- Polyamines XIV. Protonation Equilibria of Linear Tetraamines Containing two Ethylenediamine Residues
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The syntheses of the linear tetraamines H2N-(CH2)2-NH-(CH2)n-NH-(CH2)2-NH2 (n = 4 and 5) are described.The protonation of the homologous tetraamines for n = 2, 3, 4, 5, 6 and 8, as well as of N-methylethylenediamine, was investigated using potentiometric and calorimetric measurements.The results obtained are discussed taking into consideration the substituent effect on the basicity of the aminic N-atoms.
- Anderegg, Giorgio,Blaeuenstein, Peter
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- Composition, synthesis and therapeutic applications of polyamines
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This invention relates to a process of synthesis and composition of open chain (ring), closed ring, linear branched and or substituted polyamines, polyamine derived tyrosine phosphatase inhibitors and PPAR partial agonists/partial antagonists via a series of substitution reactions and optimizing the bioavailability and biological activities of the compounds. Polyamines prevent the toxicty of neutoxins and diabetogenic toxins including paraquat, methyphenyl pyridine radical, rotenone, diazoxide, streptozotocin and alloxan. These polyamines can be to treat neurological, cardiovascular, endocrine acquired and inherited mitochondrial DNA damage diseases and other disorders in mammalian subjects, and more specifically to the therapy of Parkinson's disease, Alzheimer's disease, Lou Gehrig's disease, Binswanger's disease, Olivopontine Cerebellar Degeneration, Lewy Body disease, Diabetes, Stroke, Atherosclerosis, Myocardial Ischemia, Cardiomyopathy, Nephropathy, Ischemia, Glaucoma, Presbycussis, Cancer, Osteoporosis, Rheumatoid Arthritis, Inflammatory Bowel Disease, Multiple Sclerosis and as Antidotes to Toxin Exposure.
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- Therapeutic and diagnostic domain 1 beta2GP1 polypeptides and methods of using same
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The present invention provides domain 1 β2GPI polypeptides, polynucleotides encoding these polypeptides, mimetics of these polypeptides, and methods using domain 1 β2GPI polypeptides and mimetics. Domain 1 of β2GPI has been shown to bind to anti-cardiolipin (β2GPI-dependent antiphospholipid) antibodies, which are associated with several pathologies, such as thrombosis and fetal loss. The domain 1 β2GPI polypeptides may be used to detect β2GPI-dependent antiphospholipid antibodies in a sample. The invention further provides methods of inducing tolerance using these domain 1 β2GPI polypeptides.
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- Valency platform molecules comprising aminooxy groups
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Molecules comprising aminooxy groups are provided, wherein the aminooxy groups provide attachment sites for the covalent attachment of other molecules. In one embodiment, polyoxyethylene molecules comprising aminooxy groups are provided that can be conjugated to wide variety of biologically active molecules including poly(amino acids). In another embodiment, valency platform molecules comprising aminooxy groups are provided. The aminooxy groups can be used to form covalent bonds with biological molecules such as poly(amino acids). The aminooxy groups can, for example, react with poly(amino acids) modified to contain carbonyl groups, such as glyoxyl groups, to form a conjugate of the valency platform molecule and the biologically active molecule via an oxime bond. The valency platform molecules comprising aminooxy groups are advantageously reactive in the formation of conjugates, and they also can be readily synthesized to form a composition with very low polydispersity.
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- Composition, synthesis and therapeutic applications of polyamines
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The invention relates to the preparation of novel polyamines, such as derivatives of 1,3-bis-[(2′-aminoethyl)-amino]propane (2,3,2-tetramine) and 1,4,8,11-tetraazacyclotetradecane (cyclam), which can be used to treat mitochondrial and degenerative diseases. Accordingly, in one aspect the invention is directed to compounds of the formula: wherein R1, R2, R3, R4, R5 and R6 may be the same or different and are hydrogen, alkyl, aryl, cycloalkyl, amino acid, glutathione, urate, ascorbate, estrogen, dehydroepiandrosterone, redox stabilizing substituents, a quinone, glutamate, succinate, —(CH2)n[XCH2)n]NH2— wherein n=3-6 and X=nitrogen, sulfur, phosporous or carbon, or heterocycle wherein R1 to R6 taken together are —(CH2XCH2)n— wherein n=3-6 and X=nitrogen, sulfur, phosporous or carbon. M, n, and p may be the same or different and are bridging groups of variable length from 3-12 carbons. X1 and X2 may be the same or different and are nitrogen, sulfur, phosporous or carbon.
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- Phenylglyoxal for polyamines modification and cyclam synthesis
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The bis-aminals obtained by tetraamine and phenylglyoxal condensation display various behaviours such as equilibrium between different configurations, rearrangements that lead to lactam derivatives, or amine deprotection. Our investigations about them were focused on three different linear amines, and then extended to polyazacycloalkanes cyclen and cyclam. Cyclam was also synthesised with the bis-aminals issued from condensation of linear polyamines with phenylglyoxal. The lactam derivatives described here were moreover, employed for the mono-N-functionalisation of tetraamines by phenyl-acetic acid group.
- Tripier, Rapha?l,Chuburu, Fran?oise,Le Baccon, Michel,Handel, Henri
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p. 4573 - 4579
(2007/10/03)
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- Monodisperse multifunctional carbodiimides
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Branched, monodisperse, multifunctional carbodiimides which are particularly useful as cross-linkers for carboxyl-containing resins.
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- Process for the dyeing of leather with anionic dyes and polyaminoamide resin as dyeing auxiliary
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To improve the affinity of anionic dyestuffs in the dyeing of leather materials, polycondensation products consisting of at least one amine of the formula STR1 in which the radicals have the meanings mentioned in the description with one dicarboxylic acid and, if desired, ω-aminocarboxylic acid or its lactam are highly suitable.
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- Polyfunctional carbodiimides having particular structures
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Branched polyfunctional carbodiimides of formula I wherein: M and Q are independently the residue of a compound adapted to function as a site for branching;, R1, R2, R4, R5, R6, and R7 are independently divalent organic radicals;, R3 and R8 are independently monovalent organic radicals;, a is 3 to 6; b, e, f and g are 0 to 4; and e, d, and h are 0 or 1;, are disclosed which are monodisperse, i.e., have exact functionality and molecular weight distribution. Compsoitons based on these polyfunctional carbodiimides have low viscosity relative to their molecular weight and are particularly useful as cross-linkers for carboxyl--containing resins.
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- Polyfunctional carbodiimides having particular structures
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Branched polyfunctional carbodiimides are disclosed which are monodisperse, i.e., have exact functionality and no molecular weight distribution. Compositions based on these polyfunctional carbodiimides have low viscosity relative to their molecular weight and are particularly useful as cross-linkers for carboxyl-containing resins.
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