755039-91-9Relevant academic research and scientific papers
Discovery of Potent and Novel Dual PARP/BRD4 Inhibitors for Efficient Treatment of Pancreatic Cancer
Gao, Ling-Li,Huang, Lei,Huang, Shi-Hui,Li, Yu,Lin, Qian-Wen,Meng, Liu-Qiong,Sun, Qin,Wang, Shu-Ping,Wu, Shi-Qi,Xu, Yun-Gen,Zhu, Qi-Hua,Zou, Yi
, p. 17413 - 17435 (2021/12/06)
Targeting poly(ADP-ribose) polymerase1/2 (PARP1/2) is a promising strategy for the treatment of pancreatic cancer with breast cancer susceptibility gene (BRCA) mutation. Inducing the deficiency of homologous recombination (HR) repair is an effective way t
Compound containing methotrexate structure as well as preparation method and application thereof
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Paragraph 0083-0084; 0087; 0099-0100, (2021/11/14)
The invention discloses a compound of a general formula (I) containing a tetrahydrotrexate structure and a preparation method and application thereof. The invention also discloses a composition containing the methotrexate compound or a pharmaceutically ac
Structure-Guided Design and Development of Potent and Selective Dual Bromodomain 4 (BRD4)/Polo-like Kinase 1 (PLK1) Inhibitors
Liu, Shuai,Yosief, Hailemichael O.,Dai, Lingling,Huang, He,Dhawan, Gagan,Zhang, Xiaofeng,Muthengi, Alex M.,Roberts, Justin,Buckley, Dennis L.,Perry, Jennifer A.,Wu, Lei,Bradner, James E.,Qi, Jun,Zhang, Wei
, p. 7785 - 7795 (2018/09/13)
The simultaneous inhibition of polo-like kinase 1 (PLK1) and BRD4 bromodomain by a single molecule could lead to the development of an effective therapeutic strategy for a variety of diseases in which PLK1 and BRD4 are implicated. Compound 23 has been found to be a potent dual kinase-bromodomain inhibitor (BRD4-BD1 IC50 = 28 nM, PLK1 IC50 = 40 nM). Compound 6 was found to be the most selective PLK1 inhibitor over BRD4 in our series (BRD4-BD1 IC50 = 2579 nM, PLK1 IC50 = 9.9 nM). Molecular docking studies with 23 and BRD4-BD1/PLK1 as well as with 6 corroborate the biochemical assay results.
Storage stable perfusion solution for dihydropteridinones
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Page/Page column 17, (2008/06/13)
Disclosed are storage stable aqueous infusible or injectable solutions containing an active substance of general formula (I) wherein the groups L, R1, R2, R3, R4 and R5 have the meanings given in the claims and in the specification, and an amount of a physiologically acceptable acid or mixture of acids sufficient to dissolve the active substance and act as a stabiliser, optionally together with other formulating excipients suitable for parenteral administration, and a process for preparing the infusible or injectable solutions according to the invention.
New dihydropteridinones, processes for preparing them and their use as pharmaceutical compositions
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Page/Page column 12, (2010/02/08)
The present invention relates to new dihydropteridinones of general formula (I) wherein the groups L and R1- R5 have the meanings given in the claims and specification, the isomers thereof, processes for preparing these dihydropterid
DIHYDROPTERIDINONES, METHOD FOR THE PRODUCTION AND USE THEREOF IN THE FORM OF DRUGS
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Page/Page column 39, (2010/02/08)
The invention relates to novel dihydropteridinones of general formula (I), wherein rests L, R1-R5 have the significance indicated in claims and a specification, in the isomers thereof, in a method for producing and using said dihydropteridinones in the form of drugs.
