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).
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Publication number: 20180251450Abstract: The present invention is concerned with indolin-2-one derivatives of general formula wherein the substituents are defined in claim 1. The compounds may be used in the treatment of CNS diseases related to positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, neurodegenerative disease, sleep disturbances, chronic fatigue syndrome, stiffness, inflammatory disease, asthma, Huntington's disease, ADHD, amyotrophic lateral sclerosis, effects in arthritis, autoimmune disease, viral and fungal infections, cardiovascular diseases, ophthalmology and inflammatory retinal diseases and balance problems, epilepsy and neurodevelopmental disorders with co-morbid epilepsy.Type: ApplicationFiled: May 4, 2018Publication date: September 6, 2018Applicant: Hoffmann-La Roche Inc.Inventors: Delphine Gaufreteau, Sabine Kolczewski, Jean-Marc Plancher, Theodor Stoll
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Publication number: 20180251449Abstract: The present invention is concerned with indolin-2-one derivatives of general formula wherein the substituents are defined in claim 1. The compounds may be used in the treatment of CNS diseases related to positive (psychosis) and negative symptoms of schizophrenia, substance abuse, alcohol and drug addiction, obsessive-compulsive disorders, cognitive impairment, bipolar disorders, mood disorders, major depression, treatment resistant depression, anxiety disorders, Alzheimer's disease, autism, Parkinson's disease, chronic pain, borderline personality disorder, neurodegenerative disease, sleep disturbances, chronic fatigue syndrome, stiffness, inflammatory disease, asthma, Huntington's disease, ADHD, amyotrophic lateral sclerosis, effects in arthritis, autoimmune disease, viral and fungal infections, cardiovascular diseases, ophthalmology and inflammatory retinal diseases and balance problems, epilepsy and neurodevelopmental disorders with co-morbid epilepsy.Type: ApplicationFiled: May 4, 2018Publication date: September 6, 2018Applicant: Hoffmann-La Roche Inc.Inventors: Delphine Gaufreteau, Sabine Kolczewski, Jean-Marc Plancher, Theodor Stoll, Remy Halm
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Patent number: 10030047Abstract: The present invention provides compounds of formula (I) wherein X1 to X8 and R1 to R8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.Type: GrantFiled: October 27, 2016Date of Patent: July 24, 2018Assignee: HOFFMANN-LA ROCHE INC.Inventors: Alexander Alanine, Julien Beignet, Konrad Bleicher, Bernhard Fasching, Hans Hilpert, Taishan Hu, Dwight MacDonald, Stephen Jackson, Sabine Kolczewski, Carsten Kroll, Adrian Schaeublin, Hong Shen, Theodor Stoll, Helmut Thomas, Amal Wahhab, Claudia Zampaloni
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Publication number: 20170233437Abstract: The present invention provides compounds of formula (I) wherein X1 to X8 and R1 to R8 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments for the treatment of diseases and infections caused by Acinetobacter baumannii.Type: ApplicationFiled: October 27, 2016Publication date: August 17, 2017Applicant: Hoffmann-La Roche Inc.Inventors: Alexander Alanine, Julien Beignet, Konrad Bleicher, Bernhard Fasching, Hans Hilpert, Taishan Hu, Dwight MacDonald, Stephen Jackson, Sabine Kolczewski, Carsten Kroll, Adrian Schaeublin, Hong Shen, Theodor Stoll, Helmut Thomas, Amal Wahhab, Claudia Zampaloni
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Publication number: 20170101409Abstract: The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula wherein Ar1 is phenyl or a five or six membered heteroaryl group, containing one, two or three heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+—(O?); R1 is lower alkyl, halogen, cyano or cycloalkyl; Ar2 is a five or six membered heteroaryl group, containing one, two, three or four heteroatoms, selected from N, S or O, wherein the N-heteroatom in the heteroaryl group may be oxidized to N+—(O?), or is benzo[b]thiophenyl; R2 is hydrogen, lower alkyl, halogen, cyano, lower alkyl substituted by hydroxyl, lower alkyl substituted by halogen, lower alkyl substituted by amino, lower alkyl substituted by alkoxy, lower alkyl substituted by amide, or is cycloalkyl; X is CH or N; n is 1 or 2; m is 1 or 2; as well as with a pharmaceutically acceptable salt thereof, with a racemic mixture, or with its corresponding enantiomer and/or optical isomer and/or stereoisomer thereofType: ApplicationFiled: December 22, 2016Publication date: April 13, 2017Applicant: Hoffmann-La Roche Inc.Inventors: Hans Hilpert, Sabine Kolczewski, Roland Humm, Theodor Stoll, Thorsten Muser, Jean-Marc Plancher, Delphine Gaufreteau
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Patent number: 9616053Abstract: The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula (I) wherein Ar, X, X1, R1, R2, R3, m, n and the dotted line are as defined herein which compounds are useful for treating certain central nervous system disorders as described herein.Type: GrantFiled: December 16, 2015Date of Patent: April 11, 2017Assignee: Hoffmann-La Roche Inc.Inventors: Daniela Brunner, Hans Hilpert, Sabine Kolczewski, Anja Limberg, Jessica Malberg, Eric Prinssen, Claus Riemer, Bavani G. Shankar, Theodor Stoll
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Publication number: 20170057960Abstract: The present invention is concerned with indolin-2-one and 1,3-dihydro-pyrrolo[3,2-c]pyridin-2-one derivatives of general formula I wherein Ar1, A2, R1, R2, R3, X and n are as described herein and pharmaceutically acceptable salts thereof for treatment of central nervous system disordersType: ApplicationFiled: November 16, 2016Publication date: March 2, 2017Applicant: Hoffmann-La Roche Inc.Inventors: Hans Hilpert, Sabine Kolczewski, Anja Limberg, Theodor Stoll
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Publication number: 20160095844Abstract: The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula wherein Ar is a 6-membered heteroaryl group, containing one or two N-atoms, which are the groups, pyridinyl, pyrimidinyl, pyridazinyl, or a 5-membered heteroaryl group containing from 1 to 3 heteroatoms, selected from N, S or O, which groups are imidazolyl, 1,2,4-oxadiazolyl, 1,3,4-oxadazolyl, isoxazolyl, oxazolyl, 1,3,4-thiadiazolyl or pyrazolyl; R1 is hydrogen, lower alkyl, halogen, amino, dimethylamino, cyano, lower alkyl substituted by halogen, lower alkyl substituted by hydroxy, CH(OH)CF3, (CH2)o-lower alkoxy, cycloalkyl optionally substituted by CF3, or heterocycloalkyl optionally substituted by lower alkyl; R2 is hydrogen, lower alkyl, (CH2)o-cycloalkyl, (CH2)o—O-cycloalkyl, (CH2)o-lower alkoxy, CH2)o-lower alkoxy substituted by halogen, (CH2)o-heterocycloalkyl optionally substituted by lower alkyl, (CH2)o—S(O)2-cycloalkyl, lower alkyl substituted by one or two hydroxy, lower alkyl substituted by one or two loType: ApplicationFiled: December 16, 2015Publication date: April 7, 2016Applicant: Hoffmann-La Roche Inc.Inventors: Daniela Brunner, Hans Hilpert, Sabine Kolczewski, Anja Limberg, Jessica Malberg, Eric Prinssen, Claus Riemer, Bavani G. Shankar, Theodor Stoll
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Patent number: 9221816Abstract: The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula wherein is phenyl or a heteroaryl group, selected from pyridinyl, pyrimidinyl, imidazolyl, isoxazolyl or pyrazolyl; is phenyl or pyridinyl, wherein the N atom in the pyridinyl group may be on all free positions; R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy or halogen; n is 1 or 2; if n is 2, R1 may be the same or not; R2/R2? are independently from each other lower alkyl, or form together with the carbon atom to which they are attached a C3-6-cycloalkyl ring; R3 is lower alkyl, C3-6-cycloalkyl, CH2—C3-6-cycloalkyl, C3-6-cycloalkyl wherein one ring-carbon atom is replaced by —O—, (CH2)3—O—C3-6-cycloalkyl, lower alkyl substituted by hydroxy, lower alkyl substituted by halogen, (CH2)3—S(O)2—C3-6-cycloalkyl or (CH2)2—S(O)2-lower alkyl; R4 is hydrogen, halogen or lower alkyl; m is 1 or 2; if m is 2, R4 may be the same or not; as well as with a pharmaceutically acceptable salts thType: GrantFiled: March 11, 2015Date of Patent: December 29, 2015Assignee: Hoffmann La-Roche Inc.Inventors: Daniela Brunner, Jessica Malberg, Bavani G. Shankar, Sabine Kolczewski, Anja Limberg, Eric Prinssen, Claus Riemer, Theodor Stoll
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Publication number: 20150284386Abstract: The present invention is concerned with 2-oxo-2,3-dihydro-indoles of general formula wherein is phenyl or a heteroaryl group, selected from pyridinyl, pyrimidinyl, imidazolyl, isoxazolyl or pyrazolyl; is phenyl or pyridinyl, wherein the N atom in the pyridinyl group may be on all free positions; R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen, lower alkoxy or halogen; n is 1 or 2; if n is 2, R1 may be the same or not; R2/R2? are independently from each other lower alkyl, or form together with the carbon atom to which they are attached a C3-6-cycloalkyl ring; R3 is lower alkyl, C3-6-cycloalkyl, CH2—C3-6-cycloalkyl, C3-6-cycloalkyl wherein one ring-carbon atom is replaced by —O—, (CH2)3—O—C3-6-cycloalkyl, lower alkyl substituted by hydroxy, lower alkyl substituted by halogen, (CH2)3—S(O)2—C3-6-cycloalkyl or (CH2)2—S(O)2-lower alkyl; R4 is hydrogen, halogen or lower alkyl; m is 1 or 2; if m is 2, R4 may be the same or not; as well as with a pharmaceutically acceptable salts therType: ApplicationFiled: March 11, 2015Publication date: October 8, 2015Applicant: Hoffmann-La Roche Inc.Inventors: Daniela Brunner, Jessica Malberg, Bavani G. Shankar, Sabine Kolczewski, Anja Limberg, Eric Prinssen, Claus Riemer, Theodor Stoll
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Patent number: 9067911Abstract: The present invention relates to a compound of formula I wherein R1, R2, and Ar 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 thereof. These compounds and their pharmaceutical compositions are useful in the treatment of neurological and neuropsychiatric disorders.Type: GrantFiled: February 14, 2013Date of Patent: June 30, 2015Assignee: Hoffmann-La Roche Inc.Inventors: Sabine Kolczewski, Emmanuel Pinard, Henri Stalder
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Patent number: 8524909Abstract: 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: GrantFiled: January 21, 2011Date of Patent: September 3, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Sabine Kolczewski, Emmanuel Pinard
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Patent number: 8481548Abstract: The present invention relates to imidazole derivatives 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, cognititve disorders and memory deficits, as well as chronic and acute pain.Type: GrantFiled: October 31, 2007Date of Patent: July 9, 2013Assignee: Hoffman-La Roche Inc.Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
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Patent number: 8404673Abstract: 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: GrantFiled: September 30, 2011Date of Patent: March 26, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Sabine Kolczewski, Emmanuel Pinard
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Patent number: 8399674Abstract: The present invention relates to 2-aminoquinolines of formula I wherein R1, R2 and R3 are as defined in the specification, as 5-HT5A receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of CNS disorders.Type: GrantFiled: January 27, 2012Date of Patent: March 19, 2013Assignee: Hoffman-La Roche Inc.Inventors: Sabine Kolczewski, Claus Riemer, Lucinda Steward, Juergen Wichmann, Thomas Woltering
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Patent number: 8367838Abstract: The invention relates to the use of compounds of formula I wherein the substituents are described in the description and claims for the treatment of psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders or Alzheimer's disease. The invention also relates to some compounds of formula I and pharmaceutical compositions containing them.Type: GrantFiled: May 25, 2012Date of Patent: February 5, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Sabine Kolczewski, Hans-Peter Marty, Robert Narquizian, Emmanuel Pinard, Henri Stalder
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Patent number: 8350028Abstract: The present invention is concerned with 2-aminoquinoline derivatives of formula I wherein R1 and R2 are as described herein and pharmaceutically acceptable salts thereof, pharmaceutical compositions containing them, and methods for their manufacture. These compounds are 5-HT5A receptor antagonists, useful for 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: GrantFiled: March 5, 2009Date of Patent: January 8, 2013Assignee: Hofmann-La Roche Inc.Inventors: Sabine Kolczewski, Claus Riemer, Olivier Roche, Lucinda Steward, Juergen Wichmann, Thomas Woltering
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Patent number: 8293916Abstract: The present invention relates to diazole derivatives of the general formula wherein A, E, R1, R2 and R3 are as defined in application and pharmaceutical compositions containing them. The invention also relates to use of such compounds for the treatment of diseases mediated by the metabotropic glutamate receptors (mGluR), such as anxiety, chronic and acute pain, protection against liver damage, urinary incontinence, obesity, Fragile-X and autism, Alzheimer's disease, epilepsy, schizophrenia, ischemia, Huntington's chorea, amyotrophic lateral sclerosis (ALS), dementia caused by AIDs, and Parkinson's disease.Type: GrantFiled: November 5, 2009Date of Patent: October 23, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Paul Spurr, Eric Vieira
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Publication number: 20120232033Abstract: The invention relates to the use of compounds of formula I wherein the substituents are described in the description and claims for the treatment of psychoses, dysfunction in memory and learning, schizophrenia, dementia, attention deficit disorders or Alzheimer's disease. The invention also relates to some compounds of formula I and pharmaceutical compositions containing them.Type: ApplicationFiled: May 25, 2012Publication date: September 13, 2012Inventors: Sabine Kolczewski, Hans-Peter Marty, Robert Narquizian, Emmanuel Pinnard, Henri Stalder
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Publication number: 20120136018Abstract: The present invention relates to 2-aminoquinolines of formula I wherein R1, R2 and R3 are as defined in the specification, as 5-HT5A receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use for the treatment of CNS disorders.Type: ApplicationFiled: January 27, 2012Publication date: May 31, 2012Inventors: Sabine Kolczewski, Claus Riemer, Lucinda Steward, Juergen Wichmann, Thomas Woltering