70978-61-9Relevant academic research and scientific papers
Orally bioavailable Syk inhibitors with activity in a rat PK/PD model
Thoma, Gebhard,Veenstra, Siem,Strang, Ross,Blanz, Joachim,Vangrevelinghe, Eric,Berghausen, J?rg,Lee, Christian C.,Zerwes, Hans-Günter
, p. 4642 - 4647 (2015)
Design and optimization of benzo- and pyrido-thiazoles/isothiazoles are reported leading to the discovery of the potent, orally bioavailable Syk inhibitor 5, which was found to be active in a rat PK/PD model. Compound 5 showed acceptable overall kinase se
TEAD INHIBITORS AND USES THEREOF
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Paragraph 00465; 00662, (2020/12/11)
The present invention provides compounds, compositions thereof, and methods of using the same.
SUBSTITUTED BICYCLE HETEROCYCLIC DERIVATIVES USEFUL AS ROMK CHANNEL INHIBITORS
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Page/Page column 118, (2018/06/06)
Disclosed are compounds of Formula (I) or a salt thereof, wherein R1 is (II) or (III); each W is independently NR1b or O; Z is a bond or CHR1d; and R1, R2, Rd, R3, L1, L2, R1a, R1b, R1c, and n are define herein. Also disclosed are methods of using such compounds as inhibitors of ROMK, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating cardiovascular diseases.
SUBSTITUTED NITROGEN CONTAINING COMPOUNDS
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Page/Page column 96, (2019/01/05)
Disclosed are compounds of Formula (I): or a salt thereof, Formula (II) wherein R1 is: or; each W is independently NR1b or O; Z is a bond or CHR1d; and R1, R2, Rd, R3a, R3b, L1, B, V, Y, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of ROMK, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating cardiovascular diseases.
Synthesis and evaluation of selenium-containing indole chalcone and diarylketone derivatives as tubulin polymerization inhibition agents
Zhang, Shun,An, Baijiao,Li, Jiayan,Hu, Jinhui,Huang, Ling,Li, Xingshu,Chan, Albert S. C.
, p. 7404 - 7410 (2017/09/25)
Sixteen new selenium-containing indole chalcone and diarylketone derivatives were synthesized and evaluated as tubulin polymerization inhibitors. Among them, compound 25b exhibited the most potent antiproliferative activities against six human cancer cell lines with IC50 values of 0.004-0.022 μM. A microtubule dynamics assay and an immunofluorescence assay confirmed that 25b could effectively inhibit tubulin polymerization (IC50 = 2.1 ± 0.27 μM). Further cellular mechanism studies revealed that 25b induced G2/M phase arrest, which was further evidenced by the decrease in the mitochondrial membrane potential (MMP).
Design, Synthesis, and Biological Evaluation of Novel Selenium-Containing Isocombretastatins and Phenstatins as Antitumor Agents
Pang, Yanqing,An, Baijiao,Lou, Lanlan,Zhang, Junsheng,Yan, Jun,Huang, Ling,Li, Xingshu,Yin, Sheng
, p. 7300 - 7314 (2017/09/22)
Two series of structurally related organoselenium compounds designed by fusing the anticancer agent methyl(phenyl)selane into the tubulin polymerization inhibitors isocombretastatins or phenstatins were synthesized and evaluated for antiproliferative acti
Selenium-containing benzophenone, derivatives and preparation method thereof and application in preparation of antitumor drugs
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, (2017/11/29)
The invention discloses selenium-containing benzophenone, derivatives and a preparation method thereof and application in preparation of antitumor drugs. According to the selenium-containing benzophenone and derivatives thereof, an antitumor drug molecule
Benzene fused heterocyclic derivatives having thromboxane A2 receptor antagonistic activity and prostaglandin I2 Agonistic activity and application thereof
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, (2008/06/13)
Benzene fused derivatives represented by the following formula: having strong TXA2receptor antagonistic action and PGI2receptor agonistic action, and effective for treating or preventing diseases concerning TXA2.
2'Hydroxy tetrazole-5-carboxanilides and anti-allergic use thereof
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, (2008/06/13)
New tetrazole derivatives of the general formula: STR1 [wherein R1 represents a halogen atom, a straight- or branched-chain alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl or alkylsulphamoyl group, each such group containing from 1 to 6 carbon atoms, a dialkylsulphamoyl, dialkylamino, or dialkylcarbamoyl group (wherein the two alkyl groups may be the same or different and each contains from 1 to 4 carbon atoms), a straight- or branched-chain alkanoyl, alkoxycarbonyl, alkoxycarbonylamino, alkylcarbamoyl or alkanoylamino group containing from 2 to 6 carbon atoms, a cycloalkylcarbonyl group containing from 3 to 8 carbon atoms in the cycloalkyl moiety, or a hydroxy, formyl, nitro, trifluoromethyl, trifluoroacetyl, aryl, benzyloxycarbonylamino, amino, sulphamoyl, cyano, tetrazol-5-yl, carboxy, carbamoyl, benzyloxy, aralkanoyl or aroyl group, or a group of the formula: (wherein R2 represents a hydrogen atom or a straight- or branched-chain alkyl group containing from 1 to 5 carbon atoms, an aryl, aralkyl or trifluoromethyl group, or a cycloalkyl group containing from 3 to 8 carbon atoms, and R3 represents a hydrogen atom, or a straight- or branched-chain alkyl group containing from 1 to 6 carbon atoms optionally substituted by a phenyl group, or represents an aryl group optionally substituted by one or more substituents selected from halogen atoms and straight- or branched-chain alkyl and alkoxy groups containing from 1 to 6 carbon atoms and hydroxy, trifluoromethyl and nitro groups), and m represents zero or an integer 1, 2 or 3, the substituents R1 being the same or different when m represents 2 or 3] possess pharmacological properties, in particular properties of value in the treatment of allergic conditions.
