Pyridazine derivatives with inhibitory action against interleukin-1-beta production

• Main Authors: OHGIYA, TADAAKI, MATSUDA, TAKAYUKI, OHKUCHI, MASAO, YOSHIZAKI, HIDEO, KITAMURA, TAKAHIRO, SHIGYO, HIROMICHI, KOTAKI, KYOKO, HABATA, YURIKO, KYOTANI, YOSHINORI, YAMAZAKI, YUKIYOSHI, KUMAI, NATSUYO, KOSHI, TOMOYUKI
• Format: Patent
• Language: English
• Published: 29.06.2001
• Edition: 7
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

The pyridazine derivative has the formula (1), wherein: R1 represents substituted or unsubstituted aryl; R2 represents a phenyl group substituted at least at 4-position by alkoxyl, alkylthio, alkylsulfinyl or alkylsulfonyl, and optionally has one or more substituents at the remaining positions; R3 represents H, alkoxyl, haloalkyl, cycloalkyl, substituted or unsubstituted aryl, substituted or unsubstituted aryloxy, substituted or unsubstituted nitrogen-containing heterocyclic ring residue, substituted or unsubstituted aminocarbonyl, or alkylcarbonyl; A represents a single bond or linear or branched alkylene or alkenylene group; X represents O or S; and the dashed line indicates that the carbon-carbon bond between the 4-position and the 5-position is a single bond or a double bond; with the proviso that A is a single bond when R3 is a halogenated lower alkyl group and that the following combinations are excluded: R1 and R2 are 4-methoxyphenyl groups, X is an oxygen atom, the carbon-carbon bond at the 4-position and the 5-position is a double bond, A is a single bond, and R3 is a hydrogen atom or a 2-chloroethyl group; or a salt thereof Also described is a medicine comprising, as an effective ingredient, a pyridazine derivative of formula (1) or a salt thereof. The pyridazine compounds of formula (1) are useful in the manufacture of a medicament for the treatment of a disease caused by stimulation of interleukin-1b production (e.g. immune diseases, inflammatory diseases, ischemic diseases, osteoporosis or ichorrhemia).