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).

  • Patent number: 11242349
    Abstract: The present invention relates to compounds that may be used in the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression or diabetes type 2.
    Type: Grant
    Filed: May 1, 2020
    Date of Patent: February 8, 2022
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Barbara Biemans, Georg Jaeschke, Antonio Ricci, Daniel Rueher, Fionn O'Hara
  • Publication number: 20210300844
    Abstract: The present invention relates to ethynyl derivatives of formula I with variables as defined herein, or to a pharmaceutically acceptable acid addition salt thereof Compounds of formula I are 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: June 3, 2021
    Publication date: September 30, 2021
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Eric Vieira
  • Patent number: 11117890
    Abstract: The present invention provides substituted isoindole compounds which are selective allosteric EGFR inhibitors, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances, generally of Formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 2, 2019
    Date of Patent: September 14, 2021
    Assignee: Hoffman La-Roche Inc.
    Inventors: Georg Jaeschke, Antonio Ricci, Daniel Rueher, Sandra Steiner, Martin Duplessis, Yvonne Alice Nagel, Bernd Kuhn
  • Publication number: 20210269452
    Abstract: The present invention relates to positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4) that may be used for the treatment of conditions such as Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.
    Type: Application
    Filed: May 9, 2021
    Publication date: September 2, 2021
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Barbara Biemans, Wolfgang Guba, Georg Jaeschke, Lothar Lindemann, Fionn O'Hara, Antonio Ricci, Daniel Rueher, Eric Vieira
  • Patent number: 11059766
    Abstract: The present invention relates to ethynyl derivatives of formula I with variables as defined herein, or to a pharmaceutically acceptable acid addition salt thereof. Compounds of formula I are 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: December 1, 2017
    Date of Patent: July 13, 2021
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Eric Vieira
  • Patent number: 11034699
    Abstract: The present invention relates to positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4) that may be used for the treatment of conditions such as Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.
    Type: Grant
    Filed: December 14, 2018
    Date of Patent: June 15, 2021
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Barbara Biemans, Wolfgang Guba, Georg Jaeschke, Lothar Lindemann, Fionn O'Hara, Antonio Ricci, Daniel Rueher, Eric Vieira
  • Publication number: 20210079005
    Abstract: The present invention provides compounds which are selective allosteric inhibitors of T790M/L858R, T790M/L858R/C797S, L858R, L858R/C797S containing EGFR mutants, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances.
    Type: Application
    Filed: November 25, 2020
    Publication date: March 18, 2021
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Martin Duplessis, Annick Goergler, Georg Jaeschke, Buelent Kocer, Bernd Kuhn, Kiel Lazarski, Yanke Liang, Yvonne Alice Nagel, Ulrike Obst Sander, Antonio Ricci, Daniel Rueher, Sandra Steiner
  • Publication number: 20210070739
    Abstract: The present invention provides compounds which are selective allosteric inhibitors of T790M and C797S containing EGFR mutants, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances.
    Type: Application
    Filed: November 24, 2020
    Publication date: March 11, 2021
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Martin Duplessis, Georg Jaeschke, Bernd Kuhn, Kiel Lazarski, Yanke Liang, Yvonne Alice Nagel, Antonio Ricci, Daniel Rueher, Sandra Steiner
  • Patent number: 10882848
    Abstract: The present invention provides compounds which are selective allosteric inhibitors of T790M and C797S containing EGFR mutants, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances.
    Type: Grant
    Filed: June 21, 2019
    Date of Patent: January 5, 2021
    Assignee: Hoffmann-La Roche, Inc.
    Inventors: Martin Duplessis, Georg Jaeschke, Bernd Kuhn, Kiel Lazarski, Yanke Liang, Yvonne Alice Nagel, Antonio Ricci, Daniel Rueher, Sandra Steiner
  • Publication number: 20200361930
    Abstract: The present invention provides compounds that cause specifically the degradation of EGFR via the targeted ubiquitination of EGFR protein and subsequent proteasomal degradation. The present compounds are useful for the treatment of various cancers.
    Type: Application
    Filed: August 4, 2020
    Publication date: November 19, 2020
    Applicants: Hoffmann-La Roche Inc., C4 Therapeutics, Inc.
    Inventors: Martin Duplessis, Georg Jaeschke, Bernd Kuhn, Kiel Lazarski, Yanke Liang, Yvonne Alice Nagel, Antonio Ricci, Daniel Rueher, Sandra Steiner
  • Publication number: 20200308171
    Abstract: Present invention provides bifunctional compounds that comprise an E3 Ubiquitin Ligase moiety that is linked to a moiety that inhibit EGFR, where the target protein can be proximate to the ubiquitin ligase to effect degradation of said protein. Present compounds are useful for the treatment of various cancers.
    Type: Application
    Filed: June 16, 2020
    Publication date: October 1, 2020
    Applicants: Hoffmann-La Roche Inc., C4 Therapeutics, Inc.
    Inventors: Georg Jaeschke, Bernd Kuhn, Antonio Ricci, Daniel Rueher, Sandra Steiner, Yvonne Alice Nagel, Martin Duplessis, Kiel Lazarski, Yanke Liang
  • Publication number: 20200291034
    Abstract: The present invention relates to a compound of formula wherein HetAr is a five or six membered hetaryl group, containing one, two or three heteroatoms, selected from N, O or S; R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, or lower alkoxy; R2 is lower alkyl substituted by halogen, —CH2—C3-6-cycloalkyl, substituted by one or two substituents, selected from lower alkyl substituted by halogen or halogen, or is lower alkenyl substituted by halogen; R3 is hydrogen, lower alkyl substituted by halogen, lower alkyl, halogen, C3-6-cycloalkyl or lower alkyl substituted by hydroxy; n is 1 or 2; for n=2, R1 can be independent to each other; Y is CH or N; or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.
    Type: Application
    Filed: February 13, 2020
    Publication date: September 17, 2020
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Bjoern BARTELS, Hasane RATNI, Karlheinz BAUMANN, Guido GALLEY, Georg JAESCHKE, Roland JAKOB-ROETNE, Anja LIMBERG, Werner NEIDHART, Rosa Maria RODRIGUEZ-SARMIENTO
  • Publication number: 20200291033
    Abstract: The present invention relates to compounds of formula I wherein L is a bond, a triple bond, —C(O)NH— or —NHC(O)—; R1 is phenyl or a five or six-membered heteroaryl group, optionally substituted by lower alkyl, lower alkyl substituted by halogen or lower alkoxy substituted by halogen; R2 is fluoro; R3 is fluoro or chloro; R4 is hydrogen, lower alkyl, halogen, lower alkyl substituted by hydroxy, S(O)2CH3, or is a five or six-membered heteroaryl group or a heterocycloalkyl group, which are optionally substituted by lower alkyl, hydroxy or ?O; R5 and R6 are both methyl and the dotted line is a bond, or R5 and R6 are both methyl and the dotted line is nothing, or one of R5 and R6 is hydrogen and the other is methyl, and the dotted line is nothing; or to a pharmaceutically acceptable salt or acid addition salt, to all possible tautomeric forms, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.
    Type: Application
    Filed: February 13, 2020
    Publication date: September 17, 2020
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Georg JAESCHKE, Fionn O'HARA, Eric VIEIRA
  • Publication number: 20200255440
    Abstract: The present invention relates to compounds that may be used in the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression or diabetes type 2.
    Type: Application
    Filed: May 1, 2020
    Publication date: August 13, 2020
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Barbara BIEMANS, Georg JAESCHKE, Antonio RICCI, Daniel RUEHER, Fionn O'HARA
  • Publication number: 20200102299
    Abstract: The present invention provides compounds which are selective allosteric inhibitors of TMLR, TMLRCS, LR, LACS containing EGFR mutants, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances.
    Type: Application
    Filed: December 2, 2019
    Publication date: April 2, 2020
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Antonio Ricci, Daniel Rueher, Sandra Steiner, Martin Duplessis, Yvonne Alice Nagel, Bernd Kuhn
  • Patent number: 10562903
    Abstract: The present invention relates to a compound of formula wherein HetAr is a five or six membered hetaryl group, containing one, two or three heteroatoms, selected from N, O or S; R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, halogen, or lower alkoxy; R2 is lower alkyl substituted by halogen, —CH2—C3-6-cycloalkyl, substituted by one or two substituents, selected from lower alkyl substituted by halogen or halogen, or is lower alkenyl substituted by halogen; R3 is hydrogen, lower alkyl substituted by halogen, lower alkyl, halogen, C3-6-cycloalkyl or lower alkyl substituted by hydroxy; n is 1 or 2; for n=2, R1 can be independent to each other; Y is CH or N; or to a pharmaceutically active acid addition salt thereof, to a racemic mixture or its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof.
    Type: Grant
    Filed: June 8, 2018
    Date of Patent: February 18, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bjoern Bartels, Hasane Ratni, Karlheinz Baumann, Guido Galley, Georg Jaeschke, Roland Jakob-Roetne, Anja Limberg, Werner Neidhart, Rosa Maria Rodriguez-Sarmiento
  • Publication number: 20190308955
    Abstract: The present invention provides compounds which are selective allosteric inhibitors of T790M and C797S containing EGFR mutants, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances.
    Type: Application
    Filed: June 21, 2019
    Publication date: October 10, 2019
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Martin Duplessis, Georg Jaeschke, Bernd Kuhn, Kiel Lazarski, Yanke Liang, Yvonne Alice Nagel, Antonio Ricci, Daniel Rueher, Sandra Steiner
  • Publication number: 20190144458
    Abstract: The present invention relates to compounds that may be used in the treatment of Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression or diabetes type 2.
    Type: Application
    Filed: January 17, 2019
    Publication date: May 16, 2019
    Applicant: Hoffmann-La Roche Inc.
    Inventors: BARBARA BIEMANS, GEORG JAESCHKE, ANTONIO RICCI, DANIEL RUEHER, FIONN O'HARA
  • Publication number: 20190119290
    Abstract: The present invention relates to positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4) that may be used for the treatment of conditions such as Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.
    Type: Application
    Filed: December 14, 2018
    Publication date: April 25, 2019
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Barbara Biemans, Wolfgang Guba, Georg Jaeschke, Lothar Lindemann, Fionn O'Hara, Antonio Ricci, Daniel Rueher, Eric Vieira
  • Patent number: 10189848
    Abstract: The present invention relates to positive allosteric modulators (PAMs) of metabotropic glutamate receptor 4 (mGluR4) that may be used for the treatment of conditions such as Parkinson's disease, anxiety, emesis, obsessive compulsive disorder, autism, neuroprotection, cancer, depression and diabetes type 2.
    Type: Grant
    Filed: January 12, 2018
    Date of Patent: January 29, 2019
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Barbara Biemans, Wolfgang Guba, Georg Jaeschke, Lothar Lindemann, Fionn O'Hara, Antonio Ricci, Daniel Rueher, Eric Vieira