Novel nicotinamide analog as inhibitor of nicotinamide N-methyltransferase
摘要:
Nicotinamide N-methyltransferase (NNMT) has been linked to obesity and diabetes. We have identified a novel nicotinamide (NA) analog, compound 12 that inhibited NNMT enzymatic activity and reduced the formation of 1-methyl-nicotinamide (MNA), the primary metabolite of NA by ∼80% at 2 h when dosed in mice orally at 50 mg/kg.
There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention.
electrocatalysis strategy for the catalytic dehydrochlorination of DCE at the cathode simultaneously with anodic oxidative aromatic chlorination using the released HCl as the chloride source for the efficient synthesis of value‐added (hetero)arylchlorides. The mildness and practicality of the protocol was further demonstrated by the efficient late‐stage chlorination of bioactive molecules.
[EN] SUBSTITUTED HETEROARYL COMPOUNDS AND METHODS OF USE<br/>[FR] COMPOSÉS HÉTÉROARYLE SUBSTITUÉS ET LEURS MÉTHODES D'UTILISATION
申请人:SUNSHINE LAKE PHARMA CO LTD
公开号:WO2017044434A1
公开(公告)日:2017-03-16
The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof. They are useful in preventing, managing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.
[EN] HETEROCYCLIC COMPOUNDS AS KINASE INHIBITORS, COMPOSITIONS COMPRISING THE HETEROCYCLIC COMPOUND, AND METHODS OF USE THEREOF<br/>[FR] COMPOSÉS HÉTÉROCYCLIQUES UTILISÉS EN TANT QU'INHIBITEURS DE KINASE, COMPOSITIONS COMPRENANT LE COMPOSÉ HÉTÉROCYCLIQUE, ET LEURS PROCÉDÉS D'UTILISATION
申请人:JS INNOPHARM SHANGHAI LTD
公开号:WO2020248972A1
公开(公告)日:2020-12-17
(I) Disclosed herein are compounds of formula I, and/or a stereoisomer, a stable isotope, or a pharmaceutically acceptable salt or solvate thereof; and therapeutic uses of these compounds, which are inhibitors of rearranged during transfection (RET), potentially useful in the treatment of RET-associated diseases, such as RET-associated cancers.
ARYL DIHYDROPYRIDINONE AND PIPERIDINONE MGAT2 INHIBITORS
申请人:Bristol-Myers Squibb Company
公开号:US20130143843A1
公开(公告)日:2013-06-06
The present invention provides compounds of Formula (I):
or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.