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1. 发明专利

JP2012167075A METHOD OF MANUFACTURING AND PURIFYING 5-NITROGEN-CONTAINING UNSATURATED HETEROCYCLIC RING-SUBSTITUTED BENZO [a] PHENOXATHINS OR THEIR SALTS 审中-公开
标题翻译：制备和纯化含5-氮杂环辛烷基环取代苯并[a]苯并噻唑或其盐的方法
公开(公告)号：JP2012167075A
公开(公告)日：2012-09-06
申请号：JP2011043001
申请日：2011-02-10
申请人： Synstar Japan Co Ltd , 株式会社シンスター・ジャパン
发明人： ITO ISAMU , IHARA MASATAKA
IPC分类号： C07D265/34 , C07B61/00
摘要： PROBLEM TO BE SOLVED: To provide a method of manufacturing and purifying 5-nitrogen-containing unsaturated heterocyclic ring-substituted iminobenzo [a] phenoxathins or their salts, industrially, at a high yield, at a low cost, and in a manner where the amount of remaining platinum group element catalyst is small.SOLUTION: This method of manufacturing and purifying the compound represented by general formula (III) includes a means of: making 5-iminobenzo [a] phenoxathins or their salts react with nitrogen-containing heterocyclic compound having a leaving group in the existence of platinum group element catalyst, ligand, and base; and removing the remaining platinum group element catalyst after the completion of the reaction. In the formula, Rand Rindependently show a hydrogen atom, alkyl group, alkenyl group, aryl group, heterocyclic group, alkylcarbonyl group, alkoxycarbonyl group, alkylsulfonyl group, or arylsulfonyl group; R, R, Rand Rindependently show a hydrogen atom or substituent; Rand R, Rand R, and Rand Rmay be combined with each other to form 5-member, 6-member, and 7-member ring; n shows 0, 1 or 2; Rmay be the same or different when n shows 2; and Z shows a nitrogen-containing unsaturated heterocyclic residue of 5-member or 6-member.
摘要翻译：待解决的问题：提供在工业上以低成本和低成本的方式制备和纯化5-氮杂不饱和杂环环取代的亚氨基苯并[a]吩恶嗪[或其盐]的方法剩余的铂族元素催化剂的量少的方式。解决方案：制备和纯化由通式（III）表示的化合物的方法包括：使5-亚氨基苯并[a]吩恶嗪素或其盐与存在的具有离去基团的含氮杂环化合物反应的方法的铂族元素催化剂，配体和碱; 并在反应完成后除去剩余的铂族元素催化剂。在该式中，R 1 和R 2 独立地表示氢原子，烷基，烯基，芳基，杂环基，烷基羰基，烷氧基羰基，烷基磺酰基或芳基磺酰基; R 3 ，R 4 ，R 5 ，R 6 独立地表示氢原子或取代基; R 1 和R 2 ，R 1 ，R 3 ，并且R 2 和R 5 可以彼此组合以形成5- 会员6人，7人成员; n表示0，1或2; 当n表示2时，R 6 可以相同或不同; Z表示5元或6元含氮不饱和杂环残基。版权所有（C）2012，JPO＆INPIT

2. 发明专利

JP2011037813A METHOD FOR PRODUCING 5-HETEROCYCLE SUBSTITUTED IMINO-9-DIALKYLAMINOBENZO[a]PHENOXATHIN OR SALT THEREOF 审中-公开
标题翻译：生产5-取代的取代的氨基-9-二烷基氨基苯并[a]苯并恶嗪或其盐的方法
公开(公告)号：JP2011037813A
公开(公告)日：2011-02-24
申请号：JP2009204089
申请日：2009-08-14
申请人： Synstar Japan Co Ltd , 株式会社シンスター・ジャパン
发明人： MOHAMMAD ABU BAKAR , ITO ISAMU , IHARA MASATAKA
IPC分类号： C07D413/12 , C07B61/00
摘要： PROBLEM TO BE SOLVED: To provide a high-yield and industrially inexpensive method for producing 5-heterocyclic imino-9-dialkylaminobenzo[a]phenoxathins or salts thereof.
SOLUTION: In the method for producing the 5-heterocyclic imino-9-dialkylaminobenzo[a]phenoxathins represented by formula (III) or salts thereof, a 5-imino-9-dialkylaminobenzo[a]phenoxathin or a salt thereof is reacted with a heterocyclic compound having a leaving group in the presence of a platinum group element catalyst, a ligand and a base.
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：待解决的问题：提供高产率和工业上便宜的5-杂环亚氨基-9-二烷基氨基苯并[a]吩草酚辛或其盐的制备方法。解决方案：在制备由式（III）表示的5-杂环亚氨基-9-二烷基氨基苯并[a]吩恶嗪素或其盐的方法中，5-亚氨基-9-二烷基氨基苯并[a]吩草酚或其盐是与具有离去基团的杂环化合物在铂族元素催化剂，配体和碱的存在下反应。版权所有（C）2011，JPO＆INPIT

3. 发明专利

JP2014166975A Near-infrared fluorescent compound 审中-公开
标题翻译：近红外荧光化合物
公开(公告)号：JP2014166975A
公开(公告)日：2014-09-11
申请号：JP2013054067
申请日：2013-02-28
申请人： Synstar Japan Co Ltd , 株式会社シンスター・ジャパン
发明人： GE JIANFENG , IHARA MASATAKA , ITO ISAMU
IPC分类号： C07D265/34 , A61K49/00 , G01N21/80 , G01N31/22
摘要： PROBLEM TO BE SOLVED: To provide a novel fluorescent compound including a pyridinium structure in a 5-substituted imino group of a benzo[a]phenoxathiin usable as a fluorescence probe and a fluorescence indicator.SOLUTION: A near-infrared fluorescent compound is represented by the specified general formula (1). (In the formula, n represents an integer between 2 and 4, R is a methyl group, an ethyl group or a propyl group, and Xrepresents an anion.)
摘要翻译：要解决的问题：提供一种可用作荧光探针和荧光指示剂的苯并[a]苯氧硫蛋白的5-取代亚氨基中的吡啶鎓结构的新型荧光化合物。解决方案：近红外荧光化合物由指定的通式（1）。（式中，n表示2〜4的整数，R表示甲基，乙基或丙基，X表示阴离子。）

4. 发明专利

JP2012126702A Method for producing azine-based compound having imino group at 5-position 有权
标题翻译：在五位上生产含有三嗪基的化合物的方法
公开(公告)号：JP2012126702A
公开(公告)日：2012-07-05
申请号：JP2010294708
申请日：2010-12-16
申请人： Synstar Japan Co Ltd , 株式会社シンスター・ジャパン
发明人： MIZUKAWA HIROKI , IHARA MASATAKA , ITO ISAMU
IPC分类号： C07D265/38 , C07D413/12 , C07D413/14 , C07D417/12 , C07D498/04 , C07D498/16
摘要： PROBLEM TO BE SOLVED: To provide a method for easily and industrially inexpensively producing an azine-based compound having an imino group at the 5-position or a salt thereof with high yield and high purity.SOLUTION: The method for producing the azine-based compound represented by general formula (I) includes: reducing a compound represented by general formula (II) into a compound represented by general formula (III), reacting the reduced body with a compound represented by general formula (IV) to obtain a compound represented by general formula (V), and oxidizing the compound represented by general formula (V) to obtain the compound represented by general formula (I). According to this, a compound with high purity can be easily obtained with a higher yield. In general formula (I), R, R, R, R, R, Rand Reach independently represents a hydrogen atom or a substituent, wherein Rand R, Rand R, Rand R, or Rand Rmay be mutually coupled to form a 5-membered, 6-membered or 7-membered ring; X represents -N(R)-, -O-, -S- or -SO-, wherein Rrepresents a hydrogen atom, alkyl, alkenyl, aryl or heterocyclic group; and Z represents alkyl, alkenyl, aryl or heterocyclic group.
摘要翻译：待解决的问题：提供一种在5位上容易和工业上廉价地制备具有亚氨基的吖嗪系化合物或其高收率和高纯度的方法。解决方案：由通式（I）表示的吖嗪系化合物的制造方法包括：将通式（II）表示的化合物还原成通式（III）表示的化合物，使还原体与通式（IV）表示的化合物，得到通式（V）表示的化合物，氧化通式（V）所示的化合物，得到通式（I）表示的化合物。因此，可以容易地获得高产率的化合物。在通式（I）中，R 1 ，R 2 ，R 3 ，R 4 ，R 5 ，R 6 和R 1 和R 2 ，R 1 和R 4 ，R 2 和R 3 或R 5 和R 6 可以相互耦合以形成5 6元或7元环; X表示-N（R 8 ） - ， - O - ， - S-或-SO 2 < 表示氢原子，烷基，烯基，芳基或杂环基; Z表示烷基，烯基，芳基或杂环基。版权所有（C）2012，JPO＆INPIT

5. 发明专利

JP2011037814A Combination of 5-heterocyclic ring-substituted imino-9-dialkylaminobenzo[a] phenoxathiin compound or salt thereof and artemisinin derivative for prevention or treatment of malaria plasmodium species disease 审中-公开
标题翻译： 5-取代的环取代的亚氨基-9-二烷基氨基苯并[A]苯氧基化合物或其盐及其衍生物用于预防或治疗疟疾物种疾病的组合
公开(公告)号：JP2011037814A
公开(公告)日：2011-02-24
申请号：JP2009204090
申请日：2009-08-14
申请人： Synstar Japan Co Ltd , 株式会社シンスター・ジャパン
发明人： IHARA MASATAKA , ARAI CHIKA , ITO ISAMU , SAKANOUE SEIKI
IPC分类号： A61K31/538 , A61K31/357 , A61K31/366 , A61P33/06 , A61P43/00
CPC分类号： Y02A50/411
摘要： PROBLEM TO BE SOLVED: To provide a disease prevention or a treatment for a new strain of malaria Plasmodium having a highly therapeutic effect and selective toxicity toward malaria Plasmodium-based infectious disease and capable of suppressing the emergence of a resistant malaria Plasmodium strain as compared with a case of administering an active ingredient in a monotherapy.
SOLUTION: As an active ingredient, 5-heterocyclic ring-substituted imino-9-dialkyl aminobenzo[a]phenoxathiin compound or its salt shown by Formula (I) and an artemisinin derivative are combined. In the formula, R
1 and R
2 are each independently a methyl group, ethyl group, propyl group, 2-hydroxyethyl group or 2-methanesulfoneamideethyl group; R
3 represents a 2-pyridyl group or 4-pyridyl group; R
4 represents a fluorine atom, chlorine atom, methoxy group or methyl group; R
5 is a fluorine atom, chlorine atom, methoxy group or methyl group; m represents an integer of 0 or 1; n represents an integer of 0 or 1; and an negative ion represented by X
- is a chlorine atom, bromine atom, nitric acid ion, sulfonic acid ion, p-toluenesulfonic acid ion or oxalic acid ion.
COPYRIGHT: (C)2011,JPO&INPIT
摘要翻译：要解决的问题：为新的疟疾菌株提供疾病预防或治疗具有高度治疗效果和对疟疾的选择性毒性的疟原虫疟原虫感染性疾病并能够抑制抗性疟疾疟原虫菌株的出现与在单一疗法中施用活性成分的情况相比。解决方案：作为活性成分，将5-杂环环取代的亚氨基-9-二烷基氨基苯并[a]苯氧硫蛋白化合物或其由式（I）表示的盐和青蒿素衍生物组合。在该式中，R 1和R 2各自独立地为甲基，乙基，丙基，2-羟乙基或2-甲基磺酰胺乙基; R 3表示2-吡啶基或4-吡啶基; R SP 4表示氟原子，氯原子，甲氧基或甲基; R 5 是氟原子，氯原子，甲氧基或甲基; m表示0或1的整数; n表示0或1的整数; 由X - 表示的负离子是氯原子，溴原子，硝酸离子，磺酸离子，对甲苯磺酸离子或草酸离子。版权所有（C）2011，JPO＆INPIT

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