- HETEROCYCLIC DERIVATIVES AND USE THEREOF
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Provided are certain URAT1 inhibitors, pharmaceutical compositions thereof, and methods of use thereof.
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Paragraph 182-184
(2021/01/22)
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- PYRAZOLE, ISOTHIAZOLE AND ISOXAZOLE DERIVATIVES USEFUL AS AGRICULTURAL FUNGICIDES
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The present invention relates to substituted pyrazole, isoxazole andisothiazole compounds which are of use in the field of agriculture as fungicides.
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Page/Page column 51; 52
(2019/02/13)
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- HETEROCYCLIC COMPOUND
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The present invention relates to a compound which can be useful for the treatment or prevention of SPT-related diseases including cancer and congenital diseases associated with sphingolipid accumulation (including Niemann-Pick disease).
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Paragraph 0435
(2018/03/25)
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- 4-Arylation of N-Acylamino- and Aminopyrazoles by the Suzuki-Miyaura Cross-Coupling Reaction
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Halogenated aminopyrazoles have rarely been utilized in metal-catalysed cross-coupling reactions mainly due to the complexation of the aminopyrazoles to the metal center, which deactivates the catalyst. In this paper we reveal that the appropriate combination of palladium source and ligand enables efficient Suzuki-Miyaura cross-coupling reactions with even challenging substrates such as halogenated aminopyrazoles. The combination of Pd(OAc)2 and XPhos allowed efficient coupling of halogenated N-acetylaminopyrazoles, whereas XPhos Pd G2 was needed when unprotected aminopyrazoles were used. Generally, the halogenated aminopyrazoles underwent facile cross-coupling reactions with a range of aryl-, heteroaryl-, and styrylboronic acids and esters. The resulting biaryl, bisheteroaryl, or arylalkenyl derivatives were obtained in good-to-high isolated yields.
- Jedinák, Luká?,Canka?, Petr
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p. 2013 - 2023
(2016/04/26)
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