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1. (WO1997038986) SUBSTITUTED BENZENESULFONAMIDE DERIVATIVES AS PRODRUGS OF COX-2 INHIBITORS
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/1997/038986    International Application No.:    PCT/US1997/005497
Publication Date: 23.10.1997 International Filing Date: 11.04.1997
Chapter 2 Demand Filed:    03.11.1997    
IPC:
A61K 31/18 (2006.01), A61K 31/415 (2006.01), A61K 31/42 (2006.01), A61K 31/635 (2006.01), C07C 311/16 (2006.01), C07C 311/51 (2006.01), C07D 207/33 (2006.01), C07D 231/12 (2006.01), C07D 233/54 (2006.01), C07D 261/08 (2006.01), C07D 263/32 (2006.01), C07D 307/58 (2006.01), C07D 401/04 (2006.01), C07D 417/04 (2006.01), C07D 495/04 (2006.01)
Applicants: G.D. SEARLE & CO. [US/US]; Corporate Patent Dept., P.O. Box 5110, Chicago, IL 60680-5110 (US) (For All Designated States Except US).
TALLEY, John, J. [US/US]; (US) (For US Only).
MALECHA, James, W. [US/US]; (US) (For US Only).
BERTENSHAW, Stephen [US/US]; (US) (For US Only).
GRANETO, Matthew, J. [US/US]; (US) (For US Only).
CARTER, Jeffery, S. [US/US]; (US) (For US Only).
LI, Jinglin [US/US]; (US) (For US Only).
NAGARAJAN, Srinivasan [US/US]; (US) (For US Only).
BROWN, David, L. [US/US]; (US) (For US Only).
ROGIER, Donald, J., Jr. [US/US]; (US) (For US Only).
PENNING, Thomas, D. [US/US]; (US) (For US Only).
KHANNA, Ish, K. [IN/US]; (US) (For US Only).
XU, Xiangdong [CN/US]; (US) (For US Only).
WEIER, Richard, M. [US/US]; (US) (For US Only)
Inventors: TALLEY, John, J.; (US).
MALECHA, James, W.; (US).
BERTENSHAW, Stephen; (US).
GRANETO, Matthew, J.; (US).
CARTER, Jeffery, S.; (US).
LI, Jinglin; (US).
NAGARAJAN, Srinivasan; (US).
BROWN, David, L.; (US).
ROGIER, Donald, J., Jr.; (US).
PENNING, Thomas, D.; (US).
KHANNA, Ish, K.; (US).
XU, Xiangdong; (US).
WEIER, Richard, M.; (US)
Agent: WILLIAMS, Roger, A.; G.D. Searle & Co., Corporate Patent Dept., P.O. Box 5110, Chicago, IL 60680-5110 (US).
BEIL, Hans, Chr.; Adelonstrasse 58, Postfach 80 01 40, D-65901 Frankfurt AM Main (DE)
Priority Data:
08/631,514 12.04.1996 US
Title (EN) SUBSTITUTED BENZENESULFONAMIDE DERIVATIVES AS PRODRUGS OF COX-2 INHIBITORS
(FR) DERIVES BENZENESULFONAMIDE SUBSTITUE UTILISABLES COMME PRECURSEURS DES INHIBITEURS DU COX-2
Abstract: front page image
(EN)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.
(FR)La présente invention concerne des précurseurs, inhibiteurs du COX-2, représentés par la formule générale (I) et convenant en thérapie des inflammations et des troubles liés aux inflammations ou l'un de leurs sels galéniques. Dans cette formule générale (I), 'A' est un substituant cyclique appartenant au groupe des hétérocyclyle, hétéroaryle, cycloalkényle et aryle, la substitution de 'A' se faisant éventuellement en une position admettant la substitution, et ce, au moyen d'un ou plusieurs radicaux appartenant au groupe des alkylcarbonyl, formyl, halo, alkyl, haloalkyl, oxo, cyano, nitro, carboxyl, alcoxy, aminocarbonyl, alcoxycarbonyl, carboxyalkyl, cyanoalkyl, hydroxyalkyl, haloalkylsulfonyloxy, alcoxyalkyloxyalkyl, carboxyalcoxyalkyl, cycloalkylalkyl, alkényl, alkynyl, hétérocyclyloxy, alkylthio, cycloalkyl, aryl, hétérocyclyl, cycloalkényl, aralkyl, hétérocyclyalkyl, alkylthioalkyl, arylcarbonyl, aralkylcarbonyl, aralkényl, alcoxyalkyl, arylthioalkyl, aryloxyalkyl, aralkylthioalkyl, aralcoxyalkyl, alcoxycarbonylalkyl, 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, aralcoxy, arylthio, aralkylthio, alkylsulfinyl,alkylsulfonyl, aminosulfonyl, alkylaminosulfonyl, N-aralkylaminosulfonyl, arylsulfonyl, et N-alkyl-N-arylaminosulfonyl; R?1¿ appartient au groupe des hétérocyclyle, cycloalkyle, cycloalkényle et aryle, R?1¿ étant éventuellement substitué, en une position admettant la substitution, au moyen d'un ou plusieurs radicaux appartenant au groupe des alkyl, haloalkyl, cyano, carboxyl, alcoxycarbonyl, hydroxyl, hydroxyalkyl, haloalcoxyn amino, alkylamino, arylamino, nitro, alcoxyalkyl, alkylsulfinyl, halo, alcoxy et alkylthio; R?2¿ appartient au groupe des hydrido et alcoxycarbonylalkyl; et R?3¿ appartient au groupe des alkyl, carboxyalkyl, acyl, alcoxycarbonyl, hétéroarylcarbonyl, alcoxycarbonylalkylcarbonyl, alcoxycarbonylcarbonyl, radical d'acide aminé et alkylcarbonylaminoalkylcarbonyl; 'A' ne devant être ni tétrazolium ni pyridinium; en outre 'A' ne peut être indanone lorsque R?3¿ est alkyl ou carboxyalkyl.
Designated States: AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CU, CZ, DE, DK, EE, ES, FI, GB, GE, GH, HU, IL, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, TJ, TM, TR, TT, UA, UG, US, UZ, VN, YU.
African Regional Intellectual Property Organization (GH, KE, LS, MW, SD, SZ, UG)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)