CAS: 112883-39-3; Fmoc-D-Asp(Otbu)-Oh

相似化合物

71989-14-5 152548-66-8 1676-90-0

上下游产品

氯甲酸-9-芴基甲酯 (Fluorenylmethoxy)Carbonyl Chloride 28920-43-6

氯甲酸-9-芴基甲酯,D-天冬氨酸 4-叔丁酯置于sodium Carbonate,Sodium Hydroxide体系中,用 1,4-二氧六环,水 用作溶剂,以92 %的收率获得n-芴甲氧羰基-D-天冬氨酸-4-叔丁酯
参考文献:Peptidic Inhibitors And A Fluorescent Probe For The Selective Inhibition And Labelling Of Factor Xiiia Transglutaminase
标题:Peptidic Inhibitors And A Fluorescent Probe For The Selective Inhibition And Labelling Of Factor Xiiia Transglutaminase
摘要:因子 Xiiia(fxiiia)是一种转谷氨酰胺酶,在血液凝固级联过程中起着至关重要的作用,因此对抗凝剂的开发具有重要的治疗意义.虽然已有许多 Fxiiia 抑制剂的报道,但由于它们缺乏代谢稳定性,而且对转谷氨酰胺酶 2 (Tg2) 的选择性较低,因此未能进行临床评估.此外,用于研究 Fxiiia 活性和定位的化学工具也极为有限.为了克服这些不足,我们设计,合成并评估了一个包含 21 种新型 Fxiiia 抑制剂的文库.我们改变了小分子和多肽支架上的亲电弹头,链接长度和疏水单元,以优化同工酶的选择性和效力.随后,对之前报道的一种 Fxiiia 抑制剂进行了改良,设计出了一种带有罗丹明 B 分子的探针,从而产生了创新性的 Km93,它是第一个已知的荧光探针,可选择性地标记活性 Fxiiia,具有高效率(kinact/ki = 127,300 M-1 Min-1)和比 Tg2 高 6.5 倍的选择性.Km93 探针有助于在骨髓巨噬细胞内进行荧光显微镜研究,在细胞培养中高效,选择性地标记 Fxiiia.这些新型抑制剂和探针的结构-活性趋势将有助于今后研究 Fxiiia 的活性,抑制和定位.
Doi:10.3390/molecules28041634

专利信息

专利号:WO-2014108526-A1
优先权日:2013-01-11
标题 :Synthetic process for the manufacture of pipecolidepsin compounds
发明人：PELAY GIMENO MARTA; GARCÃ?A-RAMOS YESICA; TULLA PUCHE JUDIT; ALBERICIO PALOMERA FERNANDO; MARTÃ?N LÓPEZ M JES S
权利人:PHARMA MAR SA
摘要:(I) wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 9 , R 10 , R 11 , R 12 , n and Y are as described. The invention provides a process for the synthesis of complex pipecolidepsin and related compounds of formula (I), opening a new field of compounds with useful biological properties. The invention also provides intermediates, useful in the synthesis of compounds of formula (I).

专利号:US-11472844-B2
优先权日:2017-12-11
标题:Peptidomimetics, method of synthesis and uses thereof
发明人：MARTEYN BENOIT SEBASTIEN; COIC YVES-MARIE; BALEUX FRANCOISE
权利人:PASTEUR INSTITUT; INST NAT SANTE RECH MED; CENTRE NAT RECH SCIENT
摘要:The invention relates to a peptidomimetic comprising or consisting of a D amino-acid sequence having at least 75% identity with SEQ ID NO: 1 or SEQ ID NO: 2, or variants or fragments thereof, in particular a peptidomimetic having the capability to interact at least with: neutrophils and/or neutrophil granules, and/or lactoferrin, and/or globet-cells and/or Muc2 proteins, and/or mucus and/or airway sputum. The peptidomimetic may have the capacity to adopt a multimeric, especially a trimeric, organization, and can be labelled, or associated with a reporter or a carrier entity, or associated with an active molecule. The invention also relates to a Solid-Phase Synthesis method for synthesizing a peptidomimetic of the invention, compositions comprising the same and use of the peptidomimetics as a medicamentor an inflammation marker or a neutrophilic inflammation marker. The invention also relates to the use of a peptidomimetic as a probe or marker for staining purposes, or to detect mucus production, or neutrophils, or to detect or monitor diseases or conditions, especially neutrophilic inflammation. The invention also relates to the use of a polypeptide comprising or consisting of SEQ ID NO: 3, or variants or fragments thereof, as probe or marker for staining lactoferrin, in particular neutrophil lactoferrin, or a probe or marker for investigating neutrophilic inflammation, especially in an imaging method.

专利号:US-8338565-B2
优先权日:2008-08-20
标 题 :Macrocyclic compounds for inhibition of tumor necrosis factor alpha
发明人：LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P
权利人:LEE JINBO; BOND JULIAN F; TERRETT NICHOLAS; FAVALORO JR FRANK G; WANG DANIEL; BRIGGS TIMOTHY F; SEIGAL BENJAMIN ADAM; SUN WEI-CHUAN; HALE STEPHEN P; ENSEMBLE THERAPEUTICS CORP
摘要:Disclosed herein are macrocyclic compounds and methods for their synthesis and use. In particular, macrocyclic compounds are disclosed that modulate the activity of tumor necrosis factor alpha and/or are useful in the treatment of medical conditions, such as, rheumatoid arthritis, psoriasis, and asthma.

专利号:US-9795613-B2
优先权日:2014-12-10
标题 :GLP-1 receptor modulators
发明人：BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM R; BRAHMACHARY ENUGURTHI; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; KNAGGS MICHAEL; GLYNN DANIEL; MILLS MARK
权利人:CELGENE INT II SÀRL
摘要:Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “ â€? represents either or both the R and S form of the compound): n nwhere A, B, C, Y 1 , Y 2 , Z, R 1 , R 2 , R 3 , R 4 , R 5 , W 1 , n, p and q are as defined herein.

专利号:US-9598430-B2
优先权日:2013-06-11
标 题 :GLP-1 receptor modulators
发明人：BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM R; BRAHMACHARY ENUGURTHI; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; KNAGGS MICHAEL
权利人:RECEPTOS INC; CELGENE INT II SÀRL
摘要:Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “ â€? represents either or both the R and S form of the compound): n nwhere A, B, C, Y 1 , Y 2 , Z, R 1 , R 2 , R 3 , R 4 , R 5 , W 1 , n, p and q are as defined herein.

专利号:EP-3724215-B1
优先权日:2017-12-11
标 题 :Peptidomimetics, method of synthesis and uses thereof