Kappa opioid receptor selective compounds, compositions, and uses thereof
AssigneesThe Trustees of Columbia University in the City of New York, Icahn School of Medicine at Mount Sinai
InventorsJonathan Javitch, Marie-Laure Rives, Marta Filizola, Thomas E. Prisinzano
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Abstract
The present invention provides, inter alia, compounds of formula (I): (structurally represented). Also provided are pharmaceutical compositions containing such compounds and methods for treating or ameliorating the effects of a medical condition in a subject using such compounds or pharmaceutical compositions.
Claims11
A compound of formula I:
- wherein
- X1 is N;
- n is an integer between 1 and 10;
- HET is a heteroaromatic ring;
- and
- R is a —C1-4alkylhalo;
- or
- crystalline forms, hydrates, or salts thereof.
A compound of formula II:
- wherein
- X1 and X3 are N;
- X2 is selected from the group consisting of N, O, and S;
- n is an integer between 1 and 10;
- and
- R is a —C1-4alkylhalo;
- or
- crystalline forms, hydrates, or salts thereof.
A compound of formula V:
- wherein
- n is selected from an integer between 1 and 10;
- and
- R is a —C1-4alkylhalo;
- or
- crystalline forms, hydrates, or salts thereof.
A method for treating pain in a subject comprising administering to the subject an effective amount of a non-addictive pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound of formula I:
- wherein
- X1 is N;
- n is an integer between 1 and 10;
- HET is a heteroaromatic ring;
- and
- R is a —C1-4alkylhalo;
- or
- crystalline forms, hydrates, or salts thereof;
- further wherein the compound is biased toward G protein activation over arrestin.
A compound of the structure:
- or crystalline forms, hydrates, or salts thereof.
Dependencies are inferred from the claim text.