公开(公告)号：US11773095B2

公开(公告)日：2023-10-03

申请号：US17813473

申请日：2022-07-19

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Hailin Zheng ,  Robert Davis ,  Sharon Mates ,  Kimberly Vanover ,  Gretchen Snyder

IPC: A61K31/4985 ,  C07D471/16 ,  A61P25/36 ,  A61P1/00 ,  A61P11/00 ,  A61P29/00 ,  A61K45/06

CPC classification number: C07D471/16 ,  A61K45/06 ,  A61P1/00 ,  A61P11/00 ,  A61P25/36 ,  A61P29/00 ,  A61K31/485 ,  A61K2300/00 ,  A61K31/4985 ,  A61K2300/00 ,  A61K31/137 ,  A61K2300/00

Abstract: The invention relates to particular prodrugs of substituted heterocycle fused gamma-carbolines, 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：US11053245B2

公开(公告)日：2021-07-06

申请号：US14394469

申请日：2013-04-14

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：US12195463B2

公开(公告)日：2025-01-14

申请号：US17416997

申请日：2019-12-20

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Kimberly Vanover ,  Robert Davis

IPC: C07D471/16 ,  A61P25/00

Abstract: The invention relates to a particular enantiomer of a substituted heterocycle fused gamma-carboline, 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, and pathways involving the dopamine D1 and D2 receptor signaling system.

公开(公告)号：US12173004B2

公开(公告)日：2024-12-24

申请号：US18451465

申请日：2023-08-17

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Hailin Zheng ,  Robert Davis ,  Sharon Mates ,  Kimberly Vanover ,  Gretchen Snyder

IPC: A61K31/4985 ,  A61K45/06 ,  A61P1/00 ,  A61P11/00 ,  A61P25/36 ,  A61P29/00 ,  C07D471/16

Abstract: The invention relates to particular prodrugs of substituted heterocycle fused gamma-carbolines, 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：US20240327436A1

公开(公告)日：2024-10-03

申请号：US18741739

申请日：2024-06-12

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert E. DAVIS ,  Kimberly Vanover

IPC: C07D519/00

CPC classification number: C07D519/00

Abstract: The invention relates to pharmaceutical compositions comprising the compound of Formula I,




and new methods and uses pertaining thereto, and pharmaceutical compositions thereof, such as methods of use in the treatment of diseases involving the 5-HT receptor, the serotonin transporter (SERT), and/or pathways involving dopamine D2 receptor signaling, sodium channel activity, and/or norepinephrine transporter activity.

公开(公告)号：US12090155B2

公开(公告)日：2024-09-17

申请号：US18494754

申请日：2023-10-25

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon Mates ,  Robert Davis ,  Kimberly Vanover

IPC: A61K31/4985 ,  A61K9/20 ,  A61K9/48 ,  A61P25/18 ,  A61K45/06

CPC classification number: A61K31/4985 ,  A61K9/20 ,  A61K9/48 ,  A61P25/18 ,  A61K45/06

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：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：US11753419B2

公开(公告)日：2023-09-12

申请号：US17757212

申请日：2020-12-10

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Robert E Davis ,  Kimberly Vanover

IPC: A61K31/4985 ,  C07D471/22 ,  C07D487/22 ,  C07D519/00

CPC classification number: C07D519/00

Abstract: The invention relates to a particular substituted heterocycle fused gamma carboline, the compound of Formula I,




and new methods and uses pertaining thereto, and pharmaceutical compositions thereof, such as methods of use in the treatment of diseases involving the 5-HT receptor, the serotonin transporter (SERT), and/or pathways involving dopamine D2 receptor signaling, sodium channel activity, and/or norepinephrine transporter activity.

公开(公告)号：US11026951B2

公开(公告)日：2021-06-08

申请号：US16507956

申请日：2019-07-10

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

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：US10960010B2

公开(公告)日：2021-03-30

申请号：US16443240

申请日：2019-06-17

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

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.