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：US10300064B2

公开(公告)日：2019-05-28

申请号：US15533527

申请日：2015-12-07

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Hailin Zheng ,  Gretchen Snyder ,  Lawrence P. Wennogle ,  Joseph Hendrick

IPC: C07D487/04 ,  C07D403/14 ,  C07D401/14 ,  A61K31/519 ,  A61P25/28 ,  A61P9/12 ,  C07D231/06 ,  C07D231/54

Abstract: The present invention relates to certain PDE2 inhibitory compounds, in free or salt form, pharmaceutical compositions containing such compounds and methods for the treatment of PDE2 mediated disorders.

公开(公告)号：US09938284B2

公开(公告)日：2018-04-10

申请号：US15502455

申请日：2015-08-06

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Hailin Zheng ,  Jun Zhao ,  Lawrence P. Wennogle

IPC: C07D487/14

CPC classification number: C07D487/14

Abstract: The invention relates to novel inhibitors of phosphodiesterase 1 (PDE1), useful for the treatment of diseases or disorders characterized by disruption of or damage to certain cGMP/PKG mediated pathways (e.g., in cardiac tissue). The invention further relates to pharmaceutical composition comprising the same and methods of treatment of cardiovascular disease and related disorders, e.g., congestive heart disease, atherosclerosis, myocardial infarction, and stroke.

公开(公告)号：US09556186B2

公开(公告)日：2017-01-31

申请号：US14731233

申请日：2015-06-04

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Hailin Zheng ,  Jun Zhao ,  Lawrence P. Wennogle

IPC: C07D487/14 ,  A61K31/519 ,  A61K45/06 ,  A61K31/5575

CPC classification number: A61K31/519 ,  A61K31/5575 ,  A61K31/57 ,  A61K45/06 ,  C07D487/14

Abstract: Provided are PDE1 inhibitors of Formula I, processes for their production, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

Abstract translation: 提供式I的PDE1抑制剂，其制备方法，其作为药物的用途，以及包含它们的药物组合物。

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：US09598426B2

公开(公告)日：2017-03-21

申请号：US14777446

申请日：2014-03-13

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Hailin Zheng ,  Jun Zhao ,  Lawrence Wennogle

IPC: C07D487/14 ,  A61K31/519 ,  A61K45/06 ,  A61K31/5575

CPC classification number: A61K31/519 ,  A61K31/5575 ,  A61K31/57 ,  A61K45/06 ,  C07D487/14

Abstract: Provided are PDE1 inhibitors of Formula I, processes for their production and their use as pharmaceuticals, and pharmaceutical compositions comprising them.

公开(公告)号：US12180210B2

公开(公告)日：2024-12-31

申请号：US17288225

申请日：2019-10-23

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Hailin Zheng

IPC: C07D487/04 ,  A61P25/00

Abstract: The present disclosure relates to novel PDE2 inhibitory compounds of Formula I as described herein, their use as pharmaceuticals and pharmaceutical compositions comprising them.

公开(公告)号：US10543194B2

公开(公告)日：2020-01-28

申请号：US16125373

申请日：2018-09-07

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Hailin Zheng ,  Gretchen Snyder ,  Lawrence P. Wennogle ,  Joseph Hendrick

IPC: A61K31/4162 ,  C07D471/14 ,  C07D209/58 ,  C07D403/14

Abstract: The present invention relates to certain PDE2 inhibitory compounds, in free or salt form, pharmaceutical compositions containing such compounds and methods for the treatment of PDE2 mediated disorders.

公开(公告)号：US10105349B2

公开(公告)日：2018-10-23

申请号：US15533525

申请日：2015-12-07

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Hailin Zheng ,  Gretchen Snyder ,  Lawrence P. Wennogle ,  Joseph Hendrick

IPC: A61K31/4162 ,  C07D471/14 ,  C07D403/14 ,  C07D209/58

Abstract: The present invention relates to certain PDE2 inhibitory compounds, in free or salt form, pharmaceutical compositions containing such compounds and methods for the treatment of PDE2 mediated disorders.

公开(公告)号：US10005789B2

公开(公告)日：2018-06-26

申请号：US15502464

申请日：2015-08-06

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Hailin Zheng ,  Jun Zhao ,  Lawrence P. Wennogle

IPC: A01N43/54 ,  A61K31/505 ,  C07D487/14 ,  A61K31/519 ,  A61K45/06

CPC classification number: C07D487/14 ,  A61K31/519 ,  A61K45/06

Abstract: The invention relates to novel inhibitors of phosphodiesterase 1 (PDE1), according to Formula I, below, wherein R1, R2, R3 and R4 are as defined herein, useful for the treatment of diseases or disorders characterized by disruption of or damage to certain cGMP/PKG mediated pathways (e.g., in cardiac tissue). The invention further relates to pharmaceutical composition comprising the same and methods of treatment of cardiovascular disease and related disorders, e.g., congestive heart disease, atherosclerosis, myocardial infarction, and stroke.