IP Library Granted Patent US 8,067,441
Granted Patent B2
US 8,067,441 · App. 11/996,966 · Granted Nov 29, 2011

Use of collismycin and derivatives thereof as oxidative stress inhibitors

Assignees: Neuropharma, S.A.; Instituto Biomar, S.A.
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Quick Facts
Patent No.
US 8,067,441
App. No.
11/996,966
Granted
Nov 29, 2011
Kind
B2
Abstract

The present invention relates to the use of Collismycin and derivatives thereof as inhibitors of oxidative stress in cells and their use for the preparation of medicaments for the treatment of oxidative stress-induced diseases or conditions, especially neurodegenerative diseases, such as Alzheimer's Disease and Parkinson's Disease.

Claims (41)

1. A method of inhibiting oxidative stress in a patient suffering from a disease or condition selected from the group consisting of Alzheimer's Disease, Parkinson's Disease, Huntington's Disease, Amyotrophic Lateral Sclerosis (ALS), Multiple Sclerosis (MS), Friedreich's ataxia, tardive dyskynesia, brain injuries, ischemia, reperfusion injury, stroke, myocardial infarction, schizophrenia, atherosclerosis, heart failure, diabetes, diabetes type II, epilepsy and AIDS dementia, comprising administering to the subject suffering said disease or condition an effective amount of collismycin A or a pharmaceutically acceptable salt thereof.

2. The method according to claim 1 , wherein the disease or condition is Alzheimer's Disease.

3. The method according to claim 1 , wherein the disease or condition is Parkinson's Disease.

4. A method of inhibiting oxidative stress in a patient suffering from a disease or condition selected from the group consisting of Alzheimer's Disease, Parkinson's Disease, Huntington's Disease, Amyotrophic Lateral Sclerosis (ALS), Multiple Sclerosis (MS), Friedreich's ataxia, tardive dyskynesia, brain injuries, ischemia, reperfusion injury, stroke, myocardial infarction, schizophrenia, atherosclerosis, heart failure, diabetes, diabetes type II, epilepsy and AIDS dementia, comprising administering to the subject suffering said disease or condition an effective amount of a compound of formula (I)

or a pharmaceutically acceptable salt thereof, wherein:

A 1 is selected from —C(R 3 )— and —N—;

R 1 , R 2 , R 3 , R 4 , and R 5 are each independently selected from hydrogen, substituted or unsubstituted alkyl, —CN, —O—R a , —NR b R c , —NO 2 , and halogen;

R 7 is selected from halogen, hydrogen and —S—R 9 ;

R 10 is selected from —CN, —CH═N—O—R 6 , and —CH 2 —O—R 6 ;

R 8 is selected from hydrogen, —O—R 11 , and —S—R 9 ;

R 6 and R 11 are each independently selected from hydrogen, substituted or unsubstituted alkyl, —NR b R c , and —C(═O)R d ;

R 9 is selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryl, substituted or unsubstituted heterocyclyl, substituted or unsubstituted alkoxy, substituted or unsubstituted aralkyl, substituted or unsubstituted aryloxy, and halogen; and

R a , R b , R c and R d are each independently selected from hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted alkenyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, substituted or unsubstituted heterocyclyl, and halogen;

with the proviso that at least one of R 7 and R 8 is different from hydrogen, and further wherein said compound of formula (I) is not collismycin A.

5. The method according to claim 4 , wherein R 1 , R 2 , R 3 , R 4 and R 5 are each independently selected from hydrogen, substituted or unsubstituted alkyl and halogen;

R 7 is —S—R 9 ;

R 10 is —CH═N—O—R 6 ;

R 8 is —O—R 11 ; and

R 6 , R 9 and R 11 are each independently selected from hydrogen and substituted or unsubstituted alkyl.

6. The method according to claim 4 , wherein:

R 7 is —S—R 9 ;

R 10 is —CH═N—O—R 6 ;

R 8 is —O—R 11 ; and

R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 9 and R 11 are each independently selected from hydrogen and unsubstituted alkyl.

7. The method according to claim 5 , wherein:

R 7 is —S—R 9 ;

R 10 is —CH═N—O—R 6 ;

R 8 is —O—R 11 ; and

R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 9 and R 11 are each independently selected from hydrogen and unsubstituted alkyl.

8. The method according to claim 4 , wherein:

R 1 , R 2 , R 3 , R 4 , R 5 are hydrogen;

R 7 is —S—R 9 ;

R 10 is —CH═N—OH;

R 8 is —O—R 11 , and

R 9 and R 11 are each independently selected from unsubstituted alkyl.

9. The method according to claim 4 , wherein the compound of formula (I) is selected from the group consisting of:

or a pharmaceutically acceptable salt thereof.

10. The method according to claim 4 , wherein the compound of formula (I) is

or a pharmaceutically acceptable salt thereof.

11. The method according to claim 4 , wherein the disease or condition is Alzheimer's Disease.

12. The method according to claim 4 , wherein the disease or condition is Parkinson's Disease.

Assignments (4)
CHANGE OF NAME Recorded Dec 17, 2018
From: AUBERGINE TECHNOLOGIES LLC
To: AUBERGINE PHARMACEUTICALS LLC
Reel/Frame 047942/0525 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Dec 17, 2018
From: NOSCIRA, S.A. EN LIQUIDACION
To: AUBERGINE TECHNOLOGIES LLC
Reel/Frame 049031/0555 →
CHANGE OF NAME Recorded Jan 11, 2010
From: NEUROPHARMA, S.A.
To: NOSCIRA, S.A.
Reel/Frame 023771/0091 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jun 24, 2008
From: MARTINEZ GIL, ANA; EGEA, PAOLA USAN; MEDINA PADILLA, MIGUEL; PALOMERO, ESTER GARCIA; PEREZ BAZ, JULIA; FERNANDEZ CHIMENO, ROSA ISABEL; MEDARDE FERNANDEZ, ANTONIO; CANEDO HERNANDEZ, LIBRADA MARIA; ROMERO MILLAN, FRANCISCO; CASTRO MORERA, ANA; ALONSO CASCON, MERCEDES; SANCHEZ QUESADA, JORGE
To: NEUROPHARMA, S.A.; INSTITUTO BIOMAR, S.A.
Reel/Frame 023567/0833 →
Priority Claims (1)
EP 05380175 · Jul 29, 2005 · regional
Continuity (2)
Related Publication 20080275088A1 · Nov 6, 2008
Related Publication 20100048635A2 · Feb 25, 2010