Patents by Inventor Georg Jaeschke

Georg Jaeschke 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).

  • Ethynyl derivatives
    Patent number: 9695128
    Abstract: The present invention relates to compounds of formula I having variables as described herein, which are useful for the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.
    Type: Grant
    Filed: July 8, 2016
    Date of Patent: July 4, 2017
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Barbara Biemans, Wolfgang Guba, Georg Jaeschke, Antonio Ricci, Daniel Rueher, Eric Vieira
  • Ethynyl derivatives
    Patent number: 9682959
    Abstract: The present invention relates to ethynyl derivatives as metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of, e.g., anxiety and pain, depression, Fragile-X syndrome, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).
    Type: Grant
    Filed: January 8, 2016
    Date of Patent: June 20, 2017
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Georg Jaeschke, Lothar Lindemann, Rainer E. Martin, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Ethynyl derivatives
    Patent number: 9676732
    Abstract: It has been surprisingly been found that the compounds of general formula I are positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4), useful for the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.
    Type: Grant
    Filed: September 30, 2016
    Date of Patent: June 13, 2017
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Barbara Biemans, Wolfgang Guba, Georg Jaeschke, Antonio Ricci, Daniel Rueher, Eric Vieira
  • ETHYNYL DERIVATIVES
    Publication number: 20170114028
    Abstract: It has been surprisingly been found that the compounds of general formula I are positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4), useful for the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.
    Type: Application
    Filed: September 30, 2016
    Publication date: April 27, 2017
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Barbara Biemans, Wolfgang Guba, Georg Jaeschke, Antonio Ricci, Daniel Rueher, Eric Vieira
  • ETHYNYL DERIVATIVES
    Publication number: 20170008854
    Abstract: The present invention relates to compounds useful for the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.
    Type: Application
    Filed: July 8, 2016
    Publication date: January 12, 2017
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Barbara Biemans, Wolfgang Guba, Georg Jaeschke, Antonio Ricci, Daniel Rueher, Eric Vieira
  • ETHYNYL DERIVATIVES
    Publication number: 20160362383
    Abstract: The present invention relates to compounds that may be used in the treatment or prevention of disorders relating to allosteric modulation of the mGluR4 receptor. Such compounds may be used for the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.
    Type: Application
    Filed: August 24, 2016
    Publication date: December 15, 2016
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Eric Vieira, Georg Jaeschke, Wolfgang Guba, Antonio Ricci, Daniel Rueher, Barbara Biemans, Jean-Marc Plancher, Fionn O'Hara
  • ETHYNYL DERIVATIVES
    Publication number: 20160207890
    Abstract: It has been surprisingly been found that the compounds of general formula I are positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4), useful for the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.
    Type: Application
    Filed: March 25, 2016
    Publication date: July 21, 2016
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Barbara BIEMANS, Wolfgang GUBA, Georg JAESCHKE, Antonio RICCI, Daniel RUEHER, Eric VIEIRA
  • Ethynyl derivatives
    Patent number: 9359301
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein Y is N or CH R1 is fluoro or chloro or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula I are metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of anxiety and pain, depression, Fragile-X syndrom, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).
    Type: Grant
    Filed: April 17, 2015
    Date of Patent: June 7, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • ETHYNYL DERIVATIVES
    Publication number: 20160130255
    Abstract: The present invention relates to ethynyl derivatives as metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of, e.g., anxiety and pain, depression, Fragile-X syndrome, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).
    Type: Application
    Filed: January 8, 2016
    Publication date: May 12, 2016
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Rainer E. Martin, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Arylethynyl derivatives
    Patent number: 9328090
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein R1 is phenyl, which is optionally substituted by 1-2 halogen atoms; selected from fluorine or chlorine; or to a pharmaceutically acceptable acid addition salt in enantiomerically pure form. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Grant
    Filed: October 26, 2015
    Date of Patent: May 3, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Heinz Stadler, Eric Vieira
  • Ethynyl derivatives
    Patent number: 9328070
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein Y is N or CH or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.
    Type: Grant
    Filed: April 17, 2015
    Date of Patent: May 3, 2016
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Arlethynyl derivatives
    Patent number: 9315498
    Abstract: The present invention relates to ethynyl compounds of formula I-C1 wherein R1, R2, R2?, R3, R3?, R6, U, V and W are as defined herein and to a pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to its corresponding enantiomers and/or optical isomers and/or stereoisomers thereof, which are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Grant
    Filed: November 20, 2013
    Date of Patent: April 19, 2016
    Assignee: HOFFMAN-LA ROCHE INC.
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Arylethynyl derivatives
    Publication number: 20160039787
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein R1 is phenyl, which is optionally substituted by 1-2 halogen atoms; selected from fluorine or chlorine; or to a pharmaceutically acceptable acid addition salt in enantiomerically pure form. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Application
    Filed: October 26, 2015
    Publication date: February 11, 2016
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Georg Jaeschke, Lothar Lindemann, Heinz Stadler, Eric Vieira
  • Ethynyl derivatives
    Patent number: 9227959
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein Y is N or CH R1 is fluoro or chloro R2 is hydrogen or methyl or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula I are metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of anxiety and pain, depression, Fragile-X syndrome, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).
    Type: Grant
    Filed: April 17, 2015
    Date of Patent: January 5, 2016
    Assignee: Hoffman-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Arylethynyl derivatives
    Patent number: 9221802
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein R1 is phenyl, 3-fluorophenyl, 4-fluorophenyl or 2,5-di-fluorophenyl; or to a pharmaceutically acceptable acid addition salt, in enantiomerically pure form with the absolute configuration as shown in formula I. It has now surprisingly been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5) which show advantageous biochemical-, physicochemical- and pharmacodynamic-properties compared to compounds of prior art.
    Type: Grant
    Filed: March 26, 2015
    Date of Patent: December 29, 2015
    Assignee: Hoffman-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Heinz Stadler, Eric Vieira
  • Ethynyl compounds
    Patent number: 9212171
    Abstract: The present invention relates to ethynyl derivatives of formula I X, G, R1, R2, R3, R3?, R4, R4?, R5, R6, R6?, m, and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. Compounds of formula I are positive allosteric modulators (PAM) of the metabotropic glutamate receptor subtype 5 (mGluR5). They can be used for the treatment of schizophrenia or cognitive disorders.
    Type: Grant
    Filed: January 6, 2015
    Date of Patent: December 15, 2015
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
  • Arylethynyl pyrimidines
    Patent number: 9199971
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein R1 is hydrogen or halogen; R2 is C1-3-alkyl or —(CH2)n—O—CH3; n is 2 or 3; m is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5) with improved properties for the treatment of schizophrenia, cognitive diseases, fragile X syndrome or autism.
    Type: Grant
    Filed: February 13, 2015
    Date of Patent: December 1, 2015
    Assignee: Hoffman-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Heinz Stadler, Eric Vieira
  • Ethynyl Derivatives
    Publication number: 20150225345
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein Y is N or CH R1 is fluoro or chloro or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula I are metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of anxiety and pain, depression, Fragile-X syndrom, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).
    Type: Application
    Filed: April 17, 2015
    Publication date: August 13, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Ethynyl Derivatives
    Publication number: 20150225344
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein Y is N or CH or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula I are metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of anxiety and pain, depression, Fragile-X syndrome, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).
    Type: Application
    Filed: April 17, 2015
    Publication date: August 13, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Ethynyl Derivatives
    Publication number: 20150225385
    Abstract: The present invention relates to ethynyl derivatives of formula I wherein Y is N or CH 1 is fluoro or chloro R2 is hydrogen or methyl or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has now surprisingly been found that the compounds of general formula I are metabotropic glutamate receptor antagonists (negative allosteric modulators) for use in the treatment of anxiety and pain, depression, Fragile-X syndrom, autism spectrum disorders, Parkinson's disease, and gastroesophageal reflux disease (GERD).
    Type: Application
    Filed: April 17, 2015
    Publication date: August 13, 2015
    Applicant: HOFFMANN-LA ROCHE INC.
    Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira