42754-96-1Relevant academic research and scientific papers
SHP2 INHIBITORS AND USES THEREOF
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Page/Page column 122-123, (2021/04/02)
Compounds of Formula 1 as inhibitors of protein tyrosine phosphatase SHP2 are disclosed. The pharmaceutical compositions comprising compounds of Formula 1, methods of synthesis of these compounds, methods of treatment for diseases associated with the aberrant activity of SHP2 such as cancer using these compounds or compositions containing these compounds are also disclosed.
SUBSTITUTED PENTA-FUSED HEXA-HETEROCYCLIC COMPOUNDS, PREPARATION METHOD THEREFOR, DRUG COMBINATION AND USE THEREOF
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Paragraph 0317-0320, (2020/06/16)
A type of substituted penta-fused hexa-heterocyclic compounds having selective inhibition for PIKfyve kinase, a pharmaceutically acceptable salt and pharmaceutically acceptable solvate thereof, a method for the preparation thereof, a pharmaceutical composition comprising the same, and use of these compounds in the manufacture of a medicament for preventing or treating a disease associated with PIKfyve in vivo, in particular in the manufacture of a medicament for preventing or treating tumor growth and metastasis.
Novel pyrazolo[3,4-d]pyrimidine with 4-(1H-benzimidazol-2-yl)-phenylamine as broad spectrum anticancer agents: Synthesis, cell based assay, topoisomerase inhibition, DNA intercalation and bovine serum albumin studies
Singla, Prinka,Luxami, Vijay,Singh, Raja,Tandon, Vibha,Paul, Kamaldeep
, p. 24 - 35 (2016/10/26)
A series of new pyrazolo[3,4-d]pyrimidine possessing 4-(1H-benzimidazol-2-yl)-phenylamine moiety at C4 position and primary as well as secondary amines at C6 position has been designed and synthesized. Their antitumor activities were evaluated against a panel of 60 human cancer cell lines at National Cancer Institute (NCI). Six compounds displayed potent and broad spectrum anticancer activities at 10?μM. Compounds 8, 12, 14 and 17 proved to be the most active and efficacious candidate in this series, with mean GI50values of 1.30?μM, 1.43?μM, 2.38?μM and 2.18?μM, respectively against several cancer cell lines. Further biological evaluation of these compounds suggested that these compounds induce apoptosis and inhibit human topoisomerase (Topo) IIα as a possible intracellular target. UV-visible and fluorescence studies of these compounds revealed strong interaction with ct-DNA and bovine serum albumin (BSA).
LRRK2 INHIBITORS AND METHODS OF MAKING AND USING THE SAME
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Page/Page column 119, (2016/09/22)
Compounds having the formula (I), (II), (III) are provided. Compounds of the present disclosure are useful for the treatment of neurodegenerative diseases, such as Parkinson's Disease.
Used as inhibitors of FGFR N-(1H-pyrazol-5-yl) pyrimidine and pyrazole -4,6-di-substituted amine compound (by machine translation)
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Paragraph 0019, (2016/10/31)
This invention relates to a kind of used as inhibitors of FGFR N-(1H the [...] pyrazole -5 the [...] ) pyrimidine and pyrazole -4, the 6 [...] disubstituted amine compound. The invention provides a compound of formula I or its pharmaceutically acceptable salt thereof. Also provided is the method for preparing the compound of the formula I, the compound of formula I as pharmaceutical and use in the treatment of cancer . (by machine translation)
Discovery of a pyrrolopyrimidine (JH-II-127), a highly potent, selective, and brain penetrant LRRK2 inhibitor
Hatcher, John M.,Zhang, Jinwei,Choi, Hwan Geun,Ito, Genta,Alessi, Dario R.,Gray, Nathanael S.
supporting information, p. 584 - 589 (2015/05/27)
Activating mutations in leucine-rich repeat kinase 2 (LRRK2) are present in a subset of Parkinson's disease (PD) patients and may represent an attractive therapeutic target. Here we report a 2-anilino-4-methylamino-5-chloropyrrolopyrimidine, JH-II-127 (18
COMPOUNDS THAT MODULATE EGFR ACTIVITY AND METHODS FOR TREATING OR PREVENTING CONDITIONS THEREWITH
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Page/Page column 89, (2011/07/09)
Provided are compounds and methods for treating or preventing kinase-mediated disorders therewith.
HETEROCYCLIC JAK KINASE INHIBITORS
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Page/Page column 102, (2010/04/27)
The present invention relates to compounds of Formula (I) and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds provide a treatment for myeloproliferative disorders and cancer
PI3K/MTOR KINASE INHIBITORS
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Page/Page column 60, (2010/06/15)
6-morpholin-4-yl-pyrazolo[3,4-d]pyrimidine and 2-morpholin-4-yl-7H- pyrrolo[2,3-d]pyrimidine derivatives have unexpected drug properties as inhibitors of PI3 and/or mTOR kinases and are useful in treating disorders related to abnormal PI3K/mT0R activities such as cancer, immune disorders, cardiovascular disease, viral infection, inflammation, metabolism/endocrine disorders and neurological disorders.
