Small organic molecules for use in the treatment of neuroinflammatory disorders
AssigneeThe Medical Research, Infrastructure and Health Services Fund of the Tel Aviv Medical Center
InventorArnon KARNI
Life of this patent
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Abstract
This invention provides small organic molecules useful as therapeutics of neurodegenerative diseases. Small organic molecules that act as inhibitors of bone morphogenetic proteins (BMPs) are useful in the treatment of neuroinflammatory disorders, in particular multiple sclerosis.
Claims20
1-58. (canceled)
A pharmaceutical composition comprising a compound having the general Formula (I) or a salt thereof:
- wherein
- X1 and X2 are each independently S, O or N—R4, wherein R4 is selected from the group consisting of H, alkyl, cycloalkyl, aryl and heteroaryl;
- X3 is selected from the group consisting of CN, halogen, NO2, CO—X9 and SO2X9, wherein X9 is selected from the group consisting of OH, O− and NH2;
- X4, X5, X6, X7, and X are each independently selected from the group consisting of H, alkyl, cycloalkyl, aryl, amine, halogen, alkoxy, hydroxy, heteroaryl, NO2, CN, CO—X10 and SO2X10 wherein X10 is selected from the group consisting of OH, O− and NH2;
- one of R1 and R2 is absent and the other R1 and R2 is selected from the group consisting of H, alkyl, cycloalkyl, aryl, amine, halogen, alkoxy, heteroaryl, CN, CO—X11 and SO2X11, wherein X11 is selected from the group consisting of OH, O− and NH2;
- R3 is selected from the group consisting of OR5, O− and NR6R7, wherein R5, R6, and R7 are each independently selected from the group consisting of H, alkyl, cycloalkyl and aryl;
- and
- wherein each of the dotted lines independently represents a single or a double bond.
A method of treating a neuroinflammatory disease, the method comprising the step of administering to a subject in need thereof a therapeutically effective amount of a compound having the general Formula (I) or a salt thereof:
- wherein
- X1 and X2 are each independently S, O or N—R4, wherein R4 is selected from the group consisting of H, alkyl, cycloalkyl, aryl and heteroaryl;
- X3 is selected from the group consisting of CN, halogen, NO2, CO—X9 and SO2X9, wherein X9 is selected from the group consisting of OH, O− and NH2;
- X4, X5, X6, X7, and X8 are each independently selected from the group consisting of H, alkyl, cycloalkyl, aryl, amine, halogen, alkoxy, hydroxy, heteroaryl, NO2, CN, CO—X10 and SO2X10 wherein X10 is selected from the group consisting of OH, O— and NH2;
- one of R1 and R2 is absent and the other R1 and R2 is selected from the group consisting of H, alkyl, cycloalkyl, aryl, amine, halogen, alkoxy, heteroaryl, CN, CO—X11 and SO2X11, wherein X11 is selected from the group consisting of OH, O— and NH2;
- R3 is selected from the group consisting of OR5, O— and NR6R7, wherein R5, R6, and R7 are each independently selected from the group consisting of H, alkyl, cycloalkyl and aryl;
- and
- wherein each of the dotted lines independently represents a single or a double bond.
Dependencies are inferred from the claim text.