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1. (WO1997016451) FUSED TROPANE-DERIVATIVES AS NEUROTRANSMITTER REUPTAKE INHIBITORS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1997/016451 International Application No.: PCT/EP1996/004793
Publication Date: 09.05.1997 International Filing Date: 04.11.1996
Chapter 2 Demand Filed: 01.04.1997
IPC:
C07D 471/18 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
471
Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
12
in which the condensed system contains three hetero rings
18
Bridged systems
Applicants:
NEUROSEARCH A/S [DK/DK]; Smedeland 26B DK-2600 Glostrup, DK (AllExceptUS)
SCHEEL-KRÜGER, Jørgen [DK/DK]; DK (UsOnly)
OLSEN, Gunnar, M. [DK/DK]; DK (UsOnly)
NIELSEN, Elsebet, Østergaard [DK/DK]; DK (UsOnly)
DAHL, Bjarne, Hugo [DK/DK]; DK (UsOnly)
JENSEN, Leif, Helth [DK/DK]; DK (UsOnly)
Inventors:
SCHEEL-KRÜGER, Jørgen; DK
OLSEN, Gunnar, M.; DK
NIELSEN, Elsebet, Østergaard; DK
DAHL, Bjarne, Hugo; DK
JENSEN, Leif, Helth; DK
Agent:
GRÜNECKER, KINKELDEY, STOCKMAIR & SCHWANHÄUSSER; Maximilianstrasse 58 D-80538 München, DE
Priority Data:
0146/9613.02.1996DK
1223/9502.11.1995DK
Title (EN) FUSED TROPANE-DERIVATIVES AS NEUROTRANSMITTER REUPTAKE INHIBITORS
(FR) DERIVES TROPANE CONDENSES EN TANT QU'INHIBITEURS DE RECAPTAGE DES NEUROTRANSMETTEURS
Abstract:
(EN) The present invention discloses compound of formula (I) or any of its enantiomers or any mixture thereof, a pharmaceutically acceptable addition salt thereof or the N-oxide thereof wherein X and Y together form =O, =S, =NOR2, =CR3R4, =N-CN, =N-NR7R8, -(CH2)m-, or -W'-(CH2)p-W'-, or one of X and Y is hydrogen and the other is -OR5, -SR5, or -NR5R6, Z is hydrogen, -COOR9; R3 and R4 are independently hydrogen, halogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, alcoxy, aryl, arylalkyl, or -(CH2)q-COOR2; R2, R5 and R6 are independently hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl, or arylalkyl, -CO-alkyl, or -SO2-alkyl; R7 and R8 are independently hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl, aryl or arylalkyl; R9 is alkyl, alkenyl or alkynyl; R1 is alkyl, alkenyl, alkynyl, aryl, or arylalkyl; where said aryl groups may be substituted one or more times with substituents selected from the group consisting of halogen, CF3, CN, alkoxy, cycloalkoxy, alkyl, cycloalkyl, alkenyl, alkynyl, amino and nitro; W' and W' are each independently O or S; n is 1, 2, 3 or 4; m is 2, 3, 4 or 5; p is 1, 2, 3, 4, or 5; and q is 0, 1, 2, 3, or 4. The compounds possess valuable properties as monoamine neurotransmitter, i.e dopamine, and serotonine, reuptake inhibitors.
(FR) La présente invention concerne des composés de la formule (I) ou l'un quelconque de leurs énantiomères, ou tout mélange de ceux-ci, ou un sel d'addition d'acide de ces composés, ou un N-oxyde de ceux-ci. Dans cette formule, X et Y forment ensemble =O, =S, =NOR2, =CR3R4, =N-CH, =N-NR7R8, -(CH2)m-, ou -W'-(CH2)p-W', ou bien l'un ou l'autre représente hydrogène, l'autre représentant -OR5, -SR5 ou -NR5R6, Z représente hydrogène, -COOR9, R3 et R4 représentent indépendamment hydrogène, halogène, alkyle, cycloalkyle, cycloalkylalkyle, alcényle, alcynyle, alcoxy, aryle, arylalkyle ou -(CH2)q-COOR2, R2, R5 et R6 représentent indépendamment hydrogène, alkyle, cycloalkyle, cycloalkylalkyle, alcényle, alcynyle, aryle ou arylalkyle, -CO-alkyle ou -SO2-alkyle, R7 et R8 représentent indépendamment hydrogène, alkyle, cycloalkyle, cycloalkylalkyle, alcényle, alcynyle, aryle ou arylalkyle, R9 représente alkyle, alcényle ou alcynyle, R1 représente alkyle, alcényle, alcynyle, aryle ou arylalkyle, les groupes aryles pouvant être substitués une ou plusieurs fois par des substituants choisis dans le groupe constitué par halogène, CF3, CN, alcoxy, cycloalcoxy, alkyle, cycloalkyle, alcényle, alcynyle, amino et nitro, W' et W' représentent chacun indépendamment O ou S, n vaut 1, 2, 3 ou 4, m vaut 2, 3, 4 ou 5, p vaut 1, 2, 3, 4 ou 5 et q vaut 0, 1, 2, 3 ou 4. Ces composés possèdent des propriétés appréciables en tant que neurotransmetteurs de monoamines, c'est-à-dire en tant qu'inhibiteurs de recaptage de la dopamine et de la sérotonine.
Designated States: AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CU, CZ, DE, DK, EE, ES, FI, GB, GE, HU, IL, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MD, MG, MK, MN, MW, MX, NO, NZ, PL, PT, RO, RU, SD, SE, SG, SI, SK, TJ, TM, TR, TT, UA, UG, 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:
CZPV1998-1138IS4708NO19981609SK42298TR1998/00780MXPA/a/1998/003554
IL123898EP0858461RU02162469US5998405JPH11514638CN1201461
CA2236707KR1019990064111NZ321970AU1996075631