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New spirocyclic cyclohexane derivatives useful for treating pain, depression, urinary incontinence, diarrhea, pruritis, alcohol and drug abuse, medicament dependence, lack of drive and/or anxiety

机译：新的螺环环己烷衍生物，可用于治疗疼痛，抑郁，尿失禁，腹泻，瘙痒，酒精和药物滥用，药物依赖性，缺乏动力和/或焦虑

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Spirocyclic cyclohexane derivatives (I) are new. Spirocyclic cyclohexane derivatives of formula (I) and their isomers and salts are new. R 1, R 2H or (un)saturated 1-5C alkyl, but not both H, or R 1+R 2 is CH 2CH 2OCH 2CH 2, CH 2CH 2NR 11CH 2CH 2 or (CH 2) 3-6; R 11H or (un)saturated 1-5C alkyl or 3-8C cycloalkyl or aryl, heteroaryl, aryl(1-3C)alkyl, (3-8C)cycloalkyl(1-3C)alkyl or heteroaryl(1-3C)alkyl, all optionally substituted; R 3optionally substituted aryl, heteroaryl, aryl(1-3C)alkyl or heteroaryl(1-3C)alkyl; W' : NR 4, O or S; R 4H; (un)saturated 1-5C alkyl or aryl, heteroaryl, aryl(1-3C)alkyl, cycloalkyl(1-3C)alkyl or heteroaryl(1-3C)alkyl, all optionally substituted; or COR 12, CSR 12 or SO 2R 12; R 12H; (un)saturated 1-5C alkyl or 3-8C cycloalkyl or aryl, heteroaryl, aryl(1-3C)alkyl, (3-8C)cycloalkyl(1-3C)alkyl or heteroaryl(1-3C)alkyl, all optionally substituted; OR 13 or NR 14R 15; R 5H; (un)saturated 1-5C alkyl or 3-8C cycloalkyl or aryl, heteroaryl, aryl(1-3C)alkyl, (3-8C)cycloalkyl(1-3C)alkyl or heteroaryl(1-3C)alkyl, all optionally substituted; COOR 13, CONHR 13 or OR 13; R 6H, OR 13, COOR 13, COOR 13 or NR 14R 15; or (un)saturated 1-5C alkyl or 3-8C cycloalkyl or phenyl, aryl(1-3C)alkyl or heteroaryl(1-3C)alkyl, all optionally substituted; R 7-R 10H, F, Cl, Br, NO 2m CF 3, OR 13, CN, COOR 13, NR 14R 15, 1-5C alkyl, phenyl or benzyl; R 13H or (un)saturated 1-5C alkyl or 3-8C cycloalkyl or aryl, heteroaryl, aryl(1-3C)alkyl, (3-8C)cycloalkyl(1-3C)alkyl or heteroaryl(1-3C)alkyl, all optionally substituted; R 14, R 15 H or 1-5C alkyl or R 14+R 15is CH 2CH 2OCH 2CH 2, CH 2CH 2NR 16CH 2CH 2 or (CH 2) 3-6; R 16H or (un)saturated 1-5C alkyl; X : O, S, SO, SO 2 or NR 17; R 17H, optionally substituted (un)saturated 1-5C alkyl, COR 12 or SO 2R 12. Independent claims are also included for two processes for preparing (I). [Image] ACTIVITY : Analgesic; Antidepressant; Uropathic; Antidiarrheic; Antipruritic; Antialcoholic; Antiaddictive; Tranquilizer. MECHANISM OF ACTION : Noradrenaline reuptake inhibitor; Serotonin reuptake inhibitor. At a concentration of 10 mu M, 1,1-(3-(alpha -dimethylamino-3-fluorobenzyl)pentamethylene)-3,4-dihydro-1H-2,9-diazafluorene gave 58% inhibition of noradrenaline reuptake and 64% inhibition of serotonin reuptake.

机译：螺环环己烷衍生物（Ⅰ）是新的。式（I）的螺环环己烷衍生物及其异构体和盐是新的。 R 1>，R 2> H或（不）饱和1-5C烷基，但不同时为H或R 1> + R 2>为CH 2CH 2OCH 2CH 2，CH 2CH 2NR 11> CH 2CH 2或（CH 2 ）3-6; R 11> H或（不）饱和的1-5C烷基或3-8C环烷基或芳基，杂芳基，芳基（1-3C）烷基，（3-8C）环烷基（1-3C）烷基或杂芳基（1-3C）烷基，全部任选取代; R 3＞任选取代的芳基，杂芳基，芳基（1-3C）烷基或杂芳基（1-3C）烷基; W'：NR 4>，O或S; R 4> H; （un）饱和的1-5C烷基或芳基，杂芳基，芳基（1-3C）烷基，环烷基（1-3C）烷基或杂芳基（1-3C）烷基，所有这些均任选被取代;或COR 12>，CSR 12>或SO 2R 12>; R 12> H; （非）饱和的1-5C烷基或3-8C环烷基或芳基，杂芳基，芳基（1-3C）烷基，（3-8C）环烷基（1-3C）烷基或杂芳基（1-3C）烷基，均可选地被取代;或13>或NR 14> R 15>; R 5> H; （非）饱和的1-5C烷基或3-8C环烷基或芳基，杂芳基，芳基（1-3C）烷基，（3-8C）环烷基（1-3C）烷基或杂芳基（1-3C）烷基，均可选地被取代; COOR 13>，CONHR 13>或OR 13>; R 6> H，或13>，COOR 13>，COOR 13>或NR 14> R 15>;或（不）饱和的1-5C烷基或3-8C环烷基或苯基，芳基（1-3C）烷基或杂芳基（1-3C）烷基，它们全部是任选取代的; R 7> -R 10> H，F，Cl，Br，NO 2m CF 3或OR 13>，CN，COOR 13>，NR 14> R 15>，1-5C烷基，苯基或苄基; R 13> H或（不）饱和的1-5C烷基或3-8C环烷基或芳基，杂芳基，芳基（1-3C）烷基，（3-8C）环烷基（1-3C）烷基或杂芳基（1-3C）烷基，全部任选取代; R 14>，R 15> H或1-5C烷基或R 14> + R 15>为CH 2CH 2OCH 2CH 2，CH 2CH 2NR 16> CH 2CH 2或（CH 2）3-6; R 16> H或（不）饱和的1-5C烷基; X：O，S，SO，SO 2或NR 17>; R 17> H，任选地被取代的（不）饱和的1-5C烷基，COR 12>或SO 2R 12>。还包括两个准备过程（I）的独立权利要求。 [图片]活动：止痛药;抗抑郁药尿毒症;止泻药止痒;抗酒;反吸毒镇静剂。作用机理：去甲肾上腺素再摄取抑制剂;去甲肾上腺素。血清素再摄取抑制剂。当浓度为10μM时，1,1-（3-（α-二甲基氨基-3-氟苄基）五亚甲基）-3,4-二氢-1H-2,9-二氮杂芴具有58％的去甲肾上腺素再摄取抑制作用和64％抑制5-羟色胺再摄取。

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公开/公告号DE102006019597A1

专利类型
公开/公告日2007-10-31

原文格式PDF
申请/专利权人 GRUENENTHAL GMBH;
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申请/专利号DE20061019597
发明设计人 MERLA BEATRIX;OBERBOERSCH STEFAN;SUNDERMANN BERND;ENGLBERGER WERNER;HENNIES HAGEN-HEINRICH;KOEGEL BABETTE-YVONNE;GRAUBAUM HEINZ;
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申请日2006-04-27
分类号C07D491/052;C07D471/04;A61K31/407;A61K31/437;A61P29;A61P25;
国家 DE
入库时间 2022-08-21 20:29:19

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