- Tricyclic compound serving as PRMT5 inhibitor and application of tricyclic compound
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The invention belongs to the field of medical chemistry, relates to a tricyclic compound serving as a PRMT5 inhibitor and an application of the tricyclic compound, and particularly provides a compoundshown as a formula (I) or an isomer, pharmaceutically acceptable salt, a solvate, crystal or prodrug of the compound, a preparation method thereof and pharmaceutical compositions containing the compounds and the use of these compounds or compositions for the treatment of PRMT5 mediated diseases. The compound provided by the invention shows significant inhibitory activity on PRMT5.
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Paragraph 0180; 0182-0184
(2021/01/04)
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- Synthesis and bioactivities of novel 4,5,6,7-tetrahydrothieno[2,3-c]pyridines as inhibitors of tumor necrosis factor-alpha (TNF-alpha) production.
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Novel 4,5,6,7-tetrahydrothieno[2,3-c]pyridine derivatives were synthesized and evaluated for their abilities to inhibit lipopolysaccharide (LPS)-stimulated production of TNF-alpha in rat whole blood. Several of these compounds exhibited potent inhibitory activity.
- Fujita, Masakazu,Seki, Taketsugu,Inada, Haruaki,Ikeda, Naoko
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p. 1607 - 1611
(2007/10/03)
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- TRIAZOLO-1,4-DIAZEPINE DERIVATIVES AND THEIR USE IN PHARMACEUTICALS
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A triazolo-1,4-di-azepine compound of the below given formulas and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to allergic diseases. STR1 in which R1 and R2 are hydrogen or an alkyl, R3 is hydrogen or a halogen, R4 is hydrogen or an alkyl, X is--OCO--,--NHCO--,--CO--or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.
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- Synthesis and stereospecific antipsychotic activity of (-) 1 cyclopropylmethyl 4 (3 trifluoromethylthio 5H dibenzo[a,d]cyclohepten 5 ylidene)piperidine
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The synthesis and resolution of 3-iodocyproheptadine [(±)-5a] and a-cyclopropylmethyl-4-(3-iodo-5H-dibenzo-[a,d]cyclohepten-5-ylidene) piperidine [(±)-5b] are described. The resulting atropisomers undergo reaction with trifluoromethylthiocopper to give optically active products without extensive racemization. In this manner, optically pure (+)- and (-) 3-trifluoromethylthiocyproheptadine [(+)-6a and (-)-6a, respectively] and (+)- and (-)-1-cyclopropylmethyl-4-(3-trifluoromethylthio-5H-dibenzo[a,d]cyclohepten5-ylidene) piperidine [(+)-6b and (-)-6b, respectively] have been prepared. The influence of a chiral europium shift reagent on the proton and fluorine resonance signals as a diagnostic tool for the determination of the optical purities of these atropisomers is discussed. The four compounds, (+)-6a, (-)-6a,(+)-6b, and (-)-6b, were studied in squirrel monkeys for their ability to block conditioned avoidance responding. All of the antiavoidance activity was found to reside solely in the levorotatory compounds (-)-6a and (-)-6b. Further comparison of the enantiomers (-)-6b and (+)-6b showed that the ability to antagonize apomorphine-induced stereotyped behavior is confined to the levorotatory isomer (-)-6b while weak central anticholinergic activity resides solely in the dextrorotatory isomer (+)-6b. Neither (-)-6b nor (+)-6b has significant peripheral anticholinergic activity.
- Remy,Rittle,Hunt,Anderson,Arison,Engelhardt,Hirschmann,Clineschmidt,Lotti,Bunting,Ballentine,Papp,Flataker,Witoslawski,Stone
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p. 1013 - 1019
(2007/10/10)
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