JP5543110B2 - カリウムatpチャネルオープナの塩およびその使用 - Google Patents
カリウムatpチャネルオープナの塩およびその使用 Download PDFInfo
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- JP5543110B2 JP5543110B2 JP2008549491A JP2008549491A JP5543110B2 JP 5543110 B2 JP5543110 B2 JP 5543110B2 JP 2008549491 A JP2008549491 A JP 2008549491A JP 2008549491 A JP2008549491 A JP 2008549491A JP 5543110 B2 JP5543110 B2 JP 5543110B2
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- diazoxide
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- A61K31/00—Medicinal preparations containing organic active ingredients
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
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Description
であり、R1は、水素、低級アルキル、置換低級アルキル、シクロアルキルおよび置換シクロアルキルからなる群から選択され、R1が、置換低級アルキルまたは置換シクロアルキルの場合、置換基は、アミノ基を含まず、
R2aは、水素であり、
Xは、1、2または3原子鎖であり、各原子は、独立して、炭素、硫黄および窒素から選択され、各元素は、ハロゲン、ヒドロキシル、低級アルキル、置換低級アルキル、低級アルコキシ、シクロアルキル、置換シクロアルキル、置換低級アルコキシ、で任意に置換され、前記鎖の原子が、低級アルキル、置換低級アルコキシまたは置換シクロアルキルで置換される場合、この置換基はアミノ基を含まず、
環Bが、飽和、単環不飽和、多環不飽和または芳香族であり、
上記の塩、プロドラッグおよび異性体を含む全ての生物学的等価物、である。。
であり、ここで、
R1は、水素、低級アルキル、置換低級アルキル、シクロアルキル、および置換シクロアルキルからなる群から選択され、R1が、置換低級アルキルまたは置換シクロアルキルである場合は、置換基は、アミノ基を含まず、
R2bは水素であり、
Xは、1,2または3原子鎖であり、各原子は、互いに独立して、炭素、硫黄および窒素から選択され、各原子は、ハロゲン、ヒドロキシル、低級アルキル、置換低級アルキル、低級アルコキシ、シクロアルキル、置換シクロアルキル、または、置換低級アルコキシで任意に選択され、前記鎖の原子が、置換低級アルキル、置換シクロアルキルまたは置換低級アルコキシで置換される場合、置換基にはアミノ基を含まず、
環Bは、飽和、一不飽和、多不飽和または芳香族であり、
これらの塩、プロドラッグおよび異性体を含む全ての生物学的等価物、である。
であり、ここで、
R1は、水素、低級アルキル、置換低級アルキル、シクロアルキル、および置換シクロアルキルからなる群から選択され、R1が、置換低級アルキルまたは置換シクロアルキルである場合は、置換基は、アミノ基を含まず、
R2aは水素であり、
R3は、水素、ハロゲン、低級アルキル、置換低級アルキル、シクロアルキルおよび置換シクロアルキルからなる群から選択され、R3が、置換低級アルキルである場合は、置換基はアミノ基を含まず、
R4は、水素、ハロゲン、低級アルキル、置換低級アルキル、シクロアルキルおよび置換シクロアルキルからなる群から選択され、R4が置換低級アルキルである場合、置換基はアミノ基を含まず、
こららの塩、プロドラッグ、および異性体を含む全ての生物学的等価物、である。
であり、ここで、
R1は、水素、低級アルキル、置換低級アルキル、および、シクロアルキルからなる群から選択され、R1が、置換低級アルキルである場合は、置換基は、アミノ基を含まず、
R2bは水素であり、
R3は、水素、ハロゲン、低級アルキル、置換低級アルキル、シクロアルキルおよび置換シクロアルキルからなる群から選択され、R3が、置換低級アルキルである場合は、置換基はアミノ基を含まず、
R4は、水素、ハロゲン、低級アルキル、置換低級アルキル、シクロアルキルおよび置換シクロアルキルからなる群から選択され、R4が置換低級アルキルである場合、置換基はアミノ基を含まず、
こららの塩、プロドラッグ、および異性体を含む全ての生物学的等価物、である。
であり、ここで、
R1は、置換基を有することもあるアミノ、置換基を有することもあるアルキル、置換基を有することもあるシクロアルキル、置換基を有することもあるヘテロシクリル、置換基を有することもあるヘテロシクリルアルキル、置換基を有することもあるアリール、置換基を有することもあるヘテロアリール、および、置換基を有することもあるヘテロアリールアルキル、からなる群から選択され、
R2aは、水素、および、低級アルキルからなる群から選択され、
Xは、1、2または3原子鎖であり、各原子は、互いに独立して、炭素、硫黄および窒素から選択され、各原子は、ハロゲン、ヒドロキシル、置換基を有することもある低級アルキル、置換基を有することもある低級アルキル、置換基を有することもある低級アルコキシ、置換基を有することもあるシクロアルキル、または、置換基を有することもあるアミノと選択的に置換され、
環Bは、飽和、一不飽和、多不飽和または芳香族であり、
R1またはXの置換体の少なくとも1つは、アミノ基を含み、
全ての生物学的等価物は、これらの塩、プロドラッグおよび異性体を含む。
R1は、置換基を有することもあるアミノ、置換基を有することもあるアルキル、置換基を有することもあるシクロアルキル、置換基を有することもあるヘテロシクリル、置換基を有することもあるヘテロシクリルアルキル、置換基を有することもあるアリール、置換基を有することもあるヘテロアリール、および、置換基を有することもあるヘテロアリールアルキルからなる群から選択され、
R2bは、水素および低級アルキルからなる群から選択され、
Xは、1,2または3原子鎖であり、各原子は、互いに独立して、炭素、硫黄および窒素から選択され、各原子は、ハロゲン、ヒドロキシル、置換基を有することもある低級アルキル、置換基を有することもある低級アルキル、置換基を有することもある低級アルコキシ、置換基を有することもあるシクロアルキル、または、置換基を有することもあるアミノと選択的に置換され、
環Bは、飽和、一不飽和、多不飽和または芳香族であり、
R1またはXの置換体の少なくとも1つは、アミノ基を含み、
これらの塩、プロドラッグおよび異性体を含む全ての生物学的等価物、である。
であり、ここで、
R1は、置換基を有することもあるアミノ、置換基を有することもあるアルキル、置換基を有することもあるシクロアルキル、置換基を有することもあるヘテロシクリル、置換基を有することもあるヘテロシクリルアルキル、置換基を有することもあるアリール、置換基を有することもあるヘテロアリール、および、置換基を有することもあるヘテロアリールアルキルからなる群から選択され、
R2aは、水素、低級アルキル、および置換低級アルキルからなる群から選択され、
R3は、水素、ハロゲン、置換基を有することもあるアルキル、置換基を有することもあるアミノ、置換基を有することもあるシクロアルキルおよび置換基を有することもあるアリールからなる群から選択され、
R4は、水素、ハロゲン、置換基を有することもあるアルキル、置換基を有することもあるアミノ、置換基を有することもあるシクロアルキルおよび置換基を有することもあるアリールからなる群から選択され、
R1、R2、および、R4の少なくとも1つは、アミノ基を含む置換基を含み、
これらの塩、プロドラッグ、および異性体を含む全ての生物学的等価物、である。
であり、ここで、
R1は、置換基を有することもあるアミノ、置換基を有することもあるアルキル、置換基を有することもあるシクロアルキル、置換基を有することもあるヘテロシクリル、置換基を有することもあるヘテロシクリルアルキル、置換基を有することもあるアリール、置換基を有することもあるヘテロアリール、および、置換基を有することもあるヘテロアリールアルキルからなる群から選択され、
R2bは、水素、低級アルキル、および、置換低級アルキルであり、
R3は、水素、ハロゲン、置換基を有することもあるアルキル、置換基を有することもあるアミノ、置換基を有することもあるシクロアルキルおよび置換基を有することもあるアリールからなる群から選択され、
R4は、水素、ハロゲン、置換基を有することもあるアルキル、置換基を有することもあるアミノ、置換基を有することもあるシクロアルキルおよび置換基を有することもあるアリールからなる群から選択され、
R1、R3、および、R4の少なくとも1つは、アミノ基を含む置換基を含み、
こららの塩、プロドラッグ、および異性体を含む全ての生物学的等価物、である。
群から選択され;b)塩は、式V、式VI、式VIIおよび式VIIIからなる群から選択されるKATPチャンネルオープナのアニオンを含み、c)式V、式VI、式VIIおよび式VIIIからなる群から選択されるKATPチャンネルオープナのカチオンを含み、少なくとも1つの置換基は、アミノ基を含む。
275(2)、717−720(2000)を参照されたい。スルフォニルウレア受容体のクローニングと密かにK+チャンネルの修正はIsomoto等による、J.Biol.Chem.271(40),24321〜24324(1996)により、また、D’hahan等によるPNAS、96(21), 12162〜12167(1999)に記載されている。
シクロアルキル、ヘテロシクリル、置換ヘテロシクリル、アリール、置換アリール、ヘテロアリール、置換へテロアリール、ヘテロアラルキル、置換へテロアラルキル、アラルキルまたは置換アラルキルである。
置換アシル、スルフォニルまたは置換スルフォニルである。
である。
RffおよびRuuは、独立して、アルキル、置換アルキル、アリール、置換アリール、ヘテロアリール、置換へテロアリール、アシル、置換アシル、スルフォニル、置換スルフォニルまたはシクロアルキルである。
は、独立して水素、または置換基を有することもある低級アルキルである。
置換アリールであり、Rqは、水素、または低級アルキルである。「ヘテロアリールスルフォニルアミノ」は、基−NRqS(O)2Rtを意味し、ここで、Rtは、置換基を有することもあるヘテロアリールであり、Rqは、水素または低級アルキルである。
(1)それらは、最小1年間周囲温で安定である、(2)それらは、経口投与が簡単である、(3)それらは、患者の服用順守を促進する、(4)投与されると、それらは、活性処方の高い吸収レベルを一貫して促進する、(5)1日1回又は2回経口投与されると、それらは、長時間枠に渡って式I〜VIIIの化合物の塩から選択されるKATPチャンネルオープナの放出を可能とし、そのために、式I〜VIIIの化合物の塩から選択されるKATPチャンネルオープナ、又は代謝的に活性な代謝産物の循環濃度は、治療的に有効な濃度以下に低下することはない、(6)それらは、治療される個人の消化管のpHに依存しない結果を達成する、及び、(7)それらは、胃内通過が完了する、又はほとんど完了するまで放出を遅らせる。
実施例
A.カリウムATPチャンネル活性化因子含有製剤
1.ジアゾキシド塩またはその誘導体の圧縮錠剤製剤
2.ジアゾキシド塩またはその誘導体のカプセル化かつコーティングされた微粒子製剤
3.ジアゾキシドまたはその誘導体の放出調節製剤
3.1.放出調節されるジアゾキシドまたはその誘導体の錠剤形状の製剤
3.2.ジアゾキシドまたはその誘導体を放出調製する圧縮錠剤形状の製剤
3.3.ジアゾキシドまたはその誘導体を放出調節する圧縮コーティング錠剤の製剤
3.4.ジアゾキシドコリン塩の放出調節錠剤形状の製剤
3.4.1.放出調節製剤
3.4.2.溶解試験
3.4.3.賦形剤の適合性試験
3.4.4.ジアゾキシドコリンの放出調節錠剤の安定性試験
3.5.浸透圧的な放出調節システムを用いたジアゾキシドまたはその誘導体の放出調節形態の投与量
4.ジアゾキシド塩の調製
4.1.ナトリウム塩の調製
4.2.カリウム塩の調製
4.3.コリン塩の調製
4.3.1.コリン塩の調製:薬効の実証(POC)
4.3.2.コリン塩の調製プロセス
4.3.2.1.単一の溶媒システムを具えた溶媒効率試験
4.3.2.2.二成分溶媒システムでの溶媒効率試験
4.3.2.3.共溶媒効率およびMTBEとの最適化
4.3.2.4.冷却プロファイルの最適化
4.3.2.5.共溶媒付加の最適速度
4.3.2.6.熱安定性試験
4.3.2.6. 50gスケールでのTHF中のジアゾキシドコリン塩の合成の実証
4.3.2.7. 50gスケールでの2−MeTHF中のジアゾキシドコリン塩の合成の実証
4.3.2.8. 250gスケールのTHFでのジアゾキシドコリン塩の合成
4.3.2.9. 2kgスケールのTHFでのジアゾキシドコリン塩の合成
4.4.ヘキサメチルヘキサメチレンジアンモニウムヒドロキシド塩の調製
4.5.ジアゾキシドおよびその誘導体の塩を取得することの失敗
4.5.1.アルカリ金属水酸化物からの塩を取得することの失敗
4.5.2. ’573特許によるメタノールまたはエタノールの塩の調製
4.5.3.酸性対イオンから塩を得られなかった
4.6.式V−VIIIの化合物の塩の調製
5.調製したジアゾキシド塩の特性
5.1.試験手順
5.2.フリーフォームジアゾキシドの特性
5.3.ジアゾキシドナトリウム塩の特性
5.4.カリウムジアゾキシド塩の特性
5.5.コリンジアゾキシド塩の特性
5.6.ヘキサメチルヘキサメチレンジアンモニウムヒドロキシド(HHDADH)のジアゾキシド塩の特性
6.ジアゾキシド塩の多形体
6.1.ジアゾキシドのコリン塩の多形体
6.1.1.ジアゾキシドコリン塩の多形体フォームBの実証
6.1.2.ジアゾキシドコリン塩の多形体フォームBの特性
6.1.3.ジアゾキシドコリン塩の多形体フォームBからジアゾキシドコリン塩の多形体フォームAの調製の実証
6.1.4.ジアゾキシドコリン塩の多形体フォームAの特性
6.1.5.ジアゾキシドコリン塩の多形体フォームに関するスクリーニング
6.1.5.1.有機溶媒の溶解度スクリーニング
6.1.5.2.単一溶媒結晶
6.1.5.3.二成分溶媒結晶
6.1.5.4.共溶媒として水を用いる二成分溶媒結晶
6.1.5.5.準安定ゾーン幅(MSZW)の評価
6.1.5.6.ジアゾキシドコリン塩フォームAの結晶化
6.1.5.7. 500mgスケールのジアゾキシドコリン塩フォームBの結晶
6.1.5.8. 2gスケールのジアゾキシドコリン塩フォームBの結晶
6.1.5.9.フォーム不純物の検出
6.2.ジアゾキシドカリウム塩の多形体フォーム
6.2.1.ジアゾキシドのカリウム塩の多形体フォームAの調製の実証
6.2.2.ジアゾキシドのカリウム塩の多形体フォームBの調製の実証
6.2.3.ジアゾキシドのカリウム塩の多形体フォームBの特性
6.2.4.フォームBからのジアゾキシドカリウム塩の多形体フォームAの調製の実証
6.2.5.フォームBからのジアゾキシドカリウム塩の多形体フォームCの調製
6.2.6.フォームBからのジアゾキシドカリウム塩の多形体フォームDの調製
6.2.7.フォームBからのジアゾキシドカリウム塩の多形体フォームEの調製
6.2.8.フォームBからのジアゾキシドカリウム塩の多形体フォームFの調製
6.2.9.フォームBからのジアゾキシドカリウム塩の多形体フォームGの調製
表27および28に示されるように、各種二成分溶媒システムからジアゾキシドカリウム塩を再結晶化することは、別のフォームにカリウム塩を変換することを示している。主溶媒としてのアセトニトリルを使用することは表27に示されており、主溶媒としてアセトンを使用することは、表28に示されている。表27に示されるように、第二溶媒として、メチル第三級ブチルエーテル、酢酸エチル、酢酸イソプロピル、テトラヒドロフラン、c−ヘキサン、ヘプタン、トルエンおよびジクロロメタンを用いて、アセトニトリルからジアゾキシドカリウム塩のフォームB多形体を再結晶化することによって、全てから、カリウム塩のフォームD多形体を得た。第二溶媒としてジオキサンを用いてアセトニトリルから再結晶化することによって、ジアゾキシドカリウム塩のフォームF多形体を得た。
6.2.11.ジアゾキシドカリウム塩の多形体フォームのスクリーニング
6.2.11.1.ジアゾキシドカリウム塩の多形体の溶解度スクリーニング
6.2.11.2.ジアゾキシドカリウム塩の多形体の単一溶媒スクリーニング
6.2.11.3.ジアゾキシドカリウム塩の多形体の二成分溶媒スクリーニング
6.2.11.4.ジアゾキシドカリウム塩の多形体Cの特性
6.2.11.5.ジアゾキシドカリウム塩の多形体フォームDの特性
6.2.11.6.ジアゾキシドカリウム塩の多形体フォームFの特性
B.インビボ肥満試験
1.肥満症動物モデル
2.ヒト肥満症治療
3.ジアゾキシドおよびフェタミンの同時投与によるヒト肥満症の治療
4.前ヒト糖尿病における糖尿病の予防
5.糖尿病患者治療のための、ジアゾキシドHCl及びメトフォルミンHClの徐放性放出共通製剤の使用
6.オランザピンによって治療される患者における体重増加の予防又は治療
7.肥満被験者に、プログリセム(登録商標)経口懸濁剤、または、ジアゾキシドコリン放出調節錠剤、として投与されるジアゾキシドの単一投与の比較
7.1.試験設計
7.1.1. 試験目標
7.1.2.試験の論理的根拠
7.1.3.試験対象患者基準
7.1.4.除外基準
7.1.5.無作為に抽出(Randmomization)
7.1.6.投薬
7.1.7.安全モニタ試験
7.1.8.調査評価項目
7.2.結果
7.2.1.有害事象
7.2.2.臨床化学
7.2.3.バイタルサイン
7.2.4.ジアゾキシド血漿薬物動態の予備評価
7.3.肥満被験者において、プログリセム(登録商標)経口懸濁剤、または、ジアゾキシドコリン放出調節錠剤、としてのジアゾキシドの単回投与の比較結果
Claims (25)
- a)ジアゾキシドのアニオンと;
b)コリン又はヘキサメチルヘキサメチレンジアンモニウムから選択されるカチオンと;
を含むことを特徴とする塩。 - 塩の多型であって、前記塩が、
ジアゾキシドと;
コリン又はヘキサメチルヘキサメチレンジアンモニウムからなる群から選択されるカチオンと;
を含むことを特徴とする塩の多型。 - 請求項2に記載の塩の多型において、前記カチオンがコリンであることを特徴とする塩の多型。
- 請求項3に記載の塩の多型において、前記多型のフォームAがXRPDパターンにおいて、2θ値(CuKα、40kV、40mA)が約9.8、10.5、14.9、17.8、17.9、18.5、19.5、22.1、22.6、26.2、29.6および31.2度で、特徴的ピークを有することを特徴とする塩の多型。
- 請求項3に記載の塩の多型において、前記多型のフォームBがXRPDパターンにおいて、2θ値(CuKα、40kV、40mA)が約8.9、10.3、12.0、18.3、20.6、24.1、24.5、26.3、27.1および28.9度で、特徴的ピークを有することを特徴とする塩の多型。
- ジアゾキシド塩の調製方法であって:
水酸化コリンおよびヘキサメチルヘキサメチレンジアンモニウムジヒドロキシドからなる群から選択される等モル量のカチオン源を、ジアゾキシドと反応させるステップであって、前記ジアゾキシドがアセトニトリル、低分子量のケトン、テトラヒドロフラン、ジメチルホルムアミドおよびn−メチルピロリジノンからなる群から選択される溶媒に溶解されるステップと;
前記溶媒を除去するステップと;
を具えることを特徴とするジアゾキシド塩の調製方法。 - ジアゾキシドコリン塩を生成する方法であって、当該方法が:
溶媒中にジアゾキシドを懸濁させて、コリン塩と混合するステップと;
該ジアゾキシドコリン塩の形成および析出が生じるのに十分な条件下で、共溶媒を前記懸濁液に加えるステップと;
該析出物を回収し、前記ジアゾキシドコリン塩を得るステップと;
を具えることを特徴とするジアゾキシドコリン塩を生成する方法。 - 請求項7に記載の方法において、前記溶媒がTHFまたは2−MeTHFであることを特徴とする方法。
- 請求項7に記載の方法において、前記共溶媒がMTBEであることを特徴とする方法。
- 請求項1に記載の塩において、前記カチオンがコリンであることを特徴とする塩。
- 請求項1に記載の塩において、前記カチオンがヘキサメチルヘキサメチレンジアンモニウムであることを特徴とする塩。
- 請求項1乃至11のいずれか一項に記載の塩を含む製剤。
- 請求項12に記載の製剤において、前記塩が:
a)ジアゾキシドのアニオンと;
b)コリン又はヘキサメチルヘキサメチレンジアンモニウムから選択されるカチオンと;
を含むことを特徴とする製剤。 - 請求項13に記載の製剤において、前記カチオンがコリンであることを特徴とする製剤。
- 請求項13に記載の製剤において、前記カチオンがヘキサメチルヘキサメチレンジアンモニウムであることを特徴とする製剤。
- 経口投与に適していることを特徴とする請求項12ないし15のいずれかに記載の製剤。
- 請求項12ないし15のいずれかに記載の製剤が、胃を通過した後まで前記製剤からKATPチャンネルオープナの放出を実質的に阻害する少なくとも1つの成分を更に含むことを特徴とする製剤。
- 肥満、体重超過または肥満傾向の対象に投与する製剤であって、(a)空腹時のインスリン分泌を阻害する、(b)グルコース刺激インスリン分泌を阻害する、(c)エネルギ消費を上昇させる、(d)脂肪のβ酸化を上昇させる、または(e)過食を阻害する、治療有効量の請求項12ないし15のいずれかに記載の製剤を含むことを特徴とする製剤。
- 肥満、体重超過または肥満傾向の対象に投与して体重を減量する製剤であって、治療有効量の請求項12ないし15のいずれかに記載の製剤を含むことを特徴とする製剤。
- 糖尿病前症の対象の糖尿病への移行するのを予防するために当該対象に投与する製剤であって、治療有効量の請求項12ないし15のいずれかに記載の製剤を含むことを特徴とする製剤。
- 抗精神薬で治療中の対象の体重増加、異常脂質血症、糖尿病または耐糖能障害を予防または治療するために当該対象に投与する製剤であって、治療有効量の請求項12ないし15のいずれかに記載の製剤を含むことを特徴とする製剤。
- アルツハイマ疾患またはその危険性に苦しむ当該対象を治療するために対象に投与する製剤であって、治療有効量の請求項12ないし15のいずれかに記載の製剤を含むことを特徴とする製剤。
- 低血糖症に苦しむ対象を治療するために対象に投与する製剤であって、治療有効量の請求項12ないし15のいずれかに記載の製剤を含むことを特徴とする製剤。
- 上昇したトリグリセリドによる高リポタンパク血漿を治療するために対象に投与する製剤であって、治療有効量の請求項12ないし15のいずれかに記載の製剤を含むことを特徴とする製剤。
- プラーダ・ヴィリ症候群に苦しむ対象を治療するために対象に投与する製剤であって、治療有効量の請求項12ないし15のいずれかに記載の製剤を含むことを特徴とする製剤。
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