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).
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Publication number: 20090247584Abstract: 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: ApplicationFiled: February 26, 2009Publication date: October 1, 2009Inventors: Gunter HOLZEMANN, Helmut Prucher, Kai Schiemann, Joachim Leibrock, Hartmut Greiner, Christa Burger, Laurie von Melchner
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Publication number: 20050131021Abstract: 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: ApplicationFiled: December 17, 2002Publication date: June 16, 2005Applicant: Merck Patent GmbHInventors: Gunter Holzemann, Helmut Prucher, Kai Schiemann, Joachim Leibrock, Hartmut Greiner, Christa Burger, laurie von Melchner
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Patent number: 6756370Abstract: 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: GrantFiled: February 21, 2002Date of Patent: June 29, 2004Assignee: Merck Patent GmbHInventors: Helmut Prücher, Henning Böttcher, Karl-August Ackermann, Rudolf Gottschlich, Christoph van Amsterdam, Christoph Seyfried, Jürgen Harting, Gerd Bartoszyk, Hartmut Greiner
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Patent number: 6548516Abstract: 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: GrantFiled: September 14, 2000Date of Patent: April 15, 2003Assignee: Merck Patent GmbHInventors: Helmut Prücher, Joachim Leibrock, Andrew Barber, Gerd Bartoszyk
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Patent number: 6462056Abstract: 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: GrantFiled: August 25, 1999Date of Patent: October 8, 2002Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Henning Böttcher, Helmut Prücher, Hartmut Greiner, Gerd Bartoszyk, Christoph Seyfried
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Patent number: 6413989Abstract: 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: GrantFiled: May 17, 2000Date of Patent: July 2, 2002Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Helmut Prucher, Gerd Bartoszyk, Christoph Seyfried, Rudolf Gottschlich, Joachim Leibrock
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Publication number: 20020061912Abstract: The invention relates to the compound 5-[4-(4-fluorobenzyl)piperidin-1-ylmethyl]-3-(4-hydroxyphenyl)oxazolidin-2-one of the formula I 1Type: ApplicationFiled: May 17, 2000Publication date: May 23, 2002Inventors: HELMUT PRUCHER, GERD BARTOSZYK, CHRISTOPH SEYFRIED, RUDOLF GOTTSCHLICH, JOACHIM LEIBROCK
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Patent number: 5714502Abstract: 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: GrantFiled: August 23, 1996Date of Patent: February 3, 1998Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Helmut Prucher, Gerd Bartoszyk
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Patent number: 5698553Abstract: 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: GrantFiled: October 30, 1995Date of Patent: December 16, 1997Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Helmut Prucher, Rudolf Gottschlich, Joachim Leibrock, Harry Schwartz
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Patent number: 5561145Abstract: 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: GrantFiled: July 21, 1994Date of Patent: October 1, 1996Assignee: Merck Patent Gesellschaft Mit Beshrankter HaftungInventors: Helmut Prucher, Rudolf Gottschlich, Gerd Bartoszyk, Christoph Seyfried
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Patent number: 5532266Abstract: 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: GrantFiled: May 30, 1995Date of Patent: July 2, 1996Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Rudolf Gottschlich, Karl-August Ackermann, Helmut Prucher, Christoph Seyfried, Hartmut Greiner, Gerd Bartoszyk, Frank Mauler, Manfred Stohrer, Andrew Barber
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Patent number: 5532255Abstract: 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: GrantFiled: April 29, 1994Date of Patent: July 2, 1996Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Peter Raddatz, Joachim Gante, Horst Juraczyk, Hanns Wurziger, Helmut Prucher, Sabine Bernotat-Danielowski, Guido Melzer
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Patent number: 5232978Abstract: 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: GrantFiled: November 1, 1991Date of Patent: August 3, 1993Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Rudolf Gottschlich, Karl-August Ackermann, Helmut Prucher, Andrew Barbar, Anton Haase, Hartmut Greiner, Gerd Bartoszyk
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Patent number: 5232931Abstract: 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: GrantFiled: May 28, 1991Date of Patent: August 3, 1993Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Helmut Prucher, Henning Bottcher, Christoph Seyfried, Anton Haase, Klaus-Otto Minck, Rudolf Gottschlich
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Patent number: 5026705Abstract: 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: GrantFiled: May 30, 1990Date of Patent: June 25, 1991Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Helmut Prucher, Rochus Jonas, Jaime Piulats, Michael Klockow
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Patent number: 4970217Abstract: 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: GrantFiled: July 15, 1988Date of Patent: November 13, 1990Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Helmut Prucher, Henning Bottcher, Rudolf Gottschlich, Klaus-Otto Minck, Anton Haase, Christoph Seyfried
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Patent number: 4954499Abstract: 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: GrantFiled: February 16, 1988Date of Patent: September 4, 1990Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventor: Helmut Prucher
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Patent number: 4923869Abstract: 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: GrantFiled: February 19, 1986Date of Patent: May 8, 1990Assignee: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Helmut Prucher, Rochus Jonas, Jaime Piulats, Michael Klockow
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Patent number: 4788215Abstract: 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: GrantFiled: September 18, 1987Date of Patent: November 29, 1988Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Josef Kramer, Klaus Irmscher, Helmut Prucher, Rolf-Dieter Hesch
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Patent number: 4780478Abstract: 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: GrantFiled: November 6, 1986Date of Patent: October 25, 1988Assignee: Merck Patent Gesellschaft mit berschrankter HaftungInventors: Hans-Heinrich Hausberg, Helmut Prucher, Jurgen Uhl, Christoph Seyfried, Klaus Minck