CAS: 1977-10-2; Loxapine

上下游产品

1-methyl-piperazine b,f][1,4]oxazepine2,11-dichloro-dibenzo[b,f][1,4]oxazepine methanol amoxapineb,f][1,4]oxazepine2,11-dichloro-dibenzo[b,f][1,4]oxazepine amoxapine 2-chlorodibenzo[b,f][1,4]oxazepin-11(10H)-one

📜2-Chlorodibenzo[b,F][1,4]Oxazepin-11-Amine 以85.2的收率获得洛沙平
参考文献:洛沙平的制备方法及其关键中间体
标题:洛沙平的制备方法及其关键中间体
摘要:本发明属于药物化学领域,公开了一种洛沙平的制备方法,其包含下述步骤:在有机溶剂中,化合物i与化合物ii发生缩合反应得到中间体iii;将步骤(1)制得的中间体iii还原缩合反应,得到中间体iv;将步骤(2)制得的中间体iv与 N-甲基哌嗪反应得到目标化合物tm.洛沙平用于精神分裂症的极性短期和长期维持性治疗,本发明所提供的制备发法具有所用试剂和原料易得,产品的收率和纯度较高,适合工业化生产的优点.

专利信息

专利号:US-7576211-B2
优先权日:2004-09-30
标题 :Synthesis of thienopyridinone compounds and related intermediates
发明人：DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; CHEN DONGLI; MARANTZ YAEL; SHACHAM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; BAR-HAIM SHAY; MOHANTY PRADYUMNA; LOBERA MERCEDES; WU LAURENCE
权利人:EPIX DELAWARE INC
摘要:The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

专利号:US-7309799-B2
优先权日:2004-06-01
标 题:Methods for the synthesis of milnacipran and congeners thereof
发明人：BUCHWALD STEPHEN L; SWAGER TIMOTHY M; RARIY ROMAN V
权利人:COLLEGIUM PHARMACEUTICAL INC
摘要:One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.

专利号:US-2012282255-A1
优先权日:2011-04-07
标题 :Methods and compositions for the treatment of alcoholism and alcohol dependence
发明人：PLUCINSKI GREG
权利人:PLUCINSKI GREG
摘要:The present invention provides for compositions and methods for treating or preventing addictive and compulsive diseases and disorders, particular alcohol-related diseases and disorders, disclosed herein. The GLP activators of the present invention are effective against various alcohol and drug dependency diseases. In accordance with the invention, the present compositions and methods can be used to intercede upstream or downstream in the signal transduction cascade involved in GLP action to treat various alcohol and drug dependency diseases. In one embodiment, the synthesis or release of endogenous GLP can be stimulated. In another embodiment, the endogenous synthesis or release of another molecule active in the cascade downstream from GLP, (e.g., a molecule produced in response to GLP binding to a receptor), can be stimulated. Accordingly, the methods and compositions of the invention are useful for preventing, treating, diagnosing, or monitoring the progression various alcohol and drug dependency diseases disclosed herein.

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:US-8697888-B2
优先权日:2012-01-06
标题 :Substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs as antagonists of muscarinic acetylcholine M1 receptors
发明人：LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; MELANCON BRUCE J; CHEUNG YIU-YIN
权利人:UNIV VANDERBILT
摘要:In one aspect, the invention relates to substituted (1-(methylsulfonyl)azetidin-3-yl)(heterocycloalkyl)methanone analogs, derivatives thereof, and related compounds, which are useful as antagonists of the muscarinic acetylcholine receptor M 1 (mAChR M 1 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

专利号:US-9056875-B2
优先权日:2012-08-31
标 题 :Substituted pyrazolo[3′,4′:4,5]thieno[2,3-C]pyridazin-3-amine analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M4
发明人：LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; SALOVICH JAMES M
权利人:UNIV VANDERBILT
摘要:In one aspect, the invention relates to substituted pyrazolo[3′,4′:4,5]thieno[2,3-c]pyridazine-3-amine analogs, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M 4 (mAChR M 4 ); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.