IP Library › Granted Patent US 7,098,214

Granted Patent B1

US 7,098,214 · App. 09/959,787 · Granted Aug 29, 2006

Dopamine D

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Patent No.: US 7,098,214
App. No.: 09/959,787
Granted: Aug 29, 2006
Kind: B1

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Abstract

Dopamine D 3 receptor ligands or antagonists are disclosed for use in the treatment of renal function disorders, such as diabetic nephropathy.

Claims (68)

1. A method for the treatment of renal function disorders comprising administering an effective amount of dopamine D 3 receptor ligands to a patient in need thereof, wherein the receptor ligand is

5-amino-3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)-piperazin-1-yl)-2-methylbut-2-eny-1-ylmercapto)-4-methyl-1,2,4-(4H)-triazole or

2-(3-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)propylmercaptopyrimidin-4-ol fumarate.

2. The method as claimed in claim 1 , for the treatment of diabetic nephrophathy.

3. A method for the treatment of diabetic nephropathy, comprising administering an effective amount of a dopamine D 3 receptor antagonist to a patient in need thereof.

4. The method as claimed in claim 3 , wherein the receptor antagonist is

5-amino-3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)-piperazin-1-yl)-2-methylbut-2-eny-1-ylmercapto)-4-methyl-1,2,4-(4H)-triazole or

2-(3-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)propylmercaptopyrimidin-4-ol fumarate.

5. The method of claim 3 , wherein the dopamine D 3 receptor antagonist is selected from the group consisting of

4′-acetylbiphenyl-4-carboxylic acid N-(4-(4-(2-methoxyphenyl)piperazin-1-yl)but-1-yl)amide,

thienyl-2-carboxylic acid N-(4-(4-(2,3-dichlorophenyl)piperazin-1-yl)but-1-yl)amide,

3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)but-2-ylmercapto)-4-methyl-5-methylamino-1,2,4-(4H)-triazole,

3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)2-methyleneprop-1-yl-mercapto)5-methylamino-1,2,4-(4H)-triazole,

5-amino-3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)homopiperazin-1-yl)2-methyl-but-2-en-1-ylmercapto)-4-methyl-1,2,4-(4H)-triazole,

3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)prop-1-ylmercapto)-4-methyl-5-methylamino-1,2,4-(4H)-triazole,

5-amino-3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)2-methyl-but-2-en-1-ylmercapto)-4-methyl-1,2,4-(4H)-triazole,

5-amino-3-(4-(4-(2-t-butyl-6-n-propyl)pyrimidin-4-yl)piperazin-1-yl)2-methyl-prop-1-en-1-ylmercapto)-4-methyl-1,2,4-(4H)-triazole,

5-amino-3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)2-methyl-but-2-ylmercapto)-4-methyl-1,2,4-(4H)-triazole,

2-(3-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)propoxy-pyrimidin-4-ol,

2-(3-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)propylmercaptopyrimidin-4-ol fumarate,

2-naphthoic acid N-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)homopiperazin-1-yl)but-1-ylamide,

5-amino-3-(4-(4-(2-t-butyl-6-n-propyl)pyrimidin-4-yl)piperazin-1-yl)-2-methylen-prop-1-ylmercapto)-4-methyl-1,2,4-(4H)-triazole,

3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)prop-1-ylmercapto-5-(2,5-dimethylfur-3-yl) 4 -methyl-1,2,4-(4H)-triazole,

(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)homopiperazin-1-yl)prop-1-ylmercapto-4-methyl-5-(4-methylpyrazol-5-yl)1,2,4-(4H)-triazole,

4-methyl-5-phenyl-1,2,4-(4H)-triazole-3-carboxylic acid N-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)homopiperazin-1-yl)-but-1-yl-amide,

5-amino-2-(8-(4-(3-cyanophenyl)piperazin-1-yl)octyl-1-yl-mercapto)1,3,4-thiadiazole,

2-(3-(5-(3-(trifluoromethylphenyl)-1,5-diazocin-1-yl)-propyl-mercapto)pyrimidin-4-ol,

3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)but-1-ylpyrimidin-4-ol,

4-methoxybenzoic acid N-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)homopiperazin-1-yl)but-1-ylamide,

1-benzothiophene-2-carboxylic acid N-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)but-1-ylamide,

5-methoxybenzofuran-2-carboxylic acid N-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)homopiperazin-1-yl)but-1-ylamide,

(E)-N-({2-[(7-cyano-3,4-dihydro-2(1H)-isoquinolinyl)methyl]cyclopropyl}methyl)-3-(1H-indol-5-yl)-2-propenamide and

2-(4-{[(E)-3-(1H-indol-5-yl)-2-propenoyl]amino}butyl)-1,2,3,4-tetrahydro-7-isoquinolinyl trifluoromethanesulfonate.

6. The method of claim 3 , wherein the dopamine D 3 receptor antagonist is selected from the group consisting of

3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)but-2-ylmercapto)-4-methyl-5-methylamino-1,2,4-(4H)-triazole,

3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)2-methyleneprop-1-yl-mercapto)5-methylamino-1,2,4-(4H)-triazole,

5-amino-3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)homopiperazin-1-yl) 2 -methyl-but-2-en-1-ylmercapto)-4-methyl-1,2,4-(4H)-triazole,

3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)prop-1-ylmercapto)-4-methyl-5-methylamino-1,2,4-(4H)-triazole,

5-amino-3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)2-methyl-but-2-en-1-ylmercapto)-4-methyl-1,2,4-(4H)-triazole,

5-amino-3-(4-(4-(2-t-butyl-6-n-propyl)pyrimidin-4-yl)piperazin-1-yl)2-methyl-prop-1-en-1-ylmercapto)-4-methyl-1,2,4-(4H)-triazole,

5-amino-3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)-piperazin-1-yl)2-methyl-but-2-ylmercapto)-4-methyl-1,2,4-(4H)-triazole,

2-(3-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)propoxy-pyrimidin-4-ol,

2-(3-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)propylmercaptopyrimidin-4-ol fumarate,

5-amino-3-(4-(4-(2-t-butyl-6-n-propyl)pyrimidin-4-yl)piperazin-1-yl)-2-methylen-prop-1-ylmercapto)-4-methyl-1,2,4-(4H)-triazole,

3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)prop-1-ylmercapto-5-(2,5-dimethylfur-3-yl)4-methyl-1,2,4-(4H)-triazole,

(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)homopiperazin-1-yl)prop-1-ylmercapto-4-methyl-5-(4-methylpyrazol-5-yl)1,2,4-(4H)-triazole,

4-methyl-5-phenyl-1,2,4-(4H)-triazole-3-carboxylic acid N-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)homopiperazin-1-yl)-but-1-yl-amide,

2-(3-(5-(3-(trifluoromethylphenyl)-1,5-diazocin-1-yl)-propyl-mercapto)pyrimidin-4-ol,

3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)but-1-ylpyrimidin-4-ol,

4-methoxybenzoic acid N-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)homopiperazin-1-yl)but-1-ylamide,

1-benzothiophene-2-carboxylic acid N-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)but-1-ylamide and

5-methoxybenzofuran-2-carboxylic acid N-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)homopiperazin-1-yl)but-1-ylamide.

7. The method of claim 3 , wherein the dopamine D 3 receptor antagonist is selected from the group consisting of