263012-81-3Relevant articles and documents
PCSK9 INHIBITORS AND METHODS OF USE THEREOF
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Page/Page column 192-193, (2020/07/31)
The invention relates to a novel inhibitor pharmacophore of PCSK9 and heteroaryl compounds that bind the PCSK9 protein.
PCSK9 INHIBITORS AND METHODS OF USE THEREOF
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Page/Page column 187-188, (2020/07/31)
The invention relates to novel heteroaryl compounds and pharmaceutical preparations thereof. The invention further relates to methods of treating or preventing cardiovascular diseases, and methods treating sepsis or septic shock, using the novel heterocyclic compounds disclosed herein.
Self-assembly of heteroleptic dinuclear metallosupramolecular kites from multivalent ligands via social self-sorting
Benkh?user, Christian,Lützen, Arne
, p. 693 - 700 (2015/06/08)
A Tr?ger's base-derived racemic bis(1,10-phenanthroline) ligand (rac)-1 and a bis(2,2′-bipyridine) ligand with a central 1,3-diethynylbenzene unit 2 were synthesized. Each of these ligands acts as a multivalent entity for the binding of two copper(I) ions. Upon coordination to the metal ions these two ligands undergo selective self-assembly into heteroleptic dinuclear metallosupramolecular kites in a high-fidelity social self-sorting manner as evidenced by NMR spectroscopy and mass spectrometry.
Synthesis and Structural Characterization of Ethynylene-Bridged Bisazines Featuring Various α-Substitution
Hübscher, J?rg,Seichter, Wilhelm,Gruber, Thomas,Kortus, Jens,Weber, Edwin
, p. 1062 - 1074 (2015/08/06)
A series of bispyridines and bispyrimidines 1a, 1b, 1c, 1d, 1e showing the heterocycles attached to both ends of an ethynylene unit and being α-substituted with chloro, tert-butylthio, and methoxy groups have been synthesized via cross-coupling technique and their crystal structures studied by X-ray diffraction analysis. Supramolecular interactions of C-H···N and π···π stacking type were found to largely dominate the structures according to the compound species. A trial was given to deduce the markedly differing temperatures of melting among the compounds from special features of the crystal structures.
Modular, Concise, and Efficient Synthesis of Highly Functionalized 5-Fluoropyridazines by a [2 + 1]/[3 + 2]-Cycloaddition Sequence
Tran, Ga?l,Gomez Pardo, Domingo,Tsuchiya, Tomoki,Hillebrand, Stefan,Vors, Jean-Pierre,Cossy, Janine
supporting information, p. 3414 - 3417 (2015/07/28)
An easy access to 5-fluoropyridazines by a [2 + 1]/[3 + 2]-cycloaddition sequence between terminal alkynes, a difluorocarbene, and a diazo compound is reported. This approach does not necessitate the isolation of any intermediates, and a wide range of novel 5-fluoropyridazines was synthesized from readily available starting materials. Additionally, these compounds were used as a platform to access novel and highly diversified pyridazines.
Design and synthesis of a new class of membrane-permeable triazaborolopyridinium fluorescent probes
Hapuarachchige, Sudath,Montano, Gilbert,Ramesh, Chinnasamy,Rodriguez, Delany,Henson, Lauren H.,Williams, Casey C.,Kadavakkollu, Samuel,Johnson, Dennis L.,Shuster, Charles B.,Arterburn, Jeffrey B.
supporting information; experimental part, p. 6780 - 6790 (2011/06/22)
A new class of fluorescent triazaborolopyridinium compounds was synthesized from hydrazones of 2-hydrazinylpyridine (HPY) and evaluated as potential dyes for live-cell imaging applications. The HPY dyes are small, their absorption/emission properties are
ARYLPYRAZOLES AND ARYLISOXAZOLES AND THEIR USE AS PKD MODULATORS
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Page/Page column 132, (2011/02/24)
The present invention provides novel organic compounds of formula (I) or (Ia): which may be inhibitors of a selective subset of kinases belonging to the AGC or calmodulin kinase family, such as for example PKD-1/2/3, inhibitors of histone deacetylase (HDA
Immobilization of bis(bipyridine) BINOL ligands and their use in chiral resolution
Bunzen, Jens,Kiehne, Ulf,Benkhaeuser-Schunk, Christian,Luetzen, Arne
supporting information; scheme or table, p. 4786 - 4789 (2009/12/29)
An enantlomerlcally pure bls(blpyrldlne) BINOL ligand was synthesized which was functionalized with an Iodine substituent In Its periphery. Using this halogen function, the ligand was Immobilized on a commercially available polystyrene gel via Suzuki cross-coupling. The functlonallzed gel was found to be effective In the chiral resolution of similar bis(blpyrldlne) ligands based on a Troeger's base core.
Synthesis and helicate formation of a new family of binol-based bis(bipyridine) ligands
Bunzen, Jens,Bruhn, Torsten,Bringmann, Gerhard,Luetzen, Arne
scheme or table, p. 3621 - 3630 (2009/08/14)
A new family of BINOL-based bis(bipyridine) ligands 1-3 (BINOL = 2,2 -dihydroxy-1,1 -binaphthyl) was prepared in enantiomerically pure form. Whereas the coordination of zinc(ll) ions to these ligands did not result in the selective formation of a specific metallosupramolecular aggregate,1 -3 were found to undergo highly diastereoselective self-assembly to D 2-symmetric dinuclear double-stranded helicates upon coordin ation to silver(l) and copper(l) ions and to D3-symmetric dinuclear triple-stranded helicates upon coordination to iron(ll) as demonstrated by mass spectrometry and by NMR and CD spectroscopy in combination with quantum chemical calculations.
Surprising substituent effects on the self-assembly of helicates from bis(bipyridyl) BINOL ligands
Bunzen, Jens,Hovorka, Rainer,Luetzen, Arne
supporting information; scheme or table, p. 5228 - 5236 (2009/12/04)
(Figure Presented) A number of different bis(bipyridyl) BINOL ligands were prepared using a convergent building block approach. These were studied with regard to their ability to undergo self-assembly to dinuclear helicates upon coordination to suitable late-transition-metal ions. Surprisingly, the substituents at the periphery of the ligand structure were found to have a marked influence on the outcome of the self-assembly processes with regard to the helicates composition, the stereoselectivity of the helicate formation, their redox reactivity, and their electronical properties as scrutinized by NMR- and CD-spectroscopic methods as well as ESI-mass spectrometric methods.