Organic compounds
    11.
    发明授权
    Organic compounds 有权
    有机化合物

    公开(公告)号:US08536159B2

    公开(公告)日:2013-09-17

    申请号:US13133033

    申请日:2009-12-07

    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。

    Phosphodiesterase 1-targeting tracers and methods
    15.
    发明授权
    Phosphodiesterase 1-targeting tracers and methods 有权
    磷酸二酯酶1靶向示踪剂和方法

    公开(公告)号:US08858911B2

    公开(公告)日:2014-10-14

    申请号:US13500941

    申请日:2010-10-07

    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。

    Organic compounds
    16.
    发明授权
    Organic compounds 有权
    有机化合物

    公开(公告)号:US08664207B2

    公开(公告)日:2014-03-04

    申请号:US13133101

    申请日:2009-12-07

    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。

    Organic compounds
    17.
    发明授权
    Organic compounds 有权
    有机化合物

    公开(公告)号:US08633180B2

    公开(公告)日:2014-01-21

    申请号:US13133082

    申请日:2009-12-07

    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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