ester in amorphous and crystalline forms, and processes of preparation, and pharmaceutical compositions thereof. Also provided are methods of their use for treating, preventing, or ameliorating one or more symptoms of neurological disorders and diseases including hyperkinetic movement disorders or diseases.

Polymorph Form III of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-&#x3b1;]-pyrimidin-7-yl}phenyl)acetamide, and use thereof as a sedative-hypnotic, anxiolytic, anticonvulsant, and/or skeletal muscle relaxant agent. Related compositions and methods are also disclosed, particularly with regard to treatment of insomnia.

Polymorph of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-&#x3b1;]-pyrimidin-7-yl}phenyl)acetamide and compositions and methods related thereto

A novel hydrate form of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5-&#x3b1;]-pyrimidin-7-yl}phenyl)acetamide ('Compound No. 1') and processes related to the use thereof in the synthesis of a polymorphic form of Compound No. 1.

Hydrate of N-methyl-N-(3-{3-[2-thienylcarbonyl]-pyrazol-[1,5&#x3b1;]-pyrimidin-7-yl}phenyl)acetamide and processes and methods related thereto

The invention relates to compounds of the formula:wherein: Z is O or S; V is a divalent radical which together with C* and N forms a ring having six ring atoms, where each of said ring atoms other than C* and N independently is unsubstituted or substituted by a suitable substituent, and at least one of said other ring atoms is a heteroatom selected from O, N and S, and the remainder are carbon atoms; and Ar is an aryl or heteroaryl group; and pharmaceutically acceptable prodrugs, salts and solvates thereof. The invention further relates to pharmaceutically acceptable prodrugs, salts and solvates of these compounds. The invention also relates to methods of inhibiting the activity of metalloproteinases by administering a compound of the formula I or a prodrug, salt or solvate thereof. The invention further relates to pharmaceutical compositions comprising an effective amount of these compounds, prodrugs, salts, and solvates. The invention still further relates to methods and intermediates useful for preparing these compounds, prodrugs, salts, and solvates.

Metalloproteinase inhibitors, pharmaceutical compositions containing them and their pharmaceutical uses, and methods and intermediates useful for their preparation

Metalloproteinase inhibitors-compositions, uses preparation and intermediates thereof

Methods for the preparation of chemical intermediates in the synthesis of HIV-protease inhibitors related to and including nelfinavir mesylate are disclosed. The method of this invention comprises converting tetrohydran derivatives into oxazolines to provide key reaction intermediates for the preparation of nelfinavir. Also disclosed is a method for the preparation of a chiral amino alcohol from an epoxy-tetrahydrofuran.

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San Diego, CA, United States of America

Scott E Zook