公开(公告)号：US20210299124A1

公开(公告)日：2021-09-30

申请号：US17332417

申请日：2021-05-27

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert DAVIS

IPC: A61K31/4985 ,  A61K9/48 ,  A61K9/00 ,  A61K9/16

Abstract: The present disclosure relates to pharmaceutical capsules comprising lumateperone, in free, or pharmaceutically acceptable salt form, optionally in combination with one or more additional therapeutic agents, processes for manufacture thereof and methods of use in the treatment or prophylaxis of disease.

公开(公告)号：US20210060009A1

公开(公告)日：2021-03-04

申请号：US16981639

申请日：2019-03-15

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Gretchen SNYDER ,  Robert DAVIS ,  Lawrence P. WENNOGLE

IPC: A61K31/4985 ,  A61P25/24 ,  A61K31/135 ,  A61K31/13 ,  A61K31/485 ,  A61K31/155 ,  A61K38/07 ,  A61K31/197 ,  A61K31/42 ,  A61K9/00 ,  A61K31/343 ,  A61K31/36 ,  A61K31/138 ,  A61K31/137 ,  A61K31/381 ,  A61K31/165 ,  A61K31/55 ,  A61K31/38 ,  A61K31/5513

Abstract: The disclosure provides methods for the acute treatment of depression and/or anxiety, for the enhancement of mTOR (e.g., mTORC1) signaling, and for the reduction of neuroinflammation, comprising administering to a patient in need thereof, a therapeutically effective amount of a 5-HT2A or 5-HT2A/D2 receptor ligand, e.g. lumateperone.

公开(公告)号：US20210002280A1

公开(公告)日：2021-01-07

申请号：US16926552

申请日：2020-07-10

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon MATES ,  Robert DAVIS ,  Kimberly VANOVER

IPC: C07D471/14 ,  A61K45/06 ,  A61K31/5383 ,  A61K31/4985 ,  C07D471/16 ,  A61K31/445

Abstract: Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of agitation, aggressive behaviors, posttraumatic stress disorder or impulse control disorders.

公开(公告)号：US20210000822A1

公开(公告)日：2021-01-07

申请号：US16922893

申请日：2020-07-07

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon MATES ,  Robert DAVIS ,  Kimberly VANOVER

IPC: A61K31/4985 ,  A61P25/18 ,  A61K9/20 ,  A61K9/48

Abstract: The disclosure provides methods for the treatment of Bipolar II Disorder, comprising administering to a patient in need thereof, a therapeutically effective amount of lumateperone, in free or pharmaceutically acceptable salt form, optionally in deuterated form.

公开(公告)号：US20200247806A1

公开(公告)日：2020-08-06

申请号：US16786240

申请日：2020-02-10

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon MATES ,  Peng LI ,  Lawrence P. WENNOGLE ,  Robert DAVIS

IPC: C07D471/16 ,  A61K31/4985 ,  C07B59/00 ,  A61K45/06 ,  C07D471/14 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24

Abstract: This 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：US20200069683A1

公开(公告)日：2020-03-05

申请号：US16557083

申请日：2019-08-30

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert DAVIS

IPC: A61K31/4985 ,  A61K9/48 ,  A61K9/16 ,  A61K9/00

Abstract: The present disclosure relates to pharmaceutical capsules comprising lumateperone, in free, or pharmaceutically acceptable salt form, optionally in combination with one or more additional therapeutic agents, processes for manufacture thereof and methods of use in the treatment or prophylaxis of disease.

公开(公告)号：US20190330211A1

公开(公告)日：2019-10-31

申请号：US16473693

申请日：2017-12-29

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert DAVIS

IPC: C07D471/14 ,  A61K9/51

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 the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and/or the μ-opioid receptor.

公开(公告)号：US20180271862A1

公开(公告)日：2018-09-27

申请号：US15934860

申请日：2018-03-23

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Wei YAO ,  Robert DAVIS

IPC: A61K31/4985 ,  A61K9/00 ,  A61K9/06

Abstract: The disclosure provides new transmucosal and subcutaneous pharmaceutical compositions comprising 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 or 1-(4-fluoro-phenyl)-4-((6bR,10aS)-2,2-d2-3-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 or comprising -(4-fluoro-phenyl)-4-((6bR,10aS)-1,1,2,2-d4-3-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, in free base, co-crystal or salt form, together with methods of making and using them.

公开(公告)号：US20170319580A1

公开(公告)日：2017-11-09

申请号：US15660615

申请日：2017-07-26

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Wei YAO ,  Peng LI ,  Robert DAVIS ,  Sharon MATES ,  Kimberly VANOVER ,  Gretchen SNYDER

IPC: A61K31/4985 ,  A61K45/00 ,  A61K9/16 ,  C07D241/40 ,  A61K9/00

CPC classification number: A61K31/4985 ,  A61K9/0019 ,  A61K9/16 ,  A61K31/445 ,  A61K45/00 ,  A61K45/06 ,  C07D241/40

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 the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and/or the μ-opioid receptor.