公开(公告)号：US08436210B2

公开(公告)日：2013-05-07

申请号：US12740064

申请日：2008-11-06

Applicant: Hiroaki Suga ,  Jun Igarashi

Inventor： Hiroaki Suga ,  Jun Igarashi

IPC: C07C233/31 ,  C07C235/14 ,  C07C211/00

CPC classification number: C07C233/32 ,  A01N37/18 ,  A01N37/42 ,  C07C235/14 ,  C07C235/80 ,  C07C2601/16

Abstract: The present invention provides an amide compound having antibacterial activity, and a bacterial infection control agent for agricultural and horticultural use that contains the amide compound. The novel amide compound of the present invention is represented by General Formula (1): wherein R is a —CH(R1)(R2) or a —CO(R2) group, R1 is a hydrogen atom or a hydroxyl group, and R2 is a C1-12 alkyl group.

Abstract translation: 本发明提供具有抗菌活性的酰胺化合物和含有酰胺化合物的农业和园艺用细菌感染控制剂。 本发明的新型酰胺化合物由通式（1）表示：其中R是-CH（R 1）（R 2）或-CO（R 2）基团，R 1是氢原子或羟基，R 2 是C1-12烷基。

公开(公告)号：US20100168380A1

公开(公告)日：2010-07-01

申请号：US12593221

申请日：2008-03-26

Applicant: Hiroaki Suga ,  Hiroshi Murakami ,  Yuki Goto ,  Yusuke Yamagishi ,  Hiroshi Ashigai ,  Yusuke Sako

Inventor： Hiroaki Suga ,  Hiroshi Murakami ,  Yuki Goto ,  Yusuke Yamagishi ,  Hiroshi Ashigai ,  Yusuke Sako

IPC: C07K1/00 ,  C12P21/00

CPC classification number: C07K7/56 ,  C07K7/06 ,  C07K7/08 ,  C12N15/67 ,  C12P21/02

Abstract: The objective is to provide a novel process for synthesizing a cyclic peptide compound. It is also an objective to provide a novel cyclic peptide compound. The novel process for synthesizing a cyclic peptide compound comprises the steps of: (1) translationally synthesizing a non-cyclic peptide compound having in a molecule a functional group 1 and a functional group 2, which are a pair of functional groups capable of reacting to form a bond, and (2) cyclizing the non-cyclic peptide compound by the reaction of the functional groups 1 and 2 to form a bond. The novel cyclic peptide compound can be synthesized by the process.

Abstract translation: 目的是提供一种合成环肽化合物的新方法。 提供新的环肽化合物也是目的。 用于合成环肽化合物的新方法包括以下步骤：（1）在分子中转化合成具有官能团1和官能团2的能够对 形成键，和（2）通过官能团1和2的反应使非环肽化合物环化以形成键。 可以通过该方法合成新的环肽化合物。

公开(公告)号：US07498292B2

公开(公告)日：2009-03-03

申请号：US10637940

申请日：2003-08-08

Applicant: Hiroaki Suga ,  Yigong Bu

Inventor： Hiroaki Suga ,  Yigong Bu

IPC: C40B40/02

CPC classification number: C07D285/13 ,  C07C235/74 ,  C07C237/42 ,  C07C2601/08 ,  C07C2601/14 ,  C07D309/10 ,  C07D319/06 ,  Y02P20/582

Abstract: The present invention relates to solid phase or solution phase combinatorial libraries of autoinducer analogs. The present invention also relates to autoinducer agonists and antagonists. In addition, the present invention relates to methods for identifying autoinducer agonists and antagonists, as well as methods for regulating the activity of an autoinducer receptor, regulating biofilm formation, regulating growth or virulence of an organism in a subject, inhibiting the quorum sensing mechanism of an organism, and treating an infection in a subject caused by an organism possessing a quorum sensing mechanism which use the autoinducer analogs of the present invention.

Abstract translation: 本发明涉及自动诱导剂类似物的固相或溶液相组合文库。 本发明还涉及自体诱导剂激动剂和拮抗剂。 此外，本发明还涉及用于鉴定自身诱导剂激动剂和拮抗剂的方法，以及用于调节自身诱导剂受体活性的方法，调节生物膜形成，调节受试者中生物体的生长或毒力，抑制群体感受机制 一种有机体，并且治疗由具有本发明的自动诱导剂类似物的具有群体感应机制的生物体引起的受试者感染。

公开(公告)号：US20080027115A1

公开(公告)日：2008-01-31

申请号：US11834380

申请日：2007-08-06

Applicant: Hiroaki SUGA ,  Yigong BU

Inventor： Hiroaki SUGA ,  Yigong BU

IPC: A61K31/44 ,  A61K31/34 ,  A61P43/00 ,  C07C233/00 ,  C07C233/16 ,  C07D217/00 ,  C07D231/00 ,  C07D231/56 ,  C12N1/20 ,  C12Q1/02 ,  C40B40/04 ,  G01N33/566

CPC classification number: C07D285/13 ,  C07C235/74 ,  C07C237/42 ,  C07C2601/08 ,  C07C2601/14 ,  C07D309/10 ,  C07D319/06 ,  Y02P20/582

Abstract: The present invention relates to solid phase or solution phase combinatorial libraries of autoinducer analogs. The present invention also relates to autoinducer agonists and antagonists. In addition, the present invention relates to methods for identifying autoinducer agonists and antagonists, as well as methods for regulating the activity of an autoinducer receptor, regulating biofilm formation, regulating growth or virulence of an organism in a subject, inhibiting the quorum sensing mechanism of an organism, and treating an infection in a subject caused by an organism possessing a quorum sensing mechanism which use the autoinducer analogs of the present invention.

Abstract translation: 本发明涉及自动诱导剂类似物的固相或溶液相组合文库。 本发明还涉及自体诱导剂激动剂和拮抗剂。 此外，本发明还涉及用于鉴定自身诱导剂激动剂和拮抗剂的方法，以及用于调节自身诱导剂受体活性的方法，调节生物膜形成，调节受试者中生物体的生长或毒力，抑制群体感受机制 一种有机体，并且治疗由具有本发明的自动诱导剂类似物的具有群体感应机制的生物体引起的受试者感染。

公开(公告)号：US20140018257A1

公开(公告)日：2014-01-16

申请号：US13990180

申请日：2011-12-05

Applicant: Hiroaki Suga ,  Jumpei Morimoto

Inventor： Hiroaki Suga ,  Jumpei Morimoto

IPC: B01J19/00

CPC classification number: B01J19/0046 ,  B01J2219/00725 ,  C07K7/08 ,  C07K14/705 ,  C12N15/1062 ,  C12N15/67 ,  C12Q1/34 ,  C40B50/06 ,  C40B50/08

Abstract: Object is to provide a method of constructing a library of peptides having, at a desired position in the random sequence of each peptide, an amino acid having a portion capable of binding to a target. The invention provides a method of producing a library of peptides having, at a designated position in the random sequence of each peptide, a special amino acid having a portion capable of binding to a target, including (i) preparing a library of mRNAs having, in the mRNA sequence coding for a random amino acid sequence, a base sequence having an altered codon encoding the special amino acid, (ii) preparing an aminoacyl tRNA with the special amino acid linked to a tRNA encoded by the altered codon, and (iii) translating the mRNAs by using a cell-free translation system containing the aminoacyl tRNA to obtain a library of peptides having, in the random sequence thereof, a predetermined special amino acid.

Abstract translation: 目的是提供构建肽的文库的方法，其在每个肽的随机序列中的期望位置具有具有能与靶标结合的部分的氨基酸。 本发明提供一种生产肽文库的方法，其在每个肽的随机序列中的指定位置具有具有能与靶标结合的部分的特殊氨基酸，其包括（i）制备mRNA的文库， 在编码随机氨基酸序列的mRNA序列中，具有编码特殊氨基酸的改变的密码子的碱基序列，（ii）用与被改变的密码子编码的tRNA连接的特殊氨基酸制备氨酰基tRNA，和（iii ）通过使用含有氨酰基tRNA的无细胞翻译系统来翻译mRNA，以获得其随机序列中具有预定特殊氨基酸的肽文库。

公开(公告)号：US20120296094A1

公开(公告)日：2012-11-22

申请号：US13567695

申请日：2012-08-06

Applicant: Hiroaki SUGA ,  Jun Igarashi

Inventor： Hiroaki SUGA ,  Jun Igarashi

IPC: C07D207/14 ,  C07D295/32 ,  C07D211/58

CPC classification number: C07D207/50 ,  A01N43/36 ,  A01N43/40 ,  A61K8/4913 ,  A61K8/4926 ,  A61Q11/00 ,  A61Q17/005 ,  C07D207/14 ,  C07D211/58 ,  C07D295/32

Abstract: The present invention provides a new amide compound and salt thereof that is capable of inhibiting biofilm formation or removing deposited biofilms. The present invention also provides a biofilm formation inhibitor or a biofilm remover containing the amide compound or salt thereof as an active ingredient.An amide compound or salt thereof according to the present invention is denoted by General Formula (1): wherein R1 is a hydrogen atom or a hydroxyl group, R2 is a C5-12 alkyl group, and Q is a substituent denoted by Formula (Q1) or (Q2), wherein n and m are 0 or 1.

Abstract translation: 本发明提供了能够抑制生物膜形成或去除沉积的生物膜的新的酰胺化合物及其盐。 本发明还提供了含有酰胺化合物或其盐作为活性成分的生物膜形成抑制剂或生物膜去除剂。 根据本发明的酰胺化合物或其盐由通式（1）表示：其中R1是氢原子或羟基，R2是C5-12烷基，Q是由式（Q1）表示的取代基 ）或（Q2），其中n和m为0或1。

公开(公告)号：US09657289B2

公开(公告)日：2017-05-23

申请号：US13990123

申请日：2011-12-05

Applicant: Hiroaki Suga ,  Takashi Higuchi

Inventor： Hiroaki Suga ,  Takashi Higuchi

IPC: C40B40/10 ,  C12N15/10 ,  C12P11/00 ,  C12P21/02 ,  C07K14/00 ,  C07K1/107 ,  C07K2/00 ,  A61K38/00

CPC classification number: C07K14/001 ,  A61K38/00 ,  C07C229/08 ,  C07K1/107 ,  C07K2/00 ,  C12N15/1062 ,  C12P11/00 ,  C12P21/02 ,  C40B40/10 ,  G01N33/6845

Abstract: An object of the invention is to provide a peptide having a stabilized secondary structure.The present invention provides a peptide having a secondary structure stabilized by a crosslinked structure and containing at least one combination of a special amino acid of the formula (I): (wherein, (A) represents a single bond or a linking group having, in the main chain thereof, from 1 to 10 atoms; (B) represents a group containing at least one π bond; (C) represents a hydrogen atom or an alkyl group which may be substituted with a substituent; and X represents a group substitutable by a substitution reaction with a sulfanyl group) and an amino acid having, in the side chain thereof, a sulfanyl group; and having the crosslinked structure formed through a thioether bond between the side chain of the special amino acid residue and the sulfanyl group.

公开(公告)号：US20130217599A1

公开(公告)日：2013-08-22

申请号：US13816911

申请日：2011-08-26

Applicant: Hiroaki Suga ,  Hiroshi Murakami ,  Yuki Goto

Inventor： Hiroaki Suga ,  Hiroshi Murakami ,  Yuki Goto

IPC: C12P21/00

CPC classification number: C12P21/00 ,  C12N15/67 ,  C12P21/02

Abstract: A new artificial translation-synthesis system of adding tRNAs binding special amino acids to the in vitro translation system and synthesizing peptides with special amino acids incorporated thereto according to a dual genetic code table and an artificial codon box division.

Abstract translation: 一种新的人工翻译 - 合成系统，其将特异性氨基酸结合到体外翻译系统中并根据双重遗传密码表和人造密码子分组合成具有特异氨基酸的肽。

公开(公告)号：US20130178394A1

公开(公告)日：2013-07-11

申请号：US13821940

申请日：2011-09-08

Applicant: Hiroaki Suga ,  Yusuke Yamagishi

Inventor： Hiroaki Suga ,  Yusuke Yamagishi

IPC: C12N15/10

CPC classification number: C12N15/1062 ,  C07K2/00 ,  C12N15/67 ,  C12P21/02 ,  C40B20/04 ,  C40B30/04 ,  C40B40/10 ,  C40B50/06 ,  G01N2500/00 ,  G01N2500/20

Abstract: A method for screening a non-standard peptide compound in the peptide library that binds to the target substance, comprising the steps: (i) preparing a non-standard peptide library wherein a special (non-standard) amino acid is randomly incorporated into the peptide sequence by a cell-free (in vitro) translation system comprising a tRNA acylated by a special (non-standard) amino acid; (ii) bringing the obtained peptide library in contact with a target substance; and (iii) selecting a non-standard peptide that binds to the target substance as an active peptide.

Abstract translation: 一种用于筛选结合靶物质的肽文库中的非标准肽化合物的方法，包括以下步骤：（i）制备非标准肽文库，其中将特殊（非标准）氨基酸随机并入到 通过包含通过特殊（非标准）氨基酸酰化的tRNA的无细胞（体外）翻译系统的肽序列; （ii）使获得的肽文库与目标物质接触; 和（iii）选择与靶物质结合的非标准肽作为活性肽。

公开(公告)号：US20110275119A1

公开(公告)日：2011-11-10

申请号：US12515074

申请日：2007-11-13

Applicant: Hiroaki Suga ,  Hiroshi Murakami ,  Yuki Goto ,  Atsushi Ohta

Inventor： Hiroaki Suga ,  Hiroshi Murakami ,  Yuki Goto ,  Atsushi Ohta

IPC: C12P21/00 ,  C12N9/10

CPC classification number: C12N15/67 ,  C12P21/02

Abstract: The present invention aims to synthesize a polypeptide having an unnatural structure at the N-terminus via a biosynthetic process by translation of amino acid sequence information encoded by a nucleic acid. A polypeptide having any amino acid at the N-terminus is synthesized by using an ARS ribozyme that catalyzes the acylation of tRNA with any amino acid to attach any amino acid to an initiator tRNA, thereby initiating a translation with the initiator tRNA.

Abstract translation: 本发明旨在通过生物合成方法通过翻译由核酸编码的氨基酸序列信息在N末端合成具有非天然结构的多肽。 通过使用催化tRNA与任何氨基酸酰化以将任何氨基酸连接至引发剂tRNA的ARS核酶合成在N末端具有任何氨基酸的多肽，从而开始与引发剂tRNA的翻译。