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US 10,766,873 B2Granted
Zuclopenthixol hydrochloride derivatives and Ebselen derivatives as ErbB2 inhibitors
AssigneesCentre National de la Recherche Scientifique (CNRS), Institut National De La Sante Et De La Recherche Medicale (Inserm), Universite Paris Descartes
InventorsSandrine Bourdoulous, Camille Faure
Life of this patent
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Abstract
The present invention relates to compounds of the following general formula (I) or (II): or a pharmaceutically acceptable salt and/or solvate thereof, for use in the treatment and/or in the prevention of ErbB2 dependent cancers, and pharmaceutical compositions containing such compounds.
Claims14
A method of inhibiting ErbB2 activation in an ErbB2 dependent cancer patient, the method comprising:
- selecting an ErbB2 dependent cancer patient that overexpresses ErbB2;
- and
- administering to the ErbB2 dependent cancer patient an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt and/or solvate thereof for inhibiting ErbB2 activation;
- wherein compound (I) has the general formula:
- wherein:
- the symbol represents a bond in cis or trans configuration;
- X is a sulfur atom;
- R1 is hydrogen atom, halo, —CN, —NO2, —NO, —CHO, —NR7R8, —CO2R9, —SO2R10, —SO2NR11R12, —OR13, —COR14, —SR15, —CONR16R17, —SO2(O)R18 or a group selected from saturated (C1-C6)alkyl, unsaturated (C1-C6)alkyl and aryl, said group being optionally substituted with one or several groups selected from halo, —CF3, —CN and —SO2NR19R20;
- R2 and R3 form together with the nitrogen atom to which they are chemically linked a piperazinyl group substituted with one or several groups selected from halo, —CO2R21 and a (C1-C6)alkyl group, the (C1-C6)alkyl group being optionally substituted with one or several groups selected from halo, —OR22, —SR23, —S(O)R24, —SO2R25, —SO2NR26R27, —OC(O)R28, —NR29COR30, —NR31CONR32R33, —NR34C(O)OR35, —CO2R36, —CONR37R38, —OCO2R39, —OCONR40R41, —COR42, —NO2, CF3, and —CN;
- R4, R5 and R6 are, independently of one another, hydrogen atom, halo, —CN, —NO2, —NO, —CHO, —NR43R44, —CO2R45, —S(O)R46, —SO2R47, —SO2NR48R49, —OCOR50, —NR51COR52, —NR53CO(O)R54, —NR55CONR56R57, —CO2R58, —OR59, —COR60, —SR61, —CONR62R63, —OCONR64R65, —SO2(O)R66, or a group selected from saturated (C1-C6)alkyl, unsaturated (C1-C6)alkyl and aryl, said group being optionally substituted with one or several groups selected from halo, —CF3, —CN, and —SO2NR67R68;
- R7 to R68 are, independently of one another, a hydrogen atom or a (C1-C10)alkyl, aryl or aryl(C1-C6)alkyl group, said group being optionally substituted with one or several groups selected from halo, —OH, —CF3, —CN and SO2NR69R70;
- with the proviso that R21 is not an hydrogen atom;
- R69 and R70 are independently of one another, a hydrogen atom or a (C1-C10)alkyl, aryl or aryl(C1-C6)alkyl group;
- and
- n is an integer selected from 1 to 6.
12 more elements
Dependencies are inferred from the claim text.