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 JP4049307
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.
Inventors:
John, Jay Tarry
James, W. Mercha
Stephen Barten Show
Matthew, Jay Grenato
Jeffrey, S. Carter
Jinglin Lee
Srinivasan Nagarajan
David Elle Brown
Donald, Jay Roger, Jr.
Thomas, Di. Penning
Ish, Kei. Kuhanna
Xiandon Ix
Richard, M. Weir
James, W. Mercha
Stephen Barten Show
Matthew, Jay Grenato
Jeffrey, S. Carter
Jinglin Lee
Srinivasan Nagarajan
David Elle Brown
Donald, Jay Roger, Jr.
Thomas, Di. Penning
Ish, Kei. Kuhanna
Xiandon Ix
Richard, M. Weir
Application Number:
JP2002258955A
Publication Date:
February 20, 2008
Filing Date:
September 04, 2002
Export Citation:
Assignee:
G.D.Searle, Limited, Liability, Company
International Classes:
A61K31/00; C07C311/16; A61K31/18; C07D233/64; A61K31/34; A61K31/341; 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; C07C311/39; 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
Domestic Patent References:
| JP10507445A | ||||
| JP9323971A | ||||
| JP6501919A | ||||
| JP3014569A | ||||
| JP3027370A |
Foreign References:
| WO1995000501A1 |
Attorney, Agent or Firm:
Aoyama Aoi
Kyousei Tamura
Minato Saito
Kyousei Tamura
Minato Saito