JP6356888B2 - 疾患を治療するための、NF−κBの非ホルモン性ステロイド調節因子 - Google Patents
疾患を治療するための、NF−κBの非ホルモン性ステロイド調節因子 Download PDFInfo
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Description
式中、点線は、二重結合であってもよいことを示しており、
R1、R2、R3、およびR4はそれぞれ独立して、水素、非置換の低級アルキル、低級ハロアルキル、およびハロゲンからなる群から選択され、
R5は、水素、低級アルキル、アリール、シクロアルキル、ヘテロシクロアルキル、およびヘテロアリールからなる群から選択され、前記低級アルキル、アリール、シクロアルキル、ヘテロシクロアルキル、およびヘテロアリールは、アシル、アルケニル、アルコキシ、アルキル、アルキニル、アミド、アミノ、アリール、アリールオキシ、シクロアルキル、ハロアルコキシ、ハロアルキル、ヘテロアルキル、ヘテロアリール、ヒドロキシ、ペルハロアルキコシ、およびチオールからなる群から選択された1つ以上の置換基で置換されていてもよく、
R6は、水素、ヒドロキシル、および低級アルキルからなる群から選択され、前記低級アルキルは、アルケニル、アルコキシ、アルキル、アルキニル、アリール、アリールオキシ、ハロアルコキシ、ハロアルキル、ヘテロアルキル、ヒドロキシ、およびチオールからなる群から選択された1つ以上の置換基で置換されていてもよく、
R7とR8は独立して、水素、非置換の炭素数1〜3のアルキルからなる群から選択されるか、または、R7とR8は一体となって、オキソまたは炭素数3〜6の飽和シクロアルキルを形成することができ、
R9は、水素、アシル、およびアルキルからなる群から選択され、前記アシルおよびアルキルは、アシル、アルケニル、アルコキシ、アルキル、アルキルアミノ、アルキルチオ、アルキニル、アミド、アミノ、アリール、アリールオキシ、アロイル、カルバメート、カルボキシル、シアノ、シクロアルキル、ハロゲン、ハロアルコキシ、ハロアルキル、ヘテロアルキル、ヘテロシクロアルキル、ヘテロアリール、ヒドラジニル、ヒロドキシ、メルカプチル、ニトロ、オキソ、ペルハロアルコキシ、スルホネート、アルキルスルホニル、N−スルホンアミド、S−スルホンアミド、およびチオールからなる群から選択された1つ以上の置換基で置換されていてもよい。
下記のスキームを用いて、本発明を実施することができる。
スキームI
実施例1〜3は、スキームVIに従って合成することができる。
2−オキソ−2−((6S,10R,13S)−6,10,13−トリメチル−3−オキソ−6,7,8,10,12,13,14,15−オクタヒドロ−3H−シクロペンタ[a]フェナントレン−17−イル)酢酸エチル
(10S,13S,17R)−17−ヒドロキシ−17−(2−ヒドロキシアセチル)−10,13−ジメチル−6,7,8,10,12,13,14,15,16,17−デカヒドロ−1H−シクロペンタ[a]フェナントレン−3(2H)−オン
(10S,13S,17R)−17−ヒドロキシ−17−(2−ヒドロキシアセチル)−10,13−ジメチル−6,7,8,10,12,13,14,15,16,17−デカヒドロ−3H−シクロペンタ[a]フェナントレン−3−オン
2−((10S,13S,17R)−17−ヒドロキシ−10,13−ジメチル−3−オキソ−2,3,6,7,8,10,12,13,14,15,16,17−ドデカヒドロ−1H−シクロペンタ[a]フェナントレン−17−イル)−2−オキソ酢酸エチル
(10S,13S,16R,17S)−17−(2−ヒドロキシアセチル)−10,13,16−トリメチル−6,7,8,10,12,13,14,15,16,17−デカヒドロ−3H−シクロペンタ[a]フェナントレン−3−オン
2−オキソ−2−((10S,13S,16R)−10,13,16−トリメチル−3−オキソ−6,7,8,10,12,13,14,15,16,17−デカヒドロ−3H−シクロペンタ[a]フェナントレン−17−イル)酢酸エチル
(10S,13S,16R,17S)−17−(2−ヒドロキシアセチル)−10,13,16−トリメチル−6,7,8,10,12,13,14,15,16,17−デカヒドロ−1H−シクロペンタ[a]フェナントレン−3(2H)−オン
(10S,13S,16R,17R)−17−ヒドロキシ−17−(2−ヒドロキシアセチル)−10,13,16−トリメチル−6,7,8,10,12,13,14,15,16,17−デカヒドロ−3H−シクロペンタ[a]フェナントレン−3−オン
(10S,13S,16S,17R)−17−ヒドロキシ−17−(2−ヒドロキシアセチル)−10,13,16−トリメチル−6,7,8,10,12,13,14,15,16,17−デカヒドロ−3H−シクロペンタ[a]フェナントレン−3−オン
(10S,13S,16R,17R)−17−ヒドロキシ−17−(2−ヒドロキシアセチル)−10,13,16−トリメチル−6,7,8,10,12,13,14,15,16,17−デカヒドロ−1H−シクロペンタ[a]フェナントレン−3(2H)−オン
(10S,13S,16S,17R)−17−ヒドロキシ−17−(2−ヒドロキシアセチル)−10,13,16−トリメチル−6,7,8,10,12,13,14,15,16,17−デカヒドロ−1H−シクロペンタ[a]フェナントレン−3(2H)−オン
(10S,13S,16S,17R)−17−ヒドロキシ−17−(2−ヒドロキシアセチル)−10,13−ジメチル−16−プロピル−6,7,8,10,12,13,14,15,16,17−デカヒドロ−1H−シクロペンタ[a]フェナントレン−3(2H)−オン
(10S,13S,16S,17R)−17−ヒドロキシ−17−(2−ヒドロキシアセチル)−10,13−ジメチル−16−プロピル−6,7,8,10,12,13,14,15,16,17−デカヒドロ−3H−シクロペンタ[a]フェナントレン−3−オン
(10S,13S,16S,17S)−17−(2−ヒドロキシアセチル)−10,13−ジメチル−16−プロピル−6,7,8,10,12,13,14,15,16,17−デカヒドロ−3H−シクロペンタ[a]フェナントレン−3−オン
(10S,13S,16R,17S)−17−(2−ヒドロキシアセチル)−10,13−ジメチル−16−プロピル−6,7,8,10,12,13,14,15,16,17−デカヒドロ−1H−シクロペンタ[a]フェナントレン−3(2H)−オン
(10S,13S,16R,17S)−17−(2−ヒドロキシアセチル)−10,13−ジメチル−16−フェニル−6,7,8,10,12,13,14,15,16,17−デカヒドロ−1H−シクロペンタ[a]フェナントレン−3(2H)−オン
(10S,13S,16S,17R)−17−ヒドロキシ−17−(2−ヒドロキシアセチル)−10,13−ジメチル−16−フェニル−6,7,8,10,12,13,14,15,16,17−デカヒドロ−1H−シクロペンタ[a]フェナントレン−3(2H)−オン
(10S,13S,16S,17R)−17−ヒドロキシ−17−(2−ヒドロキシアセチル)−10,13−ジメチル−16−フェニル−6,7,8,10,12,13,14,15,16,17−デカヒドロ−3H−シクロペンタ[a]フェナントレン−3−オン
(10S,13S,16R,17S)−17−(2−ヒドロキシアセチル)−10,13−ジメチル−16−フェニル−6,7,8,10,12,13,14,15,16,17−デカヒドロ−3H−シクロペンタ[a]フェナントレン−3−オン
(10S,13S,16S,17S)−17−(2−ヒドロキシアセチル)−10,13,16−トリメチル−6,7,8,10,12,13,14,15,16,17−デカヒドロ−3H−シクロペンタ[a]フェナントレン−3−オン
(10S,13S,16S,17S)−17−(2−ヒドロキシアセチル)−10,13,16−トリメチル−6,7,8,10,12,13,14,15,16,17−デカヒドロ−1H−シクロペンタ[a]フェナントレン−3(2H)−オン
2−オキソ−2−((10S,13S,16S,17S)−10,13,16−トリメチル−3−オキソ−2,3,6,7,8,10,12,13,14,15,16,17−ドデカヒドロ−1H−シクロペンタ[a]フェナントレン−17−イル)酢酸エチル
(10S,13S,16R,17S)−17−(2−ヒドロキシアセチル)−10,13,16,17−テトラメチル−6,7,8,10,12,13,14,15,16,17−デカヒドロ−1H−シクロペンタ[a]フェナントレン−3(2H)−オン
インビトロでのNF−κB阻害剤スクリーニングアッセイ
NF−κB応答配列の複数のコピーの下で調節したルシフェラーゼレポーターコンストラクト(カリフォルニア州フレモントのパノミックス)で安定的にトランスフェクションした骨格筋細胞C2C12を用いて、NF−κB阻害剤をスクリーニングした。これらの細胞は、10%ウシ胎児血清(FBS)(バージニア州マナッサスのATCC)、ペニシリン100U/ml、ストレプトマイシン100μg/ml、および100μg/mlのハイグロマイシンB(インディアナ州インディアナポリスのロシュ)を含むダルベッコ改変イーグル培地(DMEM)と共に、組織培養インキュベーター中で、37℃にて5%のCO2によって保持した。スクリーニングアッセイは、2連の96ウェルプレート中にて、筋芽細胞(10%FBSを含む培地中で増殖)内で、容積100μlのウェル当たり5×104細胞の細胞濃度で実施した。細胞は、さまざまな濃度(0.01μg/ml〜10μg/ml)の化合物で24時間、前処理してから、腫瘍壊死因子−α(TNF−α)(10ng/ml)でさらに24時間刺激した。ポジティブコントロールとして試験する各プレートには、プレドニゾロンを入れた。インキュベーションの完了後、細胞をPBSで2回洗浄し、細胞溶解緩衝液で溶解して、Centro LB960という照度計(ドイツ、バート・ヴィルドバートのベルトールドテクノロジーズ社を用いて、ルシフェラーゼ活性を測定した(ウィスコンシン州マディソンのプロメガ社)。薬物不存在下でのTNF−αの刺激による相対的発光単位を100%とみなすと共に、データは、TNF−αによって誘発されるNF−κB活性に対する阻害率(%)として表した。
+は、阻害率が80〜100%であることを示している。
++は、阻害率が60〜80%であることを示している。
+++は、阻害率が40〜60%であることを示している。
++++は、阻害率が20〜40%であることを示している。
*は、p値が0.01未満であることを示している。
TNF−αによって誘発される、NF−κBの活性化の阻害を核トランスロケーション免疫蛍光アッセイによって確認した。C2C12細胞をカバースリップ上で増殖させ、上記のようにTNF−αと最適濃度の化合物で処置した。細胞をアセトンで固定し、ウサギ抗NF−κB(p60)抗体/抗ウサギテキサスレッド(カリフォルニア州サンタクルーズのサンタクルーズ・バイオテク社)で染色し、4’,6−ジアミジノ−2−フェニルインドールHCl(DAPI)(カリフォルニア州インビトロジェン)で対比染色して、核を視覚化した。
個々のmdxマウス群(n=12〜14)をプレドニゾロン(1日当たり5mg/kg、飼料に混ぜて経口投与)、実施例1(1日当たり20および40mg/kg、飼料に混ぜて経口投与)、実施例2(1日当たり20および40mg/kg、飼料に混ぜて経口投与)で3カ月間処置した。処置期間中、すべてのマウスに対して、週に2回、30分のトレッドミル運動を行わせたところ、mdxマウスモデルの軽度の疾患表現型が明らかになった。
ロータロッド(イタリア、VAのウゴバジレ)による試験を用いて、運動神経と運動力を評価した。簡潔に言うと、マウスにロータロッド上で2日間トレーニングさせてから、データを収集した。各順化セッションは、4回のトレーニングセッション(1日2回)から構成させ、各セッションは5rpmの速度で120秒間持続させた)。各試験では、マウスを10rpmのロッド上に60秒間(安定化期間)置き、続いて、最初の25秒以内で10rpmから40rpmまで加速して、マウスがロッドから落下するか、または180秒に達するまで続けた。安定化期間中にマウスが落下したら、マウスをロッド上に戻し、セッションを最後まで行った。総試験時間は240秒であった(60秒の安定化時間と180秒の試験時間)。各試験を1日に2回(セッション間隔は2時間)、3日連続で行った。落下までの時間(秒)を記録し、6回のすべてのスコアをマウスごとに平均化した。この平均データを、3つの週齢群の各群のマウスにおける落下までの時間(秒)として表した。未処置マウスがロッド上に留まる能力には、有意な経時変化は見られなかった。
長趾伸(EDL)筋の遠位腱をサーボモーター/フォーストランスデューサー(カナダ、オンタリオ州リッチモンドヒルのオーロラ・サイエンティフィックのモデル305B)のレバーアームにしっかりと取り付け、近位腱を組織クランプに取り付けた。2本の白金電極の間で筋肉を刺激した。EDL用に、単一の0.2msの方形刺激パルスを用いて筋肉を最大上刺激して、最大単収縮力をもたらす長さ(L0)に筋長を調節した。30Hz、50Hz、80Hz、100Hz、120Hz、および150Hzという刺激周波数を用いて、筋肉をL0に保った状態で、ELD筋に関して、300msの一連の刺激パルス中に生じる最大等尺性強縮力(P0)を記録した。続いて、筋長をキャリパーで測定し、槽から筋肉を取り外した後、筋肉の質量を割り出した。各筋肉において、最適繊維長(Lf)は、事前に割り出した0.45というLf/L0比をL0に乗じることによって算出した。湿質量をLfと哺乳類の骨格筋密度(1.06mg/mm3)との積で除することによって、筋繊維の総断面積を割り出した。P0を筋繊維の総断面積で除することによって、最大等尺性比筋力(sP0)を割り出した。未処置群とプレドニゾロン処置群の比筋力には、統計的に有意な(p<0.05)差異は見られなかった。
未処置のmdxマウスの腓腹筋をヘマトキシリンおよびエオシン染色すると、有意な変性および炎症が見られる。実施例1および実施例2で処置したマウスの骨格筋では、未処置のmdxマウスおよびプレドニゾロン処置のmdxマウスと比べて、炎症、変性の有意な低下と、再生筋繊維の増大が見られた。プレドニゾロンを継続投与すると、変性が増大し、ジストロフィー骨格筋の再生が低下するようであった。
実施例の化合物の糖質コルチコイド受容体(GR)への受容体結合親和性を割り出すために、ヒトおよびマウスの糖質コルチコイド受容体α用のcDNA発現クローン(バキュロウイルス)を用いてリガンド結合アッセイを行った。さまざまなGRコンストラクトを含む肝臓抽出物を放射性標識3H−デキサメタゾン(アマシャム・ファルマシア・バイオテク)およびアッセイ緩衝液(10mMのTris−HCl、1.5mMのEDTA、10%のグリセロール、1mMのジチオトレイトール、および20mMのモリブデン酸ナトリウム、pH7.6)中の試験化合物とインキュベートした。シンチレーションプレートリーダーを用いて放射活性の量を測定した。デキサメタゾンは、マイクロモル濃度で3H−デキサメタゾンとの競合結合を示した。
Claims (9)
- アテローム硬化症、高コレステロール血症、心臓疾患、慢性心不全、虚血/再潅流、狭心症および心筋炎からなる群から選択される疾患の症候を低減するための医薬組成物であって、構造式:
- 前記疾患がアテローム硬化症である請求項1記載の組成物。
- 前記疾患が高コレステロール血症である請求項1記載の組成物。
- 前記疾患が心臓疾患である請求項1記載の組成物。
- 前記疾患が慢性心不全である請求項1記載の組成物。
- 前記疾患が虚血/再潅流である請求項1記載の組成物。
- 前記疾患が狭心症である請求項1記載の組成物。
- 前記疾患が心筋炎である請求項1記載の組成物。
- 錠剤またはカプセルを含む請求項1〜8のいずれかに記載の組成物。
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- 2009-05-28 ES ES11191434.7T patent/ES2548402T3/es active Active
- 2009-05-28 PT PT14173342T patent/PT2805720T/pt unknown
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