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公开(公告)号：US08633163B2
公开(公告)日：2014-01-21
申请号：US12524862
申请日：2007-01-29
申请人： Daniel Obrecht , Frank Gombert , Steve J. Demarco , Christian Ludin , Alexander Lederer , Christian Bisang , Odile Sellier-Kessler , Francoise Jung , Reshmi Mukherjee , Heiko Henze , Barbara Romagnoli
发明人： Daniel Obrecht , Frank Gombert , Steve J. Demarco , Christian Ludin , Alexander Lederer , Christian Bisang , Odile Sellier-Kessler , Francoise Jung , Reshmi Mukherjee , Heiko Henze , Barbara Romagnoli
IPC分类号： A61K38/00 , C07K14/72 , C07K14/705 , A61K38/04 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00
CPC分类号： C07K7/64 , A61K38/00 , C07K5/02 , C07K5/101 , C07K5/1013 , C07K5/1016 , C07K5/1021 , C07K5/1024 , C07K7/06 , C07K7/08
摘要： Template-fixed β-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 4 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, 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 agonize or to antagonize GPCR receptors such as CXCR3, urotensin and CCR10. They can be used as medicaments to treat or prevent diseases such as cardiovascular disorders, dermatological disorders, endocrine system and hormone disorders, metabolic diseases, inflammatory diseases, neurological diseases, respiratory 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）的模板固定的β-发夹肽模拟物，其中Z是4个α-氨基酸残基的模板固定链，其取决于其在链中的位置（从N-末端氨基酸开始计数）为 Gly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及其盐中定义，具有激动或拮抗GPCR受体如CXCR3，尿素调节素和CCR10的性质。 它们可以用作治疗或预防心血管疾病，皮肤病，内分泌系统和激素失调，代谢疾病，炎性疾病，神经疾病，呼吸系统疾病，血液病和癌症等疾病的药物。 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。
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公开(公告)号：US08865656B2
公开(公告)日：2014-10-21
申请号：US13319052
申请日：2009-05-07
摘要： β-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.
摘要翻译： 通式为（Xaa1-Xaa2-Xaa3-Cys4-Xaa5-Xaa6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-）的通式肽模拟物，Cys4之间的二硫键 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拮抗特性，可用于预防健康个体中的HIV感染，或用于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以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。
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公开(公告)号：US20100093644A1
公开(公告)日：2010-04-15
申请号：US12524862
申请日：2007-01-29
申请人： Daniel Obrecht , Frank Gombert , Steve J. Demarco , Christian Ludin , Alexander Lederer , Christian Bisang , Odile Sellier-Kessler , Francoise Jung , Reshmi Mukherjee , Heiko Henze , Barbara Romagnoli
发明人： Daniel Obrecht , Frank Gombert , Steve J. Demarco , Christian Ludin , Alexander Lederer , Christian Bisang , Odile Sellier-Kessler , Francoise Jung , Reshmi Mukherjee , Heiko Henze , Barbara Romagnoli
CPC分类号： C07K7/64 , A61K38/00 , C07K5/02 , C07K5/101 , C07K5/1013 , C07K5/1016 , C07K5/1021 , C07K5/1024 , C07K7/06 , C07K7/08
摘要： Template-fixed β-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 4 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid) are Gly, 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 agonize or to antagonize GPCR receptors such as CXCR3, urotensin and CCR10. They can be used as medicaments to treat or prevent diseases such as cardiovascular disorders, dermatological disorders, endocrine system and hormone disorders, metabolic diseases, inflammatory diseases, neurological diseases, respiratory 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）的模板固定和半乳糖肽模拟物，其中Z是4个α-氨基酸残基的模板固定链，其取决于其在链中的位置（从N-末端氨基酸开始计数） 是Gly，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盐中定义，具有激动或拮抗GPCR受体如CXCR3，尿素调节素和CCR10的性质。 它们可以用作治疗或预防心血管疾病，皮肤病，内分泌系统和激素失调，代谢疾病，炎性疾病，神经疾病，呼吸系统疾病，血液病和癌症等疾病的药物。 这些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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公开(公告)号：US20130023483A1
公开(公告)日：2013-01-24
申请号：US13577153
申请日：2010-02-05
申请人： Frank Otto Gombert , Alexander Lederer , Daniel Obrecht , Barbara Romagnoli , Christian Bisang , Christian Ludin
发明人： Frank Otto Gombert , Alexander Lederer , Daniel Obrecht , Barbara Romagnoli , Christian Bisang , Christian Ludin
IPC分类号： A61K38/12 , A61P17/00 , A61P3/00 , A61P29/00 , A61P31/00 , A61P25/00 , A61P9/00 , A61P11/00 , A61P1/00 , A61P27/02 , A61P31/18 , A61P3/10 , A61P19/02 , A61P35/00 , A61P35/02 , C07K7/00
摘要： Specific 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）的具体的模板固定和平滑肽模拟物，其中单个元件T或P是从下一个连接的羰基（C = O）连接点连接到氮（N）的α-氨基酸残基 元件，并且其中所述元件取决于它们在链中的位置在描述中定义，并且权利要求具有作用于受体CXCR7的性质。 因此，这些β-螺旋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，神经疾病，心血管疾病，呼吸系统疾病，胃肠疾病， 肠道疾病，泌尿科疾病，眼科疾病，口腔病，血液病和癌症; 或干细胞的动员。
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公开(公告)号：US08629112B2
公开(公告)日：2014-01-14
申请号：US13577153
申请日：2010-02-05
申请人： Frank Otto Gombert , Alexander Lederer , Daniel Obrecht , Barbara Romagnoli , Christian Bisang , Christian Ludin
发明人： Frank Otto Gombert , Alexander Lederer , Daniel Obrecht , Barbara Romagnoli , Christian Bisang , Christian Ludin
IPC分类号： A61K31/00
摘要： Specific 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 mobilization of stem cells.
摘要翻译： 通式（I）的具体的模板固定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描述中定义，并且权利要求具有作用于受体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。
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公开(公告)号：US08716242B2
公开(公告)日：2014-05-06
申请号：US13513550
申请日：2009-12-04
申请人： Sophie Barthélémy , Christian Bisang , Frank Otto Gombert , Alexander Lederer , Daniel Obrecht , Barbara Romagnoli , Jürg Zumbrunn , Tobias Remus , Guillaume Lemercier
发明人： Sophie Barthélémy , Christian Bisang , Frank Otto Gombert , Alexander Lederer , Daniel Obrecht , Barbara Romagnoli , Jürg Zumbrunn , Tobias Remus , Guillaume Lemercier
摘要： β-Hairpin peptidomimetics of the general formula Cyclo(-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-), and pharmaceutically acceptable salts thereof, with Xaa 1-Xaa 16 being amino acid residues of certain types which are defined in the description and the claims, have CXCR4 antagonizing properties and prolonged half-lives in vivo 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： （-Xaa1-Xaa2-Xaa3-Xaa4-Xaa8-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-）的通式肽模拟物及其药学上可接受的盐 其中Xaa 1-Xaa 16是在说明书和权利要求书中定义的某些类型的氨基酸残基，具有CXCR4拮抗特性和体内延长的半衰期，并且可用于预防健康个体的HIV感染或减缓 并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以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。
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公开(公告)号：US20120283196A1
公开(公告)日：2012-11-08
申请号：US13513550
申请日：2009-12-04
申请人： Sophie Barthélémy , Christian Bisang , Frank Otto Gombert , Alexander Lederer , Daniel Obrecht , Barbara Romagnoli , Jürg Zumbrunn , Tobias Remus , Guillaume Lemercier
发明人： Sophie Barthélémy , Christian Bisang , Frank Otto Gombert , Alexander Lederer , Daniel Obrecht , Barbara Romagnoli , Jürg Zumbrunn , Tobias Remus , Guillaume Lemercier
摘要： β-Hairpin peptidomimetics of the general formula Cyclo(-Xaa1-Xaa2-Xaa3-Xaa4-Xaa5-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-), and pharmaceutically acceptable salts thereof, with Xaa 1-Xaa 16 being amino acid residues of certain types which are defined in the description and the claims, have CXCR4 antagonizing properties and prolonged half-lives in vivo 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 eases 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： （-Xaa1-Xaa2-Xaa3-Xaa4-Xaa8-Xaa6-Xaa7-Xaa8-Xaa9-Xaa10-Xaa11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-）的通式肽模拟物及其药学上可接受的盐 其中Xaa 1-Xaa 16是在说明书和权利要求书中定义的某些类型的氨基酸残基，具有CXCR4拮抗特性和体内延长的半衰期，并且可用于预防健康个体的HIV感染或减缓 并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; 或在血浆分离术收集期间减少外周血干细胞和/或作为诱导干细胞调动以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。
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公开(公告)号：US20120135942A1
公开(公告)日：2012-05-31
申请号：US13319052
申请日：2009-05-07
IPC分类号： A61K38/12 , C07K7/54 , A61P35/00 , C07K1/06 , A61P31/18 , A61P37/00 , A61P37/04 , A61P7/00 , C07K7/64 , A61P29/00
摘要： β-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.
摘要翻译： 通式为（Xaa1-Xaa2-Xaa3-Cys4-Xaa5-Xaa6-Xaa7-Xaa8-Arg9-Tyr10-Cys11-Xaa12-Xaa13-Xaa14-Xaa15-Xaa16-）的通式肽模拟物，Cys4之间的二硫键 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拮抗特性，可用于预防健康个体中的HIV感染，或用于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以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。
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9.发明申请TEMPLATE-FIXED BETA-HAIRPIN PEPTIDOMIMETICS WITH CXCR4 ANTAGONIZING ACTIVITY 有权具有CXCR4拮抗活性的模板固定的BETA-HAIRPIN PEPTIDOMIMETICS公开(公告)号：US20110312879A1
公开(公告)日：2011-12-22
申请号：US13131205
申请日：2008-11-26
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, Gly, 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： 模板固定肽模拟物式（Ia）式（Ib）其中Z是14个α-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，其盐具有CXCR4拮抗特性，并且可用于 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以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。
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10.发明授权Template-fixed beta-hairpin peptidomimetics with CXCR4 antagonizing activity 有权模板固定β-发夹肽模拟物与CXCR4拮抗活性公开(公告)号：US08883720B2
公开(公告)日：2014-11-11
申请号：US13131205
申请日：2008-11-26
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, Gly, 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： 模板固定肽模拟物式（Ia）式（Ib）其中Z是14个α-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，其盐具有CXCR4拮抗特性，并且可用于 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; 或其中介导或由CXCR4受体活性引起的癌症; 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以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。
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