| 主权项 |
1. A method for the treatment of necrosis and necrosis-associated diseases comprising administering a composition which comprises an indole compound of the following formula (1), pharmaceutically acceptable salt or stereoisomer thereof as an active ingredient together with a pharmaceutically acceptable carrier or diluent to a subject in need thereof: in which n denotes a number of 0 to 3, A represents 5 membered heteroaryl or heterocycle each of which has 1 to 3 hetero atoms selected from N, O and S, R1 represents R5—X—B—X′—, B represents a direct bond, or represents 3˜10 membered heterocycle or heteroaryl each of which has 1 to 4 hetero atoms selected from N, O and S, X and X′ independently of one another represent a direct bond, or are selected from the group consisting of —NR6—, —CO—, —CONR6—, —CO2—, —OC(O)—, —S(O)m—, —O—(CH2)m—, —(CH2)m—O—, —(CH2)m—, —NR6CO—, and —NHCO2—, wherein m denotes a number of 0 to 3, and R6 represents hydrogen or C1-C6-alkyl, R5 represents hydrogen, hydroxy, C1-C6-alkyl, C1-C6-alkoxy, C4-C6-cycloalkyl or phenyl, or represents 3˜10 membered monocyclic or fused cyclic heterocycle or heteroaryl each of which has 1 to 3 hetero atoms selected from N, O and S, and is optionally substituted by oxo or C1-C6-alkyl, R2 represents —(CR8R9)p—Y—R7, p denotes a number of 0 to 2, R8 and R9 independently of one another represent hydrogen or C1-C6-alkyl, Y represents a direct bond, or is selected from the group consisting of —O—, —NR6—, —NR6C(O)—, and —S(O)q—, wherein q denotes a number of 0 to 2, R7 represents hydrogen, halogen, hydroxyl, C1-C6-alkyl, phenyl, or represents 3˜10 membered heterocycle or heteroaryl each of which has 1 to 3 hetero atoms selected from N, S and O and which optionally contains oxo, R3 represents hydrogen or C1-C6-alkyl, R4 represents C3-C6-cycloalkyl, where alkyl, alkoxy, phenyl, cycloalkyl, heterocycle and heteroaryl may be optionally substituted, and the substituents are one or more selected from the group consisting of hydroxy, halogen, amino, C1-C6-alkylamino, di-C1-C6-alkylamino, C1-C6-alkyl, halo-C1-C6-alkyl, C1-C6-alkylsulfonyl, carboxy-C1-C6alkyl, and oxo, and wherein necrosis and necrosis-associated diseases are selected from the group consisting of neurodegenerative disease, diabetes, pancreatitis, bacterial/viral sepsis, bacterial infection, viral infection, leukemia, lymphoma, spinal cord injury, muscular dystrophy and anthrax. |
