CAS: 474645-27-7; (S)-N-((3R,4S,5S)-1-((S)-2-((1R,2R)-3-(((1S,2R)-1-Hydroxy-1-Phenylpropan-2-yl)Amino)-1-Methoxy-2-Methyl-3-Oxopropyl)Pyrrolidin-1-yl)-3-Methoxy-5-Methyl-1-Oxoheptan-4-yl)-N,3-Dimethyl-2-((S)-3-Methyl-2-(Methylamino)Butanamido)Butanamide

上下游产品

(S)-2-((1R,2R)-3-(((1S,2R)-1-羟基-1-苯基丙-2-基)氨基)-1- Tert-Butyl (S)-2-((1R,2R)-3-(((1S,2R)-1-Hydroxy-1-Phenylpropan-2-yl)Amino)-1-Methoxy-2-Methyl-3-Oxopropyl)Pyrrolidine-1-Carboxylate 160800-65-7
(S)-Tert-Butyl 2-((1R,2R)-1-Methoxy-2-Methyl-3-((4R,5S)-4-Methyl-2-Oxo-5-Phenyloxazolidin-3-yl)-3-Oxopropyl)Pyrrolidine-1-Carboxylate 180715-99-5
Tert-Butyl (2S)-2-[(1R,2R)-1-Hydroxy-2-Methyl-3-[(4R,5S)-4-Methyl-2-Oxo-5-Phenyl-1,3-Oxazolidin-3-Yl]-3-Oxopropyl]Pyrrolidine-1-Carboxylate 133645-51-9
(S)-2-((1R,2R)-3-(苄氧基)-1-甲氧基-2-甲基-3-氧代丙基)吡咯烷-1-甲 Benzyl (2R,3R,2'S)-3-(N-Tert-Butoxycarbonyl-2'-Pyrrolidinyl)-3-Methoxy-2-Methylpropanoate 149606-97-3

左旋去甲麻黄碱置于二乙胺,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 二氯甲烷,N,N-二甲基甲酰胺 作为反应溶剂,化学反应生成 一甲基澳瑞他汀e
参考文献:一种靶向于egfr的抗体偶联药物及其制备 方法和其用途
标题:一种靶向于egfr的抗体偶联药物及其制备 方法和其用途
摘要:本发明公开了一种靶向于egfr的抗体偶联药物及其制备方法和其用途.所述的靶向于egfr的抗体偶联药物,命名为lr004‑vc‑mmae,其由抗体,细胞毒性药物和连接子组成,所述抗体药物偶联物具有式i所示的结构,其中,Mab为lr004单克隆抗体,N=2~8.该新型抗体偶联药物lr004‑vc‑mmae既能够靶向egfr抗原,又有强烈的杀伤肿瘤细胞的活性.且相较于lr004本身,并未影响抗体的亲和力,内吞活性和靶向性,较好的保留其生物学功能.相较于lr004,Lr004‑vc‑mmae抗体偶联药物的抑瘤效果有显著性的提高,且出现肿瘤消失的情况.相较于lr004,Lr004‑vc‑mmae抗体偶联药物总抗体呈现较长的半衰期,较慢的清除速率,血浆中游离的mmae浓度较低,且半衰期短,清除速度快,有利于降低毒性.

专利信息

专利号:US-12337038-B2
优先权日:2023-04-18
标 题 :Conjugates comprising cleavable beta-glucuronide-containing linkers
发明人：KHAN AKBAR HUSAIN; MADERNA ANDREAS LOTHAR SEVERINO; LEE MAXIMILLIAN TARO WILLIAM; COCCO MATTIA; DENG BOLIANG; BEADLE JONATHAN DAVID; GALAN COCA ALBANO; PRYYMA ALLA; BARTOLO NICOLE DANIELLE; MASTERSON LUKE; GOUNDRY WILLIAM ROBERT FRASER
权利人:ASTRAZENECA AB
摘要:The specification relates to conjugates comprising a linker of Formula (IA): n nand pharmaceutically acceptable salts thereof. The specification also relates the use of the conjugates for the treatment of diseases such as cancer, and intermediates useful for the synthesis of the conjugates.

专利号:US-2024025947-A1
优先权日:2021-03-31
标题 :Preparation and purification process of monomethyl auristain e compound
发明人：LI ZHUANGLIN; GUO WEI; SUN PENG; XIAO KAI; LI XINLI
权利人:REMEGEN CO LTD
摘要:Provided is a preparation and purification process of MMAE. The process has mild synthesis and purification conditions, can effectively prevent the change of product chirality caused by excessively high temperature, greatly reduces generation of degradation impurities, and increases the purity and yield of the product. In addition, the preparation and purification process has good stability and is more suitable for scale-up production. The MMAE prepared has purity of higher than 99%, and can perfectly meet clinical drug requirements.

专利号:US-2025073339-A1
优先权日:2023-08-15
标 题 :Conjugates comprising cleavable linkers
发明人：BEADLE JONATHAN DAVID; GALAN COCA ALBANO; COCCO MATTIA; GOUNDRY WILLIAM ROBERT FRASER
权利人:ASTRAZENECA AB
摘要:The specification relates to conjugates comprising a linker of Formula (IMA): n n n n n n n n n n and pharmaceutically acceptable salts thereof. The specification also relates the use of the conjugates for the treatment of diseases such as cancer, and intermediates useful for the synthesis of the conjugates.