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公开(公告)号:US20210107932A1
公开(公告)日:2021-04-15
申请号:US16603230
申请日:2018-04-06
发明人: David CRICH , Girish SATI , Amr SONOUSI , Guanyu YANG , Appi Reddy MANDHAPATI , Michael G. PIRRONE , Takayuki KATO , Vikram SARPE , Andrea VASELLA , Erik C. BOTTGER , Sven N. HOBBIE
IPC分类号: C07H15/232 , C07H19/01 , A61P31/04
摘要: The present disclosure relates to derivatives of neamine-based aminoglycoside antibacterial drugs modified in position C6′, C2′ and/or C5″. The modifications impart favorable properties regarding activity against ESKAPE pathogens, evasion of resistance traits and increased selectivity, enabling systemic use of the compounds.
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公开(公告)号:US20180105546A1
公开(公告)日:2018-04-19
申请号:US15629061
申请日:2017-06-21
IPC分类号: C07H15/232 , C07K14/00 , C07K1/06 , C07H21/00 , C07K4/00
摘要: The invention relates to drug development and synthetic chemistry, in particular to the manufacture of biologically active compounds based on naturally occurring molecules. It also relates to novel biologically active compounds, for example aminoglycoside antibiotics, in a substantially pure regioisomeric form. More particularly, the present invention relates to methods for the chemo- or regioselective derivatization of a target compound with multiple reactive groups, some of which may be derivatezed, and other which will not be derivatized.
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公开(公告)号:US09072761B2
公开(公告)日:2015-07-07
申请号:US12857425
申请日:2010-08-16
申请人: Dev P. Arya , Nihar Ranjan , Sunil Kumar
发明人: Dev P. Arya , Nihar Ranjan , Sunil Kumar
IPC分类号: A01N43/04 , A61K31/70 , A61K31/7034 , C07H15/232 , G06Q50/24
CPC分类号: A61K47/48061 , A61K31/7034 , A61K47/545 , C07H15/232 , G06F19/00 , G06Q50/24 , Y02A90/22 , Y10T436/143333
摘要: Disclosed herein are compounds, compositions and methods related to viral inhibition. In some forms, the compounds, compositions and methods are related to binding RNA.
摘要翻译: 本文公开了与病毒抑制有关的化合物,组合物和方法。 在一些形式中,化合物,组合物和方法与结合RNA有关。
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公开(公告)号:US20120258925A1
公开(公告)日:2012-10-11
申请号:US13441696
申请日:2012-04-06
申请人: James Bradley Aggen , Paola Dozzo , Adam Aaron Goldblum , Darin James Hildebrandt , Timothy Robert Kane , Micah James Gliedt , Martin Sheringham Linsell
发明人: James Bradley Aggen , Paola Dozzo , Adam Aaron Goldblum , Darin James Hildebrandt , Timothy Robert Kane , Micah James Gliedt , Martin Sheringham Linsell
IPC分类号: A61K31/7036 , A61P31/04 , C07H15/232
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, Q5, R1, R2, R3, Z1 and Z2 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Q 1,Q 2,Q 5,R 1,R 2,R 3,Z 1和Z 2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。
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公开(公告)号:US5595977A
公开(公告)日:1997-01-21
申请号:US141625
申请日:1993-10-27
申请人: Hjarne Dyrsting , Torben Koch
发明人: Hjarne Dyrsting , Torben Koch
IPC分类号: A61K38/14 , C07C237/26 , C07F9/117 , C07H5/10 , C07H11/00 , C07H11/04 , C07H15/22 , C07H15/232 , C07H15/234 , C07H15/236 , C07H15/238 , C07H17/08 , C08B37/02 , A61K31/70 , C07H5/00
CPC分类号: C07H17/08 , A61K38/14 , C07C237/26 , C07F9/117 , C07H11/00 , C07H11/04 , C07H15/22 , C07H15/232 , C07H15/234 , C07H15/236 , C07H15/238 , C07H5/10 , C08B37/0021
摘要: The present invention relates to novel amino glycoside salts of sucrose-octa-O-sulfonic acid of formula I:([sucrose-octa-O-sulfonic acid.sup.8- ]-[R-(NH.sub.3.sup.+).sub.x ].sub.y -M.sub.z.sup.n+) (I)(x.multidot.y)+(z.multidot.n)=8x.multidot.y.epsilon.N.vertline.[4.ltoreq.x.multidot.y.ltoreq.8], wherein N is the set of natural numbers,x.epsilon.Z.vertline.[4.ltoreq.x.ltoreq.6], wherein Z is the set of integersz.epsilon.N.vertline.[0.ltoreq.z.ltoreq.4],n.epsilon.Z.vertline.[1.ltoreq.n.ltoreq.3],wherein R is a sugar moiety of an amino glycoside and M is a metal ion or an ammonium ion, said compounds being useful for treating ulcerations of the stomach and duodenum.
摘要翻译: 本发明涉及式I的蔗糖 - 八-O-邻磺酸的新型氨基糖苷盐:([蔗糖 - 八-O-邻磺酸8 - ] - [R-(NH 3 +)x] y-Mzn +)(I) (xxy)+(zxn)= 8 xxy epsilon N | [4 xxy x = 8]其中N是自然数集合,xεZ | [4] = x] 其中Z是整数z∈N| [0
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公开(公告)号:US5538954A
公开(公告)日:1996-07-23
申请号:US265193
申请日:1994-06-24
申请人: Torben Koch , Hjarne Dyrsting
发明人: Torben Koch , Hjarne Dyrsting
IPC分类号: A61K38/14 , C07C237/26 , C07F9/117 , C07H5/10 , C07H11/00 , C07H11/04 , C07H15/22 , C07H15/232 , C07H15/234 , C07H15/236 , C07H15/238 , C07H17/08 , C08B37/02 , A61K31/70 , C07H5/00
CPC分类号: C07H17/08 , A61K38/14 , C07C237/26 , C07F9/117 , C07H11/00 , C07H11/04 , C07H15/22 , C07H15/232 , C07H15/234 , C07H15/236 , C07H15/238 , C07H5/10 , C08B37/0021 , C07C2103/46
摘要: A salt of sucrose-octa-O-sulfonic acid and a tetracycline useful in inhibiting protein synthesis of bacteria.
摘要翻译: 蔗糖 - 八-O-邻磺酸和四环素的盐可用于抑制细菌的蛋白质合成。
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公开(公告)号:US4170643A
公开(公告)日:1979-10-09
申请号:US787040
申请日:1977-04-13
申请人: Stephan Gero , Daniel Mercier , Alain Olesker , Andre Cier
发明人: Stephan Gero , Daniel Mercier , Alain Olesker , Andre Cier
IPC分类号: C07H15/232 , C12P19/52 , A61K31/71 , C07H15/22
CPC分类号: C12R1/54 , C07H15/232 , C12P19/52 , C12R1/59 , Y10S435/886 , Y10S435/896
摘要: Novel aminoglycoside-aminocyclitol derivatives corresponding to the general formula: ##STR1## wherein R.sub.1 and R.sub.2, which are different, represent hydrogen or CH.sub.2 NH.sub.2 and R is selected from the group consisting of: ##STR2## wherein R.sub.3 represents NH.sub.2 or OH and R.sub.4 represents ##STR3## wherein R.sub.5 represents hydrogen or methyl and the pharmaceutically acceptable acid addition salts thereof.They are useful as antibiotics.
摘要翻译: 对应于以下通式的新型氨基糖苷 - 氨基环醇衍生物:其中R1和R2不同,表示氢或CH2NH2,R选自:其中R3表示NH2或OH,R4表示< 其中R5代表氢或甲基及其药学上可接受的酸加成盐。
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公开(公告)号:US4166114A
公开(公告)日:1979-08-28
申请号:US837909
申请日:1977-09-29
申请人: Kikuo Igarashi
发明人: Kikuo Igarashi
IPC分类号: C07H15/23 , A61K31/7052 , C07D207/16 , C07D211/66 , C07H15/22 , C07H15/232 , C07H15/234 , C07H15/236 , A61K31/71
CPC分类号: C07H15/234 , C07D207/16 , C07D211/66
摘要: Novel aminoglycoside antibiotic derivatives and their salts containing a 2-deoxystreptamine moiety of which the 1-amino group is substituted by a group represented by the formula: ##STR1## [wherein R is hydrogen atom, lower alkyl or aralkyl; n is an integer 1 or 2]Are effective in treatment and prevention of infectious diseases caused by gram positive and negative bacteria.
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公开(公告)号:US3311607A
公开(公告)日:1967-03-28
申请号:US41283264
申请日:1964-11-20
申请人: ANGELI INST SPA
发明人: SILVANO CASADIO
IPC分类号: C07H15/232
CPC分类号: A61K31/70 , C07H15/232
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公开(公告)号:US3065147A
公开(公告)日:1962-11-20
申请号:US1837160
申请日:1960-03-29
发明人: FEDERICO ARCAMONE , MARIO GHIONE , TULLIO SCOTTI
IPC分类号: C07H15/232
CPC分类号: C07H15/232 , Y10S435/886
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