Patent number: 5977161
Abstract: Disclosed herein are pharmaceutical preparations which are suitable for the treatment of postoperative ileus and contain at least one compound of the formula I ##STR1## in which R.sup.1 is Ar, cycloalkyl having 3-7 C atoms or cycloalkylalkyl having 4-8 C atoms,R.sup.2 is Ar, orR.sub.1 and R.sup.2 together are ##STR2## R.sup.3 is H, OH, OA or A, R.sup.4 is A or phenyl which can optionally be mono- or disubstituted by Hal, OH, OA, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NHCOA, NHSO.sub.2 A and/or NA.sub.2,R.sup.5 is OH, CH.sub.2 OH,R.sup.6 and R.sup.7 in each case independently of one another are H, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA, NHCONH.sub.2, NO.sub.2 or methylenedioxy, with the oxy groups bonded to adjacent carbons on the ring,A is alkyl having 1-7 C atoms,Ar is a mono- or bicyclic aromatic radical which can optionally contain an N, O or S atom in the ring and can be mono-, di- or trisubstituted by A, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA and/or NHCONH.sub.2,D is CH.sub.
Type:
Grant
Filed:
February 20, 1998
Date of Patent:
November 2, 1999
Assignee:
Merck Patent Gesellschaft mit Beschrankter Haftung
Inventors:
Andrew Barber, Christoph Seyfried, Gerd Bartoszyk, Rudolf Gottschlich
Patent number: 5776972
Abstract: Pharmaceutical preparations which are suitable for the treatment of inflammatory bowel disorders and contain at least one compound of the formula I ##STR1## in which R.sup.1 is Ar, cycloalkyl having 3-7 C atoms or cycloalkylalkyl having 4-8 C atoms,R.sup.2 is Ar, orR.sup.1 and R.sup.2 together are ##STR2## R.sup.3 is H, OH, OA or A, R.sup.4 is A or phenyl which can optionally be mono- or disubstituted by Hal, OH, OA, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NHCOA, NHSO.sub.2 A and/or NA.sub.2,R.sup.5 is OH, CH.sub.2 OH,R.sup.6 and R.sup.7 in each case independently of one another are H, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA, NHCONH.sub.2, NO.sub.2 or methylenedioxy, with the oxy groups bonded to adjacent carbons on the ring,A is alkyl having 1-7 C atoms,Ar is a mono- or bicyclic aromatic radical which can optionally contain an N, O or S atom in the ring and can be mono-, di- or trisubstituted by A, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA and/or NHCONH.sub.2,D is CH.sub.
Type:
Grant
Filed:
June 27, 1996
Date of Patent:
July 7, 1998
Assignee:
Merck Patent Gesellschaft mit Beschrankter Haftung
Inventors:
Andrew Barber, Christoph Seyfried, Gerd Bartoszyk, Rudolf Gottschlich
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