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1. 发明授权

US5854391A Glycosylation of peptides using glycosyl phosphite reagents 失效
标题翻译：使用糖基亚磷酸酯试剂对肽进行糖基化
公开(公告)号：US5854391A
公开(公告)日：1998-12-29
申请号：US33513
申请日：1993-03-18
申请人： Chi-Huey Wong , Hirosato Kondo
发明人： Chi-Huey Wong , Hirosato Kondo
IPC分类号： C07K1/107 , C07K9/00
CPC分类号： C07K9/00 , C07K1/1077
摘要： A method for synthesizing glycosylated peptides employs a blocked carbohydrate donor and a blocked peptide acceptor. The carbohydrate donor includes an acid labile phosphite leaving group attached to the anomeric carbon. The blocked peptide acceptor includes an unprotected hydroxyl group susceptible to electrophilic attack. Serine hydroxyl is preferred. The reaction is initiated by the addition of a Lewis acid so as to activate the acid labile phosphite leaving group on the carbohydrate donor. The substitution reaction may be conducted at -78.degree. C. in a solvent such as Et.sub.3 N which favors the formation of glycosylated peptide products.
摘要翻译：合成糖基化肽的方法采用封闭的碳水化合物供体和封闭的肽受体。碳水化合物供体包括与异头碳连接的离去基团的酸不稳定的亚磷酸酯。封闭的肽受体包括易受亲电攻击的未保护的羟基。丝氨酸羟基是优选的。通过加入路易斯酸来引发反应，以活化碳水化合物供体上的酸不稳定亚磷酸酯离去基团。取代反应可以在-78℃下在有利于糖基化肽产物形成的溶剂如Et 3 N中进行。

2. 发明授权

US4853469A Quinolinecarboxylic acid derivative starting compounds 失效
标题翻译：喹啉羧酸衍生物起始化合物
公开(公告)号：US4853469A
公开(公告)日：1989-08-01
申请号：US225369
申请日：1988-07-28
申请人： Masahiro Taguchi , Hirosato Kondo , Yoshimasa Inoue , Yoshihiro Kawahata , Goro Tsukamoto
发明人： Masahiro Taguchi , Hirosato Kondo , Yoshimasa Inoue , Yoshihiro Kawahata , Goro Tsukamoto
IPC分类号： C07D513/16 , A61K31/44 , A61K31/535 , A61P31/04 , C07D513/04
CPC分类号： C07D513/04
摘要： Novel quinolinecarboxylic derivatives of the formula: ##STR1## wherein Z is ##STR2## in which R.sup.1 is hydrogen atom or a lower alkyl, R.sup.2 is hydrogen atom, hydroxyl or a lower alkyl and R.sup.3 is hydrogen atom, hydroxyl or an amino, and a pharmaceutical salt thereof have excellent antibacterial activities and are useful as an antibacterial agent.

3. 发明授权

US5597906A Carbon linked glycosyl compounds 失效
标题翻译：碳链糖基化合物
公开(公告)号：US5597906A
公开(公告)日：1997-01-28
申请号：US33608
申请日：1993-03-18
申请人： Chi-Huey Wong , Hirosato Kondo
发明人： Chi-Huey Wong , Hirosato Kondo
IPC分类号： C07D309/10 , C07H15/00
CPC分类号： C07D309/10
摘要： Carbon linked glycosyl compounds are disclosed and synthesized. The synthesis employs a blocked carbohydrate donor and a blocked glycosyl acceptor. The blocked carbohydrate donor includes an acid labile phosphite leaving group attached to the anomeric carbon. The blocked glycosyl acceptor includes an unprotected carbon susceptible to electrophilic attack. The reaction is initiated by the addition of a Lewis acid so as to activate the acid labile phosphite leaving group on the carbohydrate donor. The substitution reaction may be conducted at -78.degree. C. in a solvent which favors the formation of carbon linked glycosylation products.
摘要翻译：公开并合成了碳链糖基化合物。该合成使用封闭的碳水化合物供体和封闭的糖基受体。封闭的碳水化合物供体包括与异头碳连接的酸不稳定的亚磷酸酯离去基团。封闭的糖基受体包括易受亲电发作的未受保护的碳。通过加入路易斯酸来引发反应，以活化碳水化合物供体上的酸不稳定亚磷酸酯离去基团。取代反应可以在-78℃下在有利于形成碳连接的糖基化产物的溶剂中进行。

4. 发明授权

US4808584A Quinolinecarboxylic acid derivatives and antibacterial agent containing the same 失效
标题翻译：喹啉羧酸衍生物和含有它的抗菌剂
公开(公告)号：US4808584A
公开(公告)日：1989-02-28
申请号：US178603
申请日：1988-04-07
申请人： Masahiro Taguchi , Hirosato Kondo , Yoshimasa Inoue , Yoshihiro Kawahata , Goro Tsukamoto
发明人： Masahiro Taguchi , Hirosato Kondo , Yoshimasa Inoue , Yoshihiro Kawahata , Goro Tsukamoto
IPC分类号： C07D513/16 , A61K31/44 , A61K31/535 , A61P31/04 , C07D513/04 , C07D498/16
CPC分类号： C07D513/04
摘要： Novel quinolinecarboxylic derivatives of the formula: ##STR1## wherein Z is ##STR2## in which R.sup.1 is hydrogen atom or a lower alkyl, R.sup.2 is hydrogen atom, hydroxyl or a lower alkyl and R.sup.3 is hydrogen atom, hydroxyl or an amino, and a pharmaceutical salt thereof have excellent antibacterial activities and are useful as an antibacterial agent.

5. 发明授权

US4971967A Quinolinecarboxylic acid derivatives, antibacterial compositions and use 失效
标题翻译：喹啉羧酸衍生物，抗菌组合物及用途
公开(公告)号：US4971967A
公开(公告)日：1990-11-20
申请号：US493455
申请日：1990-03-14
申请人： Hirosato Kondo , Masahiro Taguchi , Yoshimasa Inoue , Fumio Sakamoto
发明人： Hirosato Kondo , Masahiro Taguchi , Yoshimasa Inoue , Fumio Sakamoto
IPC分类号： C07D513/16
CPC分类号： C07D513/16
摘要： Novel quinolinecarboxylic acid derivatives of the formula: ##STR1## wherein Z is ##STR2## in which R.sup.1 and R.sup.2 are each hydrogen atom or a lower alkyl, R.sup.3 is hydrogen atom, hydroxy or a lower alkyl and R.sup.4 is hydrogen atom, hydroxy, amino, aminomethyl, a (lower alkyl)aminomethyl or a di(lower alkyl)aminomethyl, and a pharmaceutically acceptable salt thereof. The compounds have excellent antibacterial activities and are useful as an antibacterial agent.

6. 发明申请

US20080113924A1 Neuramindase Inhibitor 审中-公开
标题翻译：神经酰胺糖苷酶抑制剂
公开(公告)号：US20080113924A1
公开(公告)日：2008-05-15
申请号：US11721581
申请日：2005-12-16
申请人： Shinichiro Nishimura , Hiroshi Hinou , Hirosato Kondo , Kazuhiko Fujiwara
发明人： Shinichiro Nishimura , Hiroshi Hinou , Hirosato Kondo , Kazuhiko Fujiwara
IPC分类号： A61K31/7048 , A61K31/366 , A61K31/35 , C07D311/02
CPC分类号： C07H15/203 , C07H15/26 , C07H17/075 , C12Q1/04 , C12Q1/34 , G01N2333/924 , G01N2800/26
摘要： There are provided a novel compound having irreversible inhibitory activity against neuraminidase, a therapeutic agent and a detection agent for a disease involving neuraminidase. A compound represented by the following formula (I) and a salt thereof, a production method thereof, and an application method thereof, wherein: A1 represents an aryl group optionally having a substituent group or a heteroaryl group optionally having a substituent group; A2 represents —CX2R6 or —CHXR6 wherein X represents —F, —Cl, —Br, or —I; R1 represents a hydrogen atom or an alkyl group optionally having a substituent group; R2, R3, R4, and R5 represent each independently —OC(═O)R6, —OR6, —N(R6)2, —N3, —NHC(═NH)NHR6, —NHCOR6, —OSO3R6, —OPO3(R6)2, F, Cl, Br, or I; and R6 represents each independently a hydrogen atom, an alkyl group optionally having a substituent group, an aryl group optionally having a substituent group, or an optionally substituted heteroaryl group.
摘要翻译：提供了对神经氨酸酶具有不可逆抑制活性的新型化合物，治疗剂和涉及神经氨酸酶的疾病检测剂。由下式（I）表示的化合物及其盐，其制备方法及其施加方法，其中：A 1表示任选具有取代基的芳基或杂芳基任选具有取代基; 其中X代表-F，-Cl， - ， - ， - Br或-I; R 1表示氢原子或任选具有取代基的烷基; R 2，R 3，R 4和R 5各自独立地表示-OC（-O）R 6， - 6， - （R 6）2 - ， - N 3 - ，-NHC（-NH）NHR 6，-NHCOR 6，-OSO 3，＆lt; 6＆lt; 6＆gt; -OPO 3（R 6）2，F，Cl，Br或I; 和R 6各自独立地表示氢原子，任选具有取代基的烷基，任选具有取代基的芳基或任选取代的杂芳基。

7. 发明授权

US06518418B1 Nucleotide sugars 失效
标题翻译：核苷酸糖
公开(公告)号：US06518418B1
公开(公告)日：2003-02-11
申请号：US07991182
申请日：1992-12-10
申请人： Chi-Huey Wong , Hirosato Kondo
发明人： Chi-Huey Wong , Hirosato Kondo
IPC分类号： C07H2100
CPC分类号： C07H5/02 , C07H3/06 , C07H11/04 , C07H13/04 , C07H13/08 , C07H15/18 , C07H19/20 , C12P19/18 , C12P19/26
摘要： Phosphite linked nucleotide sugars, e.g. nucleoside-monophosphite-glycosides, are synthesized using phosphoramiditing agents. The success of the synthetic method is largely independent of the choice of sugar and of nucleotide. The phosphite linked nucleotide sugars are shown to be useful, in the presence of an oxidizing agent, for the production of phosphate linked nucleotide sugars, e.g. nucleoside-monophosphate-glycosides.
摘要翻译：亚磷酸酯连接的核苷酸糖，例如核苷 - 单亚磷酸酯 - 糖苷，使用磷酰胺试剂合成。合成方法的成功在很大程度上取决于糖和核苷酸的选择。亚磷酸酯连接的核苷酸糖显示在氧化剂存在下可用于生产磷酸酯连接的核苷酸糖，例如，核苷单磷酸苷。

8. 发明授权

US5514784A Thio linked glycosyl compounds 失效
标题翻译：硫醇连接糖基化合物
公开(公告)号：US5514784A
公开(公告)日：1996-05-07
申请号：US36334
申请日：1993-03-19
申请人： Chi-Huey Wong , Hirosato Kondo
发明人： Chi-Huey Wong , Hirosato Kondo
IPC分类号： C07H15/203 , C07G3/00 , C07G11/00 , C07H15/00 , C07H17/00
CPC分类号： C07H15/203
摘要： Thio linked glycosyl compounds are disclosed and synthesized. The synthesis employs a blocked carbohydrate donor and a blocked glycosyl acceptor. The carbohydrate donor includes an acid labile phosphite leaving group attached to the anomeric carbon. The blocked glycosyl acceptor includes an unprotected thio group susceptible to electrophilic attack. The reaction is initiated by the addition of a Lewis acid so as to activate the acid labile phosphite leaving group on the carbohydrate donor. The substitution reaction may be conducted at -78.degree. C. in a solvent such as Et.sub.3 N which favors the formation of thio linked glycosylation products.
摘要翻译：公开并合成了Thio连接的糖基化合物。该合成使用封闭的碳水化合物供体和封闭的糖基受体。碳水化合物供体包括与异头碳连接的离去基团的酸不稳定的亚磷酸酯。封闭的糖基受体包括易受亲电发作攻击的未受保护的硫代基团。通过加入路易斯酸来引发反应，以活化碳水化合物供体上的酸不稳定亚磷酸酯离去基团。取代反应可以在-78℃下在诸如Et 3 N的溶剂中进行，这有利于硫代连接的糖基化产物的形成。

9. 发明授权

US5191079A Quinolinecarboxylic acid derivatives 失效
标题翻译：喹喔啉羧酸衍生物
公开(公告)号：US5191079A
公开(公告)日：1993-03-02
申请号：US907184
申请日：1992-06-30
申请人： Hirosato Kondo , Masahiro Taguchi , Yoshikazu Jinbo , Yoshimasa Inoue , Yasuo Kotera , Fumio Sakamoto
发明人： Hirosato Kondo , Masahiro Taguchi , Yoshikazu Jinbo , Yoshimasa Inoue , Yasuo Kotera , Fumio Sakamoto
IPC分类号： C07D513/16 , C07D519/00
CPC分类号： C07D513/16 , C07D519/00
摘要： Novel quinolinecarboxylic acid derivatives of the formula: ##STR1## wherein Z is ##STR2## in which R.sup.1 is hydrogen atom, a halogen atom, hydroxy or a lower alkyloxy; R.sup.2 is a halogen atom, hydroxy or a lower alkyloxy; R.sup.3 is a lower alkyl; and R.sup.4 is hydroxy or a di(lower alkyl)amino, and a pharmaceutically acceptable salt thereof, which have excellent antibacterial activities and are useful as an antibacterial agent, a pharmaceutical composition containing the same, and process for preparing the same.

10. 发明授权

US4686221A Quinolinecarboxylic acid compounds and antimicrobial agent containing the same 失效
标题翻译：喹啉羧酸化合物和含有其的抗微生物剂
公开(公告)号：US4686221A
公开(公告)日：1987-08-11
申请号：US913382
申请日：1986-09-30
申请人： Toshio Uno , Masahiro Taguchi , Toshimi Okuno , Hirosato Kondo , Mikio Sotomura , Goro Tsukamoto
发明人： Toshio Uno , Masahiro Taguchi , Toshimi Okuno , Hirosato Kondo , Mikio Sotomura , Goro Tsukamoto
IPC分类号： C07D215/56 , A61K31/495 , C07D401/04
CPC分类号： C07D215/56
摘要： Novel compounds of the formula: ##STR1## wherein R is ethyl, 2-fluoroethyl or cyclopropyl, and X is hydrogen atom or fluorine atom, and a pharmaceutically acceptable salt thereof, which have excellent antimicrobial activities in vivo and hence are useful as an antimicrobial agent, and an antimicrobial composition containing said compound as an active ingredient, and processes for the preparation of the compounds.
摘要翻译：下式的新型化合物：其中R是乙基，2-氟乙基或环丙基，X是氢原子或氟原子及其药学上可接受的盐，其在体内具有优异的抗微生物活性，因此是有用的作为抗菌剂，以及含有所述化合物作为活性成分的抗微生物组合物，以及所述化合物的制备方法。

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