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23 条记录 (耗时 0.021 秒)

    Di-or triaza-spiro [4,5] decane derivatives
    1.
    发明授权
    Di-or triaza-spiro [4,5] decane derivatives 失效
    二 - 或三氮杂螺[4,5]癸烷衍生物

    公开(公告)号：US06642247B2

    公开(公告)日：2003-11-04

    申请号：US09330724

    申请日：1999-06-11

    申请人： Geo Adam ,  Andrea Cesura ,  François Jenck ,  Sabine Kolczewski ,  Stephan Röver ,  Jürgen Wichmann

    发明人： Geo Adam ,  Andrea Cesura ,  François Jenck ,  Sabine Kolczewski ,  Stephan Röver ,  Jürgen Wichmann

    IPC分类号： A61K31438

    CPC分类号： C07D471/10 ,  C07D513/10

    摘要： The present invention relates to compounds of the general formula wherein R1 is C6-10-cycloalkyl, optionally substituted by lower alkyl or —C(O)O-lower alkyl; decahydro-naphthalen-1-yl; decahydro-naphthalen-2-yl; indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; decahydro-azulen-2-yl; bicyclo[6.2.0]dec-9-yl; acenaphthen-1-yl; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl or octahydro-inden-2-yl; R2 is hydrogen; lower alkyl; ═O or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; is cyclohexyl or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; X is —CH(OH)—; —C(O)—; —CHR3—; —CR3═; —O—; —S—; —CH(COOR4)— or C(COOR4)═; Y is —CH2—; —CH═; —CH(COOR4)—, —C(COOR4)═; or —C(CN)—; R3 is hydrogen or lower alkoxy; R4 is lower alkyl, cycloalkyl, phenyl, or benzyl and either a or b is optionally an additional bond, and to pharmaceutically acceptable acid addition salts thereof. The compounds are agonists of the orphanin FQ (QFQ) receptor and therefore useful in the treatment of diseases, related to this receptor.

    摘要翻译： 本发明涉及通式化合物R 1的化合物是任选被低级烷基或-C（O）O-低级烷基取代的C 6-10 - 环烷基; 十氢萘-1-基; 十氢萘-2-基; 茚满-1-基或茚满-2-基，任选被低级烷基取代; 十氢 - 薁-2-基; 双环[6.2.0]癸-9-基; 苊-1-基; 2,3-二氢-1H-苯并芬-1-基; 2,3,3a，4,5,6-六氢-1H-吩酚-1-基或八氢 - 茚-2-基; R 2是氢; 低级烷基 任选被低级烷基，卤素或烷氧基取代的O或苯基;是任选被低级烷基，卤素或烷氧基取代的环己基或苯基; X是-CH（OH） - ; -C（O） - ; -CHR 3 - ; -CR 3 = -O-; -S-; -CH（COOR 4） - 或C（COOR 4）=; Y是-CH 2 - ; -CH =; -CH（COOR 4） - ， - C（COOR 4）=; 或-C（CN） - ; R 3是氢或低级烷氧基; R 4是低级烷基，环烷基，苯基或苄基，a或b任选是另外的键，以及其药学上可接受的酸加成盐 该化合物是孤儿素FQ（QFQ）受体的激动剂，因此可用于治疗与该受体有关的疾病。

    Di-or triaza-spiro [4,5] decane derivatives
    4.
    发明授权
    Di-or triaza-spiro [4,5] decane derivatives 有权

    公开(公告)号：US06172075B2

    公开(公告)日：2001-01-09

    申请号：US09330724

    申请日：1999-06-11

    申请人： Geo Adam ,  Andrea Cesura ,  François Jenck ,  Sabine Kolczewski ,  Stephan Röver ,  J{umlaut over (u)}rgen Wichmann

    发明人： Geo Adam ,  Andrea Cesura ,  François Jenck ,  Sabine Kolczewski ,  Stephan Röver ,  J{umlaut over (u)}rgen Wichmann

    IPC分类号： A61K31438

    摘要： The present invention relates to compounds of the general formula wherein R1 is C6-10-cycloalkyl, optionally substituted by lower alkyl or —C(O)O-lower alkyl; decahydro-naphthalen-1-yl; decahydro-naphthalen-2-yl; indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; decahydro-azulen-2-yl; bicyclo[6.2.0]dec-9-yl; acenaphthen-1-yl; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl or octahydro-inden-2-yl; R2 is hydrogen; lower alkyl; ═O or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; {circumflex over (A)} is cyclohexyl or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; X is —CH(OH)—; —C(O)—; —CHR3—; —CR3═; —O—; —S—; —CH(COOR4)— or —C(COOR4)—; Y is —CH2—; —CH═; —CH(COOR4)—, —C(COOR4)═; or —C(CN)—; R3 is hydrogen or lower alkoxy; R4 is lower alkyl, cycloalkyl, phenyl, or benzyl and either a or b is optionally an additional bond, and to pharmaceutically acceptable acid addition salts thereof. The compounds are agonists of the orphanin FQ (QFQ) receptor and therefore useful in the treatment of diseases, related to this receptor.

    Dihydro-benzo [b][1,4]diazepin-2-one derivatives
    10.
    发明授权
    Dihydro-benzo [b][1,4]diazepin-2-one derivatives 失效
    二氢 - 苯并[b] [1,4]二氮杂-2-酮衍生物

    公开(公告)号：US06544985B2

    公开(公告)日：2003-04-08

    申请号：US10115826

    申请日：2002-04-03

    申请人： Geo Adam ,  Erwin Goetschi ,  Vincent Mutel ,  Juergen Wichmann ,  Thomas Johannes Woltering

    发明人： Geo Adam ,  Erwin Goetschi ,  Vincent Mutel ,  Juergen Wichmann ,  Thomas Johannes Woltering

    IPC分类号： C07D24312

    CPC分类号： C07D401/04 ,  C07D403/10 ,  C07D403/14 ,  C07D417/10

    摘要： This invention is a dihydro-benzo[b][1,4]diazepin-2-one derivative of the formula wherein R1, R2, R3, X and Y are as defined in the specification. The invention includes pharmaceutical compositions containing these compounds, a process for their preparation, their use in preparation of pharmaceutical compositions and administration of an effective amount of the compounds for the treatment or prevention of acute and/or chronic neurological disorders to a patient in need of such treatment.

    摘要翻译： 本发明是公式R 2，R 2，R 3，X和Y的二氢 - 苯并[b] [1,4]二氮杂-2-酮衍生物，如说明书中所定义。 本发明包括含有这些化合物的药物组合物，它们的制备方法，它们在制备药物组合物中的用途以及有效量的用于治疗或预防急性和/或慢性神经障碍的化合物给需要 这样的治疗。