公开(公告)号：US20110282028A1

公开(公告)日：2011-11-17

申请号：US13132818

申请日：2009-12-04

Applicant: Jeffery Errington ,  Kathrin Schirner

Inventor： Jeffery Errington ,  Kathrin Schirner

IPC: C12Q1/25 ,  C07C233/18 ,  C07H17/08 ,  C07K9/00 ,  C07D493/04 ,  C07D499/68 ,  C07D499/44 ,  C07D499/72 ,  C07H15/234 ,  C07H15/26

CPC classification number: C12Q1/18 ,  G01N2500/00

Abstract: The invention provides a method of identifying an inhibitor of LtaS comprising: (a) providing bacteria which comprise a mutation in the mbl gene or homologue thereof; (b) culturing the bacteria of (a) in the presence of a test substance under conditions of low magnesium; (c) monitoring the growth of the bacteria; wherein growth or more rapid growth of the bacteria compared to growth in the absence of the test substance is indicative that the test substance is an inhibitor of LtaS.

Abstract translation: 本发明提供鉴定LtaS抑制剂的方法，包括：（a）提供在mbl基因或其同源物中包含突变的细菌; （b）在低镁的条件下，在试验物质的存在下培养（a）的细菌; （c）监测细菌的生长; 其中与不存在测试物质的生长相比，细菌的生长或更快的生长指示测试物质是LtaS的抑制剂。

公开(公告)号：US06960653B2

公开(公告)日：2005-11-01

申请号：US10211411

申请日：2002-07-31

Applicant: Robert Ivan McConnell ,  Elouard Benchikh ,  Stephen Peter Fitzgerald ,  John Victor Lamont

Inventor： Robert Ivan McConnell ,  Elouard Benchikh ,  Stephen Peter Fitzgerald ,  John Victor Lamont

IPC: G01N33/53 ,  C07D499/00 ,  C07D499/40 ,  C07K16/14 ,  C07K16/44 ,  G01N33/02 ,  G01N33/536 ,  G01N33/94 ,  C07K16/00 ,  C07D499/44 ,  G01N33/532

CPC classification number: C07D499/00 ,  C07K16/44 ,  G01N33/9446 ,  G01N2415/00

Abstract: The invention provides a hapten comprising a 6-[D-α-aminoacetamido] penicillin derivative crosslinked at the α-amino group with a substituted or unsubstituted phenyldicarbaldehyde. In addition, the invention provides an immunogen comprising the aforementioned hapten coupled to an antigenicity-conferring carrier material, a conjugate comprising the aforementioned hapten coupled to a labelling agent, as well as, antibodies raised against the aforementioned immunogen and capable of binding with at least one structural epitope of an intact β-lactam ring.

Abstract translation: 本发明提供了包含在α-氨基与交联的取代或未取代的苯基二甲醛的6- [D-α-氨基乙酰胺基]青霉素衍生物的半抗原。 此外，本发明提供了一种免疫原，其包含与产生抗原性的载体材料偶联的上述半抗原，包含与标记试剂偶联的上述半抗原的缀合物，以及针对上述免疫原产生并能够至少结合的抗体 完整β-内酰胺环的一个结构表位。

公开(公告)号：US20040220399A1

公开(公告)日：2004-11-04

申请号：US10855053

申请日：2004-05-27

Applicant: Research Corporation Technologies, Inc.

Inventor： John D. Buynak ,  Akireddy Srinivasa Rao ,  Venkata Ramana Doppalapudi

IPC: C07D499/44

CPC classification number: C07D499/00

Abstract: 1 wherein R1, R2, R3, R4 and n have any of the values defined in the specification, and their pharmaceutically acceptable salts, are useful for inhibiting null-lactamase enzymes, for enhancing the activity of null-lactam antibiotics, and for treating null-lactam resistant bacterial infections in a mammal. The invention also provides pharmaceutical compositions, processes for preparing compounds of formula I, and novel intermediates useful for the synthesis of compounds of formula I.

Abstract translation: 其中R 1，R 2，R 3，R 4和n具有说​​明书中定义的任何值及其药学上可接受的盐，可用于抑制β-内酰胺酶，以增强 β-内酰胺抗生素的活性，以及​​用于治疗哺乳动物中的β-内酰胺抗性细菌感染。 本发明还提供药物组合物，制备式I化合物的方法和可用于合成式I化合物的新中间体。

公开(公告)号：US20020193588A1

公开(公告)日：2002-12-19

申请号：US10089075

申请日：2002-04-08

Inventor： Akihiro Shimabayashi ,  Ichiro Kawahara

IPC: C07D499/44

CPC classification number: C07D499/00

Abstract: The crystal of the invention is crystal of diphenylmethyl 2-methyl-2-triazolylmethylpenam-3-carboxylate which is stable substantially without decomposition or degradation of properties even when left to stand at room temperature for 1 year. The crystal of the invention can be prepared by a process comprising the steps of concentrating a solution containing diphenylmethyl 2-methyl-2-triazolylmethylpenam-3-carboxylate represented by the formula (2) 1 wherein Ph is a phenyl group, diluting the concentrate with acetic ester and mixing the diluted solution with hexane or a solvent mixture of hexane and acetic ester to crystallize the diphenylmethyl 2-methyl-2-triazolylmethylpenam-3-carboxylate.

Abstract translation: 本发明的晶体是2-甲基-2-三唑基甲基氨基-3-羧酸二苯基甲酯的结晶，即使在室温下放置1年，基本上也不会发生分解或降解的性质而稳定。 本发明的晶体可以通过以下步骤制备：将浓缩由式（2）表示的二甲基-2-甲基-2-三唑基甲基甲氨基-3-羧酸二苯甲酯的溶液，其中Ph是苯基，将浓缩物与乙酸 将稀释的溶液与己烷或己烷和乙酸酯的溶剂混合物混合，使2-甲基-2-三唑基甲基氨基-3-羧酸二苯甲酯结晶。

公开(公告)号：US5354884A

公开(公告)日：1994-10-11

申请号：US955225

申请日：1992-10-01

Applicant: Rolf Grosser ,  Walter Lange ,  Bruno Bomer ,  Dieter Arlt ,  Dietmar Bielefeldt

Inventor： Rolf Grosser ,  Walter Lange ,  Bruno Bomer ,  Dieter Arlt ,  Dietmar Bielefeldt

IPC: C07B57/00 ,  B01D15/38 ,  B01J20/285 ,  B01J20/291 ,  C07C231/02 ,  C07C233/47 ,  C07C233/49 ,  C07C237/22 ,  C07D213/54 ,  C07D277/10 ,  C07D277/12 ,  C07D499/44 ,  C08F20/52 ,  C08F20/54 ,  C08F20/56 ,  C08F20/58 ,  C08F114/18 ,  G01N30/88 ,  C07C229/30

CPC classification number: B01J20/327 ,  B01D15/3833 ,  B01J20/261 ,  B01J20/265 ,  B01J20/285 ,  B01J20/29 ,  C07C233/49 ,  C08F20/54 ,  B01J2220/54 ,  C07C2101/14 ,  C07C2102/42

Abstract: .alpha.-Fluoro-substituted N-acryloylamino acid derivatives of the formula ##STR1## are used to make polymers optionally for chromatographic resolution of racemates into their enantiomers. The fluorine atom improves performance in many instances.

Abstract translation: 式（Ⅰ）的α-氟取代的N-丙烯酰氨基酸衍生物用于制备聚合物，任选用于将外消旋物色谱拆分成其对映异构体。 在许多情况下，氟原子提高了性能。

公开(公告)号：US5292924A

公开(公告)日：1994-03-08

申请号：US976246

申请日：1992-11-13

Applicant: Rolf Grosser ,  Walter Lange ,  Bruno Bomer ,  Dieter Arlt ,  Dietmar Bielefeldt

Inventor： Rolf Grosser ,  Walter Lange ,  Bruno Bomer ,  Dieter Arlt ,  Dietmar Bielefeldt

IPC: C07B57/00 ,  B01D15/38 ,  B01J20/285 ,  B01J20/291 ,  C07C231/02 ,  C07C233/47 ,  C07C233/49 ,  C07C237/22 ,  C07D213/54 ,  C07D277/10 ,  C07D277/12 ,  C07D499/44 ,  C08F20/52 ,  C08F20/54 ,  C08F20/56 ,  C08F20/58 ,  C08F114/18 ,  G01N30/88 ,  C07C233/05 ,  C07C229/08 ,  C07C229/12 ,  C07C233/06

CPC classification number: B01J20/327 ,  B01D15/3833 ,  B01J20/261 ,  B01J20/265 ,  B01J20/285 ,  B01J20/29 ,  C07C233/49 ,  C08F20/54 ,  B01J2220/54 ,  C07C2101/14 ,  C07C2102/42

Abstract: .alpha.-Fluoro-substituted N-acryloylamino acid derivatives of the formula ##STR1## are used to make polymers optionally for chromatographic resolution of racemates into their enantiomers. The fluorine atom improves performance in many instances.

Abstract translation: 式（Ⅰ）的α-氟取代的N-丙烯酰氨基酸衍生物用于制备聚合物，任选用于将外消旋物色谱拆分成其对映异构体。 在许多情况下，氟原子提高了性能。

公开(公告)号：US4933444A

公开(公告)日：1990-06-12

申请号：US371230

申请日：1989-06-26

Applicant: Sigeru Torii ,  Hideo Tanaka ,  Motoaki Tanaka ,  Shozo Yamada ,  Akira Nakai ,  Hisashi Ohbayashi

Inventor： Sigeru Torii ,  Hideo Tanaka ,  Motoaki Tanaka ,  Shozo Yamada ,  Akira Nakai ,  Hisashi Ohbayashi

IPC: C07D499/00 ,  C07D499/04 ,  C07D499/21 ,  C07D499/42 ,  C07D499/44 ,  C07D499/86

CPC classification number: C07D499/00 ,  Y02P20/55

Abstract: Disclosed is a process for preparing 2.beta.-substituted-methylpenicillin derivative of the formula ##STR1## wherein R is H or carboxyl protecting group, R.sub.1 is H or halo, R.sub.2 is H, lower alkyl, lower alkoxy, halogen, azido, lower alkylthio, phthalimide or a group --NHR.sub.3 (wherein R.sub.3 is H or acyl), and --N Y is an optionally substituted monocyclic or bicyclic heterocyclic group having 1 to 4 nitrogen atoms in the ring structure, the process comprising reacting a compound of the formula ##STR2## wherein X is Cl or Br, and R, R.sub.1 and R.sub.2 are as defined above with a heterocyclic compound of the formula ##STR3## wherein --N Y is as defined above.

公开(公告)号：US4873301A

公开(公告)日：1989-10-10

申请号：US147722

申请日：1988-01-25

Applicant: Yasushi Saotome ,  Takeo Miyazawa ,  Takeshi Endo

Inventor： Yasushi Saotome ,  Takeo Miyazawa ,  Takeshi Endo

IPC: C07D499/46 ,  C07D499/00 ,  C07D499/32 ,  C07D499/42 ,  C07D499/44 ,  C07F7/18 ,  C08F12/26 ,  C08F18/02 ,  C08F18/22 ,  C08F20/00 ,  C08F20/52 ,  C08F20/60 ,  C08F26/00 ,  C08F26/02 ,  C08F30/08

CPC classification number: C08F20/60 ,  C07D499/00 ,  C08F12/26

Abstract: Disclosed are an optically active, ethylenically unsaturated monomer represented by the following structural formula: ##STR1## wherein: A stands for S, SO or SO.sub.2 ; X and Y each stand for a hydrogen atom or a substituent selected from the group consisting of alkyl groups and acyl groups; Z stands for a substituent selected from the group consisting of alkoxy, alkylamino, hydroxyl and silyloxy groups; and X and Y can be bonded together to form a ring with the nitrogen atom to which they are bonded or X and Y can be a single group bonded to said nitrogen atom through a double bond, with the proviso that at least one of X and Z is an alkenyl equivalent to said group, and polymers of this monomer. One typical instance of the monomer is benzyl 6-acrylaminopenicillanate.

公开(公告)号：US4610823A

公开(公告)日：1986-09-09

申请号：US460729

申请日：1983-01-25

Applicant: Frank P. DiNinno ,  William J. Leanza ,  Ronald W. Ratcliffe

Inventor： Frank P. DiNinno ,  William J. Leanza ,  Ronald W. Ratcliffe

IPC: C07D205/08 ,  A61K31/397 ,  A61K31/425 ,  A61K31/43 ,  A61P31/04 ,  C07D205/09 ,  C07D205/095 ,  C07D499/04 ,  C07D499/42 ,  C07D499/44 ,  C07D499/88 ,  C07D499/897 ,  C07F1/10 ,  C07F3/14 ,  C07F5/00 ,  C07F7/18

CPC classification number: C07D205/09 ,  C07D205/095 ,  C07D499/88 ,  C07F7/1804 ,  Y02P20/55

Abstract: Disclosed is a synthesis for preparing substituted 2-thioxopenams which are useful in the synthesis of penem antibiotics 7 which may be conducted in an enantiospecific manner; said process proceeds from azetidinone 1 via the azetidinone acetic ester 2, the 4-metallothiozetidinone 3, and the 4-dithiocarbonylazetidinone 4 to the substituted 2-thioxopenam 5: ##STR1## wherein: R.sup.6 and R.sup.7 are independently selected from: hydrogen; R.sup.6 NH-- (R.sup.6 is acyl or H); substituted and unsubstituted: alkyl, alkenyl, alkynyl, aryl, heterocyclyl, heteroaryl, cycloalkyl, and cycloalkenyl; wherein said substituents are, inter alia: halo (chloro, bromo, fluoro, iodo), hydroxyl, cyano, carboxyl, amino, and the above-recited values for R.sup.6 and R.sup.7 ; in functional terms,R.sup.2 is a group which potentially forms a stable carbonium ion, for example: trityl (--C(C.sub.6 H.sub.5).sub.3),bis(p-methoxyphenyl)methyl, ##STR2## --2,4-dimethoxybenzyl, ##STR3## 2-(diphenyl)isopropyl, ##STR4## and the like; M is a thiophilic metal such as silver, thallium, mercury, or the like;and R.sup.1 is a protecting group such as allyl, p-nitrobenzyl or a biologically removable group (pharmaceutically acceptable ester moiety), for example: pivaloyloxymethyl, pivoloyloxyethyl, ethoxycarbonyloxymethyl, phthalidyl (5-methyl-2-oxo-1,3-dioxolen-4-yl)-; and X is a methyl leaving group such as phenoxy, p-chlorophenoxy, p-nitrophenoxy, phenylthio, alkylthio, alkoxy, chloro, or the like.R.sup.8 is inter alia, substituted and unsubstituted alkyl; the final penem products 7 are known, and their various embodiments are included by this definition.

Abstract translation: 公开了用于制备可以以对映体特异性方式进行的penem抗生素7的合成的用于制备取代的2-硫代青霉烯的合成物; 所述方法从氮杂环丁酮1经由氮杂环丁酮乙酸酯2，4-金属硫代环丁酮3和4-二硫代羰基氮杂环丁酮4进行到取代的2-硫青霉素5，其中：R6 和R 7独立地选自：氢; R6NH-（R6是酰基或H）; 取代和未取代的：烷基，烯基，炔基，芳基，杂环基，杂芳基，环烷基和环烯基; 其中所述取代基特别是：卤素（氯，溴，氟，碘），羟基，氰基，羧基，氨基，以及R6和R7的上述值; 在功能上，R2是潜在形成稳定的碳鎓离子的基团，例如：三苯甲基（-C（C 6 H 5）3），双（对甲氧基苯基）甲基，2,4-二甲氧基苄基， 2-（二苯基）异丙基，等等; M是硫醇类金属如银，铊，汞等; R1为保护基团，例如烯丙基，对硝基苄基或生物可除去基团（药学上可接受的酯部分），例如：新戊酰氧基甲基，桥联合氧基乙基，乙氧基羰氧基甲基，邻苯二甲酰基（5-甲基-2-氧代-1,3-二氧杂环戊烯 - 吡啶-4-基） - ; X为甲基离去基团，例如苯氧基，对氯苯氧基，对硝基苯氧基，苯硫基，烷硫基，烷氧基，氯等。 R8尤其是取代和未取代的烷基; 最终的penem产品7是已知的，并且它们的各种实施例被该定义包括。

公开(公告)号：US4422971A

公开(公告)日：1983-12-27

申请号：US293621

申请日：1981-08-04

Applicant: Piet J. Akkerboom ,  Christophorus Oldenhof

Inventor： Piet J. Akkerboom ,  Christophorus Oldenhof

IPC: C07D499/04 ,  C07D499/00 ,  C07D499/10 ,  C07D499/22 ,  C07D499/42 ,  C07D499/44 ,  C07D499/46 ,  C07D499/68

CPC classification number: C07D499/00

Abstract: A novel process for the preparation of 6-aminopenicilanic acid-1,1-dioxide and its non-toxic, pharmaceutically acceptable salts by deacylation of a penicillin-1,1-dioxide or its salts of which the 3-carboxylic acid is protected by such an easily removable group that a "one-pot process" is possible.

Abstract translation: PCT No.PCT / NL80 / 00039 Sec。 371日期1981年8月4日 102（e）日期1981年8月4日PCT提交1980年12月10日PCT公布。 公开号WO81 / 01707 日期：1981年6月25日。一种通过将青霉素-1,1-二氧化物或其盐的脱酰作用制备6-氨基番茄酸-1,1-二氧化物及其无毒的药学上可接受的盐的新方法， 3-羧酸被这种容易去除的组保护，“一锅法”是可能的。