Abbott Laboratories Corporation

Abbvie Inc.

Melinta Therapeutics, Inc.

The Medicines Company

Sanjay R Chemburkar

Ketan M Patel

Harry O Spiwek

Daniel A Dickman

Michael J Abrahamson

Rajarathnam E Reddy

Julie J Pruyne

Rodger F Henry

David Lechuga-Ballesteros

James J Fort

Bikshandarkoil A Narayanan

John F Bauer

William Porter

Azita Saleki-Gerhardt

Philip E Bauer

Kimberly A Allen

Douglas M Reamer

Yuping Niu

Angelica B Kielbus

Adel Rafai Far

Min Ding

Gopal Krishna

Carl M Knable

James P Petzel

Yi-Yin Ku

Madhup K Dhaon

Subhash R Patel

John E Lallaman

Hemantkumar H Patel

David P Sawick

Peter J Bonk

William T Riordan

Chi-nung Hsiao

Yong Y Chen

Michael J Dart

Youssef L Bennani

William H Bunnelle

Russell Drew Cink

Sou-Jen Chang

David R Hill

Bruce W Horrom

Juliette K Busse

Travis B Dunn

Jianzhang Mei

Dilinie P Fernando

Albert V Thomas

Albert Wayne Kruger

James D Ratajczyk

Timothy B Towne

Lei Cao

Brian J Kotecki

Bhadra Shelat

Lei Wang

Mark A Lockwood

Raimundo Ho

John Pavlina

Samrat Mukherjee

Jinhua Chen

Ramesh R Patel

John N Starr

Gareth J Brown

Stefan Mix

Stephen S Ulrey

Niharika Chauhan

Stephen T Chau

Erika Crane

Alex Fabian

Brian A Roden

Jose A Restituyo

Douglas R Spaulding

Richard Lorenzini

Michael Demarco

Yi Pan

Yong Chen

Chu-Nung Hsiao

Peter Bonk

Madhup Dhaon

Ketan Patel

The present invention relates to compositions of elagolix sodium, and process and intermediates for the preparation thereof.

Elagolix sodium compositions and processes

Drug substance preparations of oritavancin having high purity are disclosed, along with pharmaceutical compositions comprising such oritavancin drug substance preparations, and drug products or dosage forms comprising such pharmaceutical compositions.

High purity oritavancin and method of producing same

Disclosed are methods of synthesizing racemic 2-(difluoromethyl)-1-(alkoxycarbonyl)-cyclopropanecarboxylic acids and 2-(vinyl)-1-(alkoxycarbonyl)-cyclopropanecarboxylic acids and their salts, such as the dicyclohexylamine salt. Also disclosed are methods for preparing enantioenriched (1R,2R)-1-((tert-butoxycarbonyl)amino)-2-(difluoromethyl)cyclopropane-1-carboxylic acid and esters of the same. These compounds are useful intermediates in the synthesis of viral protease inhibitors.

Enzymatic processes for the preparation of (&#xb1;)-2-(difluoromethyl)-1-(alkoxycarbonyl)-cyclopropanecarboxylic acid and (&#xb1;)-2-(vinyl)-1-(alkoxycarbonyl)-cyclopropanecarboxylic acid

Disclosed herein is a process for preparing enantioenriched (S)-2-aminonon-8-enoic acid by amination of 2-oxonon-8-enoic acid in the presence of an enzyme and an ammonia source.

Process for the preparation of (S)-2-amino-non-8-enoic acid

Disclosed are methods of synthesizing enantioenriched difluoroalkylcyclopropyl amino esters and their salts, such as the dicyclohexylamine salt of (1S,2R)-2-(difluoromethyl)-1-(propoxycarbonyl)cyclopropane carboxylic acid. These compounds are useful intermediates in the synthesis of viral protease inhibitors.

Enzymatic process for the preparation of (1S,2R)-2-(difluoromethyl)-1-(propoxycarbonyl)cyclopropanecarboxylic acid

Disclosed are, among other things, variant polypeptides, nucleic acids encoding the polypeptides, production of the variant polypeptides, and use of the variant polypeptides in various applications, such as screening and synthetic methods. For example, the variant polypeptides, or enzymatically-active fragments thereof, are useful for converting aliphatic keto acids to aliphatic alpha amino acids.

Variant polypeptides capable of aminating aliphatic alpha keto acids

A new crystalline polymorph of ritonavir and methods for its use and preparation are disclosed.

Polymorph of a pharmaceutical

New crystalline forms of lopinavir are disclosed.

Crystalline pharmaceutical

A process for the preparation of (2S,3aR,7aS)-octahydro-1H-indole-20carboxylic acid hydrochloride.

Process for the synthesis of (2S,3AR,7AS)-octahydro-1H-indole carboxylic acid as an intermediate for trandolapril

A single-step, one-pot process to obtain zotarolimus and other rapamycin derivatives on large scale is presented, which improves currently available synthesis schemes. In one embodiment, dried rapamycin is dissolved in isopropylacetate (IPAc). The solution is cooled, and 2,6-Lutidine is added, followed slowly adding triflic anhydride at &#x2212;30&#xb0; C. Salts are then removed by filtration. Tetrazole, followed by a tert-base diisopropylethylamine (DIEA) is added to the triflate solution. After incubation at room temperature, the product is concentrated and purified by a silica gel column using THF/heptane as eluant. The fractions containing the product are collected, concentrated, and purified again using an acetone/heptane column. The product containing fractions are concentrated. The product is dissolved in t-BME and precipitated with heptane. The solids are dissolved in acetone, treated with butylated-hydroxy toluene (BHT), and the solution concentrated. The process is repeated twice with acetone to remove solvents. At least one stabilizing agent is added, such as BHT at 0.5% before drying.

One pot synthesis of tetrazole derivatives of rapamycin

Growing community of inventors

Gurnee, IL, United States of America

Sanjay R Chemburkar