CAS: 300-54-9; 1-((2S,4R,5S)-4-Hydroxy-5-Methyltetrahydrofuran-2-yl)-N,N,N-Trimethylmethanaminium

该化合物是一种天然存在的藻类,主要见于某些蘑菇中,特别是阿曼尼塔菌类的菌类,如阿曼尼塔菌,是一种天然的藻类,是一种四甲胺化合物,其特点是能够模仿肌肉癌乙酰胆碱性受体的...

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    专利号:US-2006167025-A1
    优先权日:2004-12-22
    标 题:Tricyclic amino alcohols, processes for synthesis of same and use of same as anti-inflammatory drugs
    发明人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID
    权利人:BERGER MARKUS; SCHMEES NORBERT; SCHAECKE HEIKE; BAURLE STEFAN; REHWINKEL HARTMUT; MENGEL ANNE; KROLIKIEWICZ KONRAD; GROSSBACH DANJA; VOIGTLAENDER DAVID
    摘要:The invention relates to tricyclic amino alcohols of general formula (I) n nmethod for synthesis of same and use of same as anti-inflammatory agents.

    专利号:US-9254327-B2
    优先权日:2010-05-10
    标 题 :Methods and compositions for delivery of active agents
    发明人:MANOHARAN MUTHIAH; RAJEEV KALLANTHOTTATHIL G
    权利人:MANOHARAN MUTHIAH; RAJEEV KALLANTHOTTATHIL G; ALNYLAM PHARMACEUTICALS INC
    摘要:A lipid particle can include a cationic lipid. Synthesis of the cationic lipid can include a ylide-based reaction, such as a Wittig reaction or sulfur ylide reaction. In some cases, the synthesis can also include a Michael addition or a related addition reaction.

    专利号:US-7816375-B2
    优先权日:2000-09-11
    标 题 :Ligands for monoamine receptors and transporters, and methods of use thereof
    发明人:AQUILA BRIAN M; BANNISTER THOMAS D; CUNY GREGORY D; HAUSKE JAMES R; HOLLAND JOANNE M; PERSONS PAUL E; RADEKE HEIKE; WANG FENGJIANG; SHAO LIMING
    权利人:SEPRACOR INC
    摘要:One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.

    专利号:US-7812035-B2
    优先权日:2001-12-11
    标 题 :4-substituted piperidines, and methods of use thereof
    发明人:RADEKE HEIKE; SHAO LIMING
    权利人:SEPRACOR INC
    摘要:One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine, serotonin, or norepinephrine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, schizophrenia, Parkinson's disease, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.

    专利号:US-7217823-B2
    优先权日:2000-12-06
    标题:4,4-Disubstituted piperidines, and methods of use thereof
    发明人:HOEMANN MICHAEL Z
    权利人:SEPRACOR INC
    摘要:One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds, and the screening of those libraries for biological activity, e.g., in assays based on dopamine transporters.

    专利号:US-6872716-B2
    优先权日:2000-09-11
    标题:Antipsychotic sulfonamide-heterocycles, and methods of use thereof
    发明人:WU XINHE; AQUILA BRIAN M; SHAO LIMING; RADEKE HEIKE; CUNY GREGORY D; HAUSKE JAMES R; XIE ROGER L
    权利人:SEPRACOR INC
    摘要:One aspect of the present invention relates to heterocyclic compounds comprising a sulfonamide moiety. A second aspect of the present invention relates to the use of the heterocyclic compounds comprising a sulfonamide moiety to treat diseases, afflictions or maladies caused at least in part by abnormal activity of one or more GPCRs or ligand-gated ion channels. An additional aspect of the present invention relates to the synthesis of combinatorial libraries of the heterocyclic compounds comprising a sulfonamide moiety, and the screening of those libraries for biological activity, e.g., in animal models of psychosis.

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    主要参考文献


    1: Zhu Y, Dewell RB, Wang H, Gabbiani F. Pre-synaptic Muscarinic Excitation Enhances the Discrimination of Looming Stimuli in a Collision-Detection Neuron. Cell Rep. 2018 May 22;23(8):2365-2378. doi: 10.1016/j.celrep.2018.04.079. doi: 10.4997/JRCPE.2018.119. doi: 10.1016/j.yrtph.2018.01.012. Epub 2018 Jan 17. doi: 10.1016/j.ejphar.2017.10.034. Epub 2017 Oct 21. doi: 10.1113/JP275039. Epub 2017 Oct 19.
    6: Cárdenas AM, Fernández-Olivares P, Díaz-Franulic I, González-Jamett AM, Shimahara T, Segura-Aguilar J, Caviedes R, Caviedes P. Knockdown of Myo-Inositol Transporter SMIT1 Normalizes Cholinergic and Glutamatergic Function in an Immortalized Cell Line Established from the Cerebral Cortex of a Trisomy 16 Fetal Mouse, an Animal Model of Human Trisomy 21 (Down Syndrome). Neurotox Res. 2017 Nov;32(4):614-623. doi: 10.1007/s12640-017-9775-0. Epub 2017 Jul 10. doi: 10.3762/bjoc.13.121. eCollection 2017.
    8: Mitoh Y, Ueda H, Ichikawa H, Fujita M, Kobashi M, Matsuo R. Effects of cevimeline on excitability of parasympathetic preganglionic neurons in the superior salivatory nucleus of rats. Auton Neurosci. 2017 Sep;206:1-7. doi: 10.1016/j.autneu.2017.05.010. Epub 2017 May 30. doi: 10.3389/fphys.2017.00295. eCollection 2017.

    合成参考文献


    摘要:Naturwissenschaften., 56(615), 1969 []
    摘要:Science., 144(1100), 1964 []
    参考文献:10.1113/jphysiol.1996.sp021224
    摘要:Watkins CS, Mathie A. A non‐inactivating K+ current sensitive to muscarinic receptor activation in rat cultured cerebellar granule neurons. The Journal of Physiology. 1996 Mar;491(2):401–12. doi: 10.1113/jphysiol.1996.sp021224.
    参考文献:10.1113/jphysiol.1996.sp021225
    摘要:Shen WX, Horn JP. Presynaptic muscarinic inhibition in bullfrog sympathetic ganglia. The Journal of Physiology. 1996 Mar;491(2):413–21. doi: 10.1113/jphysiol.1996.sp021225.
    摘要:Thiebot H, Duchatelle-Gourdon I. [Regulation of muscarinic potassium channels]. C R Seances Soc Biol Fil. 1996;190(2-3):237–41.
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