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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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公开(公告)号:US20070054876A1
公开(公告)日:2007-03-08
申请号:US11594132
申请日:2006-11-08
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: A61K31/7076 , A61K31/522
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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43.
公开(公告)号:US07160892B2
公开(公告)日:2007-01-09
申请号:US10492547
申请日:2002-10-22
申请人: Hitoshi Harada , Osamu Asano , Masato Ueda , Shuhei Miyazawa , Yoshihiko Kotake , Yasuhiro Kabasawa , Masahiro Yasuda , Nobuyuki Yasuda
发明人: Hitoshi Harada , Osamu Asano , Masato Ueda , Shuhei Miyazawa , Yoshihiko Kotake , Yasuhiro Kabasawa , Masahiro Yasuda , Nobuyuki Yasuda
IPC分类号: A61K31/5377 , A61K31/513 , C07D417/02 , C07D413/02 , C07D43/02
CPC分类号: C07D239/34 , A61K31/513
摘要: The invention provides novel pyrimidone compounds exhibiting excellent antagonism against adenosine receptors (A1, A2A, and A2B receptors), particularly, compounds represented by the general formula (1), salts thereof, or solvates of both: (1) wherein R1 and R2 are each independently hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, a 5- to 14-membered nonaromatic heterocyclic group, a C6-14 aromatic hydrocarbon group, a 5- to 14-membered aromatic heterocyclic group, C1-6 acyl, or C1-6 alkylsulfonyl; R3 is hydrogen, C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl; R4 is a C6-14 aromatic hydrocarbon group; a 5- to 14-membered aromatic heterocyclic group, or a 5- to 14-membered nonaromatic heterocyclic group having at least one unsaturated bond; and R5 is a C6-14 aromatic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group (with the proviso that every group except hydrogen may be substituted).
摘要翻译: 本发明提供了对腺苷受体(A 1 SUB,A 2A和A 2B 2受体)表现出优异拮抗作用的新型嘧啶酮化合物,特别是表示的化合物 通式(1)表示的盐,其盐或两者的溶剂合物:(1)其中R 1和R 2各自独立地为氢,C 1〜 C 1-6烷基,C 2-6链烯基,C 2-6炔基,C 3-8环烷基,C 1 -C 6 - 3-8环烯基,5至14元非芳族杂环基,C 6-14芳族烃基,5至14元芳族杂环基,C 1-6酰基或C 1-6烷基磺酰基; R 3是氢,C 1-6烷基,C 2-6链烯基或C 2-6亚烷基, 炔基; R 4是C 6-14芳族烃基; 5至14元芳族杂环基或具有至少一个不饱和键的5至14元非芳族杂环基; 和R 5是C 6-14芳族烃基或5至14元芳族杂环基(条件是除了氢以外的每个基团可以被取代) 。
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公开(公告)号:US20060270674A1
公开(公告)日:2006-11-30
申请号:US11500903
申请日:2006-08-09
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: A61K31/5377 , A61K31/506 , C07D413/14 , C07D403/14
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 A2receptor 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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45.
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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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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