3998-88-7Relevant academic research and scientific papers
2-(1H-pyrazol-3-yl) pyridine derivative as well as preparation method and application thereof
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Paragraph 0071-0074, (2021/06/22)
The invention belongs to the field of medicinal chemistry, particularly relates to a compound shown in a formula I, or a stereoisomer, salt, prodrug or solvate thereof, and also relates to a preparation method of the compound and application of the compound in preparation of drugs for treating related diseases mediated by histone demethylase JMJD6.
Discovery of a new class of JMJD6 inhibitors and structure–activity relationship study
Wang, Tianqi,Zhang, Rong,Liu, Yang,Fang, Zhen,Zhang, Hailin,Fan, Yan,Yang, Shengyong,Xiang, Rong
supporting information, (2021/05/27)
JmjC domain-containing protein 6 (JMJD6) has been thought as a potential target for various diseases particularly cancer. However, few selective JMJD6 inhibitors have been reported. In this investigation, molecular docking and biological activity evaluation were performed to retrieve new JMJD6 inhibitors, which led to the identification of a hit compound, J2. Further structural optimization and structure–activity relationship (SAR) analysis towards J2 were carried out, which gave a new potent JMJD6 inhibitor, 7p. This compound showed an IC50 value of 0.681 μM against JMJD6, but displayed no activity against other tested JmjC domain-containing protein family members, indicating good selectivity (>100 fold). Collectively, this investigation offers a selective JMJD6 inhibitor, which could be taken as a lead compound for subsequent drug discovery targeting JMJD6.
NOVEL PYRIMIDINE-PYRIDINE DERIVATIVES
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Page/Page column 17, (2011/04/14)
The invention relates to novel pyrimidine-pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
PYRIDINE DERIVATIVES AS S1P1/EDG1 RECEPTOR MODULATORS
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Page/Page column 14, (2011/09/20)
The invention relates to novel pyridine derivatives of formula (D, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. Formula (I) wherein A represents and the other substituents are as defined in the claims.
3-AZA-BICYCLO[3.1.0]HEXANE DERIVATIVES
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Page/Page column 58, (2010/02/17)
The invention relates to 3-aza-bicyclo[3.1.0]hexane derivatives of formula (I) wherein A, B, n, X, and R1 are as described in the description, and salts thereof, and their use as orexin receptor antagonists.
Modulators of S1P and Methods of Making And Using
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Page/Page column 63-64, (2010/10/19)
The invention is directed to Compounds of Formula I: as well as methods of making and using the compounds.
Pyridin-4-yl derivatives as immunomodulating agents
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Page/Page column 16, (2010/04/23)
The invention relates to pyridine derivatives of Formula (I) wherein A, R1, R2, R3, R4, R5, and R6 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
PYRIDINE DERIVATIVES AS S1P1/EDG1 RECEPTOR MODULATORS
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Page/Page column 38-39; 49, (2009/04/25)
The invention relates to novel pyridine derivatives of formula (D, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. Formula (I) wherein A represents and the other substituants are as defined in the claims.
NOVEL PYRIMIDINE-PYRIDINE DERIVATIVES
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Page/Page column 42, (2009/10/22)
The invention relates to novel pyrimidine-pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. Formula I.
PYRIDIN-4-YL DERIVATIVES AS IMMUNOMODULATING AGENTS
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Page/Page column 41, (2008/06/13)
The invention relates to pyridine derivatives of Formula (I) wherein A, R1, R2, R3, R4, R5, and R6 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
