US2005143440A1PendingUtilityA1
Imidazoline compounds
Est. expiryOct 23, 2022(expired)· nominal 20-yr term from priority
Inventors:Sylvain RaultMarina KoppJean-Charles LancelotStéphane LemaitreDaniel-Henri CaignardJean-Guy Bizot-EspiardPierre Renard
A61P 3/06A61P 9/10A61P 3/04A61P 9/00A61P 25/24C07D 403/06C07D 401/06A61P 3/10C07D 409/06A61P 3/00
45
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Claims
Abstract
Compounds of formula (I): wherein: R 1 represents an optionally substituted heteroaryl group, R 2 represents an optionally substituted cycloalkyl group, R 3 represents a hydrogen atom or an alkyl group, and R 4 and R 5 are as defined in the description, and Medicinal products containing the same are useful in the treatment of non-insulin-dependent type II diabetes, obesity, type I diabetes, hyperlipidaemia, hypercholesterolaemia and cardiovascular complications thereof.
Claims
exact text as granted — not AI-modified1 . A method for treating a living animal body, including a human, afflicted with a pathology associated with hyperlipidaemia, hypercholesterolaemia and cardiovascular complications thereof, comprising the step of administering to the living animal body, including a human, an amount of a compound selected from those of formula (I):
wherein:
R 1 represents an optionally substituted 5-membered heteroaryl group,
R 2 represents an optionally substituted cycloalkyl group,
R 3 represents a hydrogen atom or an alkyl group, and
R 4 and R 5 , which may be identical or different, each represents a hydrogen atom, a halogen atom, an alkyl group or a polyhaloalkyl group,
its enantiomers, diastereoisomers and tautomers thereof, and also addition salts thereof with a pharmaceutically acceptable acid or base,
which is effective for alleviation of the pathology.
2 . The method of claim 1 , wherein R 4 and R 5 , which may be identical or different, each represents a hydrogen atom or an alkyl group.
3 . The method of claim 1 , wherein R 3 represents a hydrogen atom.
4 . The method of claim 1 , wherein R 2 represents a cyclopentyl, cyclohexyl or cycloheptyl group optionally substituted by an alkyl group.
5 . The method of claim 1 , wherein R 1 represents an optionally substituted 5-membered heteroaryl group, R 2 represents a cyclohexyl or cycloheptyl group optionally substituted by an alkyl group, R 3 represents a hydrogen atom and R 4 and R 5 , which may be identical or different, each represents a hydrogen atom or an alkyl group.
6 . The method of claim 1 , wherein the alkyl group is a methyl group.
7 . The method of claim 1 , wherein the compound of formula (I) is selected from 2-[cyclohexyl(3-thienyl)methyl]-4-methyl-4,5-dihydro-1H-imidazole, its enantiomers, diastereoisomers and tautomers thereof, and also addition salts thereof with a pharmaceutically acceptable acid.
8 . The method of claim 1 , wherein the compound of formula (I) is selected from (4S)-2-[cyclohexyl(3-thienyl)methyl]-4-methyl-4,5-dihydro-1H-imidazole, its diastereoisomers and tautomers thereof, and also addition salts thereof with a pharmaceutically acceptable acid.
9 . The method of claim 1 , wherein the compound of formula (I) is selected from (4 R)-2-[cyclohexyl(3-thienyl)methyl]-4-methyl-4,5-dihydro-1H-imidazole, its diastereoisomers and tautomers thereof, and also addition salts thereof with a pharmaceutically acceptable acid.Join the waitlist — get patent alerts
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