公开(公告)号：US09630971B2

公开(公告)日：2017-04-25

申请号：US14900589

申请日：2014-06-20

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  INTRA-CELLULAR THERAPIES, INC.

Inventor： Takashi Abe ,  Graham Buckton ,  Robert Davis ,  Mark Hooper ,  Peng Li ,  Hideaki Maruyama ,  Masahiro Takasuga ,  Lawrence P. Wennogle ,  Yuhei Yamamoto ,  Hironori Yamashita

IPC: A61K31/519 ,  C07D487/14

CPC classification number: C07D487/14

Abstract: The present invention relates to crystals of (6aR,9aS)-5,6a,7,8,9,9a-hexahydro-5-methyl-3-(phenylamino)-2-((4-(6-fluoropyridin-2-yl)phenyl)methyl)-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one, and methods of making and using such crystals.

公开(公告)号：US12297200B2

公开(公告)日：2025-05-13

申请号：US17415400

申请日：2019-12-17

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li

IPC: C07D471/16 ,  C07D471/04

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：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：US12194044B2

公开(公告)日：2025-01-14

申请号：US18339956

申请日：2023-06-22

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Wei Yao ,  Peng Li

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

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.

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：US12139490B2

公开(公告)日：2024-11-12

申请号：US17808836

申请日：2022-06-24

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： John Charles Tomesch ,  Peng Li ,  Wei Yao ,  Qiang Zhang ,  James David Beard ,  Andrew S. Thompson ,  Hua Cheng ,  Lawrence P. Wennogle

IPC: C07D471/16 ,  C07D471/04

Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines, such as the compound of Formula 2J, as shown below, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines, and as further defined herein.

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.

公开(公告)号：US11957791B2

公开(公告)日：2024-04-16

申请号：US17270573

申请日：2019-08-30

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Robert Davis ,  William Paul Findlay

IPC: A61K9/20 ,  A61K9/28 ,  A61K31/4985

CPC classification number: A61K9/2013 ,  A61K9/2009 ,  A61K9/2054 ,  A61K9/284 ,  A61K31/4985 ,  C07B2200/13

Abstract: The present disclosure relates to solid oral dosage forms 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：US11806348B2

公开(公告)日：2023-11-07

申请号：US17582516

申请日：2022-01-24

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Robert Davis

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

CPC classification number: A61K31/4985 ,  A61K9/0053 ,  A61K9/16 ,  A61K9/485 ,  A61K9/4825 ,  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：US11453670B2

公开(公告)日：2022-09-27

申请号：US16438163

申请日：2019-08-16

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Qiang Zhang

IPC: 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.