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1. 发明申请

US20180105546A1 Methods for Chemical Synthesis of Biologically Active Compounds Using Supramolecular Protective Groups and Novel Compounds Obtainable Thereby 审中-公开
公开(公告)号：US20180105546A1
公开(公告)日：2018-04-19
申请号：US15629061
申请日：2017-06-21
申请人： Rijksuniversiteit Groningen
发明人： Andreas Herrmann , Andreas Alexander Bastian , Alessio Marcozzi
IPC分类号： C07H15/232 , C07K14/00 , C07K1/06 , C07H21/00 , C07K4/00
CPC分类号： C07H15/232 , C07H21/00 , C07K1/061 , C07K4/00 , C07K14/00 , Y02P20/55
摘要： The invention relates to drug development and synthetic chemistry, in particular to the manufacture of biologically active compounds based on naturally occurring molecules. It also relates to novel biologically active compounds, for example aminoglycoside antibiotics, in a substantially pure regioisomeric form. More particularly, the present invention relates to methods for the chemo- or regioselective derivatization of a target compound with multiple reactive groups, some of which may be derivatezed, and other which will not be derivatized.

2. 发明授权

US09868759B2 Solid phase peptides synthesis processes and associated systems 有权
公开(公告)号：US09868759B2
公开(公告)日：2018-01-16
申请号：US14853683
申请日：2015-09-14
申请人： Massachusetts Institute of Technology
发明人： Mark David Simon , Bradley L. Pentelute , Andrea Adamo , Patrick Louis Heider , Klavs F. Jensen
IPC分类号： A61K38/00 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , C07K1/04 , C07K1/06 , C07K1/08
CPC分类号： C07K1/045 , C07K1/04 , C07K1/042 , C07K1/061 , C07K1/08
摘要： Systems and processes for performing solid phase peptide synthesis are generally described. Solid phase peptide synthesis is a known process in which amino acid residues are added to peptides that have been immobilized on a solid support. In certain embodiments, the inventive systems and methods can be used to perform solid phase peptide synthesis quickly while maintaining high yields. Certain embodiments relate to processes and systems that may be used to heat, transport, and/or mix reagents in ways that reduce the amount of time required to perform solid phase peptide synthesis.

3. 发明授权

US09732137B2 Semi-recombinant preparation of GLP-1 analogues 有权
公开(公告)号：US09732137B2
公开(公告)日：2017-08-15
申请号：US12810934
申请日：2008-12-22
申请人： Jesper Færgeman Lau , Asser Sloth Andersen , Paw Bloch , Jesper Lau , Patrick William Garibay , Thomas Kruse , Inga Sig Nielsen Nørby , Claus Ulrich Jessen , Caspar Christensen , Jens Christian Norrild
发明人： Jesper Færgeman Lau , Asser Sloth Andersen , Paw Bloch , Jesper Lau , Patrick William Garibay , Thomas Kruse , Inga Sig Nielsen Nørby , Claus Ulrich Jessen , Caspar Christensen , Jens Christian Norrild
IPC分类号： C07K14/605 , C07K1/107 , C07K1/02 , C07K1/06 , C07K1/36 , C07K1/00
CPC分类号： C07K14/605 , C07K1/006 , C07K1/02 , C07K1/061 , C07K1/107 , C07K1/1077
摘要： A semi-recombinant method for the production of GLP-1 analogues and derivatives with non-proteogenic amino acids in the N-terminal part combining the use of recombinant expression techniques and chemical peptide synthesis.

4. 发明授权

US09376467B2 Cross-linked peptides containing non-peptide cross-linked structure, method for synthesizing cross-linked peptides, and novel organic compound used in method 有权
公开(公告)号：US09376467B2
公开(公告)日：2016-06-28
申请号：US14004058
申请日：2012-02-28
申请人： Yusuke Kono , Shuji Fujita , Hideaki Suzuki , Mari Okumoto , Takashi Nakae , Kazuhiro Chiba
发明人： Yusuke Kono , Shuji Fujita , Hideaki Suzuki , Mari Okumoto , Takashi Nakae , Kazuhiro Chiba
IPC分类号： C07K7/08 , A61K47/48 , C07K1/00 , C07K1/113 , C07K7/06 , C07K14/00
CPC分类号： C07K7/08 , A61K38/00 , A61K47/60 , C07K1/006 , C07K1/061 , C07K1/113 , C07K7/06 , C07K14/00
摘要： The purpose of the present invention is to provide a cross-linked peptide containing a novel non-peptide cross-linked structure, and a method for synthesizing the same. A cross-linked peptide having a novel non-peptide cross-linked structure, a useful intermediate for synthesizing the cross-linked peptide, and a method for synthesizing the novel cross-linked peptide and the intermediate are provided. The cross-linked peptide is characterized by having an —NR— bond in the cross-linked structure. By using the method for synthesizing the cross-linked peptide, a cross-link can be freely designed and an change can be freely made to a cross-link.

5. 发明授权

US09284352B2 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：US09284352B2
公开(公告)日：2016-03-15
申请号：US14466709
申请日：2014-08-22
申请人： POLYPHOR AG
发明人： Daniel Obrecht , Frank Otto Gombert , Alexander Lederer , Barbara Romagnoli , Christian Bisang
IPC分类号： C07K7/08 , C07K7/02 , C07K1/06
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。

6. 发明授权

US09095547B2 Structure assessment of heterogeneous polypeptide mixture 有权
标题翻译：异构多肽混合物的结构评估
公开(公告)号：US09095547B2
公开(公告)日：2015-08-04
申请号：US13651119
申请日：2012-10-12
申请人： Momenta Pharmaceuticals, Inc.
发明人： Ramamurthi Sridharan
IPC分类号： C07K1/06 , C07K14/00 , A61K38/16
CPC分类号： G01N21/19 , A61K38/00 , A61K38/16 , C07K1/061 , C07K14/001 , C08G69/36 , G01N21/25 , Y10S514/903
摘要： Glatiramer acetate containing compositions and drug products can be manufactured using methods that include a step of measuring one or both of the alpha helical content of the glatiramer acetate and the random coil content of the glatiramer acetate. These measurements can be compared to particular values or ranges for one or both of alpha helical and random coil content. The results of the comparison can be used in determining whether a given batch of glatiramer acetate should be used to manufacture a glatiramer acetate-containing drug product. The measurement of alpha helical content of the glatiramer acetate and the random coil content can be carried out using various methods, including circular dichroism.
摘要翻译：可以使用包括测量乙酸格拉默的α螺旋含量和乙酸格拉默的无规卷曲含量之一或两者的方法的方法来制造含有格列兰酸的组合物和药物产品。这些测量可以与α螺旋和无规卷曲含量中的一个或两个的特定值或范围进行比较。比较的结果可用于确定是否应使用给定批次的醋酸格拉特酸酯来制造含醋酸格拉默的药物产品。乙酸格拉默的α螺旋含量的测定和无规卷曲含量可以采用包括圆二色性在内的各种方法进行。

7. 发明申请

US20140288268A1 METHOD OF PRODUCING PEPTIDE 审中-公开
标题翻译：生产肽的方法
公开(公告)号：US20140288268A1
公开(公告)日：2014-09-25
申请号：US14204074
申请日：2014-03-11
申请人： KANEKA CORPORATION
发明人： Hiroshi MURAO , Ken-ichiro MORIO , Masaru MITSUDA
IPC分类号： C07K1/06 , C07K1/14
CPC分类号： C07K1/061 , C07K1/02 , C07K1/14 , C07K5/06078 , C07K5/06095 , C07K5/0806 , C07K5/0808 , C07K5/101
摘要： The present invention is related to a method of producing a peptide, characterized in contacting a reaction mixture with a base after a condensation reaction to hydrolyze while a basic condition is maintained until a ratio of a remaining unreacted active ester of an acid component is decreased to 1% or less in a liquid phase peptide synthesis method. According to the invention, a target peptide of high purity can be simply and efficiently produced by a continuous liquid phase synthesis method. Further, the present invention is related to a method of producing a peptide, characterized in using an amide-type solvent immiscible with water in a liquid phase peptide synthesis method. According to the invention, various peptides can be produced by the liquid phase synthesis method without being restricted by the amino acid sequence of the target peptide.
摘要翻译：本发明涉及一种生产肽的方法，其特征在于在缩合反应之后将反应混合物与碱反应以在碱性条件保持下进行水解，直到酸组分的剩余未反应的活性酯的比例降低至在液相肽合成方法中为1％以下。根据本发明，可以通过连续液相合成法简单有效地制备高纯度的靶肽。此外，本发明涉及一种制备肽的方法，其特征在于在液相肽合成方法中使用与水不混溶的酰胺型溶剂。根据本发明，可以通过液相合成法制备各种肽，而不受目标肽的氨基酸序列的限制。

8. 发明申请

US20130203960A1 MCR DENDRIMERS 有权
公开(公告)号：US20130203960A1
公开(公告)日：2013-08-08
申请号：US13695053
申请日：2011-04-14
申请人： Ludger A. Wessjohann , Michael Henze , Oliver Kreye , Daniel Garcia Rivera
发明人： Ludger A. Wessjohann , Michael Henze , Oliver Kreye , Daniel Garcia Rivera
IPC分类号： C07K1/06
CPC分类号： C07K1/061 , A61K38/00 , C07K5/0202 , C07K5/06069 , C07K14/001 , C08G83/003
摘要： The invention relates to a method for producing peptoidic, peptidic and chimeric peptidic-peptoidic dendrimers by multiple iterative multi-component reactions (MCR), in particular Ugi or Passerini multi-component reactions, to compounds produced in this way and to the use thereof.
摘要翻译：本发明涉及通过多次迭代多组分反应（MCR），特别是Ugi或Passerini多组分反应生产拟肽，肽和嵌合肽 - 肽酰树枝状大分子的方法，涉及以这种方式生产的化合物及其用途。

9. 发明申请

US20120135942A1 BETA-HAIRPIN PEPTIDOMIMETICS 有权
公开(公告)号：US20120135942A1
公开(公告)日：2012-05-31
申请号：US13319052
申请日：2009-05-07
申请人： Daniel Obrecht , Frank Otto Gombert , Alexander Lederer , Barbara Romagnoli , Christian Bisang
发明人： Daniel Obrecht , Frank Otto Gombert , Alexander Lederer , Barbara Romagnoli , Christian Bisang
IPC分类号： A61K38/12 , C07K7/54 , A61P35/00 , C07K1/06 , A61P31/18 , A61P37/00 , A61P37/04 , A61P7/00 , C07K7/64 , A61P29/00
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。

10. 发明申请

US20110165668A1 MHC Class I Peptide Epitopes from the Human 5T4 Tumor-Associated Antigen 审中-公开
标题翻译：人类5T4肿瘤相关抗原的MHC I类肽表位
公开(公告)号：US20110165668A1
公开(公告)日：2011-07-07
申请号：US12983744
申请日：2011-01-03
申请人： Miles Carroll , Susan Kingsman , Irina Redchenko
发明人： Miles Carroll , Susan Kingsman , Irina Redchenko
IPC分类号： C12N15/63 , C12N15/12
CPC分类号： C07K1/061 , A61K39/00 , A61K2039/5154 , A61K2039/5158 , C07K14/4748
摘要： There is provided an MHC class I peptide epitope from 5T4 antigen. In particular, there is provided a peptide epitope of 5T4 which comprises one of the following: (i) the amino acid sequence shown as SEQ ID NO: 2; (ii) the minimal epitope from the amino acid sequence shown as SEQ ID NO: 3; (iii) the minimal epitope from the amino acid sequence shown as SEQ ID NO: 4; (iv) the minimal epitope from the amino acid sequence shown as SEQ ID NO: 5; (v) the minimal epitope from the amino acid sequence shown as SEQ ID NO: 6; (vi) the minimal epitope from the amino acid sequence shown as SEQ ID NO: 7. There is also provided a vaccine comprising such a peptide (or precursor thereof) and its use to treat and/or prevent a disease, in particular a cancerous disease.
摘要翻译：提供了来自5T4抗原的MHC I类肽表位。特别地，提供了5T4的肽表位，其包含以下之一：（i）SEQ ID NO：2所示的氨基酸序列; （ii）如SEQ ID NO：3所示的氨基酸序列的最小表位; （iii）如SEQ ID NO：4所示的氨基酸序列的最小表位; （iv）如SEQ ID NO：5所示的氨基酸序列的最小表位; （v）如SEQ ID NO：6所示的氨基酸序列的最小表位; （vi）如SEQ ID NO：7所示的氨基酸序列的最小表位。还提供了包含这种肽（或其前体）的疫苗及其用于治疗和/或预防疾病，特别是癌性疾病。

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