Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1996-06-25
1998-06-02
Ivy, C. Warren
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514316, 514317, 514326, 514331, 544129, 546191, 546208, 546227, 546229, 546232, A01N 31535, A01N 4340, C07D21108, C07D42100
Patent
active
057600350
DESCRIPTION:
BRIEF SUMMARY
This is the National Stage Application of PCT/EP94/03121 filed Sep. 16, 1994, published as WO/95/08535 on Mar. 30, 1995.
This invention relates to novel substituted aminoalkyl-1-(aryloxyalkyl)piperidine compounds having therapeutic activity useful in treating conditions associated with inflammation, allergy or the immune system, to therapeutic compositions containing these novel compounds and to processes for preparing these novel compounds.
It is believed that, in response to an antiinflammatory stimulus, phospholipase enzymes are activated leading to the release of arachidonic acid from phospholipids. Existing non-steroidal antiinflammatory agents (NSAIA) are believed to act primarily by blocking the conversion of this released arachidonic acid into prostaglandins via the cyclo-oxygenase pathway of the arachidonic acid cascade. Many existing NSAIA are unsuitable for use by asthmatics. We have found a series of compounds which act to block the release of arachidonic acid from phospholipids. These compounds are indicated as useful antiinflammatory compounds with a potentially broader spectrum of activity than existing NSAIA, and potentially fewer gastro-intestinal side-effects. In addition the compounds may be useful in the treatment of asthma.
U.S. Pat. No. 4,027,028 discloses that compounds of formula A ##STR2## in which R.sub.2 is a hydrogen or a lower alkyl radical; R.sub.3 is the acyl residue of an organic alkylcarboxylic acid having up to 10 carbon atoms; R.sub.4 is an optionally substituted phenyl radical; X is C.sub.2-3 alkylene radical optionally substituted by one or more lower alkyl radicals; n is 1 or 2; and Ar is inter alia optionally substituted phenyl; are useful for treating hypertension. Compounds of formula A in which R.sub.3 represents hydrogen are disclosed as intermediates but no pharmacological activity is reported for these compounds.
U.S. Pat. No. 4,348,401 discloses that compounds of formula B ##STR3## in which R.sub.1 is a hydrogen atom, an acyl radical or an optionally substituted aryl radical; R.sub.2 is a hydroxymethyl radical, a cyano group, an amidino group which is optionally substituted by hydroxyl, a 1H-tetrazol-5-yl radical or a --CO--R.sub.3 radical, R.sub.3 is a hydroxyl group, a lower alkoxy radical or an amino group which is optionally substituted by a 1H-tetrazol-1-yl radical; X is an imino group or an oxymethyl radical; A is an alkylene radical containing 2 to 4 carbon atoms and B is a valency bond or a 4-hydroxypyrimidin-2,5-diyl radical; have an anti-allergic action, especially due to their strongly anti-histaminic action. The compounds are also alleged to have anti-oedematous and anti-phlogistic effectiveness.
GB 1,052,302 discloses that compounds of formula C ##STR4## in which R.sub.1 represents a straight- or branched-chain, saturated or unsaturated aliphatic hydrocarbon group containing at least two carbon atoms, a phenoxyalkyl group, an aralkyl group or an aralkenyl group; R.sub.2 represents a straight- or branched-chain, saturated or unsaturated aliphatic hydrocarbon group, an aralkyl group, or an unsubstituted or substituted aromatic or aromatically unsaturated heterocyclic group; R.sub.3 and R.sub.4 which may be the same or different, each represents an alkyl or aralkyl group or, jointly, together with the adjacent nitrogen atom, represents a heterocyclic group which may contain a further hetero atom; and R.sub.5 represents a hydrogen atom, or a lower alkyl group in the 3-position; exhibit analgesic activity and alleges that the compounds have spasmolytic, sedative and/or cough-soothing activity. However these compounds also exhibit cardiovascular activity which is undesirable.
EP 520,882 discloses the use of intermediates. No pharmacological activity is reported for these compounds.
EP 526,342 discloses the use of intermediate. No pharmacological activity is reported for this compound.
Japanese Laid Open Patent Application No. 63-154683 (1988) discloses that certain pyridazinones are useful as heart stimulants. This application generically discloses inter
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Rafferty Paul
Tometzki Gerald Bernard
Covington Raymond
Ivy C. Warren
Knoll Aktiengesellschaft
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