Patent number: 5561145
Abstract: Novel 4-aryloxy- or 4-arylthiopiperidine derivatives of the formula I ##STR1## in which R.sup.1 and R.sup.2 are each, independently of one another, phenyl radicals which are unsubstituted or mono or disubstituted by A, OH, OA, aryloxy with 6-10 C atoms, aralkyloxy with 7-11 C atoms, --0--(CH.sub.2).sub.n --0--, Hal, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NA.sub.2, NHAc, NAAc, NHSO.sub.2 A and/or NASO.sub.2 A,X is O, S, SO or SO.sub.2,m is 1, 2 or 3,n is 1 or 2,A is an alkyl radical with 1-6 C atoms,Hal is F, Cl, Br or landAc is alkanoyl with 1-8 C atoms, aralkanoyl with 1-10 C atoms or aroyl with 7-11 C atoms,and the physiologically acceptable salts thereof, show an effect influencing the central nervous system, in particular neuroleptic effect, with a negligible cataleptic effect.
Type:
Grant
Filed:
July 21, 1994
Date of Patent:
October 1, 1996
Assignee:
Merck Patent Gesellschaft Mit Beshrankter Haftung
Inventors:
Helmut Prucher, Rudolf Gottschlich, Gerd Bartoszyk, Christoph Seyfried
Patent number: 5532241
Abstract: Piperidine and piperazine derivatives of the formula I ##STR1## wherein Ind is an indol-3-yl radical which is unsubstituted or mono- or polysubstituted by OH, OA, CN, Hal, COR.sup.2 or CH.sub.2 R.sup.2,R.sup.1 is benzofuran-5-yl or 2,3-dihydrobenzofuran-5-yl, chroman-6-yl, chroman-4-on-6-yl, 3-chromen-6-yl or chromen-4-on-6-yl, which is unsubstituted or monosubstituted by CN, CH.sub.2 OH, CH.sub.2 OA or COR.sup.2,Q is C.sub.m H.sub.2m,N or CR.sup.3,A is alkyl having 1-6 C atoms,Hal is F, C1, Br or I,R.sup.2 is OH, OA, NH.sub.2, NHA or NA.sub.2,R.sup.3 is H, OH or OA andm is 2, 3 or 4,and their physiologically acceptable salts, are active on the central nervous system.
Type:
Grant
Filed:
September 29, 1994
Date of Patent:
July 2, 1996
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Inventors:
Henning Bottcher, Christoph Seyfried, Gerd Bartoszyk, Hartmut Greiner
Patent number: 5532266
Abstract: Novel arylacetamides of the formula I ##STR1## in which Q is R.sup.4 --CH(CH.sub.2 Z)--NA--, ##STR2## R.sup.1 is Ar, cycloalkyl with 3-7 C atoms or C.sub.4 -C.sub.8 -cycloalkyl-C.sub.1 -C.sub.7 -alkyl,R.sup.2 is Ar,R.sup.3 is H, OH, OA or A,R.sup.4 is A or phenyl which can optionally be substituted once or twice by F, Cl, Br, I, OH, OA, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NHCOA, NHSO.sub.2 A or NA.sub.2,R.sup.5 and R.sup.6 are each, independently of one another, H, F, Cl, Br, I, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA, NHCONH.sub.2, NO.sub.2 or taken together are methylenedioxy,A is alkyl with 1-7 C atoms, and physiologically acceptable salts thereof.
Type:
Grant
Filed:
May 30, 1995
Date of Patent:
July 2, 1996
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Inventors:
Rudolf Gottschlich, Karl-August Ackermann, Helmut Prucher, Christoph Seyfried, Hartmut Greiner, Gerd Bartoszyk, Frank Mauler, Manfred Stohrer, Andrew Barber
Patent number: 5232978
Abstract: Novel 1-(2-arylethyl)-pyrrolidines of the formula ##STR1## in which, Ar is a phenyl group which is unsubstituted or monosubstituted by OH, --O--CO--NH.sub.2, --O--CO--NHA, --O--CO--NA.sub.2, NH.sub.2, --NH--CHO, --NH--CO--A, --NH--CO--NH.sub.2, --NH--CO--NHA or NH--SO.sub.2 --A,R.sup.1 is A,R.sup.2 is a phenyl, naphthyl, thienyl, benzothienyl or pyridyl group which is unsubstituted or mono- or disubstituted by A, Hal, CF.sub.3, OH, OA, --O--CO--NH.sub.2, --O--CO--NHA, --O--CO--NA.sub.2, NO.sub.2, NH.sub.2, --NH--CHO, --NH--CO--A, --NH--CO--NH.sub.2, --NH--CO--NHA, --NH--SO.sub.2 A, --CO--A, --CONH.sub.2, --CONHA, --CONA.sub.2, --CH.sub.2 --CONH.sub.2 and/or --O--CH.sub.2 --CONH.sub.2,R.sup.3 is OH or CH.sub.2 OH,A is alkyl with 1-4 C atoms andHal is F, Cl, Br or I,or a pharmaceutically acceptable salt thereof for use as an analgesic in humans and veterinary medicine.
Type:
Grant
Filed:
November 1, 1991
Date of Patent:
August 3, 1993
Assignee:
Merck Patent Gesellschaft Mit Beschrankter Haftung
Inventors:
Rudolf Gottschlich, Karl-August Ackermann, Helmut Prucher, Andrew Barbar, Anton Haase, Hartmut Greiner, Gerd Bartoszyk