IP Library Granted Patent US 9,181,286
Granted Patent B2
US 9,181,286 · App. 14/157,173 · Granted Nov 10, 2015

Pantothenate derivatives for the treatment of neurologic disorders

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Quick Facts
Patent No.
US 9,181,286
App. No.
14/157,173
Granted
Nov 10, 2015
Kind
B2
Abstract

The present disclosure relates to pantothenate derivatives for the treatment of neurologic disorders (such as pantothenate kinase-associated neurodegeneration), pharmaceutical compositions containing such compounds, and their use in treatment of neurologic disorders.

Claims (68)

1. A method of treating pantothenate kinase-associated neurodegeneration in a subject,

the method comprising administering to the subject an effective amount of a compound of the following formula:

or a pharmaceutically acceptable salt thereof, wherein R, R′ and R″ are selected from the group consisting of:

R (Amino Acid)

R′

R″

Me (L-Ala)

Me

Me

Me (L-Ala)

Et

Bn

Me (L-Ala)

MeCyPr

MeCyPr

MeIndole (L-Trp)

Bn

Et.

2. The method of claim 1 , wherein R, R′ and R″ are methyl.

3. The method of claim 1 , wherein R is methyl, R′ is ethyl and R″ is benzyl.

4. The method of claim 1 , wherein R is methyl, and R′ and R″ are methylcyclopropyl.

5. The method of claim 1 , wherein R is 1H-indol-3yl-methyl, R′ is benzyl and R″ is ethyl.

6. The method of claim 1 , wherein the subject is a child.

7. The method of claim 6 , wherein the child is 10 to 15 years old.

8. The method of claim 1 , wherein the subject is an adult.

9. A method of treating a subject having neuronal cells with an over accumulation of iron, the method comprising administering to the subject an effective amount of a compound of the following formula:

or a pharmaceutically acceptable salt thereof, wherein R, R′ and R″ are selected from the group consisting of:

R (Amino Acid)

R′

R″

Me (L-Ala)

Me

Me

Me (L-Ala)

Et

Bn

Me (L-Ala)

MeCyPr

MeCyPr

MeIndole (L-Trp)

Bn

Et.

10. The method of claim 9 , wherein R, R′ and R″ are methyl.

11. The method of claim 9 , wherein R is methyl, R′ is ethyl and R″ is benzyl.

12. The method of claim 9 , wherein R is methyl, and R′ and R″ are methylcyclopropyl.

13. The method of claim 9 , where R is 1H-indol-3yl-methyl, R′ is benzyl and R″ is ethyl.

14. The method of claim 9 , wherein the subject is a child.

15. The method of claim 14 , wherein the child is 10 to 15 years old.

16. The method of claim 9 , wherein the subject is an adult.

17. The method of claim 9 , wherein the subject suffers from pantothenate kinase-associated neurodegeneration.

18. A method of treating Parkinson's disease, dystonia, extrapyramidal effects, dysphagia, rigidity and/or stiffness of limbs, choreoathetosis, tremor, spasticity, muscle weakness, or seizure in a subject, the method comprising administering to the subject an effective amount of a compound of the following formula:

or a pharmaceutically acceptable salt thereof, wherein R, R′ and R″ are selected from the group consisting of:

R (Amino Acid)

R′

R″

Me (L-Ala)

Me

Me

Me (L-Ala)

Et

Bn

Me (L-Ala)

MeCyPr

MeCyPr

MeIndole (L-Trp)

Bn

Et.

19. The method of claim 18 , wherein R, R′ and R″ are methyl.

Assignments (3)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jul 8, 2016
From: VAINO, ANDREW; BIESTEK, MAREK; SHKRELI, MARTIN
To: RETROPHIN, INC.
Reel/Frame 039112/0037 →
RELEASE OF SECURITY INTEREST Recorded Aug 17, 2015
From: U.S. BANK NATIONAL ASSOCIATION, AS COLLATERAL AGENT
To: RETROPHIN, INC.; KYALIN BIOSCIENCES INC.
Reel/Frame 036342/0407 →
PATENT SECURITY AGREEMENT Recorded Jul 1, 2014
From: RETROPHIN, INC.; KYALIN BIOSCIENCES INC.
To: U.S. BANK, NATIONAL ASSOCIATION, AS COLLATERAL AGENT
Reel/Frame 033260/0948 →