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US5480888A
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Inhibitor for restenosis after percutaneous coronary arterioplasty
Assignee: Daiichi Pharmaceutical Co Ltd
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Filing: 1993-01-14
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Granted: 1996-01-02
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Expires: 2013-01-14
Abstract
Abstract An inhibitor for restenosis after percutaneous coronary arterioplasty, which comprises, as an active ingredient, a compound of the following formula (1), (1') or a pharmaceutically acceptable salt thereof: ##STR1## wherein R 1 and R 2 are independently a hydrogen atom, a halogen atom, a trifluoromethyl group, a nitro group, a C1-C6 alkyl group or a C1-C6 alkoxyl group, and R 1 and R 2 may be linked to form a methylenedioxy group; R 3 is an optionally substituted aryl group, an optionally substituted aromatic heterocyclic group, an optionally substituted 5 to 7-membered cycloalkyl or cycloalkenyl group; R 4 is a hydrogen atom, a hydroxyl group, an -S-glutathione residue, an -S-α-amino acid residue, or an aralkyl group optionally having substituent(s) in the aryl moiety; R 5 is a hydrogen atom or a C1-C6 alkyl group, and R 4 and R 5 may be linked to form a single bond; Y is an oxygen atom or a sulfur atom; n is an integer of from 0 to 5, and the selenium atom may be oxidized. The inhibitor of the present invention exhibits excellent inhibitory effect against restenosis after PTCA with low toxicity.
Inventors
- 👤 Kazuhisa Kodama
- 👤 Atsushi Hirayama
- 👤 Hiroyuki Masayasu
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-23 10:55
CPC Classifications
A; A61; A61K; A61K38/00; A61K38/04; A61K38/06; A61K38/063; A61K31/00; A61K31/28; A61K31/33; A61K31/335; A61K31/357; A61K31/36; A61K31/555; A61P; A61P9/00; A61P9/08; A61P9/10
Claims Analysis
Total Claims: 4
Claim 1
Independent Claim
160 words
An inhibitor for restenosis after percutaneous coronary arterioplasty, which comprises, as an active ingredient, a compound of the following formula (1), (1') or a pharmaceutically acceptable salt thereof: ##STR6## wherein R 1 and R 2 are independently a hydrogen atom, a halogen atom, a trifluoromethyl group, a nitro group, a C1-C6 alkyl group or a C1-C6 alkoxyl group, and R 1 and R 2 may be linked to form a methylenedioxy group; R 3 is an optionally substituted aryl group, an optionally substituted aromatic heterocyclic group, an optionally substituted 5 to 7-membered cycloalkyl or cycloalkenyl group; R 4 is a hydrogen atom, a hydroxyl group, an -S-glutathione residue, an -S-α-amino acid residue, or an aralkyl group optionally having substituent(s) in the aryl moiety; and R 5 is a hydrogen atom or a C1-C6 alkyl group; Y is an oxygen atom or a sulfur atom; n is an integer of from 0 to 5, and the selenium atom may be oxidized.
Claim 2
Dependent Claim
160 words
An inhibitor for restenosis after percutaneous coronary arterioplasty, which comprises, as an active ingredient, a compound of the following formula (1), (1') or a pharmaceutically acceptable salt thereof: ##STR6## wherein R 1 and R 2 are independently a hydrogen atom, a halogen atom, a trifluoromethyl group, a nitro group, a C1-C6 alkyl group or a C1-C6 alkoxyl group, and R 1 and R 2 may be linked to form a methylenedioxy group; R 3 is an optionally substituted aryl group, an optionally substituted aromatic heterocyclic group, an optionally substituted 5 to 7-membered cycloalkyl or cycloalkenyl group; R 4 is a hydrogen atom, a hydroxyl group, an -S-glutathione residue, an -S-α-amino acid residue, or an aralkyl group optionally having substituent(s) in the aryl moiety; and R 5 is a hydrogen atom or a C1-C6 alkyl group; Y is an oxygen atom or a sulfur atom; n is an integer of from 0 to 5, and the selenium atom may be oxidized.
Claim 3
Independent Claim
186 words
A method of inhibiting restenosis after percutaneous coronary arterioplasty, which comprises: administering a therapeutically effective amount of a compound of the formula (1), (1') or a pharmaceutically acceptable salt thereof; ##STR7## wherein R 1 and R 2 are independently a hydrogen atom, a halogen atom, a trifluoromethyl group, a nitro group, a C 1 14 C 6 alkyl group or a C 1 14 C 6 alkoxyl group, and R 1 and R 2 may be linked to form a methylenedioxy group; R 3 is an optionally substituted aryl group, an optionally substituted aromatic heterocyclic group, an optionally substituted 5 to 7-membered cycloalkyl or cycloalkenyl group; R 4 is a hydrogen atom, a hydroxyl group, an -S-glutathione residue, an -S-α-amino acid residue, or an aralkyl group optionally having substituent(s) in the aryl moiety; R 5 is a hydrogen atom or a C 1 -C 6 alkyl group; and R 4 and R 5 may be linked to form a single bond; Y is an oxygen atom or a sulfur atom; n is an integer of from 0 to 5, and the selenium atom may be oxidized.
Claim 4
Independent Claim
186 words
A method of inhibiting restenosis after percutaneous coronary arterioplasty, which comprises: administering a therapeutically effective amount of a compound of the formula (1), (1') or a pharmaceutically acceptable salt thereof; ##STR7## wherein R 1 and R 2 are independently a hydrogen atom, a halogen atom, a trifluoromethyl group, a nitro group, a C 1 14 C 6 alkyl group or a C 1 14 C 6 alkoxyl group, and R 1 and R 2 may be linked to form a methylenedioxy group; R 3 is an optionally substituted aryl group, an optionally substituted aromatic heterocyclic group, an optionally substituted 5 to 7-membered cycloalkyl or cycloalkenyl group; R 4 is a hydrogen atom, a hydroxyl group, an -S-glutathione residue, an -S-α-amino acid residue, or an aralkyl group optionally having substituent(s) in the aryl moiety; R 5 is a hydrogen atom or a C 1 -C 6 alkyl group; and R 4 and R 5 may be linked to form a single bond; Y is an oxygen atom or a sulfur atom; n is an integer of from 0 to 5, and the selenium atom may be oxidized.
References Cited (Backward Citations)
US4711961A
Cited
US5187105A
Cited
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