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1. (WO2001038316) SULFONYL OXAZOLE AMINES AND THEIR USE AS 5-HT6 RECEPTOR LIGANDS
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2001/038316 International Application No.: PCT/EP2000/011734
Publication Date: 31.05.2001 International Filing Date: 24.11.2000
Chapter 2 Demand Filed: 13.06.2001
IPC:
C07D 213/81 (2006.01) ,C07D 213/82 (2006.01) ,C07D 307/68 (2006.01) ,C07D 333/38 (2006.01) ,C07D 413/04 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
213
Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02
having three double bonds between ring members or between ring members and non-ring members
04
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60
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
78
Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
81
Amides; Imides
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
213
Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
02
having three double bonds between ring members or between ring members and non-ring members
04
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
60
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
78
Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
81
Amides; Imides
82
in position 3
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
307
Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
02
not condensed with other rings
34
having two or three double bonds between ring members or between ring members and non-ring members
56
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
68
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
333
Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
02
not condensed with other rings
04
not substituted on the ring sulfur atom
26
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
Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
Applicants:
GERICKE, Rolf [DE/DE]; DE (UsOnly)
BÖTTCHER, Henning [DE/DE]; DE (UsOnly)
GASSEN, Michael [DE/DE]; DE (UsOnly)
GREINER, Hartmut [DE/DE]; DE (UsOnly)
MERCK PATENT GMBH [DE/DE]; Frankfurter Strasse 250 64293 Darmstadt, DE (AllExceptUS)
Inventors:
GERICKE, Rolf; DE
BÖTTCHER, Henning; DE
GASSEN, Michael; DE
GREINER, Hartmut; DE
Agent:
ISENBRUCK, Günter; Bardehle, Pagenberg, Dost, Altenburg, Geissler, Isenbruck Theodor-Heuss-Anlage 12 68165 Mannheim, DE
Priority Data:
199 56 791.325.11.1999DE
Title (EN) SULFONYL OXAZOLE AMINES AND THEIR USE AS 5-HT6 RECEPTOR LIGANDS
(FR) NOUVELLES SULFONYLOXAZOLAMINES
(DE) SULFONYLOXAZOLAMINE UND DEREN VERWENDUNG ALS 5-HT6 REZEPTORLIGANDEN
Abstract:
(EN) The invention relates to compounds of the general formula (I), wherein R1 and R2 independently of one another represent H, -R6, C3-C8-cycloalkyl, -(CH2)n-R7, -(CH2)n-O-R6, -(CH2)n-NH2, -(CH2)n-NHR6, -(CH2)-N(R6)2, C2-C6-alkenyl or optionally together form a mononuclear saturated heterocycle with one or two nitrogen, oxygen and/or sulphur atoms; R3 and R4 independently of one another represent H, -R6, -CF3, -NO2, -Hal, -OH, -O-R6, -NH2, -NH-R6, or -N(R6)2; R5 represents a 5- or 6-member, saturated or unsaturated heterocycle with one or two nitrogen, oxygen and/or sulphur atoms, which is optionally monosubstituted or disubstituted by -R6, -CF3, -NO2, -Hal, -OH, -O-R6, -NH2, -NH-R6, or -N(R6)2; and R6 represents C1-C6-alkyl; R7 together with R3 and/or R4 represents substituted phenyl, n represents 0 to 2. The invention also relates to the physiologically safe salts or solvates of said compounds and to the use of the compounds of the general formula (I) as medicaments.
(FR) L'invention concerne des composés de la formule générale (I) ainsi que leurs sels ou solvats acceptables sur le plan physiologique. Dans ladite formule (I), R1 et R2 représentent indépendamment l'un de l'autre H, -R6, cycloalkyle C3-C8, -(CH2)n-R7, -(CH2)n-O-R6, -(CH2)n-NH2, -(CH2)n-NHR6, -(CH2)-N(R6)2, alcényle C2-C6 ou éventuellement forment ensemble un hétérocycle saturé ayant un noyau avec un ou deux atomes d'azote, d'hydrogène et/ou de soufre; R3 et R4 représentent indépendamment l'un de l'autre H, -R6, -CF3, -NO2, -Hal, -OH, -O-R6, -NH2, -NH-R6, ou -N(R6)2; R5 représente un hétérocycle saturé ou insaturé à 5 ou 6 chaînons avec un ou deux atomes d'azote, d'hydrogène et/ou de soufre, hétérocycle éventuellement monosubstitué ou disubstitué par -R6, -CF3, -NO2, -Hal, -OH, -O-R6, -NH2, -NH-R6, ou -N(R6)2; R6 représente alkyle C1-C6, R7 avec R3 et/ou R4 représente phényle substitué ; et n représente 0 à 2. La présente invention concerne également l'utilisation des composés de la formule générale (I) comme médicaments.
(DE) Die Erfindung betrifft Verbindungen der allgemeinen Formel (I), wobei R1 und R2 unabhängig voneinander H, -R6, C3-C8-Cycloalkyl, -(CH2)n-R7, -(CH2)n-O-R6, -(CH2)n-NH2, -(CH2)n-NHR6, -(CH2)-N(R6)2, C2-C6-Alkenyl bedeuten oder gegebenenfalls zusammen einen einkernigen gesättigten Heterocyclus mit ein oder zwei Stickstoff, Sauerstoff und/oder Schwefelatomen bilden; R3 und R4 unabhängig voneinander für H, -R6, -CF3, -NO2, -Hal, -OH, -O-R6, -NH2, -NH-R6, oder -N(R6)2 stehen; R5 einen 5- oder 6-gliedrigen, gesättigten oder ungesättigten Heterocyclus darstellt, mit ein oder zwei Stickstoff, Sauerstoff und/oder Schwefelatomen, der gegebenenfalls durch -R6, -CF3, -NO2, -Hal, -OH, -O-R6, -NH2, -NH-R6, oder -N(R6)2 mono- oder disubstituiert ist; und R6 C1-C6-Alkyl bedeutet; R7 mit R3 und/oder R4 substituiertes Phenyl bedeutet, n 0 bis 2 bedeutet, sowie deren physiologisch unbedenklichen Salze oder Solvate. Auch die Verwendung der Verbindungen der allgemeinen Formel (I) als Arzneimittel ist Gegenstand der Erfindung.
Designated States: AE, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, CA, CH, CN, CU, CZ, DE, DK, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, 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, SL, TJ, TM, TR, TT, UA, UG, US, UZ, VN, YU, ZA, ZW
African Regional Intellectual Property Organization (ARIPO) (GH, GM, KE, LS, MW, MZ, SD, SL, SZ, TZ, UG, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (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, GW, ML, MR, NE, SN, TD, TG)
Publication Language: German (DE)
Filing Language: German (DE)