Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1994-06-27
1995-12-26
McKane, Joseph K.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514380, 514340, 548247, 548248, 548245, 546275, A61K 3142, C07D26106
Patent
active
054788560
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP93/01572 filed Oct. 29, 1993.
TECHNICAL FIELD
The present invention relates to novel styrene derivatives having lipoxygenase inhibiting activity and cyclooxygenase inhibiting activity, salts thereof, and medical use thereof.
BACKGROUND ART
It is considered that leukotrienes produced by lipoxygenase from arachidonic acid and prostaglandins produced by cyclooxygenase from arachidonic acid are deeply concerned in a crisis of allergic asthma, allergic rhinitis, inflammation, etc. Consequently it is desired to inhibit both lipoxygenase and cyclooxygenase in order to strongly and properly inhibit various allergic diseases, inflammations and other diseases. The development of a drug inhibiting both enzymes is earnestly desired.
DISCLOSURE OF THE INVENTION
The present inventors have conducted a research in considering the foregoing problems in the background art, and found that novel styrene derivatives as indicated in the following formula (1) have an excellent lipoxygenase inhibiting activity and an excellent cyclooxygenase inhibiting activity, and are useful as a drug. Thus, the present invention has been accomplished.
The present invention provides styrene derivatives represented by the formula (1) or a salt thereof: ##STR2## [wherein R.sub.1 and R.sub.2 are the same or different and each is a hydrogen atom, a lower alkoxy group, a halogen atom or a lower alkyl group; R.sub.3 are the same or different and each is a hydroxy group, a lower alkoxy group, a lower alkyl group, a lower alkoxycarbonyloxy group, a lower acyloxy group, a di-loweralkyl phosphate residue or an amino acid residue which may have a protective group; 1 is an integer of 0 to 5; m is an integer of 0 to 5. X represents a formula --N(Z)CO-- {wherein Z represents a formula (CH.sub.2).sub.n A (wherein A represents a hydrogen atom, a carboxyl group, a di- or mono-loweralkylcarbamoyl group, a carbamoyl group, a lower alkoxycarbonyl group, a cyano group, a lower alkoxy group, a N-acylamino group, a phenyl group which may be substituted, a pyridyl group or a thienyl group, n is an integer of 0 to 5)} or a single bond, Y represents --C(Z').dbd.CH--, --CH.dbd.CH--C(Z').dbd.CH--, --C(Z').dbd.CH--CH.dbd.CH-- (wherein Z' is the same as Z), provided that when n=0, both Z and Z' are not hydrogen atoms, and that when 1 is O, X represents a single bond].
The compounds of the present invention represented by the formula (1) has an excellent lipoxygenase inhibiting activity and cyclooxygenase inhibiting activity. Examples of lipoxygenases are 5-lipoxygenase, 12-lipoxygenase and 15-lipoxygenase, etc. The compounds of the invention exhibit, in particular, a potent activity of 5-lipoxygenase inhibition.
The compounds of the invention have excellent lipoxygenase inhibiting and cyclooxygenase inhibiting activities and are useful as antiasthmatic agents, antiallergic agents, agents for treating encephalopathy, cardiovascular agents, agents for treating nephritis, antiinflammatory analgesic agents, antirheumatic agents, agents for treating dermatosis such as psoriasis, and liver disease agents.
Accordingly, the present invention provides antiasthmatic agents, antiallergic agents, agents for treating encephalopathy, cardiovascular agents, agents for treating nephritis, antiinflammatory analgesic agents, anti-rheumatic agents, agents for treating dermatosis such as psoriasis, and liver disease agents, the agents each comprising an effective amount of a compound of the formula (1) given above and a pharmaceutically acceptable carrier therefor.
The present invention also provides a method for treating asthma, allergy, encephalopathy, circulatory diseases, nephritis, inflammation, rheumatism, dermatosis such as psoriasis, and liver diseases which comprises administering an effective amount of a compound of the formula (1) given above to patients.
The present invention is further concerned with the use of compounds of the formula (1) given above in the treatment of asthma, allergy, encephalopathy, circulatory diseases, nephritis, i
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patent: 4983619 (1991-01-01), Gallagher et al.
CA 82: 16724t Isoxazoline . . . -4-ones. Bianchi et al., p. 490, 1975.
CA 115: 135979g Beckmann . . . -1'-ones. Chekti et al., p. 971, 1991.
CA 117: 191833r Preparation . . . inhibitors. Suzuki et al., p. 802, 1992.
CA 118: 254919s Preparation . . . inhibitors. Shindo et al., p. 886, 1993.
Basaki Yuzi
Hosoya Toshiyuki
Kozima Mitiyo
Matsuura Naosuke
Nozaki Kenzi
McKane Joseph K.
Taiho Pharmaceutical Co. Ltd.
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