达非那新置于氢溴酸体系中,用 水,丁酮 用作溶剂,化学反应生成氢溴酸达非那新 参考文献: A Method For The Preparation Of Darifenacin Hydrogen Bromide[fr] Procédé De Préparation De Darifénacine Bromhydrique 标题: A Method For The Preparation Of Darifenacin Hydrogen Bromide[fr] Procédé De Préparation De Darifénacine Bromhydrique 摘要:一种制备(3S)-L-[2-(2,3-二氢-5-苯并呋喃基)乙基]-α,α-二苯基-3-吡咯烷乙酰胺溴化氢的方法,其中3-(S)-[(I-氨基甲酰)-1,1-二苯甲基]吡咯烷或其与有机酸的盐在无机碱存在下与5-(2-溴乙基)-2,3-二氢苯并呋喃在水和c6到c9脂肪,脂环或芳香族烃类有机溶剂的异相体系中进行烷基化反应,分离两相后得到粗的达瑞那新碱基,再加入c3到c9的酮或c3到c9的醇和浓盐酸转化为溴化氢盐.
专利号:WO-2009153649-A1 优先权日:2008-06-19 标 题:Process for preparing 3-substituted pyrrolidine compounds 发明人:SOLDEVILLA MADRID NURIA 权利人:MEDICHEM SA; SOLDEVILLA MADRID NURIA 摘要:Disclosed is a process for preparing 3 -substituted pyrrolidine compounds of formula (VII) or salts thereof, wherein R1 is described herein, which are intermediate compounds useful for the synthesis of darifenacin which is indicated for the treatment of overactive bladder with symptoms of urge, urinary incontinence, and the like, and pharmaceutically acceptable salts thereof. Also disclosed is a process for preparing darifenacin and pharmaceutically acceptable salts thereof.
专利号:US-2022370487-A1 优先权日:2021-05-10 标题 :Compositions targeting sodium channel 1.6 发明人:AMBROSI CHRISTINA; WILLIAMS LUIS; LEWARCH CAITLIN; GERBER DAVID; MCMANUS OWEN; AGRAWAL SUDHIR; DEMPSEY GRAHAM T 权利人:Q STATE BIOSCIENCES INC 摘要:The invention provides therapeutic compositions that include an antisense oligonucleotide (ASO) complementary to an identified target on a Nav channel mRNA. The ASO hybridizes to its target RNA and forms a duplex that recruits RNase H to degrade the RNA, thereby downregulating Nav channel synthesis, which inhibits the neuron's ability to contribute to certain conditions such as epilepsy and pain perception. The ASO binds to one of the specific identified targets, and may be provided as a gapmer that includes a central DNA segment flanked by modified RNA wings.
1: LiverTox: Clinical and Research Information on Drug-Induced Liver Injury [Internet]. Bethesda (MD): National Institute of Diabetes and Digestive and Kidney Diseases; 2012–. Darifenacin. 2023 Jul 12. 21(13):885-92; discussion 893-4. doi: 10.2165/00002512-200421130-00005. 33(4):475-82, viii. doi: 10.1016/j.ucl.2006.06.007. 41(7):441-52. doi: 10.1358/dot.2005.41.7.891719. 45(4):420-9; discussion 429. doi: 10.1016/j.eururo.2004.01.008. 59(7):831-8. doi: 10.1111/j.1368-5031.2005.00585.x. 45(4):325-50. doi: 10.2165/00003088-200645040-00001. 8(4):511-23. doi: 10.1517/14656566.8.4.511. 65(Pt 6):o1286. doi: 10.1107/S1600536809017085. 10: Nie M, Chen N, Pang H, Jiang T, Jiang W, Tian P, Yao L, Chen Y, DeBerardinis RJ, Li W, Yu Q, Zhou C, Hu Z. Targeting acetylcholine signaling modulates persistent drug tolerance in EGFR-mutant lung cancer and impedes tumor relapse. J Clin Invest. 2022 Oct 17;132(20):e160152. doi: 10.1172/JCI160152. 11: Chapple CR. Darifenacin: a novel M3 muscarinic selective receptor antagonist for the treatment of overactive bladder. Expert Opin Investig Drugs. 2004 Nov;13(11):1493-500. doi: 10.1517/13543784.13.11.1493. 20(5):424-31. doi: 10.4140/tcp.n.2005.424.
合成参考文献
参考文献:10.1124/mol.119.115964 摘要:Lee TD, Lee OW, Brimacombe KR, Chen L, Guha R, Lusvarghi S, Tebase BG, Klumpp-Thomas C, Robey RW, Ambudkar SV, Shen M, Gottesman MM, Hall MD. A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. Molecular Pharmacology. 2019 Nov;96(5):629–40. doi: 10.1124/mol.119.115964. 参考文献:10.1186/s43094-025-00820-8 摘要:Lalan M, Menon M, Shah P, Chakraborthy GS. Development and characterization of long-acting darifenacin intravaginal ring for managing overactive bladder in women: harnessing QbD approach. Futur J Pharm Sci. 2025 Jun 02;11(1). doi: 10.1186/s43094-025-00820-8. 参考文献:10.1007/s12668-025-02223-8 摘要:Chotaliya M, Dudhat K, Prajapati B. Development of Ivabradine Hydrochloride Nanosuspension Containing Gel for Transdermal Delivery: In Vitro and Ex Vivo Characterization. BioNanoSci. 2025 Dec 17;16(1). doi: 10.1007/s12668-025-02223-8.