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1. 发明申请

US20110294702A1 TEMPLATE FIXED BETA-HAIRPIN LOOP MIMETICS AND THEIR USE IN PHAGE DISPLAY 有权
标题翻译：模板固定的BETA-HAIRPIN环状物质及其在PHAGE显示中的使用
公开(公告)号：US20110294702A1
公开(公告)日：2011-12-01
申请号：US13196658
申请日：2011-08-02
申请人： Jan Wim Vrijbloed , Daniel Obrecht , Sergio Locurio , Frank Otto Gombert , Christian Ludin , Françoise Jung
发明人： Jan Wim Vrijbloed , Daniel Obrecht , Sergio Locurio , Frank Otto Gombert , Christian Ludin , Françoise Jung
IPC分类号： C40B40/10
CPC分类号： C07K1/047 , C12N15/1037 , C40B40/02
摘要： Template-fixed β-hairpin mimetics and libraries including a plurality of these mimetics are provided. The template-fixed β-hairpin mimetics are of the following general formula: R1-Cys-Z-Cys-R2 I wherein the two cysteine residues are bridged by a disulfide bond, thereby forming a cyclic peptide; R1 and R2 are di- or tripeptide moieties of certain types, as defined herein; and Z is a chain of n amino acid residues with n being an integer from 4 to 20 and with each of these n amino acid residues being, independently, derived from any naturally occurring L-α-amino acid.
摘要翻译：提供了模板固定模板和包含多个这些模拟物的文库。模板固定和双螺旋模拟物具有以下通式：R1-Cys-Z-Cys-R2I，其中两个半胱氨酸残基通过二硫键桥接，从而形成环肽; R1和R2是如本文所定义的某些类型的二肽或三肽部分; 并且Z是n个氨基酸残基的链，n是4至20的整数，并且这些n个氨基酸残基中的每一个独立地衍生自任何天然存在的L-α-氨基酸。

2. 发明申请

US20110245155A1 TEMPLATE-FIXED BETA-HAIRPIN PEPTIDOMIMETICS WITH CXCR4 ANTAGONIZING ACTIVITY 有权
标题翻译：具有CXCR4拮抗活性的模板固定的BETA-HAIRPIN PEPTIDOMIMETICS
公开(公告)号：US20110245155A1
公开(公告)日：2011-10-06
申请号：US12828998
申请日：2010-07-01
申请人： Jürg Zumbrunn , Steven J. Demarco , Sergio Lociuro , Jan Wim Vrijbloed , Frank Gombert , Reshmi Mukherjee , Kerstin Moehle , Daniel Obrecht , John Anthony Robinson , Heiko Henze , Barbara Romagnoli , Christian Ludin
发明人： Jürg Zumbrunn , Steven J. Demarco , Sergio Lociuro , Jan Wim Vrijbloed , Frank Gombert , Reshmi Mukherjee , Kerstin Moehle , Daniel Obrecht , John Anthony Robinson , Heiko Henze , Barbara Romagnoli , Christian Ludin
IPC分类号： A61K38/12 , C07K7/00 , A61K38/10 , A61P31/18 , A61P35/00
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）的模板固定和半乳糖肽模拟物，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拮抗性质并且可以使用用于预防健康个体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。这些可以通过基于混合固相和溶液相合成策略的方法制造。

3. 发明授权

US07994118B2 Template fixed beta-hairpin loop mimetics and their use in phage display 有权
标题翻译：模板固定β-发夹环模拟物及其在噬菌体展示中的应用
公开(公告)号：US07994118B2
公开(公告)日：2011-08-09
申请号：US10579104
申请日：2003-11-15
申请人： Jan Wim Vrijbloed , Daniel Obrecht , Sergio Locurio , Frank Otto Gombert , Christian Ludin , Françoise Jung
发明人： Jan Wim Vrijbloed , Daniel Obrecht , Sergio Locurio , Frank Otto Gombert , Christian Ludin , Françoise Jung
IPC分类号： A61K38/04 , A61K38/12
CPC分类号： C07K1/047 , C12N15/1037 , C40B40/02
摘要： Template-fixed β-hairpin mimetics and libraries including a plurality of these mimetics are provided. The template-fixed β-hairpin mimetics are of the following general formula: R1-Cys-Z-Cys-R2 (I) wherein the two cysteine residues are bridged by a disulfide bond, thereby forming a cyclic peptide; R1 and R2 are di- or tripeptide moieties of certain types, as defined herein; and Z is a chain of n amino acid residues with n being an integer from 4 to 20 and with each of these n amino acid residues being, independently, derived from any naturally occurring L-α-amino acid.
摘要翻译：提供了模板固定模板和包含多个这些模拟物的文库。模板固定和模板模拟物具有以下通式：R1-Cys-Z-Cys-R2（I），其中两个半胱氨酸残基用二硫键桥连，从而形成环肽; R1和R2是如本文所定义的某些类型的二肽或三肽部分; 并且Z是n个氨基酸残基的链，n是4至20的整数，并且这些n个氨基酸残基中的每一个独立地衍生自任何天然存在的L-α-氨基酸。

4. 发明申请

US20110135576A1 DYE CONJUGATES OF TEMPLATE-FIXED PEPTIDOMIMETICS 有权
标题翻译：模板固定肽的DYE结合
公开(公告)号：US20110135576A1
公开(公告)日：2011-06-09
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： A61K38/12 , C07K7/64 , C07K7/54 , A61K49/22 , A61P35/00 , A61K49/00
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。

5. 发明授权

US07855179B2 Template-fixed peptidomimetics with antimicrobial activity 有权
标题翻译：具有抗菌活性的模板固定肽模拟物
公开(公告)号：US07855179B2
公开(公告)日：2010-12-21
申请号：US10530335
申请日：2002-10-02
申请人： Jan Wim Vrijbloed , Daniel Obrecht , John Anthony Robinson , Sergio Locurio , Frank Gombert , Christian Ludin , Alexander Lederer , Shivaprasad Shankaramma
发明人： Jan Wim Vrijbloed , Daniel Obrecht , John Anthony Robinson , Sergio Locurio , Frank Gombert , Christian Ludin , Alexander Lederer , Shivaprasad Shankaramma
IPC分类号： A61K38/10 , C07K7/08 , C07K1/36
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）的模板固定型和半乳糖肽模拟物，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，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剩余符号在说明书和权利要求书中定义，并且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。这些和平滑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造。

6. 发明授权

US07786078B2 Template-fixed δ-hairpin peptidomimetics with CXCR4 antagonizing activity 有权
标题翻译：具有CXCR4拮抗活性的模板固定的δ-发夹肽模拟物
公开(公告)号：US07786078B2
公开(公告)日：2010-08-31
申请号：US10555088
申请日：2004-04-29
申请人： Jürg Zumbrunn , Steven J. Demarco , Sergio Lociuro , Jan Wim Vrijbloed , Frank Gombert , Reshmi Mukherjee , Kerstin Moehle , Daniel Obrecht , John Anthony Robinson , Heiko Henze , Barbara Romagnoli , Christian Ludin
发明人： Jürg Zumbrunn , Steven J. Demarco , Sergio Lociuro , Jan Wim Vrijbloed , Frank Gombert , Reshmi Mukherjee , Kerstin Moehle , Daniel Obrecht , John Anthony Robinson , Heiko Henze , Barbara Romagnoli , Christian Ludin
IPC分类号： A61K38/12
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. 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）的模板固定和半乳糖肽模拟物，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盐中定义，具有CXCR4拮抗性质。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。

7. 发明授权

US07671009B2 Dermopharmaceutically and cosmetically active oligopeptides 有权
标题翻译：药物和化妆品活性寡肽
公开(公告)号：US07671009B2
公开(公告)日：2010-03-02
申请号：US10493856
申请日：2002-10-30
申请人： Christian Ludin , Marc Heidl , Hugo Ziegler
发明人： Christian Ludin , Marc Heidl , Hugo Ziegler
IPC分类号： A61K38/00
CPC分类号： C07K14/78 , A61K38/00 , C07K5/06086
摘要： Oligopeptides and derivatives thereof, peptide analogs and derivatives thereof as well as pharmaceutically acceptable salts of these compounds, which correspond to general formula (I) wherein R1 represents H, —C(O)—R7, —SO2—R7, —C(O)—OR7 or —C(O)—N(R7)2 R2 represents, independent of one another, H or —(C1-C4)-alkyl, R3 and R6 represent, independent of one another, —(CH2)q—N(R1)R8 R4 and R5 represent, independent of one another, —CH2—OR2, —CH(CH3)OR8 or —CH2—CH2—OR8 R7 represents hydrogen, optionally substituted (C1-C19)-alkyl; optionally substituted (C1-C19)-alkenyl; phenyl-(C1-C4)-alkyl whose phenyl radical is optionally substituted with amino in the para position R8 represents H, —(C1-C4)-alkyl, —C(O)—R7, —C(O)—OR7, —C(O)—N(R7)2 or —SO2—R7 X represents oxygen (—O—) or —NH—; or XR7, with X=O, also represents the esters of α-tocopherol, tocotrienol or retinol or the carboxylic acid (with R7=H) m, n, p represent, independent of one another, zero or 1 and q in R3 and R6 represent, independent of one another, an integer from 1 to 4, with the provision that the following conditions do not simultaneously occur: R4=—CH(CH3)—OH and R5=—CH(CH3)—OH and R6=—(CH2)4—NH2; dermopharmaceutically and/or cosmetically active compositions containing at least one compound of formula (I).
摘要翻译：对应于通式（I）的寡肽及其衍生物，肽类似物及其衍生物以及这些化合物的药学上可接受的盐，其中R 1表示H，-C（O）-R 7，-SO 2 -R 7，-C（O ）-OR 7或-C（O）-N（R 7）2 R 2彼此独立地表示H或 - （C 1 -C 4） - 烷基，R 3和R 6彼此独立地表示 - （CH 2）q - N（R 1）R 8 R 4和R 5彼此独立地表示-CH 2 OR 2，-CH（CH 3）OR 8或-CH 2 -CH 2 -OR 8 R 7表示氢，任选取代的（C 1 -C 19） - 烷基; 任选取代的（C 1 -C 19） - 烯基; 苯基 - （C 1 -C 4） - 烷基，其苯基任选被对位R8上的氨基取代，代表H， - （C1-C4） - 烷基，-C（O）-R7，-C（O）-OR7， -C（O）-N（R 7）2或-SO 2 -R 7 X表示氧（-O-）或-NH-; 或具有X = O的XR7也表示α-生育酚，生育三烯酚或视黄醇或羧酸（R7 = H）m，n，p表示彼此独立的零或1和q在R3和 R6代表彼此独立的1至4的整数，条件是不同时发生以下条件：R4 = -CH（CH3）-OH，R5 = -CH（CH3）-OH，R6 = - （CH 2）4 -NH 2; 含有至少一种式（I）化合物的药物和/或化妆品活性组合物。

8. 发明申请

US20110319291A1 TEMPLATE FIXED BETA-HAIRPIN LOOP MIMETICS AND THEIR USE IN PHAGE DISPLAY 有权
公开(公告)号：US20110319291A1
公开(公告)日：2011-12-29
申请号：US13196712
申请日：2011-08-02
申请人： Jan Wim Vrijbloed , Daniel Obrecht , Sergio Locurio , Frank Otto Gombert , Christian Ludin , Françoise Jung
发明人： Jan Wim Vrijbloed , Daniel Obrecht , Sergio Locurio , Frank Otto Gombert , Christian Ludin , Françoise Jung
IPC分类号： C40B30/04
CPC分类号： C07K1/047 , C12N15/1037 , C40B40/02
摘要： Template-fixed β-hairpin mimetics and libraries including a plurality of these mimetics are provided. The template-fixed β-hairpin mimetics are of the following general formula: R1-Cys-Z-Cys-R2 I wherein the two cysteine residues are bridged by a disulfide bond, thereby forming a cyclic peptide; R1 and R2 are di- or tripeptide moieties of certain types, as defined herein; and Z is a chain of n amino acid residues with n being an integer from 4 to 20 and with each of these n amino acid residues being, independently, derived from any naturally occurring L-α-amino acid.

9. 发明申请

US20070078079A1 Template-fixed beta-hairpin peptidomimetics with cxcr4 antagonizing activity 有权
标题翻译：具有cxcr4拮抗活性的模板固定β-发夹肽模拟物
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。

10. 发明申请

US20070054840A1 Template-fixed peptidomimetics with antimicrobial activity 有权
标题翻译：具有抗菌活性的模板固定肽模拟物
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。

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