Back to results
US 12,577,251 B2Granted
Modulators of the sigma-2 receptor and their method of use
AssigneeTemple University of the Commonwealth System of Higher Education
InventorsBenjamin E. Blass, Daniel J. Canney, Kevin M. Blattner
Life of this patent
Estimating the term…
Abstract
Pharmaceutical compositions of the invention comprise functionalized lactone derivatives having a disease-modifying action in the treatment of diseases associated with dysregulation of sigma-2 receptor activity.
Claims6
A compound having formula (XVII):
- or
- pharmaceutically acceptable salt thereof, wherein:
- R3 is selected from a group consisting of a benzene ring that is optionally substituted with 0 to 3 R4 groups that are not hydrogen, a 4-pyridine ring that is optionally substituted with 0 to 2 R5 groups that are not hydrogen, a 3-pyridine ring that is optionally substituted with 0 to 2 R5 groups that are not hydrogen, and a 2-pyridine ring that is optionally substituted with 0 to 2 R5 groups that are not hydrogen;
- R4 is at each occurrence independently selected from the group consisting of hydrogen, OH, NO2, halogen, CN, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, heterocyclyl, —S(C1-6 linear alkyl), S(C3-7 branched alkyl), —S(C3-7 cycloalkyl), —SO2(C1-6 linear alkyl), SO2(C3-7 branched alkyl), —SO2(C3-7 cycloalkyl), COR6, CO2R7, CONR8aR8b, SO2NR8aR8b, NR9aR9b, NR9aCOR10, NR9aSO2R11, and NR9aSO2NR12aR12b;
- the terms R4a, R4b, R4c, R4d, and R4e may be used to designate individual R4 groups on a benzene ring;
- R5 is at each occurrence independently selected from the group consisting of hydrogen, OH, NO2, halogen, CN, C1-6 linear alkyl, C3-7 branched alkyl, C3-7 cycloalkyl, C1-6 linear alkoxy, C3-7 branched alkoxy, C3-7 cycloalkoxy, C1-6 linear haloalkyl, C3-7 branched haloalkyl, C1-6 linear haloalkoxy, heterocyclyl, —S(C1-6 linear alkyl), S(C3-7 branched alkyl), —S(C3-7 cycloalkyl), COR6, CO2R7, CONR8aR8b, SO2NR8aR8b, NR9aR9b, NR9aCOR10, NR9aSO2R11, and NR9aSO2NR12aR12b;
- the terms R5a, R5b, R5c, and R5d may be used to designate individual R5 groups on a pyridine ring;
- R6 is at each occurrence independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;
- R7 is at each occurrence independently selected from the group consisting of C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;
- R8a is at each occurrence independently selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;
- R8b is at each occurrence independently selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;
- R9a is at each occurrence independently selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;
- R9b is at each occurrence independently selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;
- R9a and R9b may be taken together with the atom to which they are bound to form a ring having from 3 to 7 ring atoms optionally containing an oxygen;
- R10 is at each occurrence independently selected from the group consisting of H, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;
- R11 is at each occurrence independently selected from the group consisting of C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;
- R12a is at each occurrence independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;
- R12b is at each occurrence independently selected from the group consisting of hydrogen, C1-6 linear alkyl, C3-7 branched alkyl, and C3-7 cycloalkyl;
- and
- n is 1, 2, or 3.
17 more elements
Dependencies are inferred from the claim text.