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1. 发明授权

US08212058B2 Fluorescent photoprobe for the imaging of endothelin receptors 失效
标题翻译：用于内皮素受体成像的荧光光探针
公开(公告)号：US08212058B2
公开(公告)日：2012-07-03
申请号：US12065982
申请日：2006-09-06
申请人： Christoph Bremer , Carsten Höltke , Klaus Kopka , Michael Schäfers
发明人： Christoph Bremer , Carsten Höltke , Klaus Kopka , Michael Schäfers
IPC分类号： C07D305/12
CPC分类号： A61K49/0052 , A61K47/60 , A61K49/0032 , A61K49/0043
摘要： The present invention relates to a endothelin receptor antagonist conjugate of the formula (I) wherein R2 is an alkoxy group and one of R1 and R3 represents an alkoxy group and the other represents a group of the formula: (OCH2CH2)n—NH—X, wherein n is an integer of 1 to 100 and X represents a fluorescent dye and tautomers thereof. Furthermore, the present invention relates to a diagnostic composition comprising the compounds of the invention. The present invention also relates to the use of the compounds of the invention for the preparation of a diagnostic composition for the diagnosis of cancer, the evaluation of cancer biology and/or monitoring of anticancer therapy. In a further aspect, the present invention relates to kits comprising the compounds of the invention.
摘要翻译：本发明涉及式（I）的内皮素受体拮抗剂缀合物，其中R2是烷氧基，R1和R3之一表示烷氧基，另一个表示下式的基团：（OCH 2 CH 2）n -NH-X 其中n为1〜100的整数，X为荧光染料及其互变异构体。此外，本发明涉及包含本发明化合物的诊断组合物。本发明还涉及本发明化合物在制备用于诊断癌症的诊断组合物，癌症生物学评估和/或抗癌治疗监测中的用途。另一方面，本发明涉及包含本发明化合物的试剂盒。

2. 发明申请

US20130004430A1 FLUORESCENT PHOTOPROBE FOR THE IMAGING OF ENDOTHELIN RECEPTORS 审中-公开
标题翻译：用于成像内皮素受体的荧光光刻胶
公开(公告)号：US20130004430A1
公开(公告)日：2013-01-03
申请号：US13534738
申请日：2012-06-27
申请人： Christoph Bremer , Carsten Höltke , Klaus Kopka , Michael Schäfers
发明人： Christoph Bremer , Carsten Höltke , Klaus Kopka , Michael Schäfers
IPC分类号： A61K49/00
CPC分类号： A61K49/0052 , A61K47/60 , A61K49/0032 , A61K49/0043
摘要： The present invention relates to an endothelin receptor antagonist conjugate of the formula (I) wherein R2 is an alkoxy group and one of R1 and R3 represents an alkoxy group and the other represents a group of the formula: (OCH2CH2)n—NH—X, wherein n is an integer of 1 to 100 and X represents a fluorescent dye and tautomers thereof. Furthermore, the present invention relates to a diagnostic composition comprising the compounds of the invention. The present invention also relates to the use of the compounds of the invention for the preparation of a diagnostic composition for the diagnosis of cancer, the evaluation of cancer biology and/or monitoring of anticancer therapy. In a further aspect, the present invention relates to kits comprising the compounds of the invention.
摘要翻译：本发明涉及式（I）的内皮素受体拮抗剂缀合物，其中R2是烷氧基，R1和R3之一表示烷氧基，另一个表示下式的基团：（OCH 2 CH 2）n -NH-X 其中n为1〜100的整数，X为荧光染料及其互变异构体。此外，本发明涉及包含本发明化合物的诊断组合物。本发明还涉及本发明化合物在制备用于诊断癌症的诊断组合物，癌症生物学评估和/或抗癌治疗监测中的用途。另一方面，本发明涉及包含本发明化合物的试剂盒。

3. 发明申请

US20120213702A1 NOVEL DIAGNOSTIC AGENTS FOR THE NON-INVASIVE IN VIVO IMAGING OF AMINOPEPTIDASE N (APN/CD13) 审中-公开
标题翻译：用于非侵入性氨基转移酶N（APN / CD13）VIVO成像的新型诊断试剂
公开(公告)号：US20120213702A1
公开(公告)日：2012-08-23
申请号：US13393440
申请日：2010-08-31
申请人： Christoph Bremer , Carsten Höltke
发明人： Christoph Bremer , Carsten Höltke
IPC分类号： A61K51/04 , C07D207/16 , C07F15/02 , C07F3/00 , C07F13/00 , A61K49/00 , A61K49/10 , A61K31/40 , A61P35/00 , A61P29/00 , A61P19/02 , A61P35/02 , A61P13/12 , A61P9/00 , G01N33/53 , C07D403/14
CPC分类号： A61K51/0446 , A61K47/545 , A61K49/0032 , A61K49/0041 , A61K49/0043 , A61K49/0052 , A61K49/101
摘要： The present invention relates to aminopeptidase N (APN) inhibitor conjugates of formula I wherein W is a —CO— or an —SO2— group and at least one of R1 or R2 represents (OCH2—CH2)n-X, where n is an integer of 1 to 100 and X represents H or a detectable label or a therapeutic, and the other represents an alkoxy group or OH, and wherein R3, R3′ and R3″ is independently selected from an alkoxy group or (OCH2—CH2)n-X, where n is an integer of 1 to 100 and X represents H or a detectable label or a therapeutic, and R4 is selected from the group comprising: wherein R is an alkyl group. Furthermore, the present invention relates to a diagnostic and/or pharmaceutical composition comprising the conjugate of the invention. The present invention also relates to the conjugate or composition of the invention for use in the diagnosis or treatment of APN-associated diseases like for example angiogenesis in cancer, rheumatoid arthritis, leukemia and diabetic nephropathy, as well as to the use of the conjugate or of the composition of the invention in the diagnosis or treatment of angiogenesis in cancer, rheumatoid arthritis, leukemia and diabetic nephropathy. In a further aspect, the present invention relates to kits comprising the conjugate or composition of the invention. The conjugate or pharmaceutical/diagnostic composition of the invention can also be used in in vivo or in vitro imaging studies of aminopeptidase N.
摘要翻译：本发明涉及式I的氨基肽酶N（APN）抑制剂缀合物，其中W是-CO-或-SO 2 - 基，R 1或R 2中的至少一个表示（OCH 2 -CH 2）n X，其中n是 1〜100，X表示H或可检测标记或治疗剂，另一个表示烷氧基或OH，并且其中R3，R3'和R3“独立地选自烷氧基或（OCH2-CH2）nX，其中 n为1〜100的整数，X为H或可检测标记或治疗剂，R4选自：其中R为烷基。此外，本发明涉及包含本发明缀合物的诊断和/或药物组合物。本发明还涉及用于诊断或治疗APN相关疾病的本发明的缀合物或组合物，例如癌症，类风湿性关节炎，白血病和糖尿病性肾病中的血管生成，以及该缀合物或的本发明的组合物在癌症，类风湿性关节炎，白血病和糖尿病肾病中的血管发生的诊断或治疗中的用途。在另一方面，本发明涉及包含本发明的缀合物或组合物的试剂盒。本发明的缀合物或药物/诊断组合物也可用于氨基肽酶N的体内或体外成像研究。

4. 发明申请

US20090169483A1 FLUORESCENT PHOTOPROBE FOR THE IMAGING OF ENDOTHELIN RECEPTORS 失效
标题翻译：用于成像内皮素受体的荧光光刻胶
公开(公告)号：US20090169483A1
公开(公告)日：2009-07-02
申请号：US12065982
申请日：2006-09-06
申请人： Christoph Bremer , Carsten Höltke , Klaus Kopka , Michael Schäfers
发明人： Christoph Bremer , Carsten Höltke , Klaus Kopka , Michael Schäfers
IPC分类号： A61K49/00 , C07D311/96 , C07D209/56
CPC分类号： A61K49/0052 , A61K47/60 , A61K49/0032 , A61K49/0043
摘要： The present invention relates to a endothelin receptor antagonist conjugate of the formula (I) wherein R2 is an alkoxy group and one of R1 and R3 represents an alkoxy group and the other represents a group of the formula: (OCH2CH2)n—NH—X, wherein n is an integer of 1 to 100 and X represents a fluorescent dye and tautomers thereof. Furthermore, the present invention relates to a diagnostic composition comprising the compounds of the invention. The present invention also relates to the use of the compounds of the invention for the preparation of a diagnostic composition for the diagnosis of cancer, the evaluation of cancer biology and/or monitoring of anticancer therapy. In a further aspect, the present invention relates to kits comprising the compounds of the invention.
摘要翻译：本发明涉及式（I）的内皮素受体拮抗剂缀合物，其中R2是烷氧基，R1和R3之一表示烷氧基，另一个表示下式的基团：（OCH 2 CH 2）n -NH-X 其中n为1〜100的整数，X为荧光染料及其互变异构体。此外，本发明涉及包含本发明化合物的诊断组合物。本发明还涉及本发明化合物在制备用于诊断癌症的诊断组合物，癌症生物学评估和/或抗癌治疗监测中的用途。另一方面，本发明涉及包含本发明化合物的试剂盒。

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