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1. (WO1997016443) FARNESYL TRANSFERASE INHIBITING 2-QUINOLONE DERIVATIVES
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1997/016443 International Application No.: PCT/EP1996/004661
Publication Date: 09.05.1997 International Filing Date: 25.10.1996
Chapter 2 Demand Filed: 05.04.1997
IPC:
C07D 401/06 (2006.01) ,C07D 521/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
521
Heterocyclic compounds containing unspecified hetero rings
Applicants:
JANSSEN PHARMACEUTICA N.V. [BE/BE]; Turnhoutseweg 30 B-2340 Beerse, BE (AllExceptUS)
END, David, William [US/US]; US (UsOnly)
VENET, Marc, Gaston [FR/FR]; FR (UsOnly)
ANGIBAUD, Patrick, René [FR/FR]; FR (UsOnly)
SANZ, Gérard, Charles [FR/FR]; FR (UsOnly)
Inventors:
END, David, William; US
VENET, Marc, Gaston; FR
ANGIBAUD, Patrick, René; FR
SANZ, Gérard, Charles; FR
Agent:
DE CORTE, Filip; Janssen Pharmaceutica N.V. Patent Dept. Turnhoutseweg 30 B-2340 Beerse, BE
Priority Data:
95202945.231.10.1995EP
Title (EN) FARNESYL TRANSFERASE INHIBITING 2-QUINOLONE DERIVATIVES
(FR) DERIVES DE 2-QUINOLONE INHIBANT LA FARNESYLE TRANSFERASE
Abstract:
(EN) The present invention is concerned with compounds of formula (I), the stereoisomeric forms thereof and the pharmaceutically acceptable acid or base addition salts thereof, wherein the dotted line represents an optional bond; X is oxygen or sulfur; R1 is hydrogen, C1-12alkyl, Ar1, Ar2C1-6alkyl, quinolinylC1-6alkyl, pyridylC1-6alkyl, hydroxyC1-6alkyl, C1-6alkyloxyC1-6alkyl, mono- or di(C1-6alkyl)-aminoC1-6alkyl, aminoC1-6alkyl, or a radical of formula -Alk1-C(=O)-R9, -Alk1-S(O)-R9 or -Alk1-S(O)2-R9; R2 and R3 each independently are hydrogen, hydroxy, halo, cyano, C1-6alkyl, C1-6alkyloxy, hydroxyC1-6alkyloxy, C1-6alkyloxy-C1-6alkyloxy, aminoC1-6alkyloxy, mono- or di(C1-6alkyl)aminoC1-6alkyloxy, Ar1, Ar2C1-6alkyl, Ar2oxy, Ar2C1-6alkyloxy, hydroxycarbonyl, C1-6alkyloxycarbonyl, trihalomethyl, trihalomethoxy, C2-6alkenyl; or when on adjacent positions R2 and R3 taken together may form a bivalent radical; R4 and R5 each independently are hydrogen, Ar1, C1-6alkyl, C1-6alkyloxy-C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, amino, hydroxycarbonyl, C1-6alkyloxycarbonyl, C1-6alkylS(O)C1-6alkyl or C1-6alkylS(O)2-C1-6alkyl; R6 and R7 each independently are hydrogen, halo, cyano, C1-6alkyl, C1-6alkyloxy or Ar2oxy; R8 is hydrogen, C1-6alkyl, cyano, hydroxycarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonylC1-6alkyl, cyanoC1-6alkyl, C1-6alkyloxycarbonylC1-6alkyl, hydroxycarbonyl-C1-6alkyl, hydroxyC1-6alkyl, aminoC1-6alkyl, mono- or di(C1-6alkyl)aminoC1-6alkyl, haloC1-6alkyl, C1-6alkyloxy-C1-6alkyl, aminocarbonylC1-6alkyl, Ar1, Ar2C1-6alkyloxyC1-6alkyl, C1-6alkylthioC1-6alkyl; R10 is hydrogen, C1-6alkyl or halo; R11 is hydrogen or C1-6alkyl; having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.
(FR) La présente invention concerne des composés de la formule (I), des formes stéréo-isomères de ceux-ci, ainsi que des sels d'addition de base ou d'acide de ceux-ci, acceptables sur le plan pharmacologique. Dans cette formule, les lignes en pointillé représentent une liaison facultative, X représente oxygène ou soufre, R1 représente hydrogène, alkyle C1-12, Ar1, Ar2alkyle C1-6, quinolinyl-alkyle C1-6, pyridyl-alkyle C1-6, hydroxy-alkyle C1-6, alkyloxy C1-6-alkyle C1-6, mono ou di(alkyle C1-6)-amino-alkyle C1-6, amino-alkyle C1-6, ou un radical de la formule -Alk1-C(=O)-R9, -Alk1-S(O)-R9, ou -Alk1-S(O)2-R9, R2 et R3 représentent chacun indépendamment hydrogène, hydroxy, halo, cyano, alkyle C1-6, alkyloxy C1-6, hydroxy-alkyloxy C1-6, alkyloxy C1-6-alkyloxy C1-6, amino-alkyloxy C1-6, mono ou di(alkyle C1-6)amino-alkyloxy C1-6, Ar1, Ar2alkyle C1-6, Ar2oxy, Ar2alkyloxy C1-6, hydroxycarbonyle, alkyloxycarbonyle C1-6, trihalométhyle, trihalométhoxy, alcényle C2-6, ou bien lorsque R2 et R3 sont dans des positions adjacentes, pris ensemble, ils peuvent former un radical bivalent, R4 et R5 représentent chacun indépendamment hydrogène, Ar1, alkyle C1-6, alkyloxyC1-6-alkyle C1-6, alkyloxy C1-6, alkylthio C1-6, amino, hydroxycarbonyle, alkyloxy C1-6-carbonyle, alkyle C1-6S(O)alkyle C1-6 ou alkyle C1-6S(O)2-alkyle C1-6, R6 et R7 représentent chacun indépendamment hydrogène, halo, cyano, alkyle C1-6, alkyloxy C1-6 ou Ar2oxy, R8 représente hydrogène, alkyle C1-6, cyano, hydroxycarbonyle, alkyloxycarbonyle C1-6, alkyle C1-6-carbonyl-alkyle C1-6,cyano-alkyle C1-6, alkyloxy C1-6-carbonyl-alkyle C1-6, hydroxycarbonyl-alkyle C1-6, hydroxy-alkyle C1-6, amino-alkyle C1-6, mono ou di(alkyle C1-6)amino-alkyle C1-6, halo-alkyle C1-6, alkyloxy C1-6-alkyle C1-6, aminocarbonyle-alkyle C1-6, Ar1, Ar2alkyloxy C1-6-alkyle C1-6, alkylthio C1-6-alkyle C1-6, R10 représente hydrogène, alkyle C1-6 ou halo, R11 représente hydrogène ou alkyle C1-6. Ces composés possèdent une activité inhibitrice de la farnésyle transférase. On décrit également la préparation de ces composés, des compositions les contenant ainsi que leur utilisation en tant que médicament.
Designated States: AL, AM, AU, BA, BB, BG, BR, CA, CN, CU, CZ, EE, GE, HU, IL, IS, JP, KG, KR, LC, LK, LR, LT, LV, MD, MG, MK, MN, MX, NO, NZ, PL, RO, SG, SI, SK, TR, TT, UA, US, UZ, VN
African Regional Intellectual Property Organization (ARIPO) (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)
Also published as:
CZPV1998-1272NO19980928SK55698TR1998/00720MXPA/a/1998/002067SG51864
ES2233557EP1019395EP1106610US5968952JP4257869 JPH11514635
CN1200732CA2231143EA199800395DE000069618999DE000069632751PT1019395
KR1019990063639NZ321576DK1019395AU1996074933