JP6309589B2 - 多形体 - Google Patents
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- JP6309589B2 JP6309589B2 JP2016197147A JP2016197147A JP6309589B2 JP 6309589 B2 JP6309589 B2 JP 6309589B2 JP 2016197147 A JP2016197147 A JP 2016197147A JP 2016197147 A JP2016197147 A JP 2016197147A JP 6309589 B2 JP6309589 B2 JP 6309589B2
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- 238000010586 diagram Methods 0.000 claims description 21
- 239000000843 powder Substances 0.000 claims description 16
- -1 4-Methyl-quinazolin-2-yl Chemical group 0.000 claims description 15
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- LTXREWYXXSTFRX-QGZVFWFLSA-N Linagliptin Chemical compound N=1C=2N(C)C(=O)N(CC=3N=C4C=CC=CC4=C(C)N=3)C(=O)C=2N(CC#CC)C=1N1CCC[C@@H](N)C1 LTXREWYXXSTFRX-QGZVFWFLSA-N 0.000 claims description 10
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- PEUGKEHLRUVPAN-RXMQYKEDSA-N (3r)-piperidin-3-amine Chemical compound N[C@@H]1CCCNC1 PEUGKEHLRUVPAN-RXMQYKEDSA-N 0.000 description 1
- CXBDYQVECUFKRK-UHFFFAOYSA-N 1-methoxybutane Chemical compound CCCCOC CXBDYQVECUFKRK-UHFFFAOYSA-N 0.000 description 1
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- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical group OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 description 1
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- C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
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- C07D473/04—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms
- C07D473/06—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two oxygen atoms with radicals containing only hydrogen and carbon atoms, attached in position 1 or 3
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
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Description
該混合物を>40℃の温度まで加熱することによって得ることのできる純粋な高温形体(多形体A)は、206±3℃で融解する。粉末X線図(図3参照)では、この形体は以下のd値:11.49Å、7.60Å、7.15Å、3.86Å、3.54Å及び3.47Å(表1及び2も参照)で特徴的な反射を示す。
低温形体(多形体B)は、<10℃の温度まで冷却することによって得られる。粉末X線図(図4参照)では、この形体は以下のd値:11.25Å、9.32Å、7.46Å、6.98Å及び3.77Å(表3及び4も参照)で特徴的な反射を示す。
別の多形体(多形体C)は、粉末X線図(図5参照)において以下のd値:12.90Å、11.10Å、6.44Å、3.93Å及び3.74Å(図5も参照)で特徴的な反射を示す。
別の多形体(多形体D)は150±3℃で融解する。この多形体は、多形体Cを30-100℃の温度まで加熱し、この温度で乾燥させると得られる。
最後に、175±3℃の温度で融解する多形体Eも存在する。無水多形体Eは、多形体Dが融解すると形成される。さらに加熱すると、多形体Eは該融解物から晶出する。
以下の実施例は、本発明をより詳細に説明することを目的とする。
粗い1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンを5倍量の無水エタノールでリフラックスし、この熱い溶液を活性炭に通して濾過した。濾過物を20℃まで冷却して結晶化を開始した後、該溶液をtert.-ブチルメチルエーテルで2倍の容積まで希釈した。続いて、この懸濁液を2℃まで冷却し、2時間攪拌し、吸引濾過し、及び真空乾燥機において45℃で乾燥させた。
多形体Aは206±3℃で融解する。該DSC図では、別のわずかな吸熱信号が約25℃で見ることができる。これは、該2種のエナンチオトロピー結晶修飾A及びBの間の完全に可逆な固体-固体の相転移である。該形体Aはこの変形温度よりも高温で熱力学的に安定な修飾であり、形態Bはこの変形温度よりも低温で熱力学的に安定な修飾である。
図2は周期的なDSC図を示しており、-40℃〜120℃の相転移及びその逆が計3回起こっている。加熱中、相転移は吸熱信号として観察され、従って冷却中は発熱信号として観察される。第一の加熱サイクル中に、相転移は吸熱の二重信号か又は非常にブロードな信号としても観察され、全ての他のサイクルにおいて該信号は非常に鋭い吸熱又は発熱信号として起こり、加熱又は冷却が起こるか否かに依存する
多形体Bは、実施例1からの形体Aを<10℃の温度まで冷却することによって得られる。
粗い1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチン(26kg)を、157Lのメタノールでリフラックスし、1.3kgの活性炭と混合し、30分攪拌した後に該混合物を濾過して26Lのメタノールで漱いだ。122Lのメタノールを濾過物から蒸留し、続いて残渣を45-55℃まで冷却した。52Lのtert.-ブチルメチルエーテルを30分かけて残渣に加えた。続いて、該混合物を45-55℃でさらに60分間攪拌した。結晶化がこの時間内に起こった。さらに78Lのtert. ブチルメチルエーテルを30分かけて該懸濁液に加え、続いて45-55℃でさらに60分間再び攪拌した。
それを4倍の体積に希釈した。該懸濁液を15-25℃まで穏やかに冷却し、この温度で終夜攪拌した。該懸濁液を0-5℃まで冷却した後、結晶を吸引濾過し、2バッチのtert.-ブチルメチルエーテルで洗浄し、及び70℃の真空乾燥機で乾燥させた。
多形体Cは、実施例3からの多形体Cを30-100℃の温度まで加熱し、この温度で乾燥して得られる。
実施例5 多形体Eの結晶化
無水多形体Eは、多形体Dが融解すると得られる。さらなる加熱により、多形体Eが該融解物から晶出する。
100℃の温度で保持されたサンプルに関する粉末X線図は、出発物質からの異なるX線反射を示しており、形体Cがおよそ半水化物又は一水和物の領域にある化学量論比を有する水和物相であることを示唆している。温度制御されたサンプルは別の無水修飾Dであり、無水条件下でのみ安定である。該D形体は約150℃で融解する。別の無水結晶修飾Eは該融解物から結晶化し、さらに加熱されると約175℃で融解する。最後に、形体Aは形体Eの融解物から結晶化する。形体Eは高温でのみ起こる準安定な結晶修飾でもある。
〔1〕206±3℃で融解することを特徴とする、化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンの無水多形体A。
〔2〕粉末X線図において、以下のd値:11.49Å、7.60Å、7.15Å、3.86Å、3.54Å及び3.47Åで特徴的な反射を有する、前記〔1〕記載の多形体A。
〔3〕10-40℃の温度で前記〔1〕記載の多形体Aに可逆的に変形することを特徴とする、化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンの無水多形体B。
〔4〕粉末X線図において、以下のd値:11.25Å、9.32Å、7.46Å、6.98Å及び3.77Åで特徴的な反射を有する、前記〔3〕記載の多形体B。
〔5〕30-100℃の温度で水を失い、且つDSC図において約150及び175℃でさらなる熱効果を示すことを特徴とする、化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンの多形体C。
〔5〕’30-100℃の温度で水を失い、且つDSC図において約150〜175℃でさらなる熱効果を示すことを特徴とする、化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンの多形体C。
〔6〕粉末X線図において、以下のd値:12.90Å、11.10Å、6.44Å、3.93Å及び3.74Åで特徴的な反射を有する、前記〔5〕記載の多形体C。
〔7〕150±3℃で融解することを特徴とする、化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンの無水多形体D。
〔8〕175±3℃で融解することを特徴とする、化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンの無水多形体E。
〔9〕前記〔5〕記載の多形体Cを調製する方法であって、(a)1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンをメタノール中で還流する工程、(b)該メタノール性溶液を40-60℃の温度まで冷却する工程、(c)tert.-ブチルメチルエーテルなどの溶媒を加える工程、(d)得られた懸濁液をまずは15-25℃まで、続いて0-5℃まで冷却する工程、(e)結晶を吸引濾過する工程、及び(f)70℃の温度の真空下で乾燥する工程、を特徴とする方法。
〔10〕工程(a)の後に前記熱い溶液を濾過する、前記〔9〕記載の方法。
〔11〕I型及びII型糖尿病、前糖尿病又は減少した糖耐性、さらに関節リウマチ、肥満、又はカルシトニン誘導骨粗鬆症を有する患者、並びに同種移植が行われた患者の治療のための医薬組成物を調製するための、化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンの多形体A、B、又はCの1種の使用。
〔12〕化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンに加えて1種以上の不活性キャリア及び/又は希釈剤を含有する薬剤であって、少なくとも0.1%〜0.5%の多形体A、B、又はCの1種を含有することを特徴とする、薬剤。
Claims (10)
- 化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンの無水多形体Aの調製方法であって、無水多形体Aが、
(a)1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンを無水エタノール中でリフラックスして混合物を得、任意に該混合物を濾過する工程、
(b)工程(a)で得られた前記混合物又は濾過物を結晶化が開始するまで冷却する工程、
(c)溶媒で希釈する工程、
(d)前記溶媒混合物を吸引濾過する工程、及び
(e)工程(d)から得られた濾過物を45℃の真空下で乾燥する工程、によって調製されるか、又は、無水多形体B、或いは無水多形体Aと無水多形体Bとの混合物を>40℃の温度まで加熱することによって調製され、
ここで、無水多形体Bが、10-40℃の温度で無水多形体Aに可逆的に変形し、無水多形体Aが、25±15℃の温度でエナンチオトロピー相転移を示し、かつ、
無水多形体Aが、206±3℃で融解することを特徴とする、無水多形体Aの調製方法。 - 無水多形体Aが、さらに、粉末X線図において、以下のd値:11.59Å、7.60Å、7.15Å、3.86Å、3.54Å及び3.47Åで特徴的な反射を有する、請求項1記載の方法。
- 化合物1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンの無水多形体Bの調製方法であって、無水多形体Bが、
(a)1-[(4-メチル-キナゾリン-2-イル)メチル]-3-メチル-7-(2-ブチン-1-イル)-8-(3-(R)-アミノ-ピペリジン-1-イル)-キサンチンを無水エタノール中に溶解させてリフラックスして混合物を得、任意に該混合物を濾過する工程、
(b)工程(a)で得られた前記混合物又は濾過物を結晶化のために10℃以下の温度まで冷却する工程、
(c)溶媒で希釈する工程、
(d)前記溶媒混合物を吸引濾過する工程、及び
(e)工程(d)から得られた濾過物を10℃以下の温度の真空下で乾燥する工程、によって調製されるか、又は、無水多形体A、或いは無水多形体Aと無水多形体Bとの混合物を<10℃の温度まで冷却することによって調製され、無水多形体Bが、10-40℃の温度で請求項1記載の無水多形体Aに可逆的に変形し、無水多形体Aが、206±3℃で融解し、かつ、無水多形体Aが、25±15℃の温度でエナンチオトロピー相転移を示すことを特徴とする、無水多形体Bの調製方法。 - 多形体Bが、さらに、粉末X線図において、以下のd値:11.3Å、9.36Å、7.48Å、7Å及び3.77Åで特徴的な反射を有する、請求項3記載の方法。
- 無水多形体Aが、図3に示されるような粉末X線図を有する、請求項1、2又は5記載の方法。
- 無水多形体Bが、図4に示されるような粉末X線図を有する、請求項3、4又は6記載の方法。
- 無水多形体Aの粉末X線図が、請求項4記載の無水多形体Bの特徴的な反射を有さない、請求項1、2、5又は7に記載の方法。
- 無水多形体Bの粉末X線図が、請求項2記載の無水多形体Aの特徴的な反射を有さない、請求項3、4、6又は8に記載の方法。
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JP2018090635A (ja) * | 2006-05-04 | 2018-06-14 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | 多形体 |
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