Blockers of the growth hormone receptor in disease prevention and treatment
Compounds and methods for treating diseases or conditions affected by the activity or expression of genes/proteins related to human GH, GHR, STAT5, SOCS, IGF-1, insulin are provided. Monoclonal antibodies for treating diseases or conditions related to growth hormone and growth hormone receptor activity are also provided.
1. A compound having formula I:
or a pharmaceutically acceptable salt thereof;
wherein:
R 1 is NO 2 , SO 3 H, NH 2 , or halogen, and
R 2 is hydrogen, NO 2 , SO 3 H, NH 2 , or C 1-8 alkyl, or halogen.
2. A compound having formula II:
or a pharmaceutically acceptable salt thereof;
wherein:
R 1 is hydrogen, C 1-8 alkyl, or halogen, and
R 2 is C 1-8 alkyl, or halogen.
3. A method inhibiting GH induced phosphorylation STAT5, the method comprising:
administering to a subject a therapeutically effective amount of a compound selected from the group consisting of:
and combinations thereof and pharmaceutically acceptable salts thereof;
wherein:
R 1 is hydrogen, NO 2 , SO 3 H, NH 3 , C 1-8 alkyl, or halogen, and
R 2 is hydrogen, NO 2 , SO 3 H, NH 3 , C 1-8 alkyl, or halogen.
4. The method of claim 3 wherein the compound is selected from the group consisting of:
and
combinations thereof, and pharmaceutically acceptable salts thereof.
5. The compound of claim 1 wherein R 1 is NO 2 or SO 3 H and R 2 is hydrogen or C 1-8 alkyl.
6. The compound of claim 1 wherein R 1 is NH 2 or halogen and R 2 is hydrogen or C 1-8 alkyl.
7. The method of claim 3 wherein is hydrogen.
8. The method of claim 3 wherein R 2 is hydrogen.
9. The method of claim 3 wherein the compound is selected from the group consisting of:
and pharmaceutically acceptable salts thereof.
10. The method of claim 3 wherein the compound is selected from the group consisting of:
and pharmaceutically acceptable salts thereof.
11. The method of claim 3 wherein the compound is selected from the group consisting of:
and pharmaceutically acceptable salts thereof.