JPH10287634A - Benzene derivatives - Google Patents

Abstract

PROBLEM TO BE SOLVED: To provide benzene derivatives useful for pharmaceuticals. SOLUTION: The compounds are expressed in formula I [R<1> is a 5 to 6 membered unsaturated heterocyclic residue, etc.; R<2> is a group of formula II (m is an integer of 1 to 3; R<8> is H, a halogen, etc.); R<3> is H, a lower alkyl, etc.; R<4> is H, a lower alkyl, etc., R<5> is a lower alkenyl, etc., substituted with lower alkoxy lower alkoxyamino carbonyl, etc.], for example, 2- 4-[2- benzoyl-2-(1,2,4-triazole-1-yl)-1-methylthioethyl]benzoylamino}-benzot hiazole. This compound is obtained, for example, by carrying out a reaction of the compound of formula III and IV at least in same mole, in the presence or absence of a basic compound (sodium metal, etc.), in a proper solvent (water, etc.), normally at -80 to 150 deg.C for 0.5-50 hours. This compound is administered to be a daily dose of 0.6 to 50 mg/kg.

Description

DETAILED DESCRIPTION OF THE INVENTION

[0001]

TECHNICAL FIELD The present invention relates to a novel benzene derivative.

[0002]

SUMMARY OF THE INVENTION An object of the present invention is to provide a novel benzene derivative useful as a pharmaceutical.

[0003]

Means for Solving the Problems The benzene derivative of the present invention is a novel compound which has not been described in the literature and is represented by the following general formula (1).

[0004]

Embedded image

[Wherein R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (C ₁ -C ₁₂ alkyl group on the hetero ring) A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.); A cyano group; a carboxy group-substituted lower alkyl group; a carboxy group; An alkoxycarbonyl group; a hydrogen atom; a lower alkanoyl group; a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring; a benzoyl group;
⁶ R ⁷ (R ⁶ and R ⁷ are the same or different and represent a hydrogen atom; a lower alkyl group; a cyano-substituted lower alkyl group; or an amino lower alkyl group which may have a lower alkyl group as a substituent. ⁶ and R ⁷ may be bonded together with or without a nitrogen atom or an oxygen atom to form a 5- to 6-membered saturated heterocyclic ring together with a nitrogen atom to which a lower alkyl group is formed. May be substituted).

R ² is a group

[0007]

Embedded image

(M represents an integer of 1 to 3; m R ^{8 s} are the same or different and each is a hydrogen atom; a halogen atom; a cyano group; a carboxy group; a lower alkoxycarbonyl group; a lower alkoxy lower alkoxy group; An amino group which may have a group selected from the group consisting of a lower alkanoyl group, a lower alkyl group and an amino lower alkyl group which may have a lower alkyl group as a substituent; a nitro group;
Amino lower alkoxy group which may have a lower alkyl group as a substituent; lower alkoxy group; lower alkenyloxy group; hydroxyl group; lower alkanoyloxy group; lower alkoxycarbonyl lower alkoxy group; carboxy lower alkoxy group; lower alkoxy lower alkoxycarbonyl group An aminocarbonyl group which may have a lower alkyl group as a substituent; an amino lower alkyl group which may have a lower alkyl group as a substituent; a lower alkoxy lower alkoxy lower alkyl group; a lower alkyl group as a substituent An aminocarbonyl lower alkyl group which may have: a hydroxyl-substituted lower alkyl group;
A hydroxyl-substituted lower alkoxy group; a 1,3-dioxolanyl lower alkoxy group which may have a lower alkyl group as a substituent; an oxiranyl lower alkoxy group or a group -O
-A-NR ⁹ R ¹⁰ (A is .R ⁹ and R ¹⁰ represents a lower alkylene group which may have a hydroxyl group as a substituent are the same or different and represent a hydrogen atom or a lower alkyl group. Further, R ⁹ and R ¹⁰ may be bonded to each other via a nitrogen atom or an oxygen atom with or without a bonding nitrogen atom to form a 5- to 6-membered saturated heterocyclic ring.)); A lower alkyl group and an oxo group as substituents A 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group consisting of; a pyridylcarbonyl group; a lower alkanoyl group which may have a hydroxyl group as a substituent;
A cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent; a benzoyloxy lower alkanoyl group which may have a lower alkoxy group as a substituent on a phenyl ring; A thienylcarbonyl group; a carboxy group; a lower alkoxycarbonyl group; a pyrrolidinylcarbonyl group which may have a group selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group as a substituent; An amino lower alkoxycarbonyl group which may have; a piperidinylcarbonyl group which may have a lower alkyl group as a substituent; or a group -CO- (A ₁ ) _p -NR ¹¹ R ¹² (R ¹¹ and R ¹² are the same. Or differently, Atom; a lower alkyl group; a lower alkoxycarbonyl group; a lower alkoxy group as a substituent on the phenyl ring, a phenyl group which may have a group selected from lower alkoxy-lower alkoxy group and a hydroxyl group consisting;
Or a pyridyl group. A ₁ represents a lower alkylene group. p represents 0 or 1. ).

R ³ is a hydrogen atom; a lower alkyl group; a lower alkylthio group; a phenylthio group; a lower alkylthio group having a group selected from the group consisting of a carboxy group as a substituent and an amino group which may have a lower alkyl group as a substituent. A hydroxy-substituted lower alkylthio group; a cycloalkylthio group; a lower alkanoylthio group; or a cyano group.

N represents an integer of 1 to 3. n pieces of R ⁴ are the same or different, a hydrogen atom; a lower alkyl group; a lower alkoxy group; a hydroxyl group-substituted lower alkyl group; or a group -A ₂ -
NR ¹³ R ¹⁴ (A ₂ represents a lower alkylene group or a lower alkylenyloxy group. R ¹³ and R ¹⁴ may be the same or different and are a hydrogen atom; a lower alkyl group; and may have a lower alkyl group as a substituent. And R ¹³ and R ¹⁴ are bonded to each other via a nitrogen atom or an oxygen atom with or without a nitrogen atom to bond to form a 5- to 7-membered saturated heterocyclic ring. The heterocyclic ring may be a lower alkyl group or a group-(A ₃ ) _q NR ¹⁵ R ¹⁶ (A ₃ represents a lower alkylene group. R ¹⁵ and R ¹⁶ may be the same or different and are each a hydrogen atom; lower alkyl group;. shows a or a phenyl group also form a 5- to 6-membered saturated heterocyclic ring bonded to each other without R ¹⁵ and R ¹⁶ which directly or via a nitrogen atom or oxygen atom together with the nitrogen atom bonded And lower alkyl groups also may. Heterocycle with which may be substituted .q may have a group selected from.) The group consisting represents 0 or 1.) Shows a.

R ⁵ is lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl; hydroxyl-substituted aminocarbonyl-substituted lower alkenyl; pyridyl-substituted aminocarbonyl-substituted lower alkenyl; pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl; phenylthioureidocarbonyl; Pyridylthioureidocarbonyl group; lower alkylthioureidocarbonyl group; pyrimidylaminocarbonyl lower alkoxy group; pyridylaminocarbonyl lower alkoxy group; pyridylaminocarbonyl lower alkoxy group;

[0012]

Embedded image

[0013] (A ₄ is a lower alkylene group which may have a hydroxyl group as a substituent; a lower alkenylene group; or a group -Z-A ₅ - (Z is oxygen atom or the group -NR ²¹ - (R ²¹ is a hydrogen atom or A ₅ represents a lower alkylene group.) R represents 0 or 1. R ¹⁷ and R ¹⁸ represent a hydrogen atom, a lower alkyl group or a phenyl group. ¹⁹ represents a hydrogen atom or a lower alkyl group, and R ¹⁷ and R ¹⁸ together form a group

[0014]

Embedded image

May be formed. Here, R ²⁰ represents a hydrogen atom; a lower alkyl group; a halogen atom; a lower alkoxy group or an amino lower alkyl group which may have a lower alkyl group as a substituent. ); Group-(A ₄ ) _r COOH
(A ₄ and r are the same as above.);

[0016]

Embedded image

(A ₆ represents a lower alkenylene group; R ²⁴
Represents a hydrogen atom or a lower alkoxycarbonyl group. )
Is shown.

Further, R ¹ and R ² together form a group

[0019]

Embedded image

(R ²² represents a hydrogen atom or a 1,2,4-triazolyl lower alkoxy group; R ²³ represents a hydrogen atom or a lower alkyl group).

Side chain

[0022]

Embedded image

In the above, the carbon-carbon bond including the dotted line indicates a single bond or a double bond. The benzene derivative represented by the general formula (1) is a protein kinase C (PKC, C
a ²⁺ / phospholipid-dependent serine / threonine protein kinase)
Useful as inhibitors.

Protein kinase C inhibitors comprising the compound of the present invention as an active ingredient include, for example, autoimmune diseases such as rheumatoid arthritis, systemic lupus erythematosus, psoriasis vulgaris, atopic dermatitis, heart failure, renal failure, liver failure, It is effective in preventing and treating various ischemic diseases such as allergic diseases, collagen diseases, multiple sclerosis, diabetes, cancer, and Alzheimer's dementia.

[0025]

BEST MODE FOR CARRYING OUT THE INVENTION Each group represented by the above general formula (1) is more specifically as follows.

A nitrogen atom, an oxygen atom or a sulfur atom
Examples of the 5- or 6-membered unsaturated heterocyclic residue having a pyridyl group include pyridyl, 1,2,5,6-tetrahydropyridyl,
Furyl, thienyl, pyrrolyl, 2H-pyrrolyl, oxazolyl, isoxazolyl, pyrazolyl, 1,3,4-
Oxadiazolyl, 1,3,4-thiadiazolyl, thiazolyl, isothiazolyl, furazanyl, pyranyl, pyridazinyl, pyrimidinyl, pyrazinyl, imidazolyl,
1,2,4-triazolyl, 1,2,3-triazolyl, 1,3,4-triazolyl, 1,2,3,4-tetrazolyl, 2-pyrolinyl, 2-imidazolinyl, 2-
Pyrazolinyl, 3,4,5,6-tetrahydro-2H-
And pyranyl and 5,6-dihydro-2H-pyranyl groups.

The C ₁ -C ₁₂ alkyl group includes, for example, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, hexyl, heptyl, octyl, nonyl, decyl, undecyl, dodecyl and the like. There may be mentioned 1 to 12 straight-chain or branched alkyl groups.

Examples of the amino lower alkyl group which may have a lower alkyl group as a substituent include, for example, aminomethyl, 2-aminoethyl, 1-aminoethyl, 3-aminopropyl, 4-aminobutyl, 5-aminopentyl,
6-aminohexyl, 1,1-dimethyl-2-aminoethyl, 2-methyl-3-aminopropyl, methylaminomethyl, 1-ethylaminoethyl, 2-propylaminoethyl, 3-isopropylaminopropyl, 4-butyl Aminobutyl, 5-pentylaminopentyl, 6-hexylaminohexyl, dimethylaminomethyl, 2-diethylaminoethyl, 2-dimethylaminoethyl, (N-
It has one or two straight or branched alkyl groups having 1 to 6 carbon atoms as substituents such as ethyl-N-propylamino) methyl and 2- (N-methyl-N-hexylamino) ethyl. A linear or branched alkyl group having 1 to 6 carbon atoms and having an amino group.

Examples of the cycloalkyl group include those having 3 carbon atoms such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl groups.
To 8 cycloalkyl groups.

Examples of the heterocyclic ring substituted with a C ₁ -C ₁₂ alkyl group, an amino lower alkyl group which may have a lower alkyl group as a substituent and a cycloalkyl group include, for example, 1-methyl- 1,2,3,4
-Tetrazolyl, 1-cyclohexyl-1,2,3,4
-Tetrazolyl, 2-undecylimidazolyl, 2-dodecylimidazolyl, 1-ethyl-1,2,3,4-tetrazolyl, 1-methylimidazolyl, 1-n-butyl-1,2,3,4-tetrazolyl, -N-propyl-
1,2,3,4-tetrazolyl, 1- (2-diethylaminoethyl) -1,2,3,4-tetrazolyl, 2-methylpyridyl, 4-cyclopentyl-1,2,5,6-
Tetrahydropyridyl, 3- (3-methylaminopropyl) furyl, 2-ethylthienyl, 3-cyclopropylpyrrolyl, 2- (4-ethylaminobutyl) -2H-pyrrolyl, 4-n-propyloxazolyl, -Cyclobutylisoxazolyl, 2- (5-aminopentyl) thiazolyl, 3-tert-butylisothiazolyl, 4-
Cycloheptylfurazanyl, 3- (6-dipropylaminohexyl) pyranyl, 6-pentylpyridazinyl, 2
-Cyclooctylpyrimidinyl, 5- (diethylaminomethyl) pyrazinyl, 2-methyl-1,3,4-oxadiazolyl, 5-cyclohexyl-1,3,4-thiadiazolyl, 2- (2-di-n-butylaminoethyl) Imidazolyl, 4-hexyl-1,2,4-triazolyl, 4-cyclohexyl-1,2,3-triazolyl,
4- (3-dipentylaminopropyl) -2-pyrolinyl, 2-methyl-2-imidazolinyl, 1-methyl-
1,2,4-triazolyl, 3-cyclopropyl-1,
2,4-triazolyl, 5- (2-diethylaminoethyl) -1,2,4-triazolyl, 1- (2-diethylaminoethyl) -1,3,4-triazolyl, 2-methyl-1,3,4- Triazolyl, 5-cyclohexyl-
1,3,4-triazolyl, 2-nonylpyrimidinyl,
3-decylpyrazinyl, 3-octyl-2-pyrazolinyl, 4-cyclohexyl-3,4,5,6-tetrahydro-2H-pyranyl, 4-heptyl-5,6-dihydro-2H-pyranyl, 2,4-dimethylpyridyl , 2,
4,6-trimethylpyridyl, 1- (2-diethylaminoethyl) -3-methyl-1,2,4-triazolyl,
A C ₁ -C ₁₂ alkyl group such as a 4- (2-diethylaminoethyl) -2-methylpyrimidinyl group, having 1 or 2 straight or branched alkyl groups having 1 to 6 carbon atoms as a substituent; The above-mentioned heterocyclic ring in which a group selected from the group consisting of a straight-chain or branched-chain alkyl group having 1 to 6 carbon atoms having an amino and a cycloalkyl group having 3 to 8 carbon atoms is substituted with 1 to 3 groups can be given. .

The carboxy-substituted lower alkyl group includes
For example, carboxymethyl, 2-carboxyethyl, 1-
Alkyl moieties such as carboxyethyl, 3-carboxypropyl, 4-carboxybutyl, 5-carboxypentyl, 6-carboxyhexyl, 1,1-dimethyl-2-carboxyethyl, and 2-methyl-3-carboxypropyl have carbon atoms. Examples thereof include carboxyalkyl groups that are 1 to 6 linear or branched alkyl groups.

The lower alkoxycarbonyl group includes, for example, an alkoxy moiety such as methoxycarbonyl, ethoxycarbonyl, propoxycarbonyl, isopropoxycarbonyl, butoxycarbonyl, tert-butoxycarbonyl, pentyloxycarbonyl, hexyloxycarbonyl group having 1 to 6 carbon atoms. And alkoxycarbonyl groups which are linear or branched alkoxy groups.

Examples of the lower alkanoyl group include linear or branched alkanoyl groups having 1 to 6 carbon atoms such as formyl, acetyl, propionyl, butyryl, isobutyryl, pentanoyl, tert-butylcarbonyl and hexanoyl groups.

The piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring includes, for example, piperidinylcarbonyl, 1-methylpiperidinylcarbonyl, 1-ethylpiperidinylcarbonyl, Methyl-1-ethylpiperidinylcarbonyl,
3-methyl-1-n-propylpiperidinylcarbonyl, 3,4-dimethylpiperidinylcarbonyl, 1-isopropyl-3-methylpiperidinylcarbonyl, 4-
Methyl-1-isopropylpiperidinylcarbonyl,
1,4,5-trimethylpiperidinylcarbonyl, 1-
A linear or branched alkyl group having 1 to 6 carbon atoms as a substituent on a piperidine ring such as tert-butylpiperidinylcarbonyl, 1-pentylpiperidinylcarbonyl, 1-hexylpiperidinylcarbonyl group, etc. And piperidinylcarbonyl groups which may have up to 3 groups.

The lower alkyl group includes, for example, methyl,
Examples thereof include linear or branched alkyl groups having 1 to 6 carbon atoms, such as ethyl, propyl, isopropyl, butyl, isobutyl, tert-butyl, pentyl, and hexyl groups.

Examples of the cyano-substituted lower alkyl group include cyanomethyl, 2-cyanoethyl, 1-cyanoethyl, 3-cyanopropyl, 2,3-dicyanopropyl,
4-cyanobutyl, 5-cyanopentyl, 6-cyanohexyl, 1,1-dimethyl-2-cyanoethyl, 5,
It has 1 to 3 cyano groups such as 5,4-tricyanopentyl, 1-cyanoisopropyl, and 2-methyl-3-cyanopropyl group, and the alkyl portion has a straight or branched chain having 1 to 6 carbon atoms. A cyanoalkyl group which is an alkyl group can be exemplified.

R ⁶ and R ⁷ , R ⁹ and R ¹⁰ or R ¹⁵ and R
Examples of the 5- or 6-membered saturated heterocyclic group formed with or without a nitrogen atom or an oxygen atom together with the nitrogen atom to which ¹⁶ is bonded include, for example, pyrrolidinyl, piperidinyl, piperazinyl, morpholino group and the like.

The heterocyclic ring substituted by a lower alkyl group includes, for example, 4-methylpiperazinyl, 3,4-dimethylpiperazinyl, 3-ethylpyrrolidinyl, 2-propylpyrrolidinyl, 1-methylpyrrolidinyl Zinyl, 3,4,5
-Trimethylpiperidinyl, 4-butylpiperidinyl,
3-pentylmorpholino, 4-hexylpiperazinyl,
3-methyl-4-ethylpiperazinyl, 3-methyl-4
-N-propylpiperazinyl, 4-isopropyl-3-
The above-mentioned heterocyclic group in which 1 to 3 straight-chain or branched-chain alkyl groups having 1 to 6 carbon atoms such as methylpiperazinyl and 4-methyl-3-isopropylpiperazinyl group are substituted.

Examples of the halogen atom include a fluorine atom,
Examples include a chlorine atom, a bromine atom and an iodine atom.

The lower alkoxy group includes, for example, methoxymethoxy, 3-methoxypropoxy, ethoxymethoxy, 3-ethoxypropoxy,
Ethoxybutoxy, 5-isopropoxypentyloxy, 6-propoxyhexyloxy, 1,1-dimethyl-2-butoxyethoxy, 2-methyl-3-tert-
The alkoxy moiety such as butoxypropoxy, 2-pentyloxyethoxy and hexyloxymethoxy has 1 to 1 carbon atoms.
And 6 alkoxyalkoxy groups which are linear or branched alkoxy groups.

Examples of the amino group which may have a group selected from the group consisting of a lower alkanoyl group, a lower alkyl group as a substituent and an amino lower alkyl group which may have a lower alkyl group as a substituent include, for example, amino, formylamino , Acetylamino, propionylamino, butyrylamino, isobutyrylamino, pentanoylamino, tert-butylcarbonylamino, hexanoylamino, methylamino, ethylamino, propylamino, isopropylamino, butylamino, tert-butylamino, pentylamino , Hexylamino, dimethylamino, diethylamino, dipropylamino, dibutylamino, dipentylamino, dihexylamino, N-
Methyl-N-ethylamino, N-ethyl-N-propylamino, N-methyl-N-butylamino, N-methyl-
N-hexylamino, N-acetyl-N-methylamino, N-butyl-N-acetylamino, (2-dimethylaminoethyl) amino, (5-aminopentyl) amino, (3-isopropylaminopropyl) amino, N −
Methyl-N- (2-dimethylaminoethyl) amino, N
-Acetyl-N- (N-ethyl-N-propylamino)
A straight-chain or branched alkanoyl group having 1 to 6 carbon atoms as a substituent such as a methylamino group, a straight-chain or branched alkyl group having 1 to 6 carbon atoms and a straight-chain or branched alkyl group having 1 to 6 carbon atoms as a substituent. Having 1 or 2 groups selected from the group consisting of linear or branched alkyl groups having 1 to 6 carbon atoms and having an amino group which may have 1 to 2 chain or branched alkyl groups; Certain amino groups can be mentioned.

Examples of the amino lower alkoxy group which may have a lower alkyl group as a substituent include, for example, aminomethoxy, 2-aminoethoxy, 1-aminoethoxy,
3-aminopropoxy, 4-aminobutoxy, 5-aminopentyloxy, 6-aminohexyloxy, 1,1
-Dimethyl-2-aminoethoxy, 2-methyl-3-aminopropoxy, methylaminomethoxy, 1-ethylaminoethoxy, 2-propylaminoethoxy, 3-isopropylaminopropoxy, 4-isopropylaminobutoxy, 4-butylaminobutoxy 4-tert-butylaminobutoxy, 5-pentylaminopentyloxy, 6-hexylaminohexyloxy, dimethylaminomethoxy, 2-diethylaminoethoxy, 2-dimethylaminoethoxy, (N-ethyl-N-propylamino) methoxy, C1-C1 having an amino group which may have 1-2 C1-C6 linear or branched alkyl groups as a substituent such as 2- (N-methyl-N-hexylamino) ethoxy group or the like; To 6 linear or branched alkoxy groups. That.

Examples of the lower alkoxy group include straight-chain or branched-chain alkoxy groups having 1 to 6 carbon atoms such as methoxy, ethoxy, propoxy, isopropoxy, butoxy, tert-butoxy, pentyloxy and hexyloxy groups. be able to.

The lower alkenyloxy group includes, for example, vinyloxy, allyloxy, 2-butenyloxy, 3
Examples thereof include linear or branched alkenyloxy groups having 2 to 6 carbon atoms, such as -butenyloxy, 1-methylallyloxy, 2-pentenyloxy, 2-hexenyloxy, and 1-propenyloxy.

The lower alkanoyloxy group includes, for example, acetyloxy, propionyloxy, butyryloxy, isobutyryloxy, pentanoyloxy,
A straight-chain or branched alkanoyloxy group having 2 to 6 carbon atoms such as t-butylcarbonyloxy and hexanoyloxy groups can be exemplified.

The lower alkoxycarbonyl group includes, for example, methoxycarbonylmethoxy,
Methoxycarbonylpropoxy, ethoxycarbonylmethoxy, 3-ethoxycarbonylpropoxy, 4-ethoxycarbonylbutoxy, 5-isopropoxycarbonylpentyloxy, 6-propoxycarbonylhexyloxy, 1,1-dimethyl-2-butoxycarbonylethoxy, 2-methyl Examples of the alkoxycarbonylalkoxy group in which an alkoxy moiety such as -3-tert-butoxycarbonylpropoxy, 2-pentyloxycarbonylethoxy, hexyloxycarbonylmethoxy group is a linear or branched alkoxy group having 1 to 6 carbon atoms. Can be.

The carboxy lower alkoxy group includes
For example, carboxymethoxy, 2-carboxyethoxy,
1-carboxyethoxy, 3-carboxypropoxy,
Alkoxy moieties such as 4-carboxybutoxy, 5-carboxypentyloxy, 6-carboxyhexyloxy, 1,1-dimethyl-2-carboxyethoxy, and 2-methyl-3-carboxypropoxy groups are straight-chain having 1 to 6 carbon atoms. Or a carboxyalkoxy group which is a branched alkoxy group.

The lower alkoxy lower alkoxycarbonyl group includes, for example, methoxymethoxycarbonyl,
Methoxypropoxycarbonyl, ethoxymethoxycarbonyl, 3-ethoxypropoxycarbonyl, 4-ethoxybutoxycarbonyl, 5-isopropoxypentyloxycarbonyl, 6-propoxyhexyloxycarbonyl, 1,1-dimethyl-2-butoxyethoxycarbonyl, 2-methyl Examples of alkoxyalkoxycarbonyl groups in which the alkoxy moiety such as -3-tert-butoxypropoxycarbonyl, 2-pentyloxyethoxycarbonyl, hexyloxymethoxycarbonyl group is a linear or branched alkoxy group having 1 to 6 carbon atoms. Can be.

Examples of the aminocarbonyl group which may have a lower alkyl group as a substituent include, for example, aminocarbonyl, methylaminocarbonyl, ethylaminocarbonyl, propylaminocarbonyl, isopropylaminocarbonyl, butylaminocarbonyl, pentylaminocarbonyl, hexylamino A straight-chain or branched-chain alkyl group having 1 to 6 carbon atoms as a substituent such as carbonyl, dimethylaminocarbonyl, (N-ethyl-N-propylamino) carbonyl, or (N-methyl-N-hexylamino) carbonyl; And an aminocarbonyl group which may have 1 to 2 groups.

The lower alkoxy lower alkoxy lower alkyl group includes, for example, methoxymethoxymethyl,
(3-methoxypropoxy) propyl, ethoxymethoxymethyl, 3- (3-ethoxypropoxy) propyl,
4- (4-ethoxybutoxy) butyl, 5- (5-isopropoxypentyloxy) pentyl, 6- (6-propoxyhexyloxy) hexyl, 1,1-dimethyl-
2- (2-butoxyethoxy) ethyl, 2-methyl-3
-(3-tert-butoxypropoxy) propyl, 2
An alkoxy moiety such as-(2-pentyloxyethoxy) ethyl or hexyloxymethoxymethyl group has 1 to 1 carbon atoms;
A straight-chain or branched-chain alkyl group having 1 to 6 carbon atoms having an alkoxyalkoxy that is a straight-chain or branched-chain alkoxy group of 6 can be mentioned.

Examples of the aminocarbonyl lower alkyl group which may have a lower alkyl group as a substituent include, for example, aminocarbonylmethyl, 2-aminocarbonylethyl, 1-aminocarbonylethyl, 3-aminocarbonylpropyl, 4-aminocarbonylbutyl , 5-aminocarbonylpentyl, 6-aminocarbonylhexyl,
1,1-dimethyl-2-aminocarbonylethyl, 2-
Methyl-3-aminocarbonylpropyl, methylaminocarbonylmethyl, 1-ethylaminocarbonylethyl, 2-propylaminocarbonylethyl, 3-isopropylaminocarbonylpropyl, 4-butylaminocarbonylbutyl, 5-pentylaminocarbonylpentyl, 6- Straight chain having 1 to 6 carbon atoms as a substituent such as hexylaminocarbonylhexyl, dimethylaminocarbonylmethyl, (N-ethyl-N-propylamino) carbonylmethyl, 2- (N-methyl-N-hexylamino) carbonylethyl or the like; Alternatively, a linear or branched alkyl group having 1 to 6 carbon atoms in an alkyl moiety having an aminocarbonyl group which may have 1 to 2 branched alkyl groups can be mentioned.

Examples of the hydroxy-substituted lower alkyl group include hydroxymethyl, 2-hydroxyethyl, 1-hydroxyethyl, 3-hydroxypropyl, 2,3-dihydroxypropyl, 4-hydroxybutyl and 1,1-dimethyl-2- C1-C1 having 1 to 3 hydroxyl groups such as hydroxyethyl, 5,5,4-trihydroxypentyl, 5-hydroxypentyl, 6-hydroxyhexyl, 1-hydroxyisopropyl, 2-methyl-3-hydroxypropyl group. And 6 straight-chain or branched alkyl groups.

Examples of the hydroxy-substituted lower alkoxy group include hydroxymethoxy, 2-hydroxyethoxy,
-Hydroxyethoxy, 3-hydroxypropoxy,
2,3-dihydroxypropoxy, 4-hydroxybutoxy, 1,1-dimethyl-2-hydroxyethoxy,
5,5,4-trihydroxypentyloxy, 5-hydroxypentyloxy, 6-hydroxyhexyloxy, 1-hydroxyisopropoxy, 2-methyl-3-
Examples thereof include a linear or branched alkoxy group having 1 to 6 carbon atoms, which may have 1 to 3 hydroxyl groups such as a hydroxypropoxy group.

1, having a lower alkyl group as a substituent
Examples of the 3-dioxolanyl lower alkoxy group include (1,3-dioxolanyl) methoxy, (2,2-dimethyl-1,3-dioxolanyl) methoxy, 2- (1,
3-dioxolanyl) ethoxy, 3- (1,3-dioxolanyl) propoxy, 4- (1,3-dioxolanyl) butoxy, 5- (1,3-dioxolanyl) pentyloxy, 6- (1,3-dioxolanyl) hexyl Oxy, 1,1-dimethyl-2- (1,3-dioxolanyl) ethoxy, 2-methyl-3- (1,3-dioxolanyl) propoxy, (2-methyl-1,3-dioxolanyl) methoxy, (2 4-dimethyl-1,3-dioxolanyl) methoxy, (2,2,4-trimethyl-1,
3-dioxolanyl) methoxy, 2- (2-ethyl-
As a substituent such as 1,3-dioxolanyl) ethoxy or 3- (2-hexyl-1,3-dioxolanyl) propoxy group, it has 1 to 3 straight or branched alkyl groups having 1 to 6 carbon atoms. The alkoxy moiety may have 1 carbon atom
And 1,3-dioxolanylalkoxy groups, which are straight-chain or branched-chain alkoxy groups of 1 to 6.

The oxiranyl lower alkoxy group includes
For example, oxiranylmethoxy, 2-oxiranylethoxy, 1-oxiranylethoxy, 3-oxiranylpropoxy, 4-oxiranylbutoxy, 5-oxiranylpentyloxy, 6-oxiranylhexyloxy,
Examples thereof include linear or branched alkoxy groups having 1 to 6 carbon atoms and having an oxiranyl group such as 1,1-dimethyl-2-oxiranylethoxy and 2-methyl-3-oxiranylpropoxy groups. it can.

Examples of the lower alkylene group include methylene, ethylene, trimethylene, 2-methyltrimethylene, 2,2-dimethyltrimethylene, 1-methyltrimethylene, methylmethylene, ethylmethylene, tetramethylene, pentamethylene, hexamethylene C1 of group etc.
To 6 linear or branched alkylene groups.

The lower alkylene group which may have a hydroxyl group as a substituent includes, for example, 1-hydroxymethylene, 1-hydroxyethylene, 1,2-dihydroxyethylene, 2-hydroxytrimethylene, , 3-dihydroxytrimethylene, 1
-Hydroxy-2-methyltrimethylene, 1-hydroxy-2,2-dimethyltrimethylene, 1-methyl-2-
A straight or branched chain having 1 to 6 carbon atoms which may have 1 to 2 hydroxyl groups as a substituent such as hydroxytrimethylene, 2-hydroxytetramethylene, 3-hydroxypentamethylene or 4-hydroxyhexamethylene An alkylene group can be mentioned.

1,2,3,3 which may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent.
Examples of the 4-tetrahydroquinolylcarbonyl group include 3,4-dihydro-2-oxoquinolylcarbonyl,
1-methyl-3,4-dihydro-2-oxoquinolylcarbonyl, 1-ethyl-3,4-dihydro-2-oxoquinolylcarbonyl, 8-methyl-3,4-dihydro-
2-oxoquinolylcarbonyl, 8-ethyl-3,4-
Dihydro-2-oxoquinolylcarbonyl, 3-propyl-3,4-dihydro-2-oxoquinolylcarbonyl, 4-butyl-3,4-dihydro-2-oxoquinolylcarbonyl, 5-pentyl-3,4 -Dihydro-2-
Oxoquinolylcarbonyl, 6-hexyl-3,4-dihydro-2-oxoquinolylcarbonyl, 7-methyl-
3,4-dihydro-2-oxoquinolylcarbonyl,
1,8-dimethyl-3,4-dihydro-2-oxoquinolylcarbonyl, 4,6,7-trimethyl-3,4-dihydro-2-oxoquinolylcarbonyl, 1,2,3
4-tetrahydroquinolylcarbonyl, 1-methyl-
1,2,3,4-tetrahydroquinolylcarbonyl, 1
-Ethyl-1,2,3,4-tetrahydroquinolylcarbonyl, 8-methyl-1,2,3,4-tetrahydroquinolylcarbonyl, 8-ethyl-1,2,3,4-tetrahydroquinolylcarbonyl, 3-propyl-1,2,
3,4-tetrahydroquinolylcarbonyl, 4-butyl-1,2,3,4-tetrahydroquinolylcarbonyl,
5-pentyl-1,2,3,4-tetrahydroquinolylcarbonyl, 6-hexyl-1,2,3,4-tetrahydroquinolylcarbonyl, 7-methyl-1,2,3,4
-Tetrahydroquinolylcarbonyl, 1,8-dimethyl-1,2,3,4-tetrahydroquinolylcarbonyl,
As a substituent such as a 4,6,7-trimethyl-1,2,3,4-tetrahydroquinolylcarbonyl group, a group having 1 to 6 carbon atoms
1,2,3,4 which may have 1 to 4 groups selected from the group consisting of linear or branched alkyl groups and oxo groups
-Tetrahydroquinolylcarbonyl group.

The lower alkanoyl group which may have a hydroxyl group as a substituent includes, for example, 2-hydroxyacetyl, 3-hydroxypropanoyl, 2-hydroxypropanoyl,
Hydroxybutyryl, 5-hydroxypentanoyl, 6
-Hydroxyhexanoyl, 2,2-dimethyl-3-hydroxypropanoyl, 2-methyl-3-hydroxypropanoyl, 2,3-dihydroxypropanoyl, 5,
Examples thereof include a linear or branched alkanoyl group having 2 to 6 carbon atoms which may have 1 to 3 hydroxyl groups such as 5,4-trihydroxypentanoyl and 2-hydroxyisobutyryl group.

Examples of the cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent include, for example, cyclopropylcarbonyl, cyclobutylcarbonyl, cyclopentylcarbonyl, cyclohexylcarbonyl,
Cycloheptylcarbonyl, cyclooctylcarbonyl, 4-tert-butoxycarbonylaminomethylcyclohexylcarbonyl, 2- (2-methoxycarbonylaminoethyl) cyclopropylcarbonyl, 2- (1
-Ethoxycarbonylaminoethyl) cyclobutylcarbonyl, 3- (3-propoxycarbonylaminopropyl) cyclopentylcarbonyl, 4- (4-butoxycarbonylaminobutyl) cycloheptylcarbonyl,
-(5-pentyloxycarbonylaminopentyl) cyclooctylcarbonyl, 2- (6-hexyloxycarbonylaminohexyl) cyclohexylcarbonyl,
2,4-di (ethoxycarbonylaminomethyl) cyclohexylcarbonyl, 2,4,6-tri (methoxycarbonylaminomethyl) cyclohexylcarbonyl, 4-
Amino-substituted C1-C6 linear or branched which may have an alkoxycarbonyl group wherein the alkoxy moiety is a C1-C6 linear or branched alkoxy as a substituent such as an aminomethylcyclohexylcarbonyl group. A cycloalkylcarbonyl group in which a cycloalkyl moiety which may have 1 to 3 chain alkyl groups is a cycloalkylcarbonyl group having 3 to 8 carbon atoms can be exemplified.

Examples of the benzoyloxy lower alkanoyl group include 2-benzoyloxyacetyl, 3-benzoyloxypropanoyl, 2-benzoyloxypropanoyl, 4-benzoyloxybutyryl, 5-benzoyloxypentanoyl and 6-benzoyloxy Hexanoyl, 2,2-dimethyl-3-benzoyloxypropanoyl, 2-methyl-3-benzoyloxypropanoyl, 2,3-dibenzoyloxypropanoyl, 5,
A straight or branched alkanoyl group having 2 to 6 carbon atoms which may have 1 to 3 benzoyloxy groups such as 5,4-tribenzoyloxypentanoyl and 2-benzoyloxyisobutyryl groups. Can be.

The phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring includes, for example, phenoxycarbonyl, 4-methoxyphenoxycarbonyl, 3-methoxyphenoxycarbonyl,
2-methoxyphenoxycarbonyl, 3-ethoxyphenoxycarbonyl, 4-propoxyphenoxycarbonyl, 2-butoxyphenoxycarbonyl, 3-pentyloxyphenoxycarbonyl, 4-hexyloxyphenoxycarbonyl, 2,4-dimethoxyphenoxycarbonyl, 3,4 A phenoxycarbonyl group which may have 1 to 3 carbon atoms of a linear or branched alkoxy group having 1 to 6 carbon atoms as a substituent on a phenyl ring such as a 5-trimethoxyphenoxycarbonyl group.

Examples of the pyrrolidinylcarbonyl group which may have a group selected from the group consisting of a lower alkoxycarbonyl group and a phenyl-lower alkoxycarbonyl group as a substituent include, for example, pyridinylcarbonyl, 1-benzyloxycarbonylpyridinyl Carbonyl, 1-ter
t-butoxycarbonylpyridinylcarbonyl, 1-methoxycarbonylpyridinylcarbonyl, 2-ethoxycarbonylpyridinylcarbonyl, 3-pentyloxycarbonylpyridinylcarbonyl, 1-hexyloxycarbonylpyridinylcarbonyl, 2- ( 2-phenylethoxycarbonyl) pyridinylcarbonyl, 4- (3
-Phenylpropoxycarbonyl) pyridinylcarbonyl, 3- (4-phenylbutoxycarbonyl) pyridinylcarbonyl, 1- (5-phenylpentyloxycarbonyl) pyridinylcarbonyl, 1- (6-phenylhexyloxycarbonyl) pyro Dinylcarbonyl, 1,
3-dimethoxycarbonylpyridinylcarbonyl, 1,
2,4-ethoxycarbonylpyridinylcarbonyl, 1
An alkoxycarbonyl group having 1 to 6 carbon atoms as a substituent such as -benzyloxycarbonyl-3-methoxycarbonylpyridinylcarbonyl group, wherein the alkoxy moiety is a linear or branched alkoxy having 1 to 6 carbon atoms;
And a pyrrolidinylcarbonyl group which may have 1 to 3 groups selected from the group consisting of phenylalkoxycarbonyl groups which are straight-chain or branched alkoxy groups.

Examples of the amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent include, for example, aminomethoxycarbonyl, 2-aminoethoxycarbonyl, 1-aminoethoxycarbonyl, 3-aminopropoxycarbonyl, 4-aminobutoxycarbonyl , 5-aminopentyloxycarbonyl, 6-aminohexyloxycarbonyl, 1,1-dimethyl-2-aminoethoxycarbonyl, 2-methyl-3-aminopropoxycarbonyl, methylaminomethoxycarbonyl,
1-ethylaminoethoxycarbonyl, 2-propylaminoethoxycarbonyl, 3-isopropylaminopropoxycarbonyl, 4-butylaminobutoxycarbonyl, 5-pentylaminopentyloxycarbonyl, 6
-Hexylaminohexyloxycarbonyl, dimethylaminomethoxycarbonyl, (N-ethyl-N-propylamino) methoxycarbonyl, 2- (N-methyl-N
-Hexylamino) ethoxycarbonyl group or the like as a substituent having a straight-chain or branched alkyl group having 1 to 6 carbon atoms.
Examples thereof include an alkoxycarbonyl group in which the alkoxy moiety having an amino group which may have two is a straight or branched alkoxy having 1 to 6 carbon atoms.

The phenyl group which may have a substituent selected from the group consisting of a lower alkoxy group, a lower alkoxy lower alkoxy group and a hydroxyl group on the phenyl ring includes, for example, phenyl, 3-methoxymethoxy-4-methoxyphenyl, 3-methoxy-4-hydroxyphenyl, 4-hydroxyphenyl, 3-hydroxyphenyl, 2-hydroxyphenyl, 3,4-dihydroxyphenyl, 2,4,5-trihydroxyphenyl, 2-methoxyphenyl, 3-ethoxyphenyl , 4-propoxyphenyl, 2-butoxyphenyl, 3-pentyloxyphenyl, 4-hexyloxyphenyl, 2,4-dimethoxyphenyl, 3,4,5-trimethoxyphenyl, 3-methoxymethoxyphenyl, 2- (2 -Ethoxyethoxy) phenyl, -(3-propoxypropoxy) phenyl, 2- (4-butoxybutoxy) phenyl, 3- (5-pentyloxypentyloxy) phenyl, 4- (6-hexyloxyhexyloxy) phenyl, 2,3-di (methoxy) Methoxy) phenyl, 3,
A linear or branched alkoxy group having 1 to 6 carbon atoms as a substituent on a phenyl ring such as a 4,5-tri (methoxymethoxy) phenyl group, or a linear or branched alkoxy group having 1 to 6 carbon atoms Examples thereof include a phenyl group which may have 1 to 3 groups selected from the group consisting of an alkoxyalkoxy group which is a chain alkoxy group and a hydroxyl group.

Examples of the lower alkylthio group include linear or branched alkylthio groups having 1 to 6 carbon atoms such as methylthio, ethylthio, propylthio, isopropylthio, butylthio, isobutylthio, tert-butylthio, pentylthio and hexylthio. Can be mentioned.

Examples of the lower alkylthio group having a group selected from the group consisting of a carboxy group as a substituent and an amino group which may have a lower alkyl group as a substituent include, for example, carboxymethylthio, 2- (diethylamino) ethylthio, 2-carboxy Ethylthio, 3-carboxypropylthio, 4-carboxybutylthio, 5-carboxypentylthio, 6-carboxyhexylthio, 1,
1-dimethyl-2-carboxyethylthio, 2-methyl-3-carboxypropylthio, aminomethylthio, 1
-(Methylamino) ethylthio, 4- (ethylamino)
Butylthio, 5- (propylamino) pentylthio, 6
-(Butylamino) hexylthio, 1,1-dimethyl-
2- (pentylamino) ethylthio, 2-methyl-3-
A carboxy group as a substituent such as (hexylamino) propylthio, diethylaminomethylthio, 2- (N-methyl-N-ethylamino) ethylthio, and 3-diethylamino-1-carboxypropylthio group; Examples thereof include a linear or branched alkylthio group having 1 to 6 carbon atoms which may have a group selected from the group consisting of amino groups which may have 1 to 2 linear or branched alkyl groups. it can.

Examples of the hydroxyl-substituted lower alkylthio group include:
For example, hydroxymethylthio, 2-hydroxyethylthio, 1-hydroxyethylthio, 3-hydroxypropylthio, 4-hydroxybutylthio, 5-hydroxypentylthio, 6-hydroxyhexylthio, 1,1-dimethyl-2-hydroxyethyl Thio, 2-methyl-3-
Hydroxypropylthio, 2,3-dihydroxypropylthio, 5,5,4-trihydroxypentylthio, 1
A straight-chain or branched alkylthio group having 1 to 6 carbon atoms, which may have 1 to 3 hydroxyl groups such as -hydroxyisopropylthio group.

Examples of the cycloalkylthio group include cycloalkylthio groups having 3 to 8 carbon atoms, such as cyclopropylthio, cyclobutylthio, cyclopentylthio, cyclohexylthio, cycloheptylthio, and cyclooctylthio groups.

Examples of the lower alkanoylthio group include linear or branched alkanoylthio groups having 2 to 6 carbon atoms such as acetylthio, propionylthio, butyrylthio, pentanoylthio, hexanoylthio, tert-butyrylthio and isobutyrylthio groups. Can be given.

Examples of the lower alkylenyloxy group include methyleneoxy, ethyleneoxy, trimethyleneoxy, 2-methyltrimethyleneoxy, 2,2-dimethyltrimethyleneoxy, 1-methyltrimethyleneoxy,
Examples thereof include linear or branched alkyleneoxy groups having 1 to 6 carbon atoms such as methylmethyleneoxy, ethylmethyleneoxy, tetramethyleneoxy, bentamethyleneoxy, and hexamethyleneoxy groups.

Examples of the pyridyl lower alkyl group include (3-pyridyl) methyl, 2- (2-pyridyl) ethyl, 1- (4-pyridyl) ethyl, 3- (2-pyridyl) propyl and 4- (3- Pyridyl) butyl, 5- (4
-Pyridyl) pentyl, 6- (2-pyridyl) hexyl, 1,1-dimethyl-2- (3-pyridyl) ethyl,
Examples thereof include a linear or branched alkyl group having 1 to 6 carbon atoms and having a pyridyl group such as a 2-methyl-3- (4-pyridyl) propyl group.

Along with the nitrogen atom to which R ¹³ and R ¹⁴ are attached,
Examples of the 5- to 7-membered saturated heterocyclic group formed by bonding to each other via or without a nitrogen atom or an oxygen atom include pyrrolidinyl, piperidinyl, piperazinyl, morpholino, homopiperazinyl and homomorpholino groups.

Lower alkyl group and group-(A ₃ ) _q NR ¹⁵ R
Examples of the heterocyclic ring substituted with a group selected from the group consisting of ¹⁶ include 3-[(4-methyl-1-piperazinyl) methyl] morpholino, 2-[(1-pyrrolidinyl) methyl] pyrrolidinyl, and 2-morpholinomethylpyrrolidone. Dinyl, 4- (4-methyl-1-piperazinyl) piperidinyl, 4-morpholinopiperidinyl, 4- (1-piperidinyl) piperidinyl, 3-[(1-pyrrolidinyl) methyl] morpholino, 2-morpholinomethylmorpholino, 2
-[(4-methyl-1-piperazinyl) methyl] morpholino, 4-dimethylaminopiperidinyl, 4-methylpiperazinyl, 2-[(1-pyrrolidinyl) methyl] morpholino, 3,4-dimethylpiperazinyl , 4-ethylpiperazinyl, 4-methylhomopiperazinyl, 4-dimethylaminopiperidinyl, 4-diethylaminopiperidinyl, 4-n-butylhomopiperazinyl, 4- (2-dimethylaminoethyl) Piperazinyl, 3-methylpiperazinyl, 2-[(N-phenyl-N-methylamino) methyl] pyrrolidinyl, 4- (3-diethylaminopropyl) homopiperazinyl, 3,4,5-trimethylpiperazinyl, 4-isopropyl Piperazinyl, 3,3,4-
Trimethylpiperazinyl, 4,5-dimethylhomopiperazinyl, 3-methyl-4-ethylpiperazinyl, 3-methyl-4-n-propylpiperazinyl, 3-n-propyl-4-methylpiperazinyl , 3-methyl-4-isopropylpiperazinyl, 3-ethyl-4-methylpiperazinyl, 3-methyl-4- (2-diethylaminoethyl)
Piperazinyl, 3-isopropyl-4-methylpiperazinyl, 4-[(N-phenyl-N-ethyl) amino] piperidinyl, 4- (3,4,5-trimethyl-1-piperazinyl) morpholino, 4- (3 -Ethyl-4-methyl-1-piperazinyl) piperidinyl, a linear or branched alkyl group having 1 to 6 carbon atoms such as a 3-diethylaminomorpholino group and a group-(A ₃ ) _q NR ¹⁵ R ¹⁶ (q is Represents 0 or 1. A ₃ represents a linear or branched alkylene group having 1 to 6 carbon atoms, and R ¹⁵ and R ¹⁶ may be the same or different and represent a hydrogen atom, a linear or branched alkyl group having 1 to 6 carbon atoms. And a branched alkyl group or a phenyl group, and R ¹⁵ and R ¹⁶ may form a 5- to 6-membered saturated heterocyclic ring with or without a nitrogen atom to be bonded. The heterocyclic ring may have a substituent. 1 to 6 carbon atoms may be substituted with 1 to 3 linear or branched alkyl groups.) The above heterocyclic group having 1 to 3 groups selected from the group .

The lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group includes, for example, 2-alkoxy
(1,1-dimethyl-1-methoxymethoxyaminocarbonyl) vinyl, 2- (methoxymethoxyaminocarbonyl) vinyl, 3-[(3-methoxypropoxy) aminocarbonyl] allyl, 4- (ethoxymethoxyaminocarbonyl) -3 -Methyl-1-butenyl, 4-[(3
-Ethoxypropoxy) aminocarbonyl] -2-butenyl, 4-[(4-ethoxybutoxy) aminocarbonyl] -3-butenyl, 3-[(5-isopropoxypentyloxy) aminocarbonyl] -1-methylallyl,
5-[(6-propoxyhexyloxy) aminocarbonyl] -2-pentenyl, 6-[(1,1-dimethyl-
2-butoxyethoxy) aminocarbonyl] -2-hexenyl, 3-[(2-methyl-3-tert-butoxypropoxy) aminocarbonyl] -1-propenyl, 2
-[(2-pentyloxyethoxy) aminocarbonyl] alkoxyalkoxy wherein the alkoxy moiety such as vinyl or 3- (hexyloxymethoxyaminocarbonyl) allyl group is a linear or branched alkoxy group having 1 to 6 carbon atoms A straight-chain or branched alkenyl group having 2 to 6 carbon atoms having an aminocarbonyl group can be exemplified.

Examples of the hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group include 2- (hydroxyaminocarbonyl) vinyl and 3- (hydroxyaminocarbonyl)
Allyl, 4- (hydroxyaminocarbonyl) -3-methyl-1-butenyl, 4- (hydroxyaminocarbonyl) -2-butenyl, 4- (hydroxyaminocarbonyl) -3-butenyl, 3- (hydroxyaminocarbonyl)- Carbon having a hydroxyl-substituted aminocarbonyl group such as 1-methylallyl, 5- (hydroxyaminocarbonyl) -2-pentenyl, 6- (hydroxyaminocarbonyl) -2-hexenyl, 3- (hydroxyaminocarbonyl) -1-propenyl group Examples include straight-chain or branched alkenyl groups of the formulas 2 to 6.

Examples of the pyridyl-substituted aminocarbonyl-substituted lower alkenyl group include 2-[(2-pyridyl) aminocarbonyl] vinyl, 3-[(3-pyridyl) aminocarbonyl] allyl and 4-[(4-pyridyl) amino Carbonyl] -3-methyl-1-butenyl, 4-[(2
-Pyridyl) aminocarbonyl] -2-butenyl, 4-
[(3-pyridyl) aminocarbonyl] -3-butenyl, 3-[(4-pyridyl) aminocarbonyl] -1-
Methylallyl, 5-[(2-pyridyl) aminocarbonyl] -2-pentenyl, 6-[(3-pyridyl) aminocarbonyl] -2-hexenyl, 3-[(4-pyridyl) aminocarbonyl] -1-propenyl Examples thereof include a linear or branched alkenyl group having 2 to 6 carbon atoms having a pyridyl-substituted aminocarbonyl group such as a group.

Examples of the pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group include 2-[(2-pyrimidyl) aminocarbonyl] vinyl, 3-[(4-pyrimidyl) aminocarbonyl] allyl and 4-[(5-pyrimidyl) amino Carbonyl] -3-methyl-1-butenyl,
4-[(6-pyrimidyl) aminocarbonyl] -2-butenyl, 4-[(2-pyrimidyl) aminocarbonyl]
-3-butenyl, 3-[(4-pyrimidyl) aminocarbonyl] -1-methylallyl, 5-[(5-pyrimidyl) aminocarbonyl] -2-pentenyl, 6-[(6
-Pyrimidyl) aminocarbonyl] -2-hexenyl,
Examples thereof include a straight or branched alkenyl group having 2 to 6 carbon atoms having a pyrimidyl-substituted aminocarbonyl group such as 3-[(2-pyrimidyl) aminocarbonyl] -1-propenyl group.

The lower alkylthioureidocarbonyl group includes, for example, methylthioureidocarbonyl, ethylthioureidocarbonyl, propylthioureidocarbonyl, isopropylthioureidocarbonyl, butylthioureidocarbonyl, isobutylthioureidocarbonyl, tert-butylthioureidocarbonyl, pentylthiol An alkylthioureidocarbonyl group in which the alkyl moiety such as ureidocarbonyl and hexylthioureidocarbonyl is a linear or branched alkyl group having carbon atoms can be given.

Examples of the pyrimidylaminocarbonyl lower alkoxy group include (2-pyrimidyl) aminocarbonylmethoxy, 2- (4-pyrimidyl) aminocarbonylethoxy, 1- (5-pyrimidyl) aminocarbonylethoxy and 3- ( 2-pyrimidyl) aminocarbonylpropoxy, 4- (6-pyrimidyl) aminocarbonylbutoxy, 5- (2-pyrimidyl) aminocarbonylpentyloxy, 6- (4-pyrimidyl) aminocarbonylhexyloxy, 1,1-dimethyl-2 -(5-pyrimidyl) aminocarbonylethoxy, 2-methyl-3-
Examples thereof include a linear or branched C1-C6 alkoxy group having a pyrimidylaminocarbonyl group such as a (2-pyrimidyl) aminocarbonylpropoxy group.

Examples of the pyridylaminocarbonyl lower alkoxy group include (2-pyridyl) aminocarbonylmethoxy, 2- (3-pyridyl) aminocarbonylethoxy, 1- (4-pyridyl) aminocarbonylethoxy, and 3- (2-pyridyl) ) Aminocarbonylpropoxy, 4- (4-pyridyl) aminocarbonylbutoxy,
5- (2-pyridyl) aminocarbonylpentyloxy, 6- (3-pyridyl) aminocarbonylhexyloxy, 1,1-dimethyl-2- (4-pyridyl) aminocarbonylethoxy, 2-methyl-3- (2- Examples thereof include a linear or branched C1-C6 alkoxy group having a pyridylaminocarbonyl group such as a pyridyl) aminocarbonylpropoxy group.

Examples of the pyrazylaminocarbonyl lower alkoxy group include (2-pyrazyl) aminocarbonylmethoxy, 2- (3-pyrazyl) aminocarbonylethoxy, 1- (5-pyrazyl) aminocarbonylethoxy, and 3- (2- Pyrazyl) aminocarbonylpropoxy, 4- (2-pyrazyl) aminocarbonylbutoxy,
5- (2-pyrazyl) aminocarbonylpentyloxy, 6- (3-pyrazyl) aminocarbonylhexyloxy, 1,1-dimethyl-2- (3-pyrazyl) aminocarbonylethoxy, 2-methyl-3- (2- And a straight-chain or branched alkoxy group having 1 to 6 carbon atoms having a pyrazylaminocarbonyl group such as a pyrazyl) aminocarbonylpropoxy group.

Examples of the lower alkenylene group include vinylene, 1-propenylene, 1-methyl-1-propenylene, 2-methyl-1-propenylene, 2-propenylene, 2-butenylene, 1-butenylene, 3-butenylene, -Pentenylene, 1-pentenylene, 3-pentenylene, 4-pentenylene, 1,3-butenedienylene,
1,3-pentadienylene, 2-penten-4-inylene, 2-hexenylene, 1-hexenylene, 5-hexenylene, 3-hexenylene, 4-hexenylene, 3,3
-Dimethyl-1-propenylene, 2-ethyl-1-propenylene, 1,3-hexadienylene, 1,4-hexadienylene, 1,3,5-hexatrienylene, etc., having 1 to 3 carbon atoms having 1 to 3 double bonds. There may be mentioned 2-6 straight or branched alkenylene groups.

Examples of the 1,2,4-triazolyl-substituted lower alkoxy group include 1,2,4-triazolylmethoxy, 2- (1,2,4-triazolyl) ethoxy,
-(1,2,4-triazolyl) ethoxy, 3- (1,
2,4-triazolyl) propoxy, 4- (1,2,4
-Triazolyl) butoxy, 5- (1,2,4-triazolyl) pentyloxy, 6- (1,2,4-triazolyl) hexyloxy, 1,1-dimethyl-2- (1,
2,4-triazolyl) ethoxy, 2-methyl-3-
Examples thereof include 1,2,4-triazolyl-substituted alkoxy groups in which the alkoxy moiety such as a (1,2,4-triazolyl) propoxy group is a linear or branched alkoxy group having 1 to 6 carbon atoms.

The benzene derivatives of the general formula (1) of the present invention include the compounds of the following various embodiments. In these embodiments, R ³ and R ⁴ are all the same as defined in the general formula (1).

(1) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, R ² may be a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent.

[0087]

Embedded image

Wherein R ⁸ and m are the same as defined in the above formula (1), wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group represented by the above formula (1). Derivatives or salts thereof.

(2) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, R ² may be a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent.

[0090]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the above-mentioned formula (1) or Its salt.

(3) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, R ² may be a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent.

[0093]

Embedded image

Wherein R ⁸ and m are the same as defined in the general formula (1), and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1); Its salt.

(4) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, R ² may be a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent.

[0096]

Embedded image

Wherein R ⁸ and m are the same as defined in the above formula (1), wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.
Or a salt thereof.

(5) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, R ² may be a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent.

[0099]

Embedded image

A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above formula (1), wherein R ⁵ is a phenylthioureidocarbonyl group.

(6) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, R ² may be a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent.

[0102]

Embedded image

A benzene derivative represented by the above formula (1), wherein R ⁸ and m are the same as defined in the above formula (1), and R ⁵ is a pyridylthioureidocarbonyl group, or a salt thereof.

[0104] (7) R ¹ is a nitrogen atom, an oxygen atom or a sulfur atom 1-4 Yes to 5-6 membered unsaturated heterocyclic residue (on the heterocyclic ring, C ₁ -C ₁₂ alkyl group, R ² may be a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent.

[0105]

Embedded image

A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above general formula (1), and R ⁵ is a lower alkylthioureidocarbonyl group.

(8) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, R ² may be a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent.

[0108]

Embedded image

A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above formula (1), and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(9) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, R ² may be a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent.

[0111]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and R ⁵ is a group

[0113]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(10) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, R ² may be a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent.

[0116]

Embedded image

(R⁸And m are in the general formula (1)
R)^FiveIs a group-(A _Four)_rCOOH
(A_FourAnd r are the same as defined in the above general formula (1))
A benzene derivative represented by the general formula (1)
Its salt.

(11) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, R ² may be a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent.

[0119]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), and R ⁵ is a group

[0121]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)), and a benzene derivative represented by the general formula (1) or a salt thereof.

(12) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkyl group or an oxo group as a substituent. A 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group, wherein R ⁵ is a lower alkoxyalkoxyaminocarbonyl-substituted lower alkenyl group represented by the above general formula (1) Benzene derivatives or salts thereof.

(13) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkyl group or an oxo group as a substituent. A benzene represented by the above general formula (1), which represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group, and wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group; Derivatives or salts thereof.

(14) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkyl group or an oxo group as a substituent. A benzene represented by the above general formula (1), which represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group, and wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group; Derivatives or salts thereof.

(15) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkyl group or an oxo group as a substituent. A benzene represented by the above general formula (1), which represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group, and wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group; Derivatives or salts thereof.

(16) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkyl group or an oxo group as a substituent. A benzene derivative represented by the above general formula (1), which represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group, and wherein R ⁵ is a phenylthioureidocarbonyl group; salt.

(17) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkyl group or an oxo group as a substituent. A 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group, wherein R ⁵ is a pyridylthioureidocarbonyl group; salt.

(18) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkyl group or an oxo group as a substituent. A 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group, wherein R ⁵ is a lower alkylthioureidocarbonyl group; salt.

(19) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkyl group or an oxo group as a substituent. A benzene derivative represented by the above general formula (1) or a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group, wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group; salt.

(20) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkyl group or an oxo group as a substituent. indicates certain 1,2,3,4-tetrahydroquinolyl group which may have a group selected from the group, R ⁵ is a group

[0132]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(21) a 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkyl group or an oxo group as a substituent. A 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group, wherein R ⁵ is a group — (A ₄ ) _r COOH (A ₄ and r
Is the same as defined in the general formula (1)) or a benzene derivative represented by the general formula (1) or a salt thereof.

(22) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkyl group or an oxo group as a substituent. indicates certain 1,2,3,4-tetrahydroquinolyl group which may have a group selected from the group, R ⁵ is a group

[0136]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(23) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group, which may have a lower alkyl group as a substituent, may be substituted.), R ² represents a pyridylcarbonyl group, and R ⁵ represents a lower alkyl group. A benzene derivative represented by the above formula (1), which is an alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(24) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a pyridylcarbonyl group, and R ⁵ represents a hydroxyl group A benzene derivative represented by the above formula (1), which is a substituted aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(25) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a pyridylcarbonyl group, and R ⁵ represents pyridyl. A benzene derivative represented by the above formula (1), which is a substituted aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(26) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), R ² represents a pyridylcarbonyl group, and R ⁵ represents pyrimidyl. A benzene derivative represented by the above formula (1), which is a substituted aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(27) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a pyridylcarbonyl group, and R ⁵ represents phenyl A benzene derivative represented by the general formula (1), which is a thioureidocarbonyl group, or a salt thereof.

(28) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a pyridylcarbonyl group, and R ⁵ represents pyridyl. A benzene derivative represented by the general formula (1), which is a thioureidocarbonyl group, or a salt thereof.

(29) A 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group, which may have a lower alkyl group as a substituent, may be substituted.), R ² represents a pyridylcarbonyl group, and R ⁵ represents a lower alkyl group. A benzene derivative represented by the general formula (1), which is an alkylthioureidocarbonyl group, or a salt thereof.

[0145] (30) R ¹ is a nitrogen atom, an oxygen atom or a sulfur atom 1-4 Yes to 5-6 membered unsaturated heterocyclic residue (on the heterocyclic ring, C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a pyridylcarbonyl group, and R ⁵ represents pyridylamino A benzene derivative represented by the general formula (1), which is a carbonyl lower alkoxy group, or a salt thereof.

(31) a 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms, wherein R ¹ is a C ₁ -C ₁₂ alkyl group; A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a pyridylcarbonyl group, and R ⁵ represents a group

[0147]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(32) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a pyridylcarbonyl group, and R ⁵ represents a group A benzene derivative represented by the general formula (1) or a salt thereof, wherein-(A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1));

(33) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a pyridylcarbonyl group, and R ⁵ represents a group

[0151]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(34) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent, and R ² may have a hydroxyl group as a substituent. A benzene derivative represented by the above general formula (1) or a salt thereof, which represents an alkanoyl group and wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(35) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent, and R ² may have a hydroxyl group as a substituent. A benzene derivative represented by the above general formula (1) or a salt thereof, which represents an alkanoyl group and wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(36) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent, and R ² may have a hydroxyl group as a substituent. A benzene derivative represented by the above formula (1) or a salt thereof, wherein the benzene derivative is an alkanoyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(37) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent, and R ² may have a hydroxyl group as a substituent. A benzene derivative represented by the above general formula (1) or a salt thereof, which represents an alkanoyl group and wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

[0157] (38) R ¹ is a nitrogen atom, an oxygen atom or a sulfur atom 1-4 Yes to 5-6 membered unsaturated heterocyclic residue (on the heterocyclic ring, C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent, and R ² may have a hydroxyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, which represents an alkanoyl group and wherein R ⁵ is a phenylthioureidocarbonyl group.

(39) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent, and R ² may have a hydroxyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, which represents an alkanoyl group and wherein R ⁵ is a pyridylthioureidocarbonyl group.

(40) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent, and R ² may have a hydroxyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, which represents an alkanoyl group and wherein R ⁵ is a lower alkylthioureidocarbonyl group.

(41) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent, and R ² may have a hydroxyl group as a substituent. A benzene derivative represented by the above general formula (1) or a salt thereof, which represents an alkanoyl group and wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(42) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent, and R ² may have a hydroxyl group as a substituent. R ⁵ represents an alkanoyl group;

[0162]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(43) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (R ¹ is a C _{1 to} C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent, and R ² may have a hydroxyl group as a substituent. An alkanoyl group, wherein R ⁵ is a group — (A ₄ ) _r COOH (A ₄ and r are the above-mentioned general formula (1)
The benzene derivative represented by the general formula (1) or a salt thereof.

(44) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent, and R ² may have a hydroxyl group as a substituent. R ⁵ represents an alkanoyl group;

[0166]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)), and a benzene derivative represented by the general formula (1) or a salt thereof.

(45) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² has a lower alkoxycarbonyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, wherein the cycloalkylcarbonyl group may have an amino lower alkyl group having the formula:

(46) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² has a lower alkoxycarbonyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a hydroxy-substituted aminocarbonyl-substituted lower alkenyl group, which is a cycloalkylcarbonyl group which may have an amino lower alkyl group.

(47) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² has a lower alkoxycarbonyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group;

(48) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² has a lower alkoxycarbonyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group;

(49) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² has a lower alkoxycarbonyl group as a substituent. A benzene derivative represented by the above general formula (1), wherein R ⁵ is a phenylthioureidocarbonyl group, wherein R ⁵ is a cycloalkylcarbonyl group which may have an amino lower alkyl group;

(50) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (R ¹ is a C _{1 to} C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² has a lower alkoxycarbonyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyridylthioureidocarbonyl group;

(51) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² has a lower alkoxycarbonyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a lower alkylthioureidocarbonyl group, wherein R ⁵ is a cycloalkylcarbonyl group which may have an amino lower alkyl group.

(52) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² has a lower alkoxycarbonyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group, wherein R ⁵ is a cycloalkylcarbonyl group which may have a certain amino lower alkyl group.

(53) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² has a lower alkoxycarbonyl group as a substituent. a cycloalkyl group which may have an amino lower alkyl group which, R ⁵ is a group

[0177]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(54) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² has a lower alkoxycarbonyl group as a substituent. Wherein R ⁵ is a group — (A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)). A benzene derivative represented by the formula (1) or a salt thereof.

(55) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² has a lower alkoxycarbonyl group as a substituent. a cycloalkyl group which may have an amino lower alkyl group which, R ⁵ is a group

[0181]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(56) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ Is a lower alkoxy lower alkoxy group, an aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(57) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ Is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(58) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ Is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.
Or a salt thereof.

(59) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ Is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(60) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ Is a phenylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(61) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ Is a pyridylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(62) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ Is a lower alkylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(63) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ Is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(64) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ Is based

[0192]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(65) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ Is a group-(A ₄ ) _r COOH
(A ₄ and r are the same as defined in the general formula (1))
A benzene derivative represented by the general formula (1) or a salt thereof.

(66) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ Is based

[0196]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)), and a benzene derivative represented by the general formula (1) or a salt thereof.

(67) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkoxy group as a substituent on a phenyl ring. A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a phenoxycarbonyl group which may have R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(68) R¹Is a nitrogen atom, oxygen atom or sulfur
5-6 membered unsaturated heterocyclic residue having 1-4 yellow atoms
(On the heterocycle, C₁~ C₁₂Alkyl group and substituent
Lower alkyl which may have a lower alkyl group
A group selected from the group consisting of
It may be. ) And R^TwoIs substituted on the phenyl ring
Which may have a lower alkoxy group as a group
Represents a cyclocarbonyl group; ^FiveIs hydroxyl-substituted aminocarbo
In the above general formula (1), which is a lower-substituted alkenyl group,
Or a salt thereof.

(69) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkoxy group as a substituent on a phenyl ring. Wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a salt thereof, wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group;

(70) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkoxy group as a substituent on the phenyl ring Wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group;
Or a salt thereof.

(71) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkoxy group as a substituent on a phenyl ring. It indicates phenoxycarbonyl group which may have a benzene derivative or a salt thereof represented by the general formula R ⁵ is phenyl thioureido group (1).

(72) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkoxy group as a substituent on a phenyl ring. Wherein R ⁵ is a pyridylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(73) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkoxy group as a substituent on a phenyl ring. Wherein R ⁵ is a lower alkylthioureidocarbonyl group or a benzene derivative represented by the above general formula (1), or a salt thereof.

(74) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkoxy group as a substituent on a phenyl ring. Wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the above general formula (1), or a salt thereof.

(75) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkoxy group as a substituent on a phenyl ring. A phenoxycarbonyl group which may have R ⁵

[0207]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(76) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkoxy group as a substituent on a phenyl ring. A phenoxycarbonyl group which may have the formula: wherein R ⁵ is a group-(A ₄ ) _r COOH
(A ₄ and r are the same as defined in the general formula (1))
A benzene derivative represented by the general formula (1) or a salt thereof.

(77) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkoxy group as a substituent on a phenyl ring. A phenoxycarbonyl group which may have R ⁵

[0211]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(78) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a thienylcarbonyl group, and R ⁵ represents a lower alkyl group; A benzene derivative represented by the above formula (1), which is an alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(79) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a thienylcarbonyl group, and R ⁵ represents a hydroxyl group A benzene derivative represented by the above formula (1), which is a substituted aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(80) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a thienylcarbonyl group, and R ⁵ represents pyridyl. A benzene derivative represented by the above formula (1), which is a substituted aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(81) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a thienylcarbonyl group, and R ⁵ represents pyrimidyl. A benzene derivative represented by the above formula (1), which is a substituted aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(82) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a thienylcarbonyl group, and R ⁵ represents phenyl A benzene derivative represented by the general formula (1), which is a thioureidocarbonyl group, or a salt thereof.

[0218] (83) R ¹ is a nitrogen atom, an oxygen atom or a sulfur atom 1-4 Yes to 5-6 membered unsaturated heterocyclic residue (on the heterocyclic ring, C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a thienylcarbonyl group, and R ⁵ represents pyridyl. A benzene derivative represented by the general formula (1), which is a thioureidocarbonyl group, or a salt thereof.

(84) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a thienylcarbonyl group, and R ⁵ represents a lower alkyl group; A benzene derivative represented by the general formula (1), which is an alkylthioureidocarbonyl group, or a salt thereof.

(85) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a thienylcarbonyl group, and R ⁵ represents pyridylamino A benzene derivative represented by the general formula (1), which is a carbonyl lower alkoxy group, or a salt thereof.

(86) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a thienylcarbonyl group, and R ⁵ represents a group

[0222]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(87) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a thienylcarbonyl group, and R ⁵ represents a group A benzene derivative represented by the general formula (1) or a salt thereof, wherein-(A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1));

(88) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a thienylcarbonyl group, and R ⁵ represents a group

[0226]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(89) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a carboxy group, and R ⁵ represents a lower alkoxy group. A benzene derivative represented by the above general formula (1), which is a lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a salt thereof.

[0229] (90) R ¹ is a nitrogen atom, an oxygen atom or a sulfur atom 1-4 Yes to 5-6 membered unsaturated heterocyclic residue (on the heterocyclic ring, C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), R ² represents a carboxy group, and R ⁵ is substituted with a hydroxyl group. A benzene derivative represented by the general formula (1), which is an aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(91) a 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms, wherein R ¹ is a C ₁ -C ₁₂ alkyl group; A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent, may be substituted), R ² represents a carboxy group, and R ⁵ represents pyridyl substitution. A benzene derivative represented by the general formula (1), which is an aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(92) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a carboxy group, and R ⁵ represents pyrimidyl substitution. A benzene derivative represented by the general formula (1), which is an aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(93) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a carboxy group, and R ⁵ represents phenylthio. A benzene derivative represented by the general formula (1), which is an ureidocarbonyl group, or a salt thereof.

(94) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a carboxy group, and R ⁵ represents pyridylthio. A benzene derivative represented by the general formula (1), which is an ureidocarbonyl group, or a salt thereof.

(95) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a carboxy group, and R ⁵ represents a lower alkylthio group. A benzene derivative represented by the general formula (1), which is an ureidocarbonyl group, or a salt thereof.

(96) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a carboxy group, and R ⁵ represents pyridylaminocarbonyl A benzene derivative represented by the formula (1), which is a lower alkoxy group, or a salt thereof.

(97) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a carboxy group, and R ⁵ represents a group

[0237]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(98) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a carboxy group, and R ⁵ represents a group- (A ₄ ) The general formula (1) which is _r COOH (A ₄ and r are the same as defined in the general formula (1))
Or a salt thereof.

(99) a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a carboxy group, and R ⁵ represents a group

[0241]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(100) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a lower alkoxycarbonyl group, and R ⁵ represents A benzene derivative represented by the above formula (1), which is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(101) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a lower alkoxycarbonyl group, and R ⁵ represents A benzene derivative represented by the above formula (1), which is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(102) a 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a lower alkoxycarbonyl group, and R ⁵ represents A benzene derivative represented by the formula (1), which is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(103) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a lower alkoxycarbonyl group, and R ⁵ represents A benzene derivative represented by the above formula (1), which is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(104) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a lower alkoxycarbonyl group, and R ⁵ represents A benzene derivative represented by the general formula (1), which is a phenylthioureidocarbonyl group, or a salt thereof.

(105) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a lower alkoxycarbonyl group, and R ⁵ represents A benzene derivative represented by the general formula (1), which is a pyridylthioureidocarbonyl group, or a salt thereof.

(106) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a lower alkoxycarbonyl group, and R ⁵ represents A benzene derivative represented by the above formula (1), which is a lower alkylthioureidocarbonyl group, or a salt thereof.

(107) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a lower alkoxycarbonyl group, and R ⁵ represents A benzene derivative represented by the general formula (1), which is a pyridylaminocarbonyl lower alkoxy group, or a salt thereof.

(108) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a lower alkoxycarbonyl group, and R ⁵ represents Base

[0252]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

[0254] (109) R ¹ is a nitrogen atom, an oxygen atom or a sulfur atom 1-4 Yes to 5-6 membered unsaturated heterocyclic residue (on the heterocyclic ring, C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a lower alkoxycarbonyl group, and R ⁵ represents A benzene derivative represented by the general formula (1) or a salt thereof, which is a group-(A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(110) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen, oxygen or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), R ² represents a lower alkoxycarbonyl group, and R ⁵ represents Base

[0256]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(111) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkoxycarbonyl group or a phenyl lower group as a substituent. A benzene derivative represented by the general formula (1), wherein the pyrrolidinylcarbonyl group may have a group selected from the group consisting of an alkoxycarbonyl group, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group; Its salt.

(112) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkoxycarbonyl group or a phenyl lower group as a substituent. indicates certain pyrrolidinylcarbonyl group which may have a group selected from an alkoxycarbonyl group the group consisting of a benzene derivative or a salt thereof R ⁵ is represented by the general formula is a hydroxyl group substituted aminocarbonyl substituted lower alkenyl group (1) .

(113) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkoxycarbonyl group or a phenyl lower group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative is a pyrrolidinylcarbonyl group which may have a group selected from the group consisting of an alkoxycarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group; .

[0261] (114) R ¹ is a nitrogen atom, an oxygen atom or a sulfur atom 1-4 Yes to 5-6 membered unsaturated heterocyclic residue (on the heterocyclic ring, C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkoxycarbonyl group or a phenyl lower group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein the pyrrolidinylcarbonyl group may have a group selected from the group consisting of an alkoxycarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group; .

(115) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkoxycarbonyl group or a phenyl lower group as a substituent. A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a pyrrolidinylcarbonyl group which may have a group selected from the group consisting of an alkoxycarbonyl group and wherein R ⁵ is a phenylthioureidocarbonyl group.

(116) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (R ¹ is a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkoxycarbonyl group or a phenyl lower group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, which represents a pyrrolidinylcarbonyl group which may have a group selected from the group consisting of an alkoxycarbonyl group, and wherein R ⁵ is a pyridylthioureidocarbonyl group.

(117) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkoxycarbonyl group or a phenyl lower group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, which represents a pyrrolidinylcarbonyl group which may have a group selected from the group consisting of an alkoxycarbonyl group, and wherein R ⁵ is a lower alkylthioureidocarbonyl group.

(118) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (R ¹ is a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkoxycarbonyl group or a phenyl lower group as a substituent. A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a pyrrolidinylcarbonyl group which may have a group selected from the group consisting of alkoxycarbonyl groups, and wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(119) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkoxycarbonyl group or a phenyl lower group as a substituent. A pyrrolidinylcarbonyl group which may have a group selected from the group consisting of an alkoxycarbonyl group, wherein R ⁵ is a group

[0267]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as those defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(120) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (R ¹ is a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkoxycarbonyl group or a phenyl lower group as a substituent. A pyrrolidinylcarbonyl group which may have a group selected from the group consisting of an alkoxycarbonyl group, wherein R ⁵ is a group — (A ₄ ) _r CO 2
A benzene derivative represented by the general formula (1) or a salt thereof, which is OH (A ₄ and r are the same as defined in the general formula (1)).

(121) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² is a lower alkoxycarbonyl group or a phenyl lower group as a substituent. A pyrrolidinylcarbonyl group which may have a group selected from the group consisting of an alkoxycarbonyl group, wherein R ⁵ is a group

[0271]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(122) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), and R ² has a lower alkyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents an amino lower alkoxycarbonyl group and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(123) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), and R ² has a lower alkyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents an amino lower alkoxycarbonyl group and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(124) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), and R ² has a lower alkyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents an amino lower alkoxycarbonyl group and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(125) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), and R ² has a lower alkyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a certain amino lower alkoxycarbonyl group and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(126) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), and R ² has a lower alkyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents an amino lower alkoxycarbonyl group and R ⁵ is a phenylthioureidocarbonyl group.

(127) 5 to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), and R ² has a lower alkyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents an amino lower alkoxycarbonyl group and R ⁵ is a pyridylthioureidocarbonyl group.

[0279] (128) R ¹ is a nitrogen atom, an oxygen atom or a sulfur atom 1-4 Yes to 5-6 membered unsaturated heterocyclic residue (on the heterocyclic ring, C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), and R ² has a lower alkyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents an amino lower alkoxycarbonyl group and R ⁵ is a lower alkylthioureidocarbonyl group.

(129) 5 to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen, oxygen or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), and R ² has a lower alkyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a certain amino lower alkoxycarbonyl group and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(130) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), and R ² has a lower alkyl group as a substituent. An amino lower alkoxycarbonyl group, wherein R ⁵ is a group

[0282]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(131) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), and R ² has a lower alkyl group as a substituent. A benzene represented by the general formula (1), which represents an amino lower alkoxycarbonyl group, wherein R ⁵ is a group — (A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)); Derivatives or salts thereof.

[0285] (132) R ¹ is a nitrogen atom, an oxygen atom or a sulfur atom 1-4 Yes to 5-6 membered unsaturated heterocyclic residue (on the heterocyclic ring, C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), and R ² has a lower alkyl group as a substituent. An amino lower alkoxycarbonyl group, wherein R ⁵ is a group

[0286]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(133) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), and R ² has a lower alkyl group as a substituent. Wherein R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group which represents a piperidinylcarbonyl group;
Or a salt thereof.

(134) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), and R ² has a lower alkyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a piperidinylcarbonyl group and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(135) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), and R ² has a lower alkyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a piperidinylcarbonyl group and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(136) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), and R ² has a lower alkyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a piperidinylcarbonyl group and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(137) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), and R ² has a lower alkyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a piperidinylcarbonyl group and R ⁵ is a phenylthioureidocarbonyl group.

(138) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), and R ² has a lower alkyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a piperidinylcarbonyl group and R ⁵ is a pyridylthioureidocarbonyl group.

(139) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), and R ² has a lower alkyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a piperidinylcarbonyl group and R ⁵ is a lower alkylthioureidocarbonyl group.

(140) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), and R ² has a lower alkyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a piperidinylcarbonyl group and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(141) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), and R ² has a lower alkyl group as a substituent. R ⁵ represents a piperidinylcarbonyl group;

[0297]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(142) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), and R ² has a lower alkyl group as a substituent. A benzene represented by the general formula (1), which represents a piperidinylcarbonyl group, wherein R ⁵ is a group — (A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)); Derivatives or salts thereof.

(143) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, A group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted), and R ² has a lower alkyl group as a substituent. R ⁵ represents a piperidinylcarbonyl group;

[0301]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(144) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² represents a group —CO— (A ₁ ) _p
—NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the above formula (1)), wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group (1 Or a salt thereof.

(145) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² represents a group —CO— (A ₁ ) _p
—NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(146) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen, oxygen or sulfur atoms (a C _{1 to} C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² represents a group —CO— (A ₁ ) _p
—NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group; Or a salt thereof.

(147) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² represents a group —CO— (A ₁ ) _p
—NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group; Or a salt thereof.

(148) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² represents a group —CO— (A ₁ ) _p
—NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a phenylthioureidocarbonyl group represented by the general formula (1). Or a salt thereof.

(149) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² represents a group —CO— (A ₁ ) _p
—NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and are represented by the general formula (1) in which R ⁵ is a pyridylthioureidocarbonyl group. Or a salt thereof.

(150) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² represents a group —CO— (A ₁ ) _p
—NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the above general formula (1)), and R ⁵ is a lower alkylthioureidocarbonyl group represented by the above general formula (1). Or a salt thereof.

(151) A 5- to 6-membered unsaturated heterocyclic residue having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms (wherein R ¹ is a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² represents a group —CO— (A ₁ ) _p
—NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a pyridylaminocarbonyl lower alkoxy group represented by the general formula (1). Or a salt thereof.

(152) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² represents a group —CO— (A ₁ ) _p
—NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a group

[0312]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(153) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² represents a group —CO— (A ₁ ) _p
—NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a group — (A ₄ )
A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(154) R ¹ is a 5- to 6-membered unsaturated heterocyclic residue having 1-4 nitrogen atoms, oxygen atoms or sulfur atoms (a C ₁ -C ₁₂ alkyl group, And a group selected from the group consisting of an amino lower alkyl group and a cycloalkyl group which may have a lower alkyl group as a substituent may be substituted.), And R ² represents a group —CO— (A ₁ ) _p
—NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a group

[0316]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(155) R ¹ represents a cyano group, and R ² represents a group

[0319]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group represented by the above formula (1) Derivatives or salts thereof.

(156) R ¹ represents a cyano group, and R ² represents a group

[0322]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the above formula (1) or Its salt.

(157) R ¹ represents a cyano group, and R ² represents a group

[0325]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) or Its salt.

(158) R ¹ represents a cyano group, and R ² represents a group

[0328]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.
Or a salt thereof.

(159) R ¹ represents a cyano group, and R ² represents a group

[0331]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and the benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a phenylthioureidocarbonyl group.

(160) R ¹ represents a cyano group, and R ² represents a group

[0334]

Embedded image

A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above formula (1), and R ⁵ is a pyridylthioureidocarbonyl group.

(161) R ¹ represents a cyano group, and R ² represents a group

[0337]

Embedded image

A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above formula (1), and R ⁵ is a lower alkylthioureidocarbonyl group.

(162) R ¹ represents a cyano group, and R ² represents a group

[0340]

Embedded image

A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above formula (1), and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(163) R ¹ represents a cyano group, and R ² represents a group

[0343]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), wherein R ⁵ is a group

[0345]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(164) R ¹ represents a cyano group, and R ² represents a group

[0348]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), and R ⁵ is a group — (A ₄ ) _r COOH
(A ₄ and r are the same as defined in the general formula (1))
A benzene derivative represented by the general formula (1) or a salt thereof.

(165) R ¹ represents a cyano group, and R ² represents a group

[0351]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), and R ⁵ is a group

[0353]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(166) R ¹ is a cyano group, and R ² is a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group Wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(167) R ¹ represents a cyano group, and R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group. Wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(168) R ¹ represents a cyano group, and R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group. Wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(169) R ¹ represents a cyano group, and R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group. Wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(170) R ¹ represents a cyano group, and R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group. Wherein R ⁵ is a phenylthioureidocarbonyl group or a benzene derivative represented by the general formula (1) or a salt thereof.

(171) R ¹ represents a cyano group, and R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group. Wherein R ⁵ is a pyridylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(172) R ¹ represents a cyano group, and R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group. Wherein R ⁵ is a lower alkylthioureidocarbonyl group or a salt thereof represented by the above general formula (1).

(173) R ¹ represents a cyano group, and R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group. Wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(174) R ¹ represents a cyano group, and R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group. And R ⁵ is a group

[0364]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), and a benzene derivative represented by the general formula (1) or a salt thereof.

(175) R ¹ is a cyano group, and R ² is a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group And R ⁵ represents a group — (A ₄ ) _r C
A benzene derivative represented by the general formula (1) or a salt thereof, which is OOH (A ₄ and r are the same as defined in the general formula (1)).

(176) R ¹ represents a cyano group, and R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group. And R ⁵ is a group

[0368]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(177) A benzene derivative represented by the above general formula (1), wherein R ¹ is a cyano group, R ² is a pyridylcarbonyl group, and R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group Or a salt thereof.

(178) In the above formula (1), wherein R ¹ represents a cyano group, R ² represents a pyridylcarbonyl group, and R ⁵ represents a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.
Or a salt thereof.

(179) R ¹ is a cyano group, R ² is a pyridylcarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group; salt.

(180) A benzene derivative represented by the above general formula (1) wherein R ¹ is a cyano group, R ² is a pyridylcarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, salt.

(181) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ represents a cyano group, R ² represents a pyridylcarbonyl group, and R ⁵ represents a phenylthioureidocarbonyl group.

(182) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ represents a cyano group, R ² represents a pyridylcarbonyl group, and R ⁵ represents a pyridylthioureidocarbonyl group.

(183) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ represents a cyano group, R ² represents a pyridylcarbonyl group, and R ⁵ represents a lower alkylthioureidocarbonyl group.

(184) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ is a cyano group, R ² is a pyridylcarbonyl group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(185) R ¹ represents a cyano group, R ² represents a pyridylcarbonyl group, and R ⁵ represents a group

[0379]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(186) R ¹ represents a cyano group, R ² represents a pyridylcarbonyl group, and R ⁵ represents a group — (A ₄ ) _r COO
A benzene derivative represented by the general formula (1) or a salt thereof, which is H (A ₄ and r are the same as defined in the general formula (1)).

(187) R ¹ represents a cyano group, R ² represents a pyridylcarbonyl group, and R ⁵ represents a group

[0383]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(188) A compound of the above general formula wherein R ¹ represents a cyano group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by (1) or a salt thereof.

(189) In the above formula (1), R ¹ represents a cyano group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(190) In the above formula (1), R ¹ represents a cyano group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(191) In the above formula (1), R ¹ represents a cyano group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(192) In the above formula (1), R ¹ represents a cyano group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a phenylthioureidocarbonyl group. Or a salt thereof.

(193) In the above formula (1), R ¹ represents a cyano group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a pyridylthioureidocarbonyl group. Or a salt thereof.

(194) In the above formula (1), R ¹ represents a cyano group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a lower alkylthioureidocarbonyl group. Or a salt thereof.

(195) In the above formula (1), R ¹ represents a cyano group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a pyridylaminocarbonyl lower alkoxy group. Or a salt thereof.

(196) R ¹ represents a cyano group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a group

[0394]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a salt thereof represented by the general formula (1).

(197) R ¹ represents a cyano group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a group — (A ₄ ) _r COOH (A ₄ and r are A benzene derivative represented by the general formula (1) or a salt thereof, which is the same as defined in the general formula (1).

(198) R ¹ represents a cyano group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a group

[0398]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(199) R ¹ represents a cyano group, R ² represents a cycloalkylcarbonyl group sometimes having an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a lower alkoxycarbonyl group. A benzene derivative represented by the above general formula (1), which is a lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(200) R ¹ represents a cyano group, R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a hydroxyl group-substituted group. Formula (1) which is an aminocarbonyl-substituted lower alkenyl group
Or a salt thereof.

(201) R ¹ represents a cyano group, R ² represents a cycloalkylcarbonyl group which may have an amino-lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a pyridyl-substituted group. A benzene derivative represented by the general formula (1), which is an aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(202) R ¹ represents a cyano group, R ² represents a cycloalkylcarbonyl group which may have an amino-lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a pyrimidyl-substituted group. A benzene derivative represented by the general formula (1), which is an aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(203) R ¹ represents a cyano group, R ² represents a cycloalkylcarbonyl group sometimes having an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a phenylthio group. A benzene derivative represented by the general formula (1), which is an ureidocarbonyl group, or a salt thereof.

(204) R ¹ represents a cyano group, R ² represents a cycloalkylcarbonyl group sometimes having an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a pyridylthio group A benzene derivative represented by the general formula (1), which is an ureidocarbonyl group, or a salt thereof.

(205) R ¹ represents a cyano group, R ² represents a cycloalkylcarbonyl group sometimes having an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a lower alkylthio group. A benzene derivative represented by the general formula (1), which is an ureidocarbonyl group, or a salt thereof.

(206) R ¹ represents a cyano group, R ² represents a cycloalkylcarbonyl group which may have an amino-lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a pyridylaminocarbonyl A benzene derivative represented by the formula (1), which is a lower alkoxy group, or a salt thereof.

(207) R ¹ represents a cyano group, R ² represents a cycloalkylcarbonyl group sometimes having an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a group

[0409]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), and a benzene derivative represented by the general formula (1) or a salt thereof.

(208) R ¹ represents a cyano group, R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a group- (A ₄ ) _r COO
A benzene derivative represented by the general formula (1) or a salt thereof, which is H (A ₄ and r are the same as defined in the general formula (1)).

(209) R ¹ represents a cyano group, R ² represents a cycloalkylcarbonyl group sometimes having an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a group

[0413]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(210) Formula (1) wherein R ¹ represents a cyano group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. Benzene derivatives or salts thereof.

(211) A benzene derivative represented by the above general formula (1) wherein R ¹ represents a cyano group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(212) A benzene derivative represented by the above general formula (1), wherein R ¹ is a cyano group, R ² is a benzoyloxy lower alkanoyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(213) A benzene derivative represented by the above general formula (1), wherein R ¹ represents a cyano group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(214) A compound of the above general formula (1) wherein R ¹ represents a cyano group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a phenylthioureidocarbonyl group.
Or a salt thereof.

(215) The above-mentioned formula (1) wherein R ¹ represents a cyano group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a pyridylthioureidocarbonyl group.
Or a salt thereof.

(216) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ represents a cyano group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a lower alkylthioureidocarbonyl group. .

(217) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ represents a cyano group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a pyridylaminocarbonyl lower alkoxy group. .

(218) R ¹ represents a cyano group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a group

[0424]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)).

(219) R ¹ represents a cyano group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a group
(A ₄ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(220) R ¹ represents a cyano group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a group

[0428]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(221) R ¹ represents a cyano group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl. A benzene derivative represented by the general formula (1) or a salt thereof.

(222) R ¹ represents a cyano group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ represents a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(223) R ¹ represents a cyano group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ represents a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(224) R ¹ represents a cyano group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ represents a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(225) The above general formula wherein R ¹ represents a cyano group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ represents a phenylthioureidocarbonyl group. A benzene derivative represented by the formula (1) or a salt thereof.

(226) The above general formula wherein R ¹ represents a cyano group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ represents a pyridylthioureidocarbonyl group. A benzene derivative represented by the formula (1) or a salt thereof.

(227) The above general formula wherein R ¹ represents a cyano group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a lower alkylthioureidocarbonyl group. A benzene derivative represented by the formula (1) or a salt thereof.

(228) The above general formula wherein R ¹ represents a cyano group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group. A benzene derivative represented by the formula (1) or a salt thereof.

(229) R ¹ represents a cyano group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a group

[0439]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(230) R ¹ represents a cyano group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a group
(A ₄ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(231) R ¹ represents a cyano group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a group

[0443]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(232) A benzene derivative represented by the above formula (1) wherein R ¹ represents a cyano group, R ² represents a thienylcarbonyl group, and R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(233) A compound of the above general formula (1) wherein R ¹ represents a cyano group, R ² represents a thienylcarbonyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.
Or a salt thereof.

(234) A benzene derivative represented by the above formula (1) wherein R ¹ is a cyano group, R ² is a thienylcarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, salt.

(235) R ¹ is a cyano group, R ² is a thienylcarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group; salt.

(236) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ represents a cyano group, R ² represents a thienylcarbonyl group, and R ⁵ represents a phenylthioureidocarbonyl group.

(237) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ represents a cyano group, R ² represents a thienylcarbonyl group, and R ⁵ represents a pyridylthioureidocarbonyl group.

(238) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ represents a cyano group, R ² represents a thienylcarbonyl group, and R ⁵ represents a lower alkylthioureidocarbonyl group.

(239) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ represents a cyano group, R ² represents a thienylcarbonyl group, and R ⁵ represents a pyridylaminocarbonyl lower alkoxy group.

(240) R ¹ represents a cyano group, R ² represents a thienylcarbonyl group, and R ⁵ represents a group

[0454]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)).

(241) R ¹ represents a cyano group, R ² represents a thienylcarbonyl group, and R ⁵ represents a group — (A ₄ ) _r COO
A benzene derivative represented by the general formula (1) or a salt thereof, which is H (A ₄ and r are the same as defined in the general formula (1)).

(242) R ¹ represents a cyano group, R ² represents a thienylcarbonyl group, and R ⁵ represents a group

[0458]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(243) A benzene derivative represented by the above general formula (1), wherein R ¹ is a cyano group, R ² is a carboxy group, and R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group; Its salt.

(244) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ is a cyano group, R ² is a carboxy group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. .

(245) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ is a cyano group, R ² is a carboxy group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. .

(246) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ is a cyano group, R ² is a carboxy group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. .

(247) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ represents a cyano group, R ² represents a carboxy group, and R ⁵ represents a phenylthioureidocarbonyl group.

(248) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ represents a cyano group, R ² represents a carboxy group, and R ⁵ represents a pyridylthioureidocarbonyl group.

(249) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ is a cyano group, R ² is a carboxy group, and R ⁵ is a lower alkylthioureidocarbonyl group.

(250) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ is a cyano group, R ² is a carboxy group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(251) R ¹ represents a cyano group, R ² represents a carboxy group, and R ⁵ represents a group

[0469]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the above general formula (1)).

(252) R ¹ represents a cyano group, R ² represents a carboxy group, and R ⁵ represents a group — (A ₄ ) _r COOH (A ₄ and r are the same as defined in the above formula (1)) A benzene derivative represented by the general formula (1) or a salt thereof.

(253) R ¹ represents a cyano group, R ² represents a carboxy group, and R ⁵ represents a group

[0473]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(254) A benzene represented by the above general formula (1) wherein R ¹ is a cyano group, R ² is a lower alkoxycarbonyl group, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. Derivatives or salts thereof.

(255) R ¹ is a cyano group, R ² is a lower alkoxycarbonyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group; Its salt.

(256) A benzene derivative represented by the above general formula (1) wherein R ¹ represents a cyano group, R ² represents a lower alkoxycarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group; Its salt.

(257) R ¹ is a cyano group, R ² is a lower alkoxycarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group; Its salt.

(258) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ represents a cyano group, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a phenylthioureidocarbonyl group.

(259) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ represents a cyano group, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a pyridylthioureidocarbonyl group.

(260) R¹Represents a cyano group;^TwoIs low
A lower alkoxycarbonyl group; ^FiveIs lower alkyl
A thioureidocarbonyl group represented by the above general formula (1)
Or a salt thereof.

(261) A compound of the above general formula (1) wherein R ¹ represents a cyano group, R ² represents a lower alkoxycarbonyl group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.
Or a salt thereof.

(262) R ¹ represents a cyano group, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a group

[0484]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(263) R ¹ represents a cyano group, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a group — (A ₄ ) _r
A benzene derivative represented by the general formula (1), which is COOH (A ₄ and r are the same as defined in the general formula (1)), or a salt thereof.

(264) R ¹ represents a cyano group, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a group

[0488]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(265) R ¹ represents a cyano group; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(266) R ¹ represents a cyano group; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; A benzene derivative represented by the above formula (1) or a salt thereof, wherein ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(267) R ¹ represents a cyano group; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(268) R ¹ represents a cyano group; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(269) R ¹ represents a cyano group; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; A benzene derivative represented by the general formula (1), wherein ⁵ is a phenylthioureidocarbonyl group, or a salt thereof.

(270) R ¹ represents a cyano group; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; A benzene derivative represented by the above formula (1), wherein ⁵ is a pyridylthioureidocarbonyl group, or a salt thereof.

(271) R ¹ represents a cyano group; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a lower alkylthioureidocarbonyl group.

(272) R ¹ represents a cyano group; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(273) R ¹ represents a cyano group, R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group, ⁵ based

[0499]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), and a benzene derivative represented by the general formula (1) or a salt thereof.

(274) R ¹ represents a cyano group; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; ⁵ is a group-(A ₄ ) _r COOH (A ₄ and r are the above-mentioned general formula (1)
The benzene derivative represented by the general formula (1) or a salt thereof.

(275) R ¹ represents a cyano group; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; ⁵ based

[0503]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(276) R ¹ represents a cyano group, R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(277) wherein R ¹ is a cyano group, R ² is an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group; A benzene derivative represented by the general formula (1) or a salt thereof.

(278) wherein R ¹ represents a cyano group, R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(279) wherein R ¹ is a cyano group, R ² is an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(280) In the above formula (R), R ¹ represents a cyano group, R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a phenylthioureidocarbonyl group. A benzene derivative represented by 1) or a salt thereof.

(281) A compound represented by the above general formula ( ¹ ) wherein R ¹ represents a cyano group, R ² represents an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a pyridylthioureidocarbonyl group. A benzene derivative represented by 1) or a salt thereof.

(282) A compound represented by the above general formula ( ¹ ) wherein R ¹ represents a cyano group, R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a lower alkylthioureidocarbonyl group. A benzene derivative represented by 1) or a salt thereof.

(283) In the above general formula (R), R ¹ represents a cyano group, R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group. 1)
Or a salt thereof.

(284) R ¹ represents a cyano group, R ² represents an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[0514]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(285) R ¹ represents a cyano group, R ² represents an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group — (A ₄ ) _r
A benzene derivative represented by the general formula (1), which is COOH (A ₄ and r are the same as defined in the general formula (1)), or a salt thereof.

(286) R ¹ represents a cyano group, R ² represents an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[0518]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(287) R ¹ represents a cyano group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(288) wherein R ¹ is a cyano group, R ² is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group; A benzene derivative represented by the general formula (1) or a salt thereof.

(289) wherein R ¹ is a cyano group, R ² is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. General formula (1)
Or a salt thereof.

(290) wherein R ¹ is a cyano group, R ² is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(291) In the above general formula (R), R ¹ represents a cyano group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a phenylthioureidocarbonyl group. A benzene derivative represented by 1) or a salt thereof.

(292) The above general formula ( ¹ ) wherein R ¹ represents a cyano group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a pyridylthioureidocarbonyl group. A benzene derivative represented by 1) or a salt thereof.

(293) In the above general formula (R), R ¹ represents a cyano group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a lower alkylthioureidocarbonyl group. A benzene derivative represented by 1) or a salt thereof.

(294) The above general formula ( ¹ ) wherein R ¹ represents a cyano group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a pyridylaminocarbonyl lower alkoxy group. A benzene derivative represented by 1) or a salt thereof.

(295) R ¹ represents a cyano group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[0529]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), and the benzene derivative represented by the general formula (1) or a salt thereof.

(296) R ¹ represents a cyano group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group — (A ₄ ) _r COOH
(A ₄ and r are the same as defined in the general formula (1))
A benzene derivative represented by the general formula (1) or a salt thereof.

(297) R ¹ represents a cyano group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[0533]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(298) R ¹ represents a cyano group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R
¹² is the same as defined in the general formula (1)), and a benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(299) R ¹ represents a cyano group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R
¹² is the same as defined in the general formula (1)),
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(300) R ¹ represents a cyano group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R
¹² is the same as defined in the general formula (1)),
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(301) R ¹ represents a cyano group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R
¹² is the same as defined in the general formula (1)),
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(302) R ¹ represents a cyano group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R
¹² is the same as defined in the general formula (1)),
A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a phenylthioureidocarbonyl group.

(303) R ¹ represents a cyano group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R
¹² is the same as defined in the general formula (1)),
A benzene derivative represented by the above general formula (1), wherein R ⁵ is a pyridylthioureidocarbonyl group, or a salt thereof.

(304) R ¹ represents a cyano group and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R
¹² is the same as defined in the general formula (1)),
A benzene derivative represented by the above general formula (1), wherein R ⁵ is a lower alkylthioureidocarbonyl group, or a salt thereof.

(305) R ¹ represents a cyano group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R
¹² is the same as defined in the general formula (1)),
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(306) R ¹ represents a cyano group, R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R
¹² is the same as defined in the general formula (1)),
R ⁵ based

[0544]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(307) R ¹ represents a cyano group and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R
¹² is the same as defined in the general formula (1)),
R ⁵ is a group - (A _{4) r} COOH benzene derivative or a salt thereof (A ₄ and r are as defined in the general formula (1)) represented by the general formula is (1).

(308) R ¹ represents a cyano group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R
¹² is the same as defined in the general formula (1)),
R ⁵ based

[0548]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

[0550] (309) R ¹ represents a carboxy group, R ²
Is based

[0551]

Embedded image

(Where R ⁸ and m are the same as defined in the above formula (1)), and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group represented by the above formula (1). Derivatives or salts thereof.

[0553] (310) R ¹ represents a carboxy group, R ²
Is based

[0554]

Embedded image

(R ⁸ and m are the same as defined in the above general formula (1)), and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) or Its salt.

[0556] (311) R ¹ represents a carboxy group, R ²
Is based

[0557]

Embedded image

(R ⁸ and m are the same as defined in the above general formula (1)), and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) or Its salt.

[0559] (312) R ¹ represents a carboxy group, R ²
Is based

[0560]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.
Or a salt thereof.

[0562] (313) R ¹ represents a carboxy group, R ²
Is based

[0563]

Embedded image

[0564] A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above general formula (1), and R ⁵ is a phenylthioureidocarbonyl group.

[0565] (314) R ¹ represents a carboxy group, R ²
Is based

[0566]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), and the benzene derivative represented by the above formula (1) or a salt thereof, wherein R ⁵ is a pyridylthioureidocarbonyl group.

[0568] (315) R ¹ represents a carboxy group, R ²
Is based

[0569]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), and the benzene derivative represented by the above formula (1) or a salt thereof, wherein R ⁵ is a lower alkylthioureidocarbonyl group.

[0571] (316) R ¹ represents a carboxy group, R ²
Is based

[0572]

Embedded image

A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above general formula (1), and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(317) R ¹ represents a carboxy group, and R ²
Is based

[0575]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), and R ⁵ is a group

[0577]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

[0579] (318) R ¹ represents a carboxy group, R ²
Is based

[0580]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), wherein R ⁵ is a group — (A ₄ ) _r COOH
(A ₄ and r are the same as defined in the general formula (1))
A benzene derivative represented by the general formula (1) or a salt thereof.

[0582] (319) R ¹ represents a carboxy group, R ²
Is based

[0583]

Embedded image

(R ⁸ and m are the same as defined in the formula (1)), wherein R ⁵ is a group

[0585]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

[0587] (320) R ¹ represents a carboxy group, R ²
Represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent, and R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group A benzene derivative represented by the general formula (1) or a salt thereof.

[0588] (321) R ¹ represents a carboxy group, R ²
Represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

[0589] (322) R ¹ represents a carboxy group, R ²
Represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

[0590] (323) R ¹ represents a carboxy group, R ²
Represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

[0591] (324) R ¹ represents a carboxy group, R ²
Is a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group, and R ⁵ is a phenylthioureidocarbonyl group. A benzene derivative represented by (1) or a salt thereof.

[0592] (325) R ¹ represents a carboxy group, R ²
Is a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent, and R ⁵ is a pyridylthioureidocarbonyl group. A benzene derivative represented by (1) or a salt thereof.

[0593] (326) R ¹ represents a carboxy group, R ²
Is a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent, and R ⁵ is a lower alkylthioureidocarbonyl group. A benzene derivative represented by (1) or a salt thereof.

[0594] (327) R ¹ represents a carboxy group, R ²
Is a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group. A benzene derivative represented by (1) or a salt thereof.

[0595] (328) R ¹ represents a carboxy group, R ²
Is a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent, and R ⁵ is a group

[0596]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

[0598] (329) R ¹ represents a carboxy group, R ²
There indicates certain 1,2,3,4-tetrahydroquinolyl group which may have a group selected from the group consisting lower alkyl group and oxo group as a substituent, R ⁵ is a group - (A ₄₎
A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

[0599] (330) R ¹ represents a carboxy group, R ²
Is a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent, and R ⁵ is a group

[0600]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

[0602] (331) R ¹ represents a carboxy group, R ²
Is a pyridylcarbonyl group, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1).

[0603] (332) R ¹ represents a carboxy group, R ²
Is a pyridylcarbonyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1).

[0604] (333) R ¹ represents a carboxy group, R ²
Is a pyridylcarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1).

[0605] (334) R ¹ represents a carboxy group, R ²
Represents a pyridylcarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1).

[0606] (335) R ¹ represents a carboxy group, R ²
Is a pyridylcarbonyl group, and R ⁵ is a phenylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0607] (336) R ¹ represents a carboxy group, R ²
Is a pyridylcarbonyl group, and R ⁵ is a pyridylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0608] (337) R ¹ represents a carboxy group, R ²
Is a pyridylcarbonyl group, and R ⁵ is a lower alkylthioureidocarbonyl group or a benzene derivative represented by the general formula (1) or a salt thereof.

[0609] (338) R ¹ represents a carboxy group, R ²
Is a pyridylcarbonyl group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0610] (339) R ¹ represents a carboxy group, R ²
Represents a pyridylcarbonyl group, and R ⁵ represents a group

[0611]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

[0613] (340) R ¹ represents a carboxy group, R ²
Represents a pyridylcarbonyl group, and R ⁵ represents a group — (A ₄ ) _r C
A benzene derivative represented by the general formula (1) or a salt thereof, which is OOH (A ₄ and r are the same as defined in the general formula (1)).

[0614] (341) R ¹ represents a carboxy group, R ²
Represents a pyridylcarbonyl group, and R ⁵ represents a group

[0615]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

[0617] (342) R ¹ represents a carboxy group, R ²
Is a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group or a benzene derivative represented by the above general formula (1) or a salt thereof.

[0618] (343) R ¹ represents a carboxy group, R ²
Is a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0619] (344) R ¹ represents a carboxy group, R ²
Is a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group or a benzene derivative represented by the above general formula (1) or a salt thereof.

[0620] (345) R ¹ represents a carboxy group, R ²
Is a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

[0621] (346) R ¹ represents a carboxy group, R ²
Is a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a phenylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0622] (347) R ¹ represents a carboxy group, R ²
Is a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a pyridylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0623] (348) R ¹ represents a carboxy group, R ²
Is a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a lower alkylthioureidocarbonyl group or a benzene derivative represented by the above formula (1) or a salt thereof.

[0624] (349) R ¹ represents a carboxy group, R ²
Is a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0625] (350) R ¹ represents a carboxy group, R ²
Represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a group

[0626]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), and the benzene derivative represented by the general formula (1) or a salt thereof.

[0628] (351) R ¹ represents a carboxy group, R ²
Represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a group — (A ₄ ) _r COOH (A ₄ and r
Is the same as defined in the general formula (1)) or a benzene derivative represented by the general formula (1) or a salt thereof.

[0629] (352) R ¹ represents a carboxy group, R ²
Represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a group

[0630]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

[0632] (353) R ¹ represents a carboxy group, R ²
Is a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

[0633] (354) R ¹ represents a carboxy group, R ²
Represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

[0634] (355) R ¹ represents a carboxy group, R ²
Is a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

[0635] (356) R ¹ represents a carboxy group, R ²
Is a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

[0636] (357) R ¹ represents a carboxy group, R ²
Is a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ is a phenylthioureidocarbonyl group, and the benzene represented by the general formula (1) Derivatives or salts thereof.

[0637] (358) R ¹ represents a carboxy group, R ²
Is a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ is a pyridylthioureidocarbonyl group, and the benzene represented by the above general formula (1) Derivatives or salts thereof.

[0638] (359) R ¹ represents a carboxy group, R ²
Is a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ is a lower alkylthioureidocarbonyl group, and the benzene represented by the above general formula (1) Derivatives or salts thereof.

[0639] (360) R ¹ represents a carboxy group, R ²
Is a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group, the benzene represented by the general formula (1). Derivatives or salts thereof.

[0640] (361) R ¹ represents a carboxy group, R ²
Represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ is a group

[0641]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

[0643] (362) R ¹ represents a carboxy group, R ²
Represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a group — (A ₄ ) _r C
A benzene derivative represented by the general formula (1) or a salt thereof, which is OOH (A ₄ and r are the same as defined in the general formula (1)).

[0644] (363) R ¹ represents a carboxy group, R ²
Represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ is a group

[0645]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

[0647] (364) R ¹ represents a carboxy group, R ²
Is a benzoyloxy lower alkanoyl group, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group or a benzene derivative represented by the above general formula (1) or a salt thereof.

[0648] (365) R ¹ represents a carboxy group, R ²
Is a benzoyloxy lower alkanoyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0649] (366) R ¹ represents a carboxy group, R ²
Is a benzoyloxy lower alkanoyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1).

[0650] (367) R ¹ represents a carboxy group, R ²
Is a benzoyloxy lower alkanoyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1).

[0651] (368) R ¹ represents a carboxy group, R ²
Is a benzoyloxy lower alkanoyl group, and R ⁵ is a phenylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0652] (369) R ¹ represents a carboxy group, R ²
Is a benzoyloxy lower alkanoyl group, and R ⁵ is a pyridylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0653] (370) R ¹ represents a carboxy group, R ²
Is a benzoyloxy lower alkanoyl group, and R ⁵ is a lower alkylthioureidocarbonyl group or a benzene derivative represented by the above general formula (1) or a salt thereof.

[0654] (371) R ¹ represents a carboxy group, R ²
Is a benzoyloxy lower alkanoyl group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the above general formula (1).

[0655] (372) R ¹ represents a carboxy group, R ²
Represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a group

[0656]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

[0658] (373) R ¹ represents a carboxy group, R ²
Represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a group — (A ₄ ) _r COOH (A ₄ and r represent the above-mentioned general formula (1)
The benzene derivative represented by the general formula (1) or a salt thereof.

[0659] (374) R ¹ represents a carboxy group, R ²
Represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a group

[0660]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

[0662] (375) R ¹ represents a carboxy group, R ²
Is a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or Its salt.

[0663] (376) R ¹ represents a carboxy group, R ²
Is a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof. .

[0664] (377) R ¹ represents a carboxy group, R ²
Is a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof. .

[0665] (378) R ¹ represents a carboxy group, R ²
Is a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof. .

[0666] (379) R ¹ represents a carboxy group, R ²
Is a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ is a phenylthioureidocarbonyl group, or a benzene derivative represented by the above general formula (1).

[0667] (380) R ¹ represents a carboxy group, R ²
Is a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ is a pyridylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0668] (381) R ¹ represents a carboxy group, R ²
Is a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ is a lower alkylthioureidocarbonyl group or a benzene derivative represented by the above general formula (1).

[0669] (382) R ¹ represents a carboxy group, R ²
Is a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0670] (383) R ¹ represents a carboxy group, R ²
Represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ represents a group

[0671]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

[0673] (384) R ¹ represents a carboxy group, R ²
Represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ represents a group — (A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)) A benzene derivative represented by the general formula (1) or a salt thereof.

[0674] (385) R ¹ represents a carboxy group, R ²
Represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ represents a group

[0675]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

[0677] (386) R ¹ represents a carboxy group, R ²
Represents a thienylcarbonyl group, and R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1).

[0678] (387) R ¹ represents a carboxy group, R ²
Is a thienylcarbonyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1).

[0679] (388) R ¹ represents a carboxy group, R ²
Is a thienylcarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a salt thereof represented by the general formula (1).

[0680] (389) R ¹ represents a carboxy group, R ²
Is a thienylcarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0681] (390) R ¹ represents a carboxy group, R ²
Is a thienylcarbonyl group, and R ⁵ is a phenylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0682] (391) R ¹ represents a carboxy group, R ²
Is a thienylcarbonyl group, and R ⁵ is a pyridylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0683] (392) R ¹ represents a carboxy group, R ²
Is a thienylcarbonyl group, and R ⁵ is a lower alkylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0684] (393) R ¹ represents a carboxy group, R ²
Is a thienylcarbonyl group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0685] (394) R ¹ represents a carboxy group, R ²
Represents a thienylcarbonyl group, and R ⁵ represents a group

[0686]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

[0688] (395) R ¹ represents a carboxy group, R ²
Represents a thienylcarbonyl group, and R ⁵ represents a group — (A ₄ ) _r C
A benzene derivative represented by the general formula (1) or a salt thereof, which is OOH (A ₄ and r are the same as defined in the general formula (1)).

[0689] (396) R ¹ represents a carboxy group, R ²
Represents a thienylcarbonyl group, and R ⁵ represents a group

[0690]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

[0692] (397) R ¹ represents a carboxy group, R ²
Is a carboxy group, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

[0693] (398) R ¹ represents a carboxy group, R ²
Is a carboxy group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group;

[0694] (399) R ¹ represents a carboxy group, R ²
Is a carboxy group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0695] (400) R ¹ represents a carboxy group, R ²
Is a carboxy group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.
Or a salt thereof.

[0696] (401) R ¹ represents a carboxy group, R ²
Is a carboxy group, and R ⁵ is a phenylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0697] (402) R ¹ represents a carboxy group, R ²
Is a carboxy group, and R ⁵ is a pyridylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0698] (403) R ¹ represents a carboxy group, R ²
Is a carboxy group, and R ⁵ is a lower alkylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0699] (404) R ¹ represents a carboxy group, R ²
Is a carboxy group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0700] (405) R ¹ represents a carboxy group, R ²
Represents a carboxy group, and R ⁵ represents a group

[0701]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

[0703] (406) R ¹ represents a carboxy group, R ²
Represents a carboxy group, and R ⁵ represents a group — (A ₄ ) _r COOH
(A ₄ and r are the same as defined in the general formula (1))
A benzene derivative represented by the general formula (1) or a salt thereof.

[0704] (407) R ¹ represents a carboxy group, R ²
Represents a carboxy group, and R ⁵ represents a group

[0705]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

[0707] (408) R ¹ represents a carboxy group, R ²
Is a lower alkoxycarbonyl group, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0708] (409) R ¹ represents a carboxy group, R ²
Is a lower alkoxycarbonyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above formula (1).

[0709] (410) R ¹ represents a carboxy group, R ²
Is a lower alkoxycarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0710] (411) R ¹ represents a carboxy group, R ²
Is a lower alkoxycarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1).

[0711] (412) R ¹ represents a carboxy group, R ²
Is a lower alkoxycarbonyl group, and R ⁵ is a phenylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0712] (413) R ¹ represents a carboxy group, R ²
Is a lower alkoxycarbonyl group, and R ⁵ is a pyridylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0713] (414) R ¹ represents a carboxy group, R ²
Is a lower alkoxycarbonyl group, and R ⁵ is a lower alkylthioureidocarbonyl group.
Or a salt thereof.

[0714] (415) R ¹ represents a carboxy group, R ²
Is a lower alkoxycarbonyl group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0715] (416) R ¹ represents a carboxy group, R ²
Represents a lower alkoxycarbonyl group, and R ⁵ represents a group

[0716]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

[0718] (417) R ¹ represents a carboxy group, R ²
Represents a lower alkoxycarbonyl group, and R ⁵ represents a group-
(A ₄ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

[0719] (418) R ¹ represents a carboxy group, R ²
Represents a lower alkoxycarbonyl group, and R ⁵ represents a group

[0720]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

[0722] (419) R ¹ represents a carboxy group, R ²
Represents a pyrrolidinylcarbonyl group which may have, as a substituent, a group selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group;
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.

[0723] (420) R ¹ represents a carboxy group, R ²
Represents a pyrrolidinylcarbonyl group which may have, as a substituent, a group selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group;
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

[0724] (421) R ¹ represents a carboxy group, R ²
Represents a pyrrolidinylcarbonyl group which may have, as a substituent, a group selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group;
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

[0725] (422) R ¹ represents a carboxy group, R ²
Represents a pyrrolidinylcarbonyl group which may have, as a substituent, a group selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group;
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

[0726] (423) R ¹ represents a carboxy group, R ²
Represents a pyrrolidinylcarbonyl group which may have, as a substituent, a group selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group;
A benzene derivative represented by the general formula (1), wherein ⁵ is a phenylthioureidocarbonyl group, or a salt thereof.

[0727] (424) R ¹ represents a carboxy group, R ²
Represents a pyrrolidinylcarbonyl group which may have, as a substituent, a group selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group;
A benzene derivative represented by the above formula (1), wherein ⁵ is a pyridylthioureidocarbonyl group, or a salt thereof.

[0728] (425) R ¹ represents a carboxy group, R ²
Represents a pyrrolidinylcarbonyl group which may have, as a substituent, a group selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group;
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a lower alkylthioureidocarbonyl group.

[0729] (426) R ¹ represents a carboxy group, R ²
Represents a pyrrolidinylcarbonyl group which may have, as a substituent, a group selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group;
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a pyridylaminocarbonyl lower alkoxy group.

[0730] (427) R ¹ represents a carboxy group, R ²
Represents a pyrrolidinylcarbonyl group which may have, as a substituent, a group selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group;
⁵ based

[0731]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

[0733] (428) R ¹ represents a carboxy group, R ²
Represents a pyrrolidinylcarbonyl group which may have, as a substituent, a group selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group;
A benzene derivative represented by the general formula (1) or a salt thereof, wherein ⁵ is a group-(A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)).

[0734] (429) R ¹ represents a carboxy group, R ²
Represents a pyrrolidinylcarbonyl group which may have, as a substituent, a group selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group;
⁵ based

[0735]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

[0737] (430) R ¹ represents a carboxy group, R ²
Represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof. .

(431) R ¹ represents a carboxy group, and R ²
Represents an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group or a salt thereof represented by the above general formula (1).

[0739] (432) R ¹ represents a carboxy group, R ²
Represents an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1).

[0740] (433) R ¹ represents a carboxy group, R ²
Represents an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1).

[0741] (434) R ¹ represents a carboxy group, R ²
Represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a phenylthioureidocarbonyl group, or a benzene derivative represented by the above general formula (1).

[0742] (435) R ¹ represents a carboxy group, R ²
Represents an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0743] (436) R ¹ represents a carboxy group, R ²
Represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a lower alkylthioureidocarbonyl group.
Or a salt thereof.

[0744] (437) R ¹ represents a carboxy group, R ²
Represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

[0745] (438) R ¹ represents a carboxy group, R ²
Represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[0746]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

[0748] (439) R ¹ represents a carboxy group, R ²
Represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group-
(A ₄ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

[0749] (440) R ¹ represents a carboxy group, R ²
Represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[0750]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

[0752] (441) R ¹ represents a carboxy group, R ²
Is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof. .

[0753] (442) R ¹ represents a carboxy group, R ²
Is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above formula (1).

[0754] (443) R ¹ represents a carboxy group, R ²
Is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0755] (444) R ¹ represents a carboxy group, R ²
Is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0756] (445) R ¹ represents a carboxy group, R ²
Is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a phenylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[0757] (446) R ¹ represents a carboxy group, R ²
Represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridylthioureidocarbonyl group, or a benzene derivative represented by the above general formula (1).

[0758] (447) R ¹ represents a carboxy group, R ²
Is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a lower alkylthioureidocarbonyl group, or a salt thereof represented by the general formula (1).

[0759] (448) R ¹ represents a carboxy group, R ²
Is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the above general formula (1).

[0760] (449) R ¹ represents a carboxy group, R ²
Represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[0761]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

[0763] (450) R ¹ represents a carboxy group, R ²
Represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group — (A ₄ ) _r CO 2
A benzene derivative represented by the general formula (1) or a salt thereof, which is OH (A ₄ and r are the same as defined in the general formula (1)).

[0764] (451) R ¹ represents a carboxy group, R ²
Represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[0765]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

[0767] (452) R ¹ represents a carboxy group, R ²
Is a group -CO- (A ₁ ) _p -NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1))
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.

[0768] (453) R ¹ represents a carboxy group, R ²
Represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is hydroxyl-substituted aminocarbonyl-substituted A benzene derivative represented by the general formula (1), which is a lower alkenyl group, or a salt thereof.

[0769] (454) R ¹ represents a carboxy group, R ²
Represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is pyridyl-substituted aminocarbonyl-substituted A benzene derivative represented by the general formula (1), which is a lower alkenyl group, or a salt thereof.

[0770] (455) R ¹ represents a carboxy group, R ²
Represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is pyrimidyl-substituted aminocarbonyl-substituted A benzene derivative represented by the general formula (1), which is a lower alkenyl group, or a salt thereof.

[0771] (456) R ¹ represents a carboxy group, R ²
Represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ represents a phenylthioureidocarbonyl group A benzene derivative represented by the general formula (1) or a salt thereof.

[0772] (457) R ¹ represents a carboxy group, R ²
Represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ represents a pyridylthioureidocarbonyl group A benzene derivative represented by the general formula (1) or a salt thereof.

[0773] (458) R ¹ represents a carboxy group, R ²
Represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a lower alkylthioureidocarbonyl group A benzene derivative represented by the general formula (1) or a salt thereof.

[0774] (459) R ¹ represents a carboxy group, R ²
Represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a pyridylaminocarbonyl lower alkoxy group A benzene derivative represented by the general formula (1) or a salt thereof.

[0775] (460) R ¹ represents a carboxy group, R ²
Represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ represents a group

[0776]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

[0778] (461) R ¹ represents a carboxy group, R ²
Represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ represents a group — (A ₄ The general formula (1) wherein _r COOH (A ₄ and r are the same as defined in the general formula (1))
Or a salt thereof.

[0779] (462) R ¹ represents a carboxy group, R ²
Represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ represents a group

[0780]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(463) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a group

[0783]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group represented by the above formula (1) Derivatives or salts thereof.

(464) R ¹ is a carboxy-substituted lower alkyl group, and R ² is

[0786]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) or Its salt.

(465) R ¹ is a carboxy-substituted lower alkyl group, and R ² is

[0789]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) or Its salt.

(466) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a group

[0792]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.
Or a salt thereof.

(467) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents

[0795]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and the benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a phenylthioureidocarbonyl group.

(468) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a group

[0798]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and the benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyridylthioureidocarbonyl group.

(469) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents

[0801]

Embedded image

A benzene derivative represented by the above formula (1) wherein R ⁸ and m are the same as defined in the above formula (1), and R ⁵ is a lower alkylthioureidocarbonyl group, or a salt thereof.

(470) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a group

[0804]

Embedded image

A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above general formula (1), wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(471) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a group

[0807]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), and R ⁵ is a group

[0809]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(472) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a group

[0812]

Embedded image

(R⁸And m are in the general formula (1)
R)^FiveIs a group-(A _Four)_rCOOH
(A_FourAnd r are the same as defined in the above general formula (1))
A benzene derivative represented by the general formula (1)
Its salt.

(473) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a group

[0815]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), and R ⁵ is a group

[0817]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)), and a benzene derivative represented by the general formula (1) or a salt thereof.

(474) R ¹ is a carboxy-substituted lower alkyl group, and R ² is 1,2,3,4-tetrahydro which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group. A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a quinolylcarbonyl group and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(475) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents 1,2,3,4-tetrahydro which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group. A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative is a quinolylcarbonyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(476) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents 1,2,3,4-tetrahydro which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group. A benzene derivative represented by the general formula (1) or a salt thereof, which represents a quinolylcarbonyl group and wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(477) R ¹ is a carboxy-substituted lower alkyl group, and R ² is 1,2,3,4-tetrahydro which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a quinolylcarbonyl group and wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(478) R ¹ is a carboxy-substituted lower alkyl group, and R ² is 1,2,3,4-tetrahydro which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group A benzene derivative represented by the general formula (1) or a salt thereof, which represents a quinolylcarbonyl group and R ⁵ is a phenylthioureidocarbonyl group.

(479) R ¹ is a carboxy-substituted lower alkyl group, and R ² is 1,2,3,4-tetrahydro which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group A benzene derivative represented by the general formula (1) or a salt thereof, which represents a quinolylcarbonyl group and R ⁵ is a pyridylthioureidocarbonyl group.

(480) R ¹ is a carboxy-substituted lower alkyl group, and R ² is 1,2,3,4-tetrahydro which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group. A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a quinolylcarbonyl group and R ⁵ is a lower alkylthioureidocarbonyl group.

(481) R ¹ is a carboxy-substituted lower alkyl group, and R ² is 1,2,3,4-tetrahydro which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group. A benzene derivative represented by the general formula (1) or a salt thereof, which represents a quinolylcarbonyl group and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(482) R ¹ is a carboxy-substituted lower alkyl group, and R ² is 1,2,3,4-tetrahydro which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group A quinolylcarbonyl group, wherein R ⁵ is a group

[0828]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(483) R ¹ is a carboxy-substituted lower alkyl group, and R ² is 1,2,3,4-tetrahydro which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group. A quinolylcarbonyl group, wherein R ⁵ is a group — (A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)); Its salt.

(484) R ¹ is a carboxy-substituted lower alkyl group, and R ² is 1,2,3,4-tetrahydro which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group. A quinolylcarbonyl group, wherein R ⁵ is a group

[0832]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(485) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a pyridylcarbonyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(486) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a pyridylcarbonyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(487) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a pyridylcarbonyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(488) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a pyridylcarbonyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(489) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a pyridylcarbonyl group,
A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a phenylthioureidocarbonyl group.

(490) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a pyridylcarbonyl group,
A benzene derivative represented by the above general formula (1), wherein R ⁵ is a pyridylthioureidocarbonyl group, or a salt thereof.

(491) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a pyridylcarbonyl group,
A benzene derivative represented by the above general formula (1), wherein R ⁵ is a lower alkylthioureidocarbonyl group, or a salt thereof.

(492) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a pyridylcarbonyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(493) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a pyridylcarbonyl group,
R ⁵ based

[0843]

Embedded image

[0844] benzene derivative or a salt thereof ^{_{(A 4, r, R 17}} , R 18 and R ¹⁹ are as defined in the general formula (1)) represented by the general formula is (1).

(494) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a pyridylcarbonyl group,
R ⁵ is a group - (A _{4) r} COOH benzene derivative or a salt thereof (A ₄ and r are as defined in the general formula (1)) represented by the general formula is (1).

(495) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a pyridylcarbonyl group,
R ⁵ based

[0847]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(496) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(497) In the above formula, R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(498) wherein R ¹ is a carboxy-substituted lower alkyl group, R ² is a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

[0852] (499) R ¹ represents a carboxy group-substituted lower alkyl group, a lower alkanoyl group which R ² which may have a hydroxyl group as a substituent, wherein R ⁵ is a pyrimidyl substituted aminocarbonyl substituted lower alkenyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(500) In the above formula (R), R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a phenylthioureidocarbonyl group. A benzene derivative represented by 1) or a salt thereof.

(501) The above general formula ( ¹ ) wherein R ¹ is a carboxy-substituted lower alkyl group, R ² is a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a pyridylthioureidocarbonyl group. A benzene derivative represented by 1) or a salt thereof.

(502) In the above formula (R), R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a lower alkylthioureidocarbonyl group. A benzene derivative represented by 1) or a salt thereof.

(503) In the above formula ( ¹ ), R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a pyridylaminocarbonyl lower alkoxy group. A benzene derivative represented by 1) or a salt thereof.

(504) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a group

[0858]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(505) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a group — (A ₄ )
A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(506) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a group

[0862]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(507) R ¹ represents a carboxy-substituted lower alkyl group; R ² represents a cycloalkylcarbonyl group which may have an amino-lower alkyl group which may have a lower alkoxycarbonyl group as a substituent;
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(508) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a cycloalkylcarbonyl group which may have an amino-lower alkyl group which may have a lower alkoxycarbonyl group as a substituent,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(509) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a cycloalkylcarbonyl group which may have an amino-lower alkyl group which may have a lower alkoxycarbonyl group as a substituent,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(510) R ¹ represents a carboxy-substituted lower alkyl group; R ² represents a cycloalkylcarbonyl group which may have an amino-lower alkyl group which may have a lower alkoxycarbonyl group as a substituent;
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(511) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a cycloalkylcarbonyl group which may have an amino-lower alkyl group which may have a lower alkoxycarbonyl group as a substituent,
A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a phenylthioureidocarbonyl group.

(512) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a cycloalkylcarbonyl group which may have an amino-lower alkyl group which may have a lower alkoxycarbonyl group as a substituent,
A benzene derivative represented by the above general formula (1), wherein R ⁵ is a pyridylthioureidocarbonyl group, or a salt thereof.

(513) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a cycloalkylcarbonyl group which may have an amino-lower alkyl group which may have a lower alkoxycarbonyl group as a substituent,
A benzene derivative represented by the above general formula (1), wherein R ⁵ is a lower alkylthioureidocarbonyl group, or a salt thereof.

(514) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a cycloalkylcarbonyl group which may have an amino-lower alkyl group which may have a lower alkoxycarbonyl group as a substituent,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(515) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a cycloalkylcarbonyl group which may have an amino-lower alkyl group which may have a lower alkoxycarbonyl group as a substituent,
R ⁵ based

[0873]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(516) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a cycloalkylcarbonyl group which may have an amino-lower alkyl group which may have a lower alkoxycarbonyl group as a substituent,
R ⁵ is a group - (A _{4) r} COOH benzene derivative or a salt thereof (A ₄ and r are as defined in the general formula (1)) represented by the general formula is (1).

(517) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a cycloalkylcarbonyl group which may have an amino-lower alkyl group which may have a lower alkoxycarbonyl group as a substituent,
R ⁵ based

[0877]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(518) In the above formula (1), R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(519) In the above formula (1), R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a benzoyloxy-lower alkanoyl group, and R ⁵ represents a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(520) In the above formula (1), R ¹ represents a carboxy group-substituted lower alkyl group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(521) In the above formula (1), R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a benzoyloxy-lower alkanoyl group, and R ⁵ represents a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(522) A benzene represented by the above general formula (1) wherein R ¹ represents a carboxy group-substituted lower alkyl group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a phenylthioureidocarbonyl group. Derivatives or salts thereof.

(523) A benzene represented by the above formula (1) wherein R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a pyridylthioureidocarbonyl group. Derivatives or salts thereof.

(524) R ¹ is a carboxy-substituted lower alkyl group, R ² is a benzoyloxy lower alkanoyl group, and R ⁵ is a lower alkylthioureidocarbonyl group; Derivatives or salts thereof.

(525) Benzene represented by the above general formula (1) wherein R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a pyridylaminocarbonyl lower alkoxy group. Derivatives or salts thereof.

(526) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a group

[0888]

Embedded image

[0889] benzene derivative or a salt thereof ^{_{(A 4, r, R 17}} , R 18 and R ¹⁹ are as defined in the general formula (1)) represented by the general formula is (1).

(527) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a group — (A ₄ ) _r COOH (A ₄ and r
Is the same as defined in the general formula (1)) or a benzene derivative represented by the general formula (1) or a salt thereof.

(528) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a group

[0892]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(529) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a lower alkoxy-lower alkoxyamino A benzene derivative represented by the above formula (1), which is a carbonyl-substituted lower alkenyl group, or a salt thereof.

(530) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a hydroxyl-substituted aminocarbonyl-substituted group. A benzene derivative represented by the general formula (1), which is a lower alkenyl group, or a salt thereof.

(531) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a pyridyl-substituted aminocarbonyl-substituted group. A benzene derivative represented by the general formula (1), which is a lower alkenyl group, or a salt thereof.

(532) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a pyrimidyl-substituted aminocarbonyl-substituted group. A benzene derivative represented by the general formula (1), which is a lower alkenyl group, or a salt thereof.

(533) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a phenylthioureidocarbonyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(534) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a pyridylthioureidocarbonyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(535) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a lower alkylthioureidocarbonyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(536) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a pyridylaminocarbonyl lower alkoxy group A benzene derivative represented by the general formula (1) or a salt thereof.

(537) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a group

[0903]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(538) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a group — (A ₄ A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(539) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a group

[0907]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(540) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a thienylcarbonyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(541) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a thienylcarbonyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(542) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a thienylcarbonyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(543) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a thienylcarbonyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(544) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a thienylcarbonyl group,
A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a phenylthioureidocarbonyl group.

(545) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a thienylcarbonyl group,
A benzene derivative represented by the above general formula (1), wherein R ⁵ is a pyridylthioureidocarbonyl group, or a salt thereof.

(546) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a thienylcarbonyl group,
A benzene derivative represented by the above general formula (1), wherein R ⁵ is a lower alkylthioureidocarbonyl group, or a salt thereof.

(547) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a thienylcarbonyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(548) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a thienylcarbonyl group,
R ⁵ based

[0918]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(549) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a thienylcarbonyl group,
R ⁵ is a group - (A _{4) r} COOH benzene derivative or a salt thereof (A ₄ and r are as defined in the general formula (1)) represented by the general formula is (1).

(550) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a thienylcarbonyl group,
R ⁵ based

[0922]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(551) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a carboxy group, and R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group represented by the above formula (1) Benzene derivatives or salts thereof.

(552) R ¹ is a carboxy-substituted lower alkyl group, R ² is a carboxy group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group; Derivatives or salts thereof.

(553) A benzene represented by the above general formula (1) wherein R ¹ is a carboxy-substituted lower alkyl group, R ² is a carboxy group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. Derivatives or salts thereof.

(554) Benzene represented by the above general formula (1) wherein R ¹ is a carboxy-substituted lower alkyl group, R ² is a carboxy group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. Derivatives or salts thereof.

(555) The above general formula (1) wherein R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a carboxy group, and R ⁵ represents a phenylthioureidocarbonyl group.
Or a salt thereof.

(556) In the above formula (1), wherein R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a carboxy group, and R ⁵ represents a pyridylthioureidocarbonyl group.
Or a salt thereof.

(557) A benzene derivative represented by the above formula (1) wherein R ¹ is a carboxy-substituted lower alkyl group, R ² is a carboxy group, and R ⁵ is a lower alkylthioureidocarbonyl group, salt.

(558) A benzene derivative represented by the above formula (1) wherein R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a carboxy group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative thereof. salt.

(559) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a carboxy group, and R ⁵ represents a group

[0933]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(560) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a carboxy group, and R ⁵ represents a group
(A ₄ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(561) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a carboxy group, and R ⁵ represents a group

[0937]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)), and the benzene derivative represented by the general formula (1) or a salt thereof.

(562) In the above formula (1), R ¹ represents a carboxy group-substituted lower alkyl group, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. The represented benzene derivative or a salt thereof.

(563) In the above formula (1), R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. Benzene derivatives or salts thereof.

(564) In the above formula (1), R ¹ is a carboxy-substituted lower alkyl group, R ² is a lower alkoxycarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. Benzene derivatives or salts thereof.

(565) R ¹ represents a carboxy group-substituted lower alkyl group, R ² represents a lower alkoxycarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group; Benzene derivatives or salts thereof.

(566) A benzene derivative represented by the above general formula (1) wherein R ¹ is a lower alkyl group substituted with a carboxy group, R ² is a lower alkoxycarbonyl group, and R ⁵ is a phenylthioureidocarbonyl group. Or a salt thereof.

(567) A benzene derivative represented by the above general formula (1) wherein R ¹ is a carboxy-substituted lower alkyl group, R ² is a lower alkoxycarbonyl group, and R ⁵ is a pyridylthioureidocarbonyl group Or a salt thereof.

(568) A benzene derivative represented by the above formula (1), wherein R ¹ is a lower alkyl group substituted with a carboxy group, R ² is a lower alkoxycarbonyl group, and R ⁵ is a lower alkylthioureidocarbonyl group. Or a salt thereof.

(569) A benzene derivative represented by the above general formula (1) wherein R ¹ is a carboxy-substituted lower alkyl group, R ² is a lower alkoxycarbonyl group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group Or a salt thereof.

(570) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a group

[0948]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(571) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a group — (A ₄ ) _r COOH (A ₄ and r represent the above-mentioned general formula (1) A) a benzene derivative represented by the above general formula (1) or a salt thereof.

(572) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a group

[0952]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(573) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl-lower alkoxycarbonyl group. Wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(574) R ¹ is a carboxy-substituted lower alkyl group, and R ² is a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group. Wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(575) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group. Wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(576) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl-lower alkoxycarbonyl group. Wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(577) R ¹ is a carboxy-substituted lower alkyl group, and R ² is a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl-lower alkoxycarbonyl group. Wherein R ⁵ is a phenylthioureidocarbonyl group or a benzene derivative represented by the general formula (1) or a salt thereof.

(578) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group. Wherein R ⁵ is a pyridylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(579) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group. Wherein R ⁵ is a lower alkylthioureidocarbonyl group or a salt thereof represented by the above general formula (1).

(580) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group. Wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(581) R ¹ is a carboxy-substituted lower alkyl group, and R ² is a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group. And R ⁵ is a group

[0963]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(582) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group. Wherein R ⁵ is a group — (A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(583) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group. And R ⁵ is a group

[0967]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(584) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a lower-alkoxy-lower-alkoxyaminocarbonyl-substituted group. A benzene derivative represented by the general formula (1), which is a lower alkenyl group, or a salt thereof.

(585) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(586) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents pyridyl-substituted aminocarbonyl-substituted lower alkenyl. A benzene derivative represented by the general formula (1) or a salt thereof.

(587) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl. A benzene derivative represented by the general formula (1) or a salt thereof.

(588) R ¹ is a carboxy-substituted lower alkyl group, R ² is an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a phenylthioureidocarbonyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(589) R ¹ is a carboxy-substituted lower alkyl group, R ² is an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridylthioureidocarbonyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(590) R ¹ represents a carboxy group-substituted lower alkyl group, R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a lower alkylthioureidocarbonyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(591) R ¹ is a carboxy-substituted lower alkyl group, R ² is an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridylaminocarbonyl-lower alkoxy group A benzene derivative represented by the general formula (1) or a salt thereof.

(592) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[0978]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(593) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group — (A ₄ ) _r A benzene derivative represented by the general formula (1), which is COOH (A ₄ and r are the same as defined in the general formula (1)), or a salt thereof.

(594) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[0982]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(595) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(596) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(597) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(598) R ¹ represents a carboxy-substituted lower alkyl group; R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent;
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(599) R ¹ represents a carboxy-substituted lower alkyl group; R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent;
A benzene derivative represented by the general formula (1), wherein ⁵ is a phenylthioureidocarbonyl group, or a salt thereof.

(600) R ¹ represents a carboxy-substituted lower alkyl group; R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent;
A benzene derivative represented by the above formula (1), wherein ⁵ is a pyridylthioureidocarbonyl group, or a salt thereof.

(601) R ¹ represents a carboxy-substituted lower alkyl group; R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent;
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a lower alkylthioureidocarbonyl group.

(602) R ¹ represents a carboxy-substituted lower alkyl group; R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent;
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(603) R ¹ represents a carboxy-substituted lower alkyl group; R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent;
⁵ based

[0993]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(604) R ¹ represents a carboxy-substituted lower alkyl group; R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent;
A benzene derivative represented by the general formula (1) or a salt thereof, wherein ⁵ is a group-(A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(605) R ¹ represents a carboxy-substituted lower alkyl group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent,
⁵ based

[0997]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(606) R¹Is a carboxy-substituted lower group
A alkyl group;^TwoIs a group -CO- (A ₁)_p-NR¹¹R
¹²(A₁, P, R¹¹And R¹²Is represented by the general formula (1).
R)^FiveIs lower alkoxy lower alkoxy
The above-mentioned one which is a cyaminocarbonyl-substituted lower alkenyl group;
A benzene derivative represented by the general formula (1) or a salt thereof.

(607) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R
¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) Benzene derivatives or salts thereof.

(608) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R
¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.
Or a salt thereof.

(609) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R
¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1). Benzene derivatives or salts thereof.

(610) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R
¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), wherein R ⁵ is a phenylthioureidocarbonyl group, and the benzene derivative represented by the general formula (1) Or a salt thereof.

(611) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R
¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), wherein R ⁵ is a pyridylthioureidocarbonyl group, a benzene derivative represented by the general formula (1) Or a salt thereof.

(612) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R
¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), wherein R ⁵ is a lower alkylthioureidocarbonyl group, and the benzene derivative represented by the general formula (1) Or a salt thereof.

(613) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R
¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a pyridylaminocarbonyl lower alkoxy group represented by the general formula (1) Or a salt thereof.

(614) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R
¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a group

[1008]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(615) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R
¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), wherein R ⁵ is a group — (A ₄ ) _r COOH
(A ₄ and r are the same as defined in the general formula (1))
A benzene derivative represented by the general formula (1) or a salt thereof.

(616) R ¹ represents a carboxy-substituted lower alkyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R
¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a group

[1012]

Embedded image

[1013] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(617) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a group

[1015]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group represented by the above formula (1). Derivatives or salts thereof.

(618) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a group

[1018]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) or Its salt.

(619) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a group

[1021]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the above formula (1) or Its salt.

(620) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a group

[1024]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.
Or a salt thereof.

(621) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a group

[1027]

Embedded image

[1028] A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above general formula (1), and R ⁵ is a phenylthioureidocarbonyl group.

(622) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a group

[1030]

Embedded image

[1031] A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above general formula (1), and R ⁵ is a pyridylthioureidocarbonyl group.

(623) R ¹ represents a lower alkoxycarbonyl group; R ² represents a group

[1033]

Embedded image

[1034] A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above formula (1), and R ⁵ is a lower alkylthioureidocarbonyl group.

(624) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a group

[1036]

Embedded image

[1037] A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above formula (1), and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(625) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a group

[1039]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), and R ⁵ is a group

[1041]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(626) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a group

[1044]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), wherein R ⁵ is a group — (A ₄ ) _r COOH
(A ₄ and r are the same as defined in the general formula (1))
A benzene derivative represented by the general formula (1) or a salt thereof.

(627) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a group

[1047]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), wherein R ⁵ is a group

[1049]

Embedded image

[1050] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(628) R ¹ represents a lower alkoxycarbonyl group, and R ² may have, as a substituent, a group selected from the group consisting of a lower alkyl group and an oxo group.
A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a 2,3,4-tetrahydroquinolylcarbonyl group, wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl substituted lower alkenyl group.

(629) R ¹ represents a lower alkoxycarbonyl group, and R ² may have, as a substituent, a group selected from the group consisting of a lower alkyl group and an oxo group.
A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a 2,3,4-tetrahydroquinolylcarbonyl group and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(630) R ¹ represents a lower alkoxycarbonyl group, and R ² may have, as a substituent, a group selected from the group consisting of a lower alkyl group and an oxo group.
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein the benzene derivative represents a 2,3,4-tetrahydroquinolylcarbonyl group and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(631) R ¹ represents a lower alkoxycarbonyl group, and R ² may have, as a substituent, a group selected from the group consisting of a lower alkyl group and an oxo group.
A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a 2,3,4-tetrahydroquinolylcarbonyl group and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(632) R ¹ represents a lower alkoxycarbonyl group, and R ² may have a substituent selected from the group consisting of a lower alkyl group and an oxo group.
A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a 2,3,4-tetrahydroquinolylcarbonyl group, wherein R ⁵ is a phenylthioureidocarbonyl group.

(633) R ¹ represents a lower alkoxycarbonyl group, and R ² may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent.
A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a 2,3,4-tetrahydroquinolylcarbonyl group, wherein R ⁵ is a pyridylthioureidocarbonyl group.

(634) R ¹ represents a lower alkoxycarbonyl group, and R ² may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent.
A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a 2,3,4-tetrahydroquinolylcarbonyl group, wherein R ⁵ is a lower alkylthioureidocarbonyl group.

(635) R ¹ represents a lower alkoxycarbonyl group, and R ² may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent.
A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a 2,3,4-tetrahydroquinolylcarbonyl group and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(636) R ¹ represents a lower alkoxycarbonyl group, and R ² may have a substituent selected from the group consisting of a lower alkyl group and an oxo group,
A 2,3,4-tetrahydroquinolylcarbonyl group, wherein R ⁵ is a group

[1060]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(637) R ¹ represents a lower alkoxycarbonyl group, and R ² may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent.
A 2,3,4-tetrahydroquinolylcarbonyl group, wherein R ⁵ is a group — (A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1));
Or a salt thereof.

(638) R ¹ represents a lower alkoxycarbonyl group, and R ² may have, as a substituent, a group selected from the group consisting of a lower alkyl group and an oxo group.
A 2,3,4-tetrahydroquinolylcarbonyl group, wherein R ⁵ is a group

[1064]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(639) Formula (1) wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a pyridylcarbonyl group, and R ⁵ represents a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. Benzene derivatives or salts thereof.

(640) A benzene derivative represented by the above general formula (1), wherein R ¹ is a lower alkoxycarbonyl group, R ² is a pyridylcarbonyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group Or a salt thereof.

(641) A benzene derivative represented by the above general formula (1), wherein R ¹ is a lower alkoxycarbonyl group, R ² is a pyridylcarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group Or a salt thereof.

(642) A benzene derivative represented by the above general formula (1), wherein R ¹ is a lower alkoxycarbonyl group, R ² is a pyridylcarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group Or a salt thereof.

(643) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a pyridylcarbonyl group, and R ⁵ is a phenylthioureidocarbonyl group. .

(644) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ is a lower alkoxycarbonyl group, R ² is a pyridylcarbonyl group, and R ⁵ is a pyridylthioureidocarbonyl group .

(645) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a pyridylcarbonyl group, and R ⁵ represents a lower alkylthioureidocarbonyl group. .

(646) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ is a lower alkoxycarbonyl group, R ² is a pyridylcarbonyl group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group. .

(647) R ¹ represents a lower alkoxycarbonyl group, R ² represents a pyridylcarbonyl group, and R ⁵ represents a group

[1075]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(648) R ¹ represents a lower alkoxycarbonyl group, R ² represents a pyridylcarbonyl group, and R ⁵ represents a group — (A ₄ ) _r COOH (A ₄ and r represent the above-mentioned general formula (1)
The benzene derivative represented by the general formula (1) or a salt thereof.

(649) R ¹ represents a lower alkoxycarbonyl group, R ² represents a pyridylcarbonyl group, and R ⁵ represents a group

[1079]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(650) wherein R ¹ is a lower alkoxycarbonyl group, R ² is a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(651) wherein R ¹ is a lower alkoxycarbonyl group, R ² is a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group; A benzene derivative represented by (1) or a salt thereof.

(652) wherein R ¹ is a lower alkoxycarbonyl group; R ² is a lower alkanoyl group which may have a hydroxyl group as a substituent; and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by (1) or a salt thereof.

(653) A compound of the above general formula wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by (1) or a salt thereof.

(654) The above formula (1) in which R ¹ represents a lower alkoxycarbonyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a phenylthioureidocarbonyl group. Or a salt thereof.

(655) A compound of the above general formula (1) wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a pyridylthioureidocarbonyl group. Or a salt thereof.

(656) The above general formula (1) wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a lower alkylthioureidocarbonyl group. Or a salt thereof.

(657) The above-mentioned formula (1) wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group. Or a salt thereof.

(658) R ¹ represents a lower alkoxycarbonyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a group

[1090]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(659) R ¹ represents a lower alkoxycarbonyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a group — (A ₄ ) _r C
A benzene derivative represented by the general formula (1) or a salt thereof, which is OOH (A ₄ and r are the same as defined in the general formula (1)).

(660) R ¹ represents a lower alkoxycarbonyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a group

[1094]

Embedded image

[1095] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

[1096] (661) R ¹ represents a lower alkoxycarbonyl group, a cycloalkyl group which may have an amino lower alkyl group R ² is which may have a lower alkoxycarbonyl group as a substituent, R ⁵
Is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

[1097] (662) R ¹ represents a lower alkoxycarbonyl group, a cycloalkyl group which may have an amino lower alkyl group R ² is which may have a lower alkoxycarbonyl group as a substituent, R ⁵
Is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

[1098] (663) R ¹ represents a lower alkoxycarbonyl group, a cycloalkyl group which may have an amino lower alkyl group R ² is which may have a lower alkoxycarbonyl group as a substituent, R ⁵
Is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[1099] (664) R ¹ represents a lower alkoxycarbonyl group, a cycloalkyl group which may have an amino lower alkyl group R ² is which may have a lower alkoxycarbonyl group as a substituent, R ⁵
Is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[1100] (665) R ¹ represents a lower alkoxycarbonyl group, a cycloalkyl group which may have an amino lower alkyl group R ² is which may have a lower alkoxycarbonyl group as a substituent, R ⁵
Is a phenylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[1101] (666) R ¹ represents a lower alkoxycarbonyl group, a cycloalkyl group which may have an amino lower alkyl group R ² is which may have a lower alkoxycarbonyl group as a substituent, R ⁵
Is a pyridylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[1102] (667) R ¹ represents a lower alkoxycarbonyl group, a cycloalkyl group which may have an amino lower alkyl group R ² is which may have a lower alkoxycarbonyl group as a substituent, R ⁵
Is a lower alkylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[1103] (668) R ¹ represents a lower alkoxycarbonyl group, a cycloalkyl group which may have an amino lower alkyl group R ² is which may have a lower alkoxycarbonyl group as a substituent, R ⁵
Is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[1104] (669) R ¹ represents a lower alkoxycarbonyl group, a cycloalkyl group which may have an amino lower alkyl group R ² is which may have a lower alkoxycarbonyl group as a substituent, R ⁵
Is based

[1105]

Embedded image

[1106] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

[1107] (670) R ¹ represents a lower alkoxycarbonyl group, a cycloalkyl group which may have an amino lower alkyl group R ² is which may have a lower alkoxycarbonyl group as a substituent, R ⁵
Is a group-(A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)) or a benzene derivative represented by the general formula (1) or a salt thereof.

[1108] (671) R ¹ represents a lower alkoxycarbonyl group, a cycloalkyl group which may have an amino lower alkyl group R ² is which may have a lower alkoxycarbonyl group as a substituent, R ⁵
Is based

[1109]

Embedded image

[1110] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(672) In the above formula (1), R ¹ represents a lower alkoxycarbonyl group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(673) Formula (1) wherein R ¹ is a lower alkoxycarbonyl group, R ² is a benzoyloxy lower alkanoyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. Benzene derivatives or salts thereof.

(674) Formula (1) wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. Benzene derivatives or salts thereof.

(675) R ¹ represents a lower alkoxycarbonyl group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the above general formula (1). Benzene derivatives or salts thereof.

(676) R ¹ is a lower alkoxycarbonyl group, R ² is a benzoyloxy lower alkanoyl group, and R ⁵ is a phenylthioureidocarbonyl group; Its salt.

(677) A benzene derivative represented by the above general formula (1) wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ is a pyridylthioureidocarbonyl group; Its salt.

(678) A benzene derivative represented by the above general formula (1) wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a lower alkylthioureidocarbonyl group; Its salt.

(679) A benzene derivative represented by the above formula (1), wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a pyridylaminocarbonyl lower alkoxy group. Its salt.

(680) R ¹ represents a lower alkoxycarbonyl group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a group

[1120]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(681) R ¹ represents a lower alkoxycarbonyl group, R ² represents a benzoyloxy lower alkanoyl group, R ⁵ represents a group — (A ₄ ) _r COOH (A ₄ and r represent the above-mentioned general formula (1) The benzene derivative represented by the general formula (1) or a salt thereof.

(682) R ¹ represents a lower alkoxycarbonyl group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a group

[1124]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(683) R ¹ represents a lower alkoxycarbonyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a lower alkoxy lower alkoxyaminocarbonyl substituent Formula (1) which is a lower alkenyl group
Or a salt thereof.

(684) R ¹ represents a lower alkoxycarbonyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(685) R ¹ represents a lower alkoxycarbonyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(686) R ¹ represents a lower alkoxycarbonyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl. A benzene derivative represented by the general formula (1) or a salt thereof.

(687) R ¹ represents a lower alkoxycarbonyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ is a phenylthioureidocarbonyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(688) R ¹ represents a lower alkoxycarbonyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ is a pyridylthioureidocarbonyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(689) R ¹ represents a lower alkoxycarbonyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ is a lower alkylthioureidocarbonyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(690) R ¹ is a lower alkoxycarbonyl group, R ² is a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group A benzene derivative represented by the general formula (1) or a salt thereof.

(691) R ¹ represents a lower alkoxycarbonyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a group

[1135]

Embedded image

[1136] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(692) R ¹ represents a lower alkoxycarbonyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a group — (A ₄ ) _r A benzene derivative represented by the general formula (1), which is COOH (A ₄ and r are the same as defined in the general formula (1)), or a salt thereof.

(693) R ¹ represents a lower alkoxycarbonyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a group

[1139]

Embedded image

[1140] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(694) R ¹ represents a lower alkoxycarbonyl group, R ² represents a thienylcarbonyl group, and R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group represented by the above general formula (1) Benzene derivatives or salts thereof.

(695) A benzene derivative represented by the above formula (1), wherein R ¹ is a lower alkoxycarbonyl group, R ² is a thienylcarbonyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group Or a salt thereof.

(696) A benzene derivative represented by the above general formula (1), wherein R ¹ is a lower alkoxycarbonyl group, R ² is a thienylcarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(697) A benzene derivative represented by the above general formula (1), wherein R ¹ is a lower alkoxycarbonyl group, R ² is a thienylcarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group Or a salt thereof.

(698) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a thienylcarbonyl group, and R ⁵ represents a phenylthioureidocarbonyl group. .

(699) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a thienylcarbonyl group, and R ⁵ represents a pyridylthioureidocarbonyl group. .

(700) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a thienylcarbonyl group, and R ⁵ represents a lower alkylthioureidocarbonyl group. .

(701) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a thienylcarbonyl group, and R ⁵ represents a pyridylaminocarbonyl lower alkoxy group. .

(702) R ¹ represents a lower alkoxycarbonyl group, R ² represents a thienylcarbonyl group, and R ⁵ represents a group

[1150]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(703) R ¹ represents a lower alkoxycarbonyl group, R ² represents a thienylcarbonyl group, and R ⁵ represents a group — (A ₄ ) _r COOH (A ₄ and r represent the above-mentioned general formula (1)
The benzene derivative represented by the general formula (1) or a salt thereof.

(704) R ¹ represents a lower alkoxycarbonyl group, R ² represents a thienylcarbonyl group, and R ⁵ represents a group

[1154]

Embedded image

[1155] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(705) A benzene represented by the above general formula (1), wherein R ¹ is a lower alkoxycarbonyl group, R ² is a carboxy group, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. Derivatives or salts thereof.

(706) A benzene derivative represented by the above general formula (1) wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a carboxy group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group; Its salt.

(707) A benzene derivative represented by the above formula (1), wherein R ¹ is a lower alkoxycarbonyl group, R ² is a carboxy group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group; Its salt.

(708) R ¹ is a lower alkoxycarbonyl group, R ² is a carboxy group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group; Its salt.

(709) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ is a lower alkoxycarbonyl group, R ² is a carboxy group, and R ⁵ is a phenylthioureidocarbonyl group.

(710) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ is a lower alkoxycarbonyl group, R ² is a carboxy group, and R ⁵ is a pyridylthioureidocarbonyl group.

(711) The above-mentioned formula (1) wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a carboxy group, and R ⁵ represents a lower alkylthioureidocarbonyl group.
Or a salt thereof.

(712) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ is a lower alkoxycarbonyl group, R ² is a carboxy group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(713) R ¹ represents a lower alkoxycarbonyl group, R ² represents a carboxy group, and R ⁵ represents a group

[1165]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(714) R ¹ represents a lower alkoxycarbonyl group, R ² represents a carboxy group, and R ⁵ represents a group — (A
₄ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(715) R ¹ represents a lower alkoxycarbonyl group, R ² represents a carboxy group, and R ⁵ represents a group

[1169]

Embedded image

[1170] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(716) In the above formula (1), R ¹ represents a lower alkoxycarbonyl group, R ² represents a lower alkoxycarbonyl group, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. Benzene derivatives or salts thereof.

(717) Benzene represented by the above general formula (1), wherein R ¹ is a lower alkoxycarbonyl group, R ² is a lower alkoxycarbonyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. Derivatives or salts thereof.

(718) A benzene represented by the above general formula (1) wherein R ¹ is a lower alkoxycarbonyl group, R ² is a lower alkoxycarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. Derivatives or salts thereof.

(719) Benzene represented by the above formula (1), wherein R ¹ is a lower alkoxycarbonyl group, R ² is a lower alkoxycarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. Derivatives or salts thereof.

(720) A benzene derivative represented by the above general formula (1) wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a lower alkoxycarbonyl group, and R ⁵ is a phenylthioureidocarbonyl group, or salt.

(721) A benzene derivative represented by the above general formula (1) wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a lower alkoxycarbonyl group, and R ⁵ is a pyridylthioureidocarbonyl group, or a benzene derivative thereof. salt.

(722) A benzene derivative represented by the above general formula (1) wherein R ¹ is a lower alkoxycarbonyl group, R ² is a lower alkoxycarbonyl group, and R ⁵ is a lower alkylthioureidocarbonyl group, or salt.

(723) R ¹ is a lower alkoxycarbonyl group, R ² is a lower alkoxycarbonyl group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the above general formula (1) or salt.

(724) R ¹ represents a lower alkoxycarbonyl group, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a group

[1180]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(725) R ¹ represents a lower alkoxycarbonyl group, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a group — (A ₄ ) _r COOH (A ₄ and r are groups represented by the above general formula (1) The above general formula (1)
Or a salt thereof.

(726) R ¹ represents a lower alkoxycarbonyl group, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a group

[1184]

Embedded image

[1185] benzene derivative or a salt thereof (A ₆ and R ²⁴ are as defined in the general formula (1)) represented by the general formula is (1).

(727) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group. And R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(728) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group. Wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(729) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group. Or a salt thereof, wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, represented by the above general formula (1).

(730) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group. Or a salt thereof, wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, represented by the above general formula (1).

(731) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group. , A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a phenylthioureidocarbonyl group.

(732) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group. Wherein R ⁵ is a pyridylthioureidocarbonyl group or a benzene derivative represented by the above general formula (1) or a salt thereof.

(733) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group. Or a benzene derivative represented by the above general formula (1), wherein R ⁵ is a lower alkylthioureidocarbonyl group, or a salt thereof.

(734) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group. Or a benzene derivative represented by the above formula (1), wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group, or a salt thereof.

(735) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group. , R ⁵ is a group

[1195]

Embedded image

[1196] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(736) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group. , R ⁵ is a group — (A ₄ ) _r COOH (A ₄ and r
Is the same as defined in the general formula (1)) or a benzene derivative represented by the general formula (1) or a salt thereof.

(737) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group. , R ⁵ is a group

[1199]

Embedded image

(1200) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the above general formula (1).

(738) R ¹ represents a lower alkoxycarbonyl group, R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl A benzene derivative represented by the general formula (1) or a salt thereof.

(739) R ¹ represents a lower alkoxycarbonyl group, R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(740) R ¹ represents a lower alkoxycarbonyl group, R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(741) R ¹ represents a lower alkoxycarbonyl group, R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(742) The above general formula wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a phenylthioureidocarbonyl group. A benzene derivative represented by the formula (1) or a salt thereof.

(743) The above general formula wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridylthioureidocarbonyl group. A benzene derivative represented by the formula (1) or a salt thereof.

(744) The above general formula wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a lower alkylthioureidocarbonyl group. A benzene derivative represented by the formula (1) or a salt thereof.

(745) The above general formula wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group. A benzene derivative represented by the formula (1) or a salt thereof.

(746) R ¹ represents a lower alkoxycarbonyl group, R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[1210]

Embedded image

[1211] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(747) R ¹ represents a lower alkoxycarbonyl group, R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group — (A ₄ ) _r COOH ( A ₄ and r are the same as defined in the general formula (1).
Or a salt thereof.

(748) R ¹ represents a lower alkoxycarbonyl group, R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[1214]

Embedded image

[1215] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(749) R ¹ represents a lower alkoxycarbonyl group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl A benzene derivative represented by the general formula (1) or a salt thereof.

(750) R ¹ represents a lower alkoxycarbonyl group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(751) R ¹ represents a lower alkoxycarbonyl group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(752) R ¹ represents a lower alkoxycarbonyl group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(753) The above general formula wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a phenylthioureidocarbonyl group. A benzene derivative represented by the formula (1) or a salt thereof.

(754) The above general formula wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridylthioureidocarbonyl group. A benzene derivative represented by the formula (1) or a salt thereof.

(755) The above general formula wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a lower alkylthioureidocarbonyl group. A benzene derivative represented by the formula (1) or a salt thereof.

(756) The above general formula wherein R ¹ represents a lower alkoxycarbonyl group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group. A benzene derivative represented by the formula (1) or a salt thereof.

(757) R ¹ represents a lower alkoxycarbonyl group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[1225]

Embedded image

[1226] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(758) R ¹ represents a lower alkoxycarbonyl group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group — (A ₄ ) _r COOH ( A ₄ and r are those represented by the general formula (1)
The benzene derivative represented by the general formula (1) or a salt thereof.

(759) R ¹ represents a lower alkoxycarbonyl group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[1229]

Embedded image

[1230] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(760) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R
¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group represented by the above general formula (1). Benzene derivatives or salts thereof.

(761) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R
¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) Benzene derivatives or salts thereof.

(762) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R
¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.
Or a salt thereof.

(763) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R
¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1). Benzene derivatives or salts thereof.

(764) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R
¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), wherein R ⁵ is a phenylthioureidocarbonyl group, and the benzene derivative represented by the general formula (1) Or a salt thereof.

(765) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R
¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), wherein R ⁵ is a pyridylthioureidocarbonyl group, a benzene derivative represented by the general formula (1) Or a salt thereof.

(766) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R
¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), wherein R ⁵ is a lower alkylthioureidocarbonyl group, and the benzene derivative represented by the general formula (1) Or a salt thereof.

(767) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R
¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a pyridylaminocarbonyl lower alkoxy group represented by the general formula (1) Or a salt thereof.

(768) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R
¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a group

[1240]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(769) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R
¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), wherein R ⁵ is a group — (A ₄ ) _r COOH
(A ₄ and r are the same as defined in the general formula (1))
A benzene derivative represented by the general formula (1) or a salt thereof.

(770) R ¹ represents a lower alkoxycarbonyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R
¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a group

[1244]

Embedded image

[1245] benzene derivative or a salt thereof (A ₆ and R ²⁴ are as defined in the general formula (1)) represented by the general formula is (1).

(771) R ¹ represents a hydrogen atom, and R ² represents a group

[1247]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group represented by the above formula (1) Derivatives or salts thereof.

(772) R ¹ represents a hydrogen atom, and R ² represents a group

[1250]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) or Its salt.

(773) R ¹ represents a hydrogen atom, and R ² represents a group

[1253]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) or Its salt.

(774) R ¹ represents a hydrogen atom, and R ² represents a group

[1256]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.
Or a salt thereof.

(775) R ¹ represents a hydrogen atom, and R ² represents a group

[1259]

Embedded image

[1260] A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above general formula (1), and R ⁵ is a phenylthioureidocarbonyl group.

(776) R ¹ represents a hydrogen atom, and R ² represents a group

[1262]

Embedded image

[1263] A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above formula (1), and R ⁵ is a pyridylthioureidocarbonyl group.

(777) R ¹ represents a hydrogen atom, and R ² represents a group

[1265]

Embedded image

[1266] A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above formula (1), and R ⁵ is a lower alkylthioureidocarbonyl group.

(778) R ¹ represents a hydrogen atom, and R ² represents a group

[1268]

Embedded image

[1268] A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above formula (1), and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(779) R ¹ represents a hydrogen atom, and R ² represents a group

[1271]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), wherein R ⁵ is a group

[1273]

Embedded image

[1274] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(780) R ¹ represents a hydrogen atom, and R ² represents a group

[1276]

Embedded image

[1277] (R⁸And m are in the general formula (1)
R)^FiveIs a group-(A _Four)_rCOOH
(A_FourAnd r are the same as defined in the above general formula (1))
A benzene derivative represented by the general formula (1)
Its salt.

(781) R ¹ represents a hydrogen atom, and R ² represents a group

[1279]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), wherein R ⁵ is a group

[1281]

Embedded image

[1282] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(782) R ¹ is a hydrogen atom, and R ² is a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group Wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(783) 1,2,3,4-tetrahydroquinolylcarbonyl group in which R ¹ represents a hydrogen atom and R ² may have a substituent selected from the group consisting of a lower alkyl group and an oxo group Wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(784) R ¹ represents a hydrogen atom, and R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group Wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(785) R ¹ represents a hydrogen atom, and R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group Wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(786) 1,2,3,4-tetrahydroquinolylcarbonyl group in which R ¹ represents a hydrogen atom and R ² may have a substituent selected from the group consisting of a lower alkyl group and an oxo group Wherein R ⁵ is a phenylthioureidocarbonyl group or a benzene derivative represented by the general formula (1) or a salt thereof.

(787) R ¹ represents a hydrogen atom, and R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group Wherein R ⁵ is a pyridylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(788) R ¹ represents a hydrogen atom, and R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group Wherein R ⁵ is a lower alkylthioureidocarbonyl group or a salt thereof represented by the above general formula (1).

(789) R ¹ represents a hydrogen atom, and R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group Wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(790) R ¹ represents a hydrogen atom, and R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group And R ⁵ is a group

[1292]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(791) R ¹ is a hydrogen atom, and R ² is a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group And R ⁵ represents a group — (A ₄ ) _r C
A benzene derivative represented by the general formula (1) or a salt thereof, which is OOH (A ₄ and r are the same as defined in the general formula (1)).

(792) R ¹ represents a hydrogen atom, and R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a substituent selected from the group consisting of a lower alkyl group and an oxo group And R ⁵ is a group

[1296]

Embedded image

[1297] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(793) A benzene derivative represented by the above general formula (1), wherein R ¹ is a hydrogen atom, R ² is a pyridylcarbonyl group, and R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(794) The above formula (1) wherein R ¹ represents a hydrogen atom, R ² represents a pyridylcarbonyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.
Or a salt thereof.

(795) A benzene derivative represented by the above general formula (1) wherein R ¹ is a hydrogen atom, R ² is a pyridylcarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative thereof. salt.

(796) R ¹ is a hydrogen atom, R ² is a pyridylcarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1), salt.

(797) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ represents a hydrogen atom, R ² represents a pyridylcarbonyl group, and R ⁵ represents a phenylthioureidocarbonyl group.

(798) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ represents a hydrogen atom, R ² represents a pyridylcarbonyl group, and R ⁵ represents a pyridylthioureidocarbonyl group.

(799) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ represents a hydrogen atom, R ² represents a pyridylcarbonyl group, and R ⁵ is a lower alkylthioureidocarbonyl group.

(800) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ represents a hydrogen atom, R ² represents a pyridylcarbonyl group, and R ⁵ represents a pyridylaminocarbonyl lower alkoxy group.

(801) R ¹ represents a hydrogen atom, R ² represents a pyridylcarbonyl group, and R ⁵ represents a group

[1307]

Embedded image

[1308] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(802) R ¹ represents a hydrogen atom, R ² represents a pyridylcarbonyl group, and R ⁵ represents a group — (A ₄ ) _r COO
A benzene derivative represented by the general formula (1) or a salt thereof, which is H (A ₄ and r are the same as defined in the general formula (1)).

(803) R ¹ represents a hydrogen atom, R ² represents a pyridylcarbonyl group, and R ⁵ represents a group

[1311]

Embedded image

[1312] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(804) The above general formula wherein R ¹ represents a hydrogen atom, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by (1) or a salt thereof.

(805) In the above formula (1), R ¹ represents a hydrogen atom, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(806) In the above general formula (1), R ¹ represents a hydrogen atom, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(807) In the above formula (1), R ¹ represents a hydrogen atom, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(808) In the formula (1), R ¹ represents a hydrogen atom, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a phenylthioureidocarbonyl group. Or a salt thereof.

(809) In the above formula (1), R ¹ represents a hydrogen atom, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a pyridylthioureidocarbonyl group. Or a salt thereof.

(810) In the above formula (1), R ¹ represents a hydrogen atom, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a lower alkylthioureidocarbonyl group. Or a salt thereof.

(811) In the above formula (1), R ¹ represents a hydrogen atom, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a pyridylaminocarbonyl lower alkoxy group. Or a salt thereof.

(812) R ¹ represents a hydrogen atom, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a group

[1322]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(813) R ¹ represents a hydrogen atom, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a group — (A ₄ ) _r COOH (A ₄ and r are A benzene derivative represented by the general formula (1) or a salt thereof, which is the same as defined in the general formula (1).

(814) R ¹ represents a hydrogen atom, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a group

[1326]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(815) R ¹ represents a hydrogen atom, R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a lower alkoxy group. A benzene derivative represented by the above general formula (1), which is a lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(816) R ¹ represents a hydrogen atom, R ² represents a cycloalkylcarbonyl group sometimes having an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a hydroxyl group-substituted group. Formula (1) which is an aminocarbonyl-substituted lower alkenyl group
Or a salt thereof.

(817) R ¹ represents a hydrogen atom, R ² represents a cycloalkylcarbonyl group sometimes having an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a pyridyl substitution A benzene derivative represented by the general formula (1), which is an aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(818) R ¹ represents a hydrogen atom, R ² represents a cycloalkylcarbonyl group sometimes having an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a pyrimidyl substitution A benzene derivative represented by the general formula (1), which is an aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(819) R ¹ represents a hydrogen atom, R ² represents a cycloalkylcarbonyl group sometimes having an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a phenylthio group A benzene derivative represented by the general formula (1), which is an ureidocarbonyl group, or a salt thereof.

(820) R ¹ represents a hydrogen atom, R ² represents a cycloalkylcarbonyl group sometimes having an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a pyridylthio group A benzene derivative represented by the general formula (1), which is an ureidocarbonyl group, or a salt thereof.

(821) R ¹ represents a hydrogen atom, R ² represents a cycloalkylcarbonyl group sometimes having an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a lower alkylthio group. A benzene derivative represented by the general formula (1), which is an ureidocarbonyl group, or a salt thereof.

(822) R ¹ represents a hydrogen atom, R ² represents a cycloalkylcarbonyl group sometimes having an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a pyridylaminocarbonyl A benzene derivative represented by the formula (1), which is a lower alkoxy group, or a salt thereof.

(823) R ¹ represents a hydrogen atom, R ² represents a cycloalkylcarbonyl group sometimes having an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a group

[1337]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(824) R ¹ represents a hydrogen atom, R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a group- (A ₄ ) _r COO
A benzene derivative represented by the general formula (1) or a salt thereof, which is H (A ₄ and r are the same as defined in the general formula (1)).

(825) R ¹ represents a hydrogen atom, R ² represents a cycloalkylcarbonyl group sometimes having an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a group

[1341]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(826) In the above formula (1), R ¹ represents a hydrogen atom, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. Benzene derivatives or salts thereof.

(827) A benzene derivative represented by the above general formula (1) wherein R ¹ represents a hydrogen atom, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(828) A benzene derivative represented by the above general formula (1), wherein R ¹ represents a hydrogen atom, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(829) A benzene derivative represented by the above general formula (1) wherein R ¹ represents a hydrogen atom, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(830) The above formula (1) wherein R ¹ represents a hydrogen atom, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a phenylthioureidocarbonyl group.
Or a salt thereof.

(831) The above general formula (1) wherein R ¹ represents a hydrogen atom, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a pyridylthioureidocarbonyl group.
Or a salt thereof.

(832) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ represents a hydrogen atom, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a lower alkylthioureido carbonyl group. .

(833) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ represents a hydrogen atom, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a pyridylaminocarbonyl lower alkoxy group. .

(834) R ¹ represents a hydrogen atom, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a group

[1352]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(835) R ¹ represents a hydrogen atom, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a group
(A ₄ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(836) R ¹ represents a hydrogen atom, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a group

[1356]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(837) R ¹ represents a hydrogen atom, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl A benzene derivative represented by the general formula (1) or a salt thereof.

(838) R ¹ represents a hydrogen atom, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(839) R ¹ represents a hydrogen atom, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(840) R ¹ represents a hydrogen atom, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(841) The above general formula wherein R ¹ represents a hydrogen atom, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ is a phenylthioureidocarbonyl group. A benzene derivative represented by the formula (1) or a salt thereof.

(842) The above general formula wherein R ¹ represents a hydrogen atom, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ is a pyridylthioureidocarbonyl group. A benzene derivative represented by the formula (1) or a salt thereof.

(843) The above general formula wherein R ¹ represents a hydrogen atom, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a lower alkylthioureidocarbonyl group. A benzene derivative represented by the formula (1) or a salt thereof.

(844) The above general formula wherein R ¹ represents a hydrogen atom, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group. A benzene derivative represented by the formula (1) or a salt thereof.

(845) R ¹ represents a hydrogen atom, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a group

[1368]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(846) R ¹ represents a hydrogen atom, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a group-
(A ₄ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(847) R ¹ represents a hydrogen atom, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a group

[1371]

Embedded image

(137) A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(848) A benzene derivative represented by the above general formula (1) wherein R ¹ represents a hydrogen atom, R ² represents a thienylcarbonyl group, and R ⁵ represents a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(849) The above general formula (1) wherein R ¹ represents a hydrogen atom, R ² represents a thienylcarbonyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.
Or a salt thereof.

(850) A benzene derivative represented by the above general formula (1) wherein R ¹ represents a hydrogen atom, R ² represents a thienylcarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative thereof. salt.

(851) A benzene derivative represented by the above general formula (1) wherein R ¹ is a hydrogen atom, R ² is a thienylcarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, salt.

(852) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ represents a hydrogen atom, R ² represents a thienylcarbonyl group, and R ⁵ represents a phenylthioureidocarbonyl group.

(853) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ represents a hydrogen atom, R ² represents a thienylcarbonyl group, and R ⁵ represents a pyridylthioureidocarbonyl group.

(854) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ represents a hydrogen atom, R ² represents a thienylcarbonyl group, and R ⁵ represents a lower alkylthioureidocarbonyl group.

(855) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ represents a hydrogen atom, R ² represents a thienylcarbonyl group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(856) R ¹ represents a hydrogen atom, R ² represents a thienylcarbonyl group, and R ⁵ represents a group

[1382]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(857) R ¹ represents a hydrogen atom, R ² represents a thienylcarbonyl group, and R ⁵ represents a group — (A ₄ ) _r COO
A benzene derivative represented by the general formula (1) or a salt thereof, which is H (A ₄ and r are the same as defined in the general formula (1)).

(858) R ¹ represents a hydrogen atom, R ² represents a thienylcarbonyl group, and R ⁵ represents a group

[1386]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(859) A benzene derivative represented by the above general formula (1), wherein R ¹ is a hydrogen atom, R ² is a carboxy group, and R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group; Its salt.

(860) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ represents a hydrogen atom, R ² represents a carboxy group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. .

(861) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ is a hydrogen atom, R ² is a carboxy group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. .

(862) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ is a hydrogen atom, R ² is a carboxy group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. .

(863) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ represents a hydrogen atom, R ² represents a carboxy group, and R ⁵ represents a phenylthioureidocarbonyl group.

(864) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ represents a hydrogen atom, R ² represents a carboxy group, and R ⁵ represents a pyridylthioureidocarbonyl group.

(865) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ represents a hydrogen atom, R ² represents a carboxy group, and R ⁵ is a lower alkylthioureidocarbonyl group.

(866) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ represents a hydrogen atom, R ² represents a carboxy group, and R ⁵ represents a pyridylaminocarbonyl lower alkoxy group.

(867) R ¹ represents a hydrogen atom, R ² represents a carboxy group, and R ⁵ represents a group

[1397]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(868) R ¹ represents a hydrogen atom, R ² represents a carboxy group, and R ⁵ represents a group — (A ₄ ) _r COOH (A ₄ and r are the same as defined in the above formula (1)) A benzene derivative represented by the general formula (1) or a salt thereof.

(869) R ¹ represents a hydrogen atom, R ² represents a carboxy group, and R ⁵ represents a group

[1401]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(870) Benzene represented by the above general formula (1) wherein R ¹ represents a hydrogen atom, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. Derivatives or salts thereof.

(871) A benzene derivative represented by the above general formula (1) wherein R ¹ represents a hydrogen atom, R ² represents a lower alkoxycarbonyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group; Its salt.

(872) A benzene derivative represented by the above general formula (1) wherein R ¹ represents a hydrogen atom, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group; Its salt.

(873) R ¹ is a hydrogen atom, R ² is a lower alkoxycarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group; Its salt.

(874) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ represents a hydrogen atom, R ² represents a lower alkoxycarbonyl group, and R ⁵ is a phenylthioureidocarbonyl group.

(875) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ represents a hydrogen atom, R ² represents a lower alkoxycarbonyl group, and R ⁵ is a pyridylthioureidocarbonyl group.

(876) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ represents a hydrogen atom, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a lower alkylthioureidocarbonyl group.

(877) The above general formula (1) wherein R ¹ represents a hydrogen atom, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a pyridylaminocarbonyl lower alkoxy group.
Or a salt thereof.

(878) R ¹ represents a hydrogen atom, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a group

[1412]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(879) R ¹ represents a hydrogen atom, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a group — (A ₄ ) _r
A benzene derivative represented by the general formula (1), which is COOH (A ₄ and r are the same as defined in the general formula (1)), or a salt thereof.

(880) R ¹ represents a hydrogen atom, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a group

[1416]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(881) R ¹ represents a hydrogen atom; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(882) R ¹ represents a hydrogen atom; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(883) R ¹ represents a hydrogen atom, R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group, A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(884) R ¹ represents a hydrogen atom, R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group, A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(885) R ¹ represents a hydrogen atom, R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group, A benzene derivative represented by the general formula (1), wherein ⁵ is a phenylthioureidocarbonyl group, or a salt thereof.

(886) R ¹ represents a hydrogen atom, and R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; A benzene derivative represented by the above formula (1), wherein ⁵ is a pyridylthioureidocarbonyl group, or a salt thereof.

(887) R ¹ represents a hydrogen atom, and R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group. A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a lower alkylthioureidocarbonyl group.

(888) R ¹ represents a hydrogen atom; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; A benzene derivative represented by the above general formula (1) or a salt thereof, wherein ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(889) R ¹ represents a hydrogen atom; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; ⁵ based

[1427]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(890) R ¹ represents a hydrogen atom, R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group, ⁵ is a group-(A ₄ ) _r COOH (A ₄ and r are the above-mentioned general formula (1)
The benzene derivative represented by the general formula (1) or a salt thereof.

(891) R ¹ represents a hydrogen atom, R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group, ⁵ based

[1431]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(892) R ¹ represents a hydrogen atom, R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(893) wherein R ¹ is a hydrogen atom, R ² is an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group; A benzene derivative represented by the general formula (1) or a salt thereof.

[1435] (894) R ¹ represents a hydrogen atom, an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, wherein R ⁵ is pyridyl substituted aminocarbonyl substituted lower alkenyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(895) wherein R ¹ is a hydrogen atom, R ² is an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group; A benzene derivative represented by the general formula (1) or a salt thereof.

(896) The above general formula ( ¹ ) wherein R ¹ represents a hydrogen atom, R ² represents an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a phenylthioureidocarbonyl group. A benzene derivative represented by 1) or a salt thereof.

(897) The above general formula ( ¹ ) wherein R ¹ represents a hydrogen atom, R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a pyridylthioureidocarbonyl group. A benzene derivative represented by 1) or a salt thereof.

(898) The above general formula ( ¹ ) wherein R ¹ represents a hydrogen atom, R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a lower alkylthioureidocarbonyl group. A benzene derivative represented by 1) or a salt thereof.

(899) In the above formula (R), R ¹ represents a hydrogen atom, R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a pyridylaminocarbonyl lower alkoxy group. 1)
Or a salt thereof.

(900) R ¹ represents a hydrogen atom, R ² represents an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[1442]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(901) R ¹ represents a hydrogen atom, R ² represents an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group — (A ₄ ) _r
A benzene derivative represented by the general formula (1), which is COOH (A ₄ and r are the same as defined in the general formula (1)), or a salt thereof.

(902) R ¹ represents a hydrogen atom, R ² represents an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[1446]

Embedded image

[1447] benzene derivative or a salt thereof (A ₆ and R ²⁴ are as defined in the general formula (1)) represented by the general formula is (1).

(903) R ¹ represents a hydrogen atom, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(904) wherein R ¹ represents a hydrogen atom, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group; A benzene derivative represented by the general formula (1) or a salt thereof.

(905) wherein R ¹ represents a hydrogen atom, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group; General formula (1)
Or a salt thereof.

(906) wherein R ¹ represents a hydrogen atom, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group; A benzene derivative represented by the general formula (1) or a salt thereof.

(907) The above general formula ( ¹ ) wherein R ¹ represents a hydrogen atom, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a phenylthioureidocarbonyl group. A benzene derivative represented by 1) or a salt thereof.

(908) In the above general formula ( ¹ ), R ¹ represents a hydrogen atom, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a pyridylthioureidocarbonyl group. A benzene derivative represented by 1) or a salt thereof.

(909) The above general formula ( ¹ ) wherein R ¹ represents a hydrogen atom, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a lower alkylthioureidocarbonyl group. A benzene derivative represented by 1) or a salt thereof.

(910) The above general formula ( ¹ ) wherein R ¹ represents a hydrogen atom, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a pyridylaminocarbonyl lower alkoxy group. A benzene derivative represented by 1) or a salt thereof.

(911) R ¹ represents a hydrogen atom, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[1457]

Embedded image

[1458] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(912) R ¹ represents a hydrogen atom, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group — (A ₄ ) _r COOH
(A ₄ and r are the same as defined in the general formula (1))
A benzene derivative represented by the general formula (1) or a salt thereof.

(913) R ¹ represents a hydrogen atom, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[1461]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(914) R ¹ represents a hydrogen atom and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R
¹² is the same as defined in the general formula (1)), and a benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(915) R ¹ represents a hydrogen atom and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R
¹² is the same as defined in the general formula (1)),
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(916) R ¹ represents a hydrogen atom, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R
¹² is the same as defined in the general formula (1)),
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(917) R ¹ represents a hydrogen atom, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R
¹² is the same as defined in the general formula (1)),
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(918) R ¹ represents a hydrogen atom, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R
¹² is the same as defined in the general formula (1)),
A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a phenylthioureidocarbonyl group.

(919) R ¹ represents a hydrogen atom, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R
¹² is the same as defined in the general formula (1)),
A benzene derivative represented by the above general formula (1), wherein R ⁵ is a pyridylthioureidocarbonyl group, or a salt thereof.

(920) R ¹ represents a hydrogen atom, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R
¹² is the same as defined in the general formula (1)),
A benzene derivative represented by the above general formula (1), wherein R ⁵ is a lower alkylthioureidocarbonyl group, or a salt thereof.

(921) R ¹ represents a hydrogen atom, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R
¹² is the same as defined in the general formula (1)),
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(922) R ¹ represents a hydrogen atom, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R
¹² is the same as defined in the general formula (1)),
R ⁵ based

[1472]

Embedded image

147. A benzene derivative represented by the above general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the above general formula (1).

(923) R ¹ represents a hydrogen atom, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R
¹² is the same as defined in the general formula (1)),
R ⁵ is a group - (A _{4) r} COOH benzene derivative or a salt thereof (A ₄ and r are as defined in the general formula (1)) represented by the general formula is (1).

(924) R ¹ represents a hydrogen atom, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹ and R
¹² is the same as defined in the general formula (1)),
R ⁵ based

[1476]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(925) R ¹ represents a lower alkanoyl group, and R ² represents a group

[1479]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group represented by the above formula (1) Derivatives or salts thereof.

(926) R ¹ represents a lower alkanoyl group, and R ² represents a group

[1482]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) or Its salt.

(927) R ¹ represents a lower alkanoyl group, and R ² represents a group

[1485]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) or Its salt.

(928) R ¹ represents a lower alkanoyl group, and R ² represents a group

[1488]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.
Or a salt thereof.

(929) R ¹ represents a lower alkanoyl group, and R ² represents a group

[1491]

Embedded image

[1492] A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above formula (1), and R ⁵ is a phenylthioureidocarbonyl group.

(930) R ¹ represents a lower alkanoyl group, and R ² represents a group

[1494]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and a benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyridylthioureidocarbonyl group.

(931) R ¹ represents a lower alkanoyl group, and R ² represents a group

[1497]

Embedded image

[1498] A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above formula (1), and R ⁵ is a lower alkylthioureidocarbonyl group.

(932) R ¹ represents a lower alkanoyl group, and R ² represents a group

[1500]

Embedded image

A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above general formula (1), and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(933) R ¹ represents a lower alkanoyl group, and R ² represents a group

[1503]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), wherein R ⁵ is a group

[1505]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(934) R ¹ represents a lower alkanoyl group, and R ² represents a group

[1508]

Embedded image

[1509] (R⁸And m are in the general formula (1)
R)^FiveIs a group-(A _Four)_rCOOH
(A_FourAnd r are the same as defined in the above general formula (1))
A benzene derivative represented by the general formula (1)
Its salt.

(935) R ¹ represents a lower alkanoyl group, and R ² represents a group

[1511]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), wherein R ⁵ is a group

[1513]

Embedded image

(15) A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(936) R ¹ represents a lower alkanoyl group, and R ² may have a substituent selected from the group consisting of a lower alkyl group and an oxo group.
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein the benzene derivative represents a tetrahydroquinolylcarbonyl group and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group;

(937) R ¹ represents a lower alkanoyl group, and R ² may have a substituent selected from the group consisting of a lower alkyl group and an oxo group.
A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a tetrahydroquinolylcarbonyl group and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group;

(938) R ¹ represents a lower alkanoyl group, and R ² may have a substituent selected from the group consisting of a lower alkyl group and an oxo group.
A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a tetrahydroquinolylcarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(939) R ¹ represents a lower alkanoyl group, and R ² may have a substituent selected from the group consisting of a lower alkyl group and an oxo group.
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein the benzene derivative represents a tetrahydroquinolylcarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group;

(940) R ¹ represents a lower alkanoyl group, and R ² may have a substituent selected from the group consisting of a lower alkyl group and an oxo group.
A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a tetrahydroquinolylcarbonyl group and R ⁵ is a phenylthioureidocarbonyl group.

(941) R ¹ represents a lower alkanoyl group, and R ² may have a substituent selected from the group consisting of a lower alkyl group and an oxo group.
A benzene derivative represented by the general formula (1) or a salt thereof, which represents a tetrahydroquinolylcarbonyl group and wherein R ⁵ is a pyridylthioureidocarbonyl group;

(942) R ¹ represents a lower alkanoyl group, and R ² may have a substituent selected from the group consisting of a lower alkyl group and an oxo group.
A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a tetrahydroquinolylcarbonyl group, wherein R ⁵ is a lower alkylthioureidocarbonyl group;

(943) R ¹ represents a lower alkanoyl group, and R ² may have a substituent selected from the group consisting of a lower alkyl group and an oxo group.
A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a tetrahydroquinolylcarbonyl group and R ⁵ is a pyridylaminocarbonyl lower alkoxy group;

(944) R ¹ represents a lower alkanoyl group, and R ² may have a substituent selected from the group consisting of a lower alkyl group and an oxo group.
A tetrahydroquinolylcarbonyl group, wherein R ⁵ is a group

[1524]

Embedded image

(15) A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(945) R ¹ represents a lower alkanoyl group, and R ² may have a substituent selected from the group consisting of a lower alkyl group and an oxo group.
A benzene represented by the above general formula (1), which represents -tetrahydroquinolylcarbonyl group, wherein R ⁵ is a group-(A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)); Derivatives or salts thereof.

(946) R ¹ represents a lower alkanoyl group, and R ² may have a substituent selected from the group consisting of a lower alkyl group and an oxo group.
A tetrahydroquinolylcarbonyl group, wherein R ⁵ is a group

[1528]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(947) A benzene represented by the above formula (1), wherein R ¹ is a lower alkanoyl group, R ² is a pyridylcarbonyl group, and R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group. Derivatives or salts thereof.

(948) R ¹ is a lower alkanoyl group, R ² is a pyridylcarbonyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group; Its salt.

(949) R ¹ is a lower alkanoyl group, R ² is a pyridylcarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group; Its salt.

(950) R ¹ is a lower alkanoyl group, R ² is a pyridylcarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group; Its salt.

(951) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ represents a lower alkanoyl group, R ² represents a pyridylcarbonyl group, and R ⁵ is a phenylthioureidocarbonyl group.

(952) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ is a lower alkanoyl group, R ² is a pyridylcarbonyl group, and R ⁵ is a pyridylthioureidocarbonyl group.

(953) The above formula (1) wherein R ¹ represents a lower alkanoyl group, R ² represents a pyridylcarbonyl group, and R ⁵ is a lower alkylthioureidocarbonyl group.
Or a salt thereof.

(954) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ is a lower alkanoyl group, R ² is a pyridylcarbonyl group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(955) R ¹ represents a lower alkanoyl group, R ² represents a pyridylcarbonyl group, and R ⁵ represents a group

[1539]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(956) R ¹ represents a lower alkanoyl group, R ² represents a pyridylcarbonyl group, and R ⁵ represents a group — (A
₄ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(957) R ¹ represents a lower alkanoyl group, R ² represents a pyridylcarbonyl group, and R ⁵ represents a group

[1543]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(958) The above general formula wherein R ¹ represents a lower alkanoyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the formula (1) or a salt thereof.

(959) The above general formula ( ¹ ) wherein R ¹ is a lower alkanoyl group, R ² is a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by 1) or a salt thereof.

(960) In the above formula ( ¹ ), R ¹ represents a lower alkanoyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by 1) or a salt thereof.

(961) The above general formula ( ¹ ) wherein R ¹ is a lower alkanoyl group, R ² is a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. 1)
Or a salt thereof.

(962) In the above formula (1), R ¹ represents a lower alkanoyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a phenylthioureidocarbonyl group. The represented benzene derivative or a salt thereof.

(963) In the above formula (1), R ¹ represents a lower alkanoyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a pyridylthioureidocarbonyl group. The represented benzene derivative or a salt thereof.

(964) In the above formula (1), R ¹ represents a lower alkanoyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a lower alkylthioureidocarbonyl group. The represented benzene derivative or a salt thereof.

(965) In the above formula (1), R ¹ represents a lower alkanoyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(966) R ¹ represents a lower alkanoyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a group

[1554]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(967) R ¹ represents a lower alkanoyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a group — (A ₄ ) _r COOH
(A ₄ and r are the same as defined in the general formula (1))
A benzene derivative represented by the general formula (1) or a salt thereof.

(968) R ¹ represents a lower alkanoyl group, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a group

[1558]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

[1560] (969) R ¹ is a lower alkanoyl group, a cycloalkylcarbonyl group which may have an amino lower alkyl group R ² is which may have a lower alkoxycarbonyl group as a substituent, R ⁵ is a lower A benzene derivative represented by the above formula (1), which is an alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(970) R ¹ represents a lower alkanoyl group, R ² represents a cycloalkylcarbonyl group sometimes having an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a hydroxyl group A benzene derivative represented by the above formula (1), which is a substituted aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(971) R ¹ represents a lower alkanoyl group, R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a pyridyl group A benzene derivative represented by the above formula (1), which is a substituted aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(972) R ¹ represents a lower alkanoyl group, R ² represents a cycloalkylcarbonyl group sometimes having an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents pyrimidyl A benzene derivative represented by the above formula (1), which is a substituted aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(973) R ¹ represents a lower alkanoyl group, R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a phenyl group A benzene derivative represented by the general formula (1), which is a thioureidocarbonyl group, or a salt thereof.

(974) R ¹ represents a lower alkanoyl group, R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a pyridyl group A benzene derivative represented by the general formula (1), which is a thioureidocarbonyl group, or a salt thereof.

(975) R ¹ represents a lower alkanoyl group, R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a lower alkyl group. A benzene derivative represented by the general formula (1), which is an alkylthioureidocarbonyl group, or a salt thereof.

(976) R ¹ represents a lower alkanoyl group, R ² represents a cycloalkylcarbonyl group sometimes having an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a pyridylamino group. A benzene derivative represented by the general formula (1), which is a carbonyl lower alkoxy group, or a salt thereof.

(977) R ¹ represents a lower alkanoyl group, R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a group

[1569]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(978) R ¹ represents a lower alkanoyl group, R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a group −
(A ₄ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(979) R ¹ represents a lower alkanoyl group, R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a group

[1573]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(980) Formula (1) wherein R ¹ represents a lower alkanoyl group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. Benzene derivatives or salts thereof.

(981) Benzene represented by the above general formula (1) wherein R ¹ is a lower alkanoyl group, R ² is a benzoyloxy lower alkanoyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group Derivatives or salts thereof.

(982) Benzene represented by the above general formula (1) wherein R ¹ represents a lower alkanoyl group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. Derivatives or salts thereof.

(983) R ¹ is a lower alkanoyl group, R ² is a benzoyloxy lower alkanoyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group; Derivatives or salts thereof.

(984) A benzene derivative represented by the above general formula (1) wherein R ¹ represents a lower alkanoyl group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a phenylthioureidocarbonyl group, or a benzene derivative thereof. salt.

(985) A benzene derivative represented by the above general formula (1) wherein R ¹ represents a lower alkanoyl group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a pyridylthioureidocarbonyl group, or a benzene derivative thereof. salt.

(986) A benzene derivative represented by the above formula (1), wherein R ¹ is a lower alkanoyl group, R ² is a benzoyloxy lower alkanoyl group, and R ⁵ is a lower alkylthioureidocarbonyl group, salt.

(987) R ¹ is a lower alkanoyl group, R ² is a benzoyloxy lower alkanoyl group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the above general formula (1), or salt.

(988) R ¹ represents a lower alkanoyl group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a group

[1584]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(989) R ¹ represents a lower alkanoyl group, R ² represents a benzoyloxy lower alkanoyl group, R ⁵ represents a group — (A ₄ ) _r COOH (A ₄ and r are The above general formula (1)
Or a salt thereof.

(990) R ¹ represents a lower alkanoyl group, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a group

[1588]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(991) R ¹ represents a lower alkanoyl group; R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring;
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(992) R ¹ represents a lower alkanoyl group; R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring;
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(993) R ¹ represents a lower alkanoyl group; R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring;
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(994) R ¹ represents a lower alkanoyl group; R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring;
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(995) R ¹ represents a lower alkanoyl group; R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring;
A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a phenylthioureidocarbonyl group.

(996) R ¹ represents a lower alkanoyl group; R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring;
A benzene derivative represented by the above general formula (1), wherein R ⁵ is a pyridylthioureidocarbonyl group, or a salt thereof.

(997) R ¹ represents a lower alkanoyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring,
A benzene derivative represented by the above general formula (1), wherein R ⁵ is a lower alkylthioureidocarbonyl group, or a salt thereof.

(998) R ¹ represents a lower alkanoyl group; R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring;
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(999) R ¹ represents a lower alkanoyl group; R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring;
R ⁵ based

[1599]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1000) R ¹ represents a lower alkanoyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a group — (A ₄ ) _r COOH Wherein A ₄ and r are the same as defined in the general formula (1).
Or a salt thereof.

(1001) R ¹ represents a lower alkanoyl group, R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on a phenyl ring, and R ⁵ represents a group

[1603]

Embedded image

[1604] benzene derivative or a salt thereof (A ₆ and R ²⁴ are as defined in the general formula (1)) represented by the general formula is (1).

(1002) Benzene represented by the above formula (1), wherein R ¹ is a lower alkanoyl group, R ² is a thienylcarbonyl group, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. Derivatives or salts thereof.

(1003) A benzene derivative represented by the above general formula (1) wherein R ¹ represents a lower alkanoyl group, R ² represents a thienylcarbonyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group; Its salt.

(1004) A benzene derivative represented by the above general formula (1) wherein R ¹ is a lower alkanoyl group, R ² is a thienylcarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group; Its salt.

(1005) A benzene derivative represented by the above general formula (1) wherein R ¹ is a lower alkanoyl group, R ² is a thienylcarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group; Its salt.

(1006) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ represents a lower alkanoyl group, R ² represents a thienylcarbonyl group, and R ⁵ represents a phenylthioureidocarbonyl group.

(1007) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ represents a lower alkanoyl group, R ² represents a thienylcarbonyl group, and R ⁵ represents a pyridylthioureidocarbonyl group.

(1008) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ represents a lower alkanoyl group, R ² represents a thienylcarbonyl group, and R ⁵ represents a lower alkylthioureidocarbonyl group.

(1009) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ is a lower alkanoyl group, R ² is a thienylcarbonyl group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(1010) R ¹ represents a lower alkanoyl group, R ² represents a thienylcarbonyl group, and R ⁵ represents a group

[1614]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1011) R ¹ represents a lower alkanoyl group, R ² represents a thienylcarbonyl group, and R ⁵ represents a group-
(A ₄ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(1012) R ¹ represents a lower alkanoyl group, R ² represents a thienylcarbonyl group, and R ⁵ represents a group

[1618]

Embedded image

[1619] benzene derivative or a salt thereof (A ₆ and R ²⁴ are as defined in the general formula (1)) represented by the general formula is (1).

(1013) A benzene derivative represented by the above formula (1), wherein R ¹ is a lower alkanoyl group, R ² is a carboxy group, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group Or a salt thereof.

(1014) A benzene derivative represented by the above general formula (1) wherein R ¹ is a lower alkanoyl group, R ² is a carboxy group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, salt.

(1015) A benzene derivative represented by the above formula (1) wherein R ¹ is a lower alkanoyl group, R ² is a carboxy group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, salt.

(1016) A benzene derivative represented by the above general formula (1) wherein R ¹ is a lower alkanoyl group, R ² is a carboxy group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, salt.

(1017) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ is a lower alkanoyl group, R ² is a carboxy group, and R ⁵ is a phenylthioureidocarbonyl group.

(1018) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ is a lower alkanoyl group, R ² is a carboxy group, and R ⁵ is a pyridylthioureidocarbonyl group.

(1019) A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ¹ is a lower alkanoyl group, R ² is a carboxy group, and R ⁵ is a lower alkylthioureidocarbonyl group.

(1020) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ is a lower alkanoyl group, R ² is a carboxy group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(1021) R ¹ represents a lower alkanoyl group, R ² represents a carboxy group, and R ⁵ represents a group

[1629]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1022) R ¹ represents a lower alkanoyl group, R ² represents a carboxy group, and R ⁵ represents a group — (A ₄ ) _r C
A benzene derivative represented by the general formula (1) or a salt thereof, which is OOH (A ₄ and r are the same as defined in the general formula (1)).

(1023) R ¹ represents a lower alkanoyl group, R ² represents a carboxy group, and R ⁵ represents a group

[1633]

Embedded image

[1634] benzene derivative or a salt thereof (A ₆ and R ²⁴ are as defined in the general formula (1)) represented by the general formula is (1).

(1024) Formula (1) wherein R ¹ is a lower alkanoyl group, R ² is a lower alkoxycarbonyl group, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. Benzene derivatives or salts thereof.

(1025) A benzene derivative represented by the above general formula (1), wherein R ¹ is a lower alkanoyl group, R ² is a lower alkoxycarbonyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group Or a salt thereof.

(1026) A benzene derivative represented by the above general formula (1) wherein R ¹ is a lower alkanoyl group, R ² is a lower alkoxycarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group Or a salt thereof.

(1027) A benzene derivative represented by the above general formula (1) wherein R ¹ is a lower alkanoyl group, R ² is a lower alkoxycarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group Or a salt thereof.

(1028) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ is a lower alkanoyl group, R ² is a lower alkoxycarbonyl group, and R ⁵ is a phenylthioureidocarbonyl group .

(1029) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ is a lower alkanoyl group, R ² is a lower alkoxycarbonyl group, and R ⁵ is a pyridylthioureidocarbonyl group .

(1030) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ is a lower alkanoyl group, R ² is a lower alkoxycarbonyl group, and R ⁵ is a lower alkylthioureidocarbonyl group. .

(1031) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ represents a lower alkanoyl group, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a pyridylaminocarbonyl lower alkoxy group. .

(1032) R ¹ represents a lower alkanoyl group, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a group

[1644]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1033) R ¹ represents a lower alkanoyl group, R ² represents a lower alkoxycarbonyl group, R ⁵ represents a group — (A ₄ ) _r COOH (A ₄ and r represent the above-mentioned general formula (1)
The benzene derivative represented by the general formula (1) or a salt thereof.

(1034) R ¹ represents a lower alkanoyl group, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a group

[1648]

Embedded image

[1649] benzene derivative or a salt thereof (A ₆ and R ²⁴ are as defined in the general formula (1)) represented by the general formula is (1).

(1035) R ¹ represents a lower alkanoyl group; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; Wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group;
Or a salt thereof.

(1036) R ¹ represents a lower alkanoyl group; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1037) R ¹ represents a lower alkanoyl group; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1038) R ¹ represents a lower alkanoyl group; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1039) R ¹ represents a lower alkanoyl group; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a phenylthioureidocarbonyl group.

(1040) R ¹ represents a lower alkanoyl group; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; A benzene derivative represented by the above general formula (1), wherein R ⁵ is a pyridylthioureidocarbonyl group, or a salt thereof.

(1041) R ¹ represents a lower alkanoyl group; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; A benzene derivative represented by the above general formula (1), wherein R ⁵ is a lower alkylthioureidocarbonyl group, or a salt thereof.

(1042) R ¹ represents a lower alkanoyl group; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(1043) R ¹ represents a lower alkanoyl group; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; R ⁵ based

[1659]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1044) R ¹ represents a lower alkanoyl group; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a group — (A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(1045) R ¹ represents a lower alkanoyl group; R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; R ⁵ based

[1663]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

[1665] (1046) R ¹ is a lower alkanoyl group, an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, R ⁵
Is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

[1666] (1047) R ¹ is a lower alkanoyl group, an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, R ⁵
Is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

[1667] (1048) R ¹ is a lower alkanoyl group, an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, R ⁵
Is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[1668] (1049) R ¹ is a lower alkanoyl group, an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, R ⁵
Is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[1669] (1050) R ¹ is a lower alkanoyl group, an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, R ⁵
Is a phenylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[1670] (1051) R ¹ is a lower alkanoyl group, an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, R ⁵
Is a pyridylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[1671] (1052) R ¹ is a lower alkanoyl group, an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, R ⁵
Is a lower alkylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[1672] (1053) R ¹ is a lower alkanoyl group, an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, R ⁵
Is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[1673] (1054) R ¹ is a lower alkanoyl group, an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, R ⁵
Is based

[1674]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

[1676] (1055) R ¹ is a lower alkanoyl group, an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, R ⁵
Is a group-(A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)) or a benzene derivative represented by the general formula (1) or a salt thereof.

[1677] (1056) R ¹ is a lower alkanoyl group, an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, R ⁵
Is based

[1678]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(1057) R ¹ represents a lower alkanoyl group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(1058) R ¹ is a lower alkanoyl group, R ² is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(1059) R ¹ is a lower alkanoyl group, R ² is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(1060) R ¹ is a lower alkanoyl group, R ² is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(1061) The above general formula wherein R ¹ is a lower alkanoyl group, R ² is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a phenylthioureidocarbonyl group A benzene derivative represented by (1) or a salt thereof.

(1062) The above general formula wherein R ¹ represents a lower alkanoyl group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a pyridylthioureidocarbonyl group. A benzene derivative represented by (1) or a salt thereof.

(1063) The above general formula wherein R ¹ represents a lower alkanoyl group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a lower alkylthioureidocarbonyl group. A benzene derivative represented by (1) or a salt thereof.

(1064) The above general formula wherein R ¹ represents a lower alkanoyl group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group. A benzene derivative represented by (1) or a salt thereof.

(1065) R ¹ represents a lower alkanoyl group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[1689]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1066) R ¹ represents a lower alkanoyl group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group
(A ₄ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(1067) R ¹ represents a lower alkanoyl group, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[1693]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(1068) R ¹ represents a lower alkanoyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ ,
p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.
Or a salt thereof.

(1069) R ¹ represents a lower alkanoyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ ,
p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) or a benzene derivative thereof. salt.

(1070) R ¹ represents a lower alkanoyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ ,
p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) or a benzene derivative thereof. salt.

(1071) R¹Is a lower alkanoyl group
And R^TwoIs a group -CO- (A₁)_p-NR ¹¹R¹²(A₁,
p, R¹¹And R¹²Is the same as the definition in the general formula (1).
The same), R^FiveIs pyrimidyl-substituted aminocarbonyl
A substituted lower alkenyl group represented by the above general formula (1)
Benzene derivatives or salts thereof.

(1072) R ¹ represents a lower alkanoyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ ,
p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and the benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a phenylthioureidocarbonyl group.

(1073) R ¹ represents a lower alkanoyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ ,
p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and the benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyridylthioureidocarbonyl group.

(1074) R ¹ represents a lower alkanoyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ ,
p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and the benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a lower alkylthioureidocarbonyl group.

(1075) R ¹ represents a lower alkanoyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ ,
p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and the benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(1076) R ¹ represents a lower alkanoyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ ,
p, R ¹¹ and R ¹² are the same as defined in the general formula (1), and R ⁵ is a group

[1704]

Embedded image

[1705] benzene derivative or a salt thereof ^{_{(A 4, r, R 17}} , R 18 and R ¹⁹ are as defined in the general formula (1)) represented by the general formula is (1).

(1077) R ¹ represents a lower alkanoyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ ,
p, R ¹¹ and R ¹² are the same as defined in the general formula (1), and R ⁵ is a group — (A ₄ ) _r COOH (A ₄ and r
Is the same as defined in the general formula (1)) or a benzene derivative represented by the general formula (1) or a salt thereof.

(1078) R ¹ represents a lower alkanoyl group, and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ ,
p, R ¹¹ and R ¹² are the same as defined in the general formula (1), and R ⁵ is a group

[1708]

Embedded image

[1709] benzene derivative or a salt thereof (A ₆ and R ²⁴ are as defined in the general formula (1)) represented by the general formula is (1).

(1079) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is

[1711]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group represented by the above formula (1) Derivatives or salts thereof.

(1080) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² represents a group

[1714]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) or Its salt.

(1081) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² represents a group

[1717]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) or Its salt.

(1082) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² represents a group

[1720]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.
Or a salt thereof.

(1083) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² represents a group

[1723]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and the benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a phenylthioureidocarbonyl group.

(1084) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² represents a group

[1726]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and the benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyridylthioureidocarbonyl group.

(1085) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is

[1729]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and the benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a lower alkylthioureidocarbonyl group.

(1086) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² represents a group

[1732]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and the benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(1087) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² represents a group

[1735]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), and R ⁵ is a group

[1737]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1088) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is

[1740]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), wherein R ⁵ is a group — (A ₄ ) _r COOH
(A ₄ and r are the same as defined in the general formula (1))
A benzene derivative represented by the general formula (1) or a salt thereof.

(1089) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² represents a group

[1743]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), wherein R ⁵ is a group

[1745]

Embedded image

A benzene derivative represented by the above general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the above general formula (1).

(1090) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent A benzene derivative represented by the above general formula (1), wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have salt.

(1091) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent A benzene derivative represented by the above general formula (1) or a salt thereof, wherein the benzene derivative is a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group;

(1092) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, wherein the benzene derivative is a 1,2,3,4-tetrahydroquinolylcarbonyl group;

(1093) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, wherein the benzene derivative is a 1,2,3,4-tetrahydroquinolylcarbonyl group;

(1094) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative is a 1,2,3,4-tetrahydroquinolylcarbonyl group, wherein R ⁵ is a phenylthioureidocarbonyl group;

(1095) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative is a 1,2,3,4-tetrahydroquinolylcarbonyl group, and R ⁵ is a pyridylthioureidocarbonyl group.

(1096) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative is a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have R ⁵ and R ⁵ is a lower alkylthioureidocarbonyl group.

(1097) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent which may have a 1,2,3,4-tetrahydroquinolyl indicates a carbonyl group, a benzene derivative represented by the general formula wherein R ⁵ is pyridyl aminocarbonyl-lower alkoxy group (1).

(1098) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent which may have a shows a 1,2,3,4-tetrahydroquinolyl group, R ⁵ is a group

[1756]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1099) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent Wherein R ⁵ is a group — (A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1100) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent which may have a shows a 1,2,3,4-tetrahydroquinolyl group, R ⁵ is a group

[1760]

Embedded image

[1761] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(1101) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a pyridylcarbonyl group, and R ⁵ represents a lower alkoxy lower alkoxyaminocarbonyl A benzene derivative represented by the general formula (1), which is a substituted lower alkenyl group, or a salt thereof.

(1102) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a pyridylcarbonyl group, and R ⁵ represents a hydroxyl-substituted aminocarbonyl-substituted lower group. A benzene derivative represented by the general formula (1), which is an alkenyl group, or a salt thereof.

(1103) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a pyridylcarbonyl group, and R ⁵ represents a pyridyl-substituted aminocarbonyl-substituted lower group A benzene derivative represented by the general formula (1), which is an alkenyl group, or a salt thereof.

(1104) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² is a pyridylcarbonyl group, R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower group A benzene derivative represented by the general formula (1), which is an alkenyl group, or a salt thereof.

(1105) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² is a pyridylcarbonyl group, R ⁵ is a phenylthioureidocarbonyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(1106) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² is a pyridylcarbonyl group, R ⁵ is a pyridylthioureidocarbonyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(1107) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a pyridylcarbonyl group, and R ⁵ represents a lower alkylthioureidocarbonyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(1108) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² is a pyridylcarbonyl group, R ⁵ is a pyridylaminocarbonyl lower alkoxy group A benzene derivative represented by the general formula (1) or a salt thereof.

(1109) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a pyridylcarbonyl group, and R ⁵ represents a group

[1771]

Embedded image

( ¹⁷⁷ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1110) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a pyridylcarbonyl group, and R ⁵ represents a group — (A ₄ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(1111) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a pyridylcarbonyl group, and R ⁵ represents a group

[1775]

Embedded image

[1776] benzene derivative or a salt thereof (A ₆ and R ²⁴ are as defined in the general formula (1)) represented by the general formula is (1).

(1112) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring; R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent; A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(1113) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring; R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent; A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1114) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring; R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent; A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1115) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring; R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent; A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1116) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, Wherein R ⁵ is a phenylthioureidocarbonyl group;
Or a salt thereof.

(1117) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, R ⁵ is a pyridylthioureidocarbonyl group of the above general formula (1)
Or a salt thereof.

(1118) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, A benzene derivative represented by the above general formula (1), wherein R ⁵ is a lower alkylthioureidocarbonyl group, or a salt thereof.

(1119) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring; R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent; A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(1120) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring; R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent; R ⁵ based

[1786]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1121) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring; R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent; R ⁵ is a group
(A ₄ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(1122) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring; R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent; R ⁵ based

[1790]

Embedded image

[1791] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(1123) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is an amino-lower alkyl which may have a lower alkoxycarbonyl group as a substituent A benzene derivative represented by the above general formula (1) or a salt thereof, wherein the benzene derivative represents a cycloalkylcarbonyl group which may have a group, and R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(1124) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is an amino-lower alkyl which may have a lower alkoxycarbonyl group as a substituent A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a cycloalkylcarbonyl group which may have a group, and wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1125) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is an amino lower alkyl which may have a lower alkoxycarbonyl group as a substituent. A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a cycloalkylcarbonyl group which may have a group, and wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1126) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is an amino-lower alkyl which may have a lower alkoxycarbonyl group as a substituent A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a cycloalkylcarbonyl group which may have a group, and wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1127) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is an amino-lower alkyl which may have a lower alkoxycarbonyl group as a substituent A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a cycloalkylcarbonyl group which may have a group, and wherein R ⁵ is a phenylthioureidocarbonyl group.

(1128) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is an amino-lower alkyl group which may have a lower alkoxycarbonyl group as a substituent A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a cycloalkylcarbonyl group which may have a group, and R ⁵ is a pyridylthioureidocarbonyl group.

(1129) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is an amino-lower alkyl which may have a lower alkoxycarbonyl group as a substituent A benzene derivative represented by the general formula (1) or a salt thereof, which represents a cycloalkylcarbonyl group which may have a group, and wherein R ⁵ is a lower alkylthioureidocarbonyl group.

(1130) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is an amino-lower alkyl which may have a lower alkoxycarbonyl group as a substituent A benzene derivative represented by the above general formula (1) or a salt thereof, wherein the benzene derivative represents a cycloalkylcarbonyl group which may have a group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(1131) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is an amino-lower alkyl group which may have a lower alkoxycarbonyl group as a substituent A cycloalkylcarbonyl group which may have a group, wherein R ⁵ is a group

[1801]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1132) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is an amino-lower alkyl which may have a lower alkoxycarbonyl group as a substituent A cycloalkylcarbonyl group which may have a group, wherein R ⁵ is a group — (A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)); The represented benzene derivative or a salt thereof.

(1133) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is an amino lower alkyl which may have a lower alkoxycarbonyl group as a substituent. A cycloalkylcarbonyl group which may have a group, wherein R ⁵ is a group

[1805]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1134) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a lower alkoxy lower alkoxy group A benzene derivative represented by the general formula (1), which is an aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(1135) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a hydroxyl-substituted aminocarbonyl A benzene derivative represented by the general formula (1), which is a substituted lower alkenyl group, or a salt thereof.

(1136) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a pyridyl-substituted aminocarbonyl A benzene derivative represented by the general formula (1), which is a substituted lower alkenyl group, or a salt thereof.

(1137) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a pyrimidyl-substituted aminocarbonyl A benzene derivative represented by the general formula (1), which is a substituted lower alkenyl group, or a salt thereof.

(1138) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents phenylthioureidocarbonyl A benzene derivative represented by the general formula (1) or a salt thereof.

(1139) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a pyridylthioureidocarbonyl A benzene derivative represented by the general formula (1) or a salt thereof.

(1140) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a lower alkylthioureidocarbonyl A benzene derivative represented by the general formula (1) or a salt thereof.

(1141) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents pyridylaminocarbonyl lower alkoxy A benzene derivative represented by the general formula (1) or a salt thereof.

(1142) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a group

[1816]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1143) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a group-(A ₄ ) _r COOH (A ₄
And r are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(1144) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a group

[1820]

Embedded image

[1821] benzene derivative or a salt thereof (A ₆ and R ²⁴ are as defined in the general formula (1)) represented by the general formula is (1).

(1145) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² may have a lower alkoxy group as a substituent on the phenyl ring A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a phenoxycarbonyl group and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(1146) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² may have a lower alkoxy group as a substituent on the phenyl ring A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a phenoxycarbonyl group and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1147) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² may have a lower alkoxy group as a substituent on the phenyl ring A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a phenoxycarbonyl group and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1148) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² may have a lower alkoxy group as a substituent on the phenyl ring A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a phenoxycarbonyl group and wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1149) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² may have a lower alkoxy group as a substituent on the phenyl ring A benzene derivative represented by the general formula (1) or a salt thereof, which represents a phenoxycarbonyl group and R ⁵ is a phenylthioureidocarbonyl group.

(1150) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² may have a lower alkoxy group as a substituent on the phenyl ring A benzene derivative represented by the general formula (1) or a salt thereof, which represents a phenoxycarbonyl group and R ⁵ is a pyridylthioureidocarbonyl group.

(1151) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on a piperidine ring, and R ² may have a lower alkoxy group as a substituent on a phenyl ring A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a phenoxycarbonyl group and wherein R ⁵ is a lower alkylthioureidocarbonyl group.

(1152) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² may have a lower alkoxy group as a substituent on the phenyl ring A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a phenoxycarbonyl group and wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(1153) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² may have a lower alkoxy group as a substituent on the phenyl ring A phenoxycarbonyl group, wherein R ⁵ is a group

[1831]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1154) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² may have a lower alkoxy group as a substituent on the phenyl ring A phenoxycarbonyl group, wherein R ⁵ is a group — (A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1), or salt.

(1155) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² may have a lower alkoxy group as a substituent on the phenyl ring A phenoxycarbonyl group, wherein R ⁵ is a group

[1835]

Embedded image

[1836] benzene derivative or a salt thereof (A ₆ and R ²⁴ are as defined in the general formula (1)) represented by the general formula is (1).

(1156) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² is a thienylcarbonyl group, R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl A benzene derivative represented by the general formula (1), which is a substituted lower alkenyl group, or a salt thereof.

(1157) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² is a thienylcarbonyl group, R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower group A benzene derivative represented by the general formula (1), which is an alkenyl group, or a salt thereof.

(1158) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² is a thienylcarbonyl group, R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower group A benzene derivative represented by the general formula (1), which is an alkenyl group, or a salt thereof.

(1159) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a thienylcarbonyl group, and R ⁵ represents a pyrimidyl-substituted aminocarbonyl-substituted lower group. A benzene derivative represented by the general formula (1), which is an alkenyl group, or a salt thereof.

(1160) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² is a thienylcarbonyl group, R ⁵ is a phenylthioureidocarbonyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(1161) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² is a thienylcarbonyl group, R ⁵ is a pyridylthioureidocarbonyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(1162) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a thienylcarbonyl group, and R ⁵ represents a lower alkylthioureidocarbonyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(1163) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² is a thienylcarbonyl group, R ⁵ is a pyridylaminocarbonyl lower alkoxy group A benzene derivative represented by the general formula (1) or a salt thereof.

(1164) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a thienylcarbonyl group, and R ⁵ represents a group

[1846]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1165) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a thienylcarbonyl group, and R ⁵ represents a group — (A ₄ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1))

(1166) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a thienylcarbonyl group, and R ⁵ represents a group

[1850]

Embedded image

[1851] benzene derivative or a salt thereof (A ₆ and R ²⁴ are as defined in the general formula (1)) represented by the general formula is (1).

[1852] (1167) R ¹ represents a piperidinylcarbonyl group which may have lower alkyl group as a substituent on the piperidine ring, R ² represents a carboxy group, R ⁵
Is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

[1853] (1168) shows a piperidinylcarbonyl group which may R ¹ has a lower alkyl substituent on the piperidine ring, R ² represents a carboxy group, R ⁵
Is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

[1854] (1169) shows a piperidinylcarbonyl group which may R ¹ has a lower alkyl substituent on the piperidine ring, R ² represents a carboxy group, R ⁵
Is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[1855] (1170) shows a piperidinylcarbonyl group which may R ¹ has a lower alkyl substituent on the piperidine ring, R ² represents a carboxy group, R ⁵
Is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1171) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a carboxy group, and R ^{5 represents}
Is a phenylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[1857] (1172) shows a piperidinylcarbonyl group which may R ¹ has a lower alkyl substituent on the piperidine ring, R ² represents a carboxy group, R ⁵
Is a pyridylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[1858] (1173) shows a piperidinylcarbonyl group which may R ¹ has a lower alkyl substituent on the piperidine ring, R ² represents a carboxy group, R ⁵
Is a lower alkylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[1859] (1174) shows a piperidinylcarbonyl group which may R ¹ has a lower alkyl substituent on the piperidine ring, R ² represents a carboxy group, R ⁵
Is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the general formula (1) or a salt thereof.

[1860] (1175) shows a piperidinylcarbonyl group which may R ¹ has a lower alkyl substituent on the piperidine ring, R ² represents a carboxy group, R ⁵
Is based

[1861]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

[1863] (1176) shows a piperidinylcarbonyl group which may R ¹ has a lower alkyl substituent on the piperidine ring, R ² represents a carboxy group, R ⁵
Is a group-(A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)) or a benzene derivative represented by the general formula (1) or a salt thereof.

[1864] (1177) shows a piperidinylcarbonyl group which may R ¹ has a lower alkyl substituent on the piperidine ring, R ² represents a carboxy group, R ⁵
Is based

[1865]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(1178) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² is a lower alkoxycarbonyl group, R ⁵ is a lower alkoxy lower alkoxyamino A benzene derivative represented by the above formula (1), which is a carbonyl-substituted lower alkenyl group, or a salt thereof.

(1179) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² is a lower alkoxycarbonyl group, R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted group A benzene derivative represented by the general formula (1), which is a lower alkenyl group, or a salt thereof.

(1180) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² is a lower alkoxycarbonyl group, R ⁵ is a pyridyl-substituted aminocarbonyl-substituted group A benzene derivative represented by the general formula (1), which is a lower alkenyl group, or a salt thereof.

(1181) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² is a lower alkoxycarbonyl group, R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted group A benzene derivative represented by the general formula (1), which is a lower alkenyl group, or a salt thereof.

(1182) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a phenylthioureidocarbonyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(1183) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a pyridylthioureidocarbonyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(1184) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a lower alkylthioureidocarbonyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(1185) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a pyridylaminocarbonyl lower alkoxy group A benzene derivative represented by the general formula (1) or a salt thereof.

(1186) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a group

[1876]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1187) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a group — (A ₄ A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(1188) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a group

[1880]

Embedded image

[1881] benzene derivative or a salt thereof (A ₆ and R ²⁴ are as defined in the general formula (1)) represented by the general formula is (1).

(1189) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² represents a lower alkoxycarbonyl group or a phenyl lower alkoxycarbonyl group as a substituent A benzene derivative represented by the above general formula (1) or a salt thereof, wherein the benzene derivative represents a pyrrolidinylcarbonyl group which may have a group selected from the group consisting of R ⁵ and R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(1190) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a lower alkoxycarbonyl group or a phenyl lower alkoxycarbonyl group as a substituent A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a pyrrolidinylcarbonyl group which may have a group selected from the group consisting of R 1 and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1891) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a lower alkoxycarbonyl group or a phenyl lower alkoxycarbonyl group as a substituent A pyrrolidinylcarbonyl group which may have a group selected from the above, wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group;
Or a salt thereof.

(1192) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a lower alkoxycarbonyl group or a phenyl lower alkoxycarbonyl group as a substituent A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a pyrrolidinylcarbonyl group which may have a group selected from the group consisting of R 1 and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

[1886] (1193) R ¹ represents a piperidinylcarbonyl group which may have lower alkyl group as a substituent on the piperidine ring, R ² is a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group the group consisting of a substituent A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a pyrrolidinylcarbonyl group which may have a group selected from the group consisting of R 1 and R ⁵ is a phenylthioureidocarbonyl group.

(1194) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² represents a lower alkoxycarbonyl group or a phenyl lower alkoxycarbonyl group as a substituent A benzene derivative represented by the above general formula (1) or a salt thereof, wherein the benzene derivative represents a pyrrolidinylcarbonyl group which may have a group selected from the group consisting of R, and R ⁵ is a pyridylthioureidocarbonyl group.

(1195) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group as a substituent A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a pyrrolidinylcarbonyl group which may have a group selected from the group consisting of R ⁵ and R ⁵ is a lower alkylthioureidocarbonyl group.

(1196) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a lower alkoxycarbonyl group or a phenyl lower alkoxycarbonyl group as a substituent A benzene derivative represented by the above general formula (1) or a salt thereof, wherein the benzene derivative represents a pyrrolidinylcarbonyl group which may have a group selected from R ⁵ and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(1197) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² represents a lower alkoxycarbonyl group or a phenyl lower alkoxycarbonyl group as a substituent indicates pyrrolidinylcarbonyl group which may have a more chosen group, R ⁵ is a group

[1891]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1198) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a lower alkoxycarbonyl group or a phenyl lower alkoxycarbonyl group as a substituent A pyrrolidinylcarbonyl group which may have a group selected from the group consisting of: R ⁵ represents a group — (A ₄ ) _r COOH
(A ₄ and r are the same as defined in the general formula (1))
A benzene derivative represented by the general formula (1) or a salt thereof.

(1199) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on a piperidine ring, and R ² represents a lower alkoxycarbonyl group or a phenyl lower alkoxycarbonyl group as a substituent indicates pyrrolidinylcarbonyl group which may have a more chosen group, R ⁵ is a group

[1895]

Embedded image

[1896] benzene derivative or a salt thereof (A ₆ and R ²⁴ are as defined in the general formula (1)) represented by the general formula is (1).

(1200) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is an amino-lower alkoxycarbonyl which may have a lower alkyl group as a substituent A benzene derivative represented by the above formula (1), wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(1201) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is an amino-lower alkoxycarbonyl which may have a lower alkyl group as a substituent A benzene derivative represented by the above formula (1), wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(1202) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is an amino-lower alkoxycarbonyl which may have a lower alkyl group as a substituent A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1203) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1204) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent A benzene derivative represented by the above general formula (1), wherein R ⁵ is a phenylthioureidocarbonyl group, or a salt thereof.

(1205) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is an amino-lower alkoxycarbonyl which may have a lower alkyl group as a substituent A benzene derivative represented by the above general formula (1), wherein R ⁵ is a pyridylthioureidocarbonyl group, or a salt thereof.

(1206) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is an amino-lower alkoxycarbonyl which may have a lower alkyl group as a substituent A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a lower alkylthioureidocarbonyl group;

(1207) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group;

(1208) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is an amino-lower alkoxycarbonyl which may have a lower alkyl group as a substituent R ⁵ represents a group

[1906]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(1209) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is an amino-lower alkoxycarbonyl which may have a lower alkyl group as a substituent A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a group — (A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(1210) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is an amino-lower alkoxycarbonyl which may have a lower alkyl group as a substituent R ⁵ represents a group

[1910]

Embedded image

A benzene derivative represented by the above general formula (1) wherein A ₆ and R ²⁴ are the same as defined in the above general formula (1), or a salt thereof.

(1211) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent A benzene derivative represented by the above formula (1), wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(1212) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent A benzene derivative represented by the above formula (1), wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(1213) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a piperidinylcarbonyl which may have a lower alkyl group as a substituent A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1214) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a piperidinylcarbonyl which may have a lower alkyl group as a substituent A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1215) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a piperidinylcarbonyl which may have a lower alkyl group as a substituent A benzene derivative represented by the above general formula (1), wherein R ⁵ is a phenylthioureidocarbonyl group, or a salt thereof.

(1216) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a piperidinylcarbonyl which may have a lower alkyl group as a substituent A benzene derivative represented by the above general formula (1), wherein R ⁵ is a pyridylthioureidocarbonyl group, or a salt thereof.

(1217) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a lower alkylthioureidocarbonyl group;

(1218) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a piperidinylcarbonyl which may have a lower alkyl group as a substituent A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group;

(1219) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a piperidinylcarbonyl which may have a lower alkyl group as a substituent R ⁵ represents a group

[1921]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1220) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent Wherein R ⁵ is a group — (A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)).
Or a salt thereof.

(1221) R ¹ is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent R ⁵ represents a group

[1925]

Embedded image

A benzene derivative represented by the above general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(1222) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² represents a group —CO— (A ₁ ) _p —N
R ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(1223) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² represents a group —CO— (A ₁ ) _p —N
R ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group; Or a salt thereof.

(1224) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² represents a group —CO— (A ₁ ) _p —N
R ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group; Or a salt thereof.

(1225) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² represents a group —CO— (A ₁ ) _p —N
R ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group; Or a salt thereof.

(1226) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² represents a group —CO— (A ₁ ) _p —N
R ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and represented by the general formula (1) in which R ⁵ is a phenylthioureidocarbonyl group. Benzene derivatives or salts thereof.

(1227) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² represents a group —CO— (A ₁ ) _p —N
R ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and represented by the general formula (1) in which R ⁵ is a pyridylthioureidocarbonyl group. Benzene derivatives or salts thereof.

(1228) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² represents a group —CO— (A ₁ ) _p —N
R ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and represented by the general formula (1) in which R ⁵ is a lower alkylthioureidocarbonyl group. Benzene derivatives or salts thereof.

(1229) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² represents a group —CO— (A ₁ ) _p —N
R ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and represented by the general formula (1) in which R ⁵ is a pyridylaminocarbonyl lower alkoxy group. Benzene derivatives or salts thereof.

(1230) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² represents a group —CO— (A ₁ ) _p —N
R ^{11 represents} R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ represents a group

[1936]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1231) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² represents a group —CO— (A ₁ ) _p —N
R ¹¹ R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a group — (A ₄ )
A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(1232) R ¹ represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring, and R ² represents a group —CO— (A ₁ ) _p —N
R ^{11 represents} R ¹² (A ₁ , p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ represents a group

[1940]

Embedded image

[1941] A benzene derivative represented by the above general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the above general formula (1).

(1233) R ¹ represents a benzoyl group,
R ² is based

[1943]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group represented by the above formula (1). Derivatives or salts thereof.

(1234) R ¹ represents a benzoyl group,
R ² is based

[1946]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) or Its salt.

(1235) R ¹ represents a benzoyl group,
R ² is based

[1949]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) or Its salt.

(1236) R ¹ represents a benzoyl group,
R ² is based

[1952]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.
Or a salt thereof.

(1237) R ¹ represents a benzoyl group,
R ² is based

[1955]

Embedded image

A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above general formula (1), and R ⁵ is a phenylthioureidocarbonyl group.

(1238) R ¹ represents a benzoyl group,
R ² is based

[1958]

Embedded image

[1959] A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above general formula (1), and R ⁵ is a pyridylthioureidocarbonyl group.

(1239) R ¹ represents a benzoyl group,
R ² is based

[1961]

Embedded image

[1962] (R ⁸ and m are as defined in the general formula (1)) shows a benzene derivative or a salt thereof represented by the general formula R ⁵ is a lower alkyl thioureido group (1).

(1240) R ¹ represents a benzoyl group,
R ² is based

[1964]

Embedded image

A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ⁸ and m are the same as defined in the above formula (1), wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(1241) R ¹ represents a benzoyl group;
R ² is based

[1967]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), wherein R ⁵ is a group

[1969]

Embedded image

[1970] benzene derivative or a salt thereof ^{_{(A 4, r, R 17}} , R 18 and R ¹⁹ are as defined in the general formula (1)) represented by the general formula is (1).

(1242) R ¹ represents a benzoyl group,
R ² is based

[1972]

Embedded image

[1973] (R⁸And m are in the general formula (1)
R)^FiveIs a group-(A _Four)_rCOOH
(A_FourAnd r are the same as defined in the above general formula (1))
A benzene derivative represented by the general formula (1)
Its salt.

(1243) R ¹ represents a benzoyl group,
R ² is based

[1975]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), wherein R ⁵ is a group

[1977]

Embedded image

(196) A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(1244) R ¹ represents a benzoyl group,
R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent, and R ⁵ represents a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower group A benzene derivative represented by the general formula (1), which is an alkenyl group, or a salt thereof.

(1245) R ¹ represents a benzoyl group;
R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent, and R ⁵ represents a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(1246) R ¹ represents a benzoyl group,
R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent, and R ⁵ represents a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(1247) R ¹ represents a benzoyl group;
R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent, and R ⁵ represents a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(1248) R ¹ represents a benzoyl group,
R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent, and R ⁵ is a phenylthioureidocarbonyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(1249) R ¹ represents a benzoyl group;
R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent, and R ⁵ is a pyridylthioureidocarbonyl group; A benzene derivative represented by the general formula (1) or a salt thereof.

(1250) R ¹ represents a benzoyl group,
R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent, and R ⁵ is a lower alkylthioureidocarbonyl group; A benzene derivative represented by the general formula (1) or a salt thereof.

(1251) R ¹ represents a benzoyl group;
R ² represents a 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group; A benzene derivative represented by the general formula (1) or a salt thereof.

(1252) R ¹ represents a benzoyl group;
R ² represents a certain 1,2,3,4-tetrahydroquinolyl group which may have a group selected from the group consisting lower alkyl group and oxo group as a substituent, R ⁵ is a group

[1988]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1253) R ¹ represents a benzoyl group,
R ² represents a certain 1,2,3,4-tetrahydroquinolyl group which may have a group selected from the group consisting lower alkyl group and oxo group as a substituent, R ⁵ is a group -
(A ₄ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(1254) R ¹ represents a benzoyl group,
R ² represents a certain 1,2,3,4-tetrahydroquinolyl group which may have a group selected from the group consisting lower alkyl group and oxo group as a substituent, R ⁵ is a group

[1992]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(1255) R ¹ represents a benzoyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ² represents a pyridylcarbonyl group, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(1995) R ¹ represents a benzoyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ² represents a pyridylcarbonyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1257) R ¹ represents a benzoyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ² is a pyridylcarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1258) R ¹ represents a benzoyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ² represents a pyridylcarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1259) R ¹ represents a benzoyl group,
A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ² represents a pyridylcarbonyl group and R ⁵ is a phenylthioureidocarbonyl group.

(1260) R ¹ represents a benzoyl group,
A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ² represents a pyridylcarbonyl group and R ⁵ is a pyridylthioureidocarbonyl group.

(1261) R ¹ represents a benzoyl group;
A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ² represents a pyridylcarbonyl group, and R ⁵ is a lower alkylthioureidocarbonyl group.

(2001) R ¹ represents a benzoyl group,
R ² is a pyridylcarbonyl group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group in the above general formula (1)
Or a salt thereof.

(1263) R ¹ represents a benzoyl group,
R ² represents a pyridylcarbonyl group, and R ⁵ represents a group

[2003]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1264) R ¹ represents a benzoyl group,
R ² represents a pyridylcarbonyl group, and R ⁵ represents a group — (A ₄ ) _r
A benzene derivative represented by the general formula (1), which is COOH (A ₄ and r are the same as defined in the general formula (1)), or a salt thereof.

(1265) R ¹ represents a benzoyl group,
R ² represents a pyridylcarbonyl group, and R ⁵ represents a group

[2007]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(1266) R ¹ represents a benzoyl group,
A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(1267) R ¹ represents a benzoyl group;
A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1268) R ¹ represents a benzoyl group;
A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1269) R ¹ represents a benzoyl group,
A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1270) R ¹ represents a benzoyl group;
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a phenylthioureidocarbonyl group.

(1271) R ¹ represents a benzoyl group,
A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a pyridylthioureidocarbonyl group.

(1272) R ¹ represents a benzoyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a lower alkylthioureidocarbonyl group.

(1273) R ¹ represents a benzoyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(1274) R ¹ represents a benzoyl group,
A lower alkanoyl group which R ² which may have a hydroxyl group as a substituent, R ⁵ is a group

[2018]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), and a benzene derivative represented by the general formula (1) or a salt thereof.

(1275) R ¹ represents a benzoyl group,
R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a group — (A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)). A benzene derivative represented by the formula (1) or a salt thereof.

(1276) R ¹ represents a benzoyl group,
A lower alkanoyl group which R ² which may have a hydroxyl group as a substituent, R ⁵ is a group

[2022]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(1277) R ¹ represents a benzoyl group,
Wherein R ² is a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group; A benzene derivative represented by 1) or a salt thereof.

(1278) R ¹ represents a benzoyl group,
R ² is a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group; Or a salt thereof.

(1279) R ¹ represents a benzoyl group,
R ² is a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group; Or a salt thereof.

(1280) R ¹ represents a benzoyl group,
R ² is a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group; Or a salt thereof.

(1281) R ¹ represents a benzoyl group,
R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ is a phenylthioureidocarbonyl group represented by the general formula (1). Benzene derivatives or salts thereof.

(1282) R ¹ represents a benzoyl group,
R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ is a pyridylthioureidocarbonyl group represented by the general formula (1). Benzene derivatives or salts thereof.

(1283) R ¹ represents a benzoyl group,
R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ is a lower alkylthioureidocarbonyl group represented by the general formula (1). Benzene derivatives or salts thereof.

(1284) R ¹ represents a benzoyl group,
R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group represented by the general formula (1). Benzene derivatives or salts thereof.

(1285) R ¹ represents a benzoyl group,
R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a group

[2033]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), and a benzene derivative represented by the general formula (1) or a salt thereof.

(1286) R ¹ represents a benzoyl group,
R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a group — (A ₄ )
A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(1287) R ¹ represents a benzoyl group,
R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, and R ⁵ represents a group

[2037]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1288) R ¹ represents a benzoyl group,
R ² represents a benzoyloxy-lower alkanoyl group, R ⁵
Is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(1289) R ¹ represents a benzoyl group,
R ² represents a benzoyloxy-lower alkanoyl group, R ⁵
Is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(1290) R ¹ represents a benzoyl group,
R ² represents a benzoyloxy-lower alkanoyl group, R ⁵
Is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1291) R ¹ represents a benzoyl group,
R ² represents a benzoyloxy-lower alkanoyl group, R ⁵
Is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1292) R ¹ represents a benzoyl group,
R ² represents a benzoyloxy-lower alkanoyl group, R ⁵
Is a phenylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1293) R ¹ represents a benzoyl group,
R ² represents a benzoyloxy-lower alkanoyl group, R ⁵
Is a pyridylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1294) R ¹ represents a benzoyl group;
R ² represents a benzoyloxy-lower alkanoyl group, R ⁵
Is a lower alkylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1295) R ¹ represents a benzoyl group;
R ² represents a benzoyloxy-lower alkanoyl group, R ⁵
Is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1296) R ¹ represents a benzoyl group,
R ² represents a benzoyloxy-lower alkanoyl group, R ⁵
Is based

[2048]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1297) R ¹ represents a benzoyl group;
R ² represents a benzoyloxy-lower alkanoyl group, R ⁵
Is a group-(A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)) or a benzene derivative represented by the general formula (1) or a salt thereof.

(1298) R ¹ represents a benzoyl group;
R ² represents a benzoyloxy-lower alkanoyl group, R ⁵
Is based

[2052]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1299) R ¹ represents a benzoyl group,
R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, R ⁵
Is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(1300) R ¹ represents a benzoyl group;
R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, R ⁵
Is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(1301) R ¹ represents a benzoyl group,
R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, R ⁵
Is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1302) R ¹ represents a benzoyl group;
R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, R ⁵
Is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1303) R ¹ represents a benzoyl group;
R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, R ⁵
Is a phenylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1304) R ¹ represents a benzoyl group,
R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, R ⁵
Is a pyridylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1305) R ¹ represents a benzoyl group;
R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, R ⁵
Is a lower alkylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1306) R ¹ represents a benzoyl group,
R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, R ⁵
Is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1307) R ¹ represents a benzoyl group;
R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, R ⁵
Is based

[2063]

Embedded image

[2064] benzene derivative or a salt thereof ^{_{(A 4, r, R 17}} , R 18 and R ¹⁹ are as defined in the general formula (1)) represented by the general formula is (1).

(1308) R ¹ represents a benzoyl group,
R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, R ⁵
Is a group-(A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)) or a benzene derivative represented by the general formula (1) or a salt thereof.

(1309) R ¹ represents a benzoyl group,
R ² represents a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, R ⁵
Is based

[2067]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1310) R ¹ represents a benzoyl group;
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ² is a thienylcarbonyl group, and R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(1311) R ¹ represents a benzoyl group;
A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ² represents a thienylcarbonyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1312) R ¹ represents a benzoyl group;
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ² represents a thienylcarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1313) R ¹ represents a benzoyl group;
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ² is a thienylcarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1314) R ¹ represents a benzoyl group,
A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ² represents a thienylcarbonyl group and R ⁵ is a phenylthioureidocarbonyl group.

(1315) R ¹ represents a benzoyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ² represents a thienylcarbonyl group, and R ⁵ represents a pyridylthioureidocarbonyl group.

(1316) R ¹ represents a benzoyl group,
A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ² represents a thienylcarbonyl group, and R ⁵ is a lower alkylthioureidocarbonyl group.

(1317) R ¹ represents a benzoyl group;
Wherein R ² represents a thienylcarbonyl group, and R ⁵ represents a pyridylaminocarbonyl lower alkoxy group;
Or a salt thereof.

(1318) R ¹ represents a benzoyl group,
R ² represents a thienylcarbonyl group, and R ⁵ represents a group

[2078]

Embedded image

[2079] benzene derivative or a salt thereof ^{_{(A 4, r, R 17}} , R 18 and R ¹⁹ are as defined in the general formula (1)) represented by the general formula is (1).

(1319) R ¹ represents a benzoyl group,
R ² represents a thienylcarbonyl group, and R ⁵ represents a group — (A ₄ ) _r
A benzene derivative represented by the general formula (1), which is COOH (A ₄ and r are the same as defined in the general formula (1)), or a salt thereof.

(1320) R ¹ represents a benzoyl group,
R ² represents a thienylcarbonyl group, and R ⁵ represents a group

[2082]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1321) R ¹ represents a benzoyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ² represents a carboxy group, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(1322) R ¹ represents a benzoyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ² is a carboxy group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1323) R ¹ represents a benzoyl group,
Wherein R ² represents a carboxy group, and R ⁵ represents a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group;
Or a salt thereof.

(1324) R ¹ represents a benzoyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ² is a carboxy group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1325) R ¹ represents a benzoyl group,
A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ² represents a carboxy group and R ⁵ is a phenylthioureidocarbonyl group.

(1326) R ¹ represents a benzoyl group,
A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ² represents a carboxy group and R ⁵ is a pyridylthioureidocarbonyl group.

(1327) R ¹ represents a benzoyl group,
A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ² represents a carboxy group and R ⁵ is a lower alkylthioureidocarbonyl group.

(1328) R ¹ represents a benzoyl group,
A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ² represents a carboxy group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(1329) R ¹ represents a benzoyl group,
R ² represents a carboxy group, and R ⁵ represents a group

[2093]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the above formula (1)) or a benzene derivative represented by the formula (1) or a salt thereof.

(1330) R ¹ represents a benzoyl group;
R ² represents a carboxy group, and R ⁵ represents a group — (A ₄ ) _r COOH
(A ₄ and r are the same as defined in the general formula (1))
A benzene derivative represented by the general formula (1) or a salt thereof.

(1331) R ¹ represents a benzoyl group,
R ² represents a carboxy group, and R ⁵ represents a group

[2097]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1332) R ¹ represents a benzoyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ² represents a lower alkoxycarbonyl group, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(1333) R ¹ represents a benzoyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ² represents a lower alkoxycarbonyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1334) R ¹ represents a benzoyl group;
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ² is a lower alkoxycarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1335) R ¹ represents a benzoyl group;
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ² represents a lower alkoxycarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1336) R ¹ represents a benzoyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ² represents a lower alkoxycarbonyl group, and R ⁵ is a phenylthioureidocarbonyl group.

(1337) R ¹ represents a benzoyl group;
A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ² represents a lower alkoxycarbonyl group and R ⁵ is a pyridylthioureidocarbonyl group.

(1338) R ¹ represents a benzoyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ² represents a lower alkoxycarbonyl group, and R ⁵ is a lower alkylthioureidocarbonyl group.

(1339) R ¹ represents a benzoyl group,
A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ² represents a lower alkoxycarbonyl group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(1340) R ¹ represents a benzoyl group,
R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a group

[2108]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1341) R ¹ represents a benzoyl group;
R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a group-
(A ₄ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(1342) R ¹ represents a benzoyl group;
R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a group

[2112]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(1343) R ¹ represents a benzoyl group;
R ² represents a pyrrolidinylcarbonyl group which may have a group selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group as a substituent, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl substituted lower alkenyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(1344) R ¹ represents a benzoyl group,
R ² represents a pyrrolidinylcarbonyl group which may have a group selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group as a substituent, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the formula (1) or a salt thereof.

(1345) R ¹ represents a benzoyl group;
R ² represents a pyrrolidinylcarbonyl group which may have a group selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group as a substituent, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the formula (1) or a salt thereof.

(1346) R ¹ represents a benzoyl group,
R ² represents a pyrrolidinylcarbonyl group which may have a group selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group as a substituent, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the formula (1) or a salt thereof.

(1347) R ¹ represents a benzoyl group;
R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group, and R ⁵ is a phenylthioureidocarbonyl group. Or a salt thereof.

(1348) R ¹ represents a benzoyl group,
R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group, and R ⁵ is a pyridylthioureidocarbonyl group. Or a salt thereof.

(1349) R ¹ represents a benzoyl group,
R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group, and R ⁵ is a lower alkylthioureidocarbonyl group. Or a salt thereof.

(1350) R ¹ represents a benzoyl group,
R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group. Or a salt thereof.

(1351) R ¹ represents a benzoyl group;
R ² represents a certain pyrrolidinylcarbonyl group which may have a group selected from lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group the group consisting of a substituent group, R ⁵ is a group

[2123]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1352) R ¹ represents a benzoyl group,
R ² represents a pyrrolidinylcarbonyl group which may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group, and R ⁵ represents a group — (A ₄ ) _r COOH (A ₄ and r is the same as defined in the general formula (1)).
Or a salt thereof.

(1353) R ¹ represents a benzoyl group,
R ² represents a certain pyrrolidinylcarbonyl group which may have a group selected from lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group the group consisting of a substituent group, R ⁵ is a group

[2127]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(1354) R ¹ represents a benzoyl group,
R ² represents an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group; Its salt.

(1355) R ¹ represents a benzoyl group,
R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof. .

(1356) R ¹ represents a benzoyl group,
R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof. .

(1357) R ¹ represents a benzoyl group,
R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof. .

(1358) R ¹ represents a benzoyl group,
R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a phenylthioureidocarbonyl group;
Or a salt thereof.

(1359) R ¹ represents a benzoyl group,
R ² represents an amino-lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a pyridylthioureidocarbonyl group;
Or a salt thereof.

(1360) R ¹ represents a benzoyl group,
A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a lower alkylthioureidocarbonyl group.

(1361) R ¹ represents a benzoyl group,
A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(1362) R ¹ represents a benzoyl group,
R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[2138]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(1363) R ¹ represents a benzoyl group,
R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group-
(A ₄ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(1364) R ¹ represents a benzoyl group,
R ² represents an amino lower alkoxycarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[2142]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(1365) R ¹ represents a benzoyl group,
R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group represented by the general formula (1) or Its salt.

(1366) R ¹ represents a benzoyl group,
R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group or a benzene derivative represented by the above general formula (1) or a salt thereof. .

(1367) R ¹ represents a benzoyl group;
R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof. .

(1368) R ¹ represents a benzoyl group,
R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof. .

(1369) R ¹ represents a benzoyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a phenylthioureidocarbonyl group.

(1370) R ¹ represents a benzoyl group,
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridylthioureidocarbonyl group.

(1371) R ¹ represents a benzoyl group,
A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a lower alkylthioureidocarbonyl group.

(1372) R ¹ represents a benzoyl group,
Wherein R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group;
Or a salt thereof.

(1373) R ¹ represents a benzoyl group,
R ² represents a piperidinylcarbonyl group which may have lower alkyl group as a substituent, R ⁵ is a group

[2153]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(1374) R ¹ represents a benzoyl group,
R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group — (A ₄ ) _r
A benzene derivative represented by the general formula (1), which is COOH (A ₄ and r are the same as defined in the general formula (1)), or a salt thereof.

(1375) R ¹ represents a benzoyl group,
R ² represents a piperidinylcarbonyl group which may have lower alkyl group as a substituent, R ⁵ is a group

[2157]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1376) R ¹ represents a benzoyl group,
R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹
And R ¹² are the same as defined in the general formula (1)),
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(1377) R ¹ represents a benzoyl group,
R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹
And R ¹² are the same as defined in the general formula (1)), wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1378) R ¹ represents a benzoyl group,
R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹
And R ¹² are the same as defined in the general formula (1), wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1379) R ¹ represents a benzoyl group,
R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹
And R ¹² are the same as defined in the general formula (1), and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1380) R ¹ represents a benzoyl group,
R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹
And R ¹² are the same as defined in the general formula (1), and the benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a phenylthioureidocarbonyl group.

(1381) R ¹ represents a benzoyl group,
R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹
And R ¹² are the same as defined in the general formula (1)), and the benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyridylthioureidocarbonyl group.

(1382) R ¹ represents a benzoyl group,
R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹
And R ¹² are the same as defined in the general formula (1), wherein R ⁵ is a lower alkylthioureidocarbonyl group or a benzene derivative represented by the general formula (1) or a salt thereof.

(1383) R ¹ represents a benzoyl group,
R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹
And R ¹² are the same as defined in the general formula (1), wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1384) R ¹ represents a benzoyl group,
R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹
And R ¹² are the same as defined in the general formula (1), and R ⁵ is a group

[2168]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(1385) R ¹ represents a benzoyl group,
R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹
And R ¹² are the same as defined in the general formula (1), and R ⁵ is a group — (A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1386) R ¹ represents a benzoyl group,
R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ , p, R ¹¹
And R ¹² are the same as defined in the general formula (1), and R ⁵ is a group

[2172]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1387) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ represents the same) as defined in the general formula (1), R ² is a group

[2175]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group represented by the above formula (1) Derivatives or salts thereof.

(1388) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ represents the same) as defined in the general formula (1), R ² is a group

[2178]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) or Its salt.

(1389) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ represents the same) as defined in the general formula (1), R ² is a group

[2181]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) or Its salt.

(1390) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ represents the same) as defined in the general formula (1), R ² is a group

[2184]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.
Or a salt thereof.

(1391) R ¹ is a group represented by —CONR ⁶ R ⁷ (R ⁶
And R ⁷ represents the same) as defined in the general formula (1), R ² is a group

[2187]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and the benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a phenylthioureidocarbonyl group.

(1392) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ represents the same) as defined in the general formula (1), R ² is a group

[2190]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and the benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyridylthioureidocarbonyl group.

(1393) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ represents the same) as defined in the general formula (1), R ² is a group

[2193]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), and the benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a lower alkylthioureidocarbonyl group.

(1394) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ represents the same) as defined in the general formula (1), R ² is a group

[2196]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), and the benzene derivative represented by the above formula (1) or a salt thereof, wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(1395) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ represents the same) as defined in the general formula (1), R ² is a group

[2199]

Embedded image

(R ⁸ and m are the same as defined in the above formula (1)), and R ⁵ is a group

[2201]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1396) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ represents the same) as defined in the general formula (1), R ² is a group

[2204]

Embedded image

(R ⁸ and m are the same as defined in the general formula (1)), wherein R ⁵ is a group — (A ₄ ) _r COOH
(A ₄ and r are the same as defined in the general formula (1))
A benzene derivative represented by the general formula (1) or a salt thereof.

(1397) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ represents the same) as defined in the general formula (1), R ² is a group

[2207]

Embedded image

(R ⁸ and m are the same as defined in the formula (1)), wherein R ⁵ is a group

[2209]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1398) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent.
A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a 4-tetrahydroquinolylcarbonyl group, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(1399) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent.
A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a 4-tetrahydroquinolylcarbonyl group and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1400) R ¹ is a group represented by —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent.
A benzene derivative represented by the general formula (1) or a salt thereof, wherein the benzene derivative represents a 4-tetrahydroquinolylcarbonyl group and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1401) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent.
A benzene derivative represented by the above general formula (1) or a salt thereof, wherein the benzene derivative represents a 4-tetrahydroquinolylcarbonyl group and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1402) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent.
A benzene derivative represented by the general formula (1) or a salt thereof, which represents a 4-tetrahydroquinolylcarbonyl group and wherein R ⁵ is a phenylthioureidocarbonyl group.

(1403) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent.
A benzene derivative represented by the above general formula (1) or a salt thereof, which represents a 4-tetrahydroquinolylcarbonyl group and wherein R ⁵ is a pyridylthioureidocarbonyl group.

(1404) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent.
A benzene derivative represented by the general formula (1) or a salt thereof, which represents a 4-tetrahydroquinolylcarbonyl group and wherein R ⁵ is a lower alkylthioureidocarbonyl group.

(1405) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent.
A benzene derivative represented by the general formula (1) or a salt thereof, which represents a 4-tetrahydroquinolylcarbonyl group, and wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(1406) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent.
A 4-tetrahydroquinolylcarbonyl group, wherein R ⁵ is a group

[2220]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1407) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent.
A 4-tetrahydroquinolylcarbonyl group, wherein R ⁵ is a group — (A ₄ ) _r COOH (A ₄ and r are the same as in the general formula (1));
The benzene derivative represented by the general formula (1) or a salt thereof.

(1408) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent.
A 4-tetrahydroquinolylcarbonyl group, wherein R ⁵ is a group

[2224]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1409) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), wherein R ² is a pyridylcarbonyl group, and R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group. The represented benzene derivative or a salt thereof.

(1410) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² represents a pyridylcarbonyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1). Benzene derivatives or salts thereof.

(1411) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² is a pyridylcarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. Benzene derivatives or salts thereof.

(1412) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² represents a pyridylcarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1). Benzene derivatives or salts thereof.

(1413) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² represents a pyridylcarbonyl group, and R ⁵ is a phenylthioureidocarbonyl group. Or a salt thereof.

(1414) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² is a pyridylcarbonyl group, and R ⁵ is a pyridylthioureido carbonyl group. Or a salt thereof.

(1415) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² is a pyridylcarbonyl group, and R ⁵ is a lower alkylthioureidocarbonyl group, and the benzene derivative represented by the general formula (1) Or a salt thereof.

(1416) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the above general formula (1)), R ² represents a pyridylcarbonyl group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group represented by the above general formula (1) Or a salt thereof.

(1417) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² represents a pyridylcarbonyl group, and R ⁵ represents a group

[2235]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(1418) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² represents a pyridylcarbonyl group, and R ⁵ represents a group-
(A ₄ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(1419) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² represents a pyridylcarbonyl group, and R ⁵ represents a group

[2239]

Embedded image

[2240] benzene derivative or a salt thereof (A ₆ and R ²⁴ are as defined in the general formula (1)) represented by the general formula is (1).

(1420) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(1421) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² is a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group A benzene derivative represented by the general formula (1) or a salt thereof.

(1422) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² is a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. The general formula (1)
Or a salt thereof.

(1423) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the formula (1), R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(1224) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² is a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a phenylthioureidocarbonyl group A benzene derivative represented by (1) or a salt thereof.

(1425) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a pyridylthioureidocarbonyl group. A benzene derivative represented by (1) or a salt thereof.

(1426) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² is a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a lower alkylthioureido carbonyl group A benzene derivative represented by (1) or a salt thereof.

(1427) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² is a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group. A benzene derivative represented by (1) or a salt thereof.

(1428) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a group

[2250]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1429) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² is a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ is a group — (A ₄ ) _r COOH
(A ₄ and r are the same as defined in the general formula (1))
A benzene derivative represented by the general formula (1) or a salt thereof.

(1430) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² represents a lower alkanoyl group which may have a hydroxyl group as a substituent, and R ⁵ represents a group

[2254]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1431) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.

(1432) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1433) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1434) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1435) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, Wherein R ⁵ is a phenylthioureidocarbonyl group;
Or a salt thereof.

(1436) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, R ⁵ is a pyridylthioureidocarbonyl group of the above general formula (1)
Or a salt thereof.

(1437) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, A benzene derivative represented by the above general formula (1), wherein R ⁵ is a lower alkylthioureidocarbonyl group, or a salt thereof.

(1438) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(1439) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, R ⁵ based

[2265]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1440) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, R ⁵ is a group
(A ₄ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(1441) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² represents a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent, R ⁵ based

[2269]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1442) R ¹ is a group represented by —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² is a benzoyloxy lower alkanoyl group, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(1443) R ¹ is a group represented by —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. The represented benzene derivative or a salt thereof.

(1444) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² is a benzoyloxy lower alkanoyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. The represented benzene derivative or a salt thereof.

(1445) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² is a benzoyloxy lower alkanoyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. The represented benzene derivative or a salt thereof.

(1446) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the above general formula (1)), R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ is a phenylthioureidocarbonyl group represented by the above general formula (1). Benzene derivatives or salts thereof.

(1247) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ is a pyridylthioureidocarbonyl group represented by the general formula (1). Benzene derivatives or salts thereof.

(1448) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ is a lower alkylthioureidocarbonyl group represented by the general formula (1). Benzene derivatives or salts thereof.

(1449) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group represented by the general formula (1). Benzene derivatives or salts thereof.

(1450) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a group

[2280]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(1451) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² is a benzoyloxy lower alkanoyl group, and R ⁵ is a group — (A ₄ ) _r COOH (A ₄ and r are the same as in the general formula (1)). Formula (1), which is the same as the definition in (1).
Or a salt thereof.

(1452) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² represents a benzoyloxy lower alkanoyl group, and R ⁵ represents a group

[2284]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1453) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² is a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ is a lower alkoxy lower alkoxy group A benzene derivative represented by the general formula (1), which is an aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(1454) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² is a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ is a hydroxyl-substituted aminocarbonyl A benzene derivative represented by the general formula (1), which is a substituted lower alkenyl group, or a salt thereof.

(1455) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² is a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ is a pyridyl-substituted aminocarbonyl A benzene derivative represented by the general formula (1), which is a substituted lower alkenyl group, or a salt thereof.

(1456) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² is a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ is a pyrimidyl-substituted aminocarbonyl A benzene derivative represented by the general formula (1), which is a substituted lower alkenyl group, or a salt thereof.

(1457) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² is a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ is phenylthioureidocarbonyl A benzene derivative represented by the general formula (1) or a salt thereof.

(1458) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² is a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ is pyridylthioureidocarbonyl A benzene derivative represented by the general formula (1) or a salt thereof.

(1459) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² is a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ is a lower alkylthioureidocarbonyl A benzene derivative represented by the general formula (1) or a salt thereof.

(1460) R ¹ is a group represented by —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² is a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ is pyridylaminocarbonyl lower alkoxy. A benzene derivative represented by the general formula (1) or a salt thereof.

(1461) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² is a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ is a group

[2295]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1462) R ¹ is a group represented by —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² is a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ is a group-(A ₄ ) The above general formula (1) which is _r COOH (A ₄ and r are the same as those defined in the above general formula (1))
Or a salt thereof.

(1463) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² is a phenoxycarbonyl group which may have a lower alkoxy group as a substituent on the phenyl ring, and R ⁵ is a group

[2299]

Embedded image

[2300] A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₆ and R ²⁴ are the same as defined in the general formula (1).

(1464) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² is a thienylcarbonyl group, and R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group. The represented benzene derivative or a salt thereof.

(1465) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² is a thienylcarbonyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. Benzene derivatives or salts thereof.

(1466) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² is a thienylcarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1). Benzene derivatives or salts thereof.

(1467) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² represents a thienylcarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1). Benzene derivatives or salts thereof.

(1468) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² is a thienylcarbonyl group, and R ⁵ is a phenylthioureido carbonyl group, and the benzene derivative represented by the general formula (1) Or a salt thereof.

(1469) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the above general formula (1)), R ² is a thienylcarbonyl group, and R ⁵ is a pyridylthioureidocarbonyl group, and the benzene derivative represented by the general formula (1) Or a salt thereof.

(1470) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the above general formula (1)), R ² is a thienylcarbonyl group, and R ⁵ is a lower alkylthioureidocarbonyl group, and the benzene derivative represented by the above general formula (1) Or a salt thereof.

(1471) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the above general formula (1)), R ² is a thienylcarbonyl group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group represented by the above general formula (1) Or a salt thereof.

(1472) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² represents a thienylcarbonyl group, and R ⁵ represents a group

[2310]

Embedded image

(23) A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1473) R ¹ is a group represented by —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² represents a thienylcarbonyl group, and R ⁵ represents a group-
(A ₄ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(1474) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² represents a thienylcarbonyl group, and R ⁵ represents a group

[2314]

Embedded image

[2315] benzene derivative or a salt thereof (A ₆ and R ²⁴ are as defined in the general formula (1)) represented by the general formula is (1).

(1475) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² is a carboxy group, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(1476) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the above general formula (1)), R ² is a carboxy group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1). Benzene derivatives or salts thereof.

(1377) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² represents a carboxy group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1). Benzene derivatives or salts thereof.

(1478) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the above general formula (1)), R ² represents a carboxy group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1). Benzene derivatives or salts thereof.

(1479) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² represents a carboxy group, and R ⁵ is a phenylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or Its salt.

(1480) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² is a carboxy group, and R ⁵ is a pyridylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or Its salt.

(1481) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² represents a carboxy group, and R ⁵ is a lower alkylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or Its salt.

(1482) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² represents a carboxy group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group represented by the general formula (1) or Its salt.

(1483) R ¹ is a group represented by —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² represents a carboxy group, and R ⁵ represents a group

[2325]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(1484) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² represents a carboxy group, and R ⁵ represents a group — (A ₄ ) _r C
A benzene derivative represented by the general formula (1) or a salt thereof, which is OOH (A ₄ and r are the same as defined in the general formula (1)).

(1485) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² represents a carboxy group, and R ⁵ represents a group

[2329]

Embedded image

[2330] benzene derivative or a salt thereof (A ₆ and R ²⁴ are as defined in the general formula (1)) represented by the general formula is (1).

(1486) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² represents a lower alkoxycarbonyl group, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(1487) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² is a lower alkoxycarbonyl group, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(1488) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² is a lower alkoxycarbonyl group, and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(1489) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² represents a lower alkoxycarbonyl group, and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group. Or a salt thereof.

(1490) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² represents a lower alkoxycarbonyl group, and R ⁵ is a phenylthioureidocarbonyl group. Derivatives or salts thereof.

(1491) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² is a lower alkoxycarbonyl group, and R ⁵ is a pyridylthioureido carbonyl group. Derivatives or salts thereof.

(1492) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the above general formula (1)), R ² is a lower alkoxycarbonyl group, and R ⁵ is a lower alkylthioureido carbonyl group. Derivatives or salts thereof.

(1493) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the above general formula (1)), R ² is a lower alkoxycarbonyl group, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group represented by the above general formula (1) Derivatives or salts thereof.

(1494) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the formula (1)), R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a group

[2340]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1495) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² is a lower alkoxycarbonyl group, and R ⁵ is a group — (A ₄ ) _r COOH (A ₄ and r are the same as the general formula (1) 1)
The benzene derivative represented by the general formula (1) or a salt thereof.

(1496) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the formula (1)), R ² represents a lower alkoxycarbonyl group, and R ⁵ represents a group

[2344]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1497) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), wherein R ² may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group as a substituent. Wherein R ⁵ is a lower alkoxy-lower alkoxyaminocarbonyl-substituted lower alkenyl group;
Or a salt thereof.

(1498) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), wherein R ² may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group as a substituent. A benzene derivative represented by the above formula (1), wherein R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a salt thereof.

(1499) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), wherein R ² may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1500) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), wherein R ² may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group.

(1501) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), wherein R ² may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group as a substituent. A benzene derivative represented by the above general formula (1), wherein R ⁵ is a phenylthioureidocarbonyl group, or a salt thereof.

(1502) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), wherein R ² may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group as a substituent. A benzene derivative represented by the above general formula (1), wherein R ⁵ is a pyridylthioureidocarbonyl group, or a salt thereof.

(1503) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), wherein R ² may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group as a substituent. A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ⁵ is a lower alkylthioureidocarbonyl group;

(1504) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), wherein R ² may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group;

(1505) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), wherein R ² may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group as a substituent. R ⁵ represents a group

[2355]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(1506) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), wherein R ² may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group as a substituent. A benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a group — (A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(1507) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), wherein R ² may have a substituent selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group as a substituent. R ⁵ represents a group

[2359]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1508) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ represents the same) as defined in the general formula (1), an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, R ⁵
Is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(1509) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ represents the same) as defined in the general formula (1), an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, R ⁵
Is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(1510) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ represents the same) as defined in the general formula (1), an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, R ⁵
Is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1511) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ represents the same) as defined in the general formula (1), an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, R ⁵
Is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1512) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ represents the same) as defined in the general formula (1), an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, R ⁵
Is a phenylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1513) R ¹ is a group represented by —CONR ⁶ R ⁷ (R ⁶
And R ⁷ represents the same) as defined in the general formula (1), an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, R ⁵
Is a pyridylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1514) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ represents the same) as defined in the general formula (1), an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, R ⁵
Is a lower alkylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1515) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ represents the same) as defined in the general formula (1), an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, R ⁵
Is a pyridylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the general formula (1) or a salt thereof.

(1516) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ represents the same) as defined in the general formula (1), an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, R ⁵
Is based

[2370]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1517) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ represents the same) as defined in the general formula (1), an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, R ⁵
Is a group-(A ₄ ) _r COOH (A ₄ and r are the same as defined in the general formula (1)) or a benzene derivative represented by the general formula (1) or a salt thereof.

(1518) R ¹ is a group represented by —CONR ⁶ R ⁷ (R ⁶
And R ⁷ represents the same) as defined in the general formula (1), an amino-lower alkoxycarbonyl group which R ² may have a lower alkyl group as a substituent, R ⁵
Is based

[2374]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1519) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl A benzene derivative represented by the general formula (1), which is a substituted lower alkenyl group, or a salt thereof.

(1520) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² is a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower group A benzene derivative represented by the general formula (1), which is an alkenyl group, or a salt thereof.

(1521) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in formula (1) above, R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a pyridyl-substituted aminocarbonyl-substituted lower group. A benzene derivative represented by the general formula (1), which is an alkenyl group, or a salt thereof.

(1522) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a pyrimidyl-substituted aminocarbonyl-substituted lower group. A benzene derivative represented by the general formula (1), which is an alkenyl group, or a salt thereof.

(1523) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a phenylthioureidocarbonyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(1524) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1)), R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a pyridylthioureidocarbonyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(1525) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a lower alkylthioureidocarbonyl group. A benzene derivative represented by the general formula (1) or a salt thereof.

(1526) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ is a pyridylaminocarbonyl lower alkoxy group. A benzene derivative represented by the general formula (1) or a salt thereof.

(1527) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[2385]

Embedded image

A benzene derivative represented by the general formula (1) or a salt thereof, wherein A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1).

(1528) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group-
(A ₄ ) A benzene derivative represented by the general formula (1) or a salt thereof, wherein _r COOH (A ₄ and r are the same as defined in the general formula (1)).

(1529) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), R ² represents a piperidinylcarbonyl group which may have a lower alkyl group as a substituent, and R ⁵ represents a group

[2389]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1530) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ ,
p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group.
Or a salt thereof.

(1531) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ ,
p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) or a benzene derivative thereof. salt.

(1532) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ ,
p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) or a benzene derivative thereof. salt.

(1533) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the formula (1), wherein R ² is a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ ,
p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) or a benzene derivative thereof. salt.

(1534) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ ,
p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and the benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a phenylthioureidocarbonyl group.

(1535) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ ,
p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and the benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyridylthioureidocarbonyl group.

(1536) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ ,
p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and the benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a lower alkylthioureidocarbonyl group.

(1537) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ ,
p, R ¹¹ and R ¹² are the same as defined in the general formula (1)), and the benzene derivative represented by the general formula (1) or a salt thereof, wherein R ⁵ is a pyridylaminocarbonyl lower alkoxy group.

(1538) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ ,
p, R ¹¹ and R ¹² are the same as defined in the general formula (1), and R ⁵ is a group

[2400]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(1539) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ ,
p, R ¹¹ and R ¹² are the same as defined in the general formula (1), and R ⁵ is a group — (A ₄ ) _r COOH (A ₄ and r
Is the same as defined in the general formula (1)) or a benzene derivative represented by the general formula (1) or a salt thereof.

(1540) R ¹ is a group —CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same as defined in the general formula (1), and R ² represents a group —CO— (A ₁ ) _p —NR ¹¹ R ¹² (A ₁ ,
p, R ¹¹ and R ¹² are the same as defined in the general formula (1), and R ⁵ is a group

[2404]

Embedded image

[2405] benzene derivative or a salt thereof (A ₆ and R ²⁴ are as defined in the general formula (1)) represented by the general formula is (1).

(1541) R ¹ and R ² together form a group

[2407]

Embedded image

Wherein R ²² and R ²³ are the same as defined in the above formula (1), and R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group represented by the above formula (1) Benzene derivatives or salts thereof.

(1542) R ¹ and R ² are taken together to form a group

[2410]

Embedded image

Wherein R ²² and R ²³ are the same as defined in the general formula (1), and R ⁵ is a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) Or a salt thereof.

(1543) R ¹ and R ² are taken together to form a group

[2413]

Embedded image

Wherein R ²² and R ²³ are the same as defined in the general formula (1), and R ⁵ is a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) Or a salt thereof.

(1544) R ¹ and R ² are taken together to form a group

[2416]

Embedded image

Wherein R ²² and R ²³ are the same as defined in the general formula (1), and R ⁵ is a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group represented by the general formula (1) Or a salt thereof.

(1545) R ¹ and R ² are taken together to form a group

[2419]

Embedded image

Wherein R ²² and R ²³ are the same as defined in the general formula (1), and R ⁵ is a phenylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof .

(1546) R ¹ and R ² are taken together to form a group

[2422]

Embedded image

Wherein R ²² and R ²³ are the same as defined in the general formula (1), and R ⁵ is a pyridylthioureidocarbonyl group, or a benzene derivative represented by the general formula (1) or a salt thereof .

(1547) R ¹ and R ² are taken together to form a group

[2425]

Embedded image

Wherein R ²² and R ²³ are the same as defined in the general formula (1), and R ⁵ is a lower alkylthio ureidocarbonyl group or a benzene derivative represented by the general formula (1), or salt.

(1548) R ¹ and R ² are taken together to form a group

[2428]

Embedded image

Wherein R ²² and R ²³ are the same as defined in the general formula (1), and R ⁵ is a pyridylaminocarbonyl lower alkoxy group represented by the general formula (1) or a salt thereof .

(1549) R ¹ and R ² are taken together to form a group

[2431]

Embedded image

Wherein R ²² and R ²³ are the same as defined in the above formula (1), and R ⁵ is a group

[2433]

Embedded image

(A ₄ , r, R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as defined in the general formula (1)), or a benzene derivative represented by the general formula (1) or a salt thereof.

(1550) R ¹ and R ² are taken together to form a group

[2436]

Embedded image

(R ²² and R ²³ are the same as defined in the above formula (1)), and R ⁵ is a group — (A ₄ ) _r CO 2
A benzene derivative represented by the general formula (1) or a salt thereof, which is OH (A ₄ and r are the same as defined in the general formula (1)).

(1551) R ¹ and R ² are taken together to form a group

[2439]

Embedded image

Wherein R ²² and R ²³ are the same as defined in the above formula (1), and R ⁵ is a group

[2441]

Embedded image

(A ₆ and R ²⁴ are the same as defined in the general formula (1)). A benzene derivative represented by the general formula (1) or a salt thereof.

(1552) 2- {4- [2-benzoyl-2- (1,2,4-triazolyl-1-yl) -1-]
Ethylthioethyl] benzoylamino dibenzothiazole.

(1553) 2- {4- (2,2-diacetylvinyl) -2- [3- (4-methyl-1-piperazinyl) propyl] phenoxymethylcarbonylamino}
Benzothiazole.

(1554) A benzene derivative represented by the above formula (1), wherein R ¹ and R ² are the same as those in the above (1), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group, or a salt thereof.

(1555) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ and R ² are the same as in the above (12), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group.

(1556) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ and R ² are the same as those in the above (23), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group.

(1557) A benzene derivative represented by the above general formula (1) or a salt thereof, wherein R ¹ and R ² are the same as in the above (34), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group.

(1558) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ and R ² are the same as those in the above (45), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group.

(1559) A benzene derivative represented by the above formula (1), wherein R ¹ and R ² are the same as those in the above (56), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group, or a salt thereof.

(1560) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ and R ² are the same as those in the above (67), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group.

(1561) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ and R ² are the same as in the above (78), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group.

(1562) A benzene derivative represented by the above formula (1) or a salt thereof, wherein R ¹ and R ² are the same as those in the above (89), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group.

(1563) R ¹ and R ² are as defined in the above (100)
Wherein R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(1564) R ¹ and R ² are as defined in the above (111)
Wherein R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(1565) R ¹ and R ² are as defined in the above (122)
Wherein R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(1566) R ¹ and R ² are as defined in the above (133)
Wherein R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(1567) R ¹ and R ² are as defined in the above (144)
Wherein R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group, or a benzene derivative represented by the above general formula (1) or a salt thereof.

(1568) In the above formula (1), wherein R ¹ is the same as the above (155), R ² is the same as the above (1), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1569) In the above formula (1), R ¹ is the same as the above (155), R ² is the same as the above (12), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1570) In the above formula (1), wherein R ¹ is the same as the above (155), R ² is the same as the above (23), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1571) In the above formula (1), wherein R ¹ is the same as the above (155), R ² is the same as the above (34), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1572) In the above formula (1), wherein R ¹ is the same as the above (155), R ² is the same as the above (45), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1573) In the above formula (1), wherein R ¹ is the same as the above (155), R ² is the same as the above (56), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1574) In the above formula (1), wherein R ¹ is the same as the above (155), R ² is the same as the above (67), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1575) In the above formula (1), wherein R ¹ is the same as the above (155), R ² is the same as the above (78), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1576) In the above formula (1), wherein R ¹ is the same as the above (155), R ² is the same as the above (89), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1577) In the above formula (1), wherein R ¹ is the same as the above (155), R ² is the same as the above (100), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1578) In the above formula (1), R ¹ is the same as the above (155), R ² is the same as the above (111), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1579) In the above formula (1), wherein R ¹ is the same as the above (155), R ² is the same as the above (122), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1580) In the above formula (1), wherein R ¹ is the same as the above (155), R ² is the same as the above (133), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1581) In the above formula (1), wherein R ¹ is the same as the above (155), R ² is the same as the above (144), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1582) In the above formula (1), wherein R ¹ is the same as the above (309), R ² is the same as the above (1), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1583) In the above formula (1), wherein R ¹ is the same as in the above (309), R ² is the same as in the above (12), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1584) In the above formula (1), wherein R ¹ is the same as the above (309), R ² is the same as the above (23), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1585) In the above formula (1), R ¹ is the same as the above (309), R ² is the same as the above (34), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1586) In the above formula (1), wherein R ¹ is the same as the above (309), R ² is the same as the above (45), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1587) In the above formula (1), wherein R ¹ is the same as the above (309), R ² is the same as the above (56), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1588) In the above formula (1), wherein R ¹ is the same as the above (309), R ² is the same as the above (67), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1589) In the above formula (1), wherein R ¹ is the same as the above (309), R ² is the same as the above (78), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1590) In the above formula (1), wherein R ¹ is the same as the above (309), R ² is the same as the above (89), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1591) In the above formula (1), R ¹ is the same as the above (309), R ² is the same as the above (100), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1592) In the above formula (1), wherein R ¹ is the same as the above (309), R ² is the same as the above (111), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1593) In the above formula (1), R ¹ is the same as the above (309), R ² is the same as the above (122), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1594) In the above formula (1), wherein R ¹ is the same as the above (309), R ² is the same as the above (133), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1595) In the above formula (1), wherein R ¹ is the same as the above (309), R ² is the same as the above (144), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1596) In the above formula (1), wherein R ¹ is the same as the above (463), R ² is the same as the above (1), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1597) In the above formula (1), wherein R ¹ is the same as the above (463), R ² is the same as the above (12), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1598) In the above formula (1), wherein R ¹ is the same as the above (463), R ² is the same as the above (23), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1599) In the above formula (1), wherein R ¹ is the same as the above (463), R ² is the same as the above (34), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1600) In the above formula (1), wherein R ¹ is the same as the above (463), R ² is the same as the above (45), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1601) In the above formula (1), wherein R ¹ is the same as the above (463), R ² is the same as the above (56), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1602) In the above formula (1), wherein R ¹ is the same as the above (463), R ² is the same as the above (67), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1603) In the above formula (1), wherein R ¹ is the same as the above (463), R ² is the same as the above (78), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1604) In the above formula (1), wherein R ¹ is the same as the above (463), R ² is the same as the above (89), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1605) In the above formula (1), wherein R ¹ is the same as the above (463), R ² is the same as the above (100), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1606) In the above formula (1), wherein R ¹ is the same as the above (463), R ² is the same as the above (111), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1607) In the above formula (1), wherein R ¹ is the same as the above (463), R ² is the same as the above (122), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1608) In the above formula (1), wherein R ¹ is the same as the above (463), R ² is the same as the above (133), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1609) In the above formula (1), wherein R ¹ is the same as the above (463), R ² is the same as the above (144), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1610) In the above formula (1), wherein R ¹ is the same as the above (617), R ² is the same as the above (1), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1611) In the above formula (1), wherein R ¹ is the same as the above (617), R ² is the same as the above (12), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1612) In the above formula (1), wherein R ¹ is the same as the above (617), R ² is the same as the above (23), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1613) In the above formula (1), wherein R ¹ is the same as the above (617), R ² is the same as the above (34), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1614) In the above formula (1), wherein R ¹ is the same as the above (617), R ² is the same as the above (45), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1615) In the above formula (1), wherein R ¹ is the same as the above (617), R ² is the same as the above (56), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1616) In the above formula (1), wherein R ¹ is the same as the above (617), R ² is the same as the above (67), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1617) In the above formula (1), wherein R ¹ is the same as the above (617), R ² is the same as the above (78), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1618) In the above formula (1), wherein R ¹ is the same as the above (617), R ² is the same as the above (89), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1619) In the above formula (1), wherein R ¹ is the same as the above (617), R ² is the same as the above (100), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1620) In the above formula (1), wherein R ¹ is the same as the above (617), R ² is the same as the above (111), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1621) In the above formula (1), wherein R ¹ is the same as the above (617), R ² is the same as the above (122), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1622) In the above formula (1), wherein R ¹ is the same as the above (617), R ² is the same as the above (133), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1623) In the above formula (1), wherein R ¹ is the same as the above (617), R ² is the same as the above (144), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1624) In the above formula (1), wherein R ¹ is the same as the above (771), R ² is the same as the above (1), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1625) In the above formula (1), wherein R ¹ is the same as the above (771), R ² is the same as the above (12), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1626) In the above formula (1), wherein R ¹ is the same as the above (771), R ² is the same as the above (23), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1627) In the above formula (1), wherein R ¹ is the same as the above (771), R ² is the same as the above (34), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1628) In the above formula (1), wherein R ¹ is the same as the above (771), R ² is the same as the above (45), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1629) In the above formula (1), wherein R ¹ is the same as the above (771), R ² is the same as the above (56), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1630) In the above formula (1), wherein R ¹ is the same as the above (771), R ² is the same as the above (67), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1631) In the above formula (1), wherein R ¹ is the same as the above (771), R ² is the same as the above (78), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1632) In the above formula (1), wherein R ¹ is the same as the above (771), R ² is the same as the above (89), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1633) In the above formula (1), wherein R ¹ is the same as the above (771), R ² is the same as the above (100), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1634) In the above formula (1), wherein R ¹ is the same as the above (771), R ² is the same as the above (111), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1635) In the above formula (1), wherein R ¹ is the same as the above (771), R ² is the same as the above (122), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1636) In the above formula (1), wherein R ¹ is the same as the above (771), R ² is the same as the above (133), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1637) In the above formula (1), wherein R ¹ is the same as the above (771), R ² is the same as the above (144), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1638) In the above formula (1), wherein R ¹ is the same as the above (925), R ² is the same as the above (1), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1639) In the above formula (1), wherein R ¹ is the same as the above (925), R ² is the same as the above (12), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1640) In the above formula (1), wherein R ¹ is the same as the above (925), R ² is the same as the above (23), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1641) In the above formula (1), wherein R ¹ is the same as the above (925), R ² is the same as the above (34), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1642) In the above formula (1), wherein R ¹ is the same as the above (925), R ² is the same as the above (45), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1643) In the above formula (1), wherein R ¹ is the same as the above (925), R ² is the same as the above (56), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1644) In the above formula (1), wherein R ¹ is the same as the above (925), R ² is the same as the above (67), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1645) In the above formula (1), wherein R ¹ is the same as the above (925), R ² is the same as the above (78), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1646) In the above formula (1), wherein R ¹ is the same as the above (925), R ² is the same as the above (89), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1647) In the above formula (1), wherein R ¹ is the same as the above (925), R ² is the same as the above (100), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1648) In the above formula (1), wherein R ¹ is the same as the above (925), R ² is the same as the above (111), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1649) In the above formula (1), R ¹ is the same as the above (925), R ² is the same as the above (122), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1650) In the above formula (1), R ¹ is the same as the above (925), R ² is the same as the above (133), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1651) In the above formula (1), wherein R ¹ is the same as the above (925), R ² is the same as the above (144), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1652) In the above formula (1), wherein R ¹ is the same as the above (1079), R ² is the same as the above (1), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1653) In the above formula (1), wherein R ¹ is the same as the above (1079), R ² is the same as the above (12), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1654) In the above formula (1), wherein R ¹ is the same as the above (1079), R ² is the same as the above (23), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1655) In the above formula (1), wherein R ¹ is the same as the above (1079), R ² is the same as the above (34), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1656) In the above formula (1), wherein R ¹ is the same as the above (1079), R ² is the same as the above (45), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1657) In the above formula (1), wherein R ¹ is the same as the above (1079), R ² is the same as the above (56), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1658) In the above formula (1), wherein R ¹ is the same as the above (1079), R ² is the same as the above (67), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1659) In the above formula (1), wherein R ¹ is the same as the above (1079), R ² is the same as the above (78), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1660) In the above formula (1), R ¹ is the same as the above (1079), R ² is the same as the above (89), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1661) In the above formula (1), wherein R ¹ is the same as the above (1079), R ² is the same as the above (100), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1662) In the above formula (1), wherein R ¹ is the same as the above (1079), R ² is the same as the above (111), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1663) In the above formula (1), wherein R ¹ is the same as the above (1079), R ² is the same as the above (122), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1664) In the above formula (1), wherein R ¹ is the same as the above (1079), R ² is the same as the above (133), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1665) In the above formula (1), R ¹ is the same as the above (1079), R ² is the same as the above (144), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1666) In the above formula (1), wherein R ¹ is the same as the above (1233), R ² is the same as the above (1), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1667) In the above formula (1), wherein R ¹ is the same as the above (1233), R ² is the same as the above (12), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1668) In the above formula (1), wherein R ¹ is the same as the above (1233), R ² is the same as the above (23), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1669) In the above formula (1), wherein R ¹ is the same as the above (1233), R ² is the same as the above (34), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1670) In the above formula (1), wherein R ¹ is the same as the above (1233), R ² is the same as the above (45), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1671) In the above formula (1), wherein R ¹ is the same as the above (1233), R ² is the same as the above (56), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1672) In the above formula (1), wherein R ¹ is the same as the above (1233), R ² is the same as the above (67), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1673) In the above formula (1), wherein R ¹ is the same as the above (1233), R ² is the same as the above (78), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1674) In the above formula (1), wherein R ¹ is the same as the above (1233), R ² is the same as the above (89), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1675) In the above formula (1), wherein R ¹ is the same as the above (1233), R ² is the same as the above (100), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1676) In the above formula (1), wherein R ¹ is the same as the above (1233), R ² is the same as the above (111), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1677) In the above formula (1), wherein R ¹ is the same as the above (1233), R ² is the same as the above (122), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1678) In the above formula (1), R ¹ is the same as the above (1233), R ² is the same as the above (133), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1679) In the above formula (1), wherein R ¹ is the same as the above (1233), R ² is the same as the above (144), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1680) In the above formula (1), wherein R ¹ is the same as the above (1387), R ² is the same as the above (1), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1681) In the above formula (1), wherein R ¹ is the same as the above (1387), R ² is the same as the above (12), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1682) In the above formula (1), wherein R ¹ is the same as the above (1387), R ² is the same as the above (23), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1683) In the above formula (1), wherein R ¹ is the same as the above (1387), R ² is the same as the above (34), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1684) In the above formula (1), wherein R ¹ is the same as the above (1387), R ² is the same as the above (45), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1885) In the above formula (1), wherein R ¹ is the same as the above (1387), R ² is the same as the above (56), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1686) In the above formula (1), wherein R ¹ is the same as the above (1387), R ² is the same as the above (67), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1687) In the above formula (1), wherein R ¹ is the same as the above (1387), R ² is the same as the above (78), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1688) In the above formula (1), wherein R ¹ is the same as the above (1387), R ² is the same as the above (89), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1689) In the above formula (1), wherein R ¹ is the same as the above (1387), R ² is the same as the above (100), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1690) In the above formula (1), wherein R ¹ is the same as the above (1387), R ² is the same as the above (111), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1691) In the above formula (1), wherein R ¹ is the same as the above (1387), R ² is the same as the above (122), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1692) In the above formula (1), wherein R ¹ is the same as the above (1387), R ² is the same as the above (133), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1693) In the above formula (1), wherein R ¹ is the same as the above (1387), R ² is the same as the above (144), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1694) In the above formula (1), wherein R ¹ is the same as the above (1541), R ² is the same as the above (1), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1695) In the above formula (1), wherein R ¹ is the same as the above (1541), R ² is the same as the above (12), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1696) In the above formula (1), wherein R ¹ is the same as the above (1541), R ² is the same as the above (23), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1697) In the above formula (1), R ¹ is the same as the above (1541), R ² is the same as the above (34), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1698) In the above formula (1), wherein R ¹ is the same as the above (1541), R ² is the same as the above (45), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1699) In the above formula (1), R ¹ is the same as the above (1541), R ² is the same as the above (56), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1700) In the above formula (1), wherein R ¹ is the same as the above (1541), R ² is the same as the above (67), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1701) In the above formula (1), wherein R ¹ is the same as the above (1541), R ² is the same as the above (78), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1702) In the above formula (1), wherein R ¹ is the same as the above (1541), R ² is the same as the above (89), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1703) In the above formula (1), R ¹ is the same as the above (1541), R ² is the same as the above (100), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1704) In the above formula (1), wherein R ¹ is the same as the above (1541), R ² is the same as the above (111), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1705) In the above formula (1), wherein R ¹ is the same as the above (1541), R ² is the same as the above (122), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1706) In the above formula (1), wherein R ¹ is the same as the above (1541), R ² is the same as the above (133), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

(1707) In the above formula (1), wherein R ¹ is the same as the above (1541), R ² is the same as the above (144), and R ⁵ is a pyrimidylaminocarbonyl lower alkoxy group. The represented benzene derivative or a salt thereof.

The compound of the present invention can be produced by various methods.

[2600]

Embedded image

Wherein R ¹ , R ² , R ³ , R ⁴ , R ⁵ and n are as defined above. The reaction between the compound (2) and the compound (3) is performed in a suitable solvent in the presence or absence of a basic compound. As the basic compound to be used, inorganic bases such as sodium metal, potassium metal, sodium hydride, sodium amide, sodium hydroxide, potassium hydroxide, sodium carbonate, potassium carbonate, sodium hydrogen carbonate, sodium methylate, sodium ethylate , Potassium tert-butoxide and other metal alcoholates, methyllithium, n-butyllithium, phenyllithium, lithium diisopropylamide and other alkyl and aryllithium or lithium amides, pyridine, piperidine, quinoline, triethylamine, N, N-dimethylaniline And the like. As the solvent, any solvent can be used as long as it does not affect the reaction.Examples include water, ethers such as diethyl ether, dioxane, tetrahydrofuran, monoglyme and diglyme, and aromatic hydrocarbons such as benzene, toluene and xylene. , Chloroform,
Halogenated hydrocarbons such as dichloromethane and carbon tetrachloride, aliphatic hydrocarbons such as n-hexane, heptane and cyclohexane, pyridines, amines such as N, N-dimethylaniline, acetic acid, N, N-dimethylformamide;
Examples include aprotic polar solvents such as N, N'-dimethylpropylurea, dimethylsulfoxide, and hexamethylphosphoric acid triamide; alcohols such as methanol, ethanol, and isopropanol; and mixed solvents thereof. The reaction temperature is usually -80 to 150 ° C, preferably-
The temperature is preferably about 80 to 120 ° C., generally 0.5 to 5 ° C.
The reaction is completed in about 0 hours. When alkyl or aryl lithium or lithium amides or metal alcoholates are used as the basic compound, the solvent is preferably an anhydrous solvent. The compound (3) is usually used at least in an equimolar amount, preferably in an equimolar to 1.5-fold molar amount, relative to the compound (2).

[2602]

Embedded image

[Wherein R ¹ , R ² , R ⁴ , R ⁵ and n are as defined above. R ^3a represents a lower alkylthio group, a phenylthio group,
A lower alkylthio group, a hydroxyl-substituted lower alkylthio group, a cycloalkylthio group or a lower alkanoylthio group having a group selected from the group consisting of a carboxy group as a substituent and an amino group which may have a lower alkyl group as a substituent. M represents an alkali metal such as sodium and potassium. The reaction of the compound (1b) with the compound (4) or the compound (5) is performed in a suitable solvent. As the solvent used herein, any of the solvents used in the reaction between compound (2) and compound (3) in the above-mentioned reaction formula-1 can be used. The compound (4) or the compound (5) is usually used at least in an equimolar amount, preferably in an equimolar to 3 times molar amount, relative to the compound (1b). The reaction is carried out usually at 0 to 150 ° C., preferably at about 0 to 100 ° C., and is completed generally in about 0.5 to 5 hours.

[2604]

Embedded image

Wherein R ¹ , R ² , R ⁴ , R ⁵ and n are as defined above. R ^3b represents a lower alkyl group. Y represents lithium or MgX (X is a halogen atom). The reaction between compound (1b) and compound (6) is performed in a suitable solvent. As the solvent, any solvent can be used as long as it does not affect the reaction, for example, ethers such as diethyl ether, dioxane, tetrahydrofuran, monoglyme, diglyme, benzene, toluene,
Aromatic hydrocarbons such as xylene, n-hexane, heptane, aliphatic hydrocarbons such as cyclohexane, pyridine,
Amines such as N, N-dimethylaniline, aprotic polar solvents such as N, N-dimethylformamide, dimethylsulfoxide, hexamethylphosphoric triamide, alcohols such as methanol, ethanol, isopropanol and the like, or mixed solvents thereof Is mentioned. Compound (6)
Is generally at least equimolar, preferably equimolar to 10-fold molar amount, relative to compound (1b). In the reaction, a metal halide such as copper iodide, sodium iodide, and potassium iodide may be added to the reaction system. The reaction temperature is usually -80 to 150C, preferably -80 to
The temperature is preferably around 120 ° C., and the reaction is generally completed in about 0.5 to 20 hours.

[2606]

Embedded image

[Wherein R ¹ , R ² , R ³ , R ⁴ , n and the side chain

[2608]

Embedded image

[2609] is the same as above. R ^5a is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group,
Hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group,
Base

[2610]

Embedded image

[2611] A _'4 represents a lower alkenylene group.
R ¹⁷ , R ¹⁸ and R ¹⁹ are the same as above. ) Or group

[2612]

Embedded image

(A ₆ and R ²⁴ are the same as described above).
X ¹ represents a halogen atom. The reaction between compound (7) and compound (8) is carried out in a suitable solvent in the presence of a basic compound and a catalyst. Examples of the catalyst used here include palladium halides such as palladium chloride. As the solvent, any of the solvents used in the reaction between compound (1b) and compound (6) in the above-mentioned Reaction Formula-3 can be used. Examples of the basic compound include inorganic bases such as sodium hydroxide, potassium hydroxide, sodium carbonate, potassium carbonate, and sodium hydrogen carbonate; and organic bases such as pyridine, piperidine, quinoline, triethylamine, N, N-dimethylaniline, and sodium acetate. Can be illustrated. The compound (8) is usually used in an amount at least equimolar, preferably equimolar to 1.5-fold molar amount, relative to the compound (7). The catalyst is usually used in an amount of 0.001 mole to equimolar with respect to the compound (7),
Preferably, it is used in a molar amount of 0.001 to 0.1 times. The reaction is carried out usually at room temperature to 200 ° C., preferably at room temperature to about 150 ° C., and is completed generally in about 1 to 5 hours.

[2614]

Embedded image

Wherein R ¹ , R ² , R ³ , R ⁴ , n, A ₄ ,
r, R ¹⁷ , R ¹⁸ , R ¹⁹ and side chains

[2616]

Embedded image

[2617] is the same as above. R ²⁵ represents a carboxy-substituted lower alkenyl group or a carboxy-substituted lower alkoxy group. R ²⁶ represents a lower alkoxy lower alkoxy group, a hydroxyl group, a pyridyl group, a pyrimidyl group or a pyrazyl group.
However, when R ²⁵ represents a carboxy-substituted lower alkoxy group, R ²⁶ represents a pyridyl group, a bilimidyl group or a pyrazyl group. R ^{26 ′} is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group, a hydroxyl-substituted aminocarbonyl-substituted lower alkenyl group, a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group, a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group, a pyridylaminocarbonyl-lower alkoxy group, It represents a midylaminocarbonyl lower alkoxy group or a pyridylaminocarbonyl lower alkoxy group. The method represented by the reaction formula-5 can be performed by the method represented by the general formula (9) or (1
This is a method in which the carboxylic acid of 1) is reacted with an amine of the general formula (10) or (12) by a usual amide bond formation reaction. Known conditions for the amide bond formation reaction can be easily applied to the acid amide bond formation reaction. For example, (a) a mixed acid anhydride method, that is, a method in which an alkylhalocarbonate is reacted with a carboxylic acid (9) or (11) to form a mixed acid anhydride, and the mixed acid anhydride is reacted with an amine (10) or (12);
(B) Active ester method, that is, carboxylic acid (9) or (1)
1) is an active ester such as p-nitrophenyl ester, N-hydroxysuccinimide ester, 1-hydroxybenzotriazole ester, etc.
0) or (12), (c) Carbodiimide method, that is, the presence of an activator such as dicyclohexylcarbodiimide, carbonyldiimidazole or the like with amine (10) or (12) in carboxylic acid (9) or (11). (D) Other methods, for example, the carboxylic acid (9) or (11) is converted into a carboxylic acid anhydride with a dehydrating agent such as acetic anhydride, and the amine (10) or (1)
Method 2), carboxylic acid (9) or (11)
A method of reacting an amine (10) or (12) with an ester of a lower alcohol at a high pressure and a high temperature, and an acid halide of a carboxylic acid (9) or (11), that is, an amine (10) or (12) And the like.

The mixed acid anhydride used in the mixed acid anhydride method (a) is obtained by a reaction similar to the usual Schotten-Baumann reaction, and this is usually isolated without isolation of the amine (10) or (12). ) To produce the compound of the present invention of the general formula (1f) or (1g). The Schotten-Baumann reaction is performed in the presence of a basic compound. Examples of the basic compound used include compounds commonly used in the Schotten-Baumann reaction, for example, triethylamine, trimethylamine, pyridine, dimethylaniline, 1-methyl-2-pyrrolidinone (NMP), N-
Methylmorpholine, 1,5-diazabicyclo [4.3.
0] organic bases such as nonene-5 (DBN), 1,8-diazabicyclo [5.4.0] undecene-7 (DBU) and 1,4-diazabicyclo [2.2.2] octane (DABCO); Inorganic bases such as potassium, sodium carbonate, potassium hydrogen carbonate, sodium hydrogen carbonate and the like can be mentioned. The reaction is usually performed at about -20 to 100 ° C, preferably about -20 to 50 ° C, and the reaction time is about 5 minutes to 10 hours, preferably about 5 minutes to 2 hours.
The reaction between the obtained mixed acid anhydride and the amine (10) or (12) is usually about -20 to 150 ° C, preferably -20.
The reaction is carried out at about 50 ° C. to about 50 ° C., and the reaction time is about 5 minutes to 35 hours, preferably about 5 minutes to 30 hours. The mixed acid anhydride method is generally performed in a solvent in the presence of a basic compound. As the basic compound to be used, any of the basic compounds used in the Schotten-Baumann reaction can be used. As the solvent to be used, any of the solvents commonly used in the mixed acid anhydride method can be used. Specifically, chloroform, dichloromethane, halogenated hydrocarbons such as dichloroethane, benzene, p-chlorobenzene,
Aromatic hydrocarbons such as toluene and xylene, ethers such as diethyl ether, diisopropyl ether, tetrahydrofuran and dimethoxyethane, esters such as methyl acetate and ethyl acetate, N, N-dimethylformamide, dimethyl sulfoxide, acetonitrile, hexamethyl Examples of such solvents include aprotic polar solvents such as phosphoric acid triamide and the like and mixed solvents thereof. Examples of the alkyl halocarbonate used in the mixed acid anhydride method include methyl chloroformate, methyl bromoformate, ethyl chloroformate, ethyl bromoformate, and isobutyl chloroformate. A carboxylic acid (9) or (11) in the method,
Alkyl halocarbonate and amine (10) or (1
Although the use ratio of 2) is usually good to be equimolar,
The alkyl halocarbonate and the amine (10) or (12) can be used in an amount of about 1 to 1.5 times the molar amount of the carboxylic acid (9) or (11), respectively.

When the method of reacting a carboxylic acid halide with an amine (10) or (12) is employed among the other methods (d), the reaction is carried out in an appropriate solvent in the presence of a basic compound. Done in As the basic compound to be used, known compounds can be widely used.For example, in addition to the basic compound used for the above-mentioned Schotten-Baumann reaction, for example, sodium hydroxide, potassium hydroxide, sodium hydride, potassium hydride and the like can be used. Can be illustrated. Examples of the solvent used include, in addition to the solvent used in the mixed acid anhydride method, alcohols such as methanol, ethanol, propanol, butanol, 3-methoxy-1-butanol, ethyl cellosolve, and methyl cellosolve;
Pyridine, acetone, water and the like can be exemplified. Amine (1
The ratio of (0) or (12) to the carboxylic acid halide is not particularly limited and can be appropriately selected within a wide range. Usually, the former is at least equimolar, preferably equimolar to 5 times the molar amount of the latter. It is better to use about the amount. The reaction is usually carried out at about -20 to 180 ° C, preferably at -10 to 150 ° C.
C., and the reaction is generally completed in about 5 minutes to 30 hours.

Further, the amide bond forming reaction shown in the above reaction formula-5 is carried out by reacting a carboxylic acid (9) or (11) with an amine (1).
0) or (12) with phenylphosphine-2,2 ′
-Dithiodipyridine, diphenylphosphinyl chloride, phenyl-N-phenylphosphoramidochloridate, diethylchlorophosphate, diethyl cyanophosphate, diphenylphosphate azide, N, N'-bis (2-oxo-3-oxazolidinyl) phospho It can also be carried out by a method of reacting a phosphorus compound such as phenyl chloride in the presence of a condensing agent.

The reaction is usually carried out in the presence of a solvent and a basic compound used in the method of reacting the carboxylic acid halide with the amine (10) or (12), in the range of -20 to 150.
C., preferably at about 0-100 C.
Generally, the reaction is completed in about 5 minutes to 30 hours. The amount of the condensing agent and the amine (10) or (12) to be used is at least about an equimolar amount, preferably about equimolar to about 2 times the molar amount of the carboxylic acid (9) or (11), respectively. .

[2622]

Embedded image

[Wherein R ¹ , R ² , R ³ , R ⁴ , n and a side chain

[2624]

Embedded image

[2625] is the same as above. R ²⁷ represents a phenyl group, a pyridyl group or a lower alkyl group. The reaction for converting the compound (13) into the compound (1h) is carried out by reacting the compound (13) with ammonium thiocyanate in a suitable solvent, and subsequently reacting the compound (13) with the compound (14) in one pot.

The reaction of the compound (13) with ammonium thiocyanate is carried out under the same conditions as in the reaction of the compound (9) with the compound (10) in the aforementioned Reaction Formula-5. Among them, it is preferable to use the method of reacting an amine with the carboxylic acid halide (d), and in this case, the reaction is preferably performed in the absence of a basic compound. The subsequent reaction with the compound (14) is carried out in the same solvent as used for the reaction with ammonium thiocyanate, usually at 0 to 150 ° C, preferably at about 0 to 100 ° C, and is generally completed in about 5 minutes to 5 hours. I do. The amount of compound (14) to be used is generally at least equimolar, preferably equimolar to 1.5-fold the molar amount of compound (13).

[2627]

Embedded image

Wherein R ¹ , R ² , R ³ , R ⁴ , n, A ₄ ,
r, R ¹⁷ , R ¹⁸ , X ₁ , A ₆ and side chain

[2629]

Embedded image

[2630] is the same as above. X^TwoIndicates a halogen atom
You. R^19aRepresents a lower alkyl group. R^{twenty four a}Is a low alco
Indicates a xycarbonyl group. Reaction of Compound (1i) with Compound (15) and Compound
The reaction between (1k) and compound (16) is generally carried out by an appropriate
In an active solvent or without solvent, in the presence or absence of a basic compound
Performed in the presence. Examples of inert solvents used
For example, aromatic hydrocarbons such as benzene, toluene and xylene
, Diethyl ether, tetrahydrofuran, dioxa
Ethers such as diethylene glycol dimethyl ether
Toluene, dichloromethane, chloroform, carbon tetrachloride, etc.
Halogenated hydrocarbons, methanol, ethanol, iso
Propanol, butanol, tert-butanol, etc.
Lower alcohols, water, acetic acid, ethyl acetate, acetone,
Acetonitrile, pyridine, dimethyl sulfoxide, di
Methylformamide, hexamethylphosphoric triamide or
May be a mixed solvent thereof. Base
Sodium carbonate, potassium carbonate
Carbonic acid such as sodium bicarbonate and potassium bicarbonate
Metal hydroxide such as salt, sodium hydroxide, potassium hydroxide
Material, sodium, potassium, sodium, sodium hydride
Umamide, sodium methylate, sodium ethyla
Metal alkoxide such as nitrate, pyridine, N-ethyldiyl
Sopropylamine, dimethylaminopyridine, triethyl
Ruamine, 1,5-diazabicyclo [4.3.0] none
-5 (DBN), 1,8-diazabicyclo [5.4.
0] undecene-7 (DBU), 1,4-diazavik
B. Organic bases such as [2.2.2] octane (DABCO)
And the like. Compound (1i) and compound
Use of (15) or compound (1k) and compound (16)
The ratio is not particularly limited and may be appropriately selected in a wide range.
The latter should be at least equimolar to the former.
Degree, preferably about equimolar to about 10 times the molar amount.
No. The reaction is usually carried out at about 0 to 200 ° C, preferably at 0 to 1 ° C.
It is carried out at about 70 ° C. and generally takes about 30 minutes to 75 hours.
The reaction ends. Sodium iodide, iodide
Add alkali metal halides such as potassium, copper powder, etc.
May be added.

[2631]

Embedded image

[Wherein R ¹ , R ² , R ³ , R ⁴ , R ⁵ and the side chain

[2633]

Embedded image

[2634] is the same as above. R ²⁸ represents a group —A ₂ —X ¹ (A ₂
And X ¹ are the same as described above). R ^4a is a group —A ₂ —NR ¹³
R ¹⁴ (A ₂ , R ¹³ and R ¹⁴ are as defined above). s represents 1 or 2. The reaction between compound (17) and compound (18) is performed under the same conditions as in the reaction between compound (1i) and compound (15) in the aforementioned Reaction Formula-7.

[2635]

Embedded image

[Wherein R ² , R ³ , R ⁴ , R ⁵ , n, R ⁶ , R ⁷
And side chains

[2637]

Embedded image

The carbon-carbon bond including the dotted line in [2638] is the same as described above. R ^1a represents a lower alkoxycarbonyl group. The reaction for converting the compound (1n) into the compound (1o) can be carried out in a suitable solvent or without a solvent in the presence of an acid or a basic compound. Examples of the solvent used include water, lower alcohols such as methanol, ethanol, and isopropanol; ketones such as acetone and methyl ethyl ketone; halogenated hydrocarbons such as dichloromethane, chloroform and carbon tetrachloride; dioxane; tetrahydrofuran; and ethylene glycol dimethyl ether. And fatty acids such as acetic acid and formic acid, and a mixed solvent thereof. Examples of the acid include hydrochloric acid, sulfuric acid,
Mineral acids such as hydrobromic acid, formic acid, acetic acid, trifluoroacetic acid,
Organic acids such as aromatic sulfonic acid and the like can be mentioned. Examples of the basic compound include metal carbonates such as sodium carbonate and potassium carbonate, and sodium hydroxide, potassium hydroxide, calcium hydroxide and lithium hydroxide. And the like. The reaction is usually carried out at room temperature to
The process suitably proceeds at about 200 ° C., preferably about room temperature to about 150 ° C., and generally ends in about 10 minutes to 25 hours.

The reaction between compound (1o) and compound (19) is carried out by reacting compound (9) with compound (1) in the aforementioned reaction formula-5.
The reaction is carried out under the same conditions as in the reaction with 0).

[2640]

Embedded image

Wherein R ³ , R ⁴ , R ⁵ , R ²³ and n are as defined above. The reaction between the compound (2) and the compound (20) is performed in an appropriate solvent in the presence of a basic compound. Examples of the basic compound used herein include, in addition to sodium acetate, any of the basic compounds used in the reaction between compound (2) and compound (3) in the aforementioned reaction formula-1. . As the solvent used, in addition to acetic anhydride, any of the solvents used in the reaction between the compound (2) and the compound (3) can be used. Compound (2
0) is usually at least equimolar to compound (2),
Preferably, it is used in an equimolar to 3-fold molar amount. The reaction is usually performed at room temperature to 150 ° C, preferably at room temperature to 100 ° C.
It is performed in the vicinity, and generally ends in about 1 to 5 hours.

In each of the above reaction formulas, compound (2), compound (3), compound (9),
Compound (11), Compound (13) and Compound (17)
Is manufactured by the following method, for example.

[2643]

Embedded image

Wherein R ² and X ¹ are as defined above. R ^1b is
The heterocyclic residue of R ¹ having a group —NH— in the heterocyclic ring is shown. R ^1c represents a heterocyclic residue of the above R ¹ having a heterocyclic group> NCH ₂ R ² (R ² is as defined above). The reaction between compound (21) and compound (22) is performed under the same conditions as in the reaction between compound (1i) and compound (15) in the aforementioned Reaction Scheme-7. In this reaction, compound (21) is generally used in an amount at least equimolar, preferably equimolar to 3 times the molar amount of compound (22).

[2645]

Embedded image

[Wherein R ^1d represents a group —N (C
The heterocyclic residue of R ¹ having H ₃ ) — is shown. R ^1e is
Heterocyclic group

[2647]

Embedded image

[2648] (R ⁸ and m are the same. Above) shows the heterocyclic residue of the R ¹ having. In the reaction for converting the compound (23) into the compound (2b), the compound (23) and the compound (24) are converted under the same conditions as in the reaction between the compound (2) and the compound (3) in the aforementioned reaction formula-1. After that, the compound (1
This is carried out by treating n) under the same conditions as in the reaction leading to compound (1o).

[2649]

Embedded image

Wherein R ³ , R ⁴ , n, X ¹ and R ^5a are as defined above. The reaction between the compound (25) and the compound (8) is performed under the same conditions as in the reaction between the compound (7) and the compound (8) in the aforementioned Reaction Formula-4.

[2651]

Embedded image

[Wherein R ³ , R ⁴ , n, R ⁵ , R ¹³ , R ¹⁴ ,
R ²⁸ and R ^4a are the same as above. The reaction between the compound (26) and the compound (18) is performed under the same conditions as in the reaction between the compound (17) and the compound (18) in the aforementioned Reaction Formula-8.

[2653]

Embedded image

[Wherein R ¹ , R ² , R ³ , R ⁴ , n, Z, X ¹
And A ₅ are as defined above. R ²⁹ represents a hydroxyl group or a lower alkoxy group. The reaction between compound (27) and compound (28) is generally performed in a suitable inert solvent or without a solvent, in the presence or absence of a basic compound. Examples of the inert solvent used include aromatic hydrocarbons such as benzene, toluene, and xylene; ethers such as tetrahydrofuran, dioxane, and diethyl glycol dimethyl ether; halogenated hydrocarbons such as dichloromethane, chloroform, and carbon tetrachloride; and methanol. , Ethanol, isopropanol, butanol, lower alcohols such as tert-butanol, water, acetic acid, ethyl acetate, acetone, acetonitrile, pyridine, dimethylsulfoxide, dimethylformamide, hexamethylphosphoric triamide or a mixed solvent thereof. it can. Examples of the basic compound include sodium carbonate, potassium carbonate, sodium hydrogencarbonate, carbonates such as potassium hydrogencarbonate, sodium hydroxide, metal hydroxides such as potassium hydroxide, sodium hydride, potassium, sodium, sodium amide, and the like. Metal alcoholates such as sodium methylate, pyridine,
N-ethyldiisopropylamine, dimethylaminopyridine, triethylamine, 1,5-diazabicyclo [4.3.0] nonene-5 (DBN), 1,8-diazabicyclo [5.4.0] undecene-7 (DBU),
1,4-diazabicyclo [2.2.2] octane (DA
And organic bases such as BCO). The ratio of the compound (27) and the compound (28) to be used is not particularly limited and may be appropriately selected in a wide range, but the latter is usually at least equimolar, preferably at least equimolar to 10 times the former. It is preferable to use about a molar amount. The reaction is usually carried out at about 0 to 200 ° C, preferably about 0 to 170 ° C, and is generally completed in about 30 minutes to 75 hours.
An alkali metal halide such as sodium iodide and potassium iodide, copper powder and the like may be added to the reaction system.

(2655) A compound wherein R ²⁹ represents a lower alkoxy group (2)
The reaction for converting 9) to the compound (9a) is carried out under the same conditions as those for converting the compound (1n) to the compound (1o) in the aforementioned Reaction Formula-9.

[2656]

Embedded image

[Wherein R ¹ , R ² , R ³ , R ⁴ and n are as defined above. R ³⁰ represents a group —X ¹ (X ¹ is the same as described above);
(A ₄ ) _r COOH (A ₄ and r are as defined above), a group —R
²⁵ (R ²⁵ is as defined above) or a group -ZH (Z is as defined above). The reaction between the compound (3) and the compound (30) is performed under the same conditions as in the reaction between the compound (2) and the compound (3) in the aforementioned Reaction Formula-1.

[2658]

Embedded image

Wherein R ¹ , R ² , R ³ , R ⁴ , s, R ⁵ and R ²⁸ are as defined above. The reaction between the compound (3) and the compound (31) is carried out under the same conditions as in the reaction between the compound (2) and the compound (3) in the aforementioned Reaction Formula-1.

[2660]

Embedded image

[Wherein R ³ , R ⁴ , n and R ²⁷ are as defined above. The reaction for converting the compound (32) into the compound (3c) is carried out under the same conditions as in the reaction for converting the compound (13) into the compound (1h) in the aforementioned Reaction Formula-6.

[2662]

Embedded image

Wherein R ¹ , R ² , R ³ , R ⁴ and n are as defined above. R ²⁸ is a carboxy group or a group

[2664]

Embedded image

(R ¹⁷ , R ¹⁸ and R ¹⁹ are as defined above). The reaction for converting the compound (1r) to the compound (1s) is performed in a suitable solvent in the presence of an oxidizing agent. As the solvent used here, the compound (1i) in the aforementioned Reaction Formula-7 is used.
Any of the solvents used in the reaction of the compound (15) with the compound (15) can be used. Examples of the oxidizing agent include lower alkylamine N-oxides such as trimethylamine N-oxide and osmium tetroxide. The amount of the oxidizing agent to be used is such that the lower alkylamine N-oxide is usually used in a molar amount of 5 to 20 times, preferably 5 to 15 times the molar amount of compound (1r), and osmium tetroxide is used in a catalytic amount. Is good. The reaction is carried out usually at 0 to 100 ° C, preferably at 0 ° C.
It proceeds favorably at about 70 ° C., and generally ends in about 1 to 75 hours.

Among the compounds (1) of the present invention, the compound having an acidic group can form a salt with a pharmacologically acceptable basic compound. Such basic compounds include, for example, metal hydroxides such as sodium hydroxide, potassium hydroxide, lithium hydroxide and calcium hydroxide, alkali metal carbonates or bicarbonates such as sodium carbonate and sodium hydrogen carbonate, sodium methylate And alkali metal alcoholates such as potassium ethylate. In addition, among the compounds (1) of the present invention, a compound having basicity can easily form a salt with a usual pharmacologically acceptable acid. Such acids include, for example, inorganic acids such as sulfuric acid, nitric acid, hydrochloric acid, hydrobromic acid, acetic acid, p-toluenesulfonic acid, ethanesulfonic acid, oxalic acid, maleic acid, fumaric acid, citric acid,
Organic acids such as succinic acid and benzoic acid can be exemplified. These salts can also be used as the active ingredient compound in the present invention, similarly to the free form of the compound (1). The compound (1) includes stereoisomers and optical isomers, and these can also be used as active ingredient compounds.

The target compound obtained by the method shown in each of the above reaction schemes can be separated from the reaction system by a usual separation means and further purified. Such separation and purification means include, for example, distillation, recrystallization, column chromatography, ion exchange chromatography,
Gel chromatography, affinity chromatography, preparative thin-layer chromatography, solvent extraction and the like can be employed.

The thus obtained active ingredient compounds are effective as protein kinase C inhibitors, and these drugs are used in the form of general pharmaceutical preparations. Formulations include commonly used fillers, extenders, binders, humectants, disintegrants,
It is prepared using a diluent or excipient such as a surfactant or a lubricant. Various forms can be selected as the pharmaceutical preparation depending on the purpose of treatment, and typical examples are tablets, pills, powders, solutions, suspensions, emulsions, granules, capsules,
Suppositories, injections (solutions, suspensions, etc.) and the like can be mentioned. In molding into tablets, various carriers well-known in the art can be widely used as carriers. Examples thereof include excipients such as lactose, sucrose, sodium chloride, glucose, urea, starch, calcium carbonate, kaolin, crystalline cellulose, silicic acid, etc.
Binders such as water, ethanol, propanol, simple syrup, glucose solution, starch solution, gelatin solution, carboxymethylcellulose, shellac, methylcellulose, potassium phosphate, polyvinylpyrrolidone, dry starch,
Disintegrators such as sodium alginate, agar powder, laminaran powder, sodium hydrogen carbonate, calcium carbonate, polyoxyethylene sorbitan fatty acid esters, sodium lauryl sulfate, stearic acid monoglyceride, starch, lactose, sucrose, stearin, cocoa butter, hydrogenated oil , Quaternary ammonium salts, absorption promoters such as sodium lauryl sulfate, humectants such as glycerin and starch, adsorbents such as starch, lactose, kaolin, bentonite, colloidal silicic acid, purified talc, stearin Lubricants such as acid salts, boric acid powder and polyethylene glycol can be used. Further, the tablet can be made into a tablet coated with a usual coating, if necessary, such as a sugar-coated tablet, a gelatin-encapsulated tablet, an enteric-coated tablet, a film-coated tablet or a double tablet or a multilayer tablet. In molding into the form of pills, a wide variety of carriers conventionally known in this field can be used. Examples thereof include excipients such as glucose, lactose, starch, cocoa butter, hardened vegetable oils, kaolin, talc, binders such as gum arabic, tragacanth, gelatin, ethanol, disintegrants such as laminaran, agar, etc. Can be used. In the case of molding into a suppository form, conventionally known carriers can be widely used. Examples include polyethylene glycol, cocoa butter, higher alcohols,
Esters of higher alcohols, gelatin, semi-synthetic glycerides and the like can be mentioned. Capsules are prepared according to a conventional method, usually by mixing an active ingredient compound with the various carriers exemplified above and filling the mixture into hard gelatin capsules, soft capsules and the like. When prepared as an injection, solutions, emulsions and suspensions are preferably sterilized and isotonic with blood, and are commonly used as diluents in the art when formed into these forms. And water, ethyl alcohol, macrogol, propylene glycol, ethoxylated isostearyl alcohol, polyoxylated isostearyl alcohol, polyoxyethylene sorbitan fatty acid esters, and the like. In this case, a sufficient amount of salt, glucose or glycerin to prepare an isotonic solution may be included in the pharmaceutical preparation, and a usual solubilizer, buffer, soothing agent, etc. may be added. You may. Coloring agent if necessary,
Preservatives, flavors, flavors, sweeteners, and other pharmaceuticals can also be included in the pharmaceutical formulation.

The amount of the active ingredient compound to be contained in the pharmaceutical preparation of the present invention is not particularly limited and may be appropriately selected from a wide range, and is usually about 1 to 70% by weight, preferably about 1 to 70% by weight in the pharmaceutical composition. The content is preferably 5 to 50% by weight.

The method of administration of the pharmaceutical preparation of the present invention is not particularly limited, and may be various preparation forms, patient age, gender and other conditions,
The drug is administered according to the degree of the disease. For example, tablets,
In the case of pills, solutions, suspensions, emulsions, granules and capsules, they are administered orally. In the case of an injection, it is administered intravenously, alone or as a mixture with a normal replenisher such as glucose or amino acid, and, if necessary, intramuscularly, intradermally, subcutaneously or intraperitoneally. In the case of suppositories, they are administered rectally.

The dose of the pharmaceutical preparation of the present invention is appropriately selected depending on the usage, the age of the patient, gender and other conditions, the degree of the disease and the like. Usually, the amount of the active compound is about 0 to 1 kg / body weight per day. It is preferable to be about 0.6 to 50 mg.
In addition, the active ingredient compound is contained in a dosage unit form preparation in an amount of about 10%.
Desirably, it is contained in the range of １０００1000 mg.

[2672]

EXAMPLES Hereinafter, in order to explain the present invention in more detail, preparation examples of the pharmaceutical preparation of the present invention will be given, followed by production examples of the above-mentioned active ingredient compounds, and test examples of the active ingredient compounds.

Formulation Example 1 2- {4- [2-benzoyl-2- (1,2,4-triazol-1-yl) -1-methylthioethyl] benzoylamino} benzothiazole 150 g Avicel (trade name, Asahi Kasei Corporation) 40 g corn starch 30 g magnesium stearate 2 g hydroxypropyl methylcellulose 10 g polyethylene glycol-6000 3 g castor oil 40 g ethanol 40 g After mixing and polishing the active ingredient compound of the present invention, Avicel, corn starch and magnesium stearate, sugar coating R10 m
Tablet with m-kine. The obtained tablets were treated with hydroxypropyl methylcellulose, polyethylene glycol-600.
0, coating with a film coating agent consisting of castor oil and ethanol to produce film-coated tablets.

Formulation Example 2 2- {4- (2,2-diacetylvinyl) -2- [3- (4-methyl-1-piperazinyl) propyl] phenoxymethylcarbonylamino} benzimidazole 150 g Citric acid 1.0 g Lactose 33.5 g Dicalcium phosphate 70.0 g Pluronic F-68 30.0 g Sodium lauryl sulfate 15.0 g Polyvinyl pyrrolidone 15.0 g Polyethylene glycol (Carbowax 1500) 4.5 g Polyethylene glycol (Carbowax 6000) 45.0 g Corn starch 30.0 g dried sodium stearate 3.0 g dried magnesium stearate 3.0 g ethanol appropriate amount Active compound of the present invention, citric acid, lactose, dicalcium phosphate, Pluronic F-68 and lauryl Mix sodium sulfate.

The above mixture was designated as No. Sieve through a 60 screen and wet granulate with an alcoholic solution containing polyvinylpyrrolidone, carbowax 1500 and 6000. If necessary, alcohol is added to make the powder into a pasty mass. Add corn starch and continue mixing until uniform particles are formed. The mixture was no. Pass through 10 screens, place in trays and dry in oven at 100 ° C. for 12-14 hours. The dried particles were no. Sieve through 16 screens, add dry sodium lauryl sulfate and dry magnesium stearate, mix and compress to desired shape on tablet press.

The above core is treated with varnish, and talc is sprinkled to prevent moisture absorption. An undercoat layer is coated around the core. Apply varnish a sufficient number of times for internal use. A further subbing layer and a smooth coating are applied to make the tablet completely round and smooth. Color coating is carried out until the desired hue is obtained. After drying, the coated tablets are polished into tablets of uniform gloss.

Formulation Example 3 2- {4- [2-benzoyl-2- (imidazol-1-yl) vinyl] benzoylamino} thiazole 5 g polyethylene glycol (molecular weight: 4000) 0.3 g sodium chloride 0.9 g polyoxy Ethylene-sorbitan monooleate 0.4 g Sodium metabisulfite 0.1 g Methyl-paraben 0.18 g Propyl-paraben 0.02 g Distilled water for injection 10.0 ml While stirring the above parabens, sodium metabisulfite and sodium chloride Dissolve in about half of the above distilled water at 80 ° C. The obtained solution is cooled to 40 ° C., and the active ingredient compound of the present invention, and then polyethylene glycol and polyoxyethylene sorbitan monooleate are dissolved in the above solution. Next, distilled water for injection is added to the solution to make the final volume, and the solution is sterilized by sterile filtration using an appropriate filter paper to prepare an injection.

Reference Example 1 (4-methoxymethoxybenzoyl) methyl bromide 1
A solution of 6.6 g, 9 g of 1,2,4-triazole and 9 g of calcium carbonate in 200 ml of acetonitrile was heated under reflux for 2 hours. Water was added to the reaction solution, and extracted with ethyl acetate.
After washing with water and drying, the solvent was distilled off. The obtained residue was purified by silica gel column chromatography (eluent: dichloromethane: methanol = 100: 1) to give 1- (4
-Methoxymethoxybenzoylmethyl) -1,2,4-
11.6 g of triazole (compound a) and 2 g of 1- (4-methoxymethoxybenzoylmethyl) -1,3,4-triazole (compound b) were obtained.

Compound a: ¹ H-NMR (CDCl ₃ ) δp
pm: 3.50 (3H, s), 5.27 (2H, s),
5.63 (2H, s), 7.15 (2H, d, J = 7H)
z), 7.97 (2H, d, J = 7 Hz), 8.01
(1H, s), 8.25 (1H, s) Compound b: ¹ H-NMR (CDCl ₃ ) δ ppm: 3.5
0 (3H, s), 5.28 (2H, s), 5.50 (2
H, s), 7.16 (2H, d, J = 7 Hz), 7.9
6 (2H, d, J = 7 Hz), 8.26 (2H, s).

Reference Example 2 2.93 g of α-picoline and anhydrous tetrahydrofuran 10
1.6M-n- at an internal temperature of -30 to 40 ° C in a 0 ml solution.
63 ml of butyllithium was added dropwise. After stirring at the same temperature for 30 minutes, 10.5 ml of benzonitrile was added, and the temperature was raised to room temperature. After stirring for 1 hour, the mixture was acidified with 5% hydrochloric acid and stirred overnight. The reaction solution was made basic with 5% sodium hydroxide,
After extraction with ethyl acetate, washing with water and drying, the solvent was distilled off. The obtained residue is subjected to silica gel column chromatography (eluent; dichloromethane → dichloromethane: methanol =
100: 1) to give 2- (benzoylmethyl)
11.3 g of pyridine were obtained. This compound was a mixture of enone type: ethanol type = 2: 3.

[2681] _{^{1 H-NMR (CDCl 3)}} δppm: 4.
50 (2/5 × 2H, s), 6.08 (3/5 × 1H, s)
s), 6.9-7.75 (6H, m), 7.85 (3 /
5.times.2H, dd, J = 7.5 Hz, J = 2 Hz);
07 (2/5 × 2H, dd, J = 8 Hz, J = 1.5H
z), 8.30 (3/5 × 1H, d, J = 5 Hz),
8.57 (2 / 5H, d, J = 5 Hz), 15.49
(2/5 × 1H, brs).

Using the appropriate starting materials, the compounds shown in Tables 1 to 9 were obtained in the same manner as in Reference Examples 1 and 2.

[2683]

[Table 1]

[2684]

[Table 2]

[2685]

[Table 3]

[2686]

[Table 4]

[2687]

[Table 5]

[2688]

[Table 6]

[2689]

[Table 7]

[2690]

[Table 8]

[2691]

[Table 9]

The NMR spectrum of each compound shown in Tables 1 to 9 is as follows.

(1) ¹ H-NMR (CDCl ₃ ) δpp
m: 3.90 (3H, s), 5.36 (2H, s),
6.88-7.18 (4H, m), 7.53 (1H,
s), 7.88-8.08 (2H, m).

(2) ¹ H-NMR (DMSO-d ₆ ) δp
pm: 5.82 (2H, s), 6.95 (1H, s),
7.14 (1H, s), 7.73 (1H, s), 8.2
1-8.30 (2H, m), 8.35-8.48 (2
H, m).

(3) ¹ H-NMR (DMSO-d ₆ ) δp
pm: 6.02 (2H, s), 7.54-7.80 (3
H, m), 8.00-8.20 (2H, m), 8.54
(1H, s).

(4) ¹ H-NMR (DMSO-d ₆ ) δp
pm: 5.62 (2H, s), 6.85-7.10 (3
H, m), 7.10 (1H, s), 7.60 (1H,
s), 7.85-8.02 (2H, m), 10.57
(1H, br).

(5) ¹ H-NMR (DMSO-d ₆ ) δp
pm: 5.99 (2H, s), 7.39-7.54 (2
H, m), 8.08-8.24 (2H, m), 8.51
(1H, s).

(6) ¹ H-NMR (DMSO-d ₆ ) δp
pm: 5.99 (2H, s), 7.63-7.76 (2
H, m), 7.90-8.15 (2H, m), 8.51
(1H, s).

(7) ¹ H-NMR (DMSO-d ₆ ) δp
pm: 6.05 (2H, s), 8.00-8.30 (5
H, m), 8.51 (1H, s).

(8) ¹ H-NMR (DMSO-d ₆ ) δp
pm: 2.31 (3H, s), 5.73 (2H, s),
6.92 (1H, s), 7.11 (1H, s), 7.3
6 (2H, d, J = 8.2 Hz), 7.59 (1H,
s), 8.09 (2H, d, J = 8.2 Hz).

(9) ¹ H-NMR (CDCl ₃ ) δpp
m: 3.50 (3H, s), 5.26 (2H, s),
5.36 (2H, s), 6.95 (1H, s), 7.0
8-7.20 (3H, m), 7.51 (1H, s),
7.95-8.08 (2H, m).

(10) ¹ H-NMR (CDCl ₃ ) δpp
m: 5.99 (2H, s), 7.51-7.66 (2
H, m), 7.66-7.80 (1H, m), 7.95
-8.10 (2H, m), 8.87 (1H, s).

(11) ¹ H-NMR (CDCl ₃ ) δpp
m: 6.16 (2H, s), 7.50-7.65 (2
H, m), 7.65-7.78 (1H, m), 7.92
-8.08 (2H, m), 8.63 (1H, s).

(12) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 2.53 (2H, t, J = 7.0 Hz);
00 (2H, t, J = 7.0 Hz), 5.78 (2H, t, J = 7.0 Hz)
s), 7.03 (1H, d, J = 8.0 Hz), 7.2
1 (1H, s), 7.32 (1H, s), 7.92-
8.02 (2H, m), 8.13 (1H, s), 10.
57 (1H, s).

(13) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.25 (9H, s), 4.91 (2H, s),
6.83 (1H, t, J = 1.1 Hz), 7.07 (1
H, s), 7.38 (1H, s).

(14) ¹ H-NMR (CDCl ₃ ) δpp
m: 2.35 (6H, s), 2.77 (2H, t, J =
5.5 Hz), 4.15 (2H, t, J = 5.5H)
z), 5.34 (2H, s), 6.97 (2H, d, J
= 8.5 Hz), 7.03 (1H, s), 7.14 (1
H, s), 7.51 (1H, s), 7.94 (2H,
d, J = 8.5 Hz).

(15) ¹ H-NMR (CDCl ₃ ) δpp
m: 4.06 (3H, s), 4.70 (2H, s),
7.45-7.7 (3H, m), 8.05 (2H, d,
J = 7 Hz).

(16) ¹ H-NMR (CDCl ₃ ) δpp
m: 4.50 (2/5 × 2H, s), 6.08 (3/5
X 1H, s), 6.9-7.75 (6H, m), 7.8
5 (3/5 × 2H, dd, J = 7.5 Hz, J = 2H
z), 8.07 (2/5 × 2H, dd, J = 8 Hz, J
= 1.5 Hz), 8.30 (3/5 × 1H, d, J = 5)
Hz), 8.57 (2/5 × 2H, d, J = 5 Hz),
15.49 (2/5 × 1H, brs).

(17) ¹ H-NMR (CDCl ₃ ) δpp
m: 3.50 (3H, s), 5.27 (2H, s),
5.63 (2H, s), 7.14 (2H, d, J = 7H)
z), 7.96 (2H, d, J = 7 Hz), 8.01
(2H, s), 8.25 (1H, s).

(18) ¹ H-NMR (CDCl ₃ ) δpp
m: 3.50 (3H, s), 5.28 (2H, s),
5.50 (2H, s), 7.16 (2H, d, J = 8.
5 Hz), 7.96 (2H, d, J = 8.5 Hz),
8.26 (2H, s).

(19) ¹ H-NMR (CDCl ₃ ) δpp
m: 2.36 (6H, s), 2.78 (2H, t, J =
5.5 Hz), 4.16 (2H, t, J = 5.5H)
z), 5.63 (2H, s), 7.02 (2H, d, J
= 9 Hz), 7.96 (2H, d, J = 9 Hz), 8.
01 (1H, s), 8.25 (1H, s).

(20) ¹ H-NMR (CDCl ₃ ) δpp
m: 4.07 (36/100 × 3H, s), 4.11
(64/100 × 3H, s), 4.71 (36/100
× 2H, s), 6.09 (64/100 × 1H, s),
7.71 (64/100 × 2H, dd, J = 4.5H
z, J = 1.5 Hz), 7.84 (36/100 × 2)
H, dd, J = 4.5 Hz, J = 1.5 Hz), 8.7
5 (64/100 × 2H, dd, J = 4.5 Hz, J =
1.591), 8.91 (36/100 × 1H, dd,
J = 4.5 Hz, J = 1.5 Hz), 11.60 (1
H, brs).

(21) ¹ H-NMR (CDCl ₃ ) δpp
m: 3.62 (2/30 × 3H, s), 3.63 (1 /
3 × 3H, s), 4.45 (2/30 × 2H, s),
5.90 (１ ／ × 1H, s), 6.75 (１ ／ × 1H, s)
H, d, J = 1 Hz), 6.87 (2/3 × 1H, d,
J = 1 Hz), 6.99 (1H, d, J = 1 Hz),
7.35-7.65 (3H, m), 7.82 (1 / 3x
7. 2H, dd, J = 7.5 Hz, J = 1.5 Hz);
11 (2/3 × 2H, dd, J = 7.5 Hz, J = 1.
5 Hz).

(22) ¹ H-NMR (CDCl ₃ ) δpp
m: 3.83 (3H, s), 4.74 (2H, s),
5.62 (2H, s), 7.01 (2H, d, J = 8.
5 Hz), 7.98 (2H, d, J = 8.5 Hz),
8.01 (1H, s), 8.25 (1H, s).

(23) ¹ H-NMR (CDCl ₃ ) δpp
m: 3.57 (3H, s), 5.52 (2H, s),
5.77 (2H, s), 7.99 (1H, s), 8.0
5 (2H, d, J = 8.2 Hz), 8.20 (2H,
d, J = 8.2 Hz), 8.29 (1H, s).

(24) ¹ H-NMR (CDCl ₃ ) δpp
m: 3.98 (3H, s), 5.72 (2H, s),
7.05-7.15 (1H, m), 7.26 (1H,
d, J = 8.2 Hz), 7.59-7.80 (2H,
m), 7.99 (1H, s), 8.52 (1H, s).

(25) ¹ H-NMR (CDCl ₃ ) δpp
m: 3.54 (3H, s), 3.58 (3H, s),
5.37 (2H, s), 5.50 (2H, s), 5.6
6 (2H, s), 7.35 (1H, d, J = 8.8H)
z), 8.02 (1H, s), 8.13 (1H, dd,
J = 2.4 Hz, J = 8.8 Hz), 8.25 (1H,
s), 8.48 (1H, d, J = 2.4 Hz).

(26) ¹ H-NMR (CDCl ₃ ) δpp
m: 4.07 (3H, s), 4.95 (2H, s),
7.57 (1H, ddd, J = 7.5 Hz, J = 6H
z, J = 1.5 Hz), 7.91 (1H, dt, J =
1.5 Hz, J = 7.5 Hz), 8.08 (1 H, d
t, J = 7.5 Hz, J = 1 Hz), 8.73 (1H,
dm, J = 6 Hz).

(27) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.2-2.2 (10H, m), 4.05-5.2
5 (1H, m), 4.69 (1/2 × 2H, s), 5.
11 (1/2 × 1H, s), 6.50 (1/2 × 1H, s)
br), 7.4-8.15 (5H, m).

(28) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 6.21 (2H, s), 7.52-7.68
(2H, m), 7.68-7.83 (2H, m), 8.
00-8.20 (3H, m).

(29) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 1.93 (3H, s), 3.24 (3H,
s), 5.74 (2H, s), 6.92 (1H, s),
7.12 (1H, s), 7.52-7.67 (3H,
m), 8.08 (2H, d, J = 8.4 Hz).

(30) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 1.05-1.45 (5H, m), 1.50-
1.96 (5H, m), 2.45-2.65 (1H,
m), 5.35 (2H, m), 7.96 (1H, s),
8.41 (1H, s).

(31) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.08 (6H, t, J = 7.1 Hz), 1.58
(3H, t, J = 7.3 Hz), 2.65 (4H, q,
J = 7.1 Hz), 2.90 (2H, t, J = 6.2H)
z), 4.13 (2H, t, J = 6.2 Hz), 4.3
4 (2H, q, J = 7.3 Hz), 4.62 (2H,
s), 6.99 (2H, dt, J = 8.9 Hz, J =
2.0 Hz), 8.02 (2H, dt, J = 8.9H)
z, J = 2.0 Hz).

(32) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.09 (6H, t, J = 7.1 Hz), 2.67
(4H, q, J = 7.1 Hz), 2.92 (2H, t,
J = 6.1 Hz), 4.05 (3H, s), 4.15
(2H, t, J = 6.1 Hz), 4.64 (2H,
s), 6.99 (2H, d, J = 9.0 Hz), 8.0
1 (2H, d, J = 9.0 Hz).

Reference Example 36 30 ml of palladium chloride in 5 ml of dimethylformamide
The suspension was stirred at 140 ° C. for 30 minutes under a nitrogen atmosphere. 2
-Vinylcarbonylmethylbenzothiazole 2 g, p-
2 ml of bromobenzaldehyde and sodium acetate l.
1 g was added and the mixture was stirred at 120 ° C. for 2 hours. The reaction solution was poured into water, and the precipitated crystals were collected by filtration. After dissolution in dimethylformamide and filtration, methanol was added to the filtrate, and the crystals were collected by filtration.
1.8 g of 4- (2-benzothiazolyl) aminocarbonylvinylbenzaldehyde were obtained.

[2726] ¹ H-NMR (DMSO-d ₆ ) δ ppm:
7.09 (1H, d, J = 16.0 Hz), 7.25 −
7.39 (1H, m), 7.39-7.52 (1H,
m), 7.70-7.94 (4H, m), 7.94-
8.06 (3H, m), 10.03 (1H, s), 1
2.70 (1H, s).

Reference Example 37 2.51 g of ammonium thiocyanate in 30 m of acetone
5 g of p-formylbenzoyl chloride was added to the solution,
Refluxed for 5 minutes. Subsequently, 2.82 g of 2-aminopyridine
Reflux occurred upon addition and was further refluxed for 5 minutes using an oil bath. Thereafter, the mixture was stirred at room temperature for 2 hours, 120 ml of water was added, and the insoluble matter was collected by filtration to obtain 6.98 g of 4- (2-pyridyl) thioureidocarbonylbenzaldehyde.

[2728] pale yellow powder ^{1 H-NMR (DMSO-d} 6) δppm: 7.20-
7.37 (1H, m), 7.92-8.16 (6H,
m), 8.33-8.50 (1H, m), 8.75 (1
H, brs), 10.12 (1H, s), 12.00
(1H, brs), 13.15 (1H, brs).

Reference Example 38 4- (2-benzothiazolyl) aminocarbonylvinylbenzaldehyde (5 g) in tetrahydrofuran (100 ml)
50 mg of osmium tetroxide was added to the solution, and further a solution of 11.1 g of trimethylamine N-oxide in 10 ml of water was added. It was dissolved by adding dimethylformamide and stirred at room temperature for 3 days. Water was added to remove insolubles, and the filtrate was extracted with ethyl acetate. After drying, the solvent was distilled off, and diethyl ether was added to the residue to give 4
-[1,2-dihydroxy-2- (2-benzothiazolylaminocarbonyl) ethyl] benzaldehyde 0.7
g was obtained.

Gray powdery ¹ H-NMR (DMSO-d ₆ ) δ ppm: 4.42 (1
H, dd, J = 3 Hz, J = 7.5 Hz), 5.14
(1H, dd, J = 3 Hz, J = 6 Hz) 5.66
(1H, d, J = 7.5 Hz), 5.82 (1H, d, J
J = 6 Hz), 7.25-7.5 (2H, m), 7.6
5 (2H, d, J = 8 Hz), 7.75 (1H, d, J
= 7 Hz), 7.87 (2H, d, J = 8 Hz), 7.
99 (1H, d, J = 7 Hz), 9.98 (1H, d, J = 7 Hz)
s), 11.93 (1H, br).

Reference Example 39 A solution of 1 g of 3- (3-chloropropyl) -4-[(2-benzothiazolyl) aminocarbonylmethoxy] benzaldehyde and 760 mg of 2-morpholinomethylpyrrolidine in 30 ml of anhydrous dimethylformamide was stirred at 60 ° C. for 2 hours. Add water, extract with ethyl acetate, wash with water,
After drying, the solvent was distilled off. The residue was subjected to silica gel column chromatography (eluent; dichloromethane: methanol =
100: 1 → 10: 1) to give 3- [3- (2
-Morpholinomethylpyrrolidinyl) propyl] -4-
0.6 g of [(2-benzothiazolyl) aminocarbonylmethoxy] benzaldehyde was obtained.

[2732] _{^{1 H-NMR (CDCl 3)}} δppm: 1.
5-3.4 (15H, m), 2.40 (4H, t, J =
4.5 Hz), 3.61 (4H, t, J = 4.5H)
z), 4.88 (2H, s), 6.99 (1H, d, J
= 8.5 Hz), 7.3-7.55 (2H, m), 7.
7-7.9 (4H, m), 9.92 (1H, s).

Reference Example 40 4-formylcinnamic acid 10.1 g of dichloromethane 100
To the suspension, 5 drops of dimethylformamide and 6 ml of oxalyl chloride were added under ice-cooling, and the mixture was stirred overnight. The suspension was added dropwise to a suspension of 8.61 g of 2-aminobenzothiazole and 19.3 ml of triethylamine in 100 ml of dichloromethane under ice-cooling, and the mixture was stirred at the same temperature overnight. The precipitated crystals are collected by filtration and washed with water and methanol in this order to give 2
3.92 g of-(4-formylcinnamoylamino) benzothiazole was obtained.

[2734] Yellow powder ^{1 H-NMR (DMSO-d} 6) δppm: 7.09 (1
H, d, J = 16.0 Hz), 7.25-7.39 (1
H, m), 7.39-7.52 (1H, m), 7.70
-7.94 (4H, m), 7.94-8.06 (3H,
m), 10.03 (1H, s), 12.70 (1H,
s).

Using suitable starting materials, Reference Examples 36 and 4
Each compound described in Tables 10 to 25 was obtained in the same manner as in Example 1.

[2736]

[Table 10]

[2737]

[Table 11]

[2738]

[Table 12]

[2739]

[Table 13]

[2740]

[Table 14]

[2741]

[Table 15]

[2742]

[Table 16]

[2743]

[Table 17]

[2744]

[Table 18]

[2745]

[Table 19]

[2746]

[Table 20]

[2747]

[Table 21]

[2748]

[Table 22]

[2749]

[Table 23]

[2750]

[Table 24]

[2751]

[Table 25]

[2752] NMR of each compound shown in Tables 10 to 25
The spectrum is as follows.

(1) ¹ H-NMR (DMSO-d ₆ ) δp
pm: 2.08 (2H, q, J = 6.6 Hz), 2.6
2 (2H, t, J = 7.2 Hz), 4.13 (2H,
t, J = 4.1 Hz), 7.10 (2H, d, J = 8.
6 Hz), 7.19 (1H, d, J = 3.6 Hz),
7.45 (1H, d, J = 3.6 Hz), 7.85 (2
H, d, J = 8.6 Hz), 9.86 (1H, s), 1
2.13 (1H, s).

(2) ¹ H-NMR (CDCl ₃ ) δpp
m: 4.26 (2H, s), 7.01 (1H, d, J =
3.5 Hz), 7.06 (1H, d, J = 3.5H)
z), 8.04 (2H, d, J = 8 Hz), 8.19
(2H, d, J = 8 Hz), 10.15 (1H, s).

(3) ¹ H-NMR (CDCl ₃ ) δpp
m: 4.81 (2H, s), 7.05 (1H, d, J =
3.5Hz), 7.25-7.35 (2H, m), 7.
45-7.65 (2H, m), 7.50 (1H, d, J
= 3.5 Hz), 10.00 (1H, s), 10.06
(1H, brs).

(4) ¹ H-NMR (DMSO-d ₆ ) δp
pm: 7.09 (1H, d, J = 16.0 Hz), 7.
25-7.39 (1H, m), 7.39-7.52 (1
H, m), 7.70-7.94 (4H, m), 7.94
−8.06 (3H, m), 10.03 (1H, s), 1
2.70 (1H, s).

(5) ¹ H-NMR (DMSO-d ₆ ) δp
pm: 2.80 (2H, t, J = 7.9 Hz), 3.0
3 (2H, t, J = 7.9 Hz), 7.12-7.25
(1H, m), 7.38-7.55 (3H, m), 7.
84 (2H, d, J = 8.2 Hz), 9.96 (1H,
s) 12.12 (1H, s).

(6) ¹ H-NMR (CDCl ₃ ) δpp
m: 2.78 (2H, t, J = 7.6 Hz), 3.09
(2H, t, J = 7.6 Hz), 7.12-7.28
(2H, m), 7.28-7.45 (2H, m), 7.
60-7.95 (4H, m), 9.94 (1H, s),
11.52 (1H, s).

(7) ¹ H-NMR (DMSO-d ₆ ) δp
pm: 7.06 (1H, d, J = 15.8 Hz);
27 (1H, d, J = 3.6 Hz), 7.53 (1H,
d, J = 3.6 Hz), 7.69-8.10 (5H,
m), 10.04 (1H, s), 12.0-13.3
(1H, br).

(8) ¹ H-NMR (DMSO-d ₆ ) δp
pm: 5.07 (2H, s), 7.19 (1H, d, J
= 8.7 Hz), 7.27-7.40 (1H, m),
7.40-7.56 (1H, m), 7.77 (1H,
d, J = 7.5 Hz), 7.90 (2H, d, J = 8.
8 Hz), 7.98 (1H, d, J = 7.1 Hz),
9.89 (1H, s), 12.3-13.0 (1H, b
r).

(9) ¹ H-NMR (CDCl ₃ ) δpp
m: 7.3 to 7.45 (2H, m), 7.6 (1H,
m), 7.9 (1H, m), 8.00 (2H, d, J =
8 Hz), 8.15 (2H, d, J = 8 Hz), 10.
11 (1H, br).

(10) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 2.18 (3H, s), 2.26 (3H,
s), 6.99 (1H, d, J = 12.6 Hz), 7.
76 (1H, d, J = 12.6 Hz), 7.83 (2
H, d, J = 6.6 Hz), 7.97 (2H, d, J =
6.6 Hz), 10.03 (1H, s), 12.22
(1H, s).

(11) ¹ H-NMR (CDCl ₃ ) δpp
m: 2.38 (6H, s), 4.57 (2H, s),
7.06 (1H, d, J = 3.6 Hz), 7.51 (1
H, d, J = 3.6 Hz), 7.61 (2H, s),
9.92 (1H, s), 10.10 (1H, brs).

(12) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.13 (6H, t, J = 7.1 Hz), 2.93
(4H, q, J = 7.1 Hz), 3.79 (2H,
s), 5.01 (2H, s), 7.08 (1H, d, J
= 8.2 Hz), 7.23-7.35 (1H, m),
7.35-7.45 (1H, m), 7.74-7.87
(4H, m), 9.92 (1H, s), 10.71 (1
H, s).

(13) ¹ H-NMR (CDCl ₃ ) δpp
m: 2.33 (3H, s), 2.42-2.88 (8
H, m), 3.71 (2H, s), 4.92 (2H,
s), 7.02 (1H, d, J = 8.2 Hz), 7.2
7-7.50 (1H, m), 7.50-7.49 (1
H, m), 7.67-7.93 (4H, m), 9.93
(1H, s).

(14) ¹ H-NMR (CDCl ₃ ) δpp
m: 2.56 (3H, s), 3.74 (2H, s),
7.26-7.40 (1H, m), 7.40-7.52
(1H, m), 7.72-7.95 (3H, m), 7.
99 (1H, dd, J = 1.6 Hz, J = 8.0H
z), 8.35 (1H, d, J = 8.0 Hz);
11 (1H, s).

(15) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.29 (6H, t, J = 7.1 Hz), 2.98
-3.48 (8H, m), 5.20 (2H, s), 7.
22 (1H, d, J = 9.0 Hz), 7.35 (1H,
t, J = 7.6 Hz), 7.49 (1H, t, J = 7.
6Hz), 7.80 (1H, d, J = 7.8Hz),
7.85-7.98 (2H, m), 8.01 (1H,
d, J = 7.4 Hz), 9.91 (1H, s), 10.
36 (1H, br), 12.84 (1H, br).

(16) ¹ H-NMR (CDCl ₃ ) δpp
m: 2.86 (3H, s), 3.14-4.00 (12
H, m), 5.21 (2H, s), 7.22 (1H,
d, J = 7.8 Hz), 7.35 (1H, t, J = 7.
6Hz), 7.49 (1H, t, J = 7.6Hz),
7.78-7.87 (3H, m), 8.01 (1H,
d, J = 8.1 Hz), 9.90 (1H, s), 11.
60 (2H, br), 12.75 (1H, br).

(17) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.83-2.11 (2H, m), 3.06 (2
H, t, J = 7.3 Hz), 3.85 (2H, t, J =
5.2 Hz), 4.22 (1H, br), 4.85 (2
H, s), 6.98 (1H, d, J = 8.2 Hz),
7.28-7.41 (1H, m), 7.41-7.49
(1H, m), 7.74-7.86 (4H, m), 9.
92 (1H, s), 11.84 (1H, br).

(18) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.83-2.06 (2H, m), 2.25 (3
H, s), 2.32-2.76 (10H, m), 2.8
8 (2H, t, J = 7.7 Hz), 4.87 (2H, t, J = 7.7 Hz)
s), 6.97 (1H, d, J = 8.3 Hz), 7.3
0-7.42 (1H, m), 7.42-7.51 (1
H, m), 7.72-7.87 (4H, m), 9.94
(1H, s).

(19) ¹ H-NMR (CDCl ₃ ) δpp
m: 0.99 (6H, t, J = 7.1 Hz), 1.40
-1.61 (2H, m), 1.70-1.92 (4H,
m), 2.43-2.63 (6H, m), 3.56 (2
H, s), 3.98 (2H, t, J = 6.3 Hz),
6.86 (1H, d, J = 8.5 Hz), 7.28-
7.40 (1H, m), 7.40-7.51 (1H,
m), 7.70-7.91 (3H, m), 7.95 (1
H, d, J = 2.1 Hz), 9.89 (1H, s), 1
0.39-13.00 (1H, br).

(20) ¹ H-NMR (CDCl ₃ ) δpp
m: 0.97 (6H, t, J = 7.1 Hz), 2.10
-2.40 (2H, m), 2.40-2.68 (6H,
m), 3.54 (2H, s), 3.95-4.23 (2
H, m), 6.84 (1H, d, J = 8.5 Hz),
7.20-7.40 (2H, m), 7.58-7.88
(3H, m), 7.90 (1H, d, J = 2.1H)
z), 9.87 (1H, s). (21) ¹ H-NMR (DMSO-d ₆ ) δ ppm:
08-2.26 (2H, m), 2.74-3.02 (1
1H, m), 3.08-3.66 (6H, m), 5.2
0 (2H, s), 7.18 (1H, d, J = 9.6H)
z), 7.34 (1H, t, J = 7.6 Hz), 7.4
9 (1H, d, J = 7.6 Hz), 7.72-7.92
(3H, m), 8.01 (1H, d, J = 7.1H)
z), 9.90 (1H, s), 10.98 (2H, b
r).

(22) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.38-1.76 (2H, m), 1.76-2.
13 (6H, m), 2.13-2.70 (14H,
m), 2.88 (2H, t, J = 7.6 Hz), 2.9
5-3.18 (2H, m), 4.86 (2H, s),
6.97 (1H, d, J = 8.2 Hz), 7.31 −
7.42 (1H, m), 7.42-7.57 (1H,
m), 7.73-7.87 (4H, m), 9.91 (1
H, s).

(23) ¹ H-NMR (CDCl ₃ ) δpp
m: 3.25 (3H, s), 4.27 (2H, s),
6.83 (1H, d, J = 8.9 Hz), 7.30-
7.40 (1H, m), 7.40-7.52 (1H,
m), 7.70-7.88 (4H, m), 9.62 (1
H, br), 9.86 (1H, s).

(24) ¹ H-NMR (CDCl ₃ ) δpp
m: 2.42 (3H, s), 2.6-2.9 (8H,
m), 3.81 (2H, s), 7.25-7.5 (2
H, m), 7.75-7.95 (3H, m), 8.00
(1H, dd, J = 2 Hz, J = 8 Hz), 8.35
(1H, d, J = 8 Hz), 10.12 (1H, s),
14.5 (1H, br).

(25) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 1.92-2.45 (6H, m), 2.60-
3.21 (9H, m), 3.21-3.76 (4H,
m), 3.76-4.16 (4H, m), 5.17 (2
H, s), 7.15 (1H, d, J = 8.8 Hz),
7.31 (1H, t, J = 6.9 Hz), 7.45 (1
H, t, J = 6.9 Hz), 7.68-7.92 (3
H, m), 7.99 (1H, d, J = 7.0 Hz),
9.87 (1H, s), 10.73 (1H, br), 1
1.78 (1H, br), 12.80 (1H, s).

(26) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 1.28 (6H, t, J = 7.1 Hz), 2.
00-2.38 (6H, m), 2.68-2.90 (2
H, m), 2.90-3.25 (8H, m), 3.47
-3.83 (3H, m), 5.18 (2H, s), 7.
18 (1H, d, J = 8.7 Hz), 7.34 (1H,
t, J = 7.7 Hz), 7.45 (1H, t, J = 7.
7Hz), 7.78-7.86 (3H, m), 8.00
(1H, d, J = 7.0 Hz), 9.90 (1H,
s), 10.78 (2H, br), 12.80 (1H,
br).

(27) ¹ H-NMR (CDCl ₃ ) δpp
m: 2.31 (3H, s), 2.37-2.80 (8
H, m), 2.90 (2H, t, J = 5.7 Hz),
4.19 (2H, t, J = 5.7 Hz), 4.81 (2
H, s), 6.50-6.67 (2H, m), 7.15
-7.53 (3H, m), 7.75-7.96 (3H,
m) 10.33 (1H, s).

(28) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.09 (6H, t, J = 7.1 Hz), 2.08
(2H, quint, J = 6.2 Hz), 2.65 (4
H, q, J = 7.1 Hz), 2.73 (2H, t, J =
6.2 Hz), 4.17 (2H, t, J = 6.2H)
z), 4.83 (2H, s), 6.50-6.68 (2
H, m), 7.12-7.56 (4H, m), 7.76
-7.92 (2H, m), 10.35 (1H, s).

(29) ¹ H-NMR (CDCl ₃ ) δpp
m: 2.06 (2H, quint, J = 6.5 Hz),
2.31 (3H, s), 2.32-2.80 (10H,
m), 4.11 (2H, t, J = 6.5 Hz), 4.8
2 (2H, s), 6.52-6.63 (2H, m),
7.10-7.56 (3H, m), 7.76-7.96
(3H, m), 10.35 (1H, s).

(30) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 2.40 (3H, s), 5.06 (2H, s)
s), 7.15-7.40 (3H, m), 7.65 (1
H, d, J = 8.4 Hz), 7.77 (1H, s),
7.89 (2H, d, J = 8.6 Hz), 9.88 (1
H, s), 12.61 (1H, s).

(31) ¹ H-NMR (DMSO-d ₆ ) δ
3. ppm: 2.27 (3H, d, J = 0.9 Hz);
98 (2H, s), 6.79 (1H, d, J = 1.0H
z), 7.12-7.25 (2H, m), 7.82-
7.96 (2H, m), 9.88 (1H, s), 12.
0-12.7 (1H, br).

(32) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 1.26 (9H, s), 4.98 (2H,
s), 6.78 (1H, s), 7.15 (2H, d, J
= 8.8 Hz), 7.90 (2H, d, J = 8.8H)
z), 9.88 (1H, s), 12.42 (1H,
s).

(33) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 5.05 (2H, s), 7.19 (2H, d,
J = 8.8 Hz), 7.25-7.55 (3H, m),
7.67 (1H, s), 7.80-8.02 (4H,
m), 9.89 (1H, s), 12.60 (1H,
s).

(34) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 1.57-1.84 (7H, m), 1.84-
2.05 (3H, m), 2.20 (1H, q, J = 8.
5Hz), 2.30-2.72 (8H, m), 2.74
-3.12 (3H, m), 3.16-3.30 (1H,
m), 4.87 (2H, s), 6.97 (1H, d, J
= 8.3 Hz), 7.27-7.41 (1H, m),
7.41-7.53 (1H, m), 7.70-7.93
(4H, m), 9.91 (1H, s).

(35) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.67-2.95 (20H, m), 3.55-
3.95 (3H, m), 4.90 (2H, s), 6.9
6 (1H, d, J = 8.3 Hz), 7.25-7.53
(2H, m), 7.55-7.95 (4H, m), 9.
90 (1H, s).

(36) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.55-3.80 (23H, m), 4.91 (2
H, s), 6.96 (1H, d, J = 8.4 Hz),
7.25-7.52 (2H, m), 7.65-7.78
(4H, m), 9.88 (1H, s).

(37) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.75-2.95 (16H, m), 3.55-
3.95 (7H, m), 4.88 (2H, s), 6.9
5 (1H, d, J = 8.3 Hz), 7.28-7.55
(2H, m), 7.65-7.95 (4H, m), 9.
90 (1H, s).

(38) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.75-3.00 (20H, m), 2.27 (3
H, s), 3.58-3.98 (3H, m), 4.88
(2H, s), 6.95 (1H, d, J = 8.3H)
z), 7.30-7.52 (2H, m), 7.65-
7.90 (4H, m), 9.89 (1H, s).

(39) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.5-3.4 (15H, m), 2.40 (4H,
t, J = 4.5 Hz), 3.61 (4H, t, J = 4.
5 Hz), 4.88 (2H, s), 6.99 (1H,
d, J = 8.5 Hz), 7.3-7.55 (2H,
m), 7.7-7.9 (4H, m), 9.92 (1H,
s).

(40) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.5-3.1 (23H, m), 2.24 (3H,
s), 4.91 (2H, s), 7.00 (1H, d, J
= 8 Hz), 7.3-7.5 (2H, m), 7.7-
7.9 (4H, m), 9.91 (1H, s).

(41) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.7-2.0 (4H, m), 2.33 (3H,
s), 2.5-3.0 (12H, m), 4.87 (2
H, s), 6.97 (1H, d, J = 8 Hz), 7.3
-7.9 (6H, m), 9.91 (1H, s).

(42) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 1.30-3.51 (25H, m), 3.51
-3.75 (2H, m), 5.16 (2H, s), 7.
09 (1H, d, J = 8.9 Hz), 7.27-7.3
9 (1H, m), 7.39-7.52 (1H, m),
7.70-7.84 (3H, m), 7.98-8.09
(1H, m), 9.86 (1H, s), 10.58-1
1.17 (3H, m).

(43) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 1.25 (6H, t, J = 7.2 Hz);
00-3.50 (5H, m), 7.42 (1H, dd,
J = 1.6 Hz, J = 8.2 Hz), 7.75 (1H,
d, J = 8.4 Hz), 7.97 (1H, d, J = 1.
2 Hz), 8.07 (2H, d, J = 8.4 Hz),
8.30 (2H, d, J = 8.4 Hz) 10.13
(1H, s), 11.3-12.5 (1H, br).

(44) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 6.58 (1H, d, J = 16.8 Hz),
7.15-8.15 (11H, m), 10.00 (1
H, s), 12.65 (1H, s).

(45) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 1.45 (6H, s), 2.68-3.01
(2H, m), 2.77 (3H, s), 3.21-3.
85 (10H, m), 5.24 (2H, s), 7.10
(1H, d, J = 8.3 Hz), 7.29-7.40
(1H, m), 7.40-7.52 (1H, m), 7.
74-7.89 (3H, m), 7.93-8.05 (1
H, m), 9.89 (1H, s), 11.10-13.
0 (3H, m).

(46) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.86 (2H, quint, J = 7.5 Hz),
2.18-2.63 (10H, m), 2.30 (3H,
s), 3.05 (2H, t, J = 7.5 Hz), 4.8
2 (2H, s), 6.24-7.01 (2H, m),
7.10-7.59 (3H, m), 7.73-7.93
(3H, m) 10.17 (1H, s).

Example 1 250 mg of 2- (benzoylmethyl) pyridine, 4-
A solution of [(2-benzothiazolyl) aminocarbonyl] benzaldehyde (300 mg), 5 drops of piperidine and 5 drops of acetic acid in 30 ml of benzene was refluxed for 10 hours while removing water. After extraction with ethyl acetate, silica gel column chromatography (eluent; ethyl acetate: n-hexane = 1: 1).
After purification in 2), recrystallization from ethyl acetate-n-hexane gave 2- {4- [2-benzoyl-2- (2-pyridyl) vinyl] benzoylamino} benzothiazole.
3 g were obtained.

218-258 ° C. Light yellow powder ¹ H-NMR (DMSO-d ₆ ) δ ppm: 7.25-
8.1 (17H, m), 8.49 (1H, d, J = 5H
z), 12.83 (1H, br).

Example 2 2- {4- [2- (4-methoxymethoxy-3-methoxycarbonylbenzoyl) -2- (1,2,4-triazol-1-yl) vinyl] benzoylamino} benzothiazole 2 g Was added to a solution of dimethylformamide in 40 ml of dimethylformamide, and the mixture was stirred at room temperature for 1 hour. Water was added, the white crystals were collected by filtration, dissolved in ethyl acetate, dried, and the solvent was distilled off. Recrystallization from ethyl acetate-n-hexane gave 2- {4- [2- (4-methoxymethoxy-3-methoxycarbonylbenzoyl) -2-].
(1,2,4-triazol-1-yl) -1-ethylthioethyl] benzoylamino {benzothiazole
9 g were obtained.

[2801] _{^{1 H-NMR (CDCl 3)}} δ: 1.05-
1.4 (3H, m), 2.16 (0.45 × 2H, q,
J = 7.5 Hz), 2.43 (0.55 × 2H, q, J
= 7.5 Hz), 3.46 (0.45 × 3H, s),
3.52 (0.55 × 3H, s), 3.92 (0.45
* 3H, s), 3.94 (0.55 * 3H, s), 4.
77 (0.55 × 1H, d, J = 11 Hz), 4.88
(0.45 × 1H, d, J = 10 Hz), 5.27
(0.45 × 2H, s), 5.35 (0.55 × 2H, s)
s), 6.31 (0.45 × 1H, d, J = 10H)
z), 6.32 (0.55 × 1H, d, J = 11H)
z), 7.1-8.6 (13H, m), 10.83 (1
H, br).

Example 3 To a suspension of cuprous iodide (400 mg) in tetrahydrofuran (20 ml) was added dropwise 1.6 ml of a 1.6 M solution of n-butyllithium in n-hexane at -40 ° C over 5 minutes under an argon atmosphere. After stirring at −60 ° C. for 2 hours, 2- {4- [2-benzoyl-2- (1,2,4-triazol-1-yl) vinyl] cinnamoylamino} benzothiazole 4
80 mg was added and the mixture was stirred for 2 hours. After stirring at room temperature overnight,
Saturated aqueous ammonium chloride was added, and the mixture was extracted with ethyl acetate. After washing with water and drying, the solvent was distilled off. The obtained residue was purified by silica gel column chromatography (eluent; dichloromethane: methanol = 100: 1 → 10: 1), and crystallized from ethyl acetate-n-hexane to give 2-
60 mg of {4- [2-benzoyl-2- (1,2,4-triazol-1-yl) -1-n-butylethyl] cinnamoylamino} benzothiazole was obtained.

Melting point: 108-111 ° C. White powder Example 4 2- [4- (2-benzoyl-2-ethoxycarbonylvinyl) cinnamoylamino] benzothiazole 0.8
1 g of a 5N aqueous sodium hydroxide solution was added to a 15 ml solution of g of ethanol, and the mixture was stirred at room temperature for 30 minutes. 30 ml of water
Was added to remove insolubles by filtration, and the filtrate was acidified with hydrochloric acid.
The precipitated crystals are collected by filtration and washed with methanol and diethyl ether to give 2- [4- (2-benzoyl-2).
-Carboxyvinyl) cinnamoylamino] benzothiazole (0.66 g) was obtained.

Melting point 252-262 ° C. yellow powder Example 5 2- [4- (2-benzoyl-2-carboxyvinyl)
To 0.25 g of [cinnamoylamino] benzothiazole was added 2 ml of thionyl chloride, and the mixture was heated under reflux for 10 minutes. The residue obtained by distilling off thionyl chloride was cooled under ice-cooling to 0.12 m of N-methylpiperazine and 0.23 m of triethylamine.
ml of dichloromethane in a 5 ml solution. 1 at the same temperature
After reacting for 5 minutes, the reaction solution was washed with brine, dried over magnesium sulfate, and concentrated. The obtained residue was purified by silica gel column chromatography (eluent; dichloromethane: methanol = 20: 1), and then recrystallized from ethyl acetate-n-hexane to give 2- (4-
[2-Benzoyl-2- (4-methyl-1-piperazinyl) carbonylvinyl] cinnamoylamino} benzothiazole 0.05 g was obtained.

Melting point: 135-138 ° C. light yellow powder Example 6 4-[(2-benzothiazolyl) aminocarbonyl] benzaldehyde 5 g, N-acetylglycine 2.07
g, 1 g of sodium acetate and 20 ml of acetic anhydride at 80 ° C.
For 3 hours. 50 ml of methanol was added, the crystals were collected by filtration, washed with methanol, and recrystallized from dimethylformamide-methanol to give 2- [4
-(2-methyl-5-oxo-1,3-oxazolyl)
Methylidenebenzoylamino] benzothiazole 5.3
7 g were obtained.

[2806] Melting point: 238 ° C. (decomposition) Yellow powder: The following starting materials were used in the same manner as in Example 1 using appropriate starting materials.
1-205, 207, 209, 210, 216, 21
7, 219, 220, 222, 223, 229, 23
4, 242, 246, 247, 251-253, 25
5, 256, 258-262 and 264-330 were obtained.

Using suitable starting materials, in the same manner as in Example 2 or 3, the following Nos. 206, 208, 211 to 215,
218, 221, 224 to 228, 230 to 233, 2
35-241, 243-245, 248-250, 25
4, 257 and 263 compounds were obtained.

[2808]

[Table 26]

[2809]

[Table 27]

[2810]

[Table 28]

[2811]

[Table 29]

[2812]

[Table 30]

[2813]

[Table 31]

[2814]

[Table 32]

[2815]

[Table 33]

[2816]

[Table 34]

[2817]

[Table 35]

[2818]

[Table 36]

[2819]

[Table 37]

[2820]

[Table 38]

[2821]

[Table 39]

[2822]

[Table 40]

[2823]

[Table 41]

[2824]

[Table 42]

[2825]

[Table 43]

[2826]

[Table 44]

[2827]

[Table 45]

[2828]

[Table 46]

[2829]

[Table 47]

[2830]

[Table 48]

[2831]

[Table 49]

[2832]

[Table 50]

[2833]

[Table 51]

[2834]

[Table 52]

[2835]

[Table 53]

[2836]

[Table 54]

[2837]

[Table 55]

[2838]

[Table 56]

[2839]

[Table 57]

[2840]

[Table 58]

[2841]

[Table 59]

[2842]

[Table 60]

[2843]

[Table 61]

[2844]

[Table 62]

[2845]

[Table 63]

[2846]

[Table 64]

[2847]

[Table 65]

[2848]

[Table 66]

[2849]

[Table 67]

[2850]

[Table 68]

[2851]

[Table 69]

[2852]

[Table 70]

[2853]

[Table 71]

[2854]

[Table 72]

[2855]

[Table 73]

[2856]

[Table 74]

[2857]

[Table 75]

[2858]

[Table 76]

[2859]

[Table 77]

[2860]

[Table 78]

[2861]

[Table 79]

[2862]

[Table 80]

[2863]

[Table 81]

[2864]

[Table 82]

[2865]

[Table 83]

[2866]

[Table 84]

[2867]

[Table 85]

[2868]

[Table 86]

[2869]

[Table 87]

[2870]

[Table 88]

[2871]

[Table 89]

[2872]

[Table 90]

[2873]

[Table 91]

[2874]

[Table 92]

[2875]

[Table 93]

[2876]

[Table 94]

[2877]

[Table 95]

[2787]

[Table 96]

[2879]

[Table 97]

[2880]

[Table 98]

[2881]

[Table 99]

[2882]

[Table 100]

[2883]

[Table 101]

[2884]

[Table 102]

[2885]

[Table 103]

[2886]

[Table 104]

[2887]

[Table 105]

[2888]

[Table 106]

[2889]

[Table 107]

[2890]

[Table 108]

[2891]

[Table 109]

[2892]

[Table 110]

[2893]

[Table 111]

[2894]

[Table 112]

[2895]

[Table 113]

[2896]

[Table 114]

[2897]

[Table 115]

[2898]

[Table 116]

[2899]

[Table 117]

[2900]

[Table 118]

[2901]

[Table 119]

[2902]

[Table 120]

[2903]

[Table 121]

[2904]

[Table 122]

[2905]

[Table 123]

[2906]

[Table 124]

[2907]

[Table 125]

[2908]

[Table 126]

[2909]

[Table 127]

[2910]

[Table 128]

[2911]

[Table 129]

[2912]

[Table 130]

[2913]

[Table 131]

[2914]

[Table 132]

[2915]

[Table 133]

[2916]

[Table 134]

[2917]

[Table 135]

[2918]

[Table 136]

[2919]

[Table 137]

[2920]

[Table 138]

[2921]

[Table 139]

[2922]

[Table 140]

[2923]

[Table 141]

[2924]

[Table 142]

[2925]

[Table 143]

[2926]

[Table 144]

[2927]

[Table 145]

[2928]

[Table 146]

[2929]

[Table 147]

[2930]

[Table 148]

[2931]

[Table 149]

[2932]

[Table 150]

[2933]

[Table 151]

[2934]

[Table 152]

[2935]

[Table 153]

[2936]

[Table 154]

[2937]

[Table 155]

[2938]

[Table 156]

[2939]

[Table 157]

[2940]

[Table 158]

[2941]

[Table 159]

[2942]

[Table 160]

[2943]

[Table 161]

[2944]

[Table 162]

[2945]

[Table 163]

[2946]

[Table 164]

[2947]

[Table 165]

[2948]

[Table 166]

[2949]

[Table 167]

[2950]

[Table 168]

[2951]

[Table 169]

[2952]

[Table 170]

[2953]

[Table 171]

[2954]

[Table 172]

[2955]

[Table 173]

[2956]

[Table 174]

[2957]

[Table 175]

[2958]

[Table 176]

[2959]

[Table 177]

[2960]

[Table 178]

[2961]

[Table 179]

[2962]

[Table 180]

[2963]

[Table 181]

[2964]

[Table 182]

[2965]

[Table 183]

[2966]

[Table 184]

[2967]

[Table 185]

[2968]

[Table 186]

[2969]

[Table 187]

[2970]

[Table 188]

[2971]

[Table 189]

[2972]

[Table 190]

NM of each compound shown in Tables 26 to 190
The R spectrum is as follows.

(1) ¹ H-NMR (DMSO-d ₆ ) δp
pm: 2.48-2.55 (2H, m), 2.9-3.
1 (2H, m), 6.92-7.07 (4H, m),
7.25-7.50 (2H, m), 7.59-7.79
(7H, m), 7.99 (1H, d, J = 7 Hz),
8.29 (1H, s), 8.71 (1H, s), 10.
51 (1H, s), 12.65 (1H, s).

(2) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.21-1.31 (3H, m), 2.6-2.8
(2H, m), 2.8-3.05 (2H, m), 3.8
5-4.2 (2H, m), 6.65 (1H, d, J = 1)
5.6 Hz), 6.85-7.15 (4H, m), 7.
15-7.75 (9H, m), 7.75-8.10 (4
H, m).

(3) ¹ H-NMR (CDCl ₃ ) δpp
m: 2.65-2.8 (2H, m), 2.85-3.0
5 (2H, m), 3.39 (3H, s), 6.65 (1
H, d, J = 16.5 Hz), 6.8-7.1 (3H,
m), 7.2-7.65 (10H, m), 7.75-
8.0 (3H, m).

(4) ¹ H-NMR (DMSO-d ₆ ) δp
pm: 1.31 (6H, s), 3.24 (3H, s),
6.62 (1H, d, J = 16 Hz), 7.0 (2H,
d, J = 8.4 Hz), 7.44 (1H, d, J = 16)
Hz), 7.51-7.69 (5H, m), 7.78
(3H, dd, J = 8.4 Hz, J = 6.8 Hz),
8.29 (1H, s), 8.74 (1H, s), 10.
65 (1H, s).

(6) ¹ H-NMR (CDCl ₃ ) δpp
m: 3.50 (3H, s), 5.25 (2H, s),
6.88 (1H, s), 7.04-7.19 (5H,
m), 7.26-7.57 (5.5H, m), 7.74
-7.95 (5.5H, m).

(7) ¹ H-NMR (DMSO-d ₆ ) δp
pm: 2.203 (3H, s), 6.97-7.05
(2H, m), 7.20-7.60 (4H, m), 7.
65-7.90 (8H, m), 8.0 (1H, d, J =
7 Hz), 9.0-9.05 (1H, br), 10.6
(1H, s), 12.7 (1H, s).

(8) ¹ H-NMR (CDCl ₃ ) δpp
m: 6.8 (1H, d, J = 9 Hz), 7.02 (2
H, d, J = 8.6 Hz), 7.21 (2H, d, J =
8.3 Hz), 7.35-8.0 (8H, m), 8.2
4 (2H, d, J = 8.3 Hz), 9.23 (1H,
s).

(9) ¹ H-NMR (CDCl ₃ ) δpp
m: 3.54 (3H, s), 3.83 (3H, s),
3.93 (3H, s), 5.34 (2H, s), 7.0
0-7.62 (9H, m), 7.73-8.04 (4
H, m).

(10) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 3.78 (3H, s), 6.95 (2H, d,
J = 8.4 Hz), 7.22 (2H, d, J = 8.2H)
z), 7.29 (1H, d, J = 3.4 Hz), 7.5
6 (1H, d, J = 3.4 Hz), 7.86 (2H,
d, J = 8.4 Hz), 7.98 (1H, s), 8.0
1 (2H, d, J = 8.2 Hz), 10.61 (1H,
s), 12.70 (1H, s).

(11) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 2.85 (3H, s), 3.03 (3H,
s), 3.80 (2H, s), 6.96 (1H, d, J
= 16.5 Hz), 7.03 (2H, d, J = 9H)
z), 7.1-7.85 (14H, m), 7.99 (1
H, d, J = 7 Hz), 12.63 (1H, s).

(12) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 3.79 (3H, s), 3.84 (3H, s)
s), 6.76-8.15 (12H, m), 10.30.
(1H, s), 12.87 (1H, brs).

(13) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 3.79 (3H, s), 3.84 (3H, s)
s), 6.66-8.13 (10H, m), 10.31
(1H, s), 12.63 (1H, brs).

(14) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 3.8 (3H, s), 6.75-7.8 (12
H, m), 7.9-8.1 (3H, m), 10.17
(1H, s), 12.8-13.0 (1H, br).

(15) ¹ H-NMR (CDCl ₃ + DMS
_{O-d 6) δppm: 3.32} (3H, s), 3.50
(3H, s), 5.26 (2H, s), 7.0-7.2
(6H, m), 7.25-7.5 (2H, m), 7.5
8. (1H, s), 7.75-7.9 (4H, m),
10 (2H, d, J = 8.5 Hz), 12.54 (1
H, br).

(16) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 0.56-0.95 (3H, m), 0.95-
1.36 (2H, m), 1.36-1.94 (2H,
m), 3.96-4.53 (2H, m), 6.62-
8.12 (15H, m), 10.60 (1H, s), 1
2.66 (1H, s).

(17) ¹ H-NMR (CDCl ₃ ) δpp
m: 3.46 (1.4 H, s), 3.54 (1.6 H,
s), 3.92 (1.4H, s), 3.93 (1.6
H, s), 5.25 (0.87H, s), 5.33
(1.13H, s), 7.0-7.7 (10H, m),
7.85-7.80 [all 3H, 7.85 (d, J = 8.
5 Hz), 7.91 (d, J = 8.5 Hz)], 8.0
8-8.26 [all 2H, 8.08 (s), 8.15
(S), 8.17 (s), 8.26 (s)].

(18) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 3.40 (3H, s), 3.82 (3H, s)
s), 5.29 (2H, s), 6.96 (1H, d, J
= 16 Hz), 7.07 (2H, d, J = 8.4H)
z), 7.2 (1H, d, J = 8.4 Hz), 7.3-
7.5 (5H, m), 7.61 (2H, d, J = 8.4)
Hz), 7.71-7.76 (2H, m), 7.99
(1H, d, J = 7.8 Hz), 8.3 (1H, s),
8.73 (1H, s), 12.6 (1H, s).

(19) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 3.79 (s), 3.81 (s) [all 3H],
6.77 (0.6H, d, J = 8.2 Hz), 6.91
(0.6H, d, J = 8.4 Hz), 7.16 (0.6
H, d, J = 8.4 Hz), 7.25-7.60 (5.
5H, m), 7.7 (2H, d, J = 13.6 Hz),
8.0-8.15 (3H, m), 8.15 (0.5H,
s), 8.27 (0.5H, s), 8.71 (0.4
H, s), 9.12 (0.54H, s), 10.2
(0.53H, s), 10.38 (0.5H, s), 1
2.7-13.0 (1H, br).

(20) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 3.79 (s), 3.80 (s) [all 3H],
6.75-7.07, 7.26-7.78 [all 13H,
m], 8.0 (1H, d, J = 8 Hz), 8.14
(0.2H, s), 8.29 (0.8H, s), 8.7
1 (0.8H, s), 9.11 (0.2H, s), 10
-10.5 (1H, br), 12.64 (1H, s).

(21) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 3.81 (3H, s), 3.83 (3H, s)
s), 3.89 (3H, s), 6.90-7.24 (4
H, m), 7.24-7.88 (8H, m), 7.95
-8.09 (2H, m), 12.67 (1H, s).

(22) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.36 (3H, m), 4.39 (2H, m),
5.00 (2H, m), 6.2-8.3 (18H,
m).

(23) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 2.30 (3H, s), 3.82 (3H,
s), 7.1-7.35 (3H, m), 7.35-7.
60 (6H, m), 7.60-7.85 (3H, m),
7.90-8.10 (3H, m).

(24) ¹ H-NMR (CDCl ₃ ) δpp
m: 4.26 (2H, d, J = 6 Hz), 5.52 (1
H, br), 6.40 (1H, dt, J = 16 Hz, J
= 6 Hz), 6.58 (1H, d, J = 16 Hz),
6.85 (2H, d, J = 8 Hz), 7.0-7.7
(10H, m), 7.81 (2H, d, J = 8 Hz),
8.16 (1H, s), 8.20 (1H, s).

(25) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.37, 1.47 [all 3H, 1.37 (t, J =
6 Hz), 1.47 (t, J = 6 Hz)], 2.29,
2.36 [all 3H, 2.29 (s), 2.36
(S)], 4.11, 4.3 [all 2H, 4.11 (q,
J = 6 Hz), 4.3 (q, J = 6 Hz)], 6.6
7, 6.96, 7.3-7.5, 7.7-8.1 [all 1
6H, m, 6.67 (d, J = 12 Hz), 6.96
(D, J = 7 Hz)].

(26) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 2.17 (6H, s), 2.6 (2H, t, J
= 5.6 Hz), 4.1 (2H, t, J = 5.6H)
z), 6.9 (2H, d, J = 8.8 Hz), 7.25
−7.50 (4H, m), 7.65−7.8 (2H,
m), 7.87 (2H, d, J = 8.8 Hz), 7.9
7-8.04 (3H, m), 8.15 (1H, s),
9.18 (1H, s), 12.2-13.5 (1H, b
r).

(27) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.37 (3H, t, J = 7.3 Hz), 3.56
(3H, s), 3.93 (3H, s), 4.13 (2
H, q, J = 7.3 Hz), 5.34 (2H, s),
7.03-8.22 (13H, m).

(28) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 1.05-1.60 (3H, m), 3.72-
4.00 (3H, m), 4.05-4.67 (2H,
m), 6.75-8.80 (12H, m), 10.31
(1H, brs), 12.70 (1H, brs).

(29) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.14 (3H, t, J = 7.1 Hz), 2.71
(2H, q, J = 7.1 Hz), 3.72 (3H,
s), 6.90-8.10 (9H, m).

(30) ¹ H-NMR (CDCl ₃ ) δpp
m: 3.61 (3H, s), 3.82 (3H, s),
3.86 (6H, s), 5.23 (2H, s), 7.0
3-7.47 (5H, m), 7.13 (2H, s),
7.77-8.03 (4H, m).

(31) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 3.72 (3H, s), 3.80 (3H, s)
s), 3.83 (3H, s), 7.18 (1H, s),
7.20 (1H, s), 7.23-7.63 (4H,
m), 7.73-8.20 (5H, m), 9.64 (1
H, brs).

(32) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 1.70-2.20 (3H, m), 2.20-
2.45 (1H, m), 3.48 (2H, q, J = 6.
5 Hz), 5.06 (1H, d, J = 14.8 Hz),
5.20-5.32 (1H, m), 7.10 (1H, d
d, J = 8.6 Hz, J = 10.8 Hz), 7.23-
7.60 (7H, m), 7.78 (1H, d, J = 8.
2 Hz), 8.04 (3H, t, J = 7.8 Hz),
8.30-8.41 (3H, m), 12.95 (1H,
s).

(33) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 4.34 (1H, dd, J = 3 Hz, J = 7H
z), 5.00 (1H, dd, J = 3 Hz, J = 7H
z), 5.60 (1H, d, J = 7 Hz), 5.69
(1H, d, J = 7 Hz), 6.90 (1H, d, J =
8 Hz), 7.25-8.1 (14H, m), 8.0
8, 8.27 (1H, s), 8.70, 9.16 (1
H, s), 11.84 (1H, br).

(34) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 1.37 (9H, s), 2.99 (2H, t,
J = 6.0 Hz), 3.25 (2H, t, J = 6.0H)
z), 6.80-6.97 (1H, br), 7.11
(2H, d, J = 8.4 Hz), 7.30-7.40
(1H, m), 7.40-7.53 (1H, m), 7.
78 (1H, d, J = 7.6 Hz), 8.03 (3H,
t, J = 6.2 Hz), 8.19 (1H, s), 8.3
1 (1H, s), 8.60 (1H, s), 12.93
(1H, s).

(35) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 1.32, 1.44 (9H, each s), 1.65
-2.10, 2.15 to 2.45 (all 4H, m);
39 (2H, t, J = 7.0 Hz), 5.08-5.2
2, 5.32-5.40 (all 1H, m), 7.11 (2
H, d, J = 8.4 Hz), 7.29-7.40 (1
H, m), 7.40-7.53 (1H, m), 7.78
(1H, d, J = 8.0 Hz), 8.04 (3H, t,
J = 8.4 Hz), 8.30-8.42 (2H, m),
8.65 (1H, d, J = 4.8 Hz), 12.95
(1H, s).

(36) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.20-1.56 (6H, m), 3.54 (3
H, s), 4.03-4.23 (4H, m), 5.32
(2H, m), 7.00-8.00 (13H, m).

(37) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.31-1.55 (6H, m), 4.06-4.
43 (4H, m), 6.75-8.11 (12H,
m).

(38) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.37 (3H, t, J = 7.4 Hz), 1.41
(3H, s), 1.48 (3H, s), 3.89-4.
24 (6H, m), 4.4-4.6 (1H, m),
56 (1H, d, J = 15.6 Hz), 6.88 (2
H, d, J = 8.4 Hz), 7.0 (2H, d, J =
8.8 Hz), 7.17 (2H, d, J = 8 Hz),
7.35-7.55 (2H, m), 7.67 (1H,
s), 7.71-7.79 (2H, m), 7.89-
8.0 (3H, m).

(39) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.37 (3H, t, J = 7.4 Hz), 2.4-
2.7 (6H, m), 3.7-3.85 (4H, m),
4.05-4.25 (5H, m), 6.56 (1H,
d, J = 15.6 Hz), 6.9 (2H, d, J = 8.
5 Hz), 7.0 (2H, d, J = 8.8 Hz), 7.
2-7.26 (3H, m), 7.35-7.55 (2
H, m), 7.68-7.80 (2H, m), 7.92
(3H, d, J = 8.8 Hz), 11.6-12.0
(1H, br).

(40) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.37 (3H, t, J = 7.2 Hz), 2.75
-2.85 (1H, m), 2.95-3.0 (1H,
m), 3.35-3.5 (1H, m), 3.95-4.
15 (1H, m), 4.13 (2H, q, J = 7.2H
z), 4.3-4.45 (1H, m), 6.65 (1
H, d, J = 13.5 Hz), 6.9 (2H, d, J =
8.2 Hz), 7.02 (2H, d, J = 8.8H)
z), 7.2 (2H, d, J = 8.2 Hz), 7.35
-7.55 (2H, m), 7.68-7.8 (3H,
m), 7.92 (3H, d, J = 8.8 Hz), 11.
9-12.0 (1H, br).

(41) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 1.21 (3H, t, J = 7.2 Hz);
4-3.55 (2H, m), 3.75-4.2 (5H,
m), 6.98 (1H, d, J = 15.8 Hz), 7.
10-7.16 (4H, m), 7.3 (1H, t, J =
7.2 Hz), 7.44 (1H, t, J = 7.0H)
z), 7.62 (2H, d, J = 8.2 Hz), 7.7
1-7.78 (2H, m), 7.89-8.01 (4
H, m), 12.3-13.0 (1H, br).

(42) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.09 (6H, t, J = 7.2 Hz), 1.36
(3H, t, J = 7.2 Hz), 2.4-3.85 (7
H, m), 3.7-4.25 (5H, m), 6.59
(1H, d, J = 15.5 Hz), 6.89 (2H,
d, J = 8.5 Hz), 6.92 (2H, d, J = 9H)
z), 7.2 (2H, d, J = 8.5 Hz), 7.3-
7.5 (3H, m), 7.65-7.85 (3H,
m), 7.89-8.0 (3H, m).

(43) ¹ H-NMR (CDCl ₃ ) δpp
m: 0.96-1.43 (3H + 0.5 × 3H, m),
1.60 (0.5 × 3H, t, J = 7.2 Hz);
10-2.42 (2H, m), 3.44 (0.5 × 3
H, s), 3.49 (0.5 x 3H, s), 3.83
(0.5 × 3H, s), 3.93 (0.5 × 3H, s)
s), 4.02-4.31 (2H, m), 4.98 (1
H, d, J = 11.4 Hz), 5.24 (0.5 × 2
H, s), 5.30 (0.5 x 2H, s), 5.67
(0.5 × 1H, d, J = 11.4 Hz) 5.70
(0.5 × 1H, d, J = 11.4 Hz), 6.98−
8.19 (11H, m), 11.68 (1H, br)
s).

(44) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.04-1.14 (3H, m), 2.12-2.
43 (2H, m), 3.81 (0.5 × 3H, s),
3.88 (0.5 × 3H, s), 3.90 (0.5 × 3H, s)
H, s), 4.24 (0.5 × 3H, s), 4.96
(0.5 × 1H, d, J = 11.3 Hz), 5.02
(0.5 × 1H, d, J = 11.3 Hz), 5.75
(0.5 × 1H, d, J = 11.3 Hz), 5.78
(0.5 × 1H, d, J = 11.3 Hz), 6.82
(0.5 × 2H, d, J = 9.0 Hz), 6.96
(0.5 × 2H, d, J = 9.0 Hz), 7.20−
7.65 (5H, m), 7.80-8.03 (4H,
m), 8.14 (1H, d, J = 9.0 Hz), 11.
47 (1H, brs).

(45) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.07 (0.5 × 3H, t, J = 7.3 Hz),
1.10 (0.5 × 3H, t, J = 7.3 Hz);
05-2.44 (2H, m), 3.41 (0.5 × 3
H, s), 3.47 (0.5 × 3H, s), 3.89
(0.5 × 3H, s), 4.23 (0.5 × 3H, s)
s), 4.96 (0.5 × 1H, d, J = 11.2H)
z), 5.01 (0.5 × 1H, d, J = 11.2H)
z), 5.17 (0.5 × 2H, s), 5.24 (0.
5 × 2H, s), 5.75 (0.5 × 1H, d, J = 1)
1.2 Hz), 5.78 (0.5 × 1H, d, J = 1)
1.2 Hz), 6.97 (0.5 × 2H, d, J = 8.
9 Hz), 7.10 (0.5 × 2H, d, J = 8.9H)
z), 7.16-7.37 (3H, m), 7.40
(0.5 × 2H, d, J = 8.3 Hz), 7.53
(0.5 × 2H, d, J = 8.3 Hz), 7.87−
8.03 (4H, m), 8.13 (1H, d, J = 9.
0 Hz), 11.82 (1H, brs).

(46) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 0.93 (0.5 × 3H, t, J = 7.4H
z), 1.03 (0.5 × 3H, t, J = 7.4H)
z), 2.10-2.55 (2H, m), 3.96
(0.5 × 3H, s), 4.40 (0.5 × 3H, s)
s), 4.86 (0.5 × 1H, d, J = 11.4H)
z), 4.95 (0.5 × 1H, d, J = 11.4H)
z), 6.10 (0.5 × 1H, d, J = 11.4H)
z), 6.14 (0.5 × 1H, d, J = 11.4H)
z), 6.79 (0.5 × 2H, d, J = 8.7H)
z), 6.94 (0.5 × 2H, d, J = 8.7H)
z), 7.22-8.28 (11H, m), 10.70
(1H, brs).

(47) ¹ H-NMR (CDCl ₃ ) δpp
m: 2.42, 2.58 (1.5H, 3H, t, J =
5.6 Hz), 3.41 and 3.44 (1.5H, 3 each)
H, s), 3.53-3.84 (2H, m), 3.8
7, 4.21 (1.5H, 3H, s for each), 5.09
(0.5H, d, J = 11.3 Hz), 5.16, 5.
23 (1H, s), 5.24 (0.5H, d, J = 1)
1.7 Hz), 5.78 (0.5 H, d, J = 11.7)
Hz), 5.86 (0.5H, d, J = 11.3H)
z), 6.95 (1H, d, J = 9.0 Hz), 7.0
8 (1H, d, J = 9.0 Hz), 7.20-7.64
(5H, m), 7.79-8.00 (4H, m), 8.
13 (1H, d, J = 9.0 Hz).

(48) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 2.18-2.40 (1H, m), 2.45-
2.70 (1H, m), 3.20-3.50 (3H,
m), 4.77 (1H, q, J = 4.6 Hz), 4.9
7 (1H, t, J = 12.2 Hz), 6.85-7.1
5 (2H, m), 7.20-7.85 (10H, m),
7.90-8.10, 8.20-8.37 (all 4H,
m), 8.66, 8.96 (1H, each s), 12.59
(1H, s).

(49) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.07 (0.5 × 3H, t, J = 7.4 Hz),
1.12 (0.5 × 3H, t, J = 7.4 Hz);
34 (0.5 × 3H, t, J = 7.3 Hz), 1.61
(0.5 × 3H, t, J = 7.3 Hz), 2.12
2.43 (2H, m), 3.40 (0.5 × 3H,
s), 3.47 (0.5 × 3H, s), 4.13-4.
65 (2H, m), 4.93 (0.5 × 1H, d, J =
11.2 Hz), 4.96 (0.5 × 1H, d, J = 1)
1.2 Hz), 5.16 (0.5 × 2H, s), 5.2
4 (0.5 × 2H, s), 5.77 (0.5 × 1H, s)
d, J = 11.2 Hz), 5.82 (0.5 × 1H,
d, J = 11.2 Hz), 6.56 (0.5 × 1H,
d, J = 15.6 Hz), 6.60 (0.5 × 1H,
d, J = 15.6 Hz), 6.97 (0.5 × 2H,
d, J = 9.0 Hz), 7.11 (0.5 × 2H, d,
J = 9.0 Hz), 7.20-8.04 (10H,
m), 8.20 (1H, d, J = 8.9 Hz), 12.
13 (1H, brs).

(50) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.07 (0.5 × 3H, t, J = 7.3 Hz),
1.10 (0.5 × 3H, t, J = 7.3 Hz);
34 (0.5 × 3H, t, J = 7.4 Hz), 1.61
(0.5 × 3H, t, J = 7.4 Hz), 2.23
(0.5 × 2H, q, J = 7.3 Hz) 2.38
(0.5 × 2H, q, J = 7.3 Hz) 4.13−
4.68 (2H, m), 4.94 (0.5 × 1H, d,
J = 11.2 Hz), 4.97 (0.5 × 1H, d, J
= 11.2 Hz), 5.73 (0.5 × 1H, d, J =
11.2 Hz), 5.78 (0.5 × 1H, d, J = 1)
1.2Hz), 6.55 (0.5 × 1H, d, J = 1)
5.6 Hz), 6.61 (0.5 × 1H, d, J = 1)
5.6 Hz), 6.80 (0.5 × 2H, d, J = 8.
7 Hz), 6.93 (0.5 × 2H, d, J = 8.7H)
z), 7.16-8.16 (12H, m), 10.02
(1H, s).

(51) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.26 (0.5 × 3H, t, J = 7.2 Hz),
1.27 (0.5 × 3H, t, J = 7.2 Hz);
36-2.67 (2H, m), 3.57-3.83 (2
H, m), 4.12 (2H, q, J = 7.2 Hz),
5.12 (0.5 × 1H, d, J = 11.4 Hz),
5.20 (0.5 × 1H, d, J = 11.4 Hz),
5.72 (0.5 × 1H, d, J = 11.4 Hz),
5.75 (0.5 × 1H, d, J = 11.4 Hz),
7.23-8.23 (13H, m).

(52) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 1.05-1.30 (6H, m), 2.55-
3.40 (9H, m), 5.11 (1H, t, J = 1
1.4 Hz), 7.05-8.35 (14H, m),
8.68, 9.04 (1H, each s), 9.90-10.
30 (1H, br), 12.40-13.20 (1H,
br).

(53) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 1.28 (3H, t, J = 7.0 Hz), 2.
37 (3H, s), 4.32 (2H, q, J = 7.0H
z), 7.12 (2H, d, J = 8.4 Hz), 7.2
8-7.40 (1H, m), 7.42-7.53 (1
H, m), 7.78 (1H, d, J = 7.6 Hz),
7.95-8.15 (3H, m), 8.42 (1H,
s), 12.99 (1H, s).

(54) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.09 (6H, t, J = 7.1 Hz), 2.67
(4H, q, J = 7.1 Hz), 2.92 (2H, t,
J = 6.1 Hz), 3.82 (3H, s), 4.14
(2H, t, J = 6.1 Hz), 6.99 (2H, d,
J = 8.9 Hz), 7.12 (2H, d, J = 8.4H)
z), 7.26-7.60 (3H, m), 7.71 (1
H, s), 7.80-8.00 (5H, m).

(55) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 0.88-1.12 (3H, m), 1.12
1.37 (6H, m), 2.08-2.54 (2H,
m), 3.00-3.33 (4H, m), 3.37-
3.63 (2H, m), 3.86-4.64 (5H,
m), 4.87 (0.5 × 1H, d, J = 11.4H)
z), 4.96 (0.5 × 1H, d, J = 11.4H)
z), 6.18 (0.5 × 1H, d, J = 11.4H)
z), 6.24 (0.5 × 1H, d, J = 11.4H)
z), 7.04 (0.5 × 2H, d, J = 8.9H)
z), 7.18 (0.5 × 2H, d, J = 8.9H)
z), 7.27-7.56 (2H, m), 7.67-
8.22 (7H, m), 8.28 (1H, d, J = 9.
0 Hz), 10.43 (1H, brs).

(56) ¹ H-NMR (DMSO-d ₆ ) δ
3. ppm: 1.22 (3H, t, J = 7.3 Hz);
13 (2H, q, J = 7.3 Hz), 7.19 (2H,
d, J = 8.4 Hz), 7.34 (1H, t, J = 7.
5 Hz), 7.47 (1H, t, J = 7.5 Hz),
7.69 (2H, d, J = 6.2 Hz), 7.78 (1
H, d, J = 7.5 Hz), 8.02 (1H, d, J =
7.5 Hz), 8.08 (2H, d, J = 8.4H)
z), 8.29 (1H, s), 8.52 (2H, d, J
= 6.2 Hz), 10.88 (1H, s), 12.97
(1H, brs).

(57) ¹ H-NMR (CDCl ₃ ) δpp
m: 0.96-1.21 (9H, m), 1.21-1.
44 (3H, m), 2.17-2.47 (2H, m),
2.58 (0.5 × 4H, q, J = 7.1 Hz), 2.
63 (0.5 × 4H, q, J = 7.1 Hz), 2.82
(0.5 × 2H, t, J = 6.1 Hz), 2.88
(0.5 × 2H, t, J = 6.1 Hz), 4.02
(0.5 × 2H, t, J = 6.1 Hz), 4.10
(0.5 × 2H, t, J = 6.1 Hz) 4.18−
4.63 (2H, m), 4.92 (0.5 × 1H, d,
J = 11.3 Hz), 4.96 (0.5 × 1H, d, J)
= 11.3 Hz), 5.77 (0.5 × 1H, d, J =
11.3 Hz), 5.86 (0.5 × 1H, d, J = 1)
1.3 Hz), 6.56 (0.5 × 1H, d, J = 1)
5.5 Hz), 6.61 (0.5 × 1H, d, J = 1)
6.6 Hz), 6.82 (0.5 × 2H, d, J = 8.
9 Hz), 6.96 (0.5 × 2H, d, J = 8.9H)
z), 7.15-7.51 (5H, m), 7.67-
8.05 (5H, m), 8.21 (1H, d, J = 8.
9 Hz).

(58) ¹ H-NMR (CDCl ₃ ) δpp
m: 1.34 (3H, t, J = 7.3 Hz), 1.82
(2H, quint, J = 6.9 Hz), 2.24 (6
H, s), 2.32 (2H, t, J = 6.9 Hz),
4.08 (2H, q, J = 7.3 Hz), 4.30 (2
H, t, J = 6.9 Hz), 7.05 (2H, d, J =
8.4 Hz), 7.25-7.46 (3H, m), 7.
83-7.93 (1H, m), 7.91 (2H, d, J
= 8.4 Hz), 8.24 (1 H, s).

(59) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 1.10-1.58 (6H, m), 2.80-
3.26 (4H, m), 4.26 (2H, s), 5.1
3 (2H, s), 6.82-8.18 (13H, m),
8.33 (1H, s), 8.80 (1H, s).

(60) ¹ H-NMR (CDCl ₃ ) δpp
m: 0.68 (6H, t, J = 7.1 Hz), 2.28
(4H, q, J = 7.1 Hz), 2.64 (2H, t,
J = 6.2 Hz), 3.68 (2H, t, J = 6.2H)
z), 7.06 (2H, d, J = 8.3 Hz), 7.2
6-7.64 (5H, m), 7.82-7.96 (1
H, m), 7.96 (2H, d, J = 8.3 Hz),
8.33 (1H, s), 8.46-8.62 (2H,
m), 9.09 (1H, s).

(61) (Data of free form) ¹ H-NM
R (CDCl ₃ ) δ ppm: 0.97 (6H, t, J =
7.1 Hz), 2.76 (4H, q, J = 7.1H)
z), 3.55 (2H, s), 4.87 (2H, s),
6.83 (1H, d, J = 8.5 Hz), 7.24-
7.59 (11H, m), 7.71-7.87 (4H,
m), 7.97 (2H, d, J = 8.0 Hz);
12 (1H, br).

(62) ¹ H-NMR (CDCl ₃ ) δpp
m: 2.32 (3H, s), 2.84 (3H, s),
3.81 (3H, s), 6.71 (1H, dd, J = 2)
Hz, J = 8.5 Hz), 6.80 (1H, d, J = 2)
Hz), 7.02 (1H, d, J = 8.5z), 7.2
5-7.7 (6H, m), 7.75-7.9 (4H,
m), 8.0-8.3 (2H, m), 10.15 (1
H, br).

(63) ¹ H-NMR (CDCl ₃ ) δpp
m: 0.79 (6H, t, J = 7.2 Hz), 1.12
-1.35 (4H, m), 1.42-1.64 (4H,
m), 2.66-2.83 (4H, m), 3.58 (2
H, s), 4.90 (2H, s), 6.66-6.75
(1H, m), 6.81-7.00 (2H, m), 7.
22-7.35 (1H, m), 7.35-7.68 (5
H, m), 7.71-7.86 (4H, m), 8.19
(1H, s), 8.23 (1H, s), 8.33-9.
53 (1H, m).

(64) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 1.19-1.31 (12H, m), 2.9-
3.3 (4H, m), 4.17-4.34 (6H,
m), 5.06 (2H, s), 7.16-7.24 (2
H, m), 7.57 (1H, d, J = 8.6 Hz),
7.63 (1H, s), 7.71 (1H, s), 7.8
5-8.02 (2H, m), 8.36 (1H, d, J =
4.6 Hz), 9.8-10.0 (1H, m), 11.
22 (1H, s).

(65) ¹ H-NMR (CDCl ₃ ) δpp
m: 2.42 (3H, s), 3.08-3.27 (4
H, m), 3.59 (2H, s), 4.88 (2H,
s), 6.67-6.74 (1H, m), 6.74-
7.16 (4H, m), 7.28-7.69 (6H,
m), 7.69-7.94 (4H, m), 8.18 (1
H, s), 8.21 (1H, s), 8.39-8.48
(1H, m).

(66) ¹ H-NMR (CDCl ₃ ) δpp
m: 0.94 (6H, t, J = 7.1 Hz), 1.40
-1.97 (6H, m), 2.43 (4H, q, J =
7.1Hz), 2.40-2.60 (2H, m), 3.
43 (2H, s), 3.95 (2H, t, J = 1.9H)
z), 6.61-6.72 (2H, m), 7.05-
7.12 (1H, m), 7.25-7.67 (6H,
m), 7.71-7.89 (4H, m), 8.17 (1
H, s), 8.21 (1H, s).

(67) ¹ H-NMR (CDCl ₃ ) δpp
m: 0.95-1.18 (12H, m), 1.32 (3
H, t, J = 7.3 Hz), 1.40-1.61 (2
H, m), 1.68-1.90 (4H, m), 2.41
-2.60 (6H, m), 2.63 (4H, q, J =
7.2 Hz), 2.90 (2H, t, J = 6.2H)
z), 3.49 (2H, s), 3.89 (2H, t, J
= 6.0 Hz), 4.01-4.21 (4H, m),
6.62-6.90 (2H, m), 6.95 (2H,
d, J = 8.9 Hz), 7.08-7.15 (1H,
m), 7.17-7.49 (2H, m), 7.67-
7.77 (2H, m), 7.77-7.94 (3H,
m).

(68) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 1.15-1.40 (18H, m), 3.00
-3.65, 4.05-5.00 (all 18H, m),
7.05-7.30, 7.35-7.65, 7.65-
8.15 (all 13H, m), 10.50-10.90
(2H, br).

(691) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 2.22 (3H, s), 2.42 (3H, s)
s), 2.12-2.46 (2H, m), 2.84 (3
H, s), 3.25-4.60 (12H, m), 5.0
4 (2H, s), 6.65 (1H, dd, J = 8.7H)
z, J = 2.0 Hz), 6.81 (1H, d, J = 2.
0 Hz), 7.16 (1H, d, J = 8.7 Hz),
7.32 (1H, t, J = 7.4 Hz), 7.45 (1
H, t, J = 7.4 Hz), 7.75 (1H, s),
7.77 (1H, d, J = 7.4 Hz), 7.99 (1
H, d, J = 7.4 Hz), 12.10 (1H, br)
s).

(70) (Data of free form) ¹ H-NM
R (CDCl ₃ ) δ ppm: 0.48-2.11 (5
H, m), 2.22 (1H, q, J = 8.5 Hz),
2.30 (3H, s), 2.38-2.54 (4H,
m), 2.58-3.08 (8H, m), 3.08-
3.33 (2H, m), 3.52 (1H, dd, J =
5.4 Hz, J = 14.6 Hz), 4.73 (2H,
s), 6.60-6.78 (3H, m), 6.80 (1
H, d, J = 9.2 Hz), 7.13-7.47 (7
H, m), 7.74 (1H, d, J = 8.7 Hz),
7.83 (1H, d, J = 6.8 Hz).

(71) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 7.36-7.49 (4H, m), 7.59-
7.64 (1H, m), 7.77-7.89 (5H,
m), 8.14 (1H, s), 9.22 (1H, s).

(72) ¹ H-NMR (CDCl ₃ ) δpp
m: 3.82 (2H, s), 6.93 (2H, d, J =
8 Hz), 7.23 (2H, d, J = 8 Hz), 7.3
−7.9 (10H, m), 8.19 (3H, d, J = 8
Hz) 10.03 (1H, s).

(73) ¹ H-NMR (DMSO-d ₆ ) δ
ppm: 1.39 (6H, s), 2.27 (3H,
s), 2.40 (3H, s), 2.70-3.03 (2
H, m), 2.75 (3H, brs), 3.03-3.
90 (10H, m), 5.15 (2H, s), 7.02
(1H, d, J = 4.8 Hz), 7.27-7.52
(4H, m), 7.65 (1H, s), 7.72-7.
84 (1H, m), 7.95-8.04 (1H, m).

Pharmacological tests The test compounds used in the following pharmacological tests are as follows.

Test compound 1: 2- (4- [2-benzoyl-2- (1,2,4-triazol-1-yl) -1
-Ethylthioethyl] benzoylamino) benzothiazole Test compound 2: 2- {4- (2,2-diacetylvinyl) -2- [3- (4-methyl-1-piperazinyl) propyl] phenoxymethylcarbonylamino} Benzothiazole trihydrochloride.

(1) Inhibitory activity of protein kinase C (PKC) Method for measuring PKC activity Purification of PKC using a soluble fraction of rat brain was performed using Kikk.
awa et al. [Ushio Kikkawa, Yos]
himi Takai, Ryoji Minakuch
i, Shinichi Inohara, and Ya
sutomiNishizuka: The Journal
al of BiologicalChemistry
vol257, no. 22, pp 13341-133
48 (1982)]. PKC activity is 2
0 mM Tris-HCl buffer (pH 7.5), 200 μg
/ Ml calf thymus-derived H1 histone, 10 μM [γ- ³²
P] adenosine triphosphate (ATP), 5 mM magnesium acetate, 8 μg / ml phosphatidylserine,
2 μg / ml diacylglycerol and 0.3 mM C
It was determined by the transfer of radioactivity from [γ- ³² P] ATP to Hl histones from calf thymus in the presence of a ²⁺ . Test compounds were dissolved in dimethylformamide and added to the assay system to a final concentration of 0.8%. After incubation at 30 ° C. for 30 minutes, the reaction was stopped by adding 25% trichloroacetic acid, and the acid-insoluble protein was captured on a nitrocellulose membrane by suction filtration. The radioactivity of ³² P was measured with a scintillation counter. Table 19 shows the results.
It is shown in FIG.

[3049]

[Table 191]

(2) Rat Kidney Ischemia-Reperfusion Model [0304] The right kidney of an SD male rat was excised, the left renal artery was clamped for a certain period of time, and reperfusion was performed to prepare a renal ischemia-reperfusion model, and the compound of the present invention was used. The effect was examined.

Test compound 1 was administered at 10 mg / kg and 100 mV 24 hours before ischemia, 3 hours before ischemia, and 24 hours after reperfusion.
Oral administration at a dose of g / kg. Forty-eight hours later, venous blood was collected from the tail vein, and the blood creatinine and urea nitrogen contents were determined. As a result, blood creatinine was 6.13 ± 0.86 in the control group, 2.36 ± 0.31 in the 10 mg / kg administration group of test compound 1, and 100 mg of test compound 1
/ Kg administration group: 3.06 ± 0.88, urea nitrogen content: control group 216.3 ± 26.0, 10% of test compound 1
The mg / kg administration group was 109.8 ± 18.7, and the test compound 1 100 mg / kg administration group was 110.8 ± 27. l.

By administering the test compound 1, the amounts of creatinine and urea nitrogen in blood were significantly suppressed.

────────────────────────────────────────────────── ─── Continued on the front page (51) Int.Cl. ⁶ Identification code FI C07D 277/82 C07D 277/82 403/12 403/12 417/12 417/12 417/14 417/14 521/00 521/00 // A61K 31/425 AAB A61K 31/425 AAB AAM AAM ABA ABA ABF ABF ABG ABG ABN ABN ADD ADD ADD ADU ADU (72) Inventor Kenji Nakaya 72, Kawauchicho, Tokushima, Tokushima Prefecture Isao, No. 6, Saida, Narita-cho, Naruto-shi, Tokushima Prefecture (72) Inventor: Yuichi Shinohara 140, Maehama, Kokuwa-jima, Naruto-cho, Naruto-shi, Tokushima (72) Inventor: Kiku Tanada, character of Saida, Naruto-shi, Tokushima 19-3, east departure (72) Inventor Takahito Yamauchi 92-1, Haihama-jihara, Kitajima-cho, Itano-gun, Tokushima Prefecture Three

Claims (1)

[Claims] 1. A compound of the general formula [Wherein R ¹ represents a nitrogen atom, an oxygen atom or a sulfur atom of 1 to
5 to 6-membered unsaturated heterocyclic residue having 4 (a C _{1 to} C ₁₂ alkyl group, an amino lower alkyl group which may have a lower alkyl group as a substituent, and a cycloalkyl group A group selected from the group may be substituted)); a cyano group; a carboxy-substituted lower alkyl group;
A carboxy group; a lower alkoxycarbonyl group; a hydrogen atom; a lower alkanoyl group; a piperidinylcarbonyl group which may have a lower alkyl group as a substituent on the piperidine ring; a benzoyl group; or a group -CONR ⁶ R ⁷ (R ⁶
And R ⁷ are the same or different and represent a hydrogen atom; a lower alkyl group; a cyano-substituted lower alkyl group; or an amino lower alkyl group which may have a lower alkyl group as a substituent. R ⁶ and R ⁷ may be bonded to each other via a nitrogen atom or an oxygen atom together with or without a bonding nitrogen atom to form a 5- to 6-membered saturated heterocyclic ring. A lower alkyl group may be substituted on the heterocyclic ring. ). R ² is a group (M represents an integer of 1 to 3; m R ^{8 s} are the same or different and each is a hydrogen atom; a halogen atom; a cyano group; a carboxy group; a lower alkoxycarbonyl group; a lower alkoxy lower alkoxy group; a lower alkanoyl as a substituent An amino group which may have a group selected from the group consisting of a group, a lower alkyl group and an amino group which may have a lower alkyl group as a substituent; a nitro group; an amino group which may have a lower alkyl group as a substituent A lower alkoxy group; a lower alkoxy group; a lower alkenyloxy group; a hydroxyl group; a lower alkanoyloxy group; a lower alkoxycarbonyl lower alkoxy group; a carboxy lower alkoxy group;
Lower alkoxy lower alkoxycarbonyl group; lower alkyl group; aminocarbonyl group which may have a lower alkyl group as a substituent; amino lower alkyl group which may have a lower alkyl group as a substituent; lower alkoxy lower alkoxy lower alkyl group; Aminocarbonyl lower alkyl group which may have a lower alkyl group as a substituent; hydroxyl-substituted lower alkyl group; hydroxyl-substituted lower alkoxy group; 1,3-dioxolanyl lower alkoxy group which may have a lower alkyl group as a substituent; oxiranyl Lower alkoxy group or group -OA-NR ⁹ R ¹⁰
(A is .R ⁹ and R ¹⁰ represents a lower alkylene group which may have a hydroxyl group are the same or different and represent a hydrogen atom or a lower alkyl group as a substituent. In addition, R ⁹ and R ¹⁰
May be bonded to each other via a nitrogen atom or an oxygen atom together with or without a bonding nitrogen atom to form a 5- to 6-membered saturated heterocyclic ring. 1,2,3,4-tetrahydroquinolylcarbonyl group which may have a group selected from the group consisting of a lower alkyl group and an oxo group as a substituent; a pyridylcarbonyl group; which may have a hydroxyl group as a substituent. A lower alkanoyl group; a cycloalkylcarbonyl group which may have an amino lower alkyl group which may have a lower alkoxycarbonyl group as a substituent; a benzoyloxy lower alkanoyl group; which has a lower alkoxy group as a substituent on a phenyl ring. A phenoxycarbonyl group; a thienylcarbonyl group; a carboxy group; a lower alkoxycarbonyl group; a pyrrolidinylcarbonyl group which may have a group selected from the group consisting of a lower alkoxycarbonyl group and a phenyl lower alkoxycarbonyl group; Which may have lower alkyl group-lower alkoxycarbonyl group; which may have a lower alkyl group as a substituent piperidinylcarbonyl group; or a group -CO- (A _{1) p}
—NR ¹¹ R ¹² (R ¹¹ and R ¹² are the same or different and are each a hydrogen atom; a lower alkyl group; a lower alkoxycarbonyl group;
A phenyl group which may have a substituent selected from the group consisting of a lower alkoxy group, a lower alkoxy lower alkoxy group and a hydroxyl group as a substituent on the phenyl ring; or a pyridyl group. A ₁ represents a lower alkylene group. p represents 0 or 1. ). R ³ is a hydrogen atom; a lower alkyl group; a lower alkylthio group; a phenylthio group; a lower alkylthio group having a group selected from the group consisting of a carboxy group as a substituent and an amino group which may have a lower alkyl group as a substituent; A lower alkylthio group; a cycloalkylthio group; a lower alkanoylthio group; or a cyano group. n shows the integer of 1-3. n n R ^{4 s} are the same or different and each is a hydrogen atom; a lower alkyl group; a lower alkoxy group; a hydroxyl-substituted lower alkyl group; or a group -A ₂ -NR
¹³ R ¹⁴ (A ₂ represents a lower alkylene group or a lower alkylenyloxy group; R ¹³ and R ¹⁴ are the same or different and are a hydrogen atom; a lower alkyl group; an amino group which may have a lower alkyl group as a substituent. And R ¹³ and R ¹⁴ are bonded to each other via a nitrogen atom or an oxygen atom with or without a nitrogen atom to form a 5- to 7-membered saturated heterocyclic ring. The heterocyclic ring includes a lower alkyl group and a group-.
(A ₃ ) _q NR ¹⁵ R ¹⁶ (A ₃ represents a lower alkylene group.
R ¹⁵ and R ¹⁶ are the same or different and each represent a hydrogen atom; a lower alkyl group; or a phenyl group. R ¹⁵ and R ¹⁶ may be bonded to each other via a nitrogen atom or an oxygen atom together with or without a bonding nitrogen atom to form a 5- to 6-membered saturated heterocyclic ring. The heterocyclic ring may be substituted by a lower alkyl group. q represents 0 or 1. Or a group selected from the group consisting of: ). R ⁵ is a lower alkoxy lower alkoxyaminocarbonyl-substituted lower alkenyl group; a hydroxyl group-substituted aminocarbonyl-substituted lower alkenyl group; a pyridyl-substituted aminocarbonyl-substituted lower alkenyl group; a pyrimidyl-substituted aminocarbonyl-substituted lower alkenyl group; a phenylthioureidocarbonyl group; Carbonyl group; lower alkylthioureidocarbonyl group; pyrimidylaminocarbonyl lower alkoxy group; pyridylaminocarbonyl lower alkoxy group; pyrazylaminocarbonyl lower alkoxy group; group (A ₄ is a lower alkylene group which may have a hydroxyl group as a substituent; a lower alkenylene group; or a group -ZA _5-
(Z represents an oxygen atom or a group —NR ²¹ — (R ²¹ represents a hydrogen atom or a lower alkyl group.) A ₅ represents a lower alkylene group.). r represents 0 or 1. R ¹⁷ and R ¹⁸ represent a hydrogen atom, a lower alkyl group or a phenyl group. R ¹⁹ represents a hydrogen atom or a lower alkyl group. Further, R ¹⁷ and R ¹⁸ together form a group May be formed. Here, R ²⁰ represents a hydrogen atom; a lower alkyl group; a halogen atom; a lower alkoxy group or an amino lower alkyl group which may have a lower alkyl group as a substituent. A)-(A ₄ ) _r COOH (A ₄ and r are as defined above); or a group (A ₆ represents a lower alkenylene group; R ²⁴ represents a hydrogen atom or a lower alkoxycarbonyl group). Also, R ¹ and R ² together form a group (R ²² represents a hydrogen atom or a 1,2,4-triazolyl lower alkoxy group; R ²³ represents a hydrogen atom or a lower alkyl group). Side chain In, the carbon-carbon bond containing the dotted line indicates a single bond or a double bond. Or a salt thereof.