| 摘要 |
The present invention describes new pyrrolo pyrimidine derivatives and pharmaceutically acceptable salts thereof which appear to interact with Bruton's tyrosine kinase (Btk). Accordingly, the novel pyrrolo pyrimidines may be effective in the treatment of autoimmune disorders, inflammatory diseases, allergic diseases, airway diseases, such as asthma and chronic obstructive pulmonary disease (COPD), transplant rejection, cancers e.g. of hematopoietic origin or solid tumors. |
| 主权项 |
1. A compound of formula (I) or a pharmaceutically acceptable salt thereof; wherein, R1 is hydrogen or C1-C6 alkyl optionally substituted by hydroxy; R2 is hydrogen or halogen; R3 is hydrogen or halogen; R4 is hydrogen, R5 is phenyl optionally substituted by halogen; SF5; NR6R7; hydroxy; C1-C6 alkoxy; C1-C6 alkenyl; C1-C6 alkyl carbonyl; C1-C6 alkyl optionally substituted by hydroxy, halogen, or C1-C6 alkoxy; or C3-C6 cycloalkyl optionally substituted by halogen, hydroxy, or C1-C6 alkyl optionally substituted by halogen; or R5 is a 4-14 membered mono- or bicyclic heterocyclyl or heteroaryl ring system comprising 1, 2 or 3 heteroatoms selected from N, S and O that ring being optionally substituted by halogen; hydroxy; C1-C6 alkoxy optionally substituted by hydroxy or halogen; or C1-C6 alkyl optionally substituted by hydroxy or halogen; or R4 and R5 together with the atoms to which they are bound form a piperidone ring, optionally comprising an annulated phenyl ring, any such ring being optionally substituted by C1-C6 alkyl, C1-C6 alkoxy, or C3-C6 cycloalkyl each of which substitution member may optionally be substituted by halogen or hydroxy; R6 and R7 are independently selected from hydrogen or C1-C6 alkyl; or R6 and R7 together with the nitrogen atom to which they are bound form a 4-8 membered saturated azacycloalkane ring, optionally substituted by halogen, hydroxy or C1-C6 alkyl; X is O, S(O)n wherein n is 0, 1 or 2, orwherein q is 2 or 3, and R10 is absent;
or X is CH or N; and R10 is hydrogen, hydroxy, —NR6R7, —CO—R11, —S(O)P—R12 wherein p is 1 or 2, R 11 is C1-C6 alkyl optionally substituted by hydroxy, cyano, halogen, carboxy or C1-C6 alkoxy carbonyloxy; or NR6R7; and R12 is C1-C6 alkyl or NR6R7. |
