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1. 发明申请

US20190202861A1 N-CARBOXYANHYDRIDE-BASED-SCALE SYNTHESIS OF ELAMIPRETIDE 审中-公开
公开(公告)号：US20190202861A1
公开(公告)日：2019-07-04
申请号：US16325667
申请日：2017-08-09
申请人： STEALTH BIOTHERAPEUTICS
发明人： Scott M. Duncan , Jan Oudenes , Marc W. Andersen
IPC分类号： C07K5/11 , C07K5/072 , C07K5/09 , C07K1/06 , C07K1/10
CPC分类号： C07K5/1019 , A61K38/00 , C07K1/061 , C07K1/10 , C07K5/06078 , C07K5/06086 , C07K5/06095 , C07K5/0812 , C07K5/0817
摘要： Disclosed are methods of making elamipretide (MTP-131), a peptide compound with therapeutic potential for treating various mitochondrial myopathies. The synthesis of the peptide can be achieved via the use of N-carboxyanhydride-modified amino acid residues, which increases the efficiency of the synthetic process and the purity of the peptide product generated.

2. 发明授权

US10059738B2 Process for the production of a dipeptide derivative 有权
公开(公告)号：US10059738B2
公开(公告)日：2018-08-28
申请号：US15321792
申请日：2015-06-01
申请人： DSM IP Assets B.V.
发明人： Jonathan Alan Medlock , Peter Wikstroem
IPC分类号： C07C231/14 , C07K5/062 , C07K1/02 , C07K1/06 , C07K1/107 , C07K1/10
CPC分类号： C07K5/06069 , C07C311/13 , C07K1/02 , C07K1/061 , C07K1/10 , C07K1/1075
摘要： The present invention is related to a novel and improved process for the manufacture of compounds of formula (I) or salts thereof herein designated as benzylsulfonyl-Ser-X-4-amidinobenzylamide, wherein R is a C1 to C6 linear or branched aliphatic hydrocarbon chain optionally substituted with a C6 to C10 aromatic group.

3. 发明授权

US09969769B2 Coupling method for peptide synthesis at elevated temperatures 有权
公开(公告)号：US09969769B2
公开(公告)日：2018-05-15
申请号：US15647909
申请日：2017-07-12
申请人： CEM CORPORATION
发明人： Jonathan M. Collins , Sandeep Kumar Singh
IPC分类号： C07K1/00 , C07K1/08 , C07K1/04 , C07K14/575
CPC分类号： C07K1/006 , C07K1/04 , C07K1/045 , C07K1/08 , C07K1/084 , C07K1/10 , C07K14/57581
摘要： An improved method for coupling amino acids into peptides or peptidomimetics is disclosed that includes the steps of combining an amino acid, a carbodiimide, an activator additive, and a base at less than 1 equivalent compared to the amino acid to be activated; and carrying out the activation and coupling at a temperature greater than 30° C.

4. 发明授权

US09738685B2 Use of ruthenium complexes for preparing amides, polypeptides and cyclic dipeptides 有权
公开(公告)号：US09738685B2
公开(公告)日：2017-08-22
申请号：US15017049
申请日：2016-02-05
申请人： YEDA RESEARCH AND DEVELOPMENT CO. LTD.
发明人： David Milstein , Chidambaram Gunanathan , Yehoshua Ben-David , Ekambaram Balaraman , Boopathy Gnanaprakasam , Jing Zhang
IPC分类号： C07K5/12 , C07C209/50 , C07C213/00 , C07C231/00 , C07C231/02 , C07D307/52 , C08L79/02 , C07C67/03 , C07C45/00 , C07C51/235 , C07C67/28 , C07D241/12 , C07D295/185 , C07D487/14 , C07C29/136 , C07C67/39 , C07K1/02 , C07K1/10
CPC分类号： C07K5/12 , C07C29/136 , C07C45/002 , C07C51/235 , C07C67/03 , C07C67/28 , C07C67/39 , C07C209/50 , C07C213/00 , C07C231/00 , C07C231/02 , C07C2601/08 , C07C2601/14 , C07D241/12 , C07D295/185 , C07D307/52 , C07D487/14 , C07K1/02 , C07K1/10 , C08L79/02 , Y02P20/52 , C07C233/05 , C07C235/06 , C07C235/10 , C07C233/36 , C07C211/27 , C07C215/28 , C08L1/00 , C07C69/14 , C07C69/24 , C07C31/04 , C07C31/08 , C07C31/10 , C07C31/12
摘要： A process for preparing amides by reacting a primary amine and a primary alcohol in the presence of a Ruthenium complex to generate the amide and molecular hydrogen. Primary amines are directly acylated by equimolar amounts of alcohols to produce amides and molecular hydrogen (the only byproduct) in high yields and high turnover numbers. Also disclosed are processes for hydrogenation of amides to alcohols and amines; hydrogenation of organic carbonates to alcohols; hydrogenation of carbamates or urea derivatives to alcohols and amines; amidation of esters; acylation of alcohols using esters; coupling of alcohols with water and a base to form carboxylic acids; dehydrogenation of beta-amino alcohols to form pyrazines and cyclic dipeptides; and dehydrogenation of secondary alcohols to ketones. These reactions are catalyzed by a Ruthenium complex which is based on a dearomatized PNN-type ligand of formula A1 or precursors thereof of formulae A2 or A3.

5. 发明授权

US09676702B2 Methods for synthesizing amatoxin building block and amatoxins 有权
公开(公告)号：US09676702B2
公开(公告)日：2017-06-13
申请号：US14414143
申请日：2013-07-12
申请人： Heidelberg Pharma GmbH
发明人： Christian Lutz , Christoph Mueller , Werner Simon
IPC分类号： A61K31/33 , C07D487/04 , C07C227/16 , C07C229/22 , C07K1/06 , C07D207/16 , C07K1/10
CPC分类号： C07C227/16 , C07C229/22 , C07D207/16 , C07K1/065 , C07K1/10 , Y02P20/55
摘要： The invention relates to novel methods for synthesizing a synthon for γ,δ-dihydroxyisoleucine 1 (CAS No. 55399-94-5] as building block for the synthesis of amatoxins, and for novel methods for synthesizing amatoxins using such building block.

6. 发明申请

US20160152663A1 USE OF RUTHENIUM COMPLEXES FOR FORMATION AND/OR HYDROGENATION OF AMIDES AND RELATED CARBOXYLIC ACID DERIVATIVES 有权
标题翻译：用于形成和/或加氢酰胺和相关羧酸衍生物的方法
公开(公告)号：US20160152663A1
公开(公告)日：2016-06-02
申请号：US15017049
申请日：2016-02-05
申请人： YEDA RESEARCH AND DEVELOPMENT CO. LTD.
发明人： David MILSTEIN , Chidambaram GUNANATHAN , Yehoshua BEN-DAVID , Ekambaram BALARAMAN , Boopathy GNANAPRAKASAM , Jing ZHANG
IPC分类号： C07K5/12 , C07C231/02 , C07C45/00 , C07D241/12 , C07C51/235 , C07C67/28 , C07D487/14 , C07D295/185
CPC分类号： C07K5/12 , C07C29/136 , C07C45/002 , C07C51/235 , C07C67/03 , C07C67/28 , C07C67/39 , C07C209/50 , C07C213/00 , C07C231/00 , C07C231/02 , C07C2601/08 , C07C2601/14 , C07D241/12 , C07D295/185 , C07D307/52 , C07D487/14 , C07K1/02 , C07K1/10 , C08L79/02 , Y02P20/52 , C07C233/05 , C07C235/06 , C07C235/10 , C07C233/36 , C07C211/27 , C07C215/28 , C08L1/00 , C07C69/14 , C07C69/24 , C07C31/04 , C07C31/08 , C07C31/10 , C07C31/12
摘要： A process for preparing amides by reacting a primary amine and a primary alcohol in the presence of a Ruthenium complex to generate the amide and molecular hydrogen. Primary amines are directly acylated by equimolar amounts of alcohols to produce amides and molecular hydrogen (the only byproduct) in high yields and high turnover numbers. Also disclosed are processes for hydrogenation of amides to alcohols and amines; hydrogenation of organic carbonates to alcohols; hydrogenation of carbamates or urea derivatives to alcohols and amines; amidation of esters; acylation of alcohols using esters; coupling of alcohols with water and a base to form carboxylic acids; dehydrogenation of beta-amino alcohols to form pyrazines and cyclic dipeptides; and dehydrogenation of secondary alcohols to ketones. These reactions are catalyzed by a Ruthenium complex which is based on a dearomatized PNN-type ligand of formula A1 or precursors thereof of formulae A2 or A3.
摘要翻译：在钌络合物的存在下通过伯胺和伯醇反应制备酰胺以产生酰胺和分子氢的方法。伯胺通过等摩尔量的醇直接酰化，以高产率和高周转数产生酰胺和分子氢（仅副产物）。还公开了将酰胺氢化成醇和胺的方法; 将有机碳酸酯氢化成醇; 将氨基甲酸酯或脲衍生物氢化成醇和胺; 酯化酰胺化; 使用酯酰化醇; 醇与水和碱偶联形成羧酸; β-氨基醇的脱氢形成吡嗪和环状二肽; 并将仲醇脱氢成酮。这些反应由基于式A1的脱芳香族PNN型配体或式A2或A3的前体的钌络合物催化。

7. 发明授权

US09234003B2 Palladium catalyzed reactions executed on solid-phase peptide synthesis supports for the production of self-assembling peptides embedded with complex organic electronic subunits 有权
标题翻译：在固相肽合成中进行的钯催化反应支持用于复合有机电子亚基嵌入的自组装肽的生产
公开(公告)号：US09234003B2
公开(公告)日：2016-01-12
申请号：US14524845
申请日：2014-10-27
申请人： The Johns Hopkins University
发明人： John D. Tovar , Allix M. Sanders
IPC分类号： C07K7/00 , C07K7/04 , C07K7/08 , A61K31/38 , A61K31/381 , C07K7/06 , C07K1/10 , C07D331/00 , C07D333/00 , A61K38/00 , A61K38/02 , A61K47/48
CPC分类号： C07K7/06 , A61K38/00 , A61K38/02 , A61K47/62 , C07D331/00 , C07D333/00 , C07K1/10
摘要： Methods to synthesize self-assembling peptides embedded with complex organic electronic subunits are provided.
摘要翻译：提供了嵌入复合有机电子亚单位的自组装肽合成方法。

8. 发明申请

US20140187471A1 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：US20140187471A1
公开(公告)日：2014-07-03
申请号：US14175160
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.
摘要翻译：模板固定和通用的肽模拟物，其中Z是12个α-氨基酸残基的模板固定链，取决于它们在链中的位置（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及其盐中定义，具有选择性抑制绿脓假单胞菌等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。这些和平滑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。

9. 发明申请

US20140162339A1 Stabilized Compounds Having Secondary Structure Motifs 有权
标题翻译：具有二级结构基序的稳定化合物
公开(公告)号：US20140162339A1
公开(公告)日：2014-06-12
申请号：US14068844
申请日：2013-10-31
申请人： PRESIDENT AND FELLOWS OF HARVARD COLLEGE
发明人： GREGORY L. VERDINE , CHRISTIAN E. SCHAFMEISTER
IPC分类号： C07K1/113
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 said peptide comprises at least two moieties capable of undergoing reaction to promote carbon-carbon bond formation; and (2) contacting said 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 said crosslinked stabilized α-helical structure with MDM2.
摘要翻译：本发明提供具有二级结构基序的新型稳定化交联化合物，这些新化合物的文库，以及合成这些化合物文库的方法。这些新型稳定化合物的合成涉及（1）从选定数量的天然或非天然氨基酸合成肽，其中所述肽包含至少两个能够进行促进碳 - 碳键形成反应的部分; 和（2）使所述肽与试剂接触以产生至少一种交联剂并实现二级结构基序的稳定化。本发明在优选的实施方案中提供稳定的p53供体螺旋肽。另外，本发明提供了破坏p53 / MDM2结合相互作用的方法，其包括（1）提供交联的稳定的α-螺旋结构; 和（2）使所述交联的稳定的α-螺旋结构与MDM2接触。

10. 发明申请

US20140128572A1 Process For Extraction Of Peptides And Its Application In Liquid Phase Peptide Synthesis 审中-公开
标题翻译：肽提取方法及其在液相肽合成中的应用
公开(公告)号：US20140128572A1
公开(公告)日：2014-05-08
申请号：US14125804
申请日：2012-06-14
申请人： Didier Monnaie , Luciano Forni , Mathieu Giraud
发明人： Didier Monnaie , Luciano Forni , Mathieu Giraud
IPC分类号： C07K1/14
CPC分类号： C07K1/145 , C07K1/02 , C07K1/10 , C07K5/1008 , C07K5/1021 , C07K5/1024 , C07K7/06 , C07K7/08 , C07K14/001
摘要： A process for extraction of a peptide from a reaction mixture resulting from a peptide coupling reaction, the reaction mixture containing the peptide and a polar aprotic solvent selected from N,N-dimethylformamide, N,N-dimethylacetamide and N-methyl-2-pyrrolidone, whereby the process includes a step a) and a step b): step a) including the addition of a component a1), a component a2) and a component a3), whereby component a1) is an organic solvent 1, the organic solvent 1 is selected from 2-methyltetrahydrofuran and toluene, component a2) is water, and component a3) is an organic solvent 2, the organic solvent 2 is selected from the ethylacetate, isopropylacetate, acetonitrile, tetrahydrofuran and n-heptane to the reaction mixture, so that a biphasic system with an organic layer and an aqueous layer is obtained; step b) including the subsequent separation of the organic layer containing the peptide from the aqueous layer. The extraction step is preferably used in a process for preparation of a peptide in liquid phase.
摘要翻译：从肽偶联反应得到的反应混合物中提取肽的方法，含有肽的反应混合物和选自N，N-二甲基甲酰胺，N，N-二甲基乙酰胺和N-甲基-2-吡咯烷酮的极性非质子溶剂其中该方法包括步骤a）和步骤b）：步骤a）包括添加组分a1），组分a2）和组分a3），其中组分a1）是有机溶剂1，有机溶剂 1选自2-甲基四氢呋喃和甲苯，组分a2）为水，组分a3）为有机溶剂2，有机溶剂2选自乙酸乙酯，乙酸异丙酯，乙腈，四氢呋喃和正庚烷至反应混合物，从而获得具有有机层和水层的双相体系; 步骤b）包括随后从水层分离含有肽的有机层。提取步骤优选用于制备液相肽的方法。

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