IP Library Granted Patent US 9,278,957
Granted Patent B2
US 9,278,957 · App. 14/569,828 · Granted Mar 8, 2016

Piperazine, piperidine and tetrahydropyridine derivatives and their pharmaceutical use

Inventors: Vladimir Kogan (Rechovot, IL); Lev Tabachnik (Kiryat-Ono, IL)
Assignee: ATIR Holding S.A.
C07D405/06C07D307/91C07D407/06C07D407/12C07D407/14
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Quick Facts
Patent No.
US 9,278,957
App. No.
14/569,828
Granted
Mar 8, 2016
Kind
B2
Abstract

Novel piperazine, piperidine and tetrahydropyridine derivatives comprising a dibenzofurane moiety are provided herein, as well as pharmaceutical compositions comprising same and therapeutic uses thereof.

Claims (27)

1. A compound of the general formula Id or the general formula Ie:

wherein:

R 1 , R 2 and R 3 are independently selected from the group consisting of C1-C5 alkyl, —OH, —SH, halogen, alkoxy, NO 2 , and —CN;

m is 0, 1, 2, 3, 4 or 5;

n is 0, 1, 2 or 3; and

p is 0, 1, 2, 3 or 4.

2. A compound according to claim 1 , wherein m is 0, 1, 2 or 3, and R 1 is selected from the group consisting of hydroxy, alkoxy, halogen and cyano.

3. A compound according to claim 1 , wherein R 1 is hydroxy.

4. A compound according to claim 1 , wherein m is 1.

5. A compound according to claim 1 , wherein n is 0 and p is 0.

6. A pharmaceutical composition comprising a compound as defined in claim 1 in combination with one or more pharmaceutically acceptable carriers.

7. A method for treating CNS dyskinesia in mammals, comprising administering to said mammal a therapeutically effective amount of the compound defined in claim 1 .

8. A compound of formula I:

wherein:

Y 1 and Y 2 are independently CH, C(R 1 ) or N;

X is CH or C, with the proviso that when X is C, then the broken line represents a chemical bond;

R 1 , R 2 and R 3 are independently selected from the group consisting of C1-C5 alkyl, —OH, —SH, halogen, alkoxy, NO 2 , and —CN;

m is 0, 1, 2, 3, 4 or 5;

n is 0, 1, 2 or 3; and

p is 0, 1, 2, 3 or 4.

9. A compound according to claim 8 , having the formulas Id or Ie:

10. A compound according to claim 8 , wherein m is 0, 1, 2 or 3, and R 1 is selected from the group consisting of hydroxy, alkoxy, halogen and cyano.

11. A compound according to claim 8 , wherein R 1 is hydroxy.

12. A compound according to claim 8 , wherein m is 1.

13. A compound according to claim 8 , wherein n is 0 and p is 0.

14. A pharmaceutical composition comprising a compound as defined in claim 8 in combination with one or more pharmaceutically acceptable carriers.

15. A method for treating CNS dyskinesia in mammals, comprising administering to said mammal a therapeutically effective amount of the compound defined in claim 8 .

Assignments (2)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 2, 2017
From: GROEN BROTHERS AVIATION, INC
To: GROEN AERONAUTICS CORPORATION
Reel/Frame 041607/0867 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 22, 2015
From: KOGAN, VLADIMIR; TABACHNIK, LEV
To: ATIR HOLDING S.A.
Reel/Frame 035000/0832 →
Continuity (3)
Division 13322572
Provisional Application 61181331 · May 27, 2009
Related Publication 20150099784A1 · Apr 9, 2015