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1. 发明授权

US10053490B2 Antimicrobial peptidomimetics 有权
公开(公告)号：US10053490B2
公开(公告)日：2018-08-21
申请号：US15104186
申请日：2015-01-22
申请人： Agency for Science, Technology and Research
发明人： Brian Cheng San Chia
IPC分类号： C07K5/087 , C07K5/117 , C07K1/00 , C07K1/06 , C07K1/10 , C07K5/02 , C07K5/065 , C07K5/072 , A61K38/00
CPC分类号： C07K5/0812 , A61K38/00 , C07K1/00 , C07K1/061 , C07K1/10 , C07K5/0212 , C07K5/06078 , C07K5/06095 , C07K5/1024
摘要： The present invention relates to peptidomimetics of the formula (I) or (I)c wherein L1, L2, L3, R1, R2, R3, R4, R5, R6, n, m, Q, X, Z1 and Z2 are defined as mentioned in the description and to salts and solvates of each of these compounds and to processes for the preparation thereof, compositions containing them and the uses of such compounds. It has been found that the compounds have a high microbicide activity and are suited to combat resistant bacteria, such as meticillin-resistant Staphylococcus aureus (MRSA) strains, at very low concentrations.

2. 发明授权

US09951099B2 Stabilized compounds having secondary structure motifs 有权
公开(公告)号：US09951099B2
公开(公告)日：2018-04-24
申请号：US15287513
申请日：2016-10-06
申请人： President and Fellows of Harvard College
发明人： Gregory L. Verdine , Christian E. Schafmeister
IPC分类号： C07K1/04 , C07K14/47 , C07K1/00 , A61K38/02 , C07K1/113 , C07K14/00 , C07K1/10 , C12N15/10 , A61K38/00
CPC分类号： C07K1/00 , A61K38/00 , A61K38/02 , C07K1/04 , C07K1/047 , C07K1/10 , C07K1/113 , C07K14/001 , C07K14/4746 , C12N15/1093
摘要： The present invention provides novel stabilized crosslinked compounds having secondary structure motifs, libraries of these novel compounds, and methods for the synthesis of these compounds libraries thereof. The synthesis of these novel stabilized compounds involves (1) synthesizing a peptide from a selected number of natural or non-natural amino acids, wherein the peptide comprises at least two moieties capable of undergoing reaction to promote carbon-carbon bond formation; and (2) contacting the peptide with a reagent to generate at least one crosslinker and to effect stabilization of a secondary structure motif. The present invention, in a preferred embodiment, provides stabilized p53 donor helical peptides. Additionally, the present invention provides methods for disrupting the p53/MDM2 binding interaction comprising (1) providing a crosslinked stabilized α-helical structure; and (2) contacting the crosslinked stabilized α-helical structure with MDM2.

3. 发明授权

US09873737B2 Stable and soluble antibodies inhibiting VEGF 有权
公开(公告)号：US09873737B2
公开(公告)日：2018-01-23
申请号：US14741430
申请日：2015-06-16
申请人： ESBATech, an Alcon Biomedical Research Unit LLC
发明人： Leonardo Borras , David Urech , Tea Gunde
IPC分类号： C07K16/22 , C07K1/00 , C07K7/06 , C12N15/09 , C12N15/70 , C12N15/79
CPC分类号： C07K16/22 , C07K1/00 , C07K7/06 , C07K2317/24 , C07K2317/54 , C07K2317/55 , C07K2317/56 , C07K2317/565 , C07K2317/567 , C07K2317/622 , C07K2317/73 , C07K2317/92
摘要： The present invention relates to soluble and stable anti-VEGF imunobinders comprising CDRs from rabbit monoclonal antibodies. Said antibodies are designed for the diagnosis and/or treatment of VEGF-mediated disorders. The hybridomas, nucleic acids, vectors and host cells for expression of the recombinant antibodies of the invention, methods for isolating them and the use of said antibodies in medicine are also disclosed.

4. 发明申请

US20170275596A1 COMPOSITION AND METHOD FOR TREATING ANDROGEN-DEPENDENT DISORDERS 审中-公开
公开(公告)号：US20170275596A1
公开(公告)日：2017-09-28
申请号：US15471194
申请日：2017-03-28
申请人： TECHNION RESEARCH & DEVELOPMENT FOUNDATION LTD.
发明人： Roee AMIT , Alexey TOMSOV , Orna ATAR , Liron ABRAHAMI , Yael ANNIS , Roni COHEN , Alexandra ERESKOVSKY , Noa KATZ , Lior LEVY , Maayan LUFTON , Tal OFEK , Sagi SHEINKMAN , Nitzan SHMUEL , Inbal VAKNIN , Ruth VEKSLER , Adi YANNAI
IPC分类号： C12N9/04 , A61K38/44 , A61K9/00 , A61K35/742
CPC分类号： C12N9/0006 , A61K9/0014 , A61K35/742 , A61K38/00 , A61K38/443 , C07K1/00 , C07K19/00 , C12Y101/01225 , Y02A50/473
摘要： Chimeric polypeptides comprising a dihydrotestosterone (DHT) reductase moiety, such as 3 alpha-hydroxysteroid dehydrogenase (3α-HSD), fused to a signal peptide moiety, polynucleotides encoding same, and compositions comprising at least one microorganism cell capable of secreting the chimeric polypeptide, are provided. Further provided are methods and kits for treating, preventing or ameliorating androgen-dependent disorders, including but not limited to androgenic alopecia.

5. 发明申请

US20170067045A1 PEPTIDE LIBRARIES 审中-公开
标题翻译：肽图书馆
公开(公告)号：US20170067045A1
公开(公告)日：2017-03-09
申请号：US15354667
申请日：2016-11-17
申请人： BICYCLE THERAPEUTICS LIMITED
发明人： Gregory Paul Winter , Christian Heinis , Elise Bernard , David Loakes , Daniel Paul Teufel
IPC分类号： C12N15/10 , C07K1/00
CPC分类号： C12N15/1037 , C07K1/00 , C07K1/042 , C07K1/113 , C07K2318/00
摘要： The invention relates to a method for altering the conformational diversity of a first repertoire of polypeptide ligands, comprising a plurality of polypeptides comprising at least two reactive groups separated by a loop sequence covalently linked to a molecular scaffold which forms covalent bonds with said reactive groups, to produce a second repertoire of polypeptide ligands, comprising assembling said second repertoire from the polypeptides and structural scaffold of said first repertoire, incorporating one of the following alterations: (a) altering at least one reactive group; or (b) altering the nature of the molecular scaffold; or (c) altering the bond between at least one reactive group and the molecular scaffold; or (d) any combination of (a), (b) or (c).
摘要翻译：本发明涉及一种用于改变多肽配体的第一组分的构象多样性的方法，其包含多个多肽，所述多肽包含至少两个反应性基团，所述反应基团通过共价连接到与所述反应性基团形成共价键的分子支架的环序列分开，以产生多肽配体的第二组成成分，其包括从所述第一组合物的多肽和结构性支架组装所述第二组分，并结合以下改变之一：（a）改变至少一个反应性基团; 或（b）改变分子支架的性质; 或（c）改变至少一个反应性基团和分子支架之间的键; 或（d）（a），（b）或（c）的任何组合。

6. 发明授权

US09505706B2 Preparation of lipoamino acids and lipopeptides using salts as co-reactants 有权
标题翻译：使用盐作为共反应物制备脂氨基酸和脂肽
公开(公告)号：US09505706B2
公开(公告)日：2016-11-29
申请号：US14830082
申请日：2015-08-19
申请人： University of South Carolina
发明人： Gordon Sproul
IPC分类号： A61K38/00 , C07K1/00 , C07C231/02 , C07K1/107 , C07B43/06
CPC分类号： C07C231/02 , C07B43/06 , C07K1/00 , C07K1/1077 , C07C233/36
摘要： Methods for synthesizing a lipoamino acid and a lipopeptide are provided. The method can include reacting a fatty acid with an amino acid or a peptide and a co-reactant salt to form a lipoamino acid or a lipopeptide, respectively. The co-reactant salt is generally a magnesium sulfate, magnesium carbonate, potassium carbonate, iron (II) sulfide (troilite), or a mixture thereof.
摘要翻译：提供了合成脂氨基酸和脂肽的方法。该方法可以包括使脂肪酸与氨基酸或肽和共反应物盐反应以分别形成脂氨基酸或脂肽。共反应物盐通常是硫酸镁，碳酸镁，碳酸钾，硫化铁（II）（铁氧化物）或它们的混合物。

7. 发明申请

US20160237119A1 C-Met Protein Agonist 有权
标题翻译： C-Met蛋白激动剂
公开(公告)号：US20160237119A1
公开(公告)日：2016-08-18
申请号：US15025239
申请日：2014-10-15
申请人： THE UNIVERSITY OF TOKYO
发明人： Hiroaki SUGA , Kenichiro ITO
IPC分类号： C07K7/08 , C07K1/00
CPC分类号： C07K7/08 , A61K38/00 , C07K1/00 , C07K1/1075 , C07K14/71 , C07K2319/00
摘要： Object of the present invention is to provide a peptide functioning as a c-Met agonist. The present invention provides a peptide complex comprising two or more peptides that bind to a c-Met protein and a linker that links the two or more peptides to one another. Such a peptide complex promotes autophosphorylation of the c-Met protein and induces cell growth.
摘要翻译：本发明的目的是提供用作c-Met激动剂的肽。本发明提供了包含两个或更多个结合c-Met蛋白的肽的肽复合物和将两个或多个肽彼此连接的连接体。这种肽复合物促进c-Met蛋白的自磷酸化并诱导细胞生长。

8. 发明授权

US09371357B2 Inhibitors of viral integrase and methods of use 有权
标题翻译：病毒整合酶的抑制剂及其使用方法
公开(公告)号：US09371357B2
公开(公告)日：2016-06-21
申请号：US14197016
申请日：2014-03-04
申请人： Integratech Proteomics, LLC , The United States of America, as Represented by the Secretary, Department of Health and Human Service
发明人： Tanya Sandrock , Robert Craigie
IPC分类号： A01N37/18 , A61K38/00 , A61P31/18 , A61P31/12 , A61K38/10 , A61K38/16 , A61K38/04 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , C07K1/00 , C07K4/00 , C07K7/08 , G01N33/573 , A61K38/03 , A61K39/00 , C07K7/02 , C12Q1/68 , C12Q1/70 , C40B30/04
CPC分类号： C07K4/00 , A61K38/00 , A61K38/03 , A61K38/10 , A61K39/00 , C07K1/00 , C07K7/02 , C07K7/08 , C12Q1/68 , C12Q1/70 , C40B30/04 , G01N33/573 , G01N2333/15 , G01N2500/02
摘要： Described herein are compositions and methods for inhibiting HIV integrase activity. Also described are methods of identifying agents that inhibit HIV integrase for use in treating or preventing HIV. Also disclosed are methods of identifying agents that inhibit HIV viral mutants that are resistant to integrase inhibitors.
摘要翻译：本文描述了用于抑制HIV整合酶活性的组合物和方法。还描述了鉴定抑制HIV整合酶用于治疗或预防HIV的药剂的方法。还公开了鉴定抑制对整合酶抑制剂有抗性的HIV病毒突变体的药剂的方法。

9. 发明授权

US09334302B2 Method for removing FMOC group 有权
标题翻译：去除FMOC组的方法
公开(公告)号：US09334302B2
公开(公告)日：2016-05-10
申请号：US14305841
申请日：2014-06-16
申请人： Ajinomoto Co., Inc.
发明人： Daisuke Takahashi
IPC分类号： A61K38/04 , C07K5/00 , C07K7/00 , C07K16/00 , C07K17/00 , C07K1/00 , C07K1/06 , C07C227/16 , C07K1/08 , C07B43/04
CPC分类号： C07K1/00 , C07B43/04 , C07C227/16 , C07K1/063 , C07K1/064 , C07K1/08 , C07C227/04 , C07C229/08
摘要： The present invention relates to a method of removing an Fmoc group, including a step of mixing a compound represented by the formula (I): HS-L-COOH (I) wherein L is a C1-8 alkylene group optionally having substituent(s), an amino group-containing compound protected by an Fmoc group, and a base to give a reaction mixture containing a compound represented by the formula (II): Fm—S-L-COOH (II) wherein Fm is a 9-fluorenylmethyl group, and L is as mentioned above, and an amino group-containing compound, and a step of removing the compound represented by the formula (II) by washing the obtained reaction mixture with a basic aqueous solution. According to the present invention, a removal method of Fmoc group, which can remove a dibenzofulvene derivative as a byproduct with ease, can be provided.
摘要翻译：本发明涉及一种除去Fmoc基团的方法，包括将式（I）表示的化合物：HS-L-COOH（I）（其中L是任选具有取代基的C 1-8亚烷基）），由Fmoc基保护的含氨基的化合物和碱，得到含有式（II）表示的化合物的反应混合物：Fm-SL-COOH（II）其中Fm为9-芴基甲基，和L如上所述，含氨基化合物，以及通过用碱性水溶液洗涤所得反应混合物除去由式（II）表示的化合物的步骤。根据本发明，可以提供能够容易地除去作为副产物的二苯并菲衍生物的Fmoc基团的除去方法。

10. 发明申请

US20150274820A1 STABLE AND SOLUBLE ANTIBODIES INHIBITING VEGF 审中-公开
标题翻译：稳定和可溶性抗体抑制VEGF
公开(公告)号：US20150274820A1
公开(公告)日：2015-10-01
申请号：US14741430
申请日：2015-06-16
申请人： ESBATech, an Alcon Biomedical Research Unit LLC
发明人： Leonardo Borras , David Urech , Tea Gunde
IPC分类号： C07K16/22
CPC分类号： C07K16/22 , C07K1/00 , C07K7/06 , C07K2317/24 , C07K2317/54 , C07K2317/55 , C07K2317/56 , C07K2317/565 , C07K2317/567 , C07K2317/622 , C07K2317/73 , C07K2317/92
摘要： The present invention relates to soluble and stable anti-VEGF imunobinders comprising CDRs from rabbit monoclonal antibodies. Said antibodies are designed for the diagnosis and/or treatment of VEGF-mediated disorders. The hybridomas, nucleic acids, vectors and host cells for expression of the recombinant antibodies of the invention, methods for isolating them and the use of said antibodies in medicine are also disclosed.
摘要翻译：本发明涉及包含来自兔单克隆抗体的CDR的可溶性和稳定的抗VEGF免疫抑制剂。所述抗体被设计用于诊断和/或治疗VEGF介导的病症。还公开了用于表达本发明的重组抗体的杂交瘤，核酸，载体和宿主细胞，其分离方法和所述抗体在医学中的用途。

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