HWA-131 (I) inhibited the carrageenan-induced paw edema in rats.I also demonstrated antierythema and antipyretic activities.I was effective in attenuating the active Arthus reaction in rats.I inhibited the adjuvant- and type II-collagen-induced arthritis in rats; these effects were accompanied by restoration of the depressed mitogen-induced lymphocyte response.In the chronic graft-vs.-host disease of mice (a model of systemic lupus erythematosus), I inhibited proteinurea due to glomerulonephritis and the decrease in spleen and kidney weight and other disease parameters.I also had antioxidative activity and inhibited the formation of LTB₄ and 5-HETE formation in human polymorphonuclear leukocytes and PGE₂ formation in rabbit mucosa.I also inhibited human platelet aggregation.I did not display any ulcerogenic potential and was well tolerated.I appears appears to be an effective nonsteroidal antirheumatic agent.

01 Jan 1989·Drugs under experimental and clinical research

Substituted 3-phenyl-7H-thiazolo(3,2-b)(1,2,4)triazin-7-ones as antiinflammatory agents with immunomodulating properties.

Article

Author: Kerékjártó, B ; Schleyerbach, R ; Gebert, U ; Weithmann, K U ; Bartlett, R R ; Thorwart, W

After structure-activity relationship studies (SAR) on a novel class of substituted thiazolo(3,2-b)(1,2,4)triazin-7-ones, HWA-131 (3-(3,5-di-tert.butyl-4-hydroxyphenyl)-7H-thiazolo(3,2-b)(1,2,4)triaz in-7-one) was selected for incremental pharmacological investigations. This compound was effective in not only preventing, but also curing established arthritic disorders of rats such as adjuvant and type II collagen arthritis as well as those of mice such as chronic graft-versus-host (CGVH) disease, a model for systemic lupus erythematosus (SLE). Further, this non-immunosuppressive drug effectively inhibited the carrageenan-induced paw oedema, attenuated the active Arthus reaction, and demonstrated antierythema as well as antipyretic activity. Part of the antiinflammatory effects of this new compound is most probably related to its antioxidative activity, as well as inhibition of lipoxygenase metabolites. HWA-131's good gastric tolerance may have to do with its limited ability to inhibit the production of cyclooxygenase metabolites. Based on our data, we are sure that HWA-131 will be an effective nonsteroidal antiinflammatory agent, with immunomodulating properties, to combat human autoimmune disorders.

Drugs under Experimental and Clinical Research

Substituted 3-phenyl-7H-thiazolo(3,2-b)(1,2,4)triazin-7-ones as antiinflammatory agents with immunomodulating properties

Author: Weithmann, K. U. ; Gebert, U. ; Thorwart, W. ; Von Kerekjarto, Bela ; Schleyerbach, R. ; Bartlett, R. R.

After structure-activity relationship studies on a novel class of substituted thiazolo(3,2-b)(1,2,4)triazin-7-ones, HWA-131 (3-(3,5-di-t-butyl-4-hydroxyphenyl)-7H-thiazolo(3,2-b)(1,2,4)triazin-7-one) was selected for incremental pharmacol. investigations.This compound was effective in not only preventing, but also curing established arthritic disorders of rats such as adjuvant and type II collagen arthritis, as well as those of mice such as chronic graft-vs.-host disease, a model for systemic lupus erythematosus.Further, this non-immunosuppressive drug effectively inhibited the carrageenan-induced paw edema, attenuated the active Arthus reaction, and demonstrated antierythema as well as antipyretic activity.Part of the antiinflammatory effects of this new compound is most probably related to its antioxidative activity, as well as inhibition of lipoxygenase metabolites.HWA-131's good gastric tolerance may have to do with its limited ability to inhibit the production of cyclooxygenase metabolites.Thus, HWA-131 may be an effective nonsteroidal antiinflammatory agent, with immunomodulating properties, to combat human autoimmune disorders.

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Indication	Highest Phase	Country/Location	Organization	Date
Rheumatic Diseases	Phase 1	-	Sanofi	-

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