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US 12,187,722 B2Granted
Small molecule inhibitors of TEAD transcription factors
AssigneeThe General Hospital Corporation
InventorsXu Wu, Pranab Maiti, Chandrasekhar Abbineni, Krishna Chaitanya Talluri, Sunil Kumar Panigrahi, Gopala Krishna Jarugumilli, Yang Sun
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Abstract
The present disclosure compounds, as well as their compositions and methods of use. The compounds inhibit the activity of the TEAD transcription factor, and are useful in the treatment of diseases related to the activity of TEAD transcription factor including, e.g., cancer and other diseases.
Claims23
A compound of Formula:
- or a pharmaceutically acceptable salt thereof, wherein:
- RN is H or C1-6 alkyl;
- R1 is OH or OC1-6 alkyl;
- A3 is CR3 or N;
- A5 is CH or N;
- A7 is CH or N;
- A10 is CH or N;
- R3 is H, unsubstituted C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, halogen, C1-6 haloalkyl, CN, ORa1, SRa1, NRc1Rd1, C(O)ORal, C(O)NRc1Rd1 or C1-6 alkyl that is substituted by 1, 2, or 3 substituents each independently selected from halogen, C1-6 haloalkyl, CN, ORa1, SRa1, and NRc1Rd1,
- R8 is Cy8A, OCy8A, O(C1-3 alkylenyl)Cy8A, NHCy8A, NH(C1-3 alkylenyl)Cy8A, N(C1-6 alkyl)Cy8A, or N(C1-6 alkyl)(C1-3 alkylenyl)Cy8A;
- Cy8A is a group of one of the following formulae:
- and
- Ra1, Rb1, Rcl and Rd1 are each independently selected from H, C1-6 alkyl, HO—C1-6 alkylene, C1-6 alkoxy-C1-6 alkylene, C6-10 aryl, C2-6 alkenyl and C2-6 alkynyl.
9 more elements
A compound selected from the group consisting of:
- or a pharmaceutically acceptable salt of any of the foregoing.
A compound selected from the group consisting of:
- or a pharmaceutically acceptable salt of any of the foregoing.
Dependencies are inferred from the claim text.