JP7203083B2 - エントレクチニブを含む薬学的組成物 - Google Patents
エントレクチニブを含む薬学的組成物 Download PDFInfo
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- JP7203083B2 JP7203083B2 JP2020502346A JP2020502346A JP7203083B2 JP 7203083 B2 JP7203083 B2 JP 7203083B2 JP 2020502346 A JP2020502346 A JP 2020502346A JP 2020502346 A JP2020502346 A JP 2020502346A JP 7203083 B2 JP7203083 B2 JP 7203083B2
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- methyl
- indazol
- ylamino
- pyran
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Description
本出願は、2017年7月19日に出願された米国仮特許出願第62/534,585号の利益および優先権を主張し、その内容は、参照によりそれらの全体が本明細書に組み込まれる。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミド、無水ラクトース、ヒプロメロース、クロスポビドンの粒内部分、および酒石酸を一緒に添加し、ブレンドして、第1の混合物を形成することと、
第1の混合物をふるい分けて、ふるい分けされた第1の混合物を形成することと、
ふるい分けされた第1の混合物をブレンドして、第2の混合物を形成することと、
第2の混合物をふるい分けて、ふるい分けされた第2の混合物を形成することと、
ふるい分けされた第2の混合物をブレンドして、第3の混合物を形成することと、
ステアリン酸マグネシウムの粒内部分を第3の混合物に添加し、ブレンドして、第4の混合物を形成することと、
第4の混合物を圧縮および粉砕して、第5の混合物を形成することと、
微結晶セルロース、クロスポビドンの粒外部分、およびコロイド状二酸化ケイ素を第5の混合物に添加し、ブレンドして、第6の混合物を形成することと、
ステアリン酸マグネシウムの粒外部分を第6の混合物に添加し、ブレンドして、薬学的組成物を形成することと、を含むか、それらから本質的になるか、またはそれらからなる方法で調製される。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドおよびフマル酸を含む薬学的組成物を次のように調製した。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドおよび塩酸グリシンを含む薬学的組成物を次のように調製した。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドおよび塩酸ベタインを含む薬学的組成物を次のように調製した。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドおよび塩酸ベタインを含む薬学的組成物を次のように調製した。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドおよび塩酸ベタインを含む薬学的組成物を次のように調製した。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドおよび塩酸ベタインを含む薬学的組成物を次のように調製した。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドおよび塩酸ベタインを含む薬学的組成物を次のように調製した。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドおよびフマル酸を含む薬学的組成物を次のように調製した。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドと混合されるマレイン酸、フマル酸、クエン酸、および酒石酸の適合性を調査した。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドおよびフマル酸を含む薬学的組成物を次のように調製した。
HPLCによって測定される結果を以下に示す。
50mg、100mg、および200mgのN-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドを含むが、少なくとも1つの酸味料を含まない硬ゼラチンカプセルは、次のように調製する。
健康なヒト対象における比較薬物動態研究を実施し、200mgの投与量強度の薬学的組成物F1(実施例11に記載)を200mgの投与量強度の薬学的組成物F2(実施例10に記載)と比較した。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドおよび塩酸ベタインを含む薬学的組成物を次のように調製した。
健康なヒト対象における比較薬物動態研究を実施し、PPIランソプラゾールありまたはなしでのF2Aの単回投与を比較して、ある場合、PPIの効果を決定した。
絶食または喫食条件下PPIありでの製剤F1(N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドを含み、少なくとも1つの酸味料を含まない薬学的組成物)、F2(N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドと共に酸味料としてフマル酸を含む薬学的組成物)、およびF2A(N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドと共に酸味料としてベタイン塩酸を含む薬学的組成物)の投与についての薬物動態データを以下の表で比較する。
薬物動態パラメータを、100、200、400、および800mg/m2/日の用量でのF1の連続投与後の製剤F1の食物との投与について評価した。以下の表に示されるように、F1曝露(CmaxおよびAUC)は、100mg/m2~400mg/m2の用量に比例した用量で増加した。曝露は、各用量レベルで1日目と比較して約2倍高い傾向があった。800mg/m2では、F1の曝露は、400mg/m2投与に匹敵し、14日目に同様の蓄積を示した。28日目に、おそらく研究変数の組み合わせによって、14日目と比較してより低い曝露が見られた。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドおよび酒石酸を含む薬学的組成物を次のように調製する。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドおよび酒石酸を含む薬学的組成物は、ステップ(a)で使用されたTFC Lab Micro Roller Compactorが2,500rpmの速度および750psiの油圧に設定され、ステップ(a)で使用されたFrewitt発振器が0.80mmスクリーンを備えたことを除いて、以下に挙げる量で成分を利用し、実施例17に開示される手順と同様の手順に従って調製する。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドおよび酒石酸を含む薬学的組成物は、ステップ(a)で使用されたTFC Lab Micro Roller Compactorが2,500rpmの速度および750psiの油圧に設定され、ステップ(a)で使用されたFrewitt発振器が0.80mmスクリーンを備えたことを除いて、以下に挙げる量で成分を利用し、実施例17に開示される手順と同様の手順に従って調製する。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドおよび酒石酸を含む薬学的組成物は、ステップ(a)で使用されたTFC Lab Micro Roller Compactorが2,500rpmの速度および750psiの油圧に設定され、ステップ(a)で使用されたFrewitt発振器が0.80mmスクリーンを備えたことを除いて、以下に挙げる量で成分を利用し、実施例17に開示される手順と同様の手順に従って調製する。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドおよび酒石酸を含む薬学的組成物を次のように調製した。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドおよび酒石酸を含む薬学的組成物は、以下に挙げる量の成分を利用し、実施例21に開示される手順と同様の手順に従って調製した。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドおよび酒石酸を含む薬学的組成物は、以下に挙げる量の成分を利用し、実施例21に開示される手順と同様の手順に従って調製した。
600mgの投与量強度の薬学的組成物F05(実施例20に記載)を、600mgの投与量強度の薬学的組成物F06(実施例21に記載)と、600mgの投与量強度の薬学的組成物F07(実施例22に記載)と比較して、健康なヒト対象における比較薬物動態研究を実施し、N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドを、賦形剤と混合し、得られた薬学的組成物を封入する前に粉砕したことを除いて、600mgの投与量強度のF2A(実施例13に記載)に類似した薬学的組成物と比較した。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミドおよび酒石酸を含む薬学的組成物は、以下に挙げる量の成分を利用し、実施例21に開示される手順と同様の手順に従って調製した。
実施例26 F06およびF06-100を含むカプセルの製造プロセス
1)粒内ブレンドの製造:
1.N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-2H-ピラン-4-イルアミノ)-ベンズアミド、無水ラクトース、ヒプロメロース、酒石酸、クロスポビドン(部分1)をトートブレンダーに入れ、約125回転でブレンドする。予備ブレンドを30メッシュスクリーンに通してふるいにかける。
2.ふるいにかけた予備ブレンドをブレンダーに入れ、約250回転でブレンドする。予備ブレンドを30メッシュスクリーンに通してふるいにかける。
3.ふるいにかけた予備ブレンドをブレンダーに入れ、さらに約250回転でブレンドする。
4.ステアリン酸マグネシウム(部分1)を20メッシュスクリーンに通してふるいにかけ、ブレンダーに加え、125回転でブレンドする。
5.ブレンドをローラー圧縮して、圧縮された材料を得る。
6.ローラー圧縮された材料を0.80mmスクリーンに通す。
2)粒外ブレンドの製造:
1.粉砕された材料の収率を使用して、微結晶セルロース、クロスポビドン(部分2)、コロイド状二酸化ケイ素、およびステアリン酸マグネシウム(部分2)の必要量を調整および再計量する。
2.ステアリン酸マグネシウムを分離したまま、微結晶セルロース、クロスポビドン(部分2)、コロイド状二酸化ケイ素、およびステアリン酸マグネシウム(部分2)を20メッシュスクリーンに通してふるいにかける。
3.ふるいにかけた微結晶セルロース、クロスポビドン(部分2)、コロイド状二酸化ケイ素、および粉砕材料をブレンダーに入れ、約250回転でブレンドする。
4.ふるいにかけたステアリン酸マグネシウムをブレンダーに入れ、約125回転でブレンドして、最終乾式造粒ブレンドを作成する。
3)封入:
1.エンカプスレーターを使用して、連続監視しながら、それぞれ200mgおよび100mg強度についてサイズ0またはサイズ2のHPMCカプセルシェルに最終乾式造粒ブレンドを充填する。
4)包装:
1.100mg強度(F06-100):30個の100mgカプセルを、1つの0.5g乾燥剤キャニスターを備える40cc白色HDPEボトルに入れ、33mm白色チャイルドレジスタントキャップで封をし、誘導加熱シールした。
2.200mg強度(F06):90個の200mgカプセルを、1つの2g乾燥剤キャニスターを備える150cc白色HDPEボトルに入れ、38mm白色チャイルドレジスタントキャップで封をし、誘導加熱シールした。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後2080nM~約2100nMの当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのCmaxを送達するための手段と、を含む、薬学的組成物であって、当該組成物が、約800mgの当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドの総用量を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後約2560nMの当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのCmaxを送達するための手段と、を含む、薬学的組成物であって、当該組成物が、約800mgの当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドの総用量を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後約28,900nM*時間~約30,800nM*時間の当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(0~24)を送達するための手段と、を含む、薬学的組成物であって、当該組成物が、約800mgの当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドの総用量を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後約40,400nM*時間の当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(0~24)を送達するための手段と、を含む、薬学的組成物であって、当該組成物が、約800mgの当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドの総用量を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後約2時間~約6時間の当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのTmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後約5時間~約12時間の当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのTmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後、90パーセント信頼区間に基づいて、2080nMの80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのCmaxを送達するための手段と、を含む、薬学的組成物であって、当該組成物が、約800mgの当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドの総用量を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後、90パーセント信頼区間に基づいて、2560nMの80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのCmaxを送達するための手段と、を含む、薬学的組成物であって、当該組成物が、約800mgの当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドの総用量を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後、90パーセント信頼区間に基づいて、30,800nM*時間の80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(0~24)を送達するための手段と、を含む、薬学的組成物であって、当該組成物が、約800mgの当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドの総用量を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後、90パーセント信頼区間に基づいて、40,400nM*時間の80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(0~24)を送達するための手段と、を含む、薬学的組成物であって、当該組成物が、約800mgの当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドの総用量を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドを対象に送達するための手段と、を含む、食物効果を示さない薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後約2時間~約5時間の当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのTmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後約4時間~約6時間の当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのTmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後約4時間~約8時間の当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのTmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後約4時間~約7時間の当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのTmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後約1500nM~約2800nMの当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのCmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後約1490nM~約3030nMの当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのCmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後約1670nM~約2930nMの当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのCmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後約1810nM~約3070nMの当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのCmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後約2210nM~約2990nMの当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのCmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後約1990nM~約2810nMの当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのCmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後約34,100nM*時間~約71,700nM*時間の当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(0~120)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後約32,500nM*時間~約79,700nM*時間の当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(0~120)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後約37,100nM*時間~約77,300nM*時間の当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(0~120)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後約38,900nM*時間~約78,700nM*時間の当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(0~120)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後約58,900nM*時間~約84,700nM*時間の当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(0~120)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後約51,300nM*時間~約77,500nM*時間の当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(0~120)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後約34,700nM*時間~約72,900nM*時間の当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(無限大)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後約33,200nM*時間~約81,200nM*時間の当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(無限大)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後約37,800nM*時間~約78,800nM*時間の当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(無限大)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後約39,100nM*時間~約79,700nM*時間の当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(無限大)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後約59,400nM*時間~約87,200nM*時間の当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(無限大)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後約51,700nM*時間~約79,700nM*時間の当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(無限大)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後、90パーセント信頼区間に基づいて、3.6時間の80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのTmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後、90パーセント信頼区間に基づいて、3.5時間の80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのTmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後、90パーセント信頼区間に基づいて、3.7時間の80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのTmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後、90パーセント信頼区間に基づいて、5時間の80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのTmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後、90パーセント信頼区間に基づいて、5.8時間の80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのTmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後、90パーセント信頼区間に基づいて、5.4時間の80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのTmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後、90パーセント信頼区間に基づいて、2150nMの80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのCmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後、90パーセント信頼区間に基づいて、2260nMの80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのCmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後、90パーセント信頼区間に基づいて、2300nMの80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのCmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後、90パーセント信頼区間に基づいて、2440nMの80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのCmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後、90パーセント信頼区間に基づいて、2600nMの80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのCmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後、90パーセント信頼区間に基づいて、2400nMの80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのCmaxを送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後、90パーセント信頼区間に基づいて、52,900nM*時間の80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(0~120)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後、90パーセント信頼区間に基づいて、56,100nM*時間の80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(0~120)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後、90パーセント信頼区間に基づいて、57,200nM*時間の80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(0~120)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後、90パーセント信頼区間に基づいて、58,800nM*時間の80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(0~120)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後、90パーセント信頼区間に基づいて、71,800nM*時間の80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(0~120)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後、90パーセント信頼区間に基づいて、64,400nM*時間の80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(0~120)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後、90パーセント信頼区間に基づいて、53,800nM*時間の80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(無限大)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後、90パーセント信頼区間に基づいて、57,200nM*時間の80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(無限大)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の絶食状態の対象への投与後、90パーセント信頼区間に基づいて、58,300nM*時間の80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(無限大)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後、90パーセント信頼区間に基づいて、59,400nM*時間の80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(無限大)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後、90パーセント信頼区間に基づいて、73,300nM*時間の80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(無限大)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと、
薬学的組成物の喫食状態の対象への投与後、90パーセント信頼区間に基づいて、65,700nM*時間の80%~125%である当該対象の血漿中の当該N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのAUC(無限大)を送達するための手段と、を含む、薬学的組成物。
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミド、無水ラクトース、ヒプロメロース、クロスポビドンの第1の部分、および酒石酸を一緒に添加し、ブレンドして、第1の混合物を形成することと、
第1の混合物をふるい分けて、ふるい分けされた第1の混合物を形成することと、
ふるい分けされた第1の混合物をブレンドして、第2の混合物を形成することと、
第2の混合物をふるい分けて、ふるい分けされた第2の混合物を形成することと、
ふるい分けされた第2の混合物をブレンドして、第3の混合物を形成することと、
ステアリン酸マグネシウムの第1の部分を第3の混合物に添加し、ブレンドして、第4の混合物を形成することと、
第4の混合物を圧縮および粉砕して、第5の混合物を形成することと、
微結晶セルロース、クロスポビドンの第2の部分、およびコロイド状二酸化ケイ素を第5の混合物に添加し、ブレンドして、第6の混合物を形成することと、
ステアリン酸マグネシウムの第2の部分を第6の混合物に添加し、ブレンドして、薬学的組成物を形成することと、を含む、方法で調製される、組成物。
Claims (17)
- N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミド、酒石酸、およびラクトース、ヒプロメロース、クロスポビドン、微結晶セルロース、コロイド状二酸化ケイ素、ステアリン酸マグネシウム、またはそれらの2つ以上の任意の組み合わせを含む固体混合物を含む、薬学的組成物。
- 前記N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドと酒石酸との間のモル比が、約0.5~約2である、請求項1に記載の薬学的組成物。
- 前記薬学的組成物が、錠剤またはカプセルの形態である、請求項1または2に記載の薬学的組成物。
- 前記薬学的組成物が、約25mg~約800mgの前記N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドを含む、請求項1に記載の薬学的組成物。
- 前記薬学的組成物が開放容器において40℃および75%相対湿度で3ヶ月間保存された後、前記N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドの約2%未満が前記薬学的組成物において分解する、請求項1に記載の薬学的組成物。
- 前記薬学的組成物が、錠剤またはカプセルの形態であり、前記錠剤またはカプセルは、USP装置タイプIバスケット法において50rpmで500mLの酢酸ナトリウム緩衝液中、4.5のpHで、および約37℃で試験した場合、前記N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドの少なくとも約30%が約60分で前記錠剤またはカプセルから放出されている溶解プロファイルを有する、請求項1に記載の薬学的組成物。
- 前記薬学的組成物が、マンニトールまたはイソマルトをさらに含む、請求項1~6のいずれか一項に記載の薬学的組成物。
- 前記薬学的組成物が、デンプンをさらに含む、請求項7に記載の薬学的組成物。
- 前記薬学的組成物中の前記マンニトールまたはイソマルト対前記デンプンの重量対重量比が、約1:1~約3:1である、請求項8に記載の薬学的組成物。
- 前記薬学的組成物が、絶食状態の対象に投与された場合、前記対象における薬物動態プロファイルを提供し、前記対象の血漿中の前記N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミドのTmaxが、前記薬学的組成物の前記対象への前記投与後約2時間~6時間である、請求項1に記載の薬学的組成物。
- 前記薬学的組成物が、対象に投与されたときに食物効果を示さない、請求項1~10のいずれか一項に記載の薬学的組成物。
- 約20重量/重量%~約60重量/重量%のN-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミド、約5重量/重量%~約20重量/重量%の酒石酸、約15重量/重量%~約35重量/重量%のラクトース、約1重量/重量%~約10重量/重量%のヒプロメロース、約1重量/重量%~約5重量/重量%の微結晶セルロース、約1重量/重量%~約10重量/重量%のクロスポビドン、約0.05重量/重量%~約5重量/重量%のコロイド状二酸化ケイ素、および約0.1重量/重量%~約5重量/重量%のステアリン酸マグネシウムを含む、請求項1~11のいずれか一項に記載の薬学的組成物。
- 約40重量/重量%~約50重量/重量%のN-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミド、約10重量/重量%~約15重量/重量%の酒石酸、約25重量/重量%~約30重量/重量%のラクトース、約3重量/重量%~約5重量/重量%のヒプロメロース(ヒドロキシプロピルメチルセルロース)、約2重量/重量%~約4重量/重量%の微結晶セルロース、約4重量/重量%~約7重量/重量%のクロスポビドン、約0.1重量/重量%~約1重量/重量%のコロイド状二酸化ケイ素、および約0.5重量/重量%~約2重量/重量%のステアリン酸マグネシウムを含む、請求項1~11のいずれか一項に記載の薬学的組成物。
- ラクトースが、無水ラクトースである、請求項12または13に記載の薬学的組成物。
- 請求項14に記載の薬学的組成物を調製するための方法であって、
N-[5-(3,5-ジフルオロベンジル)-1H-インダゾール-3-イル]-4-(4-メチル-ピペラジン-1-イル)-2-(テトラヒドロ-ピラン-4-イルアミノ)-ベンズアミド、無水ラクトース、ヒプロメロース、クロスポビドンの第1の部分、および酒石酸を一緒に添加し、ブレンドして、第1の混合物を形成することと、
前記第1の混合物をふるい分けて、ふるい分けされた第1の混合物を形成することと、
前記ふるい分けされた第1の混合物をブレンドして、第2の混合物を形成することと、
前記第2の混合物をふるい分けて、ふるい分けされた第2の混合物を形成することと、
前記ふるい分けされた第2の混合物をブレンドして、第3の混合物を形成することと、
ステアリン酸マグネシウムの第1の部分を前記第3の混合物に添加し、ブレンドして、第4の混合物を形成することと、
前記第4の混合物を圧縮および粉砕して、第5の混合物を形成することと、
微結晶セルロース、クロスポビドンの第2の部分、およびコロイド状二酸化ケイ素を前記第5の混合物に添加し、ブレンドして、第6の混合物を形成することと、
ステアリン酸マグネシウムの第2の部分を前記第6の混合物に添加し、ブレンドして、前記薬学的組成物を形成することと、を含む、方法。 - がんを有する対象を治療するための、請求項1~14のいずれか一項に記載の薬学的組成物。
- ROS1、TrkA、TrkB、もしくはTrkC陽性がん、またはそれらの組み合わせを有する対象を治療するための、請求項1~14のいずれか一項に記載の薬学的組成物。
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US20200163892A1 (en) | 2020-05-28 |
TWI785074B (zh) | 2022-12-01 |
BR112020000793A2 (pt) | 2020-07-14 |
JP2020527575A (ja) | 2020-09-10 |
CN110913842A (zh) | 2020-03-24 |
TW201907924A (zh) | 2019-03-01 |
EP3654952A1 (en) | 2020-05-27 |
AU2018302170A1 (en) | 2020-01-30 |
WO2019018570A1 (en) | 2019-01-24 |
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