发明名称 Polymorphic forms of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoylbenzofuran-5-yl) piperazine hydrochloride
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 hypertension, cerebral disorders, chronic pain, acromegaly, hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.
申请公布号 US9624204(B2) 申请公布日期 2017.04.18
申请号 US201414549779 申请日期 2014.11.21
申请人 Merck Patentgesellschaft 发明人 Bathe Andreas;Helfert Bernd;Neuenfeld Steffen;Kniel Heike;Bartels Matthias;Rudolph Susanne;Bottcher Henning
分类号 C07D405/12;A61K31/496;C07D405/14 主分类号 C07D405/12
代理机构 McCarter & English, LLP 代理人 McCarter & English, LLP ;Herritt, Esq. Danielle L.;Wang, Esq. Jin
主权项 1. A compound which is 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride solvate in its crystalline modification and having at least one group of 2Theta characteristic peak values selected from the following groups: i. Group A: at least three of the characteristic peak values corresponding to 10.40±0.1, 11.19±0.1, 13.39±0.1, 13.54±0.1, 13.79±0.1, 15.84±0.1, 21.09±0.1, 23.64±0.1, 24.49±0.1 or 25.79±0.1 degrees; ii. Group B: at least three of the characteristic peak values corresponding to 10.49±0.1, 11.73±0.1, 13.12±0.1, 14.46±0.1, 16.24±0.1, 19.32±0.1, 20.05±0.1, 21.75±0.1, 23.50±0.1, or 26.35±0.1 degrees; iii. Group C: at least three of the characteristic peak values corresponding to 5.38±0.1, 9.58±0.1, 10.68±0.1, 13.76±0.1, 15.98±0.1, 22.29±0.1, 23.50±0.1, 24.77±0.1, 26.28±0.1 or 26.52±0.1 degrees; iv. Group D: at least three of the characteristic peak values corresponding to 5.58±0.1, 9.69±0.1, 10.68±0.1, 11.12±0.1, 13.48±0.1, 13.74±0.1, 16.08±0.1, 21.30±0.1, 21.49±0.1 or 24.88±0.1 degrees; v. Group E: at least three of the characteristic peak values corresponding to 8.54±0.1, 12.50±0.1, 13.17±0.1, 18.56±0.1, 19.28±0.1, 19.76±0.1, 20.94±0.1, 21.21±0.1, 25.40±0.1, or 26.26±0.1 degrees; and vi. Group F: at least three of the characteristic peak values corresponding to 5.88±0.1, 11.08±0.1, 17.10±0.1, 18.14±0.1, 21.19±0.1, 22.21±0.1 or 25.47±0.1 degrees.
地址 Darmstadt DE