Imidazole-5-carboxylic acid derivatives, the preparation method therefor and the uses thereof
AssigneeSalubris Asset Management Co., Ltd.
InventorsJianhui Guo, Dong An
Life of this patent
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Abstract
The invention discloses imidazole-5-carboxylic acid derivatives, and their preparation methods. The derivatives of the invention are Angiotensin II receptor antagonists with angiotensin II antagonistic activity and antihypertensive activity, and thereby can be used as a therapeutical agent to treat hypertension.
Claims17
A compound of formula (I), or its pharmaceutically acceptable salts,
- wherein R is
- wherein R1 and R2 are independently selected from the group consisting of hydrogen, straight or branched C1-C4alkyl, and C3-C7cycloalkyl, and wherein the alkyl or the cycloalkyl group is unsubstituted or substituted by 1-3 substituents selected from the group consisting of F, Cl, Br, NH2, and OH.
A compound selected from:
- 2-butyl-4-chloro-1-[2′-(1H-tetrazol-5-yl)1,1′-biphenyl-methyl]imidazole-5-carboxylic acid, pivaloyloxymethyl ester;
- 2-butyl-4-chloro-1-[2′-(1H-tetrazol-5-yl)1,1′-biphenyl-methyl]imidazole-5-carboxylic acid, 1-[(isopropoxycarbonyl)oxy]methyl ester;
- 2-butyl-4-chloro-1-[2′-(1H-tetrazol-5-yl)1,1′-biphenyl-methyl]imidazole-5-carboxylic acid, 1-[(ethoxycarbonyl)oxy]methyl ester;
- and
- 2-butyl-4-chloro-1-[2′-(1H-tetrazol-5-yl)1,1′-biphenyl-methyl]imidazole-5-carboxylic acid, 1-[(tert-butoxycarbonyl)oxy]methyl ester.
2-butyl-4-chloro-1-[2′-(1H-tetrazol-5-yl)1,1′-biphenyl-methyl]imidazole-5-carboxylic acid, 1-[(isopropoxycarbonyl)oxy]methyl ester of the formula:
A pharmaceutically acceptable salt of a compound selected from:
- 2-butyl-4-chloro-1-[2′-(1H-tetrazol-5-yl)1,1′-biphenyl-methyl]imidazole-5-carboxylic acid, pivaloyloxymethyl ester;
- 2-butyl-4-chloro-1-[2′-(1H-tetrazol-5-yl)1,1′-biphenyl-methyl]imidazole-5-carboxylic acid, 1-[(isopropoxycarbonyl)oxy]methyl ester;
- 2-butyl-4-chloro-1-[2′-(1H-tetrazol-5-yl)1,1′-biphenyl-methyl]imidazole-5-carboxylic acid, 1-[(ethoxycarbonyl)oxy]methyl ester;
- and
- 2-butyl-4-chloro-1-[2′-(1H-tetrazol-5-yl)1,1′-biphenyl-methyl]imidazole-5-carboxylic acid, 1-[(tert-butoxycarbonyl)oxy]methyl ester.
A pharmaceutically acceptable salt of 2-butyl-4-chloro-1-[2′-(1H-tetrazol-5-yl)1,1′-biphenyl-methyl]imidazole-5-carboxylic acid, 1-[(isopropoxycarbonyl)oxy]methyl ester.
A pharmaceutical composition comprising 2-butyl-4-chloro-1-[2′-(1H-tetrazol-5-yl)1,1′-biphenyl-methyl]imidazole-5-carboxylic acid, 1-[(isopropoxycarbonyl)oxy]methyl ester, and a pharmaceutically acceptable carrier, excipient, or diluent.
A pharmaceutical composition comprising a pharmaceutically acceptable salt of 2-butyl-4-chloro-1-[2′-(1H-tetrazol-5-yl)1,1′-biphenyl-methyl]imidazole-5-carboxylic acid, 1-[(isopropoxycarbonyl)oxy]methyl ester, and a pharmaceutically acceptable carrier, excipient, or diluent.
A method of treating hypertension, by inhibiting the type I receptor of angiotensin II, comprising administrating to a patient in need of said treating an amount effective for treating hypertension of 2-butyl-4-chloro-1-[2′-(1H-tetrazol-5-yl)1,1′-biphenyl-methyl]imidazole-5-carboxylic acid, 1-[(isopropoxycarbonyl)oxy]methyl ester.
A method of treating hypertension, by inhibiting the type I receptor of angiotensin II, comprising administrating to a patient in need of said treating an amount effective for treating hypertension of a pharmaceutically acceptable salt of 2-butyl-4-chloro-1-[2′-(1H-tetrazol-5-yl)1,1′-biphenyl-methyl]imidazole-5-carboxylic acid, 1-[(isopropoxycarbonyl)oxy]methyl ester.
Dependencies are inferred from the claim text.