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11. 发明授权

US09109009B2 Template-fixed peptidomimetics with CXCR7 modulating activity 有权
标题翻译：具有CXCR7调节活性的模板固定肽模拟物
公开(公告)号：US09109009B2
公开(公告)日：2015-08-18
申请号：US13577143
申请日：2011-02-04
申请人： Frank Otto Gombert , Alexander Lederer , Ralf Löwe , Daniel Obrecht , Barbara Romagnoli , Johann Zimmermann , Kalpana Patel
发明人： Frank Otto Gombert , Alexander Lederer , Ralf Löwe , Daniel Obrecht , Barbara Romagnoli , Johann Zimmermann , Kalpana Patel
IPC分类号： A61K38/12 , C07K7/64 , C07K14/715 , C07K14/705 , A61K38/00 , A61K38/17
CPC分类号： C07K7/64 , A61K38/00 , A61K38/17 , A61K38/177 , A61K38/1793 , C07K14/705 , C07K14/715 , C07K14/7158
摘要： Novel template-fixed β-hairpin peptidomimetics of the general formula (I), wherein the single elements T or P are α-amino acid residues connected from the carbonyl (C═O) point of attachment to the nitrogen (N) of the next element in clockwise direction and wherein said elements, depending on their positions in the chain, are defined in the description and the claims have the property to act on the receptor CXCR7. Thus, these β-hairpin peptidomimetics can be useful in the treatment or prevention of diseases or conditions in the area of dermatological disorders, metabolic diseases, inflammatory diseases, fibrotic diseases, infectious diseases, neurological diseases, cardiovascular diseases, respiratory diseases, gastro-intestinal tract disorders, urological diseases, ophthalmic diseases, stomatological diseases, haematological diseases and cancer; or the mobilization of stem cells.
摘要翻译：通式（I）的新型模板固定和平滑肽模拟物，其中单元素T或P是从连接的羰基（C = O）连接到氮（N）的连接的α-氨基酸残基顺时针方向上的下一个元件，并且其中所述元件取决于它们在链中的位置在说明书中定义，并且权利要求书具有作用于受体CXCR7的性质。因此，这些β-螺旋肽模拟物可用于治疗或预防皮肤病，代谢疾病，炎性疾病，纤维化疾病，传染病，神经疾病，心血管疾病，呼吸系统疾病，胃肠疾病，肠道疾病，泌尿科疾病，眼科疾病，口腔病，血液病和癌症; 或干细胞的动员。

12. 发明授权

US08865656B2 Beta-hairpin peptidomimetics having CXCR4 antagonizing activity 有权
标题翻译：具有CXCR4拮抗活性的β-发夹肽模拟物
公开(公告)号：US08865656B2
公开(公告)日：2014-10-21
申请号：US13319052
申请日：2009-05-07
申请人： Daniel Obrecht , Frank Gombert , Alexander Lederer , Barbara Romagnoli , Christian Bisang
发明人： Daniel Obrecht , Frank Gombert , Alexander Lederer , Barbara Romagnoli , Christian Bisang
IPC分类号： A61K38/00 , C07K7/54 , A61P35/00 , C07K7/08 , C07K7/02
CPC分类号： C07K7/08 , C07K1/061 , C07K7/02
摘要： β-Hairpin peptidomimetics of the general formula Cyclo(-Xaa1-Xaa2-Xaa3-Cys4-Xaa5-Xaa6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with Xaa1, Xaa2, Xaa3, Xaa5, Xaa6, Xaa7, Xaa8, Xaa12, Xaa13, Xaa14, Xaa15 and Xaa16 being amino acid residues of certain types which are defined in the description and the claims, 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 immunosuppression; or during apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These peptides can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.
摘要翻译：通式为（Xaa1-Xaa2-Xaa3-Cys4-Xaa5-Xaa6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-）的通式肽模拟物，Cys4之间的二硫键和Cys11及其药学上可接受的盐与在说明书和权利要求书中定义的某些类型的氨基酸残基的Xaa1，Xaa2，Xaa3，Xaa5，Xaa6，Xaa7，Xaa8，Xaa12，Xaa13，Xaa14，Xaa15和Xaa16，具有CXCR4拮抗特性，可用于预防健康个体中的HIV感染，或用于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。这些肽可以通过基于混合固相和溶液相合成策略的方法制造。

13. 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.

14. 发明授权

US08642560B2 Template fixed β-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：US08642560B2
公开(公告)日：2014-02-04
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： A61K38/10 , A61K38/08
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：提供了模板固定的β-发夹模拟物和包括多个这些模拟物的文库。模板固定的β-发夹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连，由此形成环肽; 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。

15. 发明申请

US20090118134A1 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：US20090118134A1
公开(公告)日：2009-05-07
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 , Francoise Jung
发明人： Jan Wim Vrijbloed , Daniel Obrecht , Sergio Locurio , Frank Otto Gombert , Christian Ludin , Francoise Jung
IPC分类号： C40B30/04 , C07K7/00 , C40B40/10 , C40B40/02
CPC分类号： C07K1/047 , C12N15/1037 , C40B40/02
摘要： Template-fixed β-hairpin mime tics of the general formula R1-Cys-Z-Cys-R2 (1) wherein the two Cys residues are bridged by a disulfide bond thereby forming a cyclic peptide; R1 and R2 are preferably Glu-Thr and Thr-Lys; or Lys-Thr and Thr-Glu; or Thr-Glu and Lys-Thr, or Thr-Lys and Glu-Thr; or Leu-Glu and Lys-Val; or Val-Lys and Glu-Leu; or Glu-Leu and Val-Lys; or Lys-Leu and Val-Glu; or Asn-Gly and Lys-Val; or Val-Gly and Lys-Asn; or Gly-Asn and Val-Lys; or Gly-Val and Asn-Lys; or Gly-Gly and Gly-Gly; or Glu-Leu-Lys and Glu-Val-Lys; or Lys-Val-Glu and Lys-Leu-Glu; or Leu-Glu-Lys and Glu-Lys-Val; or Val-Lys-Glu and Lys-Glu-Leu; or Glu-Lys-Leu and Val-Glu-Lys; or Lys-Glu-Val and Leu-Lys-Glu; or Lys-Glu-Leu and Val-Lys-Glu; or Glu-Lys-Val and Leu-Glu-Lys; or Lys-Val-Gly and Gly-Leu-Glu; or Glu-Leu-Gly and Gly-Val-Lys; or Val-Lys-Gly and Gly-Glu-Leu; or Leu-Glu-Gly and Gly-Lys-Val; or Val-Gly-Lys and Glu-Gly-Leu; or Leu-Gly-Glu and Lys-Gly-Val; or Gly-Gly-Gly and Gly-Gly-Gly; and Z is a chain of n amino acid residues with n being an integer form 4 to 20 and with each of these n amino acid residues being, independently, derived from any naturally occurring L-α-amino acid are provided. Libraries comprising a plurality of these templates can be used for the construction of phage display derived template-fixed β-hairpin mimetics generating phage display libraries with very high binding constants to targets, thus combining the advantage of screening of large phage display derived template-fixed β-hairpin libraries which in turn considerably facilitates structure-activity studies, and hence the discovery of new molecules with potent activities and with novel selectivities towards different types of targets.
摘要翻译：通式R1-Cys-Z-Cys-R2（1）的模板固定β-发夹制剂，其中两个Cys残基用二硫键桥接，从而形成环肽; R1和R2优选为Glu-Thr和Thr-Lys; 或Lys-Thr和Thr-Glu; 或Thr-Glu和Lys-Thr，或Thr-Lys和Glu-Thr; 或Leu-Glu和Lys-Val; 或Val-Lys和Glu-Leu; 或Glu-Leu和Val-Lys; 或Lys-Leu和Val-Glu; 或Asn-Gly和Lys-Val; 或Val-Gly和Lys-Asn; 或Gly-Asn和Val-Lys; 或Gly-Val和Asn-Lys; 或Gly-Gly和Gly-Gly; 或Glu-Leu-Lys和Glu-Val-Lys; 或Lys-Val-Glu和Lys-Leu-Glu; 或Leu-Glu-Lys和Glu-Lys-Val; 或Val-Lys-Glu和Lys-Glu-Leu; 或Glu-Lys-Leu和Val-Glu-Lys; 或Lys-Glu-Val和Leu-Lys-Glu; 或Lys-Glu-Leu和Val-Lys-Glu; 或Glu-Lys-Val和Leu-Glu-Lys; 或Lys-Val-Gly和Gly-Leu-Glu; 或Glu-Leu-Gly和Gly-Val-Lys; 或Val-Lys-Gly和Gly-Glu-Leu; 或Leu-Glu-Gly和Gly-Lys-Val; 或Val-Gly-Lys和Glu-Gly-Leu; 或Leu-Gly-Glu和Lys-Gly-Val; 或Gly-Gly-Gly和Gly-Gly-Gly; 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。包含多个这些模板的文库可用于构建噬菌体展示衍生的模板固定的β-发夹模拟物，其产生具有非常高的结合常数的靶标的噬菌体展示文库，因此结合筛选大噬菌体展示衍生模板固定的优点 β-发夹文库反过来极大地促进结构活性研究，从而发现具有有效活性和对不同类型靶标具有新选择性的新分子。

16. 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。

17. 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。

18. 发明授权

US08796183B2 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：US08796183B2
公开(公告)日：2014-08-05
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 , C07K5/00
CPC分类号： C07K1/047 , C12N15/1037 , C40B40/02
摘要： A method of screening for template-fixed β-hairpin mimetics and libraries including a plurality of these mimetics is 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：提供了一种筛选模板固定和模板模拟物的方法和包括多种这些模拟物的文库。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。

19. 发明申请

US20150218219A1 BETA-HAIRPIN PEPTIDOMIMETICS 有权
公开(公告)号：US20150218219A1
公开(公告)日：2015-08-06
申请号：US14406108
申请日：2012-06-06
申请人： Frank Otto Gombert , Daniel Obrecht , Alexander Lederer , Johann Zimmermann , Christian Oefner
发明人： Frank Otto Gombert , Daniel Obrecht , Alexander Lederer , Johann Zimmermann , Christian Oefner
IPC分类号： C07K7/54
CPC分类号： A61K38/12 , A61K38/00 , C07K7/08 , C07K7/54
摘要： β-Hairpin peptidomimetics of the general formula cyclo(-Tyr1-His2-Xaa3-Cys4-Ser5-Xaa6-DPro7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Xaa14-Xaa15-Pro16-), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with Xaa3, Xaa6, Xaa8 Xaa13, Xaa14 and Xaa15 being amino acid residues of certain types which are defined in the description and the claims, have favorable pharmacological 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 immunosuppression; or during apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These peptidomimetics can be manufactured by a process which is based on a mixed solid-and solution phase synthetic strategy.
摘要翻译：通式为（-Tyr1-His2-Xaa3-Cys4-Ser5-Xaa6-DPro7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Xaa14-Xaa15-Pro16-）的平滑肽模拟物，Cys4之间的二硫键和Cys11及其药学上可接受的盐与在说明书和权利要求书中定义的某些类型的氨基酸残基的Xaa3，Xaa6，Xaa8 Xaa13，Xaa14和Xaa15具有有利的药理学性质，并且可用于预防HIV感染健康个体或减慢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和/或作为诱导干细胞动员以调节组织修复的试剂。这些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来制造。

20. 发明授权

US09617308B2 Beta-hairpin peptidomimetics 有权
公开(公告)号：US09617308B2
公开(公告)日：2017-04-11
申请号：US14406108
申请日：2012-06-06
申请人： Frank Otto Gombert , Daniel Obrecht , Alexander Lederer , Johann Zimmermann , Christian Oefner
发明人： Frank Otto Gombert , Daniel Obrecht , Alexander Lederer , Johann Zimmermann , Christian Oefner
IPC分类号： C07K7/54 , C07K7/50 , A61K38/00 , A61K38/12 , A61K38/04 , C07K7/08
CPC分类号： A61K38/12 , A61K38/00 , C07K7/08 , C07K7/54
摘要： β-Hairpin peptidomimetics of the general formula cyclo(-Tyr1-His2-Xaa3-Cys4-Ser5-Xaa6-DPro7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Xaa14-Xaa15-Pro16-), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with Xaa3, Xaa6, Xaa8 Xaa13, Xaa14 and Xaa15 being amino acid residues of certain types which are defined in the description and the claims, have favorable pharmacological 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 immunosuppression; or during apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These peptidomimetics can be manufactured by a process which is based on a mixed solid-and solution phase synthetic strategy.

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