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1. (WO2001085699) PRODRUGS OF HIV REPLICATION INHIBITING PYRIMIDINES
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2001/085699    International Application No.:    PCT/EP2001/004990
Publication Date: 15.11.2001 International Filing Date: 03.05.2001
Chapter 2 Demand Filed:    27.09.2001    
IPC:
C07D 239/46 (2006.01), C07D 239/48 (2006.01), C07D 401/12 (2006.01)
Applicants: JANSSEN PHARMACEUTICA N.V. [BE/BE]; Turnhoutseweg 30 B-2340 Beerse (BE) (AE, AG, AL, AM, AT, AU, AZ, BA, BB, BE, BF, BG, BJ, BR, BY, BZ, CA, CF, CG, CH, CI, CM, CN, CO, CR, CU, CY, CZ, DE, DK, DM, DZ, EE, ES, FI, FR, GA, GB, GD, GE, GH, GM, GN, GR, GW, HR, HU, ID, IE, IL, IN, IS, IT, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MC, MD, MG, MK, ML, MN, MR, MW, MX, MZ, NE, NL, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, SN, SZ, TD, TG, TJ, TM, TR, TT, TZ, UA, UG, UZ, VN, YU, ZA, ZW only).
KUKLA, Michael, Joseph [US/US]; (US) (For US Only).
LUDOVICI, Donald, William [US/US]; (US) (For US Only).
KAVASH, Robert, W. [US/US]; (US) (For US Only).
DE CORTE, Bart, Lieven, Daniel [BE/US]; (US) (For US Only).
HEERES, Jan [NL/BE]; (BE) (For US Only).
JANSSEN, Paul, Adriaan, Jan [BE/BE]; (BE) (For US Only).
KOYMANS, Lucien, Maria, Henricus [NL/BE]; (BE) (For US Only).
DE JONGE, Marc, René [NL/BE]; (BE) (For US Only).
VAN AKEN, Koen, Jeanne, Alfons [BE/BE]; (BE) (For US Only).
KRIEF, Alain [FR/BE]; (BE) (For US Only)
Inventors: KUKLA, Michael, Joseph; (US).
LUDOVICI, Donald, William; (US).
KAVASH, Robert, W.; (US).
DE CORTE, Bart, Lieven, Daniel; (US).
HEERES, Jan; (BE).
JANSSEN, Paul, Adriaan, Jan; (BE).
KOYMANS, Lucien, Maria, Henricus; (BE).
DE JONGE, Marc, René; (BE).
VAN AKEN, Koen, Jeanne, Alfons; (BE).
KRIEF, Alain; (BE)
Agent: QUAGHEBEUR, Luc; Janssen Pharmaceutica N.V. Turnhoutseweg 30 B-2340 Beerse (BE)
Priority Data:
60/202,471 08.05.2000 US
Title (EN) PRODRUGS OF HIV REPLICATION INHIBITING PYRIMIDINES
(FR) PROMEDICAMENTS A BASE DE PYRIMIDINES INHIBANT LA REPLICATION DU VIH
Abstract: front page image
(EN)The present invention concerns compounds of the formula (I): (A¿1?)(A¿2?)N-R?1¿, the N-oxide forms, the pharmaceutically acceptable addition salts, the quaternary amines and stereochemically isomeric forms thereof, wherein R?1¿ is substituted C¿1-6?alkyl; -S(=O)-R?8¿; -S(=O)¿2?-R?8¿; C¿7-12?alkylcarbonyl; optionally substituted C¿1-6?alkyloxycarbonylC¿1-6?alkylcarbonyl; with R?8¿ being C¿1-6?alkyl, aryl?1¿ or Het?1¿; (A¿1?)(A¿2?)N- is the covalently bonded form of the corresponding intermediate of the formula (A¿1?)(A¿2?)N-H, which is a HIV replication inhibiting pyrimidine of formula (II).
(FR)La présente invention concerne des composés de formule (I): (A¿1?)(A¿2?)N-R?1¿, leurs formes N-oxyde, leurs sels d'addition, acceptables d'un point de vue pharmaceutique, leurs amines quaternaires, ainsi que leurs formes stéréoisomères. Dans cette formule, R?1¿ représente alkyle C¿1-6? substitué; -S(=O)-R?8¿; -S(=O)¿2?-R?8¿; alkylcarbonyle C¿7-12?; alkylcarbonyle C¿1-6? d'alkyloxycarbonyle C¿1-6? éventuellement substitué; R?8¿ étant alkyle C¿1-6?, aryle?1¿ ou Het?1¿; (A¿1?)(A¿2?)N- représente la forme à liaison covalente du produit intermédiaire correspondant, de formule (a): (A¿1?)(A¿2?)N-H, qui est une pyrimidine inhibant la réplication du VIH, de formule (II).
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, SL, TJ, TM, TR, TT, TZ, UA, UG, US, UZ, VN, YU, ZA, ZW.
African Regional Intellectual Property Organization (GH, GM, KE, LS, MW, MZ, SD, SL, SZ, TZ, UG, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, CH, CY, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GW, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)