| 摘要 |
The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic β-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes.;A spiroindoline compound represented by the general formula (1), or a salt thereof, or a solvate of the compound or the salt:;;[wherein ring A represents a nitrogen-containing 5-10 membered heteroaryl group;
R1 and R2, which are the same or different, each represent a hydrogen atom, a halogen atom, a halo C1-6 alkyl group, a C6-10 aryl group, a cyano group, a C1-6 alkyl group optionally having a substituent, a C2-6 alkenyl group optionally having a substituent, etc.; R3 represents a hydrogen atom, a C1-6 alkyl group optionally having a substituent, etc.; and R4 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally having a substituent, etc.] |
| 主权项 |
1. A spiroindoline compound represented by the following general formula (1), a salt or solvate thereof:wherein ring A represents a nitrogen-containing 5-10 membered unsaturated heterocyclic group,
R1 and R2, which are the same or different, each represent a hydrogen atom, a halogen atom, a halo C1-6 alkyl group, a C6-10 aryl group, a cyano group, a C1-6 alkyl group optionally having a substituent, a C2-6 alkenyl group optionally having a substituent, —O—R5, —S(O)l—R6, or —CO—R12, wherein R5 represents a C1-6 alkyl group optionally having a substituent, a halo C1-6 alkyl group, or a C6-10 aryl group optionally having a substituent, R6 represents a C1-6 alkyl group, a C3-8 cycloalkyl group, a mono-C1-6 alkylamino group optionally having a substituent, a di-C1-6 alkylamino group optionally having a substituent, a mono-C3-8 cycloalkylamino group, or a nitrogen-containing 3-7 membered saturated heterocyclic group optionally having a substituent, l represents an integer of 0 to 2, and R12 represents a hydroxyl group, a C1-6 alkyl group, a mono-C1-6 alkylamino group optionally having a substituent, or a di-C1-6 alkylamino group optionally having a substituent, R3 represents a hydrogen atom, a C1-6 alkyl group optionally having a substituent, —CO—R7, —S(O)m—R8, —CS—R13, or a group represented by the following formula (2): wherein R7 represents a hydrogen atom, a C1-6 alkyl group optionally having a substituent, a halo C1-6 alkyl group, a C3-8 cycloalkyl group, a C1-6 alkoxy group, a C6-10 aryl group, an amino group, a mono-C1-6 alkylamino group optionally having a substituent, a di-C1-6 alkylamino group, a carboxyl group, a C1-6 alkoxycarbonyl group, a mono-C1-6 alkylaminocarbonyl group, a di-C1-6 alkylaminocarbonyl group, a carbamoyl group, a C1-6 alkylcarbonyl group, a mono-C3-8 cycloalkylamino group optionally having a substituent, a C1-6 alkoxyamino group, or a hydroxyamino group, R8 represents a C1-6 alkyl group or a mono-C1-6 alkylamino group, m represents an integer of 0 to 2, R13 represents a mono-C1-6 alkylamino group, and R14 represents a C1-6 alkoxy group or a mono-C1-6 alkylamino group, and R4 represents a hydrogen atom, a halogen atom, a cyano group, a C1-6 alkyl group optionally having a substituent, —O—R9, —S(O)n—R10, or —CO—R11, wherein R9 represents a C1-6 alkyl group, a C6-10 aryl group optionally having a substituent, or a nitrogen-containing 5-10 membered unsaturated heterocyclic group optionally having a substituent, R10 represents a C1-6 alkyl group optionally having a substituent, n represents an integer of 0 to 2, and R11 represents a hydroxyl group, a C1-6 alkoxy group, an amino group, a mono-C1-6 alkylamino group, a di-C1-6 alkylamino group, or a nitrogen-containing 3-7 membered saturated heterocyclic group. |
