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    Heterocyclic aminoalkylpyridine derivatives as psychopharmaceuticals
    9.
    发明授权
    Heterocyclic aminoalkylpyridine derivatives as psychopharmaceuticals 失效
    杂环氨基烷基吡啶衍生物作为心理药物

    公开(公告)号：US06960599B2

    公开(公告)日：2005-11-01

    申请号：US10311286

    申请日：2001-06-19

    申请人： Dieter Dorsch ,  Henning Boettcher ,  Michael Arlt ,  Christoph Seyfried ,  Gerd Bartoszyk ,  Juergen Harting ,  Rudolf Gottschlich

    发明人： Dieter Dorsch ,  Henning Boettcher ,  Michael Arlt ,  Christoph Seyfried ,  Gerd Bartoszyk ,  Juergen Harting ,  Rudolf Gottschlich

    IPC分类号： A61K31/443 ,  A61K31/4433 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/4725 ,  A61P5/00 ,  A61P5/06 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P15/08 ,  A61P15/10 ,  A61P15/12 ,  A61P25/00 ,  A61P25/06 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P43/00 ,  C07D213/38 ,  C07D213/64 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12 ,  C07D401/02 ,  A61K31/44 ,  A61K31/47

    CPC分类号： C07D213/64 ,  C07D213/38 ,  C07D401/12 ,  C07D405/12 ,  C07D417/12

    摘要： The invention relates to heterocyclic aminoalkylpyridine derivatives of the formula I: where R1 is the radical of a heterocycle having 1 to 3 ring structures, where each ring structure is saturated, unsaturated or aromatic and optionally fused to other ring structures to give a fused ring system and the heterocycle has a total of 1 to 4 N, O and/or S atoms in the ring structures and is optionally monosubstituted, disubstituted or trisubstituted by one or more of the groups -A, —OR4, —N(R4)2, —NO2, —CN, Hal, —COOR4, —CON(R4)2, —COR4, ═O; R2 is a phenyl group which is optionally monosubstituted, disubstituted, trisubstituted, tetrasubstituted or pentasubstituted by one or more of the groups Hal, -A, —O-A, —NO2 or —CN, or is a thienyl group which is optionally monosubstituted or disubstituted by one or more of the groups Hal, -A, —O-A, -NO2, —CN or thienyl; R3 is H, -A, —CO-A, —C(R4)2R2, —C(R4)2-pyridinediyl-R2; R4 is H or -A; A is C1-C6-alkyl, where 1 to 7 hydrogen atoms are optionally replaced by fluorine; —X— is —O—, —S—, sulfinyl, sulfonyl, —C(R4)2—; —Y— is —[C(R4)2]n—; —Z— is —C(R4)2—; Hal is F, Cl, Br or I; n is 1, 2, 3 or 4; and their tolerable salts and solvates and their use as medicaments.

    摘要翻译： 本发明涉及式I的杂环氨基烷基吡啶衍生物：其中R 1是具有1至3个环结构的杂环的基团，其中每个环结构是饱和的，不饱和的或芳族的并且任选地与其它 环结构以得到稠环体系，并且杂环在环结构中总共具有1至4个N，O和/或S原子，并且任选被一个或多个基团-A，-OR单取代，二取代或三取代 -N（R 4）2，-NO 2，-CN，Hal，-COOR 2， -CON（R 4）2，-SOR 4，-O; R 2是一个苯基，其任选被一个或多个Hal，-A，-OA，-NO 2基团单取代，二取代，三取代，四取代或五取代。 或-CN，或者是任选被一个或多个Hal，-A，-OA，-NO 2，-CN或噻吩基团单取代或二取代的噻吩基; R 3是H，-A，-CO-A，-C（R 4）2 R 2， ，-C（R 4）2 - 吡啶二基-R 2; R 4是H或-A; A为C 1 -C 6 - 烷基，其中1至7个氢原子任选被氟取代; -X-是-O - ， - S-，亚磺酰基，磺酰基，-C（R 4）2 - 。 -Y-是 - [C（R 4）2）n - -Z-是-C（R 4）2 - ; - Hal是F，Cl，Br或I; n为1,2,3或4; 及其可耐受的盐和溶剂合物及其作为药物的用途。

    Substituted benzofuran-2-carboxamides derivatives
    10.
    发明授权
    Substituted benzofuran-2-carboxamides derivatives 失效
    取代的苯并呋喃-2-甲酰胺衍生物

    公开(公告)号：US07244846B2

    公开(公告)日：2007-07-17

    申请号：US10471584

    申请日：2002-02-27

    申请人： Dieter Dorsch ,  Henning Boettcher ,  Christoph van Amsterdam ,  Wilfried Rautenberg ,  Gerd Bartoszyk

    发明人： Dieter Dorsch ,  Henning Boettcher ,  Christoph van Amsterdam ,  Wilfried Rautenberg ,  Gerd Bartoszyk

    IPC分类号： A61K31/495 ,  C07D405/10

    CPC分类号： C07D405/12

    摘要： Compounds of the formula (I), in which D, R1, R2 and n are defined in Claim 1, are potent 5-HT1A agonists and 5-HT reuptake inhibitors and are suitable for the treatment of depression, anxiety states, panic attacks, obsessive-compulsive disorders, psychiatric illnesses, cerebral infarction, cerebral ischaemia, tension states, side-effects in the treatment of high blood pressure, for the prophylaxis and therapy of cerebral illnesses, acromegaly, hypogonadism, secondary amenorrhoea, premenstrual syndrome, undesired puerperal lactation, pain, sleep disorders, narcolepsy, bipolar illnesses, mania, dementia, addiction illnesses, sexual dysfunction, eating disorders, obesity or fibromyalgia

    摘要翻译： 其中D，R 1，R 2和n在权利要求1中定义的式（I）化合物是有效的5-HT 1A， SUB +激动剂和5-HT再摄取抑制剂，适用于治疗抑郁症，焦虑症，恐慌发作，强迫症，精神疾病，脑梗塞，脑缺血，紧张状态，高血压治疗中的副作用 压力，用于预防和治疗脑疾病，肢端肥大症，性腺机能减退，继发性闭经，经前期综合征，不期望的产后泌乳，疼痛，睡眠障碍，发作性睡眠，双相性疾病，躁狂症，痴呆，成瘾症，性功能障碍，进食障碍，肥胖症或 纤维肌痛