3702-12-3Relevant academic research and scientific papers
HSP90 INHIBITORS AND USES THEREOF
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Paragraph 00185; 00212; 00216, (2020/11/23)
Herein is described the design and synthesis of resorcylate aminopyrazole compounds. These compounds show broad, potent and fungal-selective Hsp90 inhibitory activity. These compounds also find use in treating Hsp90 related deseases.
Design and Synthesis of Fungal-Selective Resorcylate Aminopyrazole Hsp90 Inhibitors
Huang, David S.,Leblanc, Emmanuelle V.,Shekhar-Guturja, Tanvi,Robbins, Nicole,Krysan, Damian J.,Pizarro, Juan,Whitesell, Luke,Cowen, Leah E.,Brown, Lauren E.
, p. 2139 - 2180 (2019/10/11)
The molecular chaperone Hsp90, essential in all eukaryotes, plays a multifaceted role in promoting survival, virulence, and drug resistance across diverse pathogenic fungal species. The chaperone is also critically important, however, to the pathogen's hu
Application of 5-aminopyrazole compounds to plant growth regulation aspect
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Paragraph 0014; 0035-0037, (2018/05/16)
The invention discloses application of 5-aminopyrazole compounds to plant growth regulation aspect in the technical field of pesticide compounds, in particular to application of the 5-aminopyrazole compounds shown by the formula to the plant growth regulation aspect, particularly the application to the plant growth inhibition. The formula I is shown in the description. The compound shown in the formula I can be used as a weedicide; weeds in places such as highway and railway can be killed through regulating the concentration of the 5-aminopyrazole compounds, wherein the R1 is hydrogen or alkylor phenyl or substituted phenyl; R2 is alkyl; R3 is hydrogen or halogen.
Drug Discovery against Psoriasis: Identification of a New Potent FMS-like Tyrosine Kinase 3 (FLT3) Inhibitor, 1-(4-((1H-Pyrazolo[3,4-d]pyrimidin-4-yl)oxy)-3-fluorophenyl)-3-(5-(tert-butyl)isoxazol-3-yl)urea, That Showed Potent Activity in a Psoriatic Animal Model
Li, Guo-Bo,Ma, Shuang,Yang, Ling-Ling,Ji, Sen,Fang, Zhen,Zhang, Guo,Wang, Li-Jiao,Zhong, Jie-Min,Xiong, Yu,Wang, Jiang-Hong,Huang, Shen-Zhen,Li, Lin-Li,Xiang, Rong,Niu, Dawen,Chen, Ying-Chun,Yang, Sheng-Yong
supporting information, p. 8293 - 8305 (2016/10/03)
Psoriasis is a chronic T-cell-mediated autoimmune disease, and FMS-like tyrosine kinase 3 (FLT3) has been considered as a potential molecular target for the treatment of psoriasis. In this investigation, structural optimization was performed on a lead compound, 1-(4-(1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)phenyl)-3-(4-chloro-3-(trifluoromethyl)phenyl)urea (1), which showed a moderate inhibitory activity againt FLT3. A series of pyrazolo[3,4-d]pyrimidine derivatives were synthesized, and structure-activity relationship analysis led to the discovery of a number of potent FLT3 inhibitors. One of the most active compounds, 1-(4-(1H-pyrazolo[3,4-d]pyrimidin-4-yloxy)-3-fluorophenyl)-3-(5-tert-butylisoxazol-3-yl)urea (18b), was then chosen for in-depth antipsoriasis studies because this compound displayed the highest potency in a preliminary antipsoriasis test. Compound 18b exhibited significant antipsoriatic effects in the K14-VEGF transgenic mouse model of psoriasis, and no recurrence was found 15 days later after the last administration. Detailed mechanisms of action of compound 18b were also investigated. Collectively, compound 18b could be a potential drug candidate for psoriasis treatment.
9H-PYRIMIDO[4,5-B]INDOLES AND RELATED ANALOGS AS BET BROMODOMAIN INHIBITORS
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Paragraph 0549-0550, (2015/09/28)
The present disclosure provides substituted 9H-pyrimido[4,5-b]indoles and 5H-pyrido[4,3-b]indoles and related analogs represented by Formula I: and the pharmaceutically acceptable salts, hydrates, and solvates thereof, wherein R1a, A, B1, B2, G, X1, Y1, Y2, and Y3 are as defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a condition or disorder responsive to inhibition of BET bromodomains. Compounds of the present disclosure are especially useful for treating cancer.
PYRAZOLE DERIVATIVES
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Paragraph 0143, (2013/04/23)
Disclosed are compounds of general formula (I), wherein R, R1, Rc, Rd, Re, Rf, X, Y, Z, A and B are as defined in the application.
PYRAZOLE DERIVATIVES
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Paragraph 0259, (2013/06/26)
Disclosed are compounds of general formula (I), wherein R, R1, Rc, Rd, Re, Rf, X, Y, Z, A and B are as defined in the application.
Pharmacologically active pyrazolopyridines
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, (2008/06/13)
The present invention is directed to new 4,7-dihydro-pyrazolo[3,4-b]pyridines. The compounds possess Ca2+ -antagonist, antihypertensive, vasodilating and antiangina activity. A process for producing them as well as pharmaceutical compositions containing them are also described.
4,7-dihydropyrazolo(3,4-b) pyridine derivatives
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, (2008/06/13)
Novel Ca-blockers, 4,7-dihydropyrazolo[3,4-b]pyridine derivatives having potent antihypertensive and coronary vasodilating actions and useful in treatment for diseases in circulatory system, but without systole inhibitory action.
