Patents by Inventor Helmut Prucher

Helmut Prucher has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Publication number: 20090247584
    Abstract: Compounds of the formula (I), in which R1, R2?, R2?, R2??, R3 and n are as defined in Claim 1, are effectors of the nicotinic and/or muscarinic acetylcholine receptor and are suitable for the prophylaxis or treatment of schizophrenia, depression, anxiety states, dementia, Alzheimer's disease, Lewy bodies dementia, neurodegenerative diseases, Parkinson's disease, Huntington's disease, Tourette's syndrome, learning and memory impairments, age-related memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds.
    Type: Application
    Filed: February 26, 2009
    Publication date: October 1, 2009
    Inventors: Gunter HOLZEMANN, Helmut Prucher, Kai Schiemann, Joachim Leibrock, Hartmut Greiner, Christa Burger, Laurie von Melchner
  • Publication number: 20050131021
    Abstract: Compounds of the formula (1), in which R1, R2?, R2?, R2??, R3 and n are as defined in claim 1, are effectors of the nicotinic and/or muscarinic acetylcholine receprot and are suitable for the prophylaxis or treatment of schizophrenia, depression, anxiety states, dementia, Alzheimer's disease, Lewy bodies dementia, neurodegenerative diseases, Parkinson's disease, Huntington's disease, Tourette's syndrome, learning and memory impairments, age-related memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds.
    Type: Application
    Filed: December 17, 2002
    Publication date: June 16, 2005
    Applicant: Merck Patent GmbH
    Inventors: Gunter Holzemann, Helmut Prucher, Kai Schiemann, Joachim Leibrock, Hartmut Greiner, Christa Burger, laurie von Melchner
  • Patent number: 6756370
    Abstract: The invention relates to compounds of formula (I), wherein R1, R2 and A have the meanings given in claim 1, are potent 5-HT2A antagonists and are suitable for treating psychoses, schizophrenia, depression, neurological disorders, impaired memory, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Huntington's disease, eating disorders such as bulimia and anorexia nervosa, Pre-Menstrual Syndrome and/or for positively influencing obsessive-compulsive disorders, (OCD).
    Type: Grant
    Filed: February 21, 2002
    Date of Patent: June 29, 2004
    Assignee: Merck Patent GmbH
    Inventors: Helmut Prücher, Henning Böttcher, Karl-August Ackermann, Rudolf Gottschlich, Christoph van Amsterdam, Christoph Seyfried, Jürgen Harting, Gerd Bartoszyk, Hartmut Greiner
  • Patent number: 6548516
    Abstract: Piperidine derivatives of the formula I and their physiologically acceptable salts in which X, Y, Z, R1, R2, R3 and R4 are as defined in claim 1 can be as excitatory amino acid antagonists for combating neurodegenerative disorders including cerebrovascular diseases, epilepsy, schizophrenia, Alzheimer's disease, Parkinson's disease and Huntington's disease, cerebral ischaemias, infarcts and psychosis.
    Type: Grant
    Filed: September 14, 2000
    Date of Patent: April 15, 2003
    Assignee: Merck Patent GmbH
    Inventors: Helmut Prücher, Joachim Leibrock, Andrew Barber, Gerd Bartoszyk
  • Patent number: 6462056
    Abstract: The invention relates to novel oxazolidine derivatives of the formula in which R1, R2 and R3 have the meanings stated in claim 1, their salts and processes for preparing the compounds according to the invention. The compounds of the formula I act as 5-HT2A antagonists with a 5-HT reuptake-inhibiting, antidepressant or anxiolytic effect and can be used to produce pharmaceuticals.
    Type: Grant
    Filed: August 25, 1999
    Date of Patent: October 8, 2002
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Henning Böttcher, Helmut Prücher, Hartmut Greiner, Gerd Bartoszyk, Christoph Seyfried
  • Patent number: 6413989
    Abstract: The invention relates to the compound 5-[4-(4-fluorobenzyl) piperidin-1-ylmethyl]-3-(4-hydroxy-phenyl)oxazolidin-2-one of the formula I and to physiologically acceptable salts thereof. The compound acts as a neuroleptic.
    Type: Grant
    Filed: May 17, 2000
    Date of Patent: July 2, 2002
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Helmut Prucher, Gerd Bartoszyk, Christoph Seyfried, Rudolf Gottschlich, Joachim Leibrock
  • Publication number: 20020061912
    Abstract: The invention relates to the compound 5-[4-(4-fluorobenzyl)piperidin-1-ylmethyl]-3-(4-hydroxyphenyl)oxazolidin-2-one of the formula I 1
    Type: Application
    Filed: May 17, 2000
    Publication date: May 23, 2002
    Inventors: HELMUT PRUCHER, GERD BARTOSZYK, CHRISTOPH SEYFRIED, RUDOLF GOTTSCHLICH, JOACHIM LEIBROCK
  • Patent number: 5714502
    Abstract: The invention relates to novel piperidinylmethyloxazolidin-2-one derivatives of the formula I ##STR1## in which R.sup.1 and R.sup.2 in each case independently of one another are unsubstituted or mono- to disubstituted phenyl radicals whose substituents can be A, OA, aryloxy having 6-10 C atoms, aralkyloxy having 7-11 C atoms, --O--(CH.sub.2).sub.n --O-- (bonded in directly adjacent positions or in the meta- or para-position to one another on the phenyl ring), --O--(CH.sub.2).sub.n --OH, Hal, CF.sub.3, OH, NO.sub.2, NH.sub.2, NHA, NA.sub.2, NHR.sup.3, NAR.sup.3, SO.sub.2 NH.sub.2, SO.sub.2 NHA, SO.sub.2 NA.sub.2, SO.sub.2 NHR.sup.3 (excluding R.sup.3 =SO.sub.2 A) , SO.sub.2 N (R.sup.3).sub.2 (excluding R.sup.3 =SO.sub.2 A) or R.sup.3,R.sup.3 is COH, CO-alkyl having 1-7 C atoms in the alkyl, CO-alkyl-Ar having 8-12 C atoms, CO-Ar having 7-13 C atoms, SO.sub.2 AA is an alkyl radical having 1-6 C atomsn is 1 or 2Hal is F, Cl, Br or Iand their physiologically acceptable salts.
    Type: Grant
    Filed: August 23, 1996
    Date of Patent: February 3, 1998
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Helmut Prucher, Gerd Bartoszyk
  • Patent number: 5698553
    Abstract: A benzylpiperidine compound of formula I ##STR1## in which R.sup.1 is H, Hal or nitro,R.sup.2 is a benzyl group, which is unsubstituted or substituted by Hal on the aromatic portion, in the 2-, 3- or 4-position of the piperidine ring, with the proviso that R.sup.2 is not in the 4-position if X is --CO--, Y and Z are --CH.sub.2 and R.sup.1 is H,R.sup.3 is H or A,X is --O--, --S--, --NH--, --CO-- or --SO.sub.2 --,Y is --CH.sub.2 --, --NH--, --O--, --S--, --NH-- or alternatively --CO-- if X is --CO-- and Z is --NH-- or --NA--,Z is --CH.sub.2 --, --C(A).sub.2-, --CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --CO--, --NH--, --NA--, --O--, --S-- or a bond,wherein X--Y or Y--Z is not --O--, --S--S--, --NH--O--, --O--NH--, --NH--NH--, --O--S-- or --S--O,A is alkyl having 1-6 C atoms,B is O or both H and OH, i.e.
    Type: Grant
    Filed: October 30, 1995
    Date of Patent: December 16, 1997
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Helmut Prucher, Rudolf Gottschlich, Joachim Leibrock, Harry Schwartz
  • 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: 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: 5532255
    Abstract: Compounds of the formula ##STR1## in which R.sup.1, X and Y have the meanings defined herein, and their salts, inhibit the binding of fibrinogen to the fibrinogen receptor and can be used for treating thrombosis, stroke, cardiac infarction, inflammations, arteriosclerosis, osteoporosis and tumors.
    Type: Grant
    Filed: April 29, 1994
    Date of Patent: July 2, 1996
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Peter Raddatz, Joachim Gante, Horst Juraczyk, Hanns Wurziger, Helmut Prucher, Sabine Bernotat-Danielowski, Guido Melzer
  • 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
  • Patent number: 5232931
    Abstract: Novel oxazolidinones of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, Z and n have the meanings defined herein, and their salts have effects on the central nervous system, in particular calming effects.
    Type: Grant
    Filed: May 28, 1991
    Date of Patent: August 3, 1993
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Helmut Prucher, Henning Bottcher, Christoph Seyfried, Anton Haase, Klaus-Otto Minck, Rudolf Gottschlich
  • Patent number: 5026705
    Abstract: New benzimidazolylpyridazinones of the formula I ##STR1## in which R.sup.1 is a styryl or mononculear of binuclear heteroaryl radical which contains 1-4 heteroatoms, each of which is unsubstituted or singly or multiply substituted by alkyl, alkoxy, alkylthio, halogen, OH, SH, amino, alkylamino, dialkylamino, acylamino having 1-8 C atoms, nitro, COOH, COOalkyl and/or CN,R.sup.2 R.sup.3, R.sup.4 and R.sup.5 are each H or alkyl andR.sup.6 and R.sup.7 are each H, or together are a C--C bond, and in which the alkyl and alkoxy groups each contain 1-4 C atoms,and their salts, show positive inotropic, vasodilating and antithrombotic actions.
    Type: Grant
    Filed: May 30, 1990
    Date of Patent: June 25, 1991
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Helmut Prucher, Rochus Jonas, Jaime Piulats, Michael Klockow
  • Patent number: 4970217
    Abstract: Novel oxazolidinones of the formula I ##STR1## Z is O or S, R.sup.1 and R.sup.2 are each phenyl or benzyl radicals which are unsubstituted or mono- or disubstituted by alkyl, alkoxy, alkylthio, alkylsulfinyl and/or alkylsulfonyl having each 1-4 C atoms, alkanoyloxy and/or alkanoylamino having each 1-6 C atoms, F, Cl, Br, OH and/or CF.sub.3 or are heteroaryl radicals containing 1-4 heteroatoms and R.sup.3 and R.sup.4 are each H, alkyl or alkoxy having each 1-4 C atoms or are F, Cl, Br, OH or CF.sub.3, and also their salts have effects on the central nervous system, in particular neuroleptic effects.
    Type: Grant
    Filed: July 15, 1988
    Date of Patent: November 13, 1990
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Helmut Prucher, Henning Bottcher, Rudolf Gottschlich, Klaus-Otto Minck, Anton Haase, Christoph Seyfried
  • Patent number: 4954499
    Abstract: A pyridizinone derivative of the formula I ##STR1## wherein R is F, Cl, Br, I or R.sup.1 R.sup.2 N,R.sup.1 and R.sup.2 are each H, C.sub.1-4 -alkyl or benzyl,R.sup.3, R.sup.4 and R.sup.5 are each H or C.sub.1-4 -alkyl andwherein it is only possible for R to be benzylamino, R.sup.3 to be CH.sub.3 and R.sup.4 to H at the same time if R.sup.5 is alkyl, and salts thereof display positive inotropic properties and vasodilative properties and can be used, in particular, as intermediate products in the production of other pharmaceutical agents.
    Type: Grant
    Filed: February 16, 1988
    Date of Patent: September 4, 1990
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventor: Helmut Prucher
  • Patent number: 4923869
    Abstract: New benzimidazolylpyridazinones of the formula I ##STR1## in which R.sup.1 is a styryl or mononuclear of binuclear heteroaryl radial which contains 1-4 heteroatoms, each of which is unsubstituted or singly or multiply substituted by alkyl, alkoxy, alkylthio, halogen, OH, SH, amino, alkylamino, dialkylamino, acylamino having 1-8 C atoms, nitro, COOH, COOalkyl and/or CN,R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each H or alkyl, andR.sup.6 and R.sup.7 are each H, or together are a C--C bond,and in which the alkyl and alkoxy groups each contain 1-4 C atoms,and their salts, show positive inotropic, vasodilating and antithrombotic actions.
    Type: Grant
    Filed: February 19, 1986
    Date of Patent: May 8, 1990
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Helmut Prucher, Rochus Jonas, Jaime Piulats, Michael Klockow
  • Patent number: 4788215
    Abstract: Halogenohydroxyflavones ##STR1## in which R is alkyl having 1-3 C atoms,X is F, Cl, Br or I, andm, n and p are each 1, 2 or 3,and their esters with sulfuric acid and phosphoric acid, and the salts of these compounds, are suitable for the treatment of hyperthyroidism.
    Type: Grant
    Filed: September 18, 1987
    Date of Patent: November 29, 1988
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Josef Kramer, Klaus Irmscher, Helmut Prucher, Rolf-Dieter Hesch
  • Patent number: 4780478
    Abstract: Basic ethers of the formula ##STR1## wherein Z is CH.sub.3 --NR.sup.2 --CH.sub.2 CH.sub.2 --CHR.sup.1 --, (1-R.sup.2 -3-piperidyl)-CHR.sup.3 --, (1-R.sup.2 -2-piperidyl)--CH.sub.2 --CHR.sup.3 -- or 1-R.sup.2 -3-R.sup.4 -hexahydroazepinyl; R.sup.1 is cyclopropyl or Ar; R.sup.2 is H, alkyl of 1-4 C atoms, alkenyl of 2-4 C atoms, cycloalkylalkyl of 4-8 C atoms or benzyl; R.sup.3 is H or Ar; R.sup.4 is H or alkyl of 1-4 C atoms, Y is --O--CHQ.sup.1 --CHQ.sup.2 --CH.sub.2 --, --O--CHQ.sup.1 --CHQ.sup.2 --CO--, --O--CQ.sup.1 .dbd.CQ.sup.2 --CO-- or --CH.sub.2 --CHQ.sup.1 --CHQ.sup.2 --CO--; Q.sup.1 and Q.sup.2 are independently each H, alkyl of 1-4 C atoms, cycloalkyl or alkylcycloalkyl each of 3-6 total C atoms or Ar; and Ar is phenyl or phenyl substituted by F, Cl, alkoxy or alkylthio, each of 1-4 C atoms, methylenedioxy or CF.sub.3 ; with the proviso that when Z is (CH.sub.3).sub.2 N--CH.sub.2 CH.sub.2 --CHR.sup.1 in 7-position and Y is --O--C(C.sub.6 H.sub.5).dbd.CH--CO-- or --O--C(C.sub.6 H.sub.5).dbd.C(CH.
    Type: Grant
    Filed: November 6, 1986
    Date of Patent: October 25, 1988
    Assignee: Merck Patent Gesellschaft mit berschrankter Haftung
    Inventors: Hans-Heinrich Hausberg, Helmut Prucher, Jurgen Uhl, Christoph Seyfried, Klaus Minck