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：US10285992B2

公开(公告)日：2019-05-14

申请号：US14820323

申请日：2015-08-06

Applicant: Intra-Cellular Therapies, Inc.

Inventor： Lawrence P. Wennogle ,  Peng Li

IPC: A61K31/519 ,  A61K31/197 ,  A61K31/216 ,  A61K45/06 ,  A61K31/198 ,  A61K31/341

Abstract: The invention relates to the combination of inhibitors of phosphodiesterase 1 (PDE1) and inhibitors of Neprilysin (NEP) useful for the treatment of certain cardiovascular diseases or related disorders, e.g., hypertension, congestive heart disease, and post-myocardial infarction. In another embodiment, the invention relates to the combination of inhibitors of PDE1 and inhibitors of NEP for the treatment of diseases or disorders characterized by disruption of or damage to various cGMP/PKG mediated pathways in the cardiovascular system (e.g., in cardiac tissue or in arterial smooth muscle).

公开(公告)号：US10179776B2

公开(公告)日：2019-01-15

申请号：US15317876

申请日：2015-06-09

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Robert Davis ,  Peng Li

IPC: C07D401/06 ,  A61K45/06 ,  A61K31/454

Abstract: The invention relates to particular 2-((1-(2-hydroxy-2-phenylethyl)piperidin-4-yl)methyl)isoindolin-1-one analogs and pro-drugs, 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 that can be therapeutically and/or preventively treated by the nerve control function of sigma ligands.

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.

公开(公告)号：US09944648B2

公开(公告)日：2018-04-17

申请号：US15110613

申请日：2015-01-09

Applicant: Intra-Cellular Therapies, Inc.

Inventor： Qiang Zhang ,  Youyi Peng ,  Peng Li ,  J. David Beard ,  Lawrence P. Wennogle ,  John Tomesch

IPC: C07D487/04 ,  C07D235/30 ,  C07D277/82 ,  C07B59/00 ,  C07D401/12

CPC classification number: C07D487/04 ,  C07B59/002 ,  C07B2200/05 ,  C07D235/30 ,  C07D277/82 ,  C07D401/12

Abstract: The invention provides novel compounds, composition comprising said compounds and methods for inhibiting CK1 as well as methods of treating CK1 related disorders such as Alzheimer's disease comprising administering a therapeutically effective amount of a CK1 inhibitor to a patient in need thereof.

公开(公告)号：US09884872B2

公开(公告)日：2018-02-06

申请号：US15320280

申请日：2015-06-22

Applicant: Intra-Cellular Therapies, Inc.

Inventor： Peng Li

IPC: C07D487/14 ,  C07B59/00 ,  A61K45/06 ,  A61K31/519 ,  A61K9/00 ,  A61K8/49 ,  A61Q7/00

CPC classification number: C07D487/14 ,  A61K8/4953 ,  A61K9/0048 ,  A61K31/519 ,  A61K45/06 ,  A61Q7/00 ,  C07B59/002 ,  C07B2200/05

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

公开(公告)号：US09708294B2

公开(公告)日：2017-07-18

申请号：US14993048

申请日：2016-01-11

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: A61K31/445 ,  C07D401/12 ,  A61K31/454 ,  A61K31/4745 ,  A61K31/506 ,  A61K33/24 ,  A61K45/06 ,  A61K31/41 ,  A61K31/415 ,  A61K31/7068

CPC classification number: C07D401/12 ,  A61K31/41 ,  A61K31/415 ,  A61K31/454 ,  A61K31/4745 ,  A61K31/506 ,  A61K31/7068 ,  A61K33/24 ,  A61K45/06 ,  A61K2300/00

Abstract: The invention 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., small cell lung cancer.

公开(公告)号：US09428506B2

公开(公告)日：2016-08-30

申请号：US14394467

申请日：2013-04-14

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: A61K31/4985 ,  C07D241/38 ,  C07D471/14 ,  A61K45/06 ,  A61K31/5383 ,  C07D471/16 ,  A61K31/445

CPC classification number: C07D471/14 ,  A61K31/445 ,  A61K31/4985 ,  A61K31/5383 ,  A61K45/06 ,  C07D471/16 ,  A61K2300/00

Abstract: The invention relates to particular substituted heterocycle fused gamma-carbolines, of Formula I, 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 disease of the central nervous system.

Abstract translation: 本发明涉及如本文所述的游离，固体，药学上可接受的盐和/或基本上纯的形式的式I的特定取代的杂环稠合的γ-咔啉，其药物组合物，以及用于治疗涉及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。

公开(公告)号：US09403836B2

公开(公告)日：2016-08-02

申请号：US14461132

申请日：2014-08-15

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li

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

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

Abstract: 1- or 2-substituted (6aR,9aS)-3-(phenylamino)-5-6a,7,8,9,9a-hexahydro-5-methyl-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(1H or, 2H)-one compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.

Abstract translation: 1-或2-取代的（6aR，9aS）-3-（苯基氨基）-5-6a，7,8,9,9a-六氢-5-甲基 - 环戊[4,5]咪唑并[1,2-a] （I）的吡唑并[4,3-e]嘧啶-4（1H或2H） - 酮化合物，其制备方法，它们作为药物的用途和包含它们的药物组合物。