70240-29-8Relevant academic research and scientific papers
Metal- And additive-free C-H oxygenation of alkylarenes by visible-light photoredox catalysis
García Manche?o, Olga,Kuhlmann, Jan H.,Pérez-Aguilar, María Carmen,Piekarski, Dariusz G.,Uygur, Mustafa
supporting information, p. 3392 - 3399 (2021/05/21)
A metal- and additive-free methodology for the highly selective, photocatalyzed C-H oxygenation of alkylarenes under air to the corresponding carbonyls is presented. The process is catalyzed by an imide-acridinium that forms an extremely strong photooxidant upon visible light irradiation, which is able to activate inert alkylarenes such as toluene. Hence, this is an easy to perform, sustainable and environmentally friendly oxidation that provides valuable carbonyls from abundant, readily available compounds.
The discovery of N-((2 H-tetrazol-5-yl)methyl)-4-((R)-1-((5 r,8 R)-8-(tert-butyl)-3-(3,5-dichlorophenyl)-2-oxo-1,4-diazaspiro[4.5]dec-3-en-1-yl) -4,4-dimethylpentyl)benzamide (SCH 900822): A potent and selective glucagon receptor antagonist
Demong, Duane,Dai, Xing,Hwa, Joyce,Miller, Michael,Lin, Sue-Ing,Kang, Ling,Stamford, Andrew,Greenlee, William,Yu, Wensheng,Wong, Michael,Lavey, Brian,Kozlowski, Joseph,Zhou, Guowei,Yang, De-Yi,Patel, Bhuneshwari,Soriano, Aileen,Zhai, Ying,Sondey, Christopher,Zhang, Hongtao,Lachowicz, Jean,Grotz, Diane,Cox, Kathleen,Morrison, Richard,Andreani, Teresa,Cao, Yang,Liang, Mark,Meng, Tao,McNamara, Paul,Wong, Jesse,Bradley, Prudence,Feng, Kung-I,Belani, Jitendra,Chen, Ping,Dai, Peng,Gauuan, Jolicia,Lin, Peishan,Zhao, He
supporting information, p. 2601 - 2610 (2014/04/17)
A novel series of spiroimidazolone-based antagonists of the human glucagon receptor (hGCGR) has been developed. Our efforts have led to compound 1, N-((2H-tetrazol-5-yl)methyl)-4-((R)-1-((5r,8R)-8-(tert-butyl)-3-(3, 5-dichlorophenyl)-2-oxo-1,4-diazaspiro[4.5]dec-3-en-1-yl)-4,4-dimethylpentyl) benzamide (SCH 900822), a potent hGCGR antagonist with exceptional selectivity over the human glucagon-like peptide-1 receptor. Oral administration of 1 lowered 24 h nonfasting glucose levels in imprinting control region mice on a high fat diet with diet-induced obesity following single oral doses of 3 and 10 mg/kg. Furthermore, compound 1, when dosed orally, was found to decrease fasting blood glucose at 30 mg/kg in a streptozotocin-treated, diet-induced obesity mouse pharmacodynamic assay and blunt exogenous glucagon-stimulated glucose excursion in prediabetic mice.
NMDA RECEPTOR MODULATORS AND USES RELATED THERETO
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Page/Page column 27; 36, (2014/03/21)
This disclosure relates to NMDA modulators and used related thereto such as for treatment of central nervous system disorders. In certain embodiments, compounds disclosed herein are NR2C subunit-selective NMDA potentiators. In certain embodiments, the disclosure contemplates compounds and pharmaceutical compositions. In certain embodiments, the disclosure contemplates compounds disclosed herein as prodrugs, optionally substituted with one or more substituents, derivatives, or salts thereof. In certain embodiments, the disclosure relates to methods of treating or preventing nervous system disorders comprising administering an effective amount of a composition comprising compound disclosed herein to a subject in need thereof.
Design, synthesis, and structure-activity relationship of a novel series of GluN2C-selective potentiators
Zimmerman, Sommer S.,Khatri, Alpa,Garnier-Amblard, Ethel C.,Mullasseril, Praseeda,Kurtkaya, Natalie L.,Gyoneva, Stefka,Hansen, Kasper B.,Traynelis, Stephen F.,Liotta, Dennis C.
supporting information, p. 2334 - 2356 (2014/04/17)
NMDA receptors are tetrameric complexes composed of GluN1 and GluN2A-D subunits that mediate a slow Ca2+-permeable component of excitatory synaptic transmission. NMDA receptors have been implicated in a wide range of neurological diseases and thus represent an important therapeutic target. We herein describe a novel series of pyrrolidinones that selectively potentiate only NMDA receptors that contain the GluN2C subunit. The most active analogues tested were over 100-fold selective for recombinant GluN2C-containing receptors over GluN2A/B/D-containing NMDA receptors as well as AMPA and kainate receptors. This series represents the first class of allosteric potentiators that are selective for diheteromeric GluN2C-containing NMDA receptors.
NOVEL SPIRO IMIDAZOLONE DERIVATIVES AS GLUCAGON RECEPTOR ANTAGONISTS, COMPOSITIONS, AND METHODS FOR THEIR USE
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Page/Page column 165-166, (2011/10/13)
The present invention relates to compounds of the general formula (I): wherein ring A, ring B, G, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
NOVEL SPIRO IMIDAZOLONES AS GLUCAGON RECEPTOR ANTAGONISTS, COMPOSITIONS, AND METHODS FOR THEIR USE
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Page/Page column 196-197, (2011/10/13)
The present invention relates to compounds of the general formula: wherein ring A, ring B, R1, R3, Z, L1, and L2 are selected independently of each other and are as defined herein, to compositions comprising the compounds, and to methods of using the compounds as glucagon receptor antagonists and for the treatment or prevention of type 2 diabetes and conditions related thereto.
PYRIMIDINONE DERIVATIVES AND METHODS OF USE THEREOF
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Page/Page column 146, (2008/12/08)
The present invention relates to Pyrimidinone Derivatives, compositions comprising a Pyrimidinone Derivative, and methods of using the Pyrimidinone Derivatives for treating or preventing obesity, diabetes, a metabolic disease, a cardiovascular disease or a disorder related to the activity of GPR119 in a patient.
ARYL TRIFLUOROMETHYL KETONE HYDRATES AS PRECURSORS OF CARBOXYLIC ACIDS AND ESTERS
Delgado, Antonio,Clardy, Jon
, p. 2789 - 2790 (2007/10/02)
A simple method for the preparation of aryl carboxylic acids and esters from aryl trifluoromethyl ketone hydrates is described.
