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公开(公告)号:US20090203911A1
公开(公告)日:2009-08-13
申请号:US12189590
申请日:2008-08-11
申请人: Shuhei MIYAZAWA , Masanobu Shinoda , Tetsuya Kawahara , Nobuhisa Watanabe , Hitoshi Harada , Daisuke Iida , Hiroki Terauchi , Junichi Nagakawa , Hideaki Fujisaki , Atsuhiko Kubota , Masato Ueda
发明人: Shuhei MIYAZAWA , Masanobu Shinoda , Tetsuya Kawahara , Nobuhisa Watanabe , Hitoshi Harada , Daisuke Iida , Hiroki Terauchi , Junichi Nagakawa , Hideaki Fujisaki , Atsuhiko Kubota , Masato Ueda
IPC分类号: C07D405/14 , C07D401/12
CPC分类号: C07D491/04 , C07D405/14 , C07D493/08 , C07D493/10
摘要: A novel chemical compound useful as a therapeutic or prophylactic agent for acid-related diseases is provided, which has an excellent inhibitory effect against gastric acid secretion, an excellent effect of maintaining the inhibitory effect against gastric acid secretion, thereby maintaining intragastric pH high for a long time, and having more safety and appropriate physicochemical stability. Provided is a compound represented by where R1 and R3 may be the same or different and each represent a hydrogen atom or a C1-C6 alkyl group; R2 represents (5,5-dimethyl-1,3-dioxan-2-yl)methoxy group, 5,7-dioxaspiro[2.5]oct-6-ylmethoxy group, 1,5,9-trioxaspiro[5.5]undec-3-ylmethoxy group, or (2,2-dimethyl-1,3-dioxan-5-yl)methoxy group; R4, R5, R6 and R7 represent a hydrogen atom, halogen atom, C1-C6 alkyl group, C1-C6 haloalkyl group, C1-C6 alkoxy group or C1-C6 haloalkoxy group; and W1 represents a single bond, methylene or ethylene group, a salt thereof or a solvate of these.
摘要翻译: 提供了可用作酸性相关疾病的治疗或预防剂的新型化合物,其对胃酸分泌具有优异的抑制作用,保持对胃酸分泌的抑制作用的优异效果,从而保持胃内pH高 长时间,具有更多的安全性和适当的物理化学稳定性。 提供一种化合物,其中R 1和R 3可以相同或不同,各自表示氢原子或C 1 -C 6烷基; R2代表(5,5-二甲基-1,3-二恶烷-2-基)甲氧基,5,7-二氧杂螺[2.5]辛-6-基甲氧基,1,5,9-三氧杂螺[5.5]十一烷-3 - 甲氧基或(2,2-二甲基-1,3-二恶烷-5-基)甲氧基; R4,R5,R6和R7表示氢原子,卤素原子,C1-C6烷基,C1-C6卤代烷基,C1-C6烷氧基或C1-C6卤代烷氧基; W1表示单键,亚甲基或亚乙基,它们的盐或它们的溶剂合物。
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公开(公告)号:US07189717B2
公开(公告)日:2007-03-13
申请号:US10257091
申请日:2001-04-26
申请人: Masahiro Yasuda , Hitoshi Harada , Shuhei Miyazawa , Seiichi Kobayashi , Kokichi Harada , Takayuki Hida , Hisashi Shibata , Nobuyuki Yasuda , Osamu Asano , Yoshihiko Kotake
发明人: Masahiro Yasuda , Hitoshi Harada , Shuhei Miyazawa , Seiichi Kobayashi , Kokichi Harada , Takayuki Hida , Hisashi Shibata , Nobuyuki Yasuda , Osamu Asano , Yoshihiko Kotake
IPC分类号: A61K31/506
CPC分类号: A61K31/506 , A61K31/519 , A61K31/522 , A61K31/5377 , A61K31/7076 , H04B10/112
摘要: The present invention provides a medicament having a gentle but strong defecation-promoting action without causing diarrhea. That is, it provides a defecation-promoting agent comprising a compound having an adenosine A2 receptor antagonism, preferably an adenosine A2b receptor antagonism, or a salt thereof.
摘要翻译: 本发明提供一种具有温和但强烈的排便促进作用而不引起腹泻的药物。 也就是说,它提供了包含具有腺苷A 2受体拮抗作用的化合物,优选腺苷A 2b受体拮抗剂或其盐的排便促进剂。
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公开(公告)号:US06750232B2
公开(公告)日:2004-06-15
申请号:US10333689
申请日:2003-01-23
申请人: Hitoshi Harada , Osamu Asano , Shuhei Miyazawa , Masato Ueda , Masahiro Yasuda , Nobuyuki Yasuda
发明人: Hitoshi Harada , Osamu Asano , Shuhei Miyazawa , Masato Ueda , Masahiro Yasuda , Nobuyuki Yasuda
IPC分类号: C07D40102
CPC分类号: C07D213/80 , A61K31/4409 , A61K31/443 , A61K31/4436 , A61K31/444 , A61K31/455 , C07D213/82 , C07D213/85 , C07D405/04 , C07D405/14 , C07D409/14
摘要: A class of substituted compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (II), wherein R1 is selected from hydrido, halo, alkoxy, aryl, alkylthio, alkylamino, aralkoxy, azido and alkenyloxy; wherein R2 is selected from hydrido, cyano, hydroxyalkyl, haloalkyl, aminoalkyl, alkylaminoalkyl, alkylcarbonyloxyalkyl, aminocarbonyl and alkylcarbonylaminoalkyl; and wherein R5 and R6 are one more radicals independently selected from halo, alkylsulfonyl, aminosulfonyl, alkoxy and alkylthio; provided one of R5 and R6 is substituted with alkysulfonyl, aminosulfonyl, or haloalkylsulfonyl; or a pharmaceutically-acceptable salt thereof.
摘要翻译: 描述了一类取代的化合物用于治疗炎症和炎症相关疾病。 特别感兴趣的化合物由式(II)定义,其中R 1选自氢,卤素,烷氧基,芳基,烷硫基,烷基氨基,芳烷氧基,叠氮基和烯氧基; 氰基,羟基烷基,卤代烷基,氨基烷基,烷基氨基烷基,烷基羰氧基烷基,氨基羰基和烷基羰基氨基烷基;其中R 2选自氢,氰基, 并且其中R 5和R 6分别独立地选自卤素,烷基磺酰基,氨基磺酰基,烷氧基和烷硫基; 其中R 5和R 6之一被烷基磺酰基,氨基磺酰基或卤代烷基磺酰基取代; 或其药学上可接受的盐。
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公开(公告)号:US5998445A
公开(公告)日:1999-12-07
申请号:US679473
申请日:1996-07-09
申请人: Shigeru Souda , Norihiro Ueda , Shuhei Miyazawa , Katsuya Tagami , Seiichiro Nomoto , Makoto Okita , Naoyuki Shimomura , Toshihiko Kaneko , Masatoshi Fujimoto , Manabu Murakami , Kiyoshi Oketani , Hideaki Fujisaki , Hisashi Shibata , Tsuneo Wakabayashi
发明人: Shigeru Souda , Norihiro Ueda , Shuhei Miyazawa , Katsuya Tagami , Seiichiro Nomoto , Makoto Okita , Naoyuki Shimomura , Toshihiko Kaneko , Masatoshi Fujimoto , Manabu Murakami , Kiyoshi Oketani , Hideaki Fujisaki , Hisashi Shibata , Tsuneo Wakabayashi
IPC分类号: A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/54 , A61P1/04 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14
CPC分类号: C07D401/12 , C07D401/14 , C07D405/14 , C07D413/12 , C07D417/12 , C07D417/14
摘要: Pyridine derivatives useful for preventing or treating peptic ulcers, pharmaceutical preparations and methods of treating peptic ulcers are described.
摘要翻译: 描述了可用于预防或治疗消化性溃疡的吡啶衍生物,药物制剂和治疗消化性溃疡的方法。
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公开(公告)号:US5708013A
公开(公告)日:1998-01-13
申请号:US524109
申请日:1995-08-21
申请人: Shigeru Souda , Norihiro Ueda , Shuhei Miyazawa , Katsuya Tagami , Seiichiro Nomoto , Makoto Okita , Naoyuki Shimomura , Toshihiko Kaneko , Masatoshi Fujimoto , Manabu Murakami , Kiyoshi Oketani , Hideaki Fujisaki , Hisashi Shibata , Tsuneo Wakabayashi
发明人: Shigeru Souda , Norihiro Ueda , Shuhei Miyazawa , Katsuya Tagami , Seiichiro Nomoto , Makoto Okita , Naoyuki Shimomura , Toshihiko Kaneko , Masatoshi Fujimoto , Manabu Murakami , Kiyoshi Oketani , Hideaki Fujisaki , Hisashi Shibata , Tsuneo Wakabayashi
IPC分类号: C07D401/12 , A61K31/44
CPC分类号: C07D401/12
摘要: A pyridine compound having the formula is disclosed and useful to treat the peptic ulcer. ##STR1## wherein R.sup.1 and R.sup.2 which may be the same or different are each a hydrogen atom, a lower alkyl group, a lower alkoxy group, a halogenated lower alkyl group, or a halogen atom, R.sup.3 and R.sup.4 which may be the same or different are each a hydrogen atom or a lower alkyl group, X is a group represented by the formula --S--, a group represented by the formula ##STR2## or a group represented by the formula ##STR3## and n is an integer of 1 to 6, provided that R.sup.3 and R.sup.4 are not simultaneously hydrogen atoms when n is 1.
摘要翻译: 公开了具有下式的吡啶化合物,可用于治疗消化性溃疡。 其中可以相同或不同的R 1和R 2各自为氢原子,低级烷基,低级烷氧基,卤代低级烷基或卤素原子,可以相同的R 3和R 4, 不同的是氢原子或低级烷基,X是由式-S-表示的基团,即由式d表示的基团,当n为1时,R3和R4不同时为氢原子。
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公开(公告)号:US5578603A
公开(公告)日:1996-11-26
申请号:US337480
申请日:1994-11-08
申请人: Shuhei Miyazawa , Shigeki Hibi , Hiroyuki Yoshimura , Takashi Mori , Yorihisa Hoshino , Mitsuo Nagai , Kouichi Kikuchi , Hisashi Shibata , Kazuo Hirota , Takashi Yamanaka , Isao Yamatsu , Masanori Mizuno
发明人: Shuhei Miyazawa , Shigeki Hibi , Hiroyuki Yoshimura , Takashi Mori , Yorihisa Hoshino , Mitsuo Nagai , Kouichi Kikuchi , Hisashi Shibata , Kazuo Hirota , Takashi Yamanaka , Isao Yamatsu , Masanori Mizuno
IPC分类号: A61K31/46 , A61P1/00 , A61P1/08 , A61P25/20 , A61P43/00 , C07C229/60 , C07C229/64 , C07D451/04 , C07D451/12 , C07D405/10
CPC分类号: C07D451/04
摘要: An aminobenzoic acid derivative represented by the following formulas (I-2) or (I-3), or a pharmacologically acceptable salt thereof, which exhibits a serotonin antagonism and an acetylcholine release accelerating activity at a well-balanced activity ratio and which is efficacious as a drug for patients with gastrointestinal unindentified complaints: ##STR1## wherein R.sup.1 represents a group such as an alkynyl or cyanoalkyl group; R.sup.2 represents a group such as an amino or acylamino group; R.sup.3 represents a halogen atom; X represents --O-- or --N--; and A represents an oxygen or sulfur atom.
摘要翻译: 由下列通式(I-2)或(I-3)表示的氨基苯甲酸衍生物或其药理学上可接受的盐以良好的平衡活性比表现出5-羟色胺拮抗作用和乙酰胆碱释放促进活性, 作为胃肠道不明确投诉患者的药物:
(I-2)和 (I-3)其中R1表示诸如炔基或氰基烷基的基团; R2表示氨基或酰氨基等基团。 R3表示卤原子; X表示-O-或-N-; A表示氧或硫原子。 -
公开(公告)号:US5482937A
公开(公告)日:1996-01-09
申请号:US318971
申请日:1994-10-06
申请人: Kazuo Okano , Shuhei Miyazawa , Richard S. J. Clark , Shinya Abe , Tetsuya Kawahara , Naoyuki Shimomura , Osamu Asano , Hiroyuki Yoshimura , Mitsuaki Miyamoto , Yoshimori Sakuma , Kenzo Muramoto , Hiroshi Obaishi , Koukichi Harada , Hajime Tsunoda , Satoshi Katayama , Kouji Yamada , Shigeru Souda , Yoshimasa Machida , Kouichi Katayama , Isao Yamatsu
发明人: Kazuo Okano , Shuhei Miyazawa , Richard S. J. Clark , Shinya Abe , Tetsuya Kawahara , Naoyuki Shimomura , Osamu Asano , Hiroyuki Yoshimura , Mitsuaki Miyamoto , Yoshimori Sakuma , Kenzo Muramoto , Hiroshi Obaishi , Koukichi Harada , Hajime Tsunoda , Satoshi Katayama , Kouji Yamada , Shigeru Souda , Yoshimasa Machida , Kouichi Katayama , Isao Yamatsu
IPC分类号: C07D495/14 , C07D495/22 , C07F9/6561 , A61K31/55
CPC分类号: C07D495/14 , C07F9/6561
摘要: A triazolo-1,4-di-azepine compound of the below given formula and a pharmacologically acceptable salt thereof are useful in the pharmaceutical field, especially in treating allergic diseases. ##STR1## in which R.sup.1 and R.sup.2 are hydrogen or an alkyl, R.sup.3 is hydrogen or a halogen, R.sup.4 is hydrogen or an alkyl, X is --OCO--, and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.
摘要翻译: 以下给定式的三唑并-1,4-二氮杂化合物及其药理学上可接受的盐可用于制药领域,特别是用于治疗过敏性疾病。 其中R1和R2是氢或烷基,R3是氢或卤素,R4是氢或烷基,X是-OCO-,Y是环烷基,环烷基烷基,炔基等。
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公开(公告)号:US5476864A
公开(公告)日:1995-12-19
申请号:US129302
申请日:1993-11-10
申请人: Kazuo Okano , Osamu Asano , Naoyuki Shimomura , Tetsuya Kawahara , Shinya Abe , Shuhei Miyazawa , Mitsuaki Miyamoto , Hiroyuki Yoshimura , Koukichi Harada , Junsaku Nagaoka , Tsutomu Kawata , Tsutomu Yoshimura , Hiromasa Suzuki , Shigeru Souda , Yoshimasa Machida , Kouichi Katayama , Isao Yamatsu
发明人: Kazuo Okano , Osamu Asano , Naoyuki Shimomura , Tetsuya Kawahara , Shinya Abe , Shuhei Miyazawa , Mitsuaki Miyamoto , Hiroyuki Yoshimura , Koukichi Harada , Junsaku Nagaoka , Tsutomu Kawata , Tsutomu Yoshimura , Hiromasa Suzuki , Shigeru Souda , Yoshimasa Machida , Kouichi Katayama , Isao Yamatsu
IPC分类号: C07D213/40 , C07D401/06 , C07D401/12 , C07D405/12 , A61K31/44 , C07D213/02
CPC分类号: C07D213/40 , C07D401/06 , C07D401/12 , C07D405/12
摘要: A glycerin derivative having the following formula (I) or (I') and a pharmacologically acceptable salt thereof are useful to treat diseases caused by the platelet activating factor. ##STR1##
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公开(公告)号:US5468740A
公开(公告)日:1995-11-21
申请号:US386533
申请日:1995-02-10
申请人: Kazuo Okano , Shuhei Miyazawa , Richard S. J. Clark , Shinya Abe , Tetsuya Kawahara , Naoyuki Shimomura , Osamu Asano , Hiroyuki Yoshimura , Mitsuaki Miyamoto , Yoshimori Sakuma , Kenzo Muramoto , Hiroshi Obaishi , Koukichi Harada , Hajime Tsunoda , Satoshi Katayama , Kouji Yamada , Shigeru Souda , Yoshimasa Machida , Kouichi Katayama , Isao Yamatsu
发明人: Kazuo Okano , Shuhei Miyazawa , Richard S. J. Clark , Shinya Abe , Tetsuya Kawahara , Naoyuki Shimomura , Osamu Asano , Hiroyuki Yoshimura , Mitsuaki Miyamoto , Yoshimori Sakuma , Kenzo Muramoto , Hiroshi Obaishi , Koukichi Harada , Hajime Tsunoda , Satoshi Katayama , Kouji Yamada , Shigeru Souda , Yoshimasa Machida , Kouichi Katayama , Isao Yamatsu
IPC分类号: C07D495/14 , C07D495/22 , C07F9/6561 , A61K31/675 , C07F9/00
CPC分类号: C07D495/14 , C07F9/6561
摘要: A triazolo-1,4-di-azepine compound of the below given formula and a pharmacologically acceptable salt thereof are disclosed and useful in the pharmaceutical field, especially to allergic diseases. ##STR1## in which R.sup.1 and R.sup.2 are hydrogen or an alkyl, R.sup.3 is hydrogen or a halogen, R.sup.4 is hydrogen or an alkyl, X is --OCO--, --NHCO--, --CO-- or others and Y is a cycloalkyl, a cycloalkylalkyl, an alkynyl or others.
摘要翻译: 公开了以下给定式的三唑并-1,4-二氮杂化合物及其药理学上可接受的盐,尤其适用于过敏性疾病。 其中R 1和R 2是氢或烷基,R 3是氢或卤素,R 4是氢或烷基,X是-OCO - , - NHCO-,-CO-或其它,Y是环烷基, 环烷基烷基,炔基等。
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公开(公告)号:US5319139A
公开(公告)日:1994-06-07
申请号:US40026
申请日:1993-03-30
申请人: Hiroyuki Yoshimura , Shinya Abe , Tetsuya Kawahara , Naoyuki Shimomura , Kazuo Okano , Richard S. J. Clark , Takashi Mori , Shuhei Miyazawa , Ryoichi Hashida , Kenzo Muramoto , Koukichi Harada , Takashi Inoue , Hirsohi Shirota , Kenichi Chiba , Kenichi Kusube , Toru Horie , Takeshi Suzuki , Isao Yamatsu
发明人: Hiroyuki Yoshimura , Shinya Abe , Tetsuya Kawahara , Naoyuki Shimomura , Kazuo Okano , Richard S. J. Clark , Takashi Mori , Shuhei Miyazawa , Ryoichi Hashida , Kenzo Muramoto , Koukichi Harada , Takashi Inoue , Hirsohi Shirota , Kenichi Chiba , Kenichi Kusube , Toru Horie , Takeshi Suzuki , Isao Yamatsu
IPC分类号: A61K31/165 , A61K31/19 , A61K31/192 , A61K31/197 , A61K31/215 , A61K31/22 , A61K31/222 , A61K31/275 , A61P19/02 , A61P25/04 , A61P29/00 , A61P43/00 , C07C39/40 , C07C43/20 , C07C43/23 , C07C43/253 , C07C45/00 , C07C47/575 , C07C59/52 , C07C59/64 , C07C59/72 , C07C59/84 , C07C59/90 , C07C69/157 , C07C69/734 , C07C69/738 , C07C235/34 , C07C251/48 , C07C255/41 , C07C233/00
CPC分类号: C07C255/41 , C07C251/48 , C07C39/40 , C07C43/202 , C07C43/23 , C07C43/253 , C07C45/00 , C07C47/575 , C07C59/52 , C07C59/64 , C07C59/72 , C07C59/90 , C07C69/734 , C07C69/738 , C07C2101/08
摘要: Compounds of the formula: ##STR1## where R.sup.1 is a hydrogen atom or a lower alkyl group;R.sub.2 is a lower alkoxy group;R.sub.3 is a group ##STR2## Z is represented by the formula: ##STR3## where R.sub.2 and R.sub.3 may be the same or different from each other and each stands for a hydrogen atom or a lower alkyl;Y is represented by the formula: --(CH.sub.2).sub.n -- where n is 0 or an integer of 1 to 2 or a group represented by the formula: ##STR4## where R.sup.2 and R.sup.3 may be the same or different from each other and each stands for a lower alkyl group; andR.sup.4 represents a group of the formula: ##STR5## where p is 0 or an integer of 1 to 3 and R.sup.12 is hydrogen, a halogen atom, a lower alkyl or a lower alkoxy group a hydrogen atom, R.sup.2 is a methoxy group, R.sup.3 is a hydroxy group and R.sup.4 is a benzyl group having anti-inflammatory activity.
摘要翻译: 下式的化合物:其中R 1是氢原子或低级烷基; R2是低级烷氧基; R 3是一个基团Z由下式表示:其中R 2和R 3可以相同或不同,各代表氢原子或低级烷基; Y由下式表示: - (CH 2)n - 其中n为0或1至2的整数或由下式表示的基团:其中R 2和R 3可以彼此相同或不同, 代表低级烷基; 并且R 4表示下式的基团:其中p为0或1至3的整数,R 12为氢,卤素原子,低级烷基或低级烷氧基,氢原子,R 2为甲氧基, R3是羟基,R4是具有抗炎活性的苄基。
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