149961-53-5Relevant academic research and scientific papers
GLP-1 RECEPTOR AGONIST AND USE THEREOF
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Paragraph 212; 295; 304-307, (2021/05/21)
Disclosed are novel compounds of Chemical Formula 1, optical isomers of the compounds, and pharmaceutically acceptable salts of the compounds or the optical isomers. The compounds, isomers, and salts exhibit excellent activity as GLP-1 receptor agonists. In particular, they, as GLP-1 receptor agonists, exhibit excellent glucose tolerance, thus having a great potential to be used as therapeutic agents for metabolic diseases. Moreover, they exhibit excellent pharmacological safety for cardiovascular systems.
SUBSTITUTED 2-AMINO-PYRAZOLYL-[1,2,4]TRIAZOLO[1,5A] PYRIDINE DERIVATIVES AND USE THEREOF
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Page/Page column 444; 445, (2020/10/27)
Provided herein are 2-amino-pyrazolyl-[ 1,2,4]triazolo [1,5a]pyridine derivatives. Such compounds are useful, for example, for the treatment and/or prevention of neurodegenerative diseases or disorders such as ophthalmological neurodegenerative disorders. This disclosure also features compositions containing the same as well as methods of using and making the same.
Discovery of β-Arrestin Biased, Orally Bioavailable, and CNS Penetrant Neurotensin Receptor 1 (NTR1) Allosteric Modulators
Pinkerton, Anthony B.,Peddibhotla, Satyamaheshwar,Yamamoto, Fusayo,Slosky, Lauren M.,Bai, Yushi,Maloney, Patrick,Hershberger, Paul,Hedrick, Michael P.,Falter, Bekhi,Ardecky, Robert J.,Smith, Layton H.,Chung, Thomas D. Y.,Jackson, Michael R.,Caron, Marc G.,Barak, Lawrence S.
, p. 8357 - 8363 (2019/09/10)
Neurotensin receptor 1 (NTR1) is a G protein coupled receptor that is widely expressed throughout the central nervous system where it acts as a neuromodulator. Neurotensin receptors have been implicated in a wide variety of CNS disorders, but despite extensive efforts to develop small molecule ligands there are few reports of such compounds. Herein we describe the optimization of a quinazoline based lead to give 18 (SBI-553), a potent and brain penetrant NTR1 allosteric modulator.
HORMONE RECEPTOR MODULATORS FOR TREATING METABOLIC CONDITIONS AND DISORDERS
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Page/Page column 152, (2018/03/25)
The invention relates to activators of FXR useful in the treatment of autoimmune disorders, liver disease, intestinal disease, kidney disease, cancer, and other diseases in which FXR plays a role, having the Formula (I): (I), wherein L1, A, X1, X2, R1, R2, and R3 are described herein.
Visible Light-Mediated Decarboxylative Alkylation of Pharmaceutically Relevant Heterocycles
Sun, Alexandra C.,McClain, Edward J.,Beatty, Joel W.,Stephenson, Corey R. J.
supporting information, p. 3487 - 3490 (2018/06/26)
A net redox-neutral method for the decarboxylative alkylation of heteroarenes using photoredox catalysis is reported. Additionally, this method features the use of simple, commercially available carboxylic acid derivatives as alkylating agents, enabling the facile alkylation of a variety of biologically relevant heterocyclic scaffolds under mild conditions.
ISOXAZOLYL-CARBONYLOXY AZABICYCLO[3.2.1]OCTANYL COMPOUNDS AS FXR ACTIVATORS
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Paragraph 00456, (2018/09/25)
The disclosure relates to activators of FXR useful in the treatment of autoimmune disorders, liver disease, intestinal disease, kidney disease, cancer, and other diseases in which FXR plays a role, having the Formula (I): wherein L1, L2, A, B, R1, R2, R3, and R4 are described herein.
SMALL MOLECULE AGONISTS OF NEUROTENSIN RECEPTOR 1
HEDRICK Michael P.,HERSHBERGER Paul M.,MALONEY Patrick R.,PEDDIBHOTLA Satyamaheshwar,PINKERTON Anthony B.
Paragraph 00622; 00666, (2016/04/26)
Provided herein are small molecule neurotensin receptor agonists, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.
Process for the preparation of 1-fluoro-cyclopropane-1-carboxylic acid
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, (2008/06/13)
A new process for the preparation of 1-fluoro-cyclopropane-1-carboxylic acid of the formula STR1 which process comprises a) reacting in a first step, a 1-fluoro-cyclopropyl phenyl ketone of the formula STR2 in which R represents hydrogen, halogen, methyl, methoxy, phenyl or phenoxy, with an peroxy compound in the presence of a diluent, and b) reacting, in a second step, the resulting 1-fluoro-cyclopropane-1-carboxylate of the formula STR3 in which R has the abovementioned meaning, with a base in the presence of a diluent, and then acidifying the mixture. New 1-fluoro-cyclopropane-1-carboxylates of the above-mentioned formula.
