Phosphonic acid derivative having inhibitory activity against carboxypeptidase B

A compound represented by the following general formula (I) or a pharmacologically acceptable salt thereof, or a hydrate thereof or a solvate thereof:

• 17
• wherein R1 represents hydrogen atom, an alkyl group, a substituted alkyl group, an alkoxyl group, a substituted alkoxyl group, amino group, a substituted amino group, a carbocyclic group, a substituted carbocyclic group, a heterocyclic group, or a substituted heterocyclic group;
• R2 and R3 may be the same or different and independently represent hydrogen atom, an alkyl group, a substituted alkyl group, an alkoxyl group, a substituted alkoxyl group, amino group, a substituted amino group, a carbocyclic group, a substituted carbocyclic group, a heterocyclic group, or a substituted heterocyclic group, or R2 and R3 may form a 5 to 7 membered carbon ring together with the carbon atom to which they bind;
• X represents —CH2—, —O—, or —NH—;
• A represents a group of the following formula (II).
• 18
• [in which R7 and R8 may be the same or different and independently represent hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group, an aryloxycarbonyl group, carbamoyl group, a substituted carbamoyl group, or amidino group;
• R9 and R10 may be the same or different and independently represent hydrogen atom, a halogen atom, hydroxyl group, phenyl group, an alkyl group, an alkoxyl group, an aryloxy group, an acyl group, carboxyl group, an alkoxycarbonyl group, carbamoyl group, a substituted carbamoyl group, amino group, a substituted amino group, nitro group, —SR11 group (R11 represents an alkyl group, phenyl group, or a substituted phenyl group), —SOR12 group (R12 represents an alkyl group, phenyl group, a substituted phenyl group;
• an alkoxyl group, an aryloxy group, amino group, or a substituted amino group), or —SO2R13 group (R13 represents an alkyl group, phenyl group, a substituted phenyl group, an alkoxyl group, an aryloxy group, amino group, or a substituted amino group);
• m represents an integer of from 1 to 8;
• and
• —(C)m— represents a saturated or unsaturated carbon chain], or
• A represents a group of the following formula (III):
• 19
• [in which R7 and R8 may be the same or different and independently represent hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group, an aryloxycarbonyl group, carbamoyl group, a substituted carbamoyl group, or amidino group;
• R24, R25, R26 and R27 may be the same or different and independently represent hydrogen atom, a halogen atom, hydroxyl group, an alkyl group, amino group, or a substituted amino group;
• p and q independently represent an integer of from 0 to 2;
• —(C)p— and —(C)q— independently represent single bond, or a saturated or unsaturated carbon chain;
• and
• B represents a carbocyclic group, a substituted carbocyclic group, a heterocyclic group, or a substituted heterocyclic group], or
• A represents a group of the following formula (TV):
• 20
• [in which R20 represents hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group, carbamoyl group, an alkylcarbamoyl group, or amidino group;
• R28 and R29 may be the same or different and independently represent hydrogen atom, a halogen atom, hydroxyl group, an alkyl group, amino group, or an alkylamino group;
• n and o independently represent an integer of from 0 to 5;
• r represents an integer of from 0 to 4;
• —(C)r— independently represents single bond, or a saturated or unsaturated carbon chain;
• and
• Y represents CH or nitrogen atom], or
• A represents a group of the following formula (XIV):
• 21
• [in which R7 and R8 may be the same or different and independently represent hydrogen atom, an alkyl group, an acyl group, an alkoxycarbonyl group, an aryloxycarbonyl group, carbamoyl group, a substituted carbamoyl group, or amidino group;
• R30, R31, R32 and R33 may be the same or different and independently represent hydrogen atom, a halogen atom, hydroxyl group, an alkyl group, oxo group, amino group, or an alkylamino group;
• s represents an integer of from 0 to 3;
• t represents an integer of from 1 to 3;
• —(C)s— and —(C)t— independently represent single bond, or a saturated or unsaturated carbon chain;
• and
• V represents —O— or —NH—];
• and,
• E represents hydrogen atom, or —CH2CH2— to form together with A a piperidine ring group or a N-substituted piperidine ring group.