abstract |
FIELD: pharmaceuticals. n SUBSTANCE: invention relates to novel compounds of formula (I), or a pharmaceutically acceptable salt thereof, or a stereoisomer having the properties of a Bruton (Btk) tyrosine kinase activity inhibitor. Compounds can be used to treat autoimmune diseases or conditions, heteroimmune diseases or conditions, including lymphoma, in the treatment of β-cell proliferative disorders, in the treatment of inflammatory diseases, such as asthma, inflammatory bowel disease, appendicitis, bronchitis, etc. In general formula (I) n n n n L a is -OCH 2 -, -N(R 21 )C(O)-, -C(O)N(R 21 )- or -O-; Ar is a substituted or unsubstituted aryl, selected from phenyl, where the substituent can be selected from halogen, hydroxy, C 1 -C 6 alkoxy or C 1 -C 6 alkyl; R 3 is Y is a group selected from among C 3 -C 6 cycloalkyl, phenyl, optionally substituted C 1 -C 4 alkyl or C 1 -C 4 alkoxy; and bicyclic heteroaryl selected from a benzene ring fused to a 6-membered heterocycloalkyl comprising nitrogen and oxygen as heteroatoms; Z is C(=O) or N(R 21 )C(=O); R 21 is H or unsubstituted C 1 -C 6 alkyl; R 24 , is independently, unsubstituted C 1 -C 4 alkyl; n is 0 or 1; p is 0–2; R 6 is H or L-J-W; R 7 and R 8 , independently, is H or L-J-W; L and J, is each independently a bond, or unsubstituted C 1 -C 6 alkylene; W is H, halogen, -CN or NR 25 R 26 ; R 25 and R 26 , is each independently H, unsubstituted C 1 -C 6 alkyl, unsubstituted C 3 -C 6 cycloalkyl, unsubstituted C 1 -C 6 heteroalkyl containing oxygen as a heteroatom, unsubstituted C 5 -C 7 heterocycloalkyl containing oxygen as a heteroatom, or substituted or unsubstituted C 3- C 12 heteroaryl containing 1 to 2 nitrogen atoms as heteroatoms, where the substituent is selected from C 1 -C 4 alkyl. n EFFECT: invention has the properties of a Bruton tyrosine kinase activity inhibitor (Btk). n 15 cl, 78 ex, 2 tbl |