公开(公告)号：US06710074B2

公开(公告)日：2004-03-23

申请号：US10220244

申请日：2002-08-30

申请人： Masataka Ihara ,  Kiyosei Takasu ,  Yusuke Wataya ,  Hye-Sook Kim

发明人： Masataka Ihara ,  Kiyosei Takasu ,  Yusuke Wataya ,  Hye-Sook Kim

IPC分类号： A61K3135

CPC分类号： C07D493/10

摘要： An object of the present invention is to provide a novel compound having antimalarial acitivity and an antimalarial agent containing the novel compound as an active component. An antimalarial agent containing 12-hidroxy-2-(1-methoxy-carbonylethyl)-5-oxo-10,11,13-trioxatricyclo[7.2.0.01,6]tridecane represented by a following formula (II) as an active agent is prepared.

摘要翻译： 本发明的目的是提供具有抗疟活性的新化合物和含有新化合物作为活性成分的抗疟剂。 含有由下式（II）表示的12-羟基-2-（1-甲氧基 - 乙基乙基）-5-氧代-10,11,13-三氧杂三环[7.2.0.0 1,6]十一烷的抗疟剂作为 制备活性剂。

公开(公告)号：US20080045574A1

公开(公告)日：2008-02-21

申请号：US11576426

申请日：2005-09-29

申请人： Masataka Ihara ,  Kiyosei Takasu ,  Khanitha Pudhom ,  Hiroshi Kitaguchi ,  Masayuki Kawakami ,  Kozo Sato

发明人： Masataka Ihara ,  Kiyosei Takasu ,  Khanitha Pudhom ,  Hiroshi Kitaguchi ,  Masayuki Kawakami ,  Kozo Sato

IPC分类号： A61K31/426 ,  A61P33/00

CPC分类号： C07D417/14 ,  A61K31/428 ,  A61K31/4439 ,  A61K31/4709 ,  Y02A50/414

摘要： The present invention is to provide an anti-trypanosomiasis agent having a high selective toxicity, and high preventing or treating effect against trypanosomiasis, comprising a compound shown by the following general formula (1) as an active ingredient (wherein R1 and R2 each independently represents a hydrogen atom, halogen atom, hydroxyl group, oxygen atom, C1-5 alkyl group, C1-5 alkoxy group, C5-8 aryl group, C5-8 aryloxy group, C2-6 alkoxycarbonyl group or C2-6 alkylaminocarbonyl group, and may be bound to each other; R3, R4, and R5 each independently represents a C1-5 alkyl group or C5-8 aryl group; R6 and R7 each independently represents a hydrogen atom, halogen atom, hydroxyl group, oxygen atom, C1-8 alkyl group, C1-5 alkoxy group, C5-8 aryl group, C5-8 aryloxy group, or C2-6 alkoxycarbonyl group, and may be bound to each other; Y and Z each independently represents an atom group necessary to form a 5- or 6-membered heterocycle; m and n each represent 0 or 1; Q represents a physiologically acceptable anion; k represents an integer of 0 to 2, necessary to make the electric charge of the whole molecule 0).

摘要翻译： 本发明提供具有高选择性毒性和对锥虫病的高预防或治疗作用的抗锥虫病药，其包含由以下通式（1）表示的化合物作为活性成分（其中R 1， / O 2和R 2各自独立地表示氢原子，卤素原子，羟基，氧原子，C 1-5烷基，C 1-5 C 5〜8芳基，C 5〜8芳氧基，C 2-6烷氧基羰基或C 2-6个亚烷基氨基羰基，并且可以彼此结合; R 3，R 4和R 5 >各自独立地表示C 1-5烷基或C 5-8芳基; R 6和R 7， SUP各自独立地表示氢原子，卤素原子，羟基，氧原子，C 1-8烷基，C 1-5烷氧基，C 1〜 5-8芳基，C 5-8芳氧基，或C 1〜 并且可以相互结合; Y和Z各自独立地表示形成5-或6-元杂环所必需的原子团; m和n各自表示0或1; Q表示生理上可接受的阴离子; k表示0〜2的整数，使整个分子的电荷为0）。

公开(公告)号：US20080051598A1

公开(公告)日：2008-02-28

申请号：US11571410

申请日：2004-07-22

申请人： Kiyosei Takasu ,  Masataka Ihara ,  Kazato Inenaga

发明人： Kiyosei Takasu ,  Masataka Ihara ,  Kazato Inenaga

IPC分类号： C07C69/74

CPC分类号： C07C67/343 ,  C07F7/1804 ,  C07C69/757

摘要： The prior art required specialized substrates or reaction conditions to be used to manufacture polysubstituted cyclobutane compounds and polysubstituted cyclobutene compounds, and the method had poor generality. The type or quantity of the catalyst or solvent used was also problematic in the industrial manufacture of polysubstituted cyclobutane compounds. The present invention provides a method for manufacturing a polysubstituted cyclobutane compound with high stereoselectivity that has low environmental load (is ecologically advantageous) and is applicable to industrial manufacturing from the standpoint of operation, substrate generality, catalyst, solvent, and efficiency. A polysubstituted cyclobutane, a cyclobutene, and a bicyclo[4.2.0]octane compound can be manufactured efficiently, stereoselectively, and in an ecologically advantageous manner by causing a Brønsted acid to act on a mixture of an enol ether compound or 2-siloxydiene compound with an alkene or alkyne compound in which a carbonyl group is substituted at the 1-position in a non-aqueous solvent or without a solvent.

摘要翻译： 现有技术需要用于制备多取代环丁烷化合物和多取代环丁烯化合物的特殊底物或反应条件，并且该方法的普遍性差。 所用的催化剂或溶剂的类型或数量在多取代环丁烷化合物的工业制造中也是有问题的。 本发明提供一种具有低立体选择性的多取代环丁烷化合物的方法，其具有低的环境负荷（在生态上是有利的），并且从操作，基材通用性，催化剂，溶剂和效率的观点来看可应用于工业制造。 多取代的环丁烷，环丁烯和双环[4.2.0]辛烷化合物可以有效地，立体选择性地并且以生态有利的方式通过使布朗斯台德酸作用于烯醇醚化合物或2-硅氧烷二烯化合物的混合物 与在非水溶剂中或没有溶剂的1-位被羰基取代的烯烃或炔化合物。

公开(公告)号：US08193224B2

公开(公告)日：2012-06-05

申请号：US11576429

申请日：2005-09-30

申请人： Masataka Ihara ,  Kiyosei Takasu ,  Khanitha Pudhom ,  Hiroshi Kitaguchi ,  Masayuki Kawakami ,  Kozo Sato

发明人： Masataka Ihara ,  Kiyosei Takasu ,  Khanitha Pudhom ,  Hiroshi Kitaguchi ,  Masayuki Kawakami ,  Kozo Sato

IPC分类号： A61K31/427 ,  A61K31/428 ,  C07D277/66 ,  C07D277/04 ,  C07D277/84

CPC分类号： C07D277/84 ,  A61K31/427 ,  A61K31/428 ,  A61K31/4439 ,  A61K31/4709 ,  C07D277/64 ,  C07D417/14 ,  Y02A50/409 ,  Y02A50/411 ,  Y02A50/414

摘要： The present invention is to provide a medicinal composition for preventing or treating parasitic protozoan infections, having a high selective toxicity against parasitic protozoan infection, and a superior preventive or treating effect. A medicinal composition for preventing or treating parasitic protozoan infections comprises a compound shown by the following general formula (1) as an active ingredient (wherein R represents an alkyl group, aryl group or heterocyclic group; A and B each independently represents a 5- or 6-membered ring containing at least one hetero atom, or a condensation ring wherein 1 or more 3- to 8-membered ring is condensed thereto; Y represents S, O, Se, or —NR1— (R1 represents an alkyl group, aryl group or heterocyclic group); L1, L2, L3, L4 and L5 each independently represents a methine group; Q represents a physiologically acceptable anion; k represents an integer of 0 to 2, necessary to make the electric charge of the whole molecule 0; p and q each represents an integer of 0 to 3, wherein the sum of p and q is 1 or more, and 6 or less).

摘要翻译： 本发明提供一种用于预防或治疗对寄生原虫感染具有高选择性毒性的寄生原虫感染的药物组合物，以及优异的预防或治疗效果。 用于预防或治疗寄生原生动物感染的药物组合物包含由以下通式（1）表示的化合物作为活性成分（其中R表示烷基，芳基或杂环基; A和B各自独立地表示5-或 含有至少一个杂原子的6元环或其中1个以上3〜8元环稠合的缩合环; Y表示S，O，Se或-NR1-（R1表示烷基，芳基 基团或杂环基）; L1，L2，L3，L4和L5各自独立地表示次甲基; Q表示生理上可接受的阴离子; k表示使整个分子0的电荷所必需的0至2的整数; p和q各自表示0〜3的整数，p和q的和为1以上且6以下）。

公开(公告)号：US20090076067A1

公开(公告)日：2009-03-19

申请号：US11915286

申请日：2006-06-05

申请人： Masataka Ihara ,  Kiyosei Takasu ,  Kanitha Pudhom ,  Masayuki Kawakami ,  Hiroshi Kitaguchi ,  Kouzou Satou

发明人： Masataka Ihara ,  Kiyosei Takasu ,  Kanitha Pudhom ,  Masayuki Kawakami ,  Hiroshi Kitaguchi ,  Kouzou Satou

IPC分类号： A61K31/437 ,  C07D417/14 ,  A61K31/444

CPC分类号： C07D417/14 ,  A61K31/426 ,  A61K31/428 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4709 ,  C07D498/04 ,  C07D513/04 ,  Y02A50/409 ,  Y02A50/411 ,  Y02A50/414 ,  Y02A50/415 ,  Y02A50/421

摘要： The object of the invention is to provide pharmaceutical composition that can be used as a therapeutic and/or prophylactic agent. Particularly, the pharmaceutical composition of the invention has significant therapeutic effect and survival benefit for the disease caused by parasitic protozoa, and selective toxicity against the causative protozoa. The pharmaceutical composition comprises a compound represented by general formula (1). Particularly, the invention relates to a composition that is an effective therapeutic/prophylactic agent for malaria, leishmania, African sleeping sickness, Chagas disease, toxoplasmosis lymphatic filariasis, babesiosis, and coccidiosis, and a novel compound contained therein.

摘要翻译： 本发明的目的是提供可用作治疗和/或预防剂的药物组合物。 特别地，本发明的药物组合物对由寄生原虫引起的疾病和对致病原生动物的选择性毒性具有显着的治疗效果和生存益处。 药物组合物包含由通式（1）表示的化合物。 特别地，本发明涉及作为疟疾，利什曼原虫，非洲睡眠病，恰加斯病，弓形体病，淋巴丝虫病，贝氏菌病和球虫病的有效治疗/预防剂及其中所含的新化合物的组合物。

公开(公告)号：US20090036437A1

公开(公告)日：2009-02-05

申请号：US11815394

申请日：2006-02-07

申请人： Masataka Ihara ,  Kiyosei Takasu ,  Masayuki Kawakami ,  Hiroshi Kitaguchi ,  Kouzou Satou

发明人： Masataka Ihara ,  Kiyosei Takasu ,  Masayuki Kawakami ,  Hiroshi Kitaguchi ,  Kouzou Satou

IPC分类号： C07D265/38 ,  A61K31/538 ,  C07D413/10 ,  A61P33/02

CPC分类号： A61K31/538 ,  C07D265/38 ,  Y02A50/409 ,  Y02A50/411 ,  Y02A50/414 ,  Y02A50/415

摘要： The purpose of the present invention is therefore to provide a pharmaceutical composition, especially that for the treatment and/or prevention of parasitic infection by protozoa, which has a high therapeutic effect and selective toxicity or a life-prolongation effect for the parasitic infection by protozoa. The present invention is therefore related to a pharmaceutical composition comprising the compound represented by the following general formula (1) as an active ingredient, especially to those for the treatment and/or prevention of parasitic infection by protozoa

摘要翻译： 因此，本发明的目的是提供一种药物组合物，特别是用于治疗和/或预防原生动物寄生虫感染的药物组合物，其对原生动物的寄生虫感染具有高治疗效果和选择性毒性或延长寿命 。 因此，本发明涉及包含由以下通式（1）表示的化合物作为活性成分的药物组合物，特别是用于治疗和/或预防原生动物寄生虫感染的药物组合物

公开(公告)号：US07795285B2

公开(公告)日：2010-09-14

申请号：US11576426

申请日：2005-09-29

申请人： Masataka Ihara ,  Kiyosei Takasu ,  Khanitha Pudhom ,  Hiroshi Kitaguchi ,  Masayuki Kawakami ,  Kozo Sato

发明人： Masataka Ihara ,  Kiyosei Takasu ,  Khanitha Pudhom ,  Hiroshi Kitaguchi ,  Masayuki Kawakami ,  Kozo Sato

IPC分类号： A01N43/78

CPC分类号： C07D417/14 ,  A61K31/428 ,  A61K31/4439 ,  A61K31/4709 ,  Y02A50/414

摘要： The present invention is to provide an anti-trypanosomiasis agent having a high selective toxicity, and high preventing or treating effect against trypanosomiasis, comprising a compound shown by the following general formula (1) as an active ingredient (wherein R1 and R2 each independently represents a hydrogen atom, halogen atom, hydroxyl group, oxygen atom, C1-5 alkyl group, C1-5 alkoxy group, C5-8 aryl group, C5-8 aryloxy group, C2-6 alkoxycarbonyl group or C2-6 alkylaminocarbonyl group, and may be bound to each other; R3, R4, and R5 each independently represents a C1-5 alkyl group or C5-8 aryl group; R6 and R7 each independently represents a hydrogen atom, halogen atom, hydroxyl group, oxygen atom, C1-8 alkyl group, C1-5 alkoxy group, C5-8 aryl group, C5-8 aryloxy group, or C2-6 alkoxycarbonyl group, and may be bound to each other; Y and Z each independently represents an atom group necessary to form a 5- or 6-membered heterocycle; m and n each represent 0 or 1; Q represents a physiologically acceptable anion; k represents an integer of 0 to 2, necessary to make the electric charge of the whole molecule 0).

摘要翻译： 本发明提供具有高选择性毒性和对锥虫病的高预防或治疗作用的抗锥虫病药，其包含由以下通式（1）表示的化合物作为活性成分（其中R 1和R 2各自独立地表示 氢原子，卤素原子，羟基，氧原子，C 1-5烷基，C 1-5烷氧基，C 5-8芳基，C 5-8芳氧基，C 2-6烷氧基羰基或C 2-6烷基氨基羰基， 可以相互结合; R3，R4和R5各自独立地表示C1-5烷基或C5-8芳基; R6和R7各自独立地表示氢原子，卤素原子，羟基，氧原子，C1- 8个烷基，C 1-5烷氧基，C 5-8芳基，C 5-8芳氧基或C 2-6烷氧基羰基，并且可以彼此结合; Y和Z各自独立地表示形成 5-或6-元杂环; m和n各自表示0或1; Q表示物理 生理上可接受的阴离子 k表示0〜2的整数，使整个分子的电荷为0）。

公开(公告)号：US20100113789A1

公开(公告)日：2010-05-06

申请号：US11576429

申请日：2005-09-30

申请人： Masataka Ihara ,  Kiyosei Takasu ,  Khanitha Pudhom ,  Hiroshi Kitaguchi ,  Masayuki Kawakami ,  Kozo Sato

发明人： Masataka Ihara ,  Kiyosei Takasu ,  Khanitha Pudhom ,  Hiroshi Kitaguchi ,  Masayuki Kawakami ,  Kozo Sato

IPC分类号： C07D417/14

CPC分类号： C07D277/84 ,  A61K31/427 ,  A61K31/428 ,  A61K31/4439 ,  A61K31/4709 ,  C07D277/64 ,  C07D417/14 ,  Y02A50/409 ,  Y02A50/411 ,  Y02A50/414

摘要： The present invention is to provide a medicinal composition for preventing or treating parasitic protozoan infections, having a high selective toxicity against parasitic protozoan infection, and a superior preventive or treating effect. A medicinal composition for preventing or treating parasitic protozoan infections comprises a compound shown by the following general formula (1) as an active ingredient (wherein R represents an alkyl group, aryl group or heterocyclic group; A and B each independently represents a 5- or 6-membered ring containing at least one hetero atom, or a condensation ring wherein 1 or more 3- to 8-membered ring is condensed thereto; Y represents S, O, Se, or —NR1— (R1 represents an alkyl group, aryl group or heterocyclic group); L1, L2, L3, L4 and L5 each independently represents a methine group; Q represents a physiologically acceptable anion; k represents an integer of 0 to 2, necessary to make the electric charge of the whole molecule 0; p and q each represents an integer of 0 to 3, wherein the sum of p and q is 1 or more, and 6 or less.)

摘要翻译： 本发明提供一种用于预防或治疗对寄生原虫感染具有高选择性毒性的寄生原虫感染的药物组合物，以及优异的预防或治疗效果。 用于预防或治疗寄生原生动物感染的药物组合物包含由以下通式（1）表示的化合物作为活性成分（其中R表示烷基，芳基或杂环基; A和B各自独立地表示5-或 含有至少一个杂原子的6元环或其中1个以上3〜8元环稠合的缩合环; Y表示S，O，Se或-NR1-（R1表示烷基，芳基 基团或杂环基）; L1，L2，L3，L4和L5各自独立地表示次甲基; Q表示生理上可接受的阴离子; k表示使整个分子0的电荷所必需的0至2的整数; p和q各自表示0〜3的整数，p和q的和为1以上6以下）

公开(公告)号：US20060252800A1

公开(公告)日：2006-11-09

申请号：US10555539

申请日：2004-04-30

申请人： Masataka Ihara ,  Kiyosei Takasu ,  Hiroki Terauchi ,  Setsuko Sekita ,  Marii Takahashi

发明人： Masataka Ihara ,  Kiyosei Takasu ,  Hiroki Terauchi ,  Setsuko Sekita ,  Marii Takahashi

IPC分类号： A61K31/4439 ,  C07D417/14

CPC分类号： C07D417/14

摘要： The present invention is to provide a new anti-leishmania agent with fewer side effects, having a high cell proliferation-inhibiting effect to leishamia protozoa, and also easy to manufacture at a low cost. A compound wherein a heterocycle with a conjugated system and a nitrogen atom and a heterocycle with a nitrogen atom and a sulfur atom are bound by a carbon chain with an ethylene group, that is a compound wherein a specific 5- to 8-membered heterocyclic ring and a specific 5- to 8-membered heterocycle having a conjugated system are bound via a vinylene group, more particularly a specific rhodacyanine dye compound is used as an active ingredient of the anti-leishmania agent.

摘要翻译： 本发明提供一种具有较少副作用的新型利什曼原虫药，其具有对嗜酸性原虫的高细胞增殖抑制作用，并且也易于以低成本制造。 其中具有共轭体系和氮原子的杂环和具有氮原子和硫原子的杂环的亚乙基与碳原子键合的化合物，其中特定的5-至8-元杂环 并且具有共轭体系的具体的5-至8-元杂环通过亚乙烯基结合，更具体地，使用特定的罗丹参素染料化合物作为抗利什曼原虫剂的活性成分。

公开(公告)号：US20130053567A1

公开(公告)日：2013-02-28

申请号：US13582577

申请日：2011-03-03

申请人： Kiyosei Takasu ,  Yoshiji Takamoto ,  Kei Kurahashi

发明人： Kiyosei Takasu ,  Yoshiji Takamoto ,  Kei Kurahashi

IPC分类号： C07F7/18

CPC分类号： C07F7/188 ,  C07J1/0059 ,  C07J7/002 ,  C07J51/00

摘要： The invention relates to a method for producing silyl enol ether compound (3) by reacting ketone or aldehyde compound (1) with allylsilane compound (2) in the presence of a base and 0.00001 to 0.5 equivalents of an acid catalyst relative to ketone or aldehyde compound (1).

摘要翻译： 本发明涉及一种在碱存在下使酮或醛化合物（1）与烯丙基硅烷化合物（2）反应生成甲硅烷基烯醇醚化合物（3）的方法，相对于酮或醛为0.00001至0.5当量酸催化剂 化合物（1）。