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US 12,577,208 B2Granted
TEAD inhibitors and uses thereof
AssigneeEHE Foundation
InventorAlfredo C. Castro
Life of this patent
Estimating the term…
Abstract
The present invention provides compounds, compositions thereof, and methods of using the same.
Claims21
A method for treating cancer in a patient, or inhibiting the progress of cancer in a patient, comprising administering to the patient a compound of Formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- L1 is —NH—CH2— or —NH—C(O)—;
- Ring A is phenyl, optionally substituted 1-2 times by halogen, —CN, —NO2, or —C1-6 aliphatic substituted 0-6 times by halogen, —CN, or —NO2;
- R2 is an optionally substituted 5-membered heteroaryl ring having 2 nitrogen atoms;
- R3 is —H;
- R4 is halogen, —S(O)2N(R)2, —S(O)N(R)2, or —C(O)N(R)2;
- R6 is —H or —C1-6 aliphatic substituted 0-6 times by halogen, —CN, or —NO2;
- and
- each R is independently —H or optionally substituted —C1-6 aliphatic;
- wherein the cancer is selected from the group consisting of lung cancer, breast cancer, basal cell carcinoma, squamous cell carcinoma, cancer of head or neck, melanoma, vascular cancer, prostate cancer, pancreatic cancer, meningioma, renal cell carcinoma, colorectal cancer, schwannoma, cholangiocarcinoma, glioma, liver cancer, and gastric cancer.
7 more elements
A method for treating a patient having a disease or disorder associated with increased TEAD expression or increased TEAD activity, comprising administering to the patient a compound of Formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- L1 is —NH—CH2— or —NH—C(O)—;
- Ring A is phenyl, optionally substituted 1-2 times by halogen, —CN, —NO2, or —C1-6 aliphatic substituted 0-6 times by halogen, —CN, or —NO2;
- R2 is an optionally substituted 5-membered heteroaryl ring having 2 nitrogen atoms;
- R3 is —H;
- R4 is halogen, —S(O)2N(R)2, —S(O)N(R)2, or —C(O)N(R)2;
- R6 is —H or —C1-6 aliphatic substituted 0-6 times by halogen, —CN, or —NO2;
- and
- each R is independently-H or optionally substituted-C1-6 aliphatic.
6 more elements
A method for inhibiting TEAD activity or Hippo pathway in a patient in need thereof, comprising administering to the patient a compound of Formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- L1 is —NH—CH2— or —NH—C(O)—;
- Ring A is phenyl, optionally substituted 1-2 times by halogen, —CN, —NO2, or —C1-6 aliphatic substituted 0-6 times by halogen, —CN, or —NO2;
- R2 is an optionally substituted 5-membered heteroaryl ring having 2 nitrogen atoms;
- R3 is —H;
- R4 is halogen, —S(O)2N(R)2, —S(O)N(R)2, or —C(O)N(R)2;
- R6 is —H or —C1-6 aliphatic substituted 0-6 times by halogen, —CN, or —NO2;
- and
- each R is independently —H or optionally substituted-C1-6 aliphatic.
6 more elements
Dependencies are inferred from the claim text.