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    2-Oxy-Benzoxazinone Derivatives for the Treatment of Obesity
    12.
    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
    13.
    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
    14.
    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：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。

    2-Oxy-benzoxazinone derivatives for the treatment of obesity
    15.
    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：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。

    Amidino derivatives and their use as nitric oxide synthase inhibitors
    16.
    发明授权
    Amidino derivatives and their use as nitric oxide synthase inhibitors 失效
    脒衍生物及其作为一氧化氮合酶抑制剂的用途

    公开(公告)号：US5863931A

    公开(公告)日：1999-01-26

    申请号：US256032

    申请日：1994-06-22

    申请人： Richard Mansfield Beams ,  Harold Francis Hodson ,  Richard Michael John Palmer

    发明人： Richard Mansfield Beams ,  Harold Francis Hodson ,  Richard Michael John Palmer

    IPC分类号： C12N9/99 ,  A61K31/155 ,  A61K31/195 ,  A61K31/198 ,  A61K31/275 ,  A61P9/00 ,  A61P19/02 ,  A61P37/06 ,  A61P43/00 ,  C07C257/14 ,  C07C257/16 ,  C07C315/04 ,  C07C317/50 ,  C07C319/20 ,  C07C323/58 ,  C07C323/59 ,  A61K31/44

    CPC分类号： C07C323/58 ,  A61K31/195 ,  C07C257/14 ,  C07C2101/02

    摘要： Amidino derivatives of formula (I) and salts, and pharmaceutically acceptable esters and amides thereof, in which: 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; Q is an alkylene, alkenylene or alkynylene group having 3 to 6 carbon atoms and which may optionally be substituted by one or more C.sub.1-3 alkyl groups; a group of formula --(CH.sub.2).sub.p X(CH.sub.2).sub.q -- where p is 2 or 3, q is 1 or 2 and X is S(O).sub.x where x is 0, 1 or 2, O or NR.sup.2 where R.sup.2 is H or C.sub.1-6 alkyl; or a group of formula --(CH.sub.2).sub.r A(CH.sub.2).sub.s -- where r is 0, 1 or 2, s is 0, 1 or 2 and A is a 3 to 6 membered carbocyclic or heterocyclic ring which may optionally be substituted by one or more suitable substituents such as C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, halo, nitro, cyano, trifluoro C.sub.1-6 alkyl, amino, C.sub.1-6 alkylamino or diC.sub.1-6 alkylamino; and pharmaceutical formulations containing them are described for use in medicine novel compounds of formula (I) and the preparation of such novel compounds are also disclosed.

    摘要翻译： PCT No.PCT / GB92 / 02387第 371日期：1994年6月22日 102（e）日期1994年6月22日PCT提交1992年12月23日PCT公布。 出版物WO93 / 13055 日期：1993年7月8日（一）式（I）的脒基衍生物及其盐及其药学上可接受的酯和酰胺，其中：R1是C1-6直链或支链烷基，C2-6烯基 基团，C 2-6炔基，C 3-6环烷基或C 3-6环烷基C 1-6烷基; Q是具有3至6个碳原子的亚烷基，亚烯基或亚炔基，其可以任选地被一个或多个C 1-3烷基取代; 式（ - ）（CH2）pX（CH2）q-，其中p是2或3，q是1或2，X是S（O）x，其中x是0,1或2，O或NR2，其中R2是H 或C 1-6烷基; 或式 - （CH 2）r A（CH 2）s - 的基团，其中r为0,1或2，s为0,1或2，A为可任选被一个或多个取代基的3至6元碳环或杂环 或更合适的取代基，例如C 1-6烷基，C 1-6烷氧基，羟基，卤素，硝基，氰基，三氟C 1-6烷基，氨基，C 1-6烷基氨基或二C 1-6烷基氨基; 和含有它们的药物制剂被描述用于医药新型式（I）化合物，并且还公开了这些新化合物的制备。

    Antiallergic cyclic sulphur compounds
    17.
    发明授权
    Antiallergic cyclic sulphur compounds 失效
    抗过敏环状硫化合物

    公开(公告)号：US4103015A

    公开(公告)日：1978-07-25

    申请号：US586427

    申请日：1975-06-12

    申请人： Harold Francis Hodson ,  John Frederick Batchelor

    发明人： Harold Francis Hodson ,  John Frederick Batchelor

    IPC分类号： C07C317/14 ,  C07C317/44 ,  C07C321/26 ,  C07C323/62 ,  C07D257/04 ,  C07D335/16 ,  A61K31/41

    CPC分类号： C07D257/04 ,  C07C317/14 ,  C07C317/44 ,  C07C321/26 ,  C07C323/62 ,  C07D335/16

    摘要： Certain tricyclic thioxanthone-10,10-dioxide compounds each of which is substituted in the 1-,2-,3- or 4-position by a carboxyl or (5-tetrazolyl) group and each of which is optionally substituted in the 5-,6-,7- or 8-position by a second carboxyl or (5-tetrazolyl) group or a substituent selected from cyano, halogen, nitro, alkyl, alkoxy, acyl, amino, acylamino, thioalkyl, alkylsulphinyl and alkylsulphonyl, as well as salts, and optionally substituted esters and amides of the carboxyl substituted compounds and alkyl derivatives of the tetrazolyl substituted compounds, are useful for the relief or prophylaxis of allergic conditions.

    摘要翻译： 某些三环噻吨酮-10,10-二氧化物化合物，其各自在1-，2-，3-或4-位被羧基或（5-四唑基）基团取代，并且其各自任选在5- ，6-或7-位，由第二个羧基或（5-四唑基）基团或选自氰基，卤素，硝基，烷基，烷氧基，酰基，氨基，酰氨基，硫代烷基，烷基亚磺酰基和烷基磺酰基的取代基 作为盐和任选取代的羧基取代的化合物的酯和酰胺和四唑基取代的化合物的烷基衍生物可用于缓解或预防过敏性疾病。

    Ng-monomethyl-l-arginine hydrochloride derivatives and their use in the treatment of septic shock
    18.
    发明授权
    Ng-monomethyl-l-arginine hydrochloride derivatives and their use in the treatment of septic shock 失效
    单氢甲基-1-精氨酸盐酸盐衍生物及其在治疗败血性休克中的应用

    公开(公告)号：US5883130A

    公开(公告)日：1999-03-16

    申请号：US55786

    申请日：1998-04-07

    申请人： Harold Francis Hodson

    发明人： Harold Francis Hodson

    IPC分类号： C07C279/14 ,  A01N37/10 ,  C07C241/00

    CPC分类号： C07C279/14

    摘要： Crystalline N.sup.G -monomethyl-L-arginine hydrochloride is disclosed. At least three distinguishable isomorphic forms are present. The solid salt can be made by dissolving N.sup.G -monomethyl-L-arginine in hydrochloric acid and crystallising out N.sup.G -monomethyl-L-arginine hydrochloride. The crystallising step requires several months at low temperature. However, the process can be facilitated by seeding with crystals of N.sup.G -monomethyl-L-arginine hydrochloride. Alternatively, crystalline N.sup.G -monomethyl-L-arginine hydrochloride can be prepared by dissolving a salt of N.sup.G -monomethyl-L-arginine other than the hydrochloride salt with hydrochloric acid and removing the original salt forming ion by crystallising out the hydrochloride salt.

    摘要翻译： 公开了结晶NG-单甲基-L-精氨酸盐酸盐。 存在至少三种可区别的同构形式。 固体盐可以通过将NG-单甲基-L-精氨酸溶解在盐酸中并结晶出NG-单甲基-L-精氨酸盐酸盐。 结晶步骤在低温下需要几个月。 然而，通过用NG-单甲基-L-精氨酸盐酸盐的晶体接种可以促进该方法。 或者，可以通过将除盐酸盐以外的NG-单甲基-L-精氨酸的盐与盐酸溶解并通过使盐酸盐结晶除去原来的形成盐的方法来制备结晶NG-单甲基-L-精氨酸盐酸盐。