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    DUTPASE INHIBITORS
    1.
    发明申请
    DUTPASE INHIBITORS 失效
    DUTPASE抑制剂

    公开(公告)号：US20110021459A1

    公开(公告)日：2011-01-27

    申请号：US12849765

    申请日：2010-08-03

    申请人： Ian GILBERT ,  Corinne Nguyen ,  Gian Filippo Ruda ,  Alessandro Schipani ,  Ganasan Kasinathan ,  Nils-Gunnar Johansson ,  Dolores Gonzales Pacanowska

    发明人： Ian GILBERT ,  Corinne Nguyen ,  Gian Filippo Ruda ,  Alessandro Schipani ,  Ganasan Kasinathan ,  Nils-Gunnar Johansson ,  Dolores Gonzales Pacanowska

    IPC分类号： A61K31/695 ,  C07D239/54 ,  C07F7/10 ,  A61K31/513 ,  A61P33/06

    CPC分类号： A61K31/505 ,  A61K31/506 ,  A61K31/7072 ,  C07D239/54 ,  C07D405/06 ,  C07F7/1804 ,  Y02A50/409 ,  Y02A50/411

    摘要： Deoxyuridine derivatives of the formula where R1 is H or various substituents; D is —NHCO—, —CONH—, —O—, —C(═O)—, —CH═CH, —C≡C—, —NR5—; R4 is hydrogen or various substituents; R5 is H, C1-C4 alkyl, C1-C4 alkanoyl; E is Si or C; R6, R7 and R8 are independently selected from C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl or a stable monocyclic, bicyclic or tricyclic ring system; G is —O—, —S—, —CHR10—, —C(═O)—; J is —CH2—, or when G is CHR10 may also be —O— or —NH—; R10 is H, F, —CH3, —CH2NH2, —CH2OH, —OH; R11 is H, F, —CH3, —CH2NH2, —CH2OH, CH(OH)CH3, CH(NH2)CH3; or R10 and R11 together define an olefinic bond, or together form a —CH2-group, thereby defining a cis or trans cyclopropyl group; have utility in the prophylaxis or treatment of protozoal diseases such as malaria.

    摘要翻译： 其中R 1为H或各种取代基的下式的脱氧尿苷衍生物; D是-NHCO-，-CONH - ， - O - ， - C（= O） - ， - CH = CH，-C≡C-，-NR5-; R4是氢或各种取代基; R5是H，C1-C4烷基，C1-C4烷酰基; E为Si或C; R 6，R 7和R 8独立地选自C 1 -C 8烷基，C 2 -C 8烯基，C 2 -C 8炔基或稳定的单环，双环或三环系; G是-O - ， - S - ， - CHR 10 - ， - C（= O） - ; J是-CH 2 - ，或者当G是CHR 10时也可以是-O-或-NH-; R 10是H，F，-CH 3，-CH 2 NH 2，-CH 2 OH，-OH; R 11是H，F，-CH 3，-CH 2 NH 2，-CH 2 OH，CH（OH）CH 3，CH（NH 2）CH 3; 或R 10和R 11一起界定烯键，或一起形成-CH 2 - 基团，由此限定顺式或反式环丙基; 可用于预防或治疗诸如疟疾的原生动物疾病。

    DUTPase inhibitors
    8.
    发明授权
    DUTPase inhibitors 失效
    DUTPase抑制剂

    公开(公告)号：US07795270B2

    公开(公告)日：2010-09-14

    申请号：US10585283

    申请日：2005-01-06

    申请人： Ian Gilbert ,  Corinne Nguyen ,  Gian Filippo Ruda ,  Alessandro Schipani ,  Ganasan Kasinathan ,  Nils-Gunnar Johansson ,  Dolores Gonzalez Pacanowska

    发明人： Ian Gilbert ,  Corinne Nguyen ,  Gian Filippo Ruda ,  Alessandro Schipani ,  Ganasan Kasinathan ,  Nils-Gunnar Johansson ,  Dolores Gonzalez Pacanowska

    IPC分类号： A61K31/505 ,  C07D239/54

    CPC分类号： A61K31/505 ,  A61K31/506 ,  A61K31/7072 ,  C07D239/54 ,  C07D405/06 ,  C07F7/1804 ,  Y02A50/409 ,  Y02A50/411

    摘要： Deoxyuridine derivatives of the formula (I) where R1 is H or various substituents; D is —NHCO—, —CONH—, -0-, —C(═O)—, —CH═CH, —C≡C—, —NR5—; R4 is hydrogen or various substituents; R5 is H, C1-C4 alkyl, C1-C4 alkanoyl; E is Si or C; R6, R7 and R8 are independently selected from C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl or a stable monocyclic, bicyclic or tricyclic ring system; G is —O—, —S—, —CHR10—, —C(═O)—; J is —CH2—, or when G is CHR10 may also be —O— or —NH—; R10 is H, F, —CH3, —CH2NH2, —CH2OH; —OHR11 is H, F, —CH3, —CH2NH2, —CH2OH, —CH(OH)CH3, CH(NH3)CH3; or R10 and R11 together define an olefinic bond, or together form a —CH2-group, thereby defining a cis or trans cyclopropyl group; have utility in the prophylaxis or treatment of protozoal diseases such as malaria.

    摘要翻译： 式（I）的脱氧尿苷衍生物，其中R 1为H或各种取代基; D是-NHCO - ， - CONH - ， - O - ， - C（= O） - ， - CH = CH，-C≡C-，-NR5-; R4是氢或各种取代基; R5是H，C1-C4烷基，C1-C4烷酰基; E为Si或C; R 6，R 7和R 8独立地选自C 1 -C 8烷基，C 2 -C 8烯基，C 2 -C 8炔基或稳定的单环，双环或三环系; G是-O - ， - S - ， - CHR 10 - ， - C（= O） - ; J是-CH 2 - ，或者当G是CHR 10时也可以是-O-或-NH-; R 10是H，F，-CH 3，-CH 2 NH 2，-CH 2 OH; -OH R 11是H，F，-CH 3，-CH 2 NH 2，-CH 2 OH，-CH（OH）CH 3，CH（NH 3）CH 3; 或R 10和R 11一起界定烯键，或一起形成-CH 2 - 基团，由此限定顺式或反式环丙基; 可用于预防或治疗诸如疟疾的原生动物疾病。

    Dutpase inhibitors
    10.
    发明授权
    Dutpase inhibitors 失效
    Dutpase抑制剂

    公开(公告)号：US08017620B2

    公开(公告)日：2011-09-13

    申请号：US12849765

    申请日：2010-08-03

    申请人： Ian Gilbert ,  Corinne Nguyen ,  Alessandro Schipani ,  Ganasan Kasinathan ,  Nils-Gunnar Johansson ,  Dolores Gonzalez Pacanowska ,  Gian Filippo Ruda

    发明人： Ian Gilbert ,  Corinne Nguyen ,  Alessandro Schipani ,  Ganasan Kasinathan ,  Nils-Gunnar Johansson ,  Dolores Gonzalez Pacanowska ,  Gian Filippo Ruda

    IPC分类号： C07D239/54 ,  A61K31/505

    CPC分类号： A61K31/505 ,  A61K31/506 ,  A61K31/7072 ,  C07D239/54 ,  C07D405/06 ,  C07F7/1804 ,  Y02A50/409 ,  Y02A50/411

    摘要： Deoxyuridine derivatives of the formula where R1 is H or various substituents; D is —NHCO—, —CONH—, —O—, —C(═O)—, —CH═CH, —C≡C—, —NR5—; R4 is hydrogen or various substituents; R5 is H, C1-C4 alkyl, C1-C4 alkanoyl; E is Si or C; R6, R7 and R8 are independently selected from C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl or a stable monocyclic, bicyclic or tricyclic ring system; G is —O—, —S—, —CHR10—, —C(═O)—; J is —CH2—, or when G is CHR10 may also be —O— or —NH—; R10 is H, F, —CH3, —CH2NH2, —CH2OH, —OH; R11 is H, F, —CH3, —CH2NH2, —CH2OH, CH(OH)CH3, CH(NH2)CH3; or R10 and R11 together define an olefinic bond, or together form a —CH2-group, thereby defining a cis or trans cyclopropyl group; have utility in the prophylaxis or treatment of protozoal diseases such as malaria.

    摘要翻译： 其中R 1为H或各种取代基的下式的脱氧尿苷衍生物; D是-NHCO-，-CONH - ， - O - ， - C（= O） - ， - CH = CH，-C≡C-，-NR5-; R4是氢或各种取代基; R5是H，C1-C4烷基，C1-C4烷酰基; E为Si或C; R 6，R 7和R 8独立地选自C 1 -C 8烷基，C 2 -C 8烯基，C 2 -C 8炔基或稳定的单环，双环或三环系; G是-O - ， - S - ， - CHR 10 - ， - C（= O） - ; J是-CH 2 - ，或者当G是CHR 10时也可以是-O-或-NH-; R 10是H，F，-CH 3，-CH 2 NH 2，-CH 2 OH，-OH; R 11是H，F，-CH 3，-CH 2 NH 2，-CH 2 OH，CH（OH）CH 3，CH（NH 2）CH 3; 或R 10和R 11一起界定烯键，或一起形成-CH 2 - 基团，由此限定顺式或反式环丙基; 可用于预防或治疗诸如疟疾的原生动物疾病。