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公开(公告)号:US06498159B1
公开(公告)日:2002-12-24
申请号:US09508197
申请日:2000-03-08
申请人: Nobuhisa Watanabe , Norio Karibe , Kazuki Miyazaki , Fumihiro Ozaki , Atsushi Kamada , Shuhei Miyazawa , Yoshimitsu Naoe , Toshihiko Kaneko , Itaru Tsukada , Tadashi Nagakura , Hiroki Ishihara , Kohtarou Kodama , Hideyuki Adachi
发明人: Nobuhisa Watanabe , Norio Karibe , Kazuki Miyazaki , Fumihiro Ozaki , Atsushi Kamada , Shuhei Miyazawa , Yoshimitsu Naoe , Toshihiko Kaneko , Itaru Tsukada , Tadashi Nagakura , Hiroki Ishihara , Kohtarou Kodama , Hideyuki Adachi
IPC分类号: A61K31502
CPC分类号: C07D231/12 , C07D233/56 , C07D237/28 , C07D237/34 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D409/14 , C07D411/14 , C07D417/04 , C07D417/14 , C07D451/06 , C07D471/08 , C07D491/04 , C07D491/08 , C07D491/10
摘要: The present invention provides a phthalazine compound as a therapeutic agent for erectile dysfunction represented by the following formula, a pharmacologically acceptable salt thereof or a hydrate thereof: wherein R1 and R2 are the same as or different from each other and represent a halogen atom, a C1 to C4 alkyl group which may be substituted with a halogen atom, a C1 to C4 alkoxy group which may be substituted with a halogen atom or a cyano group; X represents a cyano group, a nitro group, a halogen atom, a hydroxyimino group which may be substituted or a heteroaryl group which may be substituted; Y represents a heteroaryl group, an aryl group which may be substituted, an alkynyl group which may substituted, an alkenyl group, an alkyl group, an optionally substituted saturated or unsaturated 4- to 8-membered amine ring, and the cyclic amine compound is a monocyclic compound, bicyclic compound or a spiro compound; l is an integer of 1 to 3; provided that the case where l is 1 or 2, X is a cyano group, a nitro group or a chlorine atom, R1 is a chlorine atom, R2 is a methoxy group and Y is a 5- or 6-membered amine ring substituted with a hydroxyl group is excluded.
摘要翻译: 本发明提供作为下述式表示的勃起功能障碍治疗剂的酞嗪化合物,其药理学上可接受的盐或其水合物:其中R1和R2彼此相同或不同,表示卤素原子, 可以被卤素原子取代的C1〜C4烷基,可被卤素原子或氰基取代的C1〜C4烷氧基; X表示氰基,硝基,卤素原子,可被取代的羟基亚氨基或可被取代的杂芳基; Y表示可以被取代的杂芳基,可以被取代的芳基,可以被取代的炔基,烯基,烷基,任选取代的饱和或不饱和的4-至8-元胺环,环胺化合物是 单环化合物,双环化合物或螺环化合物; l为1〜3的整数, 条件是其中l为1或2的情况,X为氰基,硝基或氯原子,R 1为氯原子,R 2为甲氧基,Y为被5或6元环取代的5-或6-元胺环 不包括羟基。
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2.
公开(公告)号:US06699870B2
公开(公告)日:2004-03-02
申请号:US10281194
申请日:2002-10-28
申请人: Nobuhisa Watanabe , Norio Karibe , Kazuki Miyazaki , Fumihiro Ozaki , Atsushi Kamada , Shuhei Miyazawa , Yoshimitsu Naoe , Toshihiko Kaneko , Itaru Tsukada , Tadashi Nagakura , Hiroki Ishihara , Kohtarou Kodama , Hideyuki Adachi
发明人: Nobuhisa Watanabe , Norio Karibe , Kazuki Miyazaki , Fumihiro Ozaki , Atsushi Kamada , Shuhei Miyazawa , Yoshimitsu Naoe , Toshihiko Kaneko , Itaru Tsukada , Tadashi Nagakura , Hiroki Ishihara , Kohtarou Kodama , Hideyuki Adachi
IPC分类号: A61K31502
CPC分类号: C07D231/12 , C07D233/56 , C07D237/28 , C07D237/34 , C07D249/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D409/14 , C07D411/14 , C07D417/04 , C07D417/14 , C07D451/06 , C07D471/08 , C07D491/04 , C07D491/08 , C07D491/10
摘要: The present invention provides a phthalazine compound as a therapeutic agent for erectile dysfunction represented by the following formula, a pharmacologically acceptable salt thereof or a hydrate thereof: wherein R1 and R2 are the same as or different from each other and represent a halogen atom, a C1 to C4 alkyl group which may be substituted with a halogen atom, a C1 to C4 alkoxy group which may be substituted with a halogen atom or a cyano group; X represents a cyano group, a nitro group, a halogen atom, a hydroxyimino group which may be substituted or a heteroaryl group which may be substituted; Y represents a heteroaryl group, an aryl group which may be substituted, an alkynyl group which may substituted, an alkenyl group, an alkyl group, an optionally substituted saturated or unsaturated 4- to 8-membered amine ring, and the cyclic amine compound is a monocyclic compound, bicyclic compound or a spiro compound; l is an integer of 1 to 3; provided that the case where l is 1 or 2, X is a cyano group, a nitro group or a chlorine atom, R1 is a chlorine atom, R2 is a methoxy group and Y is a 5- or 6-memberred amine ring substituted with a hydroxyl group is excluded.
摘要翻译: 本发明提供作为下式表示的勃起功能障碍治疗剂的酞嗪化合物,其药理学上可接受的盐或其水合物:其中R 1和R 2彼此相同或不同, 可以被卤素原子取代的C1〜C4烷基,可被卤素原子或氰基取代的C1〜C4烷氧基; X表示氰基,硝基,卤素原子,可被取代的羟基亚氨基或可被取代的杂芳基; Y表示可以被取代的杂芳基,可以被取代的芳基,可以被取代的炔基,烯基,烷基,任选取代的饱和或不饱和的4-至8-元胺环,环胺化合物是 单环化合物,双环化合物或螺环化合物; l为1〜3的整数, 条件是其中l为1或2,X为氰基,硝基或氯原子,R 1为氯原子,R 2为甲氧基,Y为5-或6 被羟基取代的胺基环被排除。
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3.
公开(公告)号:US06288064B1
公开(公告)日:2001-09-11
申请号:US09202422
申请日:1999-02-16
申请人: Nobuhisa Watanabe , Yasuhiro Kabasawa , Shinya Abe , Mayu Shibazaki , Hiroki Ishihara , Kohtarou Kodama , Hideyuki Adachi
发明人: Nobuhisa Watanabe , Yasuhiro Kabasawa , Shinya Abe , Mayu Shibazaki , Hiroki Ishihara , Kohtarou Kodama , Hideyuki Adachi
IPC分类号: A61K3150
CPC分类号: C07D237/34
摘要: The present invnetion provides a remedy for erectile dysfunction. The active ingredient thereof is a fused pyridazine compound represented by the following formula (I) or a pharmacologically acceptable salt thereof: (wherein the ring C represents a 5 or 6 membered ring optionally having hetero atom(s); n is an integer of from 1 to 4; R1 represents a hydrogen, a halogen, a cyano, etc.; A represents a hydrogen, a halogen, an optionally substituted amino, etc.; X represents a group represented by the formula —N═, etc.; and Y represents the formula —CO—, an optionally substituted amino, etc).
摘要翻译: 本次入院为勃起功能障碍提供补救措施。 其活性成分是由下式(I)表示的稠合哒嗪化合物或其药理学上可接受的盐:(其中环C表示任选具有杂原子的5或6元环; n为 1至4; R 1表示氢,卤素,氰基等; A表示氢,卤素,任选取代的氨基等; X表示由式-N =等表示的基团;和 Y表示式-CO-,任选取代的氨基等)。
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公开(公告)号:US5498634A
公开(公告)日:1996-03-12
申请号:US380589
申请日:1995-01-30
申请人: Yasuhiro Kabasawa , Fumihiro Ozaki , Keiji Ishibashi , Takashi Hasegawa , Hitoshi Oinuma , Toshiaki Ogawa , Hideyuki Adachi , Hiroshi Katoh , Kohtarou Kodama , Hideto Ohara , Nobuyuki Mori , Norio Minami
发明人: Yasuhiro Kabasawa , Fumihiro Ozaki , Keiji Ishibashi , Takashi Hasegawa , Hitoshi Oinuma , Toshiaki Ogawa , Hideyuki Adachi , Hiroshi Katoh , Kohtarou Kodama , Hideto Ohara , Nobuyuki Mori , Norio Minami
IPC分类号: C07D231/12 , C07D233/92 , C07D233/95 , C07D471/04 , A61K31/35 , C07D309/08
CPC分类号: C07D233/92 , C07D471/04
摘要: The present invention provides a thioformamide derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof, which is highly safe, easy to use, and useful as an excellent hypotensive or heart disease remedy: ##STR1## wherein Y represents ##STR2## or the like [wherein R.sup.7 represents benzyloxy or the like; R.sup.11 and R.sup.12 each represent hydrogen, hydroxyl, benzoyloxy, benzyloxy, ##STR3## (wherein R.sup.14 and R.sup.15 each represent hydrogen, benzyl or the like) or the like];Z represents --CH.sub.2 -- or the like; A represents imidazolyl or imidazopyridyl which may have one or two substituents, or the like; R.sup.1 and R.sup.2 each represent hydrogen, lower alkyl or the like; and R.sup.3 and R.sup.4 each represent hydrogen, lower alkyl or the like.
摘要翻译: 本发明提供由下列通式(I)表示的硫代甲酰胺衍生物或其药学上可接受的盐,其安全性高,易于使用,可用作优异的降血压或心脏病治疗药物:其中 Y表示
等[其中R7表示苄氧基等; R 11和R 12各自表示氢,羟基,苯甲酰氧基,苄氧基,(其中R 14和R 15各自表示氢,苄基等)等。 Z表示-CH 2 - 等; A表示可具有一个或两个取代基的咪唑基或咪唑并吡啶等; R 1和R 2各自表示氢,低级烷基等; R 3和R 4各自表示氢,低级烷基等。 -
公开(公告)号:US5444066A
公开(公告)日:1995-08-22
申请号:US211701
申请日:1994-04-26
申请人: Yasuhiro Kabasawa , Fumihiro Ozaki , Keiji Ishibashi , Takashi Hasegawa , Hitoshi Oinuma , Toshiaki Ogawa , Hideyuki Adachi , Hiroshi Katoh , Kohtarou Kodama , Hideto Ohara , Nobuyuki Mori , Norio Minami
发明人: Yasuhiro Kabasawa , Fumihiro Ozaki , Keiji Ishibashi , Takashi Hasegawa , Hitoshi Oinuma , Toshiaki Ogawa , Hideyuki Adachi , Hiroshi Katoh , Kohtarou Kodama , Hideto Ohara , Nobuyuki Mori , Norio Minami
IPC分类号: C07D231/12 , C07D233/92 , C07D233/95 , C07D471/04 , A61K31/435
CPC分类号: C07D233/92 , C07D471/04
摘要: The present invention provides a thioformamide derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof, which is highly safe, easy to use, and useful as an excellent hypotensive or heart disease remedy: ##STR1## wherein Y represents ##STR2## or the like [wherein R.sup.7 represents benzyloxy or the like; R.sup.11 and R.sup.12 each represent hydrogen, hydroxyl, benzoyloxy, benzyloxy, ##STR3## (wherein R.sup.14 and R.sup.15 each represent hydrogen, benzyl or the like) or the like];Z represents --CH.sub.2 -- or the like; A represents imidazolyl or imidazopyridyl which may have one or two substituents, or the like; R.sup.1 and R.sup.2 each represent hydrogen, lower alkyl or the like; and R.sup.3 and R.sup.4 each represent hydrogen, lower alkyl or the like.
摘要翻译: PCT No.PCT / JP92 / 01297 Sec。 371日期1994年04月26日 102(e)日期1994年4月26日PCT提交1992年10月6日PCT公布。 出版物WO93 / 08168 日本1994年4月29日。本发明提供由以下通式(I)表示的硫代甲酰胺衍生物或其药理学上可接受的盐,其是高度安全,易于使用的,并且可用作优异的降压药或心脏病药物: (I)其中Y表示酰氧基等; R 11和R 12各自表示氢,羟基,苯甲酰氧基,苄氧基,苯甲酰基等)等。 Z表示-CH 2 - 等; A表示可具有一个或两个取代基的咪唑基或咪唑并吡啶等; R 1和R 2各自表示氢,低级烷基等; R 3和R 4各自表示氢,低级烷基等。
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公开(公告)号:US5606061A
公开(公告)日:1997-02-25
申请号:US531335
申请日:1995-09-20
申请人: Yasuhiro Kabasawa , Fumihiro Ozaki , Keiji Ishibashi , Takashi Hasegawa , Hitoshi Oinuma , Toshiaki Ogawa , Hideyuki Adachi , Hiroshi Katoh , Kohtarou Kodama , Hideto Ohara , Nobuyuki Mori , Norio Minami
发明人: Yasuhiro Kabasawa , Fumihiro Ozaki , Keiji Ishibashi , Takashi Hasegawa , Hitoshi Oinuma , Toshiaki Ogawa , Hideyuki Adachi , Hiroshi Katoh , Kohtarou Kodama , Hideto Ohara , Nobuyuki Mori , Norio Minami
IPC分类号: C07D231/12 , C07D233/92 , C07D233/95 , C07D471/04
CPC分类号: C07D233/92 , C07D471/04
摘要: The present invention provides a thioformamide derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof, which is highly safe, easy to use, and useful as an excellent hypotensive or heart disease remedy: ##STR1## wherein Y represents ##STR2## or the like [wherein R.sup.7 represents benzyloxy or the like; R.sup.11 and R.sup.12 each represent hydrogen, hydroxyl, benzoyloxy, benzyloxy, ##STR3## (wherein R.sup.14 and R.sup.15 each represent hydrogen, benzyl or the like) or the like];Z represents --CH.sub.2 -- or the like; A represents imidazolyl or imidazopyridyl which may have one or two substituents, or the like; R.sup.1 and R.sup.2 each represent hydrogen, lower alkyl or the like; and R.sup.3 and R.sup.4 each represent hydrogen, lower alkyl or the like.
摘要翻译: 本发明提供由下列通式(I)表示的硫代甲酰胺衍生物或其药理学上可接受的盐,其是高度安全,易于使用的,并且可用作优异的降血压或心脏病治疗药物:其中 Y表示
等[其中R7表示苄氧基等; R 11和R 12各自表示氢,羟基,苯甲酰氧基,苄氧基,(其中R 14和R 15各自表示氢,苄基等)等。 Z表示-CH 2 - 等; A表示可具有一个或两个取代基的咪唑基或咪唑并吡啶等; R 1和R 2各自表示氢,低级烷基等; R 3和R 4各自表示氢,低级烷基等。 -
公开(公告)号:US20050208124A1
公开(公告)日:2005-09-22
申请号:US10506631
申请日:2003-03-11
申请人: Seiichi Araki , Mamoru Suzuki , Kohtarou Kodama , Toshio Toyosawa
发明人: Seiichi Araki , Mamoru Suzuki , Kohtarou Kodama , Toshio Toyosawa
IPC分类号: A61K31/525 , A61K31/675 , A61P1/16 , A61P1/18 , A61P9/00 , A61P9/10 , A61P17/02 , A61P29/00 , A61P37/00 , A61P43/00 , C07D475/14 , C07F9/6561 , A61K31/519
CPC分类号: C07F9/65618 , A61K31/525 , A61K31/675 , C07D475/14
摘要: A medicament is provided containing as an active ingredient at least one of riboflavin, a riboflavin derivative or a pharmacologically acceptable salt thereof, which has the action of suppressing IL-1β, IL-6, IL-10, INF-γ, TNF-α, GM-CSF, IL-8, MCP-1 and other cytokines. Moreover, a preventative or therapeutic agent for inflammatory diseases accompanied by hypercytokinemia is provided which has excellent cytokine suppression effect.
摘要翻译: 提供含有抑制IL-1β,IL-6,IL-10,INF-γ,TNF-α的作用的作为活性成分的至少一种核黄素,核黄素衍生物或其药理学上可接受的盐的药物 ,GM-CSF,IL-8,MCP-1和其他细胞因子。 此外,提供了具有优异的细胞因子抑制效果的伴有高细胞因子血症的炎性疾病的预防或治疗剂。
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