CAS: 646502-53-6; 4-((S)-2-((S)-2-(6-(2,5-Dioxo-2,5-Dihydro-1H-Pyrrol-1-yl)Hexanamido)-3-Methylbutanamido)-5-Ureidopentanamido)Benzyl ((S)-1-(((S)-1-(((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-

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-2024184661-A1
优先权日:2023-03-09
标 题 :Synthesis of bicycle toxin conjugates, and intermediates thereof
发明人：LIMB DARREN; MOSS WILLIAM; WITTY DAVID; ZHANG JIE; LIN JINGUANG
权利人:BICYCLETX LTD
摘要:The present invention relates methods of preparing Bicycle toxin conjugates, and intermediates thereof.

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.

专利号:US-2025170267-A1
优先权日:2022-02-28
标 题 :Antibody-drug conjugate precursor and intermediate for synthesis thereof
发明人：TSUZAKI YASUNORI; MIZUNO GEN; KASHIWAGI TAKAMASA; TANAKA MASAYUKI; SHIMIZU HAYATO; NONOUCHI SHIMPEI; MATSUSHITA TAKASHI; KIMURA TOMIO
权利人:UBE CORP
摘要:A method for improving the stability of an antibody-drug conjugate in a living body, and a conjugate precursor for producing a stabilized antibody-drug conjugate. An antibody-drug conjugate precursor represented by the following general formula (I) or a salt thereof, a synthetic intermediate thereof or a salt thereof, n Z-L-D  (I)n n where Z is a reactive group which can react with a functional group present in an antibody or a modified antibody; D is an antitumor drug residue in which one hydrogen atom or one hydroxy group is removed from any position of an antitumor drug molecule or an analog thereof or a derivative thereof; L is a linker which links Z to D; and at least any one of D and L has one or more lactonyl group(s) at any position(s) as substituent(s) or protecting group(s).

专利号:US-2022047711-A1
优先权日:2018-12-10
标题 :Photocrosslinking peptides for site specific conjugation to fc-containing proteins
发明人：SADOWSKY JACK; ZACHARIAS NEELIE TYANA
权利人:GENENTECH INC
摘要:Provided herein are peptides having a photocrosslinking moiety useful for the synthesis of antibody-drug conjugates as well as methods of making and using such conjugates.