- BIARYL COMPOUND, PREPARATION METHOD AND USE THEREFOR
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The present invention belongs to the technical field of chemical pharmaceuticals, and relates to a compound represented by general formula (I) or formula (II) and a preparation method thereof. The compounds are biaryl derivatives with RORγt activation activity. The biaryl derivatives disclosed in this invention can effectively activate the RORγt protein receptor, and thereby promote the differentiation of Th17 cells and increasing the production of IL-17, which can be used as an immune modulator for the treatment of various cancers or viral infection-related diseases.
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Paragraph 0122-0123
(2020/01/02)
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- NOVEL ANTIBIOTICS
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Novel aryl compounds or pharmaceutically acceptable salts thereof, and uses of the same for the treatment of Gram-negative infections.
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Page/Page column 30
(2018/02/03)
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- Synthesis of α-aryl esters and nitriles: Deaminative coupling of α-aminoesters and α-aminoacetonitriles with arylboronic acids
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Transition-metal-free synthesis of α-aryl esters and nitriles using arylboronic acids with α-aminoesters and α-aminoacetonitriles, respectively, as the starting materials has been developed. The reaction represents a rare case of converting C(sp3)-N bonds into C(sp3)-C(sp2) bonds. The reaction conditions are mild, demonstrate good functional-group tolerance, and can be scaled up. Touch base: A transition-metal-free protocol for the synthesis of α-aryl esters and nitriles by deaminative coupling is presented. Strong bases and transition-metal catalysts are not needed. The new synthetic method uses readily available starting materials and demonstrates wide substrate scope.
- Wu, Guojiao,Deng, Yifan,Wu, Chaoqiang,Zhang, Yan,Wang, Jianbo
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supporting information
p. 10510 - 10514
(2016/02/18)
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- DERIVATIVES OF 1-PHENYL-1,5-DIHYDRO-BENZO[B] [1.4]DIAZEPINE-2.4-DIONE AS INHIBITORS OF HIV REPLICATION
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Compounds of formula (I) wherein m, R1, R2, R3, X and Y are defined herein, are useful as inhibitors of HIV replication.
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Page/Page column 36
(2011/09/19)
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- Reactions of CF3-substituted boranes with α-diazocarbonyl compounds
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Boranes substituted with a CF3-group can be generated from methyl boronic esters RB(OMe)2 and Me3SiCF3/KF followed by treatment with Me3SiCl. These boranes are stable only in coordinating solvents, and due to the increased Lewis acidity of boron, react rapidly with α-diazocarbonyl compounds to give the products of transfer of the organic group from boron. Alkyl, aryl, vinyl, and alkynyl boronic esters can be used in this reaction.
- Elkin, Pavel K.,Levin, Vitalij V.,Dilman, Alexander D.,Struchkova, Marina I.,Belyakov, Pavel A.,Arkhipov, Dmitry E.,Korlyukov, Alexander A.,Tartakovsky, Vladimir A.
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p. 5259 - 5263
(2011/10/31)
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- Specific targeting highly conserved residues in the HIV-1 reverse transcriptase primer grip region. Design, synthesis, and biological evaluation of novel, potent, and broad spectrum NNRTIs with antiviral activity
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Pyrrolobenzoxazepinones (PBOs) represent a new class of human immunodeficiency virus type 1 (HIV-1) nonnucleoside reverse transcriptase (RT) inhibitors (NNRTIs) whose prototype is 5. Molecular modeling studies based on the X-ray structures of HIV-1 RT pro
- Fattorusso, Caterina,Gemma, Sandra,Butini, Stefania,Huleatt, Paul,Catalanotti, Bruno,Persico, Marco,De Angelis, Meri,Fiorini, Isabella,Nacci, Vito,Ramunno, Anna,Rodriquez, Manuela,Greco, Giovanni,Novellino, Ettore,Bergamini, Alberto,Marini, Stefano,Coletta, Massimo,Maga, Giovanni,Spadari, Silvio,Campiani, Giuseppe
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p. 7153 - 7165
(2007/10/03)
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- Biaryl isoxazolinone antibacterial agents
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In an era of increasing resistance to classical antibacterial agents, the synthetic oxazolidinone series of antibiotics has attracted much interest. Zyvox was the first oxazolidinone to be approved for clinical use against infections caused by multi-drug
- Quesnelle, Claude A.,Gill, Patrice,Roy, Stephan,Dodier, Marco,Marinier, Anne,Martel, Alain,Snyder, Lawrence B.,D'Andrea, Stanley V.,Bronson, Joanne J.,Frosco, MaryBeth,Beaulieu, Danielle,Warr, Glen A.,DenBleyker, Ken L.,Stickle, Terry M.,Yang, Hyekyung,Chaniewski, Susan E.,Ferraro, Cheryl A.,Taylor, Dennis,Russell, John W.,Santone, Kenneth S.,Clarke, Junius,Drain, Rebecca L.,Knipe, Jay O.,Mosure, Kathleen,Barrett, John F.
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p. 2728 - 2733
(2007/10/03)
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- COMPOUNDS WHICH ARE MODULATORS OF THE PPAR-TYPE RECEPTORS AND THEIR USE IN COSMETIC OR PHARMACEUTICAL COMPOSITIONS
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The invention relates to novel compounds which correspond to the general formula (I), their method of preparation, and their use in pharmaceutical compositions intended for use in human or veterinary medicine (in dermatology and in the field of cardiovasc
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Page/Page column 31
(2008/06/13)
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- COPPER-CATALYZED FORMATION OF CARBON-HETEROATOM AND CARBON-CARBON BONDS
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One aspect of the present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-sulfur bond between the sulfur atom of a thiol moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper(II)-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-carbon bond between the carbon atom of cyanide ion and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In another embodiment, the present invention relates to a copper-catalyzed method of transforming and aryl, heteroaryl, or vinyl iodide. Yet another embodiment of the present invention relates to a tandem method, which may be practiced in a single reaction vessel, wherein the first step of the method involves the copper-catalyzed formation of an aryl, heteroaryl, or vinyl iodide from the corresponding aryl, heteroaryl, or vinyl chloride or bromide; and the second step of the method involves the copper-catalyzed formation of an aryl, heteroaryl, or vinyl nitrile, amide or sulfide from the aryl, heteroaryl, or vinyl iodide formed in the first step.
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- N-SUBSTITUTED PIPERIDINE DERIVATIVES AS SEROTONIN RECPTOR AGENTS
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Disclosed herein are compounds of Formula I, or a pharmaceutically acceptable salt, amide, ester, or prodrug thereof. Also disclosed are methods of inhibiting an activity of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Disclosed are also methods of inhibiting an activation of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Furthermore, methods of treating psychotic disease using a compound of Formula I are disclosed.
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- Copper-catalyzed halogen exchange in aryl halides: An aromatic finkelstein reaction
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A mild and general method for the conversion of aryl, heteroaryl, and vinyl bromides into the corresponding iodides was developed utilizing a catalyst system comprising 5 mol % of Cul and 10 mol % of a 1,2- or 1,3-diamine ligand. A variety of polar functional groups are tolerated, and even N-H containing substrates such as sulfonamides, amides, and indoles are compatible with the reaction conditions. Both the reaction rate and the equilibrium conversion of the aryl bromide depend on the choice of the halide salt and the solvent. The best results were obtained using Nal as the halide salt and dioxane, n-butanol, or n-pentanol as the solvents. Copyright
- Klapars, Artis,Buchwald, Stephen L.
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p. 14844 - 14845
(2007/10/03)
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