发明名称 Tumour inhibiting di-heterocyclic azines - contg. one thiazolidine and one per hydro-thiaz(ep)ine ring
摘要 <p>Azines of formula (I) are new: (one of R1 and R2 is 3-6C alkenyl or 2-propynyl; the other is a similar gp. or is =6C alkyl or H; R3 and R4 are H or CH3; A is CH2, CH(CH3), CH2CH2 or propylene; one of m and n is 1 and the other is 0). They are prepd. e.g. by reacting a 2-thiosemicarbazide of a thiazine or thiazephine-2,4-dione with HOCHR4-(A)n-COOX (X = H or =6 alkyl) as their reactive esters. (I) inhibit the growth of tumours, e.g. transplanted Walker carcinoma or dimethylbenzoanthracene-induced mammary gland carcinoma in rats. They are administered at 1-150mg/kg/day in usual parenteral, oral or rectal formulations. In an example, a typical cpd., the 2,2'-azine of 3-allyl-5-methyl-2,4-thiazolidinedione and of dihydro-2H-1,3-thiazine-2,4(3H)dione, was prepd. by reacting dihydro-2H-1,3-thiazine-2,4(3H)dione-2-(4-alkyl-3-thiosemicarbazo- ne) with 2-bromopropionic acid.</p>
申请公布号 DE2632747(A1) 申请公布日期 1977.02.24
申请号 DE19762632747 申请日期 1976.07.21
申请人 CIBA-GEIGY AG 发明人 STORNI,ANGELO,DR.;MEISELS,ALEX,DR.
分类号 A61K31/54;C07D277/54;C07D279/06;C07D281/02;C07D417/12;(IPC1-7):C07D417/12 主分类号 A61K31/54
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