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US 2017/0283427 A1Published application
Compounds for the inhibition of cyclophilins and uses thereof
AssigneeMerck Patent GmbH
InventorsCatherine JORAND-LEBRUN, Theresa L. JOHNSON, Ulrich GRAEDLER, Xuliang JIANG, Santosh KULKARNI
Life of this patent
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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 C3-10 aryl, which is optionally substituted;
- each R′ is independently —R, halogen, -haloalkyl, -hydroxyalkyl, —OR, —C(O)R, —CO2R, —C(O)N(R)2, —NRC(O)R, or —N(R)2;
- each R1 is independently —H or C1-6 aliphatic which is optionally substituted;
- each R1a is independently —H or C1-6 aliphatic which is optionally substituted;
- or R1 and R1a taken together with the atom to which they are attached form a 3-7 membered carbocyclic ring optionally having 1-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, which is optionally substituted;
- each R2 is independently —H or C1-6 aliphatic which is optionally substituted;
- each R2a is independently —H or C1-6 aliphatic which is optionally substituted;
- X is CH2 or O;
- or X and the bonds attached to X are absent;
- 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;
- n is 1 or 2;
- and
- p is 1, 2, 3, 4, or 5.
16 more elements
Dependencies are inferred from the claim text.