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    Polymorphic forms of 1-′4-(5-cyanoindol-3-yl)butyl-4-(2-carbamoylbenzofuran-5-yl)piperazine hydrochloride
    5.
    发明授权
    Polymorphic forms of 1-′4-(5-cyanoindol-3-yl)butyl-4-(2-carbamoylbenzofuran-5-yl)piperazine hydrochloride 有权
    1-（4-氰基吲哚-3-基）丁基-4-（2-氨基甲酰基苯并呋喃-5-基）哌嗪盐酸盐的多晶型

    公开(公告)号：US08236804B2

    公开(公告)日：2012-08-07

    申请号：US13100948

    申请日：2011-05-04

    申请人： Andreas Bathe ,  Bernd Helfert ,  Steffen Neuenfeld ,  Heike Kniel ,  Matthias Bartels ,  Susanne Rudolph ,  Henning Böttcher

    发明人： Andreas Bathe ,  Bernd Helfert ,  Steffen Neuenfeld ,  Heike Kniel ,  Matthias Bartels ,  Susanne Rudolph ,  Henning Böttcher

    IPC分类号： A61K31/496 ,  C07D401/14

    CPC分类号： A61K31/496 ,  C07D405/12 ,  C07D405/14

    摘要： The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.

    摘要翻译： 本发明涉及1- [4-（5-氰基吲哚-3-基）丁基] -4-（2-氨基甲酰基 - 苯并呋喃-5-基） - 哌嗪的盐酸盐的新结晶改性，二盐酸盐的结晶改性 1- [4-（5-氰基吲哚-3-基）丁基] -4-（2-氨基甲酰基 - 苯并呋喃-5-基） - 哌嗪和无定形的1- [4-（5-氰基吲哚-3-基）丁基] -4-（2-氨基甲酰基 - 苯并呋喃-5-基） - 哌嗪盐酸盐，其特别适用于制备用于治疗或预防抑郁障碍，焦虑障碍，双相性精神障碍，躁狂症，痴呆，物质相关的固体药物 疾病，性功能障碍，进食障碍，肥胖症，纤维肌痛，睡眠障碍，精神障碍，脑梗死，紧张症，用于治疗性腺机能减退，继发性闭经，经前期综合征和不期望的产后泌乳的副作用。

    POLYMORPHIC FORMS OF 1-'4-(5-CYANOINDOL-3-YL)BUTYL-4-(2-CARBAMOYLBENZOFURAN-5-YL)PIPERAZINE HYDROCHLORIDE
    6.
    发明申请
    POLYMORPHIC FORMS OF 1-'4-(5-CYANOINDOL-3-YL)BUTYL-4-(2-CARBAMOYLBENZOFURAN-5-YL)PIPERAZINE HYDROCHLORIDE 有权
    1-4-（5-氰基吲哚-3-基）丁基-4-（2-羧甲基苯并呋喃-5-基）哌嗪氢氯化物的多晶型

    公开(公告)号：US20110294825A1

    公开(公告)日：2011-12-01

    申请号：US13100948

    申请日：2011-05-04

    申请人： Andreas Bathe ,  Bernd Helfert ,  Steffen Neuenfeld ,  Heike Kniel ,  Matthias Bartels ,  Susanne Rudolph ,  Henning Böttcher

    发明人： Andreas Bathe ,  Bernd Helfert ,  Steffen Neuenfeld ,  Heike Kniel ,  Matthias Bartels ,  Susanne Rudolph ,  Henning Böttcher

    IPC分类号： A61K31/496 ,  A61P25/24

    CPC分类号： A61K31/496 ,  C07D405/12 ,  C07D405/14

    摘要： The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.

    摘要翻译： 本发明涉及1- [4-（5-氰基吲哚-3-基）丁基] -4-（2-氨基甲酰基 - 苯并呋喃-5-基） - 哌嗪的盐酸盐的新结晶改性，二盐酸盐的结晶改性 1- [4-（5-氰基吲哚-3-基）丁基] -4-（2-氨基甲酰基 - 苯并呋喃-5-基） - 哌嗪和无定形的1- [4-（5-氰基吲哚-3-基）丁基] -4-（2-氨基甲酰基 - 苯并呋喃-5-基） - 哌嗪盐酸盐，其特别适用于制备用于治疗或预防抑郁障碍，焦虑障碍，双相性精神障碍，躁狂症，痴呆，物质相关的固体药物 疾病，性功能障碍，进食障碍，肥胖症，纤维肌痛，睡眠障碍，精神障碍，脑梗死，紧张症，用于治疗性腺机能减退，继发性闭经，经前期综合征和不期望的产后泌乳的副作用。

    POLYMORPHIC FORMS OF 1-'4-(5-CYANOINDOL-3-YL) BUTYL-4-(2-CARBAMOYLBENZOFURAN-5-YL) PIPERAZINE HYDROCHLORIDE
    7.
    发明申请
    POLYMORPHIC FORMS OF 1-'4-(5-CYANOINDOL-3-YL) BUTYL-4-(2-CARBAMOYLBENZOFURAN-5-YL) PIPERAZINE HYDROCHLORIDE 有权
    1-4-（5-氰基吲哚-3-基）丁基-4-（2-羧甲基苯并呋喃-5-基）哌嗪氢氯化物的多晶型

    公开(公告)号：US20110190317A1

    公开(公告)日：2011-08-04

    申请号：US12945272

    申请日：2010-11-12

    申请人： Andreas Bathe ,  Bernd Helfert ,  Steffen Neuenfeld ,  Heike Kniel ,  Matthias Bartels ,  Susanne Rudolph ,  Henning Böttcher

    发明人： Andreas Bathe ,  Bernd Helfert ,  Steffen Neuenfeld ,  Heike Kniel ,  Matthias Bartels ,  Susanne Rudolph ,  Henning Böttcher

    IPC分类号： A61K31/496 ,  A61P25/24

    CPC分类号： A61K31/496 ,  C07D405/12 ,  C07D405/14

    摘要： The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.

    摘要翻译： 本发明涉及1- [4-（5-氰基吲哚-3-基）丁基] -4-（2-氨基甲酰基 - 苯并呋喃-5-基） - 哌嗪的盐酸盐的新结晶改性，二盐酸盐的结晶改性 1- [4-（5-氰基吲哚-3-基）丁基] -4-（2-氨基甲酰基 - 苯并呋喃-5-基） - 哌嗪和无定形的1- [4-（5-氰基吲哚-3-基）丁基] -4-（2-氨基甲酰基 - 苯并呋喃-5-基） - 哌嗪盐酸盐，其特别适用于制备用于治疗或预防抑郁障碍，焦虑障碍，双相性精神障碍，躁狂症，痴呆，物质相关的固体药物 疾病，性功能障碍，进食障碍，肥胖症，纤维肌痛，睡眠障碍，精神障碍，脑梗死，紧张症，用于治疗性腺机能减退，继发性闭经，经前期综合征和不期望的产后泌乳的副作用。

    6H-oxazolo[4,5-e]indole derivatives as nicotinic acetylcholine receptor ligands and/or serotonergic ligands
    10.
    发明授权
    6H-oxazolo[4,5-e]indole derivatives as nicotinic acetylcholine receptor ligands and/or serotonergic ligands 失效
    6H-恶唑并[4,5-e]吲哚衍生物作为烟碱乙酰胆碱受体配体和/或血清素能配体

    公开(公告)号：US07291633B2

    公开(公告)日：2007-11-06

    申请号：US10476306

    申请日：2002-04-05

    申请人： Kai Schiemann ,  Henning Böttcher ,  Joachim Leibrock

    发明人： Kai Schiemann ,  Henning Böttcher ,  Joachim Leibrock

    IPC分类号： A61K31/424 ,  A61K31/445 ,  A61K31/5377 ,  C07D401/14 ,  C07D413/14 ,  C07D498/02

    CPC分类号： C07D498/04 ,  C07D519/00

    摘要： Compounds of the formula I in which R1, R2, R3 and R4 are as defined in claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia anorexia nervosa or other eating disorders, compulsvie behaviour, premenstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterised by an excess of circulating serotonin or by serotonergic hyperactivity

    摘要翻译： 其中R 1，R 2，R 3和R 4的式I化合物如 权利要求1是烟酸乙酰胆碱受体和/或血清素能配体的配体，并且适用于预防或治疗精神病，精神分裂症，抑郁症，焦虑状态，痴呆，特别是阿尔茨海默病和路易体痴呆，神经变性疾病，帕金森病， 肌萎缩性侧索硬化，亨廷顿舞蹈病，Tourette综合征，学习和记忆限制，贪食症神经性食欲障碍或其他饮食失调，强迫行为，经前综合征，年龄引起的记忆障碍，尼古丁依赖性戒断症状改善，中毒或脑损伤 ，以及用于治疗以循环血清素过量为特征的血清素多动障碍