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30 条记录 (耗时 0.068 秒)

    2-Oxy-Benzoxazinone Derivatives for the Treatment of Obesity
    23.
    发明申请
    2-Oxy-Benzoxazinone Derivatives for the Treatment of Obesity 有权
    用于治疗肥胖症的2-氧 - 苯并恶嗪酮衍生物

    公开(公告)号：US20080161301A1

    公开(公告)日：2008-07-03

    申请号：US12044318

    申请日：2008-03-07

    申请人： Harold Francis Hodson ,  Robert Downham ,  Timothy John Mitchell ,  Beverley Jane Carr ,  Christopher Robert Dunk ,  Richard Michael John Palmer

    发明人： Harold Francis Hodson ,  Robert Downham ,  Timothy John Mitchell ,  Beverley Jane Carr ,  Christopher Robert Dunk ,  Richard Michael John Palmer

    IPC分类号： A61K31/536 ,  C07D265/14 ,  C12N9/99 ,  A61P3/04

    CPC分类号： C07D265/26 ,  C07C271/28

    摘要： The use of a compound comprising formula (I): or a salt, ester, amide or prodrug thereof in the inhibition of an enzyme whose preferred mode of action is to catalyse the hydrolysis of an ester functionality, e.g. in the control and inhibition of unwanted enzymes in products and processes. The compounds are also useful in medicine e.g. in the treatment of obesity and related conditions. The invention also relates to novel compounds within formula (I), to processes for preparing them and pharmaceutical compositions containing them.In formula (I) A is a 6-membered aromatic or heteroaromatic ring; andR1 is a branched or unbranched alkyl (optionally interrupted by one or more oxygen atoms), alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced arylalkyl, arylalkenyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, reduced aryl, reduced heteroaryl, reduced heteroarylalkyl or a substituted derivative of any of the foregoing groups.

    摘要翻译： 包含式（I）的化合物或其盐，酯，酰胺或前药在抑制其优选作用模式是催化酯官能团水解的酶的用途，例如， 在产品和过程中控制和抑制不需要的酶。 这些化合物也可用于医学，例如 在治疗肥胖和相关情况。 本发明还涉及式（I）中的新化合物，其制备方法和含有它们的药物组合物。 在式（I）中，A是6元芳族或杂芳族环; 并且R 1是支链或非支链烷基（任选被一个或多个氧原子间隔开），烯基，炔基，环烷基，环烯基，芳基，芳基烷基，还原芳基烷基，芳基烯基，杂芳基，杂芳基烷基，杂芳基烯基， 还原的芳基，还原的杂芳基，还原的杂芳基烷基或任何前述基团的取代的衍生物。

    2-amino-benzoxazinone derivatives for the treatment of obesity
    24.
    发明授权
    2-amino-benzoxazinone derivatives for the treatment of obesity 失效
    2-氨基 - 苯并嗪酮衍生物用于治疗肥胖症

    公开(公告)号：US06656934B2

    公开(公告)日：2003-12-02

    申请号：US09901868

    申请日：2001-07-06

    申请人： Harold Francis Hodson ,  Robert Downham ,  Timothy John Mitchell ,  Beverley Jane Carr ,  Christopher Robert Dunk ,  Richard Michael John Palmer

    发明人： Harold Francis Hodson ,  Robert Downham ,  Timothy John Mitchell ,  Beverley Jane Carr ,  Christopher Robert Dunk ,  Richard Michael John Palmer

    IPC分类号： A61K31536

    CPC分类号： C07D265/26 ,  C07C271/28 ,  C07C271/58

    摘要： The use of a compound comprising formula (I): or a salt, ester, amide or prodrug therof in the inhibition of an enzyme whose preferred mode of action is to catalyse the hydrolysis of an ester functionality, e.g. in the control and inhibition of unwanted enzymes in products and processes. The compounds are also useful in medicine e.g. in the treatment of obesity and related conditions. The invention also relates to novel compounds within formula (I), to processes for preparing them and pharmaceutical compositions containing them. In formula (I) A is a 6-membered aromatic or heteroaromatic ring; and R1 is a branched or unbranched alkyl (optionally interrupted by one or more oxygen atoms), alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced arylalkyl, arylalkenyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, reduced aryl, reduced heteroaryl, reduced heteroarylalkyl or a substituted derivative of any of the foregoing groups.

    摘要翻译： 包含式（I）的化合物或其盐，酯，酰胺或前体药物在抑制其优选作用模式是催化酯官能团水解的酶的用途中的用途，例如， 在产品和过程中控制和抑制不需要的酶。 这些化合物也可用于医学，例如 在治疗肥胖和相关情况。 本发明还涉及式（I）中的新化合物，其制备方法和含有它们的药物组合物。在式（I）中，A是6元芳族或杂芳族环; 烯基，炔基，环烷基，环烯基，芳基，芳基烷基，还原芳基烷基，芳基烯基，杂芳基，杂芳基烷基，杂芳基烯基，还原的芳基，还原的杂芳基， 还原的杂芳基烷基或任何前述基团的取代的衍生物。

    2-OXY-BENZOXAZINONE DERIVATIVES FOR THE TREATMENT OF OBESITY
    29.
    发明申请
    2-OXY-BENZOXAZINONE DERIVATIVES FOR THE TREATMENT OF OBESITY 有权
    用于治疗肥胖症的2-氧基苯并噻嗪酮衍生物

    公开(公告)号：US20110065697A1

    公开(公告)日：2011-03-17

    申请号：US12952972

    申请日：2010-11-23

    申请人： Harold Francis Hodson ,  Robert Downham ,  Timothy John Mitchell ,  Beverley Jane Carr ,  Christopher Robert Dunk ,  Richard Michael John Palmer

    发明人： Harold Francis Hodson ,  Robert Downham ,  Timothy John Mitchell ,  Beverley Jane Carr ,  Christopher Robert Dunk ,  Richard Michael John Palmer

    IPC分类号： A61K31/536 ,  A61P3/04

    CPC分类号： C07D265/26 ,  C07C271/28

    摘要： The use of a compound comprising formula (I): or a salt, ester, amide or prodrug thereof in the inhibition of an enzyme whose preferred mode of action is to catalyse the hydrolysis of an ester functionality, e.g. in the control and inhibition of unwanted enzymes in products and processes. The compounds are also useful in medicine e.g. in the treatment of obesity and related conditions. The invention also relates to novel compounds within formula (I), to processes for preparing them and pharmaceutical compositions containing them.In formula (I) A is a 6-membered aromatic or heteroaromatic ring; and R1 is a branched or unbranched alkyl (optionally interrupted by one or more oxygen atoms), alkenyl, alkynyl, cycloalkyl, cycloalkenyl, aryl, arylalkyl, reduced arylalkyl, arylalkenyl, heteroaryl, heteroarylalkyl, heteroarylalkenyl, reduced aryl, reduced heteroaryl, reduced heteroarylalkyl or a substituted derivative of any of the foregoing groups.

    摘要翻译： 包含式（I）的化合物或其盐，酯，酰胺或前药在抑制其优选作用模式是催化酯官能团水解的酶的用途，例如， 在产品和过程中控制和抑制不需要的酶。 这些化合物也可用于医学，例如 在治疗肥胖和相关情况。 本发明还涉及式（I）中的新化合物，其制备方法和含有它们的药物组合物。 在式（I）中，A是6元芳族或杂芳族环; 烯基，炔基，环烷基，环烯基，芳基，芳基烷基，还原芳基烷基，芳基烯基，杂芳基，杂芳基烷基，杂芳基烯基，还原芳基，还原杂芳基，还原的杂芳基烷基（可以被一个或多个氧原子间隔的烷基） 或任何上述基团的取代衍生物。

    Aryl-Alkylamines And Heteroaryl-Alkylamines As Protein Kinase Inhibitors
    30.
    发明申请
    Aryl-Alkylamines And Heteroaryl-Alkylamines As Protein Kinase Inhibitors 审中-公开
    芳基烷基胺和杂芳基 - 烷基胺作为蛋白激酶抑制剂

    公开(公告)号：US20100210617A1

    公开(公告)日：2010-08-19

    申请号：US11993835

    申请日：2006-06-21

    申请人： Steven John Woodhead ,  Robert Downham ,  Christopher Hamlett ,  Steven Howard ,  Hannah Fiona Sore ,  Marinus Leendert Verdonk ,  David Winter Walker ,  Richard William Arthur Luke

    发明人： Steven John Woodhead ,  Robert Downham ,  Christopher Hamlett ,  Steven Howard ,  Hannah Fiona Sore ,  Marinus Leendert Verdonk ,  David Winter Walker ,  Richard William Arthur Luke

    IPC分类号： A61K31/4155 ,  C07D231/12 ,  C07D403/10 ,  C07D413/10 ,  C07D413/14 ,  C07D401/10 ,  A61K31/415 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/4178 ,  A61K31/4439 ,  A61K31/506 ,  A61K31/497 ,  A61K31/454 ,  A61P35/00

    CPC分类号： C07D231/12

    摘要： The invention provides a compound of the formula (II): or a salt, solvate, tautomer or N-oxide thereof; wherein n is 0 or 1; one of Y1 and Y2 is CH and the other is selected from CH, CR8 and N; q is 0, 1 or 2 provided that q is 0 or 1 when Y1 or Y2 is CR8; R1 aryl or heteroaryl group of 5 to 10 ring members; R2a and R3a each are hydrogen, C1-4 hydrocarbyl or C1-4 acyl wherein the hydrocarbyl and acyl moieties are optionally substituted by fluorine, hydroxy, amino, methylamino, dimethylamino or methoxy; or NR2aR3a forms an imidazole group or a saturated monocyclic 4-7 membered heterocyclic group optionally containing a second heteroatom ring member selected from O and N; R18 is hydrogen or methyl; R19 is hydrogen or methyl; R24 is hydrogen or R24, R2a and the intervening nitrogen atom and carbon atoms together form an azetidine, pyrrolidine or piperidine ring; R25 is hydrogen or a C1-4 alkyl group wherein the C1-4 alkyl group is optionally substituted by hydroxy or amino provided that there are at least two carbon atoms between the hydroxy or amino group and the oxygen atom to which R25 is attached; and R4 and R5 each are hydrogen or a substituent as defined in the claims

    摘要翻译： 本发明提供式（II）化合物或其盐，溶剂合物，互变异构体或N-氧化物; 其中n为0或1; Y1和Y2之一是CH，另一个选自CH，CR8和N; q为0,1或2，条件是当Y1或Y2为CR8时q为0或1; R 10芳环或5至10个环成员的杂芳基; R2a和R3a各自为氢，C1-4烃基或C1-4酰基，其中烃基和酰基部分任选被氟，羟基，氨基，甲基氨基，二甲基氨基或甲氧基取代; 或NR2aR3a形成任选含有选自O和N的第二杂原子环成员的咪唑基或饱和单环4-7元杂环基; R18是氢或甲基; R 19是氢或甲基; R 24是氢或R 24，R 2a，并且插入的氮原子和碳原子一起形成氮杂环丁烷，吡咯烷或哌啶环; R 25是氢或C 1-4烷基，其中C 1-4烷基任选被羟基或氨基取代，条件是羟基或氨基与R 25所连接的氧原子之间至少有两个碳原子; 且R 4和R 5各自为氢或如权利要求中所定义的取代基