- Phosphoramidate prodrug of nucleoside analogues, a pharmaceutical composition and applications of the phosphoramidate prodrug
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The invention relates to phosphoramidate prodrug of nucleoside analogues, or stereoisomers of the phosphoramidate prodrug, or a mixture of the stereoisomers of the phosphoramidate prodrug, or pharmaceutically acceptable salts or solvates of the phosphoramidate prodrug, and applications in the preparation of medicine for preventing or treating hepatitis B virus (HBV) and/or human immunodeficiency virus (HIV) infection alone or in combination with other medicine. The anti-HBV activity of the compound of the invention is equivalent to that of tenofovir alafenamide fumarate (TAF), and the compoundof the invention has the anti-liver fibrosis effect, can help improve the therapeutic effect of patients, and has good safety important clinical significance.
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Paragraph 0156-0158
(2019/04/10)
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- Discovery of (R)-1-(3-(4-Amino-3-(3-chloro-4-(pyridin-2-ylmethoxy)phenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one (CHMFL-EGFR-202) as a Novel Irreversible EGFR Mutant Kinase Inhibitor with a Distinct Binding Mode
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On the basis of Ibrutinib’s core pharmacophore, which was moderately active to EGFR T790M mutant, we discovered novel epidermal growth factor receptor (EGFR) inhibitor compound 19 (CHMFL-EGFR-202), which potently inhibited EGFR primary mutants (L858R, del
- Wang, Aoli,Li, Xixiang,Wu, Hong,Zou, Fengming,Yan, Xiao-E,Chen, Cheng,Hu, Chen,Yu, Kailin,Wang, Wenchao,Zhao, Peng,Wu, Jiaxin,Qi, Ziping,Wang, Wei,Wang, Beilei,Wang, Li,Ren, Tao,Zhang, Shanchun,Yun, Cai-Hong,Liu, Jing,Liu, Qingsong
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p. 2944 - 2962
(2017/04/21)
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- NOVEL OLEFIN DERIVATIVE
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The object of the present invention is to provide novel compounds having ACC2 inhibiting activity. In addition, the object of the present invention is to provide a pharmaceutical composition comprising the compound. A compound of formula (I′): wherein R1 is substituted or unsubstituted aryl etc., R2 is each independently hydrogen, substituted or unsubstituted alkyl etc., R3 is each independently hydrogen, substituted or unsubstituted alkyl etc., n is an integer from 0 to 3, R12 is hydrogen, substituted or unsubstituted alkyl etc., Ring A is aromatic carbocycle or aromatic heterocycle, R9 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl etc., m is an integer from 0 to 4, R4 and R5 is each independently hydrogen, substituted or unsubstituted alkyl etc., R6 is substituted or unsubstituted alkyl, substituted or unsubstituted alkenyl etc., R13 is hydrogen, substituted or unsubstituted alkyl etc., X5 is bond etc., R7 is hydrogen or substituted or unsubstituted alkyl, R8 is substituted or unsubstituted alkylcarbonyl, substituted or unsubstituted alkenylcarbonyl etc.
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Paragraph 0648-0650
(2015/09/28)
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- Discovery of 5-HT6 receptor ligands based on virtual HTS
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Based on a pharmacophore alignment on a 5-HT6 ligand applying 4SCan technology, a new lead series was identified and further structurally investigated. Kis down to 8 nM were achieved.
- Tasler, Stefan,Kraus, Jürgen,Wuzik, Andreas,Müller, Oliver,Aschenbrenner, Andrea,Cubero, Elena,Pascual, Rosalia,Quintana-Ruiz, Jordi-Ramon,Dordal, Alberto,Mercè, Ramon,Codony, Xavier
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p. 6224 - 6229
(2008/03/18)
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- PESTICIDAL SUBSTITUTED PHENYLETHERS
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The invention relates to the use of phenylether derivatives of formula (I), to compositions thereof for the control of pests, including arthropods and helminths.
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Page/Page column 42; 46
(2008/06/13)
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- KINASE MODULATORS AND METHODS OF USE
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The present invention relates to compounds of the Formula I and II wherein R, R21, R25-R33, m, n, X21-X23, and Q1 are defined herein. The compounds modulate protein kinase enzymatic activity to modulate cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinases, particularly p70S6 and/or Akt kinases. Methods of using and preparing the compounds, and pharmaceutical compositions thereof, to treat kinase-dependent diseases and conditions are also an aspect of the invention.
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Page/Page column 102
(2010/02/15)
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- A new stereoselective synthetic strategy for β-hydroxy-α-amino acids of vancomycin
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The synthesis of syn and anti β-hydroxy-α-amino acids representing rings C and E of vancomycin has been achieved starting from (R)- and (S)Garner's aldehydes by a stereocontrolled Grignard arylation reaction.
- Gurjar, Mukund K.,Pal, Shashwati,Mohapatra, Debendra K.
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p. 109 - 116
(2007/10/03)
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- 6-(3-SUBSTITUTED AMINO-2-HYDROXYPROPOXYARYL)-4,5-DIHYDRO-3(2H)-PYRIDAZINONES
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The compounds are 6-(3-substituted amino-2-hydroxypropoxyaryl)-4,5-dihydro-3(2H)-pyridazinones which are β-adrenergic blocking agents.
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