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1. 发明申请

US20080119568A1 Gastrointestinal Absorption Enhancer Mediated By Proton-Coupled Transporter and Its Preparing Method 审中-公开
标题翻译：通过质子耦合转运体介导的胃肠吸收增强剂及其制备方法
公开(公告)号：US20080119568A1
公开(公告)日：2008-05-22
申请号：US11971243
申请日：2008-01-09
申请人： Akira TSUJI , Ikumi Tamai , Yoshimichi Sai , Masaaki Odomi , Hidekazu Toyobuku
发明人： Akira TSUJI , Ikumi Tamai , Yoshimichi Sai , Masaaki Odomi , Hidekazu Toyobuku
IPC分类号： A61K47/30
CPC分类号： A61K47/32 , A61K9/0053 , A61K9/08 , A61K31/545 , A61K31/546
摘要： The present invention provides a pharmaceutical preparation that can improve absorption of a pharmaceutical compound in the gastrointestinal tract and that provides, through oral administration or like method, a blood concentration from which sufficient remedial effects can be expected, and a method for producing such a preparation. The invention is directed to a pharmaceutical preparation exhibiting excellent gastrointestinal absorbability comprising a compound recognized by a proton-coupled transporter and a pH-sensitive polymer in an amount sufficient for the gastrointestinal tract to acquire a pH at which the proton-coupled transporter optimally absorbs the compound into a cell.
摘要翻译：本发明提供了一种药物制剂，其可以改善胃肠道中药物化合物的吸收，并且通过口服给药或类似方法提供预期足够的补救效果的血液浓度，以及制备这种制剂的方法。本发明涉及显示出优异的胃肠吸收能力的药物制剂，其包含由质子偶联转运蛋白识别的化合物和pH敏感性聚合物，其量足以使胃肠道获得质子偶联转运蛋白最佳地吸收复合成细胞。

2. 发明申请

US20060121107A1 Agent improving proton-driven transporter-mediated absorption in digestive tract and process for producing the same 审中-公开
标题翻译：改善质子驱动的转运蛋白介导的消化道吸收及其制备方法
公开(公告)号：US20060121107A1
公开(公告)日：2006-06-08
申请号：US10541019
申请日：2004-01-08
申请人： Akira Tsuji , Ikumi Tamai , Yoshimichi Sai , Masaaki Odomi , Hidekazu Toyobuku
发明人： Akira Tsuji , Ikumi Tamai , Yoshimichi Sai , Masaaki Odomi , Hidekazu Toyobuku
IPC分类号： A61K31/401 , A61K31/198 , A61K9/20 , A61K31/716
CPC分类号： A61K47/32 , A61K9/0053 , A61K9/08 , A61K31/545 , A61K31/546
摘要： The present invention provides a pharmaceutical preparation that can improve absorption of a pharmaceutical compound in the gastrointestinal tract and that provides, through oral administration or like method, a blood concentration from which sufficient remedial effects can be expected, and a method for producing such a preparation. The invention is directed to a pharmaceutical preparation exhibiting excellent gastrointestinal absorbability comprising a compound recognized by a proton-coupled transporter and a pH-sensitive polymer in an amount sufficient for the gastrointestinal tract to acquire a pH at which the proton-coupled transporter optimally absorbs the compound into a cell.
摘要翻译：本发明提供了一种药物制剂，其可以改善胃肠道中药物化合物的吸收，并且通过口服给药或类似方法提供预期足够的补救效果的血液浓度，以及制备这种制剂的方法。本发明涉及显示出优异的胃肠吸收能力的药物制剂，其包含由质子偶联转运蛋白识别的化合物和pH敏感性聚合物，其量足以使胃肠道获得质子偶联转运蛋白最佳地吸收复合成细胞。

3. 发明授权

US08871818B2 Gastrointestinal absorption enhancer mediated by proton-coupled transporter and its preparing method 有权
标题翻译：由质子偶联转运蛋白介导的胃肠道吸收促进剂及其制备方法
公开(公告)号：US08871818B2
公开(公告)日：2014-10-28
申请号：US12254905
申请日：2008-10-21
申请人： Akira Tsuji , Ikumi Tamai , Yoshimichi Sai , Masaaki Odomi , Hidekazu Toyobuku
发明人： Akira Tsuji , Ikumi Tamai , Yoshimichi Sai , Masaaki Odomi , Hidekazu Toyobuku
IPC分类号： A61K47/30 , A61K9/14 , A61K47/00 , A61K38/00 , A61K38/55 , A61K47/32
CPC分类号： A61K47/32 , A61K9/0053 , A61K9/08 , A61K31/545 , A61K31/546
摘要： The present invention provides a pharmaceutical preparation that can improve absorption of a pharmaceutical compound in the gastrointestinal tract and that provides, through oral administration or like method, a blood concentration from which sufficient remedial effects can be expected, and a method for producing such a preparation. The invention is directed to a pharmaceutical preparation exhibiting excellent gastrointestinal absorbability comprising a compound recognized by a proton-coupled transporter and a pH-sensitive polymer in an amount sufficient for the gastrointestinal tract to acquire a pH at which the proton-coupled transporter optimally absorbs the compound into a cell.
摘要翻译：本发明提供了一种药物制剂，其可以改善胃肠道中药物化合物的吸收，并且通过口服给药或类似方法提供预期足够的补救效果的血液浓度，以及制备这种制剂的方法。本发明涉及显示出优异的胃肠吸收能力的药物制剂，其包含由质子偶联转运蛋白识别的化合物和pH敏感性聚合物，其量足以使胃肠道获得质子偶联转运蛋白最佳地吸收复合成细胞。

4. 发明申请

US20090048350A1 GASTROINTESTINAL ABSORPTION ENHANCER MEDIATED BY PROTON-COUPLED TRANSPORTER AND ITS PREPARING METHOD 审中-公开
标题翻译：由PROTON-COUPLED TRANSPORTER介绍的吸收增强剂及其制备方法
公开(公告)号：US20090048350A1
公开(公告)日：2009-02-19
申请号：US12254905
申请日：2008-10-21
申请人： Akira Tsuji , Ikumi Tamai , Yoshimichi Sai , Masaaki Odomi , Hidekazu Toyobuku
发明人： Akira Tsuji , Ikumi Tamai , Yoshimichi Sai , Masaaki Odomi , Hidekazu Toyobuku
IPC分类号： A61K47/30
CPC分类号： A61K47/32 , A61K9/0053 , A61K9/08 , A61K31/545 , A61K31/546
摘要： The present invention provides a pharmaceutical preparation that can improve absorption of a pharmaceutical compound in the gastrointestinal tract and that provides, through oral administration or like method, a blood concentration from which sufficient remedial effects can be expected, and a method for producing such a preparation. The invention is directed to a pharmaceutical preparation exhibiting excellent gastrointestinal absorbability comprising a compound recognized by a proton-coupled transporter and a pH-sensitive polymer in an amount sufficient for the gastrointestinal tract to acquire a pH at which the proton-coupled transporter optimally absorbs the compound into a cell.
摘要翻译：本发明提供了一种药物制剂，其可以改善胃肠道中药物化合物的吸收，并且通过口服给药或类似方法提供预期足够的补救效果的血液浓度，以及制备这种制剂的方法。本发明涉及显示出优异的胃肠吸收能力的药物制剂，其包含由质子偶联转运蛋白识别的化合物和pH敏感性聚合物，其量足以使胃肠道获得质子偶联转运蛋白最佳地吸收复合成细胞。

5. 发明授权

US07420029B2 Tissue-specific transporter inhibitor 失效
标题翻译：组织特异性转运蛋白抑制剂
公开(公告)号：US07420029B2
公开(公告)日：2008-09-02
申请号：US10742335
申请日：2003-12-19
申请人： Akira Tsuji , Ikumi Tamai , Yoshimichi Sai , Noubuhiko Yui , Toru Oya , Ken-ichi Miyamoto
发明人： Akira Tsuji , Ikumi Tamai , Yoshimichi Sai , Noubuhiko Yui , Toru Oya , Ken-ichi Miyamoto
IPC分类号： C07K17/00 , A61K31/74 , C07H1/00
CPC分类号： B82Y5/00 , A61K31/724 , A61K31/765 , A61K38/05 , A61K47/6949 , A61K47/6951
摘要： The present invention is to provide a tissue-specific transporter inhibitor which is not absorbed through the digestive tract and can prevent deterioration in the QOL of a patient caused by diet therapy, and a therapeutic drug for tissue dysfunction diseases and a therapeutic drug for suppressing the progress of chronic renal failure containing the inhibitor as an active ingredient. A tissue-specific transporter inhibitor which is not absorbed through the digestive tract is constructed by introducing a dipeptide which is a ligand of an oligopeptide transporter 1 into a supramolecular structure polyrotaxane wherein its structurally modified active residue is expected to be excellent in the interaction with a transmembrane transporter.
摘要翻译：本发明提供一种组织特异性转运蛋白抑制剂，其不通过消化道吸收，并且可以防止饮食治疗引起的患者生活质量的恶化，以及用于组织功能障碍疾病的治疗药物和用于抑制含有抑制剂作为活性成分的慢性肾功能衰竭进展。不通过消化道吸收的组织特异性转运蛋白抑制剂是通过将作为寡肽转运体1的配体的二肽引入超分子结构的聚轮烷而构成的，其中其结构改性的活性残基预期与跨膜转运蛋白

6. 发明申请

US20070148703A1 Method of screening remedy for breast cancer 审中-公开
标题翻译：乳腺癌筛查方法
公开(公告)号：US20070148703A1
公开(公告)日：2007-06-28
申请号：US10561504
申请日：2004-06-18
申请人： Ikumi Tamai , Takashi Nozawa
发明人： Ikumi Tamai , Takashi Nozawa
IPC分类号： G01N33/567 , A61K31/56
CPC分类号： G01N33/743 , G01N33/57415 , G01N2500/04
摘要： The present invention is a method for screening a remedy for breast cancer which does not require uptake into cells unlike aromatase inhibitors, estrogen sulfatase inhibitors, or estrogen competitive inhibitors such as tamoxifen and toremifene, and which shows excellent drug delivery property and extremely rare adverse effect. In the method, a remedy for breast cancer which inhibits transporter function is screened by the process comprising the steps of: culturing a cultured human breast cancer cell line such as MCF-7 cell line or T-47D cell line in the presence of estrone-3-sulfate and a test substance such as bromosulfophtalein; and evaluating whether the uptake of estrone-3-sulfate into cells via estrone-3-sulfate transporters expressed on the cell surface is inhibited, and whether the proliferation of MCF-7 cell line is suppressed.
摘要翻译：本发明是一种筛选与芳香酶抑制剂，雌激素硫酸酯酶抑制剂或雌激素竞争性抑制剂如他莫昔芬和托瑞米芬不同的不需要摄入细胞的乳腺癌治疗方法，其显示出优异的药物递送特性和非常罕见的副作用。在该方法中，通过包括以下步骤的方法筛选抑制转运蛋白功能的乳腺癌的治疗方法：在雌酮甾酮化合物的存在下培养培养的人乳腺癌细胞系如MCF-7细胞系或T-47D细胞系， 3-硫酸盐和一种测试物质如溴代磺酰氯; 评估在细胞表面表达的雌酮-3-硫酸转运蛋白对雌激素-3-硫酸盐摄取是否受到抑制，MCF-7细胞增殖是否被抑制。

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