78946-25-5Relevant academic research and scientific papers
Discovery of a tricyclic farnesoid X receptor agonist HEC96719, a clinical candidate for treatment of non-alcoholic steatohepatitis
Cao, Shengtian,Yang, Xinye,Zhang, Zheng,Wu, Junwen,Chi, Bo,Chen, Hong,Yu, Jianghong,Feng, Shanshan,Xu, Yulin,Li, Jing,Zhang, Yingjun,Wang, Xiaojun,Wang, Yan
supporting information, (2022/01/24)
Non-alcoholic fatty liver disease (NAFLD) is becoming the most predominant burden of chronic liver disease worldwide. Non-alcoholic steatohepatitis (NASH), the progressive form of NAFLD, can develop into cirrhosis and hepatocellular cancer. Unfortunately, current options for therapeutic treatment of NASH are very limited. Among multiple pathways in NASH, farnesoid X receptor (FXR), a nuclear bile acid receptor, is well-recognized as an important effective target. Here we report the synthesis and characterization of compound HEC96719 a novel tricyclic FXR agonist based on a prior high-affinity nonsteroidal molecule GW4064. HEC96719 exhibits excellent potency superior to GW4064 and obeticholic acid in in vitro and in vivo assays of FXR activation. It also shows higher FXR selectivity and more favorable tissue distribution dominantly in liver and intestine. Preclinical data on pharmacokinetic properties, efficacy, and safety profiles overall indicate that HEC96719 is a promising drug candidate for NASH treatment.
Cross-coupling strategy for the synthesis of diazocines
Eleya, Nadi,Li, Shuo,Staubitz, Anne
, p. 1624 - 1627 (2020/03/13)
Ethylene bridged azobenzenes are novel, promising molecular switches that are thermodynamically more stable in the (Z) than in the (E) configuration, contrary to the linear azobenzene. However, their previous synthetic routes were often not general, and yields were poorly reproducible, and sometimes very low. Here we present a new synthetic strategy that is both versatile and reliable. Starting from widely available 2-bromobenzyl bromides, the designated molecules can be obtained in three simple steps.
GLUCOSE-SENSITIVE ALBUMIN-BINDING DERIVATIVES
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, (2019/05/30)
This invention relates to glucose-sensitive albumin-binding diboron conjugates. More particularly the invention provides novel diboron compounds, and in particular diboronate or diboroxole compounds, useful as intermediate compounds for the synthesis of diboron conjugates. The diboron compounds are characterized by formula (I), which is: R1-X-R2, and wherein "X" is a mono- to multiatomic linker and where R1 and R2, which may be identical or different, each represents a group of Formula (lla) or (IIb) Also described are diboron conjugates represented by the general Formula (I'), which is: R1'-X'-R2', in which either the moeities R1' or R2' or X' carry a drug that is covalently attached to the diboron compound.
Annulated bacteriochlorins for near-infrared photophysical studies
Fujita, Hikaru,Jing, Haoyu,Krayer, Michael,Allu, Srinivasarao,Veeraraghavaiah, Gorre,Wu, Zhiyuan,Jiang, Jianbing,Diers, James R.,Magdaong, Nikki Cecil M.,Mandal, Amit K.,Roy, Arpita,Niedzwiedzki, Dariusz M.,Kirmaier, Christine,Bocian, David F.,Holten, Dewey,Lindsey, Jonathan S.
supporting information, p. 7209 - 7232 (2019/05/24)
Molecules with strong absorption in the near-infrared (NIR) spectral region are of interest for a variety of applications in the photosciences. Nature's NIR absorbers are bacteriochlorophylls, which contain a tetrahydroporphyrin chromophore accentuated by
PHTHALAZINE DERIVATIVES, AND PREPARATION METHOD, PHARMACEUTICAL COMPOSITION AND USE THEREOF
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, (2018/11/21)
The present invention provides a compound of formula I, a cis-trans isomer, an enantiomer, a diastereoisomer, a racemate, a solvate, a hydrate, or a pharmaceutical acceptable salt and ester thereof, a preparation method for preparing the same, a pharmaceutical composition comprising the same and a use of the compound as an α5-GABAA receptor regulator, wherein T, Z, A and Y are as defined in the description.
A Four-Step Synthesis of (±)-γ-Lycorane via Pd0-Catalyzed Double C(sp2)-H/C(sp3)-H Arylation
Rocaboy, Ronan,Dailler, David,Baudoin, Olivier
supporting information, p. 772 - 775 (2018/02/09)
An expedient synthesis of lycorine alkaloids is reported using a palladium(0)-catalyzed double C-X/C-H arylation as the key step. The selectivity of this reaction was controlled through the judicious choice of the two halogen atoms, and its generality was
HETEROCYCLIC COMPOUNDS AS RSV INHIBITORS
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Page/Page column 150-151, (2017/08/07)
The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, esters, or prodrugs thereof: Formula (I) which inhibit Respiratory Syncytial Virus (RSV). The present invention further relates to pharmaceutical compositions
3-PHOSPHOGLYCERATE DEHYDROGENASE INHIBITORS AND USES THEREOF
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Paragraph 00538-00540, (2017/10/06)
The present invention provides compounds, compositions thereof, and methods of using the same.
3-ALKYL-4-AMIDO-BICYCLIC [4,5,0] HYDROXAMIC ACIDS AS HDAC INHIBITORS
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Paragraph 0591-0592, (2016/08/29)
The present disclosure relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with an HDAC, e.g., HDAC6, having a Formula I: where R, L, X1, X2, X3, X4, Y1, Y2, Y3, and Y4 are described herein.
PIPERIDINE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS
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Paragraph 0269; 0270; 0271, (2015/12/12)
Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
