- PERK INHIBITING COMPOUNDS
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Provided herein are compounds of formula (I), compositions, and methods useful for inhibiting PERK and for treating related conditions, diseases, and disorders.
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Paragraph 0183-0184
(2021/03/05)
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- PERK INHIBITORS FOR TREATING VIRAL INFECTIONS
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Provided herein are methods for treating a viral infection in a patient, comprising administering to said patient a therapeutically effective amount of a PERK inhibitor selected from a compound having the structure (I):
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Page/Page column 102-103
(2021/11/20)
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- Synthesis of Amino- and Hydroxymethyl Benzoxaboroles: Prominent Scaffolds for Further Functionalization
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Herein, we describe the development of a short, simple, and efficient synthesis of amino- and hydroxymethyl-substituted benzoxaboroles. The key step in our strategy was the early stage incorporation of the boron by the borylation of an aniline. The formed boronates were then elaborated to the final products in two additional steps, usually in good yields. The synthetic sequence was amenable to be performed on a preparative scale and 4-amino benzoxaborole 4b and 6-hydroxymethyl benzoxaborole 10c have been prepared, without any significant decrease in the overall yield. The amino and hydroxymethyl present at the molecules are useful for further elaboration and/or conjugation to bioactive molecules and therefore we believe that this method should be useful in the development of new compounds for Medicinal Chemistry.
- Fuscaldo, Rodrigo S.,Vontobel, Pedro H. V.,Boeira, Eduam O.,Moro, Angélica V.,Costa, Jessie S. da
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p. 2050 - 2055
(2019/03/07)
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- The: Ortho -substituent on 2,4-bis(trifluoromethyl)phenylboronic acid catalyzed dehydrative condensation between carboxylic acids and amines
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2,4-Bis(trifluoromethyl)phenylboronic acid is a highly effective catalyst for dehydrative amidation between carboxylic acids and amines. Mechanistic studies suggest that a 2:2 mixed anhydride is expected to be the only active species, and the ortho-substituent of boronic acid plays a key role in preventing the coordination of amines to the boron atom of the active species, thus accelerating the amidation. This catalyst works for α-dipeptide synthesis.
- Wang, Ke,Lu, Yanhui,Ishihara, Kazuaki
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supporting information
p. 5410 - 5413
(2018/05/30)
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- Synthesis of trimethylstannyl arylboronate compounds by sandmeyer-type transformations and their applications in chemoselective cross-coupling reactions
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A synthetic method based on Sandmeyer-type reactions to access both tin- and boron-substituted arenes from nitroaniline derivatives is described. This transformation can be applied to the synthesis of a series of functionalized trimethylstannyl arylboronates. In addition, the chemoselective reaction of the Stille and Suzuki-Miyaura cross-coupling reactions is explored, and a series of m- and p-terphenyl derivatives have been synthesized by conducting consecutive one-pot Stille and Suzuki-Miyaura cross-coupling reactions.
- Qiu, Di,Wang, Shuai,Tang, Shengbo,Meng, He,Jin, Liang,Mo, Fanyang,Zhang, Yan,Wang, Jianbo
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p. 1979 - 1988
(2014/04/03)
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- Substituent effects on oxidation-induced formation of quinone methides from arylboronic ester precursors
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A series of arylboronic esters containing different aromatic substituents and various benzylic leaving groups (Br or N+Me3Br -) have been synthesized. The substituent effects on their reactivity with H2O2 and formation of quinone methide (QM) have been investigated. NMR spectroscopy and ethyl vinyl ether (EVE) trapping experiments were used to determine the reaction mechanism and QM formation, respectively. QMs were not generated during oxidative cleavage of the boronic esters but by subsequent transformation of the phenol products under physiological conditions. The oxidative deboronation is facilitated by electron-withdrawing substituents, such as aromatic F, NO2, or benzylic N+Me 3Br-, whereas electron-donating substituents or a better leaving group favor QM generation. Compounds containing an aromatic CH 3 or OMe group, or a good leaving group (Br), efficiently generate QMs under physiological conditions. Finally, a quantitative relationship between the structure and activity has been established for the arylboronic esters by using a Hammett plot. The reactivity of the arylboronic acids/esters and the inhibition or facilitation of QM formation can now be predictably adjusted. This adjustment is important as some applications may benefit and others may be limited by QM generation. Tunable quinone methide formation: Aromatic substituents and the benzylic leaving group strongly affect the H 2O2-induced formation of quinone methides (QMs) from arylboronic esters (see scheme). The reactivity of arylboronic esters can be predictably adjusted by varying substituents. Copyright
- Cao, Sheng,Christiansen, Robin,Peng, Xiaohua
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p. 9050 - 9058
(2013/07/26)
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- SULFONAMIDE COMPOUNDS USEFUL AS CYP17 INHIBITORS
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Disclosed are sulfonamide compounds of Formula (I): or stereoisomers, N-oxides, prodrugs, or pharmaceutically acceptable salts thereof, wherein ring A, R1, R2, R3, R4 and R5 are defined herein. Also disclosed are methods of using such compounds in the treatment of conditions related to CYP17 enzyme, such as cancer, and pharmaceutical compositions comprising such compounds.
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Page/Page column 87
(2012/02/13)
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- A Wulff-type boronate for boronate affinity capture of cis-diol compounds at medium acidic pH condition
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A new Wulff-type boronate was designed and synthesized. Upon immobilization on a polymeric monolith and acidified as boronic acid, the ligand exhibited specific boronate affinity to cis-diol compounds at medium acidic pH condition.
- Li, Hengye,Liu, Yunchun,Liu, Jing,Liu, Zhen
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scheme or table
p. 8169 - 8171
(2011/09/14)
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- OXIDATION RESISTANT INDICATOR MOLECULES
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Compounds having enhanced oxidation stability are disclosed. The compounds have an aryl boronic acid residue having one or more electron withdrawing groups on the aromatic moiety which contains the boronic acid residue, such that the molecule has enhanced
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Page/Page column 52
(2008/12/06)
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- Substituent effect on anthracene-based bisboronic acid glucose sensors
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Earlier we communicated an anthracene-based bisboronic acid sensor for glucose. Aimed at understanding the substituent effect, we have introduced various functional groups, such as the cyano, nitro, and fluoro group on the boronic acid moiety of this gluc
- Kaur, Gurpreet,Fang, Hao,Gao, Xingming,Li, Haibo,Wang, Binghe
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p. 2583 - 2589
(2007/10/03)
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