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：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.

公开(公告)号：US20230355625A1

公开(公告)日：2023-11-09

申请号：US17780660

申请日：2020-11-25

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Kimberly VANOVER ,  Robert DAVIS ,  Peng LI

IPC: A61K31/519 ,  A61K45/06 ,  A61P25/28

CPC classification number: A61K31/519 ,  A61K45/06 ,  A61P25/28

Abstract: The present disclosure relates to inhibitors of phosphodiesterase 1 (PDE1) useful for the engagement with the central nervous system. The disclosure further relates to the administration of inhibitors of phosphodiesterase 1 (PDE1) for the treatment of a condition, disease or disorder associated with the dopamine D1 receptor intracellular pathway, e.g., a condition, disease or disorder characterized by a deficit in attention, cognition, memory and/or inhibitory processing.

公开(公告)号：US20230271962A1

公开(公告)日：2023-08-31

申请号：US18314785

申请日：2023-05-09

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

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

Abstract: The invention relates to pharmaceutical compositions comprising 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)-1-(4-fluorophenyl)-butan-1-ol, and methods of use in the treatment of diseases involving 5-HT2A receptor, serotonin transporter (SERT) pathway and/or the dopamine D2 receptor pathway, and methods of treating conditions of the central nervous system therewith.

公开(公告)号：US20220354851A1

公开(公告)日：2022-11-10

申请号：US17640050

申请日：2020-09-03

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Robert DAVIS

IPC: A61K31/519 ,  A61K31/505 ,  A61K38/00 ,  A61P35/00

Abstract: The disclosure relates to the combination of inhibitors of phosphodiesterase 1 (PDE1) useful for the treatment of certain cancers or tumors, such as colon cancer. In another embodiment, the disclosure relates to the use of inhibitors of PDE1 and an optional antitumor agent for the treatment of certain cancers or tumors.

公开(公告)号：US20210361648A1

公开(公告)日：2021-11-25

申请号：US17338573

申请日：2021-06-03

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Wei YAO ,  Robert DAVIS

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

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：US20210205310A1

公开(公告)日：2021-07-08

申请号：US17059160

申请日：2019-05-24

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Lawrence P. WENNOGLE ,  Joseph HENDRICK ,  Robert DAVIS

IPC: A61K31/519 ,  A61P35/00

Abstract: The disclosure relates to the combination of inhibitors of phosphodiesterase 1 (PDE1) useful for the treatment of certain cancers or tumors, such as gliomas. In another embodiment, the disclosure relates to the combination of inhibitors of PDE1 and an antitumor agent for the treatment of certain cancers or tumors, such as gliomas.

公开(公告)号：US20210188850A1

公开(公告)日：2021-06-24

申请号：US17124224

申请日：2020-12-16

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

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：US20210093634A1

公开(公告)日：2021-04-01

申请号：US17115416

申请日：2020-12-08

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: A61K31/4985 ,  A61P25/22 ,  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/mu-opioid receptor or 5-HT2A/D1 and/or D2/mu-opioid receptor ligand.