发明名称 |
Soluble mTOR complexes and modulators thereof |
摘要 |
The present invention relates to small molecule modulators of mTORC1 and mTORC2, syntheses thereof, and intermediates thereto. Such small molecule modulators are useful in the treatment of proliferative diseases (e.g., benign neoplasms, cancers, inflammatory diseases, autoimmune diseases, diabetic retinopathy) and metabolic diseases. Novel small molecules are provided that inhibit one or more of mTORC1, mTORC2, and PI3K-related proteins. Novel methods of providing soluble mTORC1 and mTORC2 complexes are discussed, as well as methods of using the soluble complexes in a high-throughput manner to screen for inhibitory compounds. |
申请公布号 |
US8889706(B2) |
申请公布日期 |
2014.11.18 |
申请号 |
US201213670013 |
申请日期 |
2012.11.06 |
申请人 |
Whitehead Institute for Biomedical Research;Dana-Farber Cancer Institute, Inc. |
发明人 |
Gray Nathanael;Chang Jae Won;Zhang Jianming;Thoreen Carson C.;Kang Seong Woo Anthony;Sabatini David M.;Liu Qingsong |
分类号 |
A61K31/4375;C07D471/06;C07D471/04;C07D498/04;C07D471/14;C07D519/00 |
主分类号 |
A61K31/4375 |
代理机构 |
Wolf, Greenfield & Sacks, P.C. |
代理人 |
Wolf, Greenfield & Sacks, P.C. ;Backer C. Hunter;Weatherhead Robin A. |
主权项 |
1. A compound selected from the group consisting of:and pharmaceutically acceptable salts thereof. |
地址 |
Cambridge MA US |