Use of vasopeptidase inhibitors in the treatment of metabolic diseases, nephropathy and advanced glycation end-product associated diseases
View Patent ↗The invention discloses and claims the use of vasopeptidase inhibitors of formula (II) for the treatment of nephropathy in non-diabetic patients.
1. A method of treating non-diabetic nephropathy comprising administering to a patient in need of said treatment a therapeutically effective amount of a compound of formula (II)
wherein
R 1 is hydrogen or acetyl;
R 2 is hydrogen, —CH 2 O—C(O)C(CH 3 ) 3 , C 1 -C 4 -alkyl, aryl, —(C 1 -C 4 -alkyl)-aryl, or diphenylmethyl;
X is —(CH 2 ) n wherein n is an integer 0 or 1, —S—, —O—,
wherein R 3 is hydrogen, C 1 -C 4 -alkyl, aryl, or —(C 1 -C 4 -alkyl)-aryl; and R 4 is CF 3 , C 1 -C 10 -alkyl, aryl, or —(C 1 -C 4 -alkyl)-aryl;
B 1 and B 2 are each independently hydrogen, hydroxy, or —OR 5 , wherein R 5 is C 1 -C 4 -alkyl, aryl, or —(C 1 -C 4 -alkyl)-aryl or, where B 1 and B 2 are attached to adjacent carbon atoms, B 1 and B 2 can be taken together with said adjacent carbon atoms to form a benzene ring or methylenedioxy,
or a pharmaceutically acceptable salt or stereoisomer thereof.
2. The method according to claim 1 , wherein R 1 is acetyl.
3. The method according to claim 1 , wherein R 1 is hydrogen.
4. The method according to claim 1 , wherein B 1 and B 2 are hydrogen.
5. The method according to claim 1 , wherein X is —CH 2 .
6. The method according to claim 1 , wherein the compound is the compound of formula (II-A)
wherein R 1 is acetyl or hydrogen.
7. The method according to claim 6 , wherein the compound has the formula (II-B)
8. The method according to claim 6 , wherein the compound has the formula (II-C)