Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1999-04-23
2000-09-12
Lambkin, Deborah C.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
544337, A61K 31495, C07F 902
Patent
active
06117873&
DESCRIPTION:
BRIEF SUMMARY
The invention relates to compounds of the formula I ##STR2## in which R.sub.1 is hydroxyl or an aliphatic, araliphatic or aromatic radical, araliphatic, heteroarylaliphatic or aromatic radical, alkylidene and lower alkyl, halogen, trifluoromethyl, cyano or nitro, preparations comprising them.
Novel compounds of the formula I are, for example, those in which 3-methoxybenzylidene, 3-pyridylmethylene, ethylene, oxoethylene, ethylidene, 1,3-propylene, 1,3-(1-carboxy)propylene, cyclopropylene or 1,4-butylene, R.sub.1 is hydroxyl, alk is methylene and R.sub.2, R.sub.3 and R.sub.5 are hydrogen, or when X is methylene, R.sub.1 is methyl or benzyl, alk is methylene and R.sub.2, R.sub.3 and R.sub.5 are hydrogen, or when X is butylene, R.sub.1 is hydroxyl, alk is methylene, R.sub.2 is methyl and R.sub.3 and R.sub.5 are hydrogen and b1) R.sub.4 is other than bromine when X is methylene or ethylidene, R.sub.1 is hydroxyl, alk is methylene and R.sub.2, R.sub.3 and R.sub.5 are hydrogen, or, for example, those in which 3-pyridylmethylene, ethylene, oxoethylene, ethylidene, 1,3-propylene, 1,3-(1-carboxy)propylene, cyclopropylene and 1,4-butylene when R.sub.1 is hydroxyl and R.sub.2 is hydrogen, b2) X is other than 1,4-butylene when R.sub.1 is hydroxyl and R.sub.2 is methyl, and
Aliphatic radicals are, for example, lower alkyl, lower alkenyl or lower alkanoyl radicals.
Araliphatic radicals are, for example, phenyl-lower alkyl or naphthyl-lower alkyl radicals.
Aromatic radicals are, for example, phenyl or naphthyl radicals.
Divalent aliphatic radicals are, for example, lower alkylene, oxo-lower alkylene, oxo-lower alkenylene, lower alkylidene, polyhalo-lower alkylidene, carboxy-lower alkylidene, hydroxy-lower alkylidene, lower alkoxy-lower alkylidene or lower alkylthio-lower alkylidene.
Divalent cycloaliphatic radicals are, for example, unfused or benzo-fused cycloalkylene, cycloalkylidene or cycloalkenylidene radicals, such as 3- to 6-membered cycloalkylene, 3- to 6-membered cycloalkylidene or 3- to 6-membered benzocycloalkenylidene.
Divalent cycloaliphatic-aliphatic radicals are, for example, 3- to 6-membered cycloalkyl-lower alkylene or cycloalkyl-lower alkylidene radicals.
Divalent araliphatic radicals are, for example, phenyl-lower alkylene, phenyl(oxo)-lower alkylene or phenyl-lower alkylidene radicals.
Divalent heteroaryl aliphatic radicals are, for example, pyrrolyl-lower alkylidene, furyl-lower alkylidene, thienyl-lower alkylidene or pyridyl-lower alkylidene radicals.
Divalent aromatic radicals are, for example, phenylene or naphthylene radicals.
Aliphatic radicals are, for example, lower alkyl or lower alkenyl radicals.
Araliphatic radicals are, for example, phenyl-lower alkyl or naphthyl-lower alkyl radicals.
Aromatic radicals are, for example, phenyl or naphthyl radicals.
The ring system of the cycloalkylene, cycloalkylidene, unfused or benzo-fused cycloalkylene, cycloalkylidene or cycloalkenylidene, cycloalkyl-lower alkylidene, cycloalkenyl-lower alkylidene, phenyl-lower alkylene, phenyl(oxo)-lower alkylene, phenyl-lower alkylidene, furyl-lower alkylidene, thienyl-lower alkylidene, pyridyl-lower alkylidene, phenylene, naphthylene, phenyl-lower alkyl and naphthyl-lower alkyl radicals mentioned can be unsubstituted or substituted, such as mono-, di- or trisubstituted, in a customary manner, for example by lower alkyl, lower alkoxy, phenoxy, hydroxyl, halogen, trifluoromethyl, di-lower alkylamino, lower alkanoylamino, nitro, carboxyl, lower alkoxycarbonyl, carbamoyl and/or cyano.
3- to 6-membered benzocycloalkenylidene is, for example, indanylidene or tetrahydronaphthylidene, such as indan-2,2-ylidene.
3- to 6-membered cycloalkylene is, for example, cyclopropylene, 1,2-cyclobutylene, 1,2-cyclopentylene or 1,2-cyclohexylene.
3- to 6-membered cycloalkylidene is, for example, cyclopropylidene, cyclobutylidene, cyclopentylidene or cyclohexylidene.
3- to 6-membered cycloalkyl-lower alkylene is, for example, 3- to 6-membered cycloalkyl-C.sub.1 -C.sub.4 alkylene, in which cycloalkyl is, for example, cyclopropyl, cyclobuty
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Acklin Pierre
Allgeier Hans
Auberson Yves
Ofner Silvio
Veenstra Siem Jacob
Borovian Joseph J.
Lambkin Deborah C.
Novartis AG
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