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    Enhancing treatment of HIF-1 mediated disorders with adenosine A3 receptor agonists
    1.
    发明申请
    Enhancing treatment of HIF-1 mediated disorders with adenosine A3 receptor agonists 审中-公开
    用腺苷A3受体激动剂增强HIF-1介导的病症的治疗

    公开(公告)号：US20060194756A1

    公开(公告)日：2006-08-31

    申请号：US11286129

    申请日：2005-11-22

    申请人： Pier Borea ,  Pier Baraldi ,  Stefania Merighi ,  Stephen MacLennan ,  Edward Leung ,  Allan Moorman

    发明人： Pier Borea ,  Pier Baraldi ,  Stefania Merighi ,  Stephen MacLennan ,  Edward Leung ,  Allan Moorman

    IPC分类号： A61K31/7076

    CPC分类号： A61K31/7076 ,  A61K31/519 ,  C07D487/04 ,  C07D487/14 ,  C07K16/18

    摘要： The present invention relates to the use of adenosine receptor agonists, preferably A3 receptor agonists, either alone or in combination with other agents for the treatment, prevention and/or management of diseases or disorders associated with under-expression of HIF-1α and/or decreased HIF-1 α activity (e.g., ischemic related disorders). The methods of the invention are directed to methods of reducing tissue damage (e.g., substantially prevention tissue damage, inducing tissue protection) resulting from ischemia orhypoxia. The invention provides methods for treating, preventing and/or ameliorating one or more symptoms of hypoxic or HIF-1α related disorders by administering an A3 receptor agonist either alone or in combination with other agents.

    摘要翻译： 本发明涉及腺苷受体激动剂，优选A 3 N 3受体激动剂，单独使用或与其它药剂组合用于治疗，预防和/或控制与低血糖相关的疾病或病症， HIF-1α的表达和/或降低的HIF-1α活性（例如缺血性相关疾病）。 本发明的方法涉及减少由局部缺血或缺氧引起的组织损伤（例如，基本上预防组织损伤，诱导组织保护）的方法。 本发明提供了通过单独或与其它药剂组合施用A 3 O 3受体激动剂来治疗，预防和/或改善一种或多种缺氧或HIF-1α相关疾病症状的方法。

    Enhancing treatment of cancer and HIF-1 mediated disorders with adenosine A3 receptor antagonists
    2.
    发明申请
    Enhancing treatment of cancer and HIF-1 mediated disorders with adenosine A3 receptor antagonists 审中-公开
    用腺苷A3受体拮抗剂增强癌症和HIF-1介导的病症的治疗

    公开(公告)号：US20060204502A1

    公开(公告)日：2006-09-14

    申请号：US11286127

    申请日：2005-11-22

    申请人： Pier Borea ,  Pier Baraldi ,  Stefania Merighi ,  Stephen MacLennan ,  Edward Leung ,  Allan Moorman

    发明人： Pier Borea ,  Pier Baraldi ,  Stefania Merighi ,  Stephen MacLennan ,  Edward Leung ,  Allan Moorman

    IPC分类号： A61K39/395 ,  A61K31/519

    CPC分类号： A61K31/7076 ,  A61K31/519 ,  C07D487/04 ,  C07D487/14 ,  C07K16/18

    摘要： The present invention relates to the use of adenosine receptor antagonists, preferably A3 receptor antagonists, either alone or in combination with other agents for the treatment, prevention and/or management of diseases or disorders associated with overexpression of HIF-1α and/or increased HIF-1α activity (e.g., cancer, respiratory disease). The methods and compositions of the invention are particularly useful for preventing, treating, or ameliorating symptoms associated with a cancer, disease or disorder associated with hypoxia-inducible factor 1α (HIF-1α) using the A3 receptor antagonists of the invention. The present invention provides methods to inhibit the growth of tumors, particularly solid tumors and more particularly hypoxic tumors.

    摘要翻译： 本发明涉及腺苷受体拮抗剂，优选Aβ3受体拮抗剂，其单独使用或与其它药物组合用于治疗，预防和/或控制与过表达相关的疾病或病症 HIF-1α和/或增加的HIF-1α活性（如癌症，呼吸系统疾病）。 本发明的方法和组合物特别可用于预防，治疗或改善与使用Aβ受体相关的与缺氧诱导因子1α（HIF-1α）相关的癌症，疾病或病症相关症状。 本发明的拮抗剂。 本发明提供抑制肿瘤，特别是实体瘤，特别是缺氧性肿瘤生长的方法。

    Novel adenosine A3 receptor agonists
    3.
    发明申请
    Novel adenosine A3 receptor agonists 失效
    新型腺苷A3受体激动剂

    公开(公告)号：US20050250729A1

    公开(公告)日：2005-11-10

    申请号：US10944245

    申请日：2004-09-17

    申请人： Pier Baraldi ,  Allan Moorman ,  Pier Borea

    发明人： Pier Baraldi ,  Allan Moorman ,  Pier Borea

    IPC分类号： A61K31/7076 ,  C07H20060101 ,  C07H1/00 ,  C07H19/16 ,  G01N33/74

    CPC分类号： C07H19/16 ,  A61K31/7076 ,  C07H1/00 ,  G01N33/74 ,  G01N2333/726

    摘要： The compounds of the following formula: wherein Ar, R and R1 have the meanings given in the specification. This series of sulfonamido derivatives with a conserved uronamide group at the 5′ position provide superior A3 receptor affinity as well as selectivity. These new adenosine agonists are sulfonamido derivatives N-substituted with aliphatic groups (cyclic or linear) or aromatic radicals.

    摘要翻译： 下式的化合物：其中Ar，R和R 1具有说明书中给出的含义。 该系列具有5'位保守脲酰胺基团的亚磺酰氨基衍生物提供了优异的A3受体亲和力以及选择性。 这些新的腺苷激动剂是用脂肪族（环状或直链）或芳族基团N-取代的亚磺酰氨基衍生物。

    ADENOSINE A2B RECEPTOR AGONISTS
    4.
    发明申请
    ADENOSINE A2B RECEPTOR AGONISTS 失效
    腺苷A2B受体激动剂

    公开(公告)号：US20070281902A1

    公开(公告)日：2007-12-06

    申请号：US11757559

    申请日：2007-06-04

    申请人： Pier Baraldi ,  Pier Borea ,  Allan Moorman ,  Delia Preti

    发明人： Pier Baraldi ,  Pier Borea ,  Allan Moorman ,  Delia Preti

    IPC分类号： A61K31/7076 ,  C07H19/19

    CPC分类号： C07H19/19

    摘要： The present invention provides compounds of the formula wherein R1, R2, R3 and n have meaning as described in the specification, as adenosine A2B receptor agonists and, thus, may be employed for the treatment of diseases in mammals that are mediated by the A2B receptor including, but not limited to, septic shock, cystic fibrosis, impotence, diarrhea, and cardiac diseases Cardiac diseases include hyperplasia consequent to hypertension, arteriosclerosis, and heart attack

    摘要翻译： 本发明提供下式的化合物，其中R 1，R 2，R 3和n具有如说明书中所述的含义，作为腺苷 2B2受体激动剂，因此可用于治疗哺乳动物由Aβ2A受体介导的疾病，包括但不限于脓毒性休克， 囊性纤维化，阳ence，腹泻和心脏病心脏疾病包括高血压，动脉硬化和心脏病发作的增生

    ADENOSINE A3 RECEPTOR MODULATORS
    5.
    发明申请
    ADENOSINE A3 RECEPTOR MODULATORS 有权
    腺苷A3受体调节剂

    公开(公告)号：US20070249641A1

    公开(公告)日：2007-10-25

    申请号：US11774784

    申请日：2007-07-09

    申请人： Pier Baraldi ,  Pier Borea

    发明人： Pier Baraldi ,  Pier Borea

    IPC分类号： A61K31/505 ,  A61P35/00 ,  C07D239/00

    CPC分类号： A61K49/0052 ,  A61K31/519 ,  A61K49/0021 ,  A61K51/0459 ,  A61K51/0491 ,  C07B2200/05 ,  C07D471/14 ,  C07D487/14 ,  G01N33/57492 ,  G01N2333/726 ,  G01N2500/00

    摘要： The compounds of the following formula: wherein R, R2, R3 and A have the meanings given in the specification, are endowed with selective A3 adenosine receptor antagonist activity. These compounds can be used in a pharmaceutical composition to treat disorders caused by excessive activation of the A3 receptor, or can be used in a diagnostic application to determine the relative binding of other compounds to the A3 receptor. The compounds can be labeled, for example with fluorescent or radiolabels, and the labels used in vivo or in vitro to determine the presence of tumor cells which possess a high concentration of adenosine A3 receptors.

    摘要翻译： 下式的化合物：其中R，R 2，R 3和A具有说明书中给出的含义，赋予选择性A 3， 腺苷受体拮抗剂活性。 这些化合物可用于药物组合物中以治疗由过度活化的Aβ受体引起的疾病，或可用于诊断应用中以确定其它化合物与A 3受体。 化合物可以被标记，例如用荧光或放射性标记，以及在体内或体外用于确定具有高浓度腺苷A 3受体的肿瘤细胞的存在的标记。

    Novel adenosine A3 receptor modulators
    6.
    发明申请
    Novel adenosine A3 receptor modulators 失效
    新型腺苷A3受体调节剂

    公开(公告)号：US20060178385A1

    公开(公告)日：2006-08-10

    申请号：US11344295

    申请日：2006-01-31

    申请人： Pier Baraldi ,  Pier Borea ,  Delia Preti ,  Mojgan Tabrizi

    发明人： Pier Baraldi ,  Pier Borea ,  Delia Preti ,  Mojgan Tabrizi

    IPC分类号： A61K31/519 ,  C07D487/14

    CPC分类号： C07D487/14

    摘要： A class of novel antagonists for the adenosine A3 receptor are disclosed. These compounds are useful as therapeutic agents for a number of diseases and medical conditions that are mediated by the A3 receptor. The compounds of this invention are also useful as diagnostic agents for the A3 receptor.

    摘要翻译： 公开了一类用于腺苷A 3 N受体的新型拮抗剂。 这些化合物可用作多种受Aβ受体介导的疾病和医学病症的治疗剂。 本发明的化合物也可用作A 3 O 3受体的诊断剂。

    8-Heteroaryl xanthine adenosine A2B receptor antagonists
    7.
    发明申请
    8-Heteroaryl xanthine adenosine A2B receptor antagonists 失效
    8-杂芳基黄嘌呤腺苷A2B受体拮抗剂

    公开(公告)号：US20060142309A1

    公开(公告)日：2006-06-29

    申请号：US11359661

    申请日：2006-02-22

    申请人： Pier Baraldi ,  Pier Borea

    发明人： Pier Baraldi ,  Pier Borea

    IPC分类号： A61K31/522

    CPC分类号： C07D473/08 ,  C07D473/04 ,  C07D473/06 ,  Y10S436/804

    摘要： The present invention relates generally to compounds of formula (I): wherein X is a five or six-membered heteroaromatic ring, containing one to four heteroatoms, selected from nitrogen, oxygen, or sulfur, provided that at least one heteroatom is nitrogen; and G1 and G2 are independently CH or N. The present invention also relates to the preparation of the compounds, pharmaceutical formulations thereof, and their use in medicine as potent or selective A2B adenosine receptor antagonists and their uses for treating asthma, autoimmune diseases and retinal vascular diseases.

    摘要翻译： 本发明一般涉及式（I）化合物：其中X是含有一至四个选自氮，氧或硫的杂原子的五元或六元杂芳环，条件是至少一个杂原子是氮; 和G 1和G 2独立地是CH或N.本发明还涉及化合物，其药物制剂及其在药物中作为有效的或 选择性Aβ2A腺苷受体拮抗剂及其用于治疗哮喘，自身免疫性疾病和视网膜血管疾病的用途。

    Adenosine A3 receptor modulators
    8.
    发明申请
    Adenosine A3 receptor modulators 有权
    腺苷A3受体调节剂

    公开(公告)号：US20060040959A1

    公开(公告)日：2006-02-23

    申请号：US11169311

    申请日：2005-06-27

    申请人： Pier Baraldi ,  Pier Borea

    发明人： Pier Baraldi ,  Pier Borea

    IPC分类号： A61K31/519

    CPC分类号： A61K49/0052 ,  A61K31/519 ,  A61K49/0021 ,  A61K51/0459 ,  A61K51/0491 ,  C07B2200/05 ,  C07D471/14 ,  C07D487/14 ,  G01N33/57492 ,  G01N2333/726 ,  G01N2500/00

    摘要： The compounds of the following formula: wherein R, R2, R3 and A have the meanings given in the specification, are endowed with selective A3 adenosine receptor antagonist activity. These compounds can be used in a pharmaceutical composition to treat disorders caused by excessive activation of the A3 receptor, or can be used in a diagnostic application to determine the relative binding of other compounds to the A3 receptor. The compounds can be labeled, for example with fluorescent or radiolabels, and the labels used in vivo or in vitro to determine the presence of tumor cells which possess a high concentration of adenosine A3 receptors.

    摘要翻译： 下式的化合物：其中R，R 2，R 3和A具有说明书中给出的含义，赋予选择性A 3， 腺苷受体拮抗剂活性。 这些化合物可用于药物组合物中以治疗由过度活化的Aβ受体引起的疾病，或可用于诊断应用以确定其它化合物与A 3受体。 化合物可以被标记，例如用荧光或放射性标记，以及在体内或体外用于确定具有高浓度腺苷A 3受体的肿瘤细胞的存在的标记。