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    • 1. 发明申请
    • BETA-HAIRPIN PEPTIDOMIMETICS
    • WO2013182240A1
    • 2013-12-12
    • PCT/EP2012/060766
    • 2012-06-06
    • POLYPHOR AGGOMBERT, Frank OttoOBRECHT, DanielLEDERER, AlexanderZIMMERMANN, JohannOEFNER, Christian
    • GOMBERT, Frank OttoOBRECHT, DanielLEDERER, AlexanderZIMMERMANN, JohannOEFNER, Christian
    • C07K7/64
    • A61K38/12A61K38/00C07K7/08C07K7/54
    • β-Hairpin peptidomimetics of the general formula cyclo(-Tyr 1 -His 2 -Xaa 3 -Cys 4 -Ser 5 -Xaa 6 -DPro 7 -Xaa 8 -Arg 9 -Tyr 10 -Cys 11 -Tyr 12 -Xaa 13 -Xaa 14 -Xaa 15 -Pro 16 -), disulfide bond between Cys 4 and Cys 11 , and pharmaceutically acceptable salts thereof, with Xaa 3 , Xaa 6 , Xaa 8 , Xaa 13 , Xaa 14 and Xaa 15 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.
    • 通式为(-Tyr1-His2-Xaa3-Cys4-Ser5-Xaa6-DPro7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Xaa14-Xaa15-Pro16-)的β-发夹肽模拟物,Cys4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。
    • 5. 发明申请
    • BETA-HAIRPIN PEPTIDOMIMETICS HAVING CXCR4 ANTAGONIZING ACTIVITY
    • 具有CXCR4拮抗活性的BETA-HAIRPIN PEPTIDOMIMETICS
    • WO2010127704A1
    • 2010-11-11
    • PCT/EP2009/055563
    • 2009-05-07
    • POLYPHOR AGOBRECHT, DanielGOMBERT, Frank, OttoLEDERER, AlexanderROMAGNOLI, BarbaraBISANG, Christian
    • OBRECHT, DanielGOMBERT, Frank, OttoLEDERER, AlexanderROMAGNOLI, BarbaraBISANG, Christian
    • C07K7/08C07K7/02A61K38/10A61P29/00A61P31/18A61P35/00
    • C07K7/08C07K1/061C07K7/02
    • β-Hairpin peptidomimetics of the general formula Cyclo(-Xaa 1 -Xaa 2 -Xaa 3 -Cys 4 -Xaa 5 -Xaa 6 -Xaa 7 -Xaa 8 -Arg 9 -Tyr 10 -Cys 11 - Xaa 12 -Xaa 13 -Xaa 14 -Xaa 15 -Xaa 16 -), disulfide bond between Cys 4 and Cys11, and pharmaceutically acceptable salts thereof, with Xaa 1 , Xaa 2 , Xaa 3 , Xaa 5 , Xaa 6 , Xaa 7 , Xaa 8 , Xaa 12 , Xaa 13 , Xaa 14 , Xaa 15 and Xaa 16 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.
    • ß-通式为(Xaa1-Xaa2-Xaa3-Cys4-Xaa5-Xaa6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-)的发夹肽模拟物,Cys4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拮抗性,可用于预防健康个体的艾滋病毒感染,或用于缓解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。
    • 7. 发明申请
    • BETA - HAIRPIN PEPTIDOMIMETICS AS CXC4 ANTAGONISTS
    • 作为CXC4拮抗剂的BETA - HAIRPIN PEPTIDOMIMITICS
    • WO2012168336A1
    • 2012-12-13
    • PCT/EP2012/060763
    • 2012-06-06
    • POLYPHOR AGOBRECHT, DanielGOMBERT, Frank, OttoZIMMERMANN, Johann
    • OBRECHT, DanielGOMBERT, Frank, OttoZIMMERMANN, Johann
    • C07K7/64A61K38/04
    • C07K7/08A61K38/00C07K1/047C07K7/64
    • β-Hairpin peptidomimetics of the general formula cyclo(-Tyr 1 -His 2 -Xaa 3 -Cys 4 -Ser 5 - Ala 6 -Xaa 7 -Xaa 8 -Arg 9 -Tyr 10 -Cys 11 -Tyr 12 -Xaa 13 -Xaa 14-D Pro 15 -Pro 16 -), disulfide bond between Cys 4 and Cys 11 , and pharmaceutically acceptable salts thereof, with Xaa 3 , Xaa 7 , Xaa 8 , Xaa 13 and Xaa 14 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.
    • ß-通式为环(-Tyr1-His2-Xaa3-Cys4-Ser5-Ala6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Xaa14-DPro15-Pro16-)的发夹肽模拟物,Cys4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,Xaa7,Xaa8,Xaa13和Xaa14具有有利的药理学性质并且可用于预防健康个体中的HIV感染 或用于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和/或作为诱导干细胞动员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制造。