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1. (WO1997018193) ANTIMALARIAL QUINOLIN DERIVATIVES
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1997/018193 International Application No.: PCT/EP1996/004866
Publication Date: 22.05.1997 International Filing Date: 07.11.1996
Chapter 2 Demand Filed: 06.05.1997
IPC:
C07D 215/46 (2006.01) ,C07D 401/12 (2006.01) ,C07D 405/12 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
215
Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
16
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
38
Nitrogen atoms
42
attached in position 4
46
with hydrocarbon radicals, substituted by nitrogen atoms, attached to said nitrogen atoms
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
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
Applicants:
F. HOFFMANN-LA ROCHE AG [CH/CH]; Grenzacherstrasse 124 CH-4070 Basle, CH
Inventors:
HOFHEINZ, Werner; CH
MASCIADRI, Raffaello; CH
Agent:
POPPE, Regina; Grenzacherstrasse 124 CH-4070 Basle, CH
Priority Data:
3250/9516.11.1995CH
Title (EN) ANTIMALARIAL QUINOLIN DERIVATIVES
(FR) DERIVES DE QUINOLINE POSSEDANT UNE ACTIVITE ANTIPALUDEENNE
Abstract:
(EN) N1-Aralkyl-N2-quinolin-4-yl-diamine derivatives of general formula (I), wherein R1 signifies halogen or trifluoromethyl; R2 signifies hydrogen, halogen or trifluoromethyl; A signifies (a) or (C5-C6)-cycloalkylene; n signifies 1-4; R3 and R4 each independently signify hydrogen or methyl; p signifies 0-3 and B signifies aryl, as well as pharmaceutically acceptable salts of basic compounds of general formula (I), for use as therapeutically active substances, especially as active substances against malaria.
(FR) On décrit des dérivés N1-aralkyl-N2-quinolin-4-yl-diamine, ainsi que des sels de composés basiques, acceptables sur le plan pharmacologique, répondant à la formule générale (I), dans laquelle R1 représentent halogène ou trifluorométhyle, R2 représente hydrogène, halogène ou trifluorométhyle, A représente (a) ou cycloalkylène C5-C6, n vaut 1 à 4, R3 et R4 représentent chacun indépendamment hydrogène ou méthyle, p vaut 0 à 3 et B représente aryle. Ces composés sont utiles en tant que substances actives sur le plan thérapeutique, notamment en tant que principes actifs contre le paludisme.
Designated States: AL, AU, BA, BB, BG, BR, CA, CN, CZ, EE, GE, HU, IL, IS, JP, KP, KR, LK, LR, LT, LV, MG, MK, MN, MX, NO, NZ, PL, RO, SG, SI, SK, TR, TT, UA, 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:
TR1998/00854EP0876346JP3034609JPH11500749CN1202155CA2237997
KR1019990067646AU1996075669