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US 11,768,319 B2Granted
Glycyrrhetinic acid derivatives for treating hyperkalemia
AssigneeArdelyx, Inc.
InventorsGary Luehr, Dean Dragoli, Michael Leadbetter, Tao Chen, Jason Lewis
Life of this patent
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Abstract
The present invention provides a compound of formula (I) or a salt thereof: (I) wherein X, L, V, R1, R2, R3 and R4, are as defined herein. These compounds are inhibitors of 11-hydroxysteroid dehydrogenase type 2 (11-HSD-2) and are used to treat hyperkalemia.
Claims18
A compound of formula I or a salt thereof:
- wherein,
- X is a bond, —O—, —C(O)—, —N(Rx)—, —C(O)N(Rx)—, —N(Rx)—C(O)—, —S(O)n—N(Rx)— or —N(Rx)—S(O)n—;
- V is —C(O)O—, —C(O)N(R5)—, —C(O)N(R5)O—, —NH—C(O)—N(R5)— or NH—S(O)n—;
- L is a bond, alkylene wherein one or more non-adjacent methylene groups of said alkylene are replaced with —O—;
- divalent aryl or divalent heteroaryl;
- or L is alkylene-Y-alkylene wherein Y is O, NRx, S, SO, SO2 or a divalent heterocycle;
- wherein said alkylene groups are optionally substituted with OH, —C(O)O—R1, alkyl or alkyl substituted with OH or —C(O)O—R1;
- and wherein a carbon of said alkylene groups and Rx optionally together form a heterocycle;
- provided that when X is other than a bond, then L is other than a bond;
- R1 is alkyl optionally substituted with halogen, OH, amino, oxo, carboxy, acyloxy, alkoxycarbonyl, alkoxyacyloxy, alkoxycarbonyloxy, aminocarbonyl, a carbocycle optionally substituted with alkyl, haloalkyl, oxo, amino and halogen and a heterocycle optionally substituted with alkyl, oxo, amino and halogen;
- and a carbocycle or heterocycle optionally substituted with alkyl, haloalkyl, oxo, amino and halogen;
- wherein one or more non-adjacent methylene groups in any of the foregoing alkyl groups is replaced with O;
- R2 is H or R1;
- R3 is absent, Me;
- provided that when —X-L-C(O)O—R1 depends from the carbon to which R3 depends then R3 is absent;
- or R3 is —Z-L-C(O)O—R1 wherein Z is a bond, —O—, —N(Rx)—, —C(O)N(Rx)—, —N(Rx)—C(O)—, —S(O)n—N(Rx)— or —N(Rx)—S(O)n—;
- and
- R4 is absent, H or OH;
- provided that when —X-L-C(O)O—R1 depends from the carbon to which R4 depends then R4 is H or absent;
- R5 is H or alkyl;
- Rx is H, —C(O)O—R1, or alkyl optionally substituted with —C(O)O—R1;
- and
- n is 1 or 2.
20 more elements
Dependencies are inferred from the claim text.