公开(公告)号：US20140050783A1

公开(公告)日：2014-02-20

申请号：US14066987

申请日：2013-10-30

Applicant: INTRA-CELLULAR THERAPIES INC.

Inventor： Sharon MATES ,  Allen FIENBERG ,  Lawrence P. WENNOGLE

IPC: A61K31/5383 ,  A61K31/4985 ,  C07D471/14 ,  C07D498/14 ,  A61K45/06

CPC classification number: A61K31/4985 ,  A61K9/0053 ,  A61K31/198 ,  A61K31/44 ,  A61K31/5383 ,  A61K45/06 ,  C07D471/14 ,  C07D498/14

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.

Abstract translation: 公开了使用特定的取代的杂环稠合的γ-咔啉化合物作为药物和包含它们的药物组合物用于治疗涉及5-HT2A，SERT和/或多巴胺D2途径的一种或多种病症。 此外，化合物可以与其它治疗剂组合用于治疗一种或多种睡眠障碍，抑郁症，精神病，运动障碍和/或帕金森病或任何组合。

公开(公告)号：US20250127779A1

公开(公告)日：2025-04-24

申请号：US19005181

申请日：2024-12-30

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

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：US12269825B2

公开(公告)日：2025-04-08

申请号：US18067387

申请日：2022-12-16

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

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：US20250101029A1

公开(公告)日：2025-03-27

申请号：US18847121

申请日：2023-03-14

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert E. DAVIS ,  Gretchen SNYDER ,  Allen A. FIENBERG

IPC: C07D487/14 ,  A61K31/4985

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：US20250092045A1

公开(公告)日：2025-03-20

申请号：US18968542

申请日：2024-12-04

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Qiang ZHANG ,  Robert E. DAVIS

IPC: C07D471/16 ,  A61K9/16

Abstract: The invention relates to a particular substituted heterocycle fused gamma-carboline, in free, or 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), and/or pathways involving the dopamine D1 and D2 receptor signaling system.

公开(公告)号：US20240327409A1

公开(公告)日：2024-10-03

申请号：US18741740

申请日：2024-06-12

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Qiang ZHANG

IPC: C07D471/16 ,  C07D519/00

CPC classification number: C07D471/16 ,  C07D519/00

Abstract: The present invention provides improved 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.

公开(公告)号：US20240307386A1

公开(公告)日：2024-09-19

申请号：US18670391

申请日：2024-05-21

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: A61K31/4985 ,  A61K45/06 ,  A61P25/22 ,  A61P25/24

CPC classification number: A61K31/4985 ,  A61P25/22 ,  A61P25/24 ,  A61K45/06

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/mu-opioid receptor or 5-HT2A/D1 and/or D2/mu-opioid receptor ligand.

公开(公告)号：US20240279228A1

公开(公告)日：2024-08-22

申请号：US18567743

申请日：2022-06-07

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI

IPC: C07D471/16 ,  A61K31/4985

CPC classification number: C07D471/16 ,  A61K31/4985

Abstract: The disclosure provides new salts, crystals and co-crystal forms of particular substituted heterocycle fused gamma-carbolines, as described herein, together with methods of making and using them, and pharmaceutical compositions comprising them.

公开(公告)号：US20240091232A1

公开(公告)日：2024-03-21

申请号：US18501330

申请日：2023-11-03

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： David KASS ,  Toru HASHIMOTO ,  Lawrence P. WENNOGLE ,  Joseph HENDRICK ,  Robert DAVIS

IPC: A61K31/519 ,  A61K9/00 ,  A61K31/197 ,  A61K31/216 ,  A61K31/41 ,  A61K31/4178 ,  A61K31/7056 ,  A61K45/06 ,  A61P9/04

CPC classification number: A61K31/519 ,  A61K9/0053 ,  A61K31/197 ,  A61K31/216 ,  A61K31/41 ,  A61K31/4178 ,  A61K31/7056 ,  A61K45/06 ,  A61P9/04

Abstract: The disclosure provides methods, treatments and materials for enhancing the effect of an adenosine A2 receptor agonist in the treatment, mitigation or prophylaxis of a disease or condition characterized by inotropic and/or lusitropic dysfunction, and/or enhancing adenosine A2 receptor function in the treatment, mitigation or prophylaxis of a disease or condition characterized by impaired adenosine A2 receptor function, comprising administration of an effective amount of a PDE1 inhibitor to a patient in need thereof, for example a patient suffering from heart failure.

公开(公告)号：US20240024334A1

公开(公告)日：2024-01-25

申请号：US18481168

申请日：2023-10-04

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

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

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.