CAS: 745017-94-1; (S)-2-((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S)-N,3-Dimethyl-2-((S)-3-Methyl-2-(Methylamino)Butanamido)Butanamido)-3-Methoxy-5-Methylheptanoyl)Pyrrolidin-2-yl)-3-Methoxy-2-Methylpropanamido)-3-Phenylpropanoic Acid

上下游产品

methyl (2S)-2-amino-3-phenylpropanoate hydr°Chloride (2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S)-2-((tert-butoxycarbonyl)amino)-N,3-dimethylbutanamido)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropanoic acid (S)-methyl 2-((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S)-2-((tert-butoxycarbonyl)amino)-N,3-dimethylbutanamido)-3-methoxy-5-methylheptanoyl)-pyrrolidin-2-yl)-3-methoxy-2-methylpropanamido)-3-phenylpropanoate 34H56N4O7*ClHC34H56N4O7*ClH((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S)-2-((S)-2-(dimethylamino)-3-methylbutyrylamino)-N,3-dimethylbutyrylamino)-3-methoxy-5-methylheptanoyl)pyrrolidin-2-yl)-3-methoxy-2-methylpropionyl)-L-phenylalanine 51H88N6O13*ClHC51H88N6O13*ClH 52H79N7O11C52H79N7O11

Methyl (S)-2-((2R,3R)-3-((S)-1-((3R,4S,5S)-4-((S)-2-Amino-N,3-Dimethylbutanamido)-3-Methoxy-5-Methylheptanoyl)Pyrrolidin-2-yl)-3-Methoxy-2-Methylpropanamido)-3-Phenylpropanoate 在 2,6-二甲基吡啶,盐酸,Methanaminium,N-[(Dimethylamino)(3H-1,2,3-Triazolo[4,5-B]Pyridin-3-Yloxy)Methylene]-N-Methyl-,Hexafluorophosphate(1-)体系中,用 1,4-二氧六环,N,N-二甲基甲酰胺,甲苯作为反应溶剂,反应 42.0H,获得 Mmaf
参考文献:[En] Efficient Preparation Of Dolastatin And Auristatin Analogs Through A Common Intermediate[Fr] Préparation Efficace D'Analogues De Dolastatines Et D'Auristatines Par Le Biais D'Un Intermédiaire Commun
标题:[En] Efficient Preparation Of Dolastatin And Auristatin Analogs Through A Common Intermediate[Fr] Préparation Efficace D'Analogues De Dolastatines Et D'Auristatines Par Le Biais D'Un Intermédiaire Commun
摘要:制备多拉斯塔汀,奥利斯塔汀或相关化合物的方法包括以下步骤:提供通用多拉斯塔汀核心的公式(I),将c末端羧酸基团与胺(A)反应形成酰胺键,并将n末端胺基与羧酸(Ca)反应形成酰胺键,其中这些步骤可以以任意顺序执行.还提供了通用多拉斯塔汀核心的孤立盐,用于制备多拉斯塔汀,奥利斯塔汀和相关化合物.还提供了一些中间体和工艺步骤,可用于制备高纯度的多拉斯塔汀核心和高纯度的多拉斯塔汀和奥利斯塔汀化合物.

专利信息

专利号:US-2017283878-A1
优先权日:2015-12-11
标题:Modulation of globoseries glycosphingolipid synthesis and cancer biomarkers
发明人：WONG CHI-HUEY; WU CHUNG-YI; CHEUNG SARAH K C; CHUANG PO-KAI; HSU TSUI-LING
权利人:ACADEMIA SINICA
摘要:The present disclosure relates to methods and compositions which can modulate the globoseries glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globoseries glycosphingolipid SSEA-3/SSEA-4/GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globoseries synthetic pathway. Additionally, the present disclosure is also directed to vaccines, antibodies, and/or immunogenic conjugate compositions targeting the SSEA-3/SSEA-4/GLOBO H associated epitopes (natural and modified) which elicit antibodies and/or binding fragment production useful for modulating the globoseries glycosphingolipid synthesis. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and/or conditions. Furthermore, the instant disclosure also relates to cancer stem cell biomarkers for diagnostic and therapeutic uses.

专利号:WO-2024186075-A1
优先权日:2023-03-03
标题 :Synthesis method of antibody-drug conjugates using proximity effect-based site-selective antibody labeling
发明人：LEE HYUN SOO; KIM SOOIN; KWEON YONGSEOK
权利人:UNIV SOGANG RES & BUSINESS DEVELOPMENT FOUND; RESEARCH & BUSINESS FOUNDATION SUNGKYUNKWAN UNIV
摘要:The present invention relates to a method for the synthesis of an antibody-drug conjugate using proximity effect-based site-selective antibody labeling. Provided according to the present invention may be a method for the synthesis of an antibody-drug conjugate by site-selectively introducing a drug into an antibody using a pyridinium oxime derivative (labeling mediator protein) introduced into a binding protein containing a non-standard amino acid.

专利号:US-2025009786-A1
优先权日:2021-09-30
标 题 :Automated synthesis of polymeric dual drugs
发明人：MATRAY TRACY; VANBRUNT MICHAEL; MCCUTCHEON JOHN MICHAEL
权利人:SONY GROUP CORP
摘要:Compounds useful as biologically active compounds with or without fluorescent or colored dyes are disclosed. In some embodiments, the compounds have the following structure (I): (I) or a stereoisomer, tautomer or salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, L1, L2, L3, L4, L5, L6, L7, L8, L9, L10, L11, M1, M2, M3, l, m, n, p, and q are as defined herein. Additional compound, methods of preparation, pharmaceutical compositions, and methods of treatment related to compounds of Structure (I) are also provided.

专利号:US-2024350645-A1
优先权日:2021-07-22
标 题 :Automated synthesis of polymeric drugs
发明人：MATRAY TRACY; VANBRUNT MICHAEL; MCCUTCHEON JOHN MICHAEL
权利人:SONY GROUP CORP
摘要:Compounds useful as biologically active compounds are disclosed. The compounds have the following structure (I): or a stereoisomer, tautomer or salt thereof, wherein L 1 , L 2 , L 3 , R 1 R 2 , M, p, q, m, and n are as defined herein. Additional compounds, methods of preparation, pharmaceutical compositions, and methods of treatment related to compounds of Structure (I) are also provided.

专利号:US-10772971-B2
优先权日:2017-06-22
标 题:Methods of producing drug-carrying polymer scaffolds and protein-polymer-drug conjugates
发明人：GURIJALA VENU REDDY; BOLLU SATYANARAYAN REDDY; LEBLANC JACQUES; LOWINGER TIMOTHY B; MCGILLICUDDY DENNIS; YIN MAO; YURKOVETSKIY ALEKSANDR V
权利人:MERSANA THERAPEUTICS INC; MERSANA THERPEUTICS INC
摘要:The disclosure provides methods of synthesis of polymeric scaffolds, e.g., those useful for conjugating with a protein based recognition-molecule (PBRM) to form PBRM-polymer-drug conjugates, and PBRM-polymer-drug conjugates thereof. The methods according to the disclosure allow for large-scale preparation of polymeric scaffolds having a high purity. In some embodiments, the methods according to the disclosure also allow for the preparation of scaffolds and conjugates thereof in better yield than previously used methods for preparing same. Also disclosed are methods of purifying polymeric scaffolds.

专利号:WO-2023179723-A1
优先权日:2022-03-25
标题:Cleavable fragment directed by affinity fragment, design and synthesis thereof, and use thereof in preparation of site-directed drug conjugate
发明人：HUANG WEI; TANG FENG; ZENG YUE
权利人:SHANGHAI INST MATERIA MEDICA CAS
摘要:Provided in the present invention are a cleavable fragment directed by an affinity fragment, the design and the synthesis thereof, and the use thereof in the preparation of a site-directed drug conjugate. Specifically, provided in the present invention is a conjugate with a ligand affinity directing group. The conjugate is as represented by formula I: AT-CL-R (I), wherein AT is an affinity moiety for a target protein (TP); CL is a cleavable fragment which has a self-cleaving reactivity; and R is a group to be modified to the target protein.