- Electrochemical CO2 Reduction-The Effect of Chalcogenide Exchange in Ni-Isocyclam Complexes
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Among the numerous homogeneous electrochemical CO2 reduction catalysts, [Ni(cyclam)]2+ is known as one of the most potent catalysts. Likewise, [Ni(isocyclam)]2+ was reported to enable electrochemical CO2 conversion but has received significantly less attention. However, for both catalysts, a purposeful substitution of a single nitrogen donor group by chalcogen atoms was never reported. In this work, we report a series of isocyclam-based Ni complexes with {ON3}, {SN3}, {SeN3}, and {N4} moieties and investigated the influence of nitrogen/chalcogen substitution on electrochemical CO2 reduction. While [Ni(isocyclam)]2+ showed the highest selectivity toward CO2 reduction within this series with a Faradaic efficiency of 86% for the generation of CO at an overpotential of-1.20 V and acts as a homogeneous catalyst, the O-and S-containing Ni complexes revealed comparable catalytic activities at ca. 0.3 V milder overpotential but tend to form deposits on the electrode, acting as precursors for a heterogeneous catalysis. Moreover, the heterogeneous species generated from the O-and S-containing complexes enable a catalytic hydride transfer to acetonitrile, resulting in the generation of acetaldehyde. The incorporation of selenium, however, resulted in loss of CO2 reduction activity, mainly leading to hydrogen generation that is also catalyzed by a heterogeneous electrodeposit.
- Apfel, Ulf-Peter,Battistella, Beatrice,Gerschel, Philipp,Ray, Kallol,Siegmund, Daniel
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p. 1497 - 1510
(2020/04/30)
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- TRIAZACYCLODODECANSULFONAMIDE ("TCD")-BASED PROTEIN SECRETION INHIBITORS
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Provided herein are triazacyclododecansulfonamide ("TCD")-based protein secretion inhibitors, such as inhibitors of Sec61, methods for their preparation, related pharmaceutical compositions, and methods for using the same. For example, provided herein are compounds of Formula (I) and pharmaceutically acceptable salts and compositions including the same. The compounds disclosed herein may be used, for example, in the treatment of diseases including inflammation and/or cancer.
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Paragraph 00190
(2019/10/04)
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- LIPIDS FOR THERAPEUTIC AGENT DELIVERY FORMULATIONS
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The description is directed to ionizable lipids useful for enhancing the delivery of therapeutic agents in liposomes.
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Paragraph 0098; 0099
(2014/01/08)
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- COMPOUNDS FOR TARGETING DRUG DELIVERY AND ENHANCING SIRNA ACTIVITY
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Here described are compounds of formula I: wherein R1 and R2 is independently selected from a group consisting of C10 to C18 alkyl, C12 to C18 alkenyl, and oleyl group; wherein R3 and R4 are independently selected from a group consisting of C1 to C6 alkyl, and C2 to C6 alkanol; wherein X is selected from a group consisting of -CH2-, -S-, and -O- or absent; wherein Y is selected from -(CH2)n, -S(CH2)n, -O(CH2)n-, thiophene, -SO2(CH2)n-, and ester, wherein n = 1 -4; wherein a = 1 -4; wherein b=l -4; wherein c=l-4; and wherein Z is a counterion; and compounds consisting of the structure (targeting molecule)m-linker-(targeting molecule)n, wherein the targeting molecule is a retinoid or a fat soluble vitamin having a specific receptor on the target cell; wherein m and n are independently 0, 1, 2 or 3; and wherein the linker comprises a polyethylene glycol (PEG) or PEG-like molecule, as well as compositions and pharmaceutical formulations including one or both of these compounds which are useful for the delivery of therapeutic agents; and methods of using these compositions and pharmaceutical formulations.
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Page/Page column 47
(2013/02/27)
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- 16-Member ring metal chelate
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Metal chelates are useful for improving the contrast of X-ray, ultrasound, radionuclide and magnetic resonance (MR) images. However, the metal complexes must be stable and inert so that toxicity resulting from dissociation in the body can be minimized. This invention provides 16-member ring metal chelates that can provide a charge balanced metal complex having improved stability, especially for gadolinium(III) and samarium (III).
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Page/Page column 3
(2008/06/13)
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- Flexible covalent tripods in nonadentate podands: Synthesis of tris[3-(6-diethylcarbamoylpyridine-2-carboxamido)propyl]amine and its complexing properties with trivalent lanthanides
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The nonadentate podand tris[3-(6-diethylcarbamoylpyridine-2-carboxamido)propyl]amine (L14) is prepared according to a multistep strategy using the flexible tris(3-(N-methylamino)propyl)amine (Me-TRPN) covalent tripod. L14 exists as a statistical mixture of four conformers in solution whose distribution is slightly affected by protonation of the apical nitrogen atom in [L14 + H]+. The pKa value depends on the length of the spacer separating the apical nitrogen and the appended electron-withdrawing tertiary amide groups, and increases by three orders of magnitude when going from the Me-TREN tripod in [L13 + H]+ (ethylene spacer) to Me-TRPN in [L14 + H]+ (trimethylene spacer). Reactions of L14 and [L14 + H]+ with Ln(ClO4)3 (Ln = La-Lu) produce flexible and poorly stable 1:1 podates [Ln(L14)]3+ and [Ln(L14 + H)]4+ in which the terdentate chelating binding units exhibit partial dynamic on-off complexation equilibria. Comparisons of structural and thermodynamic data for [Ln(Ln)]3+ (n = 13 or 14) in solution point to a drastic decrease of the molecular organisation of the podand when the constrained Me-TREN tripod is replaced by the elongated Me-TRPN tripod in nine-co-ordinate lanthanide podates, a crucial limiting factor for the design of supramolecular lanthanide complexes with predetermined properties.
- Renaud,Decurnex,Piguet,Hopfgartner
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p. 1863 - 1871
(2007/10/03)
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- Manganese complexes of nitrogen-containing macrocyclic ligands effective as catalysts for dismutating superoxide
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The present invention is directed to low molecular weight mimics of superoxide dismutase (SOD) represented by the formula: STR1 wherein R, R', R1, R'1, R2, R'2, R3, R'3, R4, R'4, R5, R'5, R6, R'6, R7, R'7, R8, R'8, R9, and R'9 and X, Y, Z and n are as defined herein, useful as therapeutic agents for inflammatory disease states and disorders, ischemic/reperfusion injury, stroke, atherosclerosis, hypertension and all other conditions of oxidant-induced tissue damage or injury.
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- Methods of preparing manganese complexes of nitrogen-containing macrocyclic ligands
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The present invention is directed to low molecular weight mimics of superoxide dismutase (SOD) represented by the formula: STR1 wherein R, R', R1, R'1, R2, R'2, R3, R'3, R4, R'4, R5, R'5, R6, R'6, R7, R'7, R8, R'8, R9, and R'9 and X, Y, Z and n are as defined herein, useful as therapeutic agents for inflammatory disease states and disorders, ischemic/reperfusion injury, stroke, atherosclerosis, hypertension and all other conditions of oxidant-induced tissue damage or injury.
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- New linked macrocyclic systems derived from selectively protected S2N2 macrocycles
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Novel application of a protecting group strategy has enabled a simple and efficient synthesis of the new tri-linked S2N2 macrocycles 12, 15, 17 and 20. This strategy involves the introduction of complementary protecting groups (R1 and R2) into the precursor macrocycle 4, which can then be manipulated to provide a synthetically versatile set of mono-N-protected S2N2 macrocyclic building blocks 5, 7 and 8.
- Groth, Andrew M.,Lindoy, Leonard F.,Meehan, George V.
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p. 1553 - 1558
(2007/10/03)
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- First unequivocal synthesis of 1 or 8-N-monosubstituted 1,4,8,12-tetraazacyclopentadecane
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A novel method derived from Kaden's modification of the Richman and Atkins's cyclization using tosylated synthons allows the unequivocal synthesis of 1 and 8-monofunctionalized 1,4,8,12-tetraazacyclo-pentadecane. Both syntheses are described.
- Granier, Colin,Guilard, Roger
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p. 1197 - 1208
(2007/10/02)
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- Candida antarctica Lipase-Catalyzed Monoaminolysis of Diesters with Aminoalcohols. Chemoenzymatic Synthesis of Macrocycles and Aminodiols
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Candida antarctica lipase catalyzes the selective monoaminolysis of diesters using aminoalcohols as nucleophiles.The reduction of the amidoseters obtained is a way to prepare symmetrical and unsymmetrical aminodiols.Macrocyclic compounds were isolated in the lipase-catalyzed reactions between dimethyl adipate and 5-amino-1-pentanol and 6-amino-1-hexanol.
- Quiros, Margarita,Rebolledo, Francisca,Gotor, Vicente
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p. 1917 - 1934
(2007/10/02)
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- 99mTc Complexes with Hexadentate Tricatechol Ligands
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The tricatechol ligand trisamine hydrochloride, TRIPACE (9), is prepared from tris(3-chloropropyl)amine (5) and the potassium salt of 2,2-dimethyl-1,3-benzodioxol-4-ol (7).This ligand is capable of reducing the 99m- ion to lower valent 99mTc and subsequent complexation of the reduced 99mTc ion.The structures of 5 and of trisamine (8) are determined by X-ray diffration.
- Hahn, Ekkehardt F.,Rupprecht, Stefan
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p. 481 - 486
(2007/10/02)
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- STUDIES OF PENDANT-ARM MACROCYCLIC LIGANDS. PART 4. TWO PENTA-AZA MACROCYCLES BASED ON 1-(2'-DIMETHYLAMINOETHYL)-1,5,9,13-TETRA-AZACYCLOHEXADECANE AND ITS COMPLEXES WITH BIVALENT METAL IONS
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Two new pendant-arm sixteen-membered ring penta-aza macrocycles, 1-(2'-dimethylaminoethyl)-1,5,9,13-tetra-azacyclohexadecane (L1) and 1-(2'-dimethylaminoethyl)-5,9,13-trimethyl-1,5,9,13-tetra-azacyclohexadecane (L2) have been prepared and the complexes of L1 with Ni2+, Cu2+, Co2+, Zn2+, Cd2+, and Hg2+, investigated.The ions Ni2+, Cu2+, and Co2+ form high-spin five-co-ordinnate complexes.Carbon-13 n.m.r. spectroscopy shows 1)>2 to be a 1:1 mixture of two species, one symmetric and the other asymmetric, and 1)>2 is analogous but with evidence of a small amount of a third species.Attempts to prepare 1)>2+ have led to its immediate reduction to metallic mercury.
- Alcock, Nathaniel W.,Curzon, Eirian H.,Moore, Peter,Omar, Hadi, A. A.,Pierpoint, Colin
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p. 1361 - 1364
(2007/10/02)
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