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    • 3. 发明申请
    • BENZYLAMINE DERIVATIVES, THEIR PREPARATION AND THEIR APPLICATION IN THERAPEUTICS
    • 苯甲酰胺衍生物,其制备及其在治疗中的应用
    • WO1998008834A1
    • 1998-03-05
    • PCT/FR1997001514
    • 1997-08-22
    • SYNTHELABOPHILIPPO, ChristopheORTS, Marie-ClaireCRESPIN, OlivierBOVY, Philippe
    • SYNTHELABO
    • C07D307/79
    • C07D307/79
    • Compounds of general formula (I) in which: A represents either one hydrogen atom, one hydroxyl, one C1-6 hydroxyalkyl group, one thiol, one C1-6 alkylsulphanyl group, one amine group, one C1-6 alkylamine group, one di (C1-6 alkyl) amine group, one C1-6 alkyl hydroxylamine group, one C1-6 alcoxy group, one hydroxylamine group, one C1-6 N, O-dialkyl hydroxylamine group, one azide, one halogen such as fluorine, chlorine or bromine, B represents one hydrogen atom, one C1-6 alkyl, branched or linear, one C2-6 alkenyl group, one C1-6 fluoroalkyl group, one C1-2 perfluoroalkyl group, one C1-6 alcoxy group, one phenyl group, or one oxo group, X represents one oxygen or sulphur atom. The invention is useful in therapeutics.
    • 通式(I)的化合物,其中:A表示一个氢原子,一个羟基,一个C1-6羟烷基,一个硫醇,一个C1-6烷基硫烷基,一个胺基,一个C1-6烷基胺基,一个二 (C 1-6烷基)胺基,一个C 1-6烷基羟胺基,一个C 1-6烷氧基,一个羟胺基,一个C 1-6 N,O-二烷基羟胺基,一个叠氮化物,一个卤素如氟,氯 或溴,B表示一个氢原子,一个C 1-6烷基,支链或直链,一个C 2-6烯基,一个C 1-6氟烷基,一个C 1-2全氟烷基,一个C 1-6烷氧基,一个苯基 ,或一个氧代基,X表示一个氧或硫原子。 本发明在治疗中是有用的。
    • 4. 发明申请
    • 2-AMINOETHYL-BENZOFURAN DERIVATIVES, PREPARATION THEREOF AND THERAPEUTICAL USE THEREOF
    • 2-氨基乙基苯并呋喃衍生物,其制备方法及其治疗用途
    • WO1997032870A1
    • 1997-09-12
    • PCT/FR1997000383
    • 1997-03-05
    • SYNTHELABOPHILIPPO, ChristopheCOURTEMANCHE, GillesFETT, EykmarORTS, Marie, ClaireBOVY, PhilippeO'CONNOR, Stephen, EricGALZIN, Anne, Marie
    • SYNTHELABO
    • C07D307/79
    • C07D307/79
    • Compounds of formula (I), wherein A is a hydrogen atom or a hydroxyl group; B is a hydrogen atom or a C1-8 alkyl, C1-8 alkenyl, C1-8 fluoroalkyl or C1-8 perfluoroalkyl group; each of R1, R2 and R5, which are the same or different, is a hydrogen atom, a halogen such as chlorine, bromine or fluorine, a C1-8 alkyl, C1-8 alkenyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, C6, C10 or C14 aryl, C1-6 alkoxycarbonyl, C1-6 hydroxyalkyl, C1-6 alkoxyalkyl, C1-6 alkoxy, C1-8 fluoroalkyl or C1-8 perfluoroalkyl group, or R1 and R2 taken together form a C3-8 cycloalkyl, C3-8 cycloalkenyl or C6, C10 or C14 aryl ring, except for compounds in which R1 and R2 are both hydrogen; each of R3 and R4, which are the same or different, is a hydrogen atom or a C1-8 alkyl, C1-8 alkenyl, C3-8 cycloalkyl or C3-8 cycloalkenyl group, or R3 and R4 taken together form a C2-6 cycloalkyl or C3-6 cycloalkenyl ring, e.g. piperidyl, azetidinyl or pyrrolidyl; in the form of enantiomers, diastereoisomers or mixtures thereof, including racemic mixtures, as well as pharmaceutically acceptable acid addition salts thereof, are disclosed. The compounds may be used in therapy.
    • 式(I)的化合物,其中A是氢原子或羟基; B是氢原子或C 1-8烷基,C 1-8烯基,C 1-8氟烷基或C 1-8全氟烷基; R 1,R 2和R 5各自相同或不同,为氢原子,卤素如氯,溴或氟,C 1-8烷基,C 1-8烯基,C 3-8环烷基,C 3-8环烯基 ,C 6,C 10或C 14芳基,C 1-6烷氧基羰基,C 1-6羟基烷基,C 1-6烷氧基烷基,C 1-6烷氧基,C 1-8氟代烷基或C 1-8全氟烷基,或者R 1和R 2一起形成C 3-8 环烷基,C3-8环烯基或C6,C10或C14芳基环,其中R1和R2均为氢的化合物; R 3和R 4各自相同或不同,为氢原子或C 1-8烷基,C 1-8烯基,C 3-8环烷基或C 3-8环烯基,或者R 3和R 4一起形成C2- 6环烷基或C 3-6环烯基环,例如 哌啶基,氮杂环丁烷基或吡咯烷基; 公开了其对映异构体,非对映异构体或其混合物的形式,包括外消旋混合物,以及其药学上可接受的酸加成盐。 该化合物可用于治疗。