Therapeutic compounds
AssigneeUniversity of Florida Research Foundation, Inc.
InventorRaymond G. Booth
Life of this patent
Estimating the term…
Abstract
The invention relates to protein binding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C disorders, including diseases and disorders mediated by GPCRs.
Claims19
A method of treating or preventing a GPCR-mediated disorder in a subject comprising administering to the subject identified as in need thereof a PAT compound.
A method of inhibiting 5-HT2C in a subject identified as in need of such treatment, comprising administering a PAT compound.
A method of treating obesity in a subject comprising administering to the subject identified as in need thereof a PAT compound capable of selectively inhibiting the 5-HT2c relative to 5-HT2a or 5-HT2b.
A method for identifying a compound that is capable of modulating 5-HT2c activity comprising;
- (i) producing a three-dimensional representation of a molecule or molecular complex, wherein said molecule or molecular complex comprises a binding pocket defined by structure coordinates of 5-HT2c;
- or b) a three-dimensional representation of a homologue of said molecule or molecular complex, wherein said homologue comprises a binding pocket that has a root mean square deviation from the backbone atoms of said amino acids of not more than about 2.0 angstroms;
- (ii) producing a three-dimensional representation of a test compound;
- (iii) assessing the binding interaction of the test compound with the target.
A compound that is:
- wherein,
- R1 is independently H, NH2, NH(alkyl), N(alkyl)2;
- R2 is independently —(CH2)n-;
- Each n is independently 1 or 2;
- R3 is independently H, OH, or halo;
- R4 is independently H, OH, or halo
- Each R5 is independently H, alkyl, or halo;
- R6 is independently H or alkyl;
- and
- R7 independently H, N(alkyl)2;
- or salt, hydrate or solvate thereof.
A compound of the formula:
- wherein,
- R1 is independently H, NH2, NH(alkyl), N(alkyl)2;
- R2 is independently —(CH2)n-;
- Each n is independently 1 or 2;
- R3 is independently H, OH, or halo;
- R4 is independently H, OH, or halo
- Each R5 is independently H, alkyl, or halo;
- R6 is independently H or alkyl;
- R7 independently H, N(alkyl)2;
- and
- R8 is independently aryl or heteroaryl, each optionally substituted with 1-4 independent R5;
- or salt, hydrate or solvate thereof.
Dependencies are inferred from the claim text.