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US 2022/0106329 A1Published application
Bicyclic ror-gamma modulators
AssigneeEscalier Biosciences B.V.
InventorsRaju MOHAN, John NUSS, Jason HARRIS, Shendong YUAN
Life of this patent
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Abstract
Described herein are retinoic acid related-related orphan nuclear receptor (ROR) modulators and methods of utilizing ROR-gamma modulators in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.
Claims49
A compound of Formula I, or a pharmaceutically acceptable salt, solvate, or stereoisomer thereof:
- wherein:
- is phenyl, or a 5-membered or 6-membered heteroaryl ring;
- is phenyl, or a 5-membered or 6-membered heteroaryl ring;
- Q is —(CH2)n—, —CH2YCH2—, or —(CH2)mY—, wherein —(CH2)n—, —CH2YCH2—, or —(CH2)mY— is attached to the ring carbon atoms at a and b, c and d, a and c, or b and d;
- X is —N(R3a)—, —C(R3b)(R3c)—, or —O—;
- Y is —O—, —S—, or —N(R3d)—;
- Z is —(C(R1)(R2))t—;
- each R1 and each R2 are each independently hydrogen, halo, or C1-C6alkyl;
- each R3 is independently selected from halo and C1-C6alkyl;
- R3a is hydrogen, C1-C6alkyl, C1-C6 haloalkyl, C2-C9 heteroaryl, (C2-C9 heteroaryl)-C1-C6alkylene-, —S(O)2R10, —C(O)R10, —C(O)OR11, or —C(O)N(R11)2, wherein C2-C9 heteroaryl and (C2-C9 heteroaryl)-C1-C6alkylene- are optionally substituted with 1 to 3 groups independently selected from halo, C1-C6alkyl, C1-C6 haloalkyl, and hydroxyl;
- R3b is hydrogen, halo, C1-C6alkyl, C1-C6 haloalkyl, —N(R11)S(O)2R10, —S(O)2R10, —C(O)R10, —C(O)OR11, or —C(O)N(R11)2;
- R3c is hydrogen, halo, C1-C6alkyl, or C1-C6 haloalkyl;
- R3d is selected from hydrogen, C1-C6alkyl, C1-C6 haloalkyl, —S(O)2R8, —C(O)R8, —C(O)OR9, and —C(O)N(R9)2;
- each R4 and each R5 are each independently selected from halo, cyano, C1-C6alkyl, C1-C6 haloalkyl, C1-C6alkoxy, —N(R7)2, —C(O)R6, —C(O)OR7, —C(O)N(R7)2, —N(R7)C(O)R6, —N(R7)SO2R6, —SO2R6, and —SO2N(R7)2;
- each R6 is independently C1-C6alkyl or C1-C6 haloalkyl;
- each R7 is independently hydrogen, C1-C6alkyl, or C1-C6 haloalkyl;
- R8 is C1-C6alkyl or C1-C6 haloalkyl;
- each R9 is independently hydrogen, C1-C6alkyl, or C1-C6 haloalkyl;
- Rth is C1-C6alkyl, C1-C6 haloalkyl, C1-C6alkyl-O—C1-C6alkyl-, C3-C8cycloalkyl, C2-C9 heterocyclyl, phenyl, (phenyl)-C1-C6alkylene-, C2-C9 heteroaryl, or (C2-C9 heteroaryl)-C1-C6alkylene-, wherein the C3-C8cycloalkyl, C2-C9 heterocyclyl, phenyl, (phenyl)-C1-C6alkylene-, C2-C9 heteroaryl, or (C2-C9 heteroaryl)-C1-C6alkylene- is optionally substituted with 1 to 3 groups selected from halo, C1-C6alkyl, C1-C6 haloalkyl, and hydroxyl;
- each RH is independently hydrogen, C1-C6alkyl, or C1-C6 haloalkyl;
- k is 0, 1, 2, 3, or 4;
- m is 1 or 2;
- n is 1, 2, 3, or 4;
- p is 0, 1, 2, 3, or 4;
- q is 0, 1, 2, 3, or 4;
- and
- t is 0, 1, 2, or 3.
24 more elements
Dependencies are inferred from the claim text.