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1. (WO1997017325) DERIVATES OF N,N-DIMETHYL-2-(ARYLTHIO)BENZYLAMINE, THEIR SALTS, METHODS OF PREPARATION AND THEIR USE IN PHARMACEUTICAL MEDICAMENTS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1997/017325 International Application No.: PCT/CZ1996/000022
Publication Date: 15.05.1997 International Filing Date: 07.11.1996
Chapter 2 Demand Filed: 18.05.1997
IPC:
C07C 323/27 (2006.01) ,C07C 323/32 (2006.01) ,C07C 323/62 (2006.01) ,C07C 323/63 (2006.01) ,C07C 323/65 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
323
Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
23
containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
24
having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
27
the carbon skeleton being acyclic and unsaturated
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
323
Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
23
containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
31
having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
32
having at least one of the nitrogen atoms bound to an acyclic carbon atom of the carbon skeleton
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
323
Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
50
containing thio groups and carboxyl groups bound to the same carbon skeleton
62
having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
323
Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
50
containing thio groups and carboxyl groups bound to the same carbon skeleton
62
having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
63
the carbon skeleton being further substituted by nitrogen atoms, not being part of nitro or nitroso groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
323
Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
64
containing thio groups and sulfur atoms, not being part of thio groups, bound to the same carbon skeleton
65
containing sulfur atoms of sulfone or sulfoxide groups bound to the carbon skeleton
Applicants:
FARMAK A.S. [CZ/CZ]; Na Vlc^¿inci 3 771 17 Olomouc, CZ (AllExceptUS)
POLÍVKA, Zdene^¿k [CZ/CZ]; CZ (UsOnly)
DOBROVSKY, Karel [CZ/CZ]; CZ (UsOnly)
S^¿ILHÁNKOVÁ, Alexandra [CZ/CZ]; CZ (UsOnly)
S^¿INDELÁR^¿, Karel [CZ/CZ]; CZ (UsOnly)
MÍC^¿KOVÁ, Ruz^¿ena [CZ/CZ]; CZ (UsOnly)
VALENTA, Vladimír [CZ/CZ]; CZ (UsOnly)
KREJC^¿Í, Ivan [CZ/CZ]; CZ (UsOnly)
Inventors:
POLÍVKA, Zdene^¿k; CZ
DOBROVSKY, Karel; CZ
S^¿ILHÁNKOVÁ, Alexandra; CZ
S^¿INDELÁR^¿, Karel; CZ
MÍC^¿KOVÁ, Ruz^¿ena; CZ
VALENTA, Vladimír; CZ
KREJC^¿Í, Ivan; CZ
Agent:
ANDRÉS, Mirek; Belidelska 12 772 00 Olomouc, CZ
Priority Data:
PV 2935-9509.11.1995CZ
Title (EN) DERIVATES OF N,N-DIMETHYL-2-(ARYLTHIO)BENZYLAMINE, THEIR SALTS, METHODS OF PREPARATION AND THEIR USE IN PHARMACEUTICAL MEDICAMENTS
(FR) DERIVES DE N,N-DIMETHYL-2-(ARYLTHIO)BENZYLAMINE, LEURS SELS, PROCEDES DE PREPARATION ET LEUR UTILISATION DANS DES MEDICAMENTS PHARMACEUTIQUES
Abstract:
(EN) Derivatives of N,N-dimethyl-2-(arylthio)benzylamine of general formula (I), wherein the substituents R¿1? and R¿2? in the A ring in the 4 and 5 positions are hydrogen, fluorine, or chlorine atoms, while at least one of them must be a hydrogen atom and further, among the substituents R?3¿ to R?6¿ in the B ring two to three are hydrogen atoms, another one is either one fluorine or chlorine atom (only if at least one of the substituents R¿1¿ to R?2¿ in the A ring is a fluorine or chlorine atom), further, two fluorine or two chlorine atoms, an alkyl with one to three carbon atoms, trifluoromethyl, methylthio, methylsulfinyl, methoxyl or hydroxyl (only if in the B ring there is also a fluorine or chlorine atoms as a substituent), nitro, amino, hydroxymethyl - except the 2 position, carboxyl - except the 3 position, methoxycarbonyl or ethoxycarbonyl group, as well as their salts with pharmacodynamically harmless acids. Methods of preparation of these compounds have been described, as well as some of their pharmacological characteristics and ways of their use in pharmaceutical medicaments based on their ability to selectively influence serotonin transport in the central nervous system.
(FR) Dérivés de N,N-diméthyl-2-(arylthio)benzylamine représentés par la formule générale (I) dans laquelle les substituants R1 et R2 dans le noyau A aux positions 4 et 5 représentent des atomes d'hydrogène, de fluor ou de chlore, tandis qu'au moins l'un d'entre eux doit être un atome d'hydrogène et, de plus, parmi les substituants R3 à R6 dans le noyau B deux à trois sont des atomes d'hydrogène, un autre est soit un atome de fluor, soit un atome de chlore (seulement si au moins un des substituants R1 à R2 dans le noyau A est un atome de fluor ou de chlore), deux atomes de fluor ou deux atomes de chlore, un alkyle avec un à trois atomes de carbone, trifluorométhyle, méthylthio, méthylsulfinyle, méthoxyle ou hydroxyle (seulement si, dans le noyau B, se trouve également un atome de fluor ou un atome de chlore en tant que substituant), nitro, amino, hydroxyméthyle - sauf la position 2, carboxyle - sauf la position 3, un groupe méthoxycarbonyle ou éthoxycarbonyle, ainsi que leurs sels avec des acides sans nocivité pharmacodynamique. Des procédés de préparation de ces composés sont décrits, ainsi que quelques-unes de leurs caractéristiques pharmacologiques et façons de les utiliser dans des médicaments pharmaceutiques en fonction de leur aptitude à influer sélectivement sur le transport de la sérotonine dans le système nerveux central.
Designated States: HU, RO, SI, SK, US
European Patent Office (AT, BE, CH, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
SK46798EP0859757