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    Benzothiazocine and benzothiazonine derivatives and use
    11.
    发明授权
    Benzothiazocine and benzothiazonine derivatives and use 失效
    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

    Applicant: Yasunobu Sato ,  Kuniyuki Tomita ,  Shinsaku Kobayashi

    Inventor： Yasunobu Sato ,  Kuniyuki Tomita ,  Shinsaku Kobayashi

    IPC: C07D281/00 ,  C07D281/18 ,  A61K31/395 ,  A61K31/55 ,  C07D281/10

    CPC classification number: C07D281/00 ,  C07D281/18 ,  Y10S514/927

    Abstract: 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.

    Abstract translation: 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。

    Higher polyalkenyl fatty acids and esters
    12.
    发明授权
    Higher polyalkenyl fatty acids and esters 失效
    高聚烯基脂肪酸和酯

    公开(公告)号：US4199519A

    公开(公告)日：1980-04-22

    申请号：US938356

    申请日：1978-08-31

    Applicant: Hiroshi Mishima ,  Akira Ogiso ,  Shinsaku Kobayashi

    Inventor： Hiroshi Mishima ,  Akira Ogiso ,  Shinsaku Kobayashi

    IPC: C07C59/42 ,  C07D295/13 ,  C07D295/185 ,  C07D317/58 ,  C07C57/02 ,  C07C69/52

    CPC classification number: C07D295/185 ,  C07C45/68 ,  C07C59/42 ,  C07D295/13 ,  C07D317/58 ,  Y10S514/927

    Abstract: Polyprenyl derivatives having the formula ##STR1## [wherein A and B individually represent a group of the formula --CH.sub.2 OR.sup.1 (wherein R.sup.1 is hydrogen atom, an alkyl group having an intervening hetero atom in the carbon chain, carboxyl group on its salt or an aliphatic acyl group optionally having an intervening hetero atom in the carbon chain, an aromatic acyl group, a heterocyclic acyl group, an araliphatic acyl group, a heterocyclic aliphatic acyl group or a radical of an inorganic acid or its salt) or where one of A and B represents the group --CH.sub.2 OR.sup.1, the other represents a group of the formula --COOR.sup.2 (wherein R.sup.2 represents hydrogen atom, a metal atom capable of forming a salt, an organic base or an akyl group), a group of the formula ##STR2## or a group of the formula ##STR3## (wherein R.sup.3 and R.sup.4 may be the same or different and each represents hydrogen atom, an alkyl group optionally having a heterocyclic substituent, an aryl group or an aralkyl group or R.sup.3 and R.sup.4 may jointly form a ring optionally containing other hetero ring atom) and n is an integer of 0 to 4 inclusive, provided that when both A and B are the group --CH.sub.2 OR.sup.1, either of the R.sup.1 represents an alkyl group having an intervening hetero atom, carboxyl group or its salt, an aliphatic acyl group having an intervening hetero atom in the carbon chain, a heterocyclic acyl group, a heterocyclic aliphatic acyl group or a radical of an inorganic acid or its salt]. These derivatives are useful as medicines for treating peptic ulcer.

    Abstract translation: 具有式的聚丙烯衍生物[其中A和B各自表示式-CH 2 OR 1的基团（其中R 1是氢原子，在碳链中具有中间杂原子的烷基，其盐上的羧基或脂族 任选在碳链中具有中间杂原子的酰基，芳族酰基，杂环酰基，芳脂酰基，杂环脂族酰基或无机酸或其盐的基团），或者其中A和 B表示基团-CH 2 OR 1，另一个表示式-COOR 2（其中R 2表示氢原子，能够形成盐的金属原子，有机碱或烷基）的基团，式 或式（IMA）（其中R 3和R 4可以相同或不同，各自表示氢原子，任选具有杂环取代基的烷基，芳基或芳烷基或R 3和R 4可以共同形成 戒指 任选地含有其它杂环原子），n为0〜4的整数，条件是当A和B都为基团-CH 2 OR 1时，R 1表示具有杂原子的烷基，羧基或其盐 ，在碳链中具有插入杂原子的脂族酰基，杂环酰基，杂环脂族酰基或无机酸或其盐的基团]。 这些衍生物可用作治疗消化性溃疡的药物。

    9-Oxo-11.alpha.-methyl-15.EPSILON.-hyroxyprost-13(trans)-enoic acid derivatives and process for the preparaion thereof
    16.
    发明授权
    9-Oxo-11.alpha.-methyl-15.EPSILON.-hyroxyprost-13(trans)-enoic acid derivatives and process for the preparaion thereof 失效
    9-氧代-11 {60-甲基-15 {69-羟基霜霉素-13（反） - 烯酸衍生物及其制备方法

    公开(公告)号：US3996263A

    公开(公告)日：1976-12-07

    申请号：US574376

    申请日：1975-05-05

    Applicant: Kiyoshi Sakai ,  Takashi Yusa ,  Junya Ide ,  Mitsuo Yamazaki ,  Shinsaku Kobayashi

    Inventor： Kiyoshi Sakai ,  Takashi Yusa ,  Junya Ide ,  Mitsuo Yamazaki ,  Shinsaku Kobayashi

    IPC: C07C405/00 ,  C07D307/93 ,  C07D307/935 ,  C07D317/72 ,  C07C177/00

    CPC classification number: C07D307/935 ,  C07C405/00 ,  C07D307/93 ,  C07D317/72

    Abstract: Prostanoic acid derivatives having the formula ##STR1## wherein A represents an alkylene group having from 4 to 8 carbon atoms, R.sup.1 represents an alkyl group having from one to 5 carbon atoms, R.sup.2 and R.sup.3 may be the same or different and each represents hydrogen atom or an alkyl group having from one to 4 carbon atoms and R.sup.4 represents hydrogen atom or an alkyl group having from one to 4 carbon atoms and the pharmaceutically acceptable salts thereof and also relates to a process for the preparation thereof.The compounds are useful as anti-ulcerogenic agents and may be prepared by reducing a compound having the formula ##STR2## wherein A, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same above and Z represents a carbonyl-protecting group to give a compound having the formula ##STR3## wherein A, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Z are the same as above and removing the carbonyl-protecting group from the latter compound.

    Abstract translation: 具有式的前列生酸衍生物，其中A表示具有4至8个碳原子的亚烷基，R 1表示具有1至5个碳原子的烷基，R 2和R 3可以相同或不同，各自表示氢原子 或具有1至4个碳原子的烷基和R 4表示氢原子或具有1至4个碳原子的烷基及其药学上可接受的盐，并且涉及其制备方法。

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