CAS: 75747-14-7; (4E,6Z,8S,9S,10E,12S,13R,14S,16R)-19-(Allylamino)-13-Hydroxy-8,14-Dimethoxy-4,10,12,16-Tetramethyl-3,20,22-Trioxo-2-Azabicyclo[16.3.1]Docosa-1(21),4,6,10,18-Pentaen-9-Yl Carbamate

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CAS号107-11-9 丙烯胺 | CAS号30562-34-6 格尔德霉素 | CAS号857402-23-4 瑞他霉素 | CAS号64202-81-9 17-氨基格尔德霉素

📜丙烯胺,格尔德霉素 以 氯仿 作为反应溶剂,化学反应 18.0H,以99%的收率获得产物替拉替尼
参考文献: Geldanamycin And Derivatives Inhibit Cancer Invasion And Identify Novel Targets[fr] Geldanamycine Et Ses Derives Pouvant Inhiber Une Proliferation Cancereuse Et Identifier De Nouvelles Cibles
标题: Geldanamycin And Derivatives Inhibit Cancer Invasion And Identify Novel Targets[fr] Geldanamycine Et Ses Derives Pouvant Inhiber Une Proliferation Cancereuse Et Identifier De Nouvelles Cibles
摘要:盖尔达霉素衍生物可以在飞托摩尔浓度下阻断upa-纤溶酶网络,抑制胶质母细胞瘤细胞和其他肿瘤的生长和侵袭,潜在地是高活性的抗癌药物.已披露了盖尔达霉素(ga)和各种17-氨基-17-去甲氧基盖尔达霉素衍生物,可以在飞托摩尔水平下阻断hgf/sf介导的met酪氨酸激酶受体依赖的upa激活.其他吖丝霉素类化合物(马克贝辛i和ii),盖尔达霉素衍生物和雷地可(radicicol)需要更高几个数量级(>=nm)的浓度才能实现这种抑制作用.经测试的化合物的抑制活性与该类药物已知结合到hsp90的能力不符,表明存在一种新的靶标,用于抑制hgf/sf介导的肿瘤发展事件.公开了使用这类化合物来抑制癌细胞活动和治疗肿瘤的方法.用这些高活性化合物的低剂量进行治疗为治疗各种表达met的肿瘤提供了一种选择,特别是侵袭性脑癌,可以单独使用或与常规手术,化疗或放疗结合使用.

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:US-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人：MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

专利号:US-8314132-B2
优先权日:2008-04-30
标题:5-aryl-4-(5-substituted 2,4-dihydroxyphenyl)-1,2,3-thiadiazoles as inhibitors of Hsp90 chaperone and the intermediates for production thereof
发明人：MATULIS DAUMANTAS; CIKOTIENE INGA; KAZLAUSKAS EGIDIJUS; MATULIENE JURGITA
权利人:MATULIS DAUMANTAS; CIKOTIENE INGA; KAZLAUSKAS EGIDIJUS; MATULIENE JURGITA; BIOTECHNOLOGIJOS INST
摘要:Invention is related to novel compounds -5-aryl-4-(5-substituted 2,4-dihydroxyphenyl)-1,2,3-thiadiazoles with general formula (I). The compounds can be used in biomedicine as active ingredients in pharmaceutical formulations, because they inhibit Hsp90 chaperone which participate in cancer progression. This invention is also related to new intermediate compounds which are used for the synthesis of thiadiazoles of general formula (I).

专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人：YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

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:US-2008227851-A1
优先权日:2007-03-12
标题 :Laulimalide and laulimalide analogs
发明人：WENDER PAUL A
权利人:WENDER PAUL A
摘要:Novel laulimalide analogs, methods for the treatment of proliferative disease and processes for the synthesis of laulimalide and novel laulimalide analogs are described.