Trans-4-hydroxycyclohexyl phenyl amide mitofusin activators and methods of use thereof
AssigneeMitochondria Emotion, Inc.
InventorGerald W. Dorn, II
Life of this patent
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Abstract
Compounds and compositions including stereoisomers of 6-phenylhexanamide derivative small molecule mitofusin activators are described. In particular, mitofusin activators comprising derivatives of (trans-4-hydroxycyclohexyl)-6-phenylhexanamide, which are useful for treating diseases or disorders associated with a mitochondria-associated disease, disorder, or condition such as diseases or disorders associated with mitofusin-1 (MFN1) and/or mitofusin-2 (MFN2), or mitochondrial dysfunction, are described. Methods of treatment and pharmaceutical formulations are also described.
Claims18
A method comprising:
- administering a therapeutically effective amount of a composition comprising one or more of a mitofusin activator or a pharmaceutically acceptable salt thereof to a subject having or suspected of having a mitochondria-associated disease, disorder or condition, the mitofusin activator having a structure represented by the following formula:
- wherein:
- Z is phenyl or substituted phenyl;
- R2 and R3 are H;
- R4 and R5 are H;
- Y is O, CH2 or cycloalkyl;
- wherein the cycloalkyl is cyclopropyl or cyclobutyl;
- o is 0, 1, 2, 3, 4 or 5;
- p is 0 or 1;
- and
- q is 0, 1, 2, 3, 4 or 5, provided that if Y is cycloalkyl and p is 1 the sum of o+p+q is not less than 3 or greater than 5, and otherwise the sum of o+p+q is 5;
- wherein the mitofusin activator comprises about 60% trans-stereoisomer or greater on a molar basis relative to cis-stereoisomer.
A composition comprising:
- a mitofusin activator or a pharmaceutically acceptable salt thereof, the mitofusin activator having a structure represented by the following formula:
- wherein:
- Z is phenyl or substituted phenyl;
- R2 and R3 are H;
- R4 and R5 are H;
- Y is O, CH2 or cycloalkyl;
- wherein the cycloalkyl is cyclopropyl or cyclobutyl;
- o is 0, 1, 2, 3, 4 or 5;
- p is 0 or 1;
- and
- q is 0, 1, 2, 3, 4 or 5, provided that if Y is cycloalkyl and p is 1 the sum of o+p+q is not less than 3 or greater than 5, and otherwise the sum of o+p+q is 5;
- wherein the mitofusin activator comprises about 60% trans-stereoisomer or greater on a molar basis relative to cis-stereoisomer.
Dependencies are inferred from the claim text.