851435-28-4Relevant academic research and scientific papers
PIPERAZINE AMIDE DERIVATIVE, PREPARATION METHOD THEREFOR, AND USE THEREOF IN MEDICINE
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, (2022/02/27)
The present invention relates to a piperazine amide derivative as represented by formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition thereof, and use of same as a therapeutic agent, especially as a selective Rearranged During Transfection (RET) kinase inhibitor. Ring a, ring e, X1, X2, X3, X4, R1, R2, R3, R4, R4', R5, R5', R6, R6', R7, R7', R8, m, and n have the same definitions as those in the specification.
Methylpyrazole derivatives as RET inhibitor
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Paragraph 0229-0231; 0239-0241, (2021/07/21)
The invention relates to a methylpyrazole derivative as an RET inhibitor, in particular to a compound as shown in a formula (I), a stereoisomer and pharmaceutically acceptable salt thereof, a preparation method and a pharmaceutical composition thereof. The compound of the formula (I) can be used for preventing or treating diseases mediated by abnormal RET activity.
Nitrogen heterocyclic compound, pharmaceutical composition containing nitrogen heterocyclic compound, and preparation method and application of nitrogen heterocyclic compound
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Paragraph 0410; 0411; 0421-0423, (2020/08/18)
Disclosed are a nitrogen heterocyclic compound represented by a formula (I), a pharmaceutical composition comprising the same, and a preparation method and use of the nitrogen heterocyclic compound, and in particular, relates to the use of the nitrogen heterocyclic compound for prevention or treatment of diseases or conditions associated with RET activity.
Five-membered heterocyclic derivatives as well as preparation method thereof and use thereof in medicine
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Paragraph 0057; 0061-0065, (2019/10/15)
The invention provides five-membered heterocyclic derivatives or pharmaceutically acceptable salts thereof which are shown in a general formula (I), a preparation method of the five-membered heterocyclic derivatives or the pharmaceutically acceptable salts thereof, and use of the five-membered heterocyclic derivatives or the pharmaceutically acceptable salts thereof as a therapeutic agent, especially as a rearrangement (RET) kinase inhibitor during selective transfection. In the general formula (I), the definitions of A, B, C, D, E, X, R1, R2 and R3 are the same as those in the description. The general formula (I) is described in the description.
SUBSTITUTED CYCLOPENTANE-AMIDES FOR TREATING DISORDERS RELATED TO RET
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Paragraph 00178; 00179, (2018/03/01)
Described herein are compounds that inhibit wild-type RET and its resistant mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
COMPOUNDS USEFUL FOR TREATING DISORDERS RELATED TO RET
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Paragraph 00169-00171, (2018/02/21)
Described herein are compounds of formula (I) that inhibit wild- type RET and its resistant mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
INHIBITORS OF RET
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Page/Page column 42, (2017/05/20)
Inhibitors of wild-type RET and its resistant mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
INHIBITORS OF RET
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Paragraph 0210-0211, (2017/09/29)
Described herein are compounds that inhibit wild-type RET and its resistant mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
Phenotypic Identification of a Novel Autophagy Inhibitor Chemotype Targeting Lipid Kinase VPS34
Robke, Lucas,Laraia, Luca,Carnero Corrales, Marjorie A.,Konstantinidis, Georgios,Muroi, Makoto,Richters, André,Winzker, Michael,Engbring, Tobias,Tomassi, Stefano,Watanabe, Nobumoto,Osada, Hiroyuki,Rauh, Daniel,Waldmann, Herbert,Wu, Yao-Wen,Engel, Julian
supporting information, p. 8153 - 8157 (2017/06/30)
Autophagy is a critical regulator of cellular homeostasis and metabolism. Interference with this process is considered a new approach for the treatment of disease, in particular cancer and neurological disorders. Therefore, novel small-molecule autophagy modulators are in high demand. We describe the discovery of autophinib, a potent autophagy inhibitor with a novel chemotype. Autophinib was identified by means of a phenotypic assay monitoring the formation of autophagy-induced puncta, indicating accumulation of the lipidated cytosolic protein LC3 on the autophagosomal membrane. Target identification and validation revealed that autophinib inhibits autophagy induced by starvation or rapamycin by targeting the lipid kinase VPS34.
2-(PYRIDIN-3-YL)-PYRIMIDINE DERIVATIVES AS RET INHIBITORS
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Page/Page column 29, (2016/09/22)
Described herein are compounds that inhibit wild-type RET and its resistant mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.
