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).
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Patent number: 11242349Abstract: 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: GrantFiled: May 1, 2020Date of Patent: February 8, 2022Assignee: Hoffmann-La Roche Inc.Inventors: Barbara Biemans, Georg Jaeschke, Antonio Ricci, Daniel Rueher, Fionn O'Hara
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Publication number: 20210300844Abstract: 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: ApplicationFiled: June 3, 2021Publication date: September 30, 2021Applicant: Hoffmann-La Roche Inc.Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Eric Vieira
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Patent number: 11117890Abstract: 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: GrantFiled: December 2, 2019Date of Patent: September 14, 2021Assignee: Hoffman La-Roche Inc.Inventors: Georg Jaeschke, Antonio Ricci, Daniel Rueher, Sandra Steiner, Martin Duplessis, Yvonne Alice Nagel, Bernd Kuhn
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Publication number: 20210269452Abstract: 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: ApplicationFiled: May 9, 2021Publication date: September 2, 2021Applicant: Hoffmann-La Roche Inc.Inventors: Barbara Biemans, Wolfgang Guba, Georg Jaeschke, Lothar Lindemann, Fionn O'Hara, Antonio Ricci, Daniel Rueher, Eric Vieira
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Patent number: 11059766Abstract: 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: GrantFiled: December 1, 2017Date of Patent: July 13, 2021Assignee: Hoffmann-La Roche Inc.Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Eric Vieira
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Patent number: 11034699Abstract: 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: GrantFiled: December 14, 2018Date of Patent: June 15, 2021Assignee: Hoffmann-La Roche Inc.Inventors: Barbara Biemans, Wolfgang Guba, Georg Jaeschke, Lothar Lindemann, Fionn O'Hara, Antonio Ricci, Daniel Rueher, Eric Vieira
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Publication number: 20210079005Abstract: 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: ApplicationFiled: November 25, 2020Publication date: March 18, 2021Applicant: 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
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Publication number: 20210070739Abstract: 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: ApplicationFiled: November 24, 2020Publication date: March 11, 2021Applicant: Hoffmann-La Roche Inc.Inventors: Martin Duplessis, Georg Jaeschke, Bernd Kuhn, Kiel Lazarski, Yanke Liang, Yvonne Alice Nagel, Antonio Ricci, Daniel Rueher, Sandra Steiner
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Patent number: 10882848Abstract: 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: GrantFiled: June 21, 2019Date of Patent: January 5, 2021Assignee: Hoffmann-La Roche, Inc.Inventors: Martin Duplessis, Georg Jaeschke, Bernd Kuhn, Kiel Lazarski, Yanke Liang, Yvonne Alice Nagel, Antonio Ricci, Daniel Rueher, Sandra Steiner
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Publication number: 20200361930Abstract: 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: ApplicationFiled: August 4, 2020Publication date: November 19, 2020Applicants: 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
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Publication number: 20200308171Abstract: 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: ApplicationFiled: June 16, 2020Publication date: October 1, 2020Applicants: 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
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Publication number: 20200291034Abstract: 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: ApplicationFiled: February 13, 2020Publication date: September 17, 2020Applicant: 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
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Publication number: 20200291033Abstract: 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: ApplicationFiled: February 13, 2020Publication date: September 17, 2020Applicant: Hoffmann-La Roche Inc.Inventors: Georg JAESCHKE, Fionn O'HARA, Eric VIEIRA
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Publication number: 20200255440Abstract: 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: ApplicationFiled: May 1, 2020Publication date: August 13, 2020Applicant: Hoffmann-La Roche Inc.Inventors: Barbara BIEMANS, Georg JAESCHKE, Antonio RICCI, Daniel RUEHER, Fionn O'HARA
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Publication number: 20200102299Abstract: 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: ApplicationFiled: December 2, 2019Publication date: April 2, 2020Applicant: Hoffmann-La Roche Inc.Inventors: Georg Jaeschke, Antonio Ricci, Daniel Rueher, Sandra Steiner, Martin Duplessis, Yvonne Alice Nagel, Bernd Kuhn
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Patent number: 10562903Abstract: 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: GrantFiled: June 8, 2018Date of Patent: February 18, 2020Assignee: 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
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Publication number: 20190308955Abstract: 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: ApplicationFiled: June 21, 2019Publication date: October 10, 2019Applicant: Hoffmann-La Roche Inc.Inventors: Martin Duplessis, Georg Jaeschke, Bernd Kuhn, Kiel Lazarski, Yanke Liang, Yvonne Alice Nagel, Antonio Ricci, Daniel Rueher, Sandra Steiner
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Publication number: 20190144458Abstract: 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: ApplicationFiled: January 17, 2019Publication date: May 16, 2019Applicant: Hoffmann-La Roche Inc.Inventors: BARBARA BIEMANS, GEORG JAESCHKE, ANTONIO RICCI, DANIEL RUEHER, FIONN O'HARA
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Publication number: 20190119290Abstract: 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: ApplicationFiled: December 14, 2018Publication date: April 25, 2019Applicant: Hoffmann-La Roche Inc.Inventors: Barbara Biemans, Wolfgang Guba, Georg Jaeschke, Lothar Lindemann, Fionn O'Hara, Antonio Ricci, Daniel Rueher, Eric Vieira
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Patent number: 10189848Abstract: 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: GrantFiled: January 12, 2018Date of Patent: January 29, 2019Assignee: Hoffmann-La Roche Inc.Inventors: Barbara Biemans, Wolfgang Guba, Georg Jaeschke, Lothar Lindemann, Fionn O'Hara, Antonio Ricci, Daniel Rueher, Eric Vieira