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公开(公告)号：US09090656B2
公开(公告)日：2015-07-28
申请号：US13881744
申请日：2011-10-26
申请人： Jon Holbech Rasmussen , Jens Fomsgaard , Stefan Hansen , Palle Hedengran Rasmussen , Wolfgang Oliver Wachs
发明人： Jon Holbech Rasmussen , Jens Fomsgaard , Stefan Hansen , Palle Hedengran Rasmussen , Wolfgang Oliver Wachs
IPC分类号： C07K7/04 , C07K7/06 , C07K7/23 , C07K1/02 , C07K1/06 , C07K1/10 , A61K38/04 , C07K1/00 , C07K1/08 , A61K38/08 , C07K5/083 , C07K5/087 , C07K5/09
CPC分类号： C07K7/06 , A61K38/04 , A61K38/08 , C07K1/00 , C07K1/02 , C07K1/023 , C07K1/026 , C07K1/08 , C07K1/10 , C07K5/081 , C07K5/0812 , C07K5/0815 , C07K7/04 , C07K7/23 , Y02P20/55
摘要： The present invention relates to a liquid (or solution)-phase manufacturing process for preparing the decapeptide Degarelix, its protected precursor, and other useful intermediates. The invention further relates to polypeptides useful in the solution-phase manufacturing process and to the purification of Degarelix itself. Degarelix can be obtained by subjecting a Degarelix precursor according to formula (II): (P1)AA1-AA2-AA3-AA4(P4)-AA5-AA6(P6)-AA7-AA8(P8)-AA9-AA10-NH2 (II) or a salt or solvate thereof, to a treatment with a cleaving agent in an organic solvent, wherein P1 is an amino protecting groups; preferably acetyl; P4 is hydrogen or a hydroxy! protecting group, preferably a hydroxyl protecting group; P6 is hydrogen or an amino protecting groups; preferably an amino protecting groups; and P8 is an amino protecting group.
摘要翻译： 本发明涉及用于制备十肽Degarelix，其受保护的前体和其它有用的中间体的液体（或溶液）相制备方法。 本发明还涉及可用于溶液相制备方法和Degarelix本身纯化的多肽。 通过使根据式（II）的Degarelix前体：（P1）AA1-AA2-AA3-AA4（P4）-AA5-AA6（P6）-AA7-AA8（P8）-AA9-AA10-NH2（ II）或其盐或溶剂合物，在有机溶剂中用切割剂进行处理，其中P1是氨基保护基; 优选乙酰基; P4是氢或羟基！ 保护基，优选羟基保护基; P6是氢或氨基保护基; 优选氨基保护基; P8是氨基保护基。
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2.发明申请公开(公告)号：US20120213698A1
公开(公告)日：2012-08-23
申请号：US13383310
申请日：2010-07-16
申请人： Anncatrine Luisa Petersen , Palle Hedengran Rasmussen , Jonas Rosager Henriksen , Andreas Kjær , Thomas Lars Andresen
发明人： Anncatrine Luisa Petersen , Palle Hedengran Rasmussen , Jonas Rosager Henriksen , Andreas Kjær , Thomas Lars Andresen
CPC分类号： A61K51/1244 , A61K9/127 , A61K51/025 , A61K51/1234 , C07B59/00
摘要： The present invention relates to a novel composition and method for loading delivery systems such as liposome compositions with radionuclides useful in targeted diagnostic and/or therapy of target site, such as cancerous tissue and, in general, pathological conditions associated with leaky blood vessels. The composition and methods of the invention find particular use in diagnosing and imaging cancerous tissue and, in general, pathological conditions associated with leaky blood vessels in a subject. The present invention provides a new diagnostic tool for the utilization of positron emission tomography (PET) imaging technique. One specific aspect of the invention is directed to a method of producing nanoparticles with desired targeting properties for diagnostic and/or radio-therapeutic applications.
摘要翻译： 本发明涉及一种新颖的组合物和方法，其用于将靶向部位的靶向诊断和/或治疗（例如癌组织）和通常与渗漏的血管相关的病理状况用于放射性核素的脂质体组合物。 本发明的组合物和方法在癌症组织的诊断和成像以及与受试者中泄漏的血管相关的病理状况方面特别有用。 本发明提供了一种用于正电子发射断层摄影（PET）成像技术的新诊断工具。 本发明的一个具体方面涉及一种用于诊断和/或放射治疗应用的具有所需靶向特性的纳米颗粒的制备方法。
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公开(公告)号：US09226984B2
公开(公告)日：2016-01-05
申请号：US13992080
申请日：2011-12-14
申请人： Anncatrine Luisa Petersen , Jonas Rosager Henriksen , Palle Hedengran Rasmussen , Andreas Kjær , Thomas Lars Andresen
发明人： Anncatrine Luisa Petersen , Jonas Rosager Henriksen , Palle Hedengran Rasmussen , Andreas Kjær , Thomas Lars Andresen
CPC分类号： A61K51/1237 , A61K51/0408 , A61K51/0482 , A61K51/12 , A61K51/1203 , A61K51/1234
摘要： The present invention is directed to the technical field of imaging compositions useful for diagnosing cancer and other diseases in a subject. In particular, the invention relates to a class of diagnostic compounds comprising a novel liposome composition with encapsulated metal entities such as radionuclides, for example 61Cu and 64Cu copper isotopes. The invention further relates to a novel method for loading delivery systems, such as liposome compositions, with metal entities such as radionuclides, and the use of liposomes for targeted diagnosis and treatment of a target site, such as cancerous tissue and, in general, pathological conditions associated with leaky blood vessels. The present invention provides a new diagnostic tool for the utilization of positron emission tomography (PET) imaging technique.
摘要翻译： 本发明涉及用于诊断受试者中的癌症和其它疾病的成像组合物的技术领域。 特别地，本发明涉及一类诊断化合物，其包含具有包封金属实体（例如放射性核素）的新型脂质体组合物，例如61Cu和64Cu铜同位素。 本发明还涉及一种用于将载体递送系统（例如脂质体组合物）与金属实体（诸如放射性核素）一起加载的新方法，以及使用脂质体用于目标部位如癌组织的靶向诊断和治疗，以及通常病理学 与泄漏血管相关的病症。 本发明提供了一种用于正电子发射断层摄影（PET）成像技术的新诊断工具。
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4.发明授权公开(公告)号：US08920775B2
公开(公告)日：2014-12-30
申请号：US13383310
申请日：2010-07-16
申请人： Anncatrine Luisa Petersen , Palle Hedengran Rasmussen , Jonas Rosager Henriksen , Andreas Kjær , Thomas Lars Andresen
发明人： Anncatrine Luisa Petersen , Palle Hedengran Rasmussen , Jonas Rosager Henriksen , Andreas Kjær , Thomas Lars Andresen
CPC分类号： A61K51/1244 , A61K9/127 , A61K51/025 , A61K51/1234 , C07B59/00
摘要： The present invention relates to a novel composition and method for loading delivery systems such as liposome compositions with radionuclides useful in targeted diagnostic and/or therapy of target site, such as cancerous tissue and, in general, pathological conditions associated with leaky blood vessels. The composition and methods of the invention find particular use in diagnosing and imaging cancerous tissue and, in general, pathological conditions associated with leaky blood vessels in a subject. The present invention provides a new diagnostic tool for the utilization of positron emission tomography (PET) imaging technique. One specific aspect of the invention is directed to a method of producing nanoparticles with desired targeting properties for diagnostic and/or radio-therapeutic applications.
摘要翻译： 本发明涉及一种新颖的组合物和方法，其用于将靶向部位的靶向诊断和/或治疗（例如癌组织）和通常与渗漏的血管相关的病理状况用于放射性核素的脂质体组合物。 本发明的组合物和方法在癌症组织的诊断和成像以及与受试者中泄漏的血管相关的病理状况方面特别有用。 本发明提供了一种用于正电子发射断层摄影（PET）成像技术的新诊断工具。 本发明的一个具体方面涉及一种用于诊断和/或放射治疗应用的具有所需靶向特性的纳米颗粒的制备方法。
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公开(公告)号：US20130281661A1
公开(公告)日：2013-10-24
申请号：US13881744
申请日：2011-10-26
申请人： Jon Holbech Rasmusse , Jens Fomsgaard , Stefan Hansen , Palle Hedengran Rasmussen , Wolfgang Oliver Wachs
发明人： Jon Holbech Rasmusse , Jens Fomsgaard , Stefan Hansen , Palle Hedengran Rasmussen , Wolfgang Oliver Wachs
IPC分类号： C07K7/06
CPC分类号： C07K7/06 , A61K38/04 , A61K38/08 , C07K1/00 , C07K1/02 , C07K1/023 , C07K1/026 , C07K1/08 , C07K1/10 , C07K5/081 , C07K5/0812 , C07K5/0815 , C07K7/04 , C07K7/23 , Y02P20/55
摘要： The present invention relates to a liquid (or solution)-phase manufacturing process for preparing the decapeptide Degarelix, its protected precursor, and other useful intermediates. The invention further relates to polypeptides useful in the solution-phase manufacturing process and to the purification of Degarelix itself. Degarelix can be obtained by subjecting a Degarelix precursor according to formula (II): (P1)AA1-AA2-AA3-AA4(P4)-AA5-AA6(P6)-AA7-AA8(P8)-AA9-AA10-NH2 (II) or a salt or solvate thereof, to a treatment with a cleaving agent in an organic solvent, wherein P1 is an amino protecting groups; preferably acetyl; P4 is hydrogen or a hydroxy! protecting group, preferably a hydroxyl protecting group; P6 is hydrogen or an amino protecting groups; preferably an amino protecting groups; and P8 is an amino protecting group.
摘要翻译： 本发明涉及用于制备十肽Degarelix，其受保护的前体和其它有用的中间体的液体（或溶液）相制备方法。 本发明还涉及可用于溶液相制备方法和Degarelix本身纯化的多肽。 通过使根据式（II）的Degarelix前体：（P1）AA1-AA2-AA3-AA4（P4）-AA5-AA6（P6）-AA7-AA8（P8）-AA9-AA10-NH2（ II）或其盐或溶剂合物，在有机溶剂中用切割剂进行处理，其中P1是氨基保护基; 优选乙酰基; P4是氢或羟基保护基，优选羟基保护基; P6是氢或氨基保护基; 优选氨基保护基; P8是氨基保护基。
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公开(公告)号：US20130251630A1
公开(公告)日：2013-09-26
申请号：US13992080
申请日：2011-12-14
申请人： Anncatrine Luisa Petersen , Jonas Rosager Henriksen , Palle Hedengran Rasmussen , Andreas Kjær , Thomas Lars Andresen
发明人： Anncatrine Luisa Petersen , Jonas Rosager Henriksen , Palle Hedengran Rasmussen , Andreas Kjær , Thomas Lars Andresen
IPC分类号： A61K51/12
CPC分类号： A61K51/1237 , A61K51/0408 , A61K51/0482 , A61K51/12 , A61K51/1203 , A61K51/1234
摘要： The present invention is directed to the technical field of imaging compositions useful for diagnosing cancer and other diseases in a subject. In particular, the invention relates to a class of diagnostic compounds comprising a novel liposome composition with encapsulated metal entities such as radionuclides, for example 61Cu and 64Cu copper isotopes. The invention further relates to a novel method for loading delivery systems, such as liposome compositions, with metal entities such as radionuclides, and the use of liposomes for targeted diagnosis and treatment of a target site, such as cancerous tissue and, in general, pathological conditions associated with leaky blood vessels. The present invention provides a new diagnostic tool for the utilization of positron emission tomography (PET) imaging technique.
摘要翻译： 本发明涉及用于诊断受试者中的癌症和其它疾病的成像组合物的技术领域。 特别地，本发明涉及一类诊断化合物，其包含具有包封金属实体（例如放射性核素）的新型脂质体组合物，例如61Cu和64Cu铜同位素。 本发明还涉及一种用于将载体递送系统（例如脂质体组合物）与金属实体（诸如放射性核素）一起加载的新方法，以及使用脂质体用于目标部位如癌组织的靶向诊断和治疗，以及通常病理学 与泄漏血管相关的病症。 本发明提供了一种用于正电子发射断层摄影（PET）成像技术的新诊断工具。
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