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US 5,519,016 AGranted
Aryl group- or aromatic heterocyclic group-substituted aminoquinolone derivatives and anti-HIV agent
AssigneeUbe Industries, Ltd.
InventorsTomio Kimura, Tetsushi Katsube
Life of this patent
Estimating the term…
Abstract
Disclosed are an aryl group- or heterocyclic group-substituted aminoquinolone compound represented by the formula (Ia), (Ib) or (Ic): ##STR1## wherein each of the substitutents are defined in the specification, or a salt of the compound, and an AIDS curing agent containing the same as an effective ingredient.
Claims23
A compound of formula (Ia) or pharmaceutically acceptable salt or ester thereof:
- ##STR84## in which X represents a hydrogen atom or a halogen atom;
- Y represents a hydrogen atom, a halogen atom, a lower alkyl group, an unsubstituted amino group, or an amino group substituted by one or two groups selected from the .group consisting of lower alkyl and aralkyl groups;
- Z represents a protected or an unprotected carboxyl group or a 5-tetrazolyl group;
- Q represents a group of formula (d):
- ##STR85## where R.sup.2 represents a hydrogen atom, a halogen atom, an unsubstituted lower alkoxy group, a lower alkoxy group substituted by one or more halogen atoms, an unsubstituted lower alkyl group, or a lower alkyl group substituted by one or more halogen atoms;
- R.sup.1 represents:
- a hydrogen atom;
- a lower alkenyl group which is unsubstituted or substituted by one or more halogen atoms;
- a lower alkenyl group;
- an amino group which as unsubstituted or substituted by one or more lower alkyl groups;
- a cycloalkyl group which is unsubstituted or substituted by at least one halogen atom;
- a lower alkoxy group;
- an aryl group which is unsubstituted or substituted by at least one substituent R.sup.0 as defined below;
- a 5- or 6-membered aromatic heteromonocyclic group having one or two heteroatoms selected from the group consisting of N, O and S, said ring being unsubstituted or substituted by at least one substituent R.sup.0 as defined below;
- a fused aromatic group which is a benzene ring fused with a 5- or 6-membered aromatic heteromono-cyclic group as defined above, said fused group being unsubstituted or substituted by at least one substituent R.sup.0 as defined below;
- an unsubstituted lower alkyl group;
- or a lower alkyl group substituted by at least one substituent selected from the group consisting of halogen atoms, hydroxyl groups, carboxyl groups, alkanoyloxy groups, cycloalkyl groups, aryl groups which are unsubstituted or substituted by at least one substituent R.sup.0 as defined below, 5- or 6-membered aromatic heteromonocyclic groups having one or two heteroatoms selected from the group consisting of N, O and S, said ring being unsubstituted or substituted by at least one substituent R.sup.0 as defined below, fused aromatic groups as defined above, said fused group being unsubstituted or substituted by at least one substituent R.sup.0 as defined below, or an amino group represented by the formula (e):
- as defined below, or an amino group represented by the formula (e):
- ##STR86## wherein R.sup.9 and R.sup.10 separately represent a hydrogen atom or a lower alkyl group, or R.sup.9 and R.sup.10, together with the nitrogen atom to which they are attached, form a 3- to 7-membered saturated monocyclic group comprising at least one further heteroatom selected from the group consisting of N, O and S,
- R represents a group of formula (h) or (i):
- ##STR87## where R.sup.3 and R.sup.6 each represents an aryl group which is unsubstituted or substituted by at least one substituent R.sup.0 as defined below;
- a 5- or 6-membered aromatic heteromonocyclic group having one or two heteroatoms selected from the group consisting of N, O and S, said ring being unsubstituted of substituted by at least one substituent R.sup.0 as defined below;
- a fused aromatic group which is a benzene ring fused with a 5- or 6-membered aromatic heteromonocyclic group as defined above, said fused group being unsubstituted or substituted by at least one substituent R.sup.0 as defined below;
- R.sup.4, R.sup.5 and R.sup.7 are the same or different, and each represents a hydrogen atom or a lower alkyl group;
- R.sup.8 represents a hydrogen atom, a lower alkyl group, a hydroxy group or a lower alkoxy group;
- n = 1 or 2;
- m = 0 or 1;
- n' = 1 or 2;
- and
- n" = 1, 2, 3 or 4;
- and
- substituent R.sup.0 is selected from the group consisting of halogen atoms, nitro groups, hydroxy groups, lower alkyl groups which are unsubstituted or substituted with at least one halogen atom, lower alkoxy group, and amino groups which are unsubstituted or substituted with one or two lower alkyl groups, and when there are two or more substituents R.sup.0, each are the same or different, provided that R.sup.0 is not an unsubstituted or substituted amino group when R.sup.1 is a phenyl group.
29 more elements
Dependencies are inferred from the claim text.