3,4-二甲氧基苯乙酸置于三氟二甲基硫醚络合物体系中,用 二氯甲烷 用作溶剂,化学反应 24.0H,反应生成3,4-二羟基苯乙酸 参考文献: Bioispired Proteasome Activators With Antiageing Activity[fr] Activateurs Bio-Inspirés Des Protéasomes Ayant Une Activité Anti-âge 标题: Bioispired Proteasome Activators With Antiageing Activity[fr] Activateurs Bio-Inspirés Des Protéasomes Ayant Une Activité Anti-âge 摘要:本发明涉及新型生物启发的混合化合物,其化学式为i,作为蛋白酶体激活剂并具有抗衰老活性,以及其合成方法.这些混合化合物将羟基酪醇和天然抗氧化维生素e或其生物同系物的结构特征结合在一个分子支架中.化合物i的结构包括结构蛋白酶体激活剂(通过立体化学相互作用激活),可用于生产抗衰老产品,如化妆品制剂.此外,它们可以在蛋白酶体被下调的情况和疾病中使用,以及用作蛋白酶体激活控制化合物.
专利号:US-8101804-B2 优先权日:2006-07-28 标 题 :Process for the synthesis of (E)-stilbene derivatives which makes it possible to obtain resveratrol and piceatannol 发明人:SCHOUTEETEN ALAIN; JUS SEBASTIEN; VALLEJOS JEAN-CLAUDE 权利人:SCHOUTEETEN ALAIN; JUS SEBASTIEN; VALLEJOS JEAN-CLAUDE; CLARIANT SPECIALTY FINE CHEM F 摘要:A subject-matter of the present invention is a novel process for the synthesis of (E)-stilbene derivatives targeted at obtaining in particular resveratrol and piceatannol.
专利号:US-2004101523-A1 优先权日:1989-07-27 标题:Renal-selective prodrugs for control of renal smpathetic nerve activity in the treatment of hypertension 发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J 权利人:SEARLE & CO 摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-γ-glutamyl fusaric acid hydrazide (shown below) is preferred.
专利号:WO-9101724-A1 优先权日:1989-07-27 标题 :Renal-selective prodrugs for the treatment of hypertension 发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J 权利人:SEARLE & CO 摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as depa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitors compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-Y-glutamyl fusaric acid is preferred.
专利号:WO-9201667-A1 优先权日:1990-07-25 标题 :Renal-selective prodrugs for control of renal sympathetic nerve activity in the treatment of hypertension 发明人:REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J 权利人:SEARLE & CO 摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kydney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase-inhibitors, of which N-acetyl-η-glutamyl fusaric acid hydrazide [represented in formula (a)] is preferred.
专利号:US-6319905-B1 优先权日:1998-12-29 标 题 :Method of controlling L-Dopa production and of treating dopamine deficiency 发明人:MANDEL RONALD J; LEFF STUART E 权利人:CELL GENESYS INC 摘要:The present invention provides an effective approach to achieve the tightly modulated production of L-DOPA and/or dopamine at a preselected target location in the brain of a mammal by combining gene therapy approaches to supply a key enzyme in the synthesis of L-DOPA, and novel drug delivery modalities to administer a uniform level of a modulator of the activity of such key enzyme. The fine-tuned administration of the modulator establishes continuously uniform levels of modulator which in turn allow the effective modulation of L-DOPA and/or dopamine levels at a preselected target location in the brain of the mammal.
专利号:US-9453037-B2 优先权日:2011-07-28 标 题 :Methylphenidate-prodrugs, processes of making and using the same 发明人:GUENTHER SVEN; CHI GUOCHEN; BERA BINDU; MICKLE TRAVIS; BERA SANJIB 权利人:KEMPHARM INC; KEMPHARM INC 摘要:The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.
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合成参考文献
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