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AssigneeSuntory Limited
InventorsHarukazu Fukami, Motoo Sumida, Shinjiro Niwata, Saki Kakutani, Saitoh Masayuki, Shibata Hiroshi, Kiso Yoshinobu
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The invention relates to an imidazolidine derivative represented by the following general formula (1): ##STR1## wherein A and B mean individually an aromatic hydrocarbon group which may be substituted by 1-3 substituents selected from halogen atoms, C.sub.1-4 alkyl groups, C.sub.1-4 alkoxy groups, C.sub.1-4 alkylenedioxy groups, a phenoxy group, a nitro group, a cyano group, a phenyl group, C.sub.2-5 alkanoylamino groups, a carboxyl group which may be esterified with a C.sub.1-4 alkyl or alkenyl group, carboxyalkyl groups which may be esterified with a C.sub.1-4 alkyl or alkenyl group, carboxyalkyloxy groups which may be esterified with a C.sub.1-4 alkyl or alkenyl group, N-alkylpiperazinylcarbonyl groups, N-alkylpiperazinylcarbonylalkyl groups, N-alkylpiperazinylcarbonylalkyloxy groups, and a morpholinocarbonyl group; X denotes a sulfonyl or carbonyl group; and Y stands for an oxygen or sulfur atom, a chymase inhibitor comprising the same as an active ingredient, and a medicine comprising the same as an active ingredient, typified by a prophylactic and therapeutic agent for a disease of the heart or circulatory system, which is caused by the abnormal acceleration of production of angiotensin II.
An imidazolidine derivative represented by the following formula (1) ##STR5## wherein A and B are identical with or different from each other and mean individually an unsubstituted aromatic hydrocarbon group, an aromatic hydrocarbon groups substituted by 1-3 substituents selected from the group consisting of halogen atoms, alkyl groups having 1-4 carbon atoms, alkoxy groups having 1-4 carbon atom, alkylenedioxy groups having 1-4 carbon atoms, a phenoxy group, a nitro group, a cyano group, a phenyl group, alkanoylamino groups having 2-5 carbon atoms, a carboxyl group, a carboxyl group esterified with an alkyl or alkenyl group having 1-4 carbon atoms, carboxyalkyl groups, carboxyalkyl groups esterified with an alkyl or alkenyl group having 1-4 carbon atoms, carboxyalkyloxy groups, carboxyalkyloxy groups esterified with an alkyl or alkenyl group having 1-4 carbon atoms, N-alkylpiperazinylcarbonyl groups, N-alkylpiperazinylcarbonylalkyl groups, N-alkylpiperazinylcarbonylalkyloxy groups, and a morpholinicarbonyl group;
A medicinal composition comprising an imidazolidine derivative represented by the following formula (1) ##STR6## wherein A and B are identical with or different from each other and mean individually an unsubstituted aromatic hydrocarbon group, an aromatic hydrocarbon group substituted by 1-3 substituents selected from the group consisting of halogen atoms, alkyl groups having 1-4 carbon atoms, alkoxy groups having 1-4 carbon atoms, alkylenedioxy groups having 1-4 carbon atoms, a phenoxy group, a nitro group, a cyano group, a phenyl group, alkanoylamino groups having 2-5 carbon atoms, a carboxyl group, a carboxyl group esterified with an alkyl or alkenyl group having 1-4 carbon atoms, carboxyalkyl groups, carboxyalkyl groups esterified with an alkyl or alkenyl group having 1-4 carbon atoms, carboxyalkyloxy groups, carboxyalkyloxy groups esterified with an alkyl or alkenyl group having 1-4 carbon atoms, N-alkylpiperazinylcarbonyl groups, N-alkylpiperazinylcarbonylalkyl groups, N-alkylpiperazinylcarbonylalkyloxy groups, and a morpholinicarbonyl group;
A method of preventing and treating a disease of the heart or circulatory system, which is caused by the abnormal acceleration of production of angiotensin II, comprising administering to a patient an effective amount of an imidazolidine derivative represented by the following formula (1) ##STR7## wherein A and B are identical with or different from each other and mean individually an unsubstituted aromatic hydrocarbon group, an aromatic hydrocarbon group substituted by 1-3 substituents selected from the group consisting of halogen atoms, alkyl groups having 1-4 carbon atoms, alkoxy groups having 1-4 carbon atoms, alkylenedioxy groups having 1-4 carbon atoms, a phenoxy group, a nitro group, a cyano group, a phenyl group, alkanoylamino groups having 2-5 carbon atoms, a carboxyl group, a carboxyl group esterified with an alkyl or alkenyl group having 1-4 carbon atoms, carboxyalkyl groups, carboxyalkyl groups esterified with an alkyl or alkenyl group having 1-4 carbon atoms, carboxyalkyloxy groups, carboxyalkyloxy groups esterified with an alkyl or alkenyl group having 1-4 carbon atoms, N-alkylpiperazinylcarbonyl groups, N-alkylpiperazinylcarbonylalkyl groups, N-alkylpiperazinylcarbonylalkyloxy groups, and a morpholinicarbonyl group;
A method of inhibiting chymase, comprising contacting chymase with an inhibitory effective amount of an imidazolidine derivative represented by the following formula (1) ##STR8## wherein A and B are identical with or different form each other and mean individually an unsubstituted aromatic hydrocarbon group, an aromatic hydrocarbon group substituted by 1-3 substituents selected from the group consisting of halogen atoms, alkyl groups having 1-4 carbon atoms, alkoxy groups having 1-4 carbon atoms, alkylenedioxy groups having 1-4 carbon atoms, a phenoxy group, a nitro group, a cyano group, a phenyl group, alkanoylamino groups having 2-5 carbon atoms, a carboxyl group, a carboxyl group esterified with an alkyl or alkenyl group having 1-4 carbon atoms, carboxyalkyl groups, carboxyalkyl groups esterified with an alkyl or alkenyl group having 1-4 carbon atoms, carboxyalkoxy groups, carboxyalkyloxy groups esterified with an alkyl or alkenyl group having 1-4 carbon atoms, N-alkylpiperazinylcarbonyl groups, N-alkylpiperazinylcarbonylalkyl groups, N-alkylpiperazinylcarbonylalkyloxy groups, and a morpholinicarbonyl group;
Dependencies are inferred from the claim text.