200064-11-5Relevant articles and documents
Azaindole derivative myelocyte proliferation inhibitor, preparation method thereof, and application of inhibitor in pharmacy
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Paragraph 0163-0165, (2021/08/07)
The invention provides an azaindole derivative myeloid proliferation inhibitor as shown in a formula I. In the formula, R1, R2 and R33 are as defined in the specification. The compound shown in the formula I can be used for remarkably inhibiting the proliferation of myeloid cells represented by MOLM-16, HL-60 and MV-4-11 and related diseases of the myeloid cells. The compound shown in the formula I or the salt thereof or the related pharmaceutical composition provided by the invention has excellent in-vivo and in-vitro inhibitory activity, good druggability and high bioavailability, and does not have obvious injury to visceral organs. Therefore, the compound shown in the formula I or the salt thereof and the related pharmaceutical composition have huge clinical application prospects.
NOVEL COMPOUNDS AS NADPH OXIDASE INHIBITORS
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Paragraph 0265; 0266; 0267, (2020/04/09)
The present invention is related to new compounds, pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).
The Cyclopropane Ring as a Reporter of Radical Leaving-Group Reactivity for Ni-Catalyzed C(sp3)-O Arylation
Mills, L. Reginald,Monteith, John J.,Dos Passos Gomes, Gabriel,Aspuru-Guzik, Alán,Rousseaux, Sophie A. L.
supporting information, p. 13246 - 13254 (2020/09/01)
The ability to understand and predict reactivity is essential for the development of new reactions. In the context of Ni-catalyzed C(sp3)-O functionalization, we have developed a unique strategy employing activated cyclopropanols to aid the design and optimization of a redox-active leaving group for C(sp3)-O arylation. In this chemistry, the cyclopropane ring acts as a reporter of leaving-group reactivity, since the ring-opened product is obtained under polar (2e) conditions, and the ring-closed product is obtained under radical (1e) conditions. Mechanistic studies demonstrate that the optimal leaving group is redox-active and are consistent with a Ni(I)/Ni(III) catalytic cycle. The optimized reaction conditions are also used to synthesize a number of arylcyclopropanes, which are valuable pharmaceutical motifs.
INDOLE AHR INHIBITORS AND USES THEREOF
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Paragraph 00224, (2020/05/21)
The present invention provides compounds useful as inhibitors of AHR, compositions thereof, and methods of using the same.
HISTONE METHYLTRANSFERASE EZH2 INHIBITOR, PREPARATION METHOD AND PHARMACEUTICAL USE THEREOF
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Paragraph 0568-0569, (2019/11/22)
The invention relates to a histone methyltransferase EZH2 inhibitor, a preparation method and pharmaceutical use thereof. In particular, the invention relates to a compound represented by the general formula (I), a preparation method thereof, a pharmaceut
ANTHELMINTIC DEPSIPEPTIDE COMPOUNDS
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Page/Page column 221, (2018/06/06)
The present invention provides cyclic depsipeptide compounds of formula (I) wherein the stereochemical configuration of at least one carbon atom bearing the groups Cy1, Cy2, R1, R2, R3, R4, Ra and Rb is inverted compared with the naturally occurring cyclic depsipeptide PF1022A. The invention also provides compositions comprising the compounds that are effective against parasites that harm animals. The compounds and compositions may be used for combating parasites in or on mammals and birds. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in birds and mammals.
Bicyclic alkaloid compound, preparation method and applications thereof
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Paragraph 0163; 0164, (2018/11/03)
The present invention relates to a bicyclic alkaloid compound, or a tautomer, a stereoisomer, a racemate, the non-equal mixture of enantiomers, a geometric isomer, a solvate, a pharmaceutically acceptable salt or a prodrug thereof, and a pharmaceutical composition containing the compound. The invention further discloses uses of the compounds and the pharmaceutical composition thereof as drugs, especially as anti-inflammatory drugs and anti-fibrotic drugs.
Remote migratory cross-electrophile coupling and olefin hydroarylation reactions enabled by in situ generation of nih
Chen, Fenglin,Chen, Ke,Zhang, Yao,He, Yuli,Wang, Yi-Ming,Zhu, Shaolin
supporting information, p. 13929 - 13935 (2017/11/07)
A highly efficient strategy for remote reductive cross-electrophile coupling has been developed through the ligand-controlled nickel migration/arylation. This general protocol allows the use of abundant and bench-stable alkyl bromides and aryl bromides for the synthesis of a wide range of structurally diverse 1, 1-diarylalkanes in excellent yields and high regioselectivities under mild conditions. We also demonstrated that alkyl bromide could be replaced by the proposed olefin intermediate while using n-propyl bromide/Mn0 as a potential hydride source.
Inverting Conventional Chemoselectivity in Pd-Catalyzed Amine Arylations with Multiply Halogenated Pyridines
Keylor, Mitchell H.,Niemeyer, Zachary L.,Sigman, Matthew S.,Tan, Kian L.
supporting information, p. 10613 - 10616 (2017/08/15)
A new catalyst system capable of selective chloride functionalization in the Pd-catalyzed amination of 3,2- and 5,2- Br/Cl-pyridines is reported. A reaction optimization strategy employing ligand parametrization led to the identification of 1,1′-bis[bis(dimethylamino)phosphino]ferrocene "DMAPF", a readily available yet previously unutilized diphosphine, as a uniquely effective ligand for this transformation.
ANTHELMINTIC DEPSIPEPTIDE COMPOUNDS
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Page/Page column 310, (2017/07/14)
The present invention provides cyclic depsipeptide compounds of formula (I) and compositions comprising the compounds that are effective against parasites that harm animals, including humans. The compounds and compositions may be used for combating parasites in or on animals including mammals and birds. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in animals, including birds and mammals.