51716-62-2Relevant academic research and scientific papers
A synthetic approach to 5/5/6-polycyclic tetramate macrolactams of the discodermide type
Bodenschatz, Kevin,St?ckl, Julia,Winterer, Markus,Schobert, Rainer
, (2021/05/31)
A flexible synthetic route to the 16-membered tetramate-embedding macrocyclic scaffold present in various polycyclic tetramate macrolactams (PTMs) was developed which differs from the seminal synthesis of ikarugamycin by Boeckman Jr. in protecting groups and the order of connections. We also devised a short approach to various stereoisomers of the 5/5/6-tricarbocyclic motif found in discodermide and other PTMs, starting from the Weiss’ diketone.
Spirocyclic Nitroxide Biradicals: Synthesis and Evaluation as Dynamic Nuclear Polarizing Agents
Bode, Jeffrey W.,Copéret, Christophe,Gordon, Christopher P.,Jackl, Moritz K.
, (2020/12/01)
A method for the synthesis of rigid nitroxide biradicals with various spatial orientations between the radical centers is reported. Diketones were employed as substrates for tin amine protocol (SnAP) reagents to provide the parent spirocyclic diamines. Oxidation by peroxyacids provided the corresponding nitroxide biradicals. A set of four different biradicals with various interelectron distances and torsion angles between the radical planes was synthesized using this method. The exact geometries were determined by X-ray crystallography and the biradicals were investigated by EPR spectroscopy and evaluated for their dynamic nuclear polarization (DNP) performance. 1H-DNP enhancements in the range of 1.2–2.1 at 14.1 Tesla (600 MHz spectrometer) were achieved. This synthetic methodology opens a promising alternative to access nitroxide biradicals with various torsional angles and inter radical distances.
Bicyclic derivative-containing inhibitor, preparation method and applications thereof
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Paragraph 0260-0262; 0266-0268, (2020/04/17)
The invention relates to a bicyclic derivative-containing inhibitor, a preparation method and applications thereof, particularly to a compound represented by a general formula (I), and a preparation method thereof, a pharmaceutical composition containing the compound, and applications of the compound as an Acetyl-CoA Carboxylase (ACC) inhibitor in treatment of diseases or symptoms caused by fattyacid metabolic disorder.
POLYCYCLIC COMPOUND ACTING AS IDO INHIBITOR AND/OR IDO-HDAC DUAL INHIBITOR
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Paragraph 0100-0101, (2020/08/09)
The present invention provides polycyclic compounds as IDO inhibitors and/or dual inhibitors of IDO-HDAC. Specifically, the present invention provides compounds represented by the following formula (I), wherein each group is defined as described in the specification. The compounds have IDO inhibitory activity or IDO-HDAC dual inhibitory activity and can be used for preventing or treating diseases associated with IDO and/or IDO-HDAC activity or expression levels. At the same time, the compounds of the present invention can be combined with an antitumor antibody such as PD-1 and PD-L1, and such a combination can greatly increase the antitumor response rate of the antibody and broaden the types of tumors to be treated.
Octahydropentalene compound, and preparation method and medical application thereof
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Paragraph 0107-0112, (2019/12/25)
The invention relates to a novel octahydropentalene compound for regulating or inhibiting the activity of indoleamine 2,3-dioxygenase (IDO), and a preparation method and medicinal application of the octahydropentalene compound. Specifically, the invention relates to a compound as shown in a general formula (I) which is described in the specification and a pharmaceutically acceptable salt thereof,a pharmaceutical composition containing the compound or the pharmaceutically acceptable salt thereof, a method for treating and/or preventing related IDO-mediated diseases, especially tumors, by usingthe compound or the pharmaceutically acceptable salt thereof, and a preparation method for the compound or the pharmaceutically acceptable salt thereof. The invention also relates to the applicationof the compound or the pharmaceutically acceptable salt thereof or a pharmaceutical composition containing the compound or the pharmaceutically acceptable salt thereof in preparation of drugs for treating and/or preventing related IDO-mediated diseases, especially tumors. Each substituent of the general formula (I) is as defined in the specification.
HYDROXY CONTAINING FXR (NR1H4) MODULATING COMPOUNDS
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Page/Page column 90, (2016/07/05)
The present invention relates to compounds (1) which bind to the NR1 H4 receptor (FXR) and act as agonists of FXR. The invention further relates to the use of the compounds (1) for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds and to a process for the synthesis of said compounds.
IMIDAZOLE DERIVATIVES
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Page/Page column 52-53, (2013/02/27)
Described herein are compounds of formula (I), The compounds of formula I act as DGAT1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for hyperlipidemia, diabetes mellitus and obesity.
Synthesis and biological evaluation of bicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes
Cho, Tang Peng,Gang, Lin Zhi,Long, Yang Fang,Yang, Wang,Qian, Wang,Lei, Zhang,Jing, Luo Jing,Ying, Feng,Ke, Yan Pang,Ying, Leng,Jun, Feng
scheme or table, p. 3521 - 3525 (2010/08/20)
A series of novel bicyclo[3.3.0]octane derivatives have been synthesized and found to be dipeptidyl peptidase 4 (DPP-4) inhibitors. Compounds 10a and 10b demonstrate good efficacies in oral glucose tolerance tests.
Dicyclooctane Derivatives, Preparation Processes and Medical Uses Thereof
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Page/Page column 13, (2009/07/18)
The present invention relates to new dicyclooctane derivates represented by general formula (I), preparation processes and pharmaceutical compositions containing them, and to uses for treatment especially for dipeptidyl peptidase inhibitor (DPPIV), in which each substituent group of general formula (I) is as defined in specification.
DICYCLOOCTANE DERIVATES, PREPARATION PROCESSES AND MEDICAL USES THEREOF
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Page/Page column 18, (2009/01/24)
The present invention relates to new dicyclooctane derivates represented by general formula (I), preparation processes and pharmaceutical compositions containing them, and to uses for treatment especially for dipeptidyl peptidase inhibitor (DPPIV), in which each substituent group of general formula (I) is as defined in specification
