65766-32-7Relevant articles and documents
Discovery of 4,6-Disubstituted Pyrimidine Derivatives as Novel Dual VEGFR2/FGFR1 Inhibitors
Zhang, Jin-Yang,Xue, Wen-Jun,Wang, Min,Li, Wen,Dong, Ru,Li, Ming-Tao,Sun, Li-Ping
, (2021/04/26)
Abnormalities in the FGFRs signaling pathway and VEGFR2 amplification often occur in a variety of tumors, and they synergistically promote tumor angiogenesis. Studies have shown that the up-regulation of FGF-2 is closely related to the resistance of VEGFR2 inhibitors. Activation of the FGFRs signal is a signal of compensatory angiogenesis after VEGFR2 resistance. Dual VEGFR2/FGFR1 inhibitors contribute to overcoming the resistance of VEGFR2 inhibitors and inhibit tumor growth significantly. Based on this, we designed and synthesized a series of 4,6-disubstituted pyrimidine derivatives as dual VEGFR2/FGFR1 inhibitors by the molecular hybridization strategy. 3-(2,6-Dichloro-3,5-dimethoxyphenyl)-1-{6-[(4-methoxyphenyl)amino]pyrimidin-4-yl}-1-methylurea (8b) had the best inhibitory activities against VEGFR2 and FGFR1 at 10 μM (82.2 % and 101.0 %, respectively), it showed moderate antiproliferative activities against A549 and KG-1 cell lines as well. Besides, molecular docking was also carried out to study the binding mode of 3-(2,6-dichloro-3,5-dimethoxyphenyl)-1-{6-[(4-methoxyphenyl)-amino]-pyrimidin-4-yl}-1-methylurea (8b) with VEGFR2 and FGFR1. These studies reveal that this series of compounds deserve further optimization.
A model used for fibroblast growth factor receptor inhibitors and use thereof (by machine translation)
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Paragraph 0110; 0113-0116, (2018/07/30)
The invention belongs to the field of medical technology, in particular of formula (I) indicated by the fibroblast growth factor receptor 4 (FGFR4) irreversible inhibitors, their pharmaceutically acceptable salt, compound solvent, polymorphs and tautomeri
Substituted p-chlorophenyl acetylpiperazine-containing compound as well as preparation method and application thereof
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Paragraph 0116; 0139; 0200-0203, (2019/01/06)
The application provides a substituted p-chlorophenyl acetylpiperazine-containing compound as well as a preparation method and application of the substituted p-chlorophenyl acetylpiperazine-containingcompound. The compound has the structure shown in the formula (I), and has better Akt1 inhibitory activity or growth inhibitory activity to MCL cell lines.
TAM KINASE INHIBITORS
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Paragraph 0173; 0174, (2018/11/10)
Described herein are compounds, methods of making such compounds, compositions (e.g., pharmaceutical compositions/medicaments) that include such compounds, and methods of using such compounds to treat diseases, such as cancer.
CHLOROBENZENE SUBSTITUTED AZAARYL COMPOUNDS
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Paragraph 0044; 0059, (2017/02/09)
The invention provides a series of chlorobenzene substituted azaaryl compounds having activity in inhibiting cancer cell growth and low toxicity to normal cells. Particularly, the compounds of the invention have stronger inhibition effect on bladder cance
PHENYL TETRAHYDROISOQUINOLINE COMPOUND SUBSTITUTED WITH HETEROARYL
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Paragraph 0320; 0321, (2017/06/29)
The present invention provides a compound represented by the following formula [1] or a pharmaceutically acceptable salt thereof which has an excellent NHE3 inhibitory effect: ????????[Formula 15]?????A-Y [1] wherein A represents a structure represented b
NEW TRPA1 ANTAGONISTS
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Page/Page column 40; 41, (2017/05/02)
The present invention relates to bicyclic heterocyclic derivatives of Forrmula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by TRPA1 channel inhibition or antagonism.
NEW TRPA1 ANTAGONISTS
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Page/Page column 62; 63, (2017/08/01)
The present invention relates to compounds of Formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by TRPA1 channel inhibition or antagonism.
AMINE-SUBSTITUTED ARYL OR HETEROARYL COMPOUNDS AS EHMT1 AND EHMT2 INHIBITORS
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Paragraph 0950-0953, (2017/11/10)
The present disclosure relates to amine-substituted aryl or heteroaryl compounds. The present disclosure also relates to pharmaceutical compositions containing these compounds and methods of treating a disorder (e.g., sickle cell anemia) via inhibition of a methyltransferase enzyme selected from EHMT1 and EHMT2, by administering an amine-substituted aryl or heteroaryl compound disclosed herein or a pharmaceutical composition thereof to subjects in need thereof. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.
USES OF SALT-INDUCIBLE KINASE (SIK) INHIBITORS
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Paragraph 00403-00404, (2016/04/20)
The present disclosure provides methods of treating and/or preventing inflammatory bowel disease (IBD) and graft-versus-host disease (GVHD) using salt-inducible kinase (SIK) inhibitors, such as macrocyclic SIK inhibitors of Formula (I), imidazolyl SIK inh
