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1. 发明申请

US20120108581A1 FUSED PIPERIDINE COMPOUND AND PHARMACEUTICAL CONTAINING SAME 失效
标题翻译：熔融哌啶化合物和含有药物的化合物
公开(公告)号：US20120108581A1
公开(公告)日：2012-05-03
申请号：US13260711
申请日：2010-03-25
申请人： Masanori Ashikawa , Toshiharu Morimoto , Hajime Yamada , Shunji Takemura , Tatsuaki Nishiyama , Takeshi Doi , Hiroyuki Ishiwata
发明人： Masanori Ashikawa , Toshiharu Morimoto , Hajime Yamada , Shunji Takemura , Tatsuaki Nishiyama , Takeshi Doi , Hiroyuki Ishiwata
IPC分类号： A61K31/473 , A61K31/4375 , C12N5/02 , C07D495/04 , A61K31/4365 , A61P7/06 , A61K31/4745 , C07D491/052 , A61K31/4741 , C07D491/056 , C07D498/04 , A61K31/5383 , C07D471/04 , C07D221/10
CPC分类号： C07D221/06 , C07D471/04 , C07D491/052 , C07D491/056 , C07D498/04
摘要： The present invention provides a low molecular weight compound having EPO production-promoting action and/or hemoglobin production-promoting action. The present invention relates to a fused piperidine compound represented by the following general formula (1): (wherein, ring A represents a C10-14 aryl group or 5- to 10-membered heterocyclic group, X represents N—R7, a sulfur atom or an oxygen atom, R1, R2, R2′, R3 and R3′ independently represent a hydrogen atom, C1-6 alkyl group or C3-6 cycloalkyl group, and R4, R5 and R6 independently represent a hydrogen atom or halogen atom), or a salt thereof, or a solvate thereof.
摘要翻译：本发明提供具有EPO生产促进作用和/或血红蛋白生产促进作用的低分子量化合物。本发明涉及由以下通式（1）表示的稠合哌啶化合物：其中环A表示C10-14芳基或5-至10-元杂环基，X表示N-R7，硫原子或氧原子，R 1，R 2，R 2'，R 3和R 3'独立地表示氢原子，C 1-6烷基或C 3-6环烷基，R 4，R 5和R 6独立地表示氢原子或卤素原子）或其盐，或其溶剂合物。

2. 发明授权

US08604030B2 Fused piperidine compound and pharmaceutical containing same 失效
标题翻译：融合哌啶化合物和含有其的药物
公开(公告)号：US08604030B2
公开(公告)日：2013-12-10
申请号：US13260711
申请日：2010-03-25
申请人： Masanori Ashikawa , Toshiharu Morimoto , Hajime Yamada , Shunji Takemura , Tatsuaki Nishiyama , Takeshi Doi , Hiroyuki Ishiwata
发明人： Masanori Ashikawa , Toshiharu Morimoto , Hajime Yamada , Shunji Takemura , Tatsuaki Nishiyama , Takeshi Doi , Hiroyuki Ishiwata
IPC分类号： A61K31/5377 , A61K31/4706 , A61K31/47 , C07D215/08 , C07D413/12 , C07D215/233
CPC分类号： C07D221/06 , C07D471/04 , C07D491/052 , C07D491/056 , C07D498/04
摘要： The present invention provides a low molecular weight compound having EPO production-promoting action and/or hemoglobin production-promoting action. The present invention relates to a fused piperidine compound represented by the following general formula (1): (wherein, ring A represents a C10-14 aryl group or 5- to 10-membered heterocyclic group, X represents N—R7, a sulfur atom or an oxygen atom, R1, R2, R2′, R3 and R3′ independently represent a hydrogen atom, C1-6 alkyl group or C3-6 cycloalkyl group, and R4, R5 and R6 independently represent a hydrogen atom or halogen atom), or a salt thereof, or a solvate thereof.
摘要翻译：本发明提供具有EPO生产促进作用和/或血红蛋白生产促进作用的低分子量化合物。本发明涉及由以下通式（1）表示的稠合哌啶化合物：其中环A表示C10-14芳基或5-至10-元杂环基，X表示N-R7，硫原子或氧原子，R 1，R 2，R 2'，R 3和R 3'独立地表示氢原子，C 1-6烷基或C 3-6环烷基，R 4，R 5和R 6独立地表示氢原子或卤素原子）或其盐，或其溶剂合物。

3. 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。

4. 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。

5. 发明申请

US20100222347A1 PROPHYLACTIC AND/OR THERAPEUTIC AGENT FOR ANEMIA, COMPRISING TETRAHYDROQUINOLINE COMPOUND AS ACTIVE INGREDIENT 审中-公开
标题翻译：抗坏血酸和/或治疗药物，包括作为活性成分的四氢喹啉化合物
公开(公告)号：US20100222347A1
公开(公告)日：2010-09-02
申请号：US12680307
申请日：2008-09-29
申请人： Masanori Ashikawa , Junya Tagashira , Akiyasu Koketsu , Toshiharu Morimoto , Tatsuaki Nishiyama , Satoshi Goda , Masaki Yamabi , Takeshi Doi , Hiroyuki Ishiwata
发明人： Masanori Ashikawa , Junya Tagashira , Akiyasu Koketsu , Toshiharu Morimoto , Tatsuaki Nishiyama , Satoshi Goda , Masaki Yamabi , Takeshi Doi , Hiroyuki Ishiwata
IPC分类号： A61K31/5377 , C07D215/08 , A61K31/4706 , C07D413/12 , C07D215/233 , A61K31/47 , A61P7/00
CPC分类号： C07D215/48 , A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/496 , A61K31/5377 , C07D215/22 , C07D215/44 , C07D413/04 , C07D413/12
摘要： Disclosed is a low-molecular-weight compound having an EPO production-promoting activity and/or a hemoglobin expression-enhancing activity. Specifically disclosed is an EPO production promoter and/or a hemoglobin expression enhancer comprising a 1-acyl-4-(phenoxy, benzyloxy or phenylamino)-1,2,3,4-tetrahydroquinoline derivative, more specifically a tetrahydroquinoline compound represented by the 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 or an oxygen atom; R11 represents a hydrogen atom, a C1-6 alkyl group, or the like; 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EPO生产促进活性和/或血红蛋白表达增强活性的低分子量化合物。具体公开的是EPO生产促进剂和/或血红蛋白表达增强剂，其包含1-酰基-4-（苯氧基，苄氧基或苯基氨基）-1,2,3,4-四氢喹啉衍生物，更具体地是由通式公式1）; [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或氧原子; R 11表示氢原子，C 1-6烷基等; 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。

6. 发明申请

US20110237590A1 PYRIDINE-3-CARBOXYAMIDE DERIVATIVE 有权
标题翻译：吡啶-3-羧酰胺衍生物
公开(公告)号：US20110237590A1
公开(公告)日：2011-09-29
申请号：US13131561
申请日：2009-11-27
申请人： Takahiro Kitamura , Hajime Yamada , Shunji Takemura , Masanori Ashikawa , Tetsuya Ishikawa , Yoshiharu Miyake , Akiyasu Kouketsu , Seiichi Sato , Hiroyuki Ishiwata , Yuichiro Tabunoki , Manabu Shibasaki , Takatoshi Ozawa , Ryota Shigemi , Takeshi Doi , Masahiro Tamura
发明人： Takahiro Kitamura , Hajime Yamada , Shunji Takemura , Masanori Ashikawa , Tetsuya Ishikawa , Yoshiharu Miyake , Akiyasu Kouketsu , Seiichi Sato , Hiroyuki Ishiwata , Yuichiro Tabunoki , Manabu Shibasaki , Takatoshi Ozawa , Ryota Shigemi , Takeshi Doi , Masahiro Tamura
IPC分类号： A61K31/5377 , C07D213/74 , C07D401/12 , C07D413/12 , C07D211/46 , A61K31/44 , A61K31/497 , A61K31/4545 , A61P37/02 , A61P37/06
CPC分类号： C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/12 , C07D417/12
摘要： To provide a novel JAK3 inhibitor that is useful as a preventive and/or therapeutic agent for rejection and graft versus host disease (GvHD) in organ transplantation, rheumatoid arthritis, multiple sclerosis, systemic lupus erythematosus, Sjögren syndrome, Behcet's disease, type I diabetes mellitus, autoimmune thyroiditis, idiopathic thrombocytopenic purpura, ulcerative colitis, Crohn's disease, asthma, allergic rhinitis, atopic dermatitis, contact dermatitis, urticaria, eczema, psoriasis, allergic conjunctivitis, uveitis, cancer, leukemia and the like. The pyridine-3-carboxyamide derivative represented by the general formula (1): or its salt or a solvate thereof.
摘要翻译：提供可用作器官移植，类风湿关节炎，多发性硬化症，系统性红斑狼疮，Sjögren综合征，Behcet氏病，I型糖尿病的排斥反应和宿主疾病（GvHD）的预防和/或治疗剂的新型JAK3抑制剂过敏性甲状腺炎，特发性血小板减少性紫癜，溃疡性结肠炎，克罗恩病，哮喘，过敏性鼻炎，特应性皮炎，接触性皮炎，荨麻疹，湿疹，牛皮癣，过敏性结膜炎，葡萄膜炎，癌症，白血病等。由通式（1）表示的吡啶-3-甲酰胺衍生物或其盐或其溶剂合物。

7. 发明授权

US08575153B2 Pyridine-3-carboxyamide derivative 有权
标题翻译：吡啶-3-甲酰胺衍生物
公开(公告)号：US08575153B2
公开(公告)日：2013-11-05
申请号：US13131561
申请日：2009-11-27
申请人： Takahiro Kitamura , Hajime Yamada , Shunji Takemura , Masanori Ashikawa , Tetsuya Ishikawa , Yoshiharu Miyake , Akiyasu Kouketsu , Seiichi Sato , Hiroyuki Ishiwata , Yuichiro Tabunoki , Manabu Shibasaki , Takatoshi Ozawa , Ryota Shigemi , Takeshi Doi , Masahiro Tamura
发明人： Takahiro Kitamura , Hajime Yamada , Shunji Takemura , Masanori Ashikawa , Tetsuya Ishikawa , Yoshiharu Miyake , Akiyasu Kouketsu , Seiichi Sato , Hiroyuki Ishiwata , Yuichiro Tabunoki , Manabu Shibasaki , Takatoshi Ozawa , Ryota Shigemi , Takeshi Doi , Masahiro Tamura
IPC分类号： A61K31/506 , C07D239/48
CPC分类号： C07D213/82 , C07D401/12 , C07D401/14 , C07D405/12 , C07D413/12 , C07D417/12
摘要： To provide a novel JAK3 inhibitor that is useful as a preventive and/or therapeutic agent for rejection and graft versus host disease (GvHD) in organ transplantation, rheumatoid arthritis, multiple sclerosis, systemic lupus erythematosus, Sjögren syndrome, Behcet's disease, type I diabetes mellitus, autoimmune thyroiditis, idiopathic thrombocytopenic purpura, ulcerative colitis, Crohn's disease, asthma, allergic rhinitis, atopic dermatitis, contact dermatitis, urticaria, eczema, psoriasis, allergic conjunctivitis, uveitis, cancer, leukemia and the like. The pyridine-3-carboxyamide derivative represented by the general formula (1): or its salt or a solvate thereof.
摘要翻译：提供可用作器官移植，类风湿关节炎，多发性硬化症，系统性红斑狼疮，Sjögren综合征，Behcet氏病，I型糖尿病的排斥反应和宿主疾病（GvHD）的预防和/或治疗剂的新型JAK3抑制剂过敏性甲状腺炎，特发性血小板减少性紫癜，溃疡性结肠炎，克罗恩病，哮喘，过敏性鼻炎，特应性皮炎，接触性皮炎，荨麻疹，湿疹，牛皮癣，过敏性结膜炎，葡萄膜炎，癌症，白血病等。由通式（1）表示的吡啶-3-甲酰胺衍生物或其盐或其溶剂化物。

8. 发明授权

US08133864B2 PAR-2 agonist 失效
标题翻译： PAR-2激动剂
公开(公告)号：US08133864B2
公开(公告)日：2012-03-13
申请号：US11909931
申请日：2006-03-29
申请人： Hiroyuki Ishiwata , Mototsugu Kabeya , Toru Kanke
发明人： Hiroyuki Ishiwata , Mototsugu Kabeya , Toru Kanke
IPC分类号： A61K38/08 , C07K5/083 , C07K5/087
CPC分类号： C07K5/0812 , A61K38/00 , C07K5/101 , C07K5/1016
摘要： The present invention relates to a pharmaceutical composition for preventing/treating conditions associated with PAR-2. The present invention also relates to a method for preventing/treating the condition using the pharmaceutical composition and use for manufacturing the pharmaceutical composition. The pharmaceutical composition comprises a compound represented by the following general formula (1), salt or solvate thereof and a pharmaceutically acceptable carrier: Ar—CO—AA1—AA2—AA3—AA4—NH—X—Y (1) wherein, Ar represents a phenyl group or an aromatic heterocyclic group optionally having substituent(s): AA1 represents a hydrophobic amino acid: AA2 represents an amino acid absent of substituent(s) having more than two carbon atoms: AA3 represents an amino acid absent of substituent(s) having more than two carbon atoms: AA4 represents a basic amino acid: X represents a straight chain or branched bivalent saturated aliphatic hydrocarbon group having 1 to 6 carbon atoms: Y represents basic substituent(s); straight chain, branched, or cyclic bivalent saturated aliphatic hydrocarbon group having 1 to 6 carbon atoms; or an aromatic hydrocarbon group having 6 to 10 carbon atoms. The compound represented by the general formula (1) has dramatically improved PAR-2 activation potency compared to peptide comprised of 6 amino acids (Tethered receptor agonist peptide: TRAP) in spite of reduction of the number of amino acid.
摘要翻译：本发明涉及用于预防/治疗与PAR-2相关的病症的药物组合物。本发明还涉及使用药物组合物预防/治疗病症的方法以及用于制造药物组合物的方法。药物组合物包含由以下通式（1）表示的化合物，其盐或溶剂合物和药学上可接受的载体：Ar-CO-AA1-AA2-AA3-AA4-NH-X-Y（1）其中Ar表示任选具有取代基的苯基或芳族杂环基：AA1表示疏水性氨基酸：AA2表示不具有多于两个碳原子的取代基的氨基酸：AA3表示不存在取代基的氨基酸（s ）：AA4表示碱性氨基酸：X表示具有1〜6个碳原子的直链或支链二价饱和脂肪族烃基：Y表示碱性取代基; 具有1至6个碳原子的直链，支链或环状二价饱和脂族烃基; 或碳原子数为6〜10的芳香族烃基。尽管氨基酸数量的减少，但由通式（1）表示的化合物与包含6个氨基酸的肽（束缚受体激动剂肽：TRAP）相比，显着提高了PAR-2的活化效力。

9. 发明申请

US20090012006A1 Par-2 Antagonists 失效
标题翻译： Par-2拮抗剂
公开(公告)号：US20090012006A1
公开(公告)日：2009-01-08
申请号：US11576304
申请日：2005-09-30
申请人： Mototsugu Kabeya , Kyoko Yasuoka , Toru Kanke , Hiroyuki Ishiwata , Junya Tagashira
发明人： Mototsugu Kabeya , Kyoko Yasuoka , Toru Kanke , Hiroyuki Ishiwata , Junya Tagashira
IPC分类号： A61K38/06 , C07K5/083 , A61P35/00 , A61P11/06
CPC分类号： C07K5/0827 , A61K38/00 , C07D209/14 , C07K5/0806 , C07K5/0812
摘要： Compounds represented by the general formula (1) or salts thereof or solvates of both; PAR-2 antagonists containing the compounds; and preventive or therapeutic agents for PAR-2 related diseases containing the antagonists as the active ingredient: (1) wherein R1 is hydrogen, halogeno, or a group represented by the general formula (2): (wherein R11 is straight-chain or branched C1-6 alkylene or the like; and R12 and R13 together with the nitrogen atom adjacent to them form a 5- to 7-membered ring); R2 is straight-chain or branched C1-6 alkyl or the like; R3 and R4 are each independently hydrogen, one to three halogen atoms, or the like; and A1-A2-A3 is a tripeptide residue composed of α-amino acids each independently selected from the group consisting of glycine, alanine, cyclohexylalanine, and so on.
摘要翻译：由通式（1）表示的化合物或其盐或两者的溶剂合物; 含有这些化合物的PAR-2拮抗剂; 以及含有拮抗剂作为活性成分的PAR-2相关疾病的预防或治疗剂：（1）其中R1是氢，卤素或由通式（2）表示的基团：（其中R11是直链或支链的 C 1-6亚烷基等; R 12和R 13与它们相邻的氮原子一起形成5-至7-元环）; R2是直链或支链C 1-6烷基等; R3和R4各自独立地为氢，一至三个卤素原子等; 并且A1-A2-A3是由各自独立地选自甘氨酸，丙氨酸，环己基丙氨酸等的α-氨基酸组成的三肽残基。

10. 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。

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