- P2X3 MODULATORS
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Provided herein are P2X3 modulators and methods of utilizing P2X3 modulators in the treatment of diseases, disorders, or conditions. Also described herein are pharmaceutical compositions containing such compounds.
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Paragraph 00294
(2021/08/20)
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- Ni-Catalyzed Formal Cross-Electrophile Coupling of Alcohols with Aryl Halides
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Direct coupling of unactivated alcohols remains a challenge in current synthetic chemistry. We herein demonstrate a strategy building upon in situ halogenation/reductive coupling of alcohols with aryl halides to forge Csp2-Csp3 bonds. The combination of 2-chloro-3-ethylbenzo[d]oxazol-3-ium salt (CEBO) and TBAB as the mild bromination reagents enables rapid transformation of a wide range of alcohols to their bromide counterparts within one to 5 min in CH3CN and DMF, which is compatible with the Ni-catalyzed cross-electrophile coupling conditions in the presence of a chemical reductant. The present method is suitable for arylation of a myriad of structurally complex alcohols with no need for prepreparation of alkyl halides. More importantly, the mild and kinetically rapid bromination process has shown good selectivity in the bromination/arylation of symmetric diols and less sterically hindered hydroxyl groups in polyols, thus offering promise for selective functionalization of diols and polyols without laborious protecting/deprotecting operations. The practicality of this work is also evident in the arylation of a number of carbohydrates, drug compounds, and naturally occurring alcohols.
- Lin, Quan,Ma, Guobin,Gong, Hegui
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p. 14102 - 14109
(2021/11/20)
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- METHODS OF USE FOR INHIBITORS OF AKT ACTIVITY
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Invented is the use of 1 H-imidazo[4,5-c]pyridin-2-yl compounds in the treatment of specified cancers.
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- CYSTEINE PROTEASE INHIBITORS
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Stereoisomers of the formula (III) wherein R is H or C1-C3 optionally halo-substituted alkyl; or pharmaceutically acceptable salts, hydrates or N-oxides thereof have utility in the treatment of disorders mediated by inappropriate exp
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Page/Page column 28; 29
(2008/06/13)
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