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US 2017/0283425 A1Published application
Compounds for the inhibition of cyclophilins and uses thereof
AssigneeMerck Patent GmbH
InventorsCatherine JORAND-LEBRUN, Theresa L. JOHNSON, Ulrich GRAEDLER, Xuliang JIANG, Didier ROCHE, Hugues LEMOINE, Marine GILARDONE
Life of this patent
Estimating the term…
Abstract
The present invention relates to compounds, and pharmaceutically acceptable compositions thereof, useful as inhibitors of cyclophilins, and for the treatment of cyclophilin-related disorders.
Claims20
A compound of formula I,
- or a pharmaceutically acceptable salt thereof, wherein:
- Ring A is a fused 5-10 membered saturated or partially unsaturated heterocyclic mono- or bicyclic ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur;
- which is optionally substituted;
- L is
- each R1 is independently —R, halogen, -haloalkyl, -hydroxyalkyl, —OR, —C(O)R, —CO2R, —C(O)N(R)2, —NRC(O)R, or —N(R)2;
- each R2 is independently —R, halogen, -haloalkyl, -hydroxyalkyl, —OR, —C(O)R, —CO2R, —C(O)N(R)2, —NRC(O)R, or —N(R)2;
- R3 is —H or C1-6 aliphatic which is optionally substituted;
- R4 is —H, C1-6 aliphatic, C3-10 aryl, a 3-8 membered saturated or partially unsaturated carbocyclic ring, a 3-7 membered heterocylic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur;
- each of which is optionally substituted;
- or R3 and R4 taken together with the nitrogen to which they are attached to form a 3-7 membered heterocylic ring having 1-4 additional heteroatoms independently selected from nitrogen, oxygen, or sulfur, which is optionally substituted;
- each R is independently hydrogen, C1-6 aliphatic, C3-10 aryl, a 3-8 membered saturated or partially unsaturated carbocyclic ring, a 3-7 membered heterocylic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur;
- each of which is optionally substituted;
- or
- two R groups on the same atom are taken together with the atom to which they are attached to form a C3-10 aryl, a 3-8 membered saturated or partially unsaturated carbocyclic ring, a 3-7 membered heterocylic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or a 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur;
- each of which is optionally substituted;
- m is 1 or 2;
- and
- n is 0, 1, 2, or 3.
15 more elements
Dependencies are inferred from the claim text.