- 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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- An efficient synthesis of N(α)-FMOC-4(phosphonomethyl)-L- and D- phenylalanine
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A simple and efficient synthesis for N(α)-Fmoc-4-(phosphonomethyl)L- phenylalanine and N(α)-Fmoc-D-phenylalanine with high optical purity by using the commercially available L and D-phenylalanine as the starting material is described.
- Bo, Liu,Jiarong, Zhan
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p. 2293 - 2299
(2007/10/03)
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- Enantioselective synthesis of N-Fmoc protected di-tert-butyl 4-phosphonomethyl-L-phenylalanine: A hydrolytically stable analogue of O-phosphotyrosine
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Fmoc-L-Pmp(tBu)2-OH was prepared with high enantiomeric purity by an asymmetric synthetic pathway, using a camphor sultam as chiral auxiliary.
- Liu,Roques,Garbay-Jaureguiberry
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p. 647 - 650
(2007/10/02)
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- Improved synthesis of [p-phosphono and p-sulfo]methylphenylalanine. Resolution of [p-phosphono-, p-sulfo-, p-carboxy- and p-N-hydroxycarboxamido-]methylphenylalanine
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To analyse the role of post-translational phosphorylation and sulfation of tyrosine in peptides and proteins, we recently synthesized the new amino acids, p(CH2PO3H2)Phe and p(CH2SO3H)Phe (D,L mixture
- Garbay-Jaureguiberry,McCort-Tranchepain,Barbe,Ficheux,Roques
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p. 637 - 650
(2007/10/02)
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