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1. 发明申请

WO2013050346A1 TEMPLATE -FIXED PEPTIDOMIMETICS AS INHIBITORS OF FPR1 审中-公开
标题翻译：作为FPR1的抑制剂的模板化混合肽
公开(公告)号：WO2013050346A1
公开(公告)日：2013-04-11
申请号：PCT/EP2012/069412
申请日：2012-10-02
申请人： POLYPHOR AG
发明人： JUNG, Françoise , OBRECHT, Daniel , LÖWE, Ralf , ZIMMERMANN, Johann , LEMERCIER, Guillaume , CHEVALIER, Eric
IPC分类号： C07K7/64 , A61K38/04
CPC分类号： C07K7/08 , C07K7/64
摘要： Novel template-fixed β-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 -P 13 -P 14 -T 1 -T 2 ] wherein the single elements T or P are α-amino acid residues connected in either direction which, depending on their positions in the chain, are as defined in the description and the claims, and salts thereof, have the property of antagonizing the biological effect of the receptor FPR1. They can be used as medicaments to treat or prevent diseases or conditions in the areas of inflammatory diseases, allergic conditions,immunological disorders, neuroinflammation, neurological disorders, obstructive airway diseases, infectious diseases, ischemic reperfusion injuries and proliferative disorders such as e.g. cancer. 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）：环[P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-P13-P14-T1-T2]的新型模板固定β-发夹肽模拟物其中单个元件T或P是沿任一方向连接的α-氨基酸残基，根据其在链中的位置如说明书和权利要求及其盐中所定义，其具有拮抗生物效应的性质受体FPR1。它们可以用作治疗或预防炎性疾病，过敏性疾病，免疫学障碍，神经炎症，神经障碍，阻塞性气道疾病，传染病，缺血再灌注损伤和增殖性疾病如疾病或疾病的疾病或病症的药物。癌症。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。

2. 发明申请

WO2017207118A1 BETA-HAIRPIN PEPTIDOMIMETIC WITH ELASTASE INHIBITORY ACTIVITY AND AEROSOL DOSAGE FORMS THEREOF 审中-公开
标题翻译：具有弹性蛋白酶抑制活性和气溶胶剂型的β-HAIRPIN肽制剂
公开(公告)号：WO2017207118A1
公开(公告)日：2017-12-07
申请号：PCT/EP2017/025157
申请日：2017-05-31
申请人： POLYPHOR AG
发明人： BRUIJNZEEL, Piet , ZIMMERMANN, Johann , BARTH, Philip , CHEVALIER, Eric , LUDIN, Christian , KELLER, Manfred
IPC分类号： A61K8/64 , A61K38/12 , A61K9/00 , A61P11/00 , C07K7/64
摘要： The present invention relates to pharmaceutical aerosols comprising a β-hairpin peptidomimetic of formula cyclo(-OctG-Glu-Thr-Ala-Ser-lle-Pro-Pro-Gln-Lys-Tyr- D Pro-Pro-), or a pharmaceutically acceptable salt thereof, having inhibitory activity against human neutrophil elastase. It further relates to solid or liquid pharmaceutical compositions and kits for preparing and administering such aerosols. The invention can be used for the prevention, management or treatment of pulmonary diseases, such as alpha-1 antitrypsin deficiency (AATD), cystic fibrosis (CF), non-cystic fibrosis bronchiactasis (NCFB), or chronic obstructive pulmonary disease (COPD), or infections, or diseases, or conditions of the lungs, being mediated by or resulting from human neutrophil elastase activity. Thus, the invention further relates to a pharmaceutical composition or a pharmaceutical aerosol comprising the active compound cyclo(-OctG-Glu-Thr-Ala-Ser-lle-Pro-Pro-Gln-Lys-Tyr- D Pro-Pro-), or any pharmaceutically acceptable salt thereof, for use in a method for the prevention, management or treatment of diseases or conditions of the lungs being mediated by or resulting from human neutrophil elastase activity in a subject.
摘要翻译：本发明涉及药物气雾剂，其包含式环（-OctG-Glu-Thr-Ala-Ser-Ile-Pro-Pro-Gln-Lys-Tyr-）的β-发夹肽模拟物 Pro-Pro-）或其药学上可接受的盐，其对人嗜中性粒细胞弹性蛋白酶具有抑制活性。它还涉及用于制备和施用这种气雾剂的固体或液体药物组合物和试剂盒。本发明可用于预防，治疗或治疗肺部疾病，如α-1抗胰蛋白酶缺乏症（AATD），囊性纤维化（CF），非囊性纤维化支气管扩张症（NCFB）或慢性阻塞性肺病（COPD），或由人嗜中性粒细胞弹性蛋白酶活性介导或由其产生的感染，或肺的疾病或病症。因此，本发明进一步涉及包含活性化合物环（-OctG-Glu-Thr-Ala-Ser-Ile-Pro-Pro-Gln-Lys-Tyr-D-D）的药物组合物或药用气雾剂。 Pro-Pro-）或其任何药学上可接受的盐，用于预防，管理或治疗受试者中由人嗜中性粒细胞弹性蛋白酶活性介导或由其产生的肺疾病或病症的方法。

3. 发明申请

WO2011060937A1 TEMPLATE-FIXED PEPTIDOMIMETICS WITH CCR10 ANTAGONISTIC ACTIVTY 审中-公开
标题翻译：具有CCR10拮抗活性的模板固定化肽
公开(公告)号：WO2011060937A1
公开(公告)日：2011-05-26
申请号：PCT/EP2010/007016
申请日：2010-11-18
申请人： POLYPHOR AG , JUNG, Françoise , GOMBERT, Frank, Otto , OBRECHT, Daniel , BISANG, Christian , BARTHELEMY, Sophie , LEDERER, Alexander , CHEVALIER, Eric
发明人： JUNG, Françoise , GOMBERT, Frank, Otto , OBRECHT, Daniel , BISANG, Christian , BARTHELEMY, Sophie , LEDERER, Alexander , CHEVALIER, Eric
IPC分类号： C07K7/64 , C07K7/08 , A61K38/04
CPC分类号： A61K38/00 , C07K7/06 , C07K7/08 , C07K7/64
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 in either direction which, depending on their positions in the chain, are as defined in the description and the claims, and salts thereof, have the property to antagonize the receptor CCR10. They can be used as medicaments to treat or prevent diseases or conditions in the area of dermatological and cutaneous disorders, inflammation, allergic disorders, respiratory diseases, diseases of the gastro-intestinal tract, ophthalmic diseases, haematology and cancer. 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）的新型模板固定的β-发夹肽模拟物，其中单个元件T或P是沿任一方向连接的α-氨基酸残基，其取决于其在链中的位置如说明书中所定义，权利要求及其盐具有拮抗受体CCR10的性质。它们可用作治疗或预防皮肤病和皮肤病，炎症，过敏性疾病，呼吸系统疾病，胃肠道疾病，眼科疾病，血液学和癌症领域的疾病或病症的药物。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。

4. 发明申请

WO2011060832A1 TEMPLATE-FIXED PEPTIDOMIMETICS WITH CCR10 ANTAGONISTIC ACTIVITY 审中-公开
标题翻译：具有CCR10拮抗活性的模板固定肽
公开(公告)号：WO2011060832A1
公开(公告)日：2011-05-26
申请号：PCT/EP2009/065572
申请日：2009-11-20
申请人： POLYPHOR AG , JUNG, Françoise , GOMBERT, Frank Otto , OBRECHT, Daniel , BISANG, Christian , BARTHÉLÉMY, Sophie , LEDERER, Alexander , CHEVALIER, Eric
发明人： JUNG, Françoise , GOMBERT, Frank Otto , OBRECHT, Daniel , BISANG, Christian , BARTHÉLÉMY, Sophie , LEDERER, Alexander , CHEVALIER, Eric
IPC分类号： C07K7/64 , C07K7/08 , A61K38/04
CPC分类号： A61K38/00 , C07K7/06 , C07K7/08 , C07K7/64
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 in either direction which, depending on their positions in the chain are defined in the description and the claims, and salts thereof, have the property to antagonize the receptor CCR10. They can be used as medicaments to treat or prevent diseases or conditions in the area of dermatological and cutaneous disorders, inflammation, allergic disorders, respiratory diseases, diseases of the gastro-intestinal tract, ophthalmic diseases, haematological diseases and cancer. 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）的新型模板固定的β-发夹肽模拟物，其中单个元件T或P是沿任一方向连接的α-氨基酸残基，根据其在链中的位置在说明书和权利要求书中定义，及其盐具有拮抗受体CCR10的性质。它们可用作治疗或预防皮肤病和皮肤病，炎症，过敏性疾病，呼吸系统疾病，胃肠道疾病，眼科疾病，血液病和癌症等疾病或病症的药物。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。

5. 发明公开

EP2501715A1 TEMPLATE-FIXED PEPTIDOMIMETICS WITH CCR10 ANTAGONISTIC ACTIVTY 审中-公开
标题翻译：具有CCR10拮抗活性的模板固定的化学修饰
公开(公告)号：EP2501715A1
公开(公告)日：2012-09-26
申请号：EP10790345.2
申请日：2010-11-18
申请人： Polyphor Ag
发明人： JUNG, Françoise , GOMBERT, Frank, Otto , OBRECHT, Daniel , BISANG, Christian , BARTHELEMY, Sophie , LEDERER, Alexander , CHEVALIER, Eric
IPC分类号： C07K7/64 , C07K7/08 , A61K38/04
CPC分类号： C07K7/64
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 in either direction which, depending on their positions in the chain, are as defined in the description and the claims, and salts thereof, have the property to antagonize the receptor CCR10. They can be used as medicaments to treat or prevent diseases or conditions in the area of dermatological and cutaneous disorders, inflammation, allergic disorders, respiratory diseases, diseases of the gastro-intestinal tract, ophthalmic diseases, haematology and cancer. 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）的新型模板固定的β-发夹肽模拟物，其中单个元件T或P是在任一方向连接的α-氨基酸残基，取决于它们在链中的位置，如说明书中所定义的，并且权利要求及其盐，具有拮抗受体CCR10的性质。它们可以用作治疗或预防皮肤病和皮肤疾病，炎症，变应性疾病，呼吸系统疾病，胃肠道疾病，眼科疾病，血液病和癌症领域的疾病或病症的药物。这些β-发夹肽模拟物可以通过基于混合固相和液相合成策略的方法制造。

6. 发明公开

EP3463281A1 BETA-HAIRPIN PEPTIDOMIMETIC WITH ELASTASE INHIBITORY ACTIVITY AND AEROSOL DOSAGE FORMS THEREOF 有权转让
公开(公告)号：EP3463281A1
公开(公告)日：2019-04-10
申请号：EP17733738.3
申请日：2017-05-31
申请人： Polyphor AG
发明人： BRUIJNZEEL, Piet , ZIMMERMANN, Johann , BARTH, Philip , CHEVALIER, Eric , LUDIN, Christian , KELLER, Manfred
IPC分类号： A61K8/64 , A61K38/12 , A61K9/00 , A61P11/00 , C07K7/64

7. 发明授权

EP2764010B9 TEMPLATE-FIXED PEPTIDOMIMETICS AS INHIBITORS OF FPR1 有权转让
标题翻译：模板 - 固定剂PEPTIDOMIMETIKA ALS INHIBITOREN VON FPR1
公开(公告)号：EP2764010B9
公开(公告)日：2017-01-18
申请号：EP12768803.4
申请日：2012-10-02
申请人： Polyphor AG
发明人： JUNG, Françoise , OBRECHT, Daniel , LÖWE, Ralf , ZIMMERMANN, Johann , LEMERCIER, Guillaume , CHEVALIER, Eric
IPC分类号： C07K7/64 , A61K38/04
CPC分类号： C07K7/08 , C07K7/64
摘要： Novel template-fixed &bgr;-hairpin peptidomimetics of the general formula (I): cyclo[P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-P13-P14-T1-T2] wherein the single elements T or P are α-amino acid residues connected in either direction which, depending on their positions in the chain, are as defined in the description and the claims, and salts thereof, have the property of antagonizing the biological effect of the receptor FPR1. They can be used as medicaments to treat or prevent diseases or conditions in the areas of inflammatory diseases, allergic conditions, immunological disorders, neuroinflammation, neurological disorders, obstructive airway diseases, infectious diseases, ischemic reperfusion injuries and proliferative disorders such as e.g. cancer. These &bgr;-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）：环[P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-P13-P14-T1-T2]的新型模板固定和模板肽模拟物 ]其中单元素T或P是沿任一方向连接的α-氨基酸残基，其取决于其在链中的位置如说明书和权利要求及其盐所定义，具有拮抗生物效应的性质的受体FPR1。它们可以用作治疗或预防炎性疾病，过敏性疾病，免疫学障碍，神经炎症，神经障碍，阻塞性气道疾病，传染病，缺血再灌注损伤和增殖性疾病如疾病或疾病的疾病或病症的药物。癌症。这些固体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。

8. 发明授权

EP2764010B1 TEMPLATE-FIXED PEPTIDOMIMETICS AS INHIBITORS OF FPR1 有权转让
标题翻译：模板固定的肽AS FPR 1抑制剂
公开(公告)号：EP2764010B1
公开(公告)日：2016-03-16
申请号：EP12768803.4
申请日：2012-10-02
申请人： Polyphor Ag
发明人： JUNG, Françoise , OBRECHT, Daniel , LÖWE, Ralf , ZIMMERMANN, Johann , LEMERCIER, Guillaume , CHEVALIER, Eric
IPC分类号： C07K7/64 , A61K38/04
CPC分类号： C07K7/08 , C07K7/64
摘要： Novel template-fixed &bgr;-hairpin peptidomimetics of the general formula (I): cyclo[P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-P13-P14-T1-T2] wherein the single elements T or P are α-amino acid residues connected in either direction which, depending on their positions in the chain, are as defined in the description and the claims, and salts thereof, have the property of antagonizing the biological effect of the receptor FPR1. They can be used as medicaments to treat or prevent diseases or conditions in the areas of inflammatory diseases, allergic conditions, immunological disorders, neuroinflammation, neurological disorders, obstructive airway diseases, infectious diseases, ischemic reperfusion injuries and proliferative disorders such as e.g. cancer. These &bgr;-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

9. 发明公开

EP2764010A1 TEMPLATE -FIXED PEPTIDOMIMETICS AS INHIBITORS OF FPR1 有权转让
标题翻译：模板固定的肽AS FPR 1抑制剂
公开(公告)号：EP2764010A1
公开(公告)日：2014-08-13
申请号：EP12768803.4
申请日：2012-10-02
申请人： Polyphor Ag
发明人： JUNG, Françoise , OBRECHT, Daniel , LÖWE, Ralf , ZIMMERMANN, Johann , LEMERCIER, Guillaume , CHEVALIER, Eric
IPC分类号： C07K7/64 , A61K38/04
CPC分类号： C07K7/08 , C07K7/64
摘要： Novel template-fixed &bgr;-hairpin peptidomimetics of the general formula (I): cyclo[P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-P13-P14-T1-T2] wherein the single elements T or P are α-amino acid residues connected in either direction which, depending on their positions in the chain, are as defined in the description and the claims, and salts thereof, have the property of antagonizing the biological effect of the receptor FPR1. They can be used as medicaments to treat or prevent diseases or conditions in the areas of inflammatory diseases, allergic conditions, immunological disorders, neuroinflammation, neurological disorders, obstructive airway diseases, infectious diseases, ischemic reperfusion injuries and proliferative disorders such as e.g. cancer. These &bgr;-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

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