IP Library Granted Patent US 8,741,949
Granted Patent B2
US 8,741,949 · App. 13/001,422 · Granted Jun 3, 2014

Inhibitors of carnitin-palmitoyl-tranferase-1 for the treatment and prevention of disorders caused by delipidation of neural tissue

Inventor: Josephus Dirk Nieland (Arthus C, DK)
Assignee: Meta-IQ ApS
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Quick Facts
Patent No.
US 8,741,949
App. No.
13/001,422
Granted
Jun 3, 2014
Kind
B2
Abstract

Carnitin-Palmitoyl-Transferase-1 (CPT-1) inhibitor for use in treating and/or preventing disorders caused by delipidation of neural tissue.

Claims (36)

1. A method of treating disorders caused by delipidation of neural tissue, wherein the disorders are primary disorders which affect the brain directly and selectively and which are selected from the group consisting of multiple sclerosis, mental and/or behavioural disorder which are caused by psychoactive substance use, schizoid personality disorder, depression, depressive episode, recurrent depressive disorder, persistent mood disorder, mental retardation and impairment of memory and which are not secondary disorders wherein the brain is attacked as one of multiple organs of the body by administering to a patient a Carnitin-Palmitoyl-Transferase-1 (CPT-1) inhibitor in a pharmacologically effective amount, whereby the CPT-1 inhibitor is an aryloxyalkyl-substituted oxirane carboxylic acid of the following formula I

wherein

Ar is a substituted phenyl radical

R1 is a hydrogen atom;

R2 is a hydrogen atom, a halogen atom, or a 1-4 C lower alkyl group; a 1-4 C lower alkoxy group, a nitro group, a trifluoromethyl group, a fully or predominantly fluorine-substituted 1-3 C alkoxy group or

R3 is a hydrogen atom or a 1-4 C lower alkyl group;

R5 is a 1-4 C lower alkyl group;

Y is the grouping —O—;

z is 0

s is 1 or 2

r is 2-s

n and m are integer >0 with 2<n+m<8, and

as well as pharmaceutically acceptable salts or derivatives of said aryloxyalkyl-substituted oxirane carboxylic acid.

2. The method according to claim 1 , wherein the patient is a human.

3. The method according to claim 1 , wherein the disorder is a mental and/or a behavioural disorder caused by psychoactive substance use.

4. The method according to claim 1 , wherein said CPT-1 inhibitor is administered systemically or topically.

5. The method according to claim 1 , wherein said CPT-1 inhibitor is administered in combination with a further therapy.

6. The method according to claim 1 , wherein the inhibitor is administered alone as a substantially pure compound.

7. The method according to claim 1 , wherein the inhibitor is administered together with at least one excipient and/or auxiliary.

8. The method according to claim 7 , wherein the excipient and/or auxiliary is selected from the group consisting of one or more suitable adjuvant(s), one or more pharmaceutically active and/or acceptable carrier(s), diluent(s), filler(s), binder(s), disintegrant(s), lubricant(s), glident(s), coloring agent(s), flavoring agent(s), opaquing agent(s) and plasticizer(s).

9. The method according to claim 1 , wherein said aryloxyalkyl-substituted oxirane carboxylic acid of formula I is

2-(6-(4-chlorophenoxy)hexyl)oxirane-2-carboxylic acid ethyl ester (Etomoxir),

2-(6-(4-difluoromethoxyphenoxy)hexyl)oxirane-2-carboxylic acid ethyl ester,

2-(5-(4-difluoromethoxyphenoxy)pentyl)oxirane-2-carboxylic acid ethyl ester,

2-(5-(4-acetylphenoxy)pentyloxirane-2-carboxylic acid ethyl ester,

2-(6-(4-chlorophenoxy)hexyl)oxirane-2-carboxylic acid,

2-(6-(4-difluoromethoxyphenoxy)hexyl)oxirane-2-carboxylic acid,

2-(5-(4-difluoromethoxyphenoxy)pentyl)oxirane-2-carboxylic acid, or

2-(5-(4-acetylphenoxy)pentyloxirane-2-carboxylic acid.

10. The method according to claim 1 , wherein the neural tissue is myelin sheet.

11. The method according to claim 1 , wherein the disorder is schizoid personality disorder.

12. The method according to claim 1 , wherein the disorder is mental retardation.

13. The method according to claim 1 , wherein the mental and/or behavioural disorder which is caused by psychoactive substance use is due to the use of a psychoactive substance selected from alcohol, opioids, cannabinoids, cocaine, caffeine, hallucinogens, tobacco, volatile solvents and multiple drugs.

14. The method according to claim 1 , wherein the persistent mood disorder is cyclothymia or dysthymia.

15. The method according to claim 1 , wherein mental retardation is mild, moderate, severe or profound mental retardation.

16. The method according to claim 1 , wherein the impairment of memory is impairment of recent memory or impairment of remote memory.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Aug 30, 2024
From: CPT.TWO APS
To: NUMIERA THERAPEUTICS INC.
Reel/Frame 068449/0746 →
CHANGE OF NAME Recorded Jul 18, 2024
From: META-IQ APS
To: CPT.ONE BIOTECH APS
Reel/Frame 068435/0142 →
CHANGE OF NAME Recorded Jul 18, 2024
From: CPT.ONE BIOTECH APS
To: CPT.TWO APS
Reel/Frame 068435/0163 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Mar 22, 2011
From: NIELAND, JOSEPHUS DIRK
To: META-IQ APS
Reel/Frame 025998/0172 →
Continuity (2)
Provisional Application 61076316 · Jun 27, 2008
Related Publication 20110178172A1 · Jul 21, 2011