Abstract: The invention relates to substituted pyrido[3?,4?:4,5]pyrrolo[1,2,3-de]-quinoxaline compounds, represented by Formula 1, defined herein, free base or pharmaceutically acceptable salt forms of the compounds, pharmaceutical compositions thereof, and methods of treating conditions of the central nervous system therewith:
Type:
Grant
Filed:
June 21, 2017
Date of Patent:
September 11, 2018
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Peng Li, Qiang Zhang, 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:
March 12, 2018
Publication date:
July 19, 2018
Applicant:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Kimberly VANOVER, Peng LI, Sharon MATES, Robert DAVIS, Lawrence P. WENNOGLE
Abstract: The present invention relates to a new use of phosphodiesterase 1 (PDE1) inhibitors for the treatment of psychosis, schizophrenia, schizoaffective disorder, schizophreniform disorder, psychotic disorder, delusional disorder, mania, or bipolar disorder.
Type:
Grant
Filed:
September 12, 2016
Date of Patent:
July 3, 2018
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Allen A. Fienberg, Lawrence P. Wennogle, Sharon Mates
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 novel inhibitors of phosphodiesterase 1 (PDE1), according to Formula I, below, wherein R1, R2, R3 and R4 are as defined herein, 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:
June 26, 2018
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Peng Li, Hailin Zheng, Jun Zhao, 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:
December 3, 2014
Date of Patent:
May 1, 2018
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Kimberly Vanover, Peng Li, Sharon Mates, Robert Davis, Lawrence P. Wennogle
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:
Grant
Filed:
January 9, 2015
Date of Patent:
April 17, 2018
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Qiang Zhang, Youyi Peng, Peng Li, J. David Beard, Lawrence P. Wennogle, John Tomesch
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:
April 10, 2018
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Peng Li, Hailin Zheng, Jun Zhao, 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 heterocycl fused gamma-carbolines.
Type:
Application
Filed:
July 26, 2017
Publication date:
February 15, 2018
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: Provided are PDE1 inhibitors of Formula I, processes for their production, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
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 present invention relates to a product comprising a PDE1 inhibitor and a PDE2 inhibitor, in free or salt form, pharmaceutical compositions comprising them and their use as pharmaceuticals for the treatment of cAMP and/or cGMP related disorders.
Type:
Grant
Filed:
January 8, 2015
Date of Patent:
December 26, 2017
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Joseph Hendrick, Jennifer O'Brien, Gretchen Snyder, Peng Li, 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:
Application
Filed:
December 7, 2015
Publication date:
December 21, 2017
Applicant:
Intra-Cellular Therapies, Inc.
Inventors:
Peng LI, Hailin ZHENG, Gretchen SNYDER, Lawrence P. WENNOGLE, Joseph HENDRICK
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:
Application
Filed:
December 7, 2015
Publication date:
December 21, 2017
Applicant:
Intra-Cellular Therapies, Inc.
Inventors:
Peng LI, Hailin ZHENG, Gretchen SNYDER, Lawrence P. WENNOGLE, Joseph HENDRICK
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 heterocycle fused gamma-carbolines, their prodrugs, 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 involving 5-HT2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D2 receptor signaling systems.
Type:
Application
Filed:
June 21, 2017
Publication date:
October 5, 2017
Applicant:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Peng LI, Qiang ZHANG, Robert DAVIS, Lawrence P. Wennogle
Abstract: Optionally substituted (1- or 3-oxy)-4,5,7,8-tetrahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-imidazo[1,2-a]pyrrolo[3,4-e]pyrimidine or (1- or 3-oxy)-4,5,7,8,9-pentahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-pyrimido[1,2-a]pyrrolo[3,4-e]pyrimidine compounds, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising the same.
Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines of Formula 2J, as shown below, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines, such methods comprising the preparation of a Compound of Formula 2G, as shown below, and use of said compound to produce the fused gamma-carbolines of Formula 2J, as defined herein:
Type:
Grant
Filed:
March 10, 2016
Date of Patent:
September 5, 2017
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 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:
Grant
Filed:
April 3, 2015
Date of Patent:
August 29, 2017
Assignee:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Sharon Mates, Peng Li, Lawrence P. Wennogle, Robert Davis
Abstract: Provided are PDE1 inhibitors of Formula I, processes for their production, their use as pharmaceuticals, and pharmaceutical compositions comprising them.
Type:
Application
Filed:
January 30, 2017
Publication date:
August 17, 2017
Applicant:
INTRA-CELLULAR THERAPIES, INC.
Inventors:
Peng LI, Hailin ZHENG, Jun ZHAO, Lawrence P. WENNOGLE