59 results about "Eribulin" patented technology

Disclosed is a compound of formula 1, or a pharmaceutically acceptable salt thereof, where R1, R2, R3, R4, R5, R6, R7, R7′, R8, R9, R10, R11, R12 and R13 are as disclosed herein. Also, disclosed is a process for the preparation of the compound of formula 1, or a pharmaceutically acceptable salt thereof, and intermediates used therein. The compound of formula 1 can be used in the preparation of halichondrin analogs, such as Eribulin; and a process for its preparation from the compound of formula 1 is also disclosed.

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.

The invention relates to Eribulin intermediates and a preparation method thereof. Particularly, the invention relates to compound shown in a formula II, formula III and formula V, wherein Ar is a C1-10 alkyl substituted or alkyloxy substituted or unsubstituted aryl group, R1 and R2 are aldehyde acetal protecting groups or thioacetal protecting groups, R3 is hydrogen or a hydroxy protecting group,and X is halogen or a leaving group. The invention particularly relates to the preparation method of the compounds shown in the formula II, formula III and formula V. The preparation method has the advantages of mild reaction conditions, high selectivity, easy purification, low synthesis cost and the like, and is suitable for large-scale production.

The present invention relates to pyran-fused ring compounds, preparation methods thereof and use thereof, especially to pyran-fused ring compounds usable for preparing Halichondrin, Eribulin, or analogues thereof, preparation methods thereof and use thereof. Use of any of the compounds of formula (I) to (XIII) of the present invention in preparation of Halichondrin B, Eribulin, analogues thereof or C1-C13 moieties thereof. Provided in the present invention are intermediates usable for preparing Halichondrin B, Eribulin, or analogues thereof, especially the key product of C1-C13 moieties, preparation methods thereof and use thereof. The starting material for the synthesis pathway of the present invention is inexpensive and readily available with sustainable source and reliable quality. Since the structural characteristics of the reactants of theirself are made full use in choosing the method of constructing the chiral centers, the efficiency in the synthesis is considerably increased, the difficulty in and the risk on quality control of the product are reduced; and using a highly toxic and expensive high-valent osmium catalyst is avoided, which have the cost and environmental friendliness significantly improved.

The invention provides methods and compositions for use in treating diseases associated with excessive cellular proliferation, such as 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).