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11. 发明申请

US20050065090A1 Dermopharmaceutically and cosmetically active oligopeptides 有权
标题翻译：药物和化妆品活性寡肽
公开(公告)号：US20050065090A1
公开(公告)日：2005-03-24
申请号：US10493856
申请日：2002-10-30
申请人： Christian Ludin , Marc Heidl , Hugo Ziegler
发明人： Christian Ludin , Marc Heidl , Hugo Ziegler
IPC分类号： A61K38/00 , A61P17/00 , C07K5/068 , C07K14/78 , A61K38/08 , C07K7/06
CPC分类号： C07K14/78 , A61K38/00 , C07K5/06086
摘要： Oligopeptides and derivatives thereof, peptide analogs and derivatives thereof as well as pharmaceutically acceptable salts of these compounds, which correspond to general formula (I) wherein R1 represents H, —C(O)—R7, —SO2—R7, —C(O)—OR7 or —C(O)—N(R7)2 R2 represents, independent of one another, H or —(C1-C4)-alkyl, R3 and R6 represent, independent of one another, —(CH2)q—N(R1)R8 R4 and R5 represent, independent of one another, —CH2—OR2, —CH(CH3)OR8 or —CH2—CH2—OR8 R7 represents hydrogen, optionally substituted (C1-C19)-alkyl; optionally substituted (C1-C19)-alkenyl; phenyl-(C1-C4)-alkyl whose phenyl radical is optionally substituted with amino in the para position R8 represents H, —(C1-C4)-alkyl, —C(O)—R7, —C(O)—OR7, —C(O)—N(R7)2 or —SO2—R7 X represents oxygen (—O—) or —NH—; or XR7, with X=O, also represents the esters of α-tocopherol, tocotrienol or retinol or the carboxylic acid (with R7=H) m, n, p represent, independent of one another, zero or 1 and q in R3 and R6 represent, independent of one another, an integer from 1 to 4, with the provision that the following conditions do not simultaneously occur: R4=—CH(CH3)—OH and R5=—CH(CH3)—OH and R6=—(CH2)4—NH2; dermopharmaceutically and/or cosmetically active compositions containing at least one compound of formula (I).
摘要翻译：对应于通式（I）的寡肽及其衍生物，肽类似物及其衍生物以及这些化合物的药学上可接受的盐，其中R 1表示H，-C（O）-R 7，-SO 2 - R 7，-C（O）-OR 7或-C（O）-N（R 7）2 R 2彼此独立地表示H或 - （C 1 -C 4） - 烷基，R 3和R 6彼此独立地表示 - （CH 2）q N（R 1）R 8 R 4和R 5彼此独立地表示 - CH2-OR2，-CH（CH3）OR8或-CH2-CH2-OR8表示氢，任选取代的（C 1 -C 19） - 烷基; 任选取代的（C 1 -C 19） - 烯基; 苯基 - （C 1 -C 4） - 烷基，其苯基任选被对位R 8中的氨基取代，代表H， - （C 1 -C 4） - 烷基，-C（O）-R 7，-C （O）-OR 7，-C（O）-N（R 7）2或-SO 2 -R 7表示氧（-O-）或-NH-; 或XR 7，X = O也表示α-生育酚，生育三烯酚或视黄醇或羧酸（R 7 = H）m，n，p彼此独立地为0或 1和q在R 3和R 6中彼此独立地表示1至4的整数，条件是不同时发生以下条件：R 4 = -CH（CH 3） - OH和R 5 = -CH（CH 3）-OH，R 6 = - （CH 2）4 -NH 2; 含有至少一种药物的药物和/或化妆品活性组合物

12. 发明授权

US08658604B2 Template-fixed beta-hairpin peptidomimetics with protease inhibitory activity 有权
标题翻译：具有蛋白酶抑制活性的模板固定β-发夹肽模拟物
公开(公告)号：US08658604B2
公开(公告)日：2014-02-25
申请号：US11816589
申请日：2005-02-17
申请人： Steven J. DeMarco , Kerstin Moehle , Heiko Henze , Odile Sellier , Françoise Jung , Frank Gombert , Daniel Obrecht , Christian Ludin
发明人： Steven J. DeMarco , Kerstin Moehle , Heiko Henze , Odile Sellier , Françoise Jung , Frank Gombert , Daniel Obrecht , Christian Ludin
IPC分类号： A61K38/10 , A61K38/12
CPC分类号： C07K7/06 , A61K38/00 , C07K1/061 , C07K7/08 , C07K7/64
摘要： Template-fixed β-hairpin peptidomimetics of the general formulae wherein Z is a chain of 11 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 Pro(4NHCOPhe), 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 inhibit proteases, in particular serine proteases, especially Cathepsin G or Elastase or Tryptase. These β-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.
摘要翻译：具有通式的模板固定的β-发夹肽模拟物，其中Z是11个α-氨基酸残基的链，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Pro，或 Pro（4NHCOPhe）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，具有抑制蛋白酶，特别是丝氨酸蛋白酶，特别是组织蛋白酶G或弹性蛋白酶或Tryptase。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。

13. 发明授权

US08633163B2 Template-fixed peptidomimetics 有权
标题翻译：模板固定肽模拟物
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。

14. 发明申请

US20130023483A1 TEMPLATE-FIXED PEPTIDOMIMETICS WITH CXCR7 MODULATING ACTIVITY 有权
标题翻译：具有CXCR7调节活性的模板固定化肽
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
CPC分类号： C07K7/64 , A61K38/00
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。

15. 发明授权

US06495336B1 Oligopeptide derivatives for the electrochemical measurement of protease activity 有权
标题翻译：寡肽衍生物用于电化学测量蛋白酶活性
公开(公告)号：US06495336B1
公开(公告)日：2002-12-17
申请号：US09914259
申请日：2001-11-21
申请人： Christian Ludin , Peter Wikstroem , Lars G. Svendsen , Andreas Schulze
发明人： Christian Ludin , Peter Wikstroem , Lars G. Svendsen , Andreas Schulze
IPC分类号： C07K5083
CPC分类号： C07K5/0812 , C07K5/0806 , C07K5/1016 , C12Q1/37 , G01N33/86 , G01N2333/96463
摘要： The invention relates to oligopeptide derivatives whose C-terminal amino acid is arginine which is linked to the remainder of an electroactive aniline or aminoquinoline derivative by an amide bond. The oligopeptide derivatives are split by enzymes of the class of peptide hydrolases, especially proteinases and their inhibitors, of the coagulation system, the fibrinolytic system and the complement system. These oligopeptide derivatives serve as substrates for quantitatively determining such enzymes, especially thrombin, in complex sample liquids, especially capillary blood. This determination is carried out by measuring the increase in the water-soluble amperogenic aniline or aminoquinoline compound. The oligopeptide derivatives and their salts can be produced according to usual methods in peptide chemistry.
摘要翻译：本发明涉及其C-末端氨基酸是通过酰胺键与电活性苯胺或氨基喹啉衍生物的其余部分连接的精氨酸的寡肽衍生物。寡肽衍生物被肽水解酶类，特别是蛋白酶及其抑制剂，凝血系统，纤维蛋白溶解系统和补体系统的酶分裂。这些寡肽衍生物用作定量测定复杂样品液体，特别是毛细管血液中的这些酶，特别是凝血酶的底物。该测定是通过测量水溶性高产苯胺或氨基喹啉化合物的增加来进行的。寡肽衍生物及其盐可以根据肽化学中的常规方法制备。

16. 发明授权

US08895695B2 Template-fixed beta-hairpin peptidomimetics with CXCR4 antagonizing activity 有权
标题翻译：模板固定β-发夹肽模拟物与CXCR4拮抗活性
公开(公告)号：US08895695B2
公开(公告)日：2014-11-25
申请号：US12828998
申请日：2010-07-01
申请人： Jürg Zumbrunn , Steven J. Demarco , Sergio Lociuro , Jan Wim Vrijbloed , Frank Gombert , Reshmi Mukherjee , Kerstin Moehle , Daniel Obrecht , John Anthony Robinson , Heiko Henze , Barbara Romagnoli , Christian Ludin
发明人： Jürg Zumbrunn , Steven J. Demarco , Sergio Lociuro , Jan Wim Vrijbloed , Frank Gombert , Reshmi Mukherjee , Kerstin Moehle , Daniel Obrecht , John Anthony Robinson , Heiko Henze , Barbara Romagnoli , Christian Ludin
IPC分类号： C07K7/08 , C07K7/50
CPC分类号： C07K7/64 , A61K38/00 , C07K1/047 , C07K7/08
摘要： Template-fixed β-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12, 14 or 18 α-amino acid residues which, depending on their positions in the chain (counted starting from the N-terminal amino acid), are Gly, NMeGly, Pro or Pip, 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 CXCR4 antagonizing properties. 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12,14或18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）是Gly，NMeGly，Pro或Pip，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CXCR4拮抗性质。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。

17. 发明授权

US08796183B2 Template fixed beta-hairpin loop mimetics and their use in phage display 有权
标题翻译：模板固定β-发夹环模拟物及其在噬菌体展示中的应用
公开(公告)号：US08796183B2
公开(公告)日：2014-08-05
申请号：US13196712
申请日：2011-08-02
申请人： Jan Wim Vrijbloed , Daniel Obrecht , Sergio Locurio , Frank Otto Gombert , Christian Ludin , Françoise Jung
发明人： Jan Wim Vrijbloed , Daniel Obrecht , Sergio Locurio , Frank Otto Gombert , Christian Ludin , Françoise Jung
IPC分类号： C40B30/04 , C07K5/00
CPC分类号： C07K1/047 , C12N15/1037 , C40B40/02
摘要： A method of screening for template-fixed β-hairpin mimetics and libraries including a plurality of these mimetics is provided. The template-fixed β-hairpin mimetics are of the following general formula: R1-Cys-Z-Cys-R2 I wherein the two cysteine residues are bridged by a disulfide bond, thereby forming a cyclic peptide; R1 and R2 are di- or tripeptide moieties of certain types, as defined herein; and Z is a chain of n amino acid residues with n being an integer from 4 to 20 and with each of these n amino acid residues being, independently, derived from any naturally occurring L-α-amino acid.
摘要翻译：提供了一种筛选模板固定和模板模拟物的方法和包括多种这些模拟物的文库。模板固定和双螺旋模拟物具有以下通式：R1-Cys-Z-Cys-R2I，其中两个半胱氨酸残基通过二硫键桥接，从而形成环肽; R1和R2是如本文所定义的某些类型的二肽或三肽部分; 并且Z是n个氨基酸残基的链，n是4至20的整数，并且这些n个氨基酸残基中的每一个独立地衍生自任何天然存在的L-α-氨基酸。

18. 发明申请

US20130150299A1 TEMPLATE-FIXED PEPTIDOMIMETICS 审中-公开
标题翻译：模板固定蛋白质
公开(公告)号：US20130150299A1
公开(公告)日：2013-06-13
申请号：US13764099
申请日：2013-02-11
申请人： Daniel OBRECHT , Frank Gombert , Steven J. Demarco , Christian Ludin , Jan Wim Vrijbloed , Kerstin Moehle , John-Anthony Robinson , Reshmi Mukherjee , Heiko Henze , Barbara Romagnoli
发明人： Daniel OBRECHT , Frank Gombert , Steven J. Demarco , Christian Ludin , Jan Wim Vrijbloed , Kerstin Moehle , John-Anthony Robinson , Reshmi Mukherjee , Heiko Henze , Barbara Romagnoli
IPC分类号： A61K38/12
CPC分类号： C07K7/56 , A61K38/00 , A61K38/12 , C07K7/64
摘要： The template-fixed β-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro), disulfide bond between Cys4 and Gys11, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, 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 immuno suppression; or, in particular, for stem cell mobilisation of peripheral blood stem cells and/or mesenchymal stem cell (MSC) and/or other stem cells which retention depend on the CXCR4-receptor. These β-hairpin peptidomimetics can be manufactured by a process which is based on a mixed solid- and Solution phase synthetic strategy, using methods which are well known to those adequately skilled in peptide chemistry.
摘要翻译：模板固定的β-发夹肽模拟物Cyclo（-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro），Cys4和Gys11之间的二硫键和其药学上可接受的盐，其中X为Ala或Tyr，具有CXCR4拮抗性质，可用于预防健康个体的HIV感染或减缓和停止感染患者的病毒进展; 或其中癌症介导或由CXCR4受体活性产生; 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; 或特别是用于干细胞移动外周血干细胞和/或间充质干细胞（MSC）和/或其它干细胞，其保留取决于CXCR4-受体。这些β-发夹肽模拟物可以通过使用基于混合固相和溶液相合成策略的方法来制备，该方法使用肽化学中相当熟练技术人员众所周知的方法。

19. 发明授权

US08399611B2 Template-fixed peptidomimetics 有权
标题翻译：模板固定肽模拟物
公开(公告)号：US08399611B2
公开(公告)日：2013-03-19
申请号：US12528926
申请日：2007-02-28
申请人： Daniel Obrecht , Frank Gombert , Steven J. Demarco , Christian Ludin , Jan Wim Vrijbloed , Kerstin Moehle , John-Anthony Robinson , Reshmi Mukherjee , Heiko Henze , Barbara Romagnoli
发明人： Daniel Obrecht , Frank Gombert , Steven J. Demarco , Christian Ludin , Jan Wim Vrijbloed , Kerstin Moehle , John-Anthony Robinson , Reshmi Mukherjee , Heiko Henze , Barbara Romagnoli
IPC分类号： A61K38/12 , A61K38/10 , A61K38/04
CPC分类号： C07K7/56 , A61K38/00 , A61K38/12 , C07K7/64
摘要： The template-fixed β-hairpin peptidomimetics Cyclo(-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with X being Ala or Tyr, 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 immuno suppression; or for treating inflammation, or, in particular, for stem cell mobilization of peripheral blood stem cells and/or mesenchymal stem cell (MSC) and/or other stem cells which retention depend on the CXCR4-receptor.
摘要翻译：模板固定和固定肽模拟物Cyclo（-Tyr-His-X-Cys-Ser-Ala-DPro-Dab-Arg-Tyr-Cys-Tyr-Gln-Lys-DPro-Pro），Cys4和 Cys11及其药学上可接受的盐，X为Ala或Tyr，具有CXCR4拮抗性质，可用于预防健康个体的HIV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; 或用于治疗炎症，或特别是用于干细胞移动外周血干细胞和/或间充质干细胞（MSC）和/或其它干细胞，其保留取决于CXCR4受体。

20. 发明申请

US20100093644A1 TEMPLATE-FIXED PEPTIDOMIMETICS 有权
标题翻译：模板固定蛋白质
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
IPC分类号： A61K38/07 , C07K5/10
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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