Patents by Inventor Delphine Gaufreteau

Delphine Gaufreteau 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: 20240018163
    Abstract: The invention relates to a compound of formula (I) wherein R1—R4 and A1-A3 are as defined in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Application
    Filed: September 15, 2023
    Publication date: January 18, 2024
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Virginie BROM, Cosimo DOLENTE, Delphine GAUFRETEAU, Nadine GRETHER, Fionn Susannah O'HARA, Matilde PIRAS, Hasane RATNI, Michael REUTLINGER, Walter VIFIAN, Claudio ZAMBALDO
  • Publication number: 20230391778
    Abstract: 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 thereof
    Type: Application
    Filed: August 17, 2023
    Publication date: December 7, 2023
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Hans HILPERT, Sabine KOLCZEWSKI, Roland HUMM, Theodor STOLL, Thorsten MUSER, Jean-Marc PLANCHER, Delphine GAUFRETEAU
  • Publication number: 20230024096
    Abstract: The invention provides bifunctional compounds of formula (I) or a pharmaceutically acceptable salt thereof. Formula (I). The compounds cause the degradation of SMARCA2 via the targeted ubiquination of SMARCA2 protein and subsequent proteasomal degradation and are thus useful for the treatment of cancer. The targeting ligand is of formula (TL).
    Type: Application
    Filed: October 28, 2020
    Publication date: January 26, 2023
    Inventors: Martin DUPLESSIS, Delphine GAUFRETEAU, Roman HUTTER, Eleonora JOVCHEVA, Bernd KUHN, Kiel LAZARSKI, Yanke LIANG, Thomas LUEBBERS, Laetitia Janine MARTIN, Rainer E. MARTIN, Barbara Johanna MUELLER, Roger NORCROSS, Philipp SCHMID, Jean-Yves WACH
  • Publication number: 20230002367
    Abstract: The invention provides a bifunctional compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein said Targeting Ligand, Linker and Degron are as described herein.
    Type: Application
    Filed: October 26, 2020
    Publication date: January 5, 2023
    Inventors: Delphine GAUFRETEAU, Roman HUTTER, Eleonora JOVCHEVA, Bernd KUHN, Thomas LUEBBERS, Rainer E. MARTIN, Laetitia Janine MARTIN, Barbara Johanna MUELLER, Roger NORCROSS, Fabienne RICKLIN, Philipp SCHMID, Jean-Yves WACH, Juergen WICHMANN, Martin DUPLESSIS, Kiel LAZARSKI, Yanke LIANG
  • Publication number: 20220033395
    Abstract: 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 thereof
    Type: Application
    Filed: April 22, 2021
    Publication date: February 3, 2022
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Hans Hilpert, Sabine Kolczewski, Roland Humm, Theodor Stoll, Thorsten Muser, Jean-Marc Plancher, Delphine Gaufreteau
  • Publication number: 20210246133
    Abstract: 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 thereof
    Type: Application
    Filed: October 13, 2020
    Publication date: August 12, 2021
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Hans Hilpert, Sabine Kolczewski, Roland Humm, Theodor Stoll, Thorsten Muser, Jean-Marc Plancher, Delphine Gaufreteau
  • Patent number: 11066393
    Abstract: 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: Grant
    Filed: June 10, 2020
    Date of Patent: July 20, 2021
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Delphine Gaufreteau, Sabine Kolczewski, Jean-Marc Plancher, Theodor Stoll, Remy Halm
  • Publication number: 20200299278
    Abstract: 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: Application
    Filed: June 10, 2020
    Publication date: September 24, 2020
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Delphine Gaufreteau, Sabine Kolczewski, Jean-Marc Plancher, Theodor Stoll, Remy Halm
  • Patent number: 10710985
    Abstract: 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: Grant
    Filed: May 4, 2018
    Date of Patent: July 14, 2020
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Delphine Gaufreteau, Sabine Kolczewski, Jean-Marc Plancher, Theodor Stoll, Remy Halm
  • Publication number: 20200010466
    Abstract: 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 thereof
    Type: Application
    Filed: July 19, 2019
    Publication date: January 9, 2020
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Hans Hilpert, Sabine Kolczewski, Roland Humm, Theodor Stoll, Thorsten Muser, Jean-Marc Plancher, Delphine Gaufreteau
  • Patent number: 10519140
    Abstract: 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: Grant
    Filed: May 4, 2018
    Date of Patent: December 31, 2019
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Delphine Gaufreteau, Sabine Kolczewski, Jean-Marc Plancher, Theodor Stoll
  • Patent number: 10457667
    Abstract: The present invention is concerned with indolin-2-one derivatives of general formula wherein A is phenyl or a six membered heteroaryl group, containing one or two N atoms, selected from or the oxygen atom may form together with two neighboring carbon atoms from the group A an additional fused ring, selected from R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen or oxetanyl; R2 is hydrogen, lower alkyl lower alkoxy, halogen or cycloalkyl; --- the dotted line is nothing or may be —CH2—; 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 thereof.
    Type: Grant
    Filed: May 4, 2018
    Date of Patent: October 29, 2019
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Delphine Gaufreteau, Hans Hilpert, Roland Humm, Sabine Kolczewski, Thorsten Muser, Jean-Marc Plancher, Theodor Stoll
  • Patent number: 10377746
    Abstract: The present invention is concerned with indolin-2-one derivatives of general formula wherein A is phenyl or a six membered heteroaryl group, containing one or two N atoms, selected from R1 is S(O)2lower alkyl, S(O)2NR4R5, S(O)2cycloalkyl, S-lower alkyl or S(O)2-azetidin-1-yl; R4 and R5 are independently from each other hydrogen, lower alkyl or (CH2)2OCH3; or the group A-R1 may form together with two neighboring carbon atoms from the group A an additional fused ring, selected from R2 is hydrogen or cycloalkyl; R3 is methyl or halogen; n is 1 or 2; X is N, N+O? or CH; --- the dotted line may be nothing or —CH2—; 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 thereof.
    Type: Grant
    Filed: May 4, 2018
    Date of Patent: August 13, 2019
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Delphine Gaufreteau, Hans Hilpert, Roland Humm, Sabine Kolczewski, Thorsten Muser, Jean-Marc Plancher, Theodor Stoll
  • Publication number: 20180251450
    Abstract: 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: Application
    Filed: May 4, 2018
    Publication date: September 6, 2018
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Delphine Gaufreteau, Sabine Kolczewski, Jean-Marc Plancher, Theodor Stoll
  • Publication number: 20180251455
    Abstract: The present invention is concerned with indolin-2-one derivatives of general formula wherein A is phenyl or a six membered heteroaryl group, containing one or two N atoms, selected from R1 is S(O)2lower alkyl, S(O)2NR4R5, S(O)2cycloalkyl, S-lower alkyl or S(O)2-azetidin-1-yl; R4 and R5 are independently from each other hydrogen, lower alkyl or (CH2)2OCH3; or the group A-R1 may form together with two neighboring carbon atoms from the group A an additional fused ring, selected from R2 is hydrogen or cycloalkyl; R3 is methyl or halogen; n is 1 or 2; X is N, N+O? or CH; --- the dotted line may be nothing or —CH2—; 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 thereof.
    Type: Application
    Filed: May 4, 2018
    Publication date: September 6, 2018
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Delphine Gaufreteau, Hans Hilpert, Roland Humm, Sabine Kolczewski, Thorsten Muser, Jean-Marc Plancher, Theodor Stoll
  • Publication number: 20180251451
    Abstract: The present invention is concerned with indolin-2-one derivatives of general formula wherein A is phenyl or a six membered heteroaryl group, containing one or two N atoms, selected from or the oxygen atom may form together with two neighboring carbon atoms from the group A an additional fused ring, selected from R1 is hydrogen, lower alkyl, lower alkyl substituted by halogen or oxetanyl; R2 is hydrogen, lower alkyl lower alkoxy, halogen or cycloalkyl; --- the dotted line is nothing or may be —CH2—; 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 thereof.
    Type: Application
    Filed: May 4, 2018
    Publication date: September 6, 2018
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Delphine Gaufreteau, Hans Hilpert, Roland Humm, Sabine Kolczewski, Thorsten Muser, Jean-Marc Plancher, Theodor Stoll
  • Publication number: 20180251449
    Abstract: 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: Application
    Filed: May 4, 2018
    Publication date: September 6, 2018
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Delphine Gaufreteau, Sabine Kolczewski, Jean-Marc Plancher, Theodor Stoll, Remy Halm
  • Publication number: 20170101409
    Abstract: 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 thereof
    Type: Application
    Filed: December 22, 2016
    Publication date: April 13, 2017
    Applicant: Hoffmann-La Roche Inc.
    Inventors: Hans Hilpert, Sabine Kolczewski, Roland Humm, Theodor Stoll, Thorsten Muser, Jean-Marc Plancher, Delphine Gaufreteau
  • Patent number: 9290467
    Abstract: The invention relates to a compound of formula (I) wherein A, B, D and R1 to R6 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.
    Type: Grant
    Filed: January 10, 2013
    Date of Patent: March 22, 2016
    Assignee: HOFFMANN—LA ROCHE INC.
    Inventors: Lilli Anselm, David Banner, Jean-Baptiste Blanc, Delphine Gaufreteau, Wolfgang Haap, Guido Hartmann, Bernd Kuhn, Thomas Luebbers, Jens-Uwe Peters, Beat Spinnler
  • Patent number: 7544683
    Abstract: The present invention relates to compounds of formula I wherein R1 and R2 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.
    Type: Grant
    Filed: June 10, 2008
    Date of Patent: June 9, 2009
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Delphine Gaufreteau, Matthias Nettekoven, Jean-Marc Plancher, Olivier Roche, Sebastien Schmitt, Tadakatsu Takahashi