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    Phosphoramidate derivatives of nucleoside compounds for use in the treatment of cancer
    21.
    发明申请
    Phosphoramidate derivatives of nucleoside compounds for use in the treatment of cancer 有权
    用于治疗癌症的核苷化合物的氨基磷酸衍生物

    公开(公告)号：US20090215715A1

    公开(公告)日：2009-08-27

    申请号：US11886931

    申请日：2006-03-16

    申请人： Christopher McGuigan ,  Kenneth Mills ,  Costantino Congiatu

    发明人： Christopher McGuigan ,  Kenneth Mills ,  Costantino Congiatu

    IPC分类号： A61K31/7076 ,  C07H19/16 ,  A61P35/00

    CPC分类号： C07H19/20

    摘要： Phosphoramidate derivatives of nucleoside compounds such as cladribine, isocladribine, fludaribine and clofarabine have enhanced therapeutic potency in homo sapiens, in particular, enhanced potency with respect to a cancer such as leukaemia. Suitably the phosphoramidate is substituted at the P atom by Ar—O, where Ar is aryl or heteroaryl, either of which may be optionally substituted. Formula (I).

    摘要翻译： 核苷化合物如克拉屈滨，异克立哌啶，氟达拉滨和氯法拉滨的氨基磷酸衍生物具有增强的智力治疗效力，特别是增强白血病等癌症的效力。 适当地，氨基磷酸酯在P原子被Ar-O取代，其中Ar是芳基或杂芳基，其中任一个可以是任选取代的。 式（I）。

    PHOSPHORAMIDITE DERIVATIVES OF GEMCITABINE FOR USE IN THE TREATMENT CANCER
    22.
    发明申请
    PHOSPHORAMIDITE DERIVATIVES OF GEMCITABINE FOR USE IN THE TREATMENT CANCER 有权
    化疗药物用于治疗癌症的磷酰胺衍生物

    公开(公告)号：US20130252918A1

    公开(公告)日：2013-09-26

    申请号：US13877673

    申请日：2011-10-05

    申请人： Christopher McGuigan

    发明人： Christopher McGuigan

    IPC分类号： C07H19/10

    CPC分类号： C07H19/10

    摘要： Phosphorodiamidate derivatives of e.g. gemcitabine are provided for use in treating cancer. In one embodiment, the two amidate motifs each comprises NR′R″ where R′ is H and R″ is CR5R6CO2R7, where R6 is H, R5 is the side chain, including H and C1, of a naturally occurring alpha amino acid, and R7 is branched or unbranched, substituted or unsubstituted, acyclic or cyclic alkyl, including t-butyl-CH2-, benzyl and C3 to C6 cycloalkyl. Formula (I).

    摘要翻译： 磷酸二亚胺酯衍生物。 提供吉西他滨用于治疗癌症。 在一个实施方案中，两个酰氨基基序各自包含NR'R“，其中R'是H，R”是CR 5 R 6 CO 2 R 7，其中R 6是H，R 5是天然存在的α氨基酸的侧链，包括H和C1 并且R 7是支链或非支链，取代或未取代的无环或环状烷基，包括叔丁基-CH 2 - ，苄基和C 3至C 6环烷基。 式（I）。

    Compounds useful as A3 adenosine receptor agonists
    24.
    发明授权
    Compounds useful as A3 adenosine receptor agonists 失效

    公开(公告)号：US07414036B2

    公开(公告)日：2008-08-19

    申请号：US10899625

    申请日：2004-07-26

    申请人： Luis Garcia Sevillano ,  Christopher McGuigan ,  Robin Havard Davies

    发明人： Luis Garcia Sevillano ,  Christopher McGuigan ,  Robin Havard Davies

    IPC分类号： A61K31/70 ,  C07H19/16 ,  C07H19/167

    CPC分类号： C07H19/16 ,  A61K31/4745 ,  A61K31/52 ,  A61K31/7076

    摘要： Adenosine analogue-type A3 receptor agonists having the formula wherein D is N or CH; E is O; X1 is a group of the formula —CR20R2 1-CYCLE, where R20 and R21 are the same or different and are H, F or CH3; CYCLE is where G is N, CH, CF, CCH3 or CCF3, M is H, Y is —O— or N═, and Z is —N═ when Y is O, or is O when Y is —N═; R5 is H, CH3, I, Br, Cl, CF3, OH or NH2; and R8 is —NR9R10, —CHR9R10 or —N═CR9R10, where R9 and R10 are the same and are C1-C4 alkyl, C1-C4 alkenyl or C1-C4 alkoxyalkyl X2 is mono-N— or di-N,N—(C1-C4)alkylaminocarbonyl, mono-N—or di-N,N—(C3-C5)cycloalkyl-aminocarbonyl or N-(C1-C4)alkyl-N-(C3-C5)cycloalkylamino-carbonyl; X3 is OH or NH2; X4 is OH; X5 is H , halogen, (C1-C10)alkyl , (C2-C10)alkenyl , (C2-C10)alkynyl , or either of the latter two groups where terminally substituted by an aryl or heteroaryl group and, when having a terminal methyl group, optionally further terminally substituted by hydroxyl. The compounds may be used alone or with a pharmaceutically acceptable carrier or diluent to stimulate adenosine A3 receptors.

    Chemical compounds
    25.
    发明申请
    Chemical compounds 有权
    化合物

    公开(公告)号：US20060142238A1

    公开(公告)日：2006-06-29

    申请号：US10560887

    申请日：2004-07-20

    申请人： Christopher McGuigan

    发明人： Christopher McGuigan

    IPC分类号： A61K31/7072 ,  C07H19/04 ,  A61K31/675 ,  C07F9/6512

    CPC分类号： C07H19/10

    摘要： Phosphoramidate derivatives of nucleotides and their use in the treatment of cancer are described. The base moieties of, for example, each of deoxyuridine, cytarabine, gemcitabine and citidine may be substituted at the 5-position. The phosphoramidate moiety has attached to the P atom an aryl-O moiety and an α-amino acid moiety. The a-amino acid moiety may correspond to or be derived from either a naturally occurring or a non-naturally occurring amino acid.

    摘要翻译： 描述了核苷酸的氨基磷酸衍生物及其在治疗癌症中的用途。 例如，脱氧尿苷，阿糖胞苷，吉西他滨和西酞胺中的每一个的碱基部分可以在5-位被取代。 氨基磷酸酯部分已经与P原子连接了芳基-O部分和α-氨基酸部分。 α-氨基酸部分可以对应于或衍生自天然存在的或非天然存在的氨基酸。

    NUCLEOSIDE ARYL PHOSPHORAMIDATES AND THEIR USE AS ANTI-VIRAL AGENTS FOR THE TREATMENT OF HEPATITUS C VIRUS
    26.
    发明申请
    NUCLEOSIDE ARYL PHOSPHORAMIDATES AND THEIR USE AS ANTI-VIRAL AGENTS FOR THE TREATMENT OF HEPATITUS C VIRUS 失效
    核苷类氨基磷酸酯及其作为治疗乙型肝炎病毒的反病毒剂使用

    公开(公告)号：US20110124592A1

    公开(公告)日：2011-05-26

    申请号：US12516253

    申请日：2007-11-23

    申请人： Christopher McGuigan ,  Plinio Perrone ,  Johan Neyts

    发明人： Christopher McGuigan ,  Plinio Perrone ,  Johan Neyts

    IPC分类号： A61K31/7076 ,  C07H19/20 ,  A61K31/708 ,  C07H1/00 ,  A61P31/14 ,  A61P31/12

    CPC分类号： C07H19/20

    摘要： Phosphoramidate derivatives of nucleoside compounds of formula I derived from bases such as adenine and guanine have enhanced therapeutic potency, in particular, enhanced potency with respect to the prophylaxis or treatment of a viral infection such as hepatitis C virus. The glycoside moiety of the nucleoside compound is suitably substituted at the β-2′ position with methyl and the phosphoramidate group, suitably comprises 1-naphthyl linked by —O— to the P atom.

    摘要翻译： 衍生自腺嘌呤和鸟嘌呤等碱的式I核苷化合物的氨基磷酸衍生物具有增强的治疗效力，特别是在预防或治疗病毒感染如丙型肝炎病毒方面的效力增强。 核苷化合物的糖苷部分在甲基和氨基磷酸酯基的“-2”位适当地被取代，合适地包括由-O-连接到P原子上的1-萘基。

    Phosphoramidate Derivatives
    27.
    发明申请
    Phosphoramidate Derivatives 失效

    公开(公告)号：US20070275910A1

    公开(公告)日：2007-11-29

    申请号：US10586101

    申请日：2005-01-18

    申请人： Christopher McGuigan ,  Antonella Carangio ,  Bruce Caterson ,  Clare Hughes ,  Clare Curtis

    发明人： Christopher McGuigan ,  Antonella Carangio ,  Bruce Caterson ,  Clare Hughes ,  Clare Curtis

    IPC分类号： A61K31/70 ,  A61P19/02 ,  A61P25/28 ,  A61P3/10 ,  A61P35/00 ,  A61P43/00 ,  C07H1/06 ,  C07H11/04

    CPC分类号： C07H11/04 ,  Y02P20/55

    摘要： The present invention provides a phosphoramidate compound comprising the structure (I) Formula (I) wherein: X comprises a monosaccharide group comprising the structure (II) or (III), 8 Formula (II), (III) B and B are independently selected from the group consisting of —O—, —CH2— and a bond, preferably —O—; R1 is selected from the group consisting of —H, protecting groups and monovalent hydrocarbon radicals; R2 and R3 are independently selected from the group consisting of —H and monovalent hydrocarbon radicals, or R2 and R3 together form an alkylene or heteroalkylene chain so as to provide, together with the C atom to which they are attached, a cyclic system; R4 is selected from the group consisting of —H and monovalent hydrocarbon radicals; R5-R12 are independently selected from the group consisting of —H, —OH, N3, halogen, —SH, —OR13, —SR13′, NHR14, —NR142 and group Formula (I) wherein B″ is selected from the group consisting of —O—, —CH2— and a bond, preferably —O—; R1-R4 are independently selected and are as defined above, wherein R13 and R13′ are independently selected from the group consisting of —H, monovalent hydrocarbon radicals, protecting groups and —C(O)R15, and wherein R14 is selected from the group consisting of —H, monovalent hydrocarbon radicals, protecting groups and —C(O)R15, wherein R15 is selected from the group consisting of —H and monovalent hydrocarbon radicals; or a pharmaceutically acceptable derivative or metabolite of a compound of formula (I). The present invention also provides processes for the production of (I) and uses thereof.

    Phosphoramidite derivatives of gemcitabine for use in the treatment of cancer
    29.
    发明授权
    Phosphoramidite derivatives of gemcitabine for use in the treatment of cancer 有权
    吉西他滨的亚磷酰胺衍生物用于治疗癌症

    公开(公告)号：US09321798B2

    公开(公告)日：2016-04-26

    申请号：US13877673

    申请日：2011-10-05

    申请人： Christopher McGuigan

    发明人： Christopher McGuigan

    IPC分类号： A01N43/04 ,  A61K31/70 ,  C07H19/04 ,  C07H19/12 ,  C07H19/10

    CPC分类号： C07H19/10

    摘要： Phosphorodiamidate derivatives of e.g. gemcitabine are provided for use in treating cancer. In one embodiment, the two amidate motifs each comprises NR′R″ where R′ is H and R″ is CR5R6CO2R7, where R6 is H, R5 is the side chain, including H and C1, of a naturally occurring alpha amino acid, and R7 is branched or unbranched, substituted or unsubstituted, acyclic or cyclic alkyl, including t-butyl-CH2-, benzyl and C3 to C6 cycloalkyl. Formula (I).

    摘要翻译： 磷酸二亚胺酯衍生物。 提供吉西他滨用于治疗癌症。 在一个实施方案中，两个酰氨基基序各自包含NR'R“，其中R'是H，R”是CR 5 R 6 CO 2 R 7，其中R 6是H，R 5是天然存在的α氨基酸的侧链，包括H和C 1， R 7是支链或非支链，取代或未取代的无环或环状烷基，包括叔丁基-CH 2 - ，苄基和C 3至C 6环烷基。 式（I）。