Title:
ＣＯＸ―２阻害剤のプロドラッグとしての置換ベンゼンスルホンアミド誘導体
Document Type and Number:
Japanese Patent JP3382624
Kind Code:
B2
Abstract:
Prodrugs of COX-2 inhibitors of formula (I) are described as being useful in treating inflammation and inflammation-related disorders wherein A is a ring substituent selected from partially unsaturated heterocyclyl, heteroaryl, cycloalkenyl and aryl, wherein A is optionally substituted at a substitutable position with one or more radicals selected from alkylcarbonyl, formyl, halo, alkyl, haloalkyl, oxo, cyano, nitro, carboxyl, alkoxy, aminocarbonyl, alkoxycarbonyl, carboxyalkyl, cyanoalkyl, hydroxyalkyl, haloalkylsulfonyloxy, alkoxyalkyloxyalkyl, carboxyalkoxyalkyl, cycloalkylalkyl, alkenyl, alkynyl, heterocyclyloxy, alkylthio, cycloalkyl, aryl, heterocyclyl, cycloalkenyl, aralkyl, heterocyclylalkyl, alkylthioalkyl, arylcarbonyl, aralkylcarbonyl, aralkenyl, alkoxyalkyl, arylthioalkyl, aryloxyalkyl, aralkylthioalkyl, aralkoxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, alkylaminocarbonyl, N-arylaminocarbonyl, N-alkyl-N-arylaminocarbonyl, alkylaminocarbonylalkyl, alkylamino, N-arylamino, N-aralkylamino, N-alkyl-N-aralkylamino, N-alkyl-N-arylamino, aminoalkyl, alkylaminoalkyl, N-arylaminoalkyl, N-aralkylaminoalkyl, N-alkyl-N-aralkylaminoalkyl, N-alkyl-N-arylaminoalkyl, aryloxy, aralkoxy, arylthio, aralkylthio, alkylsulfinyl, alkylsulfonyl, aminosulfonyl, alkylaminosulfonyl, N-arylaminosulfonyl, arylsulfonyl, and N-alkyl-N-arylaminosulfonyl; wherein R<1> is selected from heterocyclyl, cycloalkyl, cycloalkenyl, and aryl, wherein R<1> is optionally substituted at a substitutable position with one or more radicals selected from alkyl, haloalkyl, cyano, carboxyl, alkoxycarbonyl, hydroxyl, hydroxyalkyl, haloalkoxy, amino, alkylamino, arylamino, nitro, alkoxyalkyl, alkylsulfinyl, halo, alkoxy and alkylthio; wherein R<2> is selected from hydrido and alkoxycarbonylalkyl; and wherein R<3> is selected from alkyl, carboxyalkyl, acyl, alkoxycarbonyl, heteroarylcarbonyl, alkoxycarbonylalkylcarbonyl, alkoxycarbonylcarbonyl, amino acid residue, and alkylcarbonylaminoalkylcarbonyl; provided A is not tetrazolium, or pyridinum; and further provided A is not indanone when R<3> is alkyl or carboxyalkyl; or a pharmaceutically-acceptable salt thereof.
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Inventors:
イクス，クシアンドン
ウエイアー，リチャード，エム．
カーター，ジェフリー，エス．
クハンナ，イシュ，ケイ．
グレナト，マシュー，ジェイ．
タリイ，ジョン，ジェイ．
ナガラジャン，スリニバサン
バーテンショー，スチーブン
ブラウン，デビッド，エル．
ペニング，トマス，ディ．
メールチャ，ジェームズ，ダブリュ．
リー，ジングリン
ロジャー，ドナルド，ジェイ．，ジュニア．
ウエイアー，リチャード，エム．
カーター，ジェフリー，エス．
クハンナ，イシュ，ケイ．
グレナト，マシュー，ジェイ．
タリイ，ジョン，ジェイ．
ナガラジャン，スリニバサン
バーテンショー，スチーブン
ブラウン，デビッド，エル．
ペニング，トマス，ディ．
メールチャ，ジェームズ，ダブリュ．
リー，ジングリン
ロジャー，ドナルド，ジェイ．，ジュニア．
Application Number:
JP53713997A
Publication Date:
March 04, 2003
Filing Date:
April 11, 1997
Export Citation:
Assignee:
ジー．ディー．サール アンド カンパニー
International Classes:
A61K31/00; A61K31/18; A61K31/34; A61K31/341; C07D233/64; A61K31/365; A61K31/40; A61K31/415; A61K31/4162; A61K31/4164; A61K31/42; A61K31/421; A61K31/44; A61K31/4427; A61K31/4439; A61K31/635; A61P1/02; A61P1/04; A61P3/10; A61P5/16; A61P7/06; A61P9/10; A61P11/02; A61P11/06; A61P11/08; A61P13/12; A61P15/06; A61P17/02; A61P17/04; A61P17/06; A61P19/02; A61P19/08; A61P21/00; A61P21/04; A61P25/00; A61P25/04; A61P25/28; A61P27/02; A61P27/12; A61P29/00; A61P29/02; A61P31/12; A61P35/00; A61P37/00; A61P43/00; C07C311/16; C07C311/39; C07C311/51; C07D207/32; C07D207/327; C07D207/33; C07D231/12; C07D233/54; C07D233/62; C07D261/08; C07D263/32; C07D307/46; C07D307/58; C07D401/04; C07D417/04; C07D495/04; C07D; (IPC1-7): C07C311/51; A61K31/42; A61P29/00; C07D261/08
Other References:
Ｂｉｏｏｒｇ．Ｍｅｄ．Ｃｈｅｍ．Ｌｅｔｔ．，５（１８），２１２３−８（１９９５）
Attorney, Agent or Firm:
青山 葆 （外２名）