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).

  • Patent number: 6803381
    Abstract: 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: Grant
    Filed: May 14, 2003
    Date of Patent: October 12, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Konrad Bleicher, Vincent Mutel, Eric Vieira, Jürgen Wichmann, Thomas Johannes Woltering
  • Patent number: 6642247
    Abstract: 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: Grant
    Filed: June 11, 1999
    Date of Patent: November 4, 2003
    Assignee: Hoffman-La Roche Inc.
    Inventors: Geo Adam, Andrea Cesura, François Jenck, Sabine Kolczewski, Stephan Röver, Jürgen Wichmann
  • Publication number: 20030176701
    Abstract: The present invention relates to compounds of the general formula 1
    Type: Application
    Filed: June 11, 1999
    Publication date: September 18, 2003
    Inventors: GEO ADAM, ANDREA CESURA, FRANCOIS JENCK, SABINE KOLCZEWSKI, STEPHAN ROVER, JURGEN WICHMANN
  • Patent number: 6596743
    Abstract: 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: Grant
    Filed: December 10, 2001
    Date of Patent: July 22, 2003
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Konrad Bleicher, Vincent Mutel, Eric Vieira, Jürgen Wichmann, Thomas Johannes Woltering
  • Patent number: 6462198
    Abstract: 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 formulas
    Type: Grant
    Filed: April 10, 2000
    Date of Patent: October 8, 2002
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Konrad Bleicher, Vincent Mutel, Eric Vieira, Jürgen Wichmann, Thomas Johannes Woltering
  • Publication number: 20020091150
    Abstract: The present invention is a compound of formula 1
    Type: Application
    Filed: December 10, 2001
    Publication date: July 11, 2002
    Inventors: Konrad Bleicher, Vincent Mutel, Eric Vieira, Jurgen Wichmann, Thomas Johannes Woltering
  • Patent number: 6310208
    Abstract: 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: Grant
    Filed: January 6, 1998
    Date of Patent: October 30, 2001
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Bös, Heinz Stadler, Jürgen Wichmann
  • Patent number: 6284785
    Abstract: 1-Arenesulfonyl-2-Aryl-pyrrolidine and pyridine derivatives having activity as ligands of metabotropic glutamate receptors of the formula are disclosed.
    Type: Grant
    Filed: March 24, 2000
    Date of Patent: September 4, 2001
    Assignee: Hoffmann- La Roche Inc.
    Inventors: Vincent Mutel, Eric Vieira, Jürgen Wichmann
  • Patent number: 6248901
    Abstract: 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: Grant
    Filed: May 4, 1999
    Date of Patent: June 19, 2001
    Assignee: Hoffman-La Roche Inc.
    Inventors: Geo Adam, Sabine Kolczewski, Vincent Mutel, Heinz Stadler, Jürgen Wichmann, Thomas Johannes Woltering
  • Patent number: 6166209
    Abstract: 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: Grant
    Filed: November 20, 1998
    Date of Patent: December 26, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Geo Adam, Andrea Cesura, Guido Galley, Fran.cedilla.ois Jenck, Stephan Rover, Jurgen Wichmann
  • Patent number: 6113527
    Abstract: 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: Grant
    Filed: June 11, 1999
    Date of Patent: September 5, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Geo Adam, Andrea Cesura, Fran.cedilla.ois Jenck, Sabine Kolczewski, Stephan Rover, Jurgen Wichmann
  • Patent number: 6075034
    Abstract: 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: Grant
    Filed: June 11, 1999
    Date of Patent: June 13, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Geo Adam, Frank Dautzenberg, Sabine Kolczewski, Stephan Rover, Jurgen Wichmann
  • Patent number: 6071925
    Abstract: 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: Grant
    Filed: January 20, 1998
    Date of Patent: June 6, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Geo Adam, Andrea Cesura, Guido Galley, Fran.cedilla.ois Jenck, Frederick Monsma, Jr., Stephan Rover, Jurgen Wichmann
  • Patent number: 6054588
    Abstract: 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: Grant
    Filed: May 4, 1999
    Date of Patent: April 25, 2000
    Assignee: Hoffman-La Roche Inc.
    Inventors: Geo Adam, Sabine Kolczewski, Vincent Mutel, Heinz Stadler, Jurgen Wichmann, Thomas Johannes Woltering
  • Patent number: 6043366
    Abstract: The present invention relates to compounds of formula I and pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: December 3, 1998
    Date of Patent: March 28, 2000
    Assignee: Hoffman-La Roche Inc.
    Inventors: Geo Adam, Andrea Cesura, Caido Galley, Fran.cedilla.ois Jenck, Stephan Rover, Jurgen Wichmann
  • Patent number: 6020525
    Abstract: 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: Grant
    Filed: February 23, 1999
    Date of Patent: February 1, 2000
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Geo Adam, Philippe Nicolas Huguenin-Virchaux, Jurgen Wichmann
  • Patent number: 5958931
    Abstract: 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: Grant
    Filed: July 14, 1998
    Date of Patent: September 28, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Geo Adam, Sabine Kolczewski, Vincent Mutel, Jurgen Wichmann, Thomas Johannes Woltering
  • Patent number: 5955495
    Abstract: 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: Grant
    Filed: April 14, 1997
    Date of Patent: September 21, 1999
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Bos, Heinz Stadler, Jurgen Wichmann
  • Patent number: 5646173
    Abstract: 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: Grant
    Filed: February 21, 1996
    Date of Patent: July 8, 1997
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Michael Bos, Jurgen Wichmann, Ulrich Widmer