1039948-89-4Relevant academic research and scientific papers
Star/linear polymer topology transformation facilitated by mechanical linking of polymer Chains
Aoki, Daisuke,Uchida, Satoshi,Takata, Toshikazu
, p. 6770 - 6774 (2015)
Topology transformation of a star polymer to a linear polymer is demonstrated for the first time. A three-armed star polymer possessing a mechanical linking of two polymer chains was synthesized by the living ring-opening polymerization of δ-valerolactone
Discovery of Orally Bioavailable Chromone Derivatives as Potent and Selective BRD4 Inhibitors: Scaffold Hopping, Optimization, and Pharmacological Evaluation
Liu, Zhiqing,Chen, Haiying,Wang, Pingyuan,Li, Yi,Wold, Eric A.,Leonard, Paul G.,Joseph, Sarah,Brasier, Allan R.,Tian, Bing,Tian, Bing,Zhou, Jia,Zhou, Jia,Zhou, Jia
, p. 5242 - 5256 (2020/07/10)
Bromodomain-containing protein 4 (BRD4) represents a promising drug target for anti-inflammatory therapeutics. Herein, we report the design, synthesis, and pharmacological evaluation of novel chromone derivatives via scaffold hopping to discover a new class of orally bioavailable BRD4-selective inhibitors. Two potent BRD4 bromodomain 1 (BD1)-selective inhibitors 44 (ZL0513) and 45 (ZL0516) have been discovered with high binding affinity (IC50 values of 67-84 nM) and good selectivity over other BRD family proteins and distant BD-containing proteins. Both compounds significantly inhibited the expression of Toll-like receptor-induced inflammatory genes in vitro and airway inflammation in murine models. The cocrystal structure of 45 in complex with human BRD4 BD1 at a high resolution of 2.0 ? has been solved, offering a solid structural basis for its binding validation and further structure-based optimization. These BRD4 BD1 inhibitors demonstrated impressive in vivo efficacy and overall promising pharmacokinetic properties, indicating their therapeutic potential for the treatment of inflammatory diseases.
Design, synthesis and biological evaluation of hypolipidemic compounds based on BRD4 inhibitor RVX-208
Yu, Ping,Liu, Wenjing,Ren, Jinghui,Wang, Yingying,Ning, Yao,Huang, Mingqi,Hu,Wei, Lili,Ji, Min,Cai, Jin
supporting information, p. 2168 - 2172 (2019/07/03)
Bromodomain-containing protein 4 (BRD4) is a new therapeutic target for the treatment of diseases including cardiovascular diseases, cancer, inflammation and central nervous system (CNS) disorders. In this study, we introduced the pharmacophore of fibrates to a BRD4 inhibitor, RVX-208, to design dual-active hypolipidemic compounds, and found that some of new analogues showed favorable hypolipidemic activities. Synthetic accessibility towards this class of compounds optimized RVX-208 as well as would supply more thoughts on hypolipidemic drugs.
ROTAXANE AND POLYURETHANE USING THE SAME
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Paragraph 0088; 0090, (2020/02/10)
PROBLEM TO BE SOLVED: To provide a novel rotaxane and a polyurethane using the same. SOLUTION: The rotaxane of the present invention has a crown ether and a chain molecule penetrating the ring structure of the crown ether, and is characterized to have a s
NITRIC OXIDE-RELEASING PRODRUG MOLECULE
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Paragraph 0057; 0059, (2018/08/01)
Provided are a type of compounds that can be used for treating cardiovascular diseases and compositions containing the compounds. The compounds and the compositions can improve lipid metabolism disorders by increasing high-density lipoprotein cholesterol in blood; in addition, the compounds and the compositions can also release nitric oxide, and reduce the onset risk of cardiovascular diseases by means of relaxing blood vessels, lowering blood pressure, inhibiting platelet adhesion and aggregation and maintaining vascular tension, and thus play an important role in preventing and treating the occurrence and development of cardiovascular diseases.
Preparation method for Apabetalone
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Paragraph 0057; 0058, (2018/07/30)
The invention relates to a preparation method for Apabetalone, and particularly discloses a synthesis method for Apabetalone. The preparation method comprises the following steps: (1) a first intermediate, i.e., 2-bromo-4,6-dimethoxy benzamide, is prepared; (2) a second intermediate, i.e., 4-{2-[(t-butyldimethylsilicon)oxy]ethyoxyl}-3,5-dimethyl benzaldehyde, is prepared; (3) the first intermediate and the second intermediate are sealed under the conditions of cuprous bromide, cesium carbonate, L-proline and ammonia hydroxide to react, so that Apabetalone is obtained. The preparation method disclosed by the invention is simple, and yield is high.
Used for the prevention and treatment of cardiovascular diseases
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Paragraph 0406-0410, (2016/10/08)
The invention relates to compounds that can be used for adjusting the expression of apolipoprotein A-I (ApoA-I) and usage of the compounds in treating and preventing cardiovascular diseases and related diseases, including the disorder related to cholesterol or lipids such as atherosclerosis.
TREATMENT OF DISEASES BY EPIGENETIC REGULATION
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Paragraph 0477, (2013/11/05)
The present disclosure provides non-naturally occurring polyphenol compounds that inhibit the bromodomain and extra terminal domain (BET) proteins. The disclosed compositions and methods can be used for treatment and prevention of cancer, including NUT midline carcinoma, Burkitt's Lymphoma, Acute Myelogenous Leukemia, and Multiple Myeloma; autoimmune or inflammatory diseases or conditions, and sepsis.
METHODS OF PREPARING QUINAZOLINONE DERIVATIVES
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Page/Page column 15-16, (2010/01/30)
The present disclosure relates to methods for preparing compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-l), and in the treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.
COMPOUNDS FOR THE PREVENTION AND TREATMENT OF CARDIOVASCULAR DISEASES
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Page/Page column 33, (2008/12/07)
The present disclosure relates to compounds, which are useful for regulating the expression of apolipoprotein A-I (ApoA-I), and their use for treatment and prevention of cardiovascular disease and related disease states, including cholesterol- or lipid-related disorders, such as, for example, atherosclerosis.
