NOVEL PYRAZOLE DERIVATIVE

摘要

It has been desired to develop a pharmaceutical composition, which is used in agents for preventing and/or treating various diseases related to PDE10 (e.g. mental disorder and neurodegenerative disorder). The present invention provides: compounds having PDE10 inhibitory effect, in particular, compounds having a 4-heteroarylpyrazole-5-carboxylic acid amide structure represented by the following formula (I), or their pharmaceutically acceptable salts, or their solvates; pharmaceutical compositions comprising, as active ingredients, the compounds, or their pharmaceutically acceptable salts, or their solvates; and medical use of the compounds, or their pharmaceutically acceptable salts, or their solvates.;

主权项

1. A pharmaceutical composition comprising, as an active ingredient, at least one of a compound according to the following formula (I-d), or a pharmaceutically acceptable salt thereof, or a solvate thereof; and a pharmaceutically acceptable carrier:wherein
p represents an integer of 0 to 4; q represents an integer of 0 to 3; Z represents N or CR5; R1 each independently represents a halogen atom, a hydroxyl group, a nitro group, a cyano group, a C1-6 alkyl group, a C3-8 cycloalkyl group, a halogenated C1-6 alkyl group, a C2-6 alkenyl group, a C1-6 alkoxyl group, a halogenated C1-6 alkoxyl group, a C1-6 alkoxylcarbonyl group, a hydroxy C1-6 alkyl group, a C1-6 alkoxyl C1-6 alkyl group, a C2-7 alkanoyl group, a C1-6 alkylthio group, a C1-6 alkylsulfinyl group, a C1-6 alkylsulfonyl group, an —NR7R8 group, or a —CONR7R8 group, wherein R7 and R8 in the —NR7R8 group and the —CONR7R8 group each independently represent a substituent selected from among a hydrogen atom, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a hydroxy C1-6 alkyl group, a cyanated C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, a C3-8 cycloalkyl group, a C6-14 aryl group, a C7-20 aralkyl group, a heterocyclic group, a C2-7 alkanoyl group, a hydroxy C2-7 alkanoyl group, a halogenated C2-7 alkanoyl group, a C3-8 cycloalkylcarbonyl group, a C6-14 arylcarbonyl group, a C7-20 aralkylcarbonyl group, a heterocyclic carbonyl group, a mono-/di-C1-6 alkylcarbamoyl group, a mono-/di-halogenated C1-6 alkylcarbamoyl group, a mono-/di-C3-8 cycloalkylcarbamoyl group, a mono-/di-C6-14 arylcarbamoyl group, a mono-/di-C7-20 aralkylcarbamoyl group, a mono-/di-heterocyclic carbamoyl group, a C1-6 alkylsulfonyl group, a halogenated C1-6 alkylsulfonyl group, a C3-8 cycloalkylsulfonyl group, a C6-14 arylsulfonyl group, a C7-20 aralkylsulfonyl group, a heterocyclic sulfonyl group, a mono-/di-C1-6 alkylsulfamoyl group, a mono-/di-halogenated C1-6 alkylsulfamoyl group, a mono-/di-C3-8 cycloalkylsulfamoyl group, a mono-/di-C6-14 arylsulfamoyl group, a mono-/di-C7-20 aralkylsulfamoyl group, and a mono-/di-heterocyclic sulfamoyl group; R2 represents a hydrogen atom, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a hydroxy C1-6 alkyl group, or a C1-6 alkoxyl C1-6 alkyl group; R3 each independently represents a halogen atom, a cyano group, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a hydroxy C1-6 alkyl group, a C1-6 alkoxyl group, a halogenated C1-6 alkoxyl group, or a C1-6 alkoxyl C1-6 alkyl group; R4 represents a halogen atom, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a C3-8 cycloalkyl group, a hydroxy C1-6 alkyl group, a C1-6 alkoxyl group, a halogenated C1-6 alkoxyl group, a C1-6 alkoxyl C1-6 alkyl group, a C1-6 alkylthio group, a C1-6 alkylsulfonyl group, a —CONR7R8 group, an —NR7R8 group, a C6-14 aryl group, a 3- to 14-membered non-aromatic heterocyclic group, or a 5- to 7-membered monocyclic heteroaryl group, wherein R2 and R8 in the —NR7R8 group and the —CONR7R8 group have the same definitions as those of R2 and R8 in the above R1, and wherein the C3-8 cycloalkyl group, the C6-14 aryl group, the 3- to 14-membered non-aromatic heterocyclic group, and the 5- to 7-membered monocyclic heteroaryl group, which are represented by R4, are each optionally substituted with one to three groups selected from among a hydroxyl group, a nitro group, a cyano group, a halogen atom, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a hydroxy C1-6 alkyl group, a C1-6 alkoxyl group, a halogenated C1-6 alkoxyl group, a C1-6 alkoxyl C1-6 alkyl group, a C1-6 alkylthio group, a C1-6 alkylsulfonyl group, a —CONR7R8 group, an —NR7R8 group, a C6-14 aryl group, a 3- to 14-membered non-aromatic heterocyclic group, and a 5- to 7-membered monocyclic heteroaryl group, wherein R7 and R8 in the —NR7R8 group and the —CONR7R8 group have the same definitions as those of R7 and R8 in the above R1; R5 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a C1-6 alkoxyl group, a halogenated C1-6 alkoxyl group, or a C1-6 alkoxyl C1-6 alkyl group; and ring A″ represented by the following partial structural formula (II″):is selected from the heteroaryl group consisting of the following: