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公开(公告)号：US20100240072A1
公开(公告)日：2010-09-23
申请号：US12675151
申请日：2008-09-01
IPC分类号： G01N33/567 , C07K7/64
CPC分类号： A61K51/08 , A61K47/55 , A61K51/088
摘要： A compound, or a pharmaceutically acceptable salt or ester thereof, comprises the structure: [(P1-S1j)p-L-(S2q-P2)r]t wherein: P1 and P2, which may be the same or different, are cyclic oligopeptide moieties, at least one of P1 and P2 having the motif B-Arg or B-(Me) Arg within the cyclic moiety, wherein B is a basic amino acid, a derivative thereof, or phenylalanine or a derivative thereof; S1 and S2 are spacer groups, which may be the same or different; L is a linker moiety containing at least two functional groups for attachment of the cyclic oligopeptides or spacer groups; n and q are independently 0 or 1; p and r are independently integers of 1 or more; and t is an integer of 1 or more, provided that, when t, p or r is greater than 1, the cyclic oligopeptide moiety, spacer group and/or the value of j or q may be the same or different between the multiple (P1-S1j) moieties or multiple (S2q-P2) moieties.
摘要翻译： 化合物或其药学上可接受的盐或酯包含以下结构：[（P1-S1j）pL-（S2q-P2）r] t其中：P1和P2可以相同或不同，是环状寡肽部分 在环状部分中具有基序B-Arg或B（Me）Arg的P1和P2中的至少一个，其中B是碱性氨基酸，其衍生物或苯丙氨酸或其衍生物; S1和S2是间隔基，其可以相同或不同; L是含有至少两个用于连接环状寡肽或间隔基团的官能团的连接体部分; n和q独立地为0或1; p和r独立地为1或更大的整数; 并且t为1或更大的整数，条件是当t，p或r大于1时，环状寡肽部分，间隔基团和/或j或q的值可以在多个 P1-S1j）部分或多个（S2q-P2）部分。
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公开(公告)号：US09266924B2
公开(公告)日：2016-02-23
申请号：US13641947
申请日：2011-04-20
申请人： Oliver Demmer , Horst Kessler , Hans-Jürgen Wester , Margret Schottelius , Ingrid Dijkgraaf , Andreas Konard Buck
发明人： Oliver Demmer , Horst Kessler , Hans-Jürgen Wester , Margret Schottelius , Ingrid Dijkgraaf , Andreas Konard Buck
CPC分类号： C07K7/64 , A61K51/088
摘要： The present invention, among others, relates to a compound having a structure according to formula (I) or a pharmaceutically acceptable salt thereof, wherein Xaa1 to Xaa4 are independently of each other, an optionally N-alkylated natural or unnatural amino acid, R is H or methyl, L is a linker moiety, Ar is a spacer comprising an aromatic moiety, and D comprises, preferably is i) a combination of an organic complexation agent and a detectable label; or ii) a detectable label, an organic complexation agent or an active substance, said active substance particularly being selected from cytotoxic agents, lipids, sugars, sugar conjugates, sugar derivatives, proteins and combinations thereof, with the proviso that -L-Ar-D does not comprise a 18F-benzoyl residue.
摘要翻译： 本发明尤其涉及具有式（I）结构的化合物或其药学上可接受的盐，其中Xaa1至Xaa4彼此独立，任选N-烷基化天然或非天然氨基酸，R为 H或甲基，L是连接体部分，Ar是包含芳族部分的间隔基，D包括，优选i）有机络合剂和可检测标记的组合; 或ii）可检测标记，有机络合剂或活性物质，所述活性物质特别选自细胞毒性剂，脂质，糖，糖结合物，糖衍生物，蛋白质及其组合，条件是-L-Ar- D不包含18 F-苯甲酰残基。
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公开(公告)号：US08614290B2
公开(公告)日：2013-12-24
申请号：US12675151
申请日：2008-09-01
IPC分类号： G01N33/567 , C07K7/64
CPC分类号： A61K51/08 , A61K47/55 , A61K51/088
摘要： A compound, or a pharmaceutically acceptable salt or ester thereof, comprises the structure: [(P1-S1j)p-L-(S2q-P2)r]t wherein: P1 and P2, which may be the same or different, are cyclic oligopeptide moieties, at least one of P1 and P2 having the motif B-Arg or B-(Me) Arg within the cyclic moiety, wherein B is a basic amino acid, a derivative thereof, or phenylalanine or a derivative thereof; S1 and S2 are spacer groups, which may be the same or different; L is a linker moiety containing at least two functional groups for attachment of the cyclic oligopeptides or spacer groups; n and q are independently 0 or 1; p and r are independently integers of 1 or more; and t is an integer of 1 or more, provided that, when t, p or r is greater than 1, the cyclic oligopeptide moiety, spacer group and/or the value of j or q may be the same or different between the multiple (P1-S1j) moieties or multiple (S2q-P2) moieties.
摘要翻译： 化合物或其药学上可接受的盐或酯包含以下结构：[（P1-S1j）pL-（S2q-P2）r] t其中：P1和P2可以相同或不同，是环状寡肽部分 在环状部分中具有基序B-Arg或B（Me）Arg的P1和P2中的至少一个，其中B是碱性氨基酸，其衍生物或苯丙氨酸或其衍生物; S1和S2是间隔基，其可以相同或不同; L是含有至少两个用于连接环状寡肽或间隔基团的官能团的连接体部分; n和q独立地为0或1; p和r独立地为1或更大的整数; 并且t为1或更大的整数，条件是当t，p或r大于1时，环状寡肽部分，间隔基团和/或j或q的值可以在多个 P1-S1j）部分或多个（S2q-P2）部分。
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公开(公告)号：US08628750B2
公开(公告)日：2014-01-14
申请号：US12280829
申请日：2007-02-27
申请人： Hans Jürgen Wester , Norman Koglin , Markus Schwaiger , Horst Kessler , Burkhardt Laufer , Oliver Demmer , Martina Anton
发明人： Hans Jürgen Wester , Norman Koglin , Markus Schwaiger , Horst Kessler , Burkhardt Laufer , Oliver Demmer , Martina Anton
CPC分类号： C07K7/64 , A61K51/08 , A61K51/088
摘要： Provided herein are compounds or conjugates useful for diagnostic imaging and/or therapeutic purposes. Each compound or conjugate comprises a ligand for the chemokine receptor CXCR4 and a detectable label. The ligand has a binding affinity for the CXCR4 receptor, measured as IC50 in the presence of 125I-CPCR4, of 250 nM or lower, and the ligand comprises a cyclic oligopeptide moiety having the motif B-Arg or B-(Me)Arg within the cyclic moiety, wherein B is a basic amino acid, a derivative thereof, or phenylalanine, provided that the motif is B-Arg when B is a Nα-methyl derivative of a basic amino acid.
摘要翻译： 本文提供了可用于诊断成像和/或治疗目的的化合物或缀合物。 每种化合物或缀合物包含趋化因子受体CXCR4的配体和可检测的标记。 该配体对于CXCR4受体具有结合亲和力，以125nM-CPCR4的存在下的IC 50测定为250nM或更低，并且配体包含具有基序B-Arg或B（Me）Arg的环状寡肽部分 环状部分，其中B是碱性氨基酸，其衍生物或苯丙氨酸，条件是当B是碱性氨基酸的Nalpha-甲基衍生物时，基序是B-Arg。
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公开(公告)号：US20110027175A1
公开(公告)日：2011-02-03
申请号：US12280829
申请日：2007-02-27
申请人： Hans Jürgen Wester , Norman Koglin , Markus Schwaiger , Horst Kessler , Burkhardt Laufer , Oliver Demmer , Martina Anton
发明人： Hans Jürgen Wester , Norman Koglin , Markus Schwaiger , Horst Kessler , Burkhardt Laufer , Oliver Demmer , Martina Anton
CPC分类号： C07K7/64 , A61K51/08 , A61K51/088
摘要： A compound, or a pharmaceutically acceptable salt or ester thereof, comprises a ligand for the chemokine receptor CXCR4 and a detectable label, the ligand having a binding affinity for the CXCR4 receptor, measured as IC50 in the presence of 125I-CPCR4, of 25O nM or lower, wherein the ligand comprises a cyclic oligopeptide moiety having the motif B-Arg or B-(Me)Arg within the cyclic moiety, and wherein B is a basic amino acid; a derivative thereof, or phenylalanine, provided that the motif is B-Arg when B is a Nα-methyl derivative of a basic amino acid. In preferred embodiments, the cyclic oligopeptide moiety has the sequence: cyclo[D-Tyr/(Me)D-Tyr-B-Arg/(Me)Arg-Z-(Ala)n-X] wherein: B is as defined above; Z is an amino acid containing an aromatic group in its side chain; n is 1 or 0, provided that n is 1 only when the preceding four amino acids in the cyclic moiety sequence are D-Tyr/(Me)D-Tyr-Arg-Arg-NaI, NaI being L-3-(2-naphthyl)alanine; and X is selected from Gly, (Me)Gly, Ala, Dap (diaminopropionic acid), Dap(FP) ((N-fluoropropionyl)-diaminopropionic acid), Dab (diaminobutylic acid), Dab(FP) ((N-fluoropropionyl)-diaminobutyric acid), Dab(FB) ((N-fluorobenzoyl)-diaminobutyric acid) and Dap(FB) ((N-fluorobenzoyl)-diaminopiOpionic acid). The compounds may be useful for diagnostic imaging and/or therapeutic purposes.
摘要翻译： 化合物或其药学上可接受的盐或酯包含用于趋化因子受体CXCR4的配体和可检测标记，在125I-CPCR4存在下以250nM的IC50测定的对CXCR4受体具有结合亲和力的配体 或更低，其中所述配体包含在环状部分内具有基序B-Arg或B（Me）Arg的环状寡肽部分，其中B为碱性氨基酸; 其衍生物或苯丙氨酸，条件是当B是碱性氨基酸的Nα-甲基衍生物时，基序是B-Arg。 在优选的实施方案中，环状寡肽部分具有以下顺序：环[D-Tyr /（Me）D-Tyr-B-Arg /（Me）Arg-Z-（Ala）n-X]其中：B如上所定义; Z是其侧链中含有芳基的氨基酸; n为1或0，条件是仅当环状部分序列中的前述四个氨基酸为D-Tyr /（Me）D-Tyr-Arg-Arg-NaI时，n为1，NaI为L-3-（2- 萘基）丙氨酸; 并且X选自Gly，（Me）Gly，Ala，Dap（二氨基丙酸），Dap（FP）（（N-氟丙酰基） - 二氨基丙酸），Dab（二氨基丁酸），Dab（FP）（（N-氟丙酰基 ） - 二氨基丁酸），Dab（FB）（（N-氟苯甲酰基） - 二氨基丁酸）和Dap（FB）（（N-氟苯甲酰基） - 二氨基丙酸）。 该化合物可用于诊断成像和/或治疗目的。
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