知搜-全球专利检索

  1. Login
  2. Sign Up

Search Results

33 records (took 0.05 seconds)

    Novel fluorogenic substrates for beta-lactamase gene expression
    1.
    发明申请
    Novel fluorogenic substrates for beta-lactamase gene expression 失效
    用于β-内酰胺酶基因表达的新型荧光底物

    公开(公告)号：US20050118669A1

    公开(公告)日：2005-06-02

    申请号：US10884019

    申请日：2004-07-02

    Applicant: Roger Tsien ,  Jianghong Rao

    Inventor： Roger Tsien ,  Jianghong Rao

    IPC: C07D463/00 ,  C07D501/00 ,  C07D501/14 ,  C07D505/00 ,  C07F9/6561 ,  C12Q1/18 ,  C12Q1/37

    CPC classification number: C12Q1/6897 ,  C07D463/18 ,  C07D463/20 ,  C07D501/00 ,  C07D505/00 ,  C07F9/65613

    Abstract: Fluorescent substrates for beta-lactamases having the general formula shown above are provided. Z includes a fluorophore or chromophore and includes a group that may link to the lactam-containing group; R1 and R2 are independently selected from H, aliphatic, aromatic, alkyl, and acyl; R4 may be H and lower alkyl; B may be H, physiologically acceptable salts or metal, ester groups, ammonium cations, —CHR5OCO(CH2)nCH3, —CHR5OCOC(CH3)3, acylthiomethyl, acyloxy-alpha-benz, deltabutyrolactonyl, methoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, beta-morpholinoethyl, dialkylaminoethyl, and dialkylaminocarbonyloxymethyl, in which R5 is selected from the group consisting of H and lower alkyl; n is an integer between 0 and 10, inclusive; and A may be S, O, SO, SO2 or CH2. In embodiments, the beta-lactam ring may be cleaved by a beta-lactamase enzyme effective to free a fluorophore. Methods of assaying beta-lactamase activity and monitoring expression in systems using beta-lactamase as a reporter gene are also disclosed.

    Abstract translation: 提供了具有上述通式的β-内酰胺酶的荧光底物。 Z包括荧光团或发色团，并且包括可以连接到含内酰胺基团的基团; R 1和R 2独立地选自H，脂族，芳族，烷基和酰基; R 4可以是H和低级烷基; B可以是H，生理上可接受的盐或金属，酯基，铵阳离子，-CHR 5 OCO（CH 2）n CH 2 （CH 3）3，酰基硫甲基，酰氧基-α-苯并三唑，丁内酰脲，甲氧羰基氧基甲基， 苯基，甲基亚磺酰基甲基，β-吗啉代乙基，二烷基氨基乙基和二烷基氨基羰基氧基甲基，其中R 5选自H和低级烷基; n是0和10之间的整数，包括0和10; A可以是S，O，SO，SO 2或CH 2。 在实施方案中，β-内酰胺环可以被有效释放荧光团的β-内酰胺酶切割。 还公开了使用β-内酰胺酶作为报告基因的系统中测定β-内酰胺酶活性和监​​测表达的方法。

    Carbacephalosporin compound, their preparation and use
    2.
    发明授权
    Carbacephalosporin compound, their preparation and use 失效
    碳青霉素化合物，其制备和用途

    公开(公告)号：US5665717A

    公开(公告)日：1997-09-09

    申请号：US522411

    申请日：1996-01-18

    Applicant: Richard Leonard Elliott ,  Neville Hubert Nicholson ,  Andrew Kenneth Takle

    Inventor： Richard Leonard Elliott ,  Neville Hubert Nicholson ,  Andrew Kenneth Takle

    IPC: A61K31/435 ,  A61P31/04 ,  C07D463/00 ,  A61K31/395 ,  C07D221/06

    CPC classification number: C07D463/06 ,  C07D463/18 ,  Y02P20/55

    Abstract: Carbacephalosporin compounds of formula (I), ##STR1## salts thereof, processes for their synthesis and uses thereof, wherein: R.sup.1 is hydrogen, methoxy or formamido; R.sup.2 is an acyl group; CO.sub.2 R.sup.3 is a carboxy group or a carboxylate anion, or R.sup.3 is a carboxy protecting group or a pharmaceutically acceptable salt-forming group or in vivo hydrolysable ester group; R.sup.4, R.sup.5, R.sup.6 and R.sup.7 represent hydrogen or a substituent; R.sup.4 and R.sup.7 may be replaced by a chemical bond between the two carbon atoms shown; R.sup.5 and R.sup.6 may be linked together into a cyclic system. The compounds (I) have antibacterial properties.

    Abstract translation: PCT No.PCT / EP94 / 00811 Sec。 371日期：1996年1月18日 102（e）日期1996年1月18日PCT 1994年3月10日PCT公布。 公开号WO94 / 21633 1994年9月29日，具有式（I）的乙酰菌素化合物，其化合物及其用途，其中：R1是氢，甲氧基或甲酰氨基; R2是酰基; CO 2 R 3是羧基或羧酸根阴离子，或R3是羧基保护基或药学上可接受的成盐基团或体内可水解的酯基; R4，R5，R6和R7表示氢或取代基; R4和R7可以被所示的两个碳原子之间的化学键取代; R5和R6可以连接在一起成为循环系统。 化合物（I）具有抗菌性。

    7 acylamidocarbacephem antibacterial agents
    3.
    发明授权
    7 acylamidocarbacephem antibacterial agents 失效
    7酰氨基糖芽孢杆菌抗菌剂

    公开(公告)号：US4957912A

    公开(公告)日：1990-09-18

    申请号：US812497

    申请日：1985-12-23

    Applicant: Burton G. Christenson ,  Ronald W. Ratcliffe

    Inventor： Burton G. Christenson ,  Ronald W. Ratcliffe

    IPC: C07C45/44 ,  C07C51/60 ,  C07D205/085 ,  C07D205/095 ,  C07D265/08 ,  C07D317/24 ,  C07D317/28 ,  C07D463/00 ,  C07D487/04 ,  C07D501/20 ,  C07D505/00 ,  C07F9/40 ,  C07F9/568

    CPC classification number: C07F9/5683 ,  C07C255/00 ,  C07C45/44 ,  C07C51/60 ,  C07D205/085 ,  C07D205/095 ,  C07D265/08 ,  C07D317/24 ,  C07D317/28 ,  C07D463/16 ,  C07D463/18 ,  C07D463/22 ,  C07D505/00 ,  C07F9/4006

    Abstract: Novel antibiotics of the formula: ##STR1## and its salts, esters and amides wherein R is acyl;B is H, OMe, Me or SR wherein R is lower alkyl or aryl;A.sup.1 is hydrogen, hydroxy, or an organic group; and,X is a divalent radical selected from --O--, --CH.sub.2 --, or --NY-- where Y is hydrogen or lower alkyl of from 1 to 6 carbon atoms such as methyl, ethyl, i-propyl, n-butyl, n-pentyl, n-hexyl and the like, formyl or benzyl.This invention is directed to novel antibiotics, novel intermediates useful in their preparation, and processes for preparing the novel antibiotics. The novel antibiotics are effective against gram-negative bacteria including Proteus vulgaris, E. coli and Salmonella schottmulleri, and gram-positive bacteria including Staphylococcus aureas and Bacillus subtilis and are useful in combatting bacterial infections in animals or humans in addition to various industrial applications.

    Abstract translation: 新型抗生素，分子式如下：其中R为酰基的盐，酯和酰胺; B是H，OMe，Me或SR，其中R是低级烷基或芳基; A1是氢，羟基或有机基团; X为选自-O - ， - CH 2 - 或-NY-的二价基团，其中Y为氢或1至6个碳原子的低级烷基如甲基，乙基，异丙基，正丁基，正丁基 戊基，正己基等，甲酰基或苄基。 本发明涉及新型抗生素，其制备中可用的新型中间体以及制备新型抗生素的方法。 新型抗生素对革兰氏阴性细菌有效，包括普通变形杆菌，大肠杆菌和沙门氏菌，革兰氏阳性菌，包括金黄色葡萄球菌和枯草芽孢杆菌，除了各种工业应用外，还可用于对抗动物或人类的细菌感染。

    Fluorogenic substrates for BETA-lactamase gene expression
    4.
    发明授权
    Fluorogenic substrates for BETA-lactamase gene expression 失效
    荧光底物用于BETA-内酰胺酶基因表达

    公开(公告)号：US07427680B2

    公开(公告)日：2008-09-23

    申请号：US10884019

    申请日：2004-07-02

    Applicant: Roger Y. Tsien ,  Jianghong Rao

    Inventor： Roger Y. Tsien ,  Jianghong Rao

    IPC: C07D501/24 ,  G01N33/573

    CPC classification number: C12Q1/6897 ,  C07D463/18 ,  C07D463/20 ,  C07D501/00 ,  C07D505/00 ,  C07F9/65613

    Abstract: Fluorescent substrates for beta-lactamases having the general formula shown above are provided. Z includes a fluorophore or chromophore and includes a group that may link to the lactam-containing group; R1 and R2 are independently selected from H, aliphatic, aromatic, alkyl, and acyl; R4 may be H and lower alkyl; B may be H, physiologically acceptable salts or metal, ester groups, ammonium cations, —CHR5OCO(CH2)nCH3, —CHR5OCOC(CH3)3, acylthiomethyl, acyloxy-alpha-benz, deltabutyrolactonyl, methoxycarbonyloxymethyl, phenyl, methylsulphinylmethyl, beta-morpholinoethyl, dialkylaminoethyl, and dialkylaminocarbonyloxymethyl, in which R5 is selected from the group consisting of H and lower alkyl; n is an integer between 0 and 10, inclusive; and A may be S, O, SO, SO2 or CH2. In embodiments, the beta-lactam ring may be cleaved by a beta-lactamase enzyme effective to free a fluorophore. Methods of assaying beta-lactamase activity and monitoring expression in systems using beta-lactamase as a reporter gene are also disclosed.

    Abstract translation: 提供了具有上述通式的β-内酰胺酶的荧光底物。 Z包括荧光团或发色团，并且包括可以连接到含内酰胺基团的基团; R 1和R 2独立地选自H，脂族，芳族，烷基和酰基; R 4可以是H和低级烷基; B可以是H，生理上可接受的盐或金属，酯基，铵阳离子，-CHR 5 OCO（CH 2）n CH 2 （CH 3）3，酰基硫甲基，酰氧基-α-苯并三唑，丁内酰脲，甲氧羰基氧基甲基， 苯基，甲基亚磺酰基甲基，β-吗啉代乙基，二烷基氨基乙基和二烷基氨基羰基氧基甲基，其中R 5选自H和低级烷基; n是0和10之间的整数，包括0和10; A可以是S，O，SO，SO 2或CH 2。 在实施方案中，β-内酰胺环可以被有效释放荧光团的β-内酰胺酶切割。 还公开了使用β-内酰胺酶作为报告基因的系统中测定β-内酰胺酶活性和监​​测表达的方法。

    7-substituted-amino-3-substituted-3-cephem-4-carboxylic acids
    7.
    发明授权
    7-substituted-amino-3-substituted-3-cephem-4-carboxylic acids 失效
    7-取代 - 氨基-3-取代-3-头孢烯-4-羧酸

    公开(公告)号：US5525599A

    公开(公告)日：1996-06-11

    申请号：US95383

    申请日：1993-07-21

    Applicant: Ho-Shen Lin

    Inventor： Ho-Shen Lin

    IPC: C07D463/00 ,  C07D501/00 ,  C07D501/20 ,  C07D501/34 ,  C07D501/59 ,  C07D505/00 ,  C07D498/04 ,  A61K31/535

    CPC classification number: C07D505/00 ,  C07D463/18 ,  C07D501/00 ,  Y02P20/55

    Abstract: The invention provides compounds of the formula ##STR1## wherein X is CH.sub.2, S or O; R.sub.1 is a 3 position substituent such as hydrogen, hydroxy, halo, trifluoromethyl, C.sub.2 F.sub.5, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 substituted alkyl, C.sub.1 -C.sub.6 alkenyl, C.sub.1 -C.sub.6 alkynyl, CH.sub.2 O(CO)R', CH.sub.2 O(CO)NH.sub.2, CO.sub.2 R', thio(C.sub.1 -C.sub.6)alkyl, thio(C.sub.1 C.sub.6)alkenyl, oxo(C.sub.1 -C.sub.6)alkyl, phosphine oxide, quaternary ammonium group, substituted or unsubstituted thiazolothio, or oxo(C.sub.1 -C.sub.6)alkenyl;wherein R' is hydrogen, C.sub.1 -C.sub.6 alkyl, or C.sub.1 -C.sub.6 alkenyl;R.sub.2 is hydrogen or a carboxy protecting group;R.sub.3 is ##STR2## (CH.sub.2).sub.n ; wherein R.sub.6 is hydrogen Me, CH.sub.2 F, CF.sub.3, C.sub.2 H.sub.5, CH.sub.2 CH.sub.2 F, CH.sub.2 CF.sub.3, C.sub.2 F.sub.5, CH.sub.2 CO.sub.2 R', CH.sub.2 CONH.sub.2, C(Me).sub.2 CO.sub.2 R', or C(Me).sub.2 CONH.sub.2 ; and n is 0-5;R.sub.4 is ##STR3## wherein Z is O, S, NH, or CH.sub.2 ; Y is CH or N; and R.sub.7 is hydrogen, C.sub.1 -C.sub.6 alkyl, CONH.sub.2, or CO.sub.2 R'; andR.sub.5 is ##STR4## wherein R.sub.8 is CH, N, COH, CO(C.sub.1 -C.sub.6 alkyl) CSH, or CNH.sub.2 ; and R.sub.9 is R.sub.8 as defined; said R.sub.5 optionally substituted 1-4 times with halo, OH, SH, NH.sub.2, NO.sub.2, CH.sub.3, C.sub.2 H.sub.5, CO.sub.2 R', CONH.sub.2, SO.sub.3 H, or SO.sub.2 NHR'; and salts thereof. Also, pharmaceutical formulations and methods for treating bacterial infections in man or other animals using the above compounds are disclosed.

    Abstract translation: 本发明提供式（I）的化合物，其中X是CH 2，S或O; R1是3位取代基，例如氢，羟基，卤素，三氟甲基，C2F5，C1-C6烷基，C1-C6取代的烷基，C1-C6烯基，C1-C6炔基，CH2O（CO）R'，CH2O（CO） NH 2，CO 2 R'，硫代（C 1 -C 6）烷基，硫代（C 1 -C 6）烯基，氧代（C 1 -C 6）烷基，氧化膦，季铵基，取代或未取代的噻唑硫基或氧代（C 1 -C 6） 其中R'是氢，C 1 -C 6烷基或C 1 -C 6烯基; R2是氢或羧基保护基; （CH2）n; 其中R 6是氢，CH 2 F，CF 3，C 2 H 5，CH 2 CH 2 F，CH 2 CF 3，C 2 F 5，CH 2 CO 2 R'，CH 2 CONH 2，C（Me）2 CO 2 R'或C（Me） n为0-5; R4是，其中Z是O，S，NH或CH2; Y是CH或N; 并且R 7是氢，C 1 -C 6烷基，CONH 2或CO 2 R'; 其中R 8是CH，N，COH，CO（C 1 -C 6烷基）CSH或CNH 2; 并且R 9是如所定义的R8; 所述R5任选被卤素，OH，SH，NH 2，NO 2，CH 3，C 2 H 5，CO 2 R'，CONH 2，SO 3 H或SO 2 NHR'取代1-4次; 及其盐。 此外，公开了使用上述化合物治疗人或其他动物中的细菌感染的药物制剂和方法。

Patent Agency Ranking