公开(公告)号：US12240850B2

公开(公告)日：2025-03-04

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

Abstract: The invention relates to pharmaceutical compositions comprising compounds of Formula Q: wherein W is —N(CH3)—, and Y is —CH(OH)—, 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：US12195462B2

公开(公告)日：2025-01-14

申请号：US17415565

申请日：2019-12-17

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Qiang Zhang ,  Robert Davis

IPC: C07D471/16 ,  A61K9/16

Abstract: The invention relates to a particular substituted heterocycle fused gamma-carboline, in free, or 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), and/or pathways involving the dopamine D1 and D2 receptor signaling system.

公开(公告)号：US11491150B2

公开(公告)日：2022-11-08

申请号：US15986485

申请日：2018-05-22

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Youyi Peng ,  Lawrence P. Wennogle ,  Qiang Zhang

IPC: A61K31/454 ,  A61P13/12 ,  A61P3/10

Abstract: The disclosure relates to compounds and methods of treatment relating to nicotinic receptor antagonists. For example, the compounds and methods of treatment function block the activity of certain acetylcholine receptors and subtypes therein, and are useful treating diseases and conditions mediated by nicotinic receptor stimulation, e.g., diabetes mellitus, chronic kidney disease, acute kidney failure, and reduction of blood glucose levels.

公开(公告)号：US11407751B2

公开(公告)日：2022-08-09

申请号：US16594603

申请日：2019-10-07

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： John Charles Tomesch ,  Peng Li ,  Qiang Zhang ,  Andrew S. Thompson

IPC: C07D471/16 ,  C07D471/04

Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines, such as 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：US10472359B2

公开(公告)日：2019-11-12

申请号：US16056143

申请日：2018-08-06

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

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-one in toluenesulfonic acid addition salt form: 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：US10464938B2

公开(公告)日：2019-11-05

申请号：US16439361

申请日：2019-06-12

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: A61K31/4353 ,  C07D471/06 ,  C07D471/16 ,  C07D471/04

Abstract: The present invention provides pharmaceutical compositions comprising certain optionally substituted heterocycle fused gamma-carbolines of Formula 2J, as shown below, and as further defined herein:

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：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：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.