CAS: 14663-23-1; Sodium 3-(((5-(4-Nitrophenyl)Furan-2-yl)Methylene)Amino)-2,5-Dioxoimidazolidin-1-Ide

该化合物是一种丁丁酸衍生物和骨骼肌肉放松剂,直接作用于受体(RyR1),以抑制沙眼中复微润滑液释放钙.它广泛用于临床和研究环境,用于管理恶性高温和肌肉抽搐.钠盐形式会增加溶性,使其适合静脉注射.它的高纯度和稳定性确保药物学研究和治疗应用的可靠性能.但丁烯钠盐因其在对骨骼肌肉的选择性行动而特别受到重视,而不会对心脏或光滑肌肉产生重大影响,为与肌肉有关的状况提供了有针对性的方法.

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CAS号7261-97-4 1-(((5-(4-硝基苯基)... | CAS号7147-77-5 5-对硝基苯基糠醛

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    专利信息


    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-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.

    专利号:US-9265748-B2
    优先权日:2011-08-11
    标题 :Anhydrous and hemihydrate crystalline forms of an (R)-baclofen prodrug, methods of synthesis and methods of use
    发明人:RAILLARD STEPHEN P; MANTHATI SURESH K; JOSHI SUDHIR
    权利人:XENOPORT INC
    摘要:Crystalline (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxyl)propoxy]carbonylamino}-3-(4-chlorophenyl)butanoic acid anhydrate and crystalline (3R)-4-{[(1S)-2-methyl-1-(2-methylpropanoyloxyl)propoxy]carbonylamino}-3-(4-chlorophenyl)butanoic acid hemihydrate, pharmaceutical compositions comprising such compounds, methods of making and methods of using the same are disclosed.

    专利号:US-2015313865-A1
    优先权日:2011-08-11
    标 题:Anhydrous and hemihydrate crystalline forms of an (r)-baclofen prodrug, methods of synthesis and methods of use

    专利号:US-2014066501-A1
    优先权日:2011-08-11
    标 题:Anhydrous and Hemihydrate Crystalline Forms of an (R)-Baclofen Prodrug, Methods of Synthesis and Methods of Use

    专利号:US-8580850-B2
    优先权日:2011-08-11
    标题 :Anhydrous and hemihydrate crystalline forms of an (R)-baclofen prodrug, methods of synthesis and methods of use
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    主要参考文献

    1. Kobayashi, S., Yano, M., Suetomi, T., et al. Dantrolene, a therapeutic agent for malignant hyperthermia, markedly improves the function of failing cardiomyocytes by stabilizing interdomain interactions within the ryanodine receptor. J. Am. Coll. Cardiol. 53(21), 1993-2005 (2009). 2. Oo, Y.W., Gomez-Hurtado, N., Walweel, K., et al. Essential role of calmodulin in RyR inhibition by dantrolene. Mol. Pharmacol. 88(1), 57-63 (2015). 3. Kotsias, B.A., and Muchnik, S. Reversible effect of dantrolene sodium on twitch tension of rat skeletal muscle. Arch. Neurol. 35(4), 234-236 (1978). 4. Nelson, T.E., and Flewellen, E.H. Rationale for dantrolene vs. procainamide for treatment of malignant hyperthermia. Anesthesiology 50(2), 118-122 (1979).

    合成参考文献


    参考文献:10.1007/s004240050261
    摘要:Buschman HPJ, Elzinga G, Woledge RC. The effects of the level of activation and shortening velocity on energy output in type 3 muscle fibres from Xenopus laevis. Pflgers Archiv European Journal of Physiology. 1996 Nov 18;433(1-2):153–9. doi: 10.1007/s004240050261.
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