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1.
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。
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公开(公告)号:US5859032A
公开(公告)日:1999-01-12
申请号:US818281
申请日:1997-03-17
IPC分类号: A61K31/44 , A61K31/4409 , A61K31/4418 , A61P1/04 , C07D213/40 , C07D213/70 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/81
CPC分类号: C07D213/40 , C07D213/70 , C07D213/74 , C07D213/75
摘要: A pyridine derivative or a salt thereof expressed by the following formula 1: ##STR1## wherein W represents a group expressed by the following formula 2 or formula 3; ##STR2## wherein R.sub.1 represents an alkenyloxy group;n represents 1 or 2;Ra represents a lower alkyl group; andRb represents a halogen atom; and whereineach of R.sub.2 and R.sub.3 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, or halogenated alkyl group;Y represents a group expressed by --S--, --NH-- or --CONH--;m represents an integer of 0 to 2; andp represents 0 or 1.The pyridine derivative has an anti-ulcer effect or an antibacterial activity against Helicobacter pyroli to be available for prevention or cure of ulcers.
摘要翻译: 由下式1表示的吡啶衍生物或其盐:其中W表示由下式2或式3表示的基团; 式3其中R1表示烯氧基; n表示1或2; Ra表示低级烷基; 并且R b表示卤原子; 并且其中R 2和R 3各自表示氢原子,低级烷基,低级烷氧基或卤代烷基; Y表示由-S-,-NH-或-CONH-表示的基团; m表示0〜2的整数。 并且p表示0或1.吡啶衍生物对抗幽门螺杆菌具有抗溃疡作用或抗菌活性,可用于预防或治愈溃疡。
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公开(公告)号:US6017937A
公开(公告)日:2000-01-25
申请号:US55921
申请日:1998-04-07
IPC分类号: A61K31/44 , A61K31/4409 , A61K31/4418 , A61P1/04 , C07D213/40 , C07D213/70 , C07D213/74 , C07D213/75 , C07D213/76 , C07D213/81
CPC分类号: C07D213/40 , C07D213/70 , C07D213/74 , C07D213/75
摘要: A pyridine derivative or a salt thereof expressed by the following formula 1: ##STR1## wherein W represents a group expressed by the following formula 2 or formula 3; ##STR2## wherein R.sub.1 represents an alkenyloxy group; n represents 1 or 2;Ra represents a lower alkyl group; andRb represents a halogen atom; and whereineach of R.sub.2 and R.sub.3 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, or halogenated alkyl group;Y represents a group expressed by --S--, --NH-- or --CONH--;m represents an integer of 0 to 2; andp represents 0 or 1.The pyridine derivative has an anti-ulcer effect or an antibacterial activity against Helicobacter pyroli to be available for prevention or cure of ulcers.
摘要翻译: 由下式1表示的吡啶衍生物或其盐:其中W表示由下式2或式3表示的基团; 其中R1表示烯氧基; n表示1或2; Ra表示低级烷基; 并且R b表示卤原子; 并且其中R 2和R 3各自表示氢原子,低级烷基,低级烷氧基或卤代烷基; Y表示由-S-,-NH-或-CONH-表示的基团; m表示0〜2的整数。 并且p表示0或1.吡啶衍生物对抗幽门螺杆菌具有抗溃疡作用或抗菌活性,可用于预防或治愈溃疡。
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公开(公告)号:US5912258A
公开(公告)日:1999-06-15
申请号:US157376
申请日:1998-09-21
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。
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公开(公告)号:US5814634A
公开(公告)日:1998-09-29
申请号:US842891
申请日:1997-04-17
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。
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6.
公开(公告)号:US6001880A
公开(公告)日:1999-12-14
申请号:US53667
申请日:1998-04-02
IPC分类号: A61K31/165 , A61K31/44 , A61P1/04 , A61P31/04 , C07C233/78 , C07C235/50 , C07C235/60 , C07C235/84 , C07C237/34 , C07C237/42 , C07C323/62 , C07D213/81 , C07D213/82 , C07D295/155 , A01N37/18 , C07C233/74
CPC分类号: C07D213/81 , C07C233/78 , C07C235/50 , C07C235/60 , C07C235/84 , C07C237/34 , C07C237/42 , C07C323/62 , C07D213/82 , C07D295/155
摘要: An alkylenediamine derivative or a salt thereof expressed by the following formula 1: ##STR1## wherein each of R.sub.1 and R.sub.2 represents a lower alkyl group, and W represents a group expressed by any of the following formulas 2 and 3; ##STR2## wherein all variables are as defined in the specification The alkylenediamine derivative has an anti- ulcer effect or an antibacterial activity against Helicobacter pyroli, and has also high safety to be available for prevention or cure of ulcers.
摘要翻译: 由下式1表示的亚烷基二胺衍生物或其盐:其中R 1和R 2各自表示低级烷基,W表示由下式2和3中任一个表示的基团; 其中所有变量如本说明书中所定义。亚烷基二胺衍生物对幽门螺杆菌具有抗溃疡作用或抗菌活性,并且还具有可用于预防或治愈溃疡的高安全性。
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7.
公开(公告)号:US5962456A
公开(公告)日:1999-10-05
申请号:US939912
申请日:1997-09-29
IPC分类号: C07D295/10 , A61K31/495 , A61P1/04 , A61P31/04 , C07D213/72 , C07D213/79 , C07D213/80 , C07D295/14 , C07D295/192 , C07D317/58 , C07D317/60 , C07D317/68 , C07D401/04 , C07D401/12
CPC分类号: C07D295/192 , C07D213/80 , C07D317/68
摘要: An N-acylpiperazine derivative or a salt thereof expressed by the following formula 1: ##STR1## wherein R.sub.1 represents a pyridylcarbonyloxy lower alkyl group, a benzoylamino lower alkyl group, benzyl group, carbamoyl group, pyridyl group, or diphenylmethyl group;R.sub.2 represents a lower alkyl group or a lower alkoxy group;n represents an integer of 0 to 2;R.sub.3 represents a hydrogen atom, an alkenyl group, or benzyl group; andm represents an integer of 1 to 3.The N-acylpiperazine derivative or a salt thereof has an anti-ulcer effect, an antibacterial activity against Helicobacter pyroli, and high safety to be available for prevention or cure of various ulcers.
摘要翻译: 由下式1表示的N-酰基哌嗪衍生物或其盐:其中R1表示吡啶基羰基氧基低级烷基,苯甲酰氨基低级烷基,苄基,氨基甲酰基,吡啶基或二苯基甲基; R2代表低级烷基或低级烷氧基; n表示0〜2的整数, R3表示氢原子,烯基或苄基; m表示1〜3的整数。N-酰基哌嗪衍生物或其盐具有抗溃疡作用,对幽门螺杆菌的抗菌活性,以及可用于预防或治愈各种溃疡的高安全性。
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公开(公告)号:US5925667A
公开(公告)日:1999-07-20
申请号:US53659
申请日:1998-04-02
申请人: Chikao Nishino , Tomohiro Uetake
发明人: Chikao Nishino , Tomohiro Uetake
IPC分类号: C07D401/12 , A61K31/40 , A61K31/44 , A61K31/4427 , A61K31/53 , A61P1/04 , A61P31/04 , C07D207/00 , C07D207/09 , C07D213/00 , C07D295/00 , C07D295/04 , C07D401/00 , C07D29/00
CPC分类号: C07D401/12 , C07D207/09 , Y10S514/925 , Y10S514/926 , Y10S514/927
摘要: A pyrrolidine derivative or a salt thereof expressed by the following formula 1: ##STR1## wherein R.sub.1 is an alkenyl group; R.sub.2 is a lower alkoxy group or a halogen atom;R.sub.3 is a lower alkyl group;X is a group expressed by --O-- or --S--;Y is carbon or nitrogen atom;m is an integer of 1 to 3; andn is an integer of 0 to 2.The pyrrolidine derivative has an anti-ulcer effect or an antibacterial activity against Helicobacter pyroli, and has also high safety to be available for prevention or cure of ulcers.
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公开(公告)号:US6043243A
公开(公告)日:2000-03-28
申请号:US204273
申请日:1998-12-03
申请人: Chikao Nishino , Tomohiro Uetake
发明人: Chikao Nishino , Tomohiro Uetake
IPC分类号: C07D401/12 , A61K31/40 , A61K31/44 , A61K31/4427 , A61K31/53 , A61P1/04 , A61P31/04 , C07D207/00 , C07D207/09 , C07D213/00 , C07D295/00 , C07D295/04 , C07D401/00
CPC分类号: C07D401/12 , C07D207/09 , Y10S514/925 , Y10S514/926 , Y10S514/927
摘要: A pyrrolidine derivative or a salt thereof expressed by the following formula 1: ##STR1## wherein R.sub.1 is an alkenyl group; R.sub.2 is a lower alkoxy group or a halogen atom;R.sub.3 is a lower alkyl group;X is a group expressed by --O-- or --S--;Y is carbon or nitrogen atom;m is an integer of 1 to 3; andn is an integer of 0 to 2.The pyrrolidine derivative has an anti-ulcer effect or an antibacterial activity against Helicobacter pyroli, and has also high safety to be available for prevention or cure of ulcers.
摘要翻译: 由下式1表示的吡咯烷衍生物或其盐:其中R1是烯基; R2是低级烷氧基或卤素原子; R3是低级烷基; X是由-O - 或-S-表示的基团; Y是碳或氮原子; m为1〜3的整数。 并且n为0〜2的整数。吡咯烷衍生物对幽门螺杆菌具有抗溃疡作用或抗菌活性,并且还具有可用于预防或治愈溃疡的高安全性。
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公开(公告)号:US5891890A
公开(公告)日:1999-04-06
申请号:US53666
申请日:1998-04-02
申请人: Chikao Nishino , Nao Kojima
发明人: Chikao Nishino , Nao Kojima
IPC分类号: C07D295/14 , A61K31/445 , A61P1/04 , A61P31/04 , C07D295/135 , C07D211/14
CPC分类号: C07D295/135
摘要: A benzamide derivative or a salt thereof expressed by the following formula 1: ##STR1## wherein R.sub.1 is hydrogen atom or a lower alkyl group; R.sub.2 is a benzyl or an alkenyl group; andn is an integer of 1 to 6.The benzamide derivative or a salt thereof has an anti-ulcer effect or an antibacterial activity against Hedicobacter pyroli, and has also high safety to be available for prevention or cure of ulcers.
摘要翻译: 由下式1表示的苯甲酰胺衍生物或其盐:其中R 1是氢原子或低级烷基; R2是苄基或烯基; 并且n为1〜6的整数。苯甲酰胺衍生物或其盐具有抗黑曲霉菌的抗溃疡作用或抗菌活性,并且还具有可用于预防或治愈溃疡的高安全性。
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