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61. 发明申请

US20130096119A1 Isoquinolin-3-Ylurea Derivatives 审中-公开
标题翻译：异喹啉-3-基脲衍生物
公开(公告)号：US20130096119A1
公开(公告)日：2013-04-18
申请号：US13638892
申请日：2011-03-30
申请人： Daniel Bur , Markus Gude , Christian Hubschwerlen , Philippe Panchaud
发明人： Daniel Bur , Markus Gude , Christian Hubschwerlen , Philippe Panchaud
IPC分类号： C07D471/04 , C07D413/14 , C07D401/12 , C07D217/22 , C07D401/10
CPC分类号： C07D471/04 , C07D217/22 , C07D401/04 , C07D401/10 , C07D401/12 , C07D405/04 , C07D409/04 , C07D413/14
摘要： The invention relates to isoquinolin-3-ylurea derivatives of formula (I) wherein R1 represents (C1-C3)alkyl, (C1-C3)haloalkyl or cyclopropyl, R4 represents H and the substituents R2 and R3 and R5 have the meanings disclosed in the specification; and to the salts of such compounds. These compounds are useful for the prevention or the treatment of bacterial infections.
摘要翻译：本发明涉及式（I）的异喹啉-3-基脲衍生物，其中R 1表示（C 1 -C 3）烷基，（C 1 -C 3）卤代烷基或环丙基，R 4表示H，取代基R 2和R 3和R 5具有规格; 和这些化合物的盐。这些化合物可用于预防或治疗细菌感染。

62. 发明授权

US08158797B2 Oxazolidinone-quinolone hybrid antibiotics 有权
标题翻译：恶唑烷酮 - 喹诺酮杂合抗生素
公开(公告)号：US08158797B2
公开(公告)日：2012-04-17
申请号：US10583419
申请日：2004-12-20
申请人： Christian Hubschwerlen , Jean-Luc Specklin , Daniel Baeschlin , Christine Schmitt , Stefan Müller , Michael W. Cappi
发明人： Christian Hubschwerlen , Jean-Luc Specklin , Daniel Baeschlin , Christine Schmitt , Stefan Müller , Michael W. Cappi
IPC分类号： C07D215/14 , C07D401/14 , A61K31/4375 , A61K31/4725
CPC分类号： C07D413/12 , C07D413/14 , C07D471/04 , C07F9/65583 , C07F9/6561
摘要： The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria.
摘要翻译：本发明涉及作为有用的抗微生物剂并能有效抵抗各种多重耐药性细菌的式（I）化合物。

63. 发明申请

US20090306389A1 Intermediate products for producing oxazolidinone-quinolone hybrids 有权
标题翻译：用于生产恶唑烷酮 - 喹诺酮杂交体的中间产物
公开(公告)号：US20090306389A1
公开(公告)日：2009-12-10
申请号：US12455810
申请日：2009-06-05
申请人： Christian Hubschwerlen , Jean-Luc Specklin , Jean Phillippe Surivet , Daniel Baeschlin
发明人： Christian Hubschwerlen , Jean-Luc Specklin , Jean Phillippe Surivet , Daniel Baeschlin
IPC分类号： C07D413/12 , C07D413/04 , C07D405/04 , C07D401/04
CPC分类号： C07D263/20 , C07D413/12 , C07D413/14 , C07D471/04
摘要： The present invention describes intermediates (ZP) for a novel and efficient synthesis of compounds in which the pharmacophores of quinolone and oxazolidinone are linked to one another by way of a chemically stable linker.
摘要翻译：本发明描述了中间体（ZP），用于新颖有效地合成化合物，其中喹诺酮和恶唑烷酮的药效学通过化学稳定的接头相互连接。

64. 发明申请

US20080027040A1 Oxazolidinone-Quinolone Hybrid Antibiotics 有权
标题翻译：恶唑烷酮 - 喹诺酮混合抗生素
公开(公告)号：US20080027040A1
公开(公告)日：2008-01-31
申请号：US10583419
申请日：2004-12-20
申请人： Christian Hubschwerlen , Jean-Luc Specklin , Daniel Baeschlin , Christine Schmitt , Stefan Muller , Michael W. Cappi
发明人： Christian Hubschwerlen , Jean-Luc Specklin , Daniel Baeschlin , Christine Schmitt , Stefan Muller , Michael W. Cappi
IPC分类号： A61K31/55 , A61K31/435 , A61K31/4375 , A61K31/4523 , C07D221/00 , C07D223/02 , C07D295/00 , C07D221/02 , A61P31/04 , A61K31/496 , A61K31/5383
CPC分类号： C07D413/12 , C07D413/14 , C07D471/04 , C07F9/65583 , C07F9/6561
摘要： The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:
摘要翻译：本发明涉及作为有效的抗微生物剂并能有效抵抗各种多重耐药细菌的式（I）化合物：

65. 发明申请

US20060205719A1 Novel compounds having an antibacterial activity 审中-公开
标题翻译：具有抗菌活性的新型化合物
公开(公告)号：US20060205719A1
公开(公告)日：2006-09-14
申请号：US10553731
申请日：2004-03-29
申请人： Christian Hubschwerlen , Jean Surivet , Cornelia Zumbrunn
发明人： Christian Hubschwerlen , Jean Surivet , Cornelia Zumbrunn
IPC分类号： A61K31/538 , A61K31/355 , C07D265/36 , C07D319/14
CPC分类号： C07D405/06 , C07D405/12 , C07D405/14 , C07D413/06 , C07D413/12 , C07D413/14
摘要： The present invention describes novel anti-bacterial compounds of formula (I). These compounds are, amongst others, of interest as inhibitors of Topoisomerase IV (Topo IV) as well as of DNA gyrase.
摘要翻译：本发明描述了新的式（I）抗菌化合物。这些化合物尤其是作为拓扑异构酶IV（Topo IV）的抑制剂以及DNA促旋酶的兴趣。

66. 发明申请

US20050096343A1 Dual action antibiotics 有权
标题翻译：双重作用抗生素
公开(公告)号：US20050096343A1
公开(公告)日：2005-05-05
申请号：US10491519
申请日：2002-10-04
申请人： Christian Hubschwerlen , Jean-Luc Specklin
发明人： Christian Hubschwerlen , Jean-Luc Specklin
IPC分类号： A61K31/496 , A61K31/5383 , A61P31/04 , C07D413/12 , C07D413/14 , C07D471/04 , C07D498/04 , C07D498/06 , C07D471/02 , A61K31/4709 , A61K31/4745
CPC分类号： C07D413/12 , C07D413/14 , C07D471/04
摘要： The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria.
摘要翻译：本发明涉及作为有用的抗微生物剂并能有效抵抗各种多重耐药性细菌的式（I）化合物。

67. 发明授权

US06566355B1 Bicyclic and tricyclic &bgr;-lactams 失效
标题翻译：双环和三环β-内酰胺
公开(公告)号：US06566355B1
公开(公告)日：2003-05-20
申请号：US08420957
申请日：1995-04-12
申请人： Christian Hubschwerlen , Robert Charnas , Ingrid Heinze , Klaus Gubernator
发明人： Christian Hubschwerlen , Robert Charnas , Ingrid Heinze , Klaus Gubernator
IPC分类号： C07D48704
CPC分类号： A61K31/43 , A61K31/545 , C07D487/04 , A61K31/40 , A61K2300/00
摘要： There are described compounds of the formula in which R signifies lower alkoxycarbonyl, lower alkoxy-carbonylamino, the acyl residue of an &agr;- or &bgr;-amino acid or a residue of the general formula Q—X—Y— (a) wherein Q signifies a 3- to 6-membered ring which optionally contains nitrogen, sulfur and/or oxygen and which is optionally bonded with a fused ring, X signifies a direct bond or a linear “spacer” with up to 6 atoms consisting of carbon, nitrogen, oxygen and/or sulfur, of which up to 2 atoms can be nitrogen atoms and 1 atom can be oxygen or sulfur, and Y represents one of the groups —CO—, —CS—, —CONH— and (where X contains neither sulfur nor carbonyl as a terminal component) —SO2—; and in which R1 and R2 together signify a group of the formula wherein A represents hydrogen or a residue which is usable in the 3-position of cephalosporin antibiotics, and in which R3 represents hydrogen, and pharmaceutically compatible salts of these compounds. The products have &bgr;-lactamase inhibiting properties. They are useful in combination with &bgr;-lactam antibiotics in the control of &bgr;-lactamase forming pathogens.
摘要翻译：描述的化合物是R表示低级烷氧基羰基，低级烷氧基 - 羰基氨基，α-或β-氨基酸的酰基残基或通式化合物的残基Q表示3-至6-元环，其任选地含有氮，硫和/或氧，并且其任选地与稠环键合，X表示直接键或具有多至6个碳原子，氮，氧和/或硫原子的直链“间隔”，其中最多2个原子可以是氮原子，1个原子可以是氧或硫，Y表示-CO-，-CS-，-CONH-和（其中X不含硫或羰基作为末端成分）之一的-SO 2 - ; 并且其中R 1和R 2一起表示一组甲酰胺A表示氢或可用于头孢菌素抗生素3位的残基，其中R3表示氢，以及这些化合物的药学上相容的盐。产品具有β β-内酰胺酶抑制性质。它们与β-内酰胺抗生素联合用于控制β-内酰胺酶形成病原体。

68. 发明授权

US6114330A Substituted 2,4-diaminopyrimidines 失效
标题翻译：取代的2,4-二氨基嘧啶
公开(公告)号：US6114330A
公开(公告)日：2000-09-05
申请号：US28980
申请日：1998-02-25
申请人： Philippe Guerry , Christian Hubschwerlen , Synese Jolidon , Jean-Luc Specklin , Pierre-Charles Wyss
发明人： Philippe Guerry , Christian Hubschwerlen , Synese Jolidon , Jean-Luc Specklin , Pierre-Charles Wyss
IPC分类号： A61K31/505 , A61K31/506 , A61K31/5377 , A61P31/04 , C07D401/14 , C07D403/10 , C07D403/14 , C07D405/14 , C07D409/14 , C07D247/02
CPC分类号： C07D403/10 , C07D403/14 , C07D405/14
摘要： The invention is concerned with compounds of formula ##STR1## wherein R.sup.1 is lower-alkoxy, R.sup.2 is hydroxy or lower-alkoxy, R.sup.3 is hydrogen, cyano, alkyl, alkenyl, cycloalkyl, aryl, heterocycyl, aryl-Q-alkyl, or a group of the formula --CR.sup.4 R.sup.4 'COR.sup.5 --, Q is --SO-- or --SO.sub.2 --; R.sup.4, R.sup.4 ' are each independently hydrogen, alkyl, aryl or heterocyclyl, R.sup.5 is hydrogen, alkyl, alkoxy, hydroxy, aryl or heterocycyl, or R.sup.4 and R.sup.5 together form --(CH.sub.2).sub.n --, and n is a whole number between 2 to 5 inclusive and the enantiomers, epimers, and diastereomers thereof, as well as pharmaceutically acceptable salts thereof. These compounds have valuable antibacterial activity.
摘要翻译：本发明涉及下式的化合物，其中R 1是低级烷氧基，R 2是羟基或低级烷氧基，R 3是氢，氰基，烷基，烯基，环烷基，芳基，杂环基，芳基-C-烷基或式-CR4R4'COR5-，Q是-SO-或-SO2-; R 4，R 4'各自独立地为氢，烷基，芳基或杂环基，R 5为氢，烷基，烷氧基，羟基，芳基或杂环基，或者R 4和R 5一起形成 - （CH 2）n - ，n为2 5和其对映异构体，差向异构体和非对映异构体，以及其药学上可接受的盐。这些化合物具有有价值的抗菌活性。

69. 发明授权

US5811419A Isooxacephem-derivatives 失效
标题翻译：异恶草衍生物
公开(公告)号：US5811419A
公开(公告)日：1998-09-22
申请号：US768369
申请日：1996-12-17
申请人： Christian Hubschwerlen , Jean-Luc Specklin
发明人： Christian Hubschwerlen , Jean-Luc Specklin
IPC分类号： C07D507/04 , A61K31/00 , A61K31/535 , A61K31/5375 , A61K31/5383 , A61P31/00 , C07D498/04 , C07D507/06 , C07D507/08
CPC分类号： C07D498/04 , Y02P20/55
摘要： Compounds of formula I ##STR1## wherein R.sup.1 is hydrogen or an acyl group derived from a carboxylic acid; R.sup.2 is hydrogen, hydroxy, lower alkyl, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aryl-lower alkyl, aryl, aryloxy, aryl-lower alkoxy or a heterocyclic ring; the lower alkyl, cycloalkyl, lower alkoxy, lower alkenyl, cycloalkenyl, lower alkynyl, aryl-lower alkyl, aryl, aryloxy, aryl-lower alkoxy and the heterocyclic ring being unsubstituted or substituted with at least one group selected from carboxy, amino, nitro, cyano, lower alkyl, lower alkoxy, hydroxy, halogen, --CONR.sup.21 R.sup.22, --N(R.sup.22)COOR.sup.23, R.sup.22 CO--, R.sup.22 OCO-- or R.sup.22 COO--, wherein R.sup.21 is hydrogen, lower alkyl, or cycloalkyl; R.sup.22 is hydrogen or lower alkyl; R.sup.23 is lower alkyl, lower alkenyl or a carboxylic acid protecting group; as well as readily hydrolyzable esters thereof, pharmaceutically acceptable salts of said compounds and hydrates of the compounds of formula I and of their esters and salts as provided for herein. The invention also relates to pharmaceutical compositions and methods of use of these compounds.
摘要翻译：式I的化合物其中R 1是氢或衍生自羧酸的酰基; R2是氢，羟基，低级烷基，环烷基，低级烷氧基，低级烯基，环烯基，低级炔基，芳基 - 低级烷基，芳基，芳氧基，芳基 - 低级烷氧基或杂环。低级烷基，环烷基，低级烷氧基，低级烯基，环烯基，低级炔基，芳基 - 低级烷基，芳基，芳氧基，芳基 - 低级烷氧基和杂环是未取代的或被至少一个选自羧基，氨基，硝基，氰基，低级烷基，低级烷氧基，羟基，卤素，-CONR 21 R 22，-N（R 22）COOR 23，R 22 CO-，R 22OCO-或R 22 COO-，其中R 21是氢，低级烷基或环烷基; R 22是氢或低级烷基; R 23为低级烷基，低级烯基或羧酸保护基; 以及其易水解的酯，所述化合物的药学上可接受的盐和式I化合物的水合物及其如本文所提供的酯和盐。本发明还涉及这些化合物的药物组合物和使用方法。

70. 发明授权

US5644053A Penam derivatives 失效
公开(公告)号：US5644053A
公开(公告)日：1997-07-01
申请号：US559104
申请日：1995-11-16
申请人： Christian Hubschwerlen , Hans Richter , Jean-Luc Specklin
发明人： Christian Hubschwerlen , Hans Richter , Jean-Luc Specklin
IPC分类号： A61K31/40 , A61K31/425 , A61K31/43 , A61K31/431 , A61K31/435 , A61K31/495 , A61K31/545 , A61P31/04 , A61P43/00 , C07D499/00 , C07D499/86 , C07D499/87 , C07D499/897
CPC分类号： C07D499/00
摘要： The present invention discloses compounds having the formula ##STR1## wherein one of R.sup.1 and R.sup.2 is --COR.sup.4, --CN, --CH.sub.2 R.sup.5, halogen, --CH.dbd.CHR.sup.6 or Q and the other is hydrogen or lower alkyl or both R.sup.1 and R.sup.2 together form a .gamma.-lactam ring,R.sup.3 is hydrogen, lower alkyl, aryl-alkyl, allyl or a residue which is cleavable in vivo,R.sup.4 is hydrogen, lower alkyl, lower alkoxy, benzyloxy, amino, lower alkylamino or lower alkyl-lower alkoxyamino,R.sup.5 is hydroxy, --OCONHR.sup.7, --OCONH.sub.2 or a five- or six-membered hetero-aromatic ring which contains N,S and/or O and which is linked via a nitrogen atom,R.sup.6 is --CN or CHO,R.sup.7 is --COCH.sub.2 Cl,Q is a five- or six-membered hetero-aromatic ring which contains N, S and/or O andn is 0, 1 or 2,and the pharmaceutically compatible salts thereof.These compounds are good .beta.-lactamase inhibitors. They can be used for the prevention or treatment of bacterial infections, optionally together with a .beta.-lactam antibiotic.

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