公开(公告)号：US20240208974A1

公开(公告)日：2024-06-27

申请号：US18601923

申请日：2024-03-11

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon MATES ,  Robert DAVIS ,  Kimberly VANOVER ,  Lawrence WENNOGLE

IPC: C07D471/14 ,  A61K31/445 ,  A61K31/4985 ,  A61K31/5383 ,  A61K45/06 ,  A61P25/28 ,  C07D471/16

CPC classification number: C07D471/14 ,  A61K31/445 ,  A61K31/4985 ,  A61K31/5383 ,  A61K45/06 ,  A61P25/28 ,  C07D471/16

Abstract: The present invention relates to use of particular substituted heterocycle fused gamma-carbolines as described herein, in free, pharmaceutically acceptable salt or prodrug form, and pharmaceutical composition comprising the same optionally in combination with one or more agents, for the prophylaxis or treatment of one or more disorders associated with dementia, particularly behavioral or mood disturbances (e.g., agitation/aggression), psychosis, depression and sleep disturbances among others in patients suffering from dementia.

公开(公告)号：US20240101569A1

公开(公告)日：2024-03-28

申请号：US18263302

申请日：2022-01-27

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI

IPC: C07D487/14

CPC classification number: C07D487/14

Abstract: The present disclosure relates to free base and salt crystals of 2-(4-acetylbenzyl)-3-((4-fluorophenyl)amino)-5,7,7-trimethyl-7,8-dihydro-2H-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one, composition comprising the same and the method of making and using such free base and salt crystals.

公开(公告)号：US20240059687A1

公开(公告)日：2024-02-22

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

CPC classification number: C07D471/16 ,  A61K45/06 ,  A61P1/00 ,  A61P11/00 ,  A61P25/36 ,  A61P29/00

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：US11872223B2

公开(公告)日：2024-01-16

申请号：US17655143

申请日：2022-03-16

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li

IPC: A61K31/4985 ,  A61K9/20 ,  A61K9/16 ,  A61K9/00 ,  A61K47/38 ,  A61P25/28 ,  A61P25/22 ,  A61P3/04 ,  A61P25/18 ,  A61P25/24 ,  A61P25/06 ,  A61K9/48 ,  C07D471/16 ,  A61K9/10

CPC classification number: A61K31/4985 ,  A61K9/0019 ,  A61K9/0024 ,  A61K9/0053 ,  A61K9/1617 ,  A61K9/1635 ,  A61K9/1641 ,  A61K9/1652 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/4858 ,  A61K9/4866 ,  A61K47/38 ,  A61P3/04 ,  A61P25/06 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61K9/10 ,  C07D471/16

Abstract: The disclosure provides new, stable, pharmaceutically acceptable amorphous solid dispersions of 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, together with methods of making and using them, and pharmaceutical compositions comprising them.

公开(公告)号：US20240000781A1

公开(公告)日：2024-01-04

申请号：US18468199

申请日：2023-09-15

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li

IPC: A61K31/4985 ,  A61K9/20 ,  A61K9/16 ,  A61K9/00 ,  A61K47/38 ,  A61P25/28 ,  A61P25/22 ,  A61P3/04 ,  A61P25/18 ,  A61P25/24 ,  A61P25/06 ,  A61K9/48

CPC classification number: A61K31/4985 ,  A61K9/2013 ,  A61K9/2027 ,  A61K9/2031 ,  A61K9/2054 ,  A61K9/1635 ,  A61K9/1641 ,  A61K9/1617 ,  A61K9/1652 ,  A61K9/0019 ,  A61K9/0053 ,  A61K47/38 ,  A61P25/28 ,  A61P25/22 ,  A61P3/04 ,  A61P25/18 ,  A61P25/24 ,  A61P25/06 ,  A61K9/0024 ,  A61K9/4858 ,  A61K9/4866 ,  C07D471/16

Abstract: The disclosure provides new, stable, pharmaceutically acceptable amorphous solid dispersions of 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, together with methods of making and using them, and pharmaceutical compositions comprising them.

公开(公告)号：US11844757B2

公开(公告)日：2023-12-19

申请号：US17015883

申请日：2020-09-09

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Wei Yao ,  Peng Li ,  Robert Davis ,  Sharon Mates ,  Kimberly Vanover ,  Gretchen Snyder

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

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 D1 and D2 receptor signaling system, and/or the μ-opioid receptor.

公开(公告)号：US20230372336A1

公开(公告)日：2023-11-23

申请号：US18320173

申请日：2023-05-18

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sophie DUTHEIL ,  Gretchen SNYDER ,  Peng LI ,  Robert E. DAVIS

IPC: A61K31/4985 ,  A61P25/00 ,  A61P25/18

CPC classification number: A61K31/4985 ,  A61P25/00 ,  A61P25/18

Abstract: The disclosure provides methods the treatment of psychiatric disorders caused by viral, bacterial, or autoimmune encephalitis, and for treatment of psychiatric symptoms of viral, bacterial, and autoimmune encephalitis, and for protecting or reinforcing the blood-brain barrier, comprising administering to a patient in need thereof, a therapeutically effective amount of a 5-HT2A.

公开(公告)号：US20230338385A1

公开(公告)日：2023-10-26

申请号：US18344406

申请日：2023-06-29

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

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

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：US11759465B2

公开(公告)日：2023-09-19

申请号：US16892206

申请日：2020-06-03

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： David Kass ,  Toru Hashimoto ,  Lawrence P. Wennogle ,  Joseph Hendrick ,  Robert Davis

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

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：US11723909B2

公开(公告)日：2023-08-15

申请号：US17379399

申请日：2021-07-19

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Wei Yao ,  Peng Li

IPC: A61K31/519 ,  C07D471/14 ,  A61P25/28 ,  A61K31/4985 ,  A61K45/06 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24

CPC classification number: A61K31/519 ,  A61K31/4985 ,  A61K45/06 ,  A61P25/00 ,  A61P25/18 ,  A61P25/24 ,  A61P25/28 ,  C07D471/14 ,  A61K31/4985 ,  A61K2300/00

Abstract: The invention relates to particular substituted deuterated 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.