745052-92-0Relevant academic research and scientific papers
CONDENSED RING HETEROCYCLIC COMPOUND
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, (2015/06/17)
The ring-fused heterocyclic compound or a pharmaceutically acceptable salt thereof according to the present invention has a T-type calcium channel regulatory effect, and is useful, for example, as a medicament for treating and/or preventing pruritus. The present invention provides a ring-fused heterocyclic compound represented by the following general formula (I) or a pharmaceutically acceptable salt thereof and the like which has a T-type calcium channel regulatory effect and is useful as a therapeutic and/or preventive agent for pruritus, and the like. [wherein, R1 represents optionally substituted lower alkyl and the like, R2 represents optionally substituted lower alkyl and the like, R3 represents the formula (II): (wherein, n represents 0 or 1, R3a represents a hydrogen atom and the like, R3b represents a hydrogen atom and the like, and R3c represents a hydrogen atom and the like) and the like, Q represents a hydrogen atom and the like, and W1 represents a nitrogen atom and the like, W2 represents a nitrogen atom and the like]
SAR, pharmacokinetics, safety, and efficacy of glucokinase activating 2-(4-sulfonylphenyl)-N-thiazol-2-ylacetamides: Discovery of PSN-GK1
Bertram, Lisa S.,Black, Daniel,Briner, Paul H.,Chatfield, Rosemary,Cooke, Andrew,Fyfe, Matthew C. T.,Murray, P. John,Naud, Frédéric,Nawano, Masao,Procter, Martin J.,Rakipovski, Günaj,Rasamison, Chrystelle M.,Reynet, Christine,Schofield, Karen L.,Shah, Vilas K.,Spindler, Felix,Taylor, Amanda,Turton, Roy,Williams, Geoffrey M.,Wong-Kai-In, Philippe,Yasuda, Kosuke
experimental part, p. 4340 - 4345 (2009/05/27)
Allosteric activators of the glucose-sensing enzyme glucokinase (GK) are currently attracting much interest as potential antidiabetic therapies because they can achieve powerful blood glucose lowering through actions in multiple organs. Here, the optimization of a weakly active high-throughput screening hit to (2R)-2-(4-cyclopropanesulfonylphenyl)-N-(5-fluorothiazol-2-yl)-3- (tetrahydropyran-4-yl)propionamide (PSN-GK1), a potent GK activator with an improved pharmacokinetic and safety profile, is described. Following oral administration, this compound elicited robust glucose lowering in rats.
TRICYCLO SUBSTITUTED AMIDES
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Page/Page column 13, (2008/06/13)
Compounds of Formula (I) or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.
ENANTIOSELECTIVE PROCESS
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Page/Page column 12, (2008/06/13)
A process for the production of compounds comprising the enantioselective hydrogenation of 2-substituted acrylic acid derivatives.
FLUORINATION PROCESS OF PROTECTED AMINOTHIAZOLE
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Page/Page column 14, (2010/10/20)
A process for the production of fluorinated compound formula (I) comprising fluorination of a protected aminothiazole. Compounds formula (I) are useful in the preparation of activators of glucokinase.
TRI(CYCLO) SUBSTITUTED AMIDE COMPOUNDS
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Page 31, (2008/06/13)
Compounds of Formula (I): or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.
TRI(CYCLO) SUBSTITUTED AMIDE GLUCOKINASE ACTIVATOR COMPOUNDS
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Page 29, (2010/02/08)
Compounds of Formula (I): (I) or pharmaceutically acceptable salts or N-oxides thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.
