| 摘要 |
Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. In addition, reversible inhibitors of Btk are also described. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. |
| 主权项 |
1. A compound of Formula (I) having the structure: wherein: L1 is —N(R2)C(O)— or —C(O)N(R2)—; R1 is C3-C12heteroaryl, wherein C3-C12heteroaryl is optionally substituted with at least one R3; R2 is H or C1-C4alkyl; R3 is halogen, —CF3, —CN, —NO2, —OR6, —N(R6)(R7), substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C3-C6 cycloalkyl, or substituted or unsubstituted C1-C6heteroalkyl; R4 is H, substituted or unsubstituted C1-C6alkyl, substituted or unsubstituted C1-C6heteroalkyl, substituted or unsubstituted C3-C8cycloalkyl, or substituted or unsubstituted C2-C9heterocycloalkyl; R5 is substituted or unsubstituted C3-C8cycloalkyl, or substituted or unsubstituted C2-C9heterocycloalkyl; or R4 and R5 together with the nitrogen atom to which they are attached form a C2-C9heterocycloalkyl; R6 is H, substituted or unsubstituted C1-C6alkyl, or substituted or unsubstituted C1-C6heteroalkyl; R7 is H, substituted or unsubstituted C1-C6alkyl, or substituted or unsubstituted C1-C6heteroalkyl; R10 is halogen, substituted or unsubstituted C1-C6alkyl, or substituted or unsubstituted C1-C6alkoxy; m is 1 or 2; n is 0 or 1; and p is 0, 1, or 2; or a pharmaceutically acceptable salt, or pharmaceutically acceptable solvate thereof. |
