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59 results about "Eribulin" patented technology

Eribulin is used to treat certain types of cancer (breast, liposarcoma).

Palladium-mediated ketolization

Provided herein are palladium-mediated coupling reactions useful in the preparation of ketone-containing organic molecules. The provided methods can be used for the preparation of natural products and pharmaceutical agents, including Eribulin, halichondrins, and analogs thereof. The present invention also provides novel halichondrin analogs which can be prepared via the palladium-mediated coupling reactions. The novel halichondrin analogs can be used in the prevention and / or treatment of diseases or conditions (e.g., proliferative diseases such as cancer).
Owner:PRESIDENT & FELLOWS OF HARVARD COLLEGE

Intermediate for preparing eribulin and preparation method thereof

The invention provides an intermediate for preparing eribulin and a preparation method thereof. A novel intermediate is introduced into the eribulin synthesis route, which comprises more than 60 steps. The advantages of various routes in the prior art are integrated so as to industrially produce (macro-cyclic ketone) eribulin, which is difficult to synthesize.
Owner:CHIA TAI TIANQING PHARMA GRP CO LTD

Method for preparing eribulin and intermediate thereof

The present invention relates to a method for preparing eribulin and an intermediate thereof. In particular, the invention relates to a method for preparing a compound of formula 5, R3 is selected from aldehyde or OR1, n=0 or 1, R1 is a hydroxy protecting group, and preferably the hydroxy protecting group is selected from tert-butyldimethylsilyl, tert-butyldiphenylsilyl, p-methoxybenzyl or benzyl.The invention also provides a method for preparing halichondrin and derivatives thereof such as the eribulin from the compound of formula 5.
Owner:JIANGSU HENGRUI MEDICINE CO LTD +1

Preparation method of eribulin intermediate

The invention relates to a preparation method of an eribulin intermediate. Specifically, the invention relates to a compound shown as a formula IV; R1 represents a hydroxyl protecting group, preferably (C1-10 alkyl or aryl) 3 silicon alkyl, more preferably TBDPS; R2 represents a hydroxyl protecting group, preferably benzyl or (C1-10 alkyl or aryl) 3 silicon alkyl, and more preferably benzyl or TBS. The invention particularly relates to the preparation method of the compound shown as formula IV. The method has the advantages of mild reaction conditions, simple operation, low cost for synthesis and is applicable to mass production.
Owner:UNITRIS BIOPHARMA

Eribulin intermediate and preparation method thereof

The invention relates to an eribulin intermediate and a preparation method thereof. In particular, the invention relates to a compound represented by a formula II shown in the description, wherein X is a halogen or halogenoid group, preferably chloro, bromo, iodo, or a trifluoromethanesulfonate group, and more preferably the iodo; R<1> and R<2> are acetal protecting groups or thioacetal protectinggroups, and independently C1-10 alkyloxy or C1-10 alkyl thiol, or the R<1> and the R<2> are combined to form a cyclic acetal or cyclic thioacetal structure. The R<1> and the R<2> are preferably cyclic acetal or cyclic thioacetal substituents, and more preferably a substituted or unsubstituted ethylene glycol acetal structure or a substituted or unsubstituted propylene glycol acetal structure. Theinvention particularly relates to the preparation method of the compound represented by the formula II. The method disclosed by the invention has the advantages of mild reaction conditions, high selectivity, easy purification, low synthetic costs and the like, and is suitable for large-scale production.
Owner:SELECTION BIOSCI LLC

Use of eribulin and mtor inhibitors as combination therapy for the treatment of cancer

Methods for treating cancer (e.g., breast cancer, lung cancer, pancreatic cancer, primitive neuroectodermal tumors, lung cancer, ovarian cancer, endometrial cancer, pharyngeal cancer, esophageal cancer, and sarcoma) in a subject (such as an human patient) in need thereof by administering eribulin (e.g., eribulin mesylate, i.e., E7389, Halaven) in combination with one or more mammalian target of rapamycin (mTOR) inhibitors (e.g., everolimus, ridaforolimus, and temsirolimus), and kits therefor are provided.
Owner:EISIA R&D MANAGEMENT CO LTD

Method for preparing eribulin and intermediate thereof

The present invention relates to a method for preparing eribulin and an intermediate thereof. In particular, the invention relates to a method for preparing formula 1 compound, (3R)-2,4-dihalo-3-methylbut-1-ene. The invention also provides a method for preparing halichondrin and derivatives thereof such as the eribulin from the formula 1 compound.
Owner:JIANGSU HENGRUI MEDICINE CO LTD +1

Synthesis method of eribulin intermediate

The invention discloses a synthesis method of an eribulin intermediate. The synthesis method mainly comprises the following steps: taking a compound shown as a formula 1 as a raw material to react with N-iodosuccinimide and then carrying out hydroxyl protection reaction to obtain a target product, namely a compound shown as a formula 4. The synthesis method provided by the technical scheme has theadvantages of simple and convenient operation steps, moderate reaction conditions and a few of byproducts in a reaction process; compared with the prior art, the productivity and the yield of the target product are remarkably improved and the synthesis method is very suitable for industrial production.
Owner:WUYAN PHARM TECH (SHANGHAI) CO LTD

Eribulin and detection method of related substance in preparation containing Eribulin

The invention discloses Eribulin and a detection method of related substance in a preparation containing the Eribulin. The method specifically comprises a step of quickly and accurately detecting theimpurity of the Eribulin and the degradation product condition by adopting a reverse-phase high-performance liquid chromatography, and the interference on the product purity by various impurities produced in the synthesis and preparation process is solved, and the quality of the raw medicine and the preparation can be comprehensively and reliably controlled. The method disclosed by the invention is simple in operation, good in sensitivity, good in separation degree, and capable of providing an effective analysis method for controlling the product quality.
Owner:SHANDONG ACADEMY OF PHARMACEUTICAL SCIENCES

Preparation method of eribulin intermediate

The invention provides a preparation method of an eribulin intermediate. According to the preparation method, a brand-new route and an intermediate are adopted to prepare a key intermediate ERB, compared with the prior art, the reaction route is greatly simplified, the reaction yield and the selectivity of a new chiral center of a target product are remarkably improved; and the preparation methodis especially suitable for industrial application.
Owner:NANTONG NUOTAI BIOLOGICAL PHARMA CO LTD +1

Synthetic method of eribulin intermediate ER806047

The invention discloses a synthetic method of an eribulin intermediate ER806047 shown as a formula (b), comprising the following steps of: using 1, 2-O-isopropylidene-alpha-D-glucuronic acid-6, 3-lactone as a raw material, and carrying out one-step oxidation-reduction reaction for dehydroxylation synthesis of the eribulin intermediate ER806047. The synthetic method has the advantages of short reaction route, high yield, simplicity and convenience in operation, low cost, suitability for industrial production and the like. The structure of the eribulin intermediate ER806047 disclosed by the invention is as shown in the specification.
Owner:SHANGHAI MAOSHENG KAIHUI TECH CO LTD

Liposome composition

The present invention provides a novel liposome composition containing eribulin or its pharmacologically permissible salt, and its method of manufacture.
Owner:EISIA R&D MANAGEMENT CO LTD

Intermediate for preparing eribulin, and preparation method thereof

The invention relates to a preparation method of an eribulin intermediate, concretely relates to a compound represented by formula III, formula IV or formula X (R<1> is an alkyl group or a substitutedor unsubstituted aryl group), and especially relates to a preparation method of the compound represented by formula III, formula IV or formula X. The method has the advantages of mild reaction conditions, simplicity in operation, and low synthesis cost, and is suitable for large-scale production.
Owner:SELECTION BIOSCI LLC

Method for preparing eribulin intermediate

Intermediates used in the synthesis of Eribulin and methods for preparing the intermediates are described. For example, a compound of formula IV and a method for preparing the compound are described, wherein R1 is a hydroxyl protecting group, preferably a (C1-10 alkyl group or aryl group)3silyl group, and more preferably tert-butyldiphenylsilyl (TBDPS); and R2 is a hydroxyl protecting group, preferably a benzyl group or (C1-10 alkyl group or aryl group)3silyl group, and more preferably a benzyl group or tert-butyldimethylsilyl (TBS). A method for preparing Eribulin using the intermediates is also provided. The method has the advantages of moderate reaction conditions, is simple to execute and low cost, and is thus suitable for mass production.
Owner:UNITRIS BIOPHARMA

Use of eribulin and poly (ADP ribose) polymerase (PARP) inhibitors as combination therapy for the treatment of cancer

The invention features methods for treating cancer in a patient in need thereof by administering eribulin, in combination with one or more PARP inhibitors, and, optionally, a platinum-based antineoplastic drug, and kits therefor. The invention is based in part on the observation that combinations of eribulin mesylate, a PARP inhibitor (e.g., E7449), and, optionally, a platinum-based antineo-plastic drug (e.g., carboplatin), show improved (e.g., synergistic) antitumor effects. Therefore, the present invention features methods of preventing and treating cancer (e.g., homologous recombination (HR)-deficient cancer by the use of combinations of eribulin (e.g., eribulin mesylate) and one or more PARP inhibitors (e.g., E7449 or a pharmaceutically acceptable salt thereof (e.g., the tartrate salt), optionally in combination with a platinum-based antineoplastic drug (e.g., carboplatin).
Owner:EISIA R&D MANAGEMENT CO LTD

Use of eribulin in the treatment of cancer

The invention features methods and kits for use in treating cancer in a patient in need thereof by administering eribulin or a pharmaceutically-acceptable salt thereof (e.g., eribulin mesylate) prior to a second agent.
Owner:EISIA R&D MANAGEMENT CO LTD

Intermediate of eribulin and preparation method therefor

Disclosed are an intermediate of Eribulin and a preparation method therefor. In particular, disclosed are compounds as represented by formula II, formula III and formula V and a preparation method therefor. Ar is C1-10 alkyl substituted, alkyloxy substituted or unsubstituted aryl; R1 and R2 is an acetal protecting group or a thioacetal protecting group; R3 is hydrogen or a hydroxyl protecting group; and X is halogen or a leaving group. The preparation method therefor has the advantages of mild reaction conditions, high selectivity, easy purification, low synthesis cost and the like, being suitable for large scale production.
Owner:SELECTION BIOSCI LLC
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