(R)-1-((11Bs,12S,14Ar)-13-Methoxy-2,3,5,6,11B,12-Hexahydro-1H-[1,3]Dioxolo[4',5':4,5]Benzo[1,2-D]Cyclopenta[b]Pyrrolo[1,2-A]Azepin-12-yl) 4-Methyl 2-(4-(Benzyloxy)-4-Methylpent-2-Yn-1-yl)-2-Hydroxysuccinate Hydrochloride置于氢气,Palladium(II) Hydroxide,三乙胺,溶剂黄146体系中,用 甲醇 用作溶剂,29.0~31.0 °C,115.12 Kpa 条件下,以57%的收率获得高三尖杉酯碱 参考文献: Methods And Intermediates For The Preparation Of Omacetaxine And Cephalotaxine Derivatives Thereof[fr] Méthodes Et Intermédiaires Pour La Préparation D'Omacétaxine Et De Dérivés De Céphalotaxine Associés 标题: Methods And Intermediates For The Preparation Of Omacetaxine And Cephalotaxine Derivatives Thereof[fr] Méthodes Et Intermédiaires Pour La Préparation D'Omacétaxine Et De Dérivés De Céphalotaxine Associés 摘要:本发明涉及用于制备omacetaxine和cephalotaxine衍生物的方法和中间体.所得产品在治疗增殖性疾病和传染性疾病方面具有用途.
专利号:WO-2018019549-A1 优先权日:2016-07-28 标 题:Dioxolanone intermediate useful in the synthesis of homoharringtonine 发明人:ALLEGRINI PIETRO; CATTANEO CRISTIAN; CICERI DANIELE; GAMBINI ANDREA; PETERLONGO FEDERICO; CERISOLI LUCIA; LOMBARDO MARCO 权利人:INDENA SPA 摘要:The invention discloses 2-((2R,4R)-4-(4-(benzyloxy)-4-methylpent-2-yn-1-yl)-2-(tert-butyl)-5-oxo-1,3-dioxolan-4-yl)acetic acid of formula (XIX), a process for its preparation and processes for its conversion into enantiomerically pure (R)-2-(2-methoxy-2-oxoethyl)-6,6-dimethyltetrahydro-2H-pyran-2-carboxylic acid of formula (I), a molecule useful for the synthesis of Homoharringtonine.
专利号:US-11850250-B2 优先权日:2020-03-30 标 题:Use of homoharringtonine in preparation of betacoronavirus replication inhibitor in human 发明人:WU CHUNGL; WEN HAIJUN 权利人:UNIV SUN YAT SEN; Hangzhou minsheng pharmaceutical co ltd 摘要:Disclosed is a use of homoharringtonine (HHT) in preparation of a drug against betacoronavirus infection, a use of homoharringtonine in preparation of a betacoronavirus replication inhibitor in human, and a formulation and a method for treating a disease caused by betacoronavirus. Through research, the HHT is found to not only have a good inhibitory effect on the first step of protein synthesis, but also have an unexpected inhibitory effect on each step of protein synthesis elongation, and can better inhibit the synthesis of long proteins. Because betacoronaviruses have longer ORFs and are more sensitive to the HHT, the HHT has a better replication inhibition effect on the betacoronaviruses, thus providing a feasible solution for controlling the replication of coronaviruses. The effects of the HHT on treating diseases caused by the betacoronaviruses including SARS-CoV-2 are confirmed for the first time by cell experiments and animal models.
专利号:US-8008459-B2 优先权日:2001-01-25 标 题 :Concatemers of differentially expressed multiple genes 发明人:GOLDSMITH NEIL; SORENSEN ALEXANDRA M P SANTANA; NIELSEN SOREN V S; NAESBY MICHAEL 权利人:EVOLVA SA 摘要:In the present invention are disclosed concatemers of concatenated expression cassettes and vectors that enable the synthesis of such concatemers. The concatemer comprises in the 5′→3′ direction a cassette of nucleotide sequence of the general formula [rs2-SP-PR-X-TR-SP-rs1]n wherein rs1 and rs2 together denote a functional restriction site, SP individually denotes a spacer of at least two nucleotide bases, PR denotes a promoter, capable of functioning in a cell, X denotes an expressible nucleotide sequence, TR denotes a terminator, and SP individually denotes a spacer of at least two nucleotide bases, and n>/=2, and wherein at least a first cassette is different from a second cassette. The main purpose of these concatemers is the controllable and co-ordinated expression of large numbers of heterologous genes in a single host. Furthermore, the invention relates to a concatemer of cassettes of nucleotide sequences and a method for preparing the concatemers. In a further aspect, the invention relates to transgenic host cells comprising at least one concatemer according to the invention, as well as to a method for preparing the transgenic host cells. Finally, the invention relates to a vector comprising a cassette of nucleotides, a method for preparing said vector, a nucleotide library comprising at least two primary vectors each comprising a cassette of nucleotides, a method for preparing the library.
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:US-2018140724-A1 优先权日:2015-05-27 标 题:Tumor Deliverable Iron and Protein Synthesis Inhibitors as a New Class of Drugs for the Diagnosis and Treatment of Cancer 发明人:DENG CHANGCHUN; LIPSTEIN MARK; O'CONNOR OWEN A 权利人:DENG CHANGCHUN; LIPSTEIN MARK; OCONNOR OWEN A; UNIV COLUMBIA 摘要:Tumor deliverable iron (TDI) drugs and pharmaceutical compositions and kits comprising them are provided and methods for delivering iron to tumors specifically, either intracellularly or extracellularly. As a result, TDI drugs are useful as a sensitizer for radiation therapy, radio-diagnosis, and chemotherapy, and are of interest. In other embodiments, tumor deliverable protein synthesis inhibitors (TDPSI) are provided and can be delivered to tumors, but not normal cells. These TDPSI drugs and pharmaceutical compositions and kits comprising them are useful for their treatment of cancer, either alone or in combination with other active anti-cancer drugs.
专利号:US-2023391824-A1 优先权日:2021-02-08 标题:Rationale, design, synthesis and validation of a small molecule anticancer agent 发明人:JAIN MOHIT; NARENDRAN ARUMUGAVADIVEL 权利人:NARENDRAN ARUMUGAVADIVEL 摘要:LIN28 is an RNA binding protein that binds and inhibits the expression and maturation of Iet7 microRNA that carries key tumor suppressor functions. Thus, LIN28 is a feasible and effective molecular target for directed inhibition with the potential to provide therapeutic benefit to a diverse group of aggressive malignancies. The present disclosure relates generally to the Rationale, Design, Synthesis and Validation of a Novel Small Molecule Inhibitor of LIN28, coined Compound of formula (I), for the Treatment of Adult and Pediatric Malignancies. In addition, indications of this agent to block cancer metastasis, inhibit cancer stem cells to prevent relapse, and to synergize with immunotherapy, chemotherapy and radiotherapy are also been described.
1: Klanova M, Andera L, Brazina J, Svadlenka J, Benesova S, Soukup J, Prukova D, Vejmelkova D, Jaksa R, Helman K, Vockova P, Lateckova L, Molinsky J, Maswabi BC, Alam M, Kodet R, Pytlik R, Trneny M, Klener P. Targeting of BCL2 Family Proteins with ABT-199 and Homoharringtonine Reveals BCL2- and MCL1-Dependent Subgroups of Diffuse Large B-Cell Lymphoma. Clin Cancer Res. 2016 Mar 1;22(5):1138-49. doi: 10.1158/1078-0432.CCR-15-1191. Epub 2015 Oct 14. doi: 10.1111/bph.13359. Epub 2015 Dec 1. Epub 2015 Nov 5. 4: Wu L, Li X, Chang C, Xu F, He Q, Wu D, Zhang Z, Su J, Zhou L, Song L, Chao X, Zhao Y. Efficacy and toxicity of decitabine versus CHG regimen (low-dose cytarabine, homoharringtonine and granulocyte colony-stimulating factor) in patients with higher risk myelodysplastic syndrome: a retrospective study. Leuk Lymphoma. 2015 Nov 16:1-8. [Epub ahead of print] doi: 10.1002/chir.22451. Epub 2015 May 21.
合成参考文献
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