5521-38-0Relevant academic research and scientific papers
WEE1 inhibitors as well as preparation and application thereof
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Paragraph 0430; 0441-0444, (2020/10/14)
The invention relates to WEE1 inhibitors as well as preparation and application thereof. The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts, solvates, polymorphs or isomers thereof, and their use in the preparation of medicaments for the treatment of diseases associated with WEE1 activity.
HETEROCYCLIC COMPOUNDS AND USES THEREOF
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Paragraph 0622-0624, (2019/04/25)
Heterocyclic compounds as Wee1 inhibitors are provided. The compounds may find use as therapeutic agents for the treatment of diseases and may find particular use in oncology.
Design, synthesis and biological evaluation of novel 7-amino-[1,2,4]triazolo[4,3-f]pteridinone, and 7-aminotetrazolo[1,5-f]pteridinone derivative as potent antitumor agents
Hou, Yunlei,Zhu, Liangyu,Li, Zhiwei,Shen, Qi,Xu, Qiaoling,Li, Wei,Liu, Yajing,Gong, Ping
, p. 690 - 709 (2019/01/04)
To develop novel therapeutic agents with anticancer activities, two series of novel 7-amino-[1,2,4]triazolo[4,3-f]pteridinone, and 7-aminotetrazolo[1,5-f]pteridinone derivatives were designed and synthesized. All compounds were tested for anti-proliferative activities against five cancer cell lines. The structure-activity relationships (SARs) studies were conducted through the variation in two regions, the moiety of A ring and the terminal aniline B on pteridinone core. 1-Methyl-1,2,4-triazole derivative L7 with 2,6-dimethylpiperazine showed the most potent antiproliferative activity against A549, PC-3, HCT116, MCF-7 and MDA-MB-231 cell lines with IC50 values of 0.16 μM, 0.30 μM, 0.51 μM, 0.30 μM, and 0.70 μM, respectively. Combined with the results of the molecular docking and enzymatic studies, the PLK1 was very likely to be one of the drug targets of compound L7. Furthermore, to clarify the anticancer mechanism of compound L7, further explorations in the bioactivity were conducted. The results showed that compound L7 obviously inhibited proliferation of A549 cell lines, induced a great decrease in mitochondrial membrane potential leading to apoptosis of cancer cells, suppressed the migration of tumor cells, and arrested G1 phase of A549 cells.
Novel aryl piperazines for alleviation of ‘andropause’ associated prostatic disorders and depression
Gupta, Sonal,Pandey, Deepti,Mandalapu, Dhanaraju,Sharma, Vikas,Shukla, Mahendra,Singh, Seema,Singh, Nidhi,Yadav, Santosh Kumar,Tanpula, Dilip Kumar,Singh, Surabhi,Maikhuri, Jagdamba P.,Shukla, Shubha,Lal, Jawahar,Siddiqi, Mohammad I.,Gupta, Gopal,Sharma, Vishnu L.
, p. 204 - 218 (2017/04/03)
A series of seventeen piperazine derivatives have been synthesized and biologically evaluated for the management of andropause-associated prostatic disorders and depression. Five compounds 16, 19, 20, 21 and 22 significantly inhibited proliferation of and
PYRIMIDINE DERIVATIVES AS KINASE INHIBITORS AND THEIR THERAPEUTICAL APPLICATIONS
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Paragraph 00212, (2016/09/22)
The present invention provides kinase inhibitors with anti-proliferative activity comprising substituted pyrimidine derivatives and pharmaceutically-acceptable formulations thereof. In addition, the invention provides methods for making novel compounds and methods for using the compounds.
PYRIMIDOPYRIMIDINONES USEFUL AS WEE-1 KINASE INHIBITORS
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Page/Page column 236, (2015/07/07)
The present invention relates to compounds that are useful as inhibitors of the activity of Wee-1 kinase. The present invention also relates to pharmaceutical compositions comprising these compounds and to methods of using these compounds in the treatment of cancer and methods of treating cancer.
CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
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Paragraph 0322, (2015/03/13)
Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.
2, 4 -DIAMINOPYRIMIDINE DERIVATIVES AS PROTEIN KINASE INHIBITORS
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Page/Page column 112-113, (2012/05/20)
The present invention relates to novel pyrimide derivatives of formula (I): that are useful as kinase inhibitors. More particularly, the present invention relates to novel pyrimidine compounds, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of proliferative disorders.
Synthesis of a novel series of 4-arylpiperazinyl derivatives linked to a 2-(Pyridin-3-yl)-1H-benzimidazole as new delavirdine analogues
Pessoa-Mahana, David,Nu?n?ez, Andre?s,Espinosa, Christian,Mella-Raipa?n, Jaime,Pessoa-Mahana, Herna?n
supporting information; experimental part, p. 63 - 70 (2010/08/20)
The synthesis of a series of substituted arylpiperazines linked to a 2-(pyridin-3-yl)-1H-benzo[d] imidazole scaffold through an alkylic linker is reported. The novel 1-(2-(4-arylpiperazin-1-yl) alkyl)-2-(pyridin-3-yl)-1H- benzimidazole derivatives are structurally related to the anti-HIV-1 drug Delavirdine and belong to the bis(heteroaryl)piperazines family (BHAPs), a well known HIV-1 reverse transcriptase inhibitors group.
2-AMINOPYRIMIDINE AND 2-AMINOPYRIDINE-4-CARBAMATES FOR USE IN THE TREATMENT OF AUTOIMMUNE DISEASES
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Page 59, (2010/02/10)
The present invention relates to pyrimidine or pyridine carbamate compounds having the general Formula (1) and pharmaceutically acceptable salts or derivatives thereof. Also included are methods of treatment of various diseases and conditions, including inflammation, inhibition of T cell activation and proliferation, arthritis, organ transplant, ischemic or reperfusion injury, myocardial infarction, stroke, multiple sclerosis, inflammatory bowel disease, Crohn's disease, lupus, hypersensitivity, type 1 diabetes, psoriasis, dermatitis, Hashimoto's thyroiditis, Sjogren's syndrome, autoimmune hyperthyroidism, Addison's disease, autoimmune diseases, glomerulonephritis, allergic diseases, asthma, hayfever, eczema, cancer, colon carcinoma, thymoma, just to name a few, in a mammal, the methods comprising administering a therapeutically-effective amount a compound of Formula I, or a salt or derivative form thereof, as described above.
