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：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：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：US09630971B2

公开(公告)日：2017-04-25

申请号：US14900589

申请日：2014-06-20

Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  INTRA-CELLULAR THERAPIES, INC.

Inventor： Takashi Abe ,  Graham Buckton ,  Robert Davis ,  Mark Hooper ,  Peng Li ,  Hideaki Maruyama ,  Masahiro Takasuga ,  Lawrence P. Wennogle ,  Yuhei Yamamoto ,  Hironori Yamashita

IPC: A61K31/519 ,  C07D487/14

CPC classification number: C07D487/14

Abstract: The present invention relates to crystals of (6aR,9aS)-5,6a,7,8,9,9a-hexahydro-5-methyl-3-(phenylamino)-2-((4-(6-fluoropyridin-2-yl)phenyl)methyl)-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one, and methods of making and using such crystals.

公开(公告)号：US20150259353A1

公开(公告)日：2015-09-17

申请号：US14409988

申请日：2013-06-21

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng Li ,  Lawrence P. Wennogle ,  Robert Davis ,  Graham Buckton ,  Mark Hooper

IPC: C07D487/14 ,  C07C57/15 ,  C07C55/02 ,  C07C309/04

CPC classification number: C07D487/14 ,  C07B2200/13 ,  C07C55/02 ,  C07C57/15 ,  C07C309/04

Abstract: The present invention relates to acid addition salt and salt crystals of (6aR,9aS)-5,6a,7,8,9,9a-hexahydro-5-methyl-3-(phenylamino)-2-((4-(6-fluoropyridin-2-yl)phenyl)methyl)-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one, composition comprising the same and the method of making and using such salt and crystal

Abstract translation: 本发明涉及（6aR，9aS）-5,6a，7,8,9,9a-六氢-5-甲基-3-（苯基氨基）-2 - （（4-（6 - 氟吡啶-2-基）苯基）甲基） - 环戊并[4,5]咪唑并[1,2-a]吡唑并[4,3-e]嘧啶-4（2H） - 酮，包含该组合物的组合物和方法 制作和使用这种盐和水晶

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：US12023331B2

公开(公告)日：2024-07-02

申请号：US17115416

申请日：2020-12-08

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Gretchen Snyder ,  Robert Davis ,  Lawrence P. Wennogle

IPC: A61K31/4985 ,  A61K45/06 ,  A61P25/22 ,  A61P25/24

CPC classification number: A61K31/4985 ,  A61P25/22 ,  A61P25/24 ,  A61K45/06

Abstract: The disclosure provides methods for the acute treatment of depression and/or anxiety, for the enhancement of mTOR (e.g., mTORC1) signaling, and for the reduction of neuroinflammation, comprising administering to a patient in need thereof, a therapeutically effective amount of a 5-HT2A/mu-opioid receptor or 5-HT2A/D1 and/or D2/mu-opioid receptor ligand.