796967-48-1Relevant articles and documents
Diaryl urea compounds with anti-tumor activity as well as preparation method and application of diaryl urea compounds
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Paragraph 0032; 0033, (2017/08/29)
The invention provides diaryl urea compounds with anti-tumor activity as well as a preparation method and an application of the diaryl urea compounds. A structural formula of the compounds is shown in the specification, wherein R1 represents hydrogen, and R2 represents isopropyl or halogen groups. The compounds have good inhibition activity for VEGFR-2 (vascular endothelial growth factor-2) kinase, and can block VEGFR-2 kinase induced signaling pathways and inhibit tumor cell proliferation and migration by inhibiting activity of VEGFR-2 kinase, so that the compounds can be applied to preparation of anti-tumor drugs. Besides, the preparation method of the compounds has the advantages that raw materials are easily available, reaction conditions are mild, a reaction process is simple to operate and used reagents are cheap.
Discovery of novel anti-angiogenesis agents. Part 8: Diaryl thiourea bearing 1H-indazole-3-amine as multi-target RTKs inhibitors
Sun, Ying,Shan, Yuanyuan,Li, Chuansheng,Si, Ru,Pan, Xiaoyan,Wang, Binghe,Zhang, Jie
, p. 373 - 385 (2017/10/16)
VEGFR-2, TIE-2, and EphB4 are essential for both angiogenesis and tumorigenesis. Herein, we designed and prepared three classes of multi-target inhibitors based on the extensive sequence homology along the kinase domain of angiogenic RTKs. Biological evaluation indicated that these multi-target inhibitors exhibited considerable potential as novel anti-angiogeneic and anticancer agents. Among them, a diaryl thiourea bearing 1H-indazole-3-amine (16a) displayed the most potent RTK inhibition and excellent selectivity. It also showed inhibition on viability of human umbilical vein endothelial cells and anti-proliferation against a broad spectrum of cancer cells. Therefore, 1H-indazole-3-amine could serve as a promising hinge binding group for multi-target inhibitors of VEGFR-2, Tie-2, and EphB4.
Discovery of novel anti-angiogenesis agents. Part 7: Multitarget inhibitors of VEGFR-2, TIE-2 and EphB4
Li, Chuansheng,Shan, Yuanyuan,Sun, Ying,Si, Ru,Liang, Liyuan,Pan, Xiaoyan,Wang, Binghe,Zhang, Jie
, p. 506 - 518 (2017/11/14)
Herein, we embarked on a structural optimization campaign aiming at the discovery of second generation anti-angiogenesis agents with our previously reported BPS-7 as lead compound. A library of 27 compounds has been afforded based on the highly conserved ATP-binding pocket of VEGFR-2, Tie-2, and EphB4. Several title compounds exhibited simultaneous inhibitory effects against three angiogenic RTKs. These compounds with a ‘triplet’ inhibition profile have been identified as novel anti-angiogenic and anticancer agents. The representative VDAU11 displayed prominent anti-angiogenic and anticancer potency and could be considered as a candidate for further optimization. These results indicate that N-(pyridin-2-yl)acrylamide could serve as a novel hinge-binding group of triple inhibitors.
Diarylurea compound with antitumor activity, and preparation method and application thereof
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, (2017/07/19)
The invention provides a diarylurea compound with antitumor activity, and a preparation method and application thereof. The compound has a structural formula as described in the specification. In the structural formula, R1 and R2 are selected from the group consisting of hydrogen, alkane groups or halogen groups. The compound provided by the invention has good inhibitory activity to VEGFR-2 kinase, so a signal channel induced by the VEGFR-2 kinase can be blocked through inhibition of the activity of the VEGFR-2 kinase, and proliferation and migration of tumor cells are inhibited; thus, the compound can be applied in preparation of antitumor drugs. Meanwhile, the preparation method for the compound has the following advantages: raw materials are easily available; reaction conditions are mild; the process of reaction is simple to operate; and used reagents are cheap.
COMBINED MODULATION OF IRE1
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Paragraph 0288, (2016/01/25)
Described herein, inter alia, are combined compositions of an Irel kinase modulating compound and an Irel ribonuc lease modulating compound and methods of using same.
INHIBITORS OF DIACYLGLYCEROL ACYL TRANSFERASE
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Example 327, (2011/07/30)
The present invention relates to heterocyclic compounds in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.
INHIBITORS OF DIACYLGLYCEROL O-ACYLTRANSFERASE TYPE 1 ENZYME
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Page/Page column 56, (2008/12/08)
The present invention relates to compounds of formula (I): wherein Q, G1, G2, and G3, are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.
Substituted sulphoximines as Tie2 inhibitors and salts thereof, pharmaceutical compositions comprising the same, methods of preparing the same and uses of the same
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Page/Page column 37, (2008/06/13)
The invention relates to substituted sulphoximines according to the general formula (I): in which A, E, G, X, R1, R2, R3, R4, R5, R6, R7, R8, m, p, q, are given in the
3-Amino-benzo[d]isoxazoles as novel multitargeted inhibitors of receptor tyrosine kinases
Ji, Zhiqin,Ahmed, Asma A.,Albert, Daniel H.,Bouska, Jennifer J.,Bousquet, Peter F.,Cunha, George A.,Diaz, Gilbert,Glaser, Keith B.,Guo, Jun,Harris, Christopher M.,Li, Junling,Marcotte, Patrick A.,Moskey, Maria D.,Oie, Tetsuro,Pease, Lori,Soni, Nirupama B.,Stewart, Kent D.,Davidsen, Steven K.,Michaelides, Michael R.
, p. 1231 - 1241 (2008/12/20)
A series of benzoisoxazoles and benzoisothiazoles have been synthesized and evaluated as inhibitors of receptor tyrosine kinases (RTKs). Structure-activity relationship studies led to the identification of 3-amino benzo[d]isoxazoles, incorporating a N,N′-
SUBSTITUTED 4-AMINO-PYRROLOTRIAZINE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS
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Page/Page column 199; 210, (2010/11/27)
This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
