Novel pyrazole derivative as alk5 inhibitor and uses thereof
AssigneeHanmi Pharmaceutical Co., Ltd.
InventorsKyung Ik LEE, Young Hee JUNG, Ji Young SONG, Seung Ah JUN
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Abstract
The present disclosure relates to a novel substituted pyrazole derivative having an effect of inhibiting serine/threonine kinase activity targeting receptor ALK5 of TGF-β, and a pharmaceutical composition including the compound of the present disclosure as an active ingredient may be useful in preventing and/or treating cancers, autoimmune diseases, fibrotic diseases, inflammatory diseases, neurodegenerative diseases, infectious diseases, pulmonary diseases, cardiovascular diseases or metabolic diseases, or other diseases associated with a decrease in TGF family signaling activity.
Claims18
A compound of the following Chemical Formula 1 or a pharmaceutically acceptable salt thereof:
- wherein, in Chemical Formula 1,
- X is N or CH;
- a ring A is C3-6 cycloalkylene, C6-10 arylene, C5-10 heteroarylene containing 1 to 4 heteroatoms selected from among N, O and S atoms, or a non-aromatic fused heteropolycyclic ring containing 1 to 4 heteroatoms selected from among N, O and S;
- R1s are each independently hydrogen, halogen, or linear or branched C1-6 alkyl, or halo C1-6 alkyl, and when there are a plurality of R1s, these are the same as or different from each other;
- R2s are each independently
- R3 is hydrogen, halogen, linear or branched C1-6 alkyl, linear or branched halo C1-6 alkyl, C3-10 cycloalkyl, C3-10 heterocycloalkyl unsubstituted or substituted with R4, C6-10 heterobicycloalkyl, linear or branched C2-6 alkenyl, C2-6 alkynyl, —(CH2)a—R4, —(CH2)a—OR4, —(CH2)a—O—(CH2)a—R4, —(CH2)a—S—(CH2)a—R4, —(CH2)a—O—(CH2)a—OR4, —(CH2)a—NR4R5, —(CH2)a—NO2, —(CH2)a—CN, —(CH2)a—COR4, —(CH2)a—CO2R4, —(CH2)a—CONR4R5, —(CH2)a—NHCOR4, —(CH2)a—SR4, —(CH2)a—NHSO2R4, —(CH2)aSOR6, —(CH2)a—SO2R6, —(CH2)a—SO2NHR6, —(CH2)a—SO(NH)R6 or —(CH2)a—SO2NR4R5, or when there are a plurality of R3s and they are adjacent to each other, they are linked to each other to form a 5-membered or 6-membered ring with the ring A, one or more heteroatoms selected from among N, O and S atoms are included in the ring, and the heteroatoms are further oxidized;
- R4 and R5 are each independently hydrogen, linear or branched C1-6 alkyl, linear or branched halo C1-6 alkyl, C3-10 cycloalkyl, C3-6 cycloalkenyl, C1-6 carbonyl, C6-12 aryl, —(CH2)b—NR6R7, or saturated or partially unsaturated 5-membered to 10-membered monocyclic or bicyclic heterocycloalkyl or heteroaryl containing 1 to 4 heteroatoms selected from among N, O and S;
- R6 and R7 are each independently hydrogen, hydroxy, C1-6 alkyl, halo C1-6 alkyl or C3-6 cycloalkyl;
- a and b are an integer of 0 to 4;
- and
- l, m and n are each independently an integer of 0 to 4.
Dependencies are inferred from the claim text.