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: 9328090Abstract: 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: GrantFiled: October 26, 2015Date of Patent: May 3, 2016Assignee: Hoffmann-La Roche Inc.Inventors: Georg Jaeschke, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Patent number: 9315498Abstract: 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: GrantFiled: November 20, 2013Date of Patent: April 19, 2016Assignee: HOFFMAN-LA ROCHE INC.Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
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Publication number: 20160039787Abstract: 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: ApplicationFiled: October 26, 2015Publication date: February 11, 2016Applicant: HOFFMANN-LA ROCHE INC.Inventors: Georg Jaeschke, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Patent number: 9227959Abstract: 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: GrantFiled: April 17, 2015Date of Patent: January 5, 2016Assignee: Hoffman-La Roche Inc.Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
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Patent number: 9221802Abstract: 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: GrantFiled: March 26, 2015Date of Patent: December 29, 2015Assignee: Hoffman-La Roche Inc.Inventors: Georg Jaeschke, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Patent number: 9212171Abstract: 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: GrantFiled: January 6, 2015Date of Patent: December 15, 2015Assignee: HOFFMANN-LA ROCHE INC.Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Patent number: 9199971Abstract: 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: GrantFiled: February 13, 2015Date of Patent: December 1, 2015Assignee: Hoffman-La Roche Inc.Inventors: Georg Jaeschke, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Publication number: 20150225385Abstract: 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: ApplicationFiled: April 17, 2015Publication date: August 13, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
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Publication number: 20150225344Abstract: 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: ApplicationFiled: April 17, 2015Publication date: August 13, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
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Publication number: 20150225345Abstract: 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: ApplicationFiled: April 17, 2015Publication date: August 13, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
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Publication number: 20150197510Abstract: 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: ApplicationFiled: March 26, 2015Publication date: July 16, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Georg Jaeschke, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Publication number: 20150158848Abstract: 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: ApplicationFiled: February 13, 2015Publication date: June 11, 2015Applicant: HOFFMANN-LA ROCHE INC.Inventors: Georg Jaeschke, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Publication number: 20150133505Abstract: 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: ApplicationFiled: January 15, 2015Publication date: May 14, 2015Applicant: Hoffmann-La Roche Inc.Inventors: Georg Jaeschke, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Publication number: 20150119384Abstract: The present invention relates to ethynyl derivatives of formula I X, O, R1, R2, R3, R3?, R4, R4?, R5, R6, R6?, m, and n are as defined hereinor 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: ApplicationFiled: January 6, 2015Publication date: April 30, 2015Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Patent number: 8969338Abstract: The present invention relates to ethynyl derivatives of formula I wherein U, V, Y, R1, R2, R2?, R3, R3? and R8 are described herein. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).Type: GrantFiled: September 27, 2012Date of Patent: March 3, 2015Assignee: Hoffmann-La Roche Inc.Inventors: Georg Jaeschke, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
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Patent number: 8957213Abstract: 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: GrantFiled: April 23, 2012Date of Patent: February 17, 2015Assignee: Hoffman-La Roche Inc.Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Patent number: 8933094Abstract: The present invention relates to ethynyl compounds of formula wherein X, Y, Z, and R4 are as defined herein or to a pharmaceutically acceptable salt or 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) and they are therefore useful for the treatment of diseases related to this receptor.Type: GrantFiled: October 16, 2013Date of Patent: January 13, 2015Assignee: Hoffmann-La Roche Inc.Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Heinz Stadler, Eric Vieira
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Publication number: 20140350051Abstract: 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: ApplicationFiled: July 24, 2014Publication date: November 27, 2014Inventors: Luca Gobbi, Georg Jaeschke, Olivier Roche, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
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Patent number: 8829029Abstract: 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: GrantFiled: February 21, 2013Date of Patent: September 9, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Luca Gobbi, Georg Jaeschke, Olivier Roche, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
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Patent number: 8772300Abstract: The present invention relates to ethynyl derivatives of formula I wherein Y is N or C—R3; R3 is hydrogen, methyl, halogen or nitrile; R1 is phenyl or pyridinyl, each of which is optionally substituted by halogen, lower alkyl or lower alkoxy; R2/R2? are each independently hydrogen, lower alkyl or lower alkyl substituted by halogen, or R2 and R2? together with the N-atom to which they are attached form a morpholine ring, a piperidine ring or an azetidine ring, each of which is unsubstituted or substituted one or more substituents selected from lower alkoxy, halogen, hydroxy and methyl; R4/R4? are each independently hydrogen or lower alkyl, or R4 and R4? together form a C3-5 cycloalkyl-, tetrahydrofuran- or an oxetane-ring; 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: GrantFiled: April 11, 2012Date of Patent: July 8, 2014Assignee: Hoffmann-La Roche Inc.Inventors: Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira