JNK inhibitors as anticancer agents
Inventors
Salem, Aliasger K. • Abdelrahman, Somaya Ali Mohammed Elsaid
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Assignees
University of Iowa Research Foundation UIRF
Member
Glycos Biomedical LtdWe are UK/US entity with a team based in Maryland and North Carolina comprising an expert team that has linked triggers to disease states including TBI and acute injuries associated with radiation, acute lung injury and infection.
We are UK/US entity with a team based in Maryland and North Carolina comprising an expert team that has linked triggers to disease states including TBI and acute injuries associated with radiation, acute lung injury and infection.
Publication Number
US-12624015-B2
Publication Date
2026-05-12
Expiration Date
Abstract
Compounds that inhibit JNK, e.g., JNK2 and/or JNK3, such as fused thiophenes, and methods of making and using the compounds are provided.
Core Innovation
The invention describes fused thiophene anticancer compounds that inhibit JNK2 and JNK3 (c-Jun N-terminal kinase), including compounds according to a compound of formula (I) or a compound of formula (II). The compounds include variable substituents R and X, and ring-forming substituents R1 and R2 that are selected to together form a C6 or C7 ring. The compounds are further defined to include pharmaceutically acceptable salts.
The disclosure frames the compounds as protein kinase inhibitors targeting mitogen-activated protein kinases (MAPKs), specifically JNK2 and JNK3, as part of an approach for anticancer treatment. The problem addressed in the background is the need for anticancer agents with activity through JNK2/JNK3 inhibition.
The summary explains that the compounds are associated with anticancer activity based on JNK2/JNK3 inhibition and includes in vitro screening results for representative compounds, including MTS assay data reported as IC50 values and pIC50 values. The disclosure also provides illustrative embodiments focused on fused thiophene structures and substituent classes such as benzamide, benzylamine, and urea.
The disclosure further describes formulations using nanoparticles and microparticles for delivery, including formulations using polymers such as PLGA and other polymer systems. In addition, synthetic schemes and intermediate preparation are outlined for benzamide, benzylamine, and urea derivatives within the described chemical series.
Claims Coverage
The independent claims cover a structural class of compounds of formula (I) defined by substituent constraints for R, X, and ring-forming R1/R2, and pharmaceutical compositions that include nanoparticles comprising the claimed compound. Across these independent claims, the inventive features focus on the fused thiophene compound structure defined by the formula constraints and on nanoparticle-containing pharmaceutical compositions with specified polymer components.
Compound of formula (I) with substituent constraints
A compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is hydrogen, halo, alkyl, alkenyl, alkynyl, alkoxy, haloalkyl, substituted alkyl, carbocycle or heterocycle; wherein X is CONH(C1-C6) alkyl; and wherein R1 and R2 independently are alkyl, alkenyl, alkynyl, alkoxy, or substituted alkyl or R1 and R2 together form a C6 or C7 ring.
Pharmaceutical composition with nanoparticles comprising the compound
A pharmaceutical composition containing nanoparticles comprising the compound of formula (I) or a pharmaceutically acceptable salt of that compound.
Overall, the claims define a compound class by formula (I) substituent and ring-forming constraints and extend the coverage to pharmaceutical compositions where the compound is included in nanoparticles.
Stated Advantages
Not explicitly described in patent.
Documented Applications
Not explicitly described in patent.
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