- 6,7-DIHYDROPYRAZOLO[1,5-a]PYRAZINONE DERIVATIVE AND MEDICAL APPLICATION THEREOF
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Provided are a compound that is useful for the prevention of and/or as a treatment agent for a disease in which a group II mGlu receptor is involved; and a medical application of said compound. Provided is a compound repesented by formula (I) or a pharmaceutically acceptable salt thereof. (In the formula, R1 and R2 independently represent a hydrogen atom, a C1-4 alkyl or the like; ring A represents a C6-10 aromatic carbon ring group, a 4 to 10 membered saturated heterocyclic group or the like; R3 and R4 independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl, a C1-4 alkoxy or the like; R5 and R6 independently represent a hydrogen atom, a C1-6 alkyl, a C1-6 alkoxy, an-NRaRb or the like; Ra and Rb independently represent a hydrogen atom, a C1-4 alkyl or the like; X represents a nitrogen atom or a -CRe-; and Re represents a hydrogen atom, a halogen atom, a C1-6 alkyl or the like).
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Paragraph 0159-0160
(2020/11/23)
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- Substituted thiazole derivative and application thereof
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The invention provides a compound represented by a general formula (I), or a stereoisomer, pharmaceutically acceptable salt, solvate, hydrate, chemically protective form or prodrug thereof. The compound has an effect of inhibiting adenosine receptor 2a (A2a), and can be used as an antagonist of the adenosine receptor 2a (A2A) for treating tumors.
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Paragraph 0255-0256; 0300-0304
(2019/02/13)
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- Preparation method of olprinone and 9-azaindole-5-boric acid
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The invention relates to a preparation method of olprinone and 9-azaindole-5-boric acid, in particular to a method for preparing olprinone via Suzuki coupling. In the preparation method of olprinone and 9-azaindole-5-boric acid, a converging synthetic route is innovatively designed, has high atom utilization rate as compared with existing three series synthetic processes and is better than existing synthetic routes in overall reaction yield; the preparation method has mild synthetic reaction conditions, is simple to perform and is easy to industrialize; the prepared olprinone may be further olprinone hydrochloride via salifying, and the prepared olprinone hydrochloride has the advantages such as low impurity content, high purity, high yield and good mildness of reaction conditions.
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Paragraph 0023; 0026; 27
(2017/07/15)
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