公开(公告)号：US20190117658A1

公开(公告)日：2019-04-25

申请号：US16090142

申请日：2017-03-28

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Lawrence P. WENNOGLE

IPC: A61K31/519 ,  A61K31/4985

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.

公开(公告)号：US20190071445A1

公开(公告)日：2019-03-07

申请号：US16056143

申请日：2018-08-06

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Qiang ZHANG ,  Robert DAVIS ,  Lawrence P. WENNOGLE

IPC: C07D471/16 ,  A61K9/50 ,  A61K47/38 ,  C07D471/14 ,  A61K31/4985 ,  A61K9/48 ,  A61K47/34

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.

公开(公告)号：US10221176B2

公开(公告)日：2019-03-05

申请号：US15660762

申请日：2017-07-26

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： John Charles Tomesch ,  Peng Li ,  Wei Yao ,  Qiang Zhang ,  James David Beard ,  Andrew S. Thompson ,  Hua Cheng ,  Lawrence P. Wennogle

IPC: C07D471/22 ,  C07D487/22 ,  C07D471/16 ,  C07D471/04

Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines of Formula 2F, 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 2F, as shown below and as further defined herein:

公开(公告)号：US10117867B2

公开(公告)日：2018-11-06

申请号：US15467867

申请日：2017-03-23

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon Mates ,  Allen Fienberg ,  Lawrence P. Wennogle

IPC: A61K31/44 ,  A61K31/4985 ,  A61K31/5383 ,  A61K45/06 ,  C07D471/14 ,  C07D498/14 ,  A61K9/00 ,  A61K31/198

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.

公开(公告)号：US10077267B2

公开(公告)日：2018-09-18

申请号：US15301912

申请日：2015-04-03

Applicant: Intra-Cellular Therapies, Inc.

Inventor： Sharon Mates ,  Peng Li ,  Lawrence P. Wennogle ,  Robert Davis

IPC: C07D471/16 ,  A61K31/4985 ,  C07D471/14 ,  A61K45/06 ,  C07B59/00

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.

公开(公告)号：US10072010B2

公开(公告)日：2018-09-11

申请号：US15629481

申请日：2017-06-21

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Qiang Zhang ,  Robert Davis ,  Lawrence P. Wennogle

IPC: A61K31/4985 ,  C07D487/22 ,  C07D471/16 ,  C07D471/14 ,  A61K9/48 ,  A61K9/50 ,  A61K47/34 ,  A61K47/38

CPC classification number: C07D471/16 ,  A61K9/4825 ,  A61K9/4891 ,  A61K9/5031 ,  A61K31/4985 ,  A61K47/34 ,  A61K47/38 ,  C07D471/14

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:

公开(公告)号：US09956227B2

公开(公告)日：2018-05-01

申请号：US15101874

申请日：2014-12-03

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Kimberly Vanover ,  Peng Li ,  Sharon Mates ,  Robert Davis ,  Lawrence P. Wennogle

IPC: A61K45/06 ,  A61K9/00 ,  A61K31/4985 ,  A61K31/5383 ,  A61K9/51

CPC classification number: A61K31/5383 ,  A61K9/0019 ,  A61K9/0024 ,  A61K9/5153 ,  A61K31/4985 ,  A61K45/06 ,  A61K2300/00

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.

公开(公告)号：US20170360753A1

公开(公告)日：2017-12-21

申请号：US15533525

申请日：2015-12-07

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Hailin ZHENG ,  Gretchen SNYDER ,  Lawrence P. WENNOGLE ,  Joseph HENDRICK

IPC: A61K31/4162 ,  C07D403/14 ,  C07D209/58 ,  C07D471/14

CPC classification number: A61K31/4162 ,  A61K2300/00 ,  C07D209/58 ,  C07D403/14 ,  C07D471/14

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.

公开(公告)号：US20170291904A1

公开(公告)日：2017-10-12

申请号：US15512005

申请日：2015-09-17

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Hailin ZHENG ,  Jun ZHAO ,  Lawrence WENNOGLE

IPC: C07D487/14

CPC classification number: C07D487/14

Abstract: The subject matter generally relates to compounds and 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.

公开(公告)号：US20170128453A1

公开(公告)日：2017-05-11

申请号：US15406346

申请日：2017-01-13

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Lawrence WENNOGLE

IPC: A61K31/519 ,  G01N33/84 ,  A61K31/517 ,  A61K31/527 ,  A61K31/53

CPC classification number: A61K31/519 ,  A61K31/517 ,  A61K31/527 ,  A61K31/53 ,  G01N33/84 ,  G01N2333/4727 ,  G01N2800/28

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.