- CYCLIC MOLECULES AS BRUTON'S TYROSINE KINASE INHIBITOR
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The present invention relates to a novel molecule with protein tyrosine kinase inhibitory activity, and the synthesis and usage thereof. Specifically, the present invention relates to compound by formula A, pharmaceutically acceptable salts, hydrates or solvates thereof, and the synthesis and usage thereof.
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Paragraph 0172-0174
(2021/11/26)
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- Platinum(II) cyclometallates featuring broad emission bands and their applications in color-tunable OLEDs and high color-rendering WOLEDs
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Two phosphorescent platinum(ii) cyclometallated complexes with phenoxy groups (1 and 2) have been developed. The modified organic ligands derived by combining the phenoxy moiety and 2-phenylpyridine conferred them with a more flexible structure, leading to superior intermolecular interaction properties of the resulting Pt(ii) metallophosphors. Because of the excimer formation induced by Pt(ii) complexes 1 and 2, the emission color can be tuned over a wide range from cyan to orange by simply increasing the concentration of the Pt(ii) metallophosphors. Inspired by their broad emission band, color tunability and outstanding electroluminescence (EL) performance, these two Pt(ii) phosphors complemented with blue fluorescent emitter 4,4′-bis(9-ethyl-3-carbazovinylene)-1,1′-biphenyl (BCzVBi) were employed in manufacturing high color-rendering white organic light-emitting devices (WOLEDs). In such simple two-emitter systems, 1-based WOLEDs exhibited reasonable EL performance with an external quantum efficiency (ηext) of 11.7%, luminance efficiency (ηL) of 29.1 cd A-1, power efficiency (ηp) of 16.9 lm W-1 and color rendering index (CRI) of 77, whereas 2-based WOLEDs demonstrated an ηext of 10%, ηL of 21.7 cd A-1, ηp of 10.7 lm W-1 and CRI of 88.
- Tan, Guiping,Chen, Shuming,Siu, Chi-Ho,Langlois, Adam,Qiu, Yongfu,Fan, Hongbo,Ho, Cheuk-Lam,Harvey, Pierre D.,Lo, Yih Hsing,Liu, Li,Wong, Wai-Yeung
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p. 6016 - 6026
(2016/07/06)
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- Pyrazolopyrimidine derivative, preparation method, pharmaceutical composition and application
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The invention discloses a pyrazolopyrimidine derivative, a preparation method, a pharmaceutical composition and application. The invention provides the pyrazolopyrimidine derivative as shown in a formula I and stereoisomer or solvate or pharmaceutically acceptable salts or active metabolite or prodrug thereof. The pyrazolopyrimidine derivative as shown in the formula I has good inhibitory activity on Bruton's tyrosine kinase (Btk) and particularly has good in vitro and in vivo inhibitory activity on growth of tumor cells, and a good marketization prospect is achieved. Please see the formula I in the description.
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Paragraph 0336; 0337; 0338
(2017/07/19)
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- Discovery, synthesis, and optimization of antimalarial 4(1 H)-quinolone-3-diarylethers
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The historical antimalarial compound endochin served as a structural lead for optimization. Endochin-like quinolones (ELQ) were prepared by a novel chemical route and assessed for in vitro activity against multidrug resistant strains of Plasmodium falciparum and against malaria infections in mice. Here we describe the pathway to discovery of a potent class of orally active antimalarial 4(1H)-quinolone-3-diarylethers. The initial prototype, ELQ-233, exhibited low nanomolar IC50 values against all tested strains including clinical isolates harboring resistance to atovaquone. ELQ-271 represented the next critical step in the iterative optimization process, as it was stable to metabolism and highly effective in vivo. Continued analoging revealed that the substitution pattern on the benzenoid ring of the quinolone core significantly influenced reactivity with the host enzyme. This finding led to the rational design of highly selective ELQs with outstanding oral efficacy against murine malaria that is superior to established antimalarials chloroquine and atovaquone.
- Nilsen, Aaron,Miley, Galen P.,Forquer, Isaac P.,Mather, Michael W.,Katneni, Kasiram,Li, Yuexin,Pou, Sovitj,Pershing, April M.,Stickles, Allison M.,Ryan, Eileen,Kelly, Jane Xu,Doggett, J. Stone,White, Karen L.,Hinrichs, David J.,Winter, Rolf W.,Charman, Susan A.,Zakharov, Lev N.,Bathurst, Ian,Burrows, Jeremy N.,Vaidya, Akhil B.,Riscoe, Michael K.
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p. 3818 - 3834
(2014/05/20)
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- PYRIDINE COMPOUNDS AND THE USES THEREOF
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The invention relates to substituted pyridine compounds of Formula (I) and the pharmaceutically acceptable salts, prodrugs, and solvates thereof, wherein R1a, A1, A2, E, G, Z1, and Z2 are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of sodium channels. Compounds of the present invention are especially useful for treating pain.
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Page/Page column 204-205
(2012/04/04)
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- Aryl substituted pyrazoles, and pyrroles, and the use thereof
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This invention relates to compounds having the Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein Het and R5-R13are set in the specification. The invention also is directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
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- Preparation process of fluorine substituted aromatic compound
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A preparation process of a fluorine substituted aromatic compound comprising reacting an alkali metal or alkali earth metal salt of an aromatic compound having a hydroxy group with an organic fluorinating agent is disclosed. As a representative fluorinating agent, a bis-dialkylamino-difluoromethane compound, for example, 2,2′-difluoro-1,3-dimethylimidazolidine, is exemplified. According to the process, an industrially useful fluorinated aromatic compound, for example, a fluorobenzene, a fluorine substituted benzophenone, a fluorine substituted diarylsulfone can be prepared with ease in economy without specific equipment.
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