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81. 发明授权

US5830889A Antibacterial penem esters derivatives 失效
标题翻译：抗菌青蒿酯衍生物
公开(公告)号：US5830889A
公开(公告)日：1998-11-03
申请号：US971829
申请日：1993-02-19
申请人： Hiromitsu Iwata , Takashi Nakatsuka , Rie Tanaka , Masaji Ishiguro
发明人： Hiromitsu Iwata , Takashi Nakatsuka , Rie Tanaka , Masaji Ishiguro
IPC分类号： C07D499/897 , A61K31/43 , A61K31/431 , A61P31/04 , C07D499/04 , C07D499/88 , C07D499/887 , C07D499/893 , C07D499/32
CPC分类号： C07D499/88
摘要： Antibiotic penem compounds are represented by the following formula: ##STR1## wherein R represents a group of the general formula: ##STR2## in which R.sub.1 is a linear or branched C.sub.1 -C.sub.6 alkyl group, R.sub.2 is a particular substituted or unsubstituted alkyl, aryl or aralkyl group, n is an integer of 1-6, Y is a 5- or 6-membered heterocyclic aliphatic group having 1 or 2 oxygen atoms in the ring thereof, and Z is a specific 5-substituted 2-oxo-1,3-dioxolen-4-yl group. Antibiotic compositions for oral administration are also described.
摘要翻译： PCT No.PCT / JP91 / 01098 Sec。 371日期：1993年2月19日 102（e）日期1993年2月19日PCT 1991年8月16日PCT PCT。第WO92 / 03442号公报日期：1992年3月5日抗生素Penem化合物由下式表示：其中R表示通式：其中R 1为直链或支链C 1 -C 6烷基，R 2为特定取代基或未取代的烷基，芳基或芳烷基，n为1-6的整数，Y为其环中具有1或2个氧原子的5或6元杂环脂族基团，Z为特定的5-取代的2 - 氧代-1,3-二氧杂环戊烯-4-基。还描述了用于口服给药的抗生素组合物。

82. 发明授权

US5821362A Method of desilylating silylether compounds 失效
标题翻译：脱甲硅烷基醚化合物的方法
公开(公告)号：US5821362A
公开(公告)日：1998-10-13
申请号：US579453
申请日：1995-12-27
申请人： Akira Kaneko , Tsutomu Kaku , Masaji Ishiguro , Takashi Nakatsuka
发明人： Akira Kaneko , Tsutomu Kaku , Masaji Ishiguro , Takashi Nakatsuka
IPC分类号： C07D477/00 , C07D477/02 , C07D499/88 , C07D499/897 , C07F7/18 , C07D487/00 , C07D487/04 , C07D499/00
CPC分类号： C07D499/88 , C07D477/02 , Y02P20/55
摘要： Method of desilylating a silylether compound by reacting a silylether compound of the general formula (I): ##STR1## or a salt thereof with an amine hydrogen fluoride salt or a pyridine hydrogen fluoride salt in an organic solvent to produce a compound of the general formula (IV): ##STR2## According to this method, silylether compounds that are labile under strong acidic or basic conditions can be desilylated efficiently using inexpensive reagents.
摘要翻译：通过使通式（I）的甲硅烷基醚化合物：（I）或其盐与胺氟化氢盐或吡啶氟化氢盐在有机溶剂中反应来制备甲硅烷基醚化合物的方法，以制备化合物（IV）：根据该方法，在强酸性或碱性条件下不稳定的甲硅烷基醚化合物可以使用廉价的试剂有效地脱甲硅烷基化。

83. 发明授权

US5801242A Process for making quinolonyl lactam antimicrobials and novel intermediate compounds 失效
标题翻译：制备喹诺酮内酰胺抗菌药物和新型中间体化合物的方法
公开(公告)号：US5801242A
公开(公告)日：1998-09-01
申请号：US968987
申请日：1997-11-12
申请人： Jared Lynn Randall , Jane Ellen Godlewski
发明人： Jared Lynn Randall , Jane Ellen Godlewski
IPC分类号： C07D499/897 , A61K31/397 , A61K31/47 , A61K31/545 , A61K31/546 , A61P31/00 , C07D215/56 , C07D463/00 , C07D477/00 , C07D477/14 , C07D491/06 , C07D499/00 , C07D499/88 , C07D501/00 , C07D501/34 , C07D499/04 , C07D205/12 , C07D499/08 , C07D499/12
CPC分类号： C07D215/56 , C07D463/04 , C07D477/14 , C07D499/00 , C07D499/88 , C07D501/00 , Y02P20/55
摘要： The present invention provides processes for making compounds of the structure (Q--L.sup.1)--L--(L.sup.2 --B) wherein (I) Q is a quinolone moiety; (II) B is a lactam moiety; and (III) L, L.sup.1, and L.sup.2 together comprise a linking moiety; comprising the steps of: (1) coupling a compound of Formula (III) with a lactam-containing compound to form an intermediate compound; and (2) cyclizing the intermediate by reaction with an organosilicon compound to give a compound of the formula (Q--L.sup.1)--L--(L.sup.2 --B). Preferably, the process additionally comprises a step prior to the coupling step, wherein protected forms of the compound of Formula (III) and the lactam compound are formed; and deprotection steps after the cyclization step, wherein the protecting groups are removed. Preferred antimicrobial compounds made by these processes are those where the beta-lactam moiety is a penem, a carbapenem, a cephem, or a carbacephem. Also preferred are those compounds where L.sup.1, L, and L.sup.2 form a carbamate moiety, or a secondary or tertiary amine moiety. The present invention also provides novel intermediate compounds of the formula (M--L.sup.1)--L--(L.sup.2 --B), where (I) M has a structure according to formula (IV) ##STR1## (II) B is a lactam moiety; and (III) L, L.sup.1, and L.sup.2 together comprise a linking moiety.
摘要翻译：本发明提供制备其中（I）Q为喹诺酮部分的结构（Q-L1）-L-（L2-B）化合物的方法。（II）B是内酰胺部分; 和（III）L，L1和L2一起包含连接部分; 包括以下步骤：（1）将式（III）的化合物与含内酰胺的化合物偶联以形成中间体化合物; 和（2）通过与有机硅化合物反应使中间体环化，得到式（Q-L1）-L-（L2-B）的化合物。优选地，该方法还包括在偶联步骤之前的步骤，其中形成式（III）化合物和内酰胺化合物的保护形式; 和环化步骤后的脱保护步骤，其中除去保护基团。通过这些方法制备的优选的抗微生物化合物是β-内酰胺部分是青霉烯，碳青霉烯类，头孢烯或碳水化合物的那些。还优选那些其中L 1，L 2和L 2形成氨基甲酸酯部分或仲胺或叔胺部分的那些化合物。本发明还提供式（M-L1）-L-（L2-B）的新型中间体化合物，其中（I）M具有式（IV）的结构。内酰胺部分; 和（III）L，L1和L2一起包含连接部分。

84. 发明授权

US5789584A Substituted-pyridinyl cephalosporin antibiotics active against methicillin resistant bacteria 失效
标题翻译：取代的吡啶基头孢菌素抗生素对抗甲氧西林抗性细菌有活性
公开(公告)号：US5789584A
公开(公告)日：1998-08-04
申请号：US415064
申请日：1995-03-29
申请人： Burton G. Christensen , In-Seop Cho , Tomasz W. Glinka , Scott J. Hecker
发明人： Burton G. Christensen , In-Seop Cho , Tomasz W. Glinka , Scott J. Hecker
IPC分类号： A61K31/545 , A61K31/546 , C07D463/00 , C07D477/00 , C07D477/20 , C07D498/04 , C07D499/88 , C07D501/00 , C07D501/59 , C07D503/00 , C07D505/00 , C07D513/04 , C07D501/36
CPC分类号： C07D477/00 , C07D463/18 , C07D463/22 , C07D477/20 , C07D499/88 , C07D501/00 , C07D503/00 , C07D505/00 , C07D513/04
摘要： The present invention includes (7R)-7-(acylamino)-3-(substituted-pyridinyl)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against methicillin-resistant bacteria and are therefore useful as antibacterial agents.
摘要翻译：本发明包括（7R）-7-（酰基氨基）-3-（取代的 - 吡啶基）-3-头孢烯-4-羧酸或其对耐甲氧西林细菌具有抗生素活性的药理学上可接受的盐，因此可用作抗菌剂代理商

85. 发明授权

US5756493A Cephalosporin antibiotics 失效
标题翻译：头孢菌素类抗生素
公开(公告)号：US5756493A
公开(公告)日：1998-05-26
申请号：US413713
申请日：1995-03-29
申请人： Scott Hecker , In-Seop Cho , Tomasz Glinka , Burton Christensen
发明人： Scott Hecker , In-Seop Cho , Tomasz Glinka , Burton Christensen
IPC分类号： A61K31/545 , A61K31/546 , C07D463/00 , C07D477/00 , C07D477/20 , C07D498/04 , C07D499/88 , C07D501/00 , C07D501/59 , C07D503/00 , C07D505/00 , C07D513/04 , C07D501/60
CPC分类号： C07D477/00 , C07D463/18 , C07D463/22 , C07D477/20 , C07D499/88 , C07D501/00 , C07D503/00 , C07D505/00 , C07D513/04
摘要： The present invention includes novel (7R)-7-(acylamino)-3-(arylthio)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to .beta.-lactam antibiotics and are useful as antibacterial agents. The invention also relates to novel intermediates useful for making the novel compounds of the present invention and to novel methods for producing the novel compounds and intermediate compounds.
摘要翻译：本发明包括新的（7R）-7-（酰基氨基）-3-（芳硫基）-3-头孢烯-4-羧酸或其药理学上可接受的盐，其对广谱生物体表现出抗生素活性，包括对 β-内酰胺抗生素，可用作抗菌剂。本发明还涉及可用于制备本发明的新化合物的新型中间体和用于生产新化合物和中间体化合物的新方法。

86. 发明授权

US5703068A Penem compounds 失效
标题翻译： Penem化合物
公开(公告)号：US5703068A
公开(公告)日：1997-12-30
申请号：US971827
申请日：1993-02-19
申请人： Hiromitsu Iwata , Takashi Nakatsuka , Rie Tanaka , Masaji Ishiguro
发明人： Hiromitsu Iwata , Takashi Nakatsuka , Rie Tanaka , Masaji Ishiguro
IPC分类号： A61K31/43 , A61K31/431 , A61P31/04 , C07D499/88 , C07D499/883 , C07D499/893 , C07D499/897 , C07D499/00
CPC分类号： C07D499/88
摘要： Antibiotic penem compounds are represented by the following formula: ##STR1## wherein R represents a group of the following formula: ##STR2## in which R.sub.1 is a linear or branched, C.sub.1 -C.sub.6 alkyl group, R.sub.2 is a particular substituted or unsubstituted alkyl, aryl or aralkyl group, n is an integer of 1 or 2, and R.sub.3 represents a specific substituted or unsubstituted alkyl, aryl or aralkyl group. Antibiotic compositions for oral administration are also described.
摘要翻译： PCT No.PCT / JP91 / 01100 Sec。 371日期：1993年2月19日 102（e）日期1993年2月19日PCT 1991年8月16日PCT PCT。第WO92 / 03444号公报日期：1992年3月5日抗生素penem化合物由下式表示：其中R表示下式的基团：其中R 1是直链或支链的C 1 -C 6烷基，R 2 是特定的取代或未取代的烷基，芳基或芳烷基，n为1或2的整数，R 3表示特定的取代或未取代的烷基，芳基或芳烷基。还描述了用于口服给药的抗生素组合物。

87. 发明授权

US5698547A Cephalosporin antibiotics 失效
标题翻译：头孢菌素类抗生素
公开(公告)号：US5698547A
公开(公告)日：1997-12-16
申请号：US455969
申请日：1995-05-31
申请人： Burton Christensen , In-Seop Cho , Tomasz Glinka , Scott Hecker , Ving J. Lee , Zhijia J. Zhang
发明人： Burton Christensen , In-Seop Cho , Tomasz Glinka , Scott Hecker , Ving J. Lee , Zhijia J. Zhang
IPC分类号： C07D463/00 , C07D477/00 , C07D477/20 , C07D498/04 , C07D499/88 , C07D501/00 , C07D501/59 , C07D503/00 , C07D505/00 , C07D513/04 , C07D501/60 , A61K31/545
CPC分类号： C07D477/00 , C07D463/18 , C07D463/22 , C07D477/20 , C07D499/88 , C07D501/00 , C07D503/00 , C07D505/00 , C07D513/04
摘要： The present invention includes novel (7R)-7-(acylamino)-3-(arylthio)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to .beta.-lactam antibiotics and are useful as antibacterial agents. The invention also relates to novel intermediates useful for making the novel compounds of the present invention and to novel methods for producing the novel compounds and intermediate compounds.
摘要翻译：本发明包括新的（7R）-7-（酰基氨基）-3-（芳硫基）-3-头孢烯-4-羧酸或其药理学上可接受的盐，其对广谱生物体表现出抗生素活性，包括对 β-内酰胺抗生素，可用作抗菌剂。本发明还涉及可用于制备本发明的新化合物的新型中间体和用于生产新化合物和中间体化合物的新方法。

88. 发明授权

US5604218A Cephalosporin antibiotics 失效
公开(公告)号：US5604218A
公开(公告)日：1997-02-18
申请号：US413712
申请日：1995-03-30
申请人： Scott Hecker , In-Seop Cho , Burton Christensen , Tomasz Glinka , Ving J. Lee
发明人： Scott Hecker , In-Seop Cho , Burton Christensen , Tomasz Glinka , Ving J. Lee
IPC分类号： A61K31/545 , A61K31/546 , C07D463/00 , C07D477/00 , C07D477/20 , C07D498/04 , C07D499/88 , C07D501/00 , C07D501/59 , C07D503/00 , C07D505/00 , C07D513/04 , C07D501/60
CPC分类号： C07D477/00 , C07D463/18 , C07D463/22 , C07D477/20 , C07D499/88 , C07D501/00 , C07D503/00 , C07D505/00 , C07D513/04
摘要： The present invention includes novel (7R)-7-(acylamino)-3-(arylthio)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to .beta.-lactam antibiotics and are useful as antibacterial agents. The invention also relates to novel intermediates useful for making the novel compounds of the present invention and to novel methods for producing the novel compounds and intermediate compounds.

89. 发明授权

US5593986A Cephalosporin antibiotics 失效
公开(公告)号：US5593986A
公开(公告)日：1997-01-14
申请号：US415069
申请日：1995-03-29
申请人： Burton G. Christensen , In-Seop Cho , Tomasz W. Glinka , Scott J. Hecker
发明人： Burton G. Christensen , In-Seop Cho , Tomasz W. Glinka , Scott J. Hecker
IPC分类号： A61K31/545 , A61K31/546 , C07D463/00 , C07D477/00 , C07D477/20 , C07D498/04 , C07D499/88 , C07D501/00 , C07D501/59 , C07D503/00 , C07D505/00 , C07D513/04 , C07D501/60
CPC分类号： C07D477/00 , C07D463/18 , C07D463/22 , C07D477/20 , C07D499/88 , C07D501/00 , C07D503/00 , C07D505/00 , C07D513/04
摘要： The present invention includes novel (7R)-7-(acylamino)-3-(arylthio)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to .beta.-lactam antibiotics and are useful as antibacterial agents. The invention also relates to novel intermediates useful for making the novel compounds of the present invention and to novel methods for producing the novel compounds and intermediate compounds.

90. 发明授权

US5587474A Method for removing the protecting group for carboxyl group 失效
标题翻译：去除羧基保护基的方法
公开(公告)号：US5587474A
公开(公告)日：1996-12-24
申请号：US77383
申请日：1993-06-17
申请人： Kazuhiko Kondo , Hiroshi Horikawa , Tameo Iwasaki
发明人： Kazuhiko Kondo , Hiroshi Horikawa , Tameo Iwasaki
IPC分类号： C07D463/00 , C07D477/08 , C07D499/88 , C07D501/00 , C07D503/00 , C07D505/00 , C07D403/12
CPC分类号： C07D501/00 , C07D463/06 , C07D477/08 , C07D499/88 , C07D503/00 , C07D505/00 , Y02P20/55
摘要： A method for removing substituted or unsubstituted allyl group from .beta.-lactam compound having substituted or unsubstituted allyl group-protecting carboxyl group, which comprises treating said .beta.-lactam compound with palladium catalyst in the presence of allyl-scavenger in aqueous organic solvent, by which the substituted or unsubstituted group can be easily and effectively removed under moderate conditions so that the desired compound can be obtained in high yield at low cost.
摘要翻译：一种从具有取代或未取代的烯丙基保护羧基的β-内酰胺化合物中除去取代或未取代的烯丙基的方法，该方法包括在含有机溶剂的烯丙基清除剂存在下用钯催化剂处理所述β-内酰胺化合物，取代或未取代的基团可以在中等条件下容易且有效地除去，从而可以低成本高收率地获得所需化合物。

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