- BTK Inhibitors and uses thereof
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The invention discloses a bruton's tyrosine kinase (BTK) inhibitor and use thereof. Specifically, the invention provides heteroaromatic compounds or stereoisomers, geometrical isomers, tautomers, racemates, nitrogen oxides, hydrates, solvates, metabolites and pharmaceutically acceptable salts or prodrugs thereof, and pharmaceutical compositions containing the heteroaromatic compounds; the invention also discloses use of the heteroaromatic compounds or the pharmaceutical compositions containing the heteroaromatic compounds in preparation of medicines; the medicines can be used for treating autoimmune diseases, inflammatory diseases or proliferative diseases.
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Paragraph 1667-1672
(2020/05/02)
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- BENZOSULFONYL COMPOUNDS
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Provided herein are compounds and pharmaceutical compositions comprising said compounds that are useful for treating cancers. Specific cancers include those that are mediated by YAP/TAZ or those that are modulated by the interaction between YAP/TAZ and TEAD.
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Paragraph 00459
(2019/03/12)
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- Anthracene compound, preparing method of anthracene compound and organic light-emitting device
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The invention provides an anthracene compound. The anthracene compound has a structure in the formula (I), wherein Q is the C1-60 alkyl group or the C6-60 aryl group or the C5-60 condensed ring group or the C5-60 heterocyclic group; Ar is the C6-60 aryl group or the C5-60 condensed ring group or the C5-60 heterocyclic group; and Ar1 is H, the C1-60 alkyl group, the C1-60 alkoxy group, the C1-60 ether group, the C6-60 aryl group, the C6-60 condensed ring group, the C6-60 heterocyclic group and the C6-60 arylamine group. Compared with the prior art, the anthracene compound is connected with an aromatic compound through anthracene, and the Q, Ar and Ar1 groups are introduced, so that a device emits blue light after the organic compound is applied to the organic light-emitting device; and meanwhile, the means that the above groups are used for adjusting the light-emitting wavelength is adopted, the light-emitting efficiency of the organic light-emitting device is high, and the service life is long.
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Paragraph 0121-0126
(2017/05/02)
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- Polycyclic aromatic compound
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The present invention addresses the problem of providing a novel polycyclic aromatic compound and an organic electroluminescent element using the same. The above problem is solved by providing a novel polycyclic aromatic compound in which a plurality of aromatic rings are connected by boron atoms, oxygen atoms, or the like, thereby increasing the number of options for organic EL element materials, and also solved by providing a superior organic EL element using said novel polycyclic aromatic compound as an organic EL element material.
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Paragraph 1079; 1080; 1081
(2016/10/08)
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- Visible-light-mediated synthesis of diaryl ethers from arylboronic acids and diaryliodonium salts
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With visible-light irradiation, a simple and metal-free photocatalytic system for the synthesis of diaryl ethers from arylboronic acids and diaryliodonium salts has been developed. The reaction proceeded in high yield for a range of different substrates in the presence of eosin Y under mild reaction conditions.
- Liu, Li,Tang, Jiaqi,Qiang, Jian,Li, Jian,He, Mingyang
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p. 261 - 264
(2016/07/06)
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- Anchoring of Pd(ii) complex in functionalized MCM-41 as an efficient and recoverable novel nano catalyst in C-C, C-O and C-N coupling reactions using Ph3SnCl
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Anchored palladium(ii) in functionalized MCM-41 mesoporous silica was prepared and used as an efficient, recoverable and thermally stable heterogeneous nano catalyst for C-C, C-O and C-N bond formation in cross-coupling reactions in the presence of Ph3SnCl. MCM-41 was prepared trough hydrothermal synthesis using tetraethyl orthosilicate (Si(OC2H5)4) as silica source and cetyltrimethylammonium bromide (CTAB) as a template. The structure of functionalized MCM-41 was studied by FT-IR, XRD, SEM, TEM, TGA, EDS, ICP and BET techniques.
- Ghorbani-Choghamarani, Arash,Nikpour, Farzad,Ghorbani, Farshid,Havasi, Forugh
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p. 33212 - 33220
(2015/04/27)
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- Triphenyltin chloride as a new source of phenyl group for C-heteroatom and C-C bond formation
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Ph3SnCl is introduced as a very suitable source of phenyl group for coupling with phenols, amines, and thiols in the presence of Cu(OAc)2 in Et3N at room temperature to give aryl ethers, amines, and arylthio ethers in high yields. In addition, the application of Ph3SnCl in the Stille coupling of aryl halides in the presence of Pd(0) catalyst in PEG 400 at 110C is discussed.
- Iranpoor, Nasser,Firouzabadi, Habib,Elham, Etemadi Davan,Rostami, Abed,Nematollahi, Arash
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p. 123 - 130
(2013/10/01)
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- Design, synthesis, enzyme inhibition, and tumor cell growth inhibition of 2-anilinobenzamide derivatives as SIRT1 inhibitors
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A series of 2-anilinobenzamide derivatives were designed, synthesized and evaluated for their SIRT1-inhibitory activity. Among these, compounds 3 and 5 inhibited SIRT1 activity in enzyme assays and suppressed the growth of Daudi and HCT116 cells.
- Suzuki, Takayoshi,Imai, Keiko,Imai, Erika,Iida, Shinsuke,Ueda, Ryuzo,Tsumoto, Hiroki,Nakagawa, Hidehiko,Miyata, Naoki
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experimental part
p. 5900 - 5905
(2009/12/24)
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- Organic compounds
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Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula I
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Page/Page column 25-26
(2008/06/13)
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- Structure-activity relationship studies on ortho-substituted cinnamic acids, a new class of selective EP3 antagonists
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A series of novel ortho-substituted cinnamic acids have been synthesized, and their binding activity and selectivity on the four prostaglandin E 2 receptors evaluated. Many of them are very potent and selective EP3 antagonists (Ki 3-10 nM), while compound 9 is a very good and selective EP2 agonist (Ki 8 nM). The biological profile of the EP2 agonist 9 in vivo and the metabolic profile of selected EP3 antagonists are also reported.
- Belley, Michel,Gallant, Michel,Roy, Bruno,Houde, Karine,Lachance, Nicolas,Labelle, Marc,Trimble, Laird A.,Chauret, Nathalie,Li, Chun,Sawyer, Nicole,Tremblay, Nathalie,Lamontagne, Sonia,Carriere, Marie-Claude,Denis, Danielle,Greig, Gillian M.,Slipetz, Deborah,Metters, Kathleen M.,Gordon, Robert,Chan, Chi Chung,Zamboni, Robert J.
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p. 527 - 530
(2007/10/03)
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- 2-FURANCARBOXYLIC ACID HYDRAZIDES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
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The present invention provides 2-furancarboxylic acid hydrazide compounds represented by General Formula(I) below, and prodrugs, physiologically acceptable salts, hydrates, solvates thereof, methods for producing them and pharmaceutical compositions containing them: wherein A is a group represented by Formula (a) or the like: (wherein either R4 or R5 represents cyano, nitro or the like, and the other represents a hydrogen atom or the like); either R1 or R2 represents a group: -D-(X)m-R6 or the like, and the other represents a group: -E-(Y)n-R7, hydrogen atom, aryl or the like; R3 is a hydrogen atom or the like; D and E independently represent aryl; X and Y independently represent 0 or the like; R6 and R7 independently represent alkyl, aryl, arylalkyl or the like; and m and n are independently 0 or 1, provided that the aryl is optionally substituted. Such compounds exhibit a potent antagonistic activity on glucagon receptor and are of use as preventive and/or therapeutic agents for symptoms and diseases in which glucagon is involved.
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- Synthesis and characterization of 32 polybrominated diphenyl ethers
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Polybrominated diphenyl ethers (PBDEs) are widely used as additive flame retardants in, for example, textiles, computers, television sets, and other electrical appliances. present also in humans. The environmental levels of the PBDEs are, however, still in general lower than those of polychlorinated biphenyls (PCBs). However, while the levels of PCBs generally are decreasing, those of the PBDEs are increasing in, for example, human milk. In the present study 32 individual PBDE congeners were synthesized and characterized. Physicochemical parameters including melting points and UV, 1H NMR, and mass spectra are reported Twenty-nine monobrominated to heptabrominated diphenyl ethers were synthesized by the couping between four diphenyliodonium salts and nine phenolates. One tetrabromodiphenyl ether and two hexabromodiphenyl ethers were synthesized by bromination of two different PBDEs. Twenty-one of the PBDEs and two of the iodonium salts, 2,2′,4,4′-tetrabromodiphenyliodonium chloride and 3,3′,4,4′-tatrabromodiphenyliodonium chloride, are to the authors' knowledge described for the first time. These synthesized reference compounds will aid in the identification and quantification of PBDEs present in environmental samples and will allow further assessment of PBDE toxicity.
- Marsh, Goeran,Hu, Jiwei,Jakobsson, Eva,Rahm, Sara,Bergman, Aeke
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p. 3033 - 3037
(2007/10/03)
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- Synthesis and Characterization of Polybrominated Diphenyl Ethers - Unlabelled and Radiolabelled Tetra,- Penta- and Hexa-bromodiphenyl Ethers
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Diphenyl ether, 3-bromodiphenyl ether and 3,3'-dibromodiphenyl ether have been synthesized via coupling of the appropriate phenol and bromobenzene.Each of these compounds was subsequently brominated to (i) 2,2',4,4'-tetrabromodiphenyl ether, (ii) 2,2'3,4,
- Oern, Ulrika,Eriksson, Lars,Jakobsson, Eva,Bergman, Ake
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p. 802 - 807
(2007/10/03)
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- Polar Radicals. 17. On the Mechanism of Iodine Atom Transfer. A 9-I-2 Intermediate
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The atom-transfer reaction of iodine from an aryl iodide to a phenyl radical has been shown to proceed via a 9-I-2 ntermediate.The relative kinetics of the reactions of the intermediate were investigated by studying its mode of decomposition upon formation from the reduction of a series of unsymmetrically substituted diaryliodonium salts.The iodonium salts were reduced by the electron-transfer reactions with several reagents: di-tert-butyl nitroxide, sodium 2,6-di-tert-butylphenylate, and sodium phenylate.The reduction by electron transfer of the iodonium salts by the latter reaction gives high yields of diaryl ethers.The mechanism fo ether formation has been shown to proceed by two mechanistic pathways.For the diaryliodonium salts that have a p-cyano or p-nitro substituent, the ether is formed by a nucleophilic aromatic substitution; however, when the substituents were not strongly electron withdrawing, the mechanism resulting in ether formation involved electron transfer from the phenylate anion to the iodonium salt to form the phenoxy radical and a 9-I-2 intermediate.The intermediate decomposes to an aryl radical and an aryl iodide.The ether is formed from the efficient coupling of the aryl radical and the phenoxy radical.
- Tanner, Dennis D.,Reed, Darwin W.,Setiloane, B.P.
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p. 3917 - 3923
(2007/10/02)
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- Insecticidal α-trifluoromethyl-3-phenoxybenzyl carboxylates
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New insecticides, organic esters wherein the alcohol moiety is α-trifluoromethyl-3-phenoxybenzyl alcohol and the acid moiety is a pyrethroid carboxylic acid, are described and shown to control a broad spectrum of insects, including acarids.
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- Diphenyl ethers for tobacco sucker control
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Diphenyl ethers having the formula STR1 WHERE Y and Z are halogen, alkyl, trifluoromethyl, alkoxy, hydroxy, nitro, cyano, carboxy, carbalkoxy, carbamoyl, or alkylthio, and m and n are 0, 1, 2, or 3, Are useful in controlling undesirable secondary growth in plants, particularly sucker growth in tobacco.
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