Substituted [1,2,4]triazolo[4,3-A]pyrazines for medicaments and pharmaceutical compositions
The present invention relates to derivatives of known active pharmaceutical compounds. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more reactions which may be considered to represent a change of oxidation state. We refer to these compounds generally as redox derivatives. The derivatives of the invention may be related to the original parent active pharmaceutical compound by only a single step transformation, or may be related via several synthetic steps including one or more changes of oxidation state. Exemplary derivatives have the formula
1. A compound according to formula 3 below:
wherein:
is
is independently selected from the group consisting of:
R 1 is independently at each occurrence H or COCH 3 ;
R 2 is independently at each occurrence C 1 -C 4 alkyl; and
R 3 is independently at each occurrence selected from the group consisting of: H and C 1-4 alkyl; or
is independently selected from the group consisting of:
is independently selected from the group consisting of:
R 1 is independently at each occurrence COCH 3 ;
R 2 is independently at each occurrence C 1 -C 4 alkyl; and
R 3 is independently at each occurrence selected from the group consisting of: H and C 1-4 alkyl.
2. The compound of claim 1 , wherein
3. The compound of claim 1 , wherein
4. The compound of claim 1 , wherein
5. The compound of claim 4 , wherein R 2 is methyl, ethyl, propyl, isopropyl, butyl, or tert-butyl.
6. The compound of claim 1 , wherein
7. A pharmaceutical composition comprising:
one or more pharmaceutical excipients; and
a compound according to formula 3 below:
wherein:
is
is independently selected from the group consisting of:
R 1 is independently at each occurrence H or COCH 3 ;
R 2 is independently at each occurrence H or C 1 -C 4 alkyl; and
R 3 is independently at each occurrence selected from the group consisting of: H and C 1-4 alkyl; or
is independently selected from the group consisting of:
is independently selected from the group consisting of:
R 1 is independently at each occurrence COCH 3 ;
R 2 is independently at each occurrence H or C 1 -C 4 alkyl; and
R 3 is independently at each occurrence selected from the group consisting of: H and C 1-4 alkyl.
8. The compound of claim 1 , wherein the compound is
9. The pharmaceutical composition of claim 7 , wherein the compound is
10. The pharmaceutical composition of claim 7 , wherein R 2 is independently at each occurrence C 1 -C 4 alkyl.