ECSP982564A - HYDRAZINE DERIVATIVES - Google Patents

Abstract

Hydrazine derivatives of the formula (graph), wherein Y means CO or SO2; R1 signifies lower alkyl, lower alkenyl, lower cycloalkyl, cycloalkyl-lower-lower-alkyl, aryl or aryl-lower-alkyl; R2 means lower alkyl, halo-lower alkyl, aryl-lower alkyl, aryl-lower alkenyl or aryl when Y means SO2, and means lower alkyl, halo-lower alkyl, aryl-lower alkoxy or NR5R6 when Y means CO; and R3 signifies hydrogen, lower alkyl optionally substituted by cyano, amino, hydroxy, lower alkoxy, lower alkoxycarbonyl, heterocyclic or heterocyclylcarbonyl, lower alkenyl, lower alkynyl, lower cycloalkyl, cycloalkyl-lower-lower alkyl, aryl-lower alkyl. lower, aryl-lower alkenyl, aryl or heterocyclic; or R2 and R3 together form the residue of a 5-, 6-, or 7- membered cyclic amide, cyclic imide, cyclic sulfonamide, or cyclic urethane group; R4 signifies lower alkyl, hydroxy-lower alkyl, lower alkenyl, lower cycloalkyl, cycloalkyl-lower-lower-alkyl or a group of the formula X-aryl, X-heteroaryl or - (CH2) 1-2-CH = CR7R8; X means a spacer group; R5 and R6 each individually signifies hydrogen, lower alkyl or aryl-lower alkyl; and R7 and R8 together represent a lower alkylene group in which a methylene group is optionally replaced by a heteroatom; and its pharmaceutically acceptable salts inhibit not only the release of tumor necrosis factor (TNF-a) and transformable growth factor (TGF-a) from cells, but also the proliferation of keratinocytes. They are useful as medications, especially for the treatment of inflammation, fever, bleeding, sepsis, rheumatoid arthritis, osteoarthritis, multiple sclerosis, or psoriasis.