JP2013523836A - 3−(6−(1−(2,2−ジフルオロベンゾ[d][1,3]ジオキソール−5−イル)シクロプロパンカルボキサミド)−3−メチルピリジン−2−イル)安息香酸の固体形態 - Google Patents
3−(6−(1−(2,2−ジフルオロベンゾ[d][1,3]ジオキソール−5−イル)シクロプロパンカルボキサミド)−3−メチルピリジン−2−イル)安息香酸の固体形態 Download PDFInfo
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Abstract
Description
本願は2010年4月7日付け出願の、発明の名称が「3−(6−(1−(2,2−ジフルオロベンゾ[d][1,3]ジオキソール−5−イル)シクロプロパンカルボキサミド)−3−メチルピリジン−2−イル)安息香酸」である、米国仮出願番号61/321729に対して35U.S.C第119条の下で優先権を主張するものであり、その内容を出典明示により本願明細書の一部とする。
発明の技術分野
を有する。
コンパウンド1・アセトン溶媒和物・形態A;
コンパウンド1・2−プロパノール溶媒和物・形態A;
コンパウンド1・アセトニトリル溶媒和物・形態A;
コンパウンド1・テトラヒドロフラン溶媒和物・形態A;
コンパウンド1・酢酸メチル溶媒和物・形態A;
コンパウンド1・2−ブタノン溶媒和物・形態A;
コンパウンド1・ギ酸エチル溶媒和物・形態A;および
コンパウンド1・2−メチルテトラヒドロフラン溶媒和物・形態A
を包含する。
本願明細書にて用いられるように、特記しない限り、以下の定義が当てはまる。
コンパウンド1・溶媒和物・形態A
a=16.5235(10)Å α=90°
b=12.7425(8)Å β=103.736(4)°
c=20.5512(13)Å γ=90°
コンパウンド1・塩酸塩・形態A
化合物・溶媒和物・形態Aおよびコンパウンド1・HCl塩・形態Aの合成
スキーム1 コンパウンド1の調製に使用される酸塩化物の合成
スキーム2 必要とする酸クロリドの別の合成法
スキーム3 コンパウンド1を調製するのに使用されるアミンの合成
スキーム4 コンパウンド1の酸付加塩の形成
コンパウンド1・溶媒和物・形態Aの、コンパウンド1の塩酸塩からの調製
コンパウンド1・HCl塩・形態Aのコンパウンド1の塩酸塩からの調製
コンパウンド1・溶媒和物・形態Aのコンパウンド1・形態Iからの調製
使用、組成物およい投与
医薬上許容される組成物
方法および処理
表1
実施例
方法および材料
示差走査熱量測定法(DSC)
ジェット・ミリング(Jet Milling)記載
XRPD(X−線粉末回折)
5−クロロメチル−2,2−ジフルオロ−1,3−ベンゾジオキソールの調製
(2,2−ジフルオロ−1,3−ベンゾジオキソール−5−イル)−アセトニトリルの調製
(2,2−ジフルオロ−1,3−ベンゾジオキソール−5−イル)−1−酢酸エチル−アセトニトリルの合成
(2,2−ジフルオロ−1,3−ベンゾジオキソール−5−イル)−アセトニトリルの合成
(2,2−ジフルオロ−1,3−ベンゾジオキソール−5−イル)−シクロプロパンカルボニトリルの調製
1−(2,2−ジフルオロ−1,3−ベンゾジオキソール−5−イル)−シクロプロパンカルボン酸の調製
1−(2,2−ジフルオロ−1,3−ベンゾジオキソール−5−イル)−シクロプロパンカルボニルクロリドの調製
3−(3−メチルピリジン−2−イル)安息香酸tert−ブチルの調製
2−(3−(tert−ブトキシカルボニル)フェニル)−3−メチルピリジン−1−オキシドの調製
3−(6−アミノ−3−メチルピリジン−2−イル)安息香酸tert−ブチルの調製
3−(6−(1−(2,2−ジフルオロベンゾ[d][1,3]ジオキソール−5−イル)− シクロプロパンカルボキサミド)−3−メチルピリジン−2−イル)安息香酸t−ブチルの調製
3−(6−(1−(2,2−ジフルオロベンゾ[d][1,3]ジオキソール−5−イル) シクロプロパンカルボキサミド)−3−メチルピリジン−2−イル)安息香酸・HCl塩の調製
3−(6−(1−(2,2−ジフルオロベンゾ[d][1,3]ジオキソール−5−イル) シクロプロパンカルボキサミド)−3−メチルピリジン−2−イル)安息香酸・形態I・方法Aの調製
3−(6−(1−(2,2−ジフルオロベンゾ[d][1,3]ジオキソール−5−イル) シクロプロパンカルボキサミド)−3−メチルピリジン−2−イル)安息香酸・形態I・方法Bの調製
コンパウンド1・溶媒和物・形態Aのコンパウンド1・形態Iからの調製
表4
コンパウンド1・HCl塩・形態Aの調製
表5
アッセイ
化合物のΔF508−CFTR修正特性を検出および測定するアッセイ
化合物のΔF508−CFTR修飾特性をアッセイするための膜電位光学方法
1.修正化合物の同定
2.増強剤化合物の同定
3.溶液
浴溶液#1(mM):NaCl 160、KCl 4.5、CaCl2 2、MgCl2 1、HEPES 10、NaOHを用いてpH7.4に調整)
クロリド不含の浴溶液:浴溶液#1中のクロリド塩をグルコン酸塩と置き換えた。
DMSO中10mMストック溶液として調製し、−20℃で貯蔵した。
DMSO中10mMストックとして調製し、−20℃で貯蔵した。
4.細胞培養
化合物のΔF508−CFTR調節特性をアッセイするための電気生理学的アッセイ
1.チャンバーアッセイの使用
2.修飾化合物の同定
3.増強剤としての化合物の同定
4.溶液
該溶液をNaOHでpH7.4に滴定した。
5.細胞培養
6.全細胞の記録
7.修正化合物の同定
8.増強剤化合物の同定
9.溶液
10.細胞培養
11.シングルチャネルの記録
12.溶液
13.細胞培養
Claims (55)
- コンパウンド1・溶媒和物・形態Aまたはコンパウンド1・HCl塩・形態Aとして特徴付けられる3−(6−(1−(2,2−ジフルオロベンゾ[d][1,3]ジオキソール−5−イル)シクロプロパンカルボキサミド)−3−メチルピリジン−2−イル)安息香酸(コンパウンド1)の固体形態。
- コンパウンド1・溶媒和物・形態Aが、空であるか、または少なくとも一部が溶媒で占められている、複数の反復空洞を含有するコンパウンド1の結晶格子として特徴付けられる、請求項1記載のコンパウンド1・溶媒和物・形態A。
- コンパウンド1・溶媒和物・形態Aが、複数の空洞が空である複数の反復空隙を含有するコンパウンド1の結晶格子として特徴付けられる、請求項1記載のコンパウンド1・溶媒和物・形態A。
- Cu K アルファ線を用いて得られるX−線粉末回折にて、21.5ないし21.9°、8.8ないし9.2°および10.8ないし11.2°での一または複数のピークで特徴付けられる、請求項1、2または3に記載のコンパウンド1・溶媒和物・形態A。
- Cu K アルファ線を用いて得られるX−線粉末回折にて、21.5ないし21.9°、8.8ないし9.2°、10.8ないし11.2°、18.0ないし18.4°および22.9ないし23.3°での一または複数のピークで特徴付けられる、請求項1、2または3に記載のコンパウンド1・溶媒和物・形態A。
- 21.70、8.98、11.04、18.16および23.06°での一または複数のピークで特徴付けられる、請求項1、2または3に記載のコンパウンド1・溶媒和物・形態A。
- 21.5ないし21.9°でのピークで特徴付けられる、請求項1、2または3に記載のコンパウンド1・溶媒和物・形態A。
- 21.70でのピークで特徴付けられる、請求項1、2または3に記載のコンパウンド1・溶媒和物・形態A。
- 8.8ないし9.2でのピークで特徴付けられる、請求項1、2または3に記載のコンパウンド1・溶媒和物・形態A。
- 8.98°でのピークでさらに特徴付けられる、請求項6ないし9のいずれか一項に記載のコンパウンド1・溶媒和物・形態A。
- 10.8ないし11.2°でのピークでさらに特徴付けられる、請求項6ないし10のいずれか一項に記載のコンパウンド1・溶媒和物・形態A。
- 11.04°でのピークでさらに特徴付けられる、請求項6ないし11のいずれか一項に記載のコンパウンド1・溶媒和物・形態A。
- 18.0ないし18.4°でのピークでさらに特徴付けられる、請求項6ないし12のいずれか一項に記載のコンパウンド1・溶媒和物・形態A。
- 18.16°でのピークでさらに特徴付けられる、請求項6ないし13のいずれか一項に記載のコンパウンド1・溶媒和物・形態A。
- 22.9ないし23.3°でのピークでさらに特徴付けられる、請求項6ないし14のいずれか一項に記載のコンパウンド1・溶媒和物・形態A。
- 23.06°でのピークでさらに特徴付けられる、請求項6ないし15のいずれか一項に記載のコンパウンド1・溶媒和物・形態A。
- 図1に回折パターンと実質的に同じパターンにより特徴付けられる、請求項2記載のコンパウンド1・溶媒和物・形態A。
- 溶媒和物が複数の反復空洞に適合するのに十分な大きさの有機溶媒和物からなる群より選択される、請求項2記載のコンパウンド1・溶媒和物・形態A。
- 溶媒和物がメタノール、エタノール、アセトン、イソプロパノール、アセトニトリル、テトラヒドロフラン、酢酸メチル、2−ブタノン、ギ酸エチル、酢酸エチルおよび2−メチルテトラヒドロフランからなる群より選択される、請求項18記載のコンパウンド1・溶媒和物・形態A。
- コンパウンド1・溶媒和物・形態AがTGAで測定された場合に1ないし10重量%の溶媒和物を含む、請求項18記載のコンパウンド1・溶媒和物・形態A。
- コンパウンド1・溶媒和物・形態AがTGAで測定された場合に2ないし5重量%の溶媒和物を含む、請求項20記載のコンパウンド1・溶媒和物・形態A。
- 融点が185℃から190℃までである、請求項2記載のコンパウンド1・溶媒和物・形態A。
- P21/n空間群および次の単位セルの寸法:
a=16.5235(10)Å α=90°
b=12.7425(8)Å β=103.736(4)°
c=20.5512(13)Å γ=90°
を有する、請求項2記載のコンパウンド1・溶媒和物・形態A。 - Cu K アルファ線を用いて得られるX−線粉末回折にて、8.8ないし9.2°、17.3ないし17.7°および18.2ないし18.6°での1または複数のピークにより特徴付けられる、請求項1記載のコンパウンド1・HCl塩・形態A。
- Cu K アルファ線を用いて得られるX−線粉末回折にて、8.8ないし9.2°、17.3ないし17.7°、18.2ないし18.6°、10.1ないし10.5°および15.8ないし16.2°での1または複数のピークにより特徴付けられる、請求項1記載のコンパウンド1・HCl塩・形態A。
- 8.96、17.51および18.45°での1または複数のピークにより特徴付けられる、請求項1記載のコンパウンド1・HCl塩・形態A。
- 8.96、17.51、18.45、10.33および16.01°での1または複数のピークにより特徴付けられる、請求項1記載のコンパウンド1・HCl塩・形態A。
- 8.8ないし9.2°でのピークにより特徴付けられる、請求項1記載のコンパウンド1・HCl塩・形態A。
- 8.96°でのピークにより特徴付けられる、請求項1記載のコンパウンド1・HCl塩・形態A。
- 18.2ないし18.6°でのピークによりさらに特徴付けられる、請求項28または29に記載のコンパウンド1・HCl塩・形態A。
- 18.45°でのピークによりさらに特徴付けられる、請求項28ないし30のいずれか一項に記載のコンパウンド1・HCl塩・形態A。
- 10.1ないし10.5°でのピークによりさらに特徴付けられる、請求項28ないし31のいずれか一項に記載のコンパウンド1・HCl塩・形態A。
- 10.3°でのピークによりさらに特徴付けられる、請求項28ないし32のいずれか一項に記載のコンパウンド1・HCl塩・形態A。
- 15.8ないし16.2°でのピークによりさらに特徴付けられる、請求項28ないし33のいずれか一項に記載のコンパウンド1・HCl塩・形態A。
- 16.01°でのピークによりさらに特徴付けられる、請求項28ないし34のいずれか一項に記載のコンパウンド1・HCl塩・形態A。
- 図21の回折パターンと実質的に同じパターンにより特徴付けられる請求項1記載のコンパウンド1・HCl塩・形態A。
- 図19に記載の二量体として特徴付けられる請求項1記載のコンパウンド1・HCl塩・形態A。
- 図20に記載のパッキング図により特徴付けられる請求項1記載のコンパウンド1・HCl塩・形態A。
- P−1空間群を有し、次の単位セルの寸法:
a=10.2702(2)Å、b=10.8782(2)Å、c=12.4821(3)Å、α=67.0270(10)°、β=66.1810(10)°およびγ=72.4760(10)°を有する、請求項1記載のコンパウンド1・HCl塩・形態A。 - コンパウンド1・溶媒和物・形態Aまたはコンパウンド1・HCl塩・形態Aが0.1μないし50μの粒径を有する、請求項1記載のコンパウンド1・溶媒和物・形態Aまたはコンパウンド1・HCl塩・形態A。
- コンパウンド1・溶媒和物・形態Aまたはコンパウンド1・HCl塩・形態Aが0.1μないし20μの粒径を有する、請求項1記載のコンパウンド1・溶媒和物・形態Aまたはコンパウンド1・HCl塩・形態A。
- コンパウンド1・溶媒和物・形態Aまたはコンパウンド1・HCl塩・形態Aが0.1μないし10μの粒径を有する、請求項1記載のコンパウンド1・溶媒和物・形態Aまたはコンパウンド1・HCl塩・形態A。
- コンパウンド1・溶媒和物・形態Aまたはコンパウンド1・HCl塩・形態Aが0.1μないし5μの粒径を有する、請求項1記載のコンパウンド1・溶媒和物・形態Aまたはコンパウンド1・HCl塩・形態A。
- コンパウンド1・溶媒和物・形態Aまたはコンパウンド1・HCl塩・形態Aが2.0μの粒径D50を有する、請求項1記載のコンパウンド1・溶媒和物・形態Aまたはコンパウンド1・HCl塩・形態A。
- 請求項1に記載のコンパウンド1・溶媒和物・形態Aまたはコンパウンド1・HCl塩・形態Aおよび医薬上許容される担体を含む、医薬組成物。
- 付加的な治療剤をさらに含む、請求項45記載の医薬組成物。
- 有効量の請求項1に記載のコンパウンド1・溶媒和物・形態Aまたはコンパウンド1・HCl塩・形態Aを哺乳動物に投与することを含む、該哺乳動物におけるCFTR介在疾患の治療方法。
- CFTR介在疾患が、嚢胞性線維症、喘息、喫煙誘発性COPD、慢性気管支炎、鼻副鼻腔炎、便秘、膵炎、膵機能不全、先天的な両側の輸精管の不在により惹起される男性不妊症(CBAVD)、軽度の肺疾患、突発性膵炎、アレルギー性気管支肺アスペルギルス症(ABPA)、肝疾患、遺伝的気腫、遺伝的ヘモクロマトーシス、凝固−線維素溶解 欠乏症、プロテインC欠乏症、1型遺伝的血管性浮腫、脂質処理欠乏症、家族性高コレステロール血症、1型乳糜血症、無βリポタンパク血症、リソソーム蓄積症、I−細胞疾患/シュードハーラー、ムコ多糖症、サンドホフ/テイ・サックス、クリーグラー・ナジャーII型、多腺性内分泌障害/高インスリン血症、真性糖尿病、ラロン型小人症、マイレオペルオキシダーゼ欠乏症、原発性副甲状腺機能低下症、黒色腫、グリカノシスCDG1型、先天性甲状腺機能亢進症、骨形成不全症、遺伝的低フィブリノゲン血症、ACT欠乏症、尿崩症(DI)、神経骨端軟骨性DI、神経原性DI、シャルコー−マリー−ツース症候群、ペリツェウス−メルツバッハー病、神経変性疾患s、アルツハイマー病、パーキンソン病、筋萎縮性側索硬化症、進行性核上麻痺、ピック病、数種のグルタミン神経障害、ハンチントン病、脊髄小脳変性症I型、脊髄および延髄性筋萎縮、デンタトルバル・パリドルイシャン、筋強直性ジストロフィー、海綿状脳症、遺伝的クロインフェルト−ヤコブ病プリオン蛋白の処理異常が原因、ファブリ病、ストロイスラー・シャインカー症候群、COPD、ドライアイ疾患、シェーグレン病、骨粗鬆症、骨減少症、ゴルハム症候群、クロリドチャネロパシー、先天性ミオトニー(トムソンおよびベッカー形態)、バーター症候群 type III、デント病、ビックリ病、てんかん、リソソーム蓄積症、アンジェルマン症候群、原発性線毛運動障害(PCD)、線毛の構造および/または機能の遺伝的障害、逆位したPCD、逆位していないPCDまたは線毛形成不全より選択される、請求項47記載の方法。
- CFTR介在疾患が嚢胞性線維症、気腫、COPD、ドライアイ疾患または骨粗鬆症である、請求項48記載の方法。
- CFTR介在疾患が嚢胞性線維症である、、請求項48記載の方法。
- 患者がΔF508変異の嚢胞性線維症膜貫通受容体(CFTR)を有する、請求項48ないし50のいずれか一項に記載の方法。
- 患者がR117H変異の嚢胞性線維症膜貫通受容体(CFTR)を有する、請求項48ないし50のいずれか一項に記載の方法。
- 患者がG551D変異の嚢胞性線維症膜貫通受容体(CFTR)を有する、請求項48ないし50のいずれか一項に記載の方法。
- 付加的な治療剤を投与することを含む、請求項48ないし50のいずれか一項に記載の方法。
- 請求項1に記載のコンパウンド1・溶媒和物・形態Aまたはコンパウンド1・HCl塩・形態Aおよびその使用のための説明書を含む、キット。
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Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2017533277A (ja) * | 2014-10-31 | 2017-11-09 | アッヴィ・エス・ア・エール・エル | 置換テトラヒドロピランおよび使用方法 |
Families Citing this family (76)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US20100074949A1 (en) | 2008-08-13 | 2010-03-25 | William Rowe | Pharmaceutical composition and administration thereof |
KR20060088537A (ko) | 2003-09-06 | 2006-08-04 | 버텍스 파마슈티칼스 인코포레이티드 | Atp-결합 카세트 수송체의 조절자 |
US7977322B2 (en) | 2004-08-20 | 2011-07-12 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
PL1773816T3 (pl) | 2004-06-24 | 2015-06-30 | Vertex Pharma | Modulatory transporterów posiadających kasetę wiążącą ATP |
NZ566208A (en) | 2005-08-11 | 2010-09-30 | Vertex Pharma | 2-Thiazolamide derivatives as modulators of cystic fibrosis transmembrane conductance regulators |
EP3208272B1 (en) | 2005-11-08 | 2020-01-08 | Vertex Pharmaceuticals Incorporated | Heterocyclic modulators of atp-binding cassette transporters |
EP2016065B1 (en) | 2005-12-28 | 2012-09-19 | Vertex Pharmaceuticals Incorporated | 1-(benzo[d][1,3]dioxol-5-yl)-n-(phenyl)cyclopropane-carboxamide derivatives and related compounds as modulators of atp-binding cassette transporters for the treatment of cystic fibrosis |
HUE049976T2 (hu) | 2005-12-28 | 2020-11-30 | Vertex Pharma | N-[2,4-bisz(1,1-dimetil-etil)-5-hidroxi-fenil]-1,4-dihidro-4-oxo-kinolin-3-karboxamid amorf alakjának gyógyászati kompozíciói |
US7645789B2 (en) | 2006-04-07 | 2010-01-12 | Vertex Pharmaceuticals Incorporated | Indole derivatives as CFTR modulators |
US10022352B2 (en) | 2006-04-07 | 2018-07-17 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
PL3327016T3 (pl) | 2006-04-07 | 2021-10-04 | Vertex Pharmaceuticals Incorporated | Wytwarzanie modulatorów transporterów posiadających kasetę wiążącą ATP |
US8563573B2 (en) | 2007-11-02 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Azaindole derivatives as CFTR modulators |
EP2164840A2 (en) | 2007-05-09 | 2010-03-24 | Vertex Pharmaceuticals Incorporated | Modulators of cftr |
HUE028426T2 (en) | 2007-08-24 | 2016-12-28 | Vertex Pharma | Isothiazolopyridinones for (inter alia) treating cystic fibrosis |
EP3012250B1 (en) | 2007-11-16 | 2017-11-08 | Vertex Pharmaceuticals Incorporated | Isoquinoline modulators of atp-binding cassette transporters |
RS55559B1 (sr) | 2007-12-07 | 2017-05-31 | Vertex Pharma | Čvrste forme 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioksol-5-il)ciklopropankarboksamido)-3-metilpiridin-2-il) benzoeve kiseline |
US20100036130A1 (en) | 2007-12-07 | 2010-02-11 | Vertex Pharmaceuticals Incorporated | Processes for producing cycloalkylcarboxamido-pyridine benzoic acids |
EA201070700A1 (ru) | 2007-12-07 | 2011-06-30 | Вертекс Фармасьютикалз Инкорпорейтед | Способы получения циклоалкилкарбоксамидопиридинбензойных кислот |
AU2008335439A1 (en) * | 2007-12-07 | 2009-06-18 | Vertex Pharmaceuticals Incorporated | Formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid |
JP5523352B2 (ja) | 2008-02-28 | 2014-06-18 | バーテックス ファーマシューティカルズ インコーポレイテッド | Cftr修飾因子としてのへテロアリール誘導体 |
NZ616097A (en) | 2008-03-31 | 2015-04-24 | Vertex Pharma | Pyridyl derivatives as cftr modulators |
MX2011003249A (es) * | 2008-09-29 | 2011-05-19 | Vertex Pharma | Unidades de dosificacion del acido 3-(6-(1-(2,2-difluorobenzo[d][1 ,3]dioxol-5-il)ciclopropancarboxamido)-3-metilpiridin-2-il)benzoi co. |
BRPI0919930A2 (pt) * | 2008-10-23 | 2016-02-16 | Vertex Pharma | moduladores de regulador de condutância transmembrana de fibrose cística |
KR101852173B1 (ko) | 2009-03-20 | 2018-04-27 | 버텍스 파마슈티칼스 인코포레이티드 | 낭성 섬유증 막횡단 전도도 조절자의 조정자의 제조 방법 |
GEP20156325B (en) | 2009-06-17 | 2015-07-10 | Vertex Pharma | Inhibitors of influenza viruses replication |
US8802868B2 (en) | 2010-03-25 | 2014-08-12 | Vertex Pharmaceuticals Incorporated | Solid forms of (R)-1(2,2-difluorobenzo[D][1,3]dioxo1-5-yl)-N-(1-(2,3-dihydroxypropyl-6-fluoro-2-(1-hydroxy-2-methylpropan2-yl)-1H-Indol-5-yl)-Cyclopropanecarboxamide |
NZ602838A (en) | 2010-04-07 | 2015-06-26 | Vertex Pharma | Pharmaceutical compositions of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid and administration thereof |
CN102933206A (zh) | 2010-04-07 | 2013-02-13 | 弗特克斯药品有限公司 | 3-(6-(1-(2,2-二氟苯并[d][1,3]二氧杂环戊烯-5-基)环丙烷甲酰胺基)-3-甲基吡啶-2-基)苯甲酸的固体形式 |
KR101984225B1 (ko) | 2010-04-22 | 2019-05-30 | 버텍스 파마슈티칼스 인코포레이티드 | 시클로알킬카르복스아미도-인돌 화합물의 제조 방법 |
US8563593B2 (en) | 2010-06-08 | 2013-10-22 | Vertex Pharmaceuticals Incorporated | Formulations of (R)-1-(2,2-difluorobenzo[D] [1,3] dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide |
UA118010C2 (uk) | 2011-08-01 | 2018-11-12 | Вертекс Фармасьютікалз Інкорпорейтед | Інгібітори реплікації вірусів грипу |
ME02650B (me) | 2011-11-08 | 2017-06-20 | Vertex Pharma | Modulatori atp- vezujućih kasetnih transportera |
UA114619C2 (uk) * | 2012-01-25 | 2017-07-10 | Вертекс Фармасьютікалз Інкорпорейтед | СКЛАД 3-(6-(1-(2,2-ДИФТОРОБЕНЗО[d][1,3]ДІОКСОЛ-5-ІЛ)ЦИКЛОПРОПАНКАРБОКСАМІДО)-3-МЕТИЛПІРИДИН-2-ІЛ)БЕНЗОЙНОЇ КИСЛОТИ |
BR112014021090B1 (pt) | 2012-02-27 | 2023-01-24 | Vertex Pharmaceuticals Incorporated | Composição farmacêutica e uso de n-[2,4-bis(1,1-dimetiletil)-5-hidróxifenil]-1,4-di-hidro-4-oxoquinolina3-carboxamida na preparação da mesma |
US8674108B2 (en) | 2012-04-20 | 2014-03-18 | Vertex Pharmaceuticals Incorporated | Solid forms of N-[2,4-bis(1,1-dimethylethy)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
AU2013290444B2 (en) | 2012-07-16 | 2018-04-26 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions of (R)-1-(2,2-diflurorbenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl) cyclopropanecarboxamide and administration thereof |
US8937178B2 (en) | 2013-03-13 | 2015-01-20 | Flatley Discovery Lab | Phthalazinone compounds and methods for the treatment of cystic fibrosis |
JP6963896B2 (ja) | 2013-11-12 | 2021-11-10 | バーテックス ファーマシューティカルズ インコーポレイテッドVertex Pharmaceuticals Incorporated | Cftr媒介性疾患の処置のための医薬組成物を調製する方法 |
RS59144B1 (sr) * | 2013-11-13 | 2019-09-30 | Vertex Pharma | Inhibitori replikacije virusa influence |
EP3421468B1 (en) | 2013-11-13 | 2020-11-04 | Vertex Pharmaceuticals Incorporated | Methods of preparing inhibitors of influenza viruses replication |
PT3925607T (pt) | 2014-04-15 | 2023-09-26 | Vertex Pharma | Composições farmacêuticas para o tratamento de doenças mediadas pelo regulador de condutância transmembranar da fibrose quística |
GB201415381D0 (en) | 2014-08-29 | 2014-10-15 | Algipharma As | Inhalable powder formulations of alginate oligomers |
TW202140422A (zh) | 2014-10-06 | 2021-11-01 | 美商維泰克斯製藥公司 | 囊腫纖維化症跨膜傳導調節蛋白之調節劑 |
KR20170063954A (ko) | 2014-10-07 | 2017-06-08 | 버텍스 파마슈티칼스 인코포레이티드 | 낭성 섬유증 막횡단 전도도 조절자의 조정제의 공-결정 |
RU2691136C2 (ru) | 2014-11-18 | 2019-06-11 | Вертекс Фармасьютикалз Инкорпорейтед | Способ проведения высокопроизводительной тестовой высокоэффективной жидкостной хроматографии |
GB201504878D0 (en) | 2015-03-23 | 2015-05-06 | Algipharma As | Use of alginate oligomers and CFTR modulators in the treatment of conditions associated with CFTR dysfuntion |
WO2016183116A1 (en) | 2015-05-13 | 2016-11-17 | Vertex Pharmaceuticals Incorporated | Methods of preparing inhibitors of influenza viruses replication |
WO2016183120A1 (en) | 2015-05-13 | 2016-11-17 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
WO2017017696A1 (en) * | 2015-07-27 | 2017-02-02 | Mylan Laboratories Limited | Process for the preparation of lumacaftor |
CA3000600A1 (en) | 2015-09-29 | 2017-04-06 | Mylan Laboratories Limited | Novel forms of lumacaftor and processes for the preparation thereof |
GB201517639D0 (en) | 2015-10-06 | 2015-11-18 | Algipharma As | Use of alginate oligomers to treat or prevent microbial overgrowth in the intestinal tract |
WO2017137900A1 (en) * | 2016-02-10 | 2017-08-17 | Lupin Limited | Amorphous lumacaftor and its solid dispersion |
HUP1600269A2 (hu) | 2016-04-25 | 2017-10-30 | Druggability Tech Ip Holdco Ltd | Lumacaftornak, sóinak és származékainak komplexei, eljárás azok elõállítására és azok gyógyászati készítményei |
HUP1600271A2 (hu) | 2016-04-25 | 2017-10-30 | Druggability Tech Ip Holdco Ltd | Ivacaftor és Lumacaftor sóinak és származékainak komplexei, eljárás azok elõállítására és azok gyógyszerészetileg elfogadható készítményei |
US10206915B2 (en) | 2016-04-25 | 2019-02-19 | Druggability Technologies Ip Holdco Limited | Complexes of Ivacaftor and its salts and derivatives, process for the preparation thereof and pharmaceutical compositions containing them |
US10383865B2 (en) | 2016-04-25 | 2019-08-20 | Druggability Technologies Ip Holdco Limited | Pharmaceutical combination composition comprising complex formulations of Ivacaftor and Lumacaftor and their salts and derivatives, process for their preparation thereof and pharmaceutical compositions containing them |
US10376501B2 (en) | 2016-04-25 | 2019-08-13 | Druggability Technologies Ip Holdco Limited | Complexes of lumacaftor and its salts and derivatives, process for the preparation thereof and pharmaceutical compositions containing them |
WO2018037350A1 (en) * | 2016-08-23 | 2018-03-01 | Laurus Labs Limited | Solid forms of lumacaftor, process for its preparation and pharmaceutical compositions thereof |
CN109803962B (zh) | 2016-09-30 | 2022-04-29 | 弗特克斯药品有限公司 | 囊性纤维化跨膜传导调控蛋白的调节剂、以及药物组合物 |
HUE052205T2 (hu) | 2016-12-09 | 2021-04-28 | Vertex Pharma | Cisztás fibrózis transzmembrán vezetõképesség szabályzó modulátora, gyógyszerészeti készítmények, kezelési eljárások és eljárás a modulátor elõállítására |
WO2018127846A1 (en) | 2017-01-09 | 2018-07-12 | Laurus Labs Limited | Process and crystalline forms of lumacaftor |
US11253509B2 (en) | 2017-06-08 | 2022-02-22 | Vertex Pharmaceuticals Incorporated | Methods of treatment for cystic fibrosis |
BR112020000941A2 (pt) | 2017-07-17 | 2020-07-21 | Vertex Pharmaceuticals Incorporated | métodos de tratamento para fibrose cística |
US11434201B2 (en) | 2017-08-02 | 2022-09-06 | Vertex Pharmaceuticals Incorporated | Processes for preparing pyrrolidine compounds |
CA3020592A1 (en) | 2017-10-17 | 2019-04-17 | Apotex Inc. | Novel crystalline form of lumacaftor |
WO2019079760A1 (en) | 2017-10-19 | 2019-04-25 | Vertex Pharmaceuticals Incorporated | CRYSTALLINE FORMS AND COMPOSITIONS OF CFTR MODULATORS |
CN107823643B (zh) * | 2017-11-03 | 2019-09-10 | 东南大学 | 预防或治疗阿尔茨海默症的药物、靶点及其应用 |
CN107812003B (zh) * | 2017-11-23 | 2021-02-09 | 南京市儿童医院 | Vx-809在制备治疗进行性家族性肝内胆汁淤积症药物中的应用 |
WO2019113476A2 (en) | 2017-12-08 | 2019-06-13 | Vertex Pharmaceuticals Incorporated | Processes for making modulators of cystic fibrosis transmembrane conductance regulator |
CN107982260A (zh) * | 2017-12-12 | 2018-05-04 | 南京市儿童医院 | VX-809在制备治疗Bartter综合征药物中的应用 |
TWI810243B (zh) | 2018-02-05 | 2023-08-01 | 美商維泰克斯製藥公司 | 用於治療囊腫纖化症之醫藥組合物 |
MX2020008268A (es) | 2018-02-15 | 2020-09-21 | Vertex Pharma | Macrociclos como moduladores del regulador de conductancia transmembrana de la fibrosis quistica, composiciones farmaceuticas de estos, su uso en el tratamiento de la fibrosis quistica y procesos para elaborarlos. |
US11414439B2 (en) | 2018-04-13 | 2022-08-16 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator |
TW202120517A (zh) | 2019-08-14 | 2021-06-01 | 美商維泰克斯製藥公司 | 製備cftr調節劑之方法 |
TW202115092A (zh) | 2019-08-14 | 2021-04-16 | 美商維泰克斯製藥公司 | 囊腫纖維化跨膜傳導調節蛋白之調節劑 |
BR112022002605A2 (pt) | 2019-08-14 | 2022-05-03 | Vertex Pharma | Formas cristalinas de moduladores de cftr |
Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2009073757A1 (en) * | 2007-12-07 | 2009-06-11 | Vertex Pharmaceuticals Incorporated | Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3] dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid |
Family Cites Families (101)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5304121A (en) | 1990-12-28 | 1994-04-19 | Boston Scientific Corporation | Drug delivery system making use of a hydrogel polymer coating |
US5994341A (en) | 1993-07-19 | 1999-11-30 | Angiogenesis Technologies, Inc. | Anti-angiogenic Compositions and methods for the treatment of arthritis |
HU218698B (hu) * | 1994-09-27 | 2000-11-28 | Janssen Pharmaceutica N.V. | Gyógyászati hatású N-szubsztituált piperidinil-(biciklusos benzoát)-származékok, intermedierjeik, előállításuk és alkalmazásuk |
US6099562A (en) | 1996-06-13 | 2000-08-08 | Schneider (Usa) Inc. | Drug coating with topcoat |
US6426331B1 (en) | 1998-07-08 | 2002-07-30 | Tularik Inc. | Inhibitors of STAT function |
CN1206219C (zh) * | 1998-12-18 | 2005-06-15 | 布里斯托尔-迈尔斯斯奎布药品公司 | 作为趋化因子受体活性调节剂的n-脲基烷基-哌啶化合物 |
PT1394150E (pt) | 1999-02-24 | 2011-02-17 | Hoffmann La Roche | Derivados de 4-fenilpiridina e a sua utilização como antagonistas dos receptores de nc-1 |
AU6687900A (en) * | 1999-06-18 | 2001-01-09 | Bayer Aktiengesellschaft | Phenoxy fluoropyrimidines |
TWI259180B (en) | 2000-08-08 | 2006-08-01 | Hoffmann La Roche | 4-Phenyl-pyridine derivatives |
US20100074949A1 (en) | 2008-08-13 | 2010-03-25 | William Rowe | Pharmaceutical composition and administration thereof |
WO2003084997A1 (en) | 2001-04-10 | 2003-10-16 | Transtech Pharma, Inc. | Probes, systems and methods for drug discovery |
US6627646B2 (en) * | 2001-07-17 | 2003-09-30 | Sepracor Inc. | Norastemizole polymorphs |
MXPA05003366A (es) | 2002-09-30 | 2005-10-05 | Univ California | Inhibidores de la proteina reguladora de conductancia transmembranal de la fibrosis quistica y usos de los mismos. |
US20050113423A1 (en) | 2003-03-12 | 2005-05-26 | Vangoor Frederick F. | Modulators of ATP-binding cassette transporters |
ES2624610T3 (es) | 2003-04-11 | 2017-07-17 | Ptc Therapeutics, Inc. | Compuestos de ácido 1,2,4-oxadiazol benzoico y su uso para la supresión sin sentido y el tratamiento de enfermedades |
WO2004110352A2 (en) | 2003-05-16 | 2004-12-23 | The Regents Of The University Of California | Compounds having activity in increasing ion transport by mutant-cftr and uses thereof |
ATE440825T1 (de) | 2003-06-06 | 2009-09-15 | Vertex Pharma | Pyrimidin-derivate zur verwendung als modulatoren von atp-bindende kassette transportern |
US7893094B2 (en) | 2003-06-27 | 2011-02-22 | The Henry M. Jackson Foundation For The Advancement Of Military Medicine, Inc. | Amphiphilic pyridinium compounds, method of making and use thereof |
KR20060088537A (ko) | 2003-09-06 | 2006-08-04 | 버텍스 파마슈티칼스 인코포레이티드 | Atp-결합 카세트 수송체의 조절자 |
US20050070718A1 (en) | 2003-09-30 | 2005-03-31 | Abbott Gmbh & Co. Kg | Heteroaryl-substituted 1,3-dihydroindol-2-one derivatives and medicaments containing them |
ZA200603515B (en) | 2003-10-08 | 2007-11-28 | Vertex Pharma | Modulators of ATP-binding cassette transporters |
CN101675928A (zh) | 2003-11-14 | 2010-03-24 | 沃泰克斯药物股份有限公司 | 可用作atp-结合弹夹转运蛋白调控剂的噻唑和噁唑 |
AU2005210474B2 (en) | 2004-01-30 | 2011-07-07 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-Binding cassette transporters |
US7977322B2 (en) | 2004-08-20 | 2011-07-12 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
WO2005094374A2 (en) | 2004-03-30 | 2005-10-13 | The Regents Of The University Of California | Hydrazide-containing cftr inhibitor compounds and uses thereof |
EP1765347A4 (en) | 2004-06-04 | 2008-10-01 | Univ California | COMPOUNDS WITH ION TRANSPORTER HEALING EFFECT BY MUTANT CFTR AND ITS USE |
US8354427B2 (en) | 2004-06-24 | 2013-01-15 | Vertex Pharmaceutical Incorporated | Modulators of ATP-binding cassette transporters |
US20140343098A1 (en) | 2004-06-24 | 2014-11-20 | Vertex Pharmaceuticals Incorporated | Modulators of atp-binding cassette transporters |
PL1773816T3 (pl) | 2004-06-24 | 2015-06-30 | Vertex Pharma | Modulatory transporterów posiadających kasetę wiążącą ATP |
EP1815206B1 (en) | 2004-10-13 | 2016-04-06 | PTC Therapeutics, Inc. | Compounds for nonsense suppression, and methods for their use |
US8242149B2 (en) | 2005-03-11 | 2012-08-14 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-binding cassette transporters |
KR20070114820A (ko) | 2005-03-18 | 2007-12-04 | 더 리젠츠 오브 더 유니버시티 오브 캘리포니아 | 돌연변이-cftr 처리를 보정하는데 활성을 가지는화합물 및 이것의 사용 |
US7297700B2 (en) | 2005-03-24 | 2007-11-20 | Renovis, Inc. | Bicycloheteroaryl compounds as P2X7 modulators and uses thereof |
NZ562197A (en) | 2005-04-08 | 2010-09-30 | Ptc Therapeutics Inc | Compositions of an orally active 1,2,4-oxadiazole for nonsense mutation suppression therapy |
WO2006127588A2 (en) | 2005-05-24 | 2006-11-30 | Vertex Pharmaceuticals Incorporated | Modulators of atp-binding cassette transporters |
NZ566208A (en) | 2005-08-11 | 2010-09-30 | Vertex Pharma | 2-Thiazolamide derivatives as modulators of cystic fibrosis transmembrane conductance regulators |
CA2624683A1 (en) | 2005-10-06 | 2007-04-19 | Vertex Pharmaceuticals Incorporated | Modulators of atp-binding cassette transporters |
EP3208272B1 (en) | 2005-11-08 | 2020-01-08 | Vertex Pharmaceuticals Incorporated | Heterocyclic modulators of atp-binding cassette transporters |
US20120232059A1 (en) | 2005-11-08 | 2012-09-13 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-Binding Cassette Transporters |
JP2009521468A (ja) | 2005-12-24 | 2009-06-04 | バーテックス ファーマシューティカルズ インコーポレイテッド | Abc輸送体の調節因子としてのキノリン−4−オン誘導体 |
CA2635214A1 (en) | 2005-12-27 | 2007-07-05 | Vertex Pharmaceuticals Incorporated | Compounds useful in cftr assays and methods therewith |
US7671221B2 (en) | 2005-12-28 | 2010-03-02 | Vertex Pharmaceuticals Incorporated | Modulators of ATP-Binding Cassette transporters |
HUE049976T2 (hu) | 2005-12-28 | 2020-11-30 | Vertex Pharma | N-[2,4-bisz(1,1-dimetil-etil)-5-hidroxi-fenil]-1,4-dihidro-4-oxo-kinolin-3-karboxamid amorf alakjának gyógyászati kompozíciói |
EP2016065B1 (en) | 2005-12-28 | 2012-09-19 | Vertex Pharmaceuticals Incorporated | 1-(benzo[d][1,3]dioxol-5-yl)-n-(phenyl)cyclopropane-carboxamide derivatives and related compounds as modulators of atp-binding cassette transporters for the treatment of cystic fibrosis |
US7645789B2 (en) | 2006-04-07 | 2010-01-12 | Vertex Pharmaceuticals Incorporated | Indole derivatives as CFTR modulators |
PL3327016T3 (pl) | 2006-04-07 | 2021-10-04 | Vertex Pharmaceuticals Incorporated | Wytwarzanie modulatorów transporterów posiadających kasetę wiążącą ATP |
EP2021797B1 (en) | 2006-05-12 | 2011-11-23 | Vertex Pharmaceuticals, Inc. | Compositions of n-ý2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl¨-1,4-dihydro-4-oxoquinoline-3-carboxamide |
CN101715450B (zh) | 2006-11-03 | 2013-03-13 | 沃泰克斯药物股份有限公司 | 作为cftr调控剂的氮杂吲哚衍生物 |
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US7754739B2 (en) | 2007-05-09 | 2010-07-13 | Vertex Pharmaceuticals Incorporated | Modulators of CFTR |
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EP2231671B1 (en) | 2007-12-13 | 2013-04-24 | Vertex Pharmaceuticals Incorporated | Modulators of cystic fibrosis transmembrane conductance regulator |
JP5523352B2 (ja) | 2008-02-28 | 2014-06-18 | バーテックス ファーマシューティカルズ インコーポレイテッド | Cftr修飾因子としてのへテロアリール誘導体 |
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NO2328618T3 (ja) | 2008-08-13 | 2018-04-28 | ||
US20100256184A1 (en) | 2008-08-13 | 2010-10-07 | Vertex Pharmaceuticals Incorporated | Pharmaceutical composition and administrations thereof |
MX2011003249A (es) | 2008-09-29 | 2011-05-19 | Vertex Pharma | Unidades de dosificacion del acido 3-(6-(1-(2,2-difluorobenzo[d][1 ,3]dioxol-5-il)ciclopropancarboxamido)-3-metilpiridin-2-il)benzoi co. |
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WO2012027247A2 (en) | 2010-08-23 | 2012-03-01 | Vertex Pharmaceuticals Incorporated | Pharmaceutical composition of (r)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-n-(1-(2,3-dihydroxy propyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1h-indol-5-yl) cyclopropanecarboxamide and administration therof |
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UA114619C2 (uk) | 2012-01-25 | 2017-07-10 | Вертекс Фармасьютікалз Інкорпорейтед | СКЛАД 3-(6-(1-(2,2-ДИФТОРОБЕНЗО[d][1,3]ДІОКСОЛ-5-ІЛ)ЦИКЛОПРОПАНКАРБОКСАМІДО)-3-МЕТИЛПІРИДИН-2-ІЛ)БЕНЗОЙНОЇ КИСЛОТИ |
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US8674108B2 (en) | 2012-04-20 | 2014-03-18 | Vertex Pharmaceuticals Incorporated | Solid forms of N-[2,4-bis(1,1-dimethylethy)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide |
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AU2013290444B2 (en) | 2012-07-16 | 2018-04-26 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions of (R)-1-(2,2-diflurorbenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl) cyclopropanecarboxamide and administration thereof |
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US20140221424A1 (en) | 2013-01-30 | 2014-08-07 | Vertex Pharmaceuticals Incorporated | Pharmaceutical compositions for use in the treatment of cystic fibrosis |
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Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2009073757A1 (en) * | 2007-12-07 | 2009-06-11 | Vertex Pharmaceuticals Incorporated | Solid forms of 3-(6-(1-(2,2-difluorobenzo[d][1,3] dioxol-5-yl) cyclopropanecarboxamido)-3-methylpyridin-2-yl) benzoic acid |
Non-Patent Citations (4)
Title |
---|
CHEMISTRY & INDUSTRY, vol. (16), JPN6015036501, 1989, pages 527 - 529, ISSN: 0003152947 * |
CRYSTAL GROWTH & DESIGN, vol. 9, no. 6, JPN6013060385, 2009, pages 2950 - 67, ISSN: 0002949382 * |
PHARM TECH JAPAN, vol. 25, no. 12, JPN6013060384, 2009, pages 155 - 66, ISSN: 0002949381 * |
PHARMACEUTICAL RESEARCH, vol. 12(7), JPN6015036499, 1995, pages 945 - 954, ISSN: 0003152946 * |
Cited By (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JP2017533277A (ja) * | 2014-10-31 | 2017-11-09 | アッヴィ・エス・ア・エール・エル | 置換テトラヒドロピランおよび使用方法 |
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