Patents by Inventor Wolfgang Guba

Wolfgang Guba 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).

  • Publication number: 20120238548
    Abstract: The present invention relates to 1,4-Oxazepines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Application
    Filed: March 9, 2012
    Publication date: September 20, 2012
    Inventors: Emanuele Gabellieri, Wolfgang Guba, Hans Hilpert, Harald Mauser, Alexander V. Mayweg, Mark Rogers-Evans, Didier Rombach, Andrew Thomas, Thomas Woltering, Wolfgang Wostl
  • Publication number: 20120214806
    Abstract: The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Application
    Filed: May 1, 2012
    Publication date: August 23, 2012
    Inventors: Matteo Andreini, David Banner, Emanuele Gabellieri, Wolfgang Guba, Hans Hilpert, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Eoin Power, Mark Rogers-Evans, Massimiliano Travagli, Michela Valacchi, Thomas Woltering, Wolfgang Wostl
  • Publication number: 20120184540
    Abstract: The present invention relates to 1,4 Oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Application
    Filed: January 12, 2012
    Publication date: July 19, 2012
    Inventors: Matteo Andreini, Emanuele Gabellieri, Wolfgang Guba, Hans Hilpert, Alexander V. Mayweg, Robert Narquizian, Eoin Power, Massimiliano Travagli, Thomas Woltering, Wolfgang Wostl, Harald Mauser
  • Patent number: 8188079
    Abstract: The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Grant
    Filed: August 9, 2010
    Date of Patent: May 29, 2012
    Assignees: Hoffman-La Roche Inc., Siena Biotech S.p.A.
    Inventors: Matteo Andreini, David Banner, Wolfgang Guba, Hans Hilpert, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Eoin Power, Mark Rogers-Evans, Massimiliano Travagli, Michela Valacchi, Thomas Woltering, Wolfgang Wostl
  • Publication number: 20120035195
    Abstract: This invention relates to compounds of the formula wherein R1 to R9 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as diabetes, particularly type 2 diabetes, and other metabolic disorders.
    Type: Application
    Filed: August 3, 2011
    Publication date: February 9, 2012
    Inventors: David Banner, Emanuele Gabellieri, Wolfgang Guba, Hans Hilpert, Benoit Hornsperger, Roland Humm, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Emmanuel Pinard, Mark Rogers-Evans, Thomas Woltering, Wolfgang Wostl
  • Publication number: 20110312937
    Abstract: This invention relates to compounds of the formula wherein A, B and R1 to R7 are as described below, or to pharmaceutically acceptable salts thereof. These compounds are BACE1 and/or BACE2 inhibitors and can be used as medicaments for the therapeutic and/or prophylactic treatment of diseases such as Alzheimer's disease, diabetes, particularly type 2 diabetes, and other metabolic disorders.
    Type: Application
    Filed: April 28, 2011
    Publication date: December 22, 2011
    Inventors: David Banner, Wolfgang Guba, Hans Hilpert, Roland Humm, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Eoin Power, Mark Rogers-Evans, Didier Rombach, Thomas Woltering, Wolfgang Wostl
  • Publication number: 20110251169
    Abstract: The present invention relates to ethynyl compounds of formula I wherein R1, R2, R2?, R3, R3?, R4, R4?, U, V, W, Y, m, and n 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. Compounds of formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5).
    Type: Application
    Filed: April 5, 2011
    Publication date: October 13, 2011
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindemann, Antonio Ricci, Daniel Rueher, Heinz Stadler, Eric Vieira
  • Patent number: 7989449
    Abstract: The present invention relates to a compounds of formula I wherein R1, R1?, R2, R3, R4, X, Ar, and m are as defined in the specification and claims and pharmaceutically active acid addition salts thereof. Compounds of the invention have Asp2 (?-secretase, BACE 1 or Memapsin-2) inhibitory activity and are useful for the treatment of diseases characterized by elevated ?-amyloid levels or ?-amyloid deposits, particularly Alzheimer's disease.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: August 2, 2011
    Assignees: Hoffman-La Roche Inc., Siena Biotech S.p.A.
    Inventors: Matteo Andreini, Emanuele Gabellieri, Wolfgang Guba, Guido Marconi, Robert Narquizian, Eoin Power, Massimiliano Travagli, Thomas Woltering, Wolfgang Wostl
  • Publication number: 20110152257
    Abstract: 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: Application
    Filed: December 10, 2010
    Publication date: June 23, 2011
    Inventors: Luke Green, Wolfgang Guba, Georg Jaeschke, Synese Jolidon, Lothar Lindermann, Heinz Stadler, Eric Vieira
  • Publication number: 20110144097
    Abstract: The present invention relates to 2-Amino-5,5-difluoro-5,6-dihydro-4H-[1,3]oxazin-4-yl)-phenyl]-amides of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Application
    Filed: December 3, 2010
    Publication date: June 16, 2011
    Inventors: David Banner, Wolfgang Guba, Hans Hilpert, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Emmanuel Pinard, Eoin Power, Mark Rogers-Evans, Thomas Woltering, Wolfgang Wostl
  • 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
  • Publication number: 20110046122
    Abstract: The present invention relates to 3-Amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
    Type: Application
    Filed: August 9, 2010
    Publication date: February 24, 2011
    Inventors: Matteo Andreini, David Banner, Wolfgang Guba, Hans Hilpert, Harald Mauser, Alexander V. Mayweg, Robert Narquizian, Eoin Power, Mark Roger-Evans, Massimiliano Travagli, Michela Valacchi, Thomas Woltering, Wolfgang Wostl
  • Patent number: 7772253
    Abstract: This invention is concerned with compounds of the formula wherein R1 to R5, R5? and A are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
    Type: Grant
    Filed: May 26, 2006
    Date of Patent: August 10, 2010
    Assignee: Hoffman-La Roche Inc.
    Inventors: Alfred Binggeli, Andreas Christ, Luke Gideon Granville Green, Wolfgang Guba, Hans-Peter Maerki, Rainer Eugen Martin, Peter Mohr
  • Patent number: 7645753
    Abstract: This invention is concerned with compounds of the formula wherein A, B1, B2, R1, R2 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
    Type: Grant
    Filed: March 2, 2006
    Date of Patent: January 12, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alfred Binggeli, Andreas Dominik Christ, Luke Gideon Granville Green, Wolfgang Guba, Hans-Peter Maerki, Rainer Eugen Martin, Peter Mohr
  • Publication number: 20090209529
    Abstract: The present invention relates to a compounds of formula I wherein R1, R1?, R2, R3, R4, X, Ar, and m are as defined in the specification and claims and pharmaceutically active acid addition salts thereof. Compounds of the invention have Asp2 (?-secretase, BACE 1 or Memapsin-2) inhibitory activity and are useful for the treatment of diseases characterized by elevated ?-amyloid levels or ?-amyloid deposits, particularly Alzheimer's disease.
    Type: Application
    Filed: February 12, 2009
    Publication date: August 20, 2009
    Inventors: Matteo Andreini, Emanuele Gabellieri, Wolfgang Guba, Guido Marconi, Robert Narquizian, Eoin Power, Massimiliano Travagli, Thomas Woltering, Wolfgang Wostl
  • Patent number: 7576088
    Abstract: The present invention relates to compounds of the general formula and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases such as obesity by selective modulation of CB1 receptors.
    Type: Grant
    Filed: February 22, 2005
    Date of Patent: August 18, 2009
    Assignee: Hoffman-La Roche Inc.
    Inventors: Alexander Alanine, Konrad Bleicher, Wolfgang Guba, Wolfgang Haap, Dagmar Kube, Thomas Luebbers, Jean-Marc Plancher, Olivier Roche, Mark Rogers-Evans, Gisbert Schneider, Jochen Zuegge
  • Publication number: 20090163517
    Abstract: This invention is concerned with compounds of the formula wherein X, A, B, R1, R2 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
    Type: Application
    Filed: February 23, 2009
    Publication date: June 25, 2009
    Inventors: Alfred Binggeli, Andreas Christ, Luke Gideon Granville Green, Wolfgang Guba, Hans-Peter Maerki, Rainer Eugen Martin, Peter Mohr
  • Patent number: 7323466
    Abstract: The present invention refers to chemical compounds of formula (I) as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R5 have the significance given in claim 1. These compounds can be used for the preparation of medicaments.
    Type: Grant
    Filed: January 13, 2006
    Date of Patent: January 29, 2008
    Assignees: Hoffman-La Roche Inc., Vernalis Research Limited
    Inventors: Jonathan Mark Bentley, Claire Elizabeth Dawson, Wolfgang Guba, Paul Hebeisen, Nathaniel Monck, Robert Mark Pratt, Hans Richter, Stephan Roever, Vicki Ruston
  • Patent number: 7253197
    Abstract: Compounds of formula I as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R4 have the significance given in the specification, and the compounds, salts and esters can be used for the treatment of obesity.
    Type: Grant
    Filed: August 5, 2003
    Date of Patent: August 7, 2007
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Wolfgang Guba, Patrizio Mattei, Werner Neidhart, Matthias Heinrich Nettekoven, Philippe Pflieger
  • Publication number: 20070093521
    Abstract: This invention is concerned with compounds of the formula wherein X, A, B, R1, R2 and G are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.
    Type: Application
    Filed: August 31, 2006
    Publication date: April 26, 2007
    Inventors: Alfred Binggeli, Andreas Christ, Luke Granville Green, Wolfgang Guba, Hans-Peter Maerki, Rainer Martin, Peter Mohr