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1-(4-氟苯基)-N-甲基甲亚胺置于sodium Tetrahydroborate体系中,用 甲醇 作为反应溶剂,以1.2 G的收率获得产物n-甲基-4-氟苄胺
参考文献:与钾kv7通道开放活性有关但与肝细胞毒性无关的止痛药氟吡汀n修饰衍生物的氧化电位
标题:与钾kv7通道开放活性有关但与肝细胞毒性无关的止痛药氟吡汀n修饰衍生物的氧化电位
摘要:神经元电压门控性钾离子通道(k V)的开放剂作为治疗疼痛(氟吡汀)和癫痫病(瑞替加滨)的治疗剂受到关注.为了更好地了解氟吡汀的作用机理和毒性,我们合成了九种具有不同氧化还原行为的新型类似物.氟吡汀可被氧化代谢为氮杂醌二亚胺;因此,通过循环伏安法测定了氟吡汀及其类似物的氧化电位.k V 7.2 / 3(kcnq2 / 3)打开活性是通过已建立的测定法来确定的,这些测定法过度表达了这些通道的hek293细胞.发现化合物的氧化电位与其ec 50之间存在联系钾通道开放活性的数值.另一方面,在转基因小鼠肝细胞(tamh)的培养物中,氧化电位与细胞毒性之间没有相关性.这些结果支持了氟吡汀的氧化代谢产物有助于作用机理的想法,类似于最近对乙酰氨基酚(对乙酰氨基酚)的提议,但对肝毒性没有影响.
DOI:10.1002/cmdc.201402442

专利信息

专利号:US-7186709-B2
优先权日:2002-08-27
标 题:Dihydropyrancarboxamides and uses thereof
发明人：SCHREIBER STUART L; STAVENGER ROBERT A; MITCHISON TIMOTHY J; MALIGA ZOLTAN
权利人:HARVARD COLLEGE
摘要:The present invention provides novel dihydropyrancarboxamide compounds of formula (I): n nand collections of these compounds, and provides methods for the synthesis of these compounds; wherein R 1 –R 6 are as defined herein. Additionally, the present invention provides pharmaceutical compositions and methods for treating disorders such as proliferative diseases, and cancer, to name a few.

专利号:US-10017481-B2
优先权日:2012-03-17
标 题 :Conformationally constrained, fully synthetic macrocyclic compounds
发明人：OBRECHT DANIEL; ERMERT PHILIPP; OUMOUCH SAID; PIETTRE ARNAUD; GOSALBES JEAN-FRANÇOIS; THOMMEN MARC
权利人:POLYPHOR AG
摘要:The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.

专利号:US-10766863-B2
优先权日:2014-11-17
标 题 :Monocarboxylate transport modulators and uses thereof
发明人：SANDANAYAKA VINCENT; WU QIONG
权利人:NIROGYONE THERAPEUTICS INC
摘要:The invention generally relates to the field of monocarboxylate transport modulators, e.g., monocarboxylate transport inhibitors, and more particularly to new substituted-quinolone compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in treating, modulating, forestalling and/or reducing physiological conditions associated with monocarboxylate transport activity such as in treating cancer and other neoplastic disorders, inflammatory diseases, disorders of abnormal tissue growth and fibrosis including cardiomyopathy, obesity, diabetes, cardiovascular diseases, tissue and organ transplant rejection, and malaria.

专利号:US-8513241-B2
优先权日:2008-03-28
标题 :3,4-dihydro-2H-pyrazino[1,2-A]indol-1-one derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them
发明人：CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; SALOM BARBARA
权利人:CERVI GIOVANNI; D ANELLO MATTEO; PAPEO GIANLUCA MARIANO ENRICO; SALOM BARBARA; NERVIANO MEDICAL SCIENCES SRL
摘要:Compounds which are 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them.

专利号:RU-2119482-C1
优先权日:1991-01-11
标 题:Acridine derivatives, method of synthesis, pharmaceutical composition and a method of treatment of patients with malignant tumors

专利号:WO-2012069442-A1
优先权日:2010-11-23
标题 :Diphenyl-amine derivatives: uses, process of synthesis and pharmaceutical compositions