发明申请
US20060135560A1 Prevention and treatment of cardiovascular pathologies with tamoxifen analogues
审中-公开
用他莫昔芬类似物预防和治疗心血管病变
- 专利标题: Prevention and treatment of cardiovascular pathologies with tamoxifen analogues
- 专利标题(中): 用他莫昔芬类似物预防和治疗心血管病变
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申请号: US10729056申请日: 2003-12-05
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公开(公告)号: US20060135560A1公开(公告)日: 2006-06-22
- 发明人: David Grainger , James Metcalfe , Lawrence Kunz , Robert Schroff
- 申请人: David Grainger , James Metcalfe , Lawrence Kunz , Robert Schroff
- 专利权人: NeoRx Corporation
- 当前专利权人: NeoRx Corporation
- 主分类号: A61K31/445
- IPC分类号: A61K31/445 ; A61K31/40 ; A61K31/138
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).
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