Merck Sharp + Dohme Corp.

Kallyope, Inc.

Christopher R Moyes

Scott D Edmondson

Dong-Ming Shen

Shuwen He

Songnian Lin

Cheng Zhu

Lehua Chang

Nam Fung Kar

Andrew William Stamford

Tesfaye Biftu

Philip Jones

Ravi P Nargund

Neville J Anthony

Michael W Miller

Harvey Wendt

Jeffrey John Hale

Xing Dai

Ping Liu

Danqing D Feng

Iyassu Sebhat

Lin Yan

Duane E DeMong

Harold B Wood

Gregori J Morriello

Dmitri A Pissarnitski

Santhosh Francis Neelamkavil

Joon Jung

Bing Li

Christopher Francis Thompson

Wanying Sun

Richard Berger

Mark E Scott

Ahmet Kekec

Liping Wang

Zhiqiang Zhao

Pei Huo

Yuping Zhu

Vincent Colandrea

Deyou Sha

Kallol Basu

Graham Frank Smith

Bart Harper

Zhiyong Hu

Joie Garfunkle

Carolyn Michele Cammarano

Brenda Pipik

Dawn Marie Hoffman

David N Hunter

Greg J Morriello

Erin N Guidry

Gergori J Morriello

Scott B Joseph

Byron Gabriel Dubois

Joseph L Duffy

Vincent J Colandrea

Harvey R Wendt

Michael Miller

The present disclosure relates to compounds useful as modulators of neurokinin receptor 3 (NK3) for the treatment of conditions or disorders.

NK3 modulators and uses thereof

This disclosure is directed, at least in part, to GPR119 agonists useful for the treatment of conditions or disorders involving the gut-brain axis. In some embodiments, the GPR119 agonists are gut-restricted compounds. In some embodiments, the condition or disorder is a metabolic disorder, such as diabetes, obesity, nonalcoholic steatohepatitis (NASH), or a nutritional disorder such as short bowel syndrome.

GPR119 agonists

An insulin conjugate comprising or consisting of a tri-valent sugar cluster is described. In particular aspects, the insulin conjugate displays a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose even when administered to a subject in need thereof in the absence of an exogenous multivalent saccharide-binding molecule such as Con A.

Glucose responsive insulin comprising a tri-valent sugar cluster for treatment of diabetes

Insulin conjugates comprising an insulin molecule covalently attached to at least one bi-dentate linker having two arms, each arm independently attached to a ligand comprising a saccharide and wherein at least one ligand of the linker is fucose are disclosed. The insulin conjugates display a pharmacokinetic (PK) and/or pharmacodynamic (PD) profile that is responsive to the systemic concentrations of a saccharide such as glucose or alpha-methylmannose even when administered to a subject in need thereof in the absence of an exogenous multivalent saccharide-binding molecule such as Con A.

Glucose-responsive insulin conjugates

Substituted cyclopropyl compounds of the formula I: and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included. 

Substituted cyclopropyl compounds, compositions containing such compounds, and methods of treatment

The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of &#x3b2;3-adrenoceptor. 

Pyrrolidine derived beta 3 adrenergic receptor agonists

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Westfield, NJ, United States of America

Christopher R Moyes