1036388-65-4Relevant articles and documents
Selective sodium channel regulator as well as preparation and application thereof
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Paragraph 0154; 0155; 0158-0159, (2021/02/10)
The invention provides a compound serving as a selective sodium channel regulator and a synthesis and use method, and particularly provides a compound shown as a formula (I), a preparation method of the compound and application of the compound serving as the selective sodium channel regulator. The compounds exhibit excellent activity as a regulator of sodium channels.
Cyclic-fused ASK1 inhibitor and application thereof
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Paragraph 0262; 0266-0268; 0405; 0409-0411, (2019/10/15)
The invention relates to a cyclic-fused ASK1 inhibitor and application thereof, and particularly to a compound shown in formula (I), a pharmacologically acceptable salt and ester thereof, and a stereisomer thereof. The invention further relates to a preparation method of the compound, a pharmaceutic preparation and a pharmaceutical composition containing the compound. The compound of the inventionis capable of effectively inhibiting phosphorylation of amino acid of ASK1, and inhibiting the activation of the ASK1, thereby can be used for treating and/or preventing ASK1-mediated diseases and related diseases.
1 -OXO-1,2-DIHYDROISOQUINOLIN-7-YL-(5-SUBSTITUTED-THIOPHEN-2-YL)-SULFONAMIDE COMPOUNDS, FORMULATIONS CONTAINING THOSE COMPOUNDS, AND THEIR USE AS AICARFT INHIBITORS IN THE TREATMENT OF CANCERS
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, (2016/06/28)
1-Oxo-1,2-dihydroisoquinolin-7-yl-(5-substituted-thiophen-2-yl)-sulfonamide compounds, formulations containing those compounds, and their use as AICARFT inhibitors.
Discovery of Phenylglycine Lactams as Potent Neutral Factor VIIa Inhibitors
Wurtz, Nicholas R.,Parkhurst, Brandon L.,Jiang, Wen,DeLucca, Indawati,Zhang, Xiaojun,Ladziata, Vladimir,Cheney, Daniel L.,Bozarth, Jeffrey R.,Rendina, Alan R.,Wei, Anzhi,Luettgen, Joseph M.,Wu, Yiming,Wong, Pancras C.,Seiffert, Dietmar A.,Wexler, Ruth R.,Priestley, E. Scott
, p. 1077 - 1081 (2016/12/18)
Inhibitors of Factor VIIa (FVIIa), a serine protease in the clotting cascade, have shown strong antithrombotic efficacy in preclinical thrombosis models with minimal bleeding liabilities. Discovery of potent, orally active FVIIa inhibitors has been largely unsuccessful because known chemotypes have required a highly basic group in the S1 binding pocket for high affinity. A recently reported fragment screening effort resulted in the discovery of a neutral heterocycle, 7-chloro-3,4-dihydroisoquinolin-1(2H)-one, that binds in the S1 pocket of FVIIa and can be incorporated into a phenylglycine FVIIa inhibitor. Optimization of this P1 binding group led to the first series of neutral, permeable FVIIa inhibitors with low nanomolar potency.
Design, synthesis and biological evaluation of isoquinoline-based derivatives as novel histone deacetylase inhibitors
Yang, Wei,Li, Lixuan,Wang, Yulan,Wu, Xiaowei,Li, Tingting,Yang, Nan,Su, Mingbo,Sheng, Li,Zheng, Mingyue,Zang, Yi,Li, Jia,Liu, Hong
, p. 5881 - 5890 (2015/11/11)
The design, synthesis and biological evaluation of a series of isoquinoline-based hydroxamic acid compounds as novel HDACs inhibitors were reported herein. A detailed SAR study showed most of the compounds displayed good to excellent inhibitory activities against HDAC1, 3, 6. The IC50 values of compound 10c against HDAC1, 3, 6 were 4.17 ± 0.11 nM, 4.00 ± 0.10 nM, 3.77 ± 0.07 nM, respectively. Most of the compounds showed great anti-proliferative activities against RPMI 8226, HCT 116 and Hep G2 cells. The IC50 values of compounds 10a-h against RPMI 8226 cancer cell proliferation were all below 1 μM. HCT 116 cell was sensitive to the compounds 10a, 10f-g and 18a with the IC50 values 0.3 μM. The active compounds 10a-d did not show inhibitory activity against hERG channel. All these evidence indicated these compounds had great potential as HDACs inhibitors for the further development.
SUBSTITUTED BICYCLIC COMPOUNDS AS mPGES-1 INHIBITORS
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, (2014/10/29)
The present disclosure is directed to compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases.
BICYCLIC LACTAM FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS
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Page/Page column 93, (2008/12/07)
The present invention provides novel bicyclic lactams derivatives, and analogues thereof, of Formula (I): or a stereoisomer, tautomer, pharmaceutically acceptable salt, solvate, or prodrug thereof, wherein the variables A, B, C, W, Y, Z1, Z2, Z3, Z4, R8, and R9 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.
MACROCYCLIC FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS
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Page/Page column 88, (2008/12/07)
The present invention relates generally to novel macrocycles of Formula (I) or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, or prodrugs thereof, wherein the variables A, B, C, D, L, M, W, Z1, Z2, Z3, Z4, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein. These compounds are selective inhibitors of factor VIIa which can be used as medicaments.