- Immunomodulator
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The invention discloses an immunomodulator, and particularly relates to compounds for inhibiting IL-17A and application of the compounds serving as the immunomodulator in preparation of drugs. The invention discloses an application of a compound shown as a formula I or a stereoisomer thereof in preparing medicines for inhibiting IL-17A, and provides a new choice for clinically screening and/or preparing medicines for treating diseases related to IL-17A activity.
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- Intermediate compound of immunomodulator
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The present invention relates to an intermediate compound of an IL-17A immunomodulator compound. The IL17A immunomodulator compound synthesized by the intermediate compound provided by the invention has good IL-17A inhibition activity.
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- Immunomodulator
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The invention discloses an immunomodulator, and particularly relates to a compound shown as a formula I, or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof. Experiments prove that the compound has good IL-17A inhibitory activity, can be used for preparing an IL-17A inhibitor and drugs for preventing and/or treating IL-17A mediated diseases (such as inflammation, autoimmune diseases, infectious diseases, cancers and precancerous syndromes), and provides a new medical possibility for clinical treatment of diseases related to abnormal IL-17A activity.
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- Chromium-Catalyzed Asymmetric Dearomatization Addition Reactions of Halomethyl Heteroarenes
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The first asymmetric dearomatization addition reaction of halomethyl arenes including benzofuran and benzothiophene was enabled by chromium catalysis. A variety of aldehydes served as suitable electrophiles under mild reaction conditions. Molecular complexities are quickly increased in a highly diastereo- and enantioselective manner.
- Tian, Qingshan,Bai, Jing,Chen, Bin,Zhang, Guozhu
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supporting information
p. 1828 - 1831
(2016/05/19)
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- MONOAMINE RE-UPTAKE INHIBITORS AND METHODS RELATING THERETO
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Monoamine re-uptake inhibitors and more specifically serotonin and noradrenaline re-uptake inhibitors are disclosed that have utility in the treatment of disorders of the central or peripheral nervous system in both men and women. The compounds of this invention have the structure: wherein R1, R2, R3, R4, R5, R6, m, n, W, X, Y, and Z are as defined herein, including stereoisomers, prodrugs and pharmaceutically acceptable salts, esters and solvates thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting monoamine re-uptake in a subject in need thereof.
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Page/Page column 16
(2010/11/25)
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- Biocatalytic asymmetric dihydroxylation of conjugated mono-and poly-alkenes to yield enantiopure cyclic cis-diols
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Dioxygenase-catalysed asymmetric dihydroxylation, of a series of conjugated monoalkenes and polyenes, was found to yield the corresponding monols and 1,2-dihydrodiols. The diol metabolites were obtained from monosubstituted, gem-disubstituted, cis-disubstituted, and trisubstituted alkene substrates, using whole cells of Pseudomonas putida strains containing toluene and naphthalene dioxygenases. Dioxygenase selection and alkene type were established as important factors, in the preference for dioxygenase-catalysed 1,2-dihydroxylation of conjugated alkene or arene groups, and monohydroxylation at benzylic or allylic centres. Competition from allylic hydroxylation of methyl groups was observed only when naphthalene dioxygenase was used as biocatalyst. The structures, enantiomeric excess values and absolute configurations of the bioproducts, were determined by a combination of stereochemical correlation, spectroscopy (NMR and CD) and X-ray diffraction methods. cis-1,2-Diol metabolites from arenes, cyclic alkenes and dienes were generally observed to be enantiopure (> 98% ee), while 1,2-diols from acyclic alkenes had lower enantiomeric excess values (2-symmetrical ketone.
- Boyd, Derek R.,Sharma, Narain D.,Bowers, Nigel I.,Brannigan, Ian N.,Groocock, Melanie R.,Malone, John F.,McConville, Gareth,Allen, Christopher C. R.
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p. 1081 - 1089
(2007/10/03)
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- Regioselectivity of Radical-induced Bond Cleavages in Epoxides
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Radical-induced carbon-carbon and carbon-oxygen bond cleavage reactions in a highly substituted epoxide, and in epoxides fused to other rings are reported.Substitution at the site of the developing radical assists C-C bond cleavage.In ring-fused epoxides, C-C bond cleavage was not seen where stereoelectronic factors oppose it.
- Murphy, John A.,Patterson, Christopher W.
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p. 405 - 410
(2007/10/02)
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