Patents Assigned to Intra-Cellular Therapies, Inc.
  • Organic compounds
    Patent number: 9708294
    Abstract: The invention relates to compounds and methods of treatment relating to nicotinic receptor antagonists. For example, the compounds and methods of treatment function block the activity of certain acetylcholine receptors and subtypes therein, and are useful treating diseases and conditions mediated by nicotinic receptor stimulation, e.g., small cell lung cancer.
    Type: Grant
    Filed: January 11, 2016
    Date of Patent: July 18, 2017
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Youyi Peng, John Tomesch, Lawrence P. Wennogle, Qiang Zhang
  • Substituted pyrido[3',4':4,5]pyrrolo[1,2,3-de]quinoxalines for inhibiting serotonin reuptake transporter activity
    Patent number: 9708322
    Abstract: The invention relates to substituted heterocycle fused gamma-carbolines of the Formula Q as described herein, in free base or pharmaceutically acceptable salt form, and/or pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor pathway, the serotonin transporter (SERT) pathway and/or the dopamine D2 receptor pathway signaling systems.
    Type: Grant
    Filed: March 15, 2014
    Date of Patent: July 18, 2017
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Qiang Zhang, Robert Davis, Lawrence P. Wennogle
  • ORGANIC COMPOUNDS
    Publication number: 20170197974
    Abstract: Provided are PDE1 inhibitors of Formula I, processes for their production, their use as pharmaceuticals, and pharmaceutical compositions comprising them. Previous publication WO 2009/075784 disclosed, among others, (6aR,9aS)-2-(4-(6-fluoropyridin-2-yl) benzyl)-5-methyl-3-(phenylamino)-5,6a,7,8,9,9a-hexahydrocyclopenta[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one as an inhibito of PDE1. This compound undergoes significant metabolism at several positions including the aniline ring and the cyclopentane ring. The current invention provides for Compounds of Formula I wherein such metabolism is attenuated by the substitution of hydrogen atoms for deuterium atoms at key locations discovered by the inventors.
    Type: Application
    Filed: June 22, 2015
    Publication date: July 13, 2017
    Applicant: Intra-Cellular Therapies, Inc.
    Inventor: Peng LI
  • ORGANIC COMPOUNDS
    Publication number: 20170190703
    Abstract: The invention provides novel compounds, composition comprising said compounds and methods for inhibiting CK1 as well as methods of treating CK1 related disorders such as Alzheimer's disease comprising administering a therapeutically effective amount of a CK1 inhibitor to a patient in need thereof.
    Type: Application
    Filed: January 9, 2015
    Publication date: July 6, 2017
    Applicant: Intra-Cellular Therapies, Inc.
    Inventors: Qiang Zhang, Youyi Peng, Peng Li, J. David Beard, Lawrence P. Wennogle, John Tomesch
  • METHODS AND COMPOSITIONS FOR SLEEP DISORDERS AND OTHER DISORDERS
    Publication number: 20170189398
    Abstract: Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals and pharmaceutical compositions comprising them for the treatment of one or more disorders involving the 5-HT2A, SERT and/or dopamine D2 pathways are disclosed. In addition, the compounds may be combined with other therapeutic agents for the treatment of one or more sleep disorders, depression, psychosis, dyskinesias, and/or Parkinson's disease or any combinations.
    Type: Application
    Filed: March 23, 2017
    Publication date: July 6, 2017
    Applicant: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Sharon MATES, Allen FIENBERG, Lawrence P. WENNOGLE
  • ORGANIC COMPOUNDS
    Publication number: 20170183350
    Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.
    Type: Application
    Filed: April 3, 2015
    Publication date: June 29, 2017
    Applicant: Intra-Cellular Therapies, Inc.
    Inventors: Sharon MATES, Peng LI, Lawrence P. WENNOGLE, Robert DAVIS
  • NOVEL USES
    Publication number: 20170128453
    Abstract: The subject matter generally relates to methods of treatment and/or prophylaxis of CNS diseases, disorders, and/or injuries. In one aspect, the subject matter relates to inhibitors of phosphodiesterase 1 (PDE1) as neuroprotective agents and/or neural regenerative agents. In a further aspect, the subject matter relates to individuals that are at risk for the development of CNS disease or disorder.
    Type: Application
    Filed: January 13, 2017
    Publication date: May 11, 2017
    Applicant: INTRA-CELLULAR THERAPIES, INC.
    Inventor: Lawrence WENNOGLE
  • COMPOUNDS AND METHODS OF USE TO TREAT SCHIZOPHRENIA
    Publication number: 20170114037
    Abstract: The invention relates to particular 2-((1-(2-hydroxy-2-phenylethyl)piperidin-4-yl)methyl)isoindolin-1-one analogs and pro-drugs, in free, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases that can be therapeutically and/or preventively treated by the nerve control function of sigma ligands.
    Type: Application
    Filed: June 9, 2015
    Publication date: April 27, 2017
    Applicant: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Robert DAVIS, Peng LI
  • Free base crystals
    Patent number: 9630971
    Abstract: The present invention relates to crystals of (6aR,9aS)-5,6a,7,8,9,9a-hexahydro-5-methyl-3-(phenylamino)-2-((4-(6-fluoropyridin-2-yl)phenyl)methyl)-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one, and methods of making and using such crystals.
    Type: Grant
    Filed: June 20, 2014
    Date of Patent: April 25, 2017
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Takashi Abe, Graham Buckton, Robert Davis, Mark Hooper, Peng Li, Hideaki Maruyama, Masahiro Takasuga, Lawrence P. Wennogle, Yuhei Yamamoto, Hironori Yamashita
  • Organic compounds
    Patent number: 9624230
    Abstract: The invention provides novel 7,8-dihydro-imidazo[1,2-?]pyrazolo[4,3-e]pyrimidin-4-one compounds and 7,8,9-trihydro-[1H or 2/f]-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one compounds, substituted at the 1 or 2 position with C2-g allcyl, C3-9 cycloalkyl, heteroarylalkyl, or substituted arylalkyl, in free, salt or prodrug form, processes for their production, their use as pharmaceuticals, particularly as PDE1 inhibitors, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: March 27, 2015
    Date of Patent: April 18, 2017
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Haiyan Wu
  • Methods and compositions for sleep disorders and other disorders
    Patent number: 9616061
    Abstract: Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals and pharmaceutical compositions comprising them for the treatment of one or more disorders involving the 5-HT2A, SERT and/or dopamine D2 pathways are disclosed. In addition, the compounds may be combined with other therapeutic agents for the treatment of one or more sleep disorders, depression, psychosis, dyskinesias, and/or Parkinson's disease or any combinations.
    Type: Grant
    Filed: October 16, 2015
    Date of Patent: April 11, 2017
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Sharon Mates, Allen Fienberg, Lawrence Wennogle
  • Regulatory proteins and inhibitors
    Patent number: 9605041
    Abstract: The invention provides a previously uncharacterized protein (gamma secretase activating protein or gSAP) that activates ?-secretase to produce ?-amyloid protein (A?). Deposition of A? has been associated with Alzheimer's disease and other pathologies. The invention thus additionally provides, e.g., screening methods and novel research tools, inhibitors of this novel protein, and methods of diagnosis, treatment and control of Alzheimer's disease and other neurodegenerative conditions associated with deposition of A?.
    Type: Grant
    Filed: February 6, 2012
    Date of Patent: March 28, 2017
    Assignees: INTRA-CELLULAR THERAPIES, INC., THE ROCKEFELLER UNIVERSITY
    Inventors: Paul Greengard, Wenjie Luo, Gen He, Peng Li, Lawrence Wennogle
  • Organic compounds
    Patent number: 9598426
    Abstract: Provided are PDE1 inhibitors of Formula I, processes for their production and their use as pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: March 21, 2017
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Hailin Zheng, Jun Zhao, Lawrence Wennogle
  • 4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de] quinoxalin-8(7H)-yl)-1-(4-fluorophenyl)-1-butanone toluenesulfonic acid salt crystal forms
    Patent number: 9586960
    Abstract: The present invention relates to toluenesulfonic acid addition salt crystals of 4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido[3?,4?: 4,5]pyrrolo[1,2,3-de]quinoxalin-8(7H)-yl)-1-(4-fluorophenyl)-1-butanone, and methods of using such crystals as 5-hydroxytryptamine 2 receptor agonists and antagonists in treating disorders of the central nervous system.
    Type: Grant
    Filed: November 30, 2015
    Date of Patent: March 7, 2017
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: John Tomesch, Lawrence P. Wennogle
  • ORGANIC COMPOUNDS
    Publication number: 20170037048
    Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D1/D2 receptor signaling systems, and/or the treatment of residual symptoms.
    Type: Application
    Filed: April 3, 2015
    Publication date: February 9, 2017
    Applicant: Intra-Cellular Therapies, Inc.
    Inventors: Sharon MATES, Peng LI, Lawrence P. WENNOGLE, Robert DAVIS
  • Organic compounds
    Patent number: 9556185
    Abstract: The present invention relates to optionally substituted 4,5,7,8-tetrahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-(1H or 2H)-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidine or 4,5,7,8,9-pentahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-(1H or 2H)-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidine compounds, and methods of using said compound, e.g., wherein the treatment relates to diseases involving disorders of the dopamine D1 receptor intracellular pathway, such as, among others, Parkinson's disease, depression, narcolepsy, damage to cognitive function, e.g., in schizophrenia.
    Type: Grant
    Filed: May 31, 2011
    Date of Patent: January 31, 2017
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Hailin Zheng, Jun Zhao, Lawrence P. Wennogle
  • Organic compounds
    Patent number: 9556186
    Abstract: Provided are PDE1 inhibitors of Formula I, processes for their production, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: June 4, 2015
    Date of Patent: January 31, 2017
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Hailin Zheng, Jun Zhao, Lawrence P. Wennogle
  • Method of treating a CNS injury with a PDE1 inhibitor
    Patent number: 9545406
    Abstract: The subject matter generally relates to methods of treatment and/or prophylaxis of CNS diseases, disorders, and/or injuries. In one aspect, the subject matter relates to inhibitors of phosphodiesterase 1 (PDE1) as neuroprotective agents and/or neural regenerative agents. In a further aspect, the subject matter relates to individuals that are at risk for the development of CNS disease or disorder.
    Type: Grant
    Filed: March 17, 2014
    Date of Patent: January 17, 2017
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventor: Lawrence Wennogle
  • Organic compounds
    Patent number: 9546175
    Abstract: The invention relates to novel inhibitors of phosphodiesterase 1 (PDE1), useful for the treatment of diseases or disorders characterized by disruption of or damage to certain cGMP/PKG mediated pathways (e.g., in cardiac tissue). The invention further relates to pharmaceutical composition comprising the same and methods of treatment of cardiovascular disease and related disorders, e.g., congestive heart disease, atherosclerosis, myocardial infarction, and stroke.
    Type: Grant
    Filed: August 6, 2015
    Date of Patent: January 17, 2017
    Assignee: INTRA-CELLULAR THERAPIES, INC.
    Inventors: Peng Li, Hailin Zheng, Jun Zhao, Lawrence P. Wennogle
  • ORGANIC COMPOUNDS
    Publication number: 20160326179
    Abstract: The invention provides novel compounds, composition comprising said compounds and methods for inhibiting CK1 as well as methods of treating CK1 related disorders such as Alzheimer's disease comprising administering a therapeutically effective amount of a CK1 inhibitor to a patient in need thereof.
    Type: Application
    Filed: January 9, 2015
    Publication date: November 10, 2016
    Applicant: Intra-Cellular Therapies, Inc.
    Inventors: Qiang Zhang, Youyi Peng, Peng Li, J. David Beard, Lawrence P. Wennogle, John Tomesch