6-氨基己酸置于sodium Hydroxide体系中,用 1,4-二氧六环 作为反应溶剂,化学反应生成 叔丁氧羰酰基6-氨基己酸 参考文献:Non-Peptidic Surrogates Of The Arg-Gly-Asp Sequence And Pharmaceutical 标题:Non-Peptidic Surrogates Of The Arg-Gly-Asp Sequence And Pharmaceutical 摘要:提供了非肽类的rxd类似物,可以抑制依赖于rxd识别的生物细胞和分子相互作用,其中x是氨基酸残基g,E,Y,A或f中的一个.特别地,提供了没有.Alpha.天然氨基酸序列的rgd替代物,其包含一个由11个原子构成的链分隔的鸟氨酸和羧基末端基团,其中至少有5个是碳原子.这些化合物可以抑制细胞粘附,并可用于治疗多种病理性疾病,例如血栓形成,自身免疫性疾病,转移,过敏,宿主移植反应和瘢痕组织形成的抑制.
专利号:WO-9817677-A1 优先权日:1996-10-24 标 题 :Improvements in solid-phase synthesis of peptides and related compounds 发明人:ENGLEBRETSEN DARREN 权利人:UNIV QUEENSLAND; ENGLEBRETSEN DARREN 摘要:The invention relates to spacers for use in solid-phase synthesis of peptides and peptide-related compounds, in which a spacer construct is used to ensure that the target peptide or peptide-related compound is at a distance equivalent to at least 5-15 amino acids from the solid support. Constructs of the invention are particularly applicable to the synthesis of strongly hydrophobic peptide, which are otherwise difficult, if not impossible to purify and analyse. The constructs and methods of the invention are also applicable to synthesis of peptide nucleic acids.
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-9453037-B2 优先权日:2011-07-28 标 题 :Methylphenidate-prodrugs, processes of making and using the same 发明人:GUENTHER SVEN; CHI GUOCHEN; BERA BINDU; MICKLE TRAVIS; BERA SANJIB 权利人:KEMPHARM INC; KEMPHARM INC 摘要:The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.
专利号:US-10975048-B2 优先权日:2015-12-14 标题 :Composition of 1,3,4-selenadiazole containing compounds with pharmacological activity 发明人:RUAN BENFANG HELEN; RUAN JENNIFER JIN 权利人:HANGZHOU JENNIFER BIOTECH CO LTD 摘要:The invention belongs to the field of biomedical research involving the 1,3,4-selenyldiazo derivatives that have cell protective activity. Because there are not so many heterocyclic selenium compounds, we synthesized a new type of selenium analog of BPTES. As the isoacceptor of BPTES, the compounds have antitumor activity, anti-oxidation and cell protection function. Currently many drugs contain the thiodiazo motif, so synthesis of selenyldiazo functional group could further optimize these drugs and are important in new drug development and application.
专利号:WO-02076965-A1 优先权日:2001-03-23 标 题 :Non peptide mimetics based on the active sequence s42fllr46 of the thrombin receptor for the treatment of thrombosis and cancer 发明人:MATSOUKAS JOHN; MARAGOUDAKIS MICHAEL; VLAHAKOS DEMETRIOS; ALEXOPOULOS KOSTAS 权利人:MATSOUKAS JOHN; MARAGOUDAKIS MICHAEL; VLAHAKOS DEMETRIOS; ALEXOPOULOS KOSTAS 摘要:The invention relates to novel non peptide compounds (mimetics) based on a thrombin receptor sequence and novel methods for the synthesis of these compounds. These compounds act as agonists or antagonists in a variety of cells including endothelial cells, blood platelets, vascular smooth muscle cells and tumor cells. They are useful in the treatment of thrombosis an cardiovascular diseases and modulation of angiogenesis for cancer treatment or wound healing.
专利号:US-2019276389-A1 优先权日:2015-12-18 标题:Synthesis of aryl cyclohexane ester derivatives useful as sensates in consumer products 发明人:WOS JOHN AUGUST; YELM KENNETH EDWARD; BUNKE GREGORY MARK; FREDERICK HEATH ALAN; REILLY MICHAEL; HAUGHT JOHN CHRISTIAN; SREEKRISHNA KOTI TATACHAR; LIN YAKANG 权利人:PROCTER & GAMBLE 摘要:Personal care compositions, such as oral care and skin care compositions containing a flavor/perfume system comprising one or more coolants. The pleasant cool sensation provided by a coolant is enhanced in terms of quicker onset, greater intensity, impact or longer duration, which improves appeal and acceptability of the compositions to consumers.
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