116340-67-1Relevant academic research and scientific papers
Preparation method and medical application of benzisothiazole and benzothiophene
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Paragraph 0166-0169; 0197-0200, (2021/08/19)
The invention discloses a preparation method and medical application of benzisothiazole and benzothiophene, and telates to the field of pharmaceutical chemistry. According to the invention, benzisothiazole and benzothiophene are the first type of HIF-2 agonists; compared with a compound M1001 found by the applicant in the earlier stage, the invention has better HIF-2 agonist activity, and has remarkable enhancement activity on expression of mRNA and protein of EPO, VGEF, Glut1, NDRG1 and the like at the downstream of HIF-2, so that the invention can be used for preparing drugs for treating and/or preventing chronic kidney diseases/chronic renal anemia, dyslipidemia and high cholesterol caused by abnormal expression of HIF-2; and the method has a good industrialization prospect.
INHIBITORS OF THE YAP/TAZ-TEAD INTERACTION AND THEIR USE IN THE TREATMENT OF CANCER
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Paragraph 0096, (2020/04/21)
The invention relates to compounds of formula (I): wherein R1; R2, R3, R4, R5 and are as defined in the description. The compounds of formula (I) are inhibitors of the YAP/TAZ-TEAD interaction and thu
BICYCLIC COMPOUNDS USEFUL AS GPR120 MODULATORS
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, (2018/03/28)
Provided herein are compounds, compositions including them, and methods of modulating GPR120 activity and treating diseases mediated by GPR120 by administering such compounds and compositions.
NOVEL 3-INDOL SUBSTITUTED DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS FOR USE
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, (2016/10/04)
A compound of Formula I is provided: or pharmaceutically acceptable enantiomers, salts or solvates thereof. The 5 invention further relates to the use of the compounds of Formula I as TDO2 inhibitors. The invention also relates to the use of the compounds of Formula I for the treatment and/or prevention of cancer, neurodegenerative disorders such as Parkinson's disease, Alzheimer's disease and Huntington's disease, chronic viral infections such as HCV and HIV, depression, and obesity. The invention also 10 relates to a process for manufacturing compounds of Formula I.
CYCLOALKYL NITRILE PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS
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Page/Page column 109, (2014/10/03)
Compounds of formula I are provided, which are JAK inhibitors and are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
CYCLOALKYL NITRILE PYRAZOLO PYRIDONES AS JANUS KINASE INHIBITORS
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, (2014/10/03)
The instant invention provides compounds of formula I which are JAK inhibitors, and as such are useful for the treatment of JAK-mediated diseases such as rheumatoid arthritis, asthma, COPD and cancer.
Optimization of heterocyclic substituted benzenesulfonamides as novel carbonic anhydrase IX inhibitors and their structure activity relationship
Gao, Rui,Liao, Sha,Zhang, Chen,Zhu, Weilong,Wang, Liyan,Huang, Jin,Zhao, Zhenjiang,Li, Honglin,Qian, Xuhong,Xu, Yufang
, p. 597 - 604 (2013/05/09)
In this study, starting from a lead compound discovered by virtual screening, a series of novel heterocyclic substituted benzenesulfonamides were designed and synthesized as new carbonic anhydrase IX (CA IX) inhibitors. Some compounds exhibited potent inh
SUBSTITUTED BIPHENYL DERIVATIVE
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Page/Page column 148, (2010/11/27)
The present invention relates to a biaryl derivative or a pharmacologically acceptable salt thereof having an excellent collagen-synthesis inhibition activity. A biaryl derivative having a structure represented by the following General Formula (I) or a pharmacologically acceptable salt thereof: wherein R1 represents a C6-C10 aryl group which is substituted with one to three group(s) each independently selected from the group consisting of a group defined by formula R-L-, a di-(C1-C6 alkyl)amino group, a di-(C1-C6 alkyl)aminosulfonyl group, a hydroxyaminocarbonyl group, and a halogen atom, and so on; R represents a C1-C6 alkyl group, and so on; L represents a sulfonyl group, an aminosulfonyl group, or a sulfonylamino group, and so on; R2 represents a hydrogen atom, and so on; A represents a group defined by formula (II), (III), or (IV); R3 represents a C1-C6 alkyl group, and so on; and R4 represents a C1-C6 alkyl group, and so on.
Design, synthesis, and biological evaluation of N-acetyl-2- carboxybenzenesulfonamides: A novel class of cyclooxygenase-2 (COX-2) inhibitors
Chen, Qiao-Hong,Rao, P. N. Praveen,Knaus, Edward E.
, p. 2459 - 2468 (2007/10/03)
N-Acetyl-2-carboxybenzenesulfonamide (11), and a group of analogues possessing an appropriately substituted-phenyl substituent (4-F, 2,4-F 2, 4-SO2Me, 4-OCHMe2) attached to its C-4, or C-5 position, were synthesized for ev
Pyridine derivatives and pharmaceutical compositions containing them
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, (2008/06/13)
The invention relates to novel pyridyl derivatives, their use as medicaments, pharmaceutical formulations containing them and methods for their preparation.
