专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

41. 发明授权

US08039466B2 5-hydroxymethyl-oxazolidin-2-one antibacterials 有权
标题翻译： 5-羟甲基 - 恶唑烷-2-酮抗菌剂
公开(公告)号：US08039466B2
公开(公告)日：2011-10-18
申请号：US12516335
申请日：2007-11-23
申请人： Christian Hubschwerlen , Philippe Panchaud , Jean-Luc Specklin
发明人： Christian Hubschwerlen , Philippe Panchaud , Jean-Luc Specklin
IPC分类号： C07D498/14 , C07D401/12 , A61K31/5383
CPC分类号： C07D498/14 , C07D209/52 , C07D405/14 , C07D409/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D513/04
摘要： The invention relates to novel chimeric antibiotics of formula I wherein R1 represents OH, OPO3H2 or OCOR5; R2 represents H, OH or OPO3H2; R3 represents H or halogen; R4 is H, (C1-C3)alkyl, or cycloalkyl; R5 represents piperidin-4-yl or R5 is the residue of a naturally occurring amino acid, of the enantiomer of a naturally occurring amino acid or of dimethylaminoglycine; n is 0 or 1; and to salts (in particular pharmaceutically acceptable salts) of compounds of formula I. These chimeric compounds are useful in the manufacture of medicaments for the treatment of infections (e.g. bacterial infections).
摘要翻译：本发明涉及式I的新型嵌合抗生素，其中R1代表OH，OPO3H2或OCOR5; R2表示H，OH或OPO3H2; R3表示H或卤素; R4是H，（C1-C3）烷基或环烷基; R5表示哌啶-4-基或R5是天然存在的氨基酸的残基，天然存在的氨基酸或二甲基氨基甘氨酸的对映异构体; n为0或1; 和式I化合物的盐（特别是药学上可接受的盐）。这些嵌合化合物可用于制备用于治疗感染（例如细菌感染）的药物。

42. 发明授权

US6084120A .beta.-Alkoxyacrylates against malaria 失效
标题翻译： β-丙烯酸甲酯对抗疟疾
公开(公告)号：US6084120A
公开(公告)日：2000-07-04
申请号：US102463
申请日：1998-06-22
申请人： Jawad Alzeer , Jacques Chollet , Christian Hubschwerlen , Hugues Matile , Robert George Ridley
发明人： Jawad Alzeer , Jacques Chollet , Christian Hubschwerlen , Hugues Matile , Robert George Ridley
IPC分类号： C07D317/60 , A61K31/215 , A61K31/216 , A61K31/341 , A61K31/343 , A61K31/352 , A61K31/353 , A61K31/36 , A61K31/38 , A61K31/381 , A61K31/40 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/437 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4436 , A61K31/47 , A61K31/4709 , A61K31/472 , A61K31/498 , A61K31/506 , A61K31/53 , A61P33/06 , C07C69/612 , C07C69/734 , C07C229/34 , C07C251/32 , C07C251/48 , C07C251/60 , C07C323/47 , C07C323/56 , C07D207/337 , C07D213/53 , C07D213/55 , C07D215/14 , C07D215/22 , C07D217/18 , C07D241/42 , C07D277/20 , C07D277/22 , C07D277/28 , C07D277/30 , C07D277/36 , C07D277/56 , C07D285/12 , C07D285/125 , C07D285/135 , C07D307/54 , C07D311/58 , C07D317/62 , C07D333/20 , C07D333/24 , C07D333/28 , C07D333/58 , C07D333/60 , C07D409/12 , C07D417/12 , C07D471/04 , C07C255/50 , C07D253/08 , C07D333/72
CPC分类号： C07D333/60 , A61K31/216 , A61K31/341 , A61K31/343 , A61K31/352 , A61K31/36 , A61K31/381 , A61K31/40 , A61K31/42 , A61K31/423 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/437 , A61K31/4402 , A61K31/4406 , A61K31/4409 , A61K31/4436 , A61K31/47 , A61K31/4709 , A61K31/498 , A61K31/506 , A61K31/53 , C07C251/48 , C07C69/734 , C07D213/55 , C07D215/14 , C07D277/30 , C07D307/54 , C07D333/24 , C07D333/28
摘要： The present invention relates to compounds having the formulae ##STR1## wherein R, R.sup.1, R.sup.6, R.sup.7, Rn.sup.8, X, and Z are defined herein, which are useful in the treatment or prophylaxis of malaria. The compounds of the present invention are especially useful in the treatment or prophylaxis of chloroquine-sensitive and chloroquine-resistant malaria.
摘要翻译：本发明涉及具有下式的化合物：其中R，R 1，R 6，R 7，R 8，X和Z如本文所定义，其可用于治疗或预防疟疾。本发明的化合物特别可用于治疗或预防氯喹敏感性和氯喹抗性疟疾。

43. 发明授权

US5510343A Bicyclic and tricyclic .beta.-lactams 失效
公开(公告)号：US5510343A
公开(公告)日：1996-04-23
申请号：US474207
申请日：1995-06-07
申请人： Robert Charnas , Klaus Gubernator , Ingrid Heinze , Christian Hubschwerlen
发明人： Robert Charnas , Klaus Gubernator , Ingrid Heinze , Christian Hubschwerlen
IPC分类号： A61K31/40 , A61K31/397 , A61K31/43 , A61K31/435 , A61K31/545 , A61P31/04 , A61P43/00 , B01J8/12 , C07D471/16 , C07D487/04 , C07D487/16 , C12N9/99 , A61K31/445
CPC分类号： A61K31/43 , A61K31/545 , C07D487/04
摘要： There are described compounds of the formula ##STR1## in which R signifies lower alkoxycarbonyl, lower alkoxycarbonylamino, the acyl residue of an .alpha.- or .beta.-amino acid or a residue of the general formulaQ--X--Y-- (a)wherein Q signifies a 3- to 6-membered ring which optionally contains nitrogen, sulphur 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 sulphur, of which up to 2 atoms can be nitrogen atoms and 1 atom can be oxygen or sulphur, and Y represents one of the groups --CO--, --CS--, --CONH-- and (where X contains neither sulphur nor carbonyl as a terminal component) --SO.sub.2 --;and in which R.sup.1 signifies hydrogen, halogen, carbamoyloxy, lower alkanoyloxy or a group of the formula --S--Het, wherein Het represents a 5- or 6-membered heteroaromatic group containing nitrogen, sulphur and/or oxygen, and R.sup.2 represents the sulpho group --SO.sub.3 H or R.sup.1 and R.sup.2 together signify a group of the formula ##STR2## wherein A represents hydrogen or a residue which is usable in the 3-position of cephalosporin antibiotics, and in which R.sup.3 represents hydrogen or R.sup.1 and R.sup.3 together represent a group of the formula.dbd.CH--R.sup.a (c)wherein R.sup.a signifies one of the groups--COR.sup.b (c.sup.1)--CH.sub.2 --OCOR.sup.c (c.sup.2)--CH.sub.2 --NR.sup.d R.sup.e (c.sup.3)--CH.sub.2 --S--Het (c.sup.4)in which R.sup.b represents lower alkoxy or amino, R.sup.c represents lower alkyl, phenyl or amino, R.sup.d and R.sup.e each independently represent hydrogen or lower alkyl or R.sup.d and R.sup.e together with the N atom to which they are attached represent a 5- or 6-membered N-heterocycle which optionally contains a further nitrogen, oxygen or sulphur atom and Het represents a 5- or 6-membered heteroaromatic group containing nitrogen, sulphur and/or oxygen,and pharmaceutically compatible salts of these compounds.The products have .beta.-lactamase inhibiting properties. They are useful in combination with .beta.-lactam antibiotics in the control of .beta.-lactamase forming pathogens.

44. 发明授权

US5283248A Amino substituted pyrimido[1,6-2]benzimidazoles 失效
标题翻译：氨基取代的嘧啶并[1,6-2]苯并咪唑
公开(公告)号：US5283248A
公开(公告)日：1994-02-01
申请号：US904245
申请日：1992-06-25
申请人： Christian Hubschwerlen , Ivan Kompis , Jean-Luc Specklin
发明人： Christian Hubschwerlen , Ivan Kompis , Jean-Luc Specklin
IPC分类号： C07C275/40 , C07D235/16 , C07D403/04 , C07D487/04 , A61K31/505
CPC分类号： C07D403/04 , C07C275/40 , C07D235/16 , C07D487/04
摘要： The present invention relates to novel substituted pyrimidobenzimidazole derivatives of the formula ##STR1## wherein the substituents are as described in the specification, and pharmaceutically acceptable salts thereof.The products have an inhibitory action on the DNA-gyrase activity in bacteria. They can accordingly be used for the prevention or control of bacterial infections.
摘要翻译：本发明涉及式（*化学结构*）I的新型取代的嘧啶并苯并咪唑衍生物，其中取代基如说明书中所述，及其药学上可接受的盐。该产物对细菌中的DNA-促旋酶活性具有抑制作用。因此，它们可以用于预防或控制细菌感染。

45. 发明申请

US20120135961A1 USE OF OXAZOLIDINONE-QUINOLINE HYBRID ANTIBIOTICS FOR THE TREATMENT OF ANTHRAX AND OTHER INFECTIONS 有权
公开(公告)号：US20120135961A1
公开(公告)日：2012-05-31
申请号：US12987611
申请日：2011-01-10
申请人： Christian Hubschwerlen , Jean-Luc Specklin , Daniel Baeschlin , Hans Locher , Christine Schmitt
发明人： Christian Hubschwerlen , Jean-Luc Specklin , Daniel Baeschlin , Hans Locher , Christine Schmitt
IPC分类号： A61K31/675 , C07D413/14 , C07D498/06 , A61K31/4545 , C07F9/6561 , A61K31/5383 , C07F9/6558 , A61P31/00 , A61P31/04 , A61K31/4375 , A61K31/4709 , C07D471/04 , A61K31/55
CPC分类号： A61K31/4709
摘要： The present invention relates to the use of compounds, in which the pharmacophores of quinolone and oxazolidinone are chemically linked together through a linker that is stable under physiological conditions, for the treatment of anthrax and other infections.

46. 发明授权

US08124623B2 5-hydroxymethyl-oxazolidin-2-one-derivatives and their uses as antibacterials 有权
标题翻译： 5-羟甲基 - 恶唑烷-2-酮衍生物及其用作抗菌剂
公开(公告)号：US08124623B2
公开(公告)日：2012-02-28
申请号：US12463281
申请日：2009-05-08
申请人： Christian Hubschwerlen , Hans Locher , Philippe Panchaud , Jean-Luc Specklin
发明人： Christian Hubschwerlen , Hans Locher , Philippe Panchaud , Jean-Luc Specklin
IPC分类号： A61K31/04 , C07D215/38
CPC分类号： C07D413/14 , C07D471/04
摘要： The invention relates to novel chimeric antibiotics of formula I wherein R1 represents OH, OPO3H2 or OCOR5; R2 represents H, OH or OPO3H2; A represents N or CR6; R3 represents H or fluorine; R4 is H, (C1-C3) alkyl, or cycloalkyl; R5 is the residue of a naturally occurring amino acid, of the enantiomer of a naturally occurring amino acid or of dimethylaminoglycine; R6 represents H, alkoxy or halogen; and n is 0 or 1; and to salts (in particular pharmaceutically acceptable salts) of compounds of formula I. These chimeric compounds are useful in the manufacture of medicaments for the treatment of infections (e.g. bacterial infections).
摘要翻译：本发明涉及式I的新型嵌合抗生素，其中R1代表OH，OPO3H2或OCOR5; R2表示H，OH或OPO3H2; A代表N或CR6; R3表示H或氟; R4是H，（C1-C3）烷基或环烷基; R5是天然存在的氨基酸的残基，天然存在的氨基酸或二甲基氨基甘氨酸的对映异构体; R6表示H，烷氧基或卤素; 并且n为0或1; 和式I化合物的盐（特别是药学上可接受的盐）。这些嵌合化合物可用于制备用于治疗感染（例如细菌感染）的药物。

47. 发明授权

US07557214B2 Intermediate products for producing oxazolidinone-quinolone hybrids 有权
公开(公告)号：US07557214B2
公开(公告)日：2009-07-07
申请号：US10570775
申请日：2004-09-03
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： C07D211/00 , C07D211/26
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.

48. 发明申请

US20070004769A1 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：US20070004769A1
公开(公告)日：2007-01-04
申请号：US10570775
申请日：2004-09-03
申请人： Christian Hubschwerlen , Jean-Luc Specklin , Jean Surivet , Daniel Baeschlin
发明人： Christian Hubschwerlen , Jean-Luc Specklin , Jean Surivet , Daniel Baeschlin
IPC分类号： A61K31/4745 , A61K31/4709 , C07D471/02 , C07D413/02
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。

49. 发明授权

US06232306B1 Derivatives of 3-(2-oxo-[1,3′]bipyrrolidinyl-3-ylidenemethyl)-cephams 有权
标题翻译： 3-（2-氧代 - [1,3']联吡咯烷基-3-亚甲基甲基） - 头孢的衍生物
公开(公告)号：US06232306B1
公开(公告)日：2001-05-15
申请号：US09332811
申请日：1999-06-14
申请人： Paul Hebeisen , Christian Hubschwerlen , Jean-Luc Specklin
发明人： Paul Hebeisen , Christian Hubschwerlen , Jean-Luc Specklin
IPC分类号： C07D50124
CPC分类号： C07D501/00
摘要： The present invention provides compounds of formula I wherein R1 is hydrogen, C1-6-alkyl, C1-6-alkyl substituted by fluoro, or C3-6-cycloalkyl; R2 is hydrogen or a substituent selected from the group consisting of —CH2C(═CHR)—COOR, —CH2OCOR, —CH(R)OCOR, —CH(R)OCOOR, —CH(OCOR)OCOR, —CH2COCH2OCOR and R3 is hydrogen or a substituent selected from the group consisting of —CH2C(═CH2)—COOR, —COOCH2C(═CHR)—COOR, —COOCH2OCOR, —COOCH(R)OCOR, —COOCH(R)OCOOR, —COOCH(OCOR)OCOR, —COOCH2COCH2OCOR, and with the proviso that one of R2 and R3 is hydrogen and the other is not hydrogen, R is hydrogen or C1-6-alkyl; R4 is hydrogen or hydroxy, R5 is hydrogen or &ohgr;-hydroxyalkyl; and X is CH or N, pharmaceutically acceptable salts of the compounds and hydrates of the compounds and of their salts.
摘要翻译：本发明提供式I化合物，其中R 1是氢，C 1-6 - 烷基，被氟取代的C 1-6 - 烷基或C 3-6 - 环烷基; R 2是氢或选自-CH 2 C（= CHR ）-COOR，-CH 2 OCOR，-CH（R）OCOR，-CH（R）OCOOR，-CH（OCOR）OCOR，-CH 2 COCH 2 OCOR和R 3是氢或选自-CH 2 C（= CH 2）-COOR ，-COOCH 2 C（= CHR）-COOR，-COOCH 2 OCOR，-COOCH（R）OCOR，-COOCH（R）OCOOR，-COOCH（OCOR）OCOR，-COOCH 2 COCH 2 OCOR，条件是R 2和R 3之一为氢，另一个不是氢，R是氢或C 1-6 - 烷基; R 4是氢或羟基，R 5是氢或ω-羟基烷基; 和X是CH或N，化合物及其盐的化合物和水合物的药学上可接受的盐。

50. 发明授权

US5494666A .beta.-lactam compounds 失效
公开(公告)号：US5494666A
公开(公告)日：1996-02-27
申请号：US489195
申请日：1995-06-09
申请人： Markus Bohringer , Christian Hubschwerlen , Philippe Pflieger , Jean-Luc Specklin
发明人： Markus Bohringer , Christian Hubschwerlen , Philippe Pflieger , Jean-Luc Specklin
IPC分类号： C07D507/08 , A61K31/435 , A61K31/535 , A61K31/54 , A61P31/04 , C07D463/16 , C07D471/16 , C07D487/14 , C07D498/14 , C07D498/16 , C07D513/14 , C07D513/16 , C07D513/04
CPC分类号： C07D471/16 , C07D498/16 , C07D513/16
摘要： Compounds of the formula ##STR1## where Z, A, and R are as disclosed herein and pharmaceutically compatible, readily hydrolyzable esters and salts of these compounds are disclosed.The compounds have .beta.-lactamase inhibiting properties and are useful in the control of .beta.-lactamase-forming pathogens in combination with .beta.-lactam antibiotics. They also exhibit antibacterial activity of their own and can accordingly be used themselves in the control or treatment of infectious diseases.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式