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Last Updated: April 26, 2024

Claims for Patent: 8,236,850


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Summary for Patent: 8,236,850
Title:Dimeric derivatives of artemisinin and application in anticancer therapy
Abstract: The present invention relates to dimeric derivatives of 10-trifluoromethylated artemisinin of formula (I): or a pharmaceutically acceptable salt thereof with B.sub.1 and B.sub.2 selected from C.dbd.O, CHOH and CH.sub.2, as well as to their use in treating cancer and to their preparation method. ##STR00001##
Inventor(s): Begue; Jean-Pierre (Paris, FR), Bonnet-Delpon; Danielle (Paris, FR), Crousse; Beno t (Igny, FR), Grellepois; Fabienne (Reims, FR), Chollet; Constance (Montrouge, FR), Fahy; Jacques (Labruguiere, FR), Mordant; Celine (Saint Julien En Genevois, FR)
Assignee: Pierre Fabre Medicament (Boulogne-Billancourt, FR) Centre National de la Recherche Scientifique (Paris, FR) Universite Paris-Sud 11 (Orsay, FR)
Application Number:12/808,828
Patent Claims:1. Dimeric derivative of 10-trifluoromethylated artemisinin of formula(I): ##STR00071## or a pharmaceutically acceptable salt thereof, for which: B.sub.1 and B.sub.2 are identical or different and selected from C.dbd.O, CHOH and CH.sub.2, and A represents: a divalent group selected from --S--, and --S--S--.

2. The dimeric derivative according to claim 1, wherein B.sub.1 and B.sub.2 are identical or different and selected from C.dbd.O and CH.sub.2.

3. The dimeric derivative according to claim 2, wherein B.sub.1 and B.sub.2 each represent a CH.sub.2 group.

4. The dimeric derivative according to claim 1, wherein it is selected from the following compounds: ##STR00072##

5. A pharmaceutical composition comprising at least one dimeric derivative according to claim 1 and at least one pharmaceutically acceptable carrier.

6. The pharmaceutical composition according to claim 5, further comprising another active ingredient.

7. The pharmaceutical composition according to claim 6, wherein the other active ingredient is selected from 6-mercaptopurine, fludarabine, cladribine, pentostatin, cytarabine, 5-fluorouracil, gemcitabine, methotrexate, raltitrexed, irinotecan, topotecan, etoposide, daunorubicin, doxorubicin, epirubicin, idarubicin, pirarubicin, mitoxantrone, chlormethine, cyclophosphamide, ifosfamide, melphalan, chlorambucil, busulfan, carmustine, fotemustine, streptozocin, carboplatin, cisplatin, oxaliplatin, procarbazine, dacarbazine, bleomycin, vinblastine, vincristine, vindesine, vinorelbine, paclitaxel, docetaxel, L-asparaginase, flutamide, nilutamide, bicalutamide, cyproterone acetate, triptorelin, leuprorelin, goserelin, buserelin, formestane, aminoglutethimide, anastrazole, letrozole, tamoxifen, octreotide and lanreotide.

8. A method for treating cancer comprising the administration of an effective amount of a dimeric derivative according claim 1 to a person in need thereof.

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