公开(公告)号：US20180044337A1

公开(公告)日：2018-02-15

申请号：US15660762

申请日：2017-07-26

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

CPC classification number: C07D471/16 ,  C07D471/04

Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines, intermediates useful in producing them and methods for producing such intermediates and such heterocycl fused gamma-carbolines.

公开(公告)号：US20170233399A1

公开(公告)日：2017-08-17

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

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

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：US20170183350A1

公开(公告)日：2017-06-29

申请号：US15301912

申请日：2015-04-03

Applicant: Intra-Cellular Therapies, Inc.

Inventor： Sharon MATES ,  Peng LI ,  Lawrence P. WENNOGLE ,  Robert DAVIS

IPC: C07D471/16 ,  A61K45/06 ,  A61K31/4985

CPC classification number: C07D471/16 ,  A61K31/4985 ,  A61K45/06 ,  C07B59/002 ,  C07D471/14

Abstract: The 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：US20170114037A1

公开(公告)日：2017-04-27

申请号：US15317876

申请日：2015-06-09

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Robert DAVIS ,  Peng LI

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

CPC classification number: C07D401/06 ,  A61K31/454 ,  A61K45/06 ,  C07B2200/05 ,  Y02A50/475

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：US20160145261A1

公开(公告)日：2016-05-26

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 ,  Hinori YAMASHITA

IPC: 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.

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，以及制备和使用这种晶体的方法。

公开(公告)号：US20150166540A1

公开(公告)日：2015-06-18

申请号：US14627968

申请日：2015-02-20

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Sharon MATES ,  Robert DAVIS ,  Lawrence P. WENNOGLE ,  Peng LI ,  John Charles TOMESCH ,  Qiang ZHANG

IPC: C07D471/16

CPC classification number: C07D471/16 ,  A61K31/44 ,  C07D471/04

Abstract: The 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 D2 receptor signaling systems.

公开(公告)号：US20150072965A1

公开(公告)日：2015-03-12

申请号：US14539859

申请日：2014-11-12

Applicant: Intra-Cellular Therapies, Inc.

Inventor： Peng LI ,  Jun ZHAO ,  Hailin ZHENG ,  Lawrence WENNOGLE

IPC: C07D487/14 ,  A61K45/06 ,  A61K31/165 ,  A61K31/519

CPC classification number: C07D487/14 ,  A61K31/165 ,  A61K31/519 ,  A61K31/5365 ,  A61K45/06

Abstract: Optionally substituted 4,5,7,8-tetrahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-imidazo[1,2-a]pyrrolo[3,4-e]pyrimidine or 4,5,7,8,9-pentahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-pyrimido[1,2-a]pyrrolo[3,4-e]pyrimidine compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising the same.

Abstract translation: 任选取代的4,5,7,8-四氢 - （任选4-氧代，4-硫代或4-亚氨基）-2H-咪唑并[1,2-a]吡咯并[3,4-e]嘧啶或4,5 ，7,8,9-五氢 - （任选4-氧代，4-硫代或4-亚氨基）-2H-嘧啶并[1,2-a]吡咯并[3,4-e]嘧啶化合物或式 ），其生产方法，它们作为药物的用途和包含其的药物组合物。

公开(公告)号：US20250129087A1

公开(公告)日：2025-04-24

申请号：US18833086

申请日：2023-01-31

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI

IPC: C07D487/14 ,  C07C51/43 ,  C07C51/64 ,  C07C53/00 ,  C07C53/122 ,  C07C53/126 ,  C07C53/18 ,  C07C55/02 ,  C07C55/07 ,  C07C55/10 ,  C07C55/14 ,  C07C57/15 ,  C07C59/245 ,  C07C59/255 ,  C07C62/18 ,  C07C63/08 ,  C07C65/01 ,  C07C65/10 ,  C07C65/11 ,  C07C227/42 ,  C07C229/64 ,  C07C231/24 ,  C07C235/38 ,  C07C303/44 ,  C07C309/04 ,  C07C309/05 ,  C07C309/25 ,  C07C309/29 ,  C07C309/30 ,  C07C309/35 ,  C07D213/80 ,  C07D213/803 ,  C07D239/557

Abstract: Disclosed herein are 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, compositions comprising the same as well as methods of making and using such salts and crystals.

公开(公告)号：US20250101022A1

公开(公告)日：2025-03-27

申请号：US18905607

申请日：2024-10-03

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: C07D471/16 ,  C07D471/04

Abstract: The present invention provides methods for the preparation of substituted heterocycle fused gamma-carbolines, such as the compound of Formula 1J, as shown below, intermediates useful in producing them and methods for producing such intermediates and such heterocycle fused gamma-carbolines, and as further defined herein: