公开(公告)号：EP1957507B1

公开(公告)日：2018-10-24

申请号：EP06844751.5

申请日：2006-12-01

申请人： Ionis Pharmaceuticals, Inc.

发明人： SWAYZE, Eric, E. ,  HANESSIAN, Stephen ,  SZYCHOWSKI, Janek ,  ADHIKARI, Susanta, Sekhar ,  PACHAMUTHU, Kandasamy ,  WANG, Xiaojing ,  MIGAWA, Michael, T. ,  GRIFFEY, Richard H.

IPC分类号： C07H15/23 ,  C07H15/232 ,  A61K31/70

CPC分类号： C07H15/23 ,  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.

公开(公告)号：EP3883943A1

公开(公告)日：2021-09-29

申请号：EP19886456.3

申请日：2019-11-22

申请人： Technion Research & Development Foundation Limited

发明人： BAASOV, Timor ,  SMOLKIN, Boris ,  KHONONOV, Alina ,  SHAVIT KISHKOBER, Michal ,  BELAKHOV, Valery

IPC分类号： C07H15/222 ,  C07H15/23 ,  A61K31/7036 ,  C07H15/224

公开(公告)号：EP3344641A1

公开(公告)日：2018-07-11

申请号：EP16840988.6

申请日：2016-09-02

申请人： Eloxx Pharmaceuticals Ltd.

发明人： BAASOV, Timor ,  TUVIA, Shmuel

IPC分类号： C07H15/23 ,  A61K31/7036 ,  A61P7/04 ,  A61P21/00 ,  A61P21/04 ,  C07H15/222 ,  C07H15/224

CPC分类号： C07H15/224 ,  C07H15/23

摘要： Novel aminoglycosides, represented by Formulae Ia and Ib, as defined in the instant specification, designed to exhibit stop codon mutation readthrough activity, are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic diseases and disorders, such as diseases and disorders associated with stop codon mutations.

公开(公告)号：EP3303358A1

公开(公告)日：2018-04-11

申请号：EP16804523.5

申请日：2016-06-03

申请人： PTC Therapeutics, Inc.

发明人： BAIAZITOV, Ramil, Y.

IPC分类号： C07H15/23

CPC分类号： A61K31/7036 ,  A61K45/06 ,  A61P35/00 ,  A61P43/00 ,  C07H15/236 ,  A61K2300/00

摘要： Methods of using and pharmaceutical compositions comprising (2R,3S,4R,5R,6S)-5-amino-6-(((1R,2S,3S,4R,6S)-4,6-diamino-3-(((2R,3R,4R,5R)-3,5-dihydroxy-5-methyl-4-(methylamino)tetrahydro-2H-pyran-2-yl)oxy)-2-hydroxycyclohexyl)oxy)- 2-(hydroxymethyl)tetrahydro-2H-pyran-3,4-diol are disclosed, including methods of treating or preventing a nonsense mutation mediated disease associated with premature translation termination or a premature stop codon resulting from a germline or somatic nonsense mutation.

公开(公告)号：EP3634973A1

公开(公告)日：2020-04-15

申请号：EP18814198.0

申请日：2018-06-05

申请人： Eloxx Pharmaceuticals Ltd.

发明人： BAASOV, Timor ,  FIRZON, Vera ,  BELAKHOV, Valery ,  EYLON, Bat-Hen

IPC分类号： C07H15/224 ,  C07H15/23 ,  C07H15/222 ,  A61P21/04 ,  A61P21/00

公开(公告)号：EP2864343B1

公开(公告)日：2017-09-27

申请号：EP13734863.7

申请日：2013-06-20

申请人： Rijksuniversiteit Groningen

发明人： MINNAARD, Adriaan Jacobus ,  JÄGER, Manuel ,  GOTTUMUKKALA, Aditya Lakshmi Narasimha Raju ,  DE VRIES, Johannes Gerardus ,  BASTIAN, Andreas Alexander ,  HERMANN, Andreas

IPC分类号： C07H1/00 ,  C07H3/04 ,  C07H3/06 ,  C07H15/04 ,  C07H15/18 ,  C07H23/00 ,  C07H3/02 ,  C07H5/06 ,  C07H17/04 ,  C07H15/22 ,  C07H15/23 ,  C07H15/222 ,  C07H15/224 ,  C07H15/226 ,  C07H15/228 ,  C07H15/232 ,  C07H15/234

CPC分类号： C07H15/222 ,  C07H1/00 ,  C07H3/02 ,  C07H3/04 ,  C07H3/06 ,  C07H5/06 ,  C07H15/04 ,  C07H15/18 ,  C07H15/22 ,  C07H15/224 ,  C07H15/226 ,  C07H15/228 ,  C07H15/23 ,  C07H15/232 ,  C07H15/234 ,  C07H17/04 ,  C07H23/00

摘要： The invention relates to the field of carbohydrate chemistry. Provided is a process for the regioselective oxidation of a single secondary hydroxy function of a carbohydrate substrate comprising two or more secondary hydroxy functions, comprising contacting the carbohydrate substrate in a solvent in the presence of a transition metal catalyst complex with an oxidizing agent to yield a mono-oxidized carbohydrate.

摘要翻译： 本发明涉及碳水化合物化学领域。 提供了用于包含两个或更多个仲羟基官能团的碳水化合物底物的单个仲羟基官能团的区域选择性氧化的方法，其包括使所述碳水化合物底物在过渡金属催化剂络合物存在下与溶剂中的氧化剂接触以产生 单氧化碳水化合物。

公开(公告)号：EP2665738A4

公开(公告)日：2014-06-25

申请号：EP12736727

申请日：2012-01-17

申请人： UNIV MCGILL

发明人： AUCLAIR KARINE ,  VONG KENWARD

IPC分类号： C07H15/224 ,  A61K31/7036 ,  A61K45/06 ,  A61P31/04 ,  C07H15/222 ,  C07H15/23 ,  C07H15/234

CPC分类号： C07H15/224 ,  A61K31/7036 ,  A61K45/06 ,  C07H15/23 ,  C07H15/234 ,  A61K2300/00

摘要： This invention relates to a compound of Formula 1A: or a pharmaceutically acceptable salt thereof; wherein R1 to R4, R7, R9 to R12 and Y are as defined herein. The invention further relates to pharmaceutical composition comprising said compound or a pharmaceutically acceptable salt thereof; and method of using same for reducing or reversing bacterial resistance to at least one aminoglycoside antibiotic.

公开(公告)号：EP2665738B1

公开(公告)日：2018-09-26

申请号：EP12736727.4

申请日：2012-01-17

申请人： The Royal Institution for the Advancement of Learning / McGill University

发明人： AUCLAIR, Karine ,  VONG, Kenward

IPC分类号： C07H15/23 ,  C07H15/224 ,  C07H15/234 ,  A61K31/7036 ,  A61K45/06 ,  A61P31/04

CPC分类号： C07H15/224 ,  A61K31/7036 ,  A61K45/06 ,  A61P31/04 ,  C07H15/23 ,  C07H15/234 ,  A61K2300/00

摘要： This invention relates to a compound of Formula 1A: or a pharmaceutically acceptable salt thereof; wherein R1 to R4, R7, R9 to R12 and Y are as defined herein. The invention further relates to pharmaceutical composition comprising said compound or a pharmaceutically acceptable salt thereof; and method of using same for reducing or reversing bacterial resistance to at least one aminoglycoside antibiotic.

公开(公告)号：EP3296311A1

公开(公告)日：2018-03-21

申请号：EP17192028.3

申请日：2011-11-17

申请人： Technion Research & Development Foundation Ltd.

发明人： BAASOV, Timor ,  ATIA-GLIKIN, Dana ,  KANDASAMY, Jeyakumar ,  BELAKHOV, Valery

IPC分类号： C07H15/23 ,  C07H1/00 ,  A61K31/7036 ,  A61K45/06 ,  A61P43/00

摘要： A new class of pseudo-trisaccharide aminoglycosides having an alkyl group at the 5" position, exhibiting efficient stop codon mutation readthrough activity, low cytotoxicity and high selectivity towards eukaryotic translation systems are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic disorders, as well as processes of preparing these aminoglycosides. The disclosed aminoglycosides are represented by the general formula I:

or a pharmaceutically acceptable salt thereof, wherein R 1 is selected from the group consisting of alkyl, cycloalkyl and aryl; and all other variables and features are as described in the specification.

摘要翻译： 提供了一类在5“位具有烷基的新型假三糖氨基糖苷类，其显示出有效的终止密码子突变通读活性，低的细胞毒性和对真核翻译系统的高选择性，还提供了包含其的药物组合物及其用途 所述氨基糖苷类由通式I表示：或其药学上可接受的盐，其中R 1选自烷基，环烷基和芳基;和 所有其他变量和特征如说明书中所述。

公开(公告)号：EP2640734B1

公开(公告)日：2017-10-18

申请号：EP11799501.9

申请日：2011-11-17

申请人： Technion Research & Development Foundation Ltd.

发明人： BAASOV, Timor ,  ATIA-GLIKIN, Dana ,  KANDASAMY, Jeyakumar ,  BELAKHOV, Valery

IPC分类号： C07H15/23 ,  C07H1/00 ,  A61K31/7036 ,  A61P43/00

CPC分类号： A61K31/7036 ,  A61K45/06 ,  B65D79/00 ,  C07H1/00 ,  C07H5/06 ,  C07H13/04 ,  C07H15/23

摘要： A new class of pseudo-trisaccharide aminoglycosides having an alkyl group at the 5" position, exhibiting efficient stop codon mutation readthrough activity, low cytotoxicity and high selectivity towards eukaryotic translation systems are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic disorders, as well as processes of preparing these aminoglycosides. The disclosed aminoglycosides are represented by the general formula I: or a pharmaceutically acceptable salt thereof, wherein R 1 is selected from the group consisting of alkyl, cycloalkyl and aryl; and all other variables and features are as described in the specification.