CAS: 187389-52-2; Methyl (5S,8S,11S)-11-(2-Fluoroacetyl)-5-Isopropyl-8-Methyl-3,6,9-Trioxo-1-Phenyl-2-Oxa-4,7,10-Triazatridecan-13-Oate

上下游产品

(S)-N-(benzyloxycarbonyl)valine N-[(9H-fluoren-9-ylmethoxy)carbonyl]-L-alanine tert-butyl (S)-3-{[(9H-fluoren-9-yl)methoxycarbonyl]amino}-5-bromo-4-oxopentanoate

📜Tert-Butyl (S)-3-{[(9H-Fluoren-9-yl)Methoxycarbonyl]Amino}-5-Bromo-4-Oxopentanoate置于三甲基氯硅烷,四丁基氟化铵,Sodium Acetate,对甲苯磺酸,N,N-二异丙基乙胺,三氟乙酸,N-[(Dimethylamino)-3-Oxo-1H-1,2,3-Triazolo[4,5-B]Pyridin-1-Yl-Methylene]-N-Methylmethanaminium Hexafluorophosphate体系中,用 四氢呋喃,乙醇,二氯甲烷,水,N,N-二甲基甲酰胺 用作溶剂,化学反应 19.67H,反应生成N-[苄氧羰基]-L-缬氨酰基-N-[(1S)-3-氟-1-(2-甲氧基-2-氧代乙基)-2-氧代丙基]-L-丙氨酰胺
参考文献:将氟甲基酮纳入固相肽合成技术的改进方法
标题:将氟甲基酮纳入固相肽合成技术的改进方法
摘要:描述了一种改进且方便的肽基氟甲基酮合成技术.该方法基于天冬氨酸氟甲基酮与连接体的预先偶联,并将其安装到树脂结合的甲基二苯甲基胺盐酸盐上.随后,通过利用标准 Fmoc 肽程序,合成了许多短 Z 保护肽,并评估它们是否可能是 Sars-Cov-2 (3Cl Pro ) 主要蛋白酶的抑制剂.
Doi:10.1039/d1Ra03046A

专利信息

专利号:WO-2004087679-A1
优先权日:2003-04-01
标 题 :2, 4, 6-trisubstituted pyrimidine derivatives useful for the treatment of neoplastic and autoimmune diseases
发明人：OBRECHT DANIEL; ERMERT PHILIPP; LUTHER ANATOL; EBERLE MARTIN; BACHMANN FELIX
权利人:APONETICS AG; OBRECHT DANIEL; ERMERT PHILIPP; LUTHER ANATOL; EBERLE MARTIN; BACHMANN FELIX
摘要:The invention relates to substituted pyrimidines of formula (I) wherein V represents a bond or CR6R7, W represents a bond, NR8 or oxygen, X represents sulfur, or nitrogen substituted by hydrogen or R5, Y represents -CH2-, -CH2CH2-, -CO- or -CS-, R1 represents unsubstituted or substituted aryl or heteroaryl, and the substituents R2, R3, R4, R5, R6, R7 and R8 have the meanings given in the specification. These compounds are selectively inducing apoptosis in cancer cells and can be used for the treatment of neoplastic and autoimmune diseases. The invention relates also to methods of synthesis of such compounds, to their use as medicaments, to pharmaceutical compositions containing same, and to methods of treatment of neoplastic and autoimmune diseases using such compounds of formula (I) or of pharmaceutical compositions containing same.

专利号:US-2020352889-A1
优先权日:2011-06-03
标题 :Cystathionine compositions and methods of treatment for health conditions
发明人：MACLEAN KENNETH; AUSTIN RICHARD
权利人:UNIV COLORADO REGENTS; UNIV MCMASTER
摘要:The present invention relates to uses of and methods of treatment with cystathionine. In one embodiment, cystathionine reduces the development of toxin-induced liver and/or kidney disease induced by homocystinuria and/or acute nephropathy. In one embodiment, a cystathionine synthesis inhibitor is administered to increase tumor cell apoptosis and/or increase the efficacy of chemotherapeutic treatment. More particularly, cystathionine can protect cells against toxin-induced cellular apoptosis and/or cystathionine synthesis inhibitors can increase neuroblastoma cell kill rates during chemotherapy.

专利号:US-2002049157-A1
优先权日:1999-08-25
标题 :Use of proteasome inhibitors for treating cancer, inflammation, autoimmune disease, graft rejection and septic shock
发明人：WU JIANGPING; WANG XIN
摘要:The present invention relates to compositions comprising proteasome inhibitors, such as lactacystin, DPBA and their analogs. These compositions are used for the following purposes: (1) to disrupt mitochondrial function (useful aganst cancer, inflammation, adverse immune reaction and hyperthyroidism), (2) to disrupt nitric oxide synthesis (useful against inflammation and septic shock), and (3) to reverse ongoing adverse immune reactions, such as autoimmune diseases and graft rejection. In the later case, the compositions can be administered once the patients' T cells are mostly activated. Proteasome inhibitors can also be combined to immuno-suppressinve drugs like rapamycin, cyclosporin A and FK506. Finally, a method for screening a compound having a proteasome inhibition activity is also disclosed and claimed.

专利号:US-7951957-B2
优先权日:2004-02-11
标题 :Substituted benzimidazoles and their use for inducing apoptosis
发明人：EBERLE MARTIN; BACHMANN FELIX; STREBEL ALESSANDRO; ROY SUBHO; SRIVASTAVA SUDHIR; SAHA GOUTAM
权利人:BASILEA PHARMACEUTICA AG
摘要:The invention relates to compounds of formula (I) n nwherein R represents aryl or heteroaryl, X is a bond, a carbonyl group, a derivative of a carbonyl group, an ethylene group or an ethylenecarbonyl group, R 1 is optionally substituted amino or hydroxy, and the substituents R 2 to R 6 have the meanings given in the specification, to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to intermediates, to the use of a compounds of formula (I) as a medicament and for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using such compounds of formula (I) or of pharmaceutical compositions containing same.

专利号:US-7612064-B2
优先权日:2003-05-26
标题:Sulfopyrroles
发明人：EBERLE MARTIN; ERMERT PHILIPP; OBRECHT DANIEL; LACH FRANK; LUTHER ANATOL; BACHMANN FELIX; STREBEL ALLESSANDRO
权利人:TAKEDA PHARMACEUTICAL
摘要:The invention relates to compounds of formula (I) wherein R 1 represents aryl, aralkyl or heteroaryl, R 2 is aryl or heteroaryl and R 3 is aryl, heteroaryl or optionally substituted aminomethyl, to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to the use of a compounds of formula (I) for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using compounds of formula (I) or of pharmaceutical compositions containing same.

专利号:US-7541143-B2
优先权日:1997-02-20
标题 :Homo-doubly labeled compositions for the detection of enzyme activity in biological samples
发明人：PACKARD BEVERLY; KOMORIYA AKIRA
权利人:ONCOIMMUNIN INC
摘要:The present invention provides for novel reagents whose fluorescence changes upon cleavage or a change in conformation of a backbone. The reagents comprise a backbone (e.g. nucleic acid, polypeptide, etc.) joining two fluorophores of the same species whereby the fluorophores form an H-dimer resulting in quenching of the fluorescence of the fluorophores. When the backbone is cleaved or changes conformation, the fluorophores are separated, no longer forming an H-type dimer, and are de-quenched thereby providing a detectable signal. The use of a single fluorophore rather than an “acceptor-donorâ€? fluoresecence resonance energy transfer system offers synthesis and performance advantages.