专利号:CA-2640585-A1 优先权日:2003-02-05 标题 :Synthesis of 2-butyl-3-(2'-(1-trityl-1h-tetrazol-5-yl)biphenyl-4-yl)-1,3-diazaspirol{4,4}-non-ene-4-one
专利号:US-8722887-B2 优先权日:2006-09-22 标 题:Sulfonylpyrazole and sulfonylpyrazoline carboxamidine derivatives as 5-HT6 antagonists 发明人:VAN LOEVEZIJN ARNOLD; IWEMA BAKKER WOUTER I; KEIZER HISKIAS G; ZORGDRAGER JAN; VAN DER NEUT MARTINA A W; KRUSE CORNELIS G 权利人:VAN LOEVEZIJN ARNOLD; IWEMA BAKKER WOUTER I; KEIZER HISKIAS G; ZORGDRAGER JAN; VAN DER NEUT MARTINA A W; KRUSE CORNELIS G; ABBVIE BAHAMAS LTD 摘要:This invention concerns compounds of the general formula (1): n nand derivatives thereof, which are antagonists of 5-HT 6 receptors, wherein the symbols have the meanings given in the description. The invention also concerns methods for the preparation of these compounds, to novel intermediates useful for their synthesis, and to uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in treating at least on disease or condition chosen from Parkinson's disease, Huntington's chorea, schizophrenia, anxiety, depression, manic depression, psychoses, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, binge eating disorders, panic attacks, akathisia, attention deficit hyperactivity disorder, attention deficit disorder, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, disorders associated with spinal trauma or head injury, hydrocephalus, functional bowel disorder, Irritable Bowel Syndrome, obesity and type-2 diabetes.
1: Fan J, Lin R, Xia S, Chen D, Elf SE, Liu S, Pan Y, Xu H, Qian Z, Wang M, Shan C, Zhou L, Lei QY, Li Y, Mao H, Lee BH, Sudderth J, DeBerardinis RJ, Zhang G, Owonikoko T, Gaddh M, Arellano ML, Khoury HJ, Khuri FR, Kang S, Doetsch PW, Lonial S, Boggon TJ, Curran WJ, Chen J. Tetrameric Acetyl-CoA Acetyltransferase 1 Is Important for Tumor Growth. Mol Cell. 2016 Dec 1;64(5):859-874. doi: 10.1016/j.molcel.2016.10.014. Epub 2016 Nov 17. 2: Dakkak A, El Berbri I, Petavy AF, Boué F, Bouslikhane M, Fassi Fihri O, Welburn S, Ducrotoy MJ. Echinococcus granulosus infection in dogs in Sidi Kacem Province (North-West Morocco). Acta Trop. 2017 Jan;165:26-32. doi: 10.1016/j.actatropica.2016.07.007. Epub 2016 Jul 18. Chinese. doi: 10.1371/journal.pone.0120165. eCollection 2015. 5: Saha I, Das J, Maiti B, Chatterji U. A protective role of arecoline hydrobromide in experimentally induced male diabetic rats. Biomed Res Int. 2015;2015:136738. doi: 10.1155/2015/136738. Epub 2015 Jan 28.
合成参考文献
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