Phosphonic acid derivatives and use thereof
AssigneeTakeda Chemical Industries, Ltd.
InventorsMitsuhiro Wakimasu, Masaaki Mori, Akira Kawada
Life of this patent
Estimating the term…
Abstract
A phosphonic acid derivative compound represented by formula [I ] or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 each represent hydrocarbon groups which may be substituted, except cases in which (1) R.sub.2 is unsubstituted methyl, ( 2 ) R.sub.3 is an unsubstituted hydrocarbon group having 1 to 3 carbon atoms, and (3) R.sub.1 is benzyloxycarbonylaminomethyl, R.sub.2 is isobutyl and R.sub.3 is isobutyl or phenylmethyl, which has endothelin-converting enzyme inhibiting activity and is useful as pharmaceutical drugs such as therapeutic agents for hypertension, cardiac or cerebral circulatory diseases and renal diseases.
Claims16
A compound represented by formula [I] or a pharmaceutically acceptable salt thereof:
- ##STR6## wherein R.sub.1 is (i) a C.sub.1-12 alkyl group which may substituted by C.sub.3-8 cycloalkyl, halogen, hydroxy which may be protected, C.sub.1-2 alkoxy, ketone or amino which may be protected , (ii) a 5 to 7 member cycloalkyl group which may be substituted by lower alkyl having 1 to 3 carbon atoms, halogen, hydroxy which may be protected, C.sub.1-2 alkoxy, keto, or amino which may be protected or (iii) an aralkyl group which may be substituted by lower alkyl having 1 to 3 carbon atoms, C.sub.5-6 cycloalkyl, halogen, hydroxy which may be protected, or C.sub.1-2 alkoxy;
- R.sub.2 is (i) a C.sub.1-8 alkyl group (ii) a cyclohexylmethylene group or (iii) a benzyl group;
- and
- R.sub.3 is an indolylmethyl group or a benzyl group.
A compound represented by formula [I] or a pharmaceutically acceptable salt thereof:
- ##STR7## wherein R.sub.1 is isoamyl, cyclohexylmethyl, phenethyl, naphthylmethyl or naphthylethyl, R.sub.2 is isobutyl or benzyl, and R.sub.3 is indol-3-ylmethyl.
A compound represented by formula [I] or a pharmaceutically acceptable salt thereof:
- ##STR8## wherein R.sub.1 is (i) a C.sub.1-12 alkyl group which may substituted by C.sub.3-8 cycloalkyl, halogen, hydroxy which may be protected, C.sub.1-2 alkoxy, or amino which may be protected, (ii) a 5 to 7 member cycloalkyl group which may be substituted by lower alkyl having 1 to 3 carbon atoms, halogen, hydroxy which may be protected, C.sub.1-2 alkoxy, keto, or amino which may be protected, or (iii) a C.sub.7-17 aralkyl group which may be substituted by lower alkyl having 1 to 3 carbon atoms, C.sub.5-6 cycloalkyl, halogen, hydroxy which may be protected, or C.sub.1-2 alkoxy;
- R.sub.2 is (i) a C.sub.1-8 alkyl group, (ii) a 5 to 7 member cycloalkyl group, or (iii) a benzyl group;
- and
- R.sub.3 is a C.sub.1-8 alkyl group which is substituted by 3-indolyl.
A compound represented by formula [I] or a pharmaceutically acceptable salt thereof:
- ##STR9## wherein R.sub.1 is phenethyl, isoamyl, cyclohexylmethyl, naphthylmethyl or naphthylethyl, R2 is propyl, butyl, cyclohexylmethyl or benzyl and R.sub.3 is benzyl or indolylmethyl.
A compound represented by formula [I] or a pharmaceutically acceptable salt thereof:
- ##STR10## wherein R.sub.1 is an alkyl group of 1 to 12 carbon atoms or an alkyl group having 1 to 5 carbon atoms substituted by an aromatic hydrocarbon group having 6 to 12 carbon atoms;
- R.sub.2 is an alkyl group having 1 to 8 carbon atoms;
- an alkyl group having 1 to 8 carbon atoms substituted by a cycloalkyl group having 5 to 7 carbon atoms;
- or an alkyl group having 1 to 5 carbon atoms substituted by an aromatic hydrocarbon group having 6 to 12 carbon atoms;
- and
- R.sub.3 is alkyl having 1 to 8 carbon atoms substituted by indolyl or an aromatic hydrocarbon group having to 6 to 12 carbon atoms.
Dependencies are inferred from the claim text.