335349-57-0Relevant articles and documents
Compound with AMPK agonistic activity and preparation and application of prodrug thereof
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Paragraph 0514; 0520-0521, (2021/10/27)
The invention relates to a compound with AMPK agonistic activity and a prodrug thereof, and as well as a preparation method and medical application of a prodrug thereof. The compound has the structure shown in the formula (I), and the prodrug of the compound has the structure shown in the formula (II), wherein each group and the substituent are as defined in the specification. The invention discloses a preparation method of the compound and application of the compound in prevention and treatment AMPK related diseases, and the AMPK related diseases include, but are not limited to, energy metabolism abnormality related diseases. Neurodegenerative diseases and inflammation-related diseases and the like.
INHIBITORS OF FIBROBLAST GROWTH FACTOR RECEPTOR KINASES
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Paragraph 00388-00390, (2021/12/28)
Provided herein are heteroaryl inhibitors of fibroblast growth factor receptor kinases, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.
Discovery of MK-8722: A Systemic, Direct Pan-Activator of AMP-Activated Protein Kinase
Feng, Danqing,Biftu, Tesfaye,Romero, F. Anthony,Kekec, Ahmet,Dropinski, James,Kassick, Andrew,Xu, Shiyao,Kurtz, Marc M.,Gollapudi, Anantha,Shao, Qing,Yang, Xiaodong,Lu, Ku,Zhou, Gaochao,Kemp, Daniel,Myers, Robert W.,Guan, Hong-Ping,Trujillo, Maria E.,Li, Cai,Weber, Ann,Sebhat, Iyassu K.
supporting information, p. 39 - 44 (2018/05/04)
5′-Adenosine monophosphate-activated protein kinase (AMPK) is a key regulator of mammalian energy homeostasis and has been implicated in mediating many of the beneficial effects of exercise and weight loss including lipid and glucose trafficking. As such,
Method for synthesizing 1,4-diiodo-2-methoxy-5-nitrobenzene
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Paragraph 0026-0028, (2017/08/27)
The invention relates to the field of organic synthesis and discloses a method for synthesizing 1,4-diiodo-2-methoxy-5-nitrobenzene. The method includes the steps that firstly, 5-chloro-2-nitroaniline reacts with N-iodosuccinimide to generate 2-chloro-4-c
SUBSTITUTED HETEROARYLBENZIMIDAZOLE COMPOUNDS
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Page/Page column 183, (2018/01/17)
The present invention covers substituted heteroarylbenzimidazole compounds of general formula (I) : in which R1, R2, R3, R4, R5, R6a and R6b are as defined herein, methods of pre
Hit-to-Lead Optimization and Discovery of 5-((5-([1,1′-Biphenyl]-4-yl)-6-chloro-1H-benzo[d]imidazol-2-yl)oxy)-2-methylbenzoic Acid (MK-3903): A Novel Class of Benzimidazole-Based Activators of AMP-Activated Protein Kinase
Lan, Ping,Romero, F. Anthony,Wodka, Dariusz,Kassick, Andrew J.,Dang, Qun,Gibson, Tony,Cashion, Daniel,Zhou, Gaochao,Chen, Yuli,Zhang, Xiaoping,Zhang, Aihua,Li, Ying,Trujillo, Maria E.,Shao, Qing,Wu, Margaret,Xu, Shiyao,He, Huaibing,Mackenna, Deidre,Staunton, Jocelyn,Chapman, Kevin T.,Weber, Ann,Sebhat, Iyassu K.,Makara, Gergely M.
, p. 9040 - 9052 (2017/11/14)
AMP-activated protein kinase (AMPK) plays an essential role as a cellular energy sensor and master regulator of metabolism in eukaryotes. Dysregulated lipid and carbohydrate metabolism resulting from insulin resistance leads to hyperglycemia, the hallmark of type 2 diabetes mellitus (T2DM). While pharmacological activation of AMPK is anticipated to improve these parameters, the discovery of selective, direct activators has proven challenging. We now describe a hit-to-lead effort resulting in the discovery of a potent and selective class of benzimidazole-based direct AMPK activators, exemplified by 5-((5-([1,1′-biphenyl]-4-yl)-6-chloro-1H-benzo[d]imidazol-2-yl)oxy)-2-methylbenzoic acid, 42 (MK-3903). Compound 42 exhibited robust target engagement in mouse liver following oral dosing, leading to improved lipid metabolism and insulin sensitization in mice.
Synthesis and biological evaluation of novel 2,3-dihydro-1H-1,5- benzodiazepin-2-ones; Potential imaging agents of the metabotropic glutamate 2 receptor
Gilfillan, Lynne,Blair, Adele,Morris, Brian J.,Pratt, Judith A.,Schweiger, Lutz,Pimlott, Sally,Sutherland, Andrew
supporting information, p. 1118 - 1123 (2013/07/26)
A focused library of novel 2,3-dihydro-1H-1,5-benzodiazepin-2-ones containing sites for 11C-, 18F- and 123I- labelling have been prepared and evaluated against membrane expressing human recombinant metabotropic glutamate 2 receptor (mGluR2). The compounds were found to be non-competitive antagonists with nanomolar affinity. HPLC evaluation of the physiochemical properties of these compounds identified two candidates for PET and SPECT imaging of mGluR2.
PARASITICIDAL COMPOSITIONS COMPRISING BENZIMIDAZOLE DERIVATIVES, METHODS AND USES THEREOF
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Paragraph 0148; 0150; 0151, (2013/11/05)
The invention relates to oral, topical or injectable compositions for combating liver fluke parasites in mammals, comprising at least one benzimidazole derivative active agent. The invention also provides for an improved method for eradicating and controlling liver fluke parasite infections and infestations in a mammal comprising administering the compositions of the invention to the mammal in need thereof.
PHOSPHOGLYCERATE KINASE INHIBITORS
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Page/Page column 60, (2012/04/23)
Disclosed are compounds of formula (I) or pharmaceutical acceptable salts thereof, wherein R1, R2, R3 and R4 are as defined in the description. Disclosed are also the methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as phosphoglycerate kinase.
NOVEL CYCLIC BENZIMIDAZOLE DERIVATIVES USEFUL ANTI-DIABETIC AGENTS
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Page/Page column 66, (2011/09/30)
Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK- activated protein kinase. The compounds of the present invention are useful in