- A synthetic approach to 5/5/6-polycyclic tetramate macrolactams of the discodermide type
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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.
- Bodenschatz, Kevin,St?ckl, Julia,Winterer, Markus,Schobert, Rainer
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- POLYCYCLIC COMPOUND ACTING AS IDO INHIBITOR AND/OR IDO-HDAC DUAL INHIBITOR
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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.
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Paragraph 0100-0101
(2020/08/09)
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- Spirocyclic Nitroxide Biradicals: Synthesis and Evaluation as Dynamic Nuclear Polarizing Agents
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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.
- Bode, Jeffrey W.,Copéret, Christophe,Gordon, Christopher P.,Jackl, Moritz K.
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- Bicyclic derivative-containing inhibitor, preparation method and applications thereof
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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.
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Paragraph 0260-0262; 0266-0268
(2020/04/17)
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- Octahydropentalene compound, and preparation method and medical application thereof
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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.
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Paragraph 0107-0112
(2019/12/25)
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- HYDROXY CONTAINING FXR (NR1H4) MODULATING COMPOUNDS
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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.
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Page/Page column 90
(2016/07/05)
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- IMIDAZOLE DERIVATIVES
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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.
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Page/Page column 52-53
(2013/02/27)
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- Synthesis and biological evaluation of bicyclo[3.3.0] octane derivatives as dipeptidyl peptidase 4 inhibitors for the treatment of type 2 diabetes
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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.
- 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
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scheme or table
p. 3521 - 3525
(2010/08/20)
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- Dicyclooctane Derivatives, Preparation Processes and Medical Uses Thereof
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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.
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Page/Page column 13
(2009/07/18)
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- DICYCLOOCTANE DERIVATES, PREPARATION PROCESSES AND MEDICAL USES THEREOF
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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
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Page/Page column 18
(2009/01/24)
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- Optically active carbacyclin intermediates and processes for the preparation thereof
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New intermediate, an optically active (1S,5R)-7,7-alkylenedioxy-2-alkoxycarbonylbicyclo[3.3.0]octan-3-one which is useful for the synthesis of an optically active carbacyclin. This intermediate is prepared, as a non-reduced compound, from a racemic compound, (1SR,5RS)-7,7-alkylenedioxy-2-alkoxycarbonyl-cis-bicyclo[3.3.0]octane-3-one, by treatment of the racemic compound with a microorganism. The microorganism has an ability of specifically reducing the keto group of the (1R,5S) epimer of the racemic compound.
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- Different Enzymatic Reactions of an Enantiomeric Pair: Simultaneous Dual Kinetic Resolution of a Keto Ester by Bakers' Yeast
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An example of different enzymatic reactions of an anantiomeric pair involving a simultaneous dual kinetic resolution by two different enzymes in bakers' yeast on a racemic synthetic substrate is described.The 1R,5S enantiomer of methyl (+/-)-3-oxo-7,7-(et
- Brooks, Dee W.,Wilson, Michael,Webb, Michael
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p. 2244 - 2248
(2007/10/02)
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- SUR UNE VOIE ALTERNATIVE DE SYNTHESE DE LA LOGANINE
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An original synthesis of a precursor of loganin is described starting from the bicyclooctane-3,7-dione using Shapiro's reaction.The structure of the obtained derivatives are established on the basis of 1H N.M.R., I.R., and mass spectral data.
- Caille, Jean Claude,Bellamy, Francois,Guilard, Roger
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p. 2345 - 2346
(2007/10/02)
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- EXPEDIENT PREPARATION OF A HIGHLY FUNCTIONALIZED DIQUINANE BUILDING BLOCK
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A high yield four-step synthesis of the useful α-enone ketal 7 is described.
- Paquette, Leo A.,Lau, Clifford J.
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p. 1081 - 1086
(2007/10/02)
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- SYNTHETIC STUDIES ON IRIDOID TERPENES VIA REGIOSELECTIVE SULFENYLATION OF β-KETOESTERS AND OXIDATIVE CLEAVAGE OF β-THIOALCOHOLS - A NOVEL SYNTHETIC ROUTE TO (+/-)-LOGANIN -
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Regioselective sulfenylation of ethyl 2-oxocyclopentanecarboxylate (3) and methyl 7,7-ethylenedioxy-3-oxobicyclooctane-2-carboxylate (12), followed by NaBH4 reduction and subsequent oxidative ring cleavage with lead(IV) acetate gave ethyl 2-acetoxy
- Hiroi, Kunio,Miura, Hideyuki,Kotsuji, Kumiko,Sato, Shuko
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p. 559 - 562
(2007/10/02)
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