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    Prevention and treatment of cardiovascular pathologies with tamoxifen analogues
    1.
    发明授权
    Prevention and treatment of cardiovascular pathologies with tamoxifen analogues 失效
    用他莫昔芬类似物预防和治疗心血管病变

    公开(公告)号：US06197789B1

    公开(公告)日：2001-03-06

    申请号：US08973570

    申请日：1997-12-05

    申请人： David J. Grainger ,  James C. Metcalfe ,  Lawrence L. Kunz ,  Robert W. Schroff

    发明人： David J. Grainger ,  James C. Metcalfe ,  Lawrence L. Kunz ,  Robert W. Schroff

    IPC分类号： A61K31445

    CPC分类号： A61K31/445 ,  A61K31/135 ,  A61K31/138 ,  A61K31/38 ,  A61K31/40 ,  G01N2800/32 ,  G01N2800/324 ,  Y10S514/866

    摘要： A method for treating or preventing cardiovascular pathologies by administering a compound of the formula (I): wherein Z is C═O or a covalent bond; Y is H or O(C1-C4)alkyl, R1 and R2 are individually (C1-C4)alkyl or together with N are a saturated heterocyclic group, R3 is ethyl or chloroethyl, R4 is H, R5 is I, O(C1-C4)alkyl or H and R6 is I, O(C1-C4)alkyl or H with the proviso that when R4, R5, and R6 are H, R3 is not ethyl; or a pharmaceutically acceptable salt thereof, effective to elevate the level of TGF-beta to treat and/or prevent conditions such as atherosclerosis, thrombosis, myocardial infarction, and stroke is provided. Useful compounds include idoxifene, toremifene or salts thereof. Further provided is a method for identifying an agent that elevates the level of TGF-beta. Another embodiment of the invention is an assay or kit to determine TGF-beta in vitro. Also provided is a therapeutic method comprising inhibiting smooth muscle cell proliferation associated with procedural vascular trauma employing the administration of tamoxifen or structural analogs thereof, including compounds of formula (I).

    摘要翻译： 一种治疗或预​​防心血管病变的方法，其通过给予式（I）化合物：其中Z为C = O或共价键; Y是H或O（C1-C4）烷基，R1和R2分别是（C1-C4）烷基或与N一起为饱和杂环基，R3是乙基或氯乙基，R4是H，R5是I，O（C1 -C4）烷基或H，R6是I，O（C1-C4）烷基或H，条件是当R4，R5和R6是H时，R3不是乙基; 提供有效地提高TGF-β水平以治疗和/或预防诸如动脉粥样硬化，血栓形成，心肌梗塞和中风的病症的药学上可接受的盐或其药学上可接受的盐。 有用的化合物包括异昔芬，托瑞米芬或其盐。 还提供了用于鉴定提高TGF-β水平的试剂的方法。 本发明的另一个实施方案是用于在体外测定TGF-β的测定或试剂盒。 还提供了一种治疗方法，其包括使用给予他莫昔芬或其结构类似物（包括式（I）的化合物）来抑制与程序性血管创伤相关的平滑肌细胞增殖。

    Prevention and treatment of cardiovascular pathologies
    4.
    发明授权
    Prevention and treatment of cardiovascular pathologies 失效
    预防和治疗心血管病变

    公开(公告)号：US06251920B1

    公开(公告)日：2001-06-26

    申请号：US09082643

    申请日：1998-05-21

    申请人： David J. Grainger ,  James C. Metcalfe ,  Peter L. Weissberg

    发明人： David J. Grainger ,  James C. Metcalfe ,  Peter L. Weissberg

    IPC分类号： A61K31445

    CPC分类号： A61K9/0024 ,  A61K31/00 ,  A61K31/135 ,  A61K31/138 ,  A61K31/337 ,  A61K31/38 ,  A61K31/40 ,  A61K31/4025 ,  A61K31/4035 ,  A61K31/407 ,  A61K31/715 ,  C07K14/71 ,  C07K16/22 ,  C07K2317/73 ,  G01N2800/32 ,  G01N2800/324

    摘要： A method for treating or preventing cardiovascular pathologies by administering a compound of the formula (I): wherein Z is C═O or a covalent bond; Y is H or O(C1-C4)alkyl, R1 and R2 are individually (C1-C4)alkyl or together with N are a saturated heterocyclic group, R3 is ethyl or chloroethyl, R4 is H or together with R3 is —CH2—CH2— or —S—, R5 is I, O(C1-C4)alkyl or H and R6 is I, O(C1-C4)alkyl or H with the proviso that when R4, R5, and R6 are H, R3 is not ethyl; or a pharmaceutically acceptable salt thereof, effective to activate or stimulate production of TGF-beta to treat and/or prevent conditions such as atherosclerosis, thrombosis, myocardial infarction, and stroke is provided. Useful compounds include idoxifene and salts thereof. Further provided is a method for identifying a compound that is a TGF-beta activator or production stimulator is provided. Another embodiment of the invention is an assay or kit to determine TGF-beta in vitro. Also provided is a therapeutic method comprising inhibiting smooth muscle cell proliferation associated with procedural vascular trauma employing the administration of tamoxifen or structural analogs thereof, including compounds of formula (I).

    摘要翻译： 一种治疗或预​​防心血管病变的方法，其通过给予式（I）化合物：其中Z为C = O或共价键; Y是H或O（C1-C4）烷基，R1和R2分别是（C1-C4）烷基或与N一起是饱和杂环基，R3是乙基或氯乙基，R4是H或与R3一起是-CH2- CH2-或-S-，R5是I，O（C1-C4）烷基或H，R6是I，O（C1-C4）烷基或H，条件是当R4，R5和R6是H时，R3是 不是乙基; 提供有效激活或刺激TGF-β的产生以治疗和/或预防诸如动脉粥样硬化，血栓形成，心肌梗死和中风的病症的药学上可接受的盐或其药学上可接受的盐。 有用的化合物包括异昔芬及其盐。 还提供了鉴定作为TGF-β激活剂或生产刺激剂的化合物的方法。 本发明的另一个实施方案是用于在体外测定TGF-β的测定或试剂盒。 还提供了一种治疗方法，其包括使用给予他莫昔芬或其结构类似物（包括式（I）的化合物）来抑制与程序性血管创伤相关的平滑肌细胞增殖。