Biocryst Pharmaceuticals, Inc.

Yahya El-Kattan

Yarlagadda Sudhakara Babu

Pooran Chand

Pravin L Kotian

Minwan Wu

V Satish Kumar

Tsu-Hsing Lin

Ajit K Ghosh

Shri Niwas

R Scott Rowland

Scott R Rowland

Disclosed are methods of preparing Compound I, and salts thereof. The methods of preparing Compound I are suitable for use on process scale.

Process-scale synthesis of a plasma kallikrein inhibitor

Disclosed are crystalline salts of Compound I, methods of preparing them, and related pharmaceutical preparations thereof. Also disclosed are methods of treatment using the crystalline salts of the invention.

Crystalline salts of a plasma kallikrein inhibitor

Disclosed are crystalline salts of Compound I, methods of preparing them, and related pharmaceutical preparations thereof. Also disclosed are methods of treatment using the crystalline salts of the invention. 

The invention provides methods for treating hepatitis C viral infections and related viral infections, as well as compounds and compositions that are useful for treating such infections.

Hepatitis C therapies

The invention provides compounds of formula I, II, and III as described herein, as well as pharmaceutical compositions comprising the compounds, and synthetic methods and intermediates that are useful for preparing the compounds. The compounds of formula I, II, and III are useful as anti-viral agents and/or as anti-cancer agents.

Therapeutic furopyrimidines and thienopyrimidines

Compounds represented by the formula:  Both Rand Rcan form a monocyclic ring of 4-7 atoms with N or optionally a further heteroatom in the ring;

Nucleosides, preparation thereof and use as inhibitors of RNA viral polymerases

Two syntheses are provided; one for the preparation of (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol, and other for the preparation of (3S,4R)-4-(hydroxymethyl)pyrrolidin-3-ol. (3R,4R)-4-(hydroxymethyl)pyrrolidin-3-ol is prepared using the achiral ylide prepared from benzylamine instead of phenethylamine (Scheme 3) which provides a crystalline intermediate. The synthesis of (3S,4R)-4-(hydroxymethyl)pyrrolidin-3-ol is achieved from (S)-diethylmalate as described in Scheme 4. A process for preparing camphor sultam is also provided.

Process for the preparation of substituted pyrrolidine derivatives and intermediates

Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat and/or prevent clotting disorders, and as anticoagulating agents.

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Vestavia Hills, AL, United States of America

Yahya El-Kattan