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1. 发明专利

JP2006022063A Lox-1 gene expression inhibitor 审中-公开
标题翻译： LOX-1基因表达抑制剂
公开(公告)号：JP2006022063A
公开(公告)日：2006-01-26
申请号：JP2004202889
申请日：2004-07-09
申请人： Gentier Biosystems Inc , Univ Nihon , ジェンティア・バイオシステムズ株式会社 , 学校法人日本大学
发明人： FUKUDA NOBORU , UENO TAKAHIRO , SUGIYAMA HIROSHI
IPC分类号： A61K31/787 , A61P3/06 , A61P9/10 , A61P43/00
摘要： PROBLEM TO BE SOLVED: To provide a LOX-1 gene expression inhibitor using a pyrrole-imidazole polyamide bound to the LOX-1 gene base sequence.
SOLUTION: The LOX-1 gene expression inhibitor comprises a pyrrole-imidazole polyamide comprising N-methylpyrrole units(hereafter, also referred to as Py), N-methylimidazole units(hereafter, also referred to as Im) and γ-aminobutyric acid units. The pyrrole-imidazole polyamide is such as to enable to have a U-shaped conformation by being folded at the γ-aminobutyric acid unit sites in the minor groove of a double helix domain(hereafter, referred to as a target domain) comprising part or the whole of the -130 to -11(Sequence No.2) of a lectin-like LDL receptor-1(hereafter, also referred to as LOX-1) gene promoter and the corresponding complementary strand, being such that Py/Im pair corresponds to C-G base pair, Im/Py pair to G-C base pair, and Py/Py pairs to A-T base pair and T-A base pair, respectively.
COPYRIGHT: (C)2006,JPO&NCIPI
摘要翻译：待解决的问题：使用与LOX-1基因序列结合的吡咯 - 咪唑聚酰胺来提供LOX-1基因表达抑制剂。解决方案：LOX-1基因表达抑制剂包括包含N-甲基吡咯单元（以下也称为Py）的吡咯 - 咪唑聚酰胺，N-甲基咪唑单元（以下也称为Im）和γ-氨基丁酸酸单位。吡咯 - 咪唑聚酰胺能够通过在双螺旋结构域（以下称为靶结构域）的小沟槽中的γ-氨基丁酸单元位点处折叠而形成U形构象，凝集素样LDL受体-1（以下也称为LOX-1）基因启动子和相应的互补链的-130至-11（序列号2）的整体使得Py / Im对对应于CG碱基对，对应于GC碱基对的Im / Py对，分别对应于AT碱基对和TA碱基对的Py / Py对。版权所有（C）2006，JPO＆NCIPI

2. 发明专利

JP2007176795A TGF-β gene expression inhibitor 审中-公开
标题翻译： TGF-β基因表达抑制剂
公开(公告)号：JP2007176795A
公开(公告)日：2007-07-12
申请号：JP2004238533
申请日：2004-08-18
申请人： Gentier Biosystems Inc , Univ Nihon , ジェンティア・バイオシステムズ株式会社 , 学校法人日本大学
发明人： FUKUDA NOBORU , UENO TAKAHIRO , SUGIYAMA HIROSHI
IPC分类号： A61K31/787 , A61P9/00 , A61P43/00
CPC分类号： C07D403/12
摘要： PROBLEM TO BE SOLVED: To provide a TGF-β gene expression activity inhibitor based on a pyrrole-imidazole polyamide compound having excellent specificity for inhibition of gene expression and scarcely affected by degradation with a ribonuclease or to provide a therapeutic agent for TGF-β-associated diseases. SOLUTION: The TGF-β expression inhibitor contains the pyrrole-imidazole polyamide comprising an N-methylpyrrole unit (hereinafter referred also to as Py), an N-methylimidazole unit (hereinafter referred also to as Im) and a γ-aminobutyric acid unit which can be folded into a U-shaped conformation in the γ-aminobutyric acid unit site in a minor groove of a double-stranded region (hereinafter referred to as a target region) containing a part or all of the following base sequence of -450 to -310 (sequence number 2) described below of a human transforming growth factor β1 (hereinafter referred also to as hTGF-β1) promoter and a strand complementary thereto. A Py/Im pair, an Im/Py pair and a Py/Py pair correspond, respectively to a C-G base pair, a G-C base pair and an A-T base pair and a T-A base pair. COPYRIGHT: (C)2007,JPO&INPIT
摘要翻译：要解决的问题：提供一种基于吡喃 - 咪唑聚酰胺化合物的TGF-β基因表达活性抑制剂，其对抑制基因表达具有极好的特异性，几乎不受核糖核酸酶降解的影响，或提供TGF的治疗剂 -β相关疾病。解决方案：TGF-β表达抑制剂含有包含N-甲基吡咯单元（以下也称为Py）的吡咯 - 咪唑聚酰胺，N-甲基咪唑单元（以下也称为Im）和γ-氨基丁酸酸单元，其可以在包含以下碱基序列的一部分或全部的双链区域（以下称为靶区域）的γ-氨基丁酸单元位点折叠成U形构象 -450〜-310（序列号2）的人转化生长因子β1（以下也称为hTGF-β1）启动子和与其互补的链。 Py / Im对，Im / Py对和Py / Py对分别对应于C-G碱基对，G-C碱基对和A-T碱基对和T-A碱基对。版权所有（C）2007，JPO＆INPIT

3. 发明专利

JP2007043942A Ribozyme for breaking gene of coronavirus 有权
标题翻译：用于断裂基因的RIBOZYME
公开(公告)号：JP2007043942A
公开(公告)日：2007-02-22
申请号：JP2005231051
申请日：2005-08-09
申请人： Gentier Biosystems Inc , Univ Nihon , ジェンティア・バイオシステムズ株式会社 , 学校法人日本大学
发明人： FUKUDA NOBORU , UENO TAKAHIRO , FUKUSHIMA AKIKO , KURODA KAZUMICHI
IPC分类号： C12N9/00 , A61K31/7088 , A61P31/12 , C12N15/09 , C12Q1/68
CPC分类号： C12N15/1131 , C12N2310/121 , C12Q1/701 , C12Q2521/337
摘要： PROBLEM TO BE SOLVED: To provide a ribozyme for breaking a gene of a coronavirus, and a therapeutic drug of coronavirus infectious disease. SOLUTION: The ribozyme containing a complementary base sequence is designed by retrieving a common base sequence in the coronavirus such as SARS-CoV and MHV. The therapeutic drug of the coronavirus infectious disease contains the ribozyme. COPYRIGHT: (C)2007,JPO&INPIT
摘要翻译：待解决的问题：提供用于破坏冠状病毒基因的核酶和冠状病毒感染性疾病的治疗药物。解决方案：通过检索冠状病毒如SARS-CoV和MHV中的共同碱基序列来设计含有互补碱基序列的核酶。冠状病毒感染性疾病的治疗药物含有核酶。版权所有（C）2007，JPO＆INPIT

4. 发明专利

CA2573974A1 TGF-.BETA. GENE EXPRESSION INHIBITOR 未知
公开(公告)号：CA2573974A1
公开(公告)日：2006-02-23
申请号：CA2573974
申请日：2005-08-02
申请人： GENTIER BIOSYSTEMS INC , UNIV NIHON
发明人： SUGIYAMA HIROSHI , UENO TAKAHIRO , FUKUDA NOBORU
IPC分类号： A61K31/4178 , A61P9/00 , A61P43/00 , C07D403/14
摘要： A TGF-² gene expression inhibitor containing a pyrrole-immidazole polyamide comprising an N-methylpyrrole unit (hereinafter also referred to as Py), an N-methylimidazole unit (hereinafter also referred to as Im) and a ³-aminobutyric acid unit which can be folded into an U-shaped conformation at the above-described ³-aminobutyric acid unit site in a minor groove of a double-stranded region (hereinafter referred to as the target region) containing a part or the whole of the following base sequence (SEQ ID NO: 2) corresponding to -450 to -310 of human transforming growth factor ²1 (hereinafter also referred to as h TGF-²1) promoter and a strand complementary thereto and in which a Py/Im pair, an Im/Py pair and a PY/Py pair correspond respectively to a C-G base pair, a G-C base pair and an A-T base pair and a T-A base pair.

5. 发明公开

EP1779850A4 TGF- GENE EXPRESSION INHIBITOR 审中-公开
标题翻译： TGF-BGR基因表达抑制剂
公开(公告)号：EP1779850A4
公开(公告)日：2009-05-06
申请号：EP05768778
申请日：2005-08-02
申请人： UNIV NIHON , GENTIER BIOSYSTEMS INC
发明人： FUKUDA NOBORU , UENO TAKAHIRO , SUGIYAMA HIROSHI
IPC分类号： C07D403/14 , A61K31/4178 , A61P9/00 , A61P43/00
CPC分类号： C07D403/12
摘要： A TGF-β gene expression inhibitor containing a pyrrole-imidazole polyamide comprising an N-methylpyrrole unit (hereinafter also referred to as Py), an N-methylimidazole unit (hereinafter also referred to as Im) and a Ϝ-aminobutyric acid unit which can be folded into an U-shaped conformation at the above-described Ϝ-aminobutyric acid unit site in a minor groove of a double-stranded region (hereinafter referred to as the target region) containing a part or the whole of the following base sequence (SEQ ID NO:2) corresponding to -450 to -310 of human transforming growth factor β1 (hereinafter also referred to as h TGF-β1) promoter and a strand complementary thereto and in which a Py/Im pair, an Im/Py pair and a Py/Py pair correspond respectively to a C-G base pair, a G-C base pair and an A-T base pair and a T-A base pair.

6. 发明专利

JP2012006897A Blood hdl level increasing agent, or anti-arteriosclerotic agent 审中-公开
标题翻译： BLOOD HDL水平增高剂或抗神经毒素剂
公开(公告)号：JP2012006897A
公开(公告)日：2012-01-12
申请号：JP2010146985
申请日：2010-06-28
申请人： Nihon Univ , 学校法人日本大学
发明人： UENO TAKAHIRO , FUKUDA NOBORU , TSUNEMI AKIKO , NAGASE HIROKI , WATABE TAKAYOSHI
IPC分类号： A61K31/4178 , A61P3/00 , A61P9/10 , C07D403/14 , C12N15/09
CPC分类号： C07D403/14
摘要： PROBLEM TO BE SOLVED: To provide a new PI (pyrrole imidazole) polyamide useful for increasing the blood HDL level, and also an anti-arteriosclerotic agent by using the PI polyamide as an active ingredient.SOLUTION: By synthesizing the PI polyamides (three types) capable of controlling the expression of human ABCA1 gene, the anti-arteriosclerotic agent by using one of the PI polyamides as the active ingredient is obtained.

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