- SHP2 INHIBITORS AND USES THEREOF
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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.
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Page/Page column 122-123
(2021/04/02)
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- SUBSTITUTED PENTA-FUSED HEXA-HETEROCYCLIC COMPOUNDS, PREPARATION METHOD THEREFOR, DRUG COMBINATION AND USE THEREOF
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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.
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Paragraph 0317-0320
(2020/06/16)
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- 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
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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).
- Singla, Prinka,Luxami, Vijay,Singh, Raja,Tandon, Vibha,Paul, Kamaldeep
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- COMPOUNDS
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Disclosed are novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, compositions containing them and their use in the treatment of or prevention of diseases characterized by LRRK2 kinase activity, for example Parkinson's disease, Alzheimer's disease and amyotrophic lateral sclerosis(ALS).
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Page/Page column 197
(2017/02/09)
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- LRRK2 INHIBITORS AND METHODS OF MAKING AND USING THE SAME
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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.
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Page/Page column 119
(2016/09/22)
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- 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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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)
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Paragraph 0019
(2016/10/31)
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- Discovery of a pyrrolopyrimidine (JH-II-127), a highly potent, selective, and brain penetrant LRRK2 inhibitor
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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
- Hatcher, John M.,Zhang, Jinwei,Choi, Hwan Geun,Ito, Genta,Alessi, Dario R.,Gray, Nathanael S.
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supporting information
p. 584 - 589
(2015/05/27)
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- COMPOUNDS THAT MODULATE EGFR ACTIVITY AND METHODS FOR TREATING OR PREVENTING CONDITIONS THEREWITH
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Provided are compounds and methods for treating or preventing kinase-mediated disorders therewith.
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Page/Page column 89
(2011/07/09)
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- HETEROCYCLIC JAK KINASE INHIBITORS
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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
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Page/Page column 102
(2010/04/27)
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- PI3K/MTOR KINASE INHIBITORS
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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.
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Page/Page column 60
(2010/06/15)
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- Incorporation of water-solubilizing groups in pyrazolopyrimidine mTOR inhibitors: Discovery of highly potent and selective analogs with improved human microsomal stability
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A series of highly potent and selective pyrazolopyrimidine mTOR inhibitors which contain water-solubilizing groups attached to the 6-arylureidophenyl moiety have been prepared. Such derivatives displayed superior potency to those in which these appendages
- Richard, David J.,Verheijen, Jeroen C.,Curran, Kevin,Kaplan, Joshua,Toral-Barza, Lourdes,Hollander, Irwin,Lucas, Judy,Yu, Ker,Zask, Arie
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scheme or table
p. 6830 - 6835
(2010/07/05)
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- REVERSE TRANSCRIPTASE INHIBITORS
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Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using t
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Page/Page column 139
(2009/07/10)
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- BICYCLIC PYRIMIDINE KINASE INHIBITORS
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The present invention is directed to novel bicyclic pyrimidine compounds of Formula (I) or a form or composition thereof, and the use thereof as inhibitors of ATP-protein kinase interactions.
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Page/Page column 31
(2008/06/13)
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- NITROGENOUS FUSED BICYCLIC COMPOUND
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A novel nitrogenous fused bicyclic compound represented by the following general formula [1] or a pharmacologically acceptable salt of the compound. They have excellent SK channel blocking activity and are useful as a medicine. [I] (In the formula, R 0 represents hydrogen, halogeno, etc.; R 1 represents a group represented by the formula (a) or (b); A represents a group represented by the formula (X) or (Y); D 1 , D 2 and D 3 each represents N or CH; R 2 represents halogeno or optionally halogenated lower alkyl, etc.; R 3 represents hydrogen or lower alkyl; and Q represents lower alkylene.)
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Page/Page column 58
(2010/11/26)
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- 3-(SUBSTITUTED AMINO)-PYRAZOLO[3,4-d]PYRIMIDINES AS EPHB AND VEGFR2 KINASE INHIBITORS
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The invention relates to novel pyrazolo[3,4-d]pyrimidines of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.
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Page/Page column 71
(2010/11/27)
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- PYRAZOLE DERIVATIVES AS INHIBITORS OF RECEPTOR TYROSYNE KINASES
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Compounds of formula (I): and their use in the inhibition of Trk activity are described.
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Page/Page column 108-109
(2008/06/13)
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