利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

88 条记录 (耗时 0.06 秒)

    Fluorogenic or fluorescent reporter molecules and their applications for whole-cell fluorescence screening assays for capsases and other enzymes and the use thereof
    61.
    发明授权
    Fluorogenic or fluorescent reporter molecules and their applications for whole-cell fluorescence screening assays for capsases and other enzymes and the use thereof 失效
    荧光或荧光报道分子及其在全酶抑制剂中的应用及其用途

    公开(公告)号：US06342611B1

    公开(公告)日：2002-01-29

    申请号：US09168888

    申请日：1998-10-09

    申请人： Eckard Weber ,  Sui Xiong Cai ,  John F. W. Keana ,  John A. Drewe ,  Han-Zhong Zhang

    发明人： Eckard Weber ,  Sui Xiong Cai ,  John F. W. Keana ,  John A. Drewe ,  Han-Zhong Zhang

    IPC分类号： C07D31188

    CPC分类号： G01N15/1456 ,  C12Q1/68 ,  G01N33/533 ,  G01N2015/1006 ,  G01N2015/1488 ,  Y10S436/80

    摘要： The present invention relates to novel fluorescent dyes, novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of caspases and other enzymes involved in apoptosis in whole cells, cell lines and tissue samples derived from any living organism or organ. The reporter molecules and assay processes can be used in drug screening procedures to identify compounds which act as inhibitors or inducers of the caspase cascade in whole cells or tissues. The reagents and assays described herein are also useful for determining the chemosensitivity of human cancer cells to treatment with chemotherapeutic drugs. The present invention also relates to novel fluorogenic and fluorescent reporter molecules and new enzyme assay processes that can be used to detect the activity of type 2 methionine aminopeptidase, dipeptidyl peptidase IV, calpain, aminopeptidase, HIV protease, adenovirus protease, HSV-1 protease, HCMV protease and HCV protease.

    摘要翻译： 本发明涉及新的荧光染料，新的荧光和荧光报道分子和新的酶测定方法，其可用于检测来自任何活生物体的全细胞，细胞系和组织样品中参与细胞凋亡的半胱天冬酶和其它酶的活性 或器官。 报告分子和测定方法可以用于药物筛选程序中，以鉴定在整个细胞或组织中作为半胱天冬酶级联的抑制剂或诱导剂的化合物。 本文所述的试剂和测定法也可用于确定人类癌细胞对用化学治疗药物治疗的化学敏感性。 本发明还涉及可用于检测2型甲硫氨酸氨基肽酶，二肽基肽酶IV，钙蛋白酶，氨基肽酶，HIV蛋白酶，腺病毒蛋白酶，HSV-1蛋白酶的活性的新型荧光和荧光报告分子和新的酶测定方法， HCMV蛋白酶和HCV蛋白酶。

    Tri- and tetra-substituted guanidines and their use as excitatory amino acid antagonists
    63.
    发明授权
    Tri- and tetra-substituted guanidines and their use as excitatory amino acid antagonists 失效

    公开(公告)号：US5798390A

    公开(公告)日：1998-08-25

    申请号：US446451

    申请日：1995-05-22

    申请人： Eckard Weber ,  John F. W. Keana

    发明人： Eckard Weber ,  John F. W. Keana

    IPC分类号： A61K31/155 ,  C07C279/18 ,  C07D311/18 ,  A61K31/37 ,  A61K31/655

    CPC分类号： A61K31/155 ,  C07C279/18 ,  C07D311/18

    摘要： Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

    PCP receptor ligands and the use thereof
    64.
    发明授权
    PCP receptor ligands and the use thereof 失效
    PCP受体配体及其用途

    公开(公告)号：US5688789A

    公开(公告)日：1997-11-18

    申请号：US450155

    申请日：1995-05-26

    申请人： Eckard Weber ,  John F. W. Keana ,  Peter Barmettler

    发明人： Eckard Weber ,  John F. W. Keana ,  Peter Barmettler

    IPC分类号： A61K31/439 ,  A61K31/55 ,  C07D471/08

    CPC分类号： C07D471/08 ,  A61K31/439 ,  A61K31/55

    摘要： The invention relates to 5-(iminomethano)-10,11-dihydro-5H-dibenzo�a,d!cycloheptene and derivatives thereof. The invention also relates to the use of such compounds for the treatment or prevention of neuronal loss in ischemia, hypoxia, brain or spinal chord trauma, as well as for the treatment of Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease and Down's syndrome.

    摘要翻译： 本发明涉及5-（亚氨基偶氮）-10,11-二氢-5H-二苯并[a，d]环庚烯及其衍生物。 本发明还涉及这些化合物用于治疗或预防缺血，缺氧，脑或脊髓创伤中的神经元丧失以及治疗阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿病和唐氏综合征的用途。

    Tri- and tetra-substituted guanidines and their use as excitatory amino acid antagonists
    65.
    发明授权
    Tri- and tetra-substituted guanidines and their use as excitatory amino acid antagonists 失效
    三取代和四取代的胍和它们作为兴奋性氨基酸拮抗剂的用途

    公开(公告)号：US5637622A

    公开(公告)日：1997-06-10

    申请号：US446229

    申请日：1995-05-22

    申请人： Eckard Weber ,  John F. W. Keana

    发明人： Eckard Weber ,  John F. W. Keana

    IPC分类号： A61K31/155 ,  C07C279/18 ,  C07D311/18

    CPC分类号： A61K31/155 ,  C07C279/18 ,  C07D311/18

    摘要： Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.

    摘要翻译： 表现出对苯环利定（PCP）受体的高结合亲和力，更优选对大脑σ受体的低亲和力的三取代和四取代胍基。 这些胍衍生物通过作为NMDA受体 - 离子通道复合物的离子通道的阻断剂，作为NMDA受体的谷氨酸诱导反应的非竞争性抑制剂。 因此，这些化合物发挥神经保护活性，并且可用于治疗缺氧，低血糖，脑或脊髓缺血以及脑或脊髓创伤中的神经元损失，以及用于治疗癫痫，阿尔茨海默病，肌萎缩性侧索硬化症 ，帕金森病，亨廷顿舞蹈病，唐氏综合征，柯萨科夫病和其他神经退行性疾病。

    PCP receptor ligands and the use thereof
    69.
    发明授权
    PCP receptor ligands and the use thereof 失效
    PCP受体配体及其用途

    公开(公告)号：US5011834A

    公开(公告)日：1991-04-30

    申请号：US337858

    申请日：1989-04-14

    申请人： Eckard Weber ,  John F. W. Keana ,  Peter Barmettler

    发明人： Eckard Weber ,  John F. W. Keana ,  Peter Barmettler

    IPC分类号： A61K31/55 ,  A61P25/00 ,  A61P25/28 ,  C07D487/08

    CPC分类号： A61K31/55

    摘要： The invention relates to methods for the treatment or prevention of neuronal loss in ischemia, hypoxia, hypoglycemia, brain and spinal cord trauma as well as for treatment of Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, and Down's Syndrome by administering a pharmaceutical composition comprising an effective amount of 10,5-(iminomethano)-10,11-dihydro-5H-dibenzo[a,d]cycloheptene (IDDC) or derivatives thereof to an animal.

    摘要翻译： 本发明涉及治疗或预防缺血，缺氧，低血糖，脑和脊髓创伤以及治疗阿尔茨海默病，肌萎缩性侧索硬化，亨廷顿舞蹈病和唐氏综合症的神经元损失的方法，其通过施用药物组合物，其包含 有效量的10,5-（亚氨基偶氮）-10,11-二氢-5H-二苯并[a，d]环庚烯（IDDC）或其衍生物。