专利号:US-2002040032-A1 优先权日:2000-07-07 标 题:Methods for stimulation of synthesis of synaptophysin in the central nervous system 发明人:GLASKY MICHELLE S; LAHIRI DEBOMOY K; FARLOW MARTIN R 摘要:A method of increasing the synthesis and/or secretion of synaptophysin comprises administering to a patient with a neurological disease or a patient at risk of developing a neurological disease an effective quantity of a purine derivative or analogue, a tetrahydroindolone derivative or analogue, or a pyrimidine derivative or analogue. If the compound is a purine derivative, the purine moiety can be guanine or hypoxanthine. The neurological disease can be a neurodegenerative disease such as Alzheimer's disease or a neurodevelopmental disorder such as Down's syndrome. Typically, the compound can pass through the blood-brain barrier. The purine moiety can be hypoxanthine or guanine. A particularly preferred purine derivative is N-4-carboxyphenyl-3-(6-oxohydropurin-9-yl) propanamide.
专利号:US-8541569-B2 优先权日:2008-09-06 标题:Phosphoramidites for synthetic RNA in the reverse direction, efficient RNA synthesis and convenient introduction of 3'-end ligands, chromophores and modifications of synthetic RNA 发明人:SRIVASTAVA SURESH C; SRIVASTAVA NAVEEN P 权利人:SRIVASTAVA SURESH C; SRIVASTAVA NAVEEN P; CHEMGENES CORP 摘要:The present invention provides building blocks and methods for synthesizing very pure RNA in a form that can efficiently be modified at the 3′ end. Reverse RNA monomer phosphoramidites have been developed for RNA synthesis in 5′→3′ direction, leading to very clean oligo synthesis that allows for the introduction of various modifications at the 3′-end cleanly and efficiently. Higher coupling efficiency per step have been observed during automated oligo synthesis with the reverse RNA amidites disclosed herein, resulting in a greater ability to achieve higher purity and produce very long oligonucleotides. The use of the reverse RNA phosphoramidites in the synthetic process of this invention leads to oligonucleotides free of N+1 species.
专利号:US-2004116453-A1 优先权日:2001-07-17 标 题 :Synthesis and methods of use pyrimidine analogues and derivatives 发明人:FICK DAVID B; FOREMAN MARK M; GLASKY ALVIN J 摘要:A pyrimidine derivative or analogue comprises an amino-substituted six-membered heterocyclic moiety, moiety A, linked through a linker L to a moiety B, where B is a carboxylic acid, a carboxylic acid ester, or a moiety of the structure N(Y 1 )-D, where Y 1 can be one of a variety of substituents, including hydrogen or alkyl, and D is a moiety that enhances the pharmacological effects, promotes absorption, or promotes blood-brain barrier penetration of the derivative or analogue. The moiety A can have two or three nitrogen atoms in the ring; typically, the moiety A is a pyrimidine moiety, with two nitrogen atoms in the ring. The moiety B can be one of a variety of moieties, including moieties having nootropic activity or other biological or physiological activity.
专利号:US-5717083-A 优先权日:1994-02-23 标题 :Phosphoramidate and phosphorothiomidate oligomeric compounds 发明人:COOK PHILLIP DAN; ACEVEDO OSCAR; HEBERT NORMAND 权利人:ISIS PHARMACEUTICALS INC 摘要:PCT No. PCT/US95/02267 Sec. 371 Date Aug. 19, 1996 Sec. 102(e) Date Aug. 19, 1996 PCT Filed Feb. 23, 1995 PCT Pub. No. WO95/23160 PCT Pub. Date Aug. 31, 1995Compounds are provided having structure (I), wherein the L groups are backbone segments, the Y and T groups are functional groups for interacting with target molecules of interest, the X groups are oxygen or sulfur and the E groups are H, conjugate groups or intermediate groups used during the synthesis of the compounds and wherein the compounds are prepared using H phosphonate type chemistry wherein the functional groups are added during an oxidation step or during a coupling step. (I)
专利号:WO-2010096201-A2 优先权日:2009-02-22 标 题 :Synthesis of ara-2'-o-methyl-nucleosides, corresponding phosphoramidites and oligonucleotides incorporating novel modifications for biological application in therapeutics, diagnostics, g- tetrad forming oligonucleotides and aptamers
专利号:WO-0204451-A2 优先权日:2000-07-07 标 题:Methods for stimulation of synthesis of synaptophysin in the central nervous system
参考文献:10.1186/s13045-022-01224-4 摘要:Qu J, Yan H, Hou Y, Cao W, Liu Y, Zhang E, He J, Cai Z. RNA demethylase ALKBH5 in cancer: from mechanisms to therapeutic potential. Journal of Hematology & Oncology. 2022 Jan 21;15(1):8. doi: 10.1186/s13045-022-01224-4.