Phosphonic acid derivatives
First Claim
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1. A phosphonic acid derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof:
- ##STR645## wherein R1 represents a hydrogen atom;
R2 and R3 may be the same or different from each other and each represents a hydrogen atom, a lower alkyl group which may have a substituent, an alkali metal or a prodrug ester forming group having the formula ##STR646## wherein R27 represents a hydrogen atom or a lower alkyl group; and
R28 represents an alkyl group which has 1 to 12 carbon atoms and may have a substituent, a cycloalkyl group, an aryl group which may have a substituent, an alkoxy group which has 1 to 12 carbon atoms and may have a substituent, a cycloalkyloxy group, an aryloxy group which may have a substituent, an alkylamino group which has 1 to 12 carbon atoms and may have a substituent, a cycloalkylamino group or an aromatic amino group which may have a substituent;
RA represents a group represented by the formula;
##STR647## wherein R5 represents a hydrogen atom, a lower alkyl group, an alkali metal or a prodrug ester forming group; and
R6 represents a lower alkyl group or a group represented by the formula;
--OR7 (wherein R7 represents a hydrogen atom, a lower alkyl group, an alkali metal or said prodrug ester forming group as defined above); and
RB represents a group represented by the formula;
S--T-- wherein S represents a group represented by the formula;
##STR648## wherein ring A represents a phenyl ring; and
X represents a single bond, an alkylene chain which may have a substituent, or an alkylene chain having one double bond within the chain which may have a substituent;
R8, R9, R10, R11 and R12 may be the same or different from one another and each represents(1) a hydrogen atom,(2) an alkyl group which may have a substituent,(3) an alkenyl group which may have a substituent,(4) a lower alkoxy group which may have a substituent,(5) a carbamoyl group which may have a substituent,(6) a carbamoyloxy group which may have a substituent,(7) a hydroxyl group,(8) an acyl group,(9) a halogen atom,(10) a group represented by the following formula;
##STR649## wherein R13 and R14 may be the same or different from each other and each represents a lower alkyl group which may have a substituent;
p is 0 or 1; and
q is an integer of 0 to
4) or (11) a group represented by the formula;
##STR650## wherein R15, R16, R17, R18 and R19 may be the same or different from one another and each represents a hydrogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group which may have a substituent;
ring B represents a phenyl ring; and
Y represents an alkylene chain which may have a substituent, an alkylene chain having at least one double bond in the chain which may have a substituent, an alkylene chain having at least one triple bond within the chain which may have a substituent, a group represented by the formula;
##STR651## a group represented by the formula;
--O--, or a single bond, or alternatively two adjacent groups of R8, R9, R10, R11 and R12 may together form a ring; and
T represents(1) a group represented by the formula;
##STR652## (wherein R23 represents a cycloalkyl group, a cycloalkylalkyl group, a lower alkyl group which have a substituent or a lower alkenyl group which may have a substituent;
W represents a group represented by the formula;
--O--, or a single bond; and
s and t are independent of each other and are each an integer of 0 to
4).
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Abstract
A phosphonic acid derivative which is useful for medically treating hyperlipemia, represented by the following general formula (I) or a pharmacologically acceptable salt thereof: ##STR1## Representative example of the compound according to the present invention is one represented by the following formula: ##STR2##
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Citations
21 Claims
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1. A phosphonic acid derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof:
- ##STR645## wherein R1 represents a hydrogen atom;
R2 and R3 may be the same or different from each other and each represents a hydrogen atom, a lower alkyl group which may have a substituent, an alkali metal or a prodrug ester forming group having the formula ##STR646## wherein R27 represents a hydrogen atom or a lower alkyl group; and
R28 represents an alkyl group which has 1 to 12 carbon atoms and may have a substituent, a cycloalkyl group, an aryl group which may have a substituent, an alkoxy group which has 1 to 12 carbon atoms and may have a substituent, a cycloalkyloxy group, an aryloxy group which may have a substituent, an alkylamino group which has 1 to 12 carbon atoms and may have a substituent, a cycloalkylamino group or an aromatic amino group which may have a substituent;RA represents a group represented by the formula;
##STR647## wherein R5 represents a hydrogen atom, a lower alkyl group, an alkali metal or a prodrug ester forming group; and
R6 represents a lower alkyl group or a group represented by the formula;
--OR7 (wherein R7 represents a hydrogen atom, a lower alkyl group, an alkali metal or said prodrug ester forming group as defined above); and
RB represents a group represented by the formula;
S--T-- wherein S represents a group represented by the formula;
##STR648## wherein ring A represents a phenyl ring; and
X represents a single bond, an alkylene chain which may have a substituent, or an alkylene chain having one double bond within the chain which may have a substituent;
R8, R9, R10, R11 and R12 may be the same or different from one another and each represents(1) a hydrogen atom, (2) an alkyl group which may have a substituent, (3) an alkenyl group which may have a substituent, (4) a lower alkoxy group which may have a substituent, (5) a carbamoyl group which may have a substituent, (6) a carbamoyloxy group which may have a substituent, (7) a hydroxyl group, (8) an acyl group, (9) a halogen atom, (10) a group represented by the following formula;
##STR649## wherein R13 and R14 may be the same or different from each other and each represents a lower alkyl group which may have a substituent;
p is 0 or 1; and
q is an integer of 0 to
4) or (11) a group represented by the formula;
##STR650## wherein R15, R16, R17, R18 and R19 may be the same or different from one another and each represents a hydrogen atom, a hydroxyl group, a lower alkyl group or a lower alkoxy group which may have a substituent;
ring B represents a phenyl ring; and
Y represents an alkylene chain which may have a substituent, an alkylene chain having at least one double bond in the chain which may have a substituent, an alkylene chain having at least one triple bond within the chain which may have a substituent, a group represented by the formula;
##STR651## a group represented by the formula;
--O--, or a single bond, or alternatively two adjacent groups of R8, R9, R10, R11 and R12 may together form a ring; and
T represents(1) a group represented by the formula;
##STR652## (wherein R23 represents a cycloalkyl group, a cycloalkylalkyl group, a lower alkyl group which have a substituent or a lower alkenyl group which may have a substituent;
W represents a group represented by the formula;
--O--, or a single bond; and
s and t are independent of each other and are each an integer of 0 to
4). - View Dependent Claims (2, 3, 4, 5, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21)
- ##STR645## wherein R1 represents a hydrogen atom;
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6. A phosphonic acid derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof:
- ##STR653## wherein R1 represents a hydrogen atom;
R2 and R3 may be the same or different from each other and each represents a hydrogen atom, a lower alkyl group which may have a substituent, an alkali metal or a prodrug ester forming group having the formula ##STR654## wherein R27 represents a hydrogen atom or a lower alkyl group; and
R28 represents an alkyl group which has 1 to 12 carbon atoms and may have a substituent, a cycloalkyl group, an aryl group which may have a substituent, an alkoxy group which has 1 to 12 carbon atoms and may have a substituent, a cycloalkyloxy group, an aryloxy group which may have a substituent, an alkylamino group which has 1 to 12 carbon atoms and may have a substituent, a cycloalkylamino group or an aromatic amino group which may have a substituent;RA represents a group represented by the formula;
##STR655## wherein R5 represents a hydrogen atom, a lower alkyl group, an alkali metal or a prodrug ester forming group; and
R6 represents a lower alkyl group or a group represented by the formula;
--OR7 wherein R7 represents a hydrogen atom, a lower alkyl group, an alkali metal or a prodrug ester forming group as defined above; andRB represents a group represented by the formula;
S--T-- wherein S represents a group represented by the formula;
##STR656## wherein ring A represents a phenyl ring;
X is an alkylene chain having one double bond in the chain;
R8, R9, R10, R11 and R12 each represents a hydrogen atom; and
T represents a group represented by the formula;
##STR657## (wherein R23 represents a hydrogen atom, a cycloalkyl group, a cycloalkylalkyl group, a lower alkyl group which have a substituent or a lower alkenyl group which may have a substituent;
W represents a single bond; and
s and t are independent of each other and are each an integer of 0 and 4.
- ##STR653## wherein R1 represents a hydrogen atom;
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7. A compound having the formula ##STR658##
Specification