86477-05-6Relevant articles and documents
PYRROLIDINYL UREA DERIVATIVES AND APPLICATION THEREOF IN TRKA-RELATED DISEASES
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Paragraph 0153; 0154; 0155, (2021/05/21)
The present invention relates to a class of TrkA inhibitors and an application thereof in the preparation of a drug for the treatment of diseases associated with TrkA. The present invention specifically discloses compounds represented by formula (I) and f
MACROCYCLIC INDOLES AS MCL-1 INHIBITORS
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, (2020/06/10)
Disclosed is compound of formula I and the pharmaceutically acceptable salts and solvates thereof, wherein R, R1a, R1b, R1h, L1, L2, L3, ?, ?, ? are as defined as set forth in the specification. Disclosed is compound of formula I for use to treat a condition or disorder responsive to Mcl-1 inhibition such as cancer.
MACROCYCLIC FUSED PYRRAZOLES AS MCL-1 INHIBITORS
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, (2020/08/13)
Provided are compounds represented by Formula IA: (IA), and the pharmaceutically acceptable salts and solvates thereof, wherein R, R 1a, R 1b, L 1, L 2, L 3, X, A, B and C are as defined as set forth
Big ring indole used as MCL-1 inhibitor
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, (2020/03/12)
The invention provides a compound represented by a formula (I) and a pharmaceutical salt and solvate thereof. In the formula (I), the definitions of R, R1a, R1b, R1h, L1, L2, and L3 are shown in the description. The invention also provides a compound represented by the formula (I), and the compound can be used to treat disease or disorder related with MCL-1 inhibition, such as cancers.
Design, synthesis and biological evaluation of ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors
Xie, Hongming,Lin, Xinglong,Zhang, Yingjun,Tan, Fuxing,Chi, Bo,Peng, Zhihong,Dong, Wanrong,An, Delie
supporting information, (2020/10/06)
We report herein the synthesis of novel ring-fused pyrazoloamino pyridine/pyrimidine derivatives as potential FAK inhibitors and the evaluation of pharmaceutical activity against five cancer cell lines (MDA-MB-231, BXPC-3, NCI-H1975, DU145 and 786O). Generally, the majority of compounds displayed strong anti-FAK enzymatic potencies (IC50 1 nM) and could effectively inhibit several class of cancer cell lines within the concentration of 3 μM in comparison with GSK2256098 as a reference. Among them, compound 4o is considered to be the most effective due to high sensitivity in antiproliferation. In culture, 4o could not only inhibit FAK Y397 phosphorylation in MDA-MB-231 cell line, but also trigger apoptosis in a dose-dependent manner. Furthermore, computational docking analysis also suggested that 4o and TAE-226 displayed the similar interaction with FAK kinase domain.
CDK4/6 INHIBITORS AND USE THEREOF
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, (2019/03/05)
The present disclosure relates to a compound of formula (I), or a pharmaceutically acceptable salt, a solvate, a stereoisomer, or tautomer thereof, a pharmaceutical composition comprising a compound of formula (A) or formula (B), and any subgenera thereof, and use of said compounds and compositions thereof, wherein R1, R2, R3a, R3b, R5, R6, X1, X2, Y and n are described herein.
BENZOTRIAZOLE-DERIVED AND UNSATURATED AMIDE COMPOUND USED AS TGF- R1 INHIBITOR
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, (2019/04/29)
A benzotriazole-derived α and β-unsaturated amide compound used as TGF-βR1 inhibitor or a pharmaceutically acceptable salt thereof, the structure of the compound being as shown in formula (I).
ETHANEDIAMINE-HETEROCYCLE DERIVATIVES AS INHIBITORS OF PROTEIN ARGININE METHYLTRANSFERASES
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, (2019/09/15)
The present invention relates to ethanediamine-heterocycle compounds that are able to act as inhibitors of PRMTs (protein arginine methyltransferases) for treating cancer and other diseases mediated by PRMTs.
Focal adhesion kinase inhibitor and use
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, (2019/01/08)
The invention belongs to the field of medicines, relates to a focal adhesion kinase inhibitor and use, in particular relates to a novel focal adhesion kinase inhibitor compound, or stereoisomers, geometric isomers, tautomers, oxynitrides, hydrates, solvates, metabolites, pharmaceutically acceptable salts or prodrugs thereof, further relates to the use of the compound and pharmaceutical compositions as medicines, in particular the use of the compound and pharmaceutical compositions in manufacture of medicines for treatment or prevention of cancer, pulmonary hypertension, and pathological angiogenesis-related diseases.
BIARYL COMPOUNDS USEFUL FOR THE TREATMENT OF HUMAN DISEASES IN ONCOLOGY, NEUROLOGY AND IMMUNOLOGY
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Paragraph 0544, (2015/06/25)
The present invention provides compounds and compositions thereof which are useful as inhibitors of Bruton's tyrosine kinase and which exhibit desirable characteristics for the same.