Sulphonamides derived from diarylmethanes, the processes for pre

Details Sulphonamides derived from diarylmethanes, the processes for pre Sulphonamides derived from diarylmethanes, the processes for pre

1987-11-12

1990-12-25

Gray, Bruce

Textiles: spinning, twisting, and twining

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Patent

active

049803492

DESCRIPTION:

BRIEF SUMMARY
The invention relates to new compounds, sulphonamides derived from diarylmethanes, in particular benzophenones, and from their isosteres, and also to their corresponding salts.
The invention also relates to a process for preparing these compounds.
The invention also relates to new medicinal products containing, by way of active principle, these new compounds, and also their salts with physiologically acceptable organic or inorganic acids or bases.
By medicinal products there is denoted any pharmaceutical composition containing at least one of the chemical compounds defined below, in combination with a pharmaceutically acceptable vehicle.
Il will be called that the anti-inflammatories which are known and used at present act:
either by inhibiting the biosynthesis of arachidonic acid at the phospholipase A.sub.2 level; these are the corticoid anti-inflammatories (cortisones and derivatives), the use of which is limited by their side effects;
or by inhibiting the biosynthesis of prostaglandins at the cyclooxygenase level (both the thromboxane synthetase pathway and also the prostacyclin in synthetase pathway); these are the non-steroid anti-inflammatories.
Among non-steroid anti-inflammatories, there may be mentioned salicyl derivatives such as aspirin, pyrazole derivatives such as phenylbutazone, arylalkanoic acids such as profens, and indole derivatives such as indomethacin.
As regards the non-steroid anti-inflammatories, these act in the biosynthesis of prostaglandins by blocking cyclooxygenase, thereby blocking the formation of thromboxanes and prostacyclins; in particular, they can give rise to haemorrhagic accidents when they are combined with anticoagulant treatments.
The non-steroid anti-inflammatories can cause other adverse side effects, in particular gastralgia, nausea or vomiting, and for this reason they cannot be used in the case of gastric or duodenal ulcer.
In fact, in the phenomena of inflammation, another class of mediators, the leukotrienes, which are metabolites of arachidonic acid, are involved.
The leukotrienes are powerful mediators which are involved in many inflammatory, cardiovascular, allergic, cutaneous or asthmatic conditions.
The subject of the invention is to propose new compounds which are capable of participating in the preparation of medicinal products possessing, in particular, anti-inflammatory properties.
An advantageous aspect of the invention is to propose new compounds which do not inhibit cyclooxygenase and which are involved only at a subsequent stage in the biosynthesis of prostaglandins, endowing them with a more specific action.
One of the aspects of the invention is to propose new compounds which participate in the preparation of medicinal products capable of treating inflammatory phenomena in particular, without affecting the biosynthesis of all prostaglandins.
In effect, they have little or no action on prostacyclin synthetase and do not particularly inhibit the biosynthesis of prostacyclin in (PGI.sub.2), which is vasodilatory and inhibits platelet aggregation.
In contrast, and advantageously, they are inhibitors or thromboxane synthetase, an enzyme which is involved in the biosynthesis of thromboxanes. It is known that thromboxane B.sub.2, in particular, is involved in the phenomena of vasoconstriction of vessels and of platelet aggregation.
The products of the invention hence have a more specific activity at the platelet level and are devoid of gastric side effects.
An advantageous aspect of the invention is to propose new compounds which have an effect on the biosynthesis of leukotrienes, especially inhibiting 5-lipoxygenase.
One of the aspects of the invention is to propose new compounds which inhibit the biosynthesis of leukotrienes, more especially the leukotrienes B.sub.4 (LTB.sub.4) which are involved in the inflammatory processes and are produced by the polymorphonuclear luekocytes, and also the leukotrienes C.sub.4 (LTC.sub.4) involved in allergic reactions, in particular asthma, and certain types of allergic diseases.
Another aspect of the invention i

REFERENCES:
patent: 3666779 (1972-05-01), Diery et al.
patent: 3903114 (1975-09-01), LeMartret et al.
patent: 4113463 (1978-09-01), Oshio et al.
patent: 4198519 (1980-04-01), Gordie
patent: 4443477 (1984-04-01), Witte et al.
patent: 4613618 (1986-09-01), Choay et al.

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