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21. 发明申请

US20140187472A1 TEMPLATE-FIXED PEPTIDOMIMETICS WITH ANTIMICROBIAL ACTIVITY 有权
公开(公告)号：US20140187472A1
公开(公告)日：2014-07-03
申请号：US14175193
申请日：2014-02-07
申请人： Steven J. DEMARCO , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyani Srinivas , Frank Gombert , Daniel Obrecht
发明人： Steven J. DEMARCO , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyani Srinivas , Frank Gombert , Daniel Obrecht
IPC分类号： C07K7/64 , A01N43/36 , C07K1/10
CPC分类号： C07K7/64 , A01N43/36 , A61K38/00 , C07K1/10 , C07K7/06 , C07K7/08 , C07K14/001
摘要： Template-fixed β-hairpin peptidomimetics of the general formula wherein Z is a template-fixed chain of 12 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 the property to selectively inhibit the growth of or to kill microorganisms such as Pseudomonas aeruginosa. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials, or as medicaments to treat or prevent infections.These β-hairpin peptidomimetics can be manufactured by processes which are based on a mixed solid- and solution phase synthetic strategy.

22. 发明申请

US20100240592A1 TEMPLATE-FIXED PEPTIDOMIMETICS WITH ANTIMICROBIAL ACTIVITY 有权
标题翻译：具有抗微生物活性的模板固定肽
公开(公告)号：US20100240592A1
公开(公告)日：2010-09-23
申请号：US12161065
申请日：2007-01-15
申请人： Steven J. Demarco , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyana Srinivas , Frank Gombert , Daniel Obrecht
发明人： Steven J. Demarco , Wim Vrijbloed , Ricardo Dias , John Anthony Robinson , Nityakalyana Srinivas , Frank Gombert , Daniel Obrecht
IPC分类号： A61K38/10 , C07K7/08 , A61P31/00
CPC分类号： C07K7/64 , A01N43/36 , A61K38/00 , C07K1/10 , C07K7/06 , C07K7/08 , C07K14/001
摘要： Template-fixed β-hairpin peptidomimetics of the general formula (I) wherein Z is a template-fixed chain of 12 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 the property to selectively inhibit the growth of or to kill microorganisms such as Pseudomonas aeruginosa. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials, or as medicaments to treat or prevent infections. 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：通式（I）的模板固定和半乳糖肽模拟物，其中Z是12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Pro，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中定义，以及其盐具有选择性抑制微生物生长或杀死诸如假单胞菌铜绿假单胞菌它们可以用作食品，化妆品，药物或其他含营养材料的消毒剂，或用作治疗或预防感染的药物。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。

23. 发明申请

US20110312879A1 TEMPLATE-FIXED BETA-HAIRPIN PEPTIDOMIMETICS WITH CXCR4 ANTAGONIZING ACTIVITY 有权
标题翻译：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
申请人： Frank Gombert , Daniel Obrecht , Alexander Lederer , Barbara Romagnoli
发明人： Frank Gombert , Daniel Obrecht , Alexander Lederer , Barbara Romagnoli
IPC分类号： A61K38/15 , A61P7/00 , A61P31/18 , A61P35/00 , A61P35/04 , A61P29/00 , C07K7/54 , A61P9/10
CPC分类号： C07K7/64 , C07K1/047 , C07K7/08
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。

24. 发明授权

US08865656B2 Beta-hairpin peptidomimetics having CXCR4 antagonizing activity 有权
标题翻译：具有CXCR4拮抗活性的β-发夹肽模拟物
公开(公告)号：US08865656B2
公开(公告)日：2014-10-21
申请号：US13319052
申请日：2009-05-07
申请人： Daniel Obrecht , Frank Gombert , Alexander Lederer , Barbara Romagnoli , Christian Bisang
发明人： Daniel Obrecht , Frank Gombert , Alexander Lederer , Barbara Romagnoli , Christian Bisang
IPC分类号： A61K38/00 , C07K7/54 , A61P35/00 , C07K7/08 , C07K7/02
CPC分类号： C07K7/08 , C07K1/061 , C07K7/02
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。

25. 发明申请

US20070054840A1 Template-fixed peptidomimetics with antimicrobial activity 有权
标题翻译：具有抗菌活性的模板固定肽模拟物
公开(公告)号：US20070054840A1
公开(公告)日：2007-03-08
申请号：US10530335
申请日：2002-10-02
申请人： Jan Vrijbloed , Daniel Obrecht , John Robinson , Sergio Locurio , Frank Gombert , Christian Ludin , Alexander Lederer , Shivaprasad Shankaramma
发明人： Jan Vrijbloed , Daniel Obrecht , John Robinson , Sergio Locurio , Frank Gombert , Christian Ludin , Alexander Lederer , Shivaprasad Shankaramma
IPC分类号： A61K38/12 , C07K7/60
CPC分类号： C07K7/08 , A61K38/00 , C07K7/06 , C07K7/64 , C07K14/001
摘要： Template-fixed β-hairpin peptidomimetics of the general formula (I), wherein Z is a template-fixed chain of 12 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, at least one of these residues being of the type of N-substituted glycines, which types, as the remaining symbols in the above formula, are defined in the description and the claims, and salts thereof, have the property to inhibit the growth of or to kill microorganisms. They can be used as disinfectants for foodstuffs, cosmetics, medicaments or other nutrient-containing materials or as medicaments to treat or prevent infections. 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：通式（I）的模板固定的β-发夹肽模拟物，其中Z是12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Pro，或某些类型，这些残基中的至少一种是N-取代的甘氨酸类型，其类型作为上述式中的其余符号在说明书和权利要求书中定义，以及其盐具有抑制微生物生长或杀死微生物的性质。它们可以用作食品，化妆品，药物或其他含营养材料的消毒剂，或用作治疗或预防感染的药物。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。

26. 发明授权

US08883720B2 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：US08883720B2
公开(公告)日：2014-11-11
申请号：US13131205
申请日：2008-11-26
申请人： Frank Gombert , Daniel Obrecht , Alexander Lederer , Barbara Romagnoli
发明人： Frank Gombert , Daniel Obrecht , Alexander Lederer , Barbara Romagnoli
IPC分类号： A01N37/18 , A61K38/00 , A61P29/00 , A61P35/00 , C07K14/515 , C07K7/08 , C07K7/64 , C07K1/04
CPC分类号： C07K7/64 , C07K1/047 , C07K7/08
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。

27. 发明申请

US20080318838A1 PEPTIDES 审中-公开
公开(公告)号：US20080318838A1
公开(公告)日：2008-12-25
申请号：US12169134
申请日：2008-07-08
申请人： Wilfried Bauer , Robin Breckenridge , Francois Cardinaux , Frank Gombert , Hermann Gram , Paul Ramage , Helmut Schneider , Rudolf Waelchli , Rainer Albert , Ian Lewis
发明人： Wilfried Bauer , Robin Breckenridge , Francois Cardinaux , Frank Gombert , Hermann Gram , Paul Ramage , Helmut Schneider , Rudolf Waelchli , Rainer Albert , Ian Lewis
IPC分类号： A61K38/00 , C07K7/00 , C12P21/04 , C12N15/11 , A61P19/00 , C12N15/00 , C12N1/20
CPC分类号： C07K14/005 , A61K38/00 , C07K14/635 , C07K2319/00 , C07K2319/50 , C07K2319/75 , C12N2795/10222
摘要： PTH compounds having PTH-like activity and comprising at least one modification, said modification being either 1. at least one radical selected from a L- or D-α-amino acid, C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to the terminal amino group of the PTH compound, and/or at least one radical selected from C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to one or more side chain amino groups of the PTH compound, or 2. at least one α-amino acid unit in the positions 1 to 38 of a naturally occurring PTH sequence being replaced by a natural or unnatural amino acid unit optionally in protected form, whereby the α-amino acid units present in positions 1 and 2 at the amino terminus of the PTH sequence may be replaced by a pseudo-peptide, or a combination of such modifications, in free form or in salt form, have pharmacological activity, e.g. for preventing or treating all bone conditions which are associated with increased calcium depletion or resorption or in which calcium fixation in the bone is desirable.
摘要翻译：具有PTH样活性并且包含至少一个修饰的PTH化合物，所述修饰是1.至少一个选自L-或D-α-氨基酸，C2-6羰基和任选取代的C 1-8烷基的基团，C 2-8烯基，C 2-8炔基，芳烷基，芳烯基或C 3-6环烷基-C 1-4烷基，并且连接到PTH化合物的末端氨基，和/或至少一个选自C 2-6烷氧基羰基和任选取代的C 1-8烷基基团，C 2-8烯基，C 2-8炔基，芳烷基，芳烯基或C 3-6环烷基-C 1-4烷基，并且连接到PTH化合物的一个或多个侧链氨基，或2个至少一个α-氨基酸单元的位置1至38 天然存在的PTH序列被任选以保护形式的天然或非天然氨基酸单元替代，由此存在于PTH序列的氨基末端的位置1和2中的α-氨基酸单元可被假肽替代，或这些修改的组合，免费的 m或盐形式，具有药理活性，例如。用于预防或治疗与增加的钙耗竭或吸收相关的所有骨骼状况或其中期望骨中的钙固定。

28. 发明申请

US20050009147A1 Peptides 审中-公开
标题翻译：多肽
公开(公告)号：US20050009147A1
公开(公告)日：2005-01-13
申请号：US10848279
申请日：2004-05-18
申请人： Wilfried Bauer , Robin Breckenridge , Francois Cardinaux , Frank Gombert , Hermann Gram , Paul Ramage , Helmut Schneider , Rudolf Waelchli , Rainer Albert , Ian Lewis
发明人： Wilfried Bauer , Robin Breckenridge , Francois Cardinaux , Frank Gombert , Hermann Gram , Paul Ramage , Helmut Schneider , Rudolf Waelchli , Rainer Albert , Ian Lewis
IPC分类号： C07K9/00 , A61K38/00 , A61K38/22 , A61K38/29 , A61P3/00 , A61P3/14 , A61P19/08 , A61P43/00 , C07K20060101 , C07K14/01 , C07K14/195 , C07K14/41 , C07K14/635 , C07K19/00 , C12N1/20 , C12N1/21 , C12N5/10 , C12N15/09 , C12N15/16 , C12N15/62 , C12P21/02 , C12R1/19 , C07H21/04
CPC分类号： C07K14/005 , A61K38/00 , C07K14/635 , C07K2319/00 , C07K2319/50 , C07K2319/75 , C12N2795/10222
摘要： PTH compounds having PTH-like activity and comprising at least one modification, said modification being either 1. at least one radical selected from a L- or D-α-amino acid, C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to the terminal amino group of the PTH compound, and/or at least one radical selected from C2-6alcoxycarbonyl and optionally substituted C1-8alkyl, C2-8alkenyl, C2-8alkynyl, aralkyl, aralkenyl or C3-6cycloalkyl-C1-4alkyl and attached to one or more side chain amino groups of the PTH compound, or 2. at least one α-amino acid unit in the positions 1 to 38 of a naturally occurring PTH sequence being replaced by a natural or unnatural amino acid unit optionally in protected form, whereby the α-amino acid units present in positions 1 and 2 at the amino terminus of the PTH sequence may be replaced by a pseudo-peptide, or a combination of such modifications, in free form or in salt form, have pharmacological activity, e.g. for preventing or treating all bone conditions which are associated with increased calcium depletion or resorption or in which calcium fixation in the bone is desirable.
摘要翻译：具有PTH样活性并且包含至少一个修饰的PTH化合物，所述修饰是1.至少一个选自L-或D-α-氨基酸，C2-6羰基和任选取代的C 1-8烷基的基团，C 2-8烯基，C 2-8炔基，芳烷基，芳烯基或C 3-6环烷基-C 1-4烷基，并且连接到PTH化合物的末端氨基，和/或至少一个选自C 2-6烷氧基羰基和任选取代的C 1-8烷基基团，C 2-8烯基，C 2-8炔基，芳烷基，芳烯基或C 3-6环烷基-C 1-4烷基，并且连接到PTH化合物的一个或多个侧链氨基，或2个至少一个α-氨基酸单元的位置1至38 天然存在的PTH序列被任选以保护形式的天然或非天然氨基酸单元替代，由此存在于PTH序列的氨基末端的位置1和2中的α-氨基酸单元可被假肽替代，或这些修改的组合，免费的 m或盐形式，具有药理活性，例如。用于预防或治疗与增加的钙耗竭或吸收相关的所有骨骼状况或其中期望骨中的钙固定。

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