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).

  • POSITIVE ALLOSTERIC MODULATORS (PAM)
    Publication number: 20110098313
    Abstract: The present invention relates to phenylethynyl compounds of formula I wherein R1, R2, X, L, R3, R4, R4?, cyc, and n are as defined in the specification and claims and 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 are useful for the treatment of schizophrenia or cognitive diseases.
    Type: Application
    Filed: October 20, 2010
    Publication date: April 28, 2011
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • IMIDAZOLES
    Publication number: 20110015202
    Abstract: The present invention relates to imidazole derivatives of the general formula wherein R1, R2, R3, and R4 are as defined in the specification and to pharmaceutically acceptable salts thereof. Compounds of formula I are metabotropic glutamate receptor antagonists. They can be used in the treatment or prevention of mGluR5 receptor mediated disorders.
    Type: Application
    Filed: July 9, 2010
    Publication date: January 20, 2011
    Inventors: Georg Jaeschke, Lothar Lindemann, Eric Vieira, Juergen Wichmann
  • Dand 5-HTreceptor modulators
    Patent number: 7858630
    Abstract: The present invention provides compounds of the general formula (I) wherein X, n and R1 are as described herein, as well as pharmaceutically acceptable salts and esters thereof, methods for their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, useful in the treatment and/or the prevention of cognitive disorders, drug addiction, depression, anxiety, drug dependence, dementias, memory impairment, psychotic disorders comprising schizophrenia, schizoaffective disorders, bipolar disease, mania, psychotic depression, and psychoses comprising paranoia and delusions.
    Type: Grant
    Filed: September 16, 2009
    Date of Patent: December 28, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luca Gobbi, Georg Jaeschke, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
  • Isoxazolo[4,5]pyridin-3-yl-piperazin derivatives useful as modulators of dopamine D3 receptors
    Patent number: 7825123
    Abstract: The present invention provides compounds of formula I, having affinity and selectivity for the dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the therapeutic and/or prophylactic treatment of cognitive disorders.
    Type: Grant
    Filed: September 17, 2009
    Date of Patent: November 2, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luca Gobbi, Georg Jaeschke, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
  • Ether derivatives
    Patent number: 7795437
    Abstract: The present invention relates to ether derivatives according to general formula I, and to their pharmaceutically-acceptable salts, which may be used in treating or preventing cognitive disorders, drug addiction, depression, anxiety, drug dependence, dementias, memory impairment, psychotic disorders comprising schizophrenia, schizoaffective disorders, bipolar disease, mania, psychotic depression, or psychoses comprising paranoia and delusions.
    Type: Grant
    Filed: October 22, 2007
    Date of Patent: September 14, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luca Claudio Gobbi, Georg Jaeschke, Olivier Roche, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
  • PYRIDINE-2-YL CARBOXYLIC ACID AMIDES
    Publication number: 20100227887
    Abstract: The present invention relates to pyridine-2-yl-carboxylic acid amides which act as metabotropic glutamate receptor antagonists. In particular, the present invention relates to pyridine-2-yl-carboxylic acid amides of formula I wherein R1, R2, R3, and R4 are as described in the specification.
    Type: Application
    Filed: February 24, 2010
    Publication date: September 9, 2010
    Inventors: Georg Jaeschke, Eric Vieira, Juergen Wichmann
  • PYRIDINYLPIPERAZIN DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS
    Publication number: 20100075979
    Abstract: The present invention provides compounds of provides formula I, having affinity and selectivity for the dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the therapeutic and/or prophylactic treatment of cognitive disorders.
    Type: Application
    Filed: September 16, 2009
    Publication date: March 25, 2010
    Inventors: Luca Gobbi, Georg Jaeschke, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
  • BENZO[D]ISOXAZOL-3-YL-PIPERAZIN DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS
    Publication number: 20100075985
    Abstract: The present invention provides compounds of the general formula (I), having affinity and selectivity for the dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the therapeutic and/or prophylactic treatment of cognitive disorders.
    Type: Application
    Filed: September 16, 2009
    Publication date: March 25, 2010
    Inventors: Kimberly J. Prior, Georg Jaeschke, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
  • ISOXAZOLO[4,5]PYRIDIN-3-YL-PIPERAZIN DERIVATIVES USEFUL AS MODULATORS OF DOPAMINE D3 RECEPTORS
    Publication number: 20100075981
    Abstract: The present invention provides compounds of formula I, having affinity and selectivity for the dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the therapeutic and/or prophylactic treatment of cognitive disorders.
    Type: Application
    Filed: September 17, 2009
    Publication date: March 25, 2010
    Inventors: Luca Gobbi, Georg Jaeschke, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
  • D3 AND 5-HT2A RECEPTOR MODULATORS
    Publication number: 20100075983
    Abstract: The present invention provides compounds of the general formula (I) wherein X, n and R1 are as described herein, as well as pharmaceutically acceptable salts and esters thereof, methods for their manufacture, pharmaceutical compositions containing them and their use as medicaments. The active compounds of the present invention are dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, useful in the treatment and/or the prevention of cognitive disorders, drug addiction, depression, anxiety, drug dependence, dementias, memory impairment, psychotic disorders comprising schizophrenia, schizoaffective disorders, bipolar disease, mania, psychotic depression, and psychoses comprising paranoia and delusions.
    Type: Application
    Filed: September 16, 2009
    Publication date: March 25, 2010
    Inventors: Luca Gobbi, Georg Jaeschke, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
  • Thiazole-4-carboxyamide derivatives
    Patent number: 7678815
    Abstract: The present invention is concerned with novel thiazole 4-carboxyamide derivatives of the general formula (I) and with methods for the preparation thereof, which compounds are useful as metabotropic glutamate receptor antagonists: wherein R1 to R4 are as defined in the specification.
    Type: Grant
    Filed: January 10, 2006
    Date of Patent: March 16, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
  • DIAZOLE DERIVATIVES
    Publication number: 20100048569
    Abstract: The present invention relates to diazole derivatives of the general formula wherein A, E, R1, R2 and R3 are as defined in application and pharmaceutical compositions containing them. The invention also relates to use of such compounds for the treatment of diseases mediated by the metabotropic glutamate receptors (mGluR), such as anxiety, chronic and acute pain, protection against liver damage, urinary incontinence, obesity, Fragile-X and autism, Alzheimer's disease, epilepsy, schizophrenia, ischemia, Huntington's chorea, amyotrophic lateral sclerosis (ALS), dementia caused by AIDs, and Parkinson's disease.
    Type: Application
    Filed: November 5, 2009
    Publication date: February 25, 2010
    Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Paul Spurr, Eric Vieira
  • Thiazolo[4,5-C]pyridine derivatives
    Patent number: 7659401
    Abstract: The invention relates to compounds of general formula I: wherein R1, R2 and R3 are as defined in the description such compounds are metabotropic glutamate receptor antagonists and are useful in the treatment or prevention of mGluR5 receptor mediated disorders.
    Type: Grant
    Filed: October 31, 2006
    Date of Patent: February 9, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Sabine Kolczewski, Richard H. P. Porter, Patrick Schnider, Eric Vieira
  • PYRAZINE-2-CARBOXYAMIDE DERIVATIVES
    Publication number: 20090233944
    Abstract: The present invention is concerned with novel pyrazine 2-carboxyamide derivatives of formula (I) wherein R1, R2 and R3 are as defined in the specification. These compounds are useful for the treatment of CNS disorders.
    Type: Application
    Filed: May 22, 2009
    Publication date: September 17, 2009
    Inventors: Georg Jaeschke, Sabine Kolczewski, Richard Hugh Phillip Porter, Eric Vieira
  • Imidazole derivatives
    Patent number: 7531529
    Abstract: The present invention relates to imidazole derivatives of formula I wherein R1, R2, R3 and R4 are described hereinabove. These compounds can be used in the treatment or prevention of mGluR5 receptor mediated disorders. These compounds are useful, inter alia, in the treatment of genitourinary diseases.
    Type: Grant
    Filed: December 22, 2004
    Date of Patent: May 12, 2009
    Assignee: Roche Palo Alto LLC
    Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira, Anthony P. D. W. Ford, Yu Zhong
  • Naphthyridin derivatives
    Patent number: 7511055
    Abstract: The present invention relates to heterocyclic derivatives of formula I wherein R1, R2 and R3 are as defined in the description and claims, which compounds are metabotropic glutamate receptor 5 antagonists.
    Type: Grant
    Filed: September 28, 2006
    Date of Patent: March 31, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Patrick Schnider, Eric Vieira
  • METHODS FOR THE TREATMENT OF GERD WITH MGLUR5 ANTAGONISTS
    Publication number: 20090054490
    Abstract: The present invention relates to methods for the treatment, prevention and/or delay of progression of gastro-esophageal reflux disease (GERD) by administering compounds that act as antagonists of metabotropic glutamate type-5 receptors (mGluR5 receptor antagonists), for example compounds of formula (I) wherein A, E, R1, R2, R2 and R4 are as defined in the specification.
    Type: Application
    Filed: August 13, 2008
    Publication date: February 26, 2009
    Inventors: Georg Jaeschke, Sabine Kolczewski, Will Spooren, Eric Vieira
  • BENZOYL-PIPERIDINE DERIVATIVES AS DUAL MODULATORS OF THE 5-HT2A AND D3 RECEPTORS
    Publication number: 20090042943
    Abstract: The present invention relates to compounds of formula (I) wherein R1 and A are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use as medicaments. Compounds of general formula (I) have high affinity for the dopamine D3 and serotonin (5-Hydroxytryptamine; 5-HT) 5-HT2A receptors and are effective in the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.
    Type: Application
    Filed: August 1, 2008
    Publication date: February 12, 2009
    Inventors: Luca Gobbi, Georg Jaeschke, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
  • DUAL MODULATORS OF 5HT2A AND D3 RECEPTORS
    Publication number: 20090029977
    Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, X and n are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.
    Type: Application
    Filed: July 18, 2008
    Publication date: January 29, 2009
    Inventors: Luca Gobbi, Georg Jaeschke, Olivier Roche, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
  • IMIDAZOLE DERIVATIVES
    Publication number: 20090018171
    Abstract: The present invention relates to imidazole derivatives of formula I wherein R1, R2, R3, R4, X, Y and R are described hereinabove, or a pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition comprising the imidazole derivatives of formula I, a process for preparing a compound of formula I, and a method of treating or preventing acute and/or chronic neurological disorder comprising administering to a patient in need of such treatment and/or prevention a therapeutically effective amount of said pharmaceutical composition. These disorders include Alzheimer's disease. These disorders also include mild cognitive impairment.
    Type: Application
    Filed: September 17, 2008
    Publication date: January 15, 2009
    Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira