20877-81-0Relevant academic research and scientific papers
Synthesis of novel quinoxaline-5-carboxylic acid derivatives
Kornberg, Brian E.,Nikam, Sham S.,Rafferty, Michael F.
, p. 1271 - 1277 (1999)
This paper describes the synthesis of several new 2,3-dimethoxy-6- methyl-7-nitro-quinoxaline-5-carboxylic acid derivatives (13a-m) via a multistep synthetic route from 5-methyl-1H-benzo[d][1,3]oxazine-2,4-dione (1).
Discovery of Orally Bioavailable Ligand Efficient Quinazolindiones as Potent and Selective Tankyrases Inhibitors
Qin, Donghui,Lin, Xiaojuan,Liu, Zhi,Chen, Yan,Zhang, Zhiliu,Wu, Chengde,Liu, Linlin,Pan, Yan,Laquerre, Sylvie,Emery, John,Fergusson, Jeff,Roland, Kimberly,Keenan, Rick,Oliff, Allen,Kumar, Sanjay,Cheung, Mui,Su, Dai-Shi
supporting information, p. 1005 - 1010 (2021/05/27)
We report herein the discovery of quinazolindiones as potent and selective tankyrase inhibitors. Elucidation of the structure-activity relationship of the lead compound 1g led to truncated analogues that have good potency in cells, pharmacokinetic (PK) properties, and excellent selectivity. Compound 21 exhibited excellent potencies in cells and proliferation studies, good selectivity, in vitro activities, and an excellent PK profile. Compound 21 also inhibited H292 xenograft tumor growth in nude mice. The synthesis, biological, pharmacokinetic, in vivo efficacy studies, and safety profiles of compounds are presented.
Target protein degradation inducing compound, preparation method thereof and pharmaceutical composition for preventing or treating targeted protein related diseases containing the same as an active ingredient
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Paragraph 0583; 0585-0587, (2020/05/01)
The present invention relates to a degraducer for inducing the decomposition of target protein, a producing method thereof, and a pharmaceutical composition for preventing or treating target protein-related diseases by containing the degraducer as an active ingredient. A novel compound represented by chemical formula 1, ULB-L-PTM, by the present invention, as a degraducer compound inducing the decomposition of target protein using cereblon E3 ubiquitin ligase, is able to significantly achieve a target protein degradation-inducing activity with an excellent binding activity of a cereblon E3 ubiquitin ligase binder thereby, being able to achieve an excellent protein degradation activity by targeting protein or polypeptide related to various diseases. The bromodomain-containing pharmaceutical composition for preventing or treating protein-related diseases or conditions contains the novel compound represented by chemical formula 1 as an active ingredient and has a useful effect of providing a health functional food composition for prevention or improvement.(AA) Example 22 (nM, 24h)COPYRIGHT KIPO 2020
NOVEL PIPERIDINE-2,6-DIONE DERIVATIVE AND USE THEREOF
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Paragraph 0134-0136, (2020/03/09)
The present disclosure relates to a novel piperidine-2,6-dione derivative and a use thereof and, more specifically, to a piperidine-2,6-dione derivative compound having a structure of a thalidomide analog. A compound of chemical formula 1 according to the present disclosure specifically binds with CRBN protein, and is involved in functions thereof. Therefore, the compound of the present disclosure can be favorably used in the prevention or treatment of leprosy, chronic graft versus host disease, an inflammatory disease, or cancer, which are caused by actions of CRBN protein.
Synthesis of Ring-Fused, N-Substituted 4-Quinolinones Using p Ka-Guided, Base-Promoted Annulations with Isatoic Anhydrides: Total Synthesis of Penicinotam
Khalifa, Muhammad M.,Philkhana, Satish Chandra,Golden, Jennifer E.
, p. 464 - 481 (2019/12/24)
An anionic annulation strategy employing isatoic anhydrides and a wide assortment of enolizable partners was developed to afford over 80 novel ring-fused, N-substituted 4-quinolinones, an underrepresented privileged template. Multiple factors governing the efficiency of the transformation were determined, resulting in a reliable and tunable synthetic platform applicable for a broad range of substrates with variable deprotonation susceptibility, such as tetramic and tetronic acids, cyclic 1,3-diketones, and cycloalkanones. Application to the synthesis of bioactive, pyrrolizine-fused 4-quinolinone, penicinotam 3, resulted in the most brief and highest yielding total synthesis of the alkaloid in three steps and a 36% overall yield.
Quinazoline dione derivatives and preparation method and application thereof
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Paragraph 0139; 0140; 0141; 0142, (2017/07/19)
The invention provides novel quinazoline dione derivatives and a preparation method and application thereof. The compounds include compounds with the structure shown in the general formula V in the description and pharmaceutically acceptable salts or hydrates thereof. The compounds are active ligands of novel cannabinoid II receptors (CB2) and can be used for preparing medicine for treating, preventing and relieving CB2 receptor-mediated diseases, wherein the medicine is an agonist or partial agonist or inverse agonist or antagonist of CB2 receptors.
METHOD OF IMPROVING STABILITY OF SWEET ENHANCER AND COMPOSITION CONTAINING STABILIZED SWEET ENHANCER
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Paragraph 0331, (2015/09/23)
The present invention includes methods of stabilizing one or more sweet enhancers when they are exposed to a light source as well as liquid compositions containing one or more sweet enhancers and one or more photostabilizers.
Synthesis, biological evaluation and SAR of 3-benzoates of ingenol for treatment of actinic keratosis and non-melanoma skin cancer
Grue-Sorensen, Gunnar,Liang, Xifu,Mansson, Kristoffer,Vedso, Per,Dahl Sorensen, Morten,Soor, Anke,Stahlhut, Martin,Bertelsen, Malene,Engell, Karen Margrethe,Hoegberg, Thomas
, p. 54 - 60 (2014/01/17)
Ingenol 3-benzoates were investigated with respect to chemical stability, pro-inflammatory effects, cell death induction and PKCδ activation. A correlation between structure, chemical stability and biological activity was found and compared to ingenol mebutate (ingenol 3-angelate) used for field treatment of actinic keratosis. We also provided further support for involvement of PKCδ for induction of oxidative burst and cytokine release. Molecular modeling and dynamics calculations corroborated the essential interactions between key compounds and C1 domain of PKCδ.
QUINAZOLINEDIONES AS TANKYRASE INHIBITORS
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Page/Page column 36; 37, (2014/01/07)
This invention relates to the use of quinazolinediones for the modulation, notably the inhibition of the activity of tankyrases (TNKS1 and TNKS2). Suitably, the present invention relates to the use of quinazolinediones in the treatment of cancer, fibrosis and other hyperproliferative diseases through this mechanism.
A phosgene and peroxide-free one-pot tandem synthesis of isatoic anhydrides involving anthranilic acid, boc anhydride and 2-chloro-N-methyl pyridinium iodide
Verma, Chhaya,Sharma, Somesh,Pathak, Arunendra
supporting information, p. 6897 - 6899 (2019/04/10)
A phosgene and peroxide-free approach for the synthesis of isatoic anhydrides has been described. The synthesis involves the carbamate formation with boc anhydride followed by in situ cyclization to afford the isatoic anhydride. The importance of this synthetic strategy is in the ease of operation, scalability and preparation from readily available raw materials.
