| 摘要 |
Benzothiazine and benzothiadiazine derivatives (I) their isomers and salts are new. Benzothiazine and benzothiadiazine derivatives (I) their isomers and salts are new; R1 = aryl or heteroaryl; R2 = H, halogen, or OH; A = CR4R5 or NR4, or it is N and forms with the group -CHR3 a ring of formula (i); m = 1, 2, or 3; R3 = H, 1-6C alkyl or 3-7C cycloalkyl; R4 = H or 1-6C alkyl; R5 = H or halogen; Ra, Rb = H or alkyl. Provided that: (1) aryl groups are mono or bicyclic, at least one ring of which is aromatic, and may be substituted by one or more groups selected from halogens, alkyl (optionally substituted by OH), alkoxy, perhaloalkyl, perhaloalkoxy, alkoxycarbonyl, alkylthio, carboxy, acyl, OH, CN, NO2, NH2, mono- or dialkylamino, mono- or di-acylamino, aminocarbonyl, alkylaminocarbonyl, aminosulfonyl, alkylaminosulfonyl, mono- or dialkylsulfoylamino, mono- or di-(trifluoromethylsulfonyl) amino, PO(ORa)(ORb), benzyloxy, or phenyl (optionally substituted by one or more halogen, alkyl, perhaloalkyl, hydroxy or alkoxy groups); and (2) heteroaryl groups may have up to three heteroatoms (O, N, S), may be mono or bicyclic, at least one ring being aromatic, optionally substituted by one or more groups selected from halogens, alkyl, alkoxy, perhaloalkyl, alkoxycarbonyl, carboxy, acyl, perhaloalkoxy, OH, CN, NO2, NH2, mono- or dialkylamino, aminosulfonyl, alkylaminosulfonyl, and alkylsulfonylamino. An Independent claim is also included for the preparation of (I). |
