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    Methylmethioninesulfonium compounds, process for their preparation, and pharmaceutical compositions containing them
    4.
    发明授权
    Methylmethioninesulfonium compounds, process for their preparation, and pharmaceutical compositions containing them 失效
    甲基亚氨基锍化合物，其制备方法和含有它们的药物组合物

    公开(公告)号：US4216225A

    公开(公告)日：1980-08-05

    申请号：US906567

    申请日：1978-05-16

    申请人： Masami Shiratsuchi ,  Kiyoshi Kawamura ,  Hisashi Kunieda ,  Naoki Machida ,  Toshihiro Akashi ,  Masahiko Nagakura

    发明人： Masami Shiratsuchi ,  Kiyoshi Kawamura ,  Hisashi Kunieda ,  Naoki Machida ,  Toshihiro Akashi ,  Masahiko Nagakura

    IPC分类号： A61K31/195 ,  A61K31/16 ,  A61K31/22 ,  A61P1/04 ,  C07C67/00 ,  C07C325/00 ,  C07C381/12 ,  C07D213/82 ,  A61K31/55 ,  A61K31/215

    CPC分类号： C07D213/82

    摘要： Methylmethioninesulfonium compounds of the formula ##STR1## wherein X.crclbar. represents an anion;R.sup.1 represents a hydrogen atom or an acyl group of the formula -COR.sup.3 in which R.sup.3 represents an alkyl group with 1 to 20 carbon atoms, the group --CH.sub.2).sub.2 COOH or the group ##STR2## in which Z represents a direct bond or a methylene or vinylene linkage, Y represents C or N, R.sup.4 represents a member selected from the class consisting of a hydrogen atom, lower alkyl groups, lower alkoxy groups, di-lower-alkylamino groups and a sulfamoyl group, n is a number of 1 to 3, and two or more R.sup.4 groups may be identical or different; andR.sup.2 represents the group --COOR.sup.5 in which R.sup.5 represents a hydrogen atom, an alkyl group with 1 to 5 carbon atoms or a metal- or metal complex-forming moiety, or the group ##STR3## in which R.sup.6 groups may be identical or different, and each represent a hydrogen atom or an alkyl group with 1 to 5 carbon atoms, with the proviso that when R.sup.1 represents a hydrogen atom, R.sup.2 is not --COOH; when R.sup.1 represents a hydrogen atom and R.sup.2 represents --CONH.sub.2, X.crclbar. is not Cl.crclbar.; and when R.sup.1 is --COCH.sub.3 and R.sup.2 is --COOCH.sub.3, X.crclbar. is not I.crclbar..The compounds can be easily prepared from methionine as a starting material by a combination of known unit reactions such as methylsulfonium-forming reaction, acylation, amidation, esterification and metal salt-forming reaction. These compounds are especially useful for treating ulcers.

    摘要翻译： 其中X（ - ）表示阴离子的式“IMAGE”的甲基甲硫氨onium化合物; R 1表示氢原子或式-COR 3的酰基，其中R 3表示具有1至20个碳原子的烷基，基团-CH 2）2 COOH或其中Z表示直接键或基团 亚甲基或亚乙烯基，Y表示C或N，R4表示选自氢原子，低级烷基，低级烷氧基，二低级烷基氨基和氨磺酰基的成员，n为1 至3个，并且两个或更多个R 4基团可以相同或不同; 并且R 2表示其中R 5表示氢原子，具有1至5个碳原子的烷基或金属或金属络合物形成部分的基团-COOR 5或其中R6基团可以相同或不同的基团 并且各自表示氢原子或具有1至5个碳原子的烷基，条件是当R 1表示氢原子时，R 2不是-COOH; 当R 1表示氢原子且R 2表示-CONH 2时，X（ - ）不是Cl（ - ）; 当R1是-COCH3且R2是-COOCH3时，X（ - ）不是I（ - ）。 通过已知的单元反应如甲基锍形成反应，酰化，酰胺化，酯化和金属盐形成反应的组合，可以容易地从甲硫氨酸作为原料制备化合物。 这些化合物特别适用于治疗溃疡。

    Tetrahydroxanthone derivatives
    5.
    发明授权
    Tetrahydroxanthone derivatives 失效
    四氢呫吨酮衍生物

    公开(公告)号：US4290954A

    公开(公告)日：1981-09-22

    申请号：US89403

    申请日：1979-10-30

    申请人： Kazuhiro Onogi ,  Hisashi Kunieda ,  Kiyoshi Kawamura ,  Masami Shiratsuchi ,  Masahiko Nagakura ,  Naoki Machida, deceased ,  by Takayasu Miwa, heir

    发明人： Kazuhiro Onogi ,  Hisashi Kunieda ,  Kiyoshi Kawamura ,  Masami Shiratsuchi ,  Masahiko Nagakura ,  Naoki Machida, deceased ,  by Takayasu Miwa, heir

    IPC分类号： A61K31/35 ,  A61K31/352 ,  A61K31/41 ,  A61K31/495 ,  A61K31/535 ,  A61P25/04 ,  A61P29/00 ,  A61P37/08 ,  C07D311/86 ,  C07D405/04 ,  C07D405/12 ,  C07D405/10 ,  C07D413/10

    CPC分类号： C07D311/86

    摘要： A tetrahydroxanthone derivative represented by the general formula: ##STR1## wherein R is a hydrogen atom, a hydroxyl, cyano, lower alkyl, lower alkoxy, lower acyloxy, benzoyloxy or tetrazolyl group, or ##STR2## (R.sub.3 is a hydrogen atom, R.sub.4 is a hydrogen atom, a phenyl group which may be optionally substituted, or a tetrazolyl group; or R.sub.3 and R.sub.4 commonly form a ring together with the adjacent nitrogen atom and another nitrogen atom or an oxygen atom); R.sub.1 is a hydrogen or halogen atom, a lower alkyl, cyano, carboxyl or tetrazolyl group, or ##STR3## (R.sub.5 is a hydrogen atom, R.sub.6 is a phenyl group which may be optionally substituted, or a tetrazolyl group; or R.sub.5 and R.sub.6 commonly form a ring together with the adjacent nitrogen atom and an oxygen atom); and R.sub.2 is a hydrogen or halogen atom, or a lower alkyl group; with the proviso that neither R nor R.sub.1 is a hydrogen atom; when R is --CONH.sub.2, R.sub.1 and R.sub.2 are not respectively a hydrogen atom nor a hydrogen or halogen atom, or a lower alkyl group; and R.sub.2 and R.sub.1 are not respectively a hydrogen atom nor a halogen atom or a lower alkyl group. Exhibits anti-allergic, anti-inflammatory, analgesic, inhibitory and asthma-treating activities.

    摘要翻译： 其中R是氢原子，羟基，氰基，低级烷基，低级烷氧基，低级酰氧基，苯甲酰氧基或四唑基，或者是（R 3是氢原子，R 4 是氢原子，可以被任意取代的苯基或四唑基;或者R3和R4通常与相邻的氮原子和另一个氮原子或氧原子一起形成环）; R 1是氢或卤素原子，低级烷基，氰基，羧基或四唑基，或者R 5是氢原子，R 6是任选被取代的苯基或四唑基;或R 5和R 6 通常与相邻的氮原子和氧原子一起形成环）; 并且R 2是氢或卤原子或低级烷基; 条件是R和R1都不是氢原子; 当R为-CONH 2时，R 1和R 2不分别为氢原子或氢或卤素原子或低级烷基; R2和R1不分别为氢原子或卤素原子或低级烷基。 展示抗过敏，抗炎，镇痛，抑制和哮喘治疗活动。

    Isoindoline derivatives and the acid addition salts thereof and process for the preparation of same
    8.
    发明授权
    Isoindoline derivatives and the acid addition salts thereof and process for the preparation of same 失效
    异二氢吲哚衍生物及其酸加成盐及其制备方法

    公开(公告)号：US4115398A

    公开(公告)日：1978-09-19

    申请号：US757028

    申请日：1977-01-05

    申请人： Koji Nakamura ,  Haruo Otaki ,  Yutaka Yamamoto ,  Noboru Shimizu ,  Kiyoshi Kawamura ,  Seiichi Sato

    发明人： Koji Nakamura ,  Haruo Otaki ,  Yutaka Yamamoto ,  Noboru Shimizu ,  Kiyoshi Kawamura ,  Seiichi Sato

    IPC分类号： C07D209/44

    CPC分类号： C07D209/44

    摘要： Isoindoline derivatives of the formula ##STR1## and the pharmaceutically acceptable acid addition salts thereof, wherein R represents a moiety selected from the group consisting of hydrogen, halogen, lower alkyl, lower alkoxy, nitro, hydroxy and hydroxy lower alkyl, and n is a positive number from 1 to 3, which R's may be the same or different when n is 2 or 3, and when n is 2, the two R's may be joined to the carbon atom vicinal to the phenyl ring to which the two R's are joined and may taken together form lower alkylenedioxy and the group ##STR2## and R.sub.1 is a member of the group consisting of hydrogen and lower alkyl.The compounds of this invention can be readily prepared by reacting a compound of the formula ##STR3## wherein R represents, in addition to the above defined, alkoxycarbonyloxy; R.sub.1 and n are as defined above; and X is halogen or the groups --O--SO.sub.2 --Y where Y is either lower alkyl or aryl, with isoindoline of the formula ##STR4## or a minemal acid salt thereof. The compounds are useful in such fields as, for example cardiovascular drugs.

    摘要翻译： 式（I）的异二氢吲哚衍生物及其药学上可接受的酸加成盐，其中R表示选自氢，卤素，低级烷基，低级烷氧基，硝基，羟基和羟基低级烷基的部分，和 n是1至3的正数，当n为2或3时，R可以相同或不同，当n为2时，两个R可以连接到苯环附近的碳原子上， R的连接可以一起形成低级亚烷基二氧基和基团，R 1是由氢和低级烷基组成的组的成员。