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1. 发明授权

US4328238A Benzothiazocine and benzothiazonine derivatives and use 失效
标题翻译：苯并噻嗪和苯并噻嗪衍生物和用途
公开(公告)号：US4328238A
公开(公告)日：1982-05-04
申请号：US184096
申请日：1980-09-04
申请人： Yasunobu Sato , Kuniyuki Tomita , Shinsaku Kobayashi
发明人： Yasunobu Sato , Kuniyuki Tomita , Shinsaku Kobayashi
IPC分类号： C07D281/00 , C07D281/18 , A61K31/395 , A61K31/55 , C07D281/10
CPC分类号： C07D281/00 , C07D281/18 , Y10S514/927
摘要： 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; andm 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; andm 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.
摘要翻译：式（I）的苯并噻唑啉和苯并噻唑衍生物：其中：R 1，R 2和R 3相同或不同，各自表示氢原子或烷基; X1和X2相同或不同，分别表示氢原子，烷基，烷氧基，烷基亚磺酰基，链烷磺酰基，卤素原子，三氟甲基，硝基或氰基。 n为1或2; 并且m为0或1（不包括其中：R 1，R 2，R 3，X 1和X 2都表示氢原子的那些化合物; n为1且m为0;并且其中：R 1和R 2都表示氢原子; R 3表示氢原子或甲基; X1表示9位的氯原子; X2表示氢原子，n为1，m为0），其酸加成盐为抑制胃分泌物的新化合物，因此可用于治疗和预防胃溃疡。其中m为0的化合物可以通过使相应的ω-取代的硫代烷基苯胺衍生物与卤素或活性卤素化合物反应制备，然后使产物冷凝，如果需要，在1-位引入烷基。 m为1的化合物可以通过氧化其中m为0的相应化合物来制备。

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