Benzene Compound Having 2 or More Substituents

• US 20080004301A1
• Filed: 10/26/2005
• Published: 01/03/2008
• Est. Priority Date: 10/27/2004
• Status: Active Grant

• Current Assignee: Daiichi Sankyo Company Limited
• Original Assignee: Daiichi Sankyo Company Limited
• Inventors: Nakai, Daisuke, Yamaguchi, Takahiro, Tamaki, Kazuhiko, Oda, Kozo, Terasaka, Naoki, Nakadai, Masakazu
• Granted Patent: US 7,923,573 B2
• Time in Patent Office: Days
• US Class Current: 514/275
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• CPC Class Codes: C07C 205/35 having nitro groups and etherified hydroxy groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
• CPC Class Codes: C07C 217/80 having amino groups and etherified hydroxy groups bound to carbon atoms of non-condensed six-membered aromatic rings
• CPC Class Codes: C07C 235/34 having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
• CPC Class Codes: C07C 235/46 having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
• CPC Class Codes: C07C 255/57 containing cyano groups and carboxyl groups, other than cyano groups, bound to the carbon skeleton
• CPC Class Codes: C07C 311/04 to acyclic carbon atoms of hydrocarbon radicals substituted by singly-bound oxygen atoms
• CPC Class Codes: C07C 311/08 having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
• CPC Class Codes: C07C 317/22 with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
• CPC Class Codes: C07C 317/46 the carbon skeleton being further substituted by singly-bound oxygen atoms
• CPC Class Codes: C07C 323/62 having the sulfur atom of at least one of the thio groups bound to a carbon atom of a six-membered aromatic ring of the carbon skeleton
• CPC Class Codes: C07C 45/00 Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
• CPC Class Codes: C07C 45/673 by change of size of the carbon skeleton
• CPC Class Codes: C07C 45/68 by increase in the number of carbon atoms
• CPC Class Codes: C07C 47/565 all hydroxy groups bound to the ring
• CPC Class Codes: C07C 65/24 polycyclic
• CPC Class Codes: C07C 65/30 containing —CHO groups
• CPC Class Codes: C07C 65/34 polycyclic
• CPC Class Codes: C07C 65/40 containing singly bound oxygen-containing groups
• CPC Class Codes: C07C 69/78 Benzoic acid esters
• CPC Class Codes: C07C 69/88 : with esterified carboxyl groups
• CPC Class Codes: C07C 69/92 : with etherified hydroxyl groups
• CPC Class Codes: C07C 69/94 : of polycyclic hydroxy carboxylic acids, the hydroxy groups and the carboxyl groups of which are bound to carbon atoms of six-membered aromatic rings
• CPC Class Codes: C07D 213/55 : Acids; Esters
• CPC Class Codes: C07D 213/65 : attached in position 3 or 5
• CPC Class Codes: C07D 213/71 : to which a second hetero atom is attached
• CPC Class Codes: C07D 213/79 : Acids; Esters
• CPC Class Codes: C07D 213/80 : in position 3
• CPC Class Codes: C07D 239/26 : with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
• CPC Class Codes: C07D 257/04 : Five-membered rings
• CPC Class Codes: C07D 277/30 : Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
• CPC Class Codes: C07D 307/84 : Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
• CPC Class Codes: C07D 333/24 : Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Abstract

A superior LXR modulator is provided. A compound represented by the general formula (I):
[wherein R¹: —COR⁹ (wherein R⁹: alkyl, optionally substituted alkoxy or optionally substituted amino); R²: H, OH, alkoxy, optionally substituted amino, etc.; R³: H, optionally substituted alkyl, cycloalkyl, optionally substituted alkoxy, optionally substituted amino, halogeno, etc.; R⁴ and R⁵: H, optionally substituted alkyl, halogeno, etc.; R⁶ and R⁷: H, alkyl; R⁸: —X²R¹⁰ [wherein R¹⁰: —COR¹¹ (wherein R¹¹: OH, optionally substituted alkoxy, optionally substituted amino, etc.), —SO₂R¹² (wherein R¹²: optionally substituted alkyl, optionally substituted amino, etc.), tetrazol-5-yl, etc.; X²: single bond, optionally substituted alkylene, etc.]; X¹: —NH—, —O—, —S—, etc.; Y¹: optionally substituted phenyl, optionally substituted 5- to 6-membered aromatic heterocyclyl; Y²: optionally substituted aryl, optionally substituted heterocyclyl, etc.] and the like is provided.

Claims

1. A compound represented by the general formula (I) or a pharmacologically acceptable salt or ester thereof:

2. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R¹ is a group having the formula —

COR^9a [wherein R^9a represents a C₁-C₆ alkyl group, a C₁-C₈ alkoxy group, a halogeno C₁-C₆ alkoxy group (wherein said halogeno C₁-C₆ alkoxy group represents a C₁-C₆ alkoxy group substituted with 1 to 7 halogeno groups), a C₁-C₆ alkylamino group, or a di(C₁-C₆ alkyl)amino group (wherein said alkyl groups may be the same or different and two of said alkyl groups may, together with the nitrogen atom of said amino group, form a 5- to 7-membered saturated heterocyclyl group containing 1 to 3 atoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom)].

3. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R¹ is a group having the formula —

COR^9b [wherein R^9b represents a C₁-C₆ alkoxy group or a halogeno C₁-C₄ alkoxy group (wherein said halogeno C₁-C₄ alkoxy group represents a C₁-C₄ alkoxy group substituted with 1 to 5 halogeno groups)].

4. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R¹ is a group having the formula —

COR^9c (wherein R^9c represents a C₃-C₅ alkoxy group).

5. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R¹ is a group having the formula —

COR^9d (wherein R^9d represents a 2-methyl-2-propoxy group).

6. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R² is a hydrogen atom, a trifluoromethyl group, a 2,2,2-trifluoroethyl group, a pentafluoroethyl group, a hydroxyl group, a fluoro group or a chloro group.

7. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R² is a hydrogen atom or a hydroxyl group.

8. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R² is a hydroxyl group.

9. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R³ is a hydrogen atom, a C₁-C₄ alkyl group, a halogeno C₁-C₄ alkyl group (wherein said halogeno C₁-C₄ alkyl group represents a C₁-C₄ alkyl group substituted with 1 to 5 halogeno groups), a C₃-C₅ cycloalkyl group, a C₂-C₄ alkenyl group, a C₂-C₄ alkynyl group, a hydroxyl group, a C₁-C₄ alkoxy group, a halogeno C₁-C₄ alkoxy group (wherein said halogeno C₁-C₄ alkoxy group represents a C₁-C₄ alkoxy group substituted with 1 to 5 halogeno groups), a C₁-C₄ alkylthio group, a C₁-C₄ alkylsulfinyl group, a C₁-C₄ alkylsulfonyl group, an amino group, a C₁-C₄ alkylamino group, a di(C₁-C₄ alkyl)amino group (wherein said alkyl groups may be the same or different and two of said alkyl groups may, together with the nitrogen atom of said amino group, form a 5- to 7-membered saturated heterocyclyl group containing 1 to 3 atoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom), a fluoro group, a chloro group or a bromo group.

10. A compound) or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R³ is a hydrogen atom, a C₁-C₄ alkyl group, a halogeno C₁-C₄ alkyl group (wherein said halogeno C₁-C₄ alkyl group represents a C₁-C₄ alkyl group substituted with 1 to 5 halogeno groups), a C₃-C₅ cycloalkyl group, a C₂-C₄ alkenyl group, a C₁-C₄ alkoxy group, a fluoro group or a chloro group.

11. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R³ is a methyl group, an ethyl group, a 2-propyl group, a 2-methyl-2-propyl group, a trifluoromethyl group, a 2,2,2-trifluoroethyl group, a methoxy group, a fluoro group or a chloro group.

12. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R³ is a 2-propyl group, a 2-methyl-2-propyl group, a trifluoromethyl group or a chloro group.

13. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R³ is a trifluoromethyl group.

14. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R⁴ and R⁵ may be the same or different and each is a hydrogen atom, a methyl group, an ethyl group, a trifluoromethyl group, a cyclopropyl group, a hydroxyl group, a methoxy group, a fluoro group, a chloro group or a bromo group.

15. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R⁴ is a hydrogen atom, and R⁵ is a hydrogen atom or a hydroxyl group.

16. A compound or pharmacologically acceptable salt or ester thereof according to claim 1, wherein R⁴ and R⁵ are hydrogen atoms.

17. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R⁶ and R⁷ may be the same or different and each is a hydrogen atom or a methyl group.

18. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R⁶ and R⁷ are hydrogen atoms.

19. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R⁸ is a group having the formula —

X^2aR^10a [wherein R^10a represents a group having the formula —

COR^11a [wherein R^11a represents a hydroxyl group, a C₁-C₄ alkoxy group, a (C₃-C₆ cycloalkyl)-(C₁-C₄ alkyl)oxy group, a C₃-C₆ cycloalkyloxy group, an amino group, a C₁-C₄ alkylamino group, a [(C₃-C₆ cycloalkyl)-(C₁-C₄ alkyl)]amino group, a C₃-C₆ cycloalkylamino group, a di(C₁-C₄ alkyl)amino group (wherein said alkyl groups may be the same or different and two of said alkyl groups may, together with the nitrogen atom of said amino group, form a 5- to 7-membered saturated heterocyclyl group containing 1 to 3 atoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom), a hydroxylamino group or a hydroxyl(C₁-C₄ alkyl)]amino group],

a group having the formula —

SO₂R^12a [wherein R^12a represents a C₁-C₄ alkyl group, a (C₃-C₆ cycloalkyl)-(C₁-C₄ alkyl) group, a C₃-C₆ cycloalkyl group, an amino group, a C₁-C₄ alkylamino group, a [(C₃-C₆ cycloalkyl)-(C₁-C₄ alkyl)]amino group, a C₃-C₆ cycloalkylamino group or a di(C₁-C₄ alkyl)amino group (wherein said alkyl groups may be the same or different and two of said alkyl groups may, together with the nitrogen atom of said amino group, form a 5- to 7-membered saturated heterocyclyl group containing 1 to 3 atoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom)],

a group having the formula —

N(R^13a)COR^14a [wherein R^13a represents a hydrogen atom, a C₁-C₄ alkyl group, a (C₃-C₅ cycloalkyl)-(C₁-C₂ alkyl) group or a C₃-C₅ cycloalkyl group, and R^14a represents a hydrogen atom, a C₁-C₄ alkyl group, a (C₃-C₅ cycloalkyl)-(C₁-C₂ alkyl) group or a C₃-C₅ cycloalkyl group],

a group having the formula —

N(R^13a)SO₂R^15a [wherein R^13a is the same as previously defined, and R^15a represents a C₁-C₄ alkyl group, a (C₃-C₅ cycloalkyl)-(C₁-C₂ alkyl) group or a C₃-C₅ cycloalkyl group], or a tetrazol-5-yl group, and

X^2a represents a single bond, a C₁-C₂ alkylene group or a substituted C₁-C₂ alkylene group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group γ

1, or two of said substituents may together form a methylene group, an ethylene group or a trimethylene group)]; and

,

Substituent group γ

1 is the group consisting of a methyl group, an ethyl group, a hydroxymethyl group, a hydroxyethyl group, a methoxymethyl group, a methoxyethyl group, a methylthiomethyl group, a methylthioethyl group, an aminomethyl group, an aminoethyl group, a methylaminomethyl group, an ethylaminomethyl group, a methylaminoethyl group, a cyclopropylaminomethyl group, a cyclopropylaminoethyl group, a dimethylaminomethyl group, a dimethylaminoethyl group, a (N-methyl-N-ethylamino)methyl group, a dicyclopropylaminomethyl group, a hydroxyl group, a methoxy group, an ethoxy group, a cyclopropyloxy group, a methylthio group, an ethylthio group, a cyclopropylthio group, an amino group, a methylamino group, an ethylamino group, a cyclopropylamino group, a cyclobutylamino group, a dimethylamino group, a diethylamino group, a dicyclopropylamino group, a N-cyclopropyl-N-methylamino group, a fluoro group and a chloro group.

20. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R⁸ is a group having the formula —

X^2bR^10b [wherein R^10b represents a group having the formula —

COR^11b [wherein R^11b represents a hydroxyl group, a C₁-C₄ alkoxy group, a (C₃-C₅ cycloalkyl)-(C₁-C₂ alkyl)oxy group, a C₃-C₅ cycloalkyloxy group, an amino group, a methylamino group, an ethylamino group, a dimethylamino group, a diethylamino group, a methylethylamino group or a hydroxylamino group],

a group having the formula —

SO₂R^12b [wherein R^12b represents a C₁-C₄ alkyl group, a (C₃-C₅ cycloalkyl)-(C₁-C₂ alkyl) group or a C₃-C₅ cycloalkyl group], or a tetrazol-5-yl group, and

X^2b represents a single bond, a methylene group, an ethylene group or a substituted methylene group or a substituted ethylene group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group γ

2, or two of said substituents may together form an ethylene group or a trimethylene group)]; and

,

Substituent group γ

2 represents the group consisting of a methyl group, an ethyl group, a hydroxymethyl group, a methoxymethyl group, an aminomethyl group, a methylaminomethyl group, a dimethylaminomethyl group, a (N-methyl-N-ethylamino)methyl group, a methoxy group, an ethoxy group, a methylamino group, a dimethylamino group, a fluoro group and a chloro group.

21. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R⁸ is a group having the formula —

X^2cR^10c [wherein R^10c represents a group having the formula —

COR^11c (wherein R^11c represents a hydroxyl group or a methoxy group), or

a group having the formula —

SO₂R^12c (wherein R^12c represents a methyl group), and

X^2c represents a single bond, a methylene group or a substituted methylene group (wherein said substituent is a group selected from Substituent group γ

3, or two of said substituents may together form an ethylene group)]; and

,

Substituent group γ

3 is the group consisting of a methyl group, an ethyl group, a hydroxymethyl group, a dimethylaminomethyl group, a methoxy group and an ethoxy group.

22. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R⁸ is a group having the formula —

X^2dR^10d [wherein R^10d represents a group having the formula —

COR^11d (wherein R^11d represents a hydroxyl group), and

X^2d represents a methylene group or a substituted methylene group (wherein said substituent is a group selected from Substituent group γ

4, or two of said substituents may together form an ethylene group)]; and

,

Substituent group γ

4 is the group consisting of a methyl group, an ethyl group and a hydroxymethyl group.

23. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R⁸ is a group having the formula —

X^2eR^10e [wherein R^10e represents a group having the formula —

COR^11e (wherein R^11e represents a hydroxyl group), and

X^2e represents a methylene group or a substituted methylene group (wherein said substituent is a methyl group)].

24. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R⁸ is a group having the formula —

X^2fR^10f [wherein R^10f represents a group having the formula —

SO₂R^12f (wherein R^12f represents a methyl group), and

X^2f represents a single bond].

25. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein X¹ is a group having the formula —

NH—

, —

O—

or —

S—

.

26. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein X¹ is a group having the formula —

O—

.

27. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein Y¹ is a phenyl group, a substituted phenyl group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group α

1), a 5- or 6-membered aromatic heterocyclyl group (wherein said heterocyclyl group represents a pyrrolyl group, a furyl group, a thienyl group, an imidazolyl group, an oxazolyl group, a thiazolyl group, a pyridyl group or a pyridazinyl group) or a substituted 5- or 6-membered aromatic heterocyclyl group (wherein said heterocyclyl group represents a pyrrolyl group, a furyl group, a thienyl group, an imidazolyl group, an oxazolyl group, a thiazolyl group, a pyridyl group or a pyridazinyl group, and said substituents may be the same or different and are one or two groups selected from Substituent group α

1), and

Substituent group α

1 is the group consisting of a methyl group, an ethyl group, a trifluoromethyl group, a methoxy group, an ethoxy group, a fluoro group and a chloro group.

28. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein Y¹ is a phenyl group (wherein the substitution positions where X¹ and Y² are bonded to said phenyl group are the 1 and 3 positions or the 1 and 4 positions, respectively), a substituted phenyl group (wherein said substituent is a group selected from Substituent group α

2, and the substitution positions where X¹ and Y² are bonded to said phenyl group are the 1 and 3 positions or the 1 and 4 positions, respectively), a thienyl group (wherein the substitution positions where X¹ and Y² are bonded to said thienyl group are the 2 and 5 positions, respectively), a substituted thienyl group (wherein said substituent is a group selected from Substituent group α

2, and the substitution positions where X¹ and Y² are bonded to said thienyl group are the 2 and 5 positions, respectively), a pyridyl group (wherein the substitution positions where X¹ and Y² are bonded to said pyridyl group are the 2 and 5 positions or the 5 and 2 positions, respectively) or a substituted pyridyl group (wherein said substituent is a group selected from Substituent group α

2, and the substitution positions where X¹ and Y² are bonded to said pyridyl group are the 2 and 5 positions or the 5 and 2 positions, respectively), and

Substituent group α

2 is the group consisting of a methyl group, a fluoro group and a chloro group.

29. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein Y¹ is a phenyl group (wherein the substitution positions where X¹ and Y² are bonded to said phenyl group are the 1 and 4 positions, respectively) or a pyridyl group (wherein the substitution positions where X¹ and Y² are bonded to said pyridyl group are the 5 and 2 positions, respectively).

30. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein Y¹ is a phenyl group (wherein the substitution positions where X¹ and Y² are bonded to said phenyl group are the 1 and 4 positions).

31. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein Y² is a phenyl group, a substituted phenyl group (wherein said substituents may be the same or different and are 1 to 3 groups selected from Substituent group β

1), an indanyl group or a tetrahydronaphthyl group (provided that Y¹ is bonded to a benzene ring part in said indanyl or tetrahydronaphthyl group), a substituted indanyl group or a substituted tetrahydronaphthyl group (provided that Y¹ is bonded to a benzene ring part in said indanyl or tetrahydronaphthyl group, and said substituents may be the same or different and are 1 to 3 groups selected from Substituent group β

1), a 5- or 6-membered aromatic heterocyclyl group (wherein said heterocyclyl group represents a pyrrolyl group, a furyl group, a thienyl group, an imidazolyl group, an oxazolyl group, a thiazolyl group, a pyridyl group or a pyrimidinyl group), a substituted 5- or 6-membered aromatic heterocyclyl group (wherein said heterocyclyl group represents a pyrrolyl group, a furyl group, a thienyl group, an imidazolyl group, an oxazolyl group, a thiazolyl group, a pyridyl group or a pyrimidinyl group, and said substituents may be the same or different and are 1 to 3 groups selected from Substituent group β

1), a 9- or 10-membered unsaturated heterocyclyl group (provided that Y¹ is bonded to an aromatic ring part in said unsaturated heterocyclyl group, and said unsaturated heterocyclyl group represents an indolinyl group, a dihydrobenzofuryl group, a dihydrobenzothienyl group, a tetrahydroquinolyl group or a chromanyl group), or a substituted 9- or 10-membered unsaturated heterocyclyl group (provided that Y¹ is bonded to an aromatic ring part in said unsaturated heterocyclyl group, said unsaturated heterocyclyl group represents an indolinyl group, a dihydrobenzofuryl group, a dihydrobenzothienyl group, a tetrahydroquinolyl group or a chromanyl group, and said substituents may be the same or different and are 1 to 3 groups selected from Substituent group β

1); and

,

Substituent group β

1 is the group consisting of a C₁-C₆ alkyl group, a hydroxy(C₁-C₄ alkyl) group, a carboxy(C₁-C₄ alkyl) group, a (C₁-C₄ alkoxy)carbonyl-(C₁-C₄ alkyl) group, a halogeno C₁-C₄ alkyl group (wherein said halogeno C₁-C₄ alkyl group represents a C₁-C₄ alkyl group substituted with 1 to 5 halogeno atoms), a (C₃-C₆ cycloalkyl)-(C₁-C₄ alkyl) group, a C₂-C₅ alkenyl group, a C₂-C₅ alkynyl group, a C₃-C₆ cycloalkyl group, a hydroxyl group, a C₁-C₄ alkoxy group, a halogeno C₁-C₄ alkoxy group (wherein said halogeno C₁-C₄ alkoxy group represents a C₁-C₄ alkoxy group substituted with 1 to 5 halogeno groups), a C₁-C₄ alkylthio group, a C₁-C₄ alkylsulfinyl group, a C₁-C₄ alkylsulfonyl group, an amino group, a C₁-C₄ alkylamino group, a C₃-C₆ cycloalkylamino group, a di(C₁-C₄ alkyl)amino group (wherein said alkyl groups may be the same or different and two of said alkyl groups may, together with the nitrogen atom of said amino group, form a 5- to 7-membered saturated heterocyclyl group containing 1 to 3 atoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom), a formylamino group, a (C₁-C₄ alkyl)carbonylamino group, a (C₃-C₆ cycloalkyl)carbonylamino group, a N—

[(C₁-C₄ alkyl)carbonyl]-N—

(C₁-C₄ alkyl)amino group, a N—

[(C₃-C₆ cycloalkyl)carbonyl]-N—

(C₁-C₄ alkyl)amino group, a C₁-C₄ alkylsulfonylamino group, a N—

(C₁-C₄ alkylsulfonyl)-N—

(C₁-C₄ alkyl)amino group, a formyl group, a (C₁-C₄ alkyl)carbonyl group, a carboxyl group, a (C₁-C₄ alkoxy)carbonyl group, a carbamoyl group, a (C₁-C₄ alkylamino)carbonyl group, a di(C₁-C₄ alkyl)aminocarbonyl group (wherein said alkyl groups may be the same or different and two of said alkyl groups may, together with the nitrogen atom of said amino group, form a 5- to 7-membered saturated heterocyclyl group containing 1 to 3 atoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom), a cyano group, a nitro group, a fluoro group, a chloro group and a bromo group.

32. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein Y² is a phenyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 3 positions or the 1 and 4 positions, respectively), a substituted phenyl group (wherein said substituents may be the same or different and represent one or two groups selected from Substituent group β

2, and the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 3 positions or the 1 and 4 positions, respectively), a thienyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said thienyl group are the 2 and 5 positions, respectively), a substituted thienyl group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group β

2, and the substitution positions where Y¹ and R⁸ are bonded to said thienyl group are the 2 and 5 positions, respectively), a thiazolyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said thiazolyl group are the 2 and 5 positions, respectively), a substituted thiazolyl group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group β

2, and the substitution positions where Y¹ and R⁸ are bonded to said thiazolyl group are the 2 and 5 positions, respectively), a pyridyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said pyridyl group are the 2 and 5 positions or the 3 and 5 positions, respectively) or a substituted pyridyl group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group β

2, and the substitution positions where Y¹ and R⁸ are bonded to said pyridyl group are the 2 and 5 positions or the 3 and 5 positions, respectively); and

,

Substituent group β

2 is the group consisting of a C₁-C₄ alkyl group, a hydroxymethyl group, a 1-hydroxyethyl group, a trifluoromethyl group, a 2,2,2-trifluoroethyl group, a pentafluoroethyl group, a C₂-C₄ alkenyl group, a C₂-C₄ alkynyl group, a C₃-C₄ cycloalkyl group, a hydroxyl group, a methoxy group, an ethoxy group, a methanesulfonyl group, an ethanesulfonyl group, an amino group, a methylamino group, an ethylamino group, a dimethylamino group, a diethylamino group, a formyl group, a methylcarbonyl group, an ethylcarbonyl group, a cyano group, a nitro group, a fluoro group and a chloro group.

33. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein Y² is a phenyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 4 positions, respectively), a substituted phenyl group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group β

3, and the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 4 positions, respectively), a thienyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said thienyl group are the 2 and 5 positions, respectively), a substituted thienyl group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group β

3, and the substitution positions where Y¹ and R⁸ are bonded to said thienyl group are the 2 and 5 positions, respectively), a pyridyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said pyridyl group are the 2 and 5 positions, respectively) or a substituted pyridyl group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group β

3, and the substitution positions where Y¹ and R⁸ are bonded to said pyridyl group are the 2 and 5 positions, respectively); and

,

Substituent group β

3 is the group consisting of a methyl group, an ethyl group, a 2-propyl group, a hydroxymethyl group, a trifluoromethyl group, a cyclopropyl group, a methoxy group, a methanesulfonyl group, an amino group, a methylamino group, a dimethylamino group, a methylcarbonyl group, an ethylcarbonyl group, a cyano group, a nitro group, a fluoro group and a chloro group.

34. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein Y² is a phenyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 4 positions, respectively), a substituted phenyl group (wherein said substituents may be the same or different and are a group selected from Substituent group β

3 or two groups selected from Substituent group β

4, and the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 4 positions, respectively), a thienyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said thienyl group are the 2 and 5 positions, respectively) or a substituted thienyl group (wherein said substituents may be the same or different and are a group selected from Substituent group β

3 or two groups selected from Substituent group β

4, and the substitution positions where Y¹ and R⁸ are bonded to said thienyl group are the 2 and 5 positions, respectively); and

,

Substituent group β

4 is the group consisting of a methyl group, an ethyl group and a fluoro group.

35. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein Y² is a phenyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 4 positions, respectively), or a substituted phenyl group (wherein said substituent is a group selected from Substituent group β

5, two methyl groups or two fluoro groups, and the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 4 positions, respectively); and

,

Substituent group β

5 is the group consisting of a methyl group, an ethyl group, a 2-propyl group, a trifluoromethyl group, a nitro group, a fluoro group and a chloro group.

36. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein Y² is a phenyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 3 positions, respectively), a substituted phenyl group (wherein said substituent is a group selected from Substituent group β

6, and the substitution positions where Y¹, R⁸ and the substituent are bonded to said phenyl group are the 1, 3 and 2 positions, respectively), a pyridyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said pyridyl group are the 3 and 5 positions, respectively) or a substituted pyridyl group (wherein said substituent is a group selected from Substituent group β

36, and the substitution positions where Y¹, R⁸ and the substituent are bonded to said pyridyl group are the 3, 5 and 4 positions, respectively); and

,

Substituent group β

6 is the group consisting of a C₁-C₄ alkyl group, a methoxy group, a fluoro group and a chloro group.

37. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein Y² is a phenyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 3 positions, respectively) or a substituted phenyl group (wherein said substituent is a group selected from Substituent group β

37, and the substitution positions where Y¹, R⁸ and the substituent are bonded to said phenyl group are the 1, 3 and 2 positions, respectively); and

,

Substituent group β

7 is the group consisting of a methyl group, an ethyl group, a methoxy group and a fluoro group.

38. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R¹ is a group having the formula —

COR^9a wherein R^9a represents a C₁-C₆ alkyl group, a C₁-C₈ alkoxy group, a halogeno C₁-C₆ alkoxy group (wherein said halogeno C₁-C₆ alkoxy group represents a C₁-C₆ alkoxy group substituted with 1 to 7 halogeno groups), a C₁-C₆ alkylamino group or a di(C₁-C₆ alkyl)amino group (wherein said alkyl groups may be the same or different and two of said alkyl groups may, together with the nitrogen atom of said amino group, form a 5- to 7-membered saturated heterocyclyl group containing 1 to 3 atoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom)];

R² is a hydrogen atom, a trifluoromethyl group, a 2,2,2-trifluoroethyl group, a pentafluoroethyl group, a hydroxyl group, a fluoro group or a chloro group;

R³ is a hydrogen atom, a C₁-C₄ alkyl group, a halogeno C₁-C₄ alkyl group (wherein said halogeno C₁-C₄ alkyl group represents a C₁-C₄ alkyl group substituted with 1 to 5 halogeno groups), a C₃-C₅ cycloalkyl group, a C₂-C₄ alkenyl group, a C₂-C₄ alkynyl group, a hydroxyl group, a C₁-C₄ alkoxy group, a halogeno C₁-C₄ alkoxy group (wherein said halogeno C₁-C₄ alkoxy group represents a C₁-C₄ alkoxy group substituted with 1 to 5 halogeno groups), a C₁-C₄ alkylthio group, a C₁-C₄ alkylsulfinyl group, a C₁-C₄ alkylsulfonyl group, an amino group, a C₁-C₄ alkylamino group, a di(C₁-C₄ alkyl)amino group (wherein said alkyl groups may be the same or different and two of said alkyl groups may, together with the nitrogen atom of said amino group, form a 5- to 7-membered saturated heterocyclyl group containing 1 to 3 atoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom), a fluoro group, a chloro group or a bromo group;

R⁴ and R⁵ may be the same or different and each is a hydrogen atom, a methyl group, an ethyl group, a trifluoromethyl group, a cyclopropyl group, a hydroxyl group, a methoxy group, a fluoro group, a chloro group or a bromo group;

R⁶ and R⁷ may be the same or different and each is a hydrogen atom or a methyl group;

R⁸ is a group having the formula —

X^2aR^10a [wherein R^10a represents a group having the formula —

COR^11a [wherein R^11a represents a hydroxyl group, a C₁-C₄ alkoxy group, a (C₃-C₆ cycloalkyl)-(C₁-C₄ alkyl)oxy group, a C₃-C₆ cycloalkyloxy group, an amino group, a C₁-C₄ alkylamino group, a [(C₃-C₆ cycloalkyl)-(C₁-C₄ alkyl)]amino group, a C₃-C₆ cycloalkylamino group, a di(C₁-C₄ alkyl)amino group (wherein said alkyl groups may be the same or different and two of said alkyl groups may, together with the nitrogen atom of said amino group, form a 5- to 7-membered saturated heterocyclyl group containing 1 to 3 atoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom), a hydroxylamino group or a hydroxyl(C₁-C₄ alkyl)amino group],

a group having the formula —

SO₂R^12a [wherein R^12a represents a C₁-C₄ alkyl group, a (C₃-C₆ cycloalkyl)-(C₁-C₄ alkyl) group, a C₃-C₆ cycloalkyl group, an amino group, a C₁-C₄ alkylamino group, a [(C₃-C₆ cycloalkyl)-(C₁-C₄ alkyl)]amino group, a C₃-C₆ cycloalkylamino group or a di(C₁-C₄ alkyl)amino group (wherein said alkyl groups may be the same or different and two of said alkyl groups may, together with the nitrogen atom of said amino group, form a 5- to 7-membered saturated heterocyclyl group containing 1 to 3 atoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom)],

a group having the formula —

N(R^13a)COR^14a [wherein R^13a represents a hydrogen atom, a C₁-C₄ alkyl group, a (C₃-C₅ cycloalkyl)-(C₁-C₂ alkyl) group or a C₃-C₅ cycloalkyl group, and R^14a represents a hydrogen atom, a C₁-C₄ alkyl group, a (C₃-C₅ cycloalkyl)-(C₁-C₂ alkyl) group or a C₃-C₅ cycloalkyl group],

a group having the formula —

N(R^13a)SO₂R^15a [wherein R^13a is the same as previously defined, and R^15a represents a C₁-C₄ alkyl group, a (C₃-C₅ cycloalkyl)-(C₁-C₂ alkyl) group or a C₃-C₅ cycloalkyl group], or a tetrazol-5-yl group, and

X^2a represents a single bond, a C₁-C₂ alkylene group or a substituted C₁-C₂ alkylene group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group γ

1, or two of said substituents may together form a methylene group, an ethylene group or a trimethylene group)];

X¹ is a group having the formula —

NH—

, —

O—

or —

S—

;

Y¹ is a phenyl group, a substituted phenyl group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group α

1), a 5- or 6-membered aromatic heterocyclyl group (wherein said heterocyclyl group represents a pyrrolyl group, a furyl group, a thienyl group, an imidazolyl group, an oxazolyl group, a thiazolyl group, a pyridyl group or a pyridazinyl group) or a substituted 5- or 6-membered aromatic heterocyclyl group (wherein said heterocyclyl group represents a pyrrolyl group, a furyl group, a thienyl group, an imidazolyl group, an oxazolyl group, a thiazolyl group, a pyridyl group or a pyridazinyl group, said substituents may be the same or different and are one or two groups selected from Substituent group α

1); and

,

Y² is a phenyl group, a substituted phenyl group (wherein said substituents may be the same or different and are 1 to 3 groups selected from Substituent group β

1), an indanyl or tetrahydronaphthyl group (provided that Y¹ is bonded to a benzene ring part in said indanyl or tetrahydronaphthyl group), a substituted indanyl group or a substituted tetrahydronaphthyl group (provided that Y¹ is bonded to a benzene ring part in said indanyl or tetrahydronaphthyl group, and said substituents may be the same or different and are 1 to 3 groups selected from Substituent group β

1), a 5- or 6-membered aromatic heterocyclyl group (wherein said heterocyclyl group represents a pyrrolyl group, a furyl group, a thienyl group, an imidazolyl group, an oxazolyl group, a thiazolyl group, a pyridyl group or a pyrimidinyl group), a substituted 5- or 6-membered aromatic heterocyclyl group (wherein said heterocyclyl group represents a pyrrolyl group, a furyl group, a thienyl group, an imidazolyl group, an oxazolyl group, a thiazolyl group, a pyridyl group or a pyrimidinyl group, said substituents may be the same or different and are 1 to 3 groups selected from Substituent group β

1), a 9- or 10-membered unsaturated heterocyclyl group (provided that Y¹ is bonded to an aromatic ring part in said unsaturated heterocyclyl group, and said unsaturated heterocyclyl group represents an indolinyl group, a dihydrobenzofuryl group, a dihydrobenzothienyl group, a tetrahydroquinolyl group or a chromanyl group) or a substituted 9- or 10-membered unsaturated heterocyclyl group (provided that Y¹ is bonded to an aromatic ring part in said unsaturated heterocyclyl group, said unsaturated heterocyclyl group represents an indolinyl group, a dihydrobenzofuryl group, a dihydrobenzothienyl group, a tetrahydroquinolyl group or a chromanyl group, and said substituents may be the same or different and are 1 to 3 groups selected from Substituent group β

1).

39. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R¹ is a group having the formula —

COR^9b [wherein R^9b represents a C₁-C₆ alkoxy group or a halogeno C₁-C₄ alkoxy group (wherein said halogeno C₁-C₄ alkoxy group represents a C₁-C₄ alkoxy group substituted with 1 to 5 halogeno groups)];

R² is a hydrogen atom or a hydroxyl group;

R³ is a hydrogen atom, a C₁-C₄ alkyl group, a halogeno C₁-C₄ alkyl group (wherein said halogeno C₁-C₄ alkyl group represents a C₁-C₄ alkyl group substituted with 1 to 5 halogeno groups), a C₃-C₅ cycloalkyl group, a C₂-C₄ alkenyl group, a C₁-C₄ alkoxy group, a fluoro group or a chloro group;

R⁴ is a hydrogen atom and R⁵ is a hydrogen atom or a hydroxyl group;

R⁶ and R⁷ are hydrogen atoms;

R⁸ is a group having the formula —

X^2bR^10b [wherein R^10b represents a group having the formula —

COR^11b [wherein R^11b represents a hydroxyl group, a C₁-C₄ alkoxy group, a (C₃-C₅ cycloalkyl)-(C₁-C₂ alkyl)oxy group, a C₃-C₅ cycloalkyloxy group, an amino group, a methylamino group, an ethylamino group, dimethylamino group, a diethylamino group, a methylethylamino group or a hydroxylamino group],

a group having the formula —

SO₂R^12b [wherein R^12b represents a C₁-C₄ alkyl group, a (C₃-C₅ cycloalkyl)-(C₁-C₂ alkyl) group or a C₃-C₅ cycloalkyl group], or a tetrazol-5-yl group, and

X^2b represents a single bond, a methylene group, an ethylene group or a substituted methylene group or a substituted ethylene group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group Y², or two of said substituents may together form an ethylene group or a trimethylene group)];

X¹ is a group having the formula —

O—

;

Y¹ is a phenyl group (wherein the substitution positions where X¹ and Y² are bonded to said phenyl group are the 1 and 3 positions or the 1 and 4 positions, respectively), a substituted phenyl group (wherein said substituents represent a group selected from Substituent group α

2, and the substitution positions where X¹ and Y² are bonded to said phenyl group are the 1 and 3 positions or the 1 and 4 positions, respectively), a thienyl group (wherein the substitution positions where X¹ and Y² are bonded to said thienyl group are the 2 and 5 positions, respectively), a substituted thienyl group (wherein said substituent is a group selected from Substituent group α

2, and the substitution positions where X¹ and Y² are bonded to said thienyl group are the 2 and 5 positions, respectively), a pyridyl group (wherein the substitution positions where X¹ and Y² are bonded to said pyridyl group are the 2 and 5 positions or the 5 and 2 positions, respectively) or a substituted pyridyl group (wherein said substituent is a group selected from Substituent group α

2, and the substitution positions where X¹ and Y² are bonded to said pyridyl group are the 2 and 5 positions or the 5 and 2 positions, respectively); and

,

Y² is a phenyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 3 positions or the 1 and 4 positions, respectively), a substituted phenyl group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group β

2, and the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 3 positions or the 1 and 4 positions, respectively), a thienyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said thienyl group are the 2 and 5 positions, respectively), a substituted thienyl group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group β

2, and the substitution positions where Y¹ and R⁸ are bonded to said thienyl group are the 2 and 5 positions, respectively), a thiazolyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said thiazolyl group are the 2 and 5 positions, respectively), a substituted thiazolyl group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group β

2, and the substitution positions where Y¹ and R⁸ are bonded to said thiazolyl group are the 2 and 5 positions, respectively), a pyridyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said pyridyl group are the 2 and 5 positions or the 3 and 5 positions, respectively) or a substituted pyridyl group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group β

2, and the substitution positions where Y¹ and R⁸ are bonded to said pyridyl group are the 2 and 5 positions or the 3 and 5 positions, respectively).

40. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein

R¹ is a group having the formula —

COR^9c (wherein R^9c represents a C₃-C₅ alkoxy group);

R² is a hydroxyl group;

R³ is a methyl group, an ethyl group, a 2-propyl group, a 2-methyl-2-propyl group, a trifluoromethyl group, a 2,2,2-trifluoroethyl group, a methoxy group, a fluoro group or a chloro group;

R⁴ and R⁵ are hydrogen atoms;

R⁶ and R⁷ are hydrogen atoms;

R⁸ is a group having the formula —

X^2cR^10c [wherein R^10c represents a group having the formula —

COR^11c (wherein R^11c represents a hydroxyl group or a methoxy group), or

a group having the formula —

SO₂R^12c (wherein R^12c represents a methyl group), and

X^2c represents a single bond, a methylene group or a substituted methylene group (wherein said substituent is a group selected from Substituent group γ

3, or two of said substituents may together form an ethylene group)];

X¹ is a group having the formula —

O—

;

Y¹ is a phenyl group (wherein the substitution positions where X¹ and Y² are bonded to said phenyl group are the 1 and 4 positions, respectively) or a pyridyl group (wherein the substitution positions where X¹ and Y² are bonded to said pyridyl group are the 5 and 2 positions, respectively); and

,

Y² is a phenyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 3 positions or the 1 and 4 positions, respectively), a substituted phenyl group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group β

2, and the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 3 positions or the 1 and 4 positions, respectively), a thienyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said thienyl group are the 2 and 5 positions, respectively), a substituted thienyl group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group β

2, and the substitution positions where Y¹ and R⁸ are bonded to said thienyl group are the 2 and 5 positions, respectively), a thiazolyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said thiazolyl group are the 2 and 5 positions, respectively), a substituted thiazolyl group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group β

2, and the substitution positions where Y¹ and R⁸ are bonded to said thiazolyl group are the 2 and 5 positions, respectively), a pyridyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said pyridyl group are the 2 and 5 positions or the 3 and 5 positions, respectively) or a substituted pyridyl group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group β

2, and the substitution positions where Y¹ and R⁸ are bonded to said pyridyl group are the 2 and 5 positions or the 3 and 5 positions, respectively).

41. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein

R¹ is a group having the formula —

COR^9d (wherein R^9d represents a 2-methyl-2-propoxy group);

R² is a hydroxyl group;

R³ is a 2-propyl group, a 2-methyl-2-propyl group, a trifluoromethyl group or a chloro group;

R⁴ and R⁵ are hydrogen atoms;

R⁶ and R⁷ are hydrogen atoms;

R⁸ is a group having the formula —

X^2dR^10d [wherein R^10d represents a group having the formula —

COR^11d (wherein R^11d represents a hydroxyl group), and

X^2d is a methylene group or a substituted methylene group (wherein said substituent is a group selected from Substituent group γ

4, or two of said substituents may together form an ethylene group)];

X¹ is a group having the formula —

O—

;

Y¹ is a phenyl group (wherein the substitution positions where X¹ and Y² are bonded to said phenyl group are the 1 and 4 positions, respectively) or a pyridyl group (wherein the substitution positions where X¹ and Y² are bonded to said pyridyl group are the 5 and 2 positions, respectively); and

,

Y² is a phenyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 4 positions, respectively), a substituted phenyl group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group β

3, and the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 4 positions, respectively), a thienyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said thienyl group are the 2 and 5 positions, respectively), a substituted thienyl group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group β

3, and the substitution positions where Y¹ and R⁸ are bonded to said thienyl group are the 2 and 5 positions, respectively), a pyridyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said pyridyl group are the 2 and 5 positions, respectively) or a substituted pyridyl group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group β

3, and the substitution positions where Y¹ and R⁸ are bonded to said pyridyl group are the 2 and 5 positions, respectively).

42. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein

R¹ is a group having the formula —

COR^9d (wherein R^9d represents a 2-methyl-2-propoxy group);

R² is a hydroxyl group;

R³ is a trifluoromethyl group;

R⁴ and R⁵ are hydrogen atoms;

R⁶ and R⁷ are hydrogen atoms;

R⁸ is a group having the formula —

X^2eR^10e [wherein R^10e represents a group having the formula —

COR^11e (wherein R^11e represents a hydroxyl group), and

X^2e represents a methylene group or a substituted methylene group (wherein said substituent is a methyl group)];

X¹ is a group having the formula —

O—

;

Y¹ is a phenyl group (wherein the substitution positions where X¹ and Y² are bonded to said phenyl group are the 1 and 4 positions); and

,

Y² is a phenyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 4 positions, respectively), a substituted phenyl group (wherein said substituents may be the same or different and are a group selected from Substituent group β

3 or two groups selected from Substituent group β

4, and the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 4 positions, respectively), a thienyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said thienyl group are the 2 and 5 positions, respectively), a substituted thienyl group (wherein said substituents may be the same or different and are a group selected from Substituent group β

3 or two groups selected from Substituent group β

4, and the substitution positions where Y¹ and R⁸ are bonded to said thienyl group are the 2 and 5 positions, respectively).

43. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein

R¹ is a group having the formula —

COR^9d (wherein R^9d represents a 2-methyl-2-propoxy group);

R² is a hydroxyl group;

R³ is a trifluoromethyl group;

R⁴ and R⁵ are hydrogen atoms;

R⁶ and R⁷ are hydrogen atoms;

R⁸ is a group having the formula —

X^2eR^10e [wherein R^10e represents a group having the formula —

COR^11e (wherein R^11e represents a hydroxyl group), and

X^2e represents a methylene group or a substituted methylene group (wherein said substituent is a methyl group)];

X¹ is a group having the formula —

O—

;

Y¹ is a phenyl group (wherein the substitution positions where X¹ and Y² are bonded to said phenyl group are the 1 and 4 positions); and

,

Y² is a phenyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 4 positions, respectively) or a substituted phenyl group (wherein said substituent is a group selected from Substituent group β

5, two methyl groups or two fluoro groups, and the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 4 positions, respectively).

44. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein

R¹ is a group having the formula —

COR^9d (wherein R^9d represents a 2-methyl-2-propoxy group);

R² is a hydroxyl group;

R³ is a trifluoromethyl group;

R⁴ and R⁵ are hydrogen atoms;

R⁶ and R⁷ are hydrogen atoms;

R⁸ is a group having the formula —

X^2eR^10e [wherein R^10e represents a group having the formula —

COR^11e (wherein R^11e represents a hydroxyl group), and

X^2e represents a methylene group or a substituted methylene group (wherein said substituent is a methyl group)];

X¹ is a group having the formula —

O—

;

Y¹ is a phenyl group (wherein the substitution positions where X¹ and Y² are bonded to said phenyl group are the 1 and 4 positions); and

,

Y² is a phenyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 3 positions, respectively), a substituted phenyl group (wherein said substituent is a group selected from Substituent group β

6, and the substitution positions where Y¹, R⁸ and the substituent are bonded to said phenyl group are the 1, 3 and 2 positions, respectively), a pyridyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said pyridyl group are the 3 and 5 positions, respectively) or a substituted pyridyl group (wherein said substituent is a group selected from Substituent group β

6, and the substitution positions where Y¹, R⁸ and the substituent are bonded to said pyridyl group are the 3, 5 and 4 positions, respectively).

45. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein

R¹ is a group having the formula —

COR^9d (wherein R^9d represents a 2-methyl-2-propoxy group);

R² is a hydroxyl group;

R³ is a trifluoromethyl group;

R⁴ and R⁵ are hydrogen atoms;

R⁶ and R⁷ are hydrogen atoms;

R⁸ is a group having the formula —

X^2eR^10e [wherein R^10e represents a group having the formula —

COR^11e (wherein R^11e represents a hydroxyl group), and

X^2e represents a methylene group or a substituted methylene group (wherein said substituent is a methyl group)];

X¹ is a group having the formula —

O—

;

Y¹ is a phenyl group (wherein the substitution positions where X¹ and Y² are bonded to said phenyl group are the 1 and 4 positions); and

,

Y² is a phenyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 3 positions, respectively) or a substituted phenyl group (wherein said substituent is a group selected from Substituent group β

7, and the substitution positions where Y¹, R⁸ and the substituent are bonded to said phenyl group are the 1, 3 and 2 positions, respectively).

46. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein

R¹ is a group having the formula —

COR^9d (wherein R^9d represents a 2-methyl-2-propoxy group);

R² is a hydroxyl group;

R³ is a trifluoromethyl group;

R⁴ and R⁵ are hydrogen atoms;

R⁶ and R⁷ are hydrogen atoms;

R⁸ is a group having the formula —

X^2fR^10f [wherein R^10f represents a group having the formula —

SO₂R^12f (wherein R^12f represents a methyl group), and

X^2f represents a single bond];

X¹ is a group having the formula —

O—

;

Y¹ is a phenyl group (wherein the substitution positions where X¹ and Y² are bonded to said phenyl group are the 1 and 4 positions); and

,

Y² is a phenyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 3 positions, respectively), a substituted phenyl group (wherein said substituent is a group selected from Substituent group β

6, and the substitution positions where Y¹, R⁸ and the substituent are bonded to said phenyl group are the 1, 3 and 2 positions, respectively), a pyridyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said pyridyl group are the 3 and 5 positions, respectively) or a substituted pyridyl group (wherein said substituent is a group selected from Substituent group β

6, and the substitution positions where Y¹, R⁸ and the substituent are bonded to said pyridyl group are the 3, 5 and 4 positions, respectively).

47. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein

R¹ is a group having the formula —

COR^9d (wherein R^9d represents a 2-methyl-2-propoxy group);

R² is a hydroxyl group;

R³ is a trifluoromethyl group;

R⁴ and R⁵ are hydrogen atoms;

R⁶ and R⁷ are hydrogen atoms;

R⁸ is a group having the formula —

X^2fR^10f [wherein R^10f represents a group having the formula —

SO₂R^12f (wherein R^12f represents a methyl group), and

X^2f represents a single bond];

X¹ is a group having the formula —

O—

;

Y¹ is a phenyl group (wherein the substitution positions where X¹ and Y² are bonded to said phenyl group are the 1 and 4 positions); and

,

Y² is a phenyl group (wherein the substitution positions where Y¹ and R⁸ are bonded to said phenyl group are the 1 and 3 positions, respectively) or a substituted phenyl group (wherein said substituent is a group selected from Substituent group β

7, and the substitution positions where Y¹, R⁸ and the substituent are bonded to said phenyl group are the 1, 3 and 2 positions, respectively).

48. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1 selected from the group consisting of

(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-1,1′

-biphenyl-4-yl)acetic acid,

2-(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-1,1′

-biphenyl-4-yl)propanoic acid,

1-(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-1,1′

-biphenyl-4-yl)cyclopropanecarboxylic acid,

2-(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-1,1′

-biphenyl-4-yl)-3-hydroxypropanoic acid,

2-[4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-1,1′

-biphenyl-4-yl]butanoic acid,

(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-2-methyl-1,1′

-biphenyl-3-yl)acetic acid,

(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-2-methyl-1,1′

-biphenyl-4-yl)acetic acid,

(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-2-chloro-1,1′

-biphenyl-4-yl)acetic acid,

(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-3-fluoro-1,1′

-biphenyl-4-yl)acetic acid,

(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-3-chloro-1,1′

-biphenyl-4-yl)acetic acid,

2-(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-2-methoxy-1,1′

-biphenyl-3-yl)propanoic acid,

2-(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-3-fluoro-1,1′

-biphenyl-4-yl)propanoic acid,

1-(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-3-fluoro-1,1′

-biphenyl-4-yl)cyclopropanecarboxylic acid,

(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-3-methoxy-1,1′

-biphenyl-4-yl)acetic acid,

(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-2-trifluoromethyl-1,1′

-biphenyl-4-yl)acetic acid,

(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-2-ethyl-1,1′

-biphenyl-4-yl)acetic acid,

tert-butyl 6-[({2′

-ethyl-4′

-[(methoxycarbonyl)methyl]-1,1′

-biphenyl-4-yl}oxy)methyl]-2-hydroxy-3-(trifluoromethyl)benzoate,

(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-2-nitro-1,1′

-biphenyl-4-yl)acetic acid,

(2-amino-4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-1,1′

-biphenyl-4-yl)acetic acid,

(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-2-isopropyl-1,1′

-biphenyl-4-yl)acetic acid,

(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-2-formyl-1,1′

-biphenyl-4-yl)acetic acid,

(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-2-(hydroxymethyl)-1,1′

-biphenyl-4-yl)acetic acid,

(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-2-cyano-1,1′

-biphenyl-4-yl)acetic acid,

(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-2-cyclopropyl-1,1′

-biphenyl-4-yl)acetic acid,

(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-3-ethyl-1,1′

-biphenyl-4-yl)acetic acid,

(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-2-ethyl-1,1′

-biphenyl-3-yl)acetic acid,

2-(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-3-fluoro-1,1′

-biphenyl-4-yl)-3-(dimethylamino)propanoic acid,

2-(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-2-ethyl-1,1′

-biphenyl-4-yl)propanoic acid,

[5-(4-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}phenyl)-4-methyl-2-thienyl]acetic acid,

2-(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-2-nitro-1,1′

-biphenyl-4-yl)propanoic acid,

2-[4-(5-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-2-pyridinyl)-3-methylphenyl]propanoic acid,

2-(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-2-isopropyl-1,1′

-biphenyl-4-yl)propanoic acid,

2-(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-2,3-dimethyl-1,1′

-biphenyl-4-yl)propanoic acid, and

2-(4′

-{[2-(tert-butoxycarbonyl)-3-hydroxy-4-(trifluoromethyl)benzyl]oxy}-2-cyclopropyl-1,1′

-biphenyl-4-yl)propanoic acid.

49. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R¹¹ in the group having the formula —

COR¹¹ represented in R¹⁰ of the group having the formula —

X²R¹⁰ in R⁸ is a hydroxyl group, a C₁-C₆ alkoxy group, a (C₃-C₈ cycloalkyl)-(C₁-C₆ alkyl)oxy group, a C₃-C₈ cycloalkyloxy group, an amino group, a C₁-C₆ alkylamino group, a [(C₃-C₈ cycloalkyl)-(C₁-C₆ alkyl)]amino group, a C₃-C₈ cycloalkylamino group, a di(C₁-C₆ alkyl)amino group (wherein said alkyl groups may be the same or different and two of said alkyl groups may, together with the nitrogen atom of said amino group, form a 5- to 7-membered saturated heterocyclyl group containing 1 to 3 atoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom), a di[(C₃-C₈ cycloalkyl)-(C₁-C₆ alkyl)]amino group, a di(C₃-C₈ cycloalkyl)amino group, a N—

[(C₃-C₈ cycloalkyl)-(C₁-C₆ alkyl)]-N—

(C₁-C₆ alkyl)amino group, a N—

(C₃-C₈ cycloalkyl)-N—

(C₁-C₆ alkyl)amino group, a N—

[(C₃-C₈ cycloalkyl)-(C₁-C₆ alkyl)]-N—

(C₃-C₈ cycloalkyl)amino group, a hydroxylamino group or a hydroxyl(C₁-C₆ alkyl)amino group, and

X² in the group having the formula —

X²R¹⁰ in R⁸ is a single bond, a C₁-C₄ alkylene group or a substituted C₁-C₄ alkylene group (wherein said substituents may be the same or different and are one or two groups selected from Substituent group γ

, or two of said substituents may together form an ethylene group or a trimethylene group).

50. A compound or a pharmacologically acceptable salt or ester thereof according to claim 1, wherein R⁸ is a group having the formula —

X^2gR^10g [wherein R^10g represents a group having the formula —

COR^11g [wherein R^11g represents a hydroxyl group, a C₁-C₆ alkoxy group, an amino group, a C₁-C₆ alkylamino group or a di(C₁-C₆ alkyl)amino group (wherein said alkyl groups may be the same or different and two of said alkyl groups may, together with the nitrogen atom of said amino group, form a 5- to 7-membered saturated heterocyclyl group containing 1 to 3 atoms selected from the group consisting of a nitrogen atom, an oxygen atom and a sulfur atom)], or a tetrazol-5-yl group, and

X^2g represents a single bond, a C₁-C₄ alkylene group or a substituted C₁-C₄ alkylene group (wherein said substituents may be the same or different and are one or two groups selected from a group consisting of a C₁-C₄ alkyl group and a halogeno group, and two of said substituents may together form a methylene group or a trimethylene group)];

Y¹ is a phenyl group, a substituted phenyl group (wherein said substituents may be the same or different and are 1 to 3 groups selected from Substituent group δ

), a 5- or 6-membered aromatic heterocyclyl group or a substituted 5- or 6-membered aromatic heterocyclyl group (wherein said substituents may be the same or different and are 1 to 3 groups selected from Substituent group δ

);

Y² is a phenyl group, a substituted phenyl group (wherein said substituents may be the same or different and are 1 to 3 groups selected from Substituent group δ

), a 5- or 6-membered aromatic heterocyclyl group or a substituted 5- or 6-membered aromatic heterocyclyl group (wherein said substituents may be the same or different and are 1 to 3 groups selected from Substituent group δ

); and

,

Substituent group δ

is the group consisting of a C₁-C₄ alkyl group, a halogeno C₁-C₄ alkyl group (wherein said halogeno C₁-C₄ alkyl group represents a C₁-C₄ alkyl group substituted with 1 to 5 halogeno groups), a hydroxyl group, a C₁-C₄ alkoxy group, a halogeno C₁-C₄ alkoxy group (wherein said halogeno C₁-C₄ alkoxy group represents a C₁-C₄ alkoxy group substituted with 1 to 5 halogeno groups), a C₁-C₄ alkylthio group, a C₁-C₄ alkylsulfinyl group, a C₁-C₄ alkylsulfonyl group, an amino group, a C₁-C₄ alkylamino group, a di(C₁-C₄ alkyl)amino group (wherein said alkyl groups may be the same or different), a carboxyl group, a (C₁-C₄ alkoxy)carbonyl group, a cyano group and a halogeno group.

51. An LXR modulator comprising a compound represented by the general formula (I) or a pharmacologically acceptable salt or ester thereof according to claim 1.

52. An LXR agonist comprising a compound represented by the general formula (I) or a pharmacologically acceptable salt or ester thereof according to claim 1.

53. A pharmaceutical composition comprising as an active ingredient a compound represented by the general formula (I) or a pharmacologically acceptable salt or ester thereof according to claim 1.

54. A pharmaceutical composition according to claim 53 for inducing ABCA1 expression.

55. A pharmaceutical composition according to claim 53 for promoting reverse cholesterol transport.

56. A pharmaceutical composition according to claim 53 for treating or preventing arteriosclerosis, atherosclerosis, arteriosclerosis caused by diabetes, hyperlipemia, hypercholesterolemia, lipid-associated diseases, inflammatory disease, arteriosclerotic heart disease, cardiovascular disease, coronary artery disease or diabetes.

57. A pharmaceutical composition according to claim 53 for treating or preventing arteriosclerosis, atherosclerosis, arteriosclerosis caused by diabetes, arteriosclerotic heart disease, cardiovascular disease or coronary artery disease.

58. A pharmaceutical composition according to claim 53 for treating or preventing arteriosclerosis.

59. A pharmaceutical composition according to claim 53 for treating or preventing arteriosclerotic heart disease.

65. A method for inducing ABCA1 expression by administering an effective amount of a compound represented by the general formula (I) or a pharmacologically acceptable salt or ester thereof according to claim 1 to a warm-blooded animal.

66. A method for promoting reverse cholesterol transport by administering an effective amount of a compound represented by the general formula (I) or a pharmacologically acceptable salt or ester thereof according to claim 1 to a warm-blooded animal.

67. A method for treating or preventing a disease by administering an effective amount of a compound represented by the general formula (I) or a pharmacologically acceptable salt or ester thereof according to claim 1, to a warm-blooded animal.

68. A method according to claim 67, wherein the disease is arteriosclerosis.

69. A method according to claim 67, wherein the disease is arteriosclerotic heart disease.

73. A pharmaceutical composition comprising as an active ingredient a compound represented by the general formula (I) or a pharmacologically acceptable salt or ester thereof according to claim 1;

and one or more pharmaceutical(s) selected from the group consisting of an HMG-CoA reductase inhibitor, CETP inhibitor, ACAT inhibitor, cholesterol absorption inhibitor, bile acid adsorption ion exchange resin, fibrate-based medicine, nicotinic acid derivative, angiotensin II inhibitor and diuretic.

74. A pharmaceutical composition comprising as an active ingredient a compound represented by the general formula (I) or pharmacologically acceptable salt or ester thereof according to claim 1;

and one or more pharmaceutical(s) selected from the group consisting of an HMG-CoA reductase inhibitor, CETP inhibitor and cholesterol absorption inhibitor.

75. A pharmaceutical composition comprising as an active ingredient a compound represented by the general formula (I) or a pharmacologically acceptable salt or ester thereof according to claim 1 and an HMG-CoA reductase inhibitor.

76. A pharmaceutical composition according to claim 75, wherein the HMG-CoA reductase inhibitor is pravastatin, lovastatin, simvastatin, fluvastatin, cerivastatin, atorvastatin, pitavastatin or rosuvastatin.

77. A pharmaceutical composition according to claim 75, wherein the HMG-CoA reductase inhibitor is pravastatin, atorvastatin or rosuvastatin.

78. A method according to claim 65, wherein the warm-blooded animal is a human.

79. A method according to claim 66, wherein the warm-blooded animal is a human.

80. A method according to claim 67, wherein the warm-blooded animal is a human.

81. A method according to claim 67, wherein the disease is arteriosclerosis, atherosclerosis, arteriosclerosis caused by diabetes, hyperlipemia, hypercholesterolemia, lipid-associated diseases, inflammatory disease, arteriosclerotic heart disease, cardiovascular disease, coronary artery disease or diabetes.

82. A method according to claim 67, wherein the disease is arteriosclerosis, atherosclerosis, arteriosclerosis caused by diabetes, arteriosclerotic heart disease, cardiovascular disease or coronary artery disease.

60. (canceled)

61. (canceled)

62. (canceled)

63. (canceled)

64. (canceled)

70. (canceled)

71. (canceled)

72. (canceled)