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59 条记录 (耗时 0.044 秒)

    Pro-drugs of N-thiazol-2-yl-benzamide derivatives
    21.
    发明申请
    Pro-drugs of N-thiazol-2-yl-benzamide derivatives 失效
    N-噻唑-2-基 - 苯甲酰胺衍生物的前药

    公开(公告)号：US20060264485A1

    公开(公告)日：2006-11-23

    申请号：US11409884

    申请日：2006-04-24

    申请人： Anette Sams ,  Benny Bang-Andersen ,  Gitte Mikkelsen ,  Mogens Larsen

    发明人： Anette Sams ,  Benny Bang-Andersen ,  Gitte Mikkelsen ,  Mogens Larsen

    IPC分类号： A61K31/426

    CPC分类号： C07D277/46 ,  C07D417/12

    摘要： The invention relates to compounds of the formula I A-B-Z   I wherein the variables are as defined in the claims. The compounds are pro-drugs of A2A-receptor ligands with improved aqueous solubility, and are useful in the treatment of neurological and psychiatric disorders where an A2A-receptor is implicated.

    摘要翻译： 本发明涉及式I的化合物<？in-line-formula description =“In-line Formulas”end =“lead”？> ABZ I <？in-line-formula description =“In-line Formulas”end = “尾”→其中变量如权利要求中所定义。 这些化合物是具有改善的水溶性的A 2AA-受体配体的前药，并且可用于治疗其中涉及2A2受体的神经和精神障碍 。

    4-, 5-, 6- and 7-indole derivatives useful for the treatment of CNS disorders
    27.
    发明授权
    4-, 5-, 6- and 7-indole derivatives useful for the treatment of CNS disorders 失效

    公开(公告)号：US07105543B2

    公开(公告)日：2006-09-12

    申请号：US11219544

    申请日：2005-09-01

    申请人： Benny Bang-Andersen ,  Jan Kehler

    发明人： Benny Bang-Andersen ,  Jan Kehler

    IPC分类号： A61K31/4439 ,  A61K31/454 ,  C07D401/06

    CPC分类号： C07D401/06 ,  C07D209/08 ,  C07D405/12

    摘要： The present invention relates to 4-, 5-, 6- or 7-methylene substituted indolyl derivatives of formula I wherein R is aryl or heteroaryl, where said aryl or heteroaryl groups may be substituted one or more times with a substituent seleceted from hydrogen, halogen, cyano, nitro, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, C1-6-alkoxy, C1-6-alkylthio, hydroxy, hydroxy-C1-6-alkyl trifluoromethyl, trifluoromethylsulfonyl, C1-6-alkylsulfonyl, amino, C1-6-alkylamino, di-(C1-6-alkyl)amino, acyl, aminocarbonyl and a methylene dioxy group; X is N, C or CH; provided that the dotted line indicates a bond when X is C and no bond when X is N or CH; R1 is hydrogen, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C 1-6-alkyl, aryl, aryl-C1-6-alkyl, acyl, thioacyl, C1-6-alkylsulfonyl, trifluoromethylsulfonyl or arylsulfonyl; and R2 and R3 are independently selected from hydrogen, halogen, cyano, nitro, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, C1-6-alkoxy, C1-6-alkylthio, hydroxy, hydroxy-C1-6-alkyl trifluoromethyl, trifluoromethylsulfonyl, C1-6-alkylsulfonyl, amino, C1-6-alkylamino, di-(C1-6-alkyl)amino, acyl and aminocarbonyl. The compounds of the invention are selective dopamine D4 ligands.

    4-phenyl-1-piperazinyl, -piperidinyl and -tetrahydropyridyl derivatives
    28.
    发明授权
    4-phenyl-1-piperazinyl, -piperidinyl and -tetrahydropyridyl derivatives 失效
    4-苯基-1-哌嗪基，哌啶基和四氢吡啶基衍生物

    公开(公告)号：US07074796B2

    公开(公告)日：2006-07-11

    申请号：US10186339

    申请日：2002-06-27

    申请人： Benny Bang-Andersen ,  Jan Kehler ,  Jakob Felding

    发明人： Benny Bang-Andersen ,  Jan Kehler ,  Jakob Felding

    IPC分类号： A61K31/496 ,  C07D403/06

    CPC分类号： C07D215/227 ,  C07D209/08 ,  C07D209/30 ,  C07D217/06 ,  C07D295/073

    摘要： 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.

    摘要翻译： 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。