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1. 发明申请

WO2011153138A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2011153138A1
公开(公告)日：2011-12-08
申请号：PCT/US2011/038548
申请日：2011-05-31
申请人： INTRA-CELLULAR THERAPIES, INC. , LI, Peng , ZHENG, Hailin , ZHAO, Jun , WENNOGLE, Lawrence P.
发明人： LI, Peng , ZHENG, Hailin , ZHAO, Jun , WENNOGLE, Lawrence P.
IPC分类号： C07D471/04
CPC分类号： A61K31/519 , A61K31/5575 , A61K45/06 , C07D487/14
摘要： Optionally substituted (1- or 3-oxy)-4,5,7,8-tetrahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-2H-imidazo[1,2-a]pyrrolo[3,4-e]pyrimidine or (1- or 3-oxy)-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, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising the same.
摘要翻译：任选取代的（1-或3-氧）-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[ 4-e]嘧啶或（1-或3-氧）-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，其制备方法，它们作为药物的用途和包含其的药物组合物。

2. 发明申请

WO2011153136A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2011153136A1
公开(公告)日：2011-12-08
申请号：PCT/US2011/038544
申请日：2011-05-31
申请人： INTRA-CELLULAR THERAPIES, INC. , LI, Peng , ZHENG, Hailin , ZHAO, Jun , WENNOGLE, Lawrence, P.
发明人： LI, Peng , ZHENG, Hailin , ZHAO, Jun , WENNOGLE, Lawrence, P.
IPC分类号： A61K31/519
CPC分类号： C07D487/04 , A61K31/519 , A61K45/06
摘要： The present invention relates to (1- or 2- and/or 5 and/or 7-substituted)-(3-oxy)-(4H, 4-imino, 4-thioxo or 4-oxo)-pyrazolo[3,4-d]pyrimidin-6-ones, e.g., a compound of formula II as described below, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them. Of particular interest are novel compounds useful as inhibitors of phosphodiesterase 1 (PDE1), e.g., in the treatment of diseases involving disorders of the dopamine D1 receptor intracellular pathway, such as Parkinson's disease, depression, narcolepsy, damage to cognitive function, e.g., in schizophrenia, or disorders that may be ameliorated through enhanced progesterone-signaling pathway, e.g., female sexual dysfunction.
摘要翻译：本发明涉及（1-或2-和/或5和/或7-取代的） - （3-氧） - （4H，4-亚氨基，4-硫代或4-氧代） - 吡唑并[3,4 -d]嘧啶-6-酮，例如下述的式II化合物，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。特别令人感兴趣的是可用作磷酸二酯酶1（PDE1）抑制剂的新化合物，例如用于治疗涉及多巴胺D1受体细胞内途径紊乱的疾病，例如帕金森病，抑郁症，发作性睡病，对认知功能的损害，例如精神分裂症或可通过增强的孕激素信号传导途径改善的疾病，例如女性性功能障碍。

3. 发明申请

WO2010086860A3 NEUROPROTECTIVE MULTIFUNCTIONAL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM 审中-公开
标题翻译：神经保护性多功能化合物和包含它们的药物组合物
公开(公告)号：WO2010086860A3
公开(公告)日：2011-02-24
申请号：PCT/IL2010000080
申请日：2010-01-31
申请人： YEDA RES & DEV , TECHNION RES & DEV FOUNDATION , YOUDIM MOUSSA B H , FRIDKIN MATI , ZHENG HAILIN
发明人： YOUDIM MOUSSA B H , FRIDKIN MATI , ZHENG HAILIN
IPC分类号： C07C211/38 , A61K31/131 , A61K31/135 , A61K31/47 , A61P9/00 , A61P25/00 , A61P29/00 , C07C259/10 , C07C271/40 , C07D215/34 , C07D401/12
CPC分类号： C07C259/10 , C07C211/38 , C07C271/40 , C07C2602/08 , C07C2603/74 , C07D215/34 , C07D401/06 , C07D401/12
摘要： Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and (vi) a moiety that imparts an N-methyl-D-aspartic acid receptor (NMDAR) inhibition, and pharmaceutically acceptable salts and optical isomers thereof. The multifunctional compounds are useful in the treatment or prevention of diseases, disorders or conditions that can be prevented and/or treated by iron chelation therapy, and/or neuroprotection and/or neurorestoration, and/or apoptosis inhibition and/or MAO inhibition and/or cholinesterase inhibition and/or NMADR inhibition. The present invention encompasses compounds of the formulas I to Vl.
摘要翻译：提供多官能化合物，其包含两个或多个选自以下的官能部分：（i）赋予铁螯合剂功能的部分; （ii）赋予神经保护功能的部分; （iii）赋予组合的抗细胞凋亡，神经保护和/或神经恢复功能的部分; （iv）赋予脑MAO抑制的部分，优选在肝脏和小肠中几乎没有MAO抑制作用; （v）赋予胆碱酯酶抑制功能的部分; 和（vi）赋予N-甲基-D-天冬氨酸受体（NMDAR）抑制的部分及其药学上可接受的盐和旋光异构体。多官能化合物可用于治疗或预防可通过铁螯合治疗和/或神经保护和/或神经恢复，和/或凋亡抑制和/或MAO抑制和/或MAO抑制和/或治疗的/ 或胆碱酯酶抑制和/或NMADR抑制。本发明包括式I至VI的化合物。

4. 发明申请

WO2004041151A2 NEUROPROTECTIVE IRON CHELATORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM 审中-公开
标题翻译：神经保护性铁器钳和包含它们的药物组合物
公开(公告)号：WO2004041151A2
公开(公告)日：2004-05-21
申请号：PCT/IL2003/000932
申请日：2003-11-07
申请人： TECHNION RESEARCH AND DEVELOPMENT FOUNDATION LTD. , YEDA RESEARCH AND DEVELOPMENT CO. LTD. , YOUDIM, Moussa, B., H. , FRIDKIN, Matitiyahu , ZHENG, Hailin , WARSHAWSKY, Rivka
发明人： YOUDIM, Moussa, B., H. , FRIDKIN, Matitiyahu , ZHENG, Hailin , WARSHAWSKY, Rivka
IPC分类号： A61K
CPC分类号： C07D295/15 , A61K38/00 , A61K45/06 , A61K47/547 , C07D213/69 , C07D215/26 , C07D295/205 , C07K7/06 , C07K7/22 , C07K7/23 , C07K14/57563 , C07K14/70 , Y02A50/411
摘要： Novel iron chelators exhibiting neuroprotective and good transport properties are useful in iron chelation therapy for treatment of a disease, disorder or condition associated with iron overload and oxidative stress, eg. a neurodegenerative or cerebrovascular disease or disorder, a neoplastic disease, hemochromatosis, thalassemia, a cardiovascular disease, diabetes, a inflammatory disorder, anthracycline cardiotoxicity, a viral infection, a protozoal infection, a yeast infection, retarding ageing, and prevention and/or treatment of skin ageing and skin protection against sunlight and/or UV light. The iron chelator function is provided by a 8-hydroxyquinoline, a hydroxypyridinone or a hydroxamate moiety, the neuroprotective function is imparted to the compound e.g. by a neuroprotective peptide, and a combined antiapoptotic and neuroprotective function by a propargyl group.
摘要翻译：显示出神经保护和良好转运性质的新型铁螯合剂可用于铁螯合治疗用于治疗与铁过载和氧化应激相关的疾病，病症或病症，例如，神经变性或脑血管疾病或病症，肿瘤性疾病，血色素沉着病，地中海贫血，心血管疾病，糖尿病，炎性病症，蒽环类心脏毒性，病毒感染，原生动物感染，酵母感染，延迟衰老以及预防和/或治疗的皮肤老化和皮肤防晒防晒和/或紫外线。铁螯合剂功能由8-羟基喹啉，羟基吡啶酮或异羟肟酸盐部分提供，神经保护功能被赋予化合物例如通过神经保护肽，以及由炔丙基组合的抗细胞凋亡和神经保护功能。

5. 发明申请

WO2012171016A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2012171016A1
公开(公告)日：2012-12-13
申请号：PCT/US2012/041925
申请日：2012-06-11
申请人： INTRA-CELLULAR THERAPIES, INC. , LI, Peng , ZHENG, Hailin , ZHAO, Jun , WENNOGLE, Lawrence P.
发明人： LI, Peng , ZHENG, Hailin , ZHAO, Jun , WENNOGLE, Lawrence P.
IPC分类号： A61K31/505 , C07D487/04
CPC分类号： A61K31/519 , A61K8/69 , A61K9/0048 , A61K31/165 , A61K31/19 , A61K31/565 , A61K31/57 , A61K45/06 , A61Q7/00 , C07D487/12 , C07D487/14 , A61K2300/00
摘要： The present invention relates to PDEl inhibitory compounds of Formula I as described above, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及如上所述的式I的PDE1抑制性化合物，其制备方法，其作为药物的用途和包含它们的药物组合物。

6. 发明申请

WO2011153129A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2011153129A1
公开(公告)日：2011-12-08
申请号：PCT/US2011/038527
申请日：2011-05-31
申请人： INTRA-CELLULAR THERAPIES, INC. , LI, Peng , ZHENG, Hailin , ZHAO, Jun , WENNOGLE, Lawrence, P.
发明人： LI, Peng , ZHENG, Hailin , ZHAO, Jun , WENNOGLE, Lawrence, P.
IPC分类号： C07D471/04
CPC分类号： C07D487/14 , A61K31/165 , A61K31/19 , A61K31/519 , A61K31/557 , A61K31/565 , A61K31/573 , A61K45/06 , C07D487/04
摘要： Optionally substituted 4,5,7,8-tetrahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-(1 H or 2 H )-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidine or 4,5,7,8,9-pentahydro-(optionally 4-oxo, 4-thioxo or 4-imino)-(1 H or 2 H )-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidine compounds, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
摘要翻译：任选取代的4,5,7,8-四氢 - （任选4-氧代，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4-氧代，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，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。

7. 发明申请

WO2010086860A2 NEUROPROTECTIVE MULTIFUNCTIONAL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM 审中-公开
标题翻译：神经保护性多功能化合物和包含它们的药物组合物
公开(公告)号：WO2010086860A2
公开(公告)日：2010-08-05
申请号：PCT/IL2010/000080
申请日：2010-01-31
申请人： Yeda Research and Development Co. Ltd. , Technion Research and Development Foundation Ltd. , YOUDIM, Moussa B.H. , FRIDKIN, Mati , ZHENG, Hailin
发明人： YOUDIM, Moussa B.H. , FRIDKIN, Mati , ZHENG, Hailin
IPC分类号： C07C211/38
CPC分类号： C07C259/10 , C07C211/38 , C07C271/40 , C07C2602/08 , C07C2603/74 , C07D215/34 , C07D401/06 , C07D401/12
摘要： Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and (vi) a moiety that imparts an N-methyl-D-aspartic acid receptor (NMDAR) inhibition, and pharmaceutically acceptable salts and optical isomers thereof. The multifunctional compounds are useful in the treatment or prevention of diseases, disorders or conditions that can be prevented and/or treated by iron chelation therapy, and/or neuroprotection and/or neurorestoration, and/or apoptosis inhibition and/or MAO inhibition and/or cholinesterase inhibition and/or NMADR inhibition.
摘要翻译：提供多官能化合物，其包含两个或多个选自以下的官能部分：（i）赋予铁螯合剂功能的部分; （ii）赋予神经保护功能的部分; （iii）赋予组合的抗细胞凋亡，神经保护和/或神经恢复功能的部分; （iv）赋予脑MAO抑制的部分，优选在肝脏和小肠中几乎没有MAO抑制作用; （v）赋予胆碱酯酶抑制功能的部分; 和（vi）赋予N-甲基-D-天冬氨酸受体（NMDAR）抑制的部分及其药学上可接受的盐和旋光异构体。多官能化合物可用于治疗或预防可通过铁螯合治疗和/或神经保护和/或神经恢复，和/或凋亡抑制和/或MAO抑制和/或MAO抑制和/或治疗的/ 或胆碱酯酶抑制和/或NMADR抑制。

8. 发明申请

WO2009073210A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2009073210A1
公开(公告)日：2009-06-11
申请号：PCT/US2008/013410
申请日：2008-12-06
申请人： INTRA-CELLULAR THERAPIES, INC , LI, Peng , ZHAO, Jun , ZHENG, Hailin
发明人： LI, Peng , ZHAO, Jun , ZHENG, Hailin
IPC分类号： A01N43/56
CPC分类号： C07D487/04 , A61K31/519 , A61K45/06
摘要： 1- or 2- or 7-(substituted)-3-(optionally hetero)arylamino-[lH, 2H]-pyrazolo[3,4-d] pyrimidine-4,6(5H, 7H)-dione derivatives, in free, salt or prodrug form, are useful as pharmaceuticals, particularly as phosphodiesterase 1 inhibitors, useful for the treatment of diseases involving disorders of the dopamine Dl receptor intracellular pathway, such as Parkinson's disease, depression, narcolepsy and damage to cognitive function, e.g., in schizophrenia or disorders that may be ameliorated through enhanced progesterone - signaling pathway, e.g., female sexual dysfunction.
摘要翻译： 1-或2-或7-或取代的-3-（任选杂）芳基氨基 - [1H，2H] - 吡唑并[3,4-d]嘧啶-4,6（5H，7H） - 二酮衍生物，，盐或前药形式可用作药物，特别是作为磷酸二酯酶抑制剂，可用于治疗涉及多巴胺D1受体细胞内途径疾病的疾病，例如帕金森病，抑郁症，发作性睡病和对认知功能的损害，例如，精神分裂症或可通过增强孕激素 - 信号通路（例如女性性功能障碍）改善的疾病。

9. 发明申请

WO2011153135A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：WO2011153135A1
公开(公告)日：2011-12-08
申请号：PCT/US2011/038541
申请日：2011-05-31
申请人： INTRA-CELLULAR THERAPIES, INC. , LI, Peng , ZHENG, Hailin , ZHAO, Jun , WENNOGLE, Lawrence P.
发明人： LI, Peng , ZHENG, Hailin , ZHAO, Jun , WENNOGLE, Lawrence P.
IPC分类号： A61K31/519
CPC分类号： C07D487/04 , A61K31/165 , A61K31/519 , A61K31/5575 , A61K45/06 , A61K2300/00
摘要： The present invention relates to optionally substituted (5- or 7-oxy)-3,4-dihydro-(optionally 4-oxo, 4-thioxo or 4-imino)-1H-pyrrolo[3,4-d]pyrimidin-2(3H,6H)-ones, e.g., Compounds of Formula II-A or II-B as described herein, processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
摘要翻译：本发明涉及任选取代的（5-或7-氧）-3,4-二氢 - （任选4-氧代，4-硫代或4-亚氨基）-1H-吡咯并[3,4-d]嘧啶-2 （3H，6H） - 酮，例如本文所述的式II-A或II-B的化合物，其生产方法，其用作药物和包含它们的药物组合物。

10. 发明申请

WO2011043816A1 PHOSPHODIESTERASE 1-TARGETING TRACERS AND METHODS 审中-公开
标题翻译：磷酸二酯酶1指标追踪器和方法
公开(公告)号：WO2011043816A1
公开(公告)日：2011-04-14
申请号：PCT/US2010/002707
申请日：2010-10-07
申请人： INTRA-CELLULAR THERAPIES, INC. , LI, Peng , WENNOGLE, Lawrence, P. , ZHAO, Jun , ZHENG, Hailin
发明人： LI, Peng , WENNOGLE, Lawrence, P. , ZHAO, Jun , ZHENG, Hailin
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： A61K51/0459 , C07D473/06 , G01T1/1642 , G01T1/2985
摘要： Tracers targeting phosphodiesterase1 for use in gamma radiation detection-based diagnostic techniques, particularly gamma-emitter labeled tracers for SPECT and positron emitter-labeled compositions for PET are disclosed. Radio-labeled multiple novel scaffolds as PDEl inhibitors such as substituted pyrazolo-pyrimidin- 4-one derivatives, biomarkers for phosphodiesterase 1 [PDEl) in vivo , methods for developing novel therapies for PDEl-implicated conditions such as pulmonary arterial hypertension (PAH), Central Nervous System (CNS) and Cardiovascular (CV) disorders, and methods of detection and treatment are also disclosed.
摘要翻译：针对磷酸二酯酶1的示踪剂用于基于γ辐射检测的诊断技术，特别是用于SPECT的用于SPECT的γ发射体标记的示踪剂和用于PET的正电子发射体标记的组合物。放射性标记的多种新型支架作为PDE1抑制剂，例如取代的吡唑并嘧啶-4-酮衍生物，用于磷酸二酯酶1 [PDE1]的生物标志物），用于开发PDE1介导的病症如肺动脉高压（PAH），中枢神经系统（CNS）和心血管（CV）疾病以及检测和治疗方法也被公开。

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