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    COMPOUNDS AND METHODS
    121.
    发明申请
    COMPOUNDS AND METHODS 审中-公开

    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.

    ORGANIC COMPOUNDS
    124.
    发明申请
    ORGANIC COMPOUNDS 有权

    公开(公告)号：US20170197974A1

    公开(公告)日：2017-07-13

    申请号：US15320280

    申请日：2015-06-22

    Applicant: Intra-Cellular Therapies, Inc.

    Inventor： Peng LI

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

    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. Previous publication WO 2009/075784 disclosed, among others, (6aR,9aS)-2-(4-(6-fluoropyridin-2-yl) benzyl)-5-methyl-3-(phenylamino)-5,6a,7,8,9,9a-hexahydrocyclopenta[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one as an inhibito of PDE1. This compound undergoes significant metabolism at several positions including the aniline ring and the cyclopentane ring. The current invention provides for Compounds of Formula I wherein such metabolism is attenuated by the substitution of hydrogen atoms for deuterium atoms at key locations discovered by the inventors.

    ORGANIC COMPOUNDS
    125.
    发明申请
    ORGANIC COMPOUNDS 有权
    有机化合物

    公开(公告)号：US20170037048A1

    公开(公告)日：2017-02-09

    申请号：US15301895

    申请日：2015-04-03

    Applicant: Intra-Cellular Therapies, Inc.

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

    IPC: C07D471/16 ,  A61K31/4985 ,  C07B59/00 ,  A61K45/06

    CPC classification number: C07D471/16 ,  A61K31/4985 ,  A61K45/06 ,  C07B59/002 ,  C07B2200/05

    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.

    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特定取代的杂环稠合的γ-咔啉及其前药，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D1 / D2受体信号传导系统的途径和/或残留症状的治疗。

    ORGANIC COMPOUNDS
    127.
    发明申请
    ORGANIC COMPOUNDS 有权
    有机化合物

    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。

    NOVEL COMBINATION
    128.
    发明申请
    NOVEL COMBINATION 审中-公开
    新的组合

    公开(公告)号：US20160038494A1

    公开(公告)日：2016-02-11

    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

    CPC classification number: A61K31/519 ,  A61K31/197 ,  A61K31/198 ,  A61K31/216 ,  A61K31/341 ,  A61K45/06 ,  A61K2300/00

    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).

    Abstract translation: 本发明涉及磷酸二酯酶1（PDE1）抑制剂和尼泊金溶蛋白抑制剂（NEP）的组合，其可用于治疗某些心血管疾病或相关疾病，例如高血压，充血性心脏病和心肌梗塞后。 在另一个实施方案中，本发明涉及PDE1抑制剂和NEP抑制剂的组合，用于治疗特征在于心血管系统中各种cGMP / PKG介导途径的破坏或损伤的疾病或病症（例如，在心脏组织或 动脉平滑肌）。

    ORGANIC COMPOUNDS
    129.
    发明申请
    ORGANIC COMPOUNDS 审中-公开
    有机化合物

    公开(公告)号：US20150197528A1

    公开(公告)日：2015-07-16

    申请号：US14671531

    申请日：2015-03-27

    Applicant: INTRA-CELLULAR THERAPIES, INC.

    Inventor： Peng LI ,  Haiyan WU

    IPC: C07D487/14

    CPC classification number: C07D487/14

    Abstract: The invention provides novel 7,8-dihydro-imidazo[1,2-α]pyrazolo[4,3-e]pyrimidin-4-one compounds and 7,8,9-trihydro-[1H or 2/f]-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one compounds, substituted at the 1 or 2 position with C2-g allcyl, C3-9 cycloalkyl, heteroarylalkyl, or substituted arylalkyl, in free, salt or prodrug form, processes for their production, their use as pharmaceuticals, particularly as PDE1 inhibitors, and pharmaceutical compositions comprising them.

    Abstract translation: 本发明提供新的7,8-二氢 - 咪唑并[1,2-a]吡唑并[4,3-e]嘧啶-4-酮化合物和7,8,9-三氢 - [1H或2 / f] [1,2-a]吡唑并[4,3-e]嘧啶-4（5H） - 酮化合物，其在1或2位被C2-g全酰基，C3-9环烷基，杂芳基烷基或取代的芳基烷基取代， 游离，盐或前药形式，其制备方法，其作为药物的用途，特别是作为PDE1抑制剂，以及包含它们的药物组合物。

    ORGANIC COMPOUNDS
    130.
    发明申请
    ORGANIC COMPOUNDS 审中-公开
    有机化合物

    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。

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