195457-61-5Relevant articles and documents
COMBINATION WITH CHECKPOINT INHIBITORS TO TREAT CANCER
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Paragraph 00388-00391, (2020/10/27)
A combination comprising a compound of Formula (I) and/or Formula (Ia), or a pharmaceutically acceptable salt thereof, and at least one immune checkpoint modulator. Methods for the prevention and treatment of a cancer comprises administering to a subject in need thereof, a therapeutically effective amount of a combination, the combination comprising: a compound of Formula (I) and/or Formula (Ia), or a pharmaceutically acceptable salt thereof, and at least one immune checkpoint modulator.
Design, synthesis and biological evaluation of novel 4-aminoquinazolines as dual target inhibitors of EGFR-PI3Kα
Ding, Huai-Wei,Deng, Cheng-Long,Li, Dan-Dan,Liu, Dan-Dan,Chai, Shao-Meng,Wang, Wei,Zhang, Yan,Chen, Kai,Li, Xin,Wang, Jian,Song, Shao-Jiang,Song, Hong-Rui
, p. 460 - 470 (2018/02/14)
The overexpression of EGFR correlates with rapidly progressive disease, resistance to chemotherapy and poor prognosis. In certain human cancers, PI3K works synergistically with EGFR to promote proliferation, survival, invasion and metastasis. Development
4-arylamino-6(3-sulfaminepyridine)-quinazoline derivative as well as preparation method thereof and application thereof
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Paragraph 0066; 0067; 0068; 0069, (2018/11/22)
The invention discloses a 4-arylamino-6(3-sulfaminepyridine)-quinazoline derivative as well as a preparation method thereof and application thereof. A structural formula of the derivative is as shownin formula I, wherein in the formula I, R1, R2, R3, R4,
6-pyrromonazole substituted quinazoline compound, and derivative, synthetic method and application thereof
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, (2017/08/28)
The invention discloses a compound as shown in the formula (I), (II) or (III), or salt of the compound acceptable in pharmacy, aquo-complex, a solvate, a polymorphic substance, a tautomer or a prodrug; a synthetic method of the formula (I) comprises the f
Design, synthesis, anti-tumor activity, and molecular modeling of quinazoline and pyrido[2,3-d]pyrimidine derivatives targeting epidermal growth factor receptor
Hou, Ju,Wan, Shanhe,Wang, Guangfa,Zhang, Tingting,Li, Zhonghuang,Tian, Yuanxin,Yu, Yonghuan,Wu, Xiaoyun,Zhang, Jiajie
, p. 276 - 289 (2016/05/10)
Three series of novel quinazoline and pyrido[2,3-d]pyrimidine derivatives were designed, synthesized and evaluated for their ability to inhibit EGFR tyrosine kinase and a panel of five human cancer cell lines (MCF-7, A549, BT-474, SK-BR-3, and MDA-MB-231)
SMALL MOLECULE INHIBITORS OF EGFR AND PI3K
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Page/Page column 66; 67, (2016/07/05)
This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a quinazoline structure or a quinoline structure which function as dual inhibitors of EGFR proteins and PI3K proteins, and their use as therapeutics for the treatment of cancer and other diseases.
Discovery, synthesis, and biological evaluation of thiazoloquin(az)olin(on)es as potent CD38 inhibitors
Haffner, Curt D.,Becherer, J. David,Boros, Eric E.,Cadilla, Rodolfo,Carpenter, Tiffany,Cowan, David,Deaton, David N.,Guo, Yu,Harrington, Wallace,Henke, Brad R.,Jeune, Michael R.,Kaldor, Istvan,Milliken, Naphtali,Petrov, Kim G.,Preugschat, Frank,Schulte, Christie,Shearer, Barry G.,Shearer, Todd,Smalley, Terrence L.,Stewart, Eugene L.,Stuart, J. Darren,Ulrich, John C.
, p. 3548 - 3571 (2015/05/05)
A series of thiazoloquin(az)olinones were synthesized and found to have potent inhibitory activity against CD38. Several of these compounds were also shown to have good pharmacokinetic properties and demonstrated the ability to elevate NAD levels in plasm
Synthesis and biological evaluation of substituted 6-alkynyl-4-anilinoquinazoline derivatives as potent EGFR inhibitors
Liu, Lee Tai,Yuan, Ta-Tung,Liu, Hung-Huang,Chen, Shyh-Fong,Wu, Ying-Ta
, p. 6373 - 6377 (2008/03/14)
A series of C-6 or C-3′ alkynyl-substituted 4-anilinoquinazoline derivatives was prepared straightforwardly by a Sonogashira reaction of the corresponding bromo-substituted 4-anilinoquinazolines. Bioactive assay of these compounds for in vitro EGFR kinase inhibition demonstrated that the novel 6-hydroxypropynyl-4-anilinoquinazoline 5e was a very potent EGFR kinase inhibitor with an IC50 of 14 nM.