Alpha-substituted carboxylic acid derivatives

An α-substituted carboxylic acid derivative having the general formula (III):

• 110
• wherein:
• R1, R2 and R3 are the same or different, and each is a (i) hydrogen atom, (ii) C1-C6 alkyl group, (iii) C6-C10 aryl group (optionally having 1-5,substituents α1 hereafter defined), (iv) C7-C16 aralkyl group (optionally having 1-5 substituents α1 hereafter defined on the aryl moiety thereof), (v) C1-C6 alkylsulfonyl group, (vi) C1-C6 halogenoalkylsulfonyl group, (vii) C6-C10 arylsulfonyl group (optionally having 1-5 substituents α1 hereafter defined) or (viii) C7-C16 aralkylsulfonyl group (optionally having 1-5 substituents α1 hereafter defined on the aryl moiety thereof);
• A is a nitrogen atom or a ═CH-group;
• B is an oxygen atom or a sulfur atom;
• W1 is a C1-C8 alkylene group;
• W2 is a single bond or a C1-C8 alkylene group;
• X is a (i) hydrogen atom, (ii) C1-C6 alkyl group, (iii) C1-C6 halogenoalkyl group, (iv) C1-C6 alkoxy group, (v) halogen atom, (vi) hydroxy group, (vii) cyano group, (viii) nitro group, (ix) C3-C10cycloalkyl group, (x) C6-C10 aryl group (optionally having 1-5 substituents β hereafter defined), (xi) C7-C16 aralkyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof), (xii) C1-C7 aliphatic acyl group, (xiii) C4-C11 cycloalkylcarbonyl group, (xiv) C7-C11 arylcarbonyl group (optionally having 1-5 substituents β hereafter defined), (xv) C8-C17 aralkylcarbonyl group (optionally having 1-5 substituent β hereafter defined on the aryl moiety thereof), (xvi) monocyclic type heteroaromatic ring-carbonyl group (optionally having 1-5 substituents β hereafter defined), (xvii) carbamoyl group, (xviii) C7-C11 arylaminocarbonyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof) or (xix) amino group (optionally having 1 to 2 substituents β defined hereafter);
• Y is an oxygen atom or an S(O)p group (wherein p is an integer from 0 to 2);
• Z3 is a (i) C1-C6 alkyl group, (ii) C6-C10 aryl group (optionally containing 1-5 substituents α1 hereafter defined), (iii) C7-C16 aralkyl group (optionally containing 1-5 substituents α1 hereafter defined on the aryl moiety thereof), (iv) C3-C10 cycloalkyl group or (v) saturated heterocyclic ring group (optionally containing 1-5 substituents α1 hereafter defined);
• said substituent α1 is a (i) C1-C6 alkyl group, (ii) C1-C6 halogenoalkyl group, (iii) C1-C6 alkoxy group, (iv) halogen atom, (v) hydroxy group, (vi) cyano group, (vii) nitro group, (viii) C3-C10 cycloalkyl group, (ix) C6-C10 aryl group (optionally having 1-5 substituents β hereafter defined), (x) C7-C16 aralkyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof), (xi) C1-C7 aliphatic acyl group, (xii) C4-C11 cycloalkylcarbonyl group, (xiii) C7-C11 arylcarbonyl group (optionally having 1-5 substituents β hereafter defined), (xiv) C8-C17 aralkylcarbonyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof), (xv) monocyclic type heteroaromatic ring-carbonyl group (optionally having 1-5 substituents β hereafter defined), (xvi) carbamoyl group, (xvii) C7-C11 arylaminocarbonyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof), (xviii) amino group (optionally having 1 to 2 substituents β defined hereafter) or (xix) carboxyl group;
• said substituent β is a (i) C1-C10 alkyl group, (ii) halogen atom, (iii) C6-C10 aryl group (optionally having 1-5 substituents γ hereafter defined), (iv) C7-C16 aralkyl group (optionally having 1-5 substituents γ hereafter defined on the aryl moiety thereof), (v) C1-C7 aliphatic acyl group, (vi) C7-C11 arylcarbonyl group (optionally having 1-5 substituents γ hereafter defined), (vii) C8-C17 aralkylcarbonyl group (optionally having 1-5 substituents γ hereafter defined on the aryl moiety thereof), (viii) C4-C11 cycloalkylcarbonyl group, (ix) monocyclic type heteroaromatic ring-carbonyl group (optionally having 1-5 substituents γ hereafter defined), (x) carbamoyl group or (xi) C7-C11 arylaminocarbonyl group (optionally having 1-5 substituents γ hereafter defined on the aryl moiety thereof);
• and
• said substituent γ is a C1-C6 alkyl group, a C1-C6 halogenoalkyl group, a halogen atom or a hydroxy group;
• or a pharmacologically acceptable ester thereof, a pharmacologically acceptable amide thereof or a pharmacologically acceptable salt thereof.

An α-substituted carboxylic acid derivative having the general formula (IV):

• 111
• wherein:
• R1, R2 and R3 are the same or different, and each is a (i) hydrogen atom, (ii) C1-C6 alkyl group, (iii) C6-C10 aryl group (optionally having 1-5 substituents α1 hereafter defined), (iv) C7-C16 aralkyl group (optionally having 1-5 substituents α1 hereafter defined on the aryl moiety thereof), (v) C1-C6 alkylsulfonyl group, (vi) C1-C6 halogenoalkylsulfonyl group, (vii) C6-C10 arylsulfonyl group (optionally having 1-5 substituents α1 hereafter defined) or (viii) C7-C16 aralkylsulfonyl group (optionally having 1-5 substituents α1 hereafter defined on the aryl moiety thereof);
• R4 is a (i) C1-C6 alkyl group, (ii) C6-C10aryl group (optionally having 1-5 substituents α1 hereafter defined) or (iii) C7-C16 aralkyl group (optionally having 1-5 substituents α1 hereafter defined on the aryl moiety thereof);
• A is a nitrogen atom or a ═CH-group;
• B is an oxygen atom or a sulfur atom;
• W1 is a C1-C8 alkylene group;
• W2 is a single bond or a C1-Cg alkylene group;
• X is a (i) hydrogen atom, (ii) C1-C6 alkyl group, (iii) C1-C6 halogenoalkyl group, (iv) C1-C6 alkoxy group, (v) halogen atom, (vi) hydroxy group, (vii) cyano group, (viii) nitro group, (ix) C3-C10 cycloalkyl group, (x) C6-C10 aryl group (optionally having 1-5 substituents β hereafter defined), (xi) C7-C16 aralkyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof), (xii) C1-C7 aliphatic acyl group, (xiii) C4-C11 cycloalkylcarbonyl group, (xiv) C7-C11 arylcarbonyl group (optionally having 1-5 substituents β hereafter defined), (xv) C8-C17 aralkylcarbonyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof), (xvi) monocyclic type heteroaromatic ring-carbonyl group (optionally having 1-5 substituents β hereafter defined), (xvii) carbamoyl group, (xviii) C7-C11 arylaminocarbonyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof) or (xix) amino group (optionally having 1 to 2 substituents β defined hereafter);
• Y is an oxygen atom or an S(O)p group (wherein p is an integer from 0 to 2);
• Z4 is a (i) C1-C6 alkoxy group, (ii) C1-C6 alkylthio group, (iii) halogen atom, (iv) C6-C10 aryl group (optionally having 1-5 substituents α1 hereafter defined), (v) C7-C16 aralkyl group (optionally having 1-5 substituents α1 hereafter defined on the aryl moiety thereof), (vi) C6-C10 aryloxy group (optionally having 1-5 substituents α1 hereafter defined), (vii) C7-C16 aralkyloxy group (optionally having 1-5 substituents α1 hereafter defined on the aryl moiety thereof, (viii) C3-C10 Cycloalkyloxy group, (ix) C3-C10 cycloalkylthio group, (x) saturated heterocyclic ring-oxy group (optionally having 1-5 substituents α1 hereafter defined), (xi) monocyclic type heteroaromatic ring-oxy group (optionally having 1-5 substituents α1 hereafter defined), (xii) C6-C10arylthio group (optionally having 1-5 substituents α1 hereafter defined), (xiii) C7-C16 aralkylthio group (optionally having 1-5 substituents α1 hereafter defined on the aryl moiety thereof), (xiv) saturated heterocyclic ring-thio group (optionally having 1-5 substituents α1 hereafter defined), (xv) monocyclic type heteroaromatic ring-thio group (optionally having 1-5 substituents α1 hereafter defined), (xvi) amino group (optionally having 1-2 substituents α1 hereafter defined) or (xvii) hydroxy group;
• said substituent α1 is a (i) C1-C6 alkyl group, (ii) C1-C6 halogenoalkyl group, (iii) C1-C6 alkoxy group, (iv) halogen atom, (v) hydroxy group, (vi) cyano group, (vii) nitro group, (viii) C3-C10cycloalkyl group, (ix) C6-C10 aryl group (optionally having 1-5 substituents β hereafter defined), (x) C7-C16 aralkyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof), (xi) C1-C7 aliphatic acyl group, (xii) C4-C11 cycloalkylcarbonyl group, (xiii) C7-C11 arylcarbonyl group (optionally having 1-5 substituents β hereafter defined), (xiv) C8-C17 aralkylcarbonyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof), (xv) monocyclic type heteroaromatic ring-carbonyl group (optionally having 1-5 substituents β hereafter defined), (xvi) carbamoyl group, (xvii) C7-C11 arylaminocarbonyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof), (xviii) amino group (optionally having 1 to 2 substituents β defined hereafter) or (xix) carboxyl group;
• said substituent β is a (i) C1-C10 alkyl group, (ii) halogen atom, (iii) C6-C10aryl group (optionally having 1-5 substituents γ hereafter defined), (iv) C7-C16 aralkyl group (optionally having 1-5 substituents γ hereafter defined on the aryl moiety thereof), (v) C1-C7 aliphatic acyl group, (vi) C7-C11 arylcarbonyl group (optionally having 1-5 substituents γ hereafter defined), (vii) C8-C17 aralkylcarbonyl group (optionally having 1-5 substituents γ hereafter defined on the aryl moiety thereof), (viii) C4-C11 cycloalkylcarbonyl group, (ix) monocyclic type heteroaromatic ring-carbonyl group (optionally having 1-5 substituents γ hereafter defined), (x) carbamoyl group or (xi) C7-C11 arylaminocarbonyl group (optionally having 1-5 substituents γ hereafter defined on the aryl moiety thereof);
• and
• said substituent γ is a C1-C6 alkyl group, a C1-C6 halogenoalkyl group, a halogen atom or a hydroxy group;
• or a pharmacologically acceptable ester thereof, a pharmacologically acceptable amide thereof or a pharmacologically acceptable salt thereof.

An α-substituted carboxylic acid derivative selected from the group consisting of:

• 3-[4-[6-(4-adamantan-1-ylphenoxy)-1-methyl-1H-benzimidazol-2-ylmethoxy]-phenyl]-2-(4-fluorobenzyloxy)propionic acid,
• 3-[4-[6-(3,5-di-t-butyl-4-hydroxyphenylthio)-1-methyl-1H-benzimidazol-2-ylmethoxy]phenyl]-2-(4-fluorobenzyloxy)propionic acid,
• 4-[6-(3,5-di-t-butyl-4-hydroxyphenylthio)-1-methyl-1H-benzimidazol-2-ylmethoxy]-phenyllactic acid,
• 4-[6-(4-hydroxy-2,3,5-trimethylphenoxy)-1-methyl-1H-benzimidazol-2-ylmethoxy]-phenyllactic acid,
• 4-(1-methyl-6-methoxy-1H-benzimidazol-2-ylmethoxy)phenyllactic acid,
• 2-ethoxy-3-[4-(1-methyl-6-methoxy-1H-benzimidazol-2-ylmethoxy)phenyl]-propionic acid,
• N-(2-benzoylphenyl)-4-(6-methoxy-1-methyl-1H-benzimidazol-2-ylmethoxy)-phenylalanine,
• 4-[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1H-benzimidazol-2-ylmethoxy]-N-(2-benzoylphenyl)phenylalanine,
• 4-[6-[4-(4-trifluoromethylphenylureido)-3,5-dimethylphenoxy]-1-methyl-1H-benzimidazol-2-ylmethoxy]-N-(2-benzoylphenyl)phenylalanine,
• 3-[4-(6-methoxy-1-methyl-1H-benzimidazol-2-ylmethoxy)phenyl]-2-mercaptopropionic acid,
• 3-[4-(6-methoxy-1-methyl-1H-benzimidazol-2-ylmethoxy)phenyl]-2-methylthiopropionic acid,
• 3-[4-(6-methoxy-1-methyl-1H-benzimidazol-2-ylmethoxy)phenyl]-2-methylsulfenylpropionic acid,
• 3-[4-(6-methoxy-1-methyl-1H-benzimidazol-2-ylmethoxy)phenyl]-2-methylsulfonylpropionic acid,
• 3-[4-(6-hydroxy-1-methyl-1H-benzimidazol-2-ylmethoxy)phenyl]-2-methylthiopropionic acid,
• 3-[4-[6-(β-D-glucopyranosyloxyuronic acid)-1-methyl-1H-benzimidazol-2-ylmethoxy]phenyl]-2-methylthiopropionic acid,
• 3-[4-(1-methyl-6-methylthio-1H-benzimidazol-2-ylmethoxy)phenyl]-2-methylthiopropionic acid, and
• 3-[4-(1-methyl-6-methylthio-1H-benzimidazol-2-ylmethoxy)phenyl]-2-mercaptopropionic acid,
• or a pharmacologically acceptable ester thereof, a pharmacologically acceptable amide thereof or a pharmacologically acceptable salt thereof.

A method of treatment or prophylaxis of a disease selected from the group consisting of diabetes mellitus, impaired glucose tolerance, gestational diabetes mellitus, neurosis, cataract and coronary artery diseases comprising administering to an animal in need thereof, an effective amount of an active agent, wherein said active agent is an α-substituted carboxylic acid derivative of the general formula (I):

• 112
• wherein:
• R1, R2 and R3 are the same or different, and each is a (i) hydrogen atom, (ii) C1-C6 alkyl group, (iii) C6-C10aryl group (optionally having 1-5 substituents α1 hereafter defined), (iv) C7-C16 aralkyl group (optionally having 1-5 substituents α1 hereafter defined on the aryl moiety thereof), (v) C1-C6 alkylsulfonyl group, (vi) C1-C6 halogenoalkylsulfonyl group, (vii) C6-C10 arylsulfonyl group (optionally having 1-5 substituents α1 hereafter defined) or (viii) C7-C16 aralkylsulfonyl group (optionally having 1-5 substituents α1 hereafter defined on the aryl moiety thereof);
• A is a nitrogen atom or a ═CH-group;
• B is an oxygen atom or a sulfur atom;
• W1 is a C1-C8 alkylene group;
• W2 is a single bond or a C1-C8 alkylene group;
• X is a (i) hydrogen atom, (ii) C1-C6 alkyl group, (iii) C1-C6 halogenoalkyl group, (iv) C1-C6 alkoxy group, (v) halogen atom, (vi) hydroxy group, (vii) cyano group, (viii) nitro group, (ix) C3-C10 cycloalkyl group, (x) C6-C10 aryl group (optionally having 1-5 substituents β hereafter defined), (xi) C7-C16 aralkyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof), (xii) C1-C7 aliphatic acyl group, (xiii) C4-C11 cycloalkylcarbonyl group, (xiv) C7-C11 arylcarbonyl group (optionally having 1-5 substituents β hereafter defined), (xv) C8-C17 aralkylcarbonyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof), (xvi) monocyclic type heteroaromatic ring-carbonyl group (optionally having 1-5 substituents β hereafter defined), (xvii) carbamoyl group, (xviii) C7-C11 arylaminocarbonyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof) or (xix) amino group (optionally having 1 to 2 substituents β defined hereafter);
• Y is an oxygen atom or an S(O)p group (wherein p is an integer from 0 to 2);
• Z1 is a (i) hydrogen atom, (ii) C1-C6 alkyl group, (iii) C1-C6 alkoxy group, (iv) C1-C6 alkylthio group, (v) halogen atom, (vi) C6-C10 aryl group (optionally having 1-5 substituents α1 hereafter defined), (vii) C7-C16 aralkyl group (optionally having 1-5 substituents α1 hereafter defined on the aryl moiety thereof), (viii) C6-C10 aryloxy group (optionally having 1-5 substituents α1 hereafter defined), (ix) C7-C16 aralkyloxy group (optionally having 1-5 substituents α1 hereafter defined on the aryl moiety thereof), (x) C3-C10 cycloalkyloxy group, (xi) C3-C10 cycloalkylthio group, (xii) saturated heterocyclic ring-oxy group (optionally having 1-5 substituents α1 hereafter defined), (xiii) monocyclic type heteroaromatic ring-oxy group (optionally having 1-5 substituents α1 hereafter defined), (xiv) C6-C10 arylthio group (optionally having 1-5 substituents α1 hereafter defined), (xv) C7-C16 aralkylthio group (optionally having 1-5 substituents α1 hereafter defined on the aryl moiety thereof), (xvi) saturated heterocyclic ring-thio group (optionally having 1-5 substituents α1 hereafter defined), (xvii) monocyclic type heteroaromatic ring-thio group (optionally having 1-5 substituents α1 hereafter defined), (xviii) amino group (optionally having 1-2 substituents α1 hereafter defined) or (xix) hydroxy group;
• said substituent α1 is a (i) C1-C6 alkyl group, (ii) C1-C6 halogenoalkyl group, (iii) C1-C6 alkoxy group, (iv) halogen atom, (v) hydroxy group, (vi) cyano group, (vii) nitro group, (viii) C3-C10 cycloalkyl group, (ix) C6-C10 aryl group (optionally having 1-5 substituents β hereafter defined), (x) C7-C16 aralkyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof), (xi) C1-C7 aliphatic acyl group, (xii) C4-C11 cycloalkylcarbonyl group, (xiii) C7-C11 arylcarbonyl group (optionally having 1-5 substituents β hereafter defined), (xiv) C8-C17 aralkylcarbonyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof), (xv) monocyclic type heteroaromatic ring-carbonyl group (optionally having 1-5 substituents β hereafter defined), (xvi) carbamoyl group, (xvii) C7-C11 arylaminocarbonyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof), (xviii) amino group (optionally having 1 to 2 substituents β defined hereafter) or (xix) carboxyl group;
• said substituent β is a (i) C1-C10 alkyl group, (ii) halogen atom, (iii) C6-C10 aryl group (optionally having 1-5 substituents γ hereafter defined), (iv) C7-C16 aralkyl group (optionally having 1-5 substituents γ hereafter defined on the aryl moiety thereof), (v) C1-C7 aliphatic acyl group, (vi) C7-C11 arylcarbonyl group (optionally having 1-5 substituents γ hereafter defined), (vii) C8-C17 aralkylcarbonyl group (optionally having 1-5 substituents γ hereafter defined on the aryl moiety thereof), (viii) C4-C11 cycloalkylcarbonyl group, (ix) monocyclic type heteroaromatic ring-carbonyl group (optionally having 1-5 substituents γ hereafter defined), (x) carbamoyl group or (xi) C7-C11 arylaminocarbonyl group (optionally having 1-5 substituents γ hereafter defined on the aryl moiety thereof);
• and
• said substituent γ is a C1-C6 alkyl group, a C1-C6 halogenoalkyl group, a halogen atom or a hydroxy group;
• or a pharmacologically acceptable ester thereof, a pharmacologically acceptable amide thereof or a pharmacologically acceptable salt thereof.

A method of treating an animal in need of treatment with an active agent selected from the group consisting of insulin resistance improving agents, hypoglycemic agents, immunoregulatory agents, aldose reductase inhibitors, 5-lipoxygenase inhibitors, peroxidized lipid production suppressors, PPAR activators, leukotriene antagonists, adipose cell formation promoters and calcium antagonists comprising administering an effective amount of said active agent to said animal, wherein said active agent is an α-substituted carboxylic acid derivative of the general formula (I):

• 113
• wherein:
• R1, R2 and R3 are the same or different, and each is a (i) hydrogen atom, (ii) C1-C6 alkyl group, (iii) C6-C10aryl group (optionally having 1-5 substituents α1 hereafter defined), (iv) C7-C16 aralkyl group (optionally having 1-5 substituents α1 hereafter defined on the aryl moiety thereof), (v) C1-C6 alkylsulfonyl group, (vi) C1-C6 halogenoalkylsulfonyl group, (vii) C6-C10 arylsulfonyl group (optionally having 1-5 substituents α1 hereafter defined) or (viii) C7-C16 aralkylsulfonyl group (optionally having 1-5 substituents α1 hereafter defined on the aryl moiety thereof);
• A is a nitrogen atom or a ═CH-group;
• B is an oxygen atom or a sulfur atom;
• W1 is a C1-Cg alkylene group;
• W2 is a single bond or a C1-C8 alkylene group;
• X is a (i) hydrogen atom, (ii) C1-C6 alkyl group, (iii) C1-C6 halogenoalkyl group, (iv) C1-C6 alkoxy group, (v) halogen atom, (vi) hydroxy group, (vii) cyano group, (viii) nitro group, (ix) C3-C10 cycloalkyl group, (x) C6-C10 aryl group (optionally having 1-5 substituents β hereafter defined), (xi) C7-C16 aralkyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof), (xii) C1-C7 aliphatic acyl group, (xiii) C4-C11 cycloalkylcarbonyl group, (xiv) C7-C11 arylcarbonyl group (optionally having 1-5 substituents β hereafter defined), (xv) C8-C17 aralkylcarbonyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof), (xvi) monocyclic type heteroaromatic ring-carbonyl group (optionally having 1-5 substituents β hereafter defined), (xvii) carbamoyl group, (xviii) C7-C11 arylaminocarbonyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof) or (xix) amino group (optionally having 1 to 2 substituents β defined hereafter);
• Y is an oxygen atom or an S(O)p group (wherein p is an integer from 0 to 2);
• Z1 is a (i) hydrogen atom, (ii) C1-C6 alkyl group, (iii) C1-C6 alkoxy group, (iv) C1-C6 alkylthio group, (v) halogen atom, (vi) C6-C10 aryl group (optionally having 1-5 substituents α1 hereafter defined), (vii) C7-C16 aralkyl group (optionally having 1-5 substituents α1 hereafter defined on the aryl moiety thereof), (viii) C6-C10 aryloxy group (optionally having 1-5 substituents α1 hereafter defined), (ix) C7-C16 aralkyloxy group (optionally having 1-5 substituents α1 hereafter defined on the aryl moiety thereof), (x) C3-C10cycloalkyloxy group, (xi) C3-C10 cycloalkylthio group, (xii) saturated heterocyclic ring-oxy group (optionally having 1-5 substituents α1 hereafter defined), (xiii) monocyclic type heteroaromatic ring-oxy group (optionally having 1-5 substituents α1 hereafter defined), (xiv) C6-C10 arylthio group (optionally having 1-5 substituents α1 hereafter defined), (xv) C7-C16 aralkylthio group (optionally having 1-5 substituents α1 hereafter defined on the aryl moiety thereof), (xvi) saturated heterocyclic ring-thio group (optionally having 1-5 substituents α1 hereafter defined), (xvii) monocyclic type heteroaromatic ring-thio group (optionally having 1-5 substituents α1 hereafter defined), (xviii) amino group (optionally having 1-2 substituents α1 hereafter defined) or (xix) hydroxy group;
• said substituent α1 is a (i) C1-C6 alkyl group, (ii) C1-C6 halogenoalkyl group, (iii) C1-C6 alkoxy group, (iv) halogen atom, (v) hydroxy group, (vi) cyano group, (vii) nitro group, (viii) C3-C10 cycloalkyl group, (ix) C6-C10 aryl group (optionally having 1-5 substituents β hereafter defined), (x) C7-C16 aralkyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof), (xi) C1-C7 aliphatic acyl group, (xii) C4-C11 cycloalkylcarbonyl group, (xiii) C7-C11 arylcarbonyl group (optionally having 1-5 substituents β hereafter defined), (xiv) C9-C17 aralkylcarbonyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof), (xv) monocyclic type heteroaromatic ring-carbonyl group (optionally having 1-5 substituents β hereafter defined), (xvi) carbamoyl group, (xvii) C7-C11 arylaminocarbonyl group (optionally having 1-5 substituents β hereafter defined on the aryl moiety thereof), (xviii) amino group (optionally having 1 to 2 substituents β defined hereafter) or (xix) carboxyl group;
• said substituent β is a (i) C1-C10 alkyl group, (ii) halogen atom, (iii) C6-C10 aryl group (optionally having 1-5 substituents γ hereafter defined), (iv) C7-C16 aralkyl group (optionally having 1-5 substituents γ hereafter defined on the aryl moiety thereof), (v) C1-C7 aliphatic acyl group, (vi) C7-C11 arylcarbonyl group (optionally having 1-5 substituents γ hereafter defined), (vii) C8-C17 aralkylcarbonyl group (optionally having 1-5 substituents γ hereafter defined on the aryl moiety thereof), (viii) C4-C11 cycloalkylcarbonyl group, (ix) monocyclic type heteroaromatic ring-carbonyl group (optionally having 1-5 substituents γ hereafter defined), (x) carbamoyl group or (xi) C7-C11 arylaminocarbonyl group (optionally having 1-5 substituents γ hereafter defined on the aryl moiety thereof);
• and
• said substituent γ is a C1-C6 alkyl group, a C1-C6 halogenoalkyl group, a halogen atom or a hydroxy group;
• or a pharmacologically acceptable ester thereof, a pharmacologically acceptable amide thereof or a pharmacologically acceptable salt thereof.