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    Dye conjugates of template-fixed peptidomimetics
    2.
    发明授权
    Dye conjugates of template-fixed peptidomimetics 有权
    模板固定肽模拟物的染料缀合物

    公开(公告)号：US09073973B2

    公开(公告)日：2015-07-07

    申请号：US11913511

    申请日：2005-05-02

    申请人： Steven J. DeMarco ,  Frank Gombert ,  Daniel Obrecht ,  Christian Ludin ,  Barbara Romagnoli

    发明人： Steven J. DeMarco ,  Frank Gombert ,  Daniel Obrecht ,  Christian Ludin ,  Barbara Romagnoli

    IPC分类号： A61K38/10 ,  C07K5/00 ,  C07K7/64 ,  A61K38/48

    CPC分类号： C07K7/64 ,  A61K38/4886

    摘要： Dye conjugates of template-fixed β-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 14 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly, or Pro or of certain types which, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have CXCR4 antagonizing properties, and are useful for cancer therapy; diagnostic imaging; for detection of tumors and other abnormalities; for photoacoustic tumor imaging, detection and therapy; and for sonofluorescence tumor imaging, detection and therapy. The various dyes forming part of these conjugates are useful over the range of 300-1200 nm, the exact range being dependent upon the particular dye. These dye conjugates of β-hairpin peptidomimetic can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.

    摘要翻译： 通式（I）的模板固定和平滑肽模拟物的染料缀合物，其中Z是14个α-氨基酸残基的模板固定链，这取决于它们在链中的位置（从N-末端计数 氨基酸）是Gly或Pro或某些类型，其作为上述式中的其余符号在说明书和权利要求书中定义，及其盐具有CXCR4拮抗性质，并且可用于癌症治疗; 诊断成像; 用于检测肿瘤等异常; 用于光声肿瘤成像，检测和治疗; 并用于超声荧光肿瘤成像，检测和治疗。 形成这些共轭物的一部分的各种染料在300-1200nm的范围内是有用的，确切的范围取决于特定的染料。 这些染色偶联物，可以通过基于混合固相和溶液相合成策略的方法制造。

    Template-fixed peptidomimetics with antimicrobial activity
    3.
    发明授权
    Template-fixed peptidomimetics with antimicrobial activity 有权
    具有抗菌活性的模板固定肽模拟物

    公开(公告)号：US08685922B2

    公开(公告)日：2014-04-01

    申请号：US12161065

    申请日：2007-01-15

    申请人： Steven J. Demarco ,  Wim Vrijbloed ,  Ricardo Dias ,  John Anthony Robinson ,  Nityakalyani Srinivas ,  Frank Gombert ,  Daniel Obrecht

    发明人： Steven J. Demarco ,  Wim Vrijbloed ,  Ricardo Dias ,  John Anthony Robinson ,  Nityakalyani Srinivas ,  Frank Gombert ,  Daniel Obrecht

    IPC分类号： A61K38/10 ,  C07K7/08 ,  A61P31/00

    CPC分类号： C07K7/64 ,  A01N43/36 ,  A61K38/00 ,  C07K1/10 ,  C07K7/06 ,  C07K7/08 ,  C07K14/001

    摘要： Template-fixed β-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, or Pro, or of certain types which, as the remaining Symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to selectively inhibit the growth of or to kill microorganisms such as Pseudomonas aeruginosa. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials, or as medicaments to treat or prevent infections. These β-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and Solution phase synthetic strategy.

    摘要翻译： 通式（I）的模板固定和半乳糖肽模拟物，其中Z是12个α-氨基酸残基的模板固定链，其取决于其在链中的位置（从N-末端氨基酸开始计数） 是Gly或Pro，或某些类型，其作为上述式中的其余符号在说明书和权利要求书中定义，以及其盐具有选择性抑制微生物生长或杀死诸如假单胞菌 铜绿假单胞菌 它们可以用作食品，化妆品，药​​物或其他含营养材料的消毒剂，或用作治疗或预防感染的药物。 这些可以通过基于混合固相和溶液相合成策略的方法制造。

    TEMPLATE-FIXED PEPTIDOMIMETICS
    7.
    发明申请
    TEMPLATE-FIXED PEPTIDOMIMETICS 审中-公开
    模板固定蛋白质

    公开(公告)号：US20130150299A1

    公开(公告)日：2013-06-13

    申请号：US13764099

    申请日：2013-02-11

    申请人： Daniel OBRECHT ,  Frank Gombert ,  Steven J. Demarco ,  Christian Ludin ,  Jan Wim Vrijbloed ,  Kerstin Moehle ,  John-Anthony Robinson ,  Reshmi Mukherjee ,  Heiko Henze ,  Barbara Romagnoli

    发明人： Daniel OBRECHT ,  Frank Gombert ,  Steven J. Demarco ,  Christian Ludin ,  Jan Wim Vrijbloed ,  Kerstin Moehle ,  John-Anthony Robinson ,  Reshmi Mukherjee ,  Heiko Henze ,  Barbara Romagnoli

    IPC分类号： A61K38/12

    CPC分类号： C07K7/56 ,  A61K38/00 ,  A61K38/12 ,  C07K7/64

    摘要： The template-fixed β-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro), disulfide bond between Cys4 and Gys11, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, have CXCR4 antagonizing properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where Cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immuno suppression; or, in particular, for stem cell mobilisation of peripheral blood stem cells and/or mesenchymal stem cell (MSC) and/or other stem cells which retention depend on the CXCR4-receptor. These β-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and Solution phase synthetic strategy, using methods which are well known to those adequately skilled in peptide chemistry.

    摘要翻译： 模板固定的β-发夹肽模拟物Cyclo（-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro），Cys4和Gys11之间的二硫键 和其药学上可接受的盐，其中X为Ala或Tyr，具有CXCR4拮抗性质，可用于预防健康个体的HIV感染或减缓和停止感染患者的病毒进展; 或其中癌症介导或由CXCR4受体活性产生; 或其中免疫性疾病介导或由CXCR4受体活性产生; 或用于治疗免疫抑制; 或特别是用于干细胞移动外周血干细胞和/或间充质干细胞（MSC）和/或其它干细胞，其保留取决于CXCR4-受体。 这些β-发夹肽模拟物可以通过使用基于混合固相和溶液相合成策略的方法来制备，该方法使用肽化学中相当熟练技术人员众所周知的方法。

    TEMPLATE-FIXED PEPTIDOMIMETICS
    10.
    发明申请
    TEMPLATE-FIXED PEPTIDOMIMETICS 有权
    模板固定蛋白质

    公开(公告)号：US20100048463A1

    公开(公告)日：2010-02-25

    申请号：US12528926

    申请日：2007-02-28

    申请人： Daniel Obrecht ,  Frank Gombert ,  Steven J. Demarco ,  Christian Ludin ,  Jan Wim Vrijbloed ,  Kerstin Moehle ,  John-Anthony Robinson ,  Reshmi Mukherjee ,  Heiko Henze ,  Barbara Romagnoli

    发明人： Daniel Obrecht ,  Frank Gombert ,  Steven J. Demarco ,  Christian Ludin ,  Jan Wim Vrijbloed ,  Kerstin Moehle ,  John-Anthony Robinson ,  Reshmi Mukherjee ,  Heiko Henze ,  Barbara Romagnoli

    IPC分类号： C07K7/56 ,  A61K38/12 ,  A61P31/12 ,  A61P31/18

    CPC分类号： C07K7/56 ,  A61K38/00 ,  A61K38/12 ,  C07K7/64

    摘要： The template-fixed B-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro), disulfide bond between Cys4 and Gys11, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, have CXCR4 antagonizing properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where Cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immuno suppression; or, in particular, for stem cell mobilisation of peripheral blood stem cells and/or mesenchymal stem cell (MSC) and/or other stem cells which retention depend on the CXCR4-receptor. These β-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and Solution phase synthetic strategy, using methods which are well known to those adequately skilled in peptide chemistry.

    摘要翻译： 模板固定的B发夹肽模拟物Cyclo（-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro），Cys4和Gys11之间的二硫键 和其药学上可接受的盐，其中X为Ala或Tyr，具有CXCR4拮抗性质，可用于预防健康个体的HIV感染或减缓和停止感染患者的病毒进展; 或其中癌症介导或由CXCR4受体活性产生; 或其中免疫性疾病介导或由CXCR4受体活性产生; 或用于治疗免疫抑制; 或特别是用于干细胞移动外周血干细胞和/或间充质干细胞（MSC）和/或其它干细胞，其保留取决于CXCR4-受体。 这些和包装肽模拟物可以通过使用基于混合固相和溶液相合成策略的方法，使用肽化学方面熟练的技术熟知的方法来制造。