4α-Acetoxy-2α-Benzoyloxy-5β,20-Epoxy-1β,13α-Dihydroxy-7β,10β-Dimethoxy-9-Oxo-11-Taxen-13α-Yl (2R,4S,5S)-3-Tert-Butoxycarbonyl-2-(4-Methoxyphenyl)-4-Phenyl-1,3-Oxazolidine-5-Carboxylate置于盐酸体系中,用 乙酸乙酯 用作溶剂,以71%的收率获得卡巴他赛 参考文献: Processes For The Preparation Of Cabazitaxel Involving C(7)-Oh And C(13)-Oh Silylation Or Just C(7)-Oh Silylation[fr] Procédés De Préparation Amélioré De Préparation De Cabazitaxel Impliquant La Silylation C(7)-Oh Et C(13)-Oh Ou Uniquement La Silylation C(7)-Oh 标题: Processes For The Preparation Of Cabazitaxel Involving C(7)-Oh And C(13)-Oh Silylation Or Just C(7)-Oh Silylation[fr] Procédés De Préparation Amélioré De Préparation De Cabazitaxel Impliquant La Silylation C(7)-Oh Et C(13)-Oh Ou Uniquement La Silylation C(7)-Oh
专利号:WO-2024220674-A1 优先权日:2023-04-18 标题:Timescale-guided microfluidic synthesis of polyphenol-iron iii network nanocapsules of hydrophobic drugs 发明人:YEO YOON; HAN BUMSOO; SHEN YINGNAN 权利人:PURDUE RESEARCH FOUNDATION 摘要:A scalable method of continuous microfluidic synthesis of tannic acid-iron III (TA-FeIII) network (TFN) nanocapsules of a hydrophobic drug; a scalable method of continuous microfluidic synthesis of epigallocatechin-3-gallate iron III (EGCG-FeIII) network, (EFN) nanocapsules; hydrophobic drug nanocapsules synthesized in accordance with the method; and a method of administering a hydrophobic drug to a patient in need thereof by administering to the patient the hydrophobic drug nanocapsules.
专利号:WO-2024104433-A9 优先权日:2022-11-16 标 题:Use of galectin-1 as immune checkpoint in preparation of tumor immunotherapy medicament and medicament 发明人:ZHANG YU; HONG YU; SI XIAOFANG; LIU WENJING; MAI XUEYING 权利人:NAT INSTITUTE OF BIOLOGICAL SCIENCES BEIJING 摘要:Provided are use of galectin-1 (Gal-1) as an immune checkpoint in the preparation of a tumor immunotherapy medicament and the medicament, and provided is a new tumor immunotherapy strategy targeting the new immune checkpoint. Lactose and a derivative thereof can inhibit the immune checkpoint by competing Gal-1 on the surfaces of a cancer cell and an immune cell, and do not have significant toxic and side effects. Knocking out B4GATL1 to reduce protein galactosylation can significantly reduce the level of Gal-1 transferred from a tumor to a T cell, thereby enhancing the activation and function of the T cell. In addition, a lactose synthetase component LALBA is overexpressed in a mouse tumor, and de novo synthesis of lactose in a tumor microenvironment can be realized, such that an immune response mediated by a CD8+ T cell is enhanced. In combination with the anti-tumor effect and economic cost of lactose, a wide and feasible idea is provided for cancer treatment.
专利号:WO-2022227554-A1 优先权日:2021-04-30 标题 :Larotaxel-fatty alcohol small molecule prodrug and construction of self-assembling nanoparticle thereof 发明人:LUO CONG; WANG YONGJUN; YANG JINCHENG; MA HONGDA; SUN JIN; HE ZHONGGUI; FENG YAO; MA ZHINING 权利人:SUZHOU YUTAI PHARMACEUTICAL TECH CO LTD 摘要:The synthesis of a larotaxel-fatty alcohol small molecule prodrug with a tumor reduction response characteristic and the construction of a self-assembling nanoparticle, and the use thereof in the preparation of a drug delivery system. Provided is a larotaxel-stearyl alcohol small molecule prodrug, which is prepared into a larotaxel-fatty alcohol prodrug nanoparticle. The larotaxel-fatty alcohol prodrug nanoparticle can be a non-PEGylated larotaxel-fatty alcohol prodrug nanoparticle, a PEG-modified larotaxel-fatty alcohol prodrug nanoparticle, a drug-loaded larotaxel-fatty alcohol prodrug nanoparticle, and an active targeting larotaxel-fatty alcohol prodrug nanoparticle. The larotaxel-fatty alcohol prodrug has few synthetic steps, a simple process, reduced synthesis costs, a high yield and easy purification, and the nanoparticle formed by the self-assembly of the larotaxel-fatty alcohol small molecule prodrug has an ultra-small particle size, which reduces the toxicity and side effects while improving the curative effect of larotaxel.
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-9487496-B2 优先权日:2012-11-09 标 题 :Process for the preparation of cabazitaxel and its intermediates 发明人:LOURDUSAMY METTILDA; RADU IOAN IOSIF; SAXENA RAHUL CHANDRASHAYI; PATEL RAGHVENDRA JAYANTIBHAI; SHAH SANDEEP BACHUBHAI 权利人:INTAS PHARMACEUTICALS LTD 摘要:The present invention relates to a novel process for preparation of cabazitaxel (I) starting from 10-Deacetyl baccatin or derivative that involves methylation of 7, 10 —OH groups. Also provided is a novel process using chiral bis-lactam linker for the synthesis of cabazitaxel.
专利号:US-10029014-B2 优先权日:2013-09-10 标题:Synthesis of novel asymmetric bow-tie PAMAM dendrimer-based conjugates for tumor-targeting drug delivery 发明人:OJIMA IWAO; WANG TAO; TENG YU-HAN 权利人:UNIV NEW YORK STATE RES FOUND 摘要:The present disclosure relates to a dendrimer-based conjugate of the formula V m -D-C-D′-(T-F) n , which is useful for tumor targeting drug delivery. The use of asymmetric dendrimers allow for specific targeting as well as synthetic reproducibility.
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