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1. 发明申请

WO2010034384A1 NEUE KRISTALLFORM VON CALCIUM-3-ACETYLAMINOPROPAN-1-SULFONAT 审中-公开
标题翻译：钙-3- ACETYLAMINOPROPAN -1-磺酸盐的新晶型
公开(公告)号：WO2010034384A1
公开(公告)日：2010-04-01
申请号：PCT/EP2009/006150
申请日：2009-08-25
申请人： MERCK PATENT GMBH , MUERMANN, Antje , KUEHN, Clemens , BARTELS, Matthias , SAAL, Christoph , BOSC, Nathalie
发明人： MUERMANN, Antje , KUEHN, Clemens , BARTELS, Matthias , SAAL, Christoph , BOSC, Nathalie
IPC分类号： A61K31/185 , C07C309/15
CPC分类号： C07C309/15 , C07B2200/13
摘要： Die vorliegende Erfindung betrifft eine neue Kristallform von Calcium-3- Acetylaminopropan-1-sulfonat. Verfahren zu ihrer Herstellung sowie ihre Verwendung in Arzeneimitteln.
摘要翻译：本发明涉及钙3- Acetylaminopropan -1-磺酸盐的新结晶形式。其制备方法及其在Arzeneimitteln使用。

2. 发明申请

WO2002102794A2 POLYMORPHIC FORMS OF 1-'4-(5-CYANOINDOL-3-YL)BUTYL-4-(2-CARBAMOYLBENZOFURAN-5-YL)PIPERAZINE HYDROCHLORIDE 审中-公开
标题翻译： 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：WO2002102794A2
公开(公告)日：2002-12-27
申请号：PCT/EP2002/006153
申请日：2002-06-05
申请人： MERCK PATENT GMBH , BATHE, Andreas , HELFERT, Bernd , NEUENFELD, Steffen , KNIEL, Heike , BARTELS, Matthias , RUDOLPH, Susanne , BÖTTCHER, Henning
发明人： BATHE, Andreas , HELFERT, Bernd , NEUENFELD, Steffen , KNIEL, Heike , BARTELS, Matthias , RUDOLPH, Susanne , BÖTTCHER, Henning
IPC分类号： C07D405/00
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，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。

3. 发明公开

EP1397357A2 POLYMORPHIC FORMS OF 1-'4-(5-CYANOINDOL-3-YL)BUTYL-4-(2-CARBAMOYLBENZOFURAN-5-YL)PIPERAZINE HYDROCHLORIDE 有权
标题翻译： 1- [4-（5-氰基吲哚-3-基）丁基] -4-（2-氨基甲酰基 - 苯并呋喃-5-基）哌嗪盐酸盐的多晶型形式
公开(公告)号：EP1397357A2
公开(公告)日：2004-03-17
申请号：EP02754627.4
申请日：2002-06-05
申请人： MERCK PATENT GmbH
发明人： BATHE, Andreas , HELFERT, Bernd , NEUENFELD, Steffen , KNIEL, Heike , BARTELS, Matthias , RUDOLPH, Susanne , BÖTTCHER, Henning
IPC分类号： C07D405/12
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.

4. 发明公开

EP2326322A1 NEUE KRISTALLFORM VON CALCIUM-3-ACETYLAMINOPROPAN-1-SULFONAT 有权
标题翻译：钙-3- ACETYLAMINOPROPAN -1-磺酸盐的新晶型
公开(公告)号：EP2326322A1
公开(公告)日：2011-06-01
申请号：EP09778095.1
申请日：2009-08-25
申请人： Merck Patent GmbH
发明人： MUERMANN, Antje , KUEHN, Clemens , BARTELS, Matthias , SAAL, Christoph , BOSC, Nathalie
IPC分类号： A61K31/185 , C07C309/15
CPC分类号： C07C309/15 , C07B2200/13
摘要： The present invention relates to a novel crystallization shape of calcium-3-acetyl aminopropane-1-sulfonate. The invention further relates to a method for producing the same, and to the use thereof in medications.

5. 发明授权

EP1397357B1 POLYMORPHIC FORMS OF 1-[4-(5-CYANOINDOL-3-YL)BUTYL]-4-(2-CARBAMOYLBENZOFURAN-5-YL)PIPERAZINE HYDROCHLORIDE 有权
标题翻译： 1- [4-（5-氰基吲哚-3-基）丁基] -4-（2-氨基甲酰基苯并呋喃-5-基）哌嗪盐酸盐的多晶型
公开(公告)号：EP1397357B1
公开(公告)日：2009-07-29
申请号：EP02754627.4
申请日：2002-06-05
申请人： Merck Patent GmbH
发明人： BATHE, Andreas , HELFERT, Bernd , NEUENFELD, Steffen , KNIEL, Heike , BARTELS, Matthias , RUDOLPH, Susanne , BÖTTCHER, Henning
IPC分类号： C07D405/12
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） - 哌嗪的盐酸盐的新晶体改性，二盐酸盐 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症，焦虑症，双相性精神障碍，躁狂症，痴呆症，物质相关的固体药物功能障碍，性功能障碍，进食障碍，肥胖症，纤维肌痛，睡眠障碍，精神障碍，脑梗塞，紧张症，用于治疗性腺功能减退症，继发性闭经，经前期综合症和不希望的产褥期泌乳的副作用。

6. 发明授权

EP2326322B1 NEUE KRISTALLFORM VON CALCIUM-3-ACETYLAMINOPROPAN-1-SULFONAT 有权
标题翻译：钙-3- ACETYLAMINOPROPAN -1-磺酸盐的新晶型
公开(公告)号：EP2326322B1
公开(公告)日：2015-10-14
申请号：EP09778095.1
申请日：2009-08-25
申请人： Merck Patent GmbH
发明人： MUERMANN, Antje , KUEHN, Clemens , BARTELS, Matthias , SAAL, Christoph , BOSC, Nathalie
IPC分类号： A61K31/185 , C07C309/15
CPC分类号： C07C309/15 , C07B2200/13

7. 发明授权

EP1397357B9 POLYMORPHIC FORMS OF 1-[4-(5-CYANOINDOL-3-YL)BUTYL]-4-(2-CARBAMOYLBENZOFURAN-5-YL)PIPERAZINE HYDROCHLORIDE 有权
标题翻译：多异氰酸甲酯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
公开(公告)号：EP1397357B9
公开(公告)日：2009-11-18
申请号：EP02754627.4
申请日：2002-06-05
申请人： Merck Patent GmbH
发明人： BATHE, Andreas , HELFERT, Bernd , NEUENFELD, Steffen , KNIEL, Heike , BARTELS, Matthias , RUDOLPH, Susanne , BÖTTCHER, Henning
IPC分类号： C07D405/12
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.

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