100757-91-3Relevant academic research and scientific papers
Discovery of potent and orally bioavailable indazole-based glucagon receptor antagonists for the treatment of type 2 diabetes
Xu, Guozhang,Gaul, Michael D.,Song, Fengbin,Du, Fuyong,Liang, Yin,DesJarlais, Renee L.,DiLoreto, Karen,Shook, Brian,Rentzeperis, Dennis,Santulli, Rosie,Eckardt, Annette,Demarest, Keith
, (2019)
Type 2 diabetes mellitus (T2DM) is characterized by chronically elevated plasma glucose levels. The inhibition of glucagon-induced hepatic glucose output via antagonism of the glucagon receptor (GCGR) using a small-molecule antagonist is a promising mecha
INDOLE DERIVATIVES USEFUL AS GLUCAGON RECEPTOR ANTAGONISTS
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Paragraph 0396-0397, (2018/03/24)
The present invention is directed to indole derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for example metabolic diseases such as Type II diabetes mellitus and obesity.
INDAZOLE DERIVATIVES USEFUL AS GLUCAGON RECEPTOR ANTAGONISTS
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Paragraph 0558, (2018/03/25)
The present invention is directed to indazole derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for e
INDAZOLE DERIVATIVES USEFUL AS GLUCAGON RECEPTOR ANTAGONISTS
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Paragraph 0521, (2018/03/25)
The present invention is directed to indazole derivatives, pharmaceutical compositions containing them and their use in the treatment and/or prevention of disorders and conditions ameliorated by antagonizing one or more glucagon receptors, including for e
GLUCAGON RECEPTOR MODULATORS
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Page/Page column 17-18, (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.
GLUCAGON RECEPTOR ANTAGONISTS, PREPARATION AND THERAPEUTIC USES
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Page/Page column 14, (2009/07/03)
The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the
Activation of functional arylzincs prepared from aryl iodides and highly enantioselective addition to aldehydes
DeBerardinis, Albert M.,Turlington, Mark,Pu, Lin
supporting information; experimental part, p. 2709 - 2712 (2009/05/27)
(Chemical Equation Presented) An easily available chiral ligand (S)-1 is found to activate the nucleophilic reaction of the arylzincs prepared in situ from the reaction of aryl iodides with Et2Zn. Both high yields and high enantioselectivity (u
Glucagon Receptor Antagonists, Preparation and Therapeutic Uses
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Page/Page column 13, (2009/01/20)
The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the in
GLUCAGON RECEPTOR ANTAGONISTS, PREPARATION AND THERAPEUTIC USES
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Page/Page column 46, (2008/06/13)
The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the in
GLUCAGON RECEPTOR ANTAGONISTS, PREPARATION AND THERAPEUTIC USES
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Page/Page column 30, (2010/11/28)
The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the in
