40258-99-9Relevant academic research and scientific papers
TREATMENT OF CANCER WITH ANTI-OX40 ANTIBODIES AND MULTI-KINASE INHIBITORS
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Paragraph 0089-0091, (2021/05/29)
The present disclosure provides methods of treating cancer with non-competitive, agonist anti-OX40 antibodies and antigen-binding fragments thereof that bind to human OX40 (ACT35, CD134, or TNFRSF4), in combination with a multi-kinase inhibitor.
Design and optimization of orally spleen tyrosine kinase (SYK) inhibitors for treatment of solid tumor
Fan, Yan,Huang, Zhi,Li, Yao,Qin, Zhongxiang,Wang, Cheng,Wang, Tianqi,Wang, Xin,Xiang, Rong,Yang, Shengyong
, (2020/01/28)
As the aim to discover orally SYK inhibitors for solid tumor treatment, a series of novel derivatives based on imidazo[1,2-a]pyrazine scaffold were designed, synthesized and evaluated. Structure-activity relationship study of both enzymatic and cellular assays led to the identification of compound 12f. The novel SYK inhibitor 12f showed potent antitumor activity against solid tumors with favorable drug-like properties of lipophilicity and solubility. 12f could induce cell apoptosis of ovarian and lung cancer cell lines. In SKOV3 xenograft mouse model, oral administration of 12f led to significant tumour regression without obvious toxicity. 12f improved the limited response of traditional SYK inhibitors in solid tumors in vitro and in vivo. Taken together, this compound may act as a promising lead compound for further development of new SYK inhibitors for solid tumor therapy.
Preparation method of cabozantinib nitrogen oxide impurity
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Paragraph 0025-0026; 0036-0037, (2020/08/27)
The invention discloses a preparation method of a cabozantinib nitrogen oxide impurity. The method comprises the following steps: preparation of an intermediate 1, preparation of 4-chloro-6, 7-dimethoxyquinoline, preparation of an intermediate 2, and prep
A synthesis method of card abundantly for nepal (by machine translation)
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Paragraph 0015; 0023-0024, (2018/04/01)
The present invention provides a card abundantly for nepal synthesis method, the method to 1, 1 - cyclopropyl dicarboxylic acid as the starting material, after the acylation with 4 - [(6, 7 - dimethoxy - 4 - quinolyl) oxy] aniline condensation, with 4 - f
METHOD OF PREPARING FLUORINE-18 LABELED CABOZANTINIB AND ITS ANALOGS
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Paragraph 00102; 00103, (2016/03/29)
The present invention relates to a method of preparing Cabozantinib (Cyclopropane- 1,1-dicarboxylic acid [4-(6,7-dimethoxy-quinolin-4-yloxy)-phenylo]amide (4-fluoro- phenyl)amide) and 18F labeled Cabozantinib.
DOSING OF CABOZANTINIB FORMULATIONS
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Paragraph 00140, (2015/11/11)
The invention relates to administration of various pharmaceutical formulations of N- (4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1- dicarboxamide, (cabozantinib) a c-Met inhibitor, and its metabolites, to achieve des
Bioisosteric replacement of an acylureido moiety attached to an indolin-2-one scaffold with a malonamido or a 2/4-pyridinoylamido moiety produces a selectively potent Aurora-B inhibitor
Wang, Hsiao-Chun,Jagtap, Ajit Dhananjay,Chang, Pei-Teh,Liu, Jia-Rong,Liu, Chih-Peng,Tseng, Hsiang-Wen,Chen, Grace Shiahuy,Chern, Ji-Wang
, p. 312 - 334 (2014/08/05)
Bioisosteric replacement of acylureido moiety in 6-acylureido-3- pyrrolylmethylidene-2-oxoindoline derivatives resulted in a series of malonamido derivatives with indolin-2-one scaffold (11-14). Further conformational restrictions of the malonamido moiety led to 2-oxo-1,2-dihydropyridine (21-25) or a 4-oxo-1,4-dihydropyridine derivatives (31-36). 4-Oxo-1,4-dihydropyridine derivatives were more potent Aurora B inhibitors than their 2-oxo-1,2- dihydropyridine counterparts and demonstrated cytotoxicities against A549 and HepG2 cells in the submicromolar range. In A549 cells, 31h decreased phosphorylation of histone H3, triggered polyploidy, induced expression of pro-apoptotic Fas and FasL with subsequent activation of caspase 8, resulting into apoptosis. In a Huh7-xenograft mouse model, 31h demonstrated potent in vivo efficacy with a daily dose of 5 mg/kg.
Discovery of anilinopyrimidines as dual inhibitors of c-Met and VEGFR-2: Synthesis, SAR, and cellular activity
Zhan, Zhengsheng,Ai, Jing,Liu, Qiufeng,Ji, Yinchun,Chen, Tiantian,Xu, Yechun,Geng, Meiyu,Duan, Wenhu
supporting information, p. 673 - 678 (2014/07/07)
Both c-Met and VEGFR-2 are important targets for cancer therapies. Here we report a series of potent dual c-Met and VEGFR-2 inhibitors bearing an anilinopyrimidine scaffold. Two novel synthetic protocols were employed for rapid analoguing of the designed
METABOLITES OF N-(4-{[6,7-BIS(METHYLOXY)QUINOLIN-4-YL]OXY}PHENYL)-N'-(4-FLUOROPHENYL) CYCLOPROPANE-1,1-DICARBOXAMIDE
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Paragraph 00154; 00155, (2014/09/29)
The invention relates to metabolites of cabozantinib (I) as well as uses thereof.
A DUAL MET - VEGF MODULATOR FOR TREATING OSTEOLYTIC BONE METASTASES
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Paragraph 00118, (2013/11/19)
This invention is directed to the treatment of cancer, particularly castration-resistant prostate cancer and osteolytic bone metastases, with a dual inhibitor of MET and VEGF.
