CAS: 146464-95-1; (2S)-2-(4-(1-(2,4-Diaminopteridin-6-yl)Pent-4-Yn-2-yl)Benzamido)Pentanedioic Acid

上下游产品

methyl 4-(2-methoxy-2-oxoethyl)benzoate diethyl-L-glutamate hydr°Chloride α-propargylhomoterephthalic acid dimethyl ester

2,4-二氨基-Alpha-(4-羧基苯基)-Alpha-2-丙炔基-6-蝶啶丙酸置于n-甲基吡咯烷酮,盐酸,1-羟基苯并三唑,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,N,N-二异丙基乙胺,Potassium Hydroxide,Sodium Hydroxide体系中,用 N-甲基吡咯烷酮,乙醇,二氯甲烷,水 用作溶剂,化学反应 20.0H,反应生成10-炔丙基-10-去氮杂氨基蝶呤
参考文献: Processes And Intermediates For Preparing Pralatrexate[fr] Procédés Et Intermédiaires De Préparation Du Pralatrexate
标题: Processes And Intermediates For Preparing Pralatrexate[fr] Procédés Et Intermédiaires De Préparation Du Pralatrexate
摘要:本申请描述了制备和纯化普拉曲塞的过程,以及这些过程中的中间体,普拉曲塞中间体的盐和固态形式.

专利信息

专利号:WO-2013177713-A1
优先权日:2012-05-31
标题 :Process for preparation of an antifolate agent
发明人：GIUST WALTER; BURTON RYAN; GORIN BORIS; CLAYTON JOSHUA
权利人:ALPHORA RES INC
摘要:The specification relates to a process for preparation of an antifolate compound of formula 7, such as Pralatrexate. Also, disclosed are intermediates and processes for preparation of intermediates useful in the preparation of the antifolate compound. The substituents Y, Z, R, R 1 and R 2 are as described herein. The processes and intermediates can provide an alternate route to the synthesis of the antifolate compound. Further, the processes can help to avoid distillation or evaporation of high boiling point solvents, chromatographic purification and use of hazardous combination of solvents; and can also provide a product having high purity, all of which are desirable for synthesis on a large scale.

专利号:WO-2013164856-A1
优先权日:2012-05-04
标题 :A process for preparing intermediates of 10-propargyl-10-deazaaminopterin (pralatrexate) synthesis and the intermediates thereof
发明人：ALLA RAMA RAO VENKATA; RAMARAO CHANDRASHEKAR; MICHEL PATRICK THOMAS; NITLIKAR LAKSHMIKANT HANUMANTHRAO; KALAM BHUPATHI REDDY; DUDUKA RAMPRASAD
权利人:AVRA LAB PRIVATE LTD; ALLA RAMA RAO VENKATA; RAMARAO CHANDRASHEKAR; MICHEL PATRICK THOMAS; NITLIKAR LAKSHMIKANT HANUMANTHRAO; KALAM BHUPATHI REDDY; DUDUKA RAMPRASAD
摘要:A process for preparation of 4-(1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl)benzoic acid and other key intermediates in synthesis of 10-propargyl-10-deazaaminopterin (Pralatrexate) and the intermediates thereof. The 10-propargyl-10-deazaaminopterin (Pralatrexate) is obtained by peptide formation and ester hydrolysis of the intermediate compound 4-(1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl)benzoic acid by methods known in the art.

专利号:US-2022233673-A1
优先权日:2019-06-04
标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF
发明人：BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M
权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND
摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.

专利号:US-2022118094-A1
优先权日:2019-02-21
标题:Synthesis of biomimetic cell wall structure
发明人：WANG YONG; SHI PENG
权利人:PENN STATE RES FOUND
摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.

专利号:WO-2023245091-A1
优先权日:2022-06-15
标题 :Pyridazinone-derived compounds for the modulation of myc and for medical uses
发明人：ADANVE BERTRAND; NG YAO ZONG; LAI JONATHAN
权利人:GENETIC INTELLIGENCE INC
摘要:Compositions, systems, and methods are described herein for the modulation, and in particular the reduction or inhibition, of expression or activity of MYC in a cell, animal or human subject. Such compositions, systems, and methods are useful to prevent, ameliorate, or treat diseases, including cell proliferation diseases and disorders such as cancer, particularly MYC-driven cancer. Compositions are described comprising a compound of formula (I), as well as pharmaceutical compositions or medicaments thereof. Also described are methods of use of such compositions to treat, prevent, or ameliorate diseases, including cell proliferation diseases and disorders such as cancer, in particular MYC-driven cancer. Compositions comprising conjugates and complexes of a compound of formula (I) are also described, which are also useful in the methods described herein. Methods are described comprising the use of a compound of formula (I), or pharmaceutical compositions thereof, for the reduction or inhibition of MYC expression or activity, and/or for achieving one or more desirable phenotypic outcomes such as, for example, decrease in cancer cell growth or proliferation, decrease in cancer cell viability, decrease in tumor volume (i.e., tumor regression), decrease in cancer metastasis, increase in animal or human survival, or other desired outcome with respect to particular phenotypes (e.g., body weight, metabolism, etc.). Related medicaments, kits, and methods of delivery of such compositions are described. Methods are also described for the development, manufacture, and/or synthesis of a compound of formula (I), as well as pharmaceutical compositions thereof. Furthermore, methods for diagnostics and testing comprising detecting MYC expression or activity levels, as well as compositions comprising kits for diagnostics and testing, are described.

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.