Merck + Co., Inc.

Agios Pharmaceuticals, Inc.

Merck Sharp + Dohme Corp.

Servier Pharmaceuticals LLC

Zhixiong Ye

Ravi P Nargund

Raman Kumar Bakshi

Iyassu K Sebhat

Liangqin Guo

Brenda L Palucki

Jeremy Mark Travins

Sheldon Cao

Arthur A Patchett

Janeta Popovici-Muller

Khaled J Barakat

Zhihua Sui

Feroze Ujjainwalla

Leonardus H T Van Der Ploeg

Giovanni Cianchetta

Min K Park

Zenon D Konteatis

Yingjie Lai

Francesco Gerald Salituro

Robert Zahler

Jeffrey O Saunders

Shuwen He

Jonathan R Young

Shunqi Yan

Xuefei Tan

Xiaolei Wang

Qingmei Hong

Patrick G Pollard

Thomas F Walsh

Mark T Goulet

Jian Liu

Rene Marc Lemieux

Tianying Jian

Daniel Warner

James Dellureficio

Peter H Dobbelaar

Yue Ding

James P Dellureficio

The present disclosure provides MAT2A inhibitor compounds that are useful as therapeutic agents for treating malignancies, and wherein the compounds conform to general formula (IA): wherein R, R, R, R, and Rare defined herein.

Inhibitors of cellular metabolic processes

Compounds and compositions comprising compounds that inhibit glutaminase are described herein. Also described herein are methods of using the compounds that inhibit glutaminase in the treatment of cancer.

Compounds and their methods of use

Provided are piperazine compounds of Formula I useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described here. 

Therapeutically active compositions and their methods of use

Provided are compounds of formula (I), wherein X, Y, Z, W, V, R, Rand m are defined as in the description. Their pharmaceutical compositions and their uses for treating cancers are also provided.

Phenyl and pyridinyl substituted piperidines and piperazines as inhibitors of IDH1 mutants and their use in treating cancer

Compounds of general formula I: and compositions comprising compounds of general formula I that modulate pyruvate kinase are described herein. Also described herein are methods of using the compounds that modulate pyruvate kinase in the treatment of diseases.

Therapeutic compounds and compositions

Certain novel N-acylated spiropiperidine derivatives are ligands of the human melanocortin receptor(s) and, in particular, are selective ligands of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of MC-4R, such as obesity, diabetes, nicotine addiction, alcoholism, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Acylated spiropiperidine derivatives as melanocortin-4 receptor modulators

Certain novel piperazine urea derivatives are agonists of the human melanocortin-4 receptor (MC-4R) and, in particular, are receptor-subtype selective agonists of MC-4R. They are useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity and diabetes.

Piperazine urea derivatives as melanocortin-4 receptor agonists

Certain novel N-acylated spiropiperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Acylated spiropiperidine derivatives as melanocortin-4 receptor agonists

Certain novel bicyclic N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Bicyclic piperidine derivatives as melanocortin-4 receptor agonists

Certain novel N-acylated piperazine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Acylated piperazine derivatives as melanocortin-4 receptor agonists

Certain novel bridged piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Bridged piperidine derivatives as melanocortin receptor agonists

Certain novel-substituted N-acylated piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-receptor (MC-R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.

Acylated piperidine derivatives as melanocortin-4 receptor agonists

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Princeton, NJ, United States of America

Zhixiong Ye