Patents by Inventor Roland Jakob-Roetne

Roland Jakob-Roetne 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).

  • Pyrazoles
    Patent number: 8163728
    Abstract: The present invention is concerned with isoxazole-pyrazoles of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutics. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.
    Type: Grant
    Filed: April 28, 2010
    Date of Patent: April 24, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
  • Isoxazolo-pyridazine derivatives
    Patent number: 7943619
    Abstract: The invention relates to isoxazolo-pyridazine compounds, in particular those of formula I as described above and to a pharmaceutically acceptable salts thereof, having affinity and selectivity for the GABA A ?5 receptor binding site, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers or for the treatment of cognitive disorders like Alzheimer's disease.
    Type: Grant
    Filed: November 25, 2008
    Date of Patent: May 17, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Andrew Thomas
  • Isoxazolo-pyrazine derivatives
    Patent number: 7902201
    Abstract: The invention relates to isoxazolo-pyrazine derivatives and their pharmaceutically acceptable salts having affinity and selectivity for the GABA A ?5 receptor binding site, their manufacture, and pharmaceutical compositions containing them. The compounds of the present invention are inverse agonists of GABAA?5. The invention also relates to methods for enhancing cognition and for treating cognitive disorders like Alzheimer's disease.
    Type: Grant
    Filed: May 27, 2010
    Date of Patent: March 8, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Andrew Thomas
  • Isoxazole-imidazole derivatives
    Patent number: 7851469
    Abstract: The present invention is concerned isoxazole-imidazole derivatives having affinity and selectivity for GABA A ?5 receptor binding site, their manufacture, pharmaceutical compositions containing them and their use for enhancing cognition or for the treatment of cognitive disorders like Alzheimer's disease. In particular, the present invention is concerned with aryl-isoxazol-4-yl-imidazole derivatives of formula I wherein R1, R2 and R3 are as described in the specification.
    Type: Grant
    Filed: June 16, 2008
    Date of Patent: December 14, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Andrew Thomas
  • THIAZOLES
    Publication number: 20100286116
    Abstract: The present invention is concerned with isoxazole-thiazole derivatives of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.
    Type: Application
    Filed: April 28, 2010
    Publication date: November 11, 2010
    Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
  • PYRIDINES
    Publication number: 20100286117
    Abstract: The present invention is concerned with novel isoxazoles of formula I wherein X, R1, R2, R3 and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as therapeutics.
    Type: Application
    Filed: May 3, 2010
    Publication date: November 11, 2010
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
  • PYRAZOLES
    Publication number: 20100286115
    Abstract: The present invention is concerned with isoxazole-pyrazoles of formula I, having affinity and selectivity for GABA A a5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutics. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.
    Type: Application
    Filed: April 28, 2010
    Publication date: November 11, 2010
    Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
  • PYRIDINES
    Publication number: 20100286132
    Abstract: The present invention is concerned with isoxazole-pyridines of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as pharmaceuticals. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.
    Type: Application
    Filed: April 28, 2010
    Publication date: November 11, 2010
    Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
  • ISOXAZOLES
    Publication number: 20100280020
    Abstract: The present invention is concerned with novel isoxazole derivatives of formula I wherein X, R1, R2, R3, R4 and R5 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Application
    Filed: April 23, 2010
    Publication date: November 4, 2010
    Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
  • ISOXAZOLES
    Publication number: 20100280019
    Abstract: The present invention is concerned with novel isoxazole derivatives of formula I wherein X, R1, R2, R3, R4 and R5 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Application
    Filed: April 23, 2010
    Publication date: November 4, 2010
    Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
  • SUBSTITUTED ISOXAZOLES
    Publication number: 20100256127
    Abstract: The present invention is concerned with novel hydroxy-methyl isoxazole derivatives of formula I wherein R1, R2 and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as pharmaceuticals.
    Type: Application
    Filed: March 29, 2010
    Publication date: October 7, 2010
    Inventors: Bernd Buettelmann, Stephen Deems Gabriel, Steven Paul Hanlon, Roland Jakob-Roetne, Matthew C. Lucas, Paul Spurr, Andrew Thomas, Pius Waldmeier
  • ISOXAZOLO-PYRAZINE DERIVATIVES
    Publication number: 20100256154
    Abstract: The invention relates to isoxazolo-pyrazine derivatives and their pharmaceutically acceptable salts having affinity and selectivity for the GABA A ?5 receptor binding site, their manufacture, and pharmaceutical compositions containing them. The invention also relates to methods for enhancing cognition and for treating cognitive disorders like Alzheimer's disease.
    Type: Application
    Filed: May 27, 2010
    Publication date: October 7, 2010
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Andrew Thomas
  • ISOXAZOLE-ISOXAZOLES AND ISOXAZOLE-ISOTHIAZOLES
    Publication number: 20100210651
    Abstract: The present invention is concerned with isoxazole-isoxazoles and isoxazole-isothiazoles of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.
    Type: Application
    Filed: February 12, 2010
    Publication date: August 19, 2010
    Inventors: Maria-Clemencia Hernandez, Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
  • SPIRO-5,6-DIHYDRO-4H-2,3,5,10B-TETRAAZA-BENZO[E]AZULENES
    Publication number: 20100120751
    Abstract: The present invention is concerned with spiro-dihydrotetraazabenzoazulenes, i.e. spiro-5,6-dihydro-4H-2,3,5,10b-tetraaza-benzo[e]azulenes of formula I wherein R1, R2, R3, X, Y, Z, m and n are as described herein. The compounds according to the invention act as V1a receptor modulators and are useful as therapeutics acting peripherally and centrally in the conditions of dysmenorrhea, male or female sexual dysfunction, hypertension, chronic heart failure, inappropriate secretion of vasopressin, liver cirrhosis, nephrotic syndrome, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, and aggressive behavior.
    Type: Application
    Filed: November 6, 2009
    Publication date: May 13, 2010
    Inventors: Caterina Bissantz, Erwin Goetschi, Roland Jakob-Roetne, Raffaello Masciadri, Emmanuel Pinard, Hasane Ratni, Mark Rogers-Evans, Patrick Schnider
  • ISOXAZOLO-PYRAZINE DERIVATIVES
    Publication number: 20100041886
    Abstract: The invention relates to isoxazolo-pyrazine derivatives and their pharmaceutically acceptable salts having affinity and selectivity for the GABA A ?5 receptor binding site, their manufacture, and pharmaceutical compositions containing them. The compounds of present invention are inverse agonists of GABA A ?5. The invention also relates to methods for enhancing cognition and for treating cognitive disorders like Alzheimer's disease.
    Type: Application
    Filed: October 19, 2009
    Publication date: February 18, 2010
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Andrew Thomas
  • Isoxazolo-pyrazine derivatives
    Patent number: 7618973
    Abstract: The invention relates to isoxazolo-pyrazine derivatives and their pharmaceutically acceptable salts having affinity and selectivity for the GABA A ?5 receptor binding site, their manufacture, and pharmaceutical compositions containing them. The compounds of present invention are inverse agonists of GABA A ?5. The invention also relates to methods for enhancing cognition and for treating cognitive disorders like Alzheimer's disease.
    Type: Grant
    Filed: November 25, 2008
    Date of Patent: November 17, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Andrew Thomas
  • Process for preparation of enantiomerically pure compounds
    Patent number: 7579464
    Abstract: The invention relates to a process for the optical resolution of a dibenzo[b,d]azepinone derivative of formula II, wherein R1 is hydrogen or halogen and R2 is either C1-4-alkyl optionally substituted with C3-7-cycloalkyl or benzyl which is optionally substituted with C1-4-alkoxy, to obtain a (S)-7-amino-5H,7H-dibenzo[b,d]azepin-6-one of formula I, wherein R1 is as in the compound of formula II. The (S)-7-amino-5H,7H-dibenzo[b,d]azepin-6-one of formula I can be used as a chiral building block for the preparation of malonamide derivatives which have the potential to act as ?-secretase inhibitors and therefore may be useful in the treatment of Alzheimer's disease and cancer.
    Type: Grant
    Filed: April 28, 2008
    Date of Patent: August 25, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Fabienne Hoffmann-Emery, Roland Jakob-Roetne
  • 6-oxo-6,7-dihydro-5h-dibenzo[b,d]azepin-7-yl derivatives
    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
  • ISOXAZOLO-PYRAZINE DERIVATIVES
    Publication number: 20090143407
    Abstract: The invention relates to isoxazolo-pyrazine derivatives and their pharmaceutically acceptable salts having affinity and selectivity for the GABA A ?5 receptor binding site, their manufacture, and pharmaceutical compositions containing them. The compounds of present invention are inverse agonists of GABA A ?5. The invention also relates to methods for enhancing cognition and for treating cognitive disorders like Alzheimer's disease.
    Type: Application
    Filed: November 25, 2008
    Publication date: June 4, 2009
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Andrew Thomas
  • ISOXAZOLO-PYRIDAZINE DERIVATIVES
    Publication number: 20090143385
    Abstract: The invention relates to isoxazolo-pyridazine compounds, in particular those of formula I as described above and to a pharmaceutically acceptable salts thereof, having affinity and selectivity for the GABA A ?5 receptor binding site, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers or for the treatment of cognitive disorders like Alzheimer's disease.
    Type: Application
    Filed: November 25, 2008
    Publication date: June 4, 2009
    Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Andrew Thomas