发明名称 |
N-BENZYLINDOLE MODULATORS OF PPARG |
摘要 |
<p>The invention provides molecular entities that bind with high affinity to PPARG (PPAR?), and inhibit kinase-mediated (e.g., cdk5-mediated) phosphorylation of PPARG, but do not exert an agonistic effect on PPARG. Compounds of the invention can be used for treatment of conditions in patients wherein PPARG plays a role, such as diabetes, insulin resistance, impaired glucose tolerance, pre-diabetes, hyperglycemia, hyperinsulinemia, obesity, or inflammation. Side effects of significant weight gain, edema, impairment of bone growth or formation, or cardiac hypertrophy, or any combination thereof, can be avoided in the mammal receiving the compound. Methods of preparation of the compounds, bioassay methods for evaluating compounds of the invention as non-agonistic PPARG binding compounds, and pharmaceutical compositions are also provided.</p> |
申请公布号 |
WO2012170561(A1) |
申请公布日期 |
2012.12.13 |
申请号 |
WO2012US41137 |
申请日期 |
2012.06.06 |
申请人 |
THE SCRIPPS RESEARCH INSTITUTE (T.S.R.I.);KAMENECKA, THEODORE MARK;GRIFFIN, PATRICK R.;KOENIG, MARCEL;ASTEIAN, ALICE;BLAYO, ANNE-LAURE;HE, YUANJUN;SHIN, YOUSEUNG |
发明人 |
KAMENECKA, THEODORE MARK;GRIFFIN, PATRICK R.;KOENIG, MARCEL;ASTEIAN, ALICE;BLAYO, ANNE-LAURE;HE, YUANJUN;SHIN, YOUSEUNG |
分类号 |
C07D209/42;A61K31/404;A61K31/4245;A61K31/4439;C07D401/06;C07D403/12;C07D405/12;C07D409/12 |
主分类号 |
C07D209/42 |
代理机构 |
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代理人 |
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主权项 |
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地址 |
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