CAS: 1841-19-6; 8-(4,4-Bis(4-Fluorophenyl)Butyl)-1-Phenyl-1,3,8-Triazaspiro[4.5]Decan-4-One

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📜4,4-Di(4-Fluorophenyl)-But-3-En-1-Ol置于四溴化碳,Palladium On Activated Charcoal,氢气,Sodium Carbonate,三苯基膦,Potassium Iodide体系中,用 乙醇,二氯甲烷,乙腈 用作溶剂,化学反应 46.0H,反应生成帕罗西汀 杂质c
参考文献:Fluspirilene类似物激活20S蛋白酶体并通过固有紊乱的蛋白质寡聚体克服蛋白酶体的损害.
标题:Fluspirilene类似物激活20S蛋白酶体并通过固有紊乱的蛋白质寡聚体克服蛋白酶体的损害.
摘要:聚集倾向的固有无序蛋白(idp)(例如α-突触核蛋白,淀粉样蛋白β和tau)的寡聚化已被证明与包括帕金森氏症和阿尔茨海默氏症在内的几种神经退行性疾病的发病机理有关.蛋白酶体负责调节idp的细胞水平,但是该降解途径可能失调,导致其积累和随后的聚集.尽管这些神经退行性疾病的发病机理仍在深入研究中,但已表明idp的低聚形式,包括α-突触核蛋白和淀粉样蛋白β,会损害蛋白酶体功能.这导致idp的额外积累,从而进一步促进疾病进展.在此处,我们报道了蛋白酶体20S亚复合物的小分子活化剂的使用,以恢复受损的20S蛋白酶体活性,并防止idp积累和低聚.我们发现氟吡咯烷及其新的合成类似物(16)显示出强大的20S蛋白酶体增强作用(在2μm处将20S的蛋白水解活性提高一倍,最大折叠增强率约为1000%),克服了受损的蛋白酶体功能并防止了病原idp的积累.这些发现为使用20S增强剂作为对抗神经退行性疾病的可能治疗策略提供了支持.
Doi:10.1021/acschemneuro.1C00099

专利信息

专利号:US-2008287407-A1
优先权日:2003-12-10
标题 :Nitric Oxide Releasing Pyruvate Compounds, Compositions and Methods of Use
发明人：GARVEY DAVID S; FANG XINQIN; KHANAPURE SUBHASH P; RANATUNGA RAMANI R; WEY SHIOW-JYI
权利人:NITROMED INC
摘要:The invention describes novel nitrosated and/or nitrosylated pyruvate compounds and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated pyruvate compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one pyruvate compound and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one pyruvate compound, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating diseases resulting from oxidative stress, diabetes, reperfusion injury following ischemia, preservation of tissues, organs, organ parts and/or limbs.

专利号:WO-2016071723-A1
优先权日:2014-11-03
标题:Process for the preparation of a fluspirilene intermediate
发明人：FELICIANI LAZZARO; VISCARDI ENRICO; CREMONESI GIUSEPPE
权利人:SIFAVITOR S R L
摘要:The present invention relates to a process for the preparation of a 4,4'- bis(fluorobenzene) derivative, which is an intermediate compound in the synthesis of some drugs, for example in the synthesis of fluspirilene. The invention further relates to new synthetic intermediate compounds.

专利号:US-2022019720-A1
优先权日:2020-07-17
标 题 :Framework for automated synthesis of secure, optimized system-on-chip architectures
发明人：BHUNIA SWARUP; RAY SANDIP; DEB NATH ATUL PRASAD
权利人:UNIV FLORIDA
摘要:Systems and methods generate the design of a tiled multi-core system-on-chip (SoC). Design specification defining a multitude of cores to be used in the tiled multi-core SoC is analyzed and a multitude of subsystems based on the plurality of cores is built. The subsystems are augmented with one or more network adapters to generate the design of the tiled multi-core SoC. To achieve this, a multitude of IP blocks defined by the specification are retrieved from a design library. Design metadata associated with the IP blocks are extracted. Next, a standardized interface is generated for each of the IP blocks using the design metadata. Thereafter, a bus interface is generated for the IP blocks. Next, a tiled synthesizable register-transfer level code for the SoC design is generated in accordance with received configuration information.

专利号:US-6187756-B1
优先权日:1996-09-05
标 题 :Composition and methods for treatment of neurological disorders and neurodegenerative diseases
发明人：LEE ROBERT K K; WURTMAN RICHARD J
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:It has been discovered that the stimulation of β-adrenergic receptors, which activate cAMP formation, give rise to increased APP and GFAP synthesis in astrocytes. Hence, the in vitro or in vivo exposure of neuronal cells to certain compositions comprising β-adrenergic receptor ligands or agonists, including, e.g., norepinephrine, isoproterenol and the like, increases APP mRNA transcription and consequent APP overproduction. These increases are blocked by β-adrenergic receptor antagonists, such as propranolol. The in vitro or in vivo treatment of these cells with 8Br-cAMP, prostaglandin E 2 (PG E 2 ), forskolin, and nicotine ditartrate also increased APP synthesis, including an increase in mRNA and holoprotein levels, as well as an increase in the expression of glial fibrillary acidic protein (GFAP). Compositions and methods are disclosed of regulating APP overexpression and mediating reactive astrogliosis through cAMP signaling or the activation of β-adrenergic receptors. It has further been found that the increase in APP synthesis caused by 8Br-cAMP, PG E 2 , forskolin, or nicotine ditartrate is inhibited by immunosuppressants or anti-inflammatory agents, such as cyclosporin A, and FK-506 (tacrolimus), as well as ion-channel modulators, including ion chelating agents such as EGTA, or calcium/calmodulin kinase inhibitors, such as KN93. The present invention has broad implications in the alleviation, treatment, or prevention of neurological disorders and neurodegenerative diseases, including Alzheimer's Disease.

专利号:US-9697820-B2
优先权日:2015-09-24
标 题:Unit-selection text-to-speech synthesis using concatenation-sensitive neural networks
发明人：JEON WOOJAY
权利人:APPLE INC
摘要:Systems and processes for performing unit-selection text-to-speech synthesis are provided. In one example process, a sequence of target units can represent a spoken pronunciation of text. A set of predicted acoustic model parameters of a second target unit can be determined using a set of acoustic features of a first candidate speech segment of a first target unit and a set of linguistic features of the second target unit. A likelihood score of the second candidate speech segment with respect to the first candidate speech segment can be determined using the set of predicted acoustic model parameters of the second target unit and a set of acoustic features of the second candidate speech segment of the second target unit. The second candidate speech segment can be selected for speech synthesis based on the determined likelihood score. Speech corresponding to the received text can be generated using the selected second candidate speech segment.

专利号:US-6469055-B2
优先权日:1996-09-05
标题 :Compositions and methods for treatment of neurological disorders and neurodegenerative diseases
发明人：LEE ROBERT K K; WURTMAN RICHARD J
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:It has been discovered that the stimulation of β-adrenergic receptors, which activate cAMP formation, give rise to increased APP and GFAP synthesis in astrocytes. Hence, the in vitro or in vivo exposure of neuronal cells to certain compositions comprising β-adrenergic receptor ligands or agonists, including, e.g., norepinephrine, isoproterenol and the like, increases APP mRNA transcription and consequent APP overproduction. These increases are blocked by β-adrenergic receptor antagonists, such as propranolol. The in vitro or in vivo treatment of these cells with 8Br-cAMP, prostaglandin E 2 (PG E 2 ), forskolin, and nicotine ditartrate also increased APP synthesis, including an increase in mRNA and holoprotein levels, as well as an increase in the expression of glial fibrillary acidic protein (GFAP). Compositions and methods are disclosed of regulating APP overexpression and mediating reactive astrogliosis through cAMP signaling or the activation of β-adrenergic receptors. It has further been found that the increase in APP synthesis caused by 8Br-cAMP, PG E 2 , or forskolin is inhibited by immunosuppressants, immunophilin ligands, or anti-inflammatory agents, such as cyclosporin A, and FK-506 (tacrolimus), as well as ion-channel modulators, including ion chelating agents such as EGTA, or calcium/calmodulin kinase inhibitors, such as KN93. The present invention has broad implications in the alleviation, treatment, or prevention of neurological disorders and neurodegenerative diseases, including Alzheimer's Disease.