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1. WO2020141535 - AN A3 ADENOSINE RECEPTOR LIGAND FOR USE FOR ACHIEVING A FAT LOSS EFFECT

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[ EN ]

CLAIMS:

1. An A3 adenosine receptor (A3AR) ligand for use in achieving at least one fat loss effect selected from:

(a) reducing weight of a subject;

(b) reducing body fat mass in a subject;

(c) treating obesity in a subject; and

(d) inhibiting adipocytes proliferation in a subject.

2. The A3AR ligand for use according to claim 1, wherein said ligand is in a dosage form suitable for daily administration to said subject.

3. The A3AR ligand for use according to claim 2, wherein said dosage form is suitable for administration once or twice a day.

4. The A3AR ligand for use according to any one of claims 1 to 3, wherein said ligand is in a dosage form suitable for oral administration.

5. The A3AR ligand for use according to any one of claims 1 to 4, wherein said A3AR ligand is an A3AR agonist.

6. The A3AR ligand for use according to claim 5, wherein said A3AR agonist is selected from the group consisting of N6-2- (4-aminophenyl)ethyladenosine (APNEA), N6-(4-amino-3-iodobenzyl) adenosine- 5'-(N-methyluronamide) (AB-MECA), N6-(3-iodobenzyl)-adenosine-5'-N- methyluronamide (IB-MECA) and 2-chloro-N6-(3-iodobenzyl)- adenosine-5 '-N-methyluronamide (C1-IB-MECA).

7. The A3AR ligand for use according to claim 6, wherein said A3AR agonist is

Cl-IB-MECA.

8. The A3AR ligand for use according to any one of claims 1 to 4, wherein said A3AR ligand is an A3AR allosteric modulator.

9. The A3AR ligand for use according to claim 8, wherein said A3AR allosteric modulator is selected from the group consisting of:

N-(3,4-Dichloro-phenyl)-2-cyclopentyl-lH-imidazo[4,5-c]quinolin-4-amine;

N-(3,4-Dichloro-phenyl)-2-cycloheptyl-lH-imidazo[4,5-c]quinolin-4-amine;

N-(3 ,4-Di chloro-phenyl)-2-cy clobutyl - 1 H-imidazo[4, 5 -c] quinolin-4-amine; and

N-(3,4-Dichloro-phenyl)-2-cyclohexyl-lH-imidazo[4,5-c]quinolin-4-amine.

10. The A3AR ligand for use according to any one of claims 1 to 9, in combination with an anti-obesity treatment.

11. A pharmaceutical composition comprising a pharmaceutically acceptable carrier and as active ingredient an A3AR ligand in an amount effective to achieve at least one fat loss effect selected from:

reducing weight of a subject;

reducing body fat mass in a subject

treating obesity in a subject

inhibiting adipocytes proliferation in a subject.

12. The pharmaceutical composition of claim 11, in a dosage form suitable for daily administration of said A3AR ligand to said subject.

13. The pharmaceutical composition of claim 12, in a dosage suitable for administration once or twice a day.

14. The pharmaceutical composition of any one of claims 11 to 13, for chronic treatment of said subject.

15. The pharmaceutical composition of any one of claims 11 to 14, in a dosage form suitable for is oral administration.

16. The pharmaceutical composition of any one of claims 11 to 15, wherein said A3AR ligand is an A3AR agonist.

17. The pharmaceutical composition of claim 16, wherein said A3AR agonist is Cl-IB-MECA.

18. The pharmaceutical composition of any one of claims 11 to 17, wherein said A3AR ligand is an A3AR allosteric modulator.

19. The pharmaceutical composition of claim 18, wherein said A3AR allosteric modulator is N-(3,4-Dichloro-phenyl)-2-cyclohexyl-lH-imidazo[4,5-c]quinolin-4-amine (CF602):

20. A method for treating a subject comprising administering to said subject an amount of an A3AR ligand, the amount being effective to achieve at least one fat loss effect selected from:

reduce weight of the subject;

reduce body fat mass in the subject

treat obesity in the subject

inhibiting adipocytes proliferation in a subject.

21. The method of claim 20, for treating obesity.

22. A kit comprising:

(a) a pharmaceutical composition comprising an A3AR ligand according to any one of claims 11 to 19;

(b) instructions for use of the pharmaceutical composition achieving at least one of the following effects:

reducing weight of the subject;

reducing body fat mass in the subject

treating obesity in the subject

inhibiting adipocytes proliferation in a subject.