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    Enzyme inhibitors
    2.
    发明授权
    Enzyme inhibitors 失效
    酶抑制剂

    公开(公告)号：US5889056A

    公开(公告)日：1999-03-30

    申请号：US750679

    申请日：1996-12-27

    申请人： Harold Francis Hodson ,  Richard Michael John Palmer ,  David Alan Sawyer ,  Richard Graham Knowles ,  Karl Witold Franzmann ,  Martin James Drysdale ,  Patricia Ifeyinwa Davies ,  Helen Alice Rebecca Clark ,  Barry George Shearer ,  Steven Smith

    发明人： Harold Francis Hodson ,  Richard Michael John Palmer ,  David Alan Sawyer ,  Richard Graham Knowles ,  Karl Witold Franzmann ,  Martin James Drysdale ,  Patricia Ifeyinwa Davies ,  Helen Alice Rebecca Clark ,  Barry George Shearer ,  Steven Smith

    IPC分类号： A61K31/00 ,  A61K20060101 ,  A61K31/195 ,  A61K31/198 ,  A61P5/00 ,  A61P9/00 ,  A61P43/00 ,  C07C20060101 ,  C07C257/14 ,  C07C315/02 ,  C07C317/02 ,  C07C317/48 ,  C07C317/50 ,  C07C323/60 ,  C07C327/00 ,  C07C327/58

    CPC分类号： C07C323/60 ,  C07C317/48 ,  Y02P20/55

    摘要： A compound of formula (I) ##STR1## wherein R.sup.1 is a C.sub.1-6 straight or branched chain alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a C.sub.3-6 cycloalkyl group or a C.sub.3-6 cycloalkylC.sub.1-6 alkyl group, each optionally substituted by one to three groups independently selected from: --CN; --NO.sub.2 ; a group --COR.sup.2 wherein R.sup.2 is hydrogen, C.sub.1-6 alkyl, --OR.sup.3 wherein R.sup.3 is hydrogen or C.sub.1-6 alkyl or NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently selected from hydrogen or C.sub.1-6 alkyl; a group --S(O).sub.m R.sup.6 wherein m is 0, 1 or 2, R.sup.6 is hydrogen, C.sub.1-6 alkyl, hydroxy or NR.sup.7 R.sup.8 wherein R.sup.7 and R.sup.8 are independently hydrogen or C.sub.1-6 alkyl; a group PO(OR.sup.9).sub.2 wherein R.sup.9 is hydrogen or C.sub.1-6 alkyl; a group NR.sup.10 R.sup.11 wherein R.sup.10 and R.sup.11 are independently selected from hydrogen, C.sub.1-6 alkyl, --COR.sup.12 wherein R.sup.12 is hydrogen or C.sub.1-6 alkyl, or --S(O).sub.m' R.sup.13 wherein m' is 0, 1 or 2 and R.sup.13 is hydrogen or C.sub.1-6 alkyl; halo; or a group --OR.sup.14 wherein R.sup.14 is hydrogen, C.sub.1-6 alkyl optionally substituted by one to three halo atoms, C.sub.6-10 aryl or --COR.sup.15 wherein R.sup.15 is hydrogen or C.sub.1-6 alkyl; p is 2 or 3, q is 1 or 2 and n is 0 or 1 and all salts, esters, amides and physiologically acceptable prodrugs thereof; pharmaceutical uses and formulations therefor; and processes for their preparation are disclosed.

    摘要翻译： PCT No.PCT / GB95 / 01378 Sec。 371日期1996年12月27日第 102（e）日期1996年12月27日PCT提交1995年6月14日PCT公布。 公开号WO95 / 34534 日期：1995年12月21日一种式（I）化合物其中R 1为C 1-6直链或支链烷基，C 2-6烯基，C 2-6炔基，C 3-6环烷基 或C 3-6环烷基C 1-6烷基，各自任选被一至三个独立地选自：-CN; -NO2; 基团-COR 2，其中R 2是氢，C 1-6烷基，-OR 3，其中R 3是氢或C 1-6烷基或NR 4 R 5，其中R 4和R 5独立地选自氢或C 1-6烷基; 基团-S（O）m R 6，其中m为0,1或2，R 6为氢，C 1-6烷基，羟基或NR 7 R 8，其中R 7和R 8独立地为氢或C 1-6烷基; 基团PO（OR 9）2，其中R 9是氢或C 1-6烷基; 基团NR10R11，其中R10和R11独立地选自氢，C1-6烷基，-COR12，其中R12是氢或C1-6烷基或-S（O）m'R13，其中m'是0,1或2，R13 是氢或C 1-6烷基; 光环; 或-OR 14，其中R 14是氢，任选被一至三个卤素原子取代的C 1-6烷基，C 6-10芳基或-COR 15，其中R 15是氢或C 1-6烷基; p为2或3，q为1或2，n为0或1，所有的盐，酯，酰胺和其生理上可接受的前药; 药用及其制剂; 并公开了其制备方法。

    2-oxy-benzoxazinone derivatives for the treatment of obesity
    6.
    发明授权
    2-oxy-benzoxazinone derivatives for the treatment of obesity 有权
    2-氧基 - 苯并嗪酮衍生物用于治疗肥胖症

    公开(公告)号：US08877750B2

    公开(公告)日：2014-11-04

    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： A61K31/535 ,  C07D265/26 ,  C07C271/28

    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。

    Thieno-(1,3)-oxazin-4-ones with lipase inhibiting activity
    7.
    发明授权
    Thieno-(1,3)-oxazin-4-ones with lipase inhibiting activity 失效
    具有脂肪酶抑制活性的噻吩并（1,3）恶嗪-4-酮

    公开(公告)号：US07407954B2

    公开(公告)日：2008-08-05

    申请号：US10488045

    申请日：2002-08-23

    申请人： Harold Francis Hodson ,  Christopher Robert Dunk ,  Richard Michael John Palmer ,  Dale Robert Mitchell ,  Véronique Birault ,  Russell George Hunt

    发明人： Harold Francis Hodson ,  Christopher Robert Dunk ,  Richard Michael John Palmer ,  Dale Robert Mitchell ,  Véronique Birault ,  Russell George Hunt

    IPC分类号： C07D498/04 ,  A61K31/538

    CPC分类号： C07D498/04 ,  C07D498/14

    摘要： The use of a compound comprising formula (I), or a salt, ester, amide or prodrug thereof in the treatment of obesity and related disorders. 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 an optionally substituted thienyl moiety, Y is O, S, or NR2, 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 and R2 is hydrogen or a group as defined for R1.

    摘要翻译： 包含式（I）化合物或其盐，酯，酰胺或前药的化合物在治疗肥胖症和相关病症中的用途。 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是任选取代的噻吩基部分，Y是O，S或NR 2，R 1是支链或非支链烷基（任选地被 一个或多个氧原子），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，还原的杂芳基烷基或任何前述基团的取代衍生物，R H 2是氢或R 1定义的基团。

    2-thio-4h-3, 1-benzoxazin-4-one derivatives for use as enzyme inhibitors
    8.
    发明授权
    2-thio-4h-3, 1-benzoxazin-4-one derivatives for use as enzyme inhibitors 失效
    2-硫代-4h-3,1-苯并恶嗪-4-酮衍生物，用作酶抑制剂

    公开(公告)号：US06916808B2

    公开(公告)日：2005-07-12

    申请号：US10181868

    申请日：2001-01-17

    申请人： Robert Downham ,  Richard Michael John Palmer ,  Harold Francis Hodson ,  Christopher Robert Dunk

    发明人： Robert Downham ,  Richard Michael John Palmer ,  Harold Francis Hodson ,  Christopher Robert Dunk

    IPC分类号： A23L1/30 ,  A23L3/3544 ,  A61K8/49 ,  A61K31/536 ,  A61K31/5365 ,  A61P1/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P9/12 ,  A61P43/00 ,  C07D265/24 ,  C07D498/04 ,  C07D403/14 ,  C07D405/12

    CPC分类号： C07D265/24 ,  A61K31/536 ,  A61K31/5365

    摘要： The use of a compound, comprising formula (I) or a salt, ester, amide of 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 an optionally substituted 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： 使用包含式（I）的化合物或其前体药物的盐，酯，酰胺在抑制其优选作用模式是催化酯官能团水解的酶的酶。 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是任选取代的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
    9.
    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：US07776853B2

    公开(公告)日：2010-08-17

    申请号：US10306375

    申请日：2002-11-27

    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： A61K31/535

    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 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; 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。

    2-OXY-BENZOXAZINONE DERIVATIVES FOR THE TREATMENT OF OBESITY
    10.
    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。