116247-92-8Relevant articles and documents
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.
LSD1 INHIBITORS AND USES THEREOF
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Paragraph 00638-00639, (2016/11/17)
Provided are novel compounds of Formula (I) and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with LSDl. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with LSDl.
AMINE-LINKED MULTICYCLIC COMPOUNDS AS INHIBITORS OF THE PROLINE TRANSPORTER
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Page/Page column 17, (2008/12/05)
This invention relates to multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use.
(R)-PHENYL(HETEROCYCLE)METHANOL-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM AND METHODS OF THEIR USE
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Page/Page column 23, (2008/12/05)
Multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use are described. Compounds described include those of formula I.
(S)-PHENYL(HETEROCYCLE)METHANOL-BASED COMPOUNDS, COMPOSITIONS COMPRISING THEM AND METHODS OF THEIR USE
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Page/Page column 23, (2008/12/06)
Multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use are described. Compounds described include those of formula (I).
METHODS OF TREATING COGNITIVE IMPAIRMENT AND DEMENTIA
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Page/Page column 52, (2008/12/06)
This invention relates to methods for treating, managing and preventing cognitive impairment associated with various diseases and disorders, age-associated memory impairment, and dementia.
Multicyclic compounds and methods of their use
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Page/Page column 17, (2010/11/24)
This invention relates to multicyclic compounds, pharmaceutical compositions comprising them, and methods of their use in, for example, the treatment of cognitive disorders.
Pyrazolo(4,3-c)quinolines
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, (2008/06/13)
There are disclosed compounds of the formula STR1 wherein the various substituents are defined hereinbelow, and, by virtue of their ability to inhibit interleukin 1, their use as antiinflammatory agents and in treatment of disease states involving enzymat
2-heterocyclobenzo[B][1,6]naphthyridines as inhibitors of interleukin
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, (2008/06/13)
There are disclosed compounds of the formula STR1 wherein R1 is pyridl, quinolinyl, pyrazinyl, pyridinyl, pyridazinyl, pyrimidinyl, quinoxalinyl, quinazolinyl or any of the foregoing substituted with halo, lower alkyl, lower alkyl carbonyl, ben