Compounds useful for the treatment and prevention of pain and screening methods therefor
OwnerEthan Burstein, Leila Malik +1inventors
InventorsEthan Burstein, Leila Malik, Nicholas Kelly
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Abstract
The present invention relates to the composition of compounds having the generic structure: and to a method of treatment or prevention of pain using the above compounds.
Claims13
A compound having the chemical formula:
- wherein:
- R1 is selected from the group consisting of hydrogen, unsubstituted or substituted alkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted phenyl, unsubstituted or substituted naphthyl, unsubstituted or substituted phenylalkyl, unsubstituted or substituted heteroaryl, unsubstituted or substituted heteroalicyclyl, cyano, unsubstituted or substituted acyl, unsubstituted or substituted alkoxycarbonyl, unsubstituted or substituted alkylaminocarbonyl, unsubstituted or substituted phenylaminocarbonyl, unsubstituted or substituted alkylthio, unsubstituted or substituted alkylsulfonyl, unsubstituted or substituted alkylsulfinyl, unsubstituted or substituted phenylthio, unsubstituted or substituted phenylsulfinyl, unsubstituted or substituted phenylsulfonyl and unsubstituted and substituted or unsubstited cycloalkyl;
- R2, R3, R4, R5, R6, R7, R8, R9 are independently selected from the group consisting of hydrogen, hydroxy, protected hydroxy, unsubstituted or substituted alkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted alkynyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted cycloalkenyl, unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl, unsubstituted or substituted heteroalicyclyl, unsubstituted or substituted heteroarylalkyl, unsubstituted or substituted heteroalicyclylalkyl, halogenated ether, nitro, amino, halogen, perhaloalkyl, —NX1aX1b, —CN, —C(=Z)X1a, —C(=Z)OX1a, —C(=Z)NX1aX1b, —N(X1a)—C(=Z)X1b, —N(X1a)—C(=Z)NX1bX1c, —OC(=Z)X1a, —S(═O)X1a, —S(═O)2X1a, and —SX1a, and,
- R10 is selected from the group consisting or oxygen, —NH or —NX1d wherein:
- Z is oxygen or sulfur;
- and,
- X1a, X1b, X1c and X1d are independently selected from the group consisting of hydrogen, substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl, unsubstituted or substituted heteroalicyclyl, unsubstituted or substituted alkyl, unsubstituted or substituted alkenyl, unsubstituted or substituted alkynyl, unsubstituted or substituted cycloalkyl and unsubstituted or substituted cycloalkenyl.
A compound having a chemical structure selected from the group consisting of:
A method of treating or preventing pain, comprising administering to a patient in need thereof an effective amount of at least one compound of this invention, or a salt or prodrug thereof.
A method of screening for a compound that modulates the activity of a human MrgX1, a simian MrgX1, a human MrgX2 or a simian MrgX2 receptor comprising:
- contacting a test compound with a recombinant cell comprising a recombinant nucleic acid that expresses the human MrgX1, the simian MrgX1, the human MrgX2 or the simian MrgX2 receptor, provided that the cell does not contain an endogenous nucleic acid that expresses the functional receptor;
- and,
- detecting changes in the activity of the receptor.
Dependencies are inferred from the claim text.