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Heteroaryl compounds and their use as therapeutic drugs
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a technology of heteroaryl compounds and therapeutic drugs, applied in the field of heteroaryl compounds, can solve the problems of limited potency and lack of selectivity of inhibitors, and it is difficult to find inhibitors that are specific for mer,
Active Publication Date: 2017-12-14
DONG A SOCIO HLDG CO LTD
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Benefits of technology
The present invention pertains to novel heterocyclic compounds, stereoisomers, enantiomers, or pharmaceutically acceptable salts that can effectively inhibit the activity of a protein called Mer kinase. These compounds can be used for the prevention or treatment of cancer and immune-related diseases. The invention is based on the results of studies and the use of various chemical reagents and analytical techniques. The compounds described in the patent have shown promise in this area of research.
Problems solved by technology
For this reason, it is challenging to find an inhibitor that is specific for the Mer.
This inhibitor has, however, limited potency and lack of selectivity.
Method used
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[0117]To a mixture of intermediate 2 (43 mg, 0.2 mmol) and triethylamine (24 mg, 0.24 mmol) in 2 ml of DMF was added HATU (91 mg, 0.24 mmol) followed by (1S,2S)-2-(benzyloxy)cyclopentan-1-amine (38 mg, 0.2 mmol). The mixture was stirred at room temperature for 1 hr and then saturated sodiumbicarbonate solution was added. The mixture was extracted with EtOAc, washed with brine, dried over MgSO4, and concentrated in vacuo. The crude residue was purified by preparative HPLC to afford 46 mg of the title compound.
[0122]Using trans-2-(benzyloxy)cyclopentan-1-amine, the title compound was obtained as described for the example 1.
[0123]MS (ESI, m / z): 392.2 [M+H]+
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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 receptortyrosinekinase (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.
Description
RELATED APPLICATION[0001]This application claims the benefit of priority under U.S.C. §119(e) to U.S. Provisional Patent Application Ser. No. 62 / 212,520 filed Aug. 31, 2015, which is incorporated herein by reference.TECHNICAL FIELD[0002]The present invention relates to novel heterocyclic compounds having Mer kinase inhibitory activity, a stereoisomer thereof, an enantiomer thereof, or a pharmaceutically acceptable salt thereof, the use for preparing pharmaceutical compositions, pharmaceutical compositions comprising the same, methods of treating diseases using these compositions.BACKGROUND ART[0003]Transmembrane receptortyrosine kinases (RTKs) comprise an evolutionarily conserved family of structurally related proteins. The gene Mer is a member of the Tyro3 / Axl / Mer (TAM) receptorkinase family and a proto-oncogene. Its abnormal expression and activation is found in conjunction with human cancers such as pituitary adenomas, mantle cell lymphomas, and T-cell acute lymphoblastic leuke...
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Application Information
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Patent Type & Authority Applications(United States)
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