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1. 发明申请

US20060135560A1 Prevention and treatment of cardiovascular pathologies with tamoxifen analogues 审中-公开
标题翻译：用他莫昔芬类似物预防和治疗心血管病变
公开(公告)号：US20060135560A1
公开(公告)日：2006-06-22
申请号：US10729056
申请日：2003-12-05
申请人： David Grainger , James Metcalfe , Lawrence Kunz , Robert Schroff
发明人： David Grainger , James Metcalfe , Lawrence Kunz , Robert Schroff
IPC分类号： A61K31/445 , A61K31/40 , A61K31/138
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 tamoxifin 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（C 1 -C 4）烷基，R 1和R 2各自独立地是（ C 1 -C 4烷基或与N一起为饱和杂环基，R 3是乙基或氯乙基，R 4 H，R 5是I，O（C 1 -C 4 -C 4）烷基或H和R 6 是（O）（C 1 -C 4）烷基或H，条件是当R 4，R 0 > 5，且R 6为H，R 3不为乙基; 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。

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