CN103951667A - 多晶型 - Google Patents

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CN103951667A
CN103951667A CN201410133173.0A CN201410133173A CN103951667A CN 103951667 A CN103951667 A CN 103951667A CN 201410133173 A CN201410133173 A CN 201410133173A CN 103951667 A CN103951667 A CN 103951667A
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methyl
polymorphic
piperadine
butyne
quinazoline
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彼得.西格
德克.凯默
彼得.科尔鲍尔
托马斯.尼古拉
马丁.伦兹
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Boehringer Ingelheim International GmbH
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Abstract

本发明涉及1-[(4-甲基-喹唑啉-2-基)甲基]-3-甲基-7-(2-丁炔-1-基)-8-(3-(R)-氨基-哌啶-1-基)-黄嘌呤的多晶型晶体变体、其制备方法及其在制备药物中的用途。

Description

多晶型
本申请是中国发明申请(发明名称：多晶型；申请日：2007年4月30日；申请号：200780016135.5)的分案申请。
技术领域
本发明涉及DPP-IV抑制剂的多晶型晶体变体、其制备方法及其在制备药物中的用途。
发明背景
酶DPP-IV(已知亦称为CD26)是丝氨酸蛋白酶，其促进在N-终端具有脯氨酸或丙氨酸基的蛋白中的二肽裂解。DPP-IV抑制剂因此影响生物活性肽(包括肽GLP-1)的血浆水平。此类化合物可用于预防或治疗与DPP-IV活性提高相关或可通过降低DPP-IV活性来预防或缓解的疾病或病症，尤其I型或II型糖尿病、前驱糖尿病或低葡萄糖耐受性。
WO2004/018468描述具有有价值药理性质的DPP-IV抑制剂。其中所公开抑制剂的一个实例为1-[(4-甲基-喹唑啉-2-基)甲基]-3-甲基-7-(2-丁炔-1-基)-8-(3-(R)-氨基-哌啶-1-基)-黄嘌呤。
发明描述
在本发明的范畴内，已发现1-[(4-甲基-喹唑啉-2-基)甲基]-3-甲基-7-(2-丁炔-1-基)-8-(3-(R)-氨基-哌啶-1-基)-黄嘌呤可具有各种多晶型晶体变体，且在WO2004/018468中所制备的该化合物在环境温度下是以两种互变性多晶型的混合物存在。该两种多晶型彼此转换的温度为25±15℃(参看附图1及附图2)。
可通过加热该混合物至大于40℃的温度获得的纯的高温形态(多晶型A)在206±3℃熔化。在X射线粉末图(参看附图3)中，此形态显示以下d值处的特征性衍射：(亦参看表1及表2)。
可通过以下步骤制备无水多晶型A：
(a)在无水乙醇中回流1-[(4-甲基-喹唑啉-2-基)甲基]-3-甲基-7-(2-丁炔-1-基)-8-(3-(R)-氨基-哌啶-1-基)-黄嘌呤，且任选地过滤该混合物，
(b)将该热溶液或该热滤液冷却，直至开始结晶，
(c)使用溶剂例如叔丁基甲基醚将其稀释，
(d)对该溶剂混合物进行吸滤，及
(e)在45℃下真空干燥该多晶型A。
低温形态(多晶型B)是通过冷却至小于10℃的温度而获得。在X射线粉末图(参看附图4)中，该形态显示以下d值处的特征性衍射： 及(亦参看表3及表4)。
可通过以下步骤制备无水多晶型B：
(a)在无水乙醇中溶解1-[(4-甲基-喹唑啉-2-基)甲基]-3-甲基-7-(2-丁炔-1-基)-8-(3-(R)-氨基-哌啶-1-基)-黄嘌呤且使其回流，且任选地过滤该混合物，
(b)将该热溶液或热滤液冷却至低于10℃的温度以进行结晶，
(c)使用溶剂例如叔丁基甲基醚将其稀释，
(d)对该溶剂混合物进行吸滤，及
(e)在低于10℃的温度下真空干燥该多晶型。
在X射线粉末图(参看附图5)中，另一多晶型(多晶型C)显示以下d值处的特征性衍射：(亦参看表5)。
如下获得多晶型C：
(a)在甲醇中溶解1-[(4-甲基-喹唑啉-2-基)甲基]-3-甲基-7-(2-丁炔-1-基)-8-(3-(R)-氨基-哌啶-1-基)-黄嘌呤且使其回流，且任选地在活性炭的存在下过滤，
(b)将该甲醇溶液冷却至40-60℃的温度，
(c)添加溶剂例如叔丁基甲基醚或二异丙醚，
(d)首先将所得悬浮液缓慢冷却至15-25℃，且然后冷却至0-5℃，
(e)对所形成的晶体进行吸滤，且使用叔丁基甲基醚或二异丙醚再次洗涤之，及
(f)在真空干燥器中在70℃的温度下干燥如此获得的晶体。
另一多晶型(多晶型D)在150±3℃熔化。若将多晶型C加热至30-100℃的温度或在此温度下干燥，则获得多晶型D。
最后，亦存在多晶型E，其在175±3℃熔化。若将多晶型D熔化，则形成无水多晶型E。进一步加热后，多晶型E自熔融物中结晶出。
如此获得的多晶型可以与WO2004/018468中所述的两种多晶型A及B的混合物相同的方式用于制备药物组合物，其适于治疗患有I型及II型糖尿病、前驱糖尿病或葡萄糖耐受性降低、患有类风湿性关节炎、肥胖或降钙素引发的骨质疏松症的患者，以及实施了同种异体移植的患者。除一或多种惰性载体外，这些药物含有至少0.1%至0.5%，优选至少0.5%至1.5%且尤其优选至少1%至3%的该多晶型A、B或C之一。
实施方式
以下实例意欲更详细说明本发明。
实施例1：多晶型A的结晶
使用5倍的无水乙醇回流粗制的1-[(4-甲基-喹唑啉-2-基)甲基]-3-甲基-7-(2-丁炔-1-基)-8-(3-(R)-氨基-哌啶-1-基)-黄嘌呤，且经由活性炭将热溶液过滤干净。在滤液冷却至20℃且开始结晶之后，以叔丁基甲基醚将该溶液稀释为两倍体积。然后该悬浮液经冷却至2℃、搅拌2小时、吸滤且将其在真空干燥器中在45℃下干燥。
多晶型A于206±3℃熔化。在DSC图中，在约25℃处可看到另一轻微吸热信号。此为在两个互变性晶体变体A与B之间完全可逆的固-固相变。该形态A为在此转换温度以上的热力学稳定变体，而形态B为在此转换温度以下的热力学稳定变体。
附图2显示循环DSC图，其中进行总共三次自-40℃至120℃的相转变及相反的转变。加热期间，相转变是作为吸热信号而被观测到，且相应地，冷却期间其是作为放热信号而被观测到。在第一加热周期期间，该相转变可以双吸热信号或作为极宽的信号而被观测到，而在所有其他周期中，该信号作为极尖的吸热或放热信号而发生，取决于加热或冷却。
表1：至30°2Θ的具有强度(标准化)的标记X射线反射(无水多晶型A)
表2：无水形态A的晶格量度
实施例2：多晶型B的结晶
多晶型B是通过将来自实施例1的形态A冷却至小于10℃的温度而获得。
表3：至30°2Θ的具有强度(标准化)的标记X射线反射(无水多晶型B)
表4：无水形态B的晶格量度
实施例3：多晶型C的结晶
使用157升甲醇(与1.3kg活性炭混合)回流粗制的1-[(4-甲基-喹唑啉-2-基)甲基]-3-甲基-7-(2-丁炔-1-基)-8-(3-(R)-氨基-哌啶-1-基)-黄嘌呤(26kg)，且在搅拌30分钟之后，过滤该混合物且使用26升甲醇洗涤。自滤液蒸馏出122升甲醇，然后将残余物冷却至45-55℃。经30分钟添加52升叔丁基甲基醚至该残余物中。然后在45-55℃下搅拌该混合物另外60分钟。结晶发生于此时间内。经30分钟添加另外78升叔丁基甲基醚至该悬浮液中，且然后在45-55℃下将其再次搅拌另外60分钟。将其稀释为四倍体积。缓慢冷却该悬浮液至15-25℃，且在此温度下将其搅拌过夜。在该悬浮液冷却至0-5℃之后，对该晶体进行吸滤，使用2批叔丁基甲基醚洗涤，且在真空干燥器中于70℃下干燥。
表5：至30°2Θ的具有强度(标准化)的标记X射线反射(无水多晶型C)
实施例4：多晶型D的结晶
若将来自实施例3的多晶型C加热至30-100℃的温度或在此温度下干燥，则获得多晶型D。
实施例5：多晶型E的结晶
若将多晶型D熔化，则获得无水多晶型E。进一步加热后，多晶型E自熔融物中结晶出。
在形态C的DSC图中，可观测到完整范围的信号。最强信号为在约206℃处无水形态A的熔点，该形态是于DSC实验中产生。在该熔点之前，可观测到多个其他吸热及放热信号。因此，例如，在30℃与100℃之间可看到极宽且弱的吸热信号，其与热重量法(TR)中的主要失重相关。TG/IR联合实验提供在此温度范围内仅水分自样品中逸出的信息。
对于维持在100℃的温度下的样本所测得的X射线粉末图显示不同于起始物质的X射线衍射，说明形态C为水合物相，具有半水合物或单水合物的区域中某处的化学计量。温度受控的样本为另一无水变体D，其仅在无水条件下稳定。D形态于约150℃熔化。另一无水晶体变体E自该熔融物结晶而得，且当加热时于约175℃进一步熔化。最后，形态A自形态E的熔融物结晶而得。形态E亦为亚稳晶体变体，其仅存在于高温下。
附图简述
图1：无水形态A/B的热分析；
图2：互变性相转变的循环DSC图；
图3：无水形态A的X射线粉末图；
图4：无水形态B的X射线粉末图；
图5：无水形态C的X射线粉末图；
图6：形态C的热分析。

Claims (12)

1.化合物1-[(4-甲基-喹唑啉-2-基)甲基]-3-甲基-7-(2-丁炔-1-基)-8-(3-(R)-氨基-哌啶-1-基)-黄嘌呤的多晶型C，其特征在于，其在30-100℃的温度失水，且在DSC图中，其在约150℃及175℃处显示进一步的热效应。
2.如权利要求1所述的多晶型C，其特征在于，在X射线粉末图中，其尤其在以下d值处具有特征性衍射：及。
3.化合物1-[(4-甲基-喹唑啉-2-基)甲基]-3-甲基-7-(2-丁炔-1-基)-8-(3-(R)-氨基-哌啶-1-基)-黄嘌呤的无水多晶型A，其特征在于，其在206±3℃熔化。
4.如权利要求3所述的多晶型A，其特征在于，在X射线粉末图中，其尤其在以下d值处具有特征性衍射： 及。
5.化合物1-[(4-甲基-喹唑啉-2-基)甲基]-3-甲基-7-(2-丁炔-1-基)-8-(3-(R)-氨基-哌啶-1-基)-黄嘌呤的无水多晶型B，其特征在于，在10-40℃的温度，其可逆地转换为如权利要求3所述的多晶型A。
6.如权利要求5所述的多晶型B，其特征在于，在X射线粉末图中，其尤其在以下d值处具有特征性衍射：及。
7.化合物1-[(4-甲基-喹唑啉-2-基)甲基]-3-甲基-7-(2-丁炔-1-基)-8-(3-(R)-氨基-哌啶-1-基)-黄嘌呤的无水多晶型D，其特征在于，其在150±3℃熔化。
8.化合物1-[(4-甲基-喹唑啉-2-基)甲基]-3-甲基-7-(2-丁炔-1-基)-8-(3-(R)-氨基-哌啶-1-基)-黄嘌呤的无水多晶型E，其特征在于，其在175±3℃熔化。
9.一种制备如权利要求1所述的多晶型C的方法，其特征在于：
(a)将1-[(4-甲基-喹唑啉-2-基)甲基]-3-甲基-7-(2-丁炔-1-基)-8-(3-(R)-氨基-哌啶-1-基)-黄嘌呤在甲醇中回流，
(b)将该甲醇溶液冷却至40-60℃的温度，
(c)添加溶剂例如叔丁基甲基醚，
(d)首先将所得悬浮液冷却至15-25℃，且然后冷却至0-5℃，
(e)对该晶体进行吸滤，及
(f)在70℃的温度下真空干燥。
10.如权利要求9所述的方法，其特征在于，在步骤(a)之后过滤该热溶液。
11.化合物1-[(4-甲基-喹唑啉-2-基)甲基]-3-甲基-7-(2-丁炔-1-基)-8-(3-(R)-氨基-哌啶-1-基)-黄嘌呤的多晶型A、B或C之一在制备药物组合物中的用途，该药物组合物用于治疗患有I型及II型糖尿病、前驱糖尿病或葡萄糖耐受性降低、类风湿性关节炎、肥胖或降钙素引发的骨质疏松症的患者，以及实施了同种异体移植的患者。
12.药物，含有化合物1-[(4-甲基-喹唑啉-2-基)甲基]-3-甲基-7-(2-丁炔-1-基)-8-(3-(R)-氨基-哌啶-1-基)-黄嘌呤以及一或多种惰性载体及/或稀释剂，其特征在于，其含有至少0.1%至0.5%的多晶型A、B或C之一。
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