Anti-inflammatory A-aminocyclolactam compounds
AssigneeCambridge Enterprise Limited
InventorsDavid J. Grainger, David John Fox
Life of this patent
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Abstract
The invention provides compounds, compositions, and uses of compounds of general formula (I) or pharmaceutically acceptable salts thereof, for the preparation of a medicament intended to treat an inflammatory disorder wherein y is any integer from 1 to 8; z is any integer from 1 to 8; with the proviso that y and z cannot both equal 1; X is —C —(Y)k—(R1)n or SO2—(Y)k—(R1)n; k is 0 or 1; Y is a cycloalkyl or polycyloalkyl group (such as an adamantyl, adamantanemethyl, bicyclooctyl, cyclohexyl, cyclopropyl group); or Y is a cycloalkenyl or polycycloalkenyl group.
Claims36
A pharmaceutical composition comprising, as active ingredient, a compound of formula (I):
- wherein
- y is any integer from 1 to 8;
- z is any integer from 1 to 8, with the proviso that y and z cannot both equal 1;
- X is —CO—(Y)k—(R1)n or SO2—(Y)k—(R1)n;
- k is 0 or 1;
- Y is a cycloalkyl, polycyloalkyl, cycloalkenyl or polycycloalkenyl group;
- each R1 is independently selected from hydrogen or an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl or alkylamino radical of 1 to 20 carbon atoms;
- or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl or aminodialkyl radical;
- and
- n is any integer from 1 to m, where m is the maximum number of substitutions permissible on the cyclo-group Y;
- or
- alternatively R1 is selected from a peptido radical having from 1 to 4 peptidic moieties linked together by peptide bonds;
- wherein the 1 to 4 peptidic moieties are selected from the 20 natural occurring amino acids;
- or
- a pharmaceutically acceptable salt thereof, and at least one pharmaceutically acceptable excipient and/or carrier.
A compound of general formula (I):
- wherein
- y is any integer from 1 to 8;
- z is any integer from 1 to 8, with the proviso that y and z cannot both equal 1;
- X is —CO—(Y)k—(R1)n or SO2—(Y)k—(R1)n;
- k is 0 or 1;
- Y is a cycloalkyl, polycyloalkyl, cycloalkenyl or polycycloalkenyl group;
- each R1 is independently selected from hydrogen or an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl or alkylamino radical of 1 to 20 carbon atoms;
- or
- each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl or aminodialkyl radical;
- and
- n is any integer from 1 to m, where m is the maximum number of substitutions permissible on the cyclo-group Y;
- or
- R1 is selected from a peptido radical having from 1 to 4 peptidic moieties linked together by peptide bonds wherein the 1 to 4 peptidic moieties are selected from the 20 naturally occurring amino acids.
A compound of formula (II)
- wherein:
- the bridge Q in formula (II) represents a bridging group independently selectable from the
- group consisting of alkenylene and alkylene substituted by halo, amino or hydroxy moieties having a carbon chain length of from 1 to 8;
- z is any integer from 1 to 8;
- X is —CO—(Y)k—(R1)n or SO2—(Y)k—(R1)n;
- k is 0 or 1;
- Y is a cycloalkyl, polycyloalkyl, cycloalkenyl or polycycloalkenyl group;
- each R1 is independently selected from hydrogen or an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl, or alkylamino, radical of 1 to 20 carbon atoms;
- or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl, aminodialkyl radical;
- and
- n is any integer from 1 to m, where m is the maximum number of substitutions permissible on the cyclo-group Y;
- or
- alternatively R1 may be a peptido radical having from 1 to 4 peptidic moieties linked together by peptide bonds;
- wherein the 1 to 4 peptidic moieties are selected from the 20 naturally occurring amino acids.
Dependencies are inferred from the claim text.