Patents by Inventor Wolfgang Wostl

Wolfgang Wostl 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: 20120196863
    Abstract: The present invention provides 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 25, 2012
    Publication date: August 2, 2012
    Inventors: Matteo Andreini, Emanuele Gabellieri, Robert Narquizian, Massimiliano Travagli, Wolfgang Wostl
  • Patent number: 8227505
    Abstract: The invention relates to a method for preparing enantiomerically pure 4-pyrrolidinophenylbenzyl ether derivatives of formula I: wherein R1, R21, R22, R23, R24 and n are as defined in the description and claims and to intermediates useful in the method of the invention as well as salts thereof.
    Type: Grant
    Filed: January 26, 2009
    Date of Patent: July 24, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Stefan Hildbrand, Bruno Lohri, 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
  • 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: 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: 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
  • 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
  • Publication number: 20090171100
    Abstract: The invention relates to a method for preparing enantiomerically pure 4-pyrrolidinophenylbenzyl ether derivatives of formula I: wherein R1, R21, R22, R23, R24 and n are as defined in the description and claims and to intermediates useful in the method of the invention as well as salts thereof.
    Type: Application
    Filed: January 26, 2009
    Publication date: July 2, 2009
    Inventors: Stefan Hildbrand, Bruno Lohri, Wolfgang Wostl
  • Patent number: 7544679
    Abstract: The invention relates to 6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl derivatives of formula I wherein R1, R2 and R3 are as defined herein. The compounds are ?-secretase inhibitors useful in the treatment of Alzheimer's disease or common cancer, including, but not limited to, cervical carcinomas and breast carcinomas and malignancies of the hematopoietic system.
    Type: Grant
    Filed: January 25, 2008
    Date of Patent: June 9, 2009
    Assignee: Hoffman-La Roche Inc.
    Inventors: Alexander Flohr, Roland Jakob-Roetne, Wolfgang Wostl
  • Patent number: 7501406
    Abstract: The invention relates to compounds of general formula wherein R1, R2, R3/R3?, R4/R4? and R5/R5? are as defined in the specification and to pharmaceutically acceptable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. The compounds are ?-secretase inhibitors which can be useful in the treatment of Alzheimer's disease or common cancers including, but not limited to, cervical carcinomas and breast carcinomas and malignancies of the hematopoietic system.
    Type: Grant
    Filed: August 8, 2006
    Date of Patent: March 10, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Flohr, Guido Galley, Roland Jakob-Roetne, Eric Argirios Kitas, Wolfgang Wostl
  • Patent number: 7501528
    Abstract: The invention relates to a method for preparing enantiomerically pure 4-pyrrolidinophenylbenzyl ether derivatives of formula I: wherein R1, R21, R22, R23, R24 and n are as defined in the description and claims and to intermediates useful in the method of the invention as well as salts thereof.
    Type: Grant
    Filed: March 8, 2006
    Date of Patent: March 10, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Stefan Hildbrand, Bruno Lohri, Wolfgang Wostl
  • Patent number: 7456210
    Abstract: The present invention relates to compounds of formula I wherein R1 and R2 are as defined in the specification and to pharmaceutically acceptable salts thereof for the treatment of diseases, which are mediated by monoamine oxidase B inhibitors, for example Alzheimer's disease and senile dementia.
    Type: Grant
    Filed: July 27, 2005
    Date of Patent: November 25, 2008
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Rosa Maria Rodriguez-Sarmiento, Wolfgang Wostl, Rene Wyler
  • Patent number: 7425551
    Abstract: The invention relates to malonamide derivatives of formula wherein A1, A2, R1, R2, R3, and R4 are as defined herein and to pharmaceutically acceptable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof for the treatment of Alzheimer's disease.
    Type: Grant
    Filed: March 22, 2007
    Date of Patent: September 16, 2008
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Flohr, Roland Jakob-Roetne, Wolfgang Wostl
  • Patent number: 7414049
    Abstract: The invention relates to 4-oxo-2,3,4,5-tetrahydro-benzo [b][1,4]diazepines of formula I wherein R1, R2, R3 and R4 are as defined in the description and claims, which are ?-secretase inhibitors and which may be useful in the treatment of Alzheimer's disease.
    Type: Grant
    Filed: September 14, 2007
    Date of Patent: August 19, 2008
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Alexander Flohr, Roland Jakob-Roetne, Wolfgang Wostl
  • Publication number: 20080188463
    Abstract: The invention relates to 6-oxo-6,7-dihydro-5H-dibenzo[b,d]azepin-7-yl derivatives of formula I wherein R1, R2 and R3 are as defined herein. The compounds are ?-secretase inhibitors useful in the treatment of Alzheimer's disease or common cancer, including, but not limited to, cervical carcinomas and breast carcinomas and malignancies of the hematopoietic system.
    Type: Application
    Filed: January 25, 2008
    Publication date: August 7, 2008
    Inventors: Alexander Flohr, Roland Jakob-Roetne, Wolfgang Wostl