- Discovery of pyrazolo[1,5-a]pyrimidine-3-carbonitrile derivatives as a new class of histone lysine demethylase 4D (KDM4D) inhibitors
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Herein we report the discovery of a series of new small molecule inhibitors of histone lysine demethylase 4D (KDM4D). Molecular docking was first performed to screen for new KDM4D inhibitors from various chemical databases. Two hit compounds were retrieved. Further structural optimization and structure-activity relationship (SAR) analysis were carried out to the more selective one, compound 2, which led to the discovery of several new KDM4D inhibitors. Among them, compound 10r is the most potent one with an IC50 value of 0.41?±?0.03?μM against KDM4D. Overall, compound 10r could be taken as a good lead compound for further studies.
- Fang, Zhen,Wang, Tian-qi,Li, Hui,Zhang, Guo,Wu, Xiao-ai,Yang, Li,Peng, Yu-lan,Zou, Jun,Li, Lin-li,Xiang, Rong,Yang, Sheng-yong
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supporting information
p. 3201 - 3204
(2017/06/13)
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- The pyrazole derivative or its salt in a pharmaceutical composition containing them
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PROBLEM TO BE SOLVED: To provide a novel compound and a pharmaceutical composition useful for treatment and/or prevention of HIV virus infections.SOLUTION: Provided is a pyrazole derivative represented by the general formula (I) or a salt thereof (in the
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Paragraph 0120
(2017/01/26)
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- HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
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Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.
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Paragraph 0175
(2014/05/24)
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- SUBSTITUTED PYRAZOLES AS ESTROGEN RECEPTOR LIGANDS
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The invention provides a compound of formula (I) wherein G is a pyrazole ring as defined in the specification and R4, R5, R6 and R7 are as defined in the specification; or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.
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Paragraph 0166; 0167
(2013/03/26)
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- SUBSTITUTED PYRAZOLES AS ESTROGEN RECEPTOR LIGANDS
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The invention provides a compound of formula (I) wherein G is a pyrazole ring as defined in the specification and R4, R5, R6 and R7 are as defined in the specification; or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt. The invention also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.
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Page/Page column 39
(2011/04/26)
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- PYRIMIDINE DERIVATIVES AND THEIR USE FOR CONTROLLING UNDESIRED PLANT GROWTH
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Compounds of the formula (I) and their agrochemically compatible salts and their use in the field of crop protection are described.
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Page/Page column 24
(2010/07/08)
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- PYRROLE AND PYRAZOLE DERIVATIVES AS POTENTIATORS OF GLUTAMATE RECEPTORS
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The present invention relates to pyrrole and pyrazole compounds of formula (I) and their pharmaceutically acceptable salts, and further relates to their use in treating schizophrenia, cognitive deficits associated with schizophrenia, Alzheimer's disease, dementia of the Alzheimer's type, mild cognitive impairment, or depression. The compounds act as potentiators on glutamate receptors, in particular AMPA and the GluR family.
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Page/Page column 76
(2008/06/13)
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- 5-ANILINO-4-HETEROARYLPYRAZOLE DERIVATIVES USEFUL FOR THE TREATMENT OF DIABETES
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The present invention relates to 5-anilino-4-heteroarylpyrazole compounds, pharmaceutical compositions, and methods for treating diabetes and related disorders.
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Page/Page column 45
(2008/06/13)
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- PYRAZOLOPYRIMIDINES AS KINASE INHIBITORS
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The present invention relates generally to inhibitors of the kinases and more particularly to novel pyrazolopyrimidine compounds.
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- 6-heterocyclyl pyrazolo [3,4-d]pyrimidin-4-ones and compositions and method of use thereof
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Novel 6-heterocyclyl-pyrazolo[3,4-d]pyrimidin-4-ones, useful in treating cardiovascular disease, are prepared by reacting a 5-amino-1H-pyrazole-4-carboxamide with heterocyclylcarboxaldehyde or by reacting a 5-amino-1H-pyrazole-4-carbonitrile with a heterocyclylcarboxamidine, followed by diazotization and hydrolysis of the resulting 4-amino-6-heterocyclyl-pyrazolo[3,4-d]pyrimidine.
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