122243-32-7Relevant academic research and scientific papers
ADENOSINE A2A AND A2B RECEPTOR DUAL ANTAGONISTS FOR IMMUNO-ONCOLOGY
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Page/Page column 89-90, (2022/02/05)
The present invention provides compounds of the structural Formula (I) and pharmaceutically acceptable salts thereof, wherein, are as defined herein, pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other therapeutically active agents), and methods for their preparation and use, alone and in combination with other therapeutic agents, as antagonists of A2a and/or A2b receptors, and in the treatment of a variety of diseases, conditions, or disorders that are mediated, at least in part, by the adenosine A2a receptor and/or the adenosine A2b receptor.
Nucleophilic fluorination facilitated by a CsF-CaF2 packed bed reactor in continuous flow
Johansen,Lindhardt
supporting information, p. 825 - 828 (2018/02/06)
A simple to prepare, dry and handle packed bed reactor carrying CsF on CaF2, towards nucleophilic fluorinations in continuous flow, is reported. The reactor also proved adaptable for silyl-ether deprotection and trifluoromethylations with Ruppert's reagent. The study includes reactor stability and scale-up investigations.
Flow trifluoromethylation of carbonyl compounds by Ruppert-Prakash reagent and its application for pharmaceuticals, efavirenz and HSD-016
Okusu, Satoshi,Hirano, Kazuki,Yasuda, Yoshimasa,Tokunaga, Etsuko,Shibata, Norio
, p. 82716 - 82720 (2016/11/11)
The Ruppert-Prakash reagent is the most powerful and well-documented reagent for trifluoromethylation. Despite its versatility, no general method exists for its use in a flow system. Here we report the first flow trifluoromethylation of carbonyl compounds
HETEROCYCLICALLY SUBSTITUTED ARYL COMPOUNDS AS HIF INHIBITORS
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Paragraph 1199; 1200; 1201, (2013/08/14)
The present application relates to novel aryl compounds with heterocyclic substituents, processes for their preparation, their use for treatment and/or prevention of diseases and their use for the preparation of medicaments for treatment and/or prevention
SUBSTITUTED 5-AMINOTHIENO[2,3-C]PYRIDAZINE-6-CARBOXAMIDE ANALOGS AS POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M4
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Paragraph 001037; 001038, (2013/09/12)
In one aspect, the invention relates to substituted 5-aminothieno[2,3-c]pyridazine-6- carboxamide analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M4 (mAChR M4); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Discovery of novel, potent benzamide inhibitors of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) exhibiting oral activity in an enzyme inhibition ex vivo model
Julian, Lisa D.,Wang, Zhulun,Bostick, Tracy,Caille, Seb,Choi, Rebekah,DeGraffenreid, Michael,Di, Yongmei,He, Xiao,Hungate, Randall W.,Jaen, Juan C.,Liu, Jinsong,Monshouwer, Mario,McMinn, Dustin,Rew, Yosup,Sudom, Athena,Sun, Daqing,Tu, Hua,Ursu, Stefania,Walker, Nigel,Yan, Xuelei,Ye, Qiuping,Powers, Jay P.
experimental part, p. 3953 - 3960 (2009/04/10)
We report the discovery of potent benzamide inhibitors of 11β-hydroxysteroid dehydrogenase (11β-HSD1). The optimization and correlation of in vitro and in vivo metabolic stability will be described. Through modifications to our initial lead 2, we discovered pyridyl compound 13. This compound has a favorable pharmacokinetic profile across three species and showed a dose-dependent decrease in adipose 11β-HSD1 activity in a monkey ex vivo pharmacodynamic model.
