公开(公告)号：US09849132B2

公开(公告)日：2017-12-26

申请号：US15110640

申请日：2015-01-08

Applicant: Intra-Cellular Therapies, Inc.

Inventor： Joseph Hendrick ,  Jennifer O'Brien ,  Gretchen Snyder ,  Peng Li ,  Lawrence P. Wennogle

IPC: A61K31/519 ,  A61K31/53 ,  A61K45/06 ,  C07D487/04 ,  C07D487/14 ,  A61K9/00

CPC classification number: A61K31/519 ,  A61K9/0048 ,  A61K31/53 ,  A61K45/06 ,  C07D487/04 ,  C07D487/14 ,  A61K2300/00

Abstract: The present invention relates to a product comprising a PDE1 inhibitor and a PDE2 inhibitor, in free or salt form, pharmaceutical compositions comprising them and their use as pharmaceuticals for the treatment of cAMP and/or cGMP related disorders.

公开(公告)号：US09745300B2

公开(公告)日：2017-08-29

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 ,  A61K45/06 ,  C07B59/00

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.

公开(公告)号：US09708322B2

公开(公告)日：2017-07-18

申请号：US14777466

申请日：2014-03-15

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

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

Abstract: The invention relates to substituted heterocycle fused gamma-carbolines of the Formula Q as described herein, in free base or pharmaceutically acceptable salt form, and/or pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor pathway, the serotonin transporter (SERT) pathway and/or the dopamine D2 receptor pathway signaling systems.

公开(公告)号：US20160310502A1

公开(公告)日：2016-10-27

申请号：US15101874

申请日：2014-12-03

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: A61K31/5383 ,  A61K9/00 ,  A61K31/4985 ,  A61K45/06

CPC classification number: A61K31/5383 ,  A61K9/0019 ,  A61K9/0024 ,  A61K9/5153 ,  A61K31/4985 ,  A61K45/06 ,  A61K2300/00

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.

Abstract translation: 本公开提供了特定的取代的杂环稠合的γ-咔啉化合物作为用于治疗精神病或精神分裂症残留症状的药物的用途。 本公开还提供了特定取代的杂环稠合γ-咔啉化合物的新型长效注射制剂，以及使用这种长效注射制剂来治疗精神病或精神分裂症的残留症状。

公开(公告)号：US09371324B2

公开(公告)日：2016-06-21

申请号：US14627968

申请日：2015-02-20

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon Mates ,  Robert Davis ,  Lawrence P. Wennogle ,  Peng Li ,  John Charles Tomesch ,  Qiang Zhang

IPC: A61K31/4985 ,  C07D241/38 ,  C07D471/16 ,  C07D471/04 ,  A61K31/44

CPC classification number: C07D471/16 ,  A61K31/44 ,  C07D471/04

Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, of Formula I as described herein, 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 D2 receptor signaling systems, such as diseases of the central nervous system.

Abstract translation: 本发明涉及如本文所述的本发明式I的特定的取代的杂环稠合的γ-咔啉，其前药具有本文所述的游离，固体，药学上可接受的盐和/或基本上纯的形式，其药物组合物，以及在 治疗涉及5-HT2A受体，血清素转运蛋白（SERT）和/或涉及多巴胺D2受体信号传导系统的途径（例如中枢神经系统疾病）的疾病。

公开(公告)号：US20160031885A1

公开(公告)日：2016-02-04

申请号：US14777466

申请日：2014-03-15

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

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

Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, their prodrugs, in free, 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 D2 receptor signaling systems.

Abstract translation: 本发明涉及特定的取代的杂环稠合的γ-咔啉，它们的前药，如本文所述的游离的，药学上可接受的盐和/或基本上纯的形式，其药物组合物，以及用于治疗涉及5-HT2A受体的疾病的方法， 血清素转运蛋白（SERT）和/或涉及多巴胺D2受体信号传导系统的途径。

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：US11826367B2

公开(公告)日：2023-11-28

申请号：US17659063

申请日：2022-04-13

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li

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

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：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.