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1. 发明授权

US06329519B1 Intermediates for oligonucleotide synthesis 有权
标题翻译：寡核苷酸合成中间体
公开(公告)号：US06329519B1
公开(公告)日：2001-12-11
申请号：US09202294
申请日：1999-03-15
申请人： Stephen Paul Collingwood , Heinz Ernst Moser , Karl-Heinz Altmann , Mark Edward Douglas
发明人： Stephen Paul Collingwood , Heinz Ernst Moser , Karl-Heinz Altmann , Mark Edward Douglas
IPC分类号： C07H1920
CPC分类号： C07H19/04 , Y02P20/55
摘要： A compound of formula (I) wherein B1 is a radical of a nucleoside base, R1 is hydrogen or a hydroxy-protecting group, R2 is hydrogen, hydroxy or a 2′-nucleoside-modifying atom or group, R3 is an unsubstituted or substituted C1 to C10 alkyl, C2 to C10 alkenyl, C4 to C10 cycloalkylalkyl, C6 to C10 aryl or C7 to C13 aralkyl group, and Z is halogen or a group of formula (II) where R4 and R5 are each independently an unsubstituted or substituted C1 to C10 alkyl, C2 to C10 alkenyl, C4 to C10 cycloalkylalkyl, C6 to C10 aryl or C7 to C13 aralkyl group, or R4 is said group and R5 is hydrogen or R4 and R5 together with the nitrogen atom to which they are attached denote a five- to thirteen-membered heterocyclic ring, or Z is a group of formula (III): Nuc-O—, where Nuc is the residue of a natural or synthetic nucleoside or oligonucleotide after removal of a 5′-hydroxyl group therefrom attached through a 5′-methylene thereof to the indicated oxygen atom.
摘要翻译：式（I）的化合物，其中B1是核苷碱基的基团，R1是氢或羟基保护基，R2是氢，羟基或2'-核苷修饰的原子或基团，R3是未取代或取代的 C1至C10烷基，C2至C10烯基，C4至C10环烷基烷基，C6至C10芳基或C7至C13芳烷基，Z为卤素或式（Ⅱ）基团，其中R4和R5各自独立地为未取代或取代的C1 C 10至C 10链烯基，C 4至C 10环烷基烷基，C 6至C 10芳基或C 7至C 13芳烷基，或R 4为所述基团，R 5为氢或R 4和R 5与它们所连接的氮原子一起表示 5至13元杂环，或Z为式（III）的基团：Nuc-O-，其中Nuc是除去其中的5'-羟基之后天然或合成的核苷或寡核苷酸的残基，其通过其指示氧原子的5'-亚甲基。

2. 发明授权

US06670468B1 2′-substituted nucleosides and oligonucleotide derivatives 有权
标题翻译： 2'-取代核苷和寡核苷酸衍生物
公开(公告)号：US06670468B1
公开(公告)日：2003-12-30
申请号：US09753943
申请日：2001-01-03
申请人： Bernard Cuenoud , Karl-Heinz Altmann , Pierre Martin , Heinz Ernst Moser
发明人： Bernard Cuenoud , Karl-Heinz Altmann , Pierre Martin , Heinz Ernst Moser
IPC分类号： C07H2104
CPC分类号： C07H21/00
摘要： The invention relates to an oligonucleotide derivative which comprises at least one nucleoside building block of the formula (I) The invention furthermore relates to nucleoside building blocks, intermediates and processes for preparing the oligonucleotide derivatives and the nucleoside building blocks. The invention also relates to pharmaceutical compositions and to uses of the oligonucleotide derivatives and the nucleoside building blocks.
摘要翻译：本发明涉及包含至少一种式（I）核苷结构单元的寡核苷酸衍生物。本发明还涉及核苷结构单元，中间体和制备寡核苷酸衍生物和核苷结构单元的方法。本发明还涉及药物组合物以及寡核苷酸衍生物和核苷结构单元的用途。

3. 发明授权

US08372813B2 Antibacterial aminoglycoside analogs 有权
标题翻译：抗菌氨基糖苷类似物
公开(公告)号：US08372813B2
公开(公告)日：2013-02-12
申请号：US13082143
申请日：2011-04-07
申请人： James Bradley Aggen , Martin Sheringham Linsell , Adam Aaron Goldblum , Darin James Hildebrandt , Timothy Robert Kane , Paola Dozzo , Micah James Gliedt , Heinz Ernst Moser
发明人： James Bradley Aggen , Martin Sheringham Linsell , Adam Aaron Goldblum , Darin James Hildebrandt , Timothy Robert Kane , Paola Dozzo , Micah James Gliedt , Heinz Ernst Moser
IPC分类号： A01N43/04 , A61K31/70 , C07H15/22
CPC分类号： C07H15/232
摘要： Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
摘要翻译：公开了具有抗菌活性的化合物。该化合物具有以下结构（I）：包括立体异构体，其药学上可接受的盐和前药，其中Q1，Q2，R1，R2和R3如本文所定义。还公开了与这种化合物的制备和使用相关的方法以及包含这些化合物的药物组合物。

4. 发明申请

US20080300199A1 ANTIBACTERIAL 1,4,5-SUBSTITUTED AMINOGLYCOSIDE ANALOGS 审中-公开
标题翻译：抗菌素1,4,5-取代的氨基糖苷类似物
公开(公告)号：US20080300199A1
公开(公告)日：2008-12-04
申请号：US12100981
申请日：2008-04-10
申请人： Martin Linsell , Adam Aaron Goldblum , James Aggen , Heinz Ernst Moser , Stephen Hanessian , Kandasamy Pachamuthu , Ellen Klegraf
发明人： Martin Linsell , Adam Aaron Goldblum , James Aggen , Heinz Ernst Moser , Stephen Hanessian , Kandasamy Pachamuthu , Ellen Klegraf
IPC分类号： A61K31/7036 , C07G11/00 , A61P31/04
CPC分类号： C07H15/232
摘要： The present invention is directed to analogs of aminoglycoside compounds as well as their preparation and use as prophylactic or therapeutics against microbial infection.
摘要翻译：本发明涉及氨基糖苷类化合物的类似物以及它们作为抗微生物感染的预防或治疗剂的制备和用途。

5. 发明申请

US20120172332A1 ANTIBACTERIAL AMINOGLYCOSIDE ANALOGS 有权
标题翻译：抗菌胺类化合物
公开(公告)号：US20120172332A1
公开(公告)日：2012-07-05
申请号：US13082143
申请日：2011-04-07
申请人： James Bradley Aggen , Martin Sheringham Linsell , Adam Aaron Goldblum , Darin James Hildebrandt , Timothy Robert Kane , Paola Dozzo , Micah James Gliedt , Heinz Ernst Moser
发明人： James Bradley Aggen , Martin Sheringham Linsell , Adam Aaron Goldblum , Darin James Hildebrandt , Timothy Robert Kane , Paola Dozzo , Micah James Gliedt , Heinz Ernst Moser
IPC分类号： A61K31/7008 , A61P31/04 , C07H5/06
CPC分类号： C07H15/232
摘要： Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
摘要翻译：公开了具有抗菌活性的化合物。该化合物具有以下结构（I）：包括立体异构体，其药学上可接受的盐和前药，其中Q1，Q2，R1，R2和R3如本文所定义。还公开了与这种化合物的制备和使用相关的方法以及包含这些化合物的药物组合物。

6. 发明授权

US09174978B2 Monobactam organic compounds for the treatment of bacterial infections 有权
标题翻译：单链有机化合物用于治疗细菌感染
公开(公告)号：US09174978B2
公开(公告)日：2015-11-03
申请号：US14665245
申请日：2015-03-23
申请人： Virender Singh Aulakh , Anthony Casarez , Xiaodong Lin , Mika Lindvall , Glenn McEnroe , Heinz Ernst Moser , Folkert Reck , Meiliana Tjandra , Robert Lowell Simmons , Aregahegn Yifru , Qingming Zhu
发明人： Virender Singh Aulakh , Anthony Casarez , Xiaodong Lin , Mika Lindvall , Glenn McEnroe , Heinz Ernst Moser , Folkert Reck , Meiliana Tjandra , Robert Lowell Simmons , Aregahegn Yifru , Qingming Zhu
IPC分类号： A61K31/40 , C07D417/14 , A61K31/427 , A61K31/454 , A61K31/4439 , A61K31/433 , A61K31/496 , A61K31/4545 , C07D487/04 , A61K45/06
CPC分类号： A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K45/06 , C07D417/14 , C07D487/04 , Y02A50/473 , Y02A50/481
摘要： This invention pertains generally to antibacterial compounds of Formula I, as further described herein, and pharmaceutically acceptable salts and formulations thereof. In certain aspects, the invention pertains to methods of using such compounds to treat infections such as those caused by Gram-negative bacteria.
摘要翻译：本发明一般涉及本文进一步描述的式I抗菌化合物及其药学上可接受的盐和制剂。在某些方面，本发明涉及使用这些化合物治疗诸如革兰氏阴性菌引起的感染的方法。

7. 发明授权

US08367625B2 Antibacterial aminoglycoside analogs 有权
公开(公告)号：US08367625B2
公开(公告)日：2013-02-05
申请号：US13082141
申请日：2011-04-07
申请人： James Bradley Aggen , Martin Sheringham Linsell , Adam Aaron Goldblum , Darin James Hildebrandt , Timothy Robert Kane , Paola Dozzo , Micah James Gliedt , Heinz Ernst Moser
发明人： James Bradley Aggen , Martin Sheringham Linsell , Adam Aaron Goldblum , Darin James Hildebrandt , Timothy Robert Kane , Paola Dozzo , Micah James Gliedt , Heinz Ernst Moser
IPC分类号： A01N43/04 , A61K31/70 , C07H15/22
CPC分类号： C07H15/232
摘要： Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

8. 发明申请

US20110288041A1 ANTIBACTERIAL AMINOGLYCOSIDE ANALOGS 有权
标题翻译：抗菌胺类化合物
公开(公告)号：US20110288041A1
公开(公告)日：2011-11-24
申请号：US13082141
申请日：2011-04-07
申请人： James Bradley Aggen , Martin Sheringham Linsell , Adam Aaron Goldblum , Darin James Hildebrandt , Timothy Robert Kane , Paola Dozzo , Micah James Gliedt , Heinz Ernst Moser
发明人： James Bradley Aggen , Martin Sheringham Linsell , Adam Aaron Goldblum , Darin James Hildebrandt , Timothy Robert Kane , Paola Dozzo , Micah James Gliedt , Heinz Ernst Moser
IPC分类号： A61K31/7048 , A61P31/04 , C07H15/26
CPC分类号： C07H15/232
摘要： Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, R1, R2 and R3 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
摘要翻译：公开了具有抗菌活性的化合物。该化合物具有以下结构（I）：包括立体异构体，其药学上可接受的盐和前药，其中Q1，Q2，R1，R2和R3如本文所定义。还公开了与这种化合物的制备和使用相关的方法以及包含这些化合物的药物组合物。

9. 发明授权

US08383596B2 Antibacterial aminoglycoside analogs 有权
标题翻译：抗菌氨基糖苷类似物
公开(公告)号：US08383596B2
公开(公告)日：2013-02-26
申请号：US12487427
申请日：2009-06-18
申请人： James Bradley Aggen , Adam Aaron Goldblum , Martin Sheringham Linsell , Paola Dozzo , Heinz Ernst Moser , Darin James Hildebrandt , Micah James Gliedt
发明人： James Bradley Aggen , Adam Aaron Goldblum , Martin Sheringham Linsell , Paola Dozzo , Heinz Ernst Moser , Darin James Hildebrandt , Micah James Gliedt
IPC分类号： A01N43/04 , A61K31/70 , C07H15/20 , C07H15/00 , C07H17/00
CPC分类号： C07H15/224 , A61K31/7036 , C07H15/222 , C07H15/236 , Y02A50/473
摘要： Compounds having antibacterial activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein Q1, Q2, Q3, R8 and R9 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
摘要翻译：公开了具有抗菌活性的化合物。该化合物具有以下结构（I）：包括其立体异构体，药学上可接受的盐和前药，其中Q 1，Q 2，Q 3，R 8和R 9如本文所定义。还公开了与这种化合物的制备和使用相关的方法以及包含这些化合物的药物组合物。

10. 发明申请

US20110224186A1 CARBACEPHEM BETA-LACTAM ANTIBIOTICS 审中-公开
标题翻译： CARBACEPHEM BETA-LACTAM抗生素
公开(公告)号：US20110224186A1
公开(公告)日：2011-09-15
申请号：US13044800
申请日：2011-03-10
申请人： Allan Scott Wagman , Heinz Ernst Moser
发明人： Allan Scott Wagman , Heinz Ernst Moser
IPC分类号： A61K31/397 , C07D463/22 , A61P31/04
CPC分类号： C07D463/22
摘要： Carbacephem β-lactam antibiotics having the following chemical structure (I) are disclosed: including stereoisomers, pharmaceutically acceptable salts, esters and prodrugs thereof, wherein Ar2, X, R1 and R2 are as defined herein. The compounds are useful for the treatment of bacterial infections, in particular those caused by methicillin-resistant Staphylococcus spp.
摘要翻译：公开了具有以下化学结构（I）的甘巴酸和β-内酰胺类抗生素：包括立体异构体，其药学上可接受的盐，酯和前药，其中Ar 2，X，R 1和R 2如本文所定义。这些化合物可用于治疗细菌感染，特别是由耐甲氧西林葡萄球菌引起的细菌感染。

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