📜2-(2-溴-乙基)-萘,4-(3-Trifluoromethylphenyl)-1,2,3,6-Tetrahydropyridinium Chloride置于sodium Hydroxide体系中,用 乙醇,水 用作溶剂,化学反应 5.0H,以90%的收率获得扎利罗登 参考文献:Use Of 4-Substituted Tetrahydropyridines For Making Medicines Acting On Tgf-&bgr;1 标题:Use Of 4-Substituted Tetrahydropyridines For Making Medicines Acting On Tgf-&bgr;1 摘要:该发明涉及使用化合物(I)的方法,用于制备用于增加循环,细胞和细胞外tgf-β1水平的药物组合物.
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.
专利号:WO-2024040267-A2 优先权日:2022-08-19 标题 :Direct synthesis of n-(3-substituted-chroman-4-yl)-7h- pyrrolo[2,3-d]pyrimidin-4-amines and derivatives thereof
专利号:US-9550795-B2 优先权日:2011-08-31 标 题:Hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds 发明人:BRODNEY MICHAEL AARON; BUTLER CHRISTOPHER RYAN; HELAL CHRISTOPHER JOHN; O'NEILL BRIAN THOMAS 权利人:BRODNEY MICHAEL AARON; BUTLER CHRISTOPHER RYAN; HELAL CHRISTOPHER JOHN; O'NEILL BRIAN THOMAS; 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.
专利号:WO-2012172449-A1 优先权日:2011-06-13 标题:Lactams as beta secretase inhibitors 发明人:BRODNEY MICHAEL AARON 权利人:PFIZER; BRODNEY MICHAEL AARON 摘要:Compound and pharmaceutically acceptable salts of the compound are disclosed, wherein the compound has the structure (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed. The compound of formula I is useful as beta secretase inhibitor for use in the treatment of Alzheimer's and other neurodegenerative and/or neurological disorders.
专利号:US-2016229847-A1 优先权日:2013-10-04 标 题:Novel bicyclic pyridinones as gamma-secretase modulators 发明人:PETTERSSON MARTIN YOUNGJIN; AM ENDE CHRISTOPHER WILLIAM; GREEN MICHAEL ERIC; JOHNSON DOUGLAS SCOTT; KAUFFMAN GREGORY WAYNE; O'DONNELL CHRISTOPHER WILLIAM; PATEL NANDINI CHATURBHAI; STEPAN ANTONIA FRIEDERIKE; STIFF CORY MICHAEL; SUBRAMANYAM CHAKRAPANI; TRAN TUAN PHONG; 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 II as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:US-9067934-B2 优先权日:2011-03-31 标题 :Bicyclic pyridinones 发明人:PETTERSSON MARTIN YOUNGJIN; JOHNSON DOUGLAS SCOTT; SUBRAMANYAM CHAKRAPANI; O'DONNELL CHRISTOPHER JOHN; AM ENDE CHRISTOPHER WILLIAM; FISH BENJAMIN ADAM; GREEN MICHAEL ERIC; MULLINS PATRICK BRADLEY; STIFF CORY MICHAEL; TRAN TUAN PHONG; NAVARATNAM THAYALAN 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 herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
1: Francisco SG, Rowan S. Repurposing Drugs for Treatment of Age-Related Macular Degeneration. Adv Exp Med Biol. 2023;1415:73-77. doi: 10.1007/978-3-031-27681-1_12. 28(3):423-433. doi: 10.1093/ibd/izab191. 1(1):CD011776. doi: 10.1002/14651858.CD011776.pub2. 4: Andoh T, Sakamoto A, Kuraishi Y. 5-HT1A receptor agonists, xaliproden and tandospirone, inhibit the increase in the number of cutaneous mast cells involved in the exacerbation of mechanical allodynia in oxaliplatin-treated mice. J Pharmacol Sci. 2016 Aug;131(4):284-7. doi: 10.1016/j.jphs.2016.07.008. Epub 2016 Aug 4. 22:294-310.
合成参考文献
参考文献:10.1177/039463200401700207 摘要:Appert-Collin A, Duong FH, Passilly-Degrace P, Gies JP, Warter JM, Poindron P. Quantification of neurotrophin mRNA expression in PMN mouse: modulation by xaliproden. Int J Immunopathol Pharmacol. 2004 May;17(2):157–64. doi: 10.1177/039463200401700207.