Traitement en cours

Veuillez attendre...

Paramétrages

Paramétrages

Aller à Demande

1. WO2016115144 - PROCÉDÉS POUR LE TRAITEMENT DE LA MALADIE D'ALZHEIMER

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

[ EN ]

WHAT IS CLAIMED IS:

1. A method of treating behavioral and psychological symptoms in a patient having Alzheimer’s disease, comprising administering to a patient in need thereof an effective amount of a compound of Formula I:

Formula I

or a pharmaceutically acceptable salt, isomer, racemate, or diastereomeric mixture thereof, wherein:

A is–O-(CH2)n-,–(CH2)n–, -S-(CH2)n-, -NH-(CH2)n-, -CH2-O-(CH2)n-, -(CH2)n-O-CH2-CH2-, -CH2-S-(CH2)n-, -NH-C(O)-(CH2)n-, -CH2-NH-C(O)-(CH2)n-, -CH2-C(O)-NH-(CH2)n-, or -(CH2)n-C(O)-NH-CH2-CH2-, wherein n is an integer from 1 to 7;

B is O, S, S(O)(O), or NR5; and

R1, R2, R3, R4, R6 , R7, and R8 are independently hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, arylalkyl, substituted arylalkyl, cycloalkyl, substituted cycloalkyl, alkoxy, alkoxycarbonyl, alkylsulfinyl, alkylsulfonyl, alkylthio, amino, alkylamino, dialkylamino, arylalkoxy, carboxy, carbamoyl, carbamate, carbonate, cyano, halogen, or hydroxy; wherein the hydrogen of R1, R2, R3, R4, R6 , R7 and R8 and A are optionally substituted with 2H (deuterium).

2. The method according to Claim 1, wherein A is–O-(CH2)n-.

3. The method according to Claim 1, wherein A is–(CH2)n–.

4. The method according to Claim 1, wherein A is -NH-C(O)-(CH2)n-, -CH2-NH-C(O)-(CH2)n-, -CH2-C(O)-NH-(CH2)n-, or -(CH2)n-C(O)-NH-CH2-CH2-.

5. The method according to Claim 1, wherein B is O.

6. The method according to any one of Claims 1-5, wherein R3, R4, R6, R7, and R8 are hydrogen.

7. The method according to any one of Claims 1-6, wherein R1 and R2 are independently H, halogen, or alkoxy.

8. The method according to Claim 7, wherein R1 is H, and R2 is methoxy.

9. The method according to Claim 7, wherein R1 and R2 are chloro.

10. The method according to Claim 1, wherein A is–O-(CH2)n-; B is O, and R3, R4, R6, R7, and R8 are independently hydrogen or alkyl.

11. The method according to Claim 1, wherein the compound is 6-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)butoxy)-2H-benzo[b][1,4]oxazin-3(-4H)-one, 6-(4-(4-(2-methoxyphenyl)piperazin-1-yl)butoxy)-2H-benzo[b][1,4]oxazin-3(-4H)-one, or its hydrochloride salt thereof.

12. The method according to Claim 1, wherein the compound is administered in a pharmaceutical composition comprising a pharmaceutically acceptable carrier, excipient, or diluent.

13. The method according to Claim 1, wherein the compound is orally administered.

14. The method according to Claim 1, which treats dementia.

15. The method according to Claim 1, which treats memory impairment and/or cognitive impairment in the patient.

16. The method according to Claim 1, which treats agitation in the patient.

17. The method according to Claim 1, which treats psychosis in the patient.

18. The method according to Claim 1, which treats depression in the patient.

19. The method according to Claim 1, which treats mood swing in the patient.