Patents by Inventor Jürgen Wichmann
Jürgen Wichmann 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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Patent number: 6803381Abstract: The present invention relates to compounds of formula wherein R1 is hydrogen or lower alkyl; R2, R2′ are each independently hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; X is O, S or two hydrogen atoms not forming a bridge; A1/A2 is phenyl; B is a group of formula wherein R3 is lower alkyl, lower alkenyl, lower alkinyl, benzyl, lower alkyl-cycloalkyl, lower alkyl-cyano, lower alkyl-pyridinyl, lower alkyl-lower alkoxy-phenyl, lower alkyl-phenyl, which is optionally substituted by lower alkoxy, or phenyl, which is optionally substituted by lower alkoxy, or lower alkyl-thienyl, cycloalkyl, lower alkyl-trifluoromethyl or lower alkyl-morpholinyl; Y is —O—, —S— or a bond; and Z is —O—; or a pharmaceutically acceptable salt thereof. These compounds are useful for the control or prevention of acute and/or chronic neurological disorders.Type: GrantFiled: May 14, 2003Date of Patent: October 12, 2004Assignee: Hoffmann-La Roche Inc.Inventors: Konrad Bleicher, Vincent Mutel, Eric Vieira, Jürgen Wichmann, Thomas Johannes Woltering
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Patent number: 6642247Abstract: The present invention relates to compounds of the general formula wherein R1 is C6-10-cycloalkyl, optionally substituted by lower alkyl or —C(O)O-lower alkyl; decahydro-naphthalen-1-yl; decahydro-naphthalen-2-yl; indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; decahydro-azulen-2-yl; bicyclo[6.2.Type: GrantFiled: June 11, 1999Date of Patent: November 4, 2003Assignee: Hoffman-La Roche Inc.Inventors: Geo Adam, Andrea Cesura, François Jenck, Sabine Kolczewski, Stephan Röver, Jürgen Wichmann
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Publication number: 20030176701Abstract: The present invention relates to compounds of the general formula 1Type: ApplicationFiled: June 11, 1999Publication date: September 18, 2003Inventors: GEO ADAM, ANDREA CESURA, FRANCOIS JENCK, SABINE KOLCZEWSKI, STEPHAN ROVER, JURGEN WICHMANN
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Patent number: 6596743Abstract: The present invention is a compound of formula: wherein R1, R2, R2′, X, A1/A2 and B are as defined in the specification. These compounds may be used in the control or prevention of acute and/or chronic neurological disorders such as restricted brain function caused by bypass operations or transplants, poor blood supply to the brain, spinal cord injuries, head injuries, hypoxia caused by pregnancy, cardiac arrest, hypoglycaemia, Alzheimer's disease, Huntington's chorea, ALS, dementia caused by AIDS, eye injuries, retinopathy, cognitive disorders, memory deficits, schizophrenia, idiopathic parkinsonism or parkinsonism caused by medicaments as well as conditions which lead to glutamate deficiency functions, such as e.g. muscle spasms, convulsions, migraine, urinary incontinence, nicotine addiction, psychoses, opiate addiction, anxiety, vomiting, acute and chronic pain, dyskinesia and depression.Type: GrantFiled: December 10, 2001Date of Patent: July 22, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Konrad Bleicher, Vincent Mutel, Eric Vieira, Jürgen Wichmann, Thomas Johannes Woltering
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Patent number: 6462198Abstract: The present invention relates to compounds of formula wherein R1 signifies hydrogen or lower alkyl; R2, R2′ signify, independently from each other, hydrogen, lower alkyl, lower alkoxy, halogen or trifluoromethyl; X signifies O, S or two hydrogen atoms not forming a bridge; A1/A2 signify, independently from each other, phenyl or a 6-membered heterocycle containing 1 or 2 nitrogen atoms; B is a group of formula wherein R3 signifies lower alkyl, lower alkenyl, lower alkinyl, benzyl, lower alkyl-cycloalkyl, lower alkyl-cyano, lower alkyl-pyridinyl, lower alkyl-lower alkoxy-phenyl, lower alkyl-phenyl, which is optionally substituted by lower alkoxy, or phenyl, which is optionally substituted by lower alkoxy, or lower alkyl-thienyl, cycloalkyl, lower alkyl-trifluoromethyl or lower alkyl-morpholinyl, Y signifies —O—, —S— or a bond; Z signifies —O— or —S—; or B is a 5-membered heterocyclic group of formulasType: GrantFiled: April 10, 2000Date of Patent: October 8, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Konrad Bleicher, Vincent Mutel, Eric Vieira, Jürgen Wichmann, Thomas Johannes Woltering
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Publication number: 20020091150Abstract: The present invention is a compound of formula 1Type: ApplicationFiled: December 10, 2001Publication date: July 11, 2002Inventors: Konrad Bleicher, Vincent Mutel, Eric Vieira, Jurgen Wichmann, Thomas Johannes Woltering
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Patent number: 6310208Abstract: Since the compounds in accordance with the invention can bind to serotonin receptors (5HT2), they are especially suitable for the treatment or prevention of central nervous disorders such as depressions, bipolar disorders, anxiety states, sleep and sexual disorders, psychoses, schizophrenia, migraine and other conditions associated with cephalic pain or pain of a different kind, personality disorders or obsessive-compulsive disorders, social phobias or panic attacks, mental organic disorders, mental disorders in childhood, aggressivity, age-related memory disorders and behavioral disorders, addiction, obesity, bulimia etc., nervous system damage caused by trauma, stroke, neurodegenerative diseases etc.; cardiovascular disorders such as hypertension, thrombosis, stroke etc.; and gastrointestinal disorders such as dysfunction of the gastrointestinal tract motility.Type: GrantFiled: January 6, 1998Date of Patent: October 30, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Michael Bös, Heinz Stadler, Jürgen Wichmann
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Patent number: 6284785Abstract: 1-Arenesulfonyl-2-Aryl-pyrrolidine and pyridine derivatives having activity as ligands of metabotropic glutamate receptors of the formula are disclosed.Type: GrantFiled: March 24, 2000Date of Patent: September 4, 2001Assignee: Hoffmann- La Roche Inc.Inventors: Vincent Mutel, Eric Vieira, Jürgen Wichmann
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Patent number: 6248901Abstract: The compounds of the formula wherein R signifies halogen or lower alkyl; n signifies 0-3; R1 signifies lower alkyl; cycloalkyl; benzyl optionally substituted by hydroxy, halogen, lower alkoxy or lower alkyl; benzoyl optionally substituted by amino, lower alkylamino or di-lower alkylamino; acetyl or cycloalkyl-carbonyl; and signifies an aromatic 5-membered residue which is bonded via a N-atom and which contains further 1-3 N atoms in addition to the linking N atom, as well as their pharmaceutically acceptable salts as therapeutically active substances, especially for the control or prevention of acute and/or chronic neurological disorders.Type: GrantFiled: May 4, 1999Date of Patent: June 19, 2001Assignee: Hoffman-La Roche Inc.Inventors: Geo Adam, Sabine Kolczewski, Vincent Mutel, Heinz Stadler, Jürgen Wichmann, Thomas Johannes Woltering
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Patent number: 6166209Abstract: The present invention relates to compounds of the formula ##STR1## wherein X is --O-- or --CH.sub.2 --;Y is --C(O)--, --(CH.sub.2).sub.n -- or --N(CH.sub.3)--;n is 1 or 2 orX and Y taken together are --CH.dbd.CH--Z is --NH--, --CH.sub.2 --, --O-- or .dbd.CH--;A.sup.1 is a group ##STR2## B is --(CH.sub.2).sub.m --; m is 0, 1 or 2;R.sup.1 and R.sup.2 are each independently hydrogen or lower alkyl;R.sup.3 is hydrogen or halogen;R.sup.4 is hydrogen or hydroxy andthe dotted line is (--CH.sub.2 --CH.sub.2 --).sub.n, and n' is 0 or 1 and to pharmaceutically acceptable acid addition salts thereof.The compounds of the present invention are antagonists of the OFQ receptor.Type: GrantFiled: November 20, 1998Date of Patent: December 26, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Geo Adam, Andrea Cesura, Guido Galley, Fran.cedilla.ois Jenck, Stephan Rover, Jurgen Wichmann
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Patent number: 6113527Abstract: The invention relates to compounds of the general formula ##STR1## wherein R.sup.1 is C.sub.6-12 -cycloalkyl, optionally substituted by lower alkyl or C(O)O lower alkyl, indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; acenaphthen-1-yl; bicyclo[3.3.1]non-9-yl, octahydro-inden-2-yl; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl, decahydro-azulen-2-yl; bicyclo[6.2.0]dec-9-yl; decahydro-naphthalen-1-yl, decahydro-naphthalen-2-yl; tetrahydro-naphthalen-1-yl, tetrahydro-naphthalen-2-yl or 2-oxo-1,2-diphenyl-ethyl;R.sup.2 is .dbd.O or hydrogen,R.sup.3 is hydrogen, isoindolyl-1,3-dione, lower alkoxy, lower alkyl, amino, benzyloxy, --CH.sub.2 OR.sup.5 or --CH.sub.2 N(R.sup.5).sub.2 ;R.sup.4 is hydrogen or --CH.sub.2 OR.sup.5 ;R.sup.5 is hydrogen or lower alkyl; ##STR2## is cyclohexyl or phenyl, optionally substituted by lower alkyl, halogen or alkoxy; to racemic mixtures and their corresponding enantiomers and or pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: June 11, 1999Date of Patent: September 5, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Geo Adam, Andrea Cesura, Fran.cedilla.ois Jenck, Sabine Kolczewski, Stephan Rover, Jurgen Wichmann
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Patent number: 6075034Abstract: The present invention relates to compounds of the general formula whereinR.sup.1 is C.sub.5-12 -cycloalkyl, optionally substituted by lower alkyl; decahydro-naphthalen-1-yl; decahydro-naphthalen-2-yl; indan-1-yl or indan-2-yl, optionally substituted by lower alkyl; decahydro-azulen-2-yl; bicyclo[6.2.0]dec-9-yl; acenaphthen-1-yl; bicyclo[3.3.1]non-9-yl; 2,3-dihydro-1H-phenalen-1-yl; 2,3,3a,4,5,6-hexahydro-1H-phenalen-1-yl; octahydro-inden-2-yl; 1,2,3,4-tetrahydro-naphthalen-1-yl; 1,2,3,4-tetrahydro-naphthalen-2-yl; naphthalen-lower alkyl-1-yl; naphthalen-lower alkyl-2-yl; acenaphthen-1-yl; and 5-isopropyl-2-methyl-bicyclo[3.1.0]hex-3-yl;R.sup.2, R.sup.3 are hydrogen; hydroxy; lower alkyl; .dbd.O; or phenyl, optionally substituted by lower allyl, halogen or alkoxy;R.sup.4 is hydrogen; lower alkyl; --(CH.sub.2).sub.n CH(OH)CF.sub.3 ; --(CH.sub.2).sub.n C.sub.3-6 -cycloalkyl; phenyl; benzyl; tetrahydrofuran-3-yl; --(CH.sub.2).sub.n OCH.sub.2 C.sub.6 H.sub.5 ; --(CH.sub.2).sub.Type: GrantFiled: June 11, 1999Date of Patent: June 13, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Geo Adam, Frank Dautzenberg, Sabine Kolczewski, Stephan Rover, Jurgen Wichmann
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Patent number: 6071925Abstract: The present invention relates to compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each independently hydrogen, lower alkyl, lower alkoxy or halogen;R.sup.3 is phenyl, which is unsubstituted or substituted by lower alkyl, CF.sub.3, lower alkoxy or halogen;R.sup.4 is hydrogen, lower alkyl, lower alkenyl, --C(O)-lower alkyl, --C(O)-phenyl, lower alkyl-C(O)-phenyl, lower alkylene-C(O)O-lower alkyl, lower alkantriyl-di-C(O)O-lower alkyl, hydroxy-lower alkyl, lower alkyl-O-lower alkyl, lower alkyl-CH(OH)CF.sub.3, phenyl or benzyl,R.sup.5 and R.sup.6 are each independently hydrogen, phenyl, lower alkyl or di-lower alkyl or R.sup.5 and R.sup.6 together with the carbon atoms to which they are bound form a phenyl ring, orR.sup.5 and one of R.sup.1 or R.sup.Type: GrantFiled: January 20, 1998Date of Patent: June 6, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Geo Adam, Andrea Cesura, Guido Galley, Fran.cedilla.ois Jenck, Frederick Monsma, Jr., Stephan Rover, Jurgen Wichmann
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Patent number: 6054588Abstract: The compounds of the formula ##STR1## wherein R signifies halogen or lower alkyl;n signifies 0-3;R.sup.1 signifies lower alkyl; cycloalkyl; benzyl optionally substituted by hydroxy, halogen, lower alkoxy or lower alkyl; benzoyl optionally substituted by amino, lower alkyl-amino or di-lower alkylamino; acetyl or cycloalkyl-carbonyl; and ##STR2## signifies an aromatic 5-membered residue which is bonded via a N-atom and which contains further 1-3 N atoms in addition to the linking N atom,as well as their pharmaceutically acceptable salts as therapeutically active substances, especially for the control or prevention of acute and/or chronic neurological disorders.Type: GrantFiled: May 4, 1999Date of Patent: April 25, 2000Assignee: Hoffman-La Roche Inc.Inventors: Geo Adam, Sabine Kolczewski, Vincent Mutel, Heinz Stadler, Jurgen Wichmann, Thomas Johannes Woltering
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Patent number: 6043366Abstract: The present invention relates to compounds of formula I and pharmaceutically acceptable acid addition salts thereof.Type: GrantFiled: December 3, 1998Date of Patent: March 28, 2000Assignee: Hoffman-La Roche Inc.Inventors: Geo Adam, Andrea Cesura, Caido Galley, Fran.cedilla.ois Jenck, Stephan Rover, Jurgen Wichmann
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Patent number: 6020525Abstract: This invention relates to (2S,2'R,3'R)-2-(2,3-dicarboxyl-cyclopropyl)-glycine of formula ##STR1## wherein R.sub.2 is hydrogen or tritium and to a process for the preparation thereof. The described compounds can be used as a pharmacological tool to study the function of group II mGluR (metabotropic glutamate receptor).Type: GrantFiled: February 23, 1999Date of Patent: February 1, 2000Assignee: Hoffmann-La Roche Inc.Inventors: Geo Adam, Philippe Nicolas Huguenin-Virchaux, Jurgen Wichmann
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Patent number: 5958931Abstract: The invention is concerned with compounds of the general formula ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, phenyl or benzyl,R.sup.2 is lower alkyl, lower alkoxy, --O(CH.sub.2).sub.n N(R.sup.13)(R.sup.14), --(CH.sub.2).sub.n N(R.sup.13)(R.sup.14) or --N(R.sup.15)(CH.sub.2).sub.n N(R.sup.13)(R.sup.14),R.sup.3 -R.sup.12 are hydrogen, halogen, trifluoromethyl, lower alkyl, cycloalkyl, lower alkoxy, hydroxy, nitro, cyano, --N(R.sup.13).sub.2, phenyl, phenyloxy, benzyl or benzyloxy, orR.sup.6 and R.sup.7 together are a benzene ring,R.sup.13 -R.sup.15 are hydrogen, lower alkyl or cycloalkyl andn is 1-5,as well as their pharmaceutically acceptable salts.Type: GrantFiled: July 14, 1998Date of Patent: September 28, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Geo Adam, Sabine Kolczewski, Vincent Mutel, Jurgen Wichmann, Thomas Johannes Woltering
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Patent number: 5955495Abstract: The invention is concerned with the use of compounds of the general formula ##STR1## wherein R.sup.1 -R.sup.4 signify hydrogen, halogen, lower-alkyl, lower-alkoxy, aryl, benzyloxy, lower-alkoxy-lower-alkyl, lower-alkyl-sulphanyl, lower-alkyl-sulphanyl-lower-alkyl or R.sup.1 and R.sup.2 together signify the group --O--(CH.sub.2).sub.2 -- or --(CH.sub.2).sub.2 --O-- andR.sup.5 signifies hydrogen or hydroxy,as well as their pharmaceutically acceptable salts in the control or prevention of illnesses or disorders of the central nervous system such as migraine, schizophrenia, anxiety states, sleep disorders, anorexia, Alzheimer's disease, addictions (alcohol, nicotine, benzodiazepine, cocaine, etc.), as well as disorders which result from damage to the head/brain or to the spinal column/bone marrow and, respectively, for the production of corresponding medicaments.Type: GrantFiled: April 14, 1997Date of Patent: September 21, 1999Assignee: Hoffmann-La Roche Inc.Inventors: Michael Bos, Heinz Stadler, Jurgen Wichmann
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Patent number: 5646173Abstract: The invention relates to tricyclic pyrrole derivatives useful as 5-HT selective agents of the formula ##STR1## wherein R.sup.1 to R.sup.4 are, independently, hydrogen, halogen, lower alkyl, phenyl, cycloalkyl or lower alkoxy and R.sup.2 additionally is lower alkoxycarbonyl, acyloxy or mesyloxy;R.sup.5 to R.sup.7 are, independently, hydrogen or lower alkyl;X is --CH.sub.2 CH(C.sub.6 H.sub.5)--, --CH.dbd.C(C.sub.6 H.sub.5)--, --YCH.sub.2 --, --CH.dbd.CH-- or --(CR.sup.11 R.sup.12).sub.n ;R.sup.11 and R.sup.12 are, independently, hydrogen, phenyl, lower alkyl or halogen;n is 1 to 3 andy is O or S,as well as pharmaceutically acceptable salts of basic compounds of formula I with pharmaceutically acceptable acids.Type: GrantFiled: February 21, 1996Date of Patent: July 8, 1997Assignee: Hoffmann-La Roche Inc.Inventors: Michael Bos, Jurgen Wichmann, Ulrich Widmer