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Title:
ヒドラジン誘導体
Document Type and Number:
Japanese Patent JP3801653
Kind Code:
B2
Abstract:
Hydrazine derivatives of the formulawherein Y is CO or SO2; R1 is lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl; R2 is lower alkyl, halo-lower alkyl, aryl-lower alkyl, aryl-lower alkenyl or aryl when Y is SO2 and is lower alkyl, halo-lower alkyl, lower alkoxy, lower alkoxycarbonyl, acyl, lower cycloalkyl, aryl, aryl-lower alkyl, aryl-lower alkoxy or NR5R6 when Y is CO; and R3 is hydrogen, lower alkyl optionally substituted by cyano, amino, hydroxy, lower alkoxy, lower alkoxycarbonyl, heterocyclyl or heterocyclylcarbonyl, lower alkenyl, lower alkynyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl-lower alkyl, aryl-lower alkenyl, aryl or heterocyclyl; or R2 and R3 together form the residue of a 5-, 6- or 7-membered cyclic amide, cyclic imide, cyclic sulphonamide or cyclic urethane group; R4 is lower alkyl, hydroxy-lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a group of the formula X-aryl, X-heteroaryl or -(CH2)1-2-CH=CR7R8; X is a spacer group; R5 and R6 each individually are hydrogen, lower alkyl or aryl-lower alkyl; and R7 and R8 together represent a lower alkylene group in which one methylene group is optionally replaced by a hetero atom; and their pharmaceutically acceptable salts inhibit not only the release of tumour necrosis factor (TNF-alpha) and transforming growth factor (TGF-alpha) from cells, but also keratinocyte proliferation. They are useful as medicaments, especially for the treatment of inflammation, fever, hemorrhage, sepsis, rheumatoid arthritis, osteoarthritis, multiple sclerosis or psoriasis.

Inventors:
Broadhurst, Michael John
Johnson, William Henry
Walter, Daryl Simon
Application Number:
JP50623099A
Publication Date:
July 26, 2006
Filing Date:
June 18, 1998
Export Citation:
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Assignee:
F. HOFFMANN-LA ROCHE AKTIENGESELLSCHAFT
International Classes:
C07C259/06; C07D295/14; A61K31/15; A61K31/167; A61K31/18; A61K31/351; A61K31/382; A61K31/404; A61K31/4166; A61K31/421; A61K31/44; A61K31/4409; A61K31/4468; A61K31/505; A61K31/5375; A61P19/02; A61P21/00; A61P29/00; C07C243/28; C07C243/32; C07C263/04; C07C281/02; C07C281/06; C07C311/49; C07D207/325; C07D209/14; C07D209/48; C07D211/38; C07D211/58; C07D213/42; C07D213/54; C07D213/56; C07D213/77; C07D215/38; C07D233/72; C07D233/76; C07D239/26; C07D239/42; C07D263/22; C07D275/02; C07D277/30; C07D277/56; C07D277/82; C07D279/02; C07D295/18; C07D305/06; C07D307/52; C07D307/68; C07D307/81; C07D309/04; C07D309/06; C07D309/12; C07D309/14; C07D309/30; C07D317/28; C07D333/34; C07D333/38; C07D335/02; C07D521/00; C07D207/32; A61K; C07C; C07D
Foreign References:
WO1999040063A1
Attorney, Agent or Firm:
Hajime Tsukuni
Fumio Shinoda