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11. 发明申请

US20050101634A1 Bis(5-aeyl-2-pyridyl) derivatives 失效
标题翻译：双（5-芳基-2-吡啶基）衍生物
公开(公告)号：US20050101634A1
公开(公告)日：2005-05-12
申请号：US10690671
申请日：2003-10-23
申请人： Hiroyuki Ishiwata , Seiichi Sato , Mototsugu Kabeya , Soichi Oda , Makoto Suda , Manabu Shibasaki
发明人： Hiroyuki Ishiwata , Seiichi Sato , Mototsugu Kabeya , Soichi Oda , Makoto Suda , Manabu Shibasaki
IPC分类号： A61P9/10 , A61P11/06 , A61P29/00 , A61P37/08 , A61P43/00 , C07D213/74 , C07D401/14 , C07D405/14 , C07D409/14 , C07D487/04 , A61K31/444
CPC分类号： C07D487/04 , C07D213/74 , C07D401/14 , C07D405/14 , C07D409/14
摘要： A bis(5-aryl-2-pyridyl) compound represented by formula (1) or a salt thereof: wherein A is a substituted or unsubstituted aromatic hydrocarbyl group or a substituted or unsubstituted aromatic heterocyclic group, and X is a group selected from the group consisting of moieties having formulas (2) to (5): wherein, in formula (2), m is an integer of 1 or 2; in formula (3), n is an integer of 1 to 6; and in formula (4), R is hydrogen or a lower alkyl group and p is an integer of 1 to 6.
摘要翻译：由式（1）表示的双（5-芳基-2-吡啶基）化合物或其盐：其中A是取代或未取代的芳族烃基或取代或未取代的芳族杂环基，X是选自由具有式（2）至（5）的部分组成的组：其中，在式（2）中，m为1或2的整数; 在式（3）中，n为1〜6的整数，在式（4）中，R为氢或低级烷基，p为1〜6的整数。

12. 发明授权

US06706703B2 Bis(5-aryl-2-pyridyl) derivatives 失效
标题翻译：双（5-芳基-2-吡啶基）衍生物
公开(公告)号：US06706703B2
公开(公告)日：2004-03-16
申请号：US09893698
申请日：2001-06-29
申请人： Hiroyuki Ishiwata , Seiichi Sato , Mototsugu Kabeya , Soichi Oda , Makoto Suda , Manabu Shibasaki
发明人： Hiroyuki Ishiwata , Seiichi Sato , Mototsugu Kabeya , Soichi Oda , Makoto Suda , Manabu Shibasaki
IPC分类号： C07D40104
CPC分类号： C07D487/04 , C07D213/74 , C07D401/14 , C07D405/14 , C07D409/14
摘要： A bis(5-aryl-2-pyridyl) compound represented by formula (1) or a salt thereof: wherein A is a substituted or unsubstituted aromatic hydrocarbon group or a substituted or unsubstituted aromatic heterocyclic group, and X is a group selected from the group consisting of moieties having formulas (2) to (5): wherein, in formula (2), m is an integer of 1 or 2; in formula (3), n is an integer of 1 to 6; and in formula (4), R is hydrogen or a lower alkyl group and p is an integer of 1 to 6.
摘要翻译：由式（1）表示的双（5-芳基-2-吡啶基）化合物或其盐：其中A是取代或未取代的芳族烃基或取代或未取代的芳族杂环基，X是选自由具有式（2）至（5）的部分组成的组：其中，在式（2）中，m为1或2的整数; 在式（3）中，n为1〜6的整数，在式（4）中，R为氢或低级烷基，p为1〜6的整数。

13. 发明授权

US06787653B2 Preparation process of biphenylcarboxylic acid amide derivatives 失效
标题翻译：联苯羧酸酰胺衍生物的制备方法
公开(公告)号：US06787653B2
公开(公告)日：2004-09-07
申请号：US10162602
申请日：2002-06-06
申请人： Hiroyuki Ishiwata , Seiichi Sato , Mototsugu Kabeya , Soichi Oda
发明人： Hiroyuki Ishiwata , Seiichi Sato , Mototsugu Kabeya , Soichi Oda
IPC分类号： C07D21126
CPC分类号： C07D295/192
摘要： A process for preparing a biphenylcarboxylic acid amide derivative represented by the following formula (1): wherein, R1, R2 and R3 each independently represents a hydrogen atom or a substituent, which comprises reacting, in the presence of a metal catalyst, a halogenobenzoic acid derivative represented by the following formula (2): wherein, X represents a halogen atom with a compound represented by the following formula (3): wherein, R1, R2 and R3 have the same meanings as described above, and Y represents an leaving group having an element selected from the group consisting of boron, silicon, zinc, tin and magnesium; or salt thereof. According to the present invention, biphenylcarboxylic acid amide derivatives of the formula (1) or salts thereof having excellent inhibitory activity against IgE antibody production can be prepared by the reduced number of steps, conveniently, at lower cost and in a high yield.
摘要翻译：一种制备由下式（1）表示的联苯羧酸酰胺衍生物的方法：其中R 1，R 2和R 3各自独立地表示氢原子或取代基，其包括在存在金属催化剂，由下式（2）表示的卤代苯甲酸衍生物：其中，X表示与下式（3）表示的化合物的卤素原子：其中，R 1，R 2和 R 3具有与上述相同的含义，Y表示具有选自硼，硅，锌，锡和镁的元素的离去基团; 或其盐。根据本发明，具有优异的抗IgE抗体产生抑制活性的式（1）的联苯基羧酸酰胺衍生物或其盐可以通过减少数量的步骤，以较低的成本和较高的成本产量。

14. 发明授权

US06645957B2 Cyclic amide compound 失效
标题翻译：环状酰胺化合物
公开(公告)号：US06645957B2
公开(公告)日：2003-11-11
申请号：US10173670
申请日：2002-06-19
申请人： Hiroyuki Ishiwata , Seiichi Sato , Mototsugu Kabeya , Soichi Oda , Yukio Hattori , Makoto Suda , Manabu Shibasaki , Hiroshi Nakao , Takao Nagoya
发明人： Hiroyuki Ishiwata , Seiichi Sato , Mototsugu Kabeya , Soichi Oda , Yukio Hattori , Makoto Suda , Manabu Shibasaki , Hiroshi Nakao , Takao Nagoya
IPC分类号： C07D20902
CPC分类号： C07D213/70 , C07C2601/14 , C07D211/26 , C07D211/34 , C07D211/58 , C07D213/38 , C07D213/82 , C07D295/185 , C07D295/192 , C07D401/14
摘要： The invention relates to compounds represented by the following general formula (1): wherein A is an aromatic compound which may be substituted, or the like, B is a nitrogen atom or CH, X is a lower alkylene group which may be substituted, or the like, Y is a single bond or the like; Z is a divalent residue of benzene which may be substituted, or the like, and m and n are independently an integer of 1 to 4, and medicines comprising such a compound. These compounds have an excellent inhibitory effect on the production of an IgE antibody and are hence useful as antiallergic agents and the like.
摘要翻译：本发明涉及由以下通式（1）表示的化合物：其中A是可被取代的芳族化合物等，B是氮原子或CH，X是可被取代的低级亚烷基，或类似物，Y是单键等; Z是可以被取代的苯的二价残基等，m和n分别是1〜4的整数，以及包含这种化合物的药物。这些化合物对IgE抗体的产生具有优异的抑制作用，因此可用作抗变应性剂等。

15. 发明授权

US06828316B2 Diamide compound and medicine containing the same 失效
标题翻译：二酰胺化合物和含有它的药物
公开(公告)号：US06828316B2
公开(公告)日：2004-12-07
申请号：US09978102
申请日：2001-10-17
申请人： Hiroyuki Ishiwata , Mototsugu Kabeya , Hiromichi Shigyo , Masami Shiratsuchi , Yukio Hattori , Hiroshi Nakao , Takao Nagoya , Seiichi Sato , Soichi Oda , Makoto Suda , Manabu Shibasaki
发明人： Hiroyuki Ishiwata , Mototsugu Kabeya , Hiromichi Shigyo , Masami Shiratsuchi , Yukio Hattori , Hiroshi Nakao , Takao Nagoya , Seiichi Sato , Soichi Oda , Makoto Suda , Manabu Shibasaki
IPC分类号： A61K3155
CPC分类号： C07D213/69 , C07D213/56 , C07D213/70 , C07D213/82 , C07D215/12 , C07D231/12 , C07D233/56 , C07D241/04 , C07D241/42 , C07D243/08 , C07D249/08 , C07D295/185 , C07D471/04 , C07D487/04
摘要： The present invention relates to diamide derivatives represented by the following general formula (1): wherein A is a phenyl group or the like, which may be substituted, B is —CH═CH—, —C≡C—, —(CH═CH)2—, —C≡C—CH═CH—, —CH═CH—C≡C—, phenylene or the like, and W is and medicines comprising such a compound. These compounds have an excellent inhibitory effect on the production of an IgE antibody and are hence useful as antiallergic agents and the like.
摘要翻译：本发明涉及由以下通式（1）表示的二酰胺衍生物：其中A是可被取代的苯基等，B是-CH = CH-，-C = C-， - （CH = CH）2 - ， - C = C-CH = CH - ， - CH = CH-C = C-，亚苯基等，W为包含这种化合物的药物。这些化合物对IgE抗体的产生具有优异的抑制作用，因此可用作抗变应性剂等。

16. 发明授权

US06340682B1 Diamide compound and drugs containing the same 失效
标题翻译：二酰胺化合物和含有相同药物
公开(公告)号：US06340682B1
公开(公告)日：2002-01-22
申请号：US09147711
申请日：1999-02-23
申请人： Hiroyuki Ishiwata , Mototsugu Kabeya , Hiromichi Shigyo , Masami Shiratsuchi , Yukio Hattori , Hiroshi Nakao , Takao Nagoya , Seiichi Sato , Soichi Oda , Makoto Suda , Manabu Shibasaki
发明人： Hiroyuki Ishiwata , Mototsugu Kabeya , Hiromichi Shigyo , Masami Shiratsuchi , Yukio Hattori , Hiroshi Nakao , Takao Nagoya , Seiichi Sato , Soichi Oda , Makoto Suda , Manabu Shibasaki
IPC分类号： A61K31495
CPC分类号： C07D213/69 , C07D213/56 , C07D213/70 , C07D213/82 , C07D215/12 , C07D231/12 , C07D233/56 , C07D241/04 , C07D241/42 , C07D243/08 , C07D249/08 , C07D295/185 , C07D471/04 , C07D487/04
摘要： The present invention provides diamide derivatives represented by the following general formula (1): wherein A is a phenyl group or the like, which may be substituted, B is —CH═CH—, —C═C—, —(CH═CH)2—, —C≡C—CH═CH—, —CH═CH—C≡C—, phenylene or the like, and W is or and medicines comprising such a compound. These compounds have an excellent inhibitory effect on the production of an IgE antibody and are hence useful as antiallergic agents and the like.
摘要翻译：本发明提供由以下通式（1）表示的二酰胺衍生物：其中A是可以被取代的苯基等，B是-CH = CH-，-C = C-， - （CH = CH ）2-，-C = C-CH = CH-，-CH = CH-C = C-，亚苯基等，以及含有这种化合物的W异构体药物。这些化合物对IgE抗体的产生具有优异的抑制作用，因此可用作抗变应性剂等。

17. 发明授权

US06297283B1 Diamide compounds and compositions containing the same 失效
标题翻译：二酰胺化合物和含有它们的组合物
公开(公告)号：US06297283B1
公开(公告)日：2001-10-02
申请号：US09269764
申请日：1999-04-09
申请人： Hiroyuki Ishiwata , Mototsugu Kabeya , Masami Shiratsuchi , Yukio Hattori , Hiroshi Nakao , Takao Nagoya , Seiichi Sato , Soichi Oda , Makoto Suda , Manabu Shibasaki
发明人： Hiroyuki Ishiwata , Mototsugu Kabeya , Masami Shiratsuchi , Yukio Hattori , Hiroshi Nakao , Takao Nagoya , Seiichi Sato , Soichi Oda , Makoto Suda , Manabu Shibasaki
IPC分类号： A61K31165
CPC分类号： C07D213/40 , C07C235/34 , C07C235/36 , C07C235/38 , C07C235/44 , C07C235/56 , C07C237/34 , C07C2601/14 , C07C2602/08 , C07C2602/10 , C07D207/09 , C07D207/14 , C07D213/75 , C07D213/82
摘要： The present invention relates to compounds represented by the following general formula (1): wherein A is a phenyl, naphthyl, dihydronaphthyl, indenyl, pyridyl, indolyl, isoindolyl, quinolyl or isoquinolyl group which may be substituted; X is a lower alkylene group which may be substituted, or the like; Y is a single bond or an alkylene group; Z is a group of —CH═CH—, —C≡C—, —(CH═CH)2—, —C≡C—CH═CH— or —CH═CH—C≡C—, or the like; and R is a hydrogen atom, a lower alkyl group or the like, and medicines comprising such a compound. These compounds have an excellent inhibitory effect on the production of an IgE antibody and are hence useful as antiallergic agents and the like.
摘要翻译：本发明涉及由以下通式（1）表示的化合物：其中A为可被取代的苯基，萘基，二氢萘基，茚基，吡啶基，吲哚基，异吲哚基，喹啉基或异喹啉基; X是可以被取代的低级亚烷基等; Y是单键或亚烷基; Z是-CH = CH-，-C = C - ， - （CH = CH）2 - ， - C = C-CH = CH-或-CH = CH-C = C - 等的基团; R为氢原子，低级烷基等，以及含有该化合物的药物。这些化合物对IgE抗体的产生具有优异的抑制作用，因此可用作抗变应性剂等。

18. 发明授权

US07423009B2 Method for treatment of kidney diseases 失效
标题翻译：肾脏疾病治疗方法
公开(公告)号：US07423009B2
公开(公告)日：2008-09-09
申请号：US10673380
申请日：2003-09-30
申请人： Takashi Nakagawa , Hiroyuki Ishiwata , Toshiaki Takizawa , Toru Kanke , Yasushi Wada , Junichi Kawagoe
发明人： Takashi Nakagawa , Hiroyuki Ishiwata , Toshiaki Takizawa , Toru Kanke , Yasushi Wada , Junichi Kawagoe
IPC分类号： A61K38/00 , A61K38/43 , A61K38/48
CPC分类号： A61K38/4846 , A61K38/08 , A61K38/482 , A61K38/4826 , G01N33/6893 , G01N2500/00 , G01N2800/347
摘要： The present invention relates to a composition for prevention and treatment of kidney diseases comprising one or more effective component(s) of a PAR-2 activating agent which is able to activate PAR-2 and a pharmaceutically acceptable carrier. The present invention further relates to a method for prevention and treatment of kidney diseases comprising administration of a composition for prevention and treatment of kidney diseases containing a PAR-2 activating agent which is able to activate PAR-2 to patients suffering from kidney diseases, and also relates to the use of a PAR-2 activating agent which is able to activate PAR-2 for the manufacture of a composition for prevention and treatment of kidney diseases. The present invention furthermore relates to a method for screening an effective ingredient for prevention and treatment of kidney diseases comprising screening of the activating action of the test substance to PAR-2.
摘要翻译：本发明涉及一种用于预防和治疗肾脏疾病的组合物，其包含能够激活PAR-2的PAR-2活化剂的一种或多种有效成分和药学上可接受的载体。本发明还涉及一种用于预防和治疗肾脏疾病的方法，其包括给予含有能够使患有肾脏疾病的患者PAR-2的PAR-2激活剂的肾脏疾病的预防和治疗组合物，以及还涉及能够激活PAR-2用于制备用于预防和治疗肾脏疾病的组合物的PAR-2活化剂的用途。本发明还涉及筛选用于预防和治疗肾脏疾病的有效成分的方法，其包括将测试物质的活化作用筛选到PAR-2。

19. 发明授权

US08791090B2 Prophylactic and/or therapeutic agent for anemia comprising tetrahydroquinoline compound as active ingredient 有权
标题翻译：含有四氢喹啉化合物作为活性成分的贫血的预防和/或治疗剂
公开(公告)号：US08791090B2
公开(公告)日：2014-07-29
申请号：US13256549
申请日：2010-03-31
申请人： Masanori Ashikawa , Junya Tagashira , Akiyasu Koketsu , Toshiharu Morimoto , Takahiro Kitamura , Syunji Takemura , Gen Watanabe , Tatsuaki Nishiyama , Satoshi Goda , Masaki Yamabi , Takeshi Doi , Hiroyuki Ishiwata
发明人： Masanori Ashikawa , Junya Tagashira , Akiyasu Koketsu , Toshiharu Morimoto , Takahiro Kitamura , Syunji Takemura , Gen Watanabe , Tatsuaki Nishiyama , Satoshi Goda , Masaki Yamabi , Takeshi Doi , Hiroyuki Ishiwata
IPC分类号： A01N57/00 , A61K31/385
CPC分类号： C07D215/42 , A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/69 , C07D215/233 , C07D215/44 , C07D215/46 , C07D215/48 , C07D401/04 , C07D401/12 , C07D405/12 , C07D413/04 , C07D413/12 , C07D417/12
摘要： Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin. Specifically disclosed is and EPO production enhancer and/or a hemoglobin production enhancer comprising a 1-acyl-4-(substituted oxy, substituted amino, or substituted thio)-1,2,3,4-tetrahydroquinoline derivative, more specifically a tetrahydroquinoline compound represented by general formula (1) [wherein R1, R2, R2′, R3 and R3′ independently represent a hydrogen atom, a C1-6 alkyl group, or the like; R4, R5, R6, R7, R8, R9 and R10 independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, or the like; A represents N—R11, a sulfur atom, or an oxygen atom; R11 represents a hydrogen atom, a C1-6 alkyl group, or the like; B represents a C6-14 aryl group, or a 5- to 10-membered heterocyclic group; and n represents an integer of 0 or 1], a salt of the tetrahydroquinoline compound, or a solvate of the tetrahydroquinoline compound or the salt.
摘要翻译：公开了具有低分子量且具有增强EPO产生活性和/或提高血红蛋白生成活性的化合物。具体公开的是EPO生产增强剂和/或包含1-酰基-4-（取代的氧基，取代的氨基或取代的硫代）-1,2,3,4-四氢喹啉衍生物，更具体地是四氢喹啉化合物的血红蛋白生成增强剂由通式（1）表示[其中R1，R2，R2'，R3和R3'独立地表示氢原子，C1-6烷基等; R 4，R 5，R 6，R 7，R 8，R 9和R 10独立地表示氢原子，卤素原子，C 1-6烷基等; A表示N-R11，硫原子或氧原子; R 11表示氢原子，C 1-6烷基等; B表示C 6-14芳基或5至10元杂环基; n表示0或1的整数]，四氢喹啉化合物的盐或四氢喹啉化合物或其盐的溶剂合物。

20. 发明申请

US20120004197A1 PROPHYLACTIC AND/OR THERAPEUTIC AGENT FOR ANEMIA COMPRISING TETRAHYDROQUINOLINE COMPOUND AS ACTIVE INGREDIENT 有权
标题翻译：用于包含四氢喹啉化合物的抗坏血酸和/或治疗药物作为活性成分
公开(公告)号：US20120004197A1
公开(公告)日：2012-01-05
申请号：US13256549
申请日：2010-03-31
申请人： Masanori Ashikawa , Junya Tagashira , Akiyasu Koketsu , Toshiharu Morimoto , Takahiro Kitamura , Syunji Takemura , Gen Watanabe , Tatsuaki Nishiyama , Satoshi Goda , Masaki Yamabi , Takeshi Doi , Hiroyuki Ishiwata
发明人： Masanori Ashikawa , Junya Tagashira , Akiyasu Koketsu , Toshiharu Morimoto , Takahiro Kitamura , Syunji Takemura , Gen Watanabe , Tatsuaki Nishiyama , Satoshi Goda , Masaki Yamabi , Takeshi Doi , Hiroyuki Ishiwata
IPC分类号： A61K31/4706 , C07D413/12 , C07D215/14 , C07D215/233 , C07D401/12 , A61P7/06 , C07D413/14 , A61K31/5377 , A61K31/47 , A61K31/496 , A61K31/69 , C07D215/44 , C07F5/02
CPC分类号： C07D215/42 , A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/496 , A61K31/5377 , A61K31/69 , C07D215/233 , C07D215/44 , C07D215/46 , C07D215/48 , C07D401/04 , C07D401/12 , C07D405/12 , C07D413/04 , C07D413/12 , C07D417/12
摘要： Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin. Specifically disclosed is and EPO production enhancer and/or a hemoglobin production enhancer comprising a 1-acyl-4-(substituted oxy, substituted amino, or substituted thio)-1,2,3,4-tetrahydroquinoline derivative, more specifically a tetrahydroquinoline compound represented by general formula (1) [wherein R1, R2, R2′, R3 and R3′ independently represent a hydrogen atom, a C1-6 alkyl group, or the like; R4, R5, R6, R7, R8, R9 and R10 independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, or the like; A represents N—R11, a sulfur atom, or an oxygen atom; R11 represents a hydrogen atom, a C1-6 alkyl group, or the like; B represents a C6-14 aryl group, or a 5- to 10-membered heterocyclic group; and n represents an integer of 0 or 1], a salt of the tetrahydroquinoline compound, or a solvate of the tetrahydroquinoline compound or the salt.
摘要翻译：公开了具有低分子量且具有增强EPO产生活性和/或提高血红蛋白生成活性的化合物。具体公开的是EPO生产增强剂和/或包含1-酰基-4-（取代的氧基，取代的氨基或取代的硫代）-1,2,3,4-四氢喹啉衍生物，更具体地是四氢喹啉化合物的血红蛋白生成增强剂由通式（1）表示[其中R1，R2，R2'，R3和R3'独立地表示氢原子，C1-6烷基等; R 4，R 5，R 6，R 7，R 8，R 9和R 10独立地表示氢原子，卤素原子，C 1-6烷基等; A表示N-R11，硫原子或氧原子; R 11表示氢原子，C 1-6烷基等; B表示C 6-14芳基或5至10元杂环基; n表示0或1的整数]，四氢喹啉化合物的盐或四氢喹啉化合物或其盐的溶剂合物。

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