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1. 发明授权

US08992886B2 Cyclic peptide analogues for non-invasive imaging of pancreatic beta-cells 有权
标题翻译：用于胰腺β细胞非侵入性成像的环肽类似物
公开(公告)号：US08992886B2
公开(公告)日：2015-03-31
申请号：US13263320
申请日：2010-04-06
申请人： Jung-Mo Ahn , Xiankai Sun
发明人： Jung-Mo Ahn , Xiankai Sun
IPC分类号： C07K14/06 , A61K51/08 , A61K49/14 , A61B5/055
CPC分类号： A61K51/088
摘要： Compositions, methods of using and methods of making a cyclic peptide analog imaging agent that includes at least portions of a peptide or protein that binds specifically to the GLP-1 receptor (GLP-1R) and the cyclic analog has one or more conformational restrictions including, but not limited to, lactam bridges, disulfide bridges, hydrocarbon bridges, and their combinations, salts and derivatives thereof wherein the cyclic analog is more stable than a non-cyclic analog when incubated in the presence of enzymes that degrade GLP-1 and have an increased serum half-live, wherein the cyclic analog comprises at least a portion of a GLP-1 peptide or at least a portion of an Exendin peptide salts, derivatives or combinations thereof.
摘要翻译：包含至少部分与GLP-1受体（GLP-1R）和环状类似物结合的肽或蛋白质的部分的环肽模拟成像剂的组合物，使用方法和制备方法具有一个或多个构象限制，包括但不限于，内酰胺桥，二硫桥，烃桥及其组合，其盐和衍生物，其中环状类似物在降解GLP-1的酶存在下温育时具有比非环状类似物更稳定并具有增加的血清半活性，其中所述环状类似物包含至少一部分GLP-1肽或至少一部分毒蜥外泌肽肽，其衍生物或组合。

2. 发明申请

US20120100070A1 Cyclic Peptide Analogues For Non-Invasive Imaging of Pancreatic Beta-Cells 有权
标题翻译：循环肽类似物用于胰腺β细胞的非侵入性成像
公开(公告)号：US20120100070A1
公开(公告)日：2012-04-26
申请号：US13263320
申请日：2010-04-06
申请人： Jung-Mo Ahn , Xiankai Sun
发明人： Jung-Mo Ahn , Xiankai Sun
IPC分类号： A61K51/08 , C12N11/02 , A61K49/14 , C07K14/605 , A61K49/00
CPC分类号： A61K51/088
摘要： Compositions, methods of using and methods of making a cyclic peptide analog imaging agent that includes at least portions of a peptide or protein that binds specifically to the GLP-1 receptor (GLP-1R) and the cyclic analog has one or more conformational restrictions including, but not limited to, lactam bridges, disulfide bridges, hydrocarbon bridges, and their combinations, salts and derivatives thereof wherein the cyclic analog is more stable than a non-cyclic analog when incubated in the presence of enzymes that degrade GLP-1 and have an increased serum half-live, wherein the cyclic analog comprises at least a portion of a GLP-1 peptide or at least a portion of an Exendin peptide salts, derivatives or combinations thereof.
摘要翻译：包含至少部分与GLP-1受体（GLP-1R）和环状类似物结合的肽或蛋白质的部分的环肽模拟成像剂的组合物，使用方法和制备方法具有一个或多个构象限制，包括但不限于，内酰胺桥，二硫桥，烃桥及其组合，其盐和衍生物，其中环状类似物在降解GLP-1的酶存在下温育时具有比非环状类似物更稳定并具有增加的血清半活性，其中所述环状类似物包含至少一部分GLP-1肽或至少一部分毒蜥外泌肽肽，其衍生物或组合。

3. 发明申请

US20060159619A1 Cell permeable nanoconjugates of shell-crosslinked knedel (SCK) and peptide nucleic acids ("PNAs") with uniquely expressed or over-expressed mRNA targeting sequences for early diagnosis and therapy of cancer 有权
标题翻译：具有独特表达或过表达的mRNA靶向序列的壳交联睾丸（SCK）和肽核酸（“PNA”）的细胞可渗透纳米缀合物用于癌症的早期诊断和治疗
公开(公告)号：US20060159619A1
公开(公告)日：2006-07-20
申请号：US11250830
申请日：2005-10-14
申请人： Matthew Becker , Huafeng Fang , Xiaoxu Li , Dipanjan Pan , Raffaella Rossin , Xiankai Sun , John-Stephen Taylor , Jeffrey Turner , Michael Welch , Karen Wooley
发明人： Matthew Becker , Huafeng Fang , Xiaoxu Li , Dipanjan Pan , Raffaella Rossin , Xiankai Sun , John-Stephen Taylor , Jeffrey Turner , Michael Welch , Karen Wooley
IPC分类号： A61K51/00 , C12Q1/68 , A61K48/00
CPC分类号： A61K31/7088 , A61K51/1251 , B82Y5/00 , B82Y30/00 , C01P2004/64 , C12N15/111 , C12N15/1135 , C12N2310/11 , C12N2310/3181 , C12N2310/321 , C12N2310/3231 , C12N2310/3513 , C12N2310/3517 , C12N2320/10 , C12N2320/31 , C12N2310/3525
摘要： A functional biologically active particle conjugate useful for diagnosis and treating cancer as a bioportal comprises a nanoscale particle having associated therewith an intracellular targeting ligand comprising a PNA, or another nuclease resistant oligonucleotide analog such as MOE-mRNA (2′-methoxyethyl mRNA) or LNA (locked nucleic acid), having a sequence that binds selectively to an uniquely expressed or overexpressed mRNA specific to the cancer or disease state in a living mammal. In one aspect the uniquely overexpressed target specific to the cancer or disease state is the unr mRNA which can be targeted by the antisense sequence PNA50.
摘要翻译：用于诊断和治疗癌症作为生物体的功能性生物活性粒子缀合物包含具有与其相关联的细胞内靶向配体的纳米级粒子，其包含PNA或另一种核酸酶抗性寡核苷酸类似物，例如MOE-mRNA（2'-甲氧基乙基mRNA）或LNA （锁定的核酸），其具有与活的哺乳动物中癌症或疾病状态特异性的独特表达或过表达的mRNA的选择性结合的序列。在一个方面，针对癌症或疾病状态特异性的唯一过表达的靶是可以由反义序列PNA50靶向的unr mRNA。

4. 发明授权

US07919579B2 Imaging and therapeutic targeting of prostate and bladder tissues 有权
标题翻译：前列腺和膀胱组织的成像和治疗靶向
公开(公告)号：US07919579B2
公开(公告)日：2011-04-05
申请号：US11923388
申请日：2007-10-24
申请人： Jer-Tsong Hsieh , Jian Zhou , Xiankai Sun
发明人： Jer-Tsong Hsieh , Jian Zhou , Xiankai Sun
IPC分类号： C07K7/04 , C07K7/08
CPC分类号： A61K38/08 , A61B5/0059 , A61B5/411 , A61B5/415 , A61B5/418 , A61B5/4381 , A61B6/037 , A61K47/645 , A61K51/088
摘要： The present invention provides methods for imaging and the treatment of cancer. In certain embodiments, a polyarginine (e.g., R11) may be used to selectively image prostate or bladder cells (e.g., a metastatic prostate cancer). In other embodiments, a DOC-2/DAB2 peptide, optionally conjugated to a cell permeable peptide (e.g., R11) may be used to treat a cancer, such as prostate cancer.
摘要翻译：本发明提供了用于成像和治疗癌症的方法。在某些实施方案中，聚精氨酸（例如R11）可用于选择性地成像前列腺或膀胱细胞（例如转移性前列腺癌）。在其它实施方案中，任选地缀合至细胞可渗透肽（例如R11）的DOC-2 / DAB2肽可用于治疗癌症，例如前列腺癌。

5. 发明申请

US20090123381A1 IMAGING AND THERAPEUTIC TARGETING OF PROSTATE AND BLADDER TISSUES 有权
标题翻译：前列腺和叶片组织的成像和治疗目标
公开(公告)号：US20090123381A1
公开(公告)日：2009-05-14
申请号：US11923388
申请日：2007-10-24
申请人： JER-TSONG HSIEH , Jian Zhou , Xiankai Sun
发明人： JER-TSONG HSIEH , Jian Zhou , Xiankai Sun
IPC分类号： A61K49/00 , C07K14/435 , A61K38/17 , A61P35/00
CPC分类号： A61K38/08 , A61B5/0059 , A61B5/411 , A61B5/415 , A61B5/418 , A61B5/4381 , A61B6/037 , A61K47/645 , A61K51/088
摘要： The present invention provides methods for imaging and the treatment of cancer. In certain embodiments, a polyarginine (e.g., R11) may be used to selectively image prostate or bladder cells (e.g., a metastatic prostate cancer). In other embodiments, a DOC-2/DAB2 peptide, optionally conjugated to a cell permeable peptide (e.g., R11) may be used to treat a cancer, such as prostate cancer.
摘要翻译：本发明提供了用于成像和治疗癌症的方法。在某些实施方案中，聚精氨酸（例如R11）可用于选择性地成像前列腺或膀胱细胞（例如转移性前列腺癌）。在其它实施方案中，任选地缀合至细胞可渗透肽（例如R11）的DOC-2 / DAB2肽可用于治疗癌症，例如前列腺癌。

6. 发明授权

US08354093B2 Cell permeable nanoconjugates of shell-crosslinked knedel (SCK) and peptide nucleic acids (“PNAs”) with uniquely expressed or over-expressed mRNA targeting sequences for early diagnosis and therapy of cancer 有权
标题翻译：具有独特表达或过表达的mRNA靶向序列的壳交联睾丸（SCK）和肽核酸（PNA）的细胞可渗透纳米缀合物用于癌症的早期诊断和治疗
公开(公告)号：US08354093B2
公开(公告)日：2013-01-15
申请号：US11250830
申请日：2005-10-14
申请人： Matthew L. Becker , Huafeng Fang , Xiaoxu Li , Dipanjan Pan , Raffaella Rossin , Xiankai Sun , John-Stephen Taylor , Jeffrey L. Turner , Michael John Welch , Karen L. Wooley
发明人： Matthew L. Becker , Huafeng Fang , Xiaoxu Li , Dipanjan Pan , Raffaella Rossin , Xiankai Sun , John-Stephen Taylor , Jeffrey L. Turner , Michael John Welch , Karen L. Wooley
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： A61K31/7088 , A61K51/1251 , B82Y5/00 , B82Y30/00 , C01P2004/64 , C12N15/111 , C12N15/1135 , C12N2310/11 , C12N2310/3181 , C12N2310/321 , C12N2310/3231 , C12N2310/3513 , C12N2310/3517 , C12N2320/10 , C12N2320/31 , C12N2310/3525
摘要： A functional biologically active particle conjugate useful for diagnosis and treating cancer as a bioportal comprises a nanoscale particle having associated therewith an intracellular targeting ligand comprising a PNA, or another nuclease resistant oligonucleotide analog such as MOE-mRNA (2′-methoxyethyl mRNA) or LNA (locked nucleic acid), having a sequence that binds selectively to an uniquely expressed or overexpressed mRNA specific to the cancer or disease state in a living mammal. In one aspect the uniquely overexpressed target specific to the cancer or disease state is the unr mRNA which can be targeted by the antisense sequence PNA50.
摘要翻译：用于诊断和治疗癌症作为生物体的功能性生物活性粒子缀合物包含具有与其相关联的细胞内靶向配体的纳米级粒子，其包含PNA或另一种核酸酶抗性寡核苷酸类似物，例如MOE-mRNA（2'-甲氧基乙基mRNA）或LNA （锁定的核酸），其具有与活的哺乳动物中癌症或疾病状态特异性的独特表达或过表达的mRNA的选择性结合的序列。在一个方面，针对癌症或疾病状态特异性的唯一过表达的靶是可以由反义序列PNA50靶向的unr mRNA。

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