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公开(公告)号：US20080113015A1
公开(公告)日：2008-05-15
申请号：US11569514
申请日：2005-05-24
IPC分类号： A61K9/127 , A61K38/16 , A61K31/715 , A61P43/00
CPC分类号： A61K9/1271
摘要： The present invention relates to liposomes for drug delivery, wherein a liposome includes molecules of at least one desired drug distributed within an aqueous phase in the interior of the liposome and wherein the liposome further includes molecules of the same or of another drug attached to either or both sides of the liposomal membrane. More specifically, the invention relates to liposomes, wherein at least a part of the molecules of a desired drug bear a functional group that is reactive with a functional group present in at least one lipid fraction, and wherein the drug is covalently linked to the membrane lipids by chemical bonding, e.g. by ester bonding of a hydroxyl group of a lipid molecule and an acidic residue of the drug. In a preferred embodiment, the desired drug is a glycoprotein such as erythropoietin. The invention further relates to a method of manufacture of said liposomes and to pharmaceutical compositions containing them.
摘要翻译： 本发明涉及用于药物递送的脂质体，其中脂质体包括分布在脂质体内部的水相内的至少一种所需药物的分子，并且其中所述脂质体还包括与所述脂质体或其它药物相连接的分子， 脂质体膜两侧。 更具体地，本发明涉及脂质体，其中所需药物的至少一部分分子具有与存在于至少一种脂质部分中的官能团反应的官能团，并且其中所述药物与膜共价连接 脂质通过化学键合，例如 通过脂质分子的羟基和药物的酸性残基的酯键合。 在优选的实施方案中，所需药物是糖蛋白，例如红细胞生成素。 本发明还涉及制备所述脂质体的方法和含有它们的药物组合物。
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2.发明授权Liposomal composition comprising an active ingredient for relaxing smooth muscle, the production of this composition and the therapeutic use thereof 有权包含用于松弛平滑肌的活性成分的脂质体组合物，该组合物的制备及其治疗用途公开(公告)号：US08524274B2
公开(公告)日：2013-09-03
申请号：US11577488
申请日：2005-10-14
CPC分类号： A61K9/127 , A61K9/0034 , A61K9/06 , A61K9/1277 , A61K9/1278
摘要： The invention relates to a pharmaceutical composition made from an active ingredient included in liposomes for topical application, whereby the liposomes have an aqueous medium in the interior thereof and contain at least one active ingredient therein which exerts a direct or indirect relaxing effect on smooth musculature and is preferably selected from the group of prostaglandins, adenylate cyclases, cAMP, AMP, ATP, NO-synthetases, nitrogen monoxide (NO), NO compounds, nitrates, guanylate cyclases, cGMP, GMP, GTP and phosphodiesterases, in particular, Sildenafil. The invention further relates to a method for production of said composition, optionally, in sterile form and the use of the liposomes supporting the active ingredient in various galenic forms for external application in the genital region, for prophylaxis and/or therapy of sexual disorders in men or women and/or for increase of sexual sensitivity.
摘要翻译： 本发明涉及由用于局部应用的脂质体中包含的活性成分制成的药物组合物，其中所述脂质体在其内部具有水性介质并且含有其中的至少一种活性成分，其对平滑肌肉组织施加直接或间接的缓解作用， 优选选自前列腺素，腺苷酸环化酶，cAMP，AMP，ATP，NO-合成酶，一氧化氮（NO），NO化合物，硝酸盐，鸟苷酸环化酶，cGMP，GMP，GTP和磷酸二酯酶，特别是西地那非。 本发明进一步涉及用于生产所述组合物的方法，任选地以无菌形式，以及使用支持活性成分的各种盖仑样形式的外源性生物区域用于预防和/或治疗性障碍的用途 男性或女性和/或增加性敏感性。
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3.发明申请LIPOSOMAL COMPOSITION COMPRISING AN ACTIVE INGREDIENT FOR RELAXING SMOOTH MUSCLE, THE PRODUCTION OF THIS COMPOSITION AND THE THERAPEUTIC USE THEREOF 有权包含用于放松平滑肌肉的活性成分的脂质组合物，该组合物的生产及其治疗用途公开(公告)号：US20090324698A1
公开(公告)日：2009-12-31
申请号：US11577488
申请日：2005-10-14
IPC分类号： A61K9/127 , A61P15/00 , A61K31/519 , A61K31/4985
CPC分类号： A61K9/127 , A61K9/0034 , A61K9/06 , A61K9/1277 , A61K9/1278
摘要： The invention relates to a pharmaceutical composition made from an active ingredient included in liposomes for topical application, whereby the liposomes have an aqueous medium in the interior thereof and contain at least one active ingredient therein which exerts a direct or indirect relaxing effect on smooth musculature and is preferably selected from the group of prostaglandins, adenylate cyclases, cAMP, AMP, ATP, NO-synthetases, nitrogen monoxide (NO), NO compounds, nitrates, guanylate cyclases, cGMP, GMP, GTP and phosphodiesterases, in particular, Sildenafil. The invention further relates to a method for production of said composition, optionally, in sterile form and the use of the liposomes supporting the active ingredient in various galenic forms for external application in the genital region, for prophylaxis and/or therapy of sexual disorders in men or women and/or for increase of sexual sensitivity.
摘要翻译： 本发明涉及由用于局部应用的脂质体中包含的活性成分制成的药物组合物，其中所述脂质体在其内部具有水性介质并且含有其中的至少一种活性成分，其对平滑肌肉组织施加直接或间接的缓解作用， 优选选自前列腺素，腺苷酸环化酶，cAMP，AMP，ATP，NO-合成酶，一氧化氮（NO），NO化合物，硝酸盐，鸟苷酸环化酶，cGMP，GMP，GTP和磷酸二酯酶，特别是西地那非。 本发明进一步涉及用于生产所述组合物的方法，任选地以无菌形式，以及使用支持活性成分的各种盖仑样形式的外源性生物区域用于预防和/或治疗性障碍的用途 男性或女性和/或增加性敏感性。
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公开(公告)号：US06843942B2
公开(公告)日：2005-01-18
申请号：US10415414
申请日：2001-10-31
CPC分类号： A61K9/1277 , B01J13/02 , Y10T428/2984
摘要： The invention relates to a device for producing lipid vesicles, which is equipped with a line (1) for transporting a polar liquid phase, with a line (2) for transporting an organic liquid phase containing lipids, with a collecting receptacle (7) for accommodating produced lipid vesicles, and with means for conveying the liquid phases through lines (1) and (2). At at least one location, the outer side of line (1) forms a common contact surface with line (2) inside of which a common opening (3) is provided that permits the flow of liquid and joins the inside of line (2) to the inside of line (1). Lines (1) and (2) do not contain agitating or dispersing aids in the area of the opening (3). The invention also relates to a method for the careful production of lipid vesicles, wherein the lipid phase is sprayed under pressure perpendicular to the direction of flow of the polar phase and into the same, whereupon lipid vesicles having a narrow size distribution form spontaneously and without the action of mechanical agitating or dispersing aids.
摘要翻译： 本发明涉及一种用于生产脂质囊泡的装置，其装备有用于输送极性液相的管线（1）和用于输送含有脂质的有机液相的管线（2），其中收集容器（7）用于 容纳产生的脂质囊泡，以及用于通过管线（1）和（2）输送液相的装置。 在至少一个位置处，管线（1）的外侧与管线（2）形成共同的接触表面，内部具有允许液体流动并连接管线（2）内部的公共开口（3） 到线（1）的内部。 线（1）和（2）在开口（3）的区域不包含搅拌或分散助剂。 本发明还涉及一种仔细生产脂质囊泡的方法，其中脂质相在垂直于极性相流动方向的压力下喷雾并进入脂质囊泡，由此自发地形成具有窄尺寸分布的脂质囊泡 机械搅拌或分散助剂的作用。
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5.发明授权Liposomal recombinant human superoxide-dismutase for the treatment of peyronie's disease 有权脂质体重组人超氧化物歧化酶用于治疗白喉病公开(公告)号：US06312720B1
公开(公告)日：2001-11-06
申请号：US09327174
申请日：1999-06-07
IPC分类号： A61K9133
CPC分类号： A61K9/0019 , A23L5/25 , A61K8/14 , A61K8/66 , A61K9/0014 , A61K9/127 , A61K38/446 , A61K47/36 , A61K2800/52 , A61Q17/00 , A61Q19/00 , A61Q19/004
摘要： Superoxide dismutase (SOD), preferably rhSOD, is used in liposomes, optionally mixed with hyaluronic acid and/or at least one physiologically acceptable carrier, and other optional additives, to prepare a pharmaceutical composition useful against increased concentrations of superoxide radicals and/or the damage caused thereby. The compositions are administered topically, preferably as gels or ointments, to prevent and/or heal human fibrotic tissue degeneration diseases, in particular induratio penis plastica (Peyronie's Disease).
摘要翻译： 超氧化物歧化酶（SOD），优选rhSOD，用于脂质体，任选地与透明质酸和/或至少一种生理学上可接受的载体和其它任选的添加剂混合，以制备可用于增加浓度超氧自由基和/或 造成的损害。 组合物局部给药，优选用凝胶或软膏，以预防和/或愈合人纤维化组织变性疾病，特别是阴茎勃氏塑型（Peyronie's disease）。
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公开(公告)号：US5942245A
公开(公告)日：1999-08-24
申请号：US836185
申请日：1997-05-05
IPC分类号： A23L5/20 , A61K8/14 , A61K8/66 , A61K9/00 , A61K9/127 , A61K9/133 , A61K38/44 , A61K47/36 , A61Q17/00 , A61Q19/00 , C12N9/02
CPC分类号： A61K9/0019 , A23L5/25 , A61K38/446 , A61K8/14 , A61K8/66 , A61K9/0014 , A61K9/127 , A61Q19/00 , A61K2800/52 , A61K47/36 , A61Q17/00 , A61Q19/004
摘要： Superoxide dismutase (SOD), preferably rhSOD, is used in liposomes, optionally mixed with hyaluronic acid and/or at least one physiologically acceptable carrier, and other optional additives, to prepare a pharmaceutical composition useful against increased concentrations of superoxide radicals and/or the damage caused thereby. These compositions can be administered topically, orally and/or parenterally to prevent and/or heal burns, skin lesions due to radiation, inflammations, rheumatic and arthritic diseases, bronchitis, ARDS, emphysema, allergic oedemas and other inflammatory process, possibly trigged by microbial infections. They may also be used in the cosmetic treatment of furuncles, acne and the like. They may also be used to improve the preservability of organic, preferably biogenic, materials, in particular organ transplants and liquids with organic components, as well as foodstuffs.
摘要翻译： PCT No.PCT / EP95 / 04352 Sec。 371日期1997年7月1日 102（e）日期1997年7月1日PCT提交1995年11月6日PCT公布。 WO96 / 14083 PCT出版物 日期1996年5月17日超氧化物歧化酶（SOD），优选rhSOD，用于脂质体，任选地与透明质酸和/或至少一种生理学上可接受的载体和其它任选的添加剂混合，以制备可用于增加超氧化物自由基浓度的药物组合物 和/或由此造成的损害。 这些组合物可以局部，口服和/或肠胃外给药以预防和/或愈合灼伤，由辐射引起的皮肤损伤，炎症，风湿性关节炎疾病，支气管炎，ARDS，肺气肿，过敏性水肿和其他可能由微生物触发的炎性过程 感染。 它们也可用于治疗fur，痤疮等的美容治疗。 它们也可用于改善有机，优选生物源的材料，特别是具有有机组分的器官移植物和液体以及食品的保存性。
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公开(公告)号：US07595049B2
公开(公告)日：2009-09-29
申请号：US10485525
申请日：2002-09-09
CPC分类号： C07K14/005 , A61K39/00 , A61K2039/505 , C07K16/1063 , C07K2317/21 , C07K2317/34 , C12N2740/16122
摘要： The present invention relates to neutralizing anti-HIV-1 antibodies, particularly to mAb 4E10-IgG1, which has an HIV-1 neutralizing potency comparable to the one of mAb 2F5 and 2G12. 4E10-IgG1 binds to a novel conserved epitope (NWFDIT) C-terminal of the ELDKWA epitope recognized by 2F5.1 appears that both epitopes are cryptic epitopes within a region that may be accessible in a virus-cell fusion intermediate state only. 4E10-IgG1 potently neutralizes tissue culture adapted strains but also primary isolates of different clades, including A, B, C, D, and E, inclusing viruses that were found to be resistant to 2F5. None of the tested isolates was resistant to both anti-gp41-antibodies. The invention therefore also relates to peptides containing the 4E10 epitope and to compositions made thereof, as well as to anti-idiotypic antibodies that are reactive with the paratope of 4E10-IgG1, to compositions containing an antiidiotypic antibody optionally in combination with a peptide containing the 4E10 epitope, and to anti-HIV-1 compositions comprising 4E10-IgG1, optionally in combination with another neutralizing antibody such as 2F5 and/or 2G12.
摘要翻译： 本发明涉及中和抗HIV-1抗体，特别是抗mAb 4E10-IgG1，其具有与mAb 2F5和2G12中的一种相当的HIV-1中和效力。 4E10-IgG1与2F5.1识别的ELDKWA表位的新保守表位（NWFDIT）C-末端结合似乎是两个表位是仅在病毒 - 细胞融合中间状态可以接近的区域内的隐性表位。 4E10-IgG1有力地中和组织培养适应菌株，也可以中和不同进化枝的初级分离物，包括A，B，C，D和E，包括被发现对2F5有抗性的病毒。 没有一个测试的分离株对抗gp41-抗体均有抗性。 因此，本发明还涉及含有4E10表位的肽及其制备的组合物，以及与4E10-IgG1的相互作用反应的抗独特型抗体，所述组合物含有抗独立型抗体，所述组合物任选地与含有 4E10表位，以及包含4E10-IgG1的抗HIV-1组合物，任选地与另一种中和抗体如2F5和/或2G12组合。
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公开(公告)号：US20050080240A1
公开(公告)日：2005-04-14
申请号：US10501726
申请日：2003-01-17
CPC分类号： C07K16/4225 , A61K39/00 , A61K2039/505
摘要： The invention relates to Ab2-type anti-idiotypic antibodies and fragments thereof which mimic HVI-1 epitopes that are otherwise cryptic to the immune system and which antibodies or fragments thereof are directed against potently neutralizing anti-HIV-1 antibodies. The invention further relates to a hybridoma cell line 3H6 expressing the anti-idiotypic antibody and to pharmaceutical compositions containing the antibody or fragment thereof. The invention also relates to HIV-1 neutralizing Ab3-type antibodies elicited upon administration of the Ab2-type anti-idiotypic antibody or fragment thereof and to pharmaceutical compositions containing them. The invention also relates to the use of the present antibodies or fragments thereof as screening tools or as diagnostic or therapeutic agents.
摘要翻译： 本发明涉及Ab2型抗独特型抗体及其片段，其模拟HVI-1表位，否则其对于免疫系统是隐秘的，哪些抗体或其片段针对有效中和抗HIV-1抗体。 本发明还涉及表达抗独特型抗体的杂交瘤细胞系3H6和含有抗体或其片段的药物组合物。 本发明还涉及在施用Ab2型抗独特型抗体或其片段时引发的HIV-1中和Ab3型抗体以及含有它们的药物组合物。 本发明还涉及本发明的抗体或其片段作为筛选工具或诊断或治疗剂的用途。
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9.发明授权Anti-idiotypic monoclonal antibody reactive with HIV neutralizing antibody 2F5 失效与HIV中和抗体2F5反应的抗独特型单克隆抗体公开(公告)号：US07625566B2
公开(公告)日：2009-12-01
申请号：US10501726
申请日：2003-01-17
CPC分类号： C07K16/4225 , A61K39/00 , A61K2039/505
摘要： The invention relates to Ab2-type anti-idiotypic antibodies and fragments thereof which mimic HVI-1 epitopes that are otherwise cryptic to the immune system and which antibodies or fragments thereof are directed against potently neutralizing anti-HIV-1 antibodies. The invention further relates to a hybridoma cell line 3H6 expressing the anti-idiotypic antibody and to pharmaceutical compositions containing the antibody or fragment thereof. The invention also relates to HIV-1 neutralizing Ab3-type antibodies elicited upon administration of the Ab2-type anti-idiotypic antibody or fragment thereof and to pharmaceutical compositions containing them. The invention also relates to the use of the present antibodies or fragments thereof as screening tools or as diagnostic or therapeutic agents.
摘要翻译： 本发明涉及Ab2型抗独特型抗体及其片段，其模拟HVI-1表位，否则其对于免疫系统是隐秘的，哪些抗体或其片段针对有效中和抗HIV-1抗体。 本发明还涉及表达抗独特型抗体的杂交瘤细胞系3H6和含有抗体或其片段的药物组合物。 本发明还涉及在施用Ab2型抗独特型抗体或其片段时引发的HIV-1中和Ab3型抗体以及含有它们的药物组合物。 本发明还涉及本发明的抗体或其片段作为筛选工具或诊断或治疗剂的用途。
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10.发明授权Peptides that induce antibodies which neutralize genetically divergent HIV-1 isolates 失效诱导中和遗传上不同的HIV-1分离株的抗体的肽
公开(公告)号：US5693752A
公开(公告)日：1997-12-02
申请号：US361479
申请日：1994-12-22
申请人： Hermann Katinger , Florian Ruker , Gottfried Himmler , Thomas Muster , Alexandra Trkola , Martin Purtscher , Georg Maiwald , Franz Steindl
发明人： Hermann Katinger , Florian Ruker , Gottfried Himmler , Thomas Muster , Alexandra Trkola , Martin Purtscher , Georg Maiwald , Franz Steindl
IPC分类号： A61K38/00 , A61K39/00 , A61K39/21 , A61P31/12 , A61P31/18 , C07K7/06 , C07K14/16 , C07K16/00 , C07K16/10 , C07K16/42 , C07K19/00 , C12N15/09 , C12N15/49 , C12P21/02 , C12P21/08 , C12R1/19 , A61K38/04 , A61K39/38 , C07K5/00
CPC分类号： C07K14/005 , C07K16/1063 , C07K16/4225 , A61K39/00 , C07K2319/00 , C12N2740/16122
摘要： This invention refers to peptides binding to antibodies that show neutralizing activity against different strains and clinical isolates of HIV-1 and that inhibit the fusion of cells caused by HIV-1. These peptides are applied with an adjuvant, as recombinant fusion proteins, chemically coupled to carrier molecules, as recombinant chimeric viruses or as recombinant antibodies.
摘要翻译： 本发明涉及结合抗体的肽，其显示针对HIV-1的不同菌株和临床分离物的中和活性，并且抑制由HIV-1引起的细胞融合。 这些肽用作为重组融合蛋白的佐剂施用，作为重组嵌合病毒或作为重组抗体与载体分子化学偶联。
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