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公开(公告)号：US20130323168A1
公开(公告)日：2013-12-05
申请号：US13885393
申请日：2011-11-15
CPC分类号： A61K51/0472 , A61K49/10 , A61K51/0421 , A61K51/086 , A61K51/088 , C07F9/65522 , C07F9/70 , C07F9/80 , G01N33/60
摘要： Provided herein are novel compounds based on xanthene, for example biarsenical compounds, which are useful as molecular probes. The compounds contain at least one isotope atom, such as a radioisotope atom. Methods for visualizing tetracysteine-tagged analyte molecules such as proteins using said compounds, methods for synthesizing said compounds, and methods for treating cancer or other hyperproliferative disorders using said compounds are also provided.
摘要翻译： 本文提供了基于呫吨的新型化合物，例如可用作分子探针的双缩醛化合物。 该化合物含有至少一个同位素原子，例如放射性同位素原子。 还提供了使用所述化合物显现四羧酸标记的分析物分子如蛋白质的方法，用于合成所述化合物的方法，以及使用所述化合物治疗癌症或其它过度增殖性疾病的方法。
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2.发明申请ARG-GLY-ASP-CONJUGATED ALPHA-MELANOCYTE STIMULATING HORMONE HYBRID PEPTIDE FOR USE IN DIAGNOSING AND TREATING MELANOMA, INCLUDING METASTATIC MELANOMA AND METHODS RELATED TO SAME 有权ARG-GLY-ASP-结合的阿尔法 - 梅毒素刺激性霍乱胶囊用于诊断和治疗MELANOMA，包括METASTATIC MELANOMA及其相关方法公开(公告)号：US20120107237A1
公开(公告)日：2012-05-03
申请号：US13321942
申请日：2010-05-28
申请人： Yubin Miao , Jianquan Yang
发明人： Yubin Miao , Jianquan Yang
CPC分类号： C07K14/68 , A61K38/00 , A61K51/082 , A61K51/086 , A61K51/088 , C12N9/88
摘要： The present invention is directed to novel non-invasive diagnostic and therapeutic tools/compounds comprising a hybride cyclic peptide which utilizes a cyclic peptide chelating group wherein the compound binds to a MSH receptor to image and treat cancers, especially, melanoma, including metastatic melanoma in vivo. The present invention represents a clear advance in the art which presently relies on tissue biopsy for diagnoses of these cancers. The novel imaging probes are capable of detecting cancerous melanoma cells, as well as their metastatic spread in tissues. This represents a quantum step forward in the diagnosis and treatment of melanoma, including metastatic melanoma using non-invasive molecular imaging techniques. The novel probes of the present invention will also be useful to initiate therapy for melanoma as well as monitor patients response to chemotherapy treatments and other interventions or therapies used in the treatment of melanoma/metastatic melanoma. Compound according to the present invention may be used as diagnostic tools for a number of conditions and diseases states as well as therapeutic agents for treating such conditions and disease states.
摘要翻译： 本发明涉及新颖的非侵入性诊断和治疗工具/化合物，其包含利用环肽螯合基团的杂环环肽，其中所述化合物结合MSH受体以成像和治疗癌症，特别是黑素瘤，包括转移性黑素瘤 体内。 本发明代表了目前依赖于组织活检以诊断这些癌症的本领域的明显进步。 新型成像探针能够检测癌细胞黑素瘤细胞，以及它们在组织中的转移扩散。 这代表了使用非侵入性分子成像技术在黑素瘤的诊断和治疗中包括转移性黑素瘤的量子进步。 本发明的新型探针也可用于启动黑素瘤的治疗以及监测患者对化疗治疗的反应和用于治疗黑素瘤/转移性黑色素瘤的其它干预或治疗。 根据本发明的化合物可以用作许多病症和疾病状态的诊断工具以及用于治疗这些病症和疾病状态的治疗剂。
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公开(公告)号：US20130039848A1
公开(公告)日：2013-02-14
申请号：US13381209
申请日：2010-07-02
申请人： Michelle Bradbury , Ulrich Wiesner , Oula Penate Medina , Hoosweng Ow , Andrew Burns , Jason Lewis , Steven Larson
发明人： Michelle Bradbury , Ulrich Wiesner , Oula Penate Medina , Hoosweng Ow , Andrew Burns , Jason Lewis , Steven Larson
IPC分类号： A61K49/00 , A61K49/06 , A61K49/04 , A61K9/14 , A61K39/395 , A61K31/7088 , A61K48/00 , A61K31/56 , A61K31/713 , A61K31/7105 , G01N21/64 , A61P35/00 , A61P31/04 , A61P31/00 , A61P39/06 , A61P37/06 , A61P7/02 , A61P9/08 , A61P29/00 , A61K51/12 , B82Y5/00 , B82Y15/00
CPC分类号： A61K51/1244 , A61K9/5115 , A61K9/5146 , A61K9/5169 , A61K49/0019 , A61K49/0032 , A61K49/0054 , A61K49/0056 , A61K49/0093 , A61K51/08 , A61K51/082 , A61K51/086 , A61K51/1255 , B82Y5/00 , B82Y15/00 , G01N33/54346 , G01N33/552 , G01N33/574 , G01N33/582 , G01N33/587 , G01N33/60 , Y10S977/773 , Y10S977/927
摘要： The present invention provides a fluorescent silica-based nanoparticle that allows for precise detection, characterization, monitoring and treatment of a disease such as cancer The nanoparticle has a fluorescent compound positioned within the nanoparticle, and has greater brightness and fluorescent quantum yield than the free fluorescent compound To facilitate efficient urinary excretion of the nanoparticle, it may be coated with an organic polymer, such as polyethylene glycol) (PEG) The small size of the nanoparticle, the silica base and the organic polymer coating minimizes the toxicity of the nanoparticle when administered in vivo The nanoparticle may further be conjugated to a ligand capable of binding to a cellular component associated with the specific cell type, such as a tumor marker A therapeutic agent may be attached to the nanoparticle Radionuclides/radiometals or paramagnetic ions may be conjugated to the nanoparticle to permit the nanoparticle to be detectable by various imaging techniques.
摘要翻译： 本发明提供一种荧光二氧化硅基纳米颗粒，其允许精确检测，表征，监测和治疗诸如癌症的疾病。纳米颗粒具有位于纳米颗粒内的荧光化合物，并且具有比游离荧光素更高的亮度和荧光量子产率 化合物为了促进纳米颗粒的有效的尿液排泄，可以用有机聚合物如聚乙二醇（PEG）包被）（PEG）小粒径的纳米颗粒，二氧化硅基底和有机聚合物涂层在施用时使纳米颗粒的毒性最小化 在体内纳米颗粒还可以与能够结合与特定细胞类型相关的细胞成分的配体缀合，例如肿瘤标记物A治疗剂可以连接到纳米颗粒放射性核素/放射性金属或顺磁性离子可以与 纳米颗粒以允许纳米颗粒可以通过各种i检测 搜索技巧
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4.发明授权Chelating agent conjugated α-MSH peptide derivatives, preparation method thereof and composition for diagnosis and treatment of melanoma comprising the same as an active ingredient 有权螯合剂缀合的α-MSH肽衍生物，其制备方法和用于诊断和治疗黑素瘤的组合物，包括其作为活性成分公开(公告)号：US08124054B2
公开(公告)日：2012-02-28
申请号：US12409288
申请日：2009-03-23
申请人： Young-Don Hong , Sun-Ju Choi , So-Young Lee , Kang-Hyuk Choi
发明人： Young-Don Hong , Sun-Ju Choi , So-Young Lee , Kang-Hyuk Choi
CPC分类号： C07K14/685 , A61K51/086 , A61K51/088
摘要： Disclosed are chelating agent-conjugated α-MSH peptide derivatives, preparation methods thereof, and compositions for use in a diagnosis or treatment of a melanoma tumor containing the same as an active ingredient. The novel α-MSH peptide derivatives conjugated with chelating agent according to the present invention are highly selective to the melanocortin-1 receptor which is α-MSH receptor expressing in melanoma tumor and their labeling rate of a radioactive isotope is high. Also, they remain in kidney shortly and have high taking rate of the melanoma tumor. Therefore, with the aforesaid reasons, they may be effectively used for early diagnosis or treatment of melanoma tumor.
摘要翻译： 公开了螯合剂缀合的α-MSH肽衍生物，其制备方法和用于诊断或治疗含有其作为活性成分的黑素瘤肿瘤的组合物。 与根据本发明的螯合剂缀合的新型α-MSH肽衍生物对黑素细胞-1受体具有高选择性，黑素皮质素-1受体是黑素瘤肿瘤中表达的α-MSH受体，并且其放射性同位素的标记率高。 此外，他们很快就保持在肾脏，并且具有高的黑色素瘤肿瘤的摄入率。 因此，由于上述原因，它们可以有效地用于黑色素瘤肿瘤的早期诊断或治疗。
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5.发明授权Melanotropin analogs for potential radiopharmaceuticals for diagnosis and treatment of melanoma 失效用于诊断和治疗黑素瘤的潜在放射性药物的促黄体生物类似物公开(公告)号：US06338834B1
公开(公告)日：2002-01-15
申请号：US09070276
申请日：1998-04-30
IPC分类号： A61K5100
CPC分类号： A61K51/08 , A61K51/086 , A61K51/088
摘要： A compound for use as a diagnostic or therapeutic pharmaceutical and method of using the same where the compound consists essentially of an alpha-melanotropin stimulating hormone analog which has integrally located a radionuclide. The radionuclide is administered to the body in an amount sufficient to allow uptake and retention by the tumor cells.
摘要翻译： 用作诊断或治疗药物的化合物及其使用方法，其中所述化合物基本上由一种放射性核素整体定位的α-促黑素激素类似物组成。 将放射性核素以足以允许肿瘤细胞吸收和保留的量施用于身体。
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公开(公告)号：US20190106474A1
公开(公告)日：2019-04-11
申请号：US16039858
申请日：2018-07-19
申请人： STC. UNM
发明人： Yubin Miao , Haixun Guo
CPC分类号： C07K14/68 , A61K38/00 , A61K45/06 , A61K51/08 , A61K51/086 , A61K51/088 , C07K7/54
摘要： The present invention is directed to novel non-invasive diagnostic tools/compounds to image cancers, especially, melanoma, including metastatic melanoma in vivo. The present compounds exhibit enhanced uptake in cancerous cells and tissue and decreased renal uptake in kidney, evidencing favorable pharmacokinetics of compounds of the present invention. The compounds according to the present invention represent an advance in the diagnosis and treatment of melanoma, including metastatic melanoma using non-invasive molecular imaging techniques. The novel probes of the present invention are also useful for initiating therapy for melanoma as well as monitor patients' response to chemotherapy treatments and other interventions or therapies used in the treatment of melanoma/metastatic melanoma. Compounds according to the present invention may be used as diagnostic tools for a number of conditions and diseases states as well as therapeutic agents for treating such conditions and disease states.
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公开(公告)号：US20150239952A1
公开(公告)日：2015-08-27
申请号：US14629791
申请日：2015-02-24
申请人： STC.UNM
发明人： Yubin Miao , Haixun Guo
CPC分类号： C07K14/68 , A61K38/00 , A61K45/06 , A61K51/08 , A61K51/086 , A61K51/088 , C07K7/54
摘要： The present invention is directed to novel non-invasive diagnostic tools/compounds to image cancers, especially, melanoma, including metastatic melanoma in vivo. The present compounds exhibit enhanced uptake in cancerous cells and tissue and decreased renal uptake in kidney, evidencing favorable pharmacokinetics of compounds of the present invention. The compounds according to the present invention represent an advance in the diagnosis and treatment of melanoma, including metastatic melanoma using non-invasive molecular imaging techniques. The novel probes of the present invention are also useful for initiating therapy for melanoma as well as monitor patients' response to chemotherapy treatments and other interventions or therapies used in the treatment of melanoma/metastatic melanoma. Compounds according to the present invention may be used as diagnostic tools for a number of conditions and diseases states as well as therapeutic agents for treating such conditions and disease states.
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8.发明授权Arg-Gly-Asp-conjugated alpha-melanocyte stimulating hormone hybrid peptide for use in diagnosing and treating melanoma, including metastatic melanoma and methods related to same 有权用于诊断和治疗黑素瘤的Arg-Gly-Asp-共轭α-黑素细胞刺激激素杂交肽，包括转移性黑素瘤及与其相关的方法公开(公告)号：US09005575B2
公开(公告)日：2015-04-14
申请号：US13321942
申请日：2010-05-28
申请人： Yubin Miao , Jianquan Yang
发明人： Yubin Miao , Jianquan Yang
CPC分类号： C07K14/68 , A61K38/00 , A61K51/082 , A61K51/086 , A61K51/088 , C12N9/88
摘要： The present invention is directed to novel non-invasive diagnostic and therapeutic tools/compounds comprising a hybride cyclic peptide which utilizes a cyclic peptide chelating group wherein the compound binds to a MSH receptor to image and treat cancers, especially, melanoma, including metastatic melanoma in vivo. The present invention represents a clear advance in the art which presently relies on tissue biopsy for diagnoses of these cancers. The novel imaging probes are capable of detecting cancerous melanoma cells, as well as their metastatic spread in tissues. This represents a quantum step forward in the diagnosis and treatment of melanoma, including metastatic melanoma using non-invasive molecular imaging techniques. The novel probes of the present invention will also be useful to initiate therapy for melanoma as well as monitor patients response to chemotherapy treatments and other interventions or therapies used in the treatment of melanoma/metastatic melanoma. Compound according to the present invention may be used as diagnostic tools for a number of conditions and diseases states as well as therapeutic agents for treating such conditions and disease states.
摘要翻译： 本发明涉及新颖的非侵入性诊断和治疗工具/化合物，其包含利用环肽螯合基团的杂环环肽，其中所述化合物结合MSH受体以成像和治疗癌症，特别是黑素瘤，包括转移性黑素瘤 体内。 本发明代表了目前依赖于组织活检以诊断这些癌症的本领域的明显进步。 新型成像探针能够检测癌细胞黑素瘤细胞，以及它们在组织中的转移扩散。 这代表了使用非侵入性分子成像技术在黑素瘤的诊断和治疗中包括转移性黑素瘤的量子进步。 本发明的新型探针也可用于启动黑素瘤的治疗以及监测患者对化疗治疗的反应和用于治疗黑素瘤/转移性黑色素瘤的其它干预或治疗。 根据本发明的化合物可以用作许多病症和疾病状态的诊断工具以及用于治疗这些病症和疾病状态的治疗剂。
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9.发明申请公开(公告)号：US20090136505A1
公开(公告)日：2009-05-28
申请号：US11931201
申请日：2007-10-31
申请人： Johanna Bentz , Beth Hill , Lisbeth Illum
发明人： Johanna Bentz , Beth Hill , Lisbeth Illum
IPC分类号： A61K39/395 , A61K38/43
CPC分类号： C07K16/18 , A61K9/0043 , A61K38/34 , A61K38/50 , A61K47/26 , A61K47/28 , A61K47/34 , A61K47/6811 , A61K47/6851 , A61K51/086 , A61K51/088 , C07K14/685 , C07K2319/30
摘要： Pharmaceutical compositions and methods for delivering a polypeptide to the central nervous system of a mammal via intranasal administration are provided. The polypeptide can be a catalytically active protein or an antibody, antibody fragment or antibody fragment fusion protein. The polypeptides are formulated with one or more specific agents.
摘要翻译： 提供了通过鼻内给药将多肽递送至哺乳动物的中枢神经系统的药物组合物和方法。 多肽可以是催化活性蛋白或抗体，抗体片段或抗体片段融合蛋白。 多肽用一种或多种特异性试剂配制。
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10.发明授权Melanocortin metallopeptide constructs, combinatorial libraries and applications 有权黑皮质素金属肽构建体，组合文库和应用公开(公告)号：US07049398B1
公开(公告)日：2006-05-23
申请号：US10049718
申请日：2000-06-15
申请人： Shubh D. Sharma , Yiqun Shi , Wei Yang , Hui-Zhi Cai
发明人： Shubh D. Sharma , Yiqun Shi , Wei Yang , Hui-Zhi Cai
CPC分类号： C07K5/1016 , A61K38/00 , A61K51/086 , A61K51/088 , C07K5/1008 , C07K5/1024 , C07K14/665
摘要： Metallopeptides and metallopeptide combinatorial libraries specific for melanocortin receptors are provided, for use in biological, pharmaceutical and related applications. The metallopeptides and combinatorial libraries are made of peptides, peptidomimetics and peptide-like constructs, in which the peptide, peptidomimetic or construct is conformationally fixed on complexation of a metal ion-binding portion thereof with a metal ion.
摘要翻译： 提供了特异于黑皮质素受体的金属肽和金属肽组合文库，用于生物，药物和相关应用。 金属肽和组合文库由肽，肽模拟物和肽样构建体制成，其中肽，拟肽或构建体在金属离子结合部分与金属离子的络合上被构象地固定。
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