JP5899202B2 - 11β−HSD1の阻害剤としての3,3−二置換−(8−アザ−ビシクロ[3.2.1]オクタ−8−イル)−[5−(1H−ピラゾール−4−イル)−チオフェン−3−イル]−メタノン類 - Google Patents

11β−HSD1の阻害剤としての3,3−二置換−(8−アザ−ビシクロ[3.2.1]オクタ−8−イル)−[5−(1H−ピラゾール−4−イル)−チオフェン−3−イル]−メタノン類 Download PDF

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JP5899202B2
JP5899202B2 JP2013506723A JP2013506723A JP5899202B2 JP 5899202 B2 JP5899202 B2 JP 5899202B2 JP 2013506723 A JP2013506723 A JP 2013506723A JP 2013506723 A JP2013506723 A JP 2013506723A JP 5899202 B2 JP5899202 B2 JP 5899202B2
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ウェブスター,スコット,ピーター
セクル,ジョナサン,ロバート
ウォーカー,ブライアン,ロバート
ウォード,ピーター
ペイリン,トーマス,デイビッド
ダイク,ヘイゼル,ジョーン
ペリオア,トレバー,ロバート
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ザ ユニバーシティ オブ エディンバラ
ザ ユニバーシティ オブ エディンバラ
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JP2013506723A 2010-04-29 2011-03-10 11β−HSD1の阻害剤としての3,3−二置換−(8−アザ−ビシクロ[3.2.1]オクタ−8−イル)−[5−(1H−ピラゾール−4−イル)−チオフェン−3−イル]−メタノン類 Active JP5899202B2 (ja)

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Application Number Priority Date Filing Date Title
US32945310P 2010-04-29 2010-04-29
US61/329,453 2010-04-29
PCT/GB2011/000345 WO2011135276A1 (en) 2010-04-29 2011-03-10 3, 3 -disubstituted- ( 8 - aza - bicyclo [3.2.1] oct- 8 - yl) -[5- (1h - pyrazol - 4 -yl) -thiophen-3 -yl] methanones as inhibitors of 11 (beta) -hsd1

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JP2013527162A JP2013527162A (ja) 2013-06-27
JP2013527162A5 JP2013527162A5 (enExample) 2014-03-27
JP5899202B2 true JP5899202B2 (ja) 2016-04-06

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JP2013506723A Active JP5899202B2 (ja) 2010-04-29 2011-03-10 11β−HSD1の阻害剤としての3,3−二置換−(8−アザ−ビシクロ[3.2.1]オクタ−8−イル)−[5−(1H−ピラゾール−4−イル)−チオフェン−3−イル]−メタノン類

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GB0724251D0 (en) 2007-12-12 2008-02-06 Univ Edinburgh Therapeutic compounds and their use
GB0804685D0 (en) 2008-03-13 2008-04-16 Univ Edinburgh Therapeutic compounds and their use
KR101702159B1 (ko) 2009-09-16 2017-02-02 더 유니버시티 오브 에든버러 (4―페닐―피페리딘―1―일)―[5―(1h―피라졸―4―일)―티오펜―3―일]―메탄온 화합물 및 그의 용도
ES2543692T3 (es) 2010-04-29 2015-08-21 The University Of Edinburgh (8-aza-biciclo[3.2.1biciclo[oct-8-il)-[5-(1H-pirazol-4-il)-tiofeno-3-il]-metanonas 3,3-disustituidas como inhibidores de 11beta-HSD1
FR2993563B1 (fr) * 2012-07-20 2015-12-18 Metabrain Res Derives de thiophenes utiles dans le traitement du diabete
JP6262885B2 (ja) * 2014-03-06 2018-01-17 シャンハイ ハイヤン ファーマシューティカル テクノロジー カンパニー リミテッドShanghai Haiyan Pharmaceutical Technology Co., Ltd. オレキシン受容体拮抗剤としてのピペリジン誘導体
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