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US 12,448,382 B2Granted
Heterocyclic compounds for mediating tyrosine kinase 2 activity
AssigneeGuangzhou Innocare Pharma Tech Co., Ltd.
InventorsXiangyang Chen, Yucheng Pang
Life of this patent
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Abstract
Heterocyclic compounds shown in Formula (I) suitable for inhibiting or regulating the activity of Janus kinase (JAK), particularly tyrosine kinase 2 (TYK2). The compounds are useful for preventing and/or treating relevant JAK-mediated diseases, such as autoimmune diseases, inflammatory diseases, and cancers.
Claims21
A compound of Formula (I), or a pharmaceutical acceptable salt, stable isotope, stereoisomer thereof:
- wherein:
- R1 is aryl or heteroaryl, where one or more hydrogens of the aryl and heteroaryl are optionally substituted by D, halogen, cyano, —ORb, —NRbRc, —COORb, —C(O)Rb, —NRbC(O)Rc, —C(O)NRbRc, —S(O)2Rb, —S(O)2NRbRc, —S(O)(NRb)Rc, —P(O)(CH3)2, C1-6 alkyl, C3-6 cycloalkyl, 3- to 8-membered heterocyclyl or 5- to 6-membered heteroaryl;
- R2 is H, D or —NHRa;
- R3 is H, D, halogen, cyano, C1-6 alkyl, C3-6 cycloalkyl or OC1-6 alkyl, where one or more hydrogens of the alkyl and cycloalkyl are optionally substituted by D or F;
- R4 and R5 are independently selected from H, D, halogen, C1-6 alkyl or OC1-6 alkyl, where one or more hydrogens of the alkyl are optionally substituted by D or F;
- R6 and R7 are independently selected from H, D, cyano or C1-6 alkyl, where one or more hydrogens of the alkyl is optionally substituted by D or F, or R6 and R7 combine as oxo;
- L is a bond, C1-6 alkylene, —C(O)—, —C(O)O—, —C(O)N(Ra)—, —S(O)2— or —S(O)2N(Ra)—;
- A is H, C1-6 alkyl, C3-6 cycloalkyl, 3- to 8-membered heterocyclyl, aryl or heteroaryl, where one or more hydrogens of the alkyl, cycloalkyl, heterocyclyl, aryl and heteroaryl are optionally substituted by D, halogen, cyano, —ORd, —NRdRe, C1-6 alkyl, C3-6 cycloalkyl or 3- to 8-membered heterocyclyl;
- Ra is H, C1-6 alkyl or C3-6 cycloalkyl, where one or more hydrogens of the alkyl and cycloalkyl are optionally substituted by D or F;
- Rb and Rc are independently selected from H, C1-6 alkyl, C3-6 cycloalkyl or 3- to 8-membered heterocyclyl containing N and/or O, where one or more hydrogens of the alkyl, cycloalkyl and heterocyclyl are optionally further substituted by D, halogen, CN, —OH, —NH2, C1-6 alkyl and —OC1-6 alkyl, and
- Rd and Rc are independently selected from H, C1-6 alkyl, C3-6 cycloalkyl or 3- to 8-membered heterocyclyl, where one or more hydrogens of the alkyl, cycloalkyl and heterocyclyl are optionally further substituted by D or F.
8 more elements
Dependencies are inferred from the claim text.