| abstract |
The present invention provides novel 2,3-dihydrobenzazine compounds of the formula (I), the pharmaceutically acceptable salts thereof, the N-oxides thereof and the pharmaceutically acceptable salts of said N-oxides. Formula (I) X is O or S(=O) n with n being 0, 1 or 2; R 1 is phenyl or C-bound monocyclic 5- or 6-membered heteroaryl, wherein phenyl and monocyclic 5- or 6-membered heteroaryl are unsubstituted or carry 1, 2 or 3 radicals R 1a which are identical or different; R 1a is selected from the group consisting of halogen, cyano, NO 2 , NH 2 , OH, SH, C 1 -C 10 -alkyl, C 2 -C 10 -alkenyl, C 2 -C 10 -alkynyl, C 1 -C 6 -alkoxy, C 1 -C 6 -alkylthio, hydroxy-C 1 -C 6 -alkyl, C 1 -C 4 -alkoxy-C 1 -C 4 -alkyl, fluorinated C 1 -C 2 -alkyl, SF 5 , fluorinated C 1 -C 2 -alkoxy, C(O)R 3 , NR 4 R 5 , N(OR 6 )R 7 and C(O)OR 8 , or two radicals R 1a , which are bound to adjacent carbon atoms, may also form a bridging moiety O-Alk-O, wherein AIk is selected from CH 2 , CH 2 CH 2 , CHF and CF 2 ; R 2 is phenyl or C- or N-bound monocyclic 5- or 6-membered heteroaryl, wherein phenyl and monocyclic 5- or 6-membered heteroaryl carry a CN radical and may additionally carry 1, 2 or 3 radicals R 2a which are identical or different; R 2a is selected from the group consisting of halogen, cyano, NO 2 , NH 2 , OH, SH, C1-C 10 -alkyl, C 2 -C 10 -alkenyl, C 2 -C 10 -alkynyl, C 1 -C 6 -alkoxy, C 1 -C 6 -alkylthio, hydroxy-C 1 -C 6 -alkyl, C 1 -C 4 -alkoxy-C 1 -C 4 -alkyl, fluorinated C 1 -C 2 -alkyl, SF 5 , fluorinated C 1 -C 2 -alkoxy, C(O)R 3 , NR 4 R 5 , N(OR 6 )R 7 and C(O)OR 8 , or two radicals R 2a , which are bound to adjacent carbon atoms, may also form a bridging moiety O-Alk'-O, wherein AIk' is selected from CH 2 , CH 2 CH 2 , CHF and CF 2 ; and where R 3 to R 8 are as defined in the claims and the specification. The invention relates to use of these compounds in therapy, in particular in the therapy of a disease or disorder selected from the group consisting of inflammatory diseases, a hyperproliferative disease or disorders, a hypoxia related pathology and a disease characterized by pathophysiological hyper-vascularisation. |