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    • 6. 发明授权
    • 4-phenyl-1-piperazinyl, -piperidinyl and -tetrahydropyridyl derivatives
    • 4-苯基-1-哌嗪基,哌啶基和四氢吡啶基衍生物
    • US07074796B2
    • 2006-07-11
    • US10186339
    • 2002-06-27
    • Benny Bang-AndersenJan KehlerJakob Felding
    • Benny Bang-AndersenJan KehlerJakob Felding
    • A61K31/496C07D403/06
    • C07D215/227C07D209/08C07D209/30C07D217/06C07D295/073
    • The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I wherein W is C, CH or N, and the dotted line emanating from W indicates a bond when W is C and no bond when W is N or CH; R1 and R2 are independently selected from hydrogen and halogen, provided at least one of R1 and R2 is a halogen atom; R3 is selected from hydrogen, halogen, C1-6 alkyl, trifluoromethyl, C1-6 alkoxy, aryloxy, aralkoxy, hydroxy, amino, C1-6 alkylamino, di(C1-6 alkyl)amino, nitro and cyano n is 2, 3, 4 or 5; X is CH2, O, S, CO, CS, SO or SO2; and Q is a group of formula wherein Z is a chain of 3 to 4 chain members; wherein the chain members are selected from C, CH, CH2, CO, N and NH, provided that only one of the chain members may be N or NH, and said chain optionally containing one or two double bonds; hvad med acyl?? R4, R5, R6, R7, R8, R9 and R10 are independently selected from hydrogen, halogen, C1-6 alkyl, trifluoromethyl, C1-6 alkoxy, hydroxy, amino, C1-6 alkylamino, di(C1-6 alkyl)amino nitro and cyano; provided that X is not O or S when the group Q is attached via an N atom; and any of its enantiomers and acid addition salts thereof. These compounds have high affinity for D4 receptors.
    • 本发明涉及具有式I的取代的4-苯基-1-哌嗪基衍生物,其中W是C,CH或N,当W是C时,由W发出的虚线表示键,当W是N或CH时,没有键 ; R 1和R 2独立地选自氢和卤素,条件是R 1和R 2中的至少一个和/或 >是卤原子; R 3选自氢,卤素,C 1-6烷基,三氟甲基,C 1-6烷氧基,芳氧基,芳烷氧基,羟基, 氨基,C 1-6烷基氨基,二(C 1-6烷基)氨基,硝基和氰基n为2,3,4或5; X是CH 2,O,S,CO,CS,SO或SO 2; Q为下式的基团,其中Z为3至4个链成员的链; 其中链成员选自C,CH,CH 2,CO,N和NH,条件是链中只有一个可以是N或NH,并且所述链任选地含有一个或两个双 债券 hvad med acyl? R 4,R 5,R 6,R 7,R 8, R 9和R 10独立地选自氢,卤素,C 1-6烷基,三氟甲基,C 1-6烷基, 羟基,氨基,C 1-6烷基氨基,二(C 1-6烷基)氨基硝基和氰基; 条件是当基团Q经由N原子连接时,X不为O或S; 及其任何对映异构体及其酸加成盐。 这些化合物对D 4 S受体具有高亲和力。
    • 7. 发明授权
    • Indole Derivatives useful for the treatment of CNS disorders
    • 吲哚衍生物可用于治疗CNS疾病
    • US06743809B2
    • 2004-06-01
    • US10347574
    • 2003-01-17
    • Jakob FeldingBenny Bang-AndersenGarrick Paul SmithKim Andersen
    • Jakob FeldingBenny Bang-AndersenGarrick Paul SmithKim Andersen
    • A61K31454
    • C07D401/04C07D401/14C07D405/14C07D409/14C07D417/14
    • The present invention relates to substituted indole derivatives of formula I wherein R1 is hydrogen or optionally substituted C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl or C3-8-cycloalkyl-C1-6-alkyl, or R1 is optionally substituted aryl, aryl-C1-6-alkyl, heteroaryl, heteroaryl-C1-6-alkyl or R1 is —NR′R″ wherein R′ and R″ are independently selected from hydrogen and optionally substituted C1-6-alkyl, aryl, aryl-C1-6-alkyl, heteroaryl and heteroaryl-C1-6-alkyl, or R1 is a saturated or partially saturated 5- to 6-membered ring containing one, two or three hetero atoms selected from O or S, and a group N—R9 wherein R9 is hydrogen or optionally substituted C1-6-alkyl; R2 is C1-6-alkyl W, n, X, R3-R8 are as defined in the description. The compounds of the invention are potent dopamine D4 ligands.
    • 本发明涉及式I的取代的吲哚衍生物,其中R 1是氢或任选取代的C 1-6 - 烷基,C 2-6烯基,C 2-6 - 炔基,C 3-8 - 环烷基或C 3-8 - C 1-6 - 烷基或R 1是任选取代的芳基,芳基-C 1-6 - 烷基,杂芳基,杂芳基-C 1-6 - 烷基或R 1是-NR'R“,其中R'和R “独立地选自氢和任选取代的C 1-6 - 烷基,芳基,芳基-C 1-6 - 烷基,杂芳基和杂芳基-C 1-6 - 烷基,或R 1是饱和或部分饱和的5-至 含有一个,两个或三个选自O或S的杂原子的6元环和NR 9基团,其中R 9是氢或任选取代的C 1-6 - 烷基; R 2是C 1-6 - 烷基W,n,X,R 3 -R 8如说明书中所定义。本发明的化合物是有效的多巴胺D4配体。