Triazolyl tropane derivatives
This invention relates to novel triazolyl tropane derivatives, their acceptable acid addition salts, solvates, hydrates and polymorphs thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by blocking or reducing the binding ability of the CCR5 receptor.
1. A compound of formula II:
or a salt, thereof; wherein:
each Y is independently selected from hydrogen or deuterium;
each Z is independently selected from hydrogen or deuterium; and
wherein each Y 1 is deuterium and each Y 2 is deuterium.
2. The compound of claim 1 , wherein each Z bound to the same carbon atom is the same.
3. The compound of claim 2 , wherein each Z is hydrogen.
4. The compound of claim 2 , wherein each member of at least one pair selected from Z 1 and Z 2 ; Z 3 and Z 4 ; Z 5 and Z 6 ; or Z 7 and Z 8 is simultaneously deuterium.
5. The compound of claim 1 , selected from any one of compounds set forth in the table below:
Cmpd
Y 1a
Y 1b
Y 2a
Y 2b
Y 2c
Z 1
Z 2
Z 3
Z 4
Z 5
Z 6
Z 7
Z 8
203
D
D
D
D
D
H
H
H
H
H
H
H
H
206
D
D
D
D
D
D
D
D
D
D
D
D
D
209
D
D
D
D
D
D
D
H
H
H
H
D
D
212
D
D
D
D
D
H
H
D
D
D
D
H
H.
or a pharmaceutically acceptable salt thereof.
6. The compound
or a pharmaceutically acceptable salt, thereof.
7. The compound of claim 1 , wherein any atom not designated as deuterium is present at its natural isotopic abundance.
8. A pyrogen-free composition comprising a compound of claim 1 or a pharmaceutically acceptable salt, thereof; and an acceptable carrier.
9. The composition of claim 8 formulated for pharmaceutical administration, wherein the carrier is a pharmaceutically acceptable carrier.