| 摘要 |
1303081 Phthalazine-derived amines ASPRONICHOLAS Ltd 30 April 1970 [3 May 1969] 22678/69 Heading C2C The invention comprises compounds of formula and their pharmaceutically acceptable acid addition salts and quaternary ammonium derivatives, wherein R is aryl or aralkyl; R 1 and R 2 are each H, alkyl, hydroxyalkyl, haloalkyl or aralkyl; R 3 and R 4 are each (a) H, halogen, CN, OH, NO 2 ,NH 2 , alkylamino, CO 2 H,CONH 2 , alkyl, alkylcarboxyl, alkoxy, alkoxycarbonyl, hydroxyalkyl, haloalkyl, or (b) alkyl- or arylthio, -sulphinyl or -sulphonyl; aryl means Ph optionally substituted by the radicals listed under (a), or by alkyl-, phenyl- or alkylphenylthio, -sulphinyl or -sulphonyl, but R cannot be alkoxyphenyl when NR 1 R 2 is isobutylamino; and "alkyl" contains up to 12 carbon atom and includes unsaturated analogues. These compounds are prepared by reacting a corresponding 1-X-4-R-phthalazine (X=halogen or alkyl- or aryl-thio, sulphinyl- or -sulphonyl) with HNR 1 R 2 . Therapeutic compositions for oral, parenteral, or rectal administration, comprise compounds of the above formula, which have antiinflammatory, and in some cases immunosuppressive, activity. |
