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1. 发明公开

EP4000613A1 PHARMACEUTICAL COMBINATIONS COMPRISING A PEPTIDE CXCR4 INHIBITOR AND A TAXANE FOR TREATING CANCER 审中-公开
公开(公告)号：EP4000613A1
公开(公告)日：2022-05-25
申请号：EP20020545.8
申请日：2020-11-19
申请人： Polyphor AG
发明人： Zimmermann, Johann
IPC分类号： A61K31/337 , A61K38/12 , A61K45/06 , A61P35/00 , C07K7/00
摘要： The present invention relates to pharmaceutical combinations comprising a peptidic CXCR4 inhibitor and a taxane for use in a method for the prevention, delay of progression or treatment of cancer.

2. 发明公开

EP3707153A1 BETA-HAIRPIN PEPTIDOMIMETICS 无效
公开(公告)号：EP3707153A1
公开(公告)日：2020-09-16
申请号：EP18807558.4
申请日：2018-11-12
申请人： Polyphor AG
发明人： OBRECHT, Daniel , LUTHER, Anatol , BERNARDINI, Francesca , DALE, Glenn, E. , DESJONQUERES, Nicolas , BRABET, Emile , UPERT, Grégory
IPC分类号： C07K7/64 , A61K38/00

3. 发明授权

EP2836485B1 CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS 有权
标题翻译：构象受限的完全合成的大环化合物
公开(公告)号：EP2836485B1
公开(公告)日：2018-01-10
申请号：EP13709234.2
申请日：2013-03-15
申请人： Polyphor AG
发明人： OBRECHT, Daniel , ERMERT, Philipp , OUMOUCH, Said , PIETTRE, Arnaud , GOSALBES, Jean-François , THOMMEN, Marc
IPC分类号： C07D273/02 , C07D498/04 , C07D498/18 , C07D515/06 , C07D515/18 , C07D515/22 , C07D291/08 , A61K31/395 , A61P31/04
CPC分类号： C07D273/02 , C07D291/08 , C07D498/04 , C07D498/08 , C07D498/18 , C07D515/06 , C07D515/08 , C07D515/18 , C07D515/22
摘要： The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I 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 agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.

4. 发明授权

EP2540735B1 Template-fixed beta-hairpin peptidomimetics with CXCR4 antagonizing activity 失效
标题翻译：具有CXCR4拮抗活性的模板固定的β-发夹肽模拟物
公开(公告)号：EP2540735B1
公开(公告)日：2015-07-22
申请号：EP12185905.2
申请日：2004-04-29
申请人： Polyphor AG , Universität Zürich
发明人： Zumbrunn, Jürg , Demarco, Steve J. , Mukherjee, Reshmi , Möhle, Kerstin , Robinson, John, Anthony , Henze, Heiko , Romagnoli, Barbara , Lociuro, Sergio , Vrijbloed, Jan, Wim , Gombert, Frank , Obrecht, Daniel , Ludin, Christian
IPC分类号： C07K7/64 , C07K1/04 , A61K38/12
CPC分类号： C07K7/64 , A61K38/00 , C07K1/047 , C07K7/08

5. 发明公开

EP2836485A1 CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS 有权
标题翻译： KONFORMATIONSEINGESCHRÄNKTEVOLLSYNTHETISCHE MAKROCYCLISCHE VERBINDUNGEN
公开(公告)号：EP2836485A1
公开(公告)日：2015-02-18
申请号：EP13709234.2
申请日：2013-03-15
申请人： Polyphor Ag
发明人： OBRECHT, Daniel , ERMERT, Philipp , OUMOUCH, Said , PIETTRE, Arnaud , GOSALBES, Jean-François , THOMMEN, Marc
IPC分类号： C07D273/02 , C07D498/04 , C07D498/18 , C07D515/06 , C07D515/18 , C07D515/22 , C07D291/08 , A61K31/395 , A61P31/04
CPC分类号： C07D273/02 , C07D291/08 , C07D498/04 , C07D498/08 , C07D498/18 , C07D515/06 , C07D515/08 , C07D515/18 , C07D515/22
摘要： The conformationally restricted, spatially defined macrocyclic ring system of formula (I) is constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. Macrocycles described by this ring system I 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 agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), inhibitory activity on enzymes or antimicrobial activity. In particular, these macrocycles show inhibitory activity on endothelin converting enzyme of subtype 1 (ECE-1) and/or the cysteine protease cathepsin S (CatS), and/or act as antagonists of the oxytocin (OT) receptor, thyrotropin-releasing hormone (TRH) receptor and/or leukotriene B4 (LTB4) receptor, and/or as agonists of the bombesin 3 (BB3) receptor, and/or show antimicrobial activity against at least one bacterial strain. Thus they are showing great potential as medicaments for a variety of diseases.
摘要翻译：式（I）的构象限制的空间定义的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.由该环系统描述的大环化合物易于通过平行合成或组合化学在溶液中制备或固相。它们被设计为与各种特定的生物靶标类型相互作用，其实例是对G蛋白偶联受体（GPCR）的激动或拮抗活性，对酶或抗微生物活性的抑制活性。特别地，这些大环化合物显示对亚型1（ECE-1）和/或半胱氨酸蛋白酶组织蛋白酶S（CatS）的内皮素转化酶的抑制活性，和/或作为催产素（OT）受体的拮抗剂，促甲状腺激素释放激素（TRH）受体和/或白三烯B4（LTB4）受体和/或作为铃蟾肽3（BB3）受体的激动剂，和/或显示针对至少一种细菌菌株的抗微生物活性。因此，它们作为各种疾病的药物具有巨大的潜力。

6. 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。

7. 发明授权

EP1622930B1 TEMPLATE-FIXED PEPTIDOMIMETICS AS MEDICAMENTS AGAINST HIV AND CANCER 有权
标题翻译： MATRIZENFIXIERTE肽药物抗艾滋病和癌症
公开(公告)号：EP1622930B1
公开(公告)日：2008-05-14
申请号：EP03816774.8
申请日：2003-05-02
申请人： Polyphor AG , Universität Zürich
发明人： ZUMBRUNN, Jürg , DEMARCO, J., Steven , LOCIURO, Sergio , VRIJBLOED, Jan, Wim , GOMBERT, Frank , MUKHERJEE, Reshmi , MOEHLE, Kerstin , OBRECHT, Daniel , ROBINSON, John, Anthony , ROMAGNOLI, Barbara
IPC分类号： C07K7/06 , C07K7/08 , C07K14/00
CPC分类号： C07K7/06 , C07K7/08 , C07K14/001
摘要： Template-fixed ß-hairpin peptidomimetics of the General Formula (I); wherein Z and Z are template-fixed chains of4 and 6 or 5 and 7 alpha-amino acid residues which, depending on their positions in the chain 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 the property to prevent or to reduce HIV infections or to inhibit the growth of cancer cells or to inhibit inflammation. They can be used as medicaments to treat or prevent HIV infections and/or cancer or inflammatory disorders. These beta-sheet peptidomimetics can be manufactured by a process which is based on a mixed solid- and solution phase synthetic strategy.

8. 发明授权

EP2427476B1 BETA-HAIRPIN PEPTIDOMIMETICS HAVING CXCR4 ANTAGONIZING ACTIVITY 有权
公开(公告)号：EP2427476B1
公开(公告)日：2018-08-08
申请号：EP09779424.2
申请日：2009-05-07
申请人： Polyphor AG
发明人： OBRECHT, Daniel , GOMBERT, Frank, Otto , LEDERER, Alexander , ROMAGNOLI, Barbara , BISANG, Christian
IPC分类号： C07K7/64 , A61P29/00 , A61P31/18 , A61P35/00
CPC分类号： C07K7/08 , C07K1/061 , C07K7/02
摘要： &bgr;-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.

9. 发明授权

EP2978772B1 BETA-HAIRPIN PEPTIDOMIMETICS 有权
公开(公告)号：EP2978772B1
公开(公告)日：2018-06-27
申请号：EP14713473.8
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： C07K7/64 , A61K38/12
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-p7p8p9-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 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.

10. 发明授权

EP2540736B1 Template-fixed beta-hairpin peptidomimetics with CXCR4 antagonizing activity 失效
标题翻译：模板固定的β-发夹肽与CRCX4拮抗活性
公开(公告)号：EP2540736B1
公开(公告)日：2015-11-18
申请号：EP12185927.6
申请日：2004-04-29
申请人： Polyphor AG , Universität Zürich
发明人： Zumbrunn, Jürg , Demarco, Steven, J. , Mukherjee, Reshimi , Möhle, Kerstin , Robinson, John, Anthony , Henze, Heiko , Romagnoli, Barbara , Lociuro, Sergio , Vrijbloed, Jan, Wim , Gombert, Frank , Obrecht, Daniel , Ludin, Christian
IPC分类号： C07K7/64 , C07K1/04 , A61K38/12
CPC分类号： C07K7/64 , A61K38/00 , C07K1/047 , C07K7/08

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