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Last Updated: December 16, 2025

Claims for Patent: 11,723,901


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Summary for Patent: 11,723,901
Title:Uses of piperidinyl-indole derivatives
Abstract:The present invention relates to the novel use of certain piperidinyl-indole derivatives in the treatment of patients suffering from renal diseases or disorders, and in particular for the treatment of patients suffering from C3G (C3 glomerulopathy) and IgAN (IgA nephropathy).
Inventor(s):Jörg Eder, Richard Alexander Harrison, Boerje Haraldsson, Anna Svenja Schubart
Assignee: Novartis AG , Novartis Pharma AG
Application Number:US16/642,905
Patent Claims: 1. A method of treating IgAN (immuneglobuline A nephropathy), in a patient suffering therefrom, comprising the step of administering an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof to said patient, wherein R is hydrogen, C1-C4alkyl, or C1-C6alkoxy; R1 is C1-C6alkoxy; R2 is C1-C6alkyl; R3 is C1-C6alkoxy; C1-C6alkyl; or hydroxyl; R4 is phenyl, optionally substituted by —C(O)R8, and R8 is hydroxy, C1-C4alkoxy, or amino.

2. The method of claim 1, wherein R is hydrogen or C1-C2alkyl; R1 is C1-C6alkoxy; R2 is C1-C6alkyl; R3 is C1-C6alkoxy or C1-C6alkyl; and R4 is phenyl, optionally substituted by —C(O)R8, and R8 is hydroxyl or C1-C4alkoxy.

3. The method of claim 1, wherein R is hydrogen; R1 is C1-C2alkoxy; R2 is C1-C2alkyl; R3 is C1-C2alkoxy; and R4 is phenyl, optionally substituted by —C(O)R8, and R8 is hydroxy.

4. The method of claim 1, wherein the compound of formula (I) is selected from the group consisting of: 4-(1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)-4-methylpiperidin-2-yl)benzoic acid; 4-(4-methoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl(benzoic acid; 4-(4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl(benzoic acid; 4-(5-methoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl(benzoic acid; 4-(5-hydroxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl(benzoic acid; ethyl 4-((2S,4R)-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)-4-methylpiperidin-2-yl(benzoate; and ethyl 4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl(benzoate.

5. The method of claim 1, wherein the effective amount of the compound of formula (I) or the pharmaceutically acceptable salt thereof is 25 mg, 50 mg, 100 mg or 200 mg.

6. The method of claim 1, wherein the effective amount of the compound of formula (I) or the pharmaceutically acceptable salt thereof is administered to the patient twice a day.

7. The method of claim 1, wherein 25 mg, 50 mg, 100 mg or 200 mg of the compound of formula (I) or the pharmaceutically acceptable salt thereof is administered to the patient twice a day.

8. The method of claim 1, wherein 200 mg of the compound of formula (I) or the pharmaceutically acceptable salt thereof is administered to the patient twice a day.

9. The method of claim 1, wherein the compound of formula (I) or a pharmaceutically acceptable salt thereof is administered to the patient in a unit dosage of 0.1-1000 mg, 0.1-500 mg, 0.1-250 mg, 0.1-150 mg, 0.5-100 mg, or 0.5-50 mg.

10. The method of claim 1, wherein the compound of formula (I) is 4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl(benzoic acid or a pharmaceutically acceptable salt thereof.

11. The method of claim 10, wherein the effective amount of the compound of formula (I) or the pharmaceutically acceptable salt thereof is 25 mg, 50 mg, 100 mg or 200 mg.

12. The method of claim 10, wherein the effective amount of the compound of formula (I) or the pharmaceutically acceptable salt thereof is administered to the patient twice a day.

13. The method of claim 10, wherein 25 mg, 50 mg, 100 mg or 200 mg of the compound of formula (I) or the pharmaceutically acceptable salt thereof is administered to the patient twice a day.

14. The method of claim 10, wherein 200 mg of the compound of formula (I) or the pharmaceutically acceptable salt thereof is administered to the patient twice a day.

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