1383800-57-4Relevant articles and documents
Acylation of aryl halides and α-bromo acetates with aldehydes enabled by nickel/tbadt cocatalysis
Fan, Pei,Zhang, Chang,Zhang, Linchuan,Wang, Chuan
supporting information, p. 3875 - 3878 (2020/05/14)
In this protocol aryl halides and α-bromo acetates are efficiently cross-coupled with an array of (hetero)aromatic and aliphatic aldehydes under the cooperative catalysis of nickel and tetrabutylammonium decatungstate as a hydrogen-atom-transfer photocatalyst. This method provides a concise approach to a variety of ketones with high compatibility of various functional groups.
QUINOLINYL GLUCAGON RECEPTOR MODULATORS
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, (2013/03/26)
The present invention provides a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, A1, A2, A3, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
The design and synthesis of a potent glucagon receptor antagonist with favorable physicochemical and pharmacokinetic properties as a candidate for the treatment of type 2 diabetes mellitus
Guzman-Perez, Angel,Pfefferkorn, Jeffrey A.,Lee, Esther C.Y.,Stevens, Benjamin D.,Aspnes, Gary E.,Bian, Jianwei,Didiuk, Mary T.,Filipski, Kevin J.,Moore, Dianna,Perreault, Christian,Sammons, Matthew F.,Tu, Meihua,Brown, Janice,Atkinson, Karen,Litchfield, John,Tan, Beijing,Samas, Brian,Zavadoski, William J.,Salatto, Christopher T.,Treadway, Judith
, p. 3051 - 3058 (2013/06/27)
A novel and potent small molecule glucagon receptor antagonist for the treatment of diabetes mellitus is reported. This candidate, (S)-3-[4-(1-{3,5- dimethyl-4-[4-(trifluoromethyl)-1H-pyrazol-1-yl]phenoxy}butyl)benzamido] propanoic acid, has lower molecular weight and lipophilicity than historical glucagon receptor antagonists, resulting in excellent selectivity in broad-panel screening, lower cytotoxicity, and excellent overall in vivo safety in early pre-clinical testing. Additionally, it displays low in vivo clearance and excellent oral bioavailability in both rats and dogs. In a rat glucagon challenge model, it was shown to reduce the glucagon-elicited glucose excursion in a dose-dependent manner and at a concentration consistent with its rat in vitro potency. Its properties make it an excellent candidate for further investigation.
Glucagon Receptor Modulators
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, (2012/07/13)
The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
GLUCAGON RECEPTOR MODULATORS
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, (2012/08/27)
The present invention provides a compound of Formula (I) or a pharmaceutically acceptable salt thereof wherein R1, R2, R3, A1, A2, A3, A4, L, B1, B2, B3 and B4 are as defined herein. The compounds of Formula I have been found to act as glucagon antagonists or inverse agonists. Consequently, the compounds of Formula I and the pharmaceutical compositions thereof are useful for the treatment of diseases, disorders, or conditions mediated by glucagon.
