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11 条记录 (耗时 0.016 秒)

    Rigidified compounds for modulating heparanase activity
    3.
    发明授权
    Rigidified compounds for modulating heparanase activity 有权
    用于调节乙酰肝素酶活性的刚性化合物

    公开(公告)号：US07795255B2

    公开(公告)日：2010-09-14

    申请号：US11794764

    申请日：2006-01-05

    申请人： Joel M. Van Gelder ,  Joseph Y. Klein ,  Yochai Basel ,  Anat Reizelman ,  Susanna Tchilibon ,  Orly Mouallem

    发明人： Joel M. Van Gelder ,  Joseph Y. Klein ,  Yochai Basel ,  Anat Reizelman ,  Susanna Tchilibon ,  Orly Mouallem

    IPC分类号： A61K31/5377 ,  A61K31/53 ,  A61K31/496 ,  A61K31/41 ,  A61K31/4188 ,  C07D413/14 ,  C07D253/08 ,  C07D403/14 ,  C07D257/04 ,  C07D491/147

    CPC分类号： A61K31/41

    摘要： Disclosed are novel rigidified compounds having a rhodanine-like residue and at least one aryl or heteroaryl residue linked to the rhodanine-like residue, whereby a core structure of these compounds, as defined in the specification, is characterized as having one or zero free-to-rotate bonds. Also disclosed are pharmaceutical compositions containing these rigidified compounds and uses thereof for modulating the activity of heparanase and hence in the treatment of heparanase-associated diseases and disorders, and uses thereof for modulating the activity of heparin-binding proteins and hence in the treatment of heparin-binding proteins-associated diseases and disorders as well as in the treatment of medical conditions that are at least partially treatable by rhodanine or a rhodanine analog.

    摘要翻译： 公开了具有绕丹宁样残基和连接到绕丹宁样残基的至少一个芳基或杂芳基残基的新型硬化化合物，其中如说明书中所定义的这些化合物的核心结构的特征在于具有一个或多个自由基， 旋转键。 还公开了含有这些硬化化合物的药物组合物及其用于调节乙酰肝素酶的活性，因此用于治疗乙酰肝素酶相关疾病和病症的用途及其用于调节肝素结合蛋白的活性的用途，因此用于治疗肝素 结合蛋白相关的疾病和病症，以及治疗至少部分可被罗丹宁或罗丹明类似物治疗的医学病症。

    Purine derivatives as A3 and A1 adenosine receptor agonists
    5.
    发明授权
    Purine derivatives as A3 and A1 adenosine receptor agonists 失效
    嘌呤衍生物作为A3和A1腺苷受体激动剂

    公开(公告)号：US07825126B2

    公开(公告)日：2010-11-02

    申请号：US11574779

    申请日：2005-09-02

    申请人： Kenneth A. Jacobson ,  Bhalchandra V. Joshi ,  Susanna Tchilibon

    发明人： Kenneth A. Jacobson ,  Bhalchandra V. Joshi ,  Susanna Tchilibon

    IPC分类号： C07D473/40 ,  C07D473/34 ,  C07D473/18 ,  A61K31/52 ,  A61K31/522 ,  A61P9/02 ,  C07D473/36 ,  C07D317/70 ,  C07D317/28

    CPC分类号： C07D473/00

    摘要： Disclosed are (N)-methanocarba adenine nucleosides of the formula: as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias. The invention also provides compounds that are agonists of both A1 and A3 adenosine receptors for use in cardioprotection.

    摘要翻译： 公开了下式的（N） - 甲氰胺腺嘌呤核苷：作为高效的A3腺苷受体激动剂，包含这种核苷的药物组合物，以及这些核苷的使用方法，其中R1-R6如说明书中所定义。 这些核苷被考虑用于治疗许多疾病，例如炎症，心脏缺血，中风，哮喘，糖尿病和心律失常。 本发明还提供了作为用于心脏保护的A1和A3腺苷受体的激动剂的化合物。

    Purine Derivatives as A3 and A1 Adenosine Receptor Agonists
    6.
    发明申请
    Purine Derivatives as A3 and A1 Adenosine Receptor Agonists 失效
    嘌呤衍生物作为A3和A1腺苷受体激动剂

    公开(公告)号：US20070232626A1

    公开(公告)日：2007-10-04

    申请号：US11574779

    申请日：2005-09-02

    申请人： Kenneth Jacobson ,  Bhalchandra Joshi ,  Susanna Tchilibon

    发明人： Kenneth Jacobson ,  Bhalchandra Joshi ,  Susanna Tchilibon

    IPC分类号： A61K31/52 ,  C07D473/26

    CPC分类号： C07D473/00

    摘要： Disclosed are (N)-methanocarba adenine nucleosides of the formula: [Formula] as highly potent A3 adenosine receptor agonists, pharmaceutical compositions comprising such nucleosides, and a method of use of these nucleosides, wherein R1-R6 are as defined in the specification. These nucleosides are contemplated for use in the treatment a number of diseases, for example, inflammation, cardiac ischemia, stroke, asthma, diabetes, and cardiac arrhythmias. The invention also provides compounds that are agonists of both A1 and A3 adenosine receptors for use in cardioprotection.

    摘要翻译： 公开了具有下式的（N） - 甲烷卡巴腺嘌呤核苷：作为高效A 3 N 3腺苷受体激动剂，包含这种核苷的药物组合物，以及这些核苷的使用方法，其中R < SUB> 1 6 如说明书中所定义。 这些核苷被考虑用于治疗许多疾病，例如炎症，心脏缺血，中风，哮喘，糖尿病和心律失常。 本发明还提供了用于心脏保护的作为Aβ1 N和A 3 N 3腺苷受体的激动剂的化合物。

    Rigidified Compounds for Modulating Heparanase Activity
    9.
    发明申请
    Rigidified Compounds for Modulating Heparanase Activity 有权
    用于调节肝素酶活性的刚性化合物

    公开(公告)号：US20080039456A1

    公开(公告)日：2008-02-14

    申请号：US11794764

    申请日：2006-01-05

    申请人： Joel Gelder ,  Joseph Klein ,  Yochai Basel ,  Anat Reizelman ,  Susanna Tchilibon ,  Orly Mouallem

    发明人： Joel Gelder ,  Joseph Klein ,  Yochai Basel ,  Anat Reizelman ,  Susanna Tchilibon ,  Orly Mouallem

    IPC分类号： A61K31/4188 ,  A61K31/429 ,  A61K31/437 ,  A61K31/53 ,  A61K31/5377 ,  A61P17/02 ,  A61P25/00 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P9/10 ,  C07D491/147 ,  C07D513/04 ,  C07D513/14 ,  C07D513/22

    CPC分类号： A61K31/41

    摘要： Disclosed are novel rigidified compounds having a rhodanine-like residue and at least one aryl or heteroaryl residue linked to the rhodanine-like residue, whereby a core structure of these compounds, as defined in the specification, is characterized as having one or zero free-to-rotate bonds. Also disclosed are pharmaceutical compositions containing these rigidified compounds and uses thereof for modulating the activity of heparanase and hence in the treatment of heparanase-associated diseases and disorders, and uses thereof for modulating the activity of heparin-binding proteins and hence in the treatment of heparin-binding proteins-associated diseases and disorders as well as in the treatment of medical conditions that are at least partially treatable by rhodanine or a rhodanine analog.

    摘要翻译： 公开了具有绕丹宁样残基和连接到绕丹宁样残基的至少一个芳基或杂芳基残基的新型硬化化合物，由此如说明书中所定义的这些化合物的核心结构的特征在于具有一个或多个自由基， 旋转键。 还公开了含有这些硬化化合物的药物组合物及其用于调节乙酰肝素酶的活性，因此用于治疗乙酰肝素酶相关疾病和病症的用途及其用于调节肝素结合蛋白的活性的用途，因此用于治疗肝素 结合蛋白相关的疾病和病症，以及治疗至少可以通过绕丹宁或绕丹宁类似物治疗的医学病症。

    Agonists specific for the peripheral cannabinoid receptor
    10.
    发明授权
    Agonists specific for the peripheral cannabinoid receptor 有权
    激动剂专用于外周大麻素受体

    公开(公告)号：US07214716B2

    公开(公告)日：2007-05-08

    申请号：US11043089

    申请日：2005-01-27

    申请人： Ester Fride ,  Aviva Breuer ,  Lumir Hanus ,  Susanna Tchilibon ,  Michal Horowitz ,  Raphael Mechoulam ,  Aaron Garzon

    发明人： Ester Fride ,  Aviva Breuer ,  Lumir Hanus ,  Susanna Tchilibon ,  Michal Horowitz ,  Raphael Mechoulam ,  Aaron Garzon

    IPC分类号： A61K31/075

    CPC分类号： A61K31/216 ,  A61K31/09

    摘要： The invention provides novel pharmaceutical compositions comprising as the active ingredient 4-phenyl pinene derivatives which are specific for the peripheral cannabinoid receptors. In particular, the compounds of the invention binds efficiently to CB2 but do not bind to CB1. The compounds show no activity in behavioral tests in mice which together have been shown to be specific for tetrahydrocannabinol (THC)- type activity in the central nervous system mediated by CB1 but reduce blood pressure, block intestinal motility, and elicit anti-inflammatory and peripheral analgetic activity. The invention also relates to methods of treating, preventing, or managing hypertension, inflammation, pain, gastrointestinal diseases, autoimmune diseases, and tumors with the compounds of the invention.

    摘要翻译： 本发明提供了新的药物组合物，其包含作为外周大麻素受体特异性的4-苯基蒎烯衍生物作为活性成分。 特别地，本发明的化合物有效地与CB2结合，但不结合CB1。 这些化合物在小鼠的行为测试中没有显示出活性，这些活性已被证明对于由CB1介导的中枢神经系统中的四氢大麻酚（THC）型活性而言是特异性的，但是降低血压，阻止肠蠕动，并引发抗炎和外周 止痛活动。 本发明还涉及用本发明化合物治疗，预防或控制高血压，炎症，疼痛，胃肠道疾病，自身免疫性疾病和肿瘤的方法。