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    Prevention and treatment of cardiovascular pathologies
    1.
    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。

    Prevention and treatment of cardiovascular pathologies
    6.
    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：US06262079B1

    公开(公告)日：2001-07-17

    申请号：US09306606

    申请日：1999-05-06

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

    发明人： David J. Grainger ,  James C. Metcalfe ,  Lawrence L. Kunz ,  Robert W. Schroff ,  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)allyl 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 R4F 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为H或O（C1-C4）烷基，R1和R2分别为（C1-C4）烯丙基或与N一起为饱和杂环基，R3为乙基或氯乙基，R4为H或与R3一起为-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R4F R5和R6是H时，R3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。

    Prevention and treatment of pathologies associated with abnormally proliferative smooth muscle cells
    7.
    发明授权
    Prevention and treatment of pathologies associated with abnormally proliferative smooth muscle cells 失效
    预防和治疗与异常增殖平滑肌细胞相关的病理学

    公开(公告)号：US6166090A

    公开(公告)日：2000-12-26

    申请号：US965589

    申请日：1997-11-06

    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： G01N33/566 ,  A61K31/00 ,  A61K31/135 ,  A61K31/138 ,  A61K31/40 ,  A61K39/395 ,  A61K45/00 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P43/00 ,  C07K14/71 ,  C07K16/22

    CPC分类号： A61K31/715 ,  A61K31/00 ,  A61K31/135 ,  A61K31/138 ,  A61K31/40 ,  C07K14/71 ,  C07K16/22 ,  C07K2317/73 ,  C07K2317/74 ,  G01N2800/321 ,  G01N2800/323 ,  Y10S514/824

    摘要： TGF-beta activators and TGF-beta production stimulators are employed to maintain or increase vessel lumen diameter in a diseased or injured vessel of a mammal. Conditions such as restenosis following angioplasty, vascular bypass grafts, transplanted organs, atherosclerosis or hypertension are characterized by a reduced vessel lumen diameter. In a preferred embodiment of the invention, TGF-beta activators and production stimulators inhibit abnormal proliferation of smooth muscle cells. TGF-beta activators or production stimulators that are not characterized by an undesirable systemic toxicity profile at a prophylactic dose are also amenable to chronic use for prophylactic purposes with respect to disease states involving proliferation and/or migration of vascular smooth muscle cells over time. Further provided is a method for determining TGF-beta in vitro, thereby identifying a patient at risk for atherosclerosis and monitoring a recipient that has received one or more administrations of a TGF-beta activator or production stimulator.

    摘要翻译： 使用TGF-β激活剂和TGF-β产生刺激剂来维持或增加哺乳动物的患病或受伤的血管中的血管腔直径。 血管成形术后的再狭窄，血管旁路移植物，移植器官，动脉粥样硬化或高血压等病症的特征在于血管腔直径减小。 在本发明的优选实施方案中，TGF-β激活剂和产生刺激物抑制平滑肌细胞的异常增殖。 在预防剂量下不具有不期望的全身毒性特征的TGF-β激活剂或生产刺激剂也适用于涉及血管平滑肌细胞随时间的增殖和/或迁移的疾病状态的慢性预防用途。 进一步提供了一种用于在体外测定TGF-β的方法，从而鉴定了患有动脉粥样硬化风险的患者，并监测已经接受TGF-β激活剂或产生刺激物的一次或多次给药的受体。