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：US10188758B2

公开(公告)日：2019-01-29

申请号：US15560107

申请日：2016-03-18

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: C07D213/65 ,  C07D213/69 ,  A61K31/44 ,  A61K51/04 ,  A61P25/22 ,  A61P25/24

Abstract: The present invention relates to novel pyridinoxy phenylpropanamines, their pharmaceutical compositions and methods of use. In addition, the present invention relates to therapeutic methods that penetrate the blood-brain barrier and regulate the norepinephrine and serotonin transporters (“NET/SERT”).

公开(公告)号：US10150774B2

公开(公告)日：2018-12-11

申请号：US15512005

申请日：2015-09-17

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: C07D487/14

Abstract: The subject matter generally relates to compounds and methods of treatment and/or prophylaxis of CNS diseases, disorders, and/or injuries. In one aspect, the subject matter relates to inhibitors of phosphodiesterase 1 (PDE1) as neuroprotective agents and/or neural regenerative agents. In a further aspect, the subject matter relates to individuals that are at risk for the development of CNS disease or disorder.

公开(公告)号：US10131671B2

公开(公告)日：2018-11-20

申请号：US15502144

申请日：2015-08-07

Applicant: Intra-Cellular Therapies, Inc.

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

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

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：US09546175B2

公开(公告)日：2017-01-17

申请号：US14820248

申请日：2015-08-06

Applicant: Intra-Cellular Therapies, Inc.

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

IPC: C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  A61K31/00

CPC classification number: C07D487/04 ,  A61K31/00 ,  A61K31/519 ,  A61K45/06 ,  A61K2300/00

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.

Abstract translation: 本发明涉及磷酸二酯酶1（PDE1）的新型抑制剂，其可用于治疗特征在于某些cGMP / PKG介导的途径的破坏或损伤（例如在心脏组织中）的疾病或病症。 本发明还涉及包含其的药物组合物和治疗心血管疾病和相关疾病例如充血性心脏病，动脉粥样硬化，心肌梗塞和中风的方法。

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：US20170226117A1

公开(公告)日：2017-08-10

申请号：US15502144

申请日：2015-08-07

Applicant: Intra-Cellular Therapies, Inc.

Inventor： Peng LI ,  Hailin ZHENG ,  Jun Zhao ,  Lawrence P. Wennogle

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

CPC classification number: C07D487/14 ,  A61K31/519 ,  A61K45/06 ,  A61K2300/00

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：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.