CHEN, SHUANG,NAPIER, JAMES J.,ZHANG, GEOFF G. Z.,PAUL J., BRACKEMEYER
申请号：
PE0005402013
公开号：
PE13942013A1
申请日:
2011.09.21
申请国别(地区):
PE
年份:
2014
代理人:
摘要：
Refers to a Crystalline form of a Derivative of AZA adamantane as CITRATE MONOHYDRATE diacid (4S) - 4 - (5 - phenyl - 2 - 1,3,4 - thiadiazole iloxi) - 1 - [3.3.1.1 azatriciclo 3.7] Dean has a pattern of x-ray Powder Diffraction, which includes the following Peaks 2 expressed in degrees Theta: 11.3 - 8.4 - 0.20, 0.20, 14.2 - 15.5 - 0.20, 0.20, 0.20 - 16.4, 16.6 - 17.2 - 0.20, 0.20, 19.7 - 0.20 0.20, 20.7, 21.0 - 0.20, 0.20 21.2 - 21.6 - 0.20, 0.20 and 24.8 - 26.9 - 0.20. It also relates to a Pharmaceutical Composition and a preparation method of the Crystal form comprising: (a) Dissolving (4S) - 4 - (5 - phenyl - 2 - 1,3,4 - thiadiazole iloxi) - 1 - [azatriciclo 3.3.1.1 37] Dean in a mixture of 2-propanol and water at a temperature of 65 to 85 \ufffdC (b) adjusting the temperature of the solution at a temperature of 55 to 75 \ufffdC (c) add an additional Solvent such as 2-propanol solution and mix (d) to adjust the temperature of the solutions between \ufffdC 30 and 50 (e) Add an additional Solvent such as 2-propanol to the solution (f) to maintain the slurry temperatureBetween 30 and 50 \ufffdC (g) to adjust the temperature of the slurry between 5 and 15 \ufffdC (H) MIX THE Grout for a time and (i) to recover the Crystalline Monohydrate. The Crystalline form is a Modulator of nAChR a7 nicotinic acetylcholine Receptors and a4b2, being useful in the treatment of Alzheimers Disease (AD), mild cognitive impairment, Schizophrenia, DementiaSE REFIERE A UNA FORMA CRISTALINA DE UN DERIVADO DE AZA-ADAMANTANO TAL COMO EL MONOHIDRATO DEL CITRATO DIACIDO DE (4S)-4-(5-FENIL-1,3,4-TIADIAZOL-2-ILOXI)-1-AZATRICICLO[3.3.1.1 3,7]DECANO QUE TIENE UN PATRON DE DIFRACCION DE RAYOS X EN POLVO QUE COMPRENDE LOS SIGUIENTES PICOS EXPRESADOS EN GRADOS 2 THETA: 8.4 � 0.20, 11.3 � 0.20, 14.2 � 0.20, 15.5 � 0.20, 16.4 � 0.20, 16.6 � 0.20, 17.2 � 0.20, 19.7 � 0.20, 20.7 � 0.20, 21.0 � 0.20, 21.2 � 0.20, 21.6 � 0.20, 24.8 � 0.20 Y 26.9 � 0.20. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA Y A
