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US 10,329,304 B2Granted
Compounds and methods for inhibition of hedgehog signaling and phosphodiesterase
AssigneeVanderbilt University
InventorsCharles C. Hong, Charles H. Williams, Jonathan Hempel, T K Feaster, Don H. Rubin, Gary Sulikowski, Jijun Hao, Audrey Frist
Life of this patent
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Abstract
Compounds and compositions, and methods of use thereof, are provided and have utility in inhibiting hedgehog signaling and/or phosphodiesterase-4 activity.
Claims13
A compound according to a formula selected from the group consisting of:
- or pharmaceutically-acceptable salts thereof;
- or
- or pharmaceutically-acceptable salts thereof;
- or
- or pharmaceutically-acceptable salts thereof, wherein
- (i) X is selected from
- (ii) R1 is selected from
- and
- (iii) R5 is selected from
6 more elements
A pharmaceutical composition, comprising a pharmaceutically-acceptable carrier;
- and a compound or pharmaceutically-acceptable salts thereof, and a Smo antagonist, wherein the compound is of the formula:
- or a pharmaceutically-acceptable salt thereof, wherein
- (i) X is selected from
- (ii) Y is selected from C, N, O, and S;
- (iii) R1 is selected from H, CH2CH3, (CH2)2CH3,
- (iv) R2 is selected from
- (v) R3 is selected from H, CH3,
- (vi) R4 is selected from H,
- and
- (vii) R5 is selected from
- and
- (viii) R6 is selected from CH3,
- where
- so long as when X is
- R2 is
- R6 is
- then R1 is not
- and
- so long as when X is
- R2 is
- R6 is
- then R1 is not
- and
- so long as when X is
- Y is C, R3 is CH3, R2 is
- and R6 is
- then R1 is not
- and
- so long as when X is
- R2 is
- R6 is
- then R1 is not
- and
- so long as when X is
- Y is C, R3 is CH3, R2 is
- and R6 is
- then R1 is not
34 more elements
A kit, comprising a compound;
- and a device for administration of the compound or composition containing the compound, wherein the compound is of the formula
- or a pharmaceutically-acceptable salt thereof, wherein
- (i) X is selected from
- (ii) Y is selected from C, N, O, and S;
- (iii) R1 is selected from H, CH2CH3 (CH2)2CH3,
- (iv) R2 is selected from
- (v) R3 is selected from H, CH3,
- (vi) R4 is selected from H,
- and
- (vii) R5 is selected from
- and
- (viii) R6 is selected from CH3,
- where
- so long as when X is
- R2 is
- R6 is
- then R1 is not
- and
- so long as when X is
- R2 is
- R6 is
- then R1 is not
- and
- so long as when X is
- Y is C, R3 is CH3, R2 is
- and R6 is
- then R1 is not
- and
- so long as when X is
- R2 is
- and R6 is
- then R1 is not
- and
- so long as when X is
- Y is C, R3 is CH3, R2 is
- and R6 is
- then R1 is not
34 more elements
A kit, comprising a first compound;
- and further comprising a second compound or composition having Hh signaling inhibition activity, PDE4 inhibition activity, anti-cancer or anti-tumor activity, anti-viral activity, anti-angiogenic activity, anti-metastatic activity, anti-heart failure activity, and/or anti-inflammation activity, or wherein the second compound or composition is useful for treating a condition of interest, wherein the first compound is of the formula
- or a pharmaceutically-acceptable salt thereof, wherein
- (i) X is selected from
- (ii) Y is selected from C, N, O, and S;
- (iii) R1 is selected from H, CH2CH3 (CH2)2CH3,
- (iv) R2 is selected from
- (v) R3 is selected from H, CH3,
- (vi) R4 is selected from H,
- and
- (vii) R5 is selected from
- and
- (viii) R6 is selected from CH3,
- where
- so long as when X is
- R2 is
- and R6 is
- then R1 is not
- and
- so long as when X is
- R2 is
- R6 is
- then R1 is not
- and
- so long as when X is
- Y is C, R3 is CH3, R2 is
- and R6 is
- then R1 is not
- and
- so long as when X is
- R2 is
- and R6 is
- then R1 is not
- and
- so long as when X is
- Y is C, R3 is CH3, R2 is
- and R6 is
- then R1 is not
34 more elements
Dependencies are inferred from the claim text.