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：US11839614B2

公开(公告)日：2023-12-12

申请号：US16966818

申请日：2019-01-31

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

CPC classification number: A61K31/519 ,  A61K9/0053 ,  A61K31/04 ,  A61K31/197 ,  A61K31/216 ,  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：US11806347B2

公开(公告)日：2023-11-07

申请号：US17338573

申请日：2021-06-03

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Wei Yao ,  Robert Davis

IPC: A61K31/498 ,  A61K31/4985 ,  A61K9/06 ,  A61K9/00

CPC classification number: A61K31/4985 ,  A61K9/006 ,  A61K9/0036 ,  A61K9/0043 ,  A61K9/06

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：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：US11680065B2

公开(公告)日：2023-06-20

申请号：US17072933

申请日：2020-10-16

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Qiang Zhang ,  Robert Davis ,  Lawrence P. Wennogle

IPC: A61K31/437 ,  C07D471/22 ,  C07D471/16 ,  C07D471/14 ,  A61K9/50 ,  A61K9/48 ,  A61K31/4985 ,  A61K47/34 ,  A61K47/38

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

Abstract: The invention relates to pharmaceutical compositions comprising, compounds of Formula Q:




wherein W is —N(H)—, or —N(CH3)—, and Y is —C(═O)— or —O—, in free base or pharmaceutically acceptable salt form, 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：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：US10597394B2

公开(公告)日：2020-03-24

申请号：US16054728

申请日：2018-08-03

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

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：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：US12128043B2

公开(公告)日：2024-10-29

申请号：US18602981

申请日：2024-03-12

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.