公开(公告)号：US07858617B2

公开(公告)日：2010-12-28

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： A01N43/66 ,  C07D265/12

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; 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。

公开(公告)号：US06624161B2

公开(公告)日：2003-09-23

申请号：US09901887

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： A61K31535

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 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，还原芳基，还原的芳基，还原的芳基 ，还原的杂芳基烷基或任何前述基团的取代衍生物。

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。

公开(公告)号：US20090029978A1

公开(公告)日：2009-01-29

申请号：US12178920

申请日：2008-07-24

申请人： Harold Francis HODSON ,  Christopher Robert DUNK ,  Richard Michael John PALMER ,  Dale Robert MITCHELL ,  Veronique BIRAULT ,  Russell George HUNT

发明人： Harold Francis HODSON ,  Christopher Robert DUNK ,  Richard Michael John PALMER ,  Dale Robert MITCHELL ,  Veronique BIRAULT ,  Russell George HUNT

IPC分类号： A61K31/5365 ,  C07D498/04 ,  A61P3/04 ,  A61P3/10 ,  C12N9/99

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（任选被一个或多个氧原子中断），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的衍生物，并且R 2是氢或如R1所定义的基团。

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。

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。

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

公开(公告)号：US07825113B2

公开(公告)日：2010-11-02

申请号：US10306377

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

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.

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。

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。