103977-79-3Relevant academic research and scientific papers
GCN2 MODULATOR COMPOUNDS
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, (2021/08/27)
The disclosures herein relate to novel compounds of Formula (1): or a salt thereof, wherein X, Y, R1, R2, R3, R4 and R5 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with General Control Nondepressible 2 (GCN2).
Alkylene phenylsulfonamide type selective ZAK inhibitor and application thereof
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, (2018/06/16)
The invention relates to application of an alkylene phenylsulfonamide compound with a structure of formula (I) (shown in the description) or pharmaceutically acceptable salt thereof or stereisomer thereof or a prodrug molecule thereof in preparation of a
Structure Based Design of N-(3-((1H-Pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides as Selective Leucine-Zipper and Sterile-α Motif Kinase (ZAK) Inhibitors
Chang, Yu,Lu, Xiaoyun,Shibu, Marthandam Asokan,Dai, Yi-Bo,Luo, Jinfeng,Zhang, Yan,Li, Yingjun,Zhao, Peng,Zhang, Zhang,Xu, Yong,Tu, Zheng-Chao,Zhang, Qing-Wen,Yun, Cai-Hong,Huang, Chih-Yang,Ding, Ke
, p. 5927 - 5932 (2017/07/22)
A series of N-(3-((1H-pyrazolo[3,4-b]pyridin-5-yl)ethynyl)benzenesulfonamides were designed as the first class of highly selective ZAK inhibitors. The representative compound 3h strongly inhibits the kinase activity of ZAK with an IC50 of 3.3 n
INHIBITORS OF KRAS G12C
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, (2015/04/28)
Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
N-(3-ethynyl-2,4-difluorophenyl)sulfonamide derivatives as selective Raf inhibitors
Li, Yingjun,Cheng, Huimin,Zhang, Zhang,Zhuang, Xiaoxi,Luo, Jinfeng,Long, Huoyou,Zhou, Yang,Xu, Yong,Taghipouran, Rana,Li, Dan,Patterson, Adam,Smaill, Jeff,Tu, Zhengchao,Wu, Donghai,Ren, Xiaomei,Ding, Ke
, p. 543 - 547 (2015/05/27)
A series of N-(3-ethynyl-2,4-difluorophenyl)sulfonamides were identified as new selective Raf inhibitors. The compounds potently inhibit B-RafV600E with low nanomolar IC50 values and exhibit excellent target specificity in a selectivity profiling investigation against 468 kinases. They strongly suppress proliferation of a panel of human cancer cell lines and patient-derived melanoma cells with B-RafV600E mutation while being significantly less potent to the cells with B-RafWT. The compounds also display favorable pharmacokinetic properties with a preferred example (3s) demonstrating significant in vivo antitumor efficacy in a xenograft mouse model of B-RafV600E mutated Colo205 human colorectal cancer cells, supporting it as a promising lead compound for further anticancer drug discovery.
QUINAZOLINES AND AZAQUINAZOLINES AS DUAL INHIBITORS OF RAS/RAF/MEK/ERK AND PI3K/AKT/PTEN/MTOR PATHWAYS
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Page/Page column 53, (2014/10/29)
The present application provides novel quinazolines and azaquinazolines and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in for co-regulating RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways by administering a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, T and R4, and R6 to R8' are defined herein, to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment/ the disease is cancer.
Concise route to the key intermediate for divergent synthesis of C7-substituted fluoroquinolone derivatives
Zhang, Xin,Mu, Feng,Robinson, Bobby,Wang, Pengfei
supporting information; experimental part, p. 600 - 601 (2010/04/05)
A concise route to ethyl 7-bromo-1-cyclopropyl-6,8-difluoro-4-quinolone-3-carboxylate has been developed. This compound is a key intermediate for divergent synthesis of various C7-substituted fluoroquinolones, a group of potent topoisomerase II inhibitors
IMIDAZO-TRIAZINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS
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Page/Page column 38, (2010/02/07)
A class of 7-phenylimidazo[1,2-b][1,2,4]triazine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a -NH- linkage, and substituted on the phenyl ring by one or two further substituents as defined herein, being selective ligands for GABAA receptors, in particular having good affinity for the α2 and/or α3 and/or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
Antibiotic derivatives of 7-phenyl-1,4-dihydro-4-oxo-3-quinolinecarboxylic acids
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, (2008/06/13)
1-Substituted-6-fluoro-7-aryl-(8-fluoro)-1,4-dihydroquinol-4-one 3-carboxylic acids having antibacterial activity are prepared by reacting the corresponding alkyl 1-substituted-6-fluoro-7-bromo-(8-fluoro)-1,4-dihydroquinol-4-one-3-carboxylate with an arylmetallic compound and hydrolyzing the ester formed.
