Branched polymers and their conjugates
    51.
    发明授权
    Branched polymers and their conjugates 有权
    支链聚合物及其共轭物

    公开(公告)号:US07872072B2

    公开(公告)日:2011-01-18

    申请号:US11336695

    申请日:2006-01-20

    摘要: The present invention is directed to branched reactive water-soluble polymers comprising at least two polymer arms, such as poly(ethylene glycol), attached to a central aliphatic hydrocarbon core molecule through heteroatom linkages. The branched polymers bear at least one functional group for reacting with a biologically active agent to form a biologically active conjugate. The functional group of the branched polymer can be directly attached to the aliphatic hydrocarbon core or via an intervening linkage, such as a heteroatom, -alkylene-, —O-alkylene-O—, -alkylene-O-alkylene-, -aryl-O—, —O-aryl-, (—O-alkylene-)m, or (-alkylene-O—)m linkage, wherein m is 1-10.

    摘要翻译: 本发明涉及包含通过杂原子键连接到中心脂族烃核心分子的至少两个聚合物臂(例如聚(乙二醇))的支链反应性水溶性聚合物。 支链聚合物具有至少一个用于与生物活性剂反应以形成生物活性缀合物的官能团。 支链聚合物的官能团可以直接连接到脂族烃核心上或通过插入键如杂原子, - 亚烷基 - , - - 亚烷基-O-, - 亚烷基-O-亚烷基 - , - 芳基 - O-,-O-芳基 - ,( - - 亚烷基 - )m或( - 亚烷基-O-)m键,其中m为1-10。

    Alkoxylations in ketone solvents
    55.
    发明申请
    Alkoxylations in ketone solvents 审中-公开
    酮溶剂中的烷氧化

    公开(公告)号:US20070282079A1

    公开(公告)日:2007-12-06

    申请号:US11443630

    申请日:2006-05-31

    申请人: Philip L. Leung

    发明人: Philip L. Leung

    IPC分类号: C07C41/03 C07C215/02

    摘要: Substrate or starting compounds having at least one active hydrogen may be reacted with one or more alkylene oxide in a ketone solvent at reduced temperatures compared with conventional, molten methods to give an adduct product having reduced color. Suitable ketone solvents include, but are not necessarily limited to, methyl isobutyl ketone, diethyl ketone, methyl ethyl ketone, and mixtures thereof. The alkoxylation reaction may be conducted at a temperature in the range of about 30 to about 160° C. Suitable catalysts may include tertiary amines or caustic compounds such as NaOH and KOH.

    摘要翻译: 与常规的熔融方法相比,具有至少一种活性氢的底物或起始化合物可以与酮溶剂中的一种或多种烯化氧在降低的温度下反应,得到具有降低颜色的加合物产物。 合适的酮溶剂包括但不限于甲基异丁基酮,二乙基酮,甲基乙基酮及其混合物。 烷氧基化反应可以在约30至约160℃的温度范围内进行。合适的催化剂可包括叔胺或苛性化合物如NaOH和KOH。

    Autoinducer compound to improve the productivity of natamycin streptomyces strains
    56.
    发明申请
    Autoinducer compound to improve the productivity of natamycin streptomyces strains 审中-公开
    自由诱导剂化合物,以提高游霉素链霉菌菌株的生产力

    公开(公告)号:US20060275873A1

    公开(公告)日:2006-12-07

    申请号:US10557230

    申请日:2004-05-13

    IPC分类号: C12P19/62 C12N1/21 C07C215/02

    摘要: The invention provides a compound of the formula (I). Furthermore, the invention provides a process for the production of a compound of formula (I). The present invention also provides a process for the production of natamycin by a Streptomyces strain comprising adding a composition comprising an auto inducer to the fermentation medium. The present invention furthermore provides the use of a compound of formula (I) in the manufacture of a product by fermentation of a Streptomyces strain. The present invention finally discloses a Streptomyces strain that is defective in natamycin production and that is capable of producing a compound of formula (I) wherein both R1 and R2 are hydrogen and a Streptomyces strain that is defective in production of a compound of formula (I) wherein both R1 and R2 are hydrogen and that is capable of producing natamycin in the presence of said compound.

    摘要翻译: 本发明提供式(I)化合物。 此外,本发明提供了制备式(I)化合物的方法。 本发明还提供了一种通过链霉菌菌株生产游霉素的方法,包括向发酵培养基中加入包含自动诱导剂的组合物。 本发明还提供式(I)化合物在通过链霉菌菌株发酵制造产物中的用途。 本发明最终公开了一种在游霉素生产中缺陷的链霉菌属菌株,其能够生产式(I)化合物,其中R 1和R 2都是氢 和在其中R 1和R 2都是氢的式(I)化合物的制备中有缺陷的链霉菌属菌株,并且在存在下能够产生那他霉素 的所述化合物。

    2,4-pentadienoic acid derivatives having retinoid-like biological
activity
    59.
    发明授权
    2,4-pentadienoic acid derivatives having retinoid-like biological activity 失效
    具有类视黄醇样生物活性的2,4-戊二烯酸衍生物

    公开(公告)号:US6114533A

    公开(公告)日:2000-09-05

    申请号:US390825

    申请日:1999-09-07

    摘要: Compounds of Formula 1 ##STR1## wherein Z is Formula 3, ##STR2## Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R.sub.4 groups, or Y is phenyl, said groups being optionally substituted with one or two R.sub.4 groups, the divalent Y radical being substituted by the Z and --CR.sub.1 .dbd.CR.sub.1 --CR.sub.1 .dbd.CR.sub.1 groups on adjacent carbons; X is NR.sub.5 ; R.sub.1 and R.sub.2 independently are H, lower alkyl or fluoroalkyl; R.sub.3 is hydrogen, lover alkyl, Cl or Br; R.sub.4 is lower alkyl, fluoroalkyl or halogen; R.sub.5 is H or lower alkyl, and a is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, CR.sub.7 OR.sub.13 O, or tri-lower alkylsilyl, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons, a cycloalkyl group of 5 to 10 carbons or trimethylsilylalkyl where the alkyl group has 1 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.11 is lower alkyl, phenyl or lower alkylphenyl, R.sub.12 is lower alkyl, and R.sub.13 is divalent alkyl radical of 2-5 carbons, have retinoid like biological activity.

    摘要翻译: 式1的化合物,其中Z是式3,Y是任选被一个或两个R 4基团取代的3至8个碳的环烷基或环烯基,或Y是苯基,所述基团任选被一个或两个R 4基团取代,二价Y基团 被相邻碳上的Z和-CR1 = CR1-CR1 = CR1基团取代; X是NR5; R1和R2独立地为H,低级烷基或氟代烷基; R3是氢,有情人烷基,Cl或Br; R4是低级烷基,氟烷基或卤素; R5是H或低级烷基,a是氢,COOH或其药学上可接受的盐,COOR8,CONR9R10,-CH2OH,CH2OR11,CH2OCOR11,CHO,CH(OR12)2,CHOR13O,-COR7,CR7(OR12) CR 7OR 13 O或三低级烷基甲硅烷基,其中R 7为含有1至5个碳的烷基,环烷基或烯基,R 8为碳原子数1至10的烷基,碳原子数为5至10的环烷基或烷基具有的三甲基甲硅烷基烷基 1至10个碳,或R8为苯基或低级烷基苯基,R9和R10独立地为氢,1-10个碳原子的烷基或5-10个碳原子的环烷基,或苯基或低级烷基苯基,R11为低级烷基, 苯基或低级烷基苯基,R12为低级烷基,R13为2-5个碳原子的二价烷基,具有类视黄醇类生物活性。

    2,4-Pentadienoic acid derivatives having retinoid-like biological
activity
    60.
    发明授权
    2,4-Pentadienoic acid derivatives having retinoid-like biological activity 失效
    具有类视黄醇样生物活性的2,4-二戊烯酸衍生物

    公开(公告)号:US5780647A

    公开(公告)日:1998-07-14

    申请号:US805793

    申请日:1997-02-25

    摘要: Compounds of Formula 1 ##STR1## wherein Z is selected from the group consisting of the radicals shown in Formula 2 and in Formula 3, ##STR2## Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R.sub.4 groups, or Y is selected from phenyl, pyridyl, thienyl, furyl, pyrrolyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, and imidazolyl, said groups being optionally substituted with one or two R.sub.4 groups, the divalent Y radical being substituted by the Z and --CR.sub.1 .dbd.CR.sub.1 --CR.sub.1 .dbd.CR.sub.1 groups on adjacent carbons; X is S, O, or NR.sub.5 ; n is 1 or 2; R.sub.1 and R.sub.2 independently are H, lower alkyl or fluoroalkyl; R.sub.3 is hydrogen, lower alkyl, Cl or Br; R.sub.4 is lower alkyl, fluoroalkyl or halogen; R.sub.5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.13 O, --COR.sub.7, CR.sub.7 (OR.sub.12).sub.2, CR.sub.7 OR.sub.13 O, or tri-lower alkylsilyl, where R.sub.7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R.sub.8 is an alkyl group of 1 to 10 carbons, a cycloalkyl group of 5 to 10 carbons or trimethylsilylalkyl where the alkyl group has 1 to 10 carbons, or R.sub.8 is phenyl or lower alkylphenyl, R.sub.9 and R.sub.10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R.sub.11 is lower alkyl, phenyl or lower alkylphenyl, R.sub.12 is lower alkyl, and R.sub.13 is divalent alkyl radical of 2-5 carbons, have retinoid like biological activity.

    摘要翻译: 式1的化合物其中Z选自由式2和式3所示的基团组成的组。式3 Y是3至8个碳的环烷基或环烯基,任选地 被一个或两个R 4基取代,或Y选自苯基,吡啶基,噻吩基,呋喃基,吡咯基,哒嗪基,嘧啶基,吡嗪基,噻唑基,恶唑基和咪唑基,所述基团任选被一个或两个R 4基团取代,二价 Y基团被相邻碳上的Z和-CR1 = CR1-CR1 = CR1基团取代; X是S,O或NR5; n为1或2; R1和R2独立地为H,低级烷基或氟代烷基; R3是氢,低级烷基,Cl或Br; R4是低级烷基,氟烷基或卤素; R 5是H或低级烷基,B是氢,COOH或其药学上可接受的盐,COOR8,CONR9R10,-CH2OH,CH2OR11,CH2OCOR11,CHO,CH(OR12)2,CHOR13O,-COR7,CR7(OR12) CR 7OR 13 O或三低级烷基甲硅烷基,其中R 7为含有1至5个碳的烷基,环烷基或烯基,R 8为碳原子数1至10的烷基,碳原子数为5至10的环烷基或烷基具有的三甲基甲硅烷基烷基 1至10个碳,或R8为苯基或低级烷基苯基,R9和R10独立地为氢,1-10个碳原子的烷基或5-10个碳原子的环烷基,或苯基或低级烷基苯基,R11为低级烷基, 苯基或低级烷基苯基,R12为低级烷基,R13为2-5个碳原子的二价烷基,具有类视黄醇类生物活性。