- CONDENSED RING HETEROCYCLIC COMPOUND
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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]
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Paragraph 0341
(2015/06/17)
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- SAR, pharmacokinetics, safety, and efficacy of glucokinase activating 2-(4-sulfonylphenyl)-N-thiazol-2-ylacetamides: Discovery of PSN-GK1
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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.
- 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
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experimental part
p. 4340 - 4345
(2009/05/27)
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- TRICYCLO SUBSTITUTED AMIDES
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Compounds of Formula (I) or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.
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Page/Page column 13
(2008/06/13)
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- ENANTIOSELECTIVE PROCESS
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A process for the production of compounds comprising the enantioselective hydrogenation of 2-substituted acrylic acid derivatives.
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Page/Page column 12
(2008/06/13)
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- FLUORINATION PROCESS OF PROTECTED AMINOTHIAZOLE
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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.
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Page/Page column 14
(2010/10/20)
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- TRI(CYCLO) SUBSTITUTED AMIDE COMPOUNDS
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Compounds of Formula (I): or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.
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- TRI(CYCLO) SUBSTITUTED AMIDE GLUCOKINASE ACTIVATOR COMPOUNDS
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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.
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