Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-04-27
1997-04-29
Davis, Zinna Northington
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514357, 514354, 514355, 514277, 546301, 546314, 546315, 546334, 546340, 546341, 546342, C07D21365, A61K 3144
Patent
active
056249438
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/DE93/00593 filed Jul. 1, 1993.
The invention relates to new pyridine derivatives with leukotriene-B.sub.4 antagonistic effect, a process for their production and their use as pharmaceutical agents.
Leukotriene-B.sub.4 (LTB.sub.4) ##STR1## was discovered by B. Samuelsson et al. as a metabolite of the arachidonic acid.
The nomenclature of the leukotrienes can be found in the following works:
The physiological and especially the pathophysiological importance of leukotriene-B.sub.4 is summarized in some more recent works: Bailey, Academic Press 1984. b) J. W. Gillard et alo, Drugs of the Future 12, 453 (1987). c) B. Samuelsson et al., Science 237, 1171 (1987). d) C. W. Parker, Drug Development Research 10, 277 (1987). It follows from the above that LTB.sub.4 is an important inflammation mediator for inflammatory diseases, in which leukocytes invade the diseased tissue. The effects of LTB.sub.4 are triggered on the cellular plane by the bond of LTB.sub.4 on a specific receptor.
It is known concerning LTB.sub.4 that it causes the adhesion of leukocytes on the blood vessel wall. LTB.sub.4 is chemotactically effective, i.e., it triggers a directed migration of leukocytes in the direction of a gradient of increasing concentration. Furthermore, it indirectly changes the vascular permeability based on its chemotactic activity, and a synergism with prostaglandin E.sub.2 is observed. LTB.sub.4 obviously plays a decisive role in inflammatory, allergic and immunological processes.
Leukotrienes and especially LTB.sub.4 are involved in skin diseases, which are accompanied by inflammatory processes (increased vascular permeability and formation of edemas, cellular infiltration), increased proliferation of the skin cells and itching, such as, for example, in eczemas, erythemas, psoriasis, pruritus and acne. Pathologically increased leukotriene concentrations are either causally involved in the development of many dermatitides, or there is a connection between the persistence of the dermatitides and the leukotrienes. Clearly increased leukotriene concentrations were measured, for example, in the skin of patients with psoriasis or atopic dermatitis.
Leukotrienes and especially LTB.sub.4 are also involved in diseases of the internal organs, for which an acute or chronic inflammatory component was described; e.g., rhinitis and allergies); inflammatory intestinal diseases (colitis); as well as reperfusion damages (to the heart, intestinal or renal tissue), which result by the temporary pathological obstruction of blood vessels.
Further, leukotrienes and especially LTB.sub.4 are involved in the disease of multiple sclerosis and in the clinical picture of shock (triggered by infections, burns or in complications in kidney dialysis or other extracorporeal perfusion techniques).
Leukotrienes and especially LTB.sub.4 further have an effect on the formation of white blood cells in the bone marrow, on the growth of unstriped muscle cells, of keratinocytes and of B-lymphocytes. LTB.sub.4 is therefore involved in diseases with inflammatory processes and in diseases with pathologically increased formation and growth of cells.
For example, leukemia or arteriosclerosis represent diseases with this clinical picture. By the antagonizing of the effects, especially by LTB.sub.4, the active ingredients according to the invention and their forms of administration are specific medicines for diseases of humans and animals, in which especially leukotrienes play a pathological role.
The new pyridine derivatives with leukotriene-B.sub.4 -antagonistic effect are characterized by general formula I ##STR2## in which . . . . . . . . symbolizes a single bond or a double bond, --CHOH--, --CO--, --CH.dbd.CH--, --C.dbd.C--, --CO--CO-- or --CHOH--CHOH--, atoms, a trifluoromethyl group, an alkylsulfonylamino group, a trifluoromethylsulfonylamino group, an arylsulfonylaminocarbonyl group, a free, esterified or amidated carboxyl group, or a hydroxy group, group or alkylene group with at most 8 carbon atoms or a phenyl radical, phen
Buchmann Bernd
Ekerdt Roland
Fr ohlich Wolfgang
Giesen Claudia
Heindl Josef
Davis Zinna Northington
Schering Aktiengesellschaft
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