MEK inhibitors and methods of their use
Inventors
Aay, Naing • Anand, Neel Kumar • Blazey, Charles M. • Bowles, Owen Joseph • Bussenius, Joerg • Costanzo, Simona • Curtis, Jeffry Kimo • Defina, Steven Charles • Dubenko, Larisa • Joshi, Anagha Abhijit • Kennedy, Abigail R. • Kim, Angie Inyoung • Koltun, Elena S. • Manalo, Jean-Claire Limun • Peto, Csaba J. • Rice, Kenneth D. • Tsang, Tsze H.
Assignees
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Publication Number
US-11597699-B2
Publication Date
2023-03-07
Expiration Date
Abstract
Disclosed are compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof. Such compounds are MEK inhibitors and are useful in the treatment of proliferative diseases, such as cancer. Also disclosed are pharmaceutical compositions containing such compounds as well as methods of using the compounds and compositions of the invention in the treatment of cancer.
Core Innovation
The invention relates to substituted azetidin-3-ol derivatives and pharmaceutically acceptable salts that share the core 1-({3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl}carbonyl) scaffold. The disclosed compounds vary at the azetidine substituent and include multiple described substituent types, while retaining the shared difluoro- and fluoro-iodoaryl motif and azetidin-3-ol framework.
Representative embodiments include azetidin-3-ol, azetidin-3-one, azetidin-3-one oxime, azetidin-3-amine, carboxamide, carbamate, oxime, and related analogs, together with substituted amines, cycloalkylamino, heteroaryl, piperidinyl, pyrrolidinyl, aminoalkyl, hydroxy, and hydroxy-substituted side chains. The partial content also includes structure listings and characterization information for numerous compounds, showing a range of variants within the same core motif.
The claimed therapeutic use is administration of a therapeutically effective amount of 1-({3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl}carbonyl)-3-[(2S)-piperidin-2-yl]azetidin-3-ol or a pharmaceutically acceptable salt thereof. This method is stated to arrest the development of or cause the regression of malignant fibrous histiocytoma.
Claims Coverage
The provided material includes one independent claim set centered on one inventive feature: administering a therapeutically effective amount of a specified azetidin-3-ol derivative, or a pharmaceutically acceptable salt, to treat malignant fibrous histiocytoma. The stated therapeutic outcomes are arresting development and causing regression.
Administration of a specific azetidin-3-ol derivative for malignant fibrous histiocytoma
A method of arresting the development of or causing the regression of malignant fibrous histiocytoma by administering to a patient in need thereof a therapeutically effective amount of 1-({3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl}carbonyl)-3-[(2S)-piperidin-2-yl]azetidin-3-ol or a pharmaceutically acceptable salt thereof.
Overall, the claim coverage is directed to a single therapeutic method using the specified substituted azetidin-3-ol compound, or a pharmaceutically acceptable salt, to arrest the development of or cause regression of malignant fibrous histiocytoma.
Stated Advantages
Arrests the development of malignant fibrous histiocytoma.
Causes regression of malignant fibrous histiocytoma.
Documented Applications
Treatment of malignant fibrous histiocytoma by administering the specified compound or a pharmaceutically acceptable salt to a patient in need thereof.
Treatment of hyperproliferative diseases and cancer by inhibiting MEK using compounds of Formula (I).
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