US 2006/0189597 A1 · Lactam compounds and pharmaceutical use thereof

1:

A compound of formula (I) or a pharmaceutically acceptable salt thereof:
wherein A represents an aromatic ring, a heterocyclic ring or an aliphatic ring;
R2, R3 and R4 may be the same or different from one another and independently represent a hydrogen atom, a halogen atom, a hydroxyl group, an alkyl group, a mercapto group, an alkoxyl group, an alkylthio group, an alkylsulfonyl group, an acyl group, an acyloxyl group, an amino group, an alkylamino group, a carboxyl group, an alkoxycarbonyl group, a carbamoyl group, a nitro group, a cyano group, a trifluoromethyl group, an alkenyl group which may have a substituent(s), an alkynyl group which may have a substituent(s), an aryl group which may have a substituent(s), a heteroaryl group which may have a substituent(s), a benzyloxyl group which may have a substituent(s), an aryloxyl group which may have a substituent(s), a heteroaryloxyl group which may have a substituent(s), an arylamino group which may have a substituent(s), an arylvinyl group which may have a substituent(s) or an arylethynyl group which may have a substituent(s);
B represents a fused aliphatic ring which may have a substituent(s);
—X— and —Y— may be the same or different from one another and they independently represent —NH— and —NR5—, wherein R5 represents a lower alkyl group which may have a substituent(s), an acyl group which may have a substituent(s), an alkoxycarbonyl group which may have a substituent(s), a carbamoyl group which may have a substituent(s) or a sulfonyl group which may have a substituent(s);
-Z- represents —CH2— or —CR6R7—, wherein R6 and R7 may be the same or different from each other and they independently represent a hydrogen atom, a halogen atom, a hydroxyl group, an alkyl group which may have a substituent(s), an aryl group, a mercapto group, an alkoxyl group, an alkylthio group, an alkylsulfonyl group, an acyl group, an acyloxyl group, an amino group, an alkylamino group, a carboxyl group, an alkoxycarbonyl group, a carbamoyl group, a nitro group, a cyano group or a trifluoromethyl group;
—W— represents —NR1—, wherein R1 represents a hydrogen atom, a lower alkyl group which may have a substituent(s) or an aryl group which may have a substituent(s);
and a, b and c each represent the position of carbon atom;
said heterocyclic ring is selected from the group consisting of pyridine ring, dihydropyran ring, pyridazine ring, pyrimidine ring, pyrazine ring, pyrrole ring, furan ring, thiophene ring, oxazole ring, isoxazole ring, pyrazole ring, imidazole ring, thiazole ring, isothiazole ring, thiadiazole ring, pyrrolidine ring, piperidine ring, piperazine ring, indole ring, isoindole ring, benzofuran ring, isobenzofuran ring, benzothiophene ring, benzopyrazole ring, benzoimidazole ring, benzoxazole ring, benzothiazole ring, purine ring, pyrazolopyridine ring, quinoline ring, isoquinoline ring, naphthyridine ring, quinazoline ring, benzodiazepine ring, carbazole ring, and dibenzofuran ring;
said acyl group is selected from the group consisting of formyl group, acetyl group, propionyl group, butyryl group, isobutyryl group, valeryl group, isovaleryl group, pivaloyl group, hexanoyl group, acryloyl group, methacryloyl group, crotonoyl group, isocrotonoyl group, benzoyl group, naphthoyl group, furanyl carbonyl group, thienyl carbonyl group, isoxazolyl carbonyl group, and thiazolyl carbonyl group;
said acyloxyl group is selected from the group consisting of formyloxyl group, acetyloxy group, propionyloxyl group, butyryloxyl group, isobutyryloxyl group, valeryloxyl group, isovaleryloxyl group, pivaloyloxyl group, hexanoyloxyl group, acryloyloxyl group, methacryloyloxyl group, crotonoyloxyl group, isocrotonoyloxyl group, benzoyloxyl group, and naphthoyloxyl group;
said heteroaryl group is selected from the group consisting of pyridyl group, pyridazinyl group, pyrimidinyl group, pyrazinyl group, pyrrolyl group, furanyl group, thienyl group, oxazolyl group, isoxazolyl group, pyrazolyl group, imidazolyl group, thiazolyl group, isothiazolyl group, thiadiazolyl group, indolyl group, isoindolyl group, benzofuryl group, isobenzofuryl group, benzothienyl group, benzopyrazolyl group, benzoimidazolyl group, benzoxazolyl group, benzothiazolyl group, quinolyl group, isoquinolyl group, naphthylidinyl group, quinazolyl group, oxadiazolyl group, and pyridonyl group;
said fused aliphatic ring is selected from the group consisting of cyclopropane ring, cyclobutane ring, cyclopentane ring, cyclohexane ring, cycloheptane ring, cyclooctane ring, and decalin ring, and wherein the substituent(s) is selected from the group consisting of halogen atoms, hydroxyl group, alkyl groups, mercapto group, alkoxyl groups, alkylthio groups, alkylsulfonyl groups, acyl groups, acyloxyl groups, amino group, alkylamino groups, carboxyl group, alkoxycarbonyl groups, carbamoyl groups, nitro group, cyano group, trifluoromethyl group, aryl groups and heteroaryl groups.

10 more elements

5:

The compound or pharmaceutically acceptable salt thereof according to claim 1, wherein in general formula (I), R2, R3 and R4 may be the same or different from one another and independently represent a hydrogen atom, a halogen atom, a hydroxyl group, an alkyl group, a mercapto group, an alkoxyl group, an alkylthio group, an alkylsulfonyl group, an acyl group, an acyloxyl group, an amino group, an alkylamino group, a carboxyl group, an alkoxycarbonyl group, a carbamoyl group, a nitro group, a cyano group, a trifluoromethyl group, an aryl group which may have a substituent(s), a heteroaryl group which may have a substituent(s), a benzyloxyl group which may have a substituent(s), an aryloxyl group which may have a substituent(s), a heteroaryloxyl group which may have a substituent(s), an arylamino group which may have a substituent(s), an arylvinyl group which may have a substituent(s) or an arylethynyl group which may have a substituent(s);
—X— and —Y— may be the same or different from one another and they independently represent —NH— or —NR5—, wherein R5 represents a lower alkyl group or an acyl group which may have a substituent(s);
-Z- represents —CH2— or —CR6R7—, wherein R6 and R7 may be the same or different from each other and they independently represent a hydrogen atom, a halogen atom, a hydroxyl group, an alkyl group, an aryl group, a mercapto group, an alkoxyl group, an alkylthio group, an alkylsulfonyl group, an acyl group, an acyloxyl group, an amino group, an alkylamino group, a carboxyl group, an alkoxycarbonyl group, a carbamoyl group, a nitro group, a cyano group or a trifluoromethyl group;
and wherein:
(i) the substituent(s) is selected from the group consisting of halogen atoms, hydroxyl group, alkyl groups, aryl groups, mercapto group, alkoxyl groups, alkylthio groups, alkylsulfonyl groups, acyl groups, acyloxyl groups, amino group, alkylamino groups, carboxyl group, alkoxycarbonyl groups, carbamoyl groups, nitro group, cyano group and trifluoromethyl group.

2 more elements

Lactam compounds and pharmaceutical use thereof

Life of this patent

Lactam compounds and pharmaceutical use thereof

Life of this patent

Abstract

Claims36