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    Polyprenyl derivatives
    1.
    发明授权
    Polyprenyl derivatives 失效
    聚丙烯衍生物

    公开(公告)号：US4260551A

    公开(公告)日：1981-04-07

    申请号：US11514

    申请日：1979-02-12

    申请人： Hiroshi Mishima ,  Akira Ogiso ,  Shinsaku Kobayashi

    发明人： Hiroshi Mishima ,  Akira Ogiso ,  Shinsaku Kobayashi

    IPC分类号： C07C43/00 ,  C07C69/007 ,  C07C69/767 ,  C09F5/08 ,  C07C69/76

    CPC分类号： C07C69/618 ,  C07C45/68 ,  C07C69/007 ,  C07C69/16 ,  C07C69/18 ,  C07C69/28 ,  C07C69/56 ,  C07C69/76 ,  C07C69/78

    摘要： Polyprenyl derivatives having the formula ##STR1## in which R.sup.1 and R.sup.2 may be the same or different and each represents hydrogen atom, hydroxyl group, an alkoxy group having 1-8 carbon atoms, an aliphatic acyloxy group having 2-18 carbon atoms, an aromatic acyloxy group or an araliphatic acyloxy group having 2-3 carbon atoms in the aliphatic acyl moiety, R.sup.3 represents hydrogen atom, an alkyl group having 1-8 carbon atoms, an aliphatic acyl group having 2-18 carbon atoms, an aromatic acyl group or an araliphatic acyl group having 2-3 carbon atoms in the aliphatic acyl moiety, n is an integer of 1-4 and, when n is an integer of 2-4, R.sup.2 's may be the same or different; provided that, when n is 1 or 2, at least one of R.sup.1 and R.sup.2 's is hydroxyl group, an alkoxy group, an aliphatic acyloxy group, an aromatic acyloxy group or an araliphatic acyloxy group. These derivatives are useful as medicines for treating peptic ulcer.

    摘要翻译： 其中R 1和R 2可以相同或不同并且各自表示氢原子，羟基，具有1-8个碳原子的烷氧基，具有2-羟基的脂肪族酰氧基， 18个碳原子，芳香族酰氧基或脂肪族酰基部分中具有2-3个碳原子的芳脂肪酰氧基，R3表示氢原子，具有1-8个碳原子的烷基，具有2-18个碳原子的脂族酰基 芳香族酰基或脂肪族酰基部分具有2-3个碳原子的芳脂酰基，n为1-4的整数，当n为2-4的整数时，R 2可以相同或不同， 条件是当n为1或2时，R 1和R 2中的至少一个为羟基，烷氧基，脂族酰氧基，芳香族酰氧基或芳脂族酰氧基。 这些衍生物可用作治疗消化性溃疡的药物。

    Polyprenyl derivatives
    2.
    发明授权
    Polyprenyl derivatives 失效
    聚丙烯衍生物

    公开(公告)号：US4192953A

    公开(公告)日：1980-03-11

    申请号：US1162

    申请日：1979-01-04

    申请人： Hiroshi Mishima ,  Akira Ogiso ,  Shinsaku Kobayashi

    发明人： Hiroshi Mishima ,  Akira Ogiso ,  Shinsaku Kobayashi

    IPC分类号： C07C43/00 ,  C07C69/007 ,  A61K31/07 ,  A61K31/08 ,  C07C43/02

    CPC分类号： C07C41/16 ,  C07C33/02 ,  C07C43/15 ,  C07C45/68 ,  C07C69/007 ,  C07C69/16 ,  C07C69/28 ,  C07C69/56 ,  C07C69/618 ,  C07C69/78 ,  Y10S514/926 ,  Y10S514/927

    摘要： Polyprenyl derivatives having the formula ##STR1## in which R.sup.1 and R.sup.2 may be the same or different and each represents hydrogen atom, hydroxyl group, an alkoxy group having 1-8 carbon atoms, an aliphatic acyloxy group having 2-18 carbon atoms, an aromatic acyloxy group or an araliphatic acyloxy group having 2-3 carbon atoms in the aliphatic acyl moiety, R.sup.3 represents hydrogen atom, an alkyl group having 1-8 carbon atoms, an aliphatic acyl group having 2-18 carbon atoms, an aromatic acyl group or an araliphatic acyl group having 2-3 carbon atoms in the aliphatic acyl moiety, n is an integer of 1-4 and, when n is an interger of 2-4, R.sup.2 's may be the same or different; provided that, when n is 1 or 2, at least one of R.sup.2 and R.sup.2 's is hydroxyl group, an alkoxy group, an aliphatic acyloxy group, an aromatic acyloxy group or an araliphatic acyloxy group. These derivatives are useful as medicines for treating peptic ulcer.

    摘要翻译： 其中R 1和R 2可以相同或不同并且各自表示氢原子，羟基，具有1-8个碳原子的烷氧基，具有2-羟基的脂肪族酰氧基， 18个碳原子，芳香族酰氧基或脂肪族酰基部分中具有2-3个碳原子的芳脂肪酰氧基，R3表示氢原子，具有1-8个碳原子的烷基，具有2-18个碳原子的脂族酰基 芳香酰基或脂肪族酰基部分具有2-3个碳原子的芳脂酰基，n为1-4的整数，当n为2-4的整数时，R 2可以相同或不同; 条件是当n为1或2时，R 2和R 2中的至少一个为羟基，烷氧基，脂族酰氧基，芳香族酰氧基或芳脂族酰氧基。 这些衍生物可用作治疗消化性溃疡的药物。

    Polyprenyl derivatives
    3.
    发明授权
    Polyprenyl derivatives 失效
    聚丙烯衍生物

    公开(公告)号：US4059641A

    公开(公告)日：1977-11-22

    申请号：US633097

    申请日：1975-11-18

    申请人： Hiroshi Mishima ,  Akira Ogiso ,  Shinsaku Kobayashi

    发明人： Hiroshi Mishima ,  Akira Ogiso ,  Shinsaku Kobayashi

    IPC分类号： C07C69/025 ,  A61K31/045 ,  A61K31/075 ,  A61K31/215 ,  A61P1/04 ,  C07C27/00 ,  C07C33/02 ,  C07C41/00 ,  C07C43/00 ,  C07C43/14 ,  C07C43/178 ,  C07C67/00 ,  C07C69/007

    CPC分类号： C07C45/64 ,  C07C33/02 ,  C07C41/16 ,  C07C43/15 ,  C07C45/68 ,  C07C69/007 ,  C07C69/16 ,  C07C69/18 ,  C07C69/28 ,  C07C69/56 ,  C07C69/614 ,  C07C69/618 ,  C07C69/76 ,  C07C69/78 ,  C07C69/92 ,  Y10S514/927

    摘要： Polyprenyl derivatives having the formula ##STR1## in which R.sup.1 and R.sup.2 may be the same or different and each represents hydrogen atom, hydroxyl group, an alkoxy group having 1-8 carbon atoms, an aliphatic acyloxy group having 2-18 carbon atoms, an aromatic acyloxy group or an araliphatic acyloxy group having 2-3 carbon atoms in the aliphatic acyl moiety, R.sup.3 represents hydrogen atom, an alkyl group having 1-8 carbon atoms, an aliphatic acyl group having 2-18 carbon atoms, an aromatic acyl group or an araliphatic acyl group having 2-3 carbon atoms in the aliphatic acyl moiety, n is an integer of 1-4 and, when n is an integer of 2-4, R.sup.2 's may be the same or different; provided that, when n is 1 or 2, at least one of R.sup.1 and R.sup.2 's is hydroxyl group, an alkoxy group, an aliphatic acyloxy group, an aromatic acyloxy group or an araliphatic acyloxy group. These derivatives are useful as medicines for treating peptic ulcer.

    摘要翻译： 其中R 1和R 2可以相同或不同并且各自代表氢原子，羟基，具有1-8个碳原子的烷氧基，具有2-取代基的脂肪族酰氧基的具有式 + tr 的聚丙烯基衍生物， 18个碳原子，芳香族酰氧基或脂肪族酰基部分中具有2-3个碳原子的芳脂肪酰氧基，R3表示氢原子，具有1-8个碳原子的烷基，具有2-18个碳原子的脂族酰基 芳香族酰基或脂肪族酰基部分具有2-3个碳原子的芳脂酰基，n为1-4的整数，当n为2-4的整数时，R 2可以相同或不同， 条件是当n为1或2时，R 1和R 2中的至少一个为羟基，烷氧基，脂族酰氧基，芳香族酰氧基或芳脂族酰氧基。 这些衍生物可用作治疗消化性溃疡的药物。

    Higher polyalkenyl fatty acids and esters
    4.
    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

    申请人： Hiroshi Mishima ,  Akira Ogiso ,  Shinsaku Kobayashi

    发明人： Hiroshi Mishima ,  Akira Ogiso ,  Shinsaku Kobayashi

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

    CPC分类号： C07D295/185 ,  C07C45/68 ,  C07C59/42 ,  C07D295/13 ,  C07D317/58 ,  Y10S514/927

    摘要： 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.

    摘要翻译： 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。

    Carbacyclin derivatives
    8.
    发明授权
    Carbacyclin derivatives 失效
    卡巴环素衍生物

    公开(公告)号：US4757087A

    公开(公告)日：1988-07-12

    申请号：US840920

    申请日：1986-03-18

    申请人： Koichi Kojima ,  Shinsaku Kobayashi

    发明人： Koichi Kojima ,  Shinsaku Kobayashi

    IPC分类号： A61K31/557 ,  A61P1/04 ,  C07C59/46 ,  C07C69/732 ,  C07C405/00 ,  C07H15/00 ,  C07C62/32 ,  A61K31/21

    CPC分类号： C07C405/0083 ,  Y02P20/55

    摘要： Carbacyclin derivatives with anti-ulcer activity comprise compounds of the general formula (I): ##STR1## (wherein R.sup.1 is selected from the group consisting of a hydrogen atom and an alkyl group having from 1 to 10 carbon atoms; R.sup.2 is selected from the group consisting of a hydrogen atom and a methyl group; and R.sup.3 is selected from the group consisting of a 3-butenyl group, a 4-pentenyl group and a 5-methyl-4-hexenyl group), and pharmaceutically acceptable salts thereof.

    摘要翻译： 具有抗溃疡活性的卡巴环素衍生物包括通式（I）的化合物：其中R 1选自氢原子和具有1至10个碳原子的烷基; R 2是 选自氢原子和甲基; R3选自3-丁烯基，4-戊烯基和5-甲基-4-己烯基）和药学上可接受的盐 其中。

    9-OXO-15 .xi.-HYDROXY-20-ALKYLIDENEPROST-13(TRANS)-ENOIC ACID DERIVATIVES
    9.
    发明授权
    9-OXO-15 .xi.-HYDROXY-20-ALKYLIDENEPROST-13(TRANS)-ENOIC ACID DERIVATIVES 失效
    9-OXO-15 {86-羟基-20-烷基硫代-13（反式） - 酸性衍生物

    公开(公告)号：US4064351A

    公开(公告)日：1977-12-20

    申请号：US753277

    申请日：1976-12-22

    申请人： Kiyoshi Sakai ,  Koichi Kojima ,  Junya Ide ,  Shinsaku Kobayashi

    发明人： Kiyoshi Sakai ,  Koichi Kojima ,  Junya Ide ,  Shinsaku Kobayashi

    IPC分类号： C07C405/00 ,  C07F9/40 ,  C07C177/00

    CPC分类号： C07C405/00 ,  C07F9/4015

    摘要： Prostanoic acid derivatives having the formula ##STR1## wherein A represents ethylene group or cis-vinylene group, R.sup.1 and R.sup.2 may be the same or different and each represents hydrogen atom or an alkyl group having 1-3 carbon atoms, R.sup.3 and R.sup.4 may be the same or different and each represents an alkyl group having 1-3 carbon atoms and R.sup.5 represents hydrogen atom or hydroxyl group and the pharmaceutically acceptable salts thereof and a process for the preparation thereof.The compounds are useful as anti-ulcerogenic or bronchodilating agents and may be prepared by oxidizing 9.xi.-hydroxy-15.xi.-protected-hydroxy-20-alkylideneprost-13(trans)-enoic acid derivatives.

    摘要翻译： 具有式“IMAGE”的前列腺酸衍生物，其中A表示亚乙基或顺式亚乙烯基，R 1和R 2可以相同或不同，各自表示氢原子或具有1-3个碳原子的烷基，R 3和R 4可以是 相同或不同，各自表示具有1-3个碳原子的烷基，R 5表示氢原子或羟基及其药学上可接受的盐及其制备方法。

    Benzothiazocine and benzothiazonine derivatives and use
    10.
    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

    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。