Kappa opioid receptor effectors and uses thereof
AssigneesThe Scripps Research Institute, University of Kansas
InventorsJeffrey Aube, Laura Bohn, Thomas Edward Prisinzano, Frank John Schoenen, Kevin John Frankowski
Life of this patent
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Abstract
The present invention is a selective kappa opioid receptor effector, or a pharmaceutically acceptable salt thereof, useful for treating ethanol use disorder withdrawal, anxiety and/or depression, schizophrenia, mania or post-traumatic stress disorder.
Claims10
1-12. (canceled)
A pharmaceutical composition comprising an effective amount of a kappa opioid receptor effector, or a pharmaceutically acceptable salt thereof, and a physiologically acceptable carrier, wherein the kappa opioid receptor effector is an antagonist of Formula I or agonist of Formula II:
- wherein
- X, Y and Z are independently selected from H,H;
- O;
- S or NH;
- R1 is H, a halogen group or a substituted or unsubstituted lower alkyl or alkoxy group;
- R2 is present or absent, and when present is a substituent on one or more ring atoms and is for each ring atom independently H, a halogen group, or a substituted or unsubstituted lower alkyl or alkoxy group;
- X′ is hydrogen or Br;
- each Z′ is independently C, CH or N;
- n is 0 or 1;
- R3 is phenyl, substituted phenyl, naphthyl, cycloalkyl, propargyl or allyl;
- and
- R4 is aryl, heteroaryl or cycloalkyl.
A method for selectively modulating the activity of kappa opioid receptor comprising contacting a kappa opioid receptor with a kappa opioid receptor effector, or a pharmaceutically acceptable salt thereof, wherein the kappa opioid receptor effector is an antagonist of Formula I or agonist of Formula II:
- wherein
- X, Y and Z are independently selected from H,H;
- O;
- S or NH;
- R1 is H, a halogen group or a substituted or unsubstituted lower alkyl or alkoxy group;
- R2 is present or absent, and when present is a substituent on one or more ring atoms and is for each ring atom independently H, a halogen group, or a substituted or unsubstituted lower alkyl or alkoxy group;
- X′ is hydrogen or Br;
- each Z′ is independently C, CH or N;
- n is 0 or 1;
- R3 is phenyl, substituted phenyl, naphthyl, cycloalkyl, propargyl or allyl;
- and
- R4 is aryl, heteroaryl or cycloalkyl.
A method of selectively modulating kappa opioid receptor activity in a patient comprising administering to a subject in need thereof a kappa opioid receptor effector, or a pharmaceutically acceptable salt thereof, wherein the kappa opioid receptor effector is an antagonist of Formula I or agonist of Formula II:
- wherein
- X, Y and Z are independently selected from H,H;
- O;
- S or NH;
- R1 is H, a halogen group or a substituted or unsubstituted lower alkyl or alkoxy group;
- R2 is present or absent, and when present is a substituent on one or more ring atoms and is for each ring atom independently H, a halogen group, or a substituted or unsubstituted lower alkyl or alkoxy group;
- X′ is hydrogen or Br;
- each Z′ is independently C, CH or N;
- n is 0 or 1;
- R3 is phenyl, substituted phenyl, naphthyl, cycloalkyl, propargyl or allyl;
- and
- R4 is aryl, heteroaryl or cycloalkyl.
Dependencies are inferred from the claim text.