1-(双环[2.2.1]庚-5-烯-2-基)-3-(1-哌啶基)-1-丙酮,Phenyl Magnesium 反应生成 比哌立登 参考文献:Method For The Production Of Biperidin 标题:Method For The Production Of Biperidin 摘要:本发明涉及一种生产双氢异奎尼的方法,该方法是通过将1-(双环[2.2.1]庚-5-烯-2-基)-3-哌啶基-1-丙酮的外/内混合物与苯基镁化合物反应,形成1-(双环[2.2.1]庚-5-烯-2-基)-1-苯基-3-哌啶基-1-丙醇的异构体混合物,从而通过将该混合物转化为相应的盐酸盐,分离所述盐酸盐,再转化为游离基,并结晶化所述双氢异奎尼而获得.
专利号:WO-2008065672-A3 优先权日:2006-11-27 标题 :A process for producing acetylnorbornene, an intermediate in the synthesis of biperiden 发明人:GOTTUMUKKALA VENKATA SUBBARAJU; MAMILLAPALLI RAMBHADRA SARMA; TERLI CHIRANJEEVI 权利人:SAIRAM ORGANICS PVT LTD; GOTTUMUKKALA VENKATA SUBBARAJU; MAMILLAPALLI RAMBHADRA SARMA; TERLI CHIRANJEEVI 摘要:The present invention relates to a novel process for the production of acetylnorbornene, efficiently and industrially useful manner. The process is applicable for the large scale production of acetylnorbornene and consists of preparation of 5-cyanonorbornene and its reaction with appropriate Grignard reagents. The product contains higher proportion of the exo form than the endo form, which is important for the synthesis of biperiden.
专利号:WO-2025128098-A1 优先权日:2023-12-13 标 题 :Solid oral dosage forms, kits, and methods of using the same 发明人:LI YING; LANGER ROBERT; TRAVERSO CARLO 权利人:MASSACHUSETTS INST TECHNOLOGY; BRIGHAM & WOMENS HOSPITAL INC 摘要:Provided herein are solid oral dosage forms, methods, and kits useful, e.g, for the extension of the residence time of active pharmaceutical agents in vivo by the synthesis of a polymer in situ in a subject. In particular, the solid oral dosage forms, methods, and kits disclosed herein are particularly useful for drugs that require more than once daily administration (e.g, drugs that have short half-lives).
专利号:US-2009285888-A1 优先权日:2005-05-13 标题:Derivatives of dihydroxyphenylalanine 发明人:SUSILO GISELA 权利人:SUSILO GISELA 摘要:The invention relates to derivatives of dihydroxyphenylalanine, to their synthesis and to pharmaceutical compositions containing said derivatives of dihydroxyphenylalanine. Furthermore, the invention relates to the use of said derivatives of dihydroxyphenylalanine and said pharmaceutical compositions for the treatment and prophylaxis of movement disorders, neurodegenerative diseases, Alzheimer's disease, Parkinson's disease, hemiparkinson-hemiatrophy, parkinsonian syndrome, Lewy body disease, frontotemporal dementia, Lytico-Bodig disease (parkinsonism/dementia/amyotrophic lateral sclerosis), striatonigral degeneration, Shy-Drager syndrome, sporadic olivopontocerebellar degeneration, progressive atrophy of the globus pallidus, progressive supranuclear palsy, Hallervorden-Spatz disease, Huntington's disease, X-linked dystonia-parkinsonism (Lubag), mitochondrial cytopathy with striatal necrosis, neuroacanthocytosis, restless legs syndrome, Wilson's disease.
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.
专利号:US-9073935-B2 优先权日:2011-11-11 标 题:Substituted benzylspiroindolin-2-one analogs as positive allosteric modulators of the muscarinic acetylcholine receptor M1 发明人:LINDSLEY CRAIG W; CONN P JEFFREY; WOOD MICHAEL R; HOPKINS COREY R; MELANCON BRUCE J; POSLUSNEY MICHAEL S 权利人:UNIV VANDERBILT 摘要:In one aspect, the invention relates to substituted benzylspiroindolin-2-one analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators 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.
1: Sambeth A, Riedel WJ, Klinkenberg I, Kähkönen S, Blokland A. Biperiden selectively induces memory impairment in healthy volunteers: no interaction with citalopram. Psychopharmacology (Berl). 2015 Jun;232(11):1887-97. doi: 10.1007/s00213-014-3822-9. Epub 2014 Dec 4. doi: 10.1016/j.euroneuro.2014.06.001. Epub 2014 Jun 12. Russian. doi: 10.1016/j.bbr.2014.08.036. Epub 2014 Aug 24. doi: 10.1097/JCP.0000000000000421. doi: 10.4155/bio.12.292. doi: 10.1016/j.etap.2012.04.004. Epub 2012 Apr 10. doi: 10.1016/j.yebeh.2012.09.009. Epub 2012 Nov 13. doi: 10.1186/1744-9081-9-4. 10: Ramos AC, Andersen ML, Oliveira MG, Soeiro AC, Galduróz JC. Biperiden (M₁ antagonist) impairs the expression of cocaine conditioned place preference but potentiates the expression of cocaine-induced behavioral sensitization. Behav Brain Res. 2012 May 16;231(1):213-6. doi: 10.1016/j.bbr.2012.03.030. Epub 2012 Mar 26. doi: 10.1016/j.pnpbp.2010.08.030. Epub 2010 Sep 7. doi: 10.1016/j.bbr.2011.07.050. Epub 2011 Aug 10. doi: 10.1016/j.neulet.2012.01.073. Epub 2012 Feb 7. doi: 10.1016/j.schres.2010.02.1060. Epub 2010 Mar 17. doi: 10.1017/S1461145711001647. Epub 2011 Nov 18. 17: Takahashi S, Suzuki M, Uchiyama M. A case of schizophrenia with meige syndrome induced by perospirone successfully treated with biperiden. J Neuropsychiatry Clin Neurosci. 2013 Winter;25(1):E28. doi: 10.1176/appi.neuropsych.12020029. doi: 10.1007/s00213-011-2171-1. Epub 2011 Feb 19.
合成参考文献
参考文献:10.1007/s10549-011-1595-y 摘要:Creighton CJ, Sada YH, Zhang Y, Tsimelzon A, Wong H, Dave B, Landis MD, Bear HD, Rodriguez A, Chang JC. A gene transcription signature of obesity in breast cancer. Breast Cancer Research and Treatment. 2011 Jul 13;132(3):993–1000. doi: 10.1007/s10549-011-1595-y.