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1.发明授权Use of 40-O-(2-hydroxy)ethylrapamycin for treatment of restenosis and other disorders 有权40-O-（2-羟基）乙基雷帕霉素用于治疗再狭窄和其他疾病公开(公告)号：US06384046B1
公开(公告)日：2002-05-07
申请号：US09712359
申请日：2000-11-14
IPC分类号： A61K3144
CPC分类号： A61K31/436
摘要： This invention relates to the use of 40-O-(2-hydroxy)ethyl-rapamycin for the prevention or treatment of neointimal proliferation and thickening, restenosis, and vascular occlusion following vascular injury.
摘要翻译： 本发明涉及40-O-（2-羟基）乙基 - 雷帕霉素在血管损伤后预防或治疗新生内膜增生和增厚，再狭窄和血管闭塞的用途。
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2.发明申请USE OF RAPAMYCIN DERIVATIVES IN VASCULOPATHIES AND XENOTRANSPLANTATION 审中-公开RAPAMYCIN衍生物在血管造影和XENOTRANSPLANTATION中的应用公开(公告)号：US20120177690A1
公开(公告)日：2012-07-12
申请号：US13357199
申请日：2012-01-24
IPC分类号： A61K31/436 , A61P35/00 , A61P37/06
CPC分类号： A61K31/436
摘要： Use of a rapamycin derivative of formula I as defined in the claims for preventing or treating vasculopathies and manifestations of xenotransplantation.
摘要翻译： 在权利要求中定义的式I的雷帕霉素衍生物用于预防或治疗血管病变和异种移植的表现的用途。
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公开(公告)号：US20100152105A1
公开(公告)日：2010-06-17
申请号：US12715007
申请日：2010-03-01
CPC分类号： A61K31/436
摘要： The present invention is directed to the use of a rapamycin derivative of formula I in combination with cyclosporin for preventing or treating manifestations of chronic rejection in a recipient of an organ or tissue transplant.
摘要翻译： 本发明涉及式I的雷帕霉素衍生物与环孢菌素的组合用于预防或治疗器官或组织移植受者的慢性排斥反应的表现。
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![Isothiourea derivatives of imadazo[2,1-b]Thiazoles and 5,6-dihydro derivatives thereof useful as CXCR4 chemokine receptor inhibitors](/abs-image/US/2010/03/02/US07671078B2/abs.jpg.150x150.jpg)
4.发明授权Isothiourea derivatives of imadazo[2,1-b]Thiazoles and 5,6-dihydro derivatives thereof useful as CXCR4 chemokine receptor inhibitors 失效咪唑并〔2,1-b〕噻唑及其5,6-二氢衍生物作为CXCR4趋化因子受体抑制剂有用的异硫脲衍生物公开(公告)号：US07671078B2
公开(公告)日：2010-03-02
申请号：US10590399
申请日：2005-02-25
IPC分类号： C07D513/04 , A61K31/429 , C07D513/14 , A61K31/519 , A61P35/04 , A61P37/06 , A61P31/14
CPC分类号： C07D277/42 , C07D513/04
摘要： The invention relates to isothiourea derivatives of formula I: wherein R1 is a residue of one of the following structures: where the variables are as defined in the claims of the invention, as well as processes for production of these compounds.
摘要翻译： 本发明涉及式I的异硫脲衍生物：其中R1是以下结构之一的残基：其中变量如本发明权利要求所定义，以及这些化合物的制备方法。
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公开(公告)号：US06632978B1
公开(公告)日：2003-10-14
申请号：US09693011
申请日：2000-10-20
申请人： Edgar Käslin , Marcel Luyten , Hans-Günter Zerwes
发明人： Edgar Käslin , Marcel Luyten , Hans-Günter Zerwes
IPC分类号： A01K67027
CPC分类号： C12N15/8509 , A01K67/0275 , A01K67/0276 , A01K2217/072 , A01K2217/075 , A01K2227/105 , A01K2267/0368 , A01K2267/0393 , C12N2800/30
摘要： A transgenic non-human animal (e.g., a transgenic mouse) comprising a polynucleotide encoding a soluble marker protein functionally linked to a regulatory sequence of an endogenous gene encoding E-selectin. Also described are methods for detecting modulators of the E-selectin gene using said transgenic non-human animal, and cultured cells obtained therefrom.
摘要翻译： 包含编码与编码E-选择蛋白的内源基因的调节序列功能性连接的可溶性标记蛋白的多核苷酸的转基因非人动物（例如，转基因小鼠）。 还描述了使用所述转基因非人动物检测E-选择蛋白基因的调节剂的方法，以及从其获得的培养细胞。
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公开(公告)号：US07399771B2
公开(公告)日：2008-07-15
申请号：US10529776
申请日：2003-10-06
申请人： Rainer Albert , Nigel Graham Cooke , Gebhard Thoma , Christian Bruns , François Nuninger , Markus Streiff , Hans-Günter Zerwes
发明人： Rainer Albert , Nigel Graham Cooke , Gebhard Thoma , Christian Bruns , François Nuninger , Markus Streiff , Hans-Günter Zerwes
IPC分类号： A61K31/445 , C07D401/14
CPC分类号： C07D401/14 , C07D211/58 , C07D405/14 , C07D409/14 , C07D417/14
摘要： Disclosed are compounds of formula I: wherein R1, R2, R3 and X are as defined herein, in free or salt form, which are useful as CCR5 inhibitors, e.g. in the prevention or treatment of disorders mediated by interactions between chemokine receptors and their ligands.
摘要翻译： 公开了式I化合物：其中R 1，R 2，R 3和X如本文所定义，为游离或盐形式， 其可用作CCR5抑制剂，例如 在预防或治疗由趋化因子受体及其配体之间相互作用介导的疾病。
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公开(公告)号：US07666877B2
公开(公告)日：2010-02-23
申请号：US11914570
申请日：2006-05-29
申请人： Rolf Baenteli , Fraser Glickman , Jiri Kovarik , Ian Lewis , Markus Streiff , Gebhard Thoma , Hans-Günter Zerwes
发明人： Rolf Baenteli , Fraser Glickman , Jiri Kovarik , Ian Lewis , Markus Streiff , Gebhard Thoma , Hans-Günter Zerwes
IPC分类号： A61K31/48 , C07D457/08
CPC分类号： C07D457/06 , C07D457/08
摘要： Disclosed are ergoline derivatives, Formula (I), wherein either each of R1 and R2, independently, is H; optionally R10 and/or R11-substituted-phenyl or -phenyl-C1-4alkyl; optionally R10 and/or R11-substituted-heteroaryl or -heteroaryl-C1-4alkyl; optionally R10 and/or R11-substituted heteroaryl N-oxide; optionally R10-substituted C1-C8 alkyl; optionally R10-substituted C2-C8 alkenyl, optionally R10-substituted C2-C8 alkynyl; optionally R10-substituted C3-C8 cycloalkyl, or optionally R10-substituted C4-C8 cycloalkenyl; or R1 and R2 form together with the nitrogen atom to which they are attached an optionally R10-substituted 3-8 membered ring containing in addition to the nitrogen atom up to 2 heteroatoms selected independently from N, O and S; R3 is H; OR1; CH2R1R2; (CH2)1-2NR1R2; CH2—CH2—OR1; CH2—CO—NR1R2; or CO—CH2R1R2; R4 is F; Cl; Br; I; OR1; NR1R2 or has one of the significances given for R1; and R5 has one of the significances given for R1, in free form or in salt form for preventing or treating disorders or diseases mediated by interactions between chemokine receptors and their ligands.
摘要翻译： 公开了麦角灵衍生物，式（I），其中R 1和R 2各自独立地为H; 任选的R 10和/或R 11取代的苯基或 - 苯基-C 1-4烷基; 任选的R 10和/或R 11取代的杂芳基或 - 杂芳基-C 1-4烷基; 任选的R 10和/或R 11取代的杂芳基N-氧化物; 任选的R 10取代的C 1 -C 8烷基; 任选的R 10取代的C 2 -C 8烯基，任选的R 10取代的C 2 -C 8炔基; 任选的R 10取代的C 3 -C 8环烷基，或任选的R 10取代的C 4 -C 8环烯基; 或R 1和R 2与它们所连接的氮原子一起形成任选的R 10取代的3-8元环，除了氮原子以外，还含有独立地选自N，O和S的2个杂原子; R3为H; OR1; CH2R1R2; （CH2）1-2NR1R2; CH2-CH2-OR1; CH2-CO-NR1R2; 或CO-CH 2 R 1 R 2; R4是F; Cl; Br; 一世; OR1; NR1R2或具有R1的意义之一; R5具有以游离形式或盐形式用于预防或治疗由趋化因子受体及其配体之间相互作用介导的疾病或疾病的R1的意义。
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公开(公告)号：US20100010025A1
公开(公告)日：2010-01-14
申请号：US12374524
申请日：2007-07-19
申请人： Rudolf Duthaler , Marc Gerspacher , Philipp Holzer , Markus Streiff , Gebhard Thoma , Rudolf Walchli , Hans-Günter Zerwes
发明人： Rudolf Duthaler , Marc Gerspacher , Philipp Holzer , Markus Streiff , Gebhard Thoma , Rudolf Walchli , Hans-Günter Zerwes
IPC分类号： A61K31/506 , C07D239/42 , A61K31/505 , C07D401/12 , C07D401/14
CPC分类号： C07D239/48 , C07D401/12 , C07D403/12 , C07D403/14 , C07D409/12 , C07D417/12 , C07D471/04
摘要： Disclosed are pyrimidine derivatives having interesting pharmacological properties.
摘要翻译： 公开了具有令人感兴趣的药理学性质的嘧啶衍生物。
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