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1. WO2020109506 - INHIBITEURS D'ACTIVITÉ MITOCHONDRIALE CIBLANT LE MÉTABOLISME DE CELLULE TUMORALE

Note: Texte fondé sur des processus automatiques de reconnaissance optique de caractères. Seule la version PDF a une valeur juridique

[ EN ]

CLAIMS

1. A compound of formula (I) as follows:


wherein

X1 and X2, identical or different, are NR5 or a sulfur atom, and at least one of X1 and X2 is a sulfur atom,

Y is a group (Ci-Ci0)alkanediyl,

Ar1 and Ar2, identical or different, are an aryl group optionally substituted by one or several groups selected from a halogen atom, a (Ci-C6) alkyl, -OR1 , -NR1R2 and -COOR3,

with R1 and R2, independently of each other, are a hydrogen atom, a (Ci-C6) alkyl group or a -COR4 group,

R3 and R4, independently of each other, are a hydrogen atom or a (Ci-C6) alkyl group, and

R5 is a hydrogen atom or a (Ci-C6)alkyl group,

or a pharmaceutically acceptable salt and/or solvate thereof,

for use in cancer treatment.

2. The compound of formula (I) for use according to claim 1 , wherein Y is a group -(CH2)n-and n is an integer between 1 and 10, preferably between 2 and 8, more preferably between 4 and 6.

3. The compound of formula (I) for use according to any of the preceding claims, wherein X1 and X2 are a sulfur atom.

4. The compound of formula (I) for use according to any of the preceding claims, wherein Ar1 and Ar2 are identical.

5. The compound of formula (I) for use according to any of the preceding claims, wherein Ar1 and/or Ar2 is a phenyl or a naphthyl group optionally substituted by one or several groups selected from an atom of halogen, a group -OR1 , a group -NR1 R2, and a group -COOR1.

6. The compound of formula (I) for use according to any of claims 1 to 5, wherein Ar1 and/or Ar2 is an unsubstituted aryl group, preferably an unsubstituted phenyl or naphthyl group.

7. The compound of formula (I) for use according to any of the preceding claims, selected from the group consisting of:


and the pharmaceutically acceptable salts and solvates thereof, preferably the bromide salts thereof.

8. The compound of formula (I) according to any of the preceding claims for use in treatment of haematological cancers, lung cancers, cervix cancers, prostate cancer, melanoma and neuroendocrine tumors, preferably haematological cancers, more preferably lymphoma.

9. The compound of formula (I) according to any of the preceding claims for use in treatment of a LKB-1 gene-deficient cancers.

10. A pharmaceutical composition comprising a compound of formula (I) as defined in any of claims 1 to 7 and at least one pharmaceutically acceptable excipient for use in cancer treatment, preferably for use in treatment of haematological cancers, lung cancers, cervix cancers prostate cancer, melanoma and neuroendocrine tumors, more preferably haematological cancers, even more preferably lymphoma.

1 1 . The pharmaceutical composition according to claim 10, for use in treatment of a LKB-1 gene-deficient cancers.

12. A method for treating cancer, comprising administering to a patient in need thereof an effective amount of a compound as defined in any of claims 1 to 7 or a composition as defined in claim 10.

13. A method for inhibiting mitochondrial complex I, comprising administering to a patient in need thereof an effective amount of a compound as defined in any of claims 1 to 7 or a composition as defined in claim 10.

14. A compound of formula (I) as follows:


wherein

X1 and X2, identical or different, are NR5 or a sulfur atom, and at least one of X1 and X2 is a sulfur atom,

Y is a group (Ci-Ci0)alkanediyl,

Ar1 and Ar2, identical or different, are an aryl group optionally substituted by one or several groups selected from a halogen atom, a (Ci-C6) alkyl, -OR1 , -NR1R2 and -COOR3,

with R1 and R2, independently of each other, are a hydrogen atom, a (Ci-C6) alkyl group or a -COR4 group,

R3 and R4, independently of each other, are a hydrogen atom or a (Ci-C6) alkyl group, and

R5 is a hydrogen atom or a (Ci-C6)alkyl group,

or a pharmaceutically acceptable salt and/or solvate thereof,


15. The compound according to claim 14, wherein Ar1 and Ar2 are identical.

16. The compound according to claim 14 or 15, wherein Ar1 and/or Ar2 is a phenyl or a naphthyl group optionally substituted by one or several groups selected from an atom of halogen, a group -OR1 , a group -NR1R2, and a group -COOR3.

17. The compound according to claim 16, wherein Ar1 and/or Ar2 is a naphthyl group optionally substituted by one or several groups selected from an atom of halogen, a group - OR1 , a group -NR1 R2, and a group -COOR3.

18. The compound according to claim 17, wherein Ar1 and/or Ar2 is a naphthyl, preferably Ar1 and Ar2 are a naphthyl.

19. The compound according to any one of claims 14 to 18, wherein X1 and X2 are a sulfur atom.

20. The compound according to any one of claims 14 to 19, wherein Y is a group -(CH2)n- and n is an integer between 1 and 10, preferably between 2 and 8, more preferably between

4 and 6.

21 . The compound according to any one of claims 14 to 20, selected from the group consisting of:


and the pharmaceutically acceptable salts and solvates thereof, preferably the bromide salts thereof.