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1. (WO2018055096) AZÉTIDINES, PYRROLIDINES, PIPÉRIDINES ET AZÉPANES DI-SUBSTITUÉS EN TANT QU'INHIBITEURS DE MONOAMINE OXYDASE B POUR LE TRAITEMENT DE MALADIES NEURODÉGÉNÉRATIVES
Note: Texte fondé sur des processus automatiques de reconnaissance optique de caractères. Seule la version PDF a une valeur juridique

Claims

Compound of general Formula (I):


(I)

wherein:

n: 1-5

m: 0, 1 , or 2

z: 0 or 1

L: -CH2CH2-, -CH2-, =CH2-, =CH2CH2-, trans

A: is saturated 3 to 8-membered ring optionally comprising one or more heteroatoms selected from N, O, S, and P; the ring being optionally substituted with one or more substituents independently selected from R1, wherein:

R1: Me, Et, i-Pr, t-Bu, i-Bu, CN, F, CI, Br, CF3, SR2, OR2, NR2R3

R2: H, Me, Et, n-Pr, i-Pr, t-Bu, i-Bu,

R3: H, Me, Et, n-Pr, i-Pr, t-Bu, i-Bu,

is phenyl, furan, thiophene, pyrrole, pyrazole, imidazole, thiazole, oxazole, pyridine, indole, quinoline, isoquinoline, 2,3.dihydrobenzo[i ][1 ,4]dioxine, benzo[c/][1 ,3]dioxole, indazole, bezimidazole, quinazoline, naphthalene,


R1: Me, Et, i-Pr, t-Bu, i-Bu, CN, F, CI, Br, CF3, CH2CF2, cyclopropyl, cyclobutyl, cyclopentyl, SR6, OR6, NR6R7

R6: H, Me, Et, n-Pr, i-Pr, t-Bu, i-Bu,

R7: H, Me, Et, n-Pr, i-Pr, t-Bu, i-Bu,

R2: Me, Et, i-Pr, t-Bu, i-Bu, CN, F, CI, Br, CF3, CH2CF2, cyclopropyl, cyclobutyl, cyclopentyl, SR6, OR6, NR6R7

R6: H, Me, Et, n-Pr, i-Pr, t-Bu, i-Bu,

R7: H, Me, Et, n-Pr, i-Pr, t-Bu, i-Bu,

R3: Me, Et, i-Pr, t-Bu, i-Bu, CN, F, CI, Br, CF3, CH2CF2, cyclopropyl, cyclobutyl, cyclopentyl, SR6, OR6, NR6R7

R6: H, Me, Et, n-Pr, i-Pr, t-Bu, i-Bu,

R7: H, Me, Et, n-Pr, i-Pr, t-Bu, i-Bu,

R4: Me, Et, i-Pr, t-Bu, i-Bu, CN, F, CI, Br, CF3, CH2CF2, cyclopropyl, cyclobutyl, cyclopentyl, SR6, OR6, NR6R7

R6: H, Me, Et, n-Pr, i-Pr, t-Bu, i-Bu,

R7: H, Me, Et, n-Pr, i-Pr, t-Bu, i-Bu,

R5: Me, Et, i-Pr, t-Bu, i-Bu, CN, F, CI, Br, CF3, CH2CF2, cyclopropyl, cyclobutyl, cyclopentyl, SR6, OR6, NR6R7

R6: H, Me, Et, n-Pr, i-Pr, t-Bu, i-Bu,

R7: H, Me, Et, n-Pr, i-Pr, t-Bu, i-Bu,

or a pharnnaceutically acceptable salt, hydrate or solvate thereof; in the form of a pure diastereoisomer or as a mixture of diastereomers, in the form of a pure enantiomer or as a mixture of enantiomers.

2. The compound according to claim 1 , wherein A is a saturated 3 to 8-membered ring optionally comprising one or more heteroatoms selected from N, O, S, and P; the ring being optionally substituted with one or more substituents independently selected from R1, wherein:

R1: Me, Et, i-Pr, t-Bu, i-Bu, CN, F, CI, Br, CF3, SR2, OR2, NR2R3

R >2^.: H, Me, Et, n-Pr, i-Pr, t-Bu, i-Bu,

R3: H, Me, Et, n-Pr, i-Pr, t-Bu, i-Bu.

3. The compound according to claim 2, wherein R1 is Me, i-Pr, CN, F, CI, Br or CF3.

4. The compound according to any one of claims 1 to 3, wherein L is -CH2CH2- or

trans

5. The compound according to any one of claims 1 to 4, wherein m is 1 or 2.

6. The compound according to any one of claims 1 to 5, wherein n is 1 .

7. A compound selected from the group consisting of:


and

8. The compound according to claim 1 or 7, wherein said compound is selected from the group consisting of:


and

The compound according to claim 1 or 7, wherein said compound is


The compound according to claim 1 or 7, wherein said compound


1 1 . The compound according to claim 1 or 7, wherein said compound is


12. The compound according to claim 1 or 7, wherein said compound is

13. The compound according to claim 1 or 7, wherein said compound is


14. The compound according to any one of claims 1 to 13 for use as a medicament.

15. The compound according to any one of claims 1 to 13 for use in the prevention, alleviation of symptoms or treatment of a medical condition selected from the group consisting of acute and chronic neurological disorders, cognitive and neurodegenerative diseases.

16. The compound according to any one of claims 1 to 13 for use in the prevention, alleviation of symptoms or treatment of a neurodegenerative disease, such as Parkinson's disease, Alzheimer's disease, Huntington's disease or dementia.

17. The compound according to any one of claims 1 to 13 for use in the prevention, alleviation of symptoms or treatment of Parkinson's disease, Alzheimer's disease, Huntington's disease or dementia.

18. A pharmaceutical composition comprising a therapeutically effective amount of at least one compound according to any one of claims 1 to 13 and a pharmaceutical acceptable excipient.