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    Dye conjugates of template-fixed peptidomimetics
    4.
    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
    5.
    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 BETA-HAIRPIN PEPTIDOMIMETICS WITH CXCR4 ANTAGONIZING ACTIVITY
    6.
    发明申请
    TEMPLATE-FIXED BETA-HAIRPIN PEPTIDOMIMETICS WITH CXCR4 ANTAGONIZING ACTIVITY 有权
    具有CXCR4拮抗活性的模板固定的BETA-HAIRPIN PEPTIDOMIMETICS

    公开(公告)号：US20110312879A1

    公开(公告)日：2011-12-22

    申请号：US13131205

    申请日：2008-11-26

    申请人： Frank Gombert ,  Daniel Obrecht ,  Alexander Lederer ,  Barbara Romagnoli

    发明人： Frank Gombert ,  Daniel Obrecht ,  Alexander Lederer ,  Barbara Romagnoli

    IPC分类号： A61K38/15 ,  A61P7/00 ,  A61P31/18 ,  A61P35/00 ,  A61P35/04 ,  A61P29/00 ,  C07K7/54 ,  A61P9/10

    CPC分类号： C07K7/64 ,  C07K1/047 ,  C07K7/08

    摘要： Template-fixed peptidomimetics formula (Ia) formula (Ib) wherein Z is a template-fixed chain of 14 α-amino and/or α-hydroxy acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Pro, Gly, a glycolic acid residue or of certain types which, as the remaining symbols in the above formulae, are defined in the description and the claims, and salts thereof, have CXCR4 antagonizing properties and can be used for preventing HIV infections in non-infected 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 during apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These depsipeptides can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

    摘要翻译： 模板固定肽模拟物式（Ia）式（Ib）其中Z是14个α-氨基和/或α-羟基酸残基的模板固定链，其取决于其在链中的位置（从N-末端计数 氨基酸）是Pro，Gly，乙醇酸残基或某些类型，其作为上述式中的其余符号在说明书和权利要求书及其权利要求书中定义，其盐具有CXCR4拮抗特性，并且可用于 预防未感染个体的艾滋病毒感染或减缓和阻止感染患者的病毒进展; 或由CXCR4受体活性介导或产生癌症; 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; 或在外周血干细胞的分离采集期间和/或作为诱导干细胞动员以调节组织修复的试剂。 这些脱肽可以通过基于混合固相和溶液相合成策略的方法制备。

    PEPTIDES
    8.
    发明申请
    PEPTIDES 审中-公开

    公开(公告)号：US20080318838A1

    公开(公告)日：2008-12-25

    申请号：US12169134

    申请日：2008-07-08

    申请人： Wilfried Bauer ,  Robin Breckenridge ,  Francois Cardinaux ,  Frank Gombert ,  Hermann Gram ,  Paul Ramage ,  Helmut Schneider ,  Rudolf Waelchli ,  Rainer Albert ,  Ian Lewis

    发明人： Wilfried Bauer ,  Robin Breckenridge ,  Francois Cardinaux ,  Frank Gombert ,  Hermann Gram ,  Paul Ramage ,  Helmut Schneider ,  Rudolf Waelchli ,  Rainer Albert ,  Ian Lewis

    IPC分类号： A61K38/00 ,  C07K7/00 ,  C12P21/04 ,  C12N15/11 ,  A61P19/00 ,  C12N15/00 ,  C12N1/20

    CPC分类号： C07K14/005 ,  A61K38/00 ,  C07K14/635 ,  C07K2319/00 ,  C07K2319/50 ,  C07K2319/75 ,  C12N2795/10222

    摘要： PTH compounds having PTH-like activity and comprising at least one modification, said modification being either 1. at least one radical selected from a L- or D-α-amino acid, C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to the terminal amino group of the PTH compound, and/or at least one radical selected from C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to one or more side chain amino groups of the PTH compound, or 2. at least one α-amino acid unit in the positions 1 to 38 of a naturally occurring PTH sequence being replaced by a natural or unnatural amino acid unit optionally in protected form, whereby the α-amino acid units present in positions 1 and 2 at the amino terminus of the PTH sequence may be replaced by a pseudo-peptide, or a combination of such modifications, in free form or in salt form, have pharmacological activity, e.g. for preventing or treating all bone conditions which are associated with increased calcium depletion or resorption or in which calcium fixation in the bone is desirable.

    摘要翻译： 具有PTH样活性并且包含至少一个修饰的PTH化合物，所述修饰是1.至少一个选自L-或D-α-氨基酸，C2-6羰基和任选取代的C 1-8烷基的基团，C 2-8烯基 ，C 2-8炔基，芳烷基，芳烯基或C 3-6环烷基-C 1-4烷基，并且连接到PTH化合物的末端氨基，和/或至少一个选自C 2-6烷氧基羰基和任选取代的C 1-8烷基基团，C 2-8烯基 ，C 2-8炔基，芳烷基，芳烯基或C 3-6环烷基-C 1-4烷基，并且连接到PTH化合物的一个或多个侧链氨基，或2个至少一个α-氨基酸单元的位置1至38 天然存在的PTH序列被任选以保护形式的天然或非天然氨基酸单元替代，由此存在于PTH序列的氨基末端的位置1和2中的α-氨基酸单元可被假肽替代，或 这些修改的组合，免费的 m或盐形式，具有药理活性，例如。 用于预防或治疗与增加的钙耗竭或吸收相关的所有骨骼状况或其中期望骨中的钙固定。