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1. 发明申请

US20050004092A1 Penem derivatives and antimicrobial agent containing the same 审中-公开
标题翻译： Penem衍生物和含有相同的抗微生物剂
公开(公告)号：US20050004092A1
公开(公告)日：2005-01-06
申请号：US10831694
申请日：2004-04-26
申请人： Masaji Ishiguro , Takashi Nakatsuka , Rie Tanaka , Koshi Namikawa , Shinsuke Matsuki
发明人： Masaji Ishiguro , Takashi Nakatsuka , Rie Tanaka , Koshi Namikawa , Shinsuke Matsuki
IPC分类号： C07D499/74 , C07D499/88 , A61K31/43
CPC分类号： C07D499/88 , Y02P20/55
摘要： A penem derivative represented by the following formula (I): wherein R1 represents a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted alkylthio group, a substituted or unsubstituted alkenylthio group, a substituted or unsubstituted aralkylthio group, a substituted or unsubstituted arylthio group, a substituted or unsubstituted heterocyclic group, a substituted or unsubstituted heterocyclic thio group, a substituted or unsubstituted acylthio group, a mercapto group or a hydrogen atom, and R2 represents a hydrogen atom or a carboxyl-protecting group; or a pharmacologically acceptable salt thereof. The compound (I) exhibits strong antibacterial activities, and especially, shows strong activities against MRSA. It is therefore useful not only as a general antibacterial agent but also as an antibacterial agent for MRSA against which no general antibacterial agents are recognized to be-effective.
摘要翻译：由下式（I）表示的pen嗪衍生物：其中R1表示取代或未取代的烷基，取代或未取代的烯基，取代或未取代的芳烷基，取代或未取代的芳基，取代或未取代的烷硫基，取代或未取代的链烯硫基，取代或未取代的芳烷硫基，取代或未取代的芳硫基，取代或未取代的杂环基，取代或未取代的杂环硫基，取代或未取代的酰硫基，巯基或氢原子 R 2表示氢原子或羧基保护基; 或其药理学上可接受的盐。化合物（I）表现出强烈的抗菌活性，特别是对MRSA具有较强的活性。因此，不仅可以作为一般的抗菌剂，而且作为MRSA的抗菌剂也是有用的，其中没有一般的抗菌剂被认为是有效的。

2. 发明授权

US5747483A Penem derivatives, their preparation and pharmaceutical compositions containing them 失效
标题翻译： Penem衍生物，它们的制备和含有它们的药物组合物
公开(公告)号：US5747483A
公开(公告)日：1998-05-05
申请号：US414081
申请日：1995-03-17
申请人： Maria Altamura , Federico Maria Arcamone , Enzo Perrotta , Vittorio Pestellini , Piero Sbraci , Giuseppe Cascio
发明人： Maria Altamura , Federico Maria Arcamone , Enzo Perrotta , Vittorio Pestellini , Piero Sbraci , Giuseppe Cascio
IPC分类号： C07D499/88 , A61K31/43 , A61K31/48 , A61P31/04 , C07D499/883 , C07D499/897 , C07D499/861
CPC分类号： C07D499/88
摘要： Penem derivatives of general formula (I), below, and pharmaceutically acceptable salts thereof are disclosed. ##STR1## wherein: R.sub.1 is H, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.7 cycloalkyl, or an optionally protected C.sub.1 -C.sub.6 hydroxyalkyl; R.sub.2 is a free or esterified carboxyl group or a carboxylate anion; R.sub.3 is H or C.sub.1 -C.sub.6 alkyl; R.sub.4 is H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 mercaptoalkyl, C.sub.1 -C.sub.6 aminoalkyl, C.sub.1 -C.sub.6 alkyl substituted by a quaternary ammonium group, C.sub.1 -C.sub.6 carboxyalkyl, cycloalkyl, aryl, arylalkyl, heterocyclyl-alkyl optionally substituted, saturated or unsaturated heterocycle, or R.sub.3 and R.sub.4 are linked together to form a heterocyclic ring having 3-7 atoms; R.sub.5 and R.sub.6 independently are H, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 hydroxyalkyl, C.sub.1 -C.sub.6 mercaptoalkyl, C.sub. -C.sub.6 aminoalkyl, alkenyl, cycloalkyl, aryl, arylalkyl, alkylaryl, heterocyclyl-alkyl, C.sub.1 -C.sub.6 alkyl carboxyamide, or R.sub.5 and R.sub.6 are taken together to form a heterocyclic ring having 3-7 atoms, and n is an intiger from 1 to 3.
摘要翻译：公开了下述通式（I）的苦味衍生物及其药学上可接受的盐。（I）其中：R 1是H，C 1 -C 6烷氧基，C 3 -C 7环烷基或任选保护的C 1 -C 6羟烷基; R2是游离的或酯化的羧基或羧酸根阴离子; R3是H或C1-C6烷基; R4是H，C1-C6烷基，C1-C6羟基烷基，C1-C6巯基烷基，C1-C6氨基烷基，被季铵基团取代的C1-C6烷基，C1-C6羧基烷基，环烷基，芳基，芳基烷基，取代的饱和或不饱和杂环，或者R 3和R 4连接在一起形成具有3-7个原子的杂环; R5和R6独立地是H，C1-C6烷基，C1-C6羟基烷基，C1-C6巯基烷基，C-C6氨基烷基，烯基，环烷基，芳基，芳基烷基，烷基芳基，杂环基 - 烷基，C1-C6烷基羧酰胺或R5和 R6一起形成具有3-7个原子的杂环，并且n是1至3的酸酐。

3. 发明授权

US5719275A Silyl enol ether alkylation process 失效
标题翻译：甲硅烷基烯醇醚烷基化方法
公开(公告)号：US5719275A
公开(公告)日：1998-02-17
申请号：US460546
申请日：1995-06-02
申请人： Koichi Hirai , Yuji Iwano , Takahide Nishi , Akira Yoshida , Kozo Oda , Hiroo Koyama
发明人： Koichi Hirai , Yuji Iwano , Takahide Nishi , Akira Yoshida , Kozo Oda , Hiroo Koyama
IPC分类号： C07D205/08 , C07D401/12 , C07D403/12 , C07D477/02 , C07D477/04 , C07D477/20 , C07D499/88 , C07F7/10 , C07F7/18 , C07D227/00 , C07D487/04 , C07D499/04
CPC分类号： C07D401/12 , C07D205/08 , C07D403/12 , C07D477/02 , C07D477/04 , C07D477/20 , C07D499/88 , C07F7/10 , C07F7/186 , C07F7/1892 , Y02P20/55
摘要： A method for preparing compounds of formula (I): ##STR1## wherein: R.sup.1 is hydrogen or a hydroxy-protecting group; R.sup.2 is alkyl, alkoxy, halogen, optionally substituted phenyl or optionally substituted phenoxy; R.sup.3 is optionally substituted pyridyl, optionally substituted quinolyl or phenyl group which has a substituent of formula --CYNR.sup.5 R.sup.6, where Y is oxygen or sulfur, and R.sup.5 and R.sup.6 are each alkyl, aryl or aralkyl, or R.sup.5 and R.sup.6 and the nitrogen to which they are attached together form a heterocyclic group; R.sup.4 is hydrogen or an amino-protecting group; and Z is sulfur or oxygen. The process comprises reacting a compound of formula (II): ##STR2## in which R.sup.8, R.sup.9 and R.sup.10 are the same or different and each represents an alkyl group having from 1 to 4 carbon atoms or a phenyl group, with a compound of formula (III): ##STR3## in which R.sup.11 represents an acyloxy, alkylsulfonyl, arylsulfonyl, alkylsulfinyl or arylsulfinyl group.
摘要翻译：制备式（I）化合物的方法：其中：R1是氢或羟基保护基; R 2是烷基，烷氧基，卤素，任选取代的苯基或任选取代的苯氧基; R3是任选取代的吡啶基，任选取代的具有式-CYNR 5 R 6的取代基的喹啉基或苯基，其中Y是氧或硫，R 5和R 6各自是烷基，芳基或芳烷基，或者R 5和R 6以及它们一起形成杂环基; R4是氢或氨基保护基; Z是硫或氧。该方法包括使式（II）化合物：其中R 8，R 9和R 10相同或不同并且各自表示具有1至4个碳原子的烷基或苯基的式（II）化合物与式（III）化合物：其中R 11表示酰氧基，烷基磺酰基，芳基磺酰基，烷基亚磺酰基或芳基亚磺酰基。

4. 发明授权

US5648346A Antimicrobial carbacephem-quinolones 失效
标题翻译：抗菌药物喹诺酮类药物
公开(公告)号：US5648346A
公开(公告)日：1997-07-15
申请号：US477724
申请日：1995-06-07
申请人： Ronald Eugene White , Thomas Prosser Demuth, Jr.
发明人： Ronald Eugene White , Thomas Prosser Demuth, Jr.
IPC分类号： C07D499/897 , A61K31/431 , A61K31/47 , A61K31/535 , A61K31/545 , A61K31/546 , A61P31/04 , A61P43/00 , C07D215/56 , C07D401/04 , C07D401/12 , C07D401/14 , C07D409/12 , C07D417/12 , C07D417/14 , C07D455/04 , C07D463/00 , C07D463/16 , C07D471/04 , C07D477/10 , C07D477/14 , C07D477/20 , C07D487/04 , C07D498/04 , C07D498/06 , C07D499/00 , C07D499/04 , C07D499/86 , C07D499/87 , C07D499/88 , C07D501/00 , C07D501/18 , C07D501/20 , C07D501/34 , C07D503/00 , C07D505/00 , C07D513/04 , C07D513/06 , C07D513/16 , C07D519/00 , C07D519/06 , C07D521/00 , C07F9/6561 , C07D477/06 , A61K31/40 , A61K31/435
CPC分类号： C07D401/04 , C07D215/56 , C07D401/12 , C07D401/14 , C07D417/14 , C07D455/04 , C07D463/18 , C07D463/22 , C07D471/04 , C07D477/10 , C07D487/04 , C07D499/00 , C07D501/00 , C07D503/00 , C07D505/00 , C07D513/04
摘要： A substantially flat collapsed plastic bag with an evacuation form unit insert positioned therein as manufactured to serve as a form about which the filled bag will collapse as it is emptied. The form unit comprises a ring for mounting the unit on the spout of the bag and a multi-channel form extending radially from the ring and hingedly connected thereto. A simple method is provided for manufacturing the bag with the form unit insert.
摘要翻译：一个基本平坦的折叠的塑料袋，其中设置有排出形式的单元插入物，其被制造成用作填充袋在其被排空时将塌缩的形式。该形式单元包括用于将该单元安装在袋的出口上的环和从该环径向延伸并与其铰接连接的多通道形式。提供了一种简单的方法来制造具有形式单元插入物的袋子。

5. 发明授权

US5621084A Process for removal of allyl group or allyloxycarbonyl group 失效
标题翻译：除去烯丙基或烯丙氧基羰基的方法
公开(公告)号：US5621084A
公开(公告)日：1997-04-15
申请号：US417285
申请日：1995-04-03
申请人： Msanori Honda , Hiromasa Morita , Isao Nagakura
发明人： Msanori Honda , Hiromasa Morita , Isao Nagakura
IPC分类号： B01J31/02 , B01J31/18 , B01J31/22 , B01J31/24 , C07B41/02 , C07B43/04 , C07C209/62 , C07C269/06 , C07D499/00 , C07D499/88 , C07D501/00 , C07H9/04 , C07H1/06 , C07C29/10 , C07C41/00 , C07K1/00
CPC分类号： C07D499/00 , B01J31/185 , B01J31/2239 , B01J31/2404 , C07B41/02 , C07B43/04 , C07C209/62 , C07C269/06 , C07D499/88 , C07D501/00 , C07H9/04 , B01J2531/824 , B01J31/2282
摘要： This invention relates to a process for the removal of an allyl or allyloxycarbonyl group from an allyl or allyloxycarbonyl group protected compound (such as an allylic ester, carbonate, carbamate, O-allyl derivatives or N-allyl derivatives), which comprises contacting the allyl or allyloxycarbonyl group protected compound with a sulfinic acid compound, in the presence of a palladium catalyst in a reaction-inert solvent. Preferably, the sulfinic acid compound is represented by the formula:X--SO.sub.2 M (I)wherein X is C.sub.1-20 alkyl, substituted C.sub.1-20 alkyl (wherein the substituent(s) are independently halo, nitro, sulfo, oxo, amino, cyano, carboxy, hydroxy or moieties derived therefrom), phenyl, substituted phenyl (wherein the substituent(s) are independently C.sub.1-3 alkyl, halo nitro, sulfo, oxo, amino, cyano, carboxy, hydroxy, acetamido or moieties derived therefrom), furyl or thienyl; and M is hydrogen, an alkali metal or ammonium salt residue. Of these, most preferred sulfinic acid compound is lithium p-toluenesulfinate, sodium p-toluenesulfinate, potassium p-toluenesulfinate, p-toluenesulfinic acid, ammonium p-toluenesulfinate, lithium benzenesulfinate, sodium benzenesulfinate, potassium benzenesulfinate, benzenesulfinic acid or ammonium benzenesulfinate. This invention is well suited to a process for the conversion of an allyl ester of 5R,6S-6-(1R-hydroxyethyl)-2-(1R-oxo-3S-thiolanylthio)-2-penem-3-carboxylic acid to 5R,6S-6-(1R-hydroxyethyl)-2-(1R-oxo-3S-thiolanylthio)-2-penem-3-carboxylic acid.
摘要翻译：本发明涉及从烯丙基或烯丙氧基羰基保护的化合物（例如烯丙基酯，碳酸酯，氨基甲酸酯，O-烯丙基衍生物或N-烯丙基衍生物）中除去烯丙基或烯丙氧基羰基的方法，该方法包括使烯丙基或烯丙氧基羰基保护的化合物与亚磺酸化合物在钯催化剂存在下在反应惰性溶剂中反应。优选地，亚磺酸化合物由下式表示：X-SO 2 M（I）其中X是C 1-20烷基，取代的C 1-20烷基（其中取代基独立地是卤素，硝基，磺基，氧代，氨基，氰基，羧基，羟基或由其衍生的部分），苯基，取代的苯基（其中取代基独立地为C 1-3烷基，卤代硝基，磺基，氧代，氨基，氰基，羧基，羟基，乙酰氨基或由其衍生的部分），呋喃基或噻吩基; M为氢，碱金属或铵盐残基。其中最优选的亚磺酸化合物是对甲苯亚磺酸锂，对甲苯亚磺酸钠，对甲苯亚磺酸钾，对甲苯亚磺酸，对甲苯亚磺酸铵，苯亚磺酸锂，苯亚磺酸钠，苯亚磺酸钾，苯亚磺酸或苯亚磺酸铵。本发明非常适用于将5R，6S-6-（1R-羟乙基）-2-（1R-氧代-3S-硫杂环戊基硫代）-2-青霉烯-3-羧酸的烯丙酯转化成5R ，6S-6-（1R-羟乙基）-2-（1R-氧代-3S-硫杂环戊基硫代）-2-青霉烯-3-羧酸。

6. 发明授权

US5614624A Carbapenem 失效
标题翻译：卡巴培南
公开(公告)号：US5614624A
公开(公告)日：1997-03-25
申请号：US460209
申请日：1995-06-02
申请人： Koichi Hirai , Yuji Iwano , Takahide Nishi , Akira Yoshida , Kozo Oda , Hiroo Koyama
发明人： Koichi Hirai , Yuji Iwano , Takahide Nishi , Akira Yoshida , Kozo Oda , Hiroo Koyama
IPC分类号： C07D205/08 , C07D401/12 , C07D403/12 , C07D477/02 , C07D477/04 , C07D477/20 , C07D499/88 , C07F7/10 , C07F7/18 , C07D487/04
CPC分类号： C07D401/12 , C07D205/08 , C07D403/12 , C07D477/02 , C07D477/04 , C07D477/20 , C07D499/88 , C07F7/10 , C07F7/186 , C07F7/1892 , Y02P20/55
摘要： A compound of the formula ##STR1## in which: R.sup.1' is hydrogen or a carboxy-protecting group;R.sup.41' is hydrogen or a hydroxy-protecting group;R.sup.42' is a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy, a halogen, an aryl or an aryloxy; R.sup.43' is hydrogen, a C.sub.1 -C.sub.6 alkyl, a C.sub.1 -C.sub.6 alkoxy, a hydroxy, a halogen, a cyano, a nitro or a group of the formula --NR.sup.8' R.sup.9', where R.sup.8' and R.sup.9' are independently selected from the group consisting of hydrogen, amino-protecting groups, C.sub.1 -C.sub.6 alkyl groups and phenyl groups, or R.sup.8' and R.sup.9' together represent a group --(CH.sub.2).sub.q '--O.sub.r '--(CH.sub.2).sub.s '--, where q' and s' are independently 0 or an integer of from 1 to 5 and r' is 0 or 1, provided that (q'+s') is an integer of at least 2; R.sup.45' and R.sup.46' are independently selected from the group consisting of C.sub.1 -C.sub.6 alkyl groups and aryl groups, or R.sup.45' and R.sup.46' together represent a group --(CH.sub.2).sub.q '--O.sub.r '--(CH.sub.2).sub.s '--, where q' and s' are independently 0 or an integer of from 1 to 5 and r' is 0 or 1; Y' is oxygen or sulfur; and j' is 0, 1 or 2.
摘要翻译：式（IV'）的化合物，其中：R1'是氢或羧基保护基; R 41'是氢或羟基保护基; R 42'是C 1 -C 6烷基，C 1 -C 6烷氧基，卤素，芳基或芳氧基; R 43'是氢，C 1 -C 6烷基，C 1 -C 6烷氧基，羟基，卤素，氰基，硝基或式-NR 8'R 9'基团，其中R 8'和R 9'独立地选自由氢，氨基保护基，C 1 -C 6烷基和苯基组成的组，或者R 8'和R 9'一起表示基团 - （CH 2）q'-Or' - （CH 2）s'，其中q' 和s'独立地为0或1至5的整数，r'为0或1，条件是（q'+ s'）为至少2的整数; R 45'和R 46'独立地选自C 1 -C 6烷基和芳基，或者R 45'和R 46'一起表示基团 - （CH 2）q'-Or' - （CH 2）s - ，其中 q'和s'独立地为0或1至5的整数，r'为0或1; Y'是氧或硫; 并且j'为0,1或2。

7. 发明授权

US5602250A 6-(substituted methylene)penems and intermediates 失效
标题翻译： 6-（取代亚甲基）青霉烯和中间体
公开(公告)号：US5602250A
公开(公告)日：1997-02-11
申请号：US428101
申请日：1995-04-28
申请人： Nigel J. P. Broom , Frank P. Harrington
发明人： Nigel J. P. Broom , Frank P. Harrington
IPC分类号： C07D499/897 , A61K31/431 , A61K31/542 , A61P31/00 , A61P31/04 , A61P43/00 , C07D233/42 , C07D233/90 , C07D235/00 , C07D277/00 , C07D279/00 , C07D499/00 , C07D499/04 , C07D499/88 , C07D513/04 , C07D519/00 , C07D519/06 , A61K31/43
CPC分类号： C07D513/04 , C07D233/90 , C07D499/88
摘要： Compounds of formula (I) in which: R.sup.1 is hydrogen or an organic substituent group; R.sup.2 is a fused bicyclic heterocyclic ring system of general formula (a) wherein R.sup.4 and R.sup.5 are independently hydrogen or one or more substituents replacing hydrogen atoms in the ring system shown; m is 2 or 3; p is 0, 1 or 2; and R.sup.3 is hydrogen, a salt-forming cation or an ester-forming group; and the symbol .dbd./.dbd. indicates that the double bond may be in either the E or Z configuration.
摘要翻译： PCT No.PCT / EP93 / 02894 Sec。 371日期：1995年4月28日 102（e）日期1995年4月28日PCT提交1993年10月20日PCT公布。出版物WO94 / 10178 （I）化合物（Ⅰ）其中：R 1是氢或有机取代基; R2是通式（a）的稠合双环杂环体系，其中R 4和R 5独立地是氢或一个或多个取代所示环系中的氢原子的取代基; m为2或3; p为0,1或2; 和R 3是氢，成盐阳离子或成酯基; 符号= / =表示双键可以是E或Z配置。

8. 发明授权

US5530116A Antimicrobial quinolonyl lactams 失效
标题翻译：抗菌喹诺酮内酰胺
公开(公告)号：US5530116A
公开(公告)日：1996-06-25
申请号：US361919
申请日：1994-12-22
申请人： Thomas P. Demuth, Jr. , Ronald E. White
发明人： Thomas P. Demuth, Jr. , Ronald E. White
IPC分类号： A61K31/43 , A61K31/397 , A61K31/435 , A61K31/47 , A61K31/545 , A61K31/546 , A61P31/04 , C07D20060101 , C07D401/12 , C07D463/00 , C07D471/04 , C07D477/00 , C07D477/14 , C07D477/20 , C07D487/04 , C07D498/04 , C07D499/00 , C07D499/88 , C07D501/00 , C07D501/16 , C07D501/26 , C07D501/28 , C07D501/30 , C07D501/32 , C07D501/34 , C07D501/36 , C07D519/00 , C07D501/57
CPC分类号： C07D477/14 , C07D477/20 , C07D499/00 , C07D499/88 , C07D501/00
摘要： Antimicrobial quinolonyl lactam compounds comprising a lactam-containing moiety linked to a quinolone moiety, of the formula: ##STR1## wherein (1) A.sup.1, A.sup.2, A.sup.3, R.sup.1, and R.sup.4 generally form any of a variety of quinolone, naphthyridine or related cyclic moieties known in the art to have antimicrobial activity; and(2) R.sup.6 is part of a linking moiety, linking the quinolone moiety to a lactam-containing moiety having the formula: ##STR2## wherein (3) R.sup.10, R.sup.11, R.sup.12, R.sup.13, and R.sup.14, together with bonds "a" and "b", form any of a variety of lactam-containing moieties known in the art to have antimicrobial activity; and(4) the linking moiety includes (for example) carbamate, dithiocarbamate, urea, thiourea, isouronium, isothiouronium, guanidine, carbonate, trithiocarbonate, reversed carbamate, xanthate, reversed isouronium, reversed dithiocarbamate, reversed isothiouronium, amine, imine, ammonium, heteroarylium, ether, thioether, ester, thioester, amide, and hydrazide groups.
摘要翻译：包含与喹诺酮部分连接的含内酰胺部分的抗微生物喹诺酮内酰胺化合物，其具有下式：其中（1）A1，A2，A3，R1和R4通常形成多种喹诺酮，萘啶或相关的环状本领域已知的具有抗微生物活性的部分; （2）R6是连接部分的一部分，将喹诺酮部分与具有下式的含内酰胺的部分连接：其中（3）R10，R11，R12，R13和R14连同键“a” 和“b”形成本领域已知的具有抗微生物活性的各种含内酰胺的部分; 连接部分包括（例如）氨基甲酸酯，二硫代氨基甲酸酯，脲，硫脲，异脲，异硫脲，胍，碳酸酯，三硫代碳酸酯，反相氨基甲酸酯，黄原酸酯，反式异卤素，反式二硫代氨基甲酸酯，反式异硫脲，胺，亚胺，杂芳基，醚，硫醚，酯，硫酯，酰胺和酰肼基团。

9. 发明授权

US5492903A Crystalline esters of (+)-(5R, 6S)-6-[(R)-1-hydroxyethyl]-3-(3-pyridyl)-7-oxo-4-thia-1-azabicyclo[3.2.0]h e 失效
标题翻译：（+） - （5R，6S）-6 - [（R）-1-羟乙基] -3-（3-吡啶基）-7-氧代-4-硫杂-1-氮杂双环[3.2.0]庚烷 -2-烯-2-羧酸
公开(公告)号：US5492903A
公开(公告)日：1996-02-20
申请号：US112072
申请日：1993-08-26
申请人： Yoshiharu Maeda , Yukio Ishibashi , Tetsuya Tsukamoto , Masahiro Mizuno
发明人： Yoshiharu Maeda , Yukio Ishibashi , Tetsuya Tsukamoto , Masahiro Mizuno
IPC分类号： C07D499/88 , C07D499/00 , A61K31/425
CPC分类号： C07D499/88
摘要： Crystalline acetoxymethyl and pivaloyloxymethyl esters of (+)-(5R, 6S)-6-[(R)-1-hydroxyethyl]-3-(3-pyridyl)-7-oxo-4-thia-1-azabicyclo-[3.2.0]hept-2-ene-carboxylic acid can be obtained by adding a poor solvent to a solution of acetoxymethyl or pivaloyloxymethyl ester of (+)-(5R, 6S)-6-[(R)-1-hydroxyethyl]-3-(3-pyridyl)-7-oxo-4-thia-1-azabicyclo-[3.2.0]hept-2-ene-carboxylic acid in a good solvent. The crystalline penem compounds obtained show improved stability and are useful antibacterial agents.
摘要翻译：（+） - （5R，6S）-6 - [（R）-1-羟乙基] -3-（3-吡啶基）-7-氧代-4-硫杂-1-氮杂双环[3.2 通过向（+） - （5R，6S）-6 - [（R）-1-羟乙基] - （（R）-1-羟乙基）-6 - [（R）-1-羟基乙基） - 乙酰氧基甲基酯的乙酰氧基甲基或新戊酰氧基甲基酯的溶液中加入不良溶剂， 3-（3-吡啶基）-7-氧代-4-硫杂-1-氮杂双环[3.2.0]庚-2-烯羧酸在良溶剂中反应。获得的结晶青枯烯化合物显示出改进的稳定性，并且是有用的抗菌剂。

10. 发明授权

US5122604A .beta.-lactam compounds 失效
标题翻译：（BETA）-LACTAM化合物
公开(公告)号：US5122604A
公开(公告)日：1992-06-16
申请号：US525817
申请日：1990-05-21
申请人： Makoto Sunagawa , Haruki Matsumura , Takaaki Inoue , Masatomo Fukasawa , Masuhiro Kato
发明人： Makoto Sunagawa , Haruki Matsumura , Takaaki Inoue , Masatomo Fukasawa , Masuhiro Kato
IPC分类号： A61K31/43 , C07D205/08 , C07D207/16 , C07D207/24 , C07D401/12 , C07D477/20 , C07D487/04 , C07D499/00 , C07D499/32 , C07D499/88 , C07D499/887 , C07F7/10 , C07F7/18 , C07F9/6561
CPC分类号： C07D477/20 , C07D205/08 , C07D207/16 , C07D207/24 , C07D401/12 , C07D499/88 , C07F7/10 , C07F7/186 , C07F9/65611 , Y02P20/55
摘要： Novel .beta.-lactam compounds belonging to carbapenem or penem derivatives useful as antimicrobial agents or intermediates therefor and a process for producing these compounds are disclosed.

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