Crystalline hydrate of 6-hydroxy-3-(4-[2-(piperidine-1-yl)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thio-phen hydrochloride, process for obtaining thereof, pharmaceutical composition comprising it and use for inhibition of pathological states and activation of choline acetyltransferase

The invention relates to the pharmaceutical technologies, in particular to a new crystalline form of 6-hydroxy-3-(4-[2-(piperidine-1-yl)ethoxy]phe-noxy)-2-(4-methoxy-phenyl)-benzo[b]thiophen hydrochloride, to a process for obtaining and to a composition containing it.The crystalline hydrate 6-hydroxy-3-(4-[2-(piperidine-1-yl)ethoxy]phenoxy)-2-(4-met-hoxyphenyl)benzo[b]thiophen hydrochloride (arzophene), F-III, represents a compound with a high degree of crystallinity. The pharmaceutical composition on base thereof contains one or more carriers, diluents or substituents and, optionally, estrogen, progestin, an aromatase inhibitor, a hormone analogue, releasing the luteinizing hormone (LHRH) and an acetylcholine esterase inhibitor. The process for obtaining of said compound provides for the crystallization of 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-metho-xy-phe-nyl)benzo[b]thiophen hydro-chlo--ride from the mixture of isopropanol and water, in the ratio of (1...9):1, optimally being of (3...5,6):1.The claimed compound may be used for inhibition of pathological states associated with estrogen deficiency, such as uterine fibrosis, endometriosis, restenosis, estrogen-dependent cancer (including the mammary cancer and the uterine cancer), prostate cancer, prostate benign hyperplasia, osteoporosis, cardiovascular affections, hyperlipoidemia, disorders of the CNS and the Alzheimer's disease, prevention of the mammary cancer and activation of the choline acetyltransferase. Invenţia se referă la tehnologiile farmaceutice, în special la o formă cristalină nouă de hidroclorură de 6-hidroxi-3-(4-[2-(piperidin-1-il)etoxi]fenoxi)-2-(4-metoxifenil)benzo[b]tiofen, la un procedeu de obţinere şi la o compoziţie care o conţine.Hidratul cristalin de hidroclorură de 6-hidroxi-3-(4-[2-(piperidin-1-il)etoxi]fenoxi)-2-(4-metoxifenil)benzo[b]tiofen (arzofen), F-III, reprezintă un compus cu un grad înalt de cristalizare. Compoziţia farmaceutică pe baza lui conţine unul sau mai mulţi purtători, diluanţi sau excipienţi, estrogen, progestină, un inhibitor al aromatazei, un analog al hormonului, care eliberează hormonul luteinizant (LHRH) şi un inhibitor al acetilcolinesterazei. Procedeul de obţinere a compusului menţionat prevede cristalizarea hidroclorurii de 6-hidroxi-3-(4-[2-(piperidin-1-il)etoxi]fenoxi)-2-(4-metoxifenil)benzo[b]tiofen din amestecul de izopropanol şi apă, luate în raportul de (1...9):1, optimal fiind de (3...5,6):l.Compusul declarat se poate utiliza p