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公开(公告)号：US07888516B2
公开(公告)日：2011-02-15
申请号：US11658475
申请日：2005-08-02
申请人： Noboru Fukuda , Takahiro Ueno , Hiroshi Sugiyama
发明人： Noboru Fukuda , Takahiro Ueno , Hiroshi Sugiyama
IPC分类号： C07D233/00
CPC分类号： C07D403/12
摘要： A TGF-β 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 γ-aminobutyric acid unit which can be folded into an U-shaped conformation at the above-described γ-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.
摘要翻译： 转化生长因子 含有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-氨基丁酸单元的基因表达抑制剂，其可以折叠成 在上述γ-氨基丁酸单元位置的双链区（以下称为靶区）的小槽中的U型构象，其含有部分或全部以下碱基序列（SEQ ID NO： 2）对应于-450至-310的人转化生长因子＆bgr; 1（以下也称为h TGF-β1）启动子和与其互补的链，并且其中Py / Im对，Im / Py对 并且PY / Py对分别对应于CG碱基对，GC碱基对和AT碱基对和TA碱基对。
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公开(公告)号：US07807844B2
公开(公告)日：2010-10-05
申请号：US10570159
申请日：2004-09-03
IPC分类号： C00D403/02 , C07D233/00 , C07D487/04 , C07D233/34
CPC分类号： C07D403/14
摘要： A TGF-β gene expression inhibitor containing a pyrrole-imidazole polyamide having N-methylimidazole unit (hereinafter also referred to as Py), N-methylimidazole unit (hereinafter also referred to as Im) and γ-aminobutyrate unit which can be holded into an U-shaped conformation at the γ-aminobutyrate unit in the minor groove in a double helix region (hereinafter referred to as the target region) containing a complementary chain corresponding to the sequence at the −557 to −536 in the base sequence of a human transforming growth factor β1 (hereinafter also referred to as hTGF-β1) promoter, either as a whole or a part thereof: TAAAGGAGAGCAATTCT-TACAG (SEQ ID NO: 1) wherein a Py/Im pair corresponds to a C-G base pair, an Im/Py pair corresponds to a G-C base pair, and Py/Py pairs correspond respectively to an A-A base pair and a T-A base pair.
摘要翻译： 转化生长因子 含有具有N-甲基咪唑单元（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-氨基丁酸酯单元的基因表达抑制剂，其可以被保持为U形构象 在双螺旋区域（以下称为靶区域）的小沟槽中的γ-氨基丁酸酯单元中含有对应于人转化生长因子碱基序列中的-557至-536处的序列的互补链 ; 1（以下也称为hTGF-＆bgr; 1）启动子，其全部或部分：TAAAGGAGAGCAATTCT-TACAG（SEQ ID NO：1），其中Py / Im对对应于CG碱基对， / Py对对应于GC碱基对，Py / Py对分别对应于AA碱基对和TA碱基对。
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公开(公告)号：US20090171097A1
公开(公告)日：2009-07-02
申请号：US12093651
申请日：2006-11-14
申请人： Hiroshi Sugiyama , Chikara Dohno , Noboru Fukuda
发明人： Hiroshi Sugiyama , Chikara Dohno , Noboru Fukuda
IPC分类号： C07D403/14
CPC分类号： C07D403/14 , C07D409/14
摘要： A synthesis method for pyrrole-imidazole polyamide is automated at a higher level and can produce a product with a high yield in a more stable manner. In a solid phase synthesis method, the automated synthesis of a polyimide can be promoted by using HCTU as a condensation-activator, the yield of a product can be increased by charging a monomer in a solid form, and a pyrrole-imidazole polyamide having any sequence can be synthesis by combining the synthesis method with a manual synthesis with an acid chloride.
摘要翻译： 吡咯 - 咪唑聚酰胺的合成方法在更高的水平上自动化，并且可以以更稳定的方式产生高产率的产物。 在固相合成方法中，通过使用HCTU作为缩合活化剂可以促进聚酰亚胺的自动合成，通过加入固体形式的单体可以提高产物的产率，并且可以使用具有任意形式的吡咯 - 咪唑聚酰胺 可以通过将合成方法与手性合成与酰氯组合来合成序列。
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公开(公告)号：US20080255368A1
公开(公告)日：2008-10-16
申请号：US11658475
申请日：2005-08-02
申请人： Noboru Fukuda , Takahiro Ueno
发明人： Noboru Fukuda , Takahiro Ueno
IPC分类号： C07D403/14
CPC分类号： C07D403/12
摘要： A TGF-β 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 γ-aminobutyric acid unit which can be folded into an U-shaped conformation at the above-described γ-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.
摘要翻译： 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-氨基丁酸单元的TGF-β基因表达抑制剂，其可以 在上述γ-氨基丁酸单元位置在双链区（以下称为靶区）的小沟中折叠为U形构象，其含有一部分或全部以下碱基序列（ SEQ ID NO：2）对应于人转化生长因子β1的-450至-310（以下也称为h TGF-β1）启动子和与其互补的链，并且其中Py / Im对，Im / Py对 并且PY / Py对分别对应于CG碱基对，GC碱基对和AT碱基对和TA碱基对。
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公开(公告)号：US07329237B2
公开(公告)日：2008-02-12
申请号：US11076712
申请日：2005-03-10
IPC分类号： A61M29/00
CPC分类号： A61M25/1011
摘要： To provide infusion therapy that can effectively transluminally deliver drugs or the like to a target spot without invading areas other than a diseased area. The infusion therapy is for administering a drug, cells or the like, or inserting a treatment instrument into the target diseased area. A blood vessel area including a bifurcated blood vessel connecting to the diseased area is occluded at the distal and the proximal region thereof to form an occluded area, and the drugs or the like are pumped and supplied to the occluded area, which causes the drugs or the like to flow retrogressively and retentively in the bifurcated blood vessel connecting in the occluded area, and be infused and administered to the diseased area.
摘要翻译： 提供可以有效地将药物等递送到目标点的输注治疗，而不侵入除病变区域之外的区域。 输注治疗是用于给予药物，细胞等，或者将治疗仪器插入目标患病区域。 包括与病变区域连接的分叉血管的血管区域被封闭在其远侧和近端区域处以形成闭塞区域，并且将药物等泵送并供应到闭塞区域，这导致药物或 类似物在连接在闭塞区域的分叉血管中逆行流畅地流动，并被输注并施用于患病区域。
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公开(公告)号：US20050273050A1
公开(公告)日：2005-12-08
申请号：US10527522
申请日：2003-10-08
CPC分类号： A61M25/1011 , A61M25/0023
摘要： To provide a catheter and a method for infusion therapy that can effectively transluminally deliver drugs or the like to a target spot without invading areas other than a diseased area. The catheter is a balloon catheter for insertion into a blood vessel in which four lumens extending along an axis are formed in one catheter body, and two balloons are arranged axially in parallel. The plurality of lumens include: an infusion lumen that communicates with an infusion hole between the two balloons; balloon lumens that communicate with insides of the two balloons to expand the balloons; and a guide lumen that also serves as a bypass lumen that communicates with an outside of the catheter body in each position distal and proximal, which is outside of the two balloons with respect to a tip a of the catheter body, and bypasses an occluded area formed by the two balloons to allow blood flow.
摘要翻译： 为了提供导管和输注治疗方法，其能够有效地将药物等递送到靶点而不侵入除病变区域之外的区域。 导管是用于插入血管的气囊导管，其中沿着轴线延伸的四个腔体形成在一个导管主体中，并且两个气囊被轴向平行布置。 所述多个管腔包括：输注腔，其与所述两个气囊之间的输注孔连通; 气球内腔与两个气球的内部通气以扩大气球; 以及引导腔，其也用作旁路腔，所述旁路腔与远端和近端相对于导管主体的尖端a在两个气囊外部的每个位置中与导管主体的外部连通，并绕过闭塞区域 由两个气球形成，以允许血液流动。
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公开(公告)号：US20050159703A1
公开(公告)日：2005-07-21
申请号：US11076712
申请日：2005-03-10
CPC分类号： A61M25/1011
摘要： To provide infusion therapy that can effectively transluminally deliver drugs or the like to a target spot without invading areas other than a diseased area. The infusion therapy is for administering a drug, cells or the like, or inserting a treatment instrument into the target diseased area. A blood vessel area including a bifurcated blood vessel connecting to the diseased area is occluded at the distal and the proximal region thereof to form an occluded area, and the drugs or the like are pumped and supplied to the occluded area, which causes the drugs or the like to flow retrogressively and retentively in the bifurcated blood vessel connecting in the occluded area, and be infused and administered to the diseased area.
摘要翻译： 提供可以有效地将药物等递送到目标点的输注治疗，而不侵入除病变区域之外的区域。 输注治疗是用于给予药物，细胞等，或者将治疗仪器插入目标患病区域。 包括与病变区域连接的分叉血管的血管区域被封闭在其远侧和近端区域处以形成闭塞区域，并且将药物等泵送并供应到闭塞区域，这导致药物或 类似物在连接在闭塞区域的分叉血管中逆行流畅地流动，并被输注并施用于患病区域。
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8.发明申请TOPICAL THERAPEUTIC AGENT FOR OPHTHALMIC DISEASES COMPRISING COMPOUND CAPABLE OF BINDING SPECIFICALLY TO DNA SEQUENCE 审中-公开适用于DNA序列特异性结合的化合物的眼科治疗药物的局部治疗剂公开(公告)号：US20120071628A1
公开(公告)日：2012-03-22
申请号：US13256012
申请日：2009-09-15
申请人： Hiroki Nagase , Min Chen , Tohru Sakimoto , Takayoshi Watanabe , Noboru Fukuda
发明人： Hiroki Nagase , Min Chen , Tohru Sakimoto , Takayoshi Watanabe , Noboru Fukuda
CPC分类号： C07D403/14 , A61K9/0048 , A61K31/787 , C12N15/11 , C12N15/111 , C12N15/113 , C12N15/1136 , C12N15/1137 , C12N2310/15 , C12N2310/18 , C12N2320/30
摘要： Disclosed is a topical therapeutic agent for ophthalmic diseases, which comprises a compound capable of binding specifically to a DNA sequence. More preferably disclosed is a topical therapeutic agent for ophthalmic diseases, which comprise a pyrrole-imidazole polyamide having a specific structure. The topical therapeutic agent for ophthalmic diseases comprises a pyrrole-imidazole polyamide which can inhibit transforming growth factor-β gene and matrix metalloproteinase 9 gene.
摘要翻译： 公开了一种眼科疾病的局部治疗剂，其包含能够特异性结合DNA序列的化合物。 更优选地公开的是用于眼科疾病的局部治疗剂，其包含具有特定结构的吡咯 - 咪唑聚酰胺。 用于眼科疾病的局部治疗剂包括可抑制转化生长因子-bgr的吡咯 - 咪唑聚酰胺; 基因和基质金属蛋白酶9基因。
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公开(公告)号：US20080103187A1
公开(公告)日：2008-05-01
申请号：US10570159
申请日：2004-09-03
IPC分类号： A61K31/4178 , C07D403/14
CPC分类号： C07D403/14
摘要： A TGF-β gene expression inhibitor containing a pyrrole-imidazole polyamide having N-methylimidazole unit (hereinafter also referred to as Py), N-methylimidazole unit (hereinafter also referred to as Im) and γ-aminobutyrate unit which can be holded into an U-shaped conformation at the γ-aminobutyrate unit in the minor groove in a double helix region (hereinafter referred to as the target region) containing a complementary chain corresponding to the sequence at the -557 to -536 in the base sequence of a human transforming growth factor β1 (hereinafter also referred to as hTGF-β1) promoter, either as a whole or a part thereof: TAAAGGAGAGCAATTCT-TACAG (SEQ ID NO: 1) wherein a Py/Im pair corresponds to a C-G base pair, an Im/Py pair corresponds to a G-C base pair, and Py/Py pairs correspond respectively to an A-A base pair and a T-A base pair.
摘要翻译： 含有具有N-甲基咪唑单元（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-氨基丁酸酯单元的TGF-β基因表达抑制剂，其可以保持在 在双螺旋区域（以下称为靶区域）的小沟槽中的γ-氨基丁酸酯单元处的U型构象，其含有对应于人类碱基序列中-557至-536处的序列的互补链 作为整体或其一部分的转化生长因子β1（以下也称为hTGF-β1）启动子：TAAAGGAGAGCAATTCT-TACAG（SEQ ID NO：1），其中Py / Im对对应于CG碱基对，Im / Py对对应于GC碱基对，Py / Py对分别对应于AA碱基对和TA碱基对。
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公开(公告)号：US20100273997A1
公开(公告)日：2010-10-28
申请号：US11501049
申请日：2006-08-09
IPC分类号： C07H21/02
CPC分类号： C12N15/1131 , C12N2310/121 , C12Q1/701 , C12Q2521/337
摘要： Provided is a ribozyme to cleave a coronavirus gene and a therapeutic agent for a coronavirus infectious disease. A common base sequence in coronaviruses such as SARS-CoV and MHV was searched to design a ribozyme including a base sequence complementary thereto. Moreover, a therapeutic agent for a coronavirus infectious disease including such ribozyme was obtained.
摘要翻译： 提供了切割冠状病毒基因的核酶和冠状病毒感染性疾病的治疗剂。 搜索冠状病毒如SARS-CoV和MHV中的共同碱基序列来设计包含与其互补的碱基序列的核酶。 此外，获得了包含这种核酶的冠状病毒感染性疾病的治疗剂。
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