77053-53-3Relevant academic research and scientific papers
PYRAZOLOTRIAZOLOPYRIMIDINE DERIVATIVES AS A2A RECEPTOR ANTAGONIST
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Paragraph 0307; 0310-0311, (2020/02/16)
Disclosed herein is a pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof useful as A2A receptor antagonist, and a pharmaceutical composition comprising the same. Also disclosed herein is a method of treating cancer using the pyrazolotriazolopyrimidine derivative or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof as A2A receptor antagonist.
NITROGENATED HETEROCYCLIC COMPOUND
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Paragraph 1091; 1242, (2015/03/28)
The present invention provides a compound having a PDE2A selective inhibitory action, which is useful as an agent for the prophylaxis or treatment of schizophrenia, Alzheimer's disease and the like. The present invention is a compound represented by the formula (1): wherein each symbol is as described in the specification, or a salt thereof.
Synthesis of Quinolines by Visible-Light Induced Radical Reaction of Vinyl Azides and α-Carbonyl Benzyl Bromides
Wang, Qile,Huang, Jun,Zhou, Lei
supporting information, p. 2479 - 2484 (2015/08/18)
A visible-light induced radical reaction of vinyl azides and α-carbonyl benzyl bromides was developed, which provides an efficient route to polysubstituted quinolines via a C-C and C-N bond formation sequence.
MINERALOCORTICOID RECEPTOR ANTAGONISTS
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Page/Page column 79, (2014/02/15)
The present invention is directed to compounds of the Formula I: as well as pharmaceutically acceptable salts thereof, that may be useful for treating aldosterone-mediated diseases. The invention furthermore relates to specific diastereomers and enantiome
Arylglycine derivatives as potent transient receptor potential melastatin 8 (TRPM8) antagonists
Zhu, Bin,Xia, Mingde,Xu, Xiaoqing,Ludovici, Donald W.,Tennakoon, Manomi,Youngman, Mark A.,Matthews, Jay M.,Dax, Scott L.,Colburn, Raymond W.,Qin, Ning,Hutchinson, Tasha L.,Lubin, Mary Lou,Brandt, Michael R.,Stone, Dennis J.,Flores, Christopher M.,MacIelag, Mark J.
, p. 2234 - 2237 (2013/04/23)
A series of arylglycine-based analogs was synthesized and tested for TRPM8 antagonism in a cell-based functional assay. Following structure-activity relationship studies in vitro, a number of compounds were identified as potent TRPM8 antagonists and were subsequently evaluated in an in vivo pharmacodynamic assay of icilin-induced 'wet-dog' shaking in which compound 12 was fully effective. TRPM8 antagonists of the type described here may be useful in treating pain conditions wherein cold hypersensitivity is a dominant feature.
Carbon-carbon bond-forming reactions of α-carbonyl carbocations: Exploration of a reversed-polarity equivalent of enolate chemistry
Lai, Ping-Shan,Dubland, Joshua A.,Sarwar, Mohammed G.,Chudzinski, Michael G.,Taylor, Mark S.
supporting information; experimental part, p. 7586 - 7592 (2011/10/12)
Carbon-carbon bond-forming reactions of putative α-carbonyl carbocation intermediates generated by Lewis acid- or silver-promoted ionizations of toluenesulfonate or halide leaving groups are described. This under-exploited mode of reactivity represents an 'umpolung' of conventional enolate chemistry, and enables C-C bond construction in both intra- and intermolecular contexts. Attempts to develop diastereoselective variants of this process using chiral ester and oxazolidinone-based auxiliaries are discussed.
PROCESS FOR PRODUCTION OF THIOPHENE COMPOUND AND INTERMEDIATE THEREOF
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Page/Page column 12, (2010/11/17)
To provide a novel process for producing a 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound or an intermediate thereof useful as an intermediate for production of medicines and agricultural chemicals. A 2-aryl acetate compound represented by the formula (1): wherein R1 is an aryl group or the like, R4 is a C1-3 alkyl group or the like, and X is a leaving group, is reacted with a thioacetic acid compound to form a thioacetyl compound (3), the thioacetyl compound (3) is reacted with a vinyl ketone compound to form a γ-ketosulfide compound (5), which is cyclized under basic conditions to form a dihydrothiophene compound (6), and the dihydrothiophene compound (6) is oxidized by using an oxidizing agent to produce a 2-aryl-3-hydroxy-4-substituted carbonyl thiophene compound (7).
Cold Menthol Receptor Antagonists
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Page/Page column 56, (2010/03/31)
Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, L, Q, R1, R2, and R3 /s
Photochemical synthesis of benz[h]isoquinolines
Abbott, Belinda M.,Ferrari, Frank D.,Harnor, Suzannah J.,Barnes, John C.,Marquez, Rodolfo
, p. 5072 - 5078 (2008/09/21)
The synthesis of benz[h]isoquinolines has been achieved using a highly convergent photochemical method. The approach presented provides ready access to biologically active compounds and building blocks not readily available through other methods.
ALPHA-(TRIFLUOROMETHYL-SUBSTITUTED ARYLOXY, ARYLAMINO, ARYLTHIO OR ARYLMETHYL)-TRIFLUOROMETHYL-SUBSTITUTED PHENYLACETIC ACIDS AND DERIVATIVES AS ANTIDIABETIC AGENTS
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Page/Page column 47, (2010/02/13)
Compounds having a formula (1) or a pharmaceutically acceptable salt or prodrug thereof, are provided, and are useful for the treatment of metabolic disorders.
