- Heterocyclic compound and preparation and application thereof
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The invention relates to bromodomain inhibitors, and provides a compound represented by a general formula I, a pharmaceutically acceptable salt, an enantiomer, a diastereoisomer, an atropisomer, a racemate, a polymorph, a solvate or an isotope-labeled compound (including deuterium substitution) thereof, a preparation method thereof, a pharmaceutical composition containing the same, and applicationthereof in pharmacy.
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Paragraph 0324-0326
(2020/07/24)
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- Characterization of Histone Deacetylase 8 (HDAC8) Selective Inhibition Reveals Specific Active Site Structural and Functional Determinants
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Metal-dependent histone deacetylases (HDACs) are key epigenetic regulators that represent promising therapeutic targets for the treatment of numerous human diseases. Yet the currently FDA-approved HDAC inhibitors nonspecifically target at least several of
- Marek, Martin,Shaik, Tajith B.,Heimburg, Tino,Chakrabarti, Alokta,Lancelot, Julien,Ramos-Morales, Elizabeth,Da Veiga, Cyrielle,Kalinin, Dmitrii,Melesina, Jelena,Robaa, Dina,Schmidtkunz, Karin,Suzuki, Takayoshi,Holl, Ralph,Ennifar, Eric,Pierce, Raymond J.,Jung, Manfred,Sippl, Wolfgang,Romier, Christophe
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p. 10000 - 10016
(2018/11/23)
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- TRIAZOLOPYRAZINE COMPOUNDS USEFUL FOR THE TREATMENT OF DEGENERATIVE & INFLAMMATORY DISEASES
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Novel [1.2.4]triazolo[1,5-a]pyrazine compounds are disclosed that have a formula represented by the following (formula I). The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, arthritis, inflammation, and others.
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- Fused heterocyclic benzenecarboxamide derivatives and PGD2 antagonists comprising them
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PCT No. PCT/JP97/04526 Sec. 371 Date May 28, 1999 Sec. 102(e) Date May 28, 1999 PCT Filed Dec. 10, 1997 PCT Pub. No. WO98/25915 PCT Pub. Date Jun. 18, 1998A compound, pharmaceutically acceptable salt thereof, or hydrate thereof having a PGD2-antagonistic activity, and an inhibitory activity against infiltration of eosinophils, useful for treating mast cell dysfunction-associated diseases, such as systemic mastocytosis and disorder of systemic mast cell activation, as well as tracheal contraction, asthma, allergic rhinitis, allergic conjunctivitis, urticaria, ischemic reperfusion injury, inflammation and atopic dermatitis, which is shown by the formula (I): is provided.
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