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    Thiadiazoleamide derivative and anti-ulcer drug
    4.
    发明授权
    Thiadiazoleamide derivative and anti-ulcer drug 有权
    噻二唑衍生物和抗溃疡药

    公开(公告)号：US5912258A

    公开(公告)日：1999-06-15

    申请号：US157376

    申请日：1998-09-21

    申请人： Chikao Nishino ,  Fumitaka Sato ,  Tomohiro Uetake ,  Hirotada Fukunishi ,  Nao Kojima

    发明人： Chikao Nishino ,  Fumitaka Sato ,  Tomohiro Uetake ,  Hirotada Fukunishi ,  Nao Kojima

    IPC分类号： C07D285/12 ,  C07D285/135 ,  C07D417/12 ,  C07D289/135 ,  A61K31/41

    CPC分类号： C07D285/135 ,  C07D417/12

    摘要： A thiadiazoleamide derivative or a salt thereof expressed by the following Formula 1: ##STR1## wherein each of R.sub.1 and R.sub.2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylamino group or an alkenyloxy group; wherein when either R.sub.1 or R.sub.2 is a hydrogen atom, the other is not a hydrogen atom; R.sub.3 represents a lower alkyl group, an aryl group, a pyridyl group or --N(R.sub.4)R.sub.5, wherein R.sub.4 and R.sub.5 represent lower alkyl groups or together represent a saturated heterocyclic ring having 4-8 members; wherein when R.sub.1 or R.sub.2 is a lower alkoxy group, R.sub.3 is --N(R.sub.4)R.sub.5 or a pyridyl group; and n represents an integer of 1-3. The derivatives have anti-ulcer effect to be available for preventing or curing ulcers in mammals.

    摘要翻译： 由下式1表示的噻二唑衍生物或其盐：其中R 1和R 2各自表示氢原子，低级烷基，低级烷氧基，低级烷基氨基或烯氧基; 其中当R 1或R 2是氢原子时，另一个不是氢原子; R3表示低级烷基，芳基，吡啶基或-N（R4）R5，其中R4和R5代表低级烷基或一起代表具有4-8个成员的饱和杂环; 其中当R1或R2为低级烷氧基时，R3为-N（R4）R5或吡啶基; n表示1-3的整数。 该衍生物具有抗溃疡作用，可用于预防或治疗哺乳动物的溃疡。

    Alkylenediamine derivative anti-ulcer drug and antibacterial drug
    5.
    发明授权
    Alkylenediamine derivative anti-ulcer drug and antibacterial drug 失效
    烷二胺衍生物抗溃疡药和抗菌药

    公开(公告)号：US5814634A

    公开(公告)日：1998-09-29

    申请号：US842891

    申请日：1997-04-17

    申请人： Chikao Nishino ,  Fumitaka Sato ,  Tomohiro Uetake ,  Hirotada Fukunishi ,  Nao Kojima

    发明人： Chikao Nishino ,  Fumitaka Sato ,  Tomohiro Uetake ,  Hirotada Fukunishi ,  Nao Kojima

    IPC分类号： C07D295/12 ,  A61K31/445 ,  A61K31/495 ,  A61K31/505 ,  A61K31/535 ,  A61K31/5375 ,  A61P1/04 ,  A61P31/04 ,  C07D211/14 ,  C07D239/42 ,  C07D277/20 ,  C07D277/38 ,  C07D277/82 ,  C07D295/13 ,  C07D317/58 ,  C07D211/32 ,  C07D265/30

    CPC分类号： C07D295/13

    摘要： The invention provides a compound which has anti-ulcer effect and antibacterial activity against Helicobacter pyroli. This compound is an alkylenediamine derivative or salt which has a general formula of (1): ##STR1## wherein each of R.sub.4, R.sub.5, and R.sub.6 is hydrogen or lower alkyl; n represents an integer of 1 to 6; Y is --CH.sub.2 --, --O--, or --N(R.sub.7)--, wherein R.sub.7 is lower alkyl, aryl, carbamoyl lower alkyl, aralkyl, or a heterocyclic group having 5 to 9 carbon numbers; and, W is a group expressed by formulas 2 or 3: ##STR2## wherein (1) in formula 2: each of R.sub.1 and R.sub.2 is hydrogen, lower alkoxy, alkenyloxy, or a halogen atom; each of R.sub.3 and R.sub.3 is methyl, prenyl, or geranyl; when one of R.sub.3 and R.sub.3 is prenyl or geranyl, the other must be a methyl group; and X is oxygen or sulfur; and (2) in formula 3, R.sub.10 is a lower alkyl, and R.sub.11 is a halogen atom.

    摘要翻译： 本发明提供了一种对幽门螺杆菌具有抗溃疡作用和抗菌活性的化合物。 该化合物是具有通式（1）：式1的亚烷基二胺衍生物或盐，其中R 4，R 5和R 6各自为氢或低级烷基; n表示1〜6的整数， Y是-CH 2 - ， - O-或-N（R 7） - ，其中R 7是低级烷基，芳基，氨基甲酰基低级烷基，芳烷基或具有5至9个碳数的杂环基; 式3中，式（1）中，R 1和R 2各自为氢，低级烷氧基，链烯氧基或卤素原子，式中，（1）表示2或3表示的基团。 R 3和R 3各自为甲基，异戊烯基或香叶基; 当R3和R3之一是异戊烯基或香叶基时，另一个必须是甲基; X为氧或硫; 和（2）在式3中，R 10是低级烷基，R 11是卤素原子。

    N-acylpiperazine derivative, antibacterial drug and anti-ulcer drug
    6.
    发明授权
    N-acylpiperazine derivative, antibacterial drug and anti-ulcer drug 失效
    N-酰基哌嗪衍生物，抗菌药物和抗溃疡药

    公开(公告)号：US5756505A

    公开(公告)日：1998-05-26

    申请号：US625992

    申请日：1996-04-01

    申请人： Chikao Nishino ,  Fumitaka Sato ,  Tomohiro Uetake ,  Hirotada Fukunishi ,  Nao Kojima ,  Koji Kobayashi

    发明人： Chikao Nishino ,  Fumitaka Sato ,  Tomohiro Uetake ,  Hirotada Fukunishi ,  Nao Kojima ,  Koji Kobayashi

    IPC分类号： C07D295/18 ,  A61K31/495 ,  A61P1/04 ,  A61P31/04 ,  C07D295/185 ,  C07D295/192 ,  C07D295/205 ,  C07D405/12

    CPC分类号： C07D295/185 ,  C07D295/192

    摘要： An N-acylpiperazine derivative or a salt thereof in accordance with the present invention is represented by the following formula 1: ##STR1## wherein R.sub.1 represents a lower alkyl, hydroxy lower alkyl, lower acyl, or arylcarbonyloxy lower alkyl group; R.sub.2 represents hydrogen atom or a lower alkyl, lower alkoxy, lower alkenyl, amino, or nitro group; R.sub.3 and R.sub.4, which are identical to or different from each other, represent hydrogen atoms, halogen atoms, or cyano, nitro, lower alkyl, or lower alkoxy groups; and n represents 0 or 1. The N-acylpiperazine derivative has anti-ulcer effect or an antibacterial activity against Helicobacter pyroli to be available for prevention or cure of ulsers.

    摘要翻译： 根据本发明的N-酰基哌嗪衍生物或其盐由下式1表示：其中R 1表示低级烷基，羟基低级烷基，低级酰基或芳基羰基氧基低级烷基; R2代表氢原子或低级烷基，低级烷氧基，低级烯基，氨基或硝基; R 3和R 4彼此相同或不同，表示氢原子，卤原子或氰基，硝基，低级烷基或低级烷氧基; 并且n表示0或1. N-酰基哌嗪衍生物具有抗溃疡作用或对幽门螺杆菌具有抗菌活性，可用于预防或治愈酏剂。