IP Library Granted Patent US 9,289,400
Granted Patent B2
US 9,289,400 · App. 13/764,623 · Granted Mar 22, 2016

D

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Quick Facts
Patent No.
US 9,289,400
App. No.
13/764,623
Granted
Mar 22, 2016
Kind
B2
Abstract

The present invention provides a method of inhibiting, suppressing or preventing levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of inhibiting, suppressing or preventing Parkinson's Disease in a patient, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention.

Claims (71)

1. A method of treating or ameliorating levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, said method comprising administering to said patient a therapeutically effective amount of at least one compound of formula (I):

wherein in formula (I):

R 1 , R 2 and R 3 are independently selected from the group consisting of H, cyano, halo, hydroxyl, alkoxy, nitro, C1-6 alkyl, and carboxy;

R 4 and R 5 are independently selected from the group consisting of H, C1-6 alkyl, and substituted C1-6 alkyl; and,

n is 2,

mixtures thereof, or a pharmaceutically acceptable salt thereof.

2. The method of claim 1 , wherein said at least one compound is selected from the group consisting of:

2-amino-4-(2-chlorophenyl)butan-1-ol;

2-(3-aminohexyl)phenol;

4-(2-chlorophenyl)-2-methylamino-butane;

4-(2-fluorophenyl)butan-2-amine;

4-(2-bromophenyl)butan-2-amine;

4-(2-iodophenyl)butan-2-amine;

4-(2-methoxyphenyl)butan-2-amine;

2-(3-aminobutyl)phenol;

3-(3,4-diethoxyphenyl)propan-1-amine;

4-(4-chlorophenyl)butan-2-amine;

4-(4-methoxyphenyl)butan-2-amine;

mixtures thereof, or a pharmaceutically acceptable salt thereof.

3. The method of claim 1 , wherein said patient is further administered a drug selected from the group consisting of levodopa, clozapine, bromocriptine, pergolide, pramipexole, ropinirole, piribedil, cabergoline, apomorphine, and lisuride, a salt thereof and mixtures thereof.

4. The method of claim 1 , wherein said compound is co-administered to said patient with a second pharmaceutical composition comprising levodopa.

5. The method of claim 1 , wherein said compound is administered to said patient a given period of time before a second pharmaceutical composition comprising levodopa is administered to said patient.

6. The method of claim 5 , wherein said given period of time varies from about 2 minutes to about 24 hours.

7. The method of claim 1 , wherein said patient is human.

8. A method of treating or ameliorating Parkinson's Disease in a patient in need thereof, said method comprising administering to said patient a therapeutically effective amount of at least one compound of formula (I):

wherein in formula (I):

R 1 , R 2 and R 3 are independently selected from the group consisting of H, cyano, halo, hydroxyl, alkoxy, nitro, C1-6 alkyl, and carboxy;

R 4 and R 5 are independently selected from the group consisting of H, C1-6 alkyl, and substituted C1-6 alkyl; and,

n is 2,

mixtures thereof, or a pharmaceutically acceptable salt thereof.

9. The method of claim 8 , wherein said at least one compound is selected from the group consisting of:

2-amino-4-(2-chlorophenyl)butan-1-ol;

2-(3-aminohexyl)phenol;

4-(2-chlorophenyl)-2-methylamino-butane;

4-(2-fluorophenyl)butan-2-amine;

4-(2-bromophenyl)butan-2-amine;

4-(2-iodophenyl)butan-2-amine;

4-(2-methoxyphenyl)butan-2-amine;

2-(3-aminobutyl)phenol;

3-(3,4-diethoxyphenyl)propan-1-amine;

4-(4-chlorophenyl)butan-2-amine;

4-(4-methoxyphenyl)butan-2-amine;

mixtures thereof, or a pharmaceutically acceptable salt thereof.

10. The method of claim 8 , wherein said compound is administered to said patient as a composition that further comprises at least one drug selected from the group consisting of levodopa, clozapine, bromocriptine, pergolide, pramipexole, ropinirole, piribedil, cabergoline, apomorphine, and lisuride, a salt thereof and mixtures thereof.

11. The method of claim 8 , wherein said patient is further administered a second pharmaceutical composition comprising at least one drug selected from the group consisting of levodopa, clozapine, bromocriptine, pergolide, pramipexole, ropinirole, piribedil, cabergoline, apomorphine, and lisuride, a salt thereof and mixtures thereof.

12. A method of treating or ameliorating levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, said method comprising administering to said patient a therapeutically effective amount of at least one compound selected from the group consisting of:

2-amino-4-(2-chlorophenyl)butan-1-ol;

2-(3-aminohexyl)phenol;

4-(2-chlorophenyl)-2-methylamino-butane;

4-(2-fluorophenyl)butan-2-amine;

4-(2-bromophenyl)butan-2-amine;

4-(2-iodophenyl)butan-2-amine;

4-(2-methoxyphenyl)butan-2-amine;

2-(3-aminobutyl)phenol;

3-(3,4-diethoxyphenyl)propan-1-amine;

4-(4-chlorophenyl)butan-2-amine;

4-(4-methoxyphenyl)butan-2-amine;

mixtures thereof, or a pharmaceutically acceptable salt thereof.

13. A method of treating or ameliorating Parkinson's Disease in a patient, said method comprising administering to said patient a therapeutically effective amount of at least one compound selected from the group consisting of:

2-amino-4-(2-chlorophenyl)butan-1-ol;

2-(3-aminohexyl)phenol;

4-(2-chlorophenyl)-2-methylamino-butane;

4-(2-fluorophenyl)butan-2-amine;

4-(2-bromophenyl)butan-2-amine;

4-(2-iodophenyl)butan-2-amine;

4-(2-methoxyphenyl)butan-2-amine;

2-(3-aminobutyl)phenol;

3-(3,4-diethoxyphenyl)propan-1-amine;

4-(4-chlorophenyl)butan-2-amine;

4-(4-methoxyphenyl)butan-2-amine;

mixtures thereof, or a pharmaceutically acceptable salt thereof.

Assignments (4)
MERGER Recorded Jan 14, 2015
From: PHILADELPHIA HEALTH & EDUCATION CORPORATION
To: DREXEL UNIVERSITY
Reel/Frame 034764/0236 →
NUNC PRO TUNC ASSIGNMENT Recorded Aug 13, 2014
From: THE UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEY
To: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEY
Reel/Frame 033525/0369 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 22, 2013
From: KORTAGERE, SANDHYA
To: PHILADELPHIA HEALTH & EDUCATION CORPORATION D/B/A DREXEL UNIVERSITY COLLEGE OF MEDICINE
Reel/Frame 031060/0736 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 22, 2013
From: KUZHIKANDATHIL, ELDO V.
To: UNIVERSITY OF MEDICINE AND DENISTRY OF NEW JERSEY
Reel/Frame 031060/0847 →