Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines.
Type:
Application
Filed:
October 7, 2019
Publication date:
March 19, 2020
Applicant:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
John Charles TOMESCH, Peng LI, Wei YAO, Qiang ZHANG, James David BEARD, Andrew S. THOMPSON, Hua CHENG, Lawrence P. WENNOGLE
Abstract: The present invention relates to PDEI inhibitory compounds of Formula I as described herein, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
Type:
Grant
Filed:
June 11, 2012
Date of Patent:
February 18, 2020
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Peng Li, Hailin Zheng, Jun Zhao, Lawrence P. Wennogle
Abstract: The present invention relates to certain PDE2 inhibitory compounds, in free or salt form, pharmaceutical compositions containing such compounds and methods for the treatment of PDE2 mediated disorders.
Type:
Grant
Filed:
September 7, 2018
Date of Patent:
January 28, 2020
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Peng Li, Hailin Zheng, Gretchen Snyder, Lawrence P. Wennogle, Joseph Hendrick
Abstract: The invention provides methods for the prophylaxis or treatment of one or more disorders associated with dementia comprising administering to a patient in need thereof, a therapeutically effective amount of (i) a 5-HT2A or 5-HT2A/D2 receptor ligand and (ii) a PDE1 inhibitor, and pharmaceutical compositions comprising (i) a 5-HT2A or 5-HT2A/D2 receptor ligand and (ii) a PDE1 inhibitor.
Abstract: The present invention relates to use of particular substituted heterocycle fused gamma-carbolines as described herein, in free, pharmaceutically acceptable salt or prodrug form, and pharmaceutical composition comprising the same optionally in combination with one or more agents, for the prophylaxis or treatment of one or more disorders associated with dementia, particularly behavioral or mood disturbances (e.g., agitation/aggression), psychosis, depression and sleep disturbances among others in patients suffering from dementia.
Type:
Application
Filed:
September 27, 2019
Publication date:
January 16, 2020
Applicant:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Sharon MATES, Robert DAVIS, Kimberly VANOVER, Lawrence WENNOGLE
Abstract: The disclosure provides new, stable, pharmaceutically acceptable co-crystal forms of 1-(4-fluoro-phenyl)-4-((6bR, 10aS)-3-methyl-2,3,6b,9, 10, 10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de[quinoxalin-8-yl)-butan-1-one, together with methods of making and using them, and pharmaceutical compositions comprising them.
Abstract: The invention relates to pharmaceutical compositions comprising 4-((6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H,7H-pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]quinoxalin-8-yl)-1-(4-fluorophenyl)butan-1-one in toluenesulfonic acid addition salt form: 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:
August 6, 2018
Date of Patent:
November 12, 2019
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Peng Li, Qiang Zhang, Robert Davis, Lawrence P. Wennogle
Abstract: The present invention provides pharmaceutical compositions comprising certain optionally substituted heterocycle fused gamma-carbolines of Formula 2J, as shown below, and as further defined herein:
Type:
Grant
Filed:
June 12, 2019
Date of Patent:
November 5, 2019
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
John Charles Tomesch, Peng Li, Wei Yao, Qiang Zhang, James David Beard, Andrew S. Thompson, Hua Cheng, Lawrence P. Wennogle
Abstract: The disclosure provides the use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of residual symptoms of psychosis or schizophrenia. The disclosure also provides novel long acting injectable formulations of particular substituted heterocycle fused gamma-carboline compounds and use of such long acting injectable formulations for the treatment of residual symptoms of psychosis or schizophrenia.
Type:
Application
Filed:
July 10, 2019
Publication date:
October 31, 2019
Applicant:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Kimberly VANOVER, Peng LI, Sharon MATES, Robert DAVIS, Lawrence P. WENNOGLE
Abstract: The disclosure provides the use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of residual symptoms of psychosis or schizophrenia. The disclosure also provides novel long acting injectable formulations of particular substituted heterocycle fused gamma-carboline compounds and use of such long acting injectable formulations for the treatment of residual symptoms of psychosis or schizophrenia.
Type:
Application
Filed:
June 17, 2019
Publication date:
October 3, 2019
Applicant:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Kimberly VANOVER, Peng LI, Sharon MATES, Robert DAVIS, Lawrence P. WENNOGLE
Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines.
Type:
Application
Filed:
June 12, 2019
Publication date:
September 26, 2019
Applicant:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
John Charles TOMESCH, Peng LI, Wei YAO, Qiang ZHANG, James David BEARD, Andrew S. THOMPSON, Hua CHENG, Lawrence P. WENNOGLE
Abstract: The disclosure provides the use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of residual symptoms of psychosis or schizophrenia. The disclosure also provides novel long acting injectable formulations of particular substituted heterocycle fused gamma-carboline compounds and use of such long acting injectable formulations for the treatment of residual symptoms of psychosis or schizophrenia.
Type:
Application
Filed:
April 23, 2019
Publication date:
September 26, 2019
Applicant:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Kimberly VANOVER, Peng LI, Sharon MATES, Robert DAVIS, Lawrence P. WENNOGLE
Abstract: The invention relates to the combination of inhibitors of phosphodiesterase 1 (PDE1) and inhibitors of Neprilysin (NEP) useful for the treatment of certain cardiovascular diseases or related disorders, e.g., hypertension, congestive heart disease, and post-myocardial infarction. In another embodiment, the invention relates to the combination of inhibitors of PDE1 and inhibitors of NEP for the treatment of diseases or disorders characterized by disruption of or damage to various cGMP/PKG mediated pathways in the cardiovascular system (e.g., in cardiac tissue or in arterial smooth muscle).
Abstract: The invention relates to the administration of inhibitors of phosphodiesterase 1 (PDE1) for the treatment of diseases or disorders characterized by disruption of or damage to various cGMP/PKG mediated pathways. In one embodiment the invention relates to inhibitors of phosphodiesterase 1 (PDE1) for treatment of cardiovascular disease and related disorders, e.g., congestive heart disease, atherosclerosis, myocardial infarction, and stroke.
Abstract: The invention relates to particular substituted deuterated 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.
Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines
Type:
Application
Filed:
January 10, 2019
Publication date:
July 18, 2019
Applicant:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
John Charles TOMESCH, Peng LI, Wei YAO, Qiang ZHANG, James David BEARD, Andrew S. THOMPSON, Hua CHENG, Lawrence P. WENNOGLE
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.
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:
October 19, 2018
Publication date:
June 20, 2019
Applicant:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Sharon MATES, Allen FIENBERG, Lawrence P. WENNOGLE
Abstract: The disclosure provides the use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of residual symptoms of psychosis or schizophrenia. The disclosure also provides novel long acting injectable formulations of particular substituted heterocycle fused gamma-carboline compounds and use of such long acting injectable formulations for the treatment of residual symptoms of psychosis or schizophrenia.
Type:
Grant
Filed:
March 12, 2018
Date of Patent:
June 18, 2019
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Kimberly Vanover, Peng Li, Sharon Mates, Robert Davis, Lawrence P. Wennogle
Abstract: The present invention relates to certain PDE2 inhibitory compounds, in free or salt form, pharmaceutical compositions containing such compounds and methods for the treatment of PDE2 mediated disorders.
Type:
Grant
Filed:
December 7, 2015
Date of Patent:
May 28, 2019
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Peng Li, Hailin Zheng, Gretchen Snyder, Lawrence P. Wennogle, Joseph Hendrick