公开(公告)号：US20110275668A1

公开(公告)日：2011-11-10

申请号：US13067191

申请日：2011-05-16

申请人： Tsunehiko Higuchi ,  Hirohisa Omiya ,  Naoki Umezawa ,  Hye-Sook Kim ,  Yusuke Wataya

发明人： Tsunehiko Higuchi ,  Hirohisa Omiya ,  Naoki Umezawa ,  Hye-Sook Kim ,  Yusuke Wataya

IPC分类号： A61K31/4709 ,  A61P33/06 ,  C07D215/46

CPC分类号： C07D401/12

摘要： Compounds with high antimalarial activity; and antimalarial drugs containing the same as an active ingredient. There are provided compounds with antimalarial activity represented by the chemical formula: (wherein R1 is H, Cl or OCH3; R2 is H or CH3; R3 is CH, CH2, C(CH3), CH(CH3) or C(CH3)2; Ar is imidazole, triazole, pyridine, benzene, pyrrole, furan, thiophene or derivatives thereof; n is 1 to 5; and m is 1 to 5). Further, there are provided antimalarial drugs containing these compounds with antimalarial activity or pharmacologically acceptable salts thereof as active ingredients.

公开(公告)号：US06914048B2

公开(公告)日：2005-07-05

申请号：US10246441

申请日：2002-09-18

申请人： Samuel H. Gellman ,  Naoki Umezawa ,  Michael A. Gelman ,  Ronald T. Raines ,  Terra Potocky

发明人： Samuel H. Gellman ,  Naoki Umezawa ,  Michael A. Gelman ,  Ronald T. Raines ,  Terra Potocky

IPC分类号： A61K47/48 ,  C07K7/06 ,  C07K7/08 ,  A61K38/08 ,  A61K38/10 ,  C07K7/02

CPC分类号： C07K7/08 ,  A61K47/645 ,  C07K7/06

摘要： Disclosed are β-peptides and β-peptide conjugates that are capable of diffusing or otherwise being transported across the cell membranes of living cells. The β-peptides contain at least six β-amino acid residues, at leastsix of which are preferably β3-homoarginine residues. It has been found that when pharmacologically-active agents are conjugated to these types of β-peptides, the resulting conjugates (also disclosed herein) are also capable of diffusing or otherwise being transported across the cell membranes of living cells, including mammalian cells.

摘要翻译： 公开了能够扩散或以其它方式被传输通过活细胞细胞膜的β-肽和β-肽缀合物。 β-肽含有至少六个β-氨基酸残基，其中至少有七个是优质β-OH-精氨酸残基。 已经发现，当药理活性剂与这些类型的β-肽缀合时，所得到的缀合物（本文也公开）也能够扩散或以其它方式被传输穿过包括哺乳动物细胞的活细胞的细胞膜。

公开(公告)号：US07973027B2

公开(公告)日：2011-07-05

申请号：US12224387

申请日：2007-02-26

申请人： Tsunehiko Higuchi ,  Hirohisa Omiya ,  Naoki Umezawa ,  Hye-Sook Kim ,  Yusuke Wataya

发明人： Tsunehiko Higuchi ,  Hirohisa Omiya ,  Naoki Umezawa ,  Hye-Sook Kim ,  Yusuke Wataya

IPC分类号： A61K31/47 ,  C07D215/46

CPC分类号： C07D401/12

摘要： Compounds with high antimalarial activity; and antimalarial drugs containing the same as an active ingredient. There are provided compounds with antimalarial activity represented by the chemical formula: (wherein R1 is H, Cl or OCH3; R2 is H or CH3; R3 is CH, CH2, C(CH3), CH(CH3) or C(CH3)2; Ar is imidazole, triazole, pyridine, benzene, pyrrole, furan, thiophene or derivatives thereof; n is 1 to 5; and m is 1 to 5). Further, there are provided antimalarial drugs containing these compounds with antimalarial activity or pharmacologically acceptable salts thereof as active ingredients.

摘要翻译： 抗疟活性高的化合物 和含有与活性成分相同的抗疟药。 提供具有化学式表示的抗疟活性化合物：其中R1为H，Cl或OCH3; R2为H或CH3; R3为CH，CH2，C（CH3），CH（CH3）或C（CH3）2 ; Ar为咪唑，三唑，吡啶，苯，吡咯，呋喃，噻吩或其衍生物; n为1至5; m为1至5）。 此外，提供了含有抗疟活性化合物的抗疟药物或其药理学上可接受的盐作为活性成分。

公开(公告)号：US20090275612A1

公开(公告)日：2009-11-05

申请号：US12224387

申请日：2007-02-26

申请人： Tsunehiko Higuchi ,  Hirohisa Omiya ,  Naoki Umezawa ,  Hye-Sook Kim ,  Yusuke Wataya

发明人： Tsunehiko Higuchi ,  Hirohisa Omiya ,  Naoki Umezawa ,  Hye-Sook Kim ,  Yusuke Wataya

IPC分类号： A61K31/4709 ,  C07D215/38 ,  A61P33/06

CPC分类号： C07D401/12

摘要： Compounds with high antimalarial activity; and antimalarial drugs containing the same as an active ingredient. There are provided compounds with antimalarial activity represented by the chemical formula: (wherein R1 is H, Cl or OCH3; R2 is H or CH3; R3 is CH, CH2, C(CH3), CH(CH3) or C(CH3)2; Ar is imidazole, triazole, pyridine, benzene, pyrrole, furan, thiophene or derivatives thereof; n is 1 to 5; and m is 1 to 5). Further, there are provided antimalarial drugs containing these compounds with antimalarial activity or pharmacologically acceptable salts thereof as active ingredients.

摘要翻译： 抗疟活性高的化合物 和含有与活性成分相同的抗疟药。 提供具有化学式表示的抗疟活性化合物：其中R1为H，Cl或OCH3; R2为H或CH3; R3为CH，CH2，C（CH3），CH（CH3）或C（CH3）2 ; Ar为咪唑，三唑，吡啶，苯，吡咯，呋喃，噻吩或其衍生物; n为1至5; m为1至5）。 此外，提供了含有抗疟活性化合物的抗疟药物或其药理学上可接受的盐作为活性成分。

公开(公告)号：US06525088B1

公开(公告)日：2003-02-25

申请号：US09623515

申请日：2001-01-03

申请人： Tetsuo Nagano ,  Naoki Umezawa

发明人： Tetsuo Nagano ,  Naoki Umezawa

IPC分类号： A61K31357

CPC分类号： C07D493/08 ,  C07D311/82 ,  C07D493/10 ,  G01N31/225 ,  Y10S436/80

摘要： Compounds represented by the following general formula (I): wherein R1, R2, R3, R4, R5, and R6 independently represent a hydrogen atom, a halogen atom, a C1-6 alkyl group, or a C1-6 alkoxyl group, R7 and R8 independently represent a C1-6 alkyl group or an aryl group which may be substituted, R9 and R10 independently represent a hydrogen atom, a C1-6 alkyl group, or a C1-6 alkoxyl group, and R11 represents a hydrogen atom or a C1-6 alkanoyl group, or salts thereof. The aforementioned compounds are substantially non-fluorescent and react with singlet oxygen under a physiological condition to give a fluorescent substance, and therefore they are useful as agents for measurement of singlet oxygen.

摘要翻译： 由以下通式（I）表示的化合物：其中R1，R2，R3，R4，R5和R6独立地表示氢原子，卤素原子，C1-6烷基或C1-6烷氧基，R7 R8独立地表示可被取代的C1-6烷基或芳基，R9和R10独立地表示氢原子，C1-6烷基或C1-6烷氧基，R11表示氢原子或 C 1-6烷酰基，或其盐。 上述化合物基本上是非荧光的，并且在生理条件下与单线态氧反应以产生荧光物质，因此它们可用作测量单线态氧的试剂。