- Methylpyrazole derivatives as RET inhibitor
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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.
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Paragraph 0368-0373; 0483-0488; 0849-0854; 0899-0904
(2021/07/21)
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- 2-thioxothiazolidin-4-one analogs as pan-pim kinase inhibitors
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Proviral integration site for Moloney murine leukemia virus (PIM) kinases are proto-oncogenic kinases involved in the regulation of several cellular processes. PIM kinases are promising targets for new drug development because they play a major role in many cancer-specific pathways, such as survival, apoptosis, proliferation, cell cycle regulation, and migration. Here, 2-thioxothiazolidin-4-one derivatives were synthesized and evaluated as potent pan-PIM kinase inhibitors. Optimized compounds showed single-digit nanomolar IC50 values against all three PIM kinases with high selectivity over 14 other kinases. Compound 17 inhibited the growth of Molm-16 cell lines (EC50 = 14 nM) and modulated the expression of pBAD and p4EBP1 in a dose-dependent manner.
- Yun, Yanghwan,Hong, Victor Sukbong,Jeong, Seungik,Choo, Hyeonseong,Kim, Shin,Lee, Jinho
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p. 854 - 861
(2021/09/06)
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- NOVEL NITROGEN-CONTAINING AROMATIC HETEROCYCLIC COMPOUND
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A compound represented by general formula [1] wherein X represents N or the like, Y represents CH or the like; RA represents a cycloalkyl group which may be substituted or the like, R1 represents an alkyl group or the like, R2 represents an alkyl group which may be substituted or the like, R3 represents a hydrogen atom or an alkyl group, or a pharmaceutically acceptable salt thereof has an inhibitory activity on aldosterone synthetase, and is useful as a prophylactic and/or therapeutic agent for various diseases or symptoms associated with aldosterone.
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Paragraph 0153
(2018/10/15)
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- PHARMACEUTICAL COMPOUNDS AS INHIBITORS OF SPHINGOSINE KINASE
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The present invention relates to compounds that are useful as inhibitors of the activity of one or more isoforms of sphingosine kinase. Particularly, although not exclusively, the present invention also relates to pharmaceutical compositions comprising th
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Page/Page column 65
(2012/06/15)
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- Discovery of novel 3,5-disubstituted indole derivatives as potent inhibitors of Pim-1, Pim-2, and Pim-3 protein kinases
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A series of novel 3,5-disubstituted indole derivatives as potent and selective inhibitors of all three members of the Pim kinase family is described. High throughput screen identified a pan-Pim kinase inhibitor with a promiscuous scaffold. Guided by struc
- Nishiguchi, Gisele A.,Atallah, Gordana,Bellamacina, Cornelia,Burger, Matthew T.,Ding, Yu,Feucht, Paul H.,Garcia, Pablo D.,Han, Wooseok,Klivansky, Liana,Lindvall, Mika
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supporting information; experimental part
p. 6366 - 6369
(2011/12/02)
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- AMIDE COMPOUND
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An object of the present invention is to provide a novel fused-ring compound which has a FAAH inhibitory effect and is useful as an analgesic. The present invention relates to a compound represented by formula (I): wherein symbols are as defined in the specification, or salt thereof.
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Page/Page column 35
(2009/07/10)
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- THERAPEUTIC COMPOUNDS
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The present invention relates to pyrazine substituted pyrrolopyridines which are inhibitors of JAK kinases (JAKl, JAK2, JAK3 and/or TYK2) and/or PDKl and are thus useful for the treatment of myeloproliferative disorders or cancer.
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Page/Page column 46-47
(2009/05/30)
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- Parallel synthesis of N-arylpiperazines using polymer-assisted reactions
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A series of N-arylpiperazines were prepared in a parallel fashion using palladium-catalyzed cross-coupling, or nucleophilic aromatic displacement chemistries, and polymer-assisted sequestration and purification techniques as key steps.
- Duncton, Matthew A. J.,Roffey, Jonathan R. A.,Hamlyn, Richard J.,Adams, David R.
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p. 2549 - 2552
(2007/10/03)
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- Piperazinylacylpiperidine derivatives, their preparation and therapeutic use thereof
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The invention relates to substituted 1-piperazinylacylpiperidine derivatives of general formula (I) in which: n is 1 or 2; p is 1 or 2; R1 represents a halogen atom; a trifluoromethyl radical; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethoxy radical; R2 represents a hydrogen atom or a halogen atom; R3 represents a hydrogen atom; a group —OR5; a group —CH2OR5; a group —NR6R7; a group —NR8COR9; a group —NR8CONR10R11; a group —CH2NR12R13; a group —CH2NR8CONR14R15; a (C1-C4)alkoxycarbonyl; a group —CONR16R17; or else R3 constitutes a double bond between the carbon atom to which it is attached and the adjacent carbon atom of the piperidine ring; R4 represents an aromatic group selected from: the said aromatic groups being unsubstituted or being mono- or disubstituted by a substituent selected independently from a halogen atom; a (C1-C4)alkyl; a (C1-C4)alkoxy; a trifluoromethyl radical; Preparation process and therapeutic application.
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Page/Page column 22
(2008/06/13)
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- BENZOYL-PIPERAZINE DERIVATIVES
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The invention relates to compounds of formula wherein the substituents are described herein. The compounds may be used in the treatment of illnesses based on the glycine uptake inhibitor, such as psychoses, pain, neurodegenerative disfunction in memory and learning, schizophrenia, dementia and other diseases in which cognitive processes are impaired, such as attention deficit disorders or Alzheimer's disease.
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Page/Page column 50
(2008/06/13)
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- PHENYLPYRIDINE CARBONYL PIPERAZINE DERIVATIVE
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The present invention relates to a compound which is represented by the following general formula and has type 4 phosphodiesterase inhibitory action, and uses and an intermediate compound thereof. (whereinR1, R2: hydrogen, a halogen, a lower alkyl, a lower alkoxy, or the like,R3, R4: hydrogen, a (substituted) lower alkyl, a halogen, or the like,R5: hydrogen, a lower alkyl, a lower alkoxycarbonyl, or the like, andn: 0 or 1).
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- Novel compounds and their use
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A compound of the general formula (I): wherein R1, R2, X, Y and Z are as described in the specification.
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