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Japanese Patent JP3798245

B2

The invention provides hydrazine derivatives of the formulawherein R1 is lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl, aryl or aryl-lower alkyl; R2 is an acyl group derived from an alpha-, beta-, gamma- or delta-(amino, hydroxy or thiol)carboxylic acid in which the amino, hydroxy or thiol group is optionally lower alkylated or the amino group is optionally acylated, sulphonylated or amidated and in which any functional group present in a side-chain is optionally protected, or a group of the formula Het(CH2)mCO; R3 is hydrogen, lower alkyl, halo-lower alkyl, cyano-lower alkyl, amino-lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, lower alkoxycarbonyl-lower alkyl, lower cycloalkyl-lower alkyl, aryl-lower alkyl, heterocyclyl-lower alkyl, heterocyclylcarbonyl-lower alkyl, lower alkenyl, lower alkynyl, lower cycloalkyl, aryl-lower alkenyl, aryl or heterocyclyl; R4 is lower alkyl, lower alkenyl, lower cycloalkyl, lower cycloalkyl-lower alkyl or a grouping of the formula X-aryl, X-heteroaryl or -(CH2)n-CH=CR5R6; R5 and R6 together are lower alkylene in which one CH2 group is optionally replaced by a hetero atom; Het is heterocyclyl; X is a spacer group; m is 0, 1, 2, 3 or 4; and n is 1 or 2; and their pharmaceutically acceptable salts inhibit the release of tumour necrosis factor alpha (TNF-alpha) from cells. They can be used as medicaments, especially in the treatment of inflammatory and autoimmune diseases, osteoarthritis, respiratory diseases, tumours, cachexia, cardiovascular diseases, fever, haemorrhage and sepsis.

Broadhurst, Michael John
Johnson, William Henry
Walter, Daryl Simon

JP2000557226A

July 19, 2006

June 17, 1999

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F. HOFFMANN-LA ROCHE AKTIENGESELLSCHAFT

C07C259/06; A61K31/16; A61K31/165; A61K31/341; A61K31/343; A61K31/351; A61K31/381; A61K31/382; A61K31/397; A61K31/40; A61K31/401; A61K31/4015; A61K31/403; A61K31/4035; A61K31/404; A61K31/41; A61K31/415; A61K31/4164; A61K31/426; A61K31/433; A61K31/4402; A61K31/4406; A61K31/4409; A61K31/445; A61K31/4453; A61K31/4458; A61K31/4462; A61K31/4465; A61K31/4468; A61K31/495; A61K31/513; A61K31/5375; A61K31/54; A61P7/00; A61P7/04; A61P9/00; A61P9/02; A61P11/00; A61P19/02; A61P29/00; A61P35/00; A61P37/06; C07C317/44; C07C323/60; C07D205/04; C07D207/16; C07D207/28; C07D207/327; C07D207/34; C07D207/416; C07D209/18; C07D209/48; C07D211/14; C07D211/34; C07D211/60; C07D211/62; C07D213/54; C07D213/56; C07D213/81; C07D213/86; C07D213/87; C07D231/04; C07D231/12; C07D233/46; C07D233/54; C07D233/60; C07D233/64; C07D239/54; C07D249/04; C07D249/08; C07D257/04; C07D277/20; C07D277/36; C07D279/12; C07D285/06; C07D295/14; C07D295/15; C07D295/215; C07D307/24; C07D307/68; C07D309/04; C07D309/06; C07D309/08; C07D309/12; C07D309/14; C07D333/24; C07D333/38; C07D333/68; C07D335/02; C07D405/12; C07D407/12; C07D409/12; C07D417/12; C07D521/00; C07D207/32

WO1999040063A1
WO1999001428A1

Hajime Tsukuni
Fumio Shinoda

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