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    • 1. 发明申请
    • TRIAZABENZO (A)NAPHTHO(2,1,8-CDE) AZULENE COMPOUNDS.
    • 三氮杂萘(A)萘(2,1,8-CDE)亚苄基化合物。
    • US20100105666A1
    • 2010-04-29
    • US12448627
    • 2008-01-04
    • Jean-Daniel BrionMaud HervetAnne MoreauZafiarisoa Dolor RenkoAlain Le RidantCatherine Harpey
    • Jean-Daniel BrionMaud HervetAnne MoreauZafiarisoa Dolor RenkoAlain Le RidantCatherine Harpey
    • A61K31/551C07D487/22A61P25/22A61P25/16A61P25/24
    • C07D471/22
    • Compounds of formula (I): wherein: R1 represents hydrogen, (C1-C6)alkyl, (C1-C6)aminoalkyl or (C1-C6)hydroxyalkyl, R2 represents hydrogen, or R1 and R2, together with the carbon atoms carrying them, form a carbon-carbon bond, R3 represents hydrogen, R4 represents hydrogen, methyl or (C3-C6)alkyl, (C1-C6)aminoalkyl, (C1-C6)hydroxyalkyl, aryl-(C1-C6)alkyl or heterocycloalkyl-(C1-C6)alkyl, or R3 and R4 together with the carbon atoms carrying them, form a carbon-carbon bond, R5, R6, R7 and R8 represent hydrogen, or a pair of geminal substituents (R5 and R6 and/or R7 and R8) form an oxo, thioxo or imino group, R9 represents hydrogen, halogen, (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, cyano, nitro, (C1-C6)polyhaloalkyl or optionally substituted amino, R10 and R11 represent hydrogen, halogen, (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, cyano, nitro, (C1-C6)polyhaloalkyl or optionally substituted amino, n represents an integer between 0 and 4 inclusive, m represents an integer between 0 and 2 inclusive, p represents an integer between 0 and 3 inclusive, X represents a group NR12, R12 represents hydrogen, (C1-C6)alkyl, (C2-C6)alkenyl, aryl-(C1-C6)alkyl or (C1-C6)polyhaloalkyl, their enantiomers, diastereoisomers and N-oxides, and also addition salts thereof with a pharmaceutically acceptable acid or base.
    • 式(I)化合物:其中:R1表示氢,(C1-C6)烷基,(C1-C6)氨基烷基或(C1-C6)羟基烷基,R2表示氢,或R1和R2以及携带它们的碳原子 (C 1 -C 6)烷基,(C 1 -C 6)羟基烷基,芳基 - (C 1 -C 6)烷基或杂环烷基 - (C 1 -C 6) (C1-C6)烷基或R3和R4与携带它们的碳原子一起形成碳 - 碳键,R5,R6,R7和R8表示氢或一对偕取代基(R5和R6和/或R7 卤素,(C1-C6)烷基,(C1-C6)烷氧基,羟基,氰基,硝基,(C1-C6)多卤代烷基或任意取代的氨基,R10 并且R 11表示氢,卤素,(C 1 -C 6)烷基,(C 1 -C 6)烷氧基,羟基,氰基,硝基,(C 1 -C 6)多卤代烷基或任选取代的氨基,n表示0至4的整数, 0和2之间的整数,包括0和2, p表示0〜3的整数,X表示NR12,R12表示氢,(C1-C6)烷基,(C2-C6)烯基,芳基 - (C1-C6)烷基或(C1-C6)多卤代烷基, 它们的对映异构体,非对映异构体和N-氧化物,以及其与药学上可接受的酸或碱的加成盐。
    • 9. 发明授权
    • Beta-carboline compounds
    • β-咔啉化合物
    • US06350757B1
    • 2002-02-26
    • US09621742
    • 2000-07-21
    • Solo GoldsteinGuillaume PoissonnetJean-Gilles ParmentierJean-Daniel BrionMark MillanAnne DekeyneJean Boutin
    • Solo GoldsteinGuillaume PoissonnetJean-Gilles ParmentierJean-Daniel BrionMark MillanAnne DekeyneJean Boutin
    • C07D47114
    • C07D471/04
    • A compound selected from those of formula (I): wherein: represents single or double bond, R1 represents hydrogen, alkyl, —R6-aryl, —R6-cycloalkyl, —R6-heterocycle, —CO2R7—, —COR8, or —CONHR8, wherein R6, R7, and R8 are as defined in the description, R2 represents cyano, mono- or di-alkylaminoalkylaminocarbonyl, —CO2R8, —CONHR8, —NR8R9, —NHCO2R7, or —COR8 wherein R7, R8, and R9 are as defined in the description, R3 and R4 together form (C3-C10)cycloalkyl, R5 represents hydrogen, alkyl, or arylalkyl, Ra, Rb, Rc, Rd, which may be identical or different, represent a group as defined in the description, its isomers, and pharmaceutically-acceptable acid or base addition salts thereof, and medicinal products containing the same which are useful in the treatment of CNS disorders.
    • 选自式(I)的化合物:其中:CUSTOM-CHARACTER FILE =“US06350757-20020226-P00900.TIF”ID =“CUSTOM-CHARACTER-00001”>表示单键或双键,R1表示氢,烷基, -R6-芳基,-R6-环烷基,-R6-杂环,-CO2R7-,-COR8或-CONHR8,其中R6,R7和R8如说明书中所定义,R 2表示氰基,单或二烷基氨基烷基氨基羰基 ,-CO 2 R 8,-CONHR 8,-NR 8 R 9,-NHCO 2 R 7或-COR 8,其中R 7,R 8和R 9如说明书中所定义,R 3和R 4一起形成(C 3 -C 10)环烷基,R 5表示氢,烷基或芳烷基 可以相同或不同的R a,R b,R c,R d表示本说明书中定义的基团,其异构体及其药学上可接受的酸或碱加成盐,以及含有该基团的药物,其可用于 治疗中枢神经系统疾病。