Patent classifications
C07D239/48
BRD4-kinase inhibitors as cancer therapeutics
Disclosed herein are compounds that are inhibitors of BDR4 and their use in the treatment of cancer. Methods of screening for selective inhibitors of BDR4 are also disclosed. In certain aspects, disclosed are compounds of Formula I through IV.
PIKFYVE KINASE INHIBITORS
The present invention relates to compounds useful as inhibitors of phosphatidylinositol-3-phosphate 5-kinase (PIKfyve) as well as their use for treating diseases and disorders associated with PIKfyve.
PIKFYVE KINASE INHIBITORS
The present invention relates to compounds useful as inhibitors of phosphatidylinositol-3-phosphate 5-kinase (PIKfyve) as well as their use for treating diseases and disorders associated with PIKfyve.
CYANO-PYRIMIDINE INHIBITORS OF EGFR/HER2
Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with EGFR and/or HER2 activity.
CYANO-PYRIMIDINE INHIBITORS OF EGFR/HER2
Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with EGFR and/or HER2 activity.
EGFR INHIBITOR, COMPOSITION, AND METHOD FOR PREPARATION THEREOF
Provided are the compounds of Formula I, a method for using these compounds as an EGFR inhibitor, and a pharmaceutical composition comprising the compounds. The compound is used for treatment, prevention or amelioration of diseases or conditions such as cancer or infection.
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EGFR INHIBITOR, COMPOSITION, AND METHOD FOR PREPARATION THEREOF
Provided are the compounds of Formula I, a method for using these compounds as an EGFR inhibitor, and a pharmaceutical composition comprising the compounds. The compound is used for treatment, prevention or amelioration of diseases or conditions such as cancer or infection.
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INHIBITORS OF ULK1/2 AND METHODS OF USING SAME
The present disclosure is directed to compounds, compositions, formulations and methods of use thereof in the treatment and prevention of ULK mediated diseases, including cancer.
2,4-DIAMINO-PYRIMIDINE COMPOUNDS AND METHOD FOR MAKING AND USING THE COMPOUNDS
Compounds within the scope of the present invention have a Formula 1
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or a salt or prodrug thereof, where ring A is selected from cycloaliphatic; ring B is aryl; R.sup.1 is selected from (C1-C10)alkyl, (C3-C10)cycloalkyl, halo, aryl, and heteroaryl; and R.sup.2 and R.sup.3 are independently selected from hydrogen and (C1-C6)alkyl. Disclosed compounds may have an IRAK4 IC.sub.50 of from 0.003 μM to 3.7 μM; a TAK1 IC.sub.50 of from 0.008 μM to 132 μM; and/or an IRAK4/TAK1 selectivity of from 1 to 450. Particular compounds may have an IRAK4/TAK1 selectivity of from 100 to 500. Disclosed compositions may be formulated as pharmaceutical compositions. A method for using the compounds and/or compositions also are disclosed. The method may comprise administering to a subject an effective amount of a compound within the scope of the present invention, particularly to selectively inhibit IRAK 1 and/or IRAK4 over TAK1.
Inhibitors of ACK1/TNK2 tyrosine kinase
Described are cancer therapies and anti-cancer compounds. In particular, disclosed are inhibitors of Ack1 tyrosine kinase and their use in the treatment of cancer. Methods of screening for new Ack1 tyrosine kinase inhibitors are also disclosed. In specific example, compound having Formula I through IV are disclosed.