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51. 发明授权

EP2882771B1 COMBINATIONS WITH A BACKBONE-CYCLIZED PEPTIDE 有权
标题翻译：与骨架 - 循环肽的组合
公开(公告)号：EP2882771B1
公开(公告)日：2017-06-14
申请号：EP13745848.5
申请日：2013-08-07
申请人： Polyphor AG
发明人： DALE, Glenn E. , OBRECHT, Daniel , BERNARDINI, Francesca
IPC分类号： C07K7/64 , A61K38/12
CPC分类号： A61K38/12 , A61K31/405 , A61K31/407 , A61K31/496 , A61K31/7036 , A61K31/7052 , A61K38/00 , A61K45/06 , A61K47/6809 , C07K5/12 , C07K7/64 , A61K2300/00

52. 发明授权

EP2882770B1 COMBINATIONS WITH A BACKBONE-CYCLIZED PEPTIDE 有权
标题翻译：与骨架 - 循环肽的组合
公开(公告)号：EP2882770B1
公开(公告)日：2017-05-31
申请号：EP13745432.8
申请日：2013-08-07
申请人： Polyphor AG
发明人： DALE, Glenn E. , OBRECHT, Daniel , BERNARDINI, Francesca
IPC分类号： C07K7/64 , A61K38/12
CPC分类号： A61K38/12 , A61K31/65 , A61K38/10 , A61K47/6809 , A61L2300/406 , C07K7/08 , C07K7/50 , C07K7/64 , A61K2300/00

53. 发明授权

EP2499148B1 CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS 有权转让
标题翻译：构象VOLLSYNTHETSCHE大环化合物
公开(公告)号：EP2499148B1
公开(公告)日：2017-01-18
申请号：EP10743003.5
申请日：2010-08-03
申请人： Polyphor AG
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： C07D497/18 , C07D498/04 , C07D498/18

54. 发明公开

EP2718307A1 BETA - HAIRPIN PEPTIDOMIMETICS AS CXC4 ANTAGONISTS 有权
标题翻译：与CRCX4拮抗作用BETA发夹肽
公开(公告)号：EP2718307A1
公开(公告)日：2014-04-16
申请号：EP12725829.1
申请日：2012-06-06
申请人： Polyphor AG
发明人： OBRECHT, Daniel , GOMBERT, Frank, Otto , ZIMMERMANN, Johann
IPC分类号： C07K7/64 , A61K38/04
CPC分类号： A61K38/00 , 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.

55. 发明公开

EP2531520A1 TEMPLATE-FIXED PEPTIDOMIMETICS WITH CXCR7 MODULATING ACTIVITY 失效
标题翻译：与CXCR7调节作用MATRIZENFIXIERTE肽
公开(公告)号：EP2531520A1
公开(公告)日：2012-12-12
申请号：EP11702229.3
申请日：2011-02-04
申请人： Polyphor AG
发明人： GOMBERT, Frank, Otto , LEDERER, Alexander , LÖWE, Ralf , OBRECHT, Daniel , ROMAGNOLI, Barbara , ZIMMERMANN, Johann , PATEL, Kalpana
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.

56. 发明公开

EP2462147A1 CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS 有权转让
标题翻译：构象VOLLSYNTHETSCHE大环化合物
公开(公告)号：EP2462147A1
公开(公告)日：2012-06-13
申请号：EP09781527.8
申请日：2009-08-05
申请人： Polyphor Ag
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 type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT2B (5-HT2B receptor), and on the prostaglandin F2•receptor (FP receptor). They are thus potentially useful for the treatment of hypomotility disorders of the gastrointestinal tract such as diabetic gastroparesis and constipation type irritable bowl syndrome; of CNS related diseases like migraine, schizophrenia, psychosis or depression; of ocular hypertension such as associated with glaucoma and preterm labour.

57. 发明公开

EP2324047A2 TEMPLATE-FIXED PEPTIDOMIMETICS 有权
标题翻译：在支架固定肽
公开(公告)号：EP2324047A2
公开(公告)日：2011-05-25
申请号：EP08787073.9
申请日：2008-08-08
申请人： Polyphor Ag , Universität Zürich
发明人： ROBINSON, John Anthony , MÖHLE, Kerstin , SEITZ, Markus , MAILLARD, Ludovic T. , MOUNME, Roba , GOMBERT, Frank Otto , SELLIER-KESSLER, Odile , HENZE, Heiko , OBRECHT, Daniel , BISANG, Christian , LEDERER, Alexander
IPC分类号： C07K7/56 , C07K7/64 , C07K1/02
CPC分类号： C07K1/02 , C07K7/56 , C07K7/64
摘要： Template-fixed &bgr;-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 8 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 agonizing or antagonizing activity against urotensin II or show inhibition of the STAT6/NCoA-1 interaction and can be used for preventing or treating diseases or disorders related to urotensin II, STAT6 and NCoA-1. These &bgr;-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

58. 发明授权

EP2978771B1 BETA-HAIRPIN PEPTIDOMIMETICS 有权
公开(公告)号：EP2978771B1
公开(公告)日：2019-07-24
申请号：EP14714670.8
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： C07K7/08 , C07K7/64

59. 发明公开

EP3201219A1 BETA-HAIRPIN PEPTIDOMIMETICS 有权
标题翻译： BETA-HAIRPIN多肽
公开(公告)号：EP3201219A1
公开(公告)日：2017-08-09
申请号：EP15778876.1
申请日：2015-09-29
申请人： Polyphor AG
发明人： OBRECHT, Daniel , LUTHER, Anatol , BERNARDINI, Francesca , ZBINDEN, Peter , BARTHELEMY, Sophie , 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[P1-P2-P3-P4-P5-P6-P7-P8-P9-P10-P11-P12-T1-T2] and pharmaceutically acceptable salts thereof, with P1 to P12, T1 and T2 being elements as defined in the description and the claims, have Gramnegative 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-P7-P8-P9-P10-P11-P12-T1-T2]及其药学上可接受的盐与P1 到P12，T1和T2是说明书和权利要求书中定义的元素，对例如具有革兰氏阴性抗微生物活性抑制生长或杀死微生物如肺炎克雷伯氏菌和/或鲍曼不动杆菌和/或大肠杆菌。它们可以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液相合成策略的方法制造。

60. 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。

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