Isis Pharmaceuticals, Inc.

Takeda Pharmaceutical Company Limited

Takeda San Diego, Inc.

Metabasis Therapeutics, Inc.

Takeda California, Inc.

Zacharia S Cheruvallath

Vasulinga T Ravikumar

Douglas L Cole

Mingnam Tang

Stephen L Gwaltney

Daniel C Capaldi

Mark Sabat

Jun Feng

Joanne Miura

Christopher McBride

John David Lawson

Prasuna Guntupalli

Huikai Sun

Kristin Schleicher

Jason Green

Haxia Wang

Jeffrey Alan Stafford

Andrew John Jennings

Mallareddy Komandla

Ben Johnson

Stephen W Kaldor

Ruth F Nutt

Joseph Edward Semple

Jing Wang

Beverly Lynn Wolgast

Sean Timothy Murphy

Haixia Wang

Hengyi Zhu

Darryl Rideout

Philip Erickson

Huong-Thu Ton-Nu

Colin J Loweth

Feiyue Wu

Shankari Mylvaganam

Jianzhong Sun

Christopher Mcbride

Disclosed are compounds of Formula (1), and pharmaceutically acceptable salts thereof, wherein n, R, R, R, R, R, R, R, R, R, R, X, Xand Xare defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula (1), to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with SSTR4.

N-(heterocyclyl and heterocyclylalkyl)-3-benzylpyridin-2-amine derivatives as SSTR4 agonists

Disclosed are compounds of Formula 1, stereoisomers thereof, and pharmaceutically acceptable salts thereof, wherein L, r, s, R, R, R, R, R, R, R, X, X, X, X, X, and Xare defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating diseases, disorders, and conditions associated with SSTR4.

Piperidinyl-3-(aryloxy)propanamides and propanoates

Disclosed are compounds of Formula 1, stereoisomers thereof and pharmaceutically acceptable salts of the compounds and stereoisomers, wherein Rand Rare defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating obesity and related diseases, disorders, and conditions associated with MetAP2.

Fumagillol derivatives

Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein L, R, R, R, R, R, R, and Rare defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating obesity and related diseases, disorders, and conditions associated with MetAP2.

Substituted-1,4-dihydropyrazolo[4,3-b]indoles

Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R, R, R, R, R, and Rare defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating obesity and related diseases, disorders, and conditions associated with MetAP2.

Indazole derivatives

Compounds are provided for use with glucokinase that comprise the formula: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

Glucokinase activators

Pyrazole and fused pyrazole glucokinase activators

Compounds of the following formula are provided for use with glucokinase: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.

Methods for the formation of sulfurized oligonucleotides are provided. The methods allow for the formation of phosphorothioate linkages in the oligonucleotides or derivatives, without the need for complex solvent mixtures and repeated washing or solvent changes. Oligonucleotides having from about 8, and up to about 50, nucleotides can be sulfurized according to the methods of the invention with higher yields than have been previously reported.

Synthesis of sulfurized oligonucleotides

Compounds and compositions are provided for modulating the activity of protein tyrosine phosphatases. In one embodiment, the compounds and compositions are thiazoles and thiadiazoles that inhibit the activity of protein tyrosine phosphatase 1B.

Thiazole and thiadiazole inhibitors of tyrosine phosphatases

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San Diego, CA, United States of America

Zacharia S Cheruvallath