73505-48-3Relevant academic research and scientific papers
CYCLIC PENTAMER COMPOUNDS AS PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9) INHIBITORS FOR THE TREATMENT OF METABOLIC DISORDER
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Page/Page column 443-444, (2020/06/19)
The disclosure relates to inhibitors of PCSK9 useful in the treatment of cholesterol lipid metabolism, and other diseases in which PCSK9 plays a role, having the Formula (I):, or a pharmaceutically acceptable salt, hydrate, solvate, prodrug, stereoisomer, N-oxide, or tautomer thereof, wherein X1, R1, R2, R3, R4, R5, R6, R6', R7, R7', R8, R9, R9', R10, R11, R12, and n are described herein.
COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF ENHANCER OF ZESTE HOMOLOG 2 POLYPEPTIDE
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Paragraph 1151-1154, (2018/07/15)
The present disclosure relates to bifunctional compounds, which find utility as modulators of enhancer of zeste homolog 2 (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
Method for constructing dihydrobenzofuran skeleton compound by oxidative coupling of two C-H bonds
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Paragraph 0089; 0090; 0091, (2018/03/25)
The invention discloses a method for constructing a dihydrobenzofuran skeleton compound by oxidative coupling of two C-H bonds. According to the method, an intramolecular oxidative coupling reaction of carbon-hydrogen bonds is carried out on a carbon hydrogen bond C(sp)-H at the ortho-position of carboxyl on an aromatic ring in an alkoxy substituted benzoic acid derivative and a carbon-hydrogenbond C(sp) on an alkoxy group for constructing a carbon-carbon bond, and then the dihydrobenzofuran skeleton compound is obtained. The method provided by the invention has an important applicationvalue.
PHENYL AMINO PIPERIDINE mTORC INHIBITORS AND USES THEREOF
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Paragraph 0385-0386, (2018/05/24)
The present invention provides compounds, compositions thereof, and methods of using the same.
PYRAZOLO[1,5a]PYRIMIDINE DERIVATIVES AS IRAK4 MODULATORS
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Page/Page column 186, (2019/01/10)
Compounds of Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V), Formula (VI), Formula (VII), Formula (VIII), and methods of use as lnterleukin-1 Receptor Associated Kinase (IRAK4) inhibitors are described herein.
PHENYL mTORC INHIBITORS AND USES THEREOF
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Paragraph 00345, (2018/05/27)
The present invention provides compounds, compositions thereof, and methods of using the same.
Structural development studies of pyrazoloketone-derived acetyl-CoA carboxylase inhibitors
Okazaki, Shogo,Sakai, Taki,Ishikawa, Minoru,Hashimoto, Yuichi,Yamaguchi, Takao
, p. 595 - 607 (2019/05/21)
Acetyl-CoA carboxylase (ACC) plays a key role in fatty acid homeostasis in humans, and inhibitors of ACC are expected to inhibit fatty acid biosynthesis and to activate fatty acid β-oxidation. Therefore, they are considered to be candidates for treatment of metabolic syndrome and related diseases. In this context, an upstream kinase of ACC, adenosine monophosphate-activated protein kinase (AMPK), has also recently emerged as a potential therapeutic target, because it phosphorylates and inactivates ACC. Here, we designed a fused molecule consisting of a pyrazoloketone-type ACC inhibitor and a recently discovered AMPK activator, aiming to develop a novel combined ACC inhibitor/AMPK activator to regulate fatty acid levels. The designed compound was prepared through a convergent synthetic route. This compound and its methyl ester analogue showed potent ACC2-inhibitory activity with IC50 values of 8.8 and 1.3 μM, respectively. Exomethylene derivatives, obtained from an unexpected side reaction during deprotection, also exhibited ACC2-inhibitory activity.
METHOD FOR PREPARING PHENOLICS USING A CATALYST
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Paragraph 10; 11; 12, (2017/07/14)
The invention is directed to a method for preparing a phenolic compound comprising reacting a furanic compound with a dienophile in the presence of a catalyst comprising yttrium.
Synthesis, structure-activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics
Yang, Feipu,Jiang, Xiangrui,Li, Jianfeng,Wang, Yu,Liu, Yongjian,Bi, Minghao,Wu, Chunhui,Zhao, Qingjie,Chen, Weiming,Yin, Jingjing,Zhang, Jian,Xie, Yuanchao,Hu, Tianwen,Xu, Mingshuo,Guo, Shuang,Wang, Zhen,He, Yang,Shen, Jingshan
supporting information, p. 3141 - 3147 (2016/06/13)
In the present study, a series of benzamides, endowed with potent dopamine D2, serotonin 5-HT1A and 5-HT2A receptors properties, was synthesized and evaluated as potential antipsychotics. Among them, 3-(4-(4-(6-fluorobenzo[d]isoxazol-3-yl)-piperidin-1-yl)butoxy)-N-methylbenzamide (21) and its fluoro-substituted analogue (22) held the best pharmacological binding profiles. They not only presented potent activities for D2, 5-HT1A, and 5-HT2A receptors, but were also endowed with low activities for 5-HT2C, H1 receptors and hERG channels, suggesting a low propensity of inducing weight gain and QT prolongation. In animal models, compounds 21 and 22 reduced phencyclidine-induced hyperactivity with a high threshold for catalepsy induction. It thus provides potential candidates for further preclinical studies.
Asymmetric synthesis of (+)-17-: Epi -methoxy-kauran-3-one through tandem oxidative polycyclization-pinacol process
Maertens, Ga?tan,Desjardins, Samuel,Canesi, Sylvain
supporting information, p. 6744 - 6750 (2016/07/21)
A synthesis of (+)-17-epi-methoxy-kauran-3-one, an O-methylated isomer of the natural diterpene 17-hydroxy-kauran-3-one, has been achieved. The strategy is based on a diastereoselective oxidative polycyclization-pinacol tandem process consisting of transforming a functionalized phenol into a compact and complex tetracycle, which represents the main core of kaurane family members. The synthesis also includes an enantioselective Yamamoto's allylation, a diastereoselective Ru-catalyzed hydrocyanation, a ring-closing metathesis and a reductive isomerization process as key steps. The structure of our synthetic substrate was determined through comparison with an O-methylated derivative of the natural compound.
