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US 5,451,700 AGranted
Amidino compounds, their manufacture and methods of treatment
AssigneeCiba-Geigy Corporation
InventorsMichael M. Morrissey, Hongsuk Suh
Life of this patent
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Abstract
The invention relates to the compounds of the formula ##STR1## wherein the C(.dbd.NH)--NHR.sub.3 group may be in tautomeric or isomeric form, and phamaceutically acceptable salts thereof. The compounds are useful as selective LTB.sub.4 receptor antagonists.
Claims24
A compound of the formula ##STR17## wherein the C(.dbd.NH)--NHR.sub.3 group may be in tautomeric or isomeric form,
- R.sub.1 is amino which is mono- or disubstituted by a substituent selected from an aliphatic hydrocarbon radical, an araliphatic hydrocarbon radical, an aromatic radical, and a cycloaliphatic hydrocarbon radical, or is amino which is disubstituted by lower alkylene radical or a said radical interrupted by oxygen;
- R.sub.2 is hydrogen, halogen, trifluoromethyl, an aliphatic hydrocarbon radical, or is hydroxy which is etherified by an aliphatic alcohol, araliphatic alcohol, or aromatic alcohol or which is esterified by an aliphatic or araliphatic carboxylic acid;
- or R.sub.2 is hydroxy;
- or R.sub.2 is hydroxy which is etherified by an aliphatic alcohol which is substituted by carboxy, by esterified carboxy or by amidated carboxy;
- R.sub.3 is hydrogen or an acyl radical which is derived from an organic carbonic acid, an organic carboxylic acid, a sulfonic acid, or a carbamic acid;
- X.sub.1 and X.sub.3, independently of one another, are oxygen (--O--) or sulphur (--S--);
- and
- X.sub.2 is a divalent aliphatic hydrocarbon radical which may be interrupted by an aromatic radical;
- wherein the phenyl rings of formula I may be, independently of one another, further substituted by one or more substituents selected from halogen, trifluoromethyl, an aliphatic hydrocarbon radical, hydroxy, and hydroxy which is etherified by an aliphatic alcohol or which is esterified by an aliphatic or araliphatic carboxylic acid;
- wherein aryl in the above definitions may be, independently of one another, further substituted by one or more substituents selected from halogen, trifluoromethyl, an aliphatic hydrocarbon radical, hydroxy, and hydroxy which is etherified by an aliphatic alcohol or which is esterified by an aliphatic or araliphatic carboxylic acid;
- wherein a cycloaliphatic hydrocarbon radical may be substituted by an aliphatic radical;
- or a pharmaceutically acceptable salt thereof.
9 more elements
Dependencies are inferred from the claim text.