JP5635909B2 - Axl阻害剤として有用な多環アリール置換トリアゾール及び多環ヘテロアリール置換トリアゾール - Google Patents

Axl阻害剤として有用な多環アリール置換トリアゾール及び多環ヘテロアリール置換トリアゾール Download PDF

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JP5635909B2
JP5635909B2 JP2010530989A JP2010530989A JP5635909B2 JP 5635909 B2 JP5635909 B2 JP 5635909B2 JP 2010530989 A JP2010530989 A JP 2010530989A JP 2010530989 A JP2010530989 A JP 2010530989A JP 5635909 B2 JP5635909 B2 JP 5635909B2
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JP2011500801A5 (enExample
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ゴフ,ダン
チャン,ジン
シング,ラジンダー
ホランド,サチャ
ユー,ジャキシン
ヘックロッド,シロ
ディン,ピンギュ
リトバック,ジョアン
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ライジェル ファーマシューティカルズ, インコーポレイテッド
ライジェル ファーマシューティカルズ, インコーポレイテッド
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    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
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    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2010530989A 2007-10-26 2007-12-29 Axl阻害剤として有用な多環アリール置換トリアゾール及び多環ヘテロアリール置換トリアゾール Expired - Fee Related JP5635909B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US98310707P 2007-10-26 2007-10-26
US60/983,107 2007-10-26
PCT/US2007/089178 WO2009054864A1 (en) 2007-10-26 2007-12-29 Polycyclic aryl substituted triazoles and polycyclic heteroaryl substituted triazoles useful as axl inhibitors

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JP2011500801A JP2011500801A (ja) 2011-01-06
JP2011500801A5 JP2011500801A5 (enExample) 2012-09-06
JP5635909B2 true JP5635909B2 (ja) 2014-12-03

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US (2) US7935693B2 (enExample)
EP (1) EP2205592B1 (enExample)
JP (1) JP5635909B2 (enExample)
CA (1) CA2704052C (enExample)
ES (1) ES2424259T3 (enExample)
SI (1) SI2205592T1 (enExample)
WO (1) WO2009054864A1 (enExample)

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