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1. (WO2003004028) TETRAHYDROQUINOLINE DERIVATIVES
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2003/004028    International Application No.:    PCT/EP2002/007053
Publication Date: 16.01.2003 International Filing Date: 25.06.2002
Chapter 2 Demand Filed:    22.11.2002    
IPC:
A61K 31/47 (2006.01), A61K 31/4709 (2006.01), C07D 215/08 (2006.01), C07D 215/20 (2006.01), C07D 215/38 (2006.01), C07D 215/48 (2006.01)
Applicants: AKZO NOBEL N.V. [NL/NL]; Velperweg 76, NL-6824 AB Arnhem (NL) (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, EC, EE, ES, FI, FR, GA, GB, GD, GE, GH, GM, GN, GQ, 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, PH, 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, ZM, ZW only).
VAN STRATEN, Nicole, Corine, Renée [NL/NL]; (NL) (For US Only).
VAN SOMEREN, Rudolf, Gijsbertus [NL/NL]; (NL) (For US Only).
SCHULZ, Jurgen [DE/GB]; (GB) (For US Only)
Inventors: VAN STRATEN, Nicole, Corine, Renée; (NL).
VAN SOMEREN, Rudolf, Gijsbertus; (NL).
SCHULZ, Jurgen; (GB)
Agent: VAN WEZENBEEK, P., M., G., F.; P.O. Box 20, NL-5340 BH Oss (NL)
Priority Data:
01202531.8 02.07.2001 EP
Title (EN) TETRAHYDROQUINOLINE DERIVATIVES
(FR) DERIVES DE TETRAHYDROQUINOLINE
Abstract: front page image
(EN)The present invention relates to tetrahydroquinoline derivatives having general formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 is formyl, (1-6C)alkylcarbonyl or (1-6C)alkylsulfonyl; R2 and R3 are H or (1-4C)alkyl; R4 is phenyl; R5 is (1-4C)alkyl; Y-X is (CO)-O, (SO)2-O, NHC(O)-O, NHC(S)-O, OC(O)-O, bond-O, C(O)-NH, S(O)2-NH, NHC(O)-NH, NHC(S)-NH, OC(O)-NH, bond-NH, NH-C(O), O-C(O), NH-S(O)2, or O-S(O)2 or Y-X is a bond; R6 is H, trifluormethyl, (1-6C)alkyl, 1- or 2-adamantyl(1-4C)alkyl, (2-6C)alkenyl, (3-9C)heteroaryl, (3-6C)cycloalkyl, (2-6C)heterocycloalkyl, (1-4C)alkylthio(1-4C)alkyl, (6-10C)aryl(1-4C)alkyl, (3-9C)heteroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl(1-4C)alkyl, R8, R9-aminocarbonyl(1-4C)alkyl, R8, R9-amino(1-4C)alkyl, R8-oxycarbonyl(1-4C)alkyl, R8-oxy(1-4C)alkyl, R8-carbonyl(1-4C)alkyl or (6-10C)aryl; R7 is H, (1-4C)alkyl, (1-4C)alkoxy, halogen, trifluoromethyl, cyano, nitro hydroxyl; and R8 and/or R9 is H, (1-4C)alkyl, (2-4C)alkenyl, (2-4C)alkynyl, (6-10C)aryl, (3-9C)heteroaryl, (6-10C)aryl(1-4C)alkyl, (3-9C)heteroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)heterocycloalkyl(1-4C)alkyl, (1-4C)(di)alkylamino(1-4C)alkyl, (1-4C)alkoxy(1-4C)alkyl, (1-4C)alkylthio(1-4C)alkyl, (1-4C)alkylcarbonylamino(1-4C)alkyl, (1-4C)alkoxycarbonyl(1-4C)alkyl, (1-4C)alkoxycarbonylamino(1-4C)alkyl, (3-6C)cycloalkyl, (2-6C)heterocycloylkyl, or R8 and R9 may be joined in a (2-6C)heterocycloalkyl ring. The present invention also relates to pharmaceutical compositions comprising said derivatives and the use of these derivatives to control fertility.
(FR)L'invention se rapporte à des dérivés de tétrahydroquinoline représentés par la formule (I) ou à un sel de ces derniers pharmaceutiquement acceptable. Dans cette formule, R1 est formyle, (1-6C)alkylcarbonyl ou (1-6C)alkylsulfonyl; R2 et R3 sont H ou (1-4C)alkyl; R4 est phényle; R5 est (1-4C)alkyl; Y-X est (CO)-O, (SO)2-O, NHC(O)-O, NHC(S)-O, OC(O)-O, une liaison O, C(O)-NH, S(O)2-NH, NHC(O)-NH, NHC(S)-NH, OC(O)-NH, une liaison NH, NH-C(O), O-C(O), NH-S(O)2, ou O-S(O)2 ou Y-X est une liaison; R6 est H, trifluorométhyl, (1-6C)alkyl, 1- or 2-adamantyl(1-4C)alkyl, (2-6C)alkényl, (3-9C)hétéroaryl, (3-6C)cycloalkyl, (2-6C)hétérocycloalkyl, (1-4C)alkylthio(1-4C)alkyl, (6-10C)aryl(1-4C)alkyl, (3-9C)hétéroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)hétérocycloalkyl(1-4C)alkyl, R8, R9-aminocarbonyl(1-4C)alkyl, R8, R9-amino(1-4C)alkyl, R8-oxycarbonyl(1-4C)alkyl, R8-oxy(1-4C)alkyl, R8-carbonyl(1-4C)alkyl ou (6-10C)aryl; R7 est H, (1-4C)alkyl, (1-4C)alkoxy, halogène, trifluorométhyl, cyano, nitro hydroxyl; et R8 et/ou R9 est H, (1-4C)alkyl, (2-4C)alkényl, (2-4C)alkynyl, (6-10C)aryl, (3-9C)hétéroaryl, (6-10C)aryl(1-4C)alkyl, (3-9C)hétéroaryl(1-4C)alkyl, (3-6C)cycloalkyl(1-4C)alkyl, (2-6C)hétérocycloalkyl(1-4C)alkyl, (1-4C)(di)alkylamino(1-4C)alkyl, (1-4C)alkoxy(1-4C)alkyl, (1-4C)alkylthio(1-4C)alkyl, (1-4C)alkylcarbonylamino(1-4C)alkyl, (1-4C)alkoxycarbonyl(1-4C)alkyl, (1-4C)alkoxycarbonylamino(1-4C)alkyl, (3-6C)cycloalkyl, (2-6C)hétérocycloylkyl, ou R8 et R9 peuvent être joints dans un noyau (2-6C)hétérocycloalkyl. L'invention concerne aussi des compositions pharmaceutiques contenant lesdits dérivés et l'utilisation de ces dérivés dans le contrôle de la fertilité.
Designated States: AE, AG, AL, AU, BA, BB, BG, BR, BZ, CA, CN, CO, CR, CU, CZ, DM, DZ, EC, EE, GD, GE, HR, HU, ID, IL, IN, IS, JP, KE, KP, KR, LC, LK, LR, LT, LV, MA, MG, MK, MN, MX, MZ, NO, NZ, PH, PL, RO, RU, SG, SI, SK, TT, UA, US, UZ, VN, YU, ZA.
African Regional Intellectual Property Organization (GH, GM, KE, LS, MW, MZ, SD, SL, SZ, TZ, UG, ZM, 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, GQ, GW, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)