公开(公告)号：US10960009B2

公开(公告)日：2021-03-30

申请号：US16392409

申请日：2019-04-23

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: A61K9/00 ,  A61K9/51 ,  A61K31/5383 ,  A61K45/06 ,  A61K31/4985

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.

公开(公告)号：US10899762B2

公开(公告)日：2021-01-26

申请号：US16786240

申请日：2020-02-10

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: C07D471/16 ,  C07D471/14 ,  A61K45/06 ,  A61K31/4985 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  C07B59/00

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：US10654854B2

公开(公告)日：2020-05-19

申请号：US16090144

申请日：2017-03-28

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Edwin Aret

IPC: C07D471/16 ,  A61P25/18

Abstract: The disclosure provides new, stable, pharmaceutically acceptable salt forms 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：US10597395B2

公开(公告)日：2020-03-24

申请号：US16244796

申请日：2019-01-10

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 certain optionally substituted heterocycle fused gamma-carbolines of Formula 2J, as shown below and as further defined herein:

公开(公告)号：US10322134B2

公开(公告)日：2019-06-18

申请号：US15918955

申请日：2018-03-12

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: A61K9/00 ,  A61K9/51 ,  A61K31/5383 ,  A61K45/06 ,  A61K31/4985

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.

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：US09315504B2

公开(公告)日：2016-04-19

申请号：US14323545

申请日：2014-07-03

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: C07D241/38 ,  C07D471/16 ,  C07D471/04

CPC classification number: C07D471/16 ,  C07D471/04

Abstract: The present invention provides methods for the preparation of 4-(3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido-[3′,4′:4,5]-pyrrolo[1,2,3-de]quinoxalin-8-(7H)-yl)-1-(4-fluorophenyl)-1-butanone in free form or a salt thereof.

Abstract translation: 本发明提供了制备4-（3-甲基-2,3,6b，9,10,10a-六氢-1H-吡啶并[3'，4'：4,5] - 吡咯并[ 2,3-de]喹喔啉-8-（7H） - 基）-1-（4-氟苯基）-1-丁酮或其盐。