69526-89-2Relevant academic research and scientific papers
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.
HETEROCYCLIC MODULATORS OF LIPID SYNTHESIS FOR USE AGAINST CANCER AND VIRAL INFECTIONS
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Page/Page column 36-37, (2016/03/29)
Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatly acid synthase pathway by the administration of such compounds. (I)
HETEROCYCLIC MODULATORS OF LIPID SYNTHESIS AND COMBINATIONS THEREOF
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Page/Page column 80; 81, (2015/07/07)
Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds and combinations of such compounds and other therapeutic agents.
HETEROCYCLIC MODULATORS OF LIPID SYNTHESIS
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Page/Page column 66, (2014/01/18)
Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds.
Imidazopyridine-based fatty acid synthase inhibitors that show anti-HCV activity and in vivo target modulation
Oslob, Johan D.,Johnson, Russell J.,Cai, Haiying,Feng, Shirley Q.,Hu, Lily,Kosaka, Yuko,Lai, Julie,Sivaraja, Mohanram,Tep, Samnang,Yang, Hanbiao,Zaharia, Cristiana A.,Evanchik, Marc J.,McDowell, Robert S.
supporting information, p. 113 - 117 (2013/02/26)
Potent imidazopyridine-based inhibitors of fatty acid synthase (FASN) are described. The compounds are shown to have antiviral (HCV replicon) activities that track with their biochemical activities. The most potent analogue (compound 19) also inhibits rat FASN and inhibits de novo palmitate synthesis in vitro (cell-based) as well as in vivo.
NOVEL AMINOMETHYL BENZENE DERIVATIVES
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, (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
