33771-04-9Relevant academic research and scientific papers
1,5,7-TRISUBSTITUTED ISOQUINOLINE DERIVATIVES, PREPARATION THEREOF, AND USE THEREOF IN MEDICINES
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Paragraph 0181; 0183; 0253-0254, (2020/08/30)
The present disclosure relates to 1,5,7-trisubstituted isoquinoline derivatives, their preparation and pharmaceutical use. In particular, the present disclosure discloses a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof, and a preparation method and use thereof. The definitions of the groups in the formula can be found in the specification and claims.
Discovery of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific glucokinase activators: Design, synthesis, and biological evaluation
Wang, Zhengyu,Shi, Xiaofan,Zhang, Huan,Yu, Liang,Cheng, Yanhua,Zhang, Hefeng,Zhang, Huibin,Zhou, Jinpei,Chen, Jing,Shen, Xu,Duan, Wenhu
, p. 128 - 152 (2017/08/10)
Glucokinase (GK) activators are being developed for the treatment of type 2 diabetes mellitus (T2DM). However, existing GK activators have risks of hypoglycemia caused by over-activation of GK in islet cells and dyslipidemia caused by over-activation of intrahepatic GK. In the effort to mitigate risks of hypoglycemia and dyslipidemia while maintaining the promising efficacy of GK activator, we investigated a series of cycloalkyl-fused N-thiazol-2-yl-benzamides as tissue non-specific partial GK activators, which led to the identification of compound 72 that showed a good balance between in vitro potency and enzyme kinetic parameters, and protected β-cells from streptozotocin-induced apoptosis. Chronic treatment of compound 72 demonstrated its potent activity in regulation of glucose homeostasis and low risk of dyslipidemia with diabetic db/db mice in oral glucose tolerance test (OGTT). Moreover, acute treatment of compound 72 did not induce hypoglycemia in C57BL/6J mice even at 200 mg/kg via oral administration.
CXCR4 Receptor Antagonists
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Paragraph 0122; 0123, (2013/11/06)
Disclosed are compounds that are antagonists of the CXCR4 receptor.
CXCR4 RECEPTOR ANTAGONISTS
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Page/Page column 34, (2012/05/04)
The compounds of formula (I) are antagonists of the CXCR4 receptor Wherein R1, X, Y and R2 are as defined in the claims.
QUINAZOLINE AND QUINOLINE DERIVATIVES AS IRREVERSIBLE PROTEIN TYROSINE KINASE INHIBITORS
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Page/Page column 11, (2009/05/29)
A compound of formula (I), a pharmaceutically acceptable salt, or hydrate thereof, and a method of preparing the same. A method of treating or preventing a physiological disorder caused by abnormal protein tyrosine kinase activity in a mammal comprising administering to said mammal a pharmaceutical composition comprising a compound of formula (I).
INREVERSIBLE PROTEIN TYROSINE KINASES INHIBITORS AND THE PREPARATION METHODS AND USES THEREOF
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Page/Page column 19, (2011/08/10)
The compounds which could inhibit protein tyrosine kinases activity or the pharmaceutical acceptable salts or hydrates thereof. The uses of the compounds in treating or preventing physiological abnormal induced by protein tyrosine kinases overexpression in mammal. The preparation methods of the compounds.
Pharmaceutical compounds
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Page/Page column 91, (2008/06/13)
Compounds of Formulae Ia and Ib, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia and Ib for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
