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1. (WO2000027828) 2,4-DISUBSTITUTED TRIAZINE DERIVATIVES WITH ANTI HIV ACTIVITY
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2000/027828    International Application No.:    PCT/EP1999/008688
Publication Date: 18.05.2000 International Filing Date: 04.11.1999
Chapter 2 Demand Filed:    02.06.2000    
IPC:
A61K 9/14 (2006.01)
Applicants: JANSSEN PHARMACEUTICA N.V. [BE/BE]; Patent Department Turnhoutseweg 30 B-2340 Beerse (BE) (For All Designated States Except US).
DE CORTE, Bart [BE/US]; (US) (For US Only).
DE JONGE, Marc, René [NL/NL]; (NL) (For US Only).
HEERES, Jan [NL/BE]; (BE) (For US Only).
JANSSEN, Paul, Adriaan, Jan [BE/BE]; (BE) (For US Only).
KAVASH, Robert, W. [US/US]; (US) (For US Only).
KOYMANS, Lucien, Maria, Henricus [NL/BE]; (BE) (For US Only).
KUKLA, Michael, Joseph [US/US]; (US) (For US Only).
LUDOVICI, Donald, William [US/US]; (US) (For US Only).
VAN AKEN, Koen, Jeanne, Alfons [BE/BE]; (BE) (For US Only)
Inventors: DE CORTE, Bart; (US).
DE JONGE, Marc, René; (NL).
HEERES, Jan; (BE).
JANSSEN, Paul, Adriaan, Jan; (BE).
KAVASH, Robert, W.; (US).
KOYMANS, Lucien, Maria, Henricus; (BE).
KUKLA, Michael, Joseph; (US).
LUDOVICI, Donald, William; (US).
VAN AKEN, Koen, Jeanne, Alfons; (BE)
Agent: BOULT WADE TENNANT; Verulam Gardens, 70 Gray's Inn Road London WC1X 8BT (GB)
Priority Data:
60/107,799 10.11.1998 US
99203128.6 24.09.1999 EP
Title (EN) 2,4-DISUBSTITUTED TRIAZINE DERIVATIVES WITH ANTI HIV ACTIVITY
(FR) DERIVES DE TRIAZINE 2,4-DISUBSTITUES
Abstract: front page image
(EN)This invention concerns the use of the compounds of formula (I), the $i(N)-oxides, the pharmaceutically acceptable addition salts, quaternary amines and the stereochemically isomeric forms thereof, wherein -a?1¿=a?2¿-a?3¿=a?4¿- forms a phenyl, pyridinyl, pyrimidinyl, pyridazinyl or pyrazinyl with the attached vinyl group; n is 0 to 4; and where possible 5; R?1¿ is hydrogen, aryl, formyl, C¿1-6?alkylcarbonyl, C¿1-6?alkyl, C¿1-6?alkyloxycarbonyl or substituted C¿1-6?alkyl; each R?2¿ independently is hydroxy, halo, optionally substituted C¿1-6?alkyl, C¿2-6?alkenyl or C¿2-6?alkynyl, C¿3-7?cycloalkyl, C¿1-6?alkyloxy, C¿1-6?alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C¿1-6?alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, -S(=O)¿p?R?4¿, -NH-S(=O)¿p?R?4¿, -C(=O)R?4¿, -NHC(=O)H, -C(=O)NHNH¿2?, -NHC(=O)R?4¿, -C(=NH)R?4¿ or a 5-membered heterocyclic ring; p is 1 or 2; L is optionally substituted C¿1-10?alkyl, C¿2-10?alkenyl, C¿2-10?alkynyl or C¿3-7?cycloalkyl; or L is -X-R?3¿ wherein R?3¿ is optionally substituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl or pyridazinyl; X is -NR?1¿-, -NH-NH-, -N=N-, -O-, -C(=O)-, -CHOH-, -S-, -S(=O)- or -S(=O)¿2?-; aryl is optionally substituted phenyl; for the manufacture of a medicine for the treatment of subjects suffering from HIV (Human Immunodeficiency Virus) infection.
(FR)L'invention concerne l'utilisation des composés correspondant à la formule (I), des $i(N)-oxydes, des sels d'addition pharmaceutiquement acceptables, des amines quaternaires et leurs formes stéréochimiquement isomères, dans laquelle -a?1¿=a?2¿-a?3¿=a?4¿- forme un phényle, pyridinyle, pyrimidinyle, pyridazinyle ou pyrazinyle avec le groupe vinyle attaché; n est 0 à 4 et si possible 5; R?1¿ est hydrogène, aryle, formyle, C¿1-6?alkylcarbonyle, C¿1-6?alkyle, C¿1-6?alkyloxycarbonyle ou alkyle C¿1-6 ?substitué; chaque R?2¿ est indépendamment hydroxy, halo, éventuellement alkyle C¿1-6? substitué, C¿2-6?alcényle ou C¿2-6?alkynyle, C¿3-7?cycloalkyle, C¿1-6?alkyloxy, C¿1-6?alkyloxycarbonyle, carboxyle, cyano, nitro, amino, mono- ou di(C¿1-6?alkyl)amino, polyhalométhyle, polyhalométhyloxy, polyhalométhylthio, -S(=O)¿p?R?4¿, -NH-S(=O)¿p?R?4¿, -C(=O)R?4¿, -NHC(=O)H, -C(=O)NHNH¿2?, -NHC(=O)R?4¿, -C(=NH)R?4¿ ou un noyau hétérocyclique à 5 éléments; p est 1 ou 2; L est C¿1-10?alkyle, C¿2-10?alcényle, C¿2-10?alkynyle ou C¿3-7?cycloalkyle éventuellement substitués; ou L est -X-R?3¿ dans laquelle R?3¿ est phényle, pyridinyle, pyrimidinyle, pyrazinyle ou pyridazinyle éventuellement substitués; X est -NR?1¿-, -NH-NH-, -N=N-, -O-, -C(=O)-, -CHOH-, -S-, -S(=O)- or -S(=O)¿2?-; et aryle est phényle éventuellement substitué. Le composé sert à fabriquer un médicament destiné à traiter les sujets souffrant d'une infection par le VIH (virus de l'immunodéficience humaine).
Designated States: AE, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CR, CU, CZ, DE, DK, DM, 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, 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, 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)
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)