1082041-85-7Relevant academic research and scientific papers
Discovery of a Novel Series of Pyridone-Based EP3 Antagonists for the Treatment of Type 2 Diabetes
Zhang, Xuqing,Zhu, Bin,Guo, Lili,Bakaj, Ivona,Rankin, Matthew,Ho, George,Kauffman, Jack,Lee, Seunghun P.,Norquay, Lisa,MacIelag, Mark J.
supporting information, p. 451 - 458 (2021/04/06)
A novel series of pyridones were discovered as potent EP3 antagonists. Optimization guided by EP3 binding and functional assays as well as by eADME and PK profiling led to multiple compounds with good physical properties, excellent oral bioavailability, and a clean in vitro safety profile. Compound 13 was identified as a lead compound as evidenced by the reversal of sulprostone-induced suppression of glucose-stimulated insulin secretion in INS 1E β-cells in vitro and in a rat ivGTT model in vivo. A glutathione adduction liability was eliminated by replacing the naphthalene of structure 13 with the indazole ring of structure 43.
Compounds and their use in treatment on hepatitis B
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Paragraph 0129-0130; 0132; 0138-0139; 0141, (2020/07/15)
The invention provides compounds, a pharmaceutical composition containing the compounds and an application of the compounds. The compound is a compound shown in a formula (I) or a stereoisomer, a tautomer, nitric oxide, hydrate, solvate, metabolite, pharmaceutically acceptable salt or prodrug of the compound shown in the formula (I). The compound provided by the invention can interfere with the shell assembly process of hepatitis B virus, thereby inhibiting hepatitis B virus replication. Moreover, the compound has good absorption, relatively high biological activity and availability and low toxicity, particularly has relatively strong stability in vivo, is not easy to decompose and has long drug effect time, so that an effect of treating hepatitis B is achieved and the compound has a goodapplication prospect.
COMPOUNDS FOR USE IN THE TREATMENT OF FASCIOLIASIS
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Page/Page column 29, (2020/02/22)
The present invention relates to compounds of formula (1a), (1b), (1c), (1d) or (1e) and pharmaceutically acceptable salts or solvates thereof for use in the treatment or prevention of fascioliasis. Some of these compounds are novel per se and also have activity as inhibitors of Schistosoma growth. The invention also relates to pharmaceutical compositions comprising such novel compounds, salts or solvates and to the use of such novel compounds as medicaments, in particular in the treatment or prevention of schistosomiasis, also known as bilharzia.
PYRIDIN-2-ONE DERIVATIVES OF FORMULA (II) USEFUL AS EP3 RECEPTOR ANTAGONISTS
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Paragraph 0661; 0664; 0665, (2019/02/24)
The present invention is directed to pyridin-2-one derivatives, pharmaceutical compositions containing them and their use as antagonists of the EP3 receptor, for the treatment of for example, impaired oral glucose tolerance, elevated fasting glucose, Type II Diabetes Mellitus, Syndrome X (also known as Metabolic Syndrome) and related disorders and complications thereof.
PYRIDIN-2-ONE DERIVATIVES OF FORMULA (III) USEFUL AS EP3 RECEPTOR ANTAGONISTS
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Paragraph 0661-0662, (2019/02/24)
The present invention is directed to pyridin-2-one derivatives, pharmaceutical compositions containing them and their use as antagonists of the EP3 receptor, for the treatment of for example, impaired oral glucose tolerance, elevated fasting glucose, Type II Diabetes Mellitus, Syndrome X (also known as Metabolic Syndrome) and related disorders and complications thereof.
PYRIDIN-2-ONE DERIVATIVES OF FORMULA (I) USEFUL AS EP3 RECEPTOR ANTAGONISTS
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Paragraph 0661-0662, (2019/02/24)
The present invention is directed to pyridin-2-one derivatives, pharmaceutical compositions containing them and their use as antagonists of the EP3 receptor, for the treatment of for example, impaired oral glucose tolerance, elevated fasting glucose, Type II Diabetes Mellitus, Syndrome X (also known as Metabolic Syndrome) and related disorders and complications thereof.
Method for synthesizing 5-bromo-4-fluoro-1H-indazole
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, (2019/11/28)
The invention belongs to the field of organic synthesis, and discloses a method for synthesizing 5-bromo-4-fluoro-1H-indazole. The synthesis method comprises the steps: adopting 3-fluoro-2-methylaniline as a raw material, and performing three steps of rea
COMPOUNDS AND THEIR USE IN THE TREATMENT OF SCHISTOSOMIASIS
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Page/Page column 26, (2018/08/03)
The present invention relates to novel compounds and pharmaceutically acceptable salts or solvates thereof which have activity as inhibitors of Schistosoma growth. The invention also relates to pharmaceutical compositions comprising such compounds, salts or solvates and to the use of such compounds as medicaments, in particular in the treatment or prevention of schistosomiasis, also known as bilharzia.
3-(1H-PYRROLO[2,3-B]PYRIDIN-2-YL)-1H-INDAZOLES AND THERAPEUTIC USES THEREOF
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Paragraph 0629; 0631, (2017/02/28)
Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
3-(1H-PYRROLO[2,3-C]PYRIDIN-2-YL)-1H-INDAZOLES AND THERAPEUTIC USES THEREOF
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Paragraph 0629; 0631, (2017/03/08)
Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
