JP5977347B2 - Hbv感染に対する抗ウイルス剤としてのスルファモイルベンズアミド誘導体 - Google Patents
Hbv感染に対する抗ウイルス剤としてのスルファモイルベンズアミド誘導体 Download PDFInfo
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- JP5977347B2 JP5977347B2 JP2014519057A JP2014519057A JP5977347B2 JP 5977347 B2 JP5977347 B2 JP 5977347B2 JP 2014519057 A JP2014519057 A JP 2014519057A JP 2014519057 A JP2014519057 A JP 2014519057A JP 5977347 B2 JP5977347 B2 JP 5977347B2
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Description
本出願は、2011年7月1日に出願された米国仮出願No.61/503830の利益を請求し、これは全範囲において参照として本明細書に組み込まれる。
本発明は、プレゲノムRNAカプシド形成阻害剤として有益な、B型肝炎ウィルス(HBV)感染および関連疾患の処置のために有用な化合物および方法を記載する。
B型肝炎ウィルス(HBV)感染は、依然として主要な公衆衛生問題のままである。現在、世界中で推計3億5千万人の人々および米国内で140万人が、慢性的にHBVに感染している(McMahon, 2005)。処置せずに放置した場合、これらの個人の約3分の1が、肝硬変および肝細胞癌などの重篤な肝疾患により死亡するであろう(Lee, 1997; Lok, 2004)。
臨床的に、プレゲノムRNA(pg)カプシド形成の阻害は以下の治療的利点を提供する:第1に、プレゲノムRNA(pg)カプシド形成の阻害は、現在の医薬に耐性がない、または現在の医薬から利益を享受しない患者の部分母集団のための追加の選択肢を提供することにより、現在の医薬を補完するであろう(Akbar et al., 2009; Liaw, 2009; Peters, 2009; Wiegand, van Bommel, およびBerg)。第2に、これらの特徴のある抗ウィルス機構に基づいて、プレゲノムRNA(pg)カプシド形成の阻害は、現在入手可能なDNAポリメラーゼ阻害剤に耐性のあるHBV変異体に対し有効であろう(ZoulimおよびLocarnini, 2009)。第3に、ヒト免疫不全ウイルス(HIV)感染のための高活性抗レトロウイルス療法(HAART)のように(EsteおよびCihlar)、プレゲノムRNA(pg)カプシド形成の阻害剤のDNAポリメラーゼ阻害剤との併用治療は、HVB複製を相乗的に抑制し、薬剤耐性の発生を回避し、およびしたがって慢性B型肝炎感染のためのより安全かつより効果的な処置を提供するであろう。
発明の概要
R1は、水素である;
R2は、水素、メチル、トリフルオロメチル、フッ素および塩素からなる群から選択される;
R3は、水素、メチル、フッ素および塩素からなる群から選択される;
R4は、水素、フッ素、塩素およびメチルからなる群から選択される;
R5は、水素および塩素からなる群から選択される;
R7は、水素、塩素、フッ素および臭素からなる群から選択される;
R9は、水素、メチル、フッ素および塩素からなる群から選択される;
Rxは、NH2,
Rxは、
R10は、水素、メチル、塩素および臭素からなる群から選択される;
Ryは、
プレゲノムRNAカプシド形成阻害剤
R1は、水素である;
R2は、水素、メチル、トリフルオロメチル、フッ素および塩素からなる群から選択される;
R3は、水素、メチル、フッ素および塩素からなる群から選択される;
R4は、水素、フッ素、塩素およびメチルからなる群から選択される;
R5は、水素および塩素からなる群から選択される;
R7は、水素、塩素、フッ素および臭素からなる群から選択される;
R9は、水素、メチル、フッ素および塩素からなる群から選択される;
Rxは、NH2,
Rxは、
R10は、水素、メチル、塩素および臭素からなる群から選択される;
Ryは、
例
配合物
手順
Claims (7)
- 少なくとも1種の式(I):
R1は、水素であり;
R2は、水素、メチル、トリフルオロメチル、フッ素および塩素からなる群から選択され;
R3は、水素、フッ素および塩素からなる群から選択され;
R4は、水素、フッ素、塩素およびメチルからなる群から選択され;
R5は、水素および塩素からなる群から選択され;
R7は、水素、塩素、フッ素および臭素からなる群から選択され;
R9は、水素、メチル、フッ素および塩素からなる群から選択され;
Rxは、NH2,
を有する化合物、その水和物、溶媒和物、プロドラッグ、複合体または薬学的に許容可能な塩形態を含み、任意に、少なくとも1種の薬学的に許容可能な賦形剤をさらに含む、B型肝炎ウィルス(HBV)感染および関連疾患の処置のための組成物。 - 少なくとも1種の化合物が、
2−クロロ−5−スルファモイル−N−3−メチルフェニル−ベンズアミド;
4−フルオロ−3−スルファモイル−N−(3−トリフルオロメチル−フェニル)−ベンズアミド;
N−(2−クロロ−5−トリフルオロメチル−フェニル)−4−フルオロ−3−スルファモイル−ベンズアミド;
N−フェニル−3−スルファモイル−ベンズアミド;
5−sec−ブチルスルファモイル−N−(3,4−ジフルオロフェニル)−2−フルオロ−ベンズアミド;
5−シクロヘプチルスルファモイル−N−(3,4−ジフルオロフェニル)−2−フルオロ−ベンズアミド;
N−(3,4−ジフルオロフェニル)−4−フルオロ−3−(2−メチル−シクロヘキシルスルファモイル)−ベンズアミド;
3−シクロペンチルスルファモイル−N−フェニル−ベンズアミド;
5−シクロペンチルスルファモイル−N−(3,4−ジフルオロフェニル)−2−フルオロ−ベンズアミド;
5−シクロペンチルスルファモイル−2−フルオロ−N−(4−フルオロ−フェニル)−ベンズアミド;
5−シクロペンチルスルファモイル−N−(3,5−ジメチルフェニル)−2−フルオロ−ベンズアミド;
3−シクロペンチルスルファモイル−4−フルオロ−N−3−メチルフェニル−ベンズアミド;
5−シクロペンチルスルファモイル−N−(3,5−ジクロロフェニル)−2−フルオロ−ベンズアミド;
3−[(フラン−2−イルメチル)−スルファモイル]−N−フェニル−ベンズアミド;
N−(3−クロロ−4−フルオロ−フェニル)−5−[(フラン−2−イルメチル)−スルファモイル]−2−フルオロ−ベンズアミド;
2−フルオロ−N−(3−フルオロ−フェニル)−5−[(フラン−2−イルメチル)−スルファモイル]−ベンズアミド;
N−(3,5−ジクロロフェニル)−2−フルオロ−5−[(フラン−2−イルメチル)−スルファモイル]−ベンズアミド;
4−フルオロ−3−[(フラン−2−イルメチル)−スルファモイル]−N−3−メチルフェニル−ベンズアミド;
5−[(4−クロロ−3−フェニルカルバモイル−ベンゼンスルホニルアミノ)−メチル]−フラン−2−カルボン酸メチルエステル;
N−フェニル−3−[(ピリジン−3−イルメチル)−スルファモイル]−ベンズアミド;
N−(3−クロロ−フェニル)−4−フルオロ−3−[(ピリジン−3−イルメチル)−スルファモイル]−ベンズアミド;
N−(3,4−ジフルオロフェニル)−2−フルオロ−5−フェネチルスルファモイル−ベンズアミド;
N−(3−クロロ−フェニル)−2−フルオロ−5−フェネチルスルファモイル−ベンズアミド;
5−ベンジルスルファモイル−N−(3−クロロ−4−フルオロ−フェニル)−2−フルオロ−ベンズアミド;
5−ベンジルスルファモイル−2−クロロ−N−フェニル−ベンズアミド;
N−(4−クロロ−フェニル)−5−[2−(3,4−ジメトキシ−フェニル)−エチルスルファモイル]−2−フルオロ-ベンズアミド;
5−(2−クロロ−ベンジルスルファモイル)−N−(3,4−ジフルオロフェニル)−2−フルオロ−ベンズアミド;
3−(2−クロロ−ベンジルスルファモイル)−N−(4−クロロ−フェニル)−4−フルオロ−ベンズアミド;
2−フルオロ−5−(4−メトキシ−フェニルスルファモイル)−N−3−メチルフェニル−ベンズアミド;
N−(4−クロロ−フェニル)−3−2−メチルフェニルスルファモイル−ベンズアミド;
N−フェニル−3−m−トリルスルファモイル−ベンズアミド;
N−フェニル−3−o−トリルスルファモイル−ベンズアミド;
3−(ベンジル−エチル−スルファモイル)−N−(3,4−ジフルオロフェニル)−4−フルオロ−ベンズアミド;
4−クロロ−N−フェニル−3−(チオモルホリン4−スルホニル)−ベンズアミド;
からなる群から選択される少なくとも1種である、請求項1に記載の組成物。 - 少なくとも1種の式(II):
Rxは、
を有する化合物、その水和物、溶媒和物、薬学的に許容可能な塩、プロドラッグまたは複合体を含み、任意に、少なくとも1種の薬学的に許容可能な賦形剤をさらに含む、B型肝炎ウィルス(HBV)感染および関連疾患の処置のための組成物。 - 少なくとも1種の化合物が、
5−ジエチルスルファモイル−N−(3,4−ジフルオロフェニル)−2−フルオロ−ベンズアミド;
5−アリルスルファモイル−N−(3,4−ジフルオロフェニル)−2−フルオロ−ベンズアミド;
N−(3,4−ジフルオロフェニル)−5−ジプロピルスルファモイル−2−フルオロ−ベンズアミド;
5−(アゼパン−1−スルホニル)−N−(3,4−ジフルオロフェニル)−2−フルオロ−ベンズアミド;
5−シクロヘキシルスルファモイル−N−(3,4−ジフルオロフェニル)−2−フルオロ−ベンズアミド;
およびこれらの薬学的に許容可能な形態からなる群から選択される少なくとも1種である、請求項3に記載の組成物。 - 少なくとも1種の式(III):
R10は、水素、メチル、塩素および臭素からなる群から選択され;
Ryは、
を有する化合物、その水和物、溶媒和物、薬学的に許容可能な塩、プロドラッグまたは複合体を含み、任意に、少なくとも1種の薬学的に許容可能な賦形剤をさらに含む、B型肝炎ウィルス(HBV)感染および関連疾患の処置のための組成物。 - 少なくとも1種の化合物が、
3−(アゼパン−1−スルホニル)−N−ベンジル−4−クロロ−ベンズアミド;
N−ベンジル−4−クロロ−3−(ピペリジン−1−スルホニル)−ベンズアミド;
N−ベンジル−4−メチル−3−(4−メチル−ピペリジン−1−スルホニル)−ベンズアミド;
N−ベンジル−3−ベンジルスルファモイル−4−メチル−ベンズアミド;
3−(3−ベンジルカルバモイル−ベンゼンスルホニルアミノ)−安息香酸;
N−ベンジル−4−ブロモ−3−ジエチルスルファモイル−ベンズアミド;
およびこれらの薬学的に許容可能な形態からなる群から選択される少なくとも1種である、請求項5に記載の組成物。 - 式(IV):
3−ジエチルスルファモイル−N−フェニル−ベンズアミド;
2−クロロ−5−ジエチルスルファモイル−N−m−トリル−ベンズアミド;
N−(4−クロロ−フェニル)−3−ジエチルスルファモイル−ベンズアミド;
5−シクロヘプチルスルファモイル−2−フルオロ−N−p−トリル−ベンズアミド;
2−ブロモ−5−シクロヘキシルスルファモイル−N−フェニル−ベンズアミド;
4−クロロ−3−シクロヘキシルスルファモイル−N−(4−フルオロ−フェニル)−ベンズアミド;
3−シクロヘキシルスルファモイル−4−メチル−N−フェニル−ベンズアミド;
N−(3−クロロ−フェニル)−5−(2−シクロヘキサ−1−エニル−エチルスルファモイル)−2−フルオロ−ベンズアミド;
5−(2−シクロヘキサ−1−エニル−エチルスルファモイル)−N−(3,5−ジメチルフェニル)−2−フルオロ−ベンズアミド;
2−フルオロ−5−(4−フルオロ−フェニルスルファモイル)−N−3−メチルフェニル−ベンズアミド;
N−(4−クロロ−フェニル)−3−(3−フルオロ−フェニルスルファモイル)−ベンズアミド;
4−メチル−N−フェニル−3−(ピペリジン−1−スルホニル)−ベンズアミド;
4−クロロ−N−(4−フルオロ−フェニル)−3−(ピペリジン−1−イルスルホニル)−ベンズアミド;
4−クロロ−N−(3−フルオロ−フェニル)−3−(モルホリン−4−スルホニル)−ベンズアミド;
これらの水和物、溶媒和物、プロドラッグ、複合体および薬学的に許容可能な塩形態、からなる群から選択される少なくとも1種を含み、任意に、少なくとも1種の薬学的に許容可能な賦形剤をさらに含む、B型肝炎ウィルス(HBV)感染および関連疾患の処置のための組成物。
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JP2019034943A (ja) * | 2012-12-27 | 2019-03-07 | ドレクセル ユニバーシティ | Hbv感染に対する新規抗ウイルス剤 |
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CN103889953B (zh) | 2016-06-08 |
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US20160101074A1 (en) | 2016-04-14 |
US9758477B2 (en) | 2017-09-12 |
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