Heteroaryl compounds and their use as therapeutic drugs
Inventors
Kim, Myeong-Seop • KIM, Sumin • Kim, Jin Kwan • Kim, Hadong • RYU, Ki Moon • Park, Seong Jin • Park, Taesun • SHEEN, Joon-Ho • Yoon, Taeyoung • JANG, Mi Yeon
Assignees
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Publication Number
US-12195446-B2
Publication Date
2025-01-14
Expiration Date
Abstract
The present invention provides heterocyclic compounds, the stereoisomer thereof, the enantiomer thereof, or the pharmaceutically acceptable salt, which are capable of modulating the activity of Mer receptor tyrosine kinase (MERTK). This invention also provides pharmaceutical compositions thereof, methods to prepare the said compounds, and the use of such compounds as a medicament.The present invention is directed to MERTK inhibitory compounds with marked potency, thereby having an outstanding potential for a pharmaceutical intervention of cancer and any other diseases related to MERTK dysregulation.
Core Innovation
The invention relates to a method of treating a cancer influenced by inhibition of Mer kinase by administering to a mammal in need thereof a composition comprising, as an active ingredient, a heterocyclic compound represented by Formula Ib, including stereoisomers, enantiomers, or pharmaceutically acceptable salts thereof. The heterocyclic compounds are defined by structural variables including X, W, V1, V2, X1 to X5, and substituent groups R3, R8, R9, R10, R11, R13 and R13', R14, R15 and R16, R17, and linker group L with l and m.
The disclosed subject matter further identifies specific heterocyclic nicotinamide derivatives as example compounds within the claimed scope, including multiple named examples and analogs with varied aryl, heteroaryl, biphenyl, piperazine, pyridyl, pyrazolyl, thienyl, morpholinomethyl, benzyloxy, and substituted phenyl side chains. The examples include stereochemical designations such as (1S,2S), (1R,2R), trans, and cis, and are characterized by 1H NMR, LC/ESI-MS, and ESI-MS data.
The document links the Formula Ib heterocyclic scaffold and the example compounds to Mer kinase inhibition, and states that the heterocyclic compounds inhibit Mer activity and are useful for cancer prevention/treatment. The cancer types expressly listed include anaplastic astrocytoma, lung cancer, cervical carcinoma, colon cancer, ovarian cancer, breast cancer, prostate cancer, renal cell carcinoma, bladder carcinoma, melanoma, rhabdomyosarcoma, neuroblastoma, leukemia, and metastatic lesions secondary therefrom.
Claims Coverage
The consolidated claim coverage includes two independent method claims. Both claims cover treating a cancer influenced by inhibition of Mer kinase by administering to a mammal a composition containing a heterocyclic active ingredient, either represented by Formula Ib or by any one of the listed example compounds, with stereoisomer, enantiomer, and pharmaceutically acceptable salt coverage.
Mer kinase inhibition treatment with formula Ib heterocyclic compounds
A method of treating a cancer influenced by inhibition of Mer kinase by administering to a mammal in need thereof a composition comprising, as an active ingredient, a heterocyclic compound represented by Formula Ib, a stereoisomer thereof, an enantiomer thereof, or a pharmaceutically acceptable salt thereof.
Mer kinase inhibition treatment with listed heterocyclic compounds
A method of treating a cancer influenced by inhibition of Mer kinase by administering to a mammal in need thereof a composition comprising, as an active ingredient, a heterocyclic compound represented by any one of the following compounds, a stereoisomer thereof, an enantiomer thereof, or a pharmaceutically acceptable salt thereof.
Overall, the claims are directed to administering a Mer kinase-inhibiting heterocyclic composition to treat cancers influenced by Mer kinase inhibition, with coverage defined either by Formula Ib or by specified example compounds, and including stereoisomers, enantiomers, and pharmaceutically acceptable salts.
Stated Advantages
The heterocyclic compounds inhibit Mer activity.
The heterocyclic compounds are useful for cancer prevention/treatment.
Stated advantageous effects of Mer kinase inhibition for prevention/treatment of immune-related diseases or cancer.
Documented Applications
Method of treating a cancer influenced by inhibition of Mer kinase by administering a composition containing the disclosed heterocyclic compounds to a mammal.
Treatment of cancer influenced by inhibition of Mer kinase, including the explicitly listed cancer types and metastatic lesions secondary therefrom, in a mammal (including humans).
Prevention and/or treatment of immune-related diseases using the claimed heterocyclic Mer kinase inhibitors.
Prevention and/or treatment of cancer by administering the claimed heterocyclic Mer kinase inhibitors.
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