Thrombopoietin mimetics
View Patent ↗Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative.
1. A compound represented by the following formula:
wherein AR is a polycyclic aromatic ring containing 3 to 16 carbon atoms and containing one or more heteroatoms, provided that when the number of carbon atoms is 3 the aromatic ring contains at least two heteroatoms and when the number of carbon atoms is 4 the aromatic ring contains at least one heteroatom, and optionally substituted with one or more substituents selected from the group consisting of: alkyl, trifluoromethyl and hydroxy; and
R 1 and R 2 are independently selected from hydrogen and alkyl, provided that R 1 and R 2 are not both hydrogen;
or a pharmaceutically acceptable salt thereof.
2. A compound according to claim 1 wherein: the AR contains one or two heteroatoms and is substituted with one or more substituents selected from the group consisting of: alkyl, trifluoromethyl and hydroxy; and
R 1 and R 2 are independently selected from hydrogen and alkyl, provided that R 1 and R 2 are not both hydrogen;
or a pharmaceutically acceptable salt thereof.
3. A compound according to claim 2 wherein: the AR is substituted with one or two substituents selected from the group consisting of: alkyl, trifluoromethyl and hydroxy; and
R 1 and R 2 are independently selected from hydrogen and alkyl, provided that R 1 and R 2 are not both hydrogen;
or a pharmaceutically acceptable salt thereof.
4. A compound according to claim 3 wherein: R 1 and R 2 are both methyl;
or a pharmaceutically acceptable salt thereof.
5. A compound according to claim 3 wherein: one of R 1 and R 2 is hydrogen and the other is propyl;
or a pharmaceutically acceptable salt thereof.
6. A pharmaceutical composition which comprises a compound of claim 1 and a pharmaceutically acceptable carrier.
7. A process for preparing a pharmaceutical composition containing a pharmaceutically acceptable carrier or diluent and an effective amount of the compound of claim 1 , which process comprises bringing said compound into association with the pharmaceutically acceptable carrier or diluent.
8. A pharmaceutical composition which comprises a compound of claim 2 and a pharmaceutically acceptable carrier.
9. A pharmaceutical composition which comprises a compound of claim 3 and a pharmaceutically acceptable carrier.
10. A pharmaceutical composition which comprises a compound of claim 4 and a pharmaceutically acceptable carrier.
11. A pharmaceutical composition which comprises a compound of claim 5 and a pharmaceutically acceptable carrier.