- 2-(1H-pyrazol-3-yl) pyridine derivative as well as preparation method and application thereof
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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.
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Paragraph 0071-0074
(2021/06/22)
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- Discovery of a new class of JMJD6 inhibitors and structure–activity relationship study
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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.
- Wang, Tianqi,Zhang, Rong,Liu, Yang,Fang, Zhen,Zhang, Hailin,Fan, Yan,Yang, Shengyong,Xiang, Rong
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supporting information
(2021/05/27)
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- NOVEL PYRIMIDINE-PYRIDINE DERIVATIVES
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The invention relates to novel pyrimidine-pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.
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Page/Page column 17
(2011/04/14)
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- PYRIDINE DERIVATIVES AS S1P1/EDG1 RECEPTOR MODULATORS
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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.
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Page/Page column 14
(2011/09/20)
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- 3-AZA-BICYCLO[3.1.0]HEXANE DERIVATIVES
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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.
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Page/Page column 58
(2010/02/17)
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- Modulators of S1P and Methods of Making And Using
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The invention is directed to Compounds of Formula I: as well as methods of making and using the compounds.
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Page/Page column 63-64
(2010/10/19)
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- Pyridin-4-yl derivatives as immunomodulating agents
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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.
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Page/Page column 16
(2010/04/23)
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- PYRIDINE DERIVATIVES AS S1P1/EDG1 RECEPTOR MODULATORS
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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.
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Page/Page column 38-39; 49
(2009/04/25)
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- NOVEL PYRIMIDINE-PYRIDINE DERIVATIVES
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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.
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Page/Page column 42
(2009/10/22)
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- PYRIDIN-4-YL DERIVATIVES AS IMMUNOMODULATING AGENTS
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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.
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Page/Page column 41
(2008/06/13)
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- Chemical compounds
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The invention relates to quinazoline derivatives of the formula: [wherein: Y1represents —O—, —S—, —CH2—, —SO—, —SO2—, —NR5CO—, —CONR6—, —SO2NR7—, —NR8SO2— or —NR9— (wherein R5, R6, R8and R9each independently represents hydrogen, alkyl or alkoxyalkyl); R1represents hydrogen, hydroxy, halogeno, nitro, trifluoromethyl, cyano, alkyl, alkoxy, alkylthio, amino or alkylamino. R2represents hydrogen, hydroxy, halogeno, alkyl, alkoxy, trifluoromethyl, cyano, amino or nitro; m is an integer from 1 to 5; R3represents hydroxy, halogeno, alkyl, alkoxy, alkanoyloxy, trifluoromethyl, cyano, amino or nitro; R4represents a group which is or which contains an optionally substituted pyridone, phenyl or aromatic heterocyclic group] and salts thereof; processes for their preparation and pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.
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