98021-79-5Relevant academic research and scientific papers
6-HETEROARYLOXY BENZIMIDAZOLES AND AZABENZIMIDAZOLES AS JAK2 INHIBITORS
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Paragraph 0434; 0437, (2021/11/13)
The present disclosure provides 6-heteroaryloxy benzimidazole and azabenzimidazole compounds and compositions thereof useful for inhibiting JAK2.
Enantioselective Construction of Sulfur-Containing Tetrasubstituted Stereocenters via Asymmetric Functionalizations of α-Sulfanyl Cyclic Ketones
Ye, Xueqian,Pan, Yongkai,Chen, Yunrong,Yang, Xiaoyu
supporting information, p. 3374 - 3379 (2020/07/16)
Asymmetric functionalizations of α-sulfanyl cyclic ketones were realized via chiral phosphoric acid catalyzed enantioselective addition reactions with aldimines, azodicarboxylates and allenamides. A series of chiral organosulfur compounds possessing sulfur-containing tetrasubstituted stereocenters were accessed via these methods, with excellent regioselectivities and high stereoselectivities. (Figure presented.).
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.
Cyclic Urea Derivatives As Androgen Receptor Antagonists
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Paragraph 0432; 0433, (2014/11/13)
The present invention is directed to compounds of formula (I) wherein R1, R2, R3, and A are defined herein. The present invention also provides for pharmaceutical compositions comprising a compound of formula (I) as well as to the use of such compounds as androgen receptor antagonists for the treatment of diseases and conditions mediated by the androgen receptor, such as prostate cancer.
CYCLIC UREA DERIVATIVES AS ANDROGEN RECEPTOR ANTAGONISTS
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Page/Page column 73, (2013/06/27)
The present invention is directed to compounds of formula (I) wherein R1, R2, R3, and A are defined herein. The present invention also provides for pharmaceutical compositions comprising a compound of formula (I) as well as to the use of such compounds as androgen receptor antagonists for the treatment of diseases and conditions mediated by the androgen receptor, such as prostate cancer.
COMPOUNDS FOR THE REDUCTION OF β-AMYLOID PRODUCTION
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Page/Page column 74, (2012/08/08)
The present disclosure provides a series of compounds of the formula (I), which modulate β-amyloid peptide (β-ΑΡ) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-ΑΡ) production.
Synthesis of quinoxaline analogues
Chang, Meng-Yang,Lee, Tein-Wei,Hsu, Ru-Ting,Yen, Tzu-Lin
experimental part, p. 3143 - 3151 (2011/10/30)
Substituted tricyclic or tetracyclic quinoxalines, tricyclic pyridoquinoxalines and bis-quinoxalines were synthesized in high yields starting from cyclic ketones by the -bromination of cyclic ketones with N-bromosuccinimide (NBS) followed by condensation of the resulting -bromo ketones with 1,2-diaminobenzene, 3,4-diaminopyridine, or 3,3-diaminobenzidine. Georg Thieme Verlag Stuttgart New York.
COMPOUNDS FOR THE REDUCTION OF β-AMYLOID PRODUCTION
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Page/Page column 89-90, (2011/02/24)
The present disclosure provides a series of compounds of the formula (I) which modulate β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by β-amyloid peptide (β-AP) production.
OXOPIPERIDINYL AND PYRANYL SULFONAMIDES AS AMPA POTENTIATORS
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Page/Page column 50-51, (2010/04/27)
The invention is directed to a class of compounds, including the pharmaceutically acceptable salts of the compounds, having the structure of Formula (I) : as defined in the specification. The invention is also directed to compositions containing the compo
CYCLOALKYLIDENE AND HETEROCYCLOALKYLIDENE INHIBITOR COMPOUNDS
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Page/Page column 93-94, (2010/02/17)
The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
