公开(公告)号：US20220372035A1

公开(公告)日：2022-11-24

申请号：US17813473

申请日：2022-07-19

Applicant: INTRA-CELLULAR THERAPIES, INC.

Inventor： Peng LI ,  Hailin ZHENG ,  Robert DAVIS ,  Sharon MATES ,  Kimberly VANOVER ,  Gretchen SNYDER

IPC: C07D471/16 ,  A61P25/36 ,  A61P1/00 ,  A61P11/00 ,  A61P29/00 ,  A61K45/06

Abstract: The invention relates to particular prodrugs of substituted heterocycle fused gamma-carbolines, 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 the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and/or the μ-opioid receptor.

公开(公告)号：US20190144460A1

公开(公告)日：2019-05-16

申请号：US16186272

申请日：2018-11-09

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：US20160039835A1

公开(公告)日：2016-02-11

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 ,  A61K45/06 ,  A61K31/5575 ,  A61K31/519

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.

Abstract translation: 提供式I的PDE1抑制剂，其制备方法及其作为药物的用途，以及包含它们的药物组合物。

公开(公告)号：US20160039829A1

公开(公告)日：2016-02-11

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 ,  A61K45/06 ,  A61K31/519

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：US20140315868A1

公开(公告)日：2014-10-23

申请号：US14252511

申请日：2014-04-14

Applicant: Intra-Cellular Therapies, Inc.

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

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

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61K31/522 ,  A61K31/56 ,  A61K45/06 ,  A61K2300/00

Abstract: The present invention relates to optionally substituted 3-amino-4,5-dihydro-(1H or 2H)-pyrazolo[3,4-d]pyrimidin-6(7H)-ones and their 4-imino or 4-thioxo derivatives, e.g., 3-amino-4-(thioxo or imino)-4,5-dihydro-2H-pyrazolo[3,4-d]pyrimidin-6(7H)-ones, 3-amino-4-(thioxo or imino)-4,5-dihydro-2H-pyrazolo[3,4-d]pyrimidin-6(7H)-ones, 3-amino-4-(thioxo or imino)-4,5-dihydro-1H-pyrazolo[3,4-d]pyrimidin-6(7H)-ones, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.

Abstract translation: 本发明涉及任选取代的3-氨基-4,5-二氢 - （1H或2H） - 吡唑并[3,4-d]嘧啶-6（7H） - 酮及其4-亚氨基或4-硫代衍生物， 例如3-氨基-4-（硫代或亚氨基）-4,5-二氢-2H-吡唑并[3,4-d]嘧啶-6（7H） - 酮，3-氨基-4-（硫代或亚氨基） -4,5-二氢-2H-吡唑并[3,4-d]嘧啶-6（7H） - 酮，3-氨基-4-（硫代或亚氨基）-4,5-二氢-1H-吡唑并[ 4-d]嘧啶-6（7H） - 酮，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。

公开(公告)号：US20140011783A1

公开(公告)日：2014-01-09

申请号：US14019950

申请日：2013-09-06

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

CPC classification number: C07D487/14 ,  A61K31/519 ,  A61K31/5575 ,  A61K45/06

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

Abstract translation: 任选取代的4,5,7,8-四氢 - （任选4-硫代或4-亚氨基） - （1H或2H） - 咪唑并[1,2-a]吡唑并[4,3-e]嘧啶或4,5 ，7,8,9-五氢 - （任选的4-硫代或4-亚氨基） - （1H或2H） - 嘧啶并[1,2-a]吡唑并[4,3-e]嘧啶化合物或式 ），其生产方法，它们作为药物的用途以及包含它们的药物组合物。

公开(公告)号：US20170217975A1

公开(公告)日：2017-08-03

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：US20160031895A1

公开(公告)日：2016-02-04

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

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：US20150080357A1

公开(公告)日：2015-03-19

申请号：US14296145

申请日：2014-06-04

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

IPC: C07D487/14 ,  A61K31/5575 ,  A61K31/519

CPC classification number: C07D487/14 ,  A61K31/519 ,  A61K31/5575 ,  A61K45/06

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

Abstract translation: 任选取代的4,5,7,8-四氢 - （任选4-硫代或4-亚氨基） - （1H或2H） - 咪唑并[1,2-a]吡唑并[4,3-e]嘧啶或4,5 ，7,8,9-五氢 - （任选的4-硫代或4-亚氨基） - （1H或2H） - 嘧啶并[1,2-a]吡唑并[4,3-e]嘧啶化合物或式 ），其生产方法，它们作为药物的用途以及包含它们的药物组合物。

公开(公告)号：US20140148421A1

公开(公告)日：2014-05-29

申请号：US14169352

申请日：2014-01-31

Applicant: INTRA-CELLULAR THERAPIES, INC.

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

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

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。