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US 12,606,556 B2Granted
TYK-2 inhibitor
AssigneeBeOne Medicines I GmbH
InventorsQiuwen Wang, Yunhang Guo, Zhiwei Wang
Life of this patent
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Abstract
Disclosed herein is a compound of Formula (I) for inhibiting TYK2 and treating disease associated with undesirable tyk-2 activity (tyk-2 related diseases), a method of using the compounds disclosed herein for treating inflammatory or autoimmune disease, and a pharmaceutical composition comprising the same.
Claims17
A compound of Formula (I):
- or a stereoisomer or pharmaceutically acceptable salt hereof wherein:
- R1 is hydrogen, C1-6alkyl or C3-6cycloalkyl, wherein said C1-6alkyl and C3-6cycloalkyl are each optionally substituted with 0-7 R1a;
- R1a at each occurrence is independently hydrogen, deuterium, halogen, —CN or —OMe;
- R2 is —C(O)R2a or a 4-10 membered heterocyclyl containing 1-2 heteroatoms selected from nitrogen, oxygen or sulfur, wherein said 4-10 membered heterocyclyl is optionally substituted with 0-4 R2b;
- R2a is independently C1-6alkyl or C3-6cycloalkyl;
- R2b at each occurrence is independently hydrogen, ═O, halo, —CN, —(CH2)r—C3-6cycloalkyl, or a —(CH2)r-3-10 membered heterocyclyl comprising carbon atoms and 1-4 heteroatoms selected from nitrogen, oxygen or sulfur, wherein said —(CH2)r—C3-6cycloalkyl and —(CH2)r-3-10 membered heterocyclyl are each optionally substituted with 0-2 R2c;
- R2c at each occurrence is independently hydrogen, -haloC1-3alkyl or —C1-3alkyl;
- R3 is
- wherein n is an integer selected from 0, 1, 2, 3 and 4;
- and
- R3a at each occurrence is independently hydrogen, halogen, —CN, —C1-6alkyl, —C1-6alkoxyl, —P(O)R3dR3e, -(L1)r-CyA;
- or CyA, wherein said —C1-6alkyl, and —C1-6alkoxyl are each optionally substituted with 0-3 R3d;
- L1 at each occurrence is independently —O—, —S—, —C(O)—, —NH—, —CH2— or —NHC(O)—;
- CyA is C3-10 cycloalkyl, 3-10 membered heterocyclyl comprising carbon atoms and 1-4 heteroatoms selected from nitrogen, oxygen or sulfur, 6-10 membered aryl, or 4-10 membered heteroaryl comprising carbon atoms and 1-4 heteroatoms selected from nitrogen, oxygen or sulfur, wherein said C3-10 cycloalkyl, 3-10 membered heterocyclyl, 6-10 membered aryl and 4-10 membered heteroaryl are each substituted with 0-3 R3b;
- R3b at each occurrence is independently hydrogen, halogen, —C1-6alkyl, -oxo-, —OR3c, —C(O)R3d, —S(O)2R3d, —NR3dR3e, C3-10cycloalkyl, a 3-10 membered heterocyclyl containing 1-4 heteroatoms selected from nitrogen, oxygen or sulfur, a 6-10 membered aryl, or a 4-10 membered heteroaryl comprising carbon atoms and 1-4 heteroatoms selected from nitrogen, oxygen or sulfur;
- wherein said-C1-6alkyl, C3-10 cycloalkyl, 3-10 membered heterocyclyl, 6-10 membered aryl and 4-10 membered heteroaryl are each optionally substituted with 0-3 —R3d;
- R3c and R3d at each occurrence are independently hydrogen, halogen, —CN, hydroxyl, —C1-6alkyl, —C1-6alkoxy, a 5-6 membered aryl, a 3-6 membered heterocyclyl containing 1-2 heteroatoms selected from nitrogen, oxygen or sulfur, or a 5-6 membered heteroaryl comprising carbon atoms and 1-3 heteroatoms selected from nitrogen, oxygen or sulfur, wherein said —C1-6alkyl, —C1-6alkoxy, 5-6 membered aryl, 3-6 membered heterocyclyl, 5-6 membered heteroaryl are optionally substituted by -halogen, —CN, hydroxyl, —C1-6alkyl, —C1-6alkoxyl, C1-6alkylamino, diC1-6alkylamino, a 3-6 membered heterocyclyl, a 6-10 membered aryl or a 5-10 membered heteroaryl;
- R3e at each occurrence is independently selected from —H, —C1-6alkyl, —S(O)2R3f or —C(O)R3f, wherein R3f is independently C1-6alkyl or C3-6cycloalkyl;
- and
- r is an integer of 0, 1 or 2.
17 more elements
Dependencies are inferred from the claim text.