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1. 发明申请

WO2022028738A1 ANTIMICROBIAL PEPTIDOMIMETICS 审中-公开
公开(公告)号：WO2022028738A1
公开(公告)日：2022-02-10
申请号：PCT/EP2021/025302
申请日：2021-08-05
申请人： POLYPHOR AG , UNIVERSITÄT ZÜRICH
发明人： OBRECHT, Daniel , LUTHER, Anatol , UPERT, Grégory , DESJONQUERES, Nicolas , BRABET, Emilie , ZBINDEN, Peter , ZERBE, Oliver , MÖHLE, Kerstin
IPC分类号： C07K7/08 , C07K14/47 , A61P31/02 , A61K38/00
摘要： The present invention is directed to peptidomimetics having antibacterial activity, especially against Gram-negative bacteria. The peptidomimetics of the invention are compounds of the general formula (I), [X3]t-[X2]S-X1-P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-P13-P14-P15-P16 and pharmaceutically acceptable salts thereof, as described in the description and in the claims. The invention is also directed to therapeutic uses of the peptidomimetics for the treatment or prevention of bacterial infections and diseases related to bacterial infections and to non-therapeutic uses of the peptidomimetics for preserving or disinfecting foodstuffs, cosmetics, medicaments or other nutrient-containing materials. In addition, the present invention provides an efficient synthetic process by which these compounds can, if desired, be made in parallel library-format. Moreover, the peptidomimetics of the invention show improved antimicrobial activity, low or no hemolysis of red blood cells and reduced cytotoxicity.

2. 发明申请

WO2016050360A1 BETA-HAIRPIN PEPTIDOMIMETICS 审中-公开
公开(公告)号：WO2016050360A1
公开(公告)日：2016-04-07
申请号：PCT/EP2015/025067
申请日：2015-09-29
申请人： POLYPHOR AG
发明人： OBRECHT, Daniel , LUTHER, Anatol , BERNARDINI, Francesca , DENIAU, Gildas , LEDERER, Alexander
IPC分类号： C07K7/64
CPC分类号： C07K7/64 , A61K38/00 , Y02A50/473
摘要： Beta-hairpin peptidomimetics of the general formula (I), cyclo[P 1 -P 2 -P 3 -P 4 -P 5 -P 6 - P 7 -P 8 -P 9 -P 10 -P 11 -P 12 -T 1 -T 2 ], and pharmaceutically acceptable salts thereof, with P 1 to P 12 , T 1 and T 2 being elements as defined in the description and the claims, have Gramegative antimicrobial activity to e.g. inhibit the growth or to kill microorganisms such as Klebsiella pneumoniae and/or Acinetobacter baumannii and/or Escherichia coli . They can be used as medicaments to treat or prevent infections or as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials. 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（I），环[P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P-P-P-P-P-P9-P10-P-P-P2-T1-T2] P1至P12，T1和T2是说明书和权利要求书中定义的元件，具有例如抗抑郁活性抑制生长或杀死肺炎克雷伯杆菌和/或鲍氏不动杆菌和/或大肠杆菌等微生物。它们可用作治疗或预防感染的药物，或用作食品，化妆品，药物或其他含营养材料的消毒剂。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。

3. 发明申请

WO2013182240A1 BETA-HAIRPIN PEPTIDOMIMETICS 审中-公开
公开(公告)号：WO2013182240A1
公开(公告)日：2013-12-12
申请号：PCT/EP2012/060766
申请日：2012-06-06
申请人： POLYPHOR AG , GOMBERT, Frank Otto , OBRECHT, Daniel , LEDERER, Alexander , ZIMMERMANN, Johann , OEFNER, Christian
发明人： GOMBERT, Frank Otto , OBRECHT, Daniel , LEDERER, Alexander , ZIMMERMANN, Johann , OEFNER, Christian
IPC分类号： C07K7/64
CPC分类号： A61K38/12 , A61K38/00 , C07K7/08 , C07K7/54
摘要： 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.
摘要翻译：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。

4. 发明申请

WO2012168336A1 BETA - HAIRPIN PEPTIDOMIMETICS AS CXC4 ANTAGONISTS 审中-公开
标题翻译：作为CXC4拮抗剂的BETA - HAIRPIN PEPTIDOMIMITICS
公开(公告)号：WO2012168336A1
公开(公告)日：2012-12-13
申请号：PCT/EP2012/060763
申请日：2012-06-06
申请人： POLYPHOR AG , OBRECHT, Daniel , GOMBERT, Frank, Otto , ZIMMERMANN, Johann
发明人： OBRECHT, Daniel , GOMBERT, Frank, Otto , ZIMMERMANN, Johann
IPC分类号： C07K7/64 , A61K38/04
CPC分类号： C07K7/08 , A61K38/00 , C07K1/047 , C07K7/64
摘要： 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.
摘要翻译： 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。

5. 发明申请

WO2011095218A1 TEMPLATE-FIXED PEP TIDOMIME TICS WITH CXCR7 MODULATING ACTIVITY 审中-公开
标题翻译：模板固定PEP TIDOMIME TICS与CXCR7调节活动
公开(公告)号：WO2011095218A1
公开(公告)日：2011-08-11
申请号：PCT/EP2010/051417
申请日：2010-02-05
申请人： POLYPHOR AG , GOMBERT, Frank Otto , LEDERER, Alexander , OBRECHT, Daniel , ROMAGNOLI, Barbara , LÖWE, Ralf , ZIMMERMANN, Johann
发明人： GOMBERT, Frank Otto , LEDERER, Alexander , OBRECHT, Daniel , ROMAGNOLI, Barbara , LÖWE, Ralf , ZIMMERMANN, Johann
IPC分类号： C07K7/64
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 mobilisation of stem cells.
摘要翻译：通式（I）的新型模板固定β-发夹肽模拟物，其中单个元件T或P是从连接的羰基（C = O）连接到下一个元素的氮（N）连接的α-氨基酸残基顺时针方向，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-发夹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，神经系统疾病，心血管疾病，呼吸系统疾病，胃肠道疾病或疾病泌尿系疾病，眼科疾病，口腔病，血液病和癌症; 或干细胞的动员。

6. 发明申请

WO2011014973A2 CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS 审中-公开
标题翻译：一致的约束，全合成大环化合物
公开(公告)号：WO2011014973A2
公开(公告)日：2011-02-10
申请号：PCT/CH2010/000191
申请日：2010-08-03
申请人： POLYPHOR AG , OBRECHT, Daniel , ERMERT, Philipp , OUMOUCH, Said , LACH, Franck , LUTHER, Anatol , MARX, Karsten , MÖHLE, Kerstin
发明人： OBRECHT, Daniel , ERMERT, Philipp , OUMOUCH, Said , LACH, Franck , LUTHER, Anatol , MARX, Karsten , MÖHLE, Kerstin
IPC分类号： C07D498/04 , C07D498/18 , C07F7/08 , A61K31/4745 , A61K31/695 , A61P1/06 , A61P25/24
CPC分类号： C07D498/04 , A61K31/407 , A61K31/437 , A61K31/4985 , C07D497/18 , C07D498/18
摘要： Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of formulae Ia and Ib are constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. These macrocycles Ia and Ib are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being the agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), ion channels and signal transduction pathways. In particular, these macrocycles act as antagonists of the motilin receptor, the FP receptor and the purinergic receptors P2Y 1 , as modulators of the serotonin receptor of subtype 5-HT 2B , as blockers of the voltage-gated potassium channel K v 1.3 and as inhibitors of the β-catenin-dependent "canonical" Wnt pathway. Thus they are showing great potential as medicaments for a variety of diseases.
摘要翻译：构型限制，式Ia和Ib的空间限定的12-30元大环环系由三个不同的分子部分构成：模板A，构象调节剂B和桥C.这些大环Ia和Ib容易通过平行合成或组合化学溶液或固相。它们被设计为与多种特异性生物靶标类型相互作用，其实例是对G蛋白偶联受体（GPCR），离子通道和信号转导通路的激动或拮抗活性。特别地，这些大环化合物作为拮抗剂作为拮抗剂，作为5-HT2B亚型的5-羟色胺受体的调节剂作为电压门控钾通道Kv1.3的阻断剂和作为抑制剂的拮抗剂，作为拮抗剂受体，FP受体和嘌呤能受体P2Y1 ß-连环蛋白依赖的“规范”Wnt通路。因此，它们作为各种疾病的药物具有巨大的潜力。

7. 发明申请

WO2010060479A1 TEMPLATE-FIXED BETA-HAIRPIN PEPTIDOMIMETICS WITH CXCR4 ANTAGONIZING ACTIVITY 审中-公开
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：WO2010060479A1
公开(公告)日：2010-06-03
申请号：PCT/EP2008/066270
申请日：2008-11-26
申请人： POLYPHOR AG , GOMBERT, Frank, O. , OBRECHT, Daniel , LEDERER, Alexander , ROMAGNOLI, Barbara
发明人： GOMBERT, Frank, O. , OBRECHT, Daniel , LEDERER, Alexander , ROMAGNOLI, Barbara
IPC分类号： C07K7/08 , C07K7/64 , C07K1/04 , A61K38/04
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, GIy, 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：模板固定的拟肽式（Ia）式（Ib）其中Z是14个氨基和/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，及其盐具有CXCR4拮抗性质，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。

8. 发明申请

WO2022106063A2 COMPOSITIONS OF A BETA-HAIRPIN PEPTIDOMIMETIC AND AEROSOL DOSAGE FORMS THEREOF 审中-公开
公开(公告)号：WO2022106063A2
公开(公告)日：2022-05-27
申请号：PCT/EP2021/025457
申请日：2021-11-23
申请人： POLYPHOR AG
发明人： UPERT, Grégory , BENGHEZAL, Mohammed , LE POUPON, Karen , OBRECHT, Daniel
IPC分类号： A61K9/00 , A61K9/08 , A61K38/00 , A61P11/00 , A61K47/02 , A61K9/0078
摘要： The invention relates to pharmaceutical aerosols comprising the active compound cyclo(- Thr-Trp-lle-Dab-Orn-DDab-Dab-Trp-Dab-Dab-Ala-Ser-DPro-Pro), or any pharmaceutically acceptable salt thereof. It further relates to liquid compositions comprising the active compound cyclo(-Thr-Trp-lle-Dab-Orn-DDab-Dab-Trp-Dab-Dab-Ala-Ser-DPro-Pro), dilutions thereof, kits comprising the liquid compositions, pharmaceutical compositions and kits for preparing and administering such aerosols. The invention can be used for the prevention, management or treatment of diseases or conditions of the lungs such as cystic fibrosis (CF), non-cystic fibrosis bronchiectasis (NCFB), asthma, chronic obstructive pulmonary disease (COPD), ventilator-associated pneumonia (VAP), ventilator-associated bacterial pneumonia (VABP), hospital-acquired pneumonia (HAP), hospital-acquired bacterial pneumonia (HABP), or healthcare-associated pneumonia (HCAP).

9. 发明申请

WO2016150576A1 BETA-HAIRPIN PEPTIDOMIMETICS 审中-公开
公开(公告)号：WO2016150576A1
公开(公告)日：2016-09-29
申请号：PCT/EP2016/025027
申请日：2016-03-23
申请人： POLYPHOR AG
发明人： OBRECHT, Daniel , LUTHER, Anatol , BERNARDINI, Francesca , ZBINDEN, Peter , LEDERER, Alexander
IPC分类号： C07K7/08 , C07K7/60 , C07K7/64
CPC分类号： C07K7/64 , A61K38/00 , C07K7/08 , C07K7/62 , C07K2319/00
摘要： Beta-hairpin peptidomimetics of the general formula (I), and pharmaceutically acceptable salts thereof, with P, T, Q., and optionally L being elements as defined in the description and the claims, have Gram-negative antimicrobial activity to e.g. inhibit the growth or to kill microorganisms such as Klebsiella pneumoniae and/or Acinetobacter baumannii and/or Escherichia coli and/or Pseudomonas aeruginosa . They ca n be used as medicaments to treat or prevent infections or as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials. 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（I）的β-发夹肽模拟物及其药学上可接受的盐与P，T，Q和任选的L是说明书和权利要求书中定义的元素，其具有革兰氏阴性的抗微生物活性。抑制生长或杀死肺炎克雷伯菌和/或鲍氏不动杆菌和/或大肠杆菌和/或铜绿假单胞菌的微生物。它们可用作治疗或预防感染的药物，或用作食品，化妆品，药物或其他含营养物质的消毒剂。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。

10. 发明申请

WO2014161782A1 BETA-HAIRPIN PEPTIDOMIMETICS 审中-公开
公开(公告)号：WO2014161782A1
公开(公告)日：2014-10-09
申请号：PCT/EP2014/056285
申请日：2014-03-28
申请人： POLYPHOR AG
发明人： OBRECHT, Daniel , LUTHER, Anatol , BERNARDINI, Francesca , ZBINDEN, Peter
IPC分类号： C07K7/64 , A61K38/12
CPC分类号： C07K7/64 , A61K38/00 , Y02A50/473
摘要： Beta-hairpin peptidomimetics of the general formula (I), cyclo(P 1 -p 2 -p 3 -p 4 -p 5 -p 6 - p 7 p 8 p 9 -p 10 -p 11 -p 12 -T 1 -T 2 ], a nd pharmaceutically acceptable salts thereof, with P 1 to P 12 , T 1 and T 2 being elements as defined in the description and the claims, have broad spectrum Gram-negative antimicrobial activity to e.g. inhibit the growth or to kill microorganisms such as Klebsiella pneumoniae and/or Acinetobacter baumannii and/or Escherichia coli. They can be used as medicaments to treat or prevent infections or as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials. 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（I）的β-发夹肽模拟物，环（P1-p2-p3-p4-p5-p6-p7p8p9-p10-p11-p12-T1-T2）及其药学上可接受的盐与P1至P12 ，T1和T2是描述和权利要求中定义的元件，具有广谱革兰氏阴性抗微生物活性，例如抑制生长或杀死肺炎克雷伯杆菌和/或鲍氏不动杆菌和/或大肠杆菌等微生物，它们可以是用作治疗或预防感染的药物，或用作食品，化妆品，药物或其他含营养物质的消毒剂，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。

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