- Discovery of novel VEGFR-2 inhibitors. Part II: Biphenyl urea incorporated with salicylaldoxime
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A series of novel VEGFR-2 inhibitors containing oxime as hinge binding fragment were described. A strategy of pseudo six-membered ring formed through intramolecular hydrogen bond was employed to mimic the planar quinazoline. The oxime group was firstly introduced to interact with hinge region of VEGFR-2. Most of compounds tested showed moderate to high VEGFR-2 inhibitory activity. In particular, 12l, 12p and 12y exhibited significant enzymatic inhibitory activity as well as potent antiproliferative activity against cancer cells. Molecular docking suggested that the salicylaldoxime formed two hydrogen bonds with hinge region. These biphenylureas could serve as promising lead compounds for developing novel anticancer agents.
- Gao, Hongping,Su, Ping,Shi, Yaling,Shen, Xiuxiu,Zhang, Yanmin,Dong, Jinyun,Zhang, Jie
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- HISTONE ACETYLTRANSFERASE (HAT) INHIBITOR AND USE THEREOF
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The present invention relates to a histone acetyltransferase (HAT) inhibitor. Provided are a compound represented by general formula I, a pharmaceutically acceptable salt, a stereoisomer, an enantiomer, a diastereomer, an atropisomer, a racemate, a polymorph, a solvate or an isotope-labeled compound (including deuterium substitution) thereof, a preparation method therefor, a pharmaceutical composition comprising the same, and use thereof in the treatment of various HAT-related diseases or conditions.
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Paragraph 0765-0766
(2021/02/25)
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- Condensed tricyclic compound and applications thereof in medicines
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The invention relates to a condensed tricyclic compound and applications thereof in medicines, particularly to applications of the condensed tricyclic compound as a drug for treating and/or preventinghepatitis B, specifically to a compound represented by a general formula (I) or a stereoisomer, a tautomer, a nitrogen oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrugthereof, wherein variables are defined in the specification. The invention further relates to applications of the compound represented by the general formula (I) or the stereoisomer, the tautomer, thenitric oxide, the solvate, the metabolite, the pharmaceutically acceptable salt or the prodrug thereof as a drug, particularly applications of the compound as a drug for treating and/or preventing hepatitis B.
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Paragraph 0352-0354
(2020/04/17)
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- FUSED TRICYCLIC COMPOUNDS AND USES THEREOF IN MEDICINE
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The present invention relates to a fused tricyclic compound and use thereof as a medicament, in particular as a medicament for the treatment and/or prevention of hepatitis B. Specifically, the invention relates to a compound having Formula (I) or a stereoisomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, wherein each variate is as defined in specification. The invention also relates to the use of the compound having Formula (I) or a stereoisomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof as a medicament, especially as a medicament for the treatment and/or prevention of hepatitis B.
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Paragraph 00332
(2019/01/05)
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- SULFONAMIDE DERIVATIVE HAVING PGD2 RECEPTOR ANTAGONISTIC ACTIVITY
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A sulfonamide derivative having DP receptor antagonistic activity; and a medicinal composition and a therapeutic agent for allergic diseases which each contains the compound as an active ingredient. The derivative is a compound represented by the general formula (II): (II) (wherein ring A is an aromatic carbocycle, etc.; ring B is a nitrogenous nonaromatic heterocycle, etc.; ring C is an aromatic carbocycle, etc.; R1 is carboxy, etc.; R2's each independently is halogeno, etc.; R3 is optionally substituted alkyloxy, etc.; R4's each independently is halogeno, etc.; R5's each independently is optionally substituted alkyl, etc.; M is sulfonyl, etc.; Y is a single bond, etc.; L1 is a single bond, etc.; L2 is a single bond, etc.; k is 0, 1, 2, 3, or 4; n is 0, 1, or 2; and q is 0, 1, 2, or 3, provided that, for example, a) when ring B is a 6-membered nitrogenous heterocycle containing one or two nitrogen atoms and ring C is a benzene ring, then k is not 0), a pharmaceutically acceptable salt of the compound, or a hydrate of either.
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Page/Page column 137
(2010/11/26)
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