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51. 发明申请

WO2017165843A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2017165843A1
公开(公告)日：2017-09-28
申请号：PCT/US2017/024137
申请日：2017-03-24
申请人： INTRA-CELLULAR THERAPIES, INC.
发明人： YAO, Wei , LI, Peng
IPC分类号： A61K31/4985 , A61K31/5383 , C07D471/14
摘要： The invention relates to particular substituted deuterated 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.
摘要翻译：本发明涉及如本文所述的游离的，固体的，药学上可接受的盐和/或基本上纯的形式的特定的经取代的氘化杂环稠合的γ-咔啉，其前药，其药物组合物和使用方法用于治疗涉及5-HT 2A受体，5-羟色胺转运蛋白（SERT）和/或涉及多巴胺D1 / D2受体信号系统的途径的疾病，和/或治疗残留症状。

52. 发明申请

WO2017165755A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2017165755A1
公开(公告)日：2017-09-28
申请号：PCT/US2017/023998
申请日：2017-03-24
申请人： INTRA-CELLULAR THERAPIES, INC.
发明人： WENNOGLE, Lawrence P. , LI, Peng
IPC分类号： A61K31/4985 , A61P25/18 , C07D471/14
摘要： The invention relates to particular substituted fluorinated 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-HT 2A receptor, serotonin transporter (SERT) and/or pathways involving dopamine D 1 /D 2 receptor signaling systems, and/or the treatment of residual symptoms.
摘要翻译：本发明涉及如本文所述的游离的，固体的，药学上可接受的盐和/或基本上纯的形式的特定的经取代的氟化杂环稠合的γ-咔啉，其前药，其药物组合物和使用方法在治疗涉及5-HT 2A受体，5-羟色胺转运蛋白（SERT）和/或涉及多巴胺D 1 / D 2受体的途径的疾病信号系统和/或治疗残留症状。

53. 发明申请

WO2016044667A1 COMPOUNDS AND METHODS 审中-公开
标题翻译：化合物和方法
公开(公告)号：WO2016044667A1
公开(公告)日：2016-03-24
申请号：PCT/US2015/050814
申请日：2015-09-17
申请人： INTRA-CELLULAR THERAPIES, INC.
发明人： LI, Peng , ZHENG, Hailin , ZHAO, Jun , WENNOGLE, Lawrence
IPC分类号： A61K31/519
CPC分类号： C07D487/14
摘要： 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.
摘要翻译：主题通常涉及治疗和/或预防CNS疾病，障碍和/或损伤的化合物和方法。一方面，本发明涉及磷酸二酯酶1（PDE1）作为神经保护剂和/或神经再生剂的抑制剂。另一方面，该主题涉及处于CNS疾病或病症发展风险的个体。

54. 发明申请

WO2016022893A1 ORGANIC COMPOUNDS 审中-公开
公开(公告)号：WO2016022893A1
公开(公告)日：2016-02-11
申请号：PCT/US2015/044164
申请日：2015-08-07
申请人： INTRA-CELLULAR THERAPIES, INC.
发明人： LI, Peng , ZHENG, Hailin , ZHAO, Jun , WENNOGLE, Lawrence P.
IPC分类号： C07D487/14 , A61K31/519
CPC分类号： A61K31/519 , A61K45/06 , C07D487/14 , A61K2300/00
摘要： 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.

55. 发明申请

WO2015196186A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2015196186A1
公开(公告)日：2015-12-23
申请号：PCT/US2015/036890
申请日：2015-06-22
申请人： INTRA-CELLULAR THERAPIES, INC.
发明人： LI, Peng
IPC分类号： C07D487/14
CPC分类号： C07D487/14 , A61K8/4953 , A61K9/0048 , A61K31/519 , A61K45/06 , A61Q7/00 , C07B59/002 , C07B2200/05
摘要： 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.
摘要翻译：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。以前公开的WO 2009/075784公开了（6aR，9aS）-2-（4-（6-氟吡啶-2-基）苄基）-5-甲基-3-（苯基氨基）-5,6a， 8,9,9a-六氢环戊二烯并[4,5]咪唑并[1,2-a]吡唑并[4,3-e]嘧啶-4（2H） - 酮作为PDE1的抑制剂。该化合物在包括苯胺环和环戊烷环在内的几个位置处经历显着的代谢。本发明提供式I化合物，其中通过在发明人发现的关键位置用氢原子取代氘原子来减弱其代谢。

56. 发明申请

WO2015191554A1 COMPOUNDS AND METHODS OF USE TO TREAT SCHIZOPHRENIA 审中-公开
标题翻译：化合物和使用方法研究
公开(公告)号：WO2015191554A1
公开(公告)日：2015-12-17
申请号：PCT/US2015/034863
申请日：2015-06-09
申请人： INTRA-CELLULAR THERAPIES, INC.
发明人： DAVIS, Robert , LI, Peng
IPC分类号： C07D401/06
CPC分类号： C07D401/06 , A61K31/454 , A61K45/06 , C07B2200/05
摘要： 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.
摘要翻译：本发明涉及游离的药学上可接受的盐和/或基本上纯的（ - （（1-（2-（2-羟基-2-苯乙基）哌啶-4-基）甲基）异二氢吲哚-1-酮类似物和前药本文所述的形式，其药物组合物，以及用于治疗可通过σ配体的神经控制功能治疗和/或预防性治疗的疾病的方法。

57. 发明申请

WO2014205354A3 FREE BASE CRYSTALS 审中-公开
标题翻译：免费碱性水晶
公开(公告)号：WO2014205354A3
公开(公告)日：2015-05-28
申请号：PCT/US2014043422
申请日：2014-06-20
申请人： TAKEDA PHARMACEUTICAL , INTRA CELLULAR THERAPIES INC
发明人： ABE TAKASHI , BUCKTON GRAHAM , DAVIS ROBERT , HOOPER MARK , LI PENG , MARUYAMA HIDEAKI , TAKASUGA MASAHIRO , WENNOGLE LAWRENCE P , YAMAMOTO YUHEI , YAMASHITA HIRONORI
IPC分类号： A61K31/57 , A61K31/519
CPC分类号： C07D487/14
摘要： 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.
摘要翻译：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。

58. 发明申请

WO2014127331A1 NOVEL USES 审中-公开
标题翻译：新用途
公开(公告)号：WO2014127331A1
公开(公告)日：2014-08-21
申请号：PCT/US2014/016741
申请日：2014-02-17
申请人： INTRA-CELLULAR THERAPIES, INC.
发明人： WENNOGLE, Lawrence P. , DAVIS, Robert
IPC分类号： A61K31/519 , C07D487/04 , C07D487/14
CPC分类号： A61K31/519 , A61K45/06
摘要： The invention relates to the administration of inhibitors of phosphodiesterase 1 (PDE1) for the treatment of diseases or disorders characterized by disruption of or damage to various cGMP/PKG mediated pathways. In one embodiment the invention relates to inhibitors of phosphodiesterase 1 (PDE1) for treatment of cardiovascular disease and related disorders, e.g., congestive heart disease, atherosclerosis, myocardial infarction, and stroke.
摘要翻译：本发明涉及用于治疗特征在于各种cGMP / PKG介导途径的破坏或损伤的疾病或病症的磷酸二酯酶1（PDE1）抑制剂的给药。在一个实施方案中，本发明涉及用于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，心肌梗死和中风的磷酸二酯酶1（PDE1）的抑制剂。

59. 发明申请

WO2013155505A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2013155505A1
公开(公告)日：2013-10-17
申请号：PCT/US2013/036514
申请日：2013-04-14
申请人： INTRA-CELLULAR THERAPIES, INC
发明人： MATES, Sharon , DAVIS, Robert , LI, Peng , WENNOGLE, Lawrence , LERNER, Richard A.
IPC分类号： A61K31/4985
CPC分类号： C07D471/14 , A61K31/445 , A61K31/4985 , A61K31/5383 , A61K45/06 , C07D471/16 , A61K2300/00
摘要： 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..
摘要翻译：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D2受体信号传导系统的途径。

60. 发明申请

WO2013155504A1 NOVEL METHODS 审中-公开
标题翻译：新方法
公开(公告)号：WO2013155504A1
公开(公告)日：2013-10-17
申请号：PCT/US2013/036512
申请日：2013-04-14
申请人： INTRA-CELLULAR THERAPIES, INC.
发明人： MATES, Sharon , DAVIS, Robert , VANOVER, Kimberly , WENNOGLE, Lawrence
IPC分类号： A61K31/4985
CPC分类号： C07D471/14 , A61K31/445 , A61K31/4985 , A61K31/5383 , A61K45/06 , C07D471/16 , A61K2300/00
摘要： Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of agitation, aggressive behaviors, posttraumatic stress disorder or impulse control disorders. In an embodiment, the effective amount is about 1 mg to about 140 mg per dose per day, in another embodiment about 2.5 mg to about 100 mg, in another embodiment about 10 mg to about 100 mg per dose per day, in another embodiment about 10 mg to about 60 mg per dose per day, in another embodiment about 10 mg to about 40 mg per day, in another embodiment about 20 mg to about 40 mg per day, in another embodiment about 40-60 mg per day, in another embodiment, about 1mg-10mg per day.
摘要翻译：使用特定的取代的杂环稠合的γ-咔啉化合物作为药物用于治疗激动，侵袭行为，创伤后应激障碍或冲动控制障碍。在一个实施方案中，有效量为每剂量每天约1mg至约140mg，在另一个实施方案中为约2.5mg至约100mg，在另一个实施方案中为约10mg至约100mg /剂量/天，在另一个实施方案中为约 10mg至约60mg /天，在另一个实施方案中为约10mg至约40mg /天，在另一个实施方案中为约20mg至约40mg /天，在另一个实施方案中为约40-60mg /天，另外每天约1mg-10mg。

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