- Anti-hepatitis B application of conjugate
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The invention mainly provides application of a conjugate in preparation of a medicine for treating hepatitis B virus infection. The conjugate is obtained by connecting formyl in an orlistat structureto amino in a phenylaminopyrimidine compound structure,
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Paragraph 0041; 0081-0083
(2020/12/30)
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- Imatinib dinitrogen oxide as well as preparation method and application thereof
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The invention relates to an imatinib nitric oxide as well as a preparation method and medical application thereof, in particular to an imatinib dinitrogen oxide shown as a formula (I) in the description, or pharmaceutically acceptable salt of the imatinib
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Paragraph 0035; 0036; 0037; 0038
(2018/03/26)
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- Design, synthesis and anti-inflammatory activity of pyrimidine scaffold benzamide derivatives as epidermal growth factor receptor tyrosine kinase inhibitors
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Novel serious of pyrimidine scaffold benzamide derivatives (9 a-k) were synthesized and characterized by IR, HRMS, and NMR. Docking study of compounds 9 g, 9 h exhibited H-bonding interacts with Met769 into ATP binding site of EGFR-TK which showed similar binding mode to Lapitinib (PDB code: 1M17). Results indicated the ability to potent and selective inhibitors of the Epidermal Growth Factor Receptor tyrosine kinase (EGFR-TK). The molecular electrostatic potential (MEP), frontier molecular orbitals (FMOs) and HOMO-LUMO energy gap of the title compounds were investigated by using the B3LYP/6-31G method. The synthesized compounds were screened for in vitro anti-inflammatory activity.
- Thirumurugan,Lakshmanan, Sivalingam,Govindaraj, Dharman,Daniel Prabu, D. Sam,Ramalakshmi,Arul Antony
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p. 541 - 550
(2018/06/20)
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- INTERMEDIATES FOR A NOVEL PROCESS OF PREPARING IMATINIB AND RELATED TYROSINE KINASE INHIBITORS
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4-Oxo-2-phenylaminopyrimidine derivatives as intermediates for synth of tyrosine kinase inhibitors, in particular imatinib and nilotinib.
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- Synthesis and docking study of 2-phenylaminopyrimidine Abl tyrosine kinase inhibitors
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Six analogs of imatinib, an Abl kinase inhibitor clinically used as a first-line therapeutic agent for chronic myeloid leukaemia (CML), have been synthesized and characterized. And their potency as Abl kinase inhibitors have been screened by a robust virt
- Lü, Shuang,Luo, Qun,Hao, Xiang,Li, Xianchan,Ji, Liyun,Zheng, Wei,Wang, Fuyi
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experimental part
p. 6964 - 6968
(2012/01/05)
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- Pyridylpyrimidine derivatives as effective compounds against prion diseases
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The present invention relates to pyridylpyrimidine derivatives of the general formula (I): wherein R represents hydrogen or methyl and Z represents nitrogen containing functional groups, the use of the pyridylpyrimidine derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of prion infections and prion diseases, as well as compositions containing at least one pyridylpyrimidine derivative and/or pharmaceutically acceptable salt thereof. Furthermore, the present invention is directed to methods for preventing and/or treating prion infections and prion diseases using said pyridylpyrimidine derivatives. Human cellular protein kinases, phosphatases and cellular signal transduction molecules are disclosed as targets for detecting, preventing and/or treating prion infections and diseases, especially BSE, vCJD, or CJD which can be inhibited by the inventive pyridylpyrimidine derivatives.
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- Potent and selective inhibitors of the Abl-kinase: Phenylaminopyrimidine (PAP) derivatives
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Due to its relatively clear etiology, chronic myelogenous leukemia (CML) represents an ideal disease target for a therapy using a selective inhibitor of the Bcr-Abl tyrosine protein kinase. Extensive optimization of the class of phenylamino-pyrimidines yielded highly potent and selective Bcr-Abl kinase inhibitors. Compound 1 shows high potency (IC50 = 38 nM) and selectivity for the Abl tyrosine protein kinase at the in vitro level.
- Zimmermann, Juerg,Buchdunger, Elisabeth,Mett, Helmut,Meyer, Thomas,Lydon, Nicholas B.
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p. 187 - 192
(2007/10/03)
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- Phenylamino-pyrimidine (PAP) - Derivatives: A new class of potent and highly selective PDGF-Receptor autophosphorylation inhibitors
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Phenylamino-pyrimidines represent a novel class of inhibitors of the PDGF-receptor autophosphorylation with a high degree of selectivity versus other tyrosine and serine/threonine kinases. Optimum activity of ca 10 nM (IC50) was observed when the phenylamino-group which is attached to the pyrimidine carries a benzamide-moiety with a lipophilic substituent in 4-position. Copyright
- Zimmermann, Juerg,Buchdunger, Elisabeth,Mett, Helmut,Meyer, Thomas,Lydon, Nicholas B.,Traxler, Peter
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p. 1221 - 1226
(2007/10/03)
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