Benzene compound having 2 or more substituents

• US 7,923,573 B2
• Filed: 10/26/2005
• Issued: 04/12/2011
• Est. Priority Date: 10/27/2004
• Status: Expired due to Fees

• Current Assignee: Daiichi Sankyo Company Limited
• Original Assignee: Daiichi Sankyo Company Limited
• Inventors: Nakai, Daisuke, Tamaki, Kazuhiko, Oda, Kozo, Terasaka, Naoki, Nakadai, Masakazu, Yamaguchi, Takahiro
• Primary Examiner(s): Puttlitz; Karl J
• Application Number:
  US11/577,822
• Publication Number:
  US 20080004301A1
• Time in Patent Office: 1,994 Days
• Field of Search: None
• US Class Current: 560/61
• 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 consisiting 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 consisiting 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 or 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), and

Substituent group α

1 is the group consisiting 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) or 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), 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).

30. 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); 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.

31. 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); 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.

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 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); 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.

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 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); and

,

Substituent group β

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

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 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); 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.

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) 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); and

,

Substituent group β

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

37. 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 or 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); 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).

38. 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 γ

2, 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); 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).

39. 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); 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) or 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).

40. 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); 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 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).

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 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).

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) 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).

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 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).

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) 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).

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^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

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).

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) 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).

47. 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,

2-(4′

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

-biphenyl-4-yl)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.

48. 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 is 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).

49. 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 or a substituted phenyl 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 or a substituted phenyl 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.

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

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

52. 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.

53. A pharmaceutical composition according to claim 52 for inducing ABCA1 expression.

54. A pharmaceutical composition according to claim 52 for promoting reverse cholesterol transport.

55. A pharmaceutical composition according to claim 52 for treating arteriosclerosis, atherosclerosis, arteriosclerosis caused by diabetes, hyperlipemia, hypercholesterolemia, lipid-associated diseases, inflammatory disease, arteriosclerotic heart disease, cardiovascular disease, coronary artery disease or diabetes.

56. A pharmaceutical composition according to claim 52 for treating arteriosclerosis, atherosclerosis, arteriosclerosis caused by diabetes, arteriosclerotic heart disease, cardiovascular disease or coronary artery disease.

57. A pharmaceutical composition according to claim 52 for treating arteriosclerosis.

58. A pharmaceutical composition according to claim 52 for treating arteriosclerotic heart disease.

59. 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.

60. 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.

61. A method for treating arteriosclerosis, atherosclerosis, arteriosclerosis caused by diabetes, hyperlipemia, hypercholesterolemia, lipid-associated diseases, inflammatory disease, arteriosclerotic heart disease, cardiovascular disease, coronary artery disease or diabetes 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.

62. A method according to claim 61, wherein the disease is arteriosclerosis.

63. A method according to claim 61, wherein the disease is arteriosclerotic heart disease.

64. 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.

65. 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.

66. 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.

67. A pharmaceutical composition according to claim 66, wherein the HMG-CoA reductase inhibitor is pravastatin, lovastatin, simvastatin, fluvastatin, cerivastatin, atorvastatin, pitavastatin or rosuvastatin.

68. A pharmaceutical composition according to claim 66, wherein the HMG-CoA reductase inhibitor is pravastatin, atorvastatin or rosuvastatin.

69. A method according to claim 59, wherein the warm-blooded animal is a human.

70. A method according to claim 60, wherein the warm-blooded animal is a human.

71. A method according to claim 61, wherein the warm-blooded animal is a human.

72. A method according to claim 61, wherein the disease is arteriosclerosis, atherosclerosis, arteriosclerosis caused by diabetes, arteriosclerotic heart disease, cardiovascular disease or coronary artery disease.

73. A method according to claim 62, wherein the warm-blooded animal is a human.

74. A method according to claim 63, wherein the warm-blooded animal is a human.

75. A method according to claim 72, wherein the warm-blooded animal is a human.