发明名称 |
QUINAZOLINES AND AZAQUINAZOLINES AS DUAL INHIBITORS OF RAS/RAF/MEK/ERK AND PI3K/AKT/PTEN/MTOR PATHWAYS |
摘要 |
The present application provides novel quinazolines and azaquinazolines and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in for co-regulating RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways by administering a therapeutically effective amount of one or more of the compounds of formula (I), wherein X, Y, T and R4, and R6 to R8′ are defined herein, to a patient. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR pathways. A variety of conditions can be treated using these compounds and include diseases which are characterized by abnormal cellular proliferation. In one embodiment, the disease is cancer.; |
申请公布号 |
US2017027953(A1) |
申请公布日期 |
2017.02.02 |
申请号 |
US201615290788 |
申请日期 |
2016.10.11 |
申请人 |
Asana BioSciences, LLC |
发明人 |
Thompson Scott K.;Smith Roger A.;Reddy Sanjeeva;John Tyler M.;Nyavanandi Vijay Kumar;Subramanya Hosahalli;Potluri Vijay;Panigrahi Sunil Kumar;Nadipalli Prabhakara Rao;Sengupta Saumitra |
分类号 |
A61K31/5377 |
主分类号 |
A61K31/5377 |
代理机构 |
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代理人 |
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主权项 |
1. A method for co-regulating RAS/RAF/MEK/ERK and PI3K/AKT/PTEN/mTOR, said method comprising administering a therapeutically effective amount of a compound of formula (I) to a patient in need thereof: wherein:
X is CH or N;Y is H, optionally substituted C1-C6 alkyl, OR1 or NR2R3;T is H or C1-C6 alkoxy;R1 is optionally substituted C1-C6 alkyl, optionally substituted (C1-C6 alkyl)OH, optionally substituted (C1-C6 alkyl)OC1-C6 alkyl, optionally substituted C3-C8 cycloalkyl, optionally substituted (C1-C6 alkyl)NH2, optionally substituted (C1-C6 alkyl)CO2H, or optionally substituted (C1-C6 alkyl)CONH2;R2 and R3 are joined to form an optionally substituted heterocycle;R4 is optionally substituted morpholine;R6 is optionally substituted aryl or optionally substituted heteroaryl;R7 is optionally substituted aryl, optionally substituted C1-C6 alkyl, or optionally substituted heteroaryl;R8 is H or halogen; andR8′ is halogen. |
地址 |
Lawrenceville NJ US |