CHEN SHUANG,NAPIER JAMES J.,ZHANG GEOFF,BRACKEMEYER PAUL
申请号：
CO13098843
公开号：
CO6720965A2
申请日:
2013.04.17
申请国别(地区):
CO
年份:
2013
代理人:
摘要：
The Invention relates to Derivatives of AZA adamantane and, more particularly, with Crystalline forms monohidratas AZA adamantane Derivatives, to compositions comprising these compounds and processes for preparing these compounds. In One aspect, The Invention relates to the form Cris Talin Monohydrate Citrate diacid (4S) - 4 - (5 - phenyl - 1, 3 - 2 - 4 - thiadiazole iloxi) - 1 - [3 azatriciclo.3.1.1] Dean, which shows at least a characteristic peak in the x-ray diffraction pattern of Powder in degrees two Theta values of 8.4 11.3 + + 0.20, 0.20, 0.20 14.2 (15.5 (0.20, 0.20 + 16.4, 16.6 (17.2 (0.20, 0.20, 19,7 u00b1 20.7 (0.20, 0.20 (+ 21.2 21.0, 0.20, 0.20, 21.6 (0.20, 0.20 and 24.8 (26.9 + 0.20.Additionally, the present Invention relates to a process for preparing a Crystalline Monohydrate of dihydrogen citrate (4S) - 4 - (5 - phenyl - 1, 3 - 2 - 4 - thiadiazole iloxi) - 1 - [3.3.1.1 azatriciclo] Dean, wherein Said process comprises the steps of: (a) Dissolving (4S) - 4 - (5 - phenyl - 1, 3 - 2 - 4 - thiadiazole iloxi) - 1 - [azatriciclo 3.3.1.1] Dean in a Solvent at a temperature that varies in a range of between approximately 65 c and approximately 85 c； (b) adjusting the temperature of the solution to a temperature that varies in a range of between approximately Fifty Fifth C and approximately 75 C； (c) Adding at least one sun Additional come to the solution and mix； (d) to adjust the temperature of the solutions to a temperature that VAr u00eda in a range between approximately 30 and approximately 50 C C； (e) to add at least an additional Solvent to the solution； (f) to maintain the slurry to a temperature that varies in a range of between approximately 30 and approximately 50 C C； (g) to adjust the temperature of the slurry to U Na temperature varies in a range of between approximately 5 and approximately 15o C - C； mixing the L (H)Cast for at least an hour； and (i) to recover the Crystalline Monohydrate of dihydrogen citrate (4S) - 4 - (5 - phenyl - 1, 3 - 2
