84184-51-0Relevant academic research and scientific papers
ARYL CYCLOPROPYL-AMINO-ISOQUINOLINYL AMIDE COMPOUNDS
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Page/Page column 103, (2018/10/25)
Provided herein are arylcyclopropyl amino-isoquinoline amide compounds. In particular, the disclosure provides compounds that affect the function of kinases in a cell and that are useful as therapeutic agents or with therapeutic agents. The compounds of t
Vitamin D3 analogues that contain modified A- and seco-B-rings as hedgehog pathway inhibitors
Deberardinis, Albert M.,Raccuia, Daniel S.,Thompson, Evrett N.,Maschinot, Chad A.,Hadden, M. Kyle
, p. 156 - 171 (2015/02/19)
The hedgehog (Hh) signaling pathway is a developmental signaling pathway that has been implicated as a target for anti-cancer drug development in a variety of human malignancies. Several natural and synthetic vitamin D-based seco-steroids have been identified as potent inhibitors of Hh signaling with chemotherapeutic potential. These include the previously characterized analogue 4, which contains the northern CD-ring/side chain region of vitamin D3 (VD3) linked to an aromatic A-ring mimic through an ester bond. To further explore structure-activity relationships for this class of VD3-based Hh pathway inhibitors, we have designed, synthesized and evaluated several series of compounds that modify the length, composition, and stereochemical orientation of the ester linker. These studies have identified compounds 54 and 55, which contain an amine linker and an aromatic A-ring incorporating a para-phenol, as new lead compounds with enhanced potency against the Hh pathway (IC50 values Combining double low line 0.40 and 0.32 μM, respectively).
Stellatolides, a new cyclodepsipeptide family from the sponge ecionemia acervus: Isolation, solid-phase total synthesis, and full structural assignment of stellatolide a
Martin, Maria Jesus,Rodriguez-Acebes, Raquel,Garcia-Ramos, Yésica,Martinez, Valentin,Murcia, Carmen,Digon, Isabel,Marco, Isabel,Pelay-Gimeno, Marta,Fernández, Rogelio,Reyes, Fernando,Francesch, Andrés M.,Munt, Simon,Tulla-Puche, Judit,Albericio, Fernando,Cuevas, Carmen
supporting information, p. 6754 - 6762 (2014/05/20)
The marine environment is a rich source of metabolites with potential therapeutic properties and applications for humans. Here we describe the first isolation, solid-phase total synthesis, and full structural assignment of a new class of cyclodepsipeptides from the Madagascan sponge Ecionemia acervus that shows in vitro cytotoxic activities at submicromolar concentrations. Seven structures belonging to a new family of compounds, given the general name stellatolides, were characterized. The sequence and stereochemistry of all the amino acids in these molecules were established by a combination of spectroscopic analysis, chemical degradation, and derivatization studies. Furthermore, the complete structure of stellatolide A was confirmed by an efficient solid-phase method for the first total synthesis and the full structural assignment of this molecule, including the asymmetric synthesis of the unique B-hydroxy acid moiety (Z)-3-hydroxy-6,8-dimethylnon-4-enoic acid.
METHODS OF TREATMENT USING ARYLCYCLOPROPYLAMINE COMPOUNDS
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Paragraph 0303-0304; 0309, (2014/12/09)
Described herein are methods of treating breast cancer using arylcyclopropylamine compounds.
METHOD FOR PRODUCING A CROSS-COUPLING PRODUCT OF A BENZENOID DIAZONIUM SALT
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Paragraph 0040; 0041; 0042; 0043; 0044, (2013/03/26)
The invention relates to a method for producing a cross-coupling product of a benzenoid dizonium salt according to the general formula (I), wherein the groups R1, R2, R3, R4, and R5 represent hydrogen, halogen, an alkyl, alkenyl, aryl, alkoxy, aryloxy, nitro, cyano, hydroxy, acetyl, and/or diazo groups independently of each, and X represents BF4, Cl, F, SO3CH3, CO2CH3, PF6, ClO2CH3, or CIO4, comprising the following steps: (a) providing a benzenoid amide, which with the exception of the diazo function has the same substituents R1, R2, R3, R4, and R5 as the benzenoid diazonium salt of the general formula (I), and hydrolytically cleaving the amide to form an amine or providing a corresponding amine, (b) diazotizing the amine thus obtained or provided with a nitrite, and (c) subsequently reacting the benzenoid diazonium salt with a coupling partner in the presence of a catalyst to form a cross-coupling product, wherein the coupling parter is represented by the general formula (II), R6, R7, and R8 are the same or different and represent hydrogen, carboxyalkyl groups, carboxyaryl groups, alkyl groups, aryl groups, alkoxy groups, aryloxy groups, wherein the groups can each contain Si, N, S, O, and or halogen atoms, or R6 and R7 with the double bound form an aromatic ring, which can be provided with R8 and one to four further substituents, independently of each other, selected from the group comprising a straight-chain or branched (C1-C6) alkyl group, a (C3-C7) cycloalkyl group, a straight-chain or branched (C1-C6) alkenyl group, a straight-chain or branched (C1-C6) alkyoxy group, halogen, the hydroxy group, an amino, di(C1-C6) alkylamino, nitro, acetyl, cyan, benzyl, 4-methoxybenzyl, 4-nitrobenzyl, phenyl, and 4-methoxyphenyl group and represents Y=H, —B(OR)2, —SnR3, —ZnR, —SiR3, or Mg (halogen), and wherein at least the steps (b) and (c) are performed without intermediate isolation of an intermediate product. According to said method, cross-couplings can be performed more simply and with improved yield without the hydroxyl group in aromatic reactants containing hydroxyl groups having to be provided with a protective group.
METHODS OF TREATMENT USING ARYLCYCLOPROPYLAMINE COMPOUNDS
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Paragraph 0221; 0222; 0227, (2013/07/19)
Described herein are methods of treating Parkinson's disease using arylcyclopropylamine compounds.
NOVEL FLAVANONE DERIVATIVE
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, (2012/06/18)
Provided is a novel antimicrobial agent. More specifically, provided is a novel antimicrobial agent capable of effectively acting on various resistant bacteria such as VSSA, MRSA, VISA, VRE, and VRSA. A novel flavanone derivative having a six-membered monosaccharide derivative, specifically, a glucose derivative or a galactose derivative is capable of effectively acting on the bacteria. More specifically, a compound represented by the general formula (I) is capable of effectively acting on the bacteria. (In the formula: X represents a six-membered monosaccharide derivative; and Y is substituted by a hydroxyl group.)
Total synthesis of (±)-decinine via an oxidative biaryl coupling with defined axial chirality
Shan, Zhen-Hua,Liu, Ji,Xu, Ling-Min,Tang, Ye-Feng,Chen, Jia-Hua,Yang, Zhen
supporting information; experimental part, p. 3712 - 3715 (2012/09/21)
The total synthesis of (±)-decinine has been achieved. The key steps in the synthesis involved the formation of lasubine II via a gold catalyzed annulation of 1-(but-3-yn-1-yl)piperidine and the formation of the 12-membered ring of decinine (1) with complementary atropselectivity via a VOF 3-mediated oxidative biaryl coupling reaction.
ALKANOIC ACID DERIVATIVES AND THEIR THERAPEUTIC USE AS HDAC INHIBITORS
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Page/Page column 103-104, (2010/08/05)
The invention related to alkanoic acid derivatives of Formula (IIa) and (IIb). These compounds of the invention were found to have activity as HDAC inhibitors.
Mizoroki-heck reactions with 4-phenoldiazonium salts
Schmidt, Bernd,Hoelter, Frank,Berger, Rene,Jessel, Soenke
supporting information; experimental part, p. 2463 - 2473 (2010/12/25)
Significantly better yields were achieved in Mizoroki-Heck reactions using 4-phenoldiazonium salts instead of their O-alkylated analogues under otherwise identical conditions. We found that a one-flask deacetylation-diazotation- precipitation sequence starting from paracetamol or acetanilides derived thereof provides a convenient access to the required diazonium tetrafluoroborates. The utility of these arylating agents in palladium-catalyzed C-C bond forming reactions was demonstrated for a one-flask-synthesis of the heterocyclic core of the drug aripiprazole. Notably, the diazonium salt formation from an acetanilide could be combined with two Pd-catalyzed steps in a one-flask sequence, without any exchange of solvents or isolation of intermediates.
