公开(公告)号：US20070078079A1

公开(公告)日：2007-04-05

申请号：US10555088

申请日：2004-04-29

申请人： Jurg Zumbrunn ,  Steven Demarco ,  Sergio Lociuro ,  Jan Vrijbloed ,  Frank Gombert ,  Reshmi Mukherjee ,  Kerstin Moehle ,  Daniel Obrecht ,  John Robinson ,  Heiko Henze ,  Barbara Romagnoli ,  Christian Ludin

发明人： Jurg Zumbrunn ,  Steven Demarco ,  Sergio Lociuro ,  Jan Vrijbloed ,  Frank Gombert ,  Reshmi Mukherjee ,  Kerstin Moehle ,  Daniel Obrecht ,  John Robinson ,  Heiko Henze ,  Barbara Romagnoli ,  Christian Ludin

IPC分类号： A61K38/12 ,  C07K5/12

CPC分类号： C07K7/64 ,  A61K38/00 ,  C07K1/047 ,  C07K7/08

摘要： Template-fixed β-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12, 14 or 18 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly, NMeGly, Pro or Pip, 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 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 during apheresis collections of peripheral blood stem cells. These β-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid and solution phase synthetic strategy.

摘要翻译： 通式（I）的模板固定的β-发夹肽模拟物，其中Z是12,14或18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-末端开始计数 氨基酸）是Gly，NMeGly，Pro或Pip，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，及其盐具有CXCR4拮抗特性，可用于 预防健康人中的艾滋病毒感染或减缓和停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。 这些β-发夹肽模拟物可以通过基于混合固相和溶液相合成策略的方法制备。

公开(公告)号：US20070054840A1

公开(公告)日：2007-03-08

申请号：US10530335

申请日：2002-10-02

申请人： Jan Vrijbloed ,  Daniel Obrecht ,  John Robinson ,  Sergio Locurio ,  Frank Gombert ,  Christian Ludin ,  Alexander Lederer ,  Shivaprasad Shankaramma

发明人： Jan Vrijbloed ,  Daniel Obrecht ,  John Robinson ,  Sergio Locurio ,  Frank Gombert ,  Christian Ludin ,  Alexander Lederer ,  Shivaprasad Shankaramma

IPC分类号： A61K38/12 ,  C07K7/60

CPC分类号： C07K7/08 ,  A61K38/00 ,  C07K7/06 ,  C07K7/64 ,  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, at least one of these residues being of the type of N-substituted glycines, which types, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to inhibit the growth of or to kill microorganisms. 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）的模板固定的β-发夹肽模拟物，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，这些残基中的至少一种是N-取代的甘氨酸类型，其类型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 具有抑制微生物生长或杀死微生物的性质。 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β-发夹肽模拟物可以通过基于混合固相和溶液相合成策略的方法制备。

公开(公告)号：US20050239693A1

公开(公告)日：2005-10-27

申请号：US11062021

申请日：2005-02-18

申请人： Jan Vrijbloed ,  Daniel Obrecht ,  John Robinson ,  Odile Sellier ,  Marc Kessler

发明人： Jan Vrijbloed ,  Daniel Obrecht ,  John Robinson ,  Odile Sellier ,  Marc Kessler

IPC分类号： A61K38/00 ,  A61P31/04 ,  C07K1/04 ,  C07K5/078 ,  C07K7/64 ,  A61K38/12 ,  C07K5/12

CPC分类号： C07K5/06165 ,  A61K38/00 ,  C07K1/047 ,  C07K7/64 ,  Y02A50/473

摘要： Template-fixed β-hairpin peptidomimetics of the general formula 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 and Acinetobacter. 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： 模板固定的β-发夹肽模拟物，其通式如下：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）为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及其盐中定义，具有选择性抑制绿脓假单胞菌和不动杆菌等微生物生长或杀死微生物的性质。 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β-发夹肽模拟物可以通过基于混合固相和溶液相合成策略的方法制备。