681508-62-3Relevant articles and documents
TETRAHYDRONAPHTHALENE DERIVATIVE
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Paragraph 0141, (2018/12/13)
A compound shown by general formula (I-1) (in the formula, all symbols are as stated in the specification.) has selective S1P5 receptor-binding activity. Adjusting this activity make s it possible to obtain a therapeutic agent for S1P5-mediated diseases,
Structure-activity relationship studies and sleep-promoting activity of novel 1-chloro-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as dual orexin receptor antagonists. Part 2
Sifferlen, Thierry,Koberstein, Ralf,Cottreel, Emmanuelle,Boller, Amandine,Weller, Thomas,Gatfield, John,Brisbare-Roch, Catherine,Jenck, Francois,Boss, Christoph
, p. 3857 - 3863 (2013/07/27)
Replacement of the dimethoxyphenyl moiety in the core skeleton of almorexant by appropriately substituted imidazoles afforded novel 1-chloro-5,6,7,8-tetrahydroimidazo[1,5-a]pyrazine derivatives as potent dual orexin receptor antagonists. We describe in th
The inhibition of monoamine oxidase by 8-(2-phenoxyethoxy)caffeine analogues
Strydom,Bergh,Petzer
, p. 513 - 518 (2013/01/15)
Previous studies have documented that substituted 8-oxycaffeines act as inhibitors of human monoamine oxidase (MAO) B. A particularly potent inhibitor among the reported compounds was 8-(2-phenoxyethoxy)caffeine with an IC 50 value of 0.383M towards MAO-B. In an attempt to improve on the inhibition potency of this compound and to discover highly potent reversible MAO-B inhibitors, in the present study, a series of 8-(2-phenoxyethoxy)caffeine analogues containing various substituents on C4 of the phenoxy ring, were synthesized and evaluated as inhibitors of human MAO-A and -B. The results show that the 8-(2-phenoxyethoxy)caffeine analogues are selective and reversible MAO-B inhibitors with the most potent homologue, 8-{2-[4-(trifluoromethyl) phenoxy]ethoxy}caffeine, exhibiting an IC50 value of 0.061μM. These highly potent inhibitors are useful leads in the design of therapies for neurodegenerative disorders such as Parkinsons disease. Georg Thieme Verlag KG Stuttgart New York.
NOVEL DICHLOROPROPENE DERIVATIVES
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Page/Page column 44, (2010/02/14)
Formula (I), wherein X represents a group -O-A1- or a group -N=A2-, Y represents a single bond, O or S, or X and Y together may represent O, Q represents an aryl group that may be optionally substituted, a heterocyclic group that may
Amination of aryl halides using copper catalysis
Lang, Fengrui,Zewge, Daniel,Houpis, Ioannis N.,Volante
, p. 3251 - 3254 (2007/10/03)
Bromopyridine 4 was converted into aminopyridine 5 under Cu2O catalysis with an ethylene glycol solution of ammonia in excellent yield (90%). The amination reaction features low (0.5 mol%) catalyst loading, mild reaction temperature (80°C) and low reaction pressure (50 psi). This protocol is further studied in the amination of a variety of aryl halides.