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：USRE39576E1

公开(公告)日：2007-04-17

申请号：US10407204

申请日：1995-06-14

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： A61K31/195

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

摘要： A compound of formula (I) wherein R1 is a C1-6 straight or branched chain alkyl group, a C2-6alkenyl group, a C2-6 alkynyl group, a C3-6cycloalkyl group or a C3-6cycloalkylC1-6alkyl group, each optionally substituted by one to three groups independently selected from: —CN; —NO2; a group —COR2 wherein R2 is hydrogen, C1-6 alkyl, —OR3 wherein R3 is hydrogen or C1-6alkyl or NR4R5 wherein R4 and R5 are independently selected from hydrogen or C1-6 alkyl; a group —S(O)mR6 wherein m is 0, 1 or 2, R6 is hydrogen, C1-6 alkyl, hydroxy or NR7R8 wherein R7 and R8 are independently hydrogen or C1-6 alkyl; a group PO(OR9)2 wherein R9 is hydrogen or C1-6 alkyl; a group NR10R11 wherein R10 and R11 are independently selected from hydrogen, C1-6 alkyl, —COR12 wherein R12 is hydrogen or C1-6 alkyl, or —S(O)m′R13 wherein m′ is 0, 1 or 2 and R13 is hydrogen or C1-6 alkyl; halo; or a group —OR14 wherein R14 is hydrogen, C1-6 alkyl optionally substituted by one to three halo atoms, C6-10 aryl or —COR15 wherein R15 is hydrogen or C1-6 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： 式的化合物

公开(公告)号：US06369272B1

公开(公告)日：2002-04-09

申请号：US09341220

申请日：1999-08-24

申请人： Richard Mansfield Beams ,  Martin James Drysdale ,  Karl Witold Franzmann ,  Anthony Joseph Frend ,  Harold Francis Hodson ,  Richard Graham Knowles ,  Daryl David Rees ,  David Alan Sawyer

发明人： Richard Mansfield Beams ,  Martin James Drysdale ,  Karl Witold Franzmann ,  Anthony Joseph Frend ,  Harold Francis Hodson ,  Richard Graham Knowles ,  Daryl David Rees ,  David Alan Sawyer

IPC分类号： A61K31195

CPC分类号： C07C323/58 ,  C07C323/59

摘要： The present invention relates to novel amidino compound of formula (I). to a process for their manufacture, to pharmaceutical compositions containing them, and to their use in therapy, in particular their use as selective inhibitors of inducible nitric oxide synthase.

摘要翻译： 本发明涉及式（I）的新的脒基化合物，其制备方法，含有它们的药物组合物及其在治疗中的用途，特别是其作为诱导型一氧化氮合酶选择性抑制剂的用途。

公开(公告)号：US5874472A

公开(公告)日：1999-02-23

申请号：US569085

申请日：1996-03-18

申请人： Barry George Shearer ,  Karl Witold Franzmann ,  Harold Francis Hodson

发明人： Barry George Shearer ,  Karl Witold Franzmann ,  Harold Francis Hodson

IPC分类号： C07D333/20 ,  A61K31/195 ,  A61K31/198 ,  A61K31/38 ,  A61K31/381 ,  A61K31/425 ,  A61K31/426 ,  A61P9/00 ,  A61P43/00 ,  C07C257/14 ,  C07C279/04 ,  C07C279/18 ,  C07C335/22 ,  C07C335/32 ,  C07D277/20 ,  C07D277/22 ,  C07D277/28 ,  C07D277/42 ,  C07D277/48 ,  C07D277/56 ,  C07D333/24 ,  C07D333/36 ,  C07C233/00 ,  C07C241/00

CPC分类号： C07C279/18 ,  C07C257/14 ,  C07C335/22 ,  C07C335/32 ,  C07D333/24 ,  C07D333/36 ,  C07C2101/02

摘要： Compounds of formula (I) and salts, esters and amides thereof, wherein R.sup.1 is a C.sub.1-6 straight or branched chain alkyl group, a C.sub.3-6 cycloalkyl group, a thiol group optionally substituted by a C.sub.1-6 alkyl group, or an amino group optionally substituted by one or two alkyl or alkenyl groups; R.sup.2 is H, C.sub.1-7 straight or branched chain alkyl, C.sub.3-6 cycloalkyl, C.sub.2-7 alkenyl or benzyl; A is a 5 or 6 membered aromatic 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 di C.sub.1-6 alkylamino; r is 0, 1 or 2; their use in medicine and in particular for conditions requiring inhibition of the NO Synthase enzyme, pharmaceutical formulations and processes for the preparation thereof are disclosed. ##STR1##

摘要翻译： PCT No.PCT / GB94 / 01325 Sec。 371日期：1996年3月18日 102（e）1996年3月18日PCT 1994年6月20日PCT公布。 公开号WO95 / 日期1月5日，式（I）化合物及其盐，酯和酰胺的化合物，其中R1是C1-6直链或支链烷基，C3-6环烷基，任选被C1-6取代的硫醇基 烷基或任选被一个或两个烷基或烯基取代的氨基; R2是H，C1-7直链或支链烷基，C3-6环烷基，C2-7烯基或苄基; A是5或6元芳族碳环或杂环，其可任选被一个或多个合适的取代基取代，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; r为0,1或2; 它们在药物中的用途，特别是用于需要抑制NO合酶的条件，药物制剂及其制备方法。 （一）

公开(公告)号：US5767312A

公开(公告)日：1998-06-16

申请号：US862468

申请日：1997-05-23

申请人： Harold Francis Hodson

发明人： Harold Francis Hodson

IPC分类号： C07C279/14 ,  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。

公开(公告)号：US4039556A

公开(公告)日：1977-08-02

申请号：US634456

申请日：1975-11-24

申请人： Harold Francis Hodson ,  John Frederick Batchelor

发明人： Harold Francis Hodson ,  John Frederick Batchelor

IPC分类号： C07D219/06 ,  C07D219/08 ,  C07D257/04 ,  C07D311/86

CPC分类号： C07D257/04 ,  C07D219/06 ,  C07D219/08 ,  C07D311/86 ,  C07C2103/18 ,  Y10S514/826

摘要： Fluorenone and anthraquinone compounds substituted by at least one tetrazolyl group in one ring, and further substituted in the other ring, optionally for the fluorenones, have antiallergic activity.

摘要翻译： 在一个环中被至少一个四唑基取代并在另一个环中进一步取代的芴酮和蒽醌化合物任选地用于芴酮，具有抗过敏活性。

公开(公告)号：US4012499A

公开(公告)日：1977-03-15

申请号：US586426

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： C07C317/44 ,  C07C323/62 ,  A61K9/14 ,  A61K31/41

CPC分类号： C07C317/44 ,  C07C323/62 ,  Y10S514/826

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。

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。