Patents by Inventor Sabine Kolczewski

Sabine Kolczewski 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).

  • Patent number: 8188284
    Abstract: The present invention relates to compounds of formula (I) wherein A, R1, R2, R3, R4, and R5 are as described herein, pharmaceutical compositions containing them, and methods for their manufacture. These compounds are 5-HT5A receptor antagonists and are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: May 29, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Sabine Kolczewski, Claus Riemer, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
  • Patent number: 8183380
    Abstract: The present invention is concerned with 2-aminoquinoline derivatives of formula I where R1, R2, R3, R4, R5, R6, A, and n are as defined in the specification and claims, their use 5-HT5A receptor antagonists, their manufacture, and pharmaceutical compositions containing them.
    Type: Grant
    Filed: February 26, 2009
    Date of Patent: May 22, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Sabine Kolczewski, Claus Riemer, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
  • Patent number: 8163740
    Abstract: The present invention is concerned with 6-substituted benzoxazine derivatives of formula (I) wherein X, Y, R1 and R2 are as described herein, their manufacture, and pharmaceutical compositions containing them. The active compounds of the present invention are 5-HT5A receptor antagonists, useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders, Parkinson's disease, psychiatric disorders or gastrointestinal disorders.
    Type: Grant
    Filed: August 28, 2009
    Date of Patent: April 24, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Sabine Kolczewski, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
  • Patent number: 8153653
    Abstract: The present invention relates to a compound of formula I wherein R1, R2 and R3 are each independently hydrogen, lower alkyl, lower alkoxy, cycloalkyl, lower alkyl substituted by halogen or S-lower alkyl; or to a pharmaceutically acceptable acid addition salt, racemic mixture, or corresponding enantiomer and/or optical isomer thereof. The compounds of formula I are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors. The compounds can be used in the treatment of neurological and neuropsychiatric disorders.
    Type: Grant
    Filed: June 15, 2011
    Date of Patent: April 10, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Patent number: 8143273
    Abstract: The present invention relates to a compound of formula I-A or I-B wherein X, R1, R2 and R3 are defined herein; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. The compounds of formulas I-A and I-B are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors, suitable in the treatment of neurological and neuropsychiatric disorders.
    Type: Grant
    Filed: June 16, 2011
    Date of Patent: March 27, 2012
    Assignee: Hoffman-La Roche Inc.
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Publication number: 20120022042
    Abstract: The present invention relates to the use of a compound of formula I wherein R1, R2, R3, R4, X and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.
    Type: Application
    Filed: September 30, 2011
    Publication date: January 26, 2012
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Publication number: 20110312993
    Abstract: The present invention relates to a compound of formula I wherein R1, R2 and R3 are each independently hydrogen, lower alkyl, lower alkoxy, cycloalkyl, lower alkyl substituted by halogen or S-lower alkyl; or to a pharmaceutically acceptable acid addition salt, racemic mixture, or corresponding enantiomer and/or optical isomer thereof. The compounds of formula I are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors. The compounds can be used in the treatment of neurological and neuropsychiatric disorders.
    Type: Application
    Filed: June 15, 2011
    Publication date: December 22, 2011
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Publication number: 20110313165
    Abstract: The present invention relates to a compound of formula I-A or I-B wherein X, R1, R2 and R3 are defined herein; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer thereof. The compounds of formulas I-A and I-B are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors, suitable in the treatment of neurological and neuropsychiatric disorders.
    Type: Application
    Filed: June 16, 2011
    Publication date: December 22, 2011
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Patent number: 8080541
    Abstract: The present invention relates to the use of a compound of formula I wherein R1, R2, R3, R4, X and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.
    Type: Grant
    Filed: August 19, 2010
    Date of Patent: December 20, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Patent number: 8063098
    Abstract: The present invention relates to a compound of formula I wherein R1, R2, X, Ar1 and Ar2 are as defined herein and to pharmaceutically acceptable acid addition salts, to a racemic mixtures, or to their corresponding enantiomers and/or optical isomers thereof. Compounds of the invention are good inhibitors of the glycine transporter 1 (GlyT-1), and have a good selectivity to glycine transporter 2 (GlyT-2) inhibitors.
    Type: Grant
    Filed: August 14, 2009
    Date of Patent: November 22, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Sabine Kolczewski, Robert Narquizian, Emmanuel Pinard
  • Patent number: 8044047
    Abstract: The present invention is concerned with 5-substituted benzoxazine derivatives of formula (I) wherein X, R1 and R2 are as described herein, as well as their manufacture, pharmaceutical compositions containing them. Compounds of the present invention are 5-HT5A receptor antagonists, and are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.
    Type: Grant
    Filed: August 28, 2009
    Date of Patent: October 25, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Sabine Kolczewski, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
  • Patent number: 7994324
    Abstract: The present invention is concerned with 2-aminoquinoline derivatives, in particular compounds of formula (I) wherein R1 and R2 are as described herein, pharmaceutical compositions containing such compounds, and methods for their manufacture. The compounds of the invention are 5-HT5A receptor antagonists useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: August 9, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Sabine Kolczewski, Claus Riemer, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
  • Publication number: 20110190349
    Abstract: The present invention relates to a compound of formula I wherein R1/R2 are independently from each other hydrogen, (CR2)o-cycloalkyl, optionally substituted by lower alkyl or hydroxy, or are lower alkyl or heterocycloalkyl, and o is 0 or 1; and R may be the same or different and is hydrogen or lower alkyl; or R1 and R2 may form together with the N atom to which they are attached a heterocycloalkyl group, selected from the group consisting of pyrrolidinyl, piperidinyl, 3-aza-bicyclo[3.1.0]hex-3-yl or 2-aza-bicyclo[3.1.
    Type: Application
    Filed: January 21, 2011
    Publication date: August 4, 2011
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Patent number: 7989628
    Abstract: The present invention is concerned with 2-aminoquinoline derivatives of formula I wherein Z, R1, and Ar1 are as defined herein, pharmaceutical compositions containing them, methods for their manufacture. The compounds are 5-HT5A receptor antagonists and are useful in the prevention and/or treatment of depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders or gastrointestinal disorders.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: August 2, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Sabine Kolczewski, Claus Riemer, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
  • Patent number: 7973165
    Abstract: The present invention relates to process for the preparation of an imidazole derivative of formula I, wherein R1, R2, R3 and R4 are described hereinabove. These compounds can be used in the treatment or prevention of mGluR5 receptor mediated disorders. These compounds are useful, inter alia, in the treatment or prevention of acute and/or chronic neurological disorders such as psychosis, epilepsy, schizophrenia, Alzheimer' disease, cognitive disorders and memory deficits, as well as chronic and acute pain.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: July 5, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
  • Patent number: 7964620
    Abstract: The present invention relates to imidazole derivatives of formula I wherein R1, R2, R3, R4, X, Y and R are described hereinabove, or a pharmaceutically acceptable salt thereof. The invention also relates to a pharmaceutical composition comprising the imidazole derivatives of formula I, a process for preparing a compound of formula I, and a method of treating or preventing acute and/or chronic neurological disorder comprising administering to a patient in need of such treatment and/or prevention a therapeutically effective amount of said pharmaceutical composition. These disorders include Alzheimer's disease. These disorders also include mild cognitive impairment.
    Type: Grant
    Filed: September 17, 2008
    Date of Patent: June 21, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
  • Patent number: 7947685
    Abstract: The present invention is concerned with novel pyrazine 2-carboxyamide derivatives of formula (I) wherein R1, R2 and R3 are as defined in the specification. These compounds are useful for the treatment of CNS disorders.
    Type: Grant
    Filed: May 22, 2009
    Date of Patent: May 24, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
  • Patent number: 7923561
    Abstract: The present invention relates to 2-Aminoquinoline derivatives of general formula I and pharmaceutically-acceptable acid-addition salts thereof, wherein R1, R2 and X are as defined in the specification. The compounds may be used as 5-HT5A receptor antagonists. The present invention relates also to processes for making such a compound and a pharmaceutical composition comprising such a compound. Compounds of the present invention are useful in the prevention and/or treatment of anxiety depression, anxiety disorders, schizophrenia, panic disorders, agoraphobia, social phobia, obsessive compulsive disorders, post-traumatic stress disorders, pain, memory disorders, dementia, disorders of eating behaviors, sexual dysfunction, sleep disorders, withdrawal from abuse of drugs, motor disorders such as Parkinson's disease, psychiatric disorders and gastrointestinal disorders.
    Type: Grant
    Filed: November 29, 2007
    Date of Patent: April 12, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Sabine Kolczewski, Claus Riemer, Lucinda Steward, Juergen Wichmann, Thomas Woltering
  • Publication number: 20110053904
    Abstract: The present invention relates to the use of a compound of formula I wherein R1, R2, R3, R4, X and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.
    Type: Application
    Filed: August 19, 2010
    Publication date: March 3, 2011
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Patent number: 7875645
    Abstract: The present invention relates a method for treating depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders which comprises administering to an individual a therapeutically effective amount of a compound of formula I wherein R, R1, R2, A and n are as defined in the specification and to their pharmaceutically active salts. The invention also relates to novel compounds of formula I, pharmaceutical compositions containing them, and methods for their preparation.
    Type: Grant
    Filed: January 19, 2007
    Date of Patent: January 25, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Guido Galley, Katrin Groebke Zbinden, Marius Hoener, Sabine Kolczewski, Roger Norcross, Henri Stalder