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    Certain arylaliphatic and heteroaryl-aliphatic piperazinyl pyrazines and their use in the treatment of serotonin-related diseases
    4.
    发明授权
    Certain arylaliphatic and heteroaryl-aliphatic piperazinyl pyrazines and their use in the treatment of serotonin-related diseases 失效
    某些芳基脂族和杂芳基 - 脂族哌嗪基吡嗪及其在治疗5-羟色胺相关疾病中的应用

    公开(公告)号：US07534794B2

    公开(公告)日：2009-05-19

    申请号：US10269670

    申请日：2002-10-11

    申请人： Björn Nilsson ,  Jan Tejbrant ,  Benjamin Pelcman ,  Erik Ringberg ,  Markus Thor ,  Jonas Nilsson ,  Mattias Jönsson

    发明人： Björn Nilsson ,  Jan Tejbrant ,  Benjamin Pelcman ,  Erik Ringberg ,  Markus Thor ,  Jonas Nilsson ,  Mattias Jönsson

    IPC分类号： A61K31/50 ,  C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  C07D411/00 ,  C07D413/00 ,  C07D417/00 ,  C07D419/00

    CPC分类号： C07D401/12 ,  C07D241/18 ,  C07D241/20 ,  C07D403/12 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D491/04

    摘要： The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2—, —NH—, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R4)(R5)—, —OC(R4)(R5)—, —N(R6)C(R4)(R5)—, —N(R6)—, —O—, —S— or —SO2—; R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl; R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group —[C(R4)(R5)]xN(R2a)(R3a)]; R2a, R3a, R4, R5, R6 and x are as defined in the claims, and n is 0 or 1; and pharmaceutically acceptable salts, hydrates and prodrug forms thereof. The compounds may be prepared by per se conventional methods and can be used for treating a human or animal subject suffering from a serotonin-related disorder, such as eating disorders, especially obesity, memory disorders, schizophrenia, mood disorders, anxiety disorders, pain, sexual dysfunctions, and urinary disorders The invention also relates to such use as well as to pharmaceutical compositions comprising a compound of formula (I).

    摘要翻译： 本发明涉及通式（I）的化合物：其中Ar为任选取代的芳基或杂芳基; A是（ⅰ）-O - ， - S - ， - SO 2 - ， - NH - ，（ⅱ）C 1-4 - 烷基 - 或C 1-6 - 酰基取代的氮原子或（ⅲ） 亚烷基链或具有2至8个链原子的杂亚烷基链，其任选地包含至少一个不饱和键，并且其可以被取代和/或含有桥以形成具有3-8个环成员的饱和或部分或完全不饱和的环; B是-C（R 4）（R 5） - ， - OC（R 4）（R 5） - ， - N（R 6） 或-SO 2 - ; R是任选取代的C 3-8 - 环烷基，芳基或杂芳基; R1是（i）饱和或不饱和的氮杂环或氨基氮杂环或饱和的二氮环或氨基二氮环，其具有4至7个环成员，或具有7至10个环成员的饱和氨基氮杂双环，氮杂双环或二氮杂双环，其任选地环 在一个或多个位置被取代，或基团 - [C（R 4）（R 5）] x N（R 2a）（R 3a）]; R2a，R3a，R4，R5，R6和x如权利要求中所定义，n为0或1; 及其药学上可接受的盐，水合物和前药形式。 化合物可以通过本身的常规方法制备，并且可以用于治疗患有5-羟色胺相关病症的人或动物受试者，例如进食障碍，特别是肥胖，记忆障碍，精神分裂症，情绪障碍，焦虑症，疼痛， 性功能障碍和尿失调本发明还涉及这样的用途以及包含式（I）化合物的药物组合物。

    Beta-carbolines as growth hormone secretagogue receptor (GHSR) antagonists
    5.
    发明申请
    Beta-carbolines as growth hormone secretagogue receptor (GHSR) antagonists 审中-公开
    β-咔啉作为生长激素促分泌素受体（GHSR）拮抗剂

    公开(公告)号：US20050288316A1

    公开(公告)日：2005-12-29

    申请号：US10995067

    申请日：2004-11-22

    申请人： Roger Crossley ,  Annika Jensen ,  Peter Brandt ,  Ulf Bremberg ,  Malin Nordberg ,  Erik Ringberg ,  Terry Ward

    发明人： Roger Crossley ,  Annika Jensen ,  Peter Brandt ,  Ulf Bremberg ,  Malin Nordberg ,  Erik Ringberg ,  Terry Ward

    IPC分类号： A61K20060101 ,  A61K31/407 ,  A61K31/4747 ,  C07D471/20 ,  C07D491/14 ,  C07D491/20

    CPC分类号： C07D471/20 ,  C07D491/20

    摘要： The present invention relates to compounds of Formula (I): wherein R3-R8, X, and Y are as described herein, processes for preparing the compounds, pharmaceutical compositions comprising the compounds, and use of the compounds and compositions in the prophylaxis or treatment of a GHSR receptor-related disorder. Examples of such disorders are obesity and related disorders such as diabetes type II, dyslipidemia and the metabolic syndrome Prader-Willi syndrome, cardiovascular diseases such as atherosclerotic vascular disease, angina pectoris, myocardial infarction and stroke, acromegaly and cancer, in particular breast, lung, prostate, thyroid and endocrine pituary carcinomas.

    摘要翻译： 本发明涉及式（I）的化合物：其中R 3，R 8，X和Y如本文所述，制备化合物的方法，药物组合物 包括化合物，以及化合物和组合物在预防或治疗GHSR受体相关病症中的用途。 这种障碍的例子是肥胖症和相关疾病，例如II型糖尿病，血脂异常和代谢综合征Prader-Willi综合征，心血管疾病如动脉粥样硬化性血管疾病，心绞痛，心肌梗塞和中风，肢端肥大症和癌症，特别是乳腺，肺 ，前列腺，甲状腺和内分泌胰腺癌。

    Certain arylaliphatic and heteroaryl-aliphatic piperazinyl pyrazines and their use in the treatment of serotonin-related diseases
    7.
    发明授权
    Certain arylaliphatic and heteroaryl-aliphatic piperazinyl pyrazines and their use in the treatment of serotonin-related diseases 有权

    公开(公告)号：US06759401B2

    公开(公告)日：2004-07-06

    申请号：US10269670

    申请日：2002-10-11

    申请人： Björn Nilsson ,  Jan Tejbrant ,  Benjamin Pelcman ,  Erik Ringberg ,  Markus Thor ,  Jonas Nilsson ,  Mattias Jönsson

    发明人： Björn Nilsson ,  Jan Tejbrant ,  Benjamin Pelcman ,  Erik Ringberg ,  Markus Thor ,  Jonas Nilsson ,  Mattias Jönsson

    IPC分类号： A61K3133

    摘要： The invention relates to compounds of the general formula (I): wherein Ar is optionally substituted aryl or heteroaryl; A is (i) —O—, —S—, —SO2—, —NH—, (ii) a C1-4-alkyl- or C1-6-acyl-substituted nitrogen atom or (iii) a C1-8-alkylene chain or a heteroalkylene chain having 2 to 8 chain atoms, which optionally contains at least one unsaturation, and which may be substituted and/or contain a bridge to form a saturated or partially or fully unsaturated ring having 3-8 ring members; B is —C(R4)(R5)—, —OC(R4)(R5)—, —N(R6)C(R4)(R5)—, —N(R6)—, —O—, —S— or —SO2—; R is optionally substituted C3-8-cycloalkyl, aryl or heteroaryl; R1 is (i) a saturated or unsaturated azacyclic or aminoazacyclic ring, or a saturated diazacyclic or aminodiazacyclic ring, which has 4 to 7 ring members, or a saturated aminoazabicyclic, azabicyclic or diazabicyclic ring which has 7 to 10 ring members, which rings optionally are substituted in one or more positions, or a group —[C(R4)(R5)]xN(R2a)(R3a)]; R2a, R3a, R4, R5, R6 and x are as defined in the claims, and n is 0 or 1; and pharmaceutically acceptable salts, hydrates and prodrug forms thereof The compounds may be prepared by per se conventional methods and can be used for treating a human or animal subject suffering from a serotonin-related disorder, such as eating disorders, especially obesity, memory disorders, schizophrenia, mood disorders, anxiety disorders, pain, sexual dysfunctions, and urinary disorders The invention also relates to such use as well as to pharmaceutical compositions comprising a compound of formula (I)