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公开(公告)号：US20140316104A1
公开(公告)日：2014-10-23
申请号：US14241126
申请日：2012-08-29
申请人： Gunter Fischer , Miroslav Malesevic , Frank Erdmann , Jan Kuhling , Michael Bukrinsky , Stephanie Constant , Gerd Ruhter , Peter Nussbaumer , Klaus Dinkel
发明人： Gunter Fischer , Miroslav Malesevic , Frank Erdmann , Jan Kuhling , Michael Bukrinsky , Stephanie Constant , Gerd Ruhter , Peter Nussbaumer , Klaus Dinkel
IPC分类号： C07K7/64
CPC分类号： C07K7/645 , C12N9/90 , C12Y502/01008
摘要： The present invention relates to novel cyclosporin derivatives that do not cross the cellular membrane. The compounds according to the invention are used in medicine, more particularly in the treatment/diagnosis of acute and chronic inflammatory diseases, viral infections, cancer, degenerative muscle diseases, neurodegenerative diseases and damage that is associated with calcium homeostasis impairment. The novel cyclosporin derivatives additionally have no immunosuppressive effect.
摘要翻译： 本发明涉及不与细胞膜交叉的新型环孢菌素衍生物。 根据本发明的化合物用于医学中，更特别地用于治疗/诊断急性和慢性炎性疾病，病毒感染，癌症，退行性肌肉疾病，神经变性疾病以及与钙稳态损伤相关的损伤。 新型环孢菌素衍生物另外没有免疫抑制作用。
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公开(公告)号：US09453051B2
公开(公告)日：2016-09-27
申请号：US14241126
申请日：2012-08-29
申请人： Gunter Fischer , Miroslav Malesevic , Frank Erdmann , Jan Kuhling , Michael Bukrinsky , Stephanie Constant , Gerd Ruhter , Peter Nussbaumer , Klaus Dinkel
发明人： Gunter Fischer , Miroslav Malesevic , Frank Erdmann , Jan Kuhling , Michael Bukrinsky , Stephanie Constant , Gerd Ruhter , Peter Nussbaumer , Klaus Dinkel
CPC分类号： C07K7/645 , C12N9/90 , C12Y502/01008
摘要： The present invention relates to novel cyclosporin derivatives that do not cross the cellular membrane. The compounds according to the invention are used in medicine, more particularly in the treatment/diagnosis of acute and chronic inflammatory diseases, viral infections, cancer, degenerative muscle diseases, neurodegenerative diseases and damage that is associated with calcium homeostasis impairment. The novel cyclosporin derivatives additionally have no immunosuppressive effect.
摘要翻译： 本发明涉及不与细胞膜交叉的新型环孢菌素衍生物。 根据本发明的化合物用于医学中，更特别地用于治疗/诊断急性和慢性炎性疾病，病毒感染，癌症，退行性肌肉疾病，神经变性疾病以及与钙稳态损伤相关的损伤。 新型环孢菌素衍生物另外没有免疫抑制作用。
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公开(公告)号：US08618065B2
公开(公告)日：2013-12-31
申请号：US13397256
申请日：2012-02-15
申请人： Gunter Fischer , Miroslav Malesevic , Frank Erdmann , Jan Kühling , Michael Bukrinsky , Stephanie Constant
发明人： Gunter Fischer , Miroslav Malesevic , Frank Erdmann , Jan Kühling , Michael Bukrinsky , Stephanie Constant
摘要： A cyclosporin derivative of general Formula (I) or a pharmaceutically compatible salt thereof, which have a pharmaceutical effectiveness, for example in the case of chronic inflammatory diseases. The cyclosporin derivatives are preferably free from a peptide section capable of passing through the membrane of a biological cell.
摘要翻译： 具有药物有效性的通式（I）的环孢菌素衍生物或其药学上相容的盐，例如在慢性炎性疾病的情况下。 环孢菌素衍生物优选不含能够通过生物细胞膜的肽段。
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公开(公告)号：US20120196749A1
公开(公告)日：2012-08-02
申请号：US13397256
申请日：2012-02-15
申请人： Gunter Fischer , Miroslav Malesevic , Frank Erdmann , Jan Kühling , Michael Bukrinsky , Stephanie Constant
发明人： Gunter Fischer , Miroslav Malesevic , Frank Erdmann , Jan Kühling , Michael Bukrinsky , Stephanie Constant
IPC分类号： A01N43/713 , A61K38/13 , A61P29/00 , A61P11/06 , A01P21/00 , A61P17/06 , A61P25/00 , A61P1/04 , C12N5/071 , A01P13/00 , C07K7/64 , A61P19/02
摘要： A cyclosporin derivative of general Formula (I) or a pharmaceutically compatible salt thereof, which have a pharmaceutical effectiveness, for example in the case of chronic inflammatory diseases. The cyclosporin derivatives are preferably free from a peptide section capable of passing through the membrane of a biological cell.
摘要翻译： 具有药物有效性的通式（I）的环孢菌素衍生物或其药学上相容的盐，例如在慢性炎性疾病的情况下。 环孢菌素衍生物优选不含能够通过生物细胞膜的肽段。
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公开(公告)号：US5808068A
公开(公告)日：1998-09-15
申请号：US912076
申请日：1997-08-15
申请人： Senliang Pan , Michael Bukrinsky , Omar K. Haffar
发明人： Senliang Pan , Michael Bukrinsky , Omar K. Haffar
IPC分类号： A61K31/505 , A61P31/18 , C07D239/46 , C07D239/48 , C07D239/50 , C07D239/24 , A61K31/495
CPC分类号： C07D239/47 , C07D239/48
摘要： There is disclosed a genus of compounds that have anti-HIV infection therapeutic activity and inhibit nuclear localization of the HIV preintegration complex.
摘要翻译： 公开了具有抗HIV感染治疗活性并抑制HIV预整合复合物的核定位的化合物属。
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公开(公告)号：US6019979A
公开(公告)日：2000-02-01
申请号：US911879
申请日：1997-08-15
申请人： Michael Bukrinsky , Massimo Alfano
发明人： Michael Bukrinsky , Massimo Alfano
IPC分类号： A61K45/00 , A61K38/00 , A61K38/16 , A61K39/12 , A61K39/21 , A61K39/39 , A61P31/04 , A61P31/12 , A61P31/18 , A61P37/04 , A01N37/18
CPC分类号： A61K38/164 , A61K39/12 , A61K39/21 , A61K39/39 , A61K2039/55544 , C12N2740/16034
摘要： There is disclosed a method for anti-viral therapy treatment with the Pertussis toxin beta subunit oligomer, wherein the oligomer is composed of from two to ten subunits of PTX selected from the group consisting of S2, S3, S4, S5, and combinations thereof.
摘要翻译： 公开了一种用百日咳毒素β亚基低聚物进行抗病毒治疗的方法，其中低聚物由选自S2，S3，S4，S5及其组合的PTX的2至10个亚基组成。
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7.发明授权Method of suppressing human immunodeficiency virus (HIV) replication in a subject by administering a liver X receptor (LXR) agonist 失效通过施用肝脏X受体（LXR）激动剂来抑制受试者中的人类免疫缺陷病毒（HIV）复制的方法公开(公告)号：US08470526B2
公开(公告)日：2013-06-25
申请号：US11528431
申请日：2006-09-28
申请人： Michael Bukrinsky , Dmitri Sviridov
发明人： Michael Bukrinsky , Dmitri Sviridov
IPC分类号： C12Q1/70
CPC分类号： A61K39/42
摘要： The present invention provides novel methods for treating and preventing coronary artery disease in HIV-1-infected individuals by interfering with Nef-mediated effect on ABCA1. The invention further provides novel methods for suppressing HIV infection by stimulating cholesterol efflux from cells by stimulating expression of ABCA1 in HIV-1-infected individuals. These methods take advantage of the finding that Nef, a regulatory protein of HIV-1, (1) diminishes expression of ATP-binding cassette transporter A1 (ABCA1), the main transporter of cholesterol from cells to extracellular acceptors; and (2) impairs cholesterol efflux from HIV-1-infected macrophages leading to cholesterol accumulation and formation of foam cells, which is a characteristic feature of atherosclerosis.
摘要翻译： 本发明提供了通过干扰Nef介导的对ABCA1的作用来治疗和预防HIV-1感染个体的冠状动脉疾病的新方法。 本发明还提供了通过刺激HIV-1感染个体中ABCA1的表达来刺激来自细胞的胆固醇流出来抑制HIV感染的新方法。 这些方法利用了HIV-1的调节蛋白Nef（1）降低了ATP结合盒转运蛋白A1（ABCA1）的表达的结果，这是胆固醇从细胞到细胞外受体的主要转运体; 和（2）损害从HIV-1感染的巨噬细胞胆固醇流出导致胆固醇积聚和形成泡沫细胞，这是动脉粥样硬化的特征。
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公开(公告)号：US5849793A
公开(公告)日：1998-12-15
申请号：US911883
申请日：1997-08-15
申请人： Senliang Pan , Michael Bukrinsky , Omar K. Haffar
发明人： Senliang Pan , Michael Bukrinsky , Omar K. Haffar
IPC分类号： A61K45/00 , A61K31/216 , A61K31/235 , A61K31/427 , A61K31/496 , A61P31/18 , A61P37/04 , A61P43/00 , C07C69/738 , C07C69/76 , C07C321/00 , C07C323/00 , A61K31/22
CPC分类号： C07C69/738
摘要： There is disclosed a structural genus of compounds, defined according to coordinates in three-dimensional space, that binds amino moieties on neighboring lysine residues in a tyrosine residue 29 pocket of the matrix protein component of the HIV preintegration complex (PIC), thereby preventing the PIC from binding to karyopherin .alpha. and preventing nuclear importation and integration of the HIV viral genome into the host cell DNA, thereby preventing viral infection.
摘要翻译： 公开了根据三维空间坐标定义的化合物的结构类，其结合HIV预整合复合物（PIC）的基质蛋白组分的酪氨酸残基29口袋中的相邻赖氨酸残基上的氨基部分，从而防止 PIC与结合核糖蛋白α并防止HIV病毒基因组进入宿主细胞DNA进入和整合，从而防止病毒感染。
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9.发明授权Guanylhydrazones useful for treating diseases associated with T cell activation 失效可用于治疗与T细胞活化有关的疾病的脒腙公开(公告)号：US07741372B2
公开(公告)日：2010-06-22
申请号：US10619426
申请日：2003-07-16
IPC分类号： A61K31/15 , A61K31/155 , A61K31/505 , A61K45/06
CPC分类号： A61K31/167 , Y02A50/401 , Y02A50/409 , Y10S514/934
摘要： There is disclosed a method for treating diseases and disorders involving T cell activation and HIV-infection using the p38 mitogen activated protein kinase (MAPK) signaling pathway as a target for intervention. There is further disclosed a use for guanylhydrazone-substituted compounds to treat diseases and disorders related to T cell activation and HIV-infection.
摘要翻译： 公开了使用p38丝裂原活化蛋白激酶（MAPK）信号传导途径作为干预对象，治疗涉及T细胞活化和HIV感染的疾病和病症的方法。 进一步公开了用于脒腙取代的化合物治疗与T细胞活化和HIV感染相关的疾病和病症的用途。
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10.发明授权Guanylhydrazones useful for treating diseases associated with T cell activation 失效可用于治疗与T细胞活化有关的疾病的脒腙
公开(公告)号：US06143728A
公开(公告)日：2000-11-07
申请号：US970973
申请日：1997-11-14
IPC分类号： A61K45/00 , A61K31/15 , A61K31/155 , A61K31/167 , A61K38/00 , A61P3/10 , A61P17/06 , A61P29/00 , A61P31/12 , A61P31/18 , A61P37/00 , A01N43/04 , A01N47/28 , C12Q1/68 , C07H19/00
CPC分类号： A61K31/167 , Y10S514/934
摘要： There is disclosed a method for treating diseases and disorders involving T cell activation and HIV-infection, using the p38 mitogen activated protein kinase (MAPK) signaling pathway as a target for intervention. There is further disclosed a use for guanylhydrazone-substituted compounds to treat diseases and disorders related to T cell activation and HIV-infection.
摘要翻译： 公开了使用p38丝裂原活化蛋白激酶（MAPK）信号传导途径作为干预对象的治疗涉及T细胞活化和HIV感染的疾病和病症的方法。 进一步公开了用于脒腙取代的化合物治疗与T细胞活化和HIV感染相关的疾病和病症的用途。
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