申请人:Sankyo Company Limited
公开号:US04328238A1
公开(公告)日:1982-05-04
Benzothiazocine and benzothiazonine derivatives of formula (I): ##STR1## in which: R.sup.1, R.sup.2 and R.sup.3 are the same or different and each represents a hydrogen atom or an alkyl group; X.sup.1 and X.sup.2 are the same or different and each represents a hydrogen atom, an alkyl group, an alkoxy group, an alkanesulphinyl group, an alkanesulphonyl group, a halogen atom, a trifluoromethyl group, a nitro group or a cyano group; n is 1 or 2; and m is 0 or 1 (excluding those compounds wherein: R.sup.1, R.sup.2, R.sup.3, X.sup.1 and X.sup.2 all represent hydrogen atoms; n is 1 and m is 0; and wherein: R.sup.1 and R.sup.2 both represent hydrogen atoms; R.sup.3 represents a hydrogen atom or a methyl group; X.sup.1 represents a chlorine atom at the 9-position; X.sup.2 represents a hydrogen atom; n is 1; and m is 0) and acid addition salts thereof are novel compounds which have been found to suppress gastric secretions and are thus useful in the treatment and prevention of gastric ulcers. Compounds in which m is 0 may be prepared by reacting a corresponding .omega.-substituted thioalkylaniline derivative with a halogen or an active halogen compound and then condensing the product and, if necessary, introducing an alkyl group at the 1-position. Compounds in which m is 1 may be prepared by oxidizing the corresponding compound wherein m is 0.
苯并噻唑啉和苯并噻唑啉衍生物的化学式(I)如下:##STR1##其中:R.sup.1,R.sup.2和R.sup.3相同或不同,每个代表氢原子或烷基;X.sup.1和X.sup.2相同或不同,每个代表氢原子、烷基、烷氧基、烷磺酰基、烷磺基、卤素原子、三氟甲基、硝基或氰基;n为1或2;m为0或1(不包括那些化合物,其中:R.sup.1,R.sup.2,R.sup.3,X.sup.1和X.sup.2都代表氢原子;n为1且m为0;以及其中:R.sup.1和R.sup.2都代表氢原子;R.sup.3代表氢原子或甲基;X.sup.1代表9位的氯原子;X.sup.2代表氢原子;n为1;m为0),以及其酸盐是新颖的化合物,已发现能抑制胃酸分泌,因此在胃溃疡的治疗和预防中有用。其中m为0的化合物可以通过将相应的.ω.-取代硫代烷基苯胺衍生物与卤素或活性卤素化合物反应,然后缩合产物,并在必要时在1位引入烷基来制备。其中m为1的化合物可以通过氧化相应的m为0的化合物制备。