Bristol-myers Squibb Compnay

University of Illinois

Viiv Healthcare UK (no.5) Limited

Eric P Gillis

Paul Michael Scola

Martin D Burke

Li-Qiang Sun

Eric Mull

Michael S Bowsher

Qian Zhao

Michael Matthew Miller

David M Knapp

David R Langley

Kap-Sun Yeung

Claudio Mapelli

Kandhasamy Sarkunam

Nicholas A Meanwell

Kenneth M Boy

Ramkumar Rajamani

Patrick Reid

Tao Wang

Zhongxing Zhang

Manoj Patel

Kyle E Parcella

Katharine A Grant-Young

John F Kadow

Michael A Poss

B Narasimhulu Naidu

Makonen Belema

John A Bender

Kaitlyn C Gray

Mark George Saulnier

Jason T Goodrich

Alan Xiangdong Wang

Kevin M Peese

David Bertil Frennesson

Kevin W Gillman

Yunhui Zhang

Martin Patrick Allen

Pulicharla Nagalakshmi

Kishore V Renduchintala

Maude A Poirier

Junqi Li

Juliang Zhu

Graham R Dick

Jenna A Klubnick

Daniel J Tenney

Nishith Sanghvi

Ling Li

Sheldon Hiebert

Christiana Iwuagwu

Steven G Ballmer

Pvk Suresh Babu

Lyndon A M Cornelius

P V K Suresh Babu

Suk Joong Lee

M Nicholas Meanwell

Patrick C Reid

Suresh PVK Babu

Jason Goodrich

Nicolas A Meanwell

Lyndon Am Cornelius

The compound and pharmaceutically acceptable salts thereof, and compositions and methods for treating human immunodeficiency virus (HIV) infection are set forth.

Pyrido [2,3-d]pyrimidine derivatives as inhibitors of human immunodeficiency virus replication

Compounds of Formula I, including pharmaceutically acceptable salts thereof, and compositions and methods for treating human immunodeficiency virus (HIV) infection are set forth: 

Inhibitors of human immunodeficiency virus replication

4-oxo-3,4-dihydroquinazoline compounds as inhibitors of human immunodeficiency virus replication

Provided are methods for making and using chiral, non-racemic protected organoboronic acids, including pinene-derived iminodiacetic acid (PIDA) boronates, to direct and enable stereoselective synthesis of organic molecules. Also provided are methods for purifying PIDA boronates from solution. Also provided are methods for deprotection of boronic acids from their PIDA ligands. The purification and deprotection methods may be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chiral, non-racemic compounds. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated stereoselective synthesis of chiral, non-racemic small molecules using iterative cycles of deprotection, coupling, and purification.

Automated synthesis of small molecules using chiral, non-racemic boronates

The present disclosure provides novel macrocyclic peptides which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.

Macrocyclic inhibitors of the PD-1/PD-L1 and CD80(B7-1)/PD-L1 protein/protein interactions

Immunomodulators

The present disclosure provides novel macrocyclic compounds which inhibit the PD-1/PD-L1 and PD-L1/CD80 protein/protein interaction, and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.

Described are methods of forming protected boronic acids that provide in a manner that is straightforward, scalable, and cost-effective a wide variety of building blocks, such as building blocks containing complex and/or pharmaceutically important structures, and/or provide simple or complex protected organoboronic acid building blocks. A first method includes reacting an imino-di-carboxylic acid and an organoboronate salt. A second method includes reacting a N-substituted morpholine dione and an organoboronic acid.

Methods for forming protected organoboronic acids

Compounds of Formula I, including pharmaceutically acceptable salts thereof, are set forth, in addition to compositions and methods of using these compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. 

Macrocyclic molecules as HCV entry inhibitors

Provided are methods for purifying N-methyliminodiacetic acid (MIDA) boronates from solution. Also provided are methods for deprotection of boronic acids from their MIDA ligands. The purification and deprotection methods can be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chemical compounds of interest. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated synthesis of small molecules using iterative cycles of deprotection, coupling, and purification in accordance with methods of the invention. Coupling and other reactions embraced by the invention include, without limitation, Suzuki-Miyaura coupling, oxidation, Swern oxidation, 'Jones reagents' oxidation, reduction, Evans' aldol reaction, HWE olefination, Takai olefination, alcohol silylation, desilylation, p-methoxybenzylation, iodination, Negishi cross-coupling, Heck coupling, Miyaura borylation, Stille coupling, and Sonogashira coupling.

Apparatus and methods for the automated synthesis of small molecules

Growing community of inventors

Wallingford, CT, United States of America

Eric P Gillis