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    • 1. 发明申请
    • BIS-2-AMINOPYRIDINES, PREPARATION METHOD THEREFOR AND USE THEREOF FOR CONTROLLING PARASITIC INFECTIONS
    • BIS-2-氨基吡啶,其制备方法及其用途,用于控制PARASITIC感染
    • WO1996011910A1
    • 1996-04-25
    • PCT/FR1995001349
    • 1995-10-13
    • LABORATOIRES VIRBACVIAL, HenriCALAS, MichèleBOURGUIGNON, Jean-JacquesANCELIN, Marie-LaureGIRAL, Louis
    • LABORATOIRES VIRBAC
    • C07D213/73
    • C07D213/73
    • Substituted bis-2-aminopyridines of general formula (I), wherein Q is a C6-20 alkyl grouping, an optionally substituted aryl grouping, or a cycloalkyl grouping, and forms, between the two pyridine rings, a hydrocarbon chain including 6-34 carbon atoms in all; n is a number from 0 to 7; and R1, R2, R3 and R4, which are the same or different, are a hydrogen atom, a straight or branched optionally substituted C1-6 alkyl grouping, an aryl grouping optionally substituted by one or more halogen atoms, or C1-6 alkyl or C1-6 alkoxy radicals, a benzyl grouping, a thienyl grouping, a furyl grouping, a halogen atom or an alkoxy or benzyloxy grouping, with the proviso that at least one of radicals R1, R2, R3 and R4 is not a hydrogen atom when Q is a (CH2)m chain wherein m is 6-20; and addition salts thereof. A method for preparing said substituted or unsubstituted bis-2-aminopyridines, and the use thereof as a drug and in particular as active drugs for controlling parasitic infections within red blood cells, e.g. malaria or babesiasis (or piroplasmosis), are also disclosed.
    • 取代的通式(I)的二-2-氨基吡啶,其中Q是C6-20烷基,任选取代的芳基或环烷基,并且在两个吡啶环之间形成包含6-34 全部碳原子; n是从0到7的数字; R 1,R 2,R 3和R 4相同或不同,为氢原子,直链或支链任选取代的C 1-6烷基,任选被一个或多个卤素原子取代的芳基,或C 1-6烷基 或C 1-6烷氧基,苄基,噻吩基,呋喃基,卤素原子或烷氧基或苄氧基,条件是基团R 1,R 2,R 3和R 4中的至少一个不是氢原子 当Q是(CH2)m链,其中m是6-20; 及其加成盐。 制备所述取代或未取代的双-2-氨基吡啶的方法及其作为药物的用途,特别是用于控制红细胞内的寄生虫感染的活性药物,例如, 疟疾或贝氏病(或卵母细胞瘤)也被公开。