134597-95-8Relevant academic research and scientific papers
CYCLIC PENTAMER COMPOUNDS AS PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9) INHIBITORS FOR THE TREATMENT OF METABOLIC DISORDER
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Page/Page column 327-329, (2020/06/19)
The disclosure relates to inhibitors of PCSK9 useful in the treatment of cholesterol lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I):, or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, N-oxide, or tautomer thereof, wherein X1, R1, R2, R3, R4, R5, R6, R6', R7, R7', R8, R9, R9', R10, R11, R12, and n are described herein.
NITROGENOUS HETEROCYCLIC COMPOUND, PREPARATION METHOD, INTERMEDIATE, COMPOSITION AND USE
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Paragraph 0469, (2019/01/17)
Disclosed are a nitrogenous heterocyclic compound, intermediates, a preparation method, a composition and use thereof. The nitrogenous heterocyclic compound in the present invention is as shown in formula I. The compound has a high inhibitory activity towards ErbB2 tyrosine kinase and a relatively good inhibitory activity towards human breast cancer BT-474 and human gastric cancer cell NCI-N87 which express ErbB2 at a high level, and at the same time has a relatively weak inhibitory activity towards EGFR kinase. Namely, the compound is a highly selective small-molecule inhibitor targeted at ErbB2, and hence it has a high degree of safety, and can effectively enlarge the safety window in the process of taking the drug.
CK2 INHIBITORS, COMPOSITIONS AND METHODS THEREOF
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Paragraph 0598; 0601, (2018/02/01)
The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula (I), or a stereoisomer, a tautomer or a pharmaceutically acceptable salt thereof. For Formula (I) compounds R1, R2, R3, Ar and Z are as defined in the specification. The inventive Formula (I) compounds are inhibitors of CK2 and find utility in any number of therapeutic applications, including but not limited to treatment of proliferative disorders such as cancer, inflammation and immunological disorders.
Biphenyl/diphenyl ether renin inhibitors: Filling the S1 pocket of renin via the S3 pocket
Yuan, Jing,Simpson, Robert D.,Zhao, Wei,Tice, Colin M.,Xu, Zhenrong,Cacatian, Salvacion,Jia, Lanqi,Flaherty, Patrick T.,Guo, Joan,Ishchenko, Alexey,Wu, Zhongren,McKeever, Brian M.,Scott, Boyd B.,Bukhtiyarov, Yuri,Berbaum, Jennifer,Panemangalore, Reshma,Bentley, Ross,Doe, Christopher P.,Harrison, Richard K.,McGeehan, Gerard M.,Singh, Suresh B.,Dillard, Lawrence W.,Baldwin, John J.,Claremon, David A.
, p. 4836 - 4843 (2011/09/16)
Structure-based design led to the discovery of a novel class of renin inhibitors in which an unprecedented phenyl ring filling the S1 site is attached to the phenyl ring filling the S3 pocket. Optimization for several parameters including potency in the p
NOVEL 3-METHYL-7-BUTINYL-XANTHINES, PRODUCTION THEREOF, AND USE THEREOF AS MEDICAMENTS
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Page/Page column 30, (2008/06/13)
The invention relates to novel substituted xanthines of general formula (I), wherein R1, R2, and X are defined as mentioned in the claims, the tautomers, enantiomers, diastereomers, mixtures, and salts thereof, which have valuable pharmaceutical properties, especially an inhibitive effect on the activity of the dipeptidyl peptidase-IV (DPP-IV) enzyme.
