公开(公告)号：US20170037048A1

公开(公告)日：2017-02-09

申请号：US15301895

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 ,  C07B59/00 ,  A61K45/06

CPC classification number: C07D471/16 ,  A61K31/4985 ,  A61K45/06 ,  C07B59/002 ,  C07B2200/05

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.

Abstract translation: 本发明涉及如本文所述的游离，固体，药学上可接受的盐和/或基本上纯的形式的特定取代的杂环稠合的γ-咔啉及其前药，其药物组合物，以及用于治疗涉及5-HT2A 受体，血清素转运蛋白（SERT）和/或涉及多巴胺D1 / D2受体信号传导系统的途径和/或残留症状的治疗。

公开(公告)号：US20240374586A1

公开(公告)日：2024-11-14

申请号：US18777765

申请日：2024-07-19

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon MATES ,  Robert DAVIS ,  Kimberly VANOVER

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

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：US20240207259A1

公开(公告)日：2024-06-27

申请号：US18596349

申请日：2024-03-05

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert DAVIS

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

CPC classification number: A61K31/4985 ,  A61K9/0053 ,  A61K9/16 ,  A61K9/4825 ,  A61K9/485 ,  A61K9/4858 ,  A61K9/4891

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：US20240165111A1

公开(公告)日：2024-05-23

申请号：US18502460

申请日：2023-11-06

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: A61K31/4985 ,  A61K9/00 ,  A61K9/16 ,  A61K31/445 ,  A61K45/00 ,  A61K45/06 ,  A61P25/00 ,  C07D241/40 ,  C07D471/16

CPC classification number: A61K31/4985 ,  A61K9/0019 ,  A61K9/16 ,  A61K31/445 ,  A61K45/00 ,  A61K45/06 ,  A61P25/00 ,  C07D241/40 ,  C07D471/16

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 Di and D2 receptor signaling system, and/or the wopioid receptor.

公开(公告)号：US20240066030A1

公开(公告)日：2024-02-29

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

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：US20240033262A1

公开(公告)日：2024-02-01

申请号：US18478482

申请日：2023-09-29

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert DAVIS

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

CPC classification number: A61K31/4985 ,  A61K9/4858 ,  A61K9/4825 ,  A61K9/0053 ,  A61K9/4891 ,  A61K9/16 ,  A61K9/485

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：US20220356187A1

公开(公告)日：2022-11-10

申请号：US17753472

申请日：2020-09-03

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert DAVIS

IPC: C07D487/14 ,  A61K38/00

Abstract: The present invention relates to PDE1 inhibitory compounds useful in the treatment of diseases involving disorders of the dopamine D1 receptor intracellular pathway, such as, among others, Parkinson's disease, depression, narcolepsy, psychosis, damage to cognitive function, e.g., in schizophrenia, or disorders that may be ameliorated through enhanced progesterone-signaling pathway, as well as their use as pharmaceuticals and pharmaceutical compositions comprising them. Methods of making and methods of use related to such compounds are further described.

公开(公告)号：US20220184240A1

公开(公告)日：2022-06-16

申请号：US17594356

申请日：2020-04-10

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: A61K51/04 ,  C07D487/14

Abstract: The present invention relates to novel compounds having a capacity for PDE1 inhibition which may be used as tracers for use in diagnostic techniques, biomarkers for phosphodiesterase 1 (PDE1) in vivo, methods for treating and/or developing novel therapies for PDE1-associated conditions, and to methods of detection and treatment.

公开(公告)号：US20220072003A1

公开(公告)日：2022-03-10

申请号：US17421303

申请日：2020-01-07

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Gretchen SNYDER ,  Lawrence P. WENNOGLE ,  Jennifer O'BRIEN ,  Joseph HENDRICK ,  Robert DAVIS

IPC: A61K31/519 ,  A61P35/00

Abstract: The disclosure relates to the use of phosphodiesterase 1 (PDE1) inhibitors for the treatment of cancers and tumors, including for inhibiting tumor recruitment of macrophages and other cells to the tumor or cancer, for complementing and enhancing checkpoint inhibitor therapies, and for mitigating the side effects (i.e., inflammatory-related adverse events) associated with checkpoint inhibitor therapies.

公开(公告)号：US20210315891A1

公开(公告)日：2021-10-14

申请号：US17271965

申请日：2019-08-29

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert DAVIS

IPC: A61K31/4985 ,  A61K9/70

Abstract: The disclosure provides new transdermal 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.