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公开(公告)号:US08536159B2
公开(公告)日:2013-09-17
申请号:US13133033
申请日:2009-12-07
Applicant: Peng Li , Jun Zhao , Hailin Zeng , Lawrence Wennogle
Inventor: Peng Li , Jun Zhao , Hailin Zeng , Lawrence Wennogle
IPC: A61K31/565 , A61K31/519 , A61K31/57 , C07D487/14
CPC classification number: C07D487/14 , A61K31/5025 , A61K31/519 , A61K31/529 , A61K31/5575 , A61K45/06 , C07D487/04
Abstract: Optionally substituted 3-(thio, sulfonyl or sulfonyl)-7,8-dihydro-(1H or 2H)-imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one or a substituted 3-(thio, sulfinyl or sulfonyl)-7,8,9-trihydro-(1H or 2H)-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidin-4(5H)-one compounds or Compounds of Formula (I), processes for their production, their use as pharmaceuticals and pharmaceutical compositions comprising them.
Abstract translation: 取代的3-(硫代,磺酰基或磺酰基)-7,8-二氢 - (1H或2H) - 咪唑并〔1,2-a〕吡唑并〔4,3-e〕嘧啶-4(5H) 取代的3-(硫代亚磺酰基或磺酰基)-7,8,9-三氢 - (1H或2H) - 嘧啶并[1,2-a]吡唑并[4,3-e]嘧啶-4(5H) - 酮化合物 或式(I)的化合物,其制备方法,它们作为药物的用途以及包含它们的药物组合物。
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公开(公告)号:US20130085123A1
公开(公告)日:2013-04-04
申请号:US13701235
申请日:2011-05-31
Applicant: Peng Li , Hailin Zheng , Jun Zhao , Lawrence P. Wennogle
Inventor: Peng Li , Hailin Zheng , Jun Zhao , Lawrence P. Wennogle
IPC: C07D487/14 , A61K45/06 , A61K31/557 , A61K31/19 , A61K31/565 , A61K31/573 , A61K31/519 , A61K31/165
CPC classification number: C07D487/14 , A61K31/165 , A61K31/19 , A61K31/519 , A61K31/557 , A61K31/565 , A61K31/573 , A61K45/06 , C07D487/04
Abstract: Optionally substituted 4,5,7,8-tetrahydro-(optionally 4-oxo, 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-oxo, 4-thioxo or 4-imino)-(1H or 2H)-pyrimido[1,2-a]pyrazolo[4,3-e]pyrimidine compounds, 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-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。
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公开(公告)号:US20120071450A1
公开(公告)日:2012-03-22
申请号:US13133082
申请日:2009-12-07
Applicant: Peng Li , Jun Zhao , Hailin Zheng , Lawrence Wennogle
Inventor: Peng Li , Jun Zhao , Hailin Zheng , Lawrence Wennogle
IPC: A61K31/57 , A61K31/519 , A61K31/565 , A61P25/16 , A61P25/14 , A61P25/00 , A61P25/28 , A61P25/24 , A61P25/20 , A61P25/22 , A61P25/30 , A61P9/00 , A61P9/12 , A61P15/00 , A61P11/06 , A61P11/00 , A61P11/02 , A61P37/06 , A61P29/00 , A61P5/14 , A61P15/08 , A61P19/10 , A61P13/08 , A61P35/00 , A61P27/06 , A61P27/02 , A61P25/18 , 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。
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公开(公告)号:US09073936B2
公开(公告)日:2015-07-07
申请号:US14209258
申请日:2014-03-13
Applicant: Peng Li , Hailin Zheng , Jun Zhao , Lawrence P. Wennogle
Inventor: Peng Li , Hailin Zheng , Jun Zhao , Lawrence P. Wennogle
IPC: C07D487/14
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。
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公开(公告)号:US08858911B2
公开(公告)日:2014-10-14
申请号:US13500941
申请日:2010-10-07
Applicant: Peng Li , Lawrence P. Wennogle , Jun Zhao , Hailin Zheng
Inventor: Peng Li , Lawrence P. Wennogle , Jun Zhao , Hailin Zheng
IPC: A61K51/04 , A61K31/565
CPC classification number: A61K51/0459 , C07D473/06 , G01T1/1642 , G01T1/2985
Abstract: Tracers targeting phosphodiesterase 1 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 PDE1 inhibitors such as substituted pyrazolo-pyrimidin-4-one derivatives, biomarkers for phosphodiesterase 1 [PDE1) in vivo, methods for developing novel therapies for PDE1-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.
Abstract translation: 针对磷酸二酯酶1的追踪剂用于基于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介导性疾病如肺动脉高压(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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公开(公告)号:US08664207B2
公开(公告)日:2014-03-04
申请号:US13133101
申请日:2009-12-07
Applicant: Peng Li , Jun Zhao , Hailin Zheng , Lawrence Wennogle
Inventor: Peng Li , Jun Zhao , Hailin Zheng , Lawrence Wennogle
IPC: A61K31/565 , A61K31/57 , A61K31/519 , C07D471/14
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。
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公开(公告)号:US08633180B2
公开(公告)日:2014-01-21
申请号:US13133082
申请日:2009-12-07
Applicant: Peng Li , Jun Zhao , Hailin Zeng , Lawrence Wennogle
Inventor: Peng Li , Jun Zhao , Hailin Zeng , Lawrence Wennogle
IPC: A61K31/565 , A61K31/57 , A61K31/519 , 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。
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公开(公告)号:US20120094966A1
公开(公告)日:2012-04-19
申请号:US13132955
申请日:2009-12-07
Applicant: Peng Li , Jun Zhao , Hailin Zheng , Lawrence Wennogle
Inventor: Peng Li , Jun Zhao , Hailin Zheng , Lawrence Wennogle
IPC: A61K31/519 , A61K31/565 , A61K31/57 , A61P25/16 , A61P25/14 , A61P25/28 , A61P25/24 , A61P25/00 , A61P25/22 , A61P25/18 , A61P25/20 , A61P25/30 , A61P9/00 , A61P9/12 , A61P15/00 , A61P11/06 , A61P11/00 , A61P11/02 , A61P37/06 , A61P29/00 , A61P15/12 , A61P5/14 , A61P15/08 , A61P19/10 , A61P13/08 , A61P35/00 , A61P43/00 , A61P27/06 , A61P27/02 , C07D487/04
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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公开(公告)号:US20110237561A1
公开(公告)日:2011-09-29
申请号:US13133101
申请日:2009-12-07
Applicant: Peng Li , Jun Zhao , Hailin Zeng , Lawrence Wennogle
Inventor: Peng Li , Jun Zhao , Hailin Zeng , Lawrence Wennogle
IPC: A61K31/57 , C07D471/14 , A61K31/519 , A61K31/565 , A61P25/16 , A61P25/24 , A61P25/18 , A61P27/06
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。
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公开(公告)号:US20100173951A1
公开(公告)日:2010-07-08
申请号:US12663114
申请日:2008-06-04
Applicant: Lawrence Wennogle , Peng Li , Jun Zhao
Inventor: Lawrence Wennogle , Peng Li , Jun Zhao
IPC: A61K31/44 , C07D213/69 , C07D213/61 , C07D213/68 , C07D213/64 , A61K31/4409 , A61K31/4406 , C07D213/65 , A61K31/4402 , A61P25/22 , A61P25/24 , A61P25/00 , A61P25/32 , A61P25/30 , A61P15/10 , A61P43/00 , A61P3/00
CPC classification number: C07D213/65 , C07D213/69 , C07D213/74
Abstract: The invention relates to the novel chemical compounds of the formula (I): (I) in free or salt form, its use in the treatment of NET and/or SERT mediated conditions, e.g., depression, vasomotor symptoms, e.g., hot flashes and other diseases or conditions mediated by NET and/or SERT.
Abstract translation: 本发明涉及游离或盐形式的式(I):(I)的新型化合物,其用于治疗NET和/或SERT介导的病症,例如抑郁症,血管舒缩症状,例如潮热和 由NET和/或SERT介导的其他疾病或病症。
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