952041-75-7Relevant academic research and scientific papers
Boron-containing small molecule compound, and preparation method and application thereof
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Paragraph 0074-0076, (2020/07/13)
The invention discloses a novel compound with an anti-tumor effect as shown in a formula I, and a preparation method and application thereof. NOD-SCID mouse transplanted tumor model experiments show that the compounds can inhibit tumor growth. Further res
Construction of spirofused tricyclic frameworks by NHC-catalyzed intramolecular stetter reaction of a benzaldehyde tether with a cyclic exsnone
Hsu, Day-Shin,Cheng, Chiao-Yun
, p. 10832 - 10842 (2019/09/30)
Various benzaldehyde tethers with a cyclic enone were prepared from commercially available 2-hydroxybenzaldehydes via a three-step sequence involving triflate formation, Sonogashira cross-coupling, and regioselective hydrogenation. These substrates were t
Novel S1P1 receptor agonists - Part 4: Alkylaminomethyl substituted aryl head groups
Lescop, Cyrille,Müller, Claus,Mathys, Boris,Birker, Magdalena,De Kanter, Ruben,Kohl, Christopher,Hess, Patrick,Nayler, Oliver,Rey, Markus,Sieber, Patrick,Steiner, Beat,Weller, Thomas,Bolli, Martin H.
supporting information, p. 222 - 238 (2016/04/20)
In a previous communication we reported on the discovery of alkylamino pyridine derivatives (e.g. 1) as a new class of potent, selective and efficacious S1P1 receptor (S1PR1) agonists. However, more detailed profiling revealed that this compound class is phototoxic in vitro. Here we describe a new class of potent S1PR1 agonists wherein the exocyclic nitrogen was moved away from the pyridine ring (e.g. 11c). Further structural modifications led to the identification of novel alkylaminomethyl substituted phenyl and thienyl derivatives as potent S1PR1 agonists. These new alkylaminomethyl aryl compounds showed no phototoxic potential. Based on their in vivo efficacy and ability to penetrate the brain, the 5-alkyl-aminomethyl thiophenes appeared to be the most interesting class. Potent and selective S1PR1 agonist 20e, for instance, maximally reduced the blood lymphocyte count (LC) for 24 h after oral administration of 10 mg/kg to rat and its brain concentrations reached >500 ng/g over 24 h.
SPIROCYCLIC GPR40 MODULATORS
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Page/Page column 225; 226, (2010/04/30)
The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula IA, IB, I'A or I'B, where the definitions of the variables are provided herein. The present invention also
NOVEL AMINOMETHYL BENZENE DERIVATIVES
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Page/Page column 44, (2009/10/22)
The invention relates to novel aminomethyl benzene derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. (I) wherein A represents one of the groups (I), (I), (I) and
CONFORMATIONALLY CONSTRAINED CARBOXYLIC ACID DERIVATIVES USEFUL FOR TREATING METABOLIC DISORDERS
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Page/Page column 239-240, (2009/10/22)
The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I or the general formula III: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.
Synthesis of isocoumarins via palladium catalyzed reactions of methyl 2- (2',2'-dibromovinyl)benzoates
Wang, Le,Shen, Wang
, p. 7625 - 7628 (2007/10/03)
3-Substituted isocoumarins are synthesized in good to excellent yields via palladium catalyzed coupling of 2-(2',2'-dibromovinyl)benzoates and organostannanes. The process involves a Stille reaction, and a subsequent annulation reaction.
