- SELECTIVE INHIBITORS OF PROTEIN ARGININE METHYLTRANSFERASE 5 (PRMT5)
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The disclosure is directed to pharmaceutically acceptable salts of the compound of Formula I (I). Pharmaceutical compositions comprising pharmaceutically acceptable salts of the compound of Formula I, as well as methods of their use and preparation, are also described.
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Paragraph 00226
(2021/04/01)
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- Enantioselective Construction of Spiro Quaternary Carbon Stereocenters via Pd-Catalyzed Intramolecular α-Arylation
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We herein report the development of a sterically hindered and electron-rich P-chiral monophosphorus biaryl ligand that has enabled a general and efficient enantioselective intramolecular α-arylation, providing access to a wide series of [4.4], [4.5], and [4.6]-spirocycles with chiral benzylic quaternary carbons in high yields with good to excellent enantioselectivities. A pronounced water effect on enantioselectivity is observed.
- Wu, Ting,Kang, Xuehua,Bai, Heng,Xiong, Wenrui,Xu, Guangqing,Tang, Wenjun,Tang, Wenjun
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supporting information
p. 4602 - 4607
(2020/06/29)
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- PYRIDO-PYRIMIDINYL COMPOUNDS AND METHODS OF USE
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Provided herein are compounds of formula (I) and pharmaceutically acceptable salts thereof useful in the treatment of IRE 1-related diseases and disorders described herein.
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Paragraph 0806-0807
(2020/09/08)
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- SELECTIVE INHIBITORS OF PROTEIN ARGININE METHYLTRANSFERASE 5
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The disclosure is directed to methods of treatment using compounds of Formula (I).
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Paragraph 00316
(2020/10/19)
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- SPIRO-SULFONAMIDE DERIVATIVES AS INHIBITORS OF MYELOID CELL LEUKEMIA-1 (MCL-1) PROTEIN
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The disclosure is directed to compounds of Formula I (I) Pharmaceutical compositions comprising compounds of Formula I as well as methods of their use and preparation, are also described.
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Paragraph 00485
(2020/06/01)
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- SELECTIVE INHIBITORS OF PROTEIN ARGININE METHYLTRANSFERASE 5 (PRMT5)
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The disclosure is directed to compounds of Formula I Pharmaceutical compositions comprising compounds of Formula I, as well as methods of their use and preparation, are also described.
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- Intramolecular Homolytic Substitution Enabled by Photoredox Catalysis: Sulfur, Phosphorus, and Silicon Heterocycle Synthesis from Aryl Halides
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Aryl radical generation and manipulation constitutes a long-standing challenge in organic synthesis. Photocatalytic single-electron reduction of aryl halides has been established as a premier activation pathway to reach these intermediates. The current st
- Garrido-Castro, Alberto F.,Salaverri, Noelia,Maestro, M. Carmen,Alemán, José
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supporting information
p. 5295 - 5300
(2019/07/03)
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- Substitution-Controlled Selective Formation of Hexahydrobenz[ e]isoindoles and 3-Benzazepines via In(OTf)3-Catalyzed Tandem Annulations
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A dramatic N-substituent controlled tandem annulation of 2-(2-(2-bromoethyl)phenyl)-1-sulfonylaziridines with 1,3-dicarbonyl compounds has been developed. When the N-substituent was a 4-methylbenzenesulfonyl group (Ts), sequential ring opening of aziridin
- Xing, Siyang,Gu, Nan,Wang, Xin,Liu, Jingyi,Xing, Chunyan,Wang, Kui,Zhu, Bolin
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supporting information
p. 5680 - 5683
(2018/09/25)
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- COMPOUNDS USEFUL AS INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE
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The present invention relates to compounds useful as inhibitors of indoleamine 2,3-dioxygenase (IDO). The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various disease
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Paragraph 00181
(2014/06/11)
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- Hydrogen-bonding catalysis and inhibition by simple solvents in the stereoselective kinetic epoxide-opening spirocyclization of glycal epoxides to form spiroketals
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Mechanistic investigations of a MeOH-induced kinetic epoxide-opening spirocyclization of glycal epoxides have revealed dramatic, specific roles for simple solvents in hydrogen-bonding catalysis of this reaction to form spiroketal products stereoselectively with inversion of configuration at the anomeric carbon. A series of electronically tuned C1-aryl glycal epoxides was used to study the mechanism of this reaction based on differential reaction rates and inherent preferences for SN2 versus SN1 reaction manifolds. Hammett analysis of reaction kinetics with these substrates is consistent with an SN2 or SN2-like mechanism (ρ = -1.3 vs ρ = -5.1 for corresponding SN1 reactions of these substrates). Notably, the spirocyclization reaction is second-order dependent on MeOH, and the glycal ring oxygen is required for second-order MeOH catalysis. However, acetone cosolvent is a first-order inhibitor of the reaction. A transition state consistent with the experimental data is proposed in which one equivalent of MeOH activates the epoxide electrophile via a hydrogen bond while a second equivalent of MeOH chelates the side-chain nucleophile and glycal ring oxygen. A paradoxical previous observation that decreased MeOH concentration leads to increased competing intermolecular methyl glycoside formation is resolved by the finding that this side reaction is only first-order dependent on MeOH. This study highlights the unusual abilities of simple solvents to act as hydrogen-bonding catalysts and inhibitors in epoxide-opening reactions, providing both stereoselectivity and discrimination between competing reaction manifolds. This spirocyclization reaction provides efficient, stereocontrolled access to spiroketals that are key structural motifs in natural products.
- Wurst, Jacqueline M.,Liu, Guodong,Tan, Derek S.
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p. 7916 - 7925
(2011/07/08)
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- CYCLIC SULFONAMIDE DERIVATIVES AND METHODS OF THEIR USE
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The present invention is directed to cyclic sulfonamide derivatives of formula (I): or a pharmaceutically acceptable salt thereof, which are monoamine reuptake inhibitors, compositions containing these derivatives, and methods of their use for the prevent
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Page/Page column 209
(2008/12/06)
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