# US 8,785,447 B2 · Use of dopamine D3 receptor ligands for the production of drugs for treating renal function disorders

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- Number: US 8,785,447 B2
- Document ID: US8785447B2
- Status: Granted
- Kind: B2
- Application number: 11/424,739
- Filed: 2006-06-16
- Published: 2006-10-05
- Granted: 2014-07-22
- Earliest claimed: 2006-06-16
- Assignees: AbbVie Deutschland GmbH & Co. KG
- Applicants: Bernd Mühlbauer; Gerhard Groβ; Dorothea Starck; Hans-Jörg Treiber
- Inventors: Bernd Mühlbauer; Gerhard Groβ; Dorothea Starck; Hans-Jörg Treiber
- Web page: https://patentgrep.com/patent/US8785447B2

## CPC

- A61K 31/517: ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
- A61K 31/00: Medicinal preparations containing organic active ingredients
- A61K 31/4725: containing further heterocyclic rings
- A61K 31/495: having six-membered rings with two {or more} nitrogen atoms as the only ring heteroatoms, e.g. piperazine {or tetrazines}(A61K31/48 takes precedence {; with three nitrogen atoms A61K31/53})
- A61K 31/496: Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
- A61K 31/506: not condensed and containing further heterocyclic rings
- A61P 1/00: Drugs for disorders of the alimentary tract or the digestive system
- A61P 13/12: of the kidneys
- A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D)
- A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS

## Abstract

The invention relates to the use of dopamine D3 receptor ligands for the production of drugs for treating renal function disorders.

## Claims

### Claim 1

A method for the treatment of a renal function disorder comprising administering an effective amount of dopamine D3 receptor antagonists to a patient in need thereof, wherein the renal function disorder is selected from the group consisting of
renal function disorders with glomerular hyperfiltration,
renal function disorders caused by diabetes mellitus,
renal function disorders caused by nonrenal hypertension,
renal function disorders caused by glomerulonephritis,
renal function disorders caused by ascending urinary tract infections,
renal function disorders caused by sickle cell anemia,
renal function disorders caused by compensatory hypertrophy after unilateral nephrectomy, and
renal function disorders caused by mesangial dysfunction.

### Claim 2 (depends on 1)

The method as claimed in claim 1, 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.

### Claim 3 (depends on 1)

The method of claim 1, wherein the dopamine D3 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)homo-piperazin-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.

### Claim 4 (depends on 1)

The method of claim 1, wherein the dopamine D3 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)-propylmercapto)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.

### Claim 5 (depends on 1)

The method of claim 1, wherein the dopamine D3 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,
3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)but-1-ylpyrimidin-4-ol and 4-methoxybenzoic acid N-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)homopiperazin-1-yl)but-1-ylamide.

### Claim 6

A method for the treatment of a renal function disorder associated with glomerular hyperfiltration in a patient which comprises administering to said patient an effective amount of a dopamine D3 receptor antagonist.

### Claim 7 (depends on 6)

The method of claim 6, wherein the dopamine D3 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-carboxylicacid 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)-propylmercapto)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-prop enamide and
2-(4-{[(E)-3-(1H-indol-5-yl)-2-propenoyl]amino}butyl)-1,2,3,4-tetrahydro-7-isoquinolinyl trifluoromethanesulfonate.

### Claim 8 (depends on 6)

The method of claim 6, wherein the dopamine D3 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.

### Claim 9 (depends on 6)

The method of claim 6, wherein the dopamine D3 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,
3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)but-1-ylpyrimidin-4-ol and 4-methoxybenzoic acid N-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)homopiperazin-1-yl)but-1-ylamide.

### Claim 10 (depends on 6)

The method as claimed in claim 6, 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.

### Claim 11

A method for the treatment of a renal function disorder associated with albuminurea in a patient which comprises administering to said patient an effective amount of a dopamine D3 receptor antagonist.

### Claim 12 (depends on 11)

The method of claim 11, wherein the dopamine D3 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)homo-piperazin-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.

### Claim 13 (depends on 11)

The method of claim 11, wherein the dopamine D3 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)propylmercapto)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.

### Claim 14 (depends on 11)

The method of claim 11, wherein the dopamine D3 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,
3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)but-1-ylpyrimidin-4-ol and
4-methoxybenzoic acid N-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)homopiperazin-1-yl)but-1-ylamide.

### Claim 15 (depends on 11)

The method as claimed in claim 11, 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.

### Claim 16

A method for the treatment of a renal function disorder associated with glomerular hypertrophy in a patient which comprises administering to said patient an effective amount of a dopamine D3 receptor antagonist.

### Claim 17 (depends on 16)

The method of claim 16, wherein the dopamine D3 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)homo-piperazin-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-prop enamide and
2-(4-{[(E)-3-(1H-indol-5-yl)-2-propenoyl]amino}butyl)-1,2,3,4-tetrahydro-7-isoquinolinyl trifluoromethanesulfonate.

### Claim 18 (depends on 16)

The method of claim 16, wherein the dopamine D3 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)propylmercapto)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.

### Claim 19 (depends on 16)

The method of claim 16, wherein the dopamine D3 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,
3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)but-1-ylpyrimidin-4-ol and
4-methoxybenzoic acid N-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)homopiperazin-1-yl)but-1-ylamide.

### Claim 20 (depends on 16)

The method as claimed in claim 16, 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.

### Claim 21

A method for the treatment of diabetic nephropathy comprising administering an effective amount of dopamine D3 receptor antagonists to a patient in need thereof.

### Claim 22 (depends on 21)

The method as claimed in claim 21, 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.

### Claim 23 (depends on 21)

The method of claim 21, wherein the dopamine D3 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)homo-piperazin-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-carboxylicacid 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-prop enamide and
2-(4-{[(E)-3-(1H-indol-5-yl)-2-propenoyl]amino}butyl)-1,2,3,4-tetrahydro-7-isoquinolinyl trifluoromethanesulfonate.

### Claim 24 (depends on 21)

The method of claim 21, wherein the dopamine D3 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-carboxylicacid 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)-propylmercapto)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.

### Claim 25 (depends on 21)

The method of claim 21, wherein the dopamine D3 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,
3-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)piperazin-1-yl)but-1-ylpyrimidin-4-ol and 4-methoxybenzoic acid N-(4-(4-(2-t-butyl-6-trifluoromethyl)pyrimidin-4-yl)homopiperazin-1-yl)but-1-ylamide.