CAS: 142761-12-4; (S)-O-Desmethylvenlafaxine

该化合物是抗抑郁性Venlafaxine的主要活代谢物, 展示了选择性的血清素和无肾上腺素再摄入抑制剂(SSNRI) . 这个对应物与其种族对应物相比, 显示更高的能量和更好的药效动力特性, 为...

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    (S)-1-(2-(dimethylamino)-1-(4-methoxyphenyl)ethyl)cyclohexanolN-oxide of (S)-4-[2-dimethylamino-1-(1-hydroxy-cyclohexyl)-ethyl]-phenol

    合成工艺路线路线简述

      📜1-[2-(二甲基氨基)-1-(4-甲氧基苯基)乙基]环己醇置于正丁基锂,二苯基膦,盐酸,碳酸氢钠体系中,用 四氢呋喃,正己烷,水 用作溶剂,化学反应 18.67H,以76%的收率获得4-[(1S)-2-(二甲基氨基)-1-(1-羟基环己基)乙基]苯酚
      参考文献:N-Oxides Of Venlafaxine And O-Desmethylvenlafaxine As Prodrugs
      标题:N-Oxides Of Venlafaxine And O-Desmethylvenlafaxine As Prodrugs
      摘要:本发明实施例涉及一种具有式(1)的化合物,或其互变异构体,立体异构体,水合物或溶剂合物,其中r1为h或ch3.本发明的其他实施例涉及含有这些化合物的药物组合物,制备这些化合物的方法,以及制备含有这些化合物的组合物的方法.本发明的另一实施例涉及这些化合物及含有它的组合物的用途,例如用于制造治疗选择自抑郁症,重性抑郁障碍,广泛性焦虑障碍,强迫症,社交焦虑障碍,惊恐障碍,一般性抑郁障碍,糖尿病性神经病,偏头痛和潮热的药物和药物组合物.

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      专利信息


      专利号:US-12234200-B2
      优先权日:2019-04-16
      标 题:Synthetic methods of preparing esketamine
      发明人:CHEN CHENG YI
      权利人:JANSSEN PHARMACEUTICA NV
      摘要:The present invention is directed to methods for the asymmetric synthesis of esketamine. The present invention is further directed to key intermediates in the asymmetric esketamine synthesis. In one embodiment, the invention is an asymmetric synthesis of esketamine comprising the conversion of (S)-2′-chloro-2-methoxy-3,4,5,6-5 tetrahydro-[1, 1′-biphenyl]-3-yl carbamate to (S)-2′-chloro-1-isocyanato-6-methoxy-1,2,3,4-tetrahydro-1,1′-biphenyl.

      专利号:US-9884844-B2
      优先权日:2012-12-31
      标 题:Heterocyclic compounds and methods of use thereof
      发明人:FANG QUN KEVIN; CAMPBELL UNA; SPEAR KERRY L
      权利人:SUNOVION PHARMACEUTICALS INC; SUNOVION PHARMACEUTICALS INC
      摘要:Provided herein are heterocyclyl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or management of various neurological disorders, including but not limited to, psychosis and schizophrenia.

      专利号:WO-2008084057-A1
      优先权日:2007-01-10
      标题:Compounds with a combination of cannabinoid-cb1 antagonism and serotonin reuptake inhibition
      发明人:LANGE JOSEPHUS H M; KRUSE CORNELIS G
      权利人:SOLVAY PHARM BV; LANGE JOSEPHUS H M; KRUSE CORNELIS G
      摘要:This invention relates to compounds with a combination of cannabinoid-CB1antagonism and serotonin reuptake inhibition to pharmaceutical compositions containing these compounds, to methods for preparing the compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing compositions. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in psychosis, anxiety, depression, attention deficits, cognitive disorders, obesity, drug dependence, Parkinson's disease, Alzheimer's disease, pain disorders, neuropathic pain disorders and sexual disorders. In particular the invention relates to compoundsof the general formula (I): wherein the symbols have the meanings given in the specification.

      专利号:US-8883831-B2
      优先权日:2008-11-05
      标题 :Compositions and methods for minimizing or reversing agonist-induced desensitization
      发明人:BEAR DAVID M; KESSLER ROBERT M
      权利人:PHARMORX THERAPEUTICS INC
      摘要:Methods and compositions are provided for preventing or reversing loss of the therapeutic effect of a drug, where the loss is associated with the repeated administration of the drug to a patient. The method includes administering to the patient a dopamine receptor agonist or partial agonist or a drug that increases the extracellular level of dopamine by enhancing release of dopamine, decreasing the removal of dopamine from the extracellular space, enhancing the synthesis of dopamine within the brain, or decreasing metabolic degradation of dopamine; and also administering to the patient an opioid receptor antagonist in an ultra-low dose amount, wherein the ultra-low dose amount is effective to prevent or reverse loss of therapeutic effects associated with the repeated administration of the drug to the patient. The methods are useful for various treatments, including treating Parkinson's Disease, Restless Leg Syndrome, depression, schizophrenia, psychostimulant drug abuse, or attention deficit disorder.

      专利号:US-8138174-B2
      优先权日:2007-01-10
      标 题:Compounds with a combination of cannabinoid CB1 antagonism and serotonin reuptake inhibition
      发明人:LANGE JOSEPHUS H M; KRUSE CORNELIS G
      权利人:LANGE JOSEPHUS H M; KRUSE CORNELIS G; SOLVAY PHARM BV
      摘要:Compounds with a combination of cannabinoid CB 1 antagonism and serotonin reuptake inhibition, pharmaceutical compositions containing these compounds, methods for preparing these compounds, methods for preparing novel intermediates useful for their synthesis, and methods for preparing these compositions are disclosed. Uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in psychosis, anxiety, depression, attention deficits, cognitive disorders, obesity, drug dependence, Parkinson's disease, Alzheimer's disease, pain disorders, neuropathic pain disorders and sexual disorders are disclosed. n In at least one embodiment, the invention relates to compounds of the general formula (1): n nwherein the substitutents have the definitions given in the specification.

      专利号:US-9751877-B2
      优先权日:2012-09-21
      标题 :Substituted pyrido[1,2-a]pyrazines for the treatment of neurodegenerative and neurological disorders
      发明人:PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; PATEL NANDINI CHATURBHAI; STIFF CORY MICHAEL; TRAN TUAN PHONG; KAUFFMAN GREGORY WAYNE; STEPAN ANTONIA FRIEDERIKE; VERHOEST PATRICK ROBERT
      权利人:PFIZER
      摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n nas defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

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      合成参考文献


      参考文献:10.1152/ajpgi.00044.2011
      摘要:Dai F, Lei Y, Chen JDZ. Inhibitory effects of desvenlafaxine on gastric slow waves, antral contractions, and gastric accommodation mediated via the sympathetic mechanism in dogs. American Journal of Physiology-Gastrointestinal and Liver Physiology. 2011 Oct;301(4):G707–12. doi: 10.1152/ajpgi.00044.2011.
      参考文献:10.4103/0019-5545.82558
      摘要:Andrade C. How to write a good abstract for a scientific paper or conference presentation. Indian J Psychiatry. 2011 Apr;53(2):172–5.
      参考文献:10.3389/fpsyg.2011.00159
      摘要:Andrews PW, Kornstein SG, Halberstadt LJ, Gardner CO, Neale MC. Blue again: perturbational effects of antidepressants suggest monoaminergic homeostasis in major depression. Front Psychol. 2011;2():159.
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