公开(公告)号：US20050176791A1

公开(公告)日：2005-08-11

申请号：US10640476

申请日：2003-08-14

申请人： Alexander Oxford ,  Richard Borman ,  Robert Coleman ,  Kenneth Clark ,  George Hynd ,  Janet Archer ,  Amanda Aley ,  Neil Harris ,  Andrew Goulter

发明人： Alexander Oxford ,  Richard Borman ,  Robert Coleman ,  Kenneth Clark ,  George Hynd ,  Janet Archer ,  Amanda Aley ,  Neil Harris ,  Andrew Goulter

IPC分类号： A61K31/421 ,  A61P9/04 ,  C07D263/48 ,  C07D413/04

CPC分类号： C07D263/48 ,  A61K31/421 ,  C07D413/04

摘要： The present invention relates to compounds which include compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein one of R1 and R4 is selected from the group consisting of H, and optionally substituted C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-4 alkyl, and phenyl-C1-4 alkyl; and the other of R1 and R4 is an optionally substituted C9-14 aryl group; R2 and R3 are either: (i) independently selected from H, R, R′, SO2R, C(═O)R, (CH2)nNR5R6, where n is from 1 to 4 and R5 and R6 are independently selected from H and R, where R is optionally substituted C1-4 alkyl, and R′ is optionally substituted phenyl-C1-4 alkyl, or (ii) together with the nitrogen atom to which they are attached, form an optionally substituted C5-7 heterocyclic group. The compounds are useful in the treatment of conditions including conditions which can be alleviated by antagonism of a 5-HT2B receptor such as GI disorders and congestive heart failure.

摘要翻译： 本发明涉及包括式I化合物或其药学上可接受的盐的化合物，其中R 1和R 4中的一个选自由以下组成的组： H和任选取代的C 1-6烷基，C 3-7环烷基，C 3-7环烷基-C 1〜 4烷基和苯基-C 1-4烷基; R 1和R 4中的另一个是任选取代的C 9-14芳基; R 2和R 3是：（i）独立地选自H，R，R'，SO 2 R，C（-O ）R，（CH 2）2 NR 6，其中n为1至4，R H和R 6独立地选自H和R，其中R是任选取代的C 1-4烷基，R'任选被取代 苯基-C 1-4烷基，或（ii）与它们所连接的氮原子一起形成任选取代的C 5-7杂环基。 所述化合物可用于治疗包括可通过拮抗5-HT 2B受体如GI病症和充血性心力衰竭而缓解的病症的病症。

公开(公告)号：US20070123575A1

公开(公告)日：2007-05-31

申请号：US11615024

申请日：2006-12-22

申请人： Alexander Oxford ,  Richard Davis ,  Robert Coleman ,  Kenneth Clark ,  David Clark ,  Neil Harris ,  Garry Fenton ,  George Hynd ,  Keith Stuttle ,  Jonathan Sutton ,  Christopher Newton

发明人： Alexander Oxford ,  Richard Davis ,  Robert Coleman ,  Kenneth Clark ,  David Clark ,  Neil Harris ,  Garry Fenton ,  George Hynd ,  Keith Stuttle ,  Jonathan Sutton ,  Christopher Newton

IPC分类号： A61K31/41 ,  A61K31/34 ,  C07D405/02

CPC分类号： C07D307/54 ,  A61K31/34 ,  A61K31/341 ,  A61K31/4155 ,  A61K31/443 ,  C07D307/64 ,  C07D307/68 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

摘要： Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(═O), S(═O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(═O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): ; or (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.

摘要翻译： 式（I）的化合物：其中：R 2是H或任选取代的C 1-4烷基; Y是 - （CH 2）n -X-，其中n是1或2，X是O，S，S（-O），S（-O ）N 2，或NR 11，其中R 0,1选自H或任选取代的C 1-4烷基 ，或Y是-C（-O）NR N2 - ，其中R N2选自H和任选取代的C 1-7 - 烷基或C 5-20-20芳基; R 3是与另外任选取代的C 6 -C 6芳基连接的任选取代的C 6-14芳基，其中如果两个C 6 芳基是苯环，两个环之间可能有一个氧桥，与两个环上的连接相邻; A是单键或C 1-3-3亚烷基; 和R 5是：（i）羧基; （ii）式（II）的组： 或（iii）式（III）的基团：其中R是任选取代的C 1-7烷基，C 5-20-20芳基或NR N 3， 其中R“N 3”和“R”N 4“独立地选自任选取代的C 1-4烷基 ; （ⅳ）四唑-5-基。

公开(公告)号：US20050256170A1

公开(公告)日：2005-11-17

申请号：US11055724

申请日：2005-02-11

申请人： Alexander Oxford ,  Richard Davis ,  Robert Coleman ,  Kenneth Clark ,  David Clark ,  Neil Harris ,  Garry Fenton ,  George Hynd ,  Keith Stuttle ,  Jonathan Sutton ,  Mark Ashton ,  Edward Boyd ,  Shirley Brunton

发明人： Alexander Oxford ,  Richard Davis ,  Robert Coleman ,  Kenneth Clark ,  David Clark ,  Neil Harris ,  Garry Fenton ,  George Hynd ,  Keith Stuttle ,  Jonathan Sutton ,  Mark Ashton ,  Edward Boyd ,  Shirley Brunton

IPC分类号： A61K31/4178 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4439 ,  C07C233/75 ,  C07C233/81 ,  C07C235/84 ,  C07D213/81 ,  C07D233/90 ,  C07D257/04 ,  C07D277/24 ,  C07D277/26 ,  C07D277/56 ,  C07D307/46 ,  C07D307/68 ,  C07D307/91 ,  C07D333/38 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/12 ,  C07D413/02 ,  C07D417/02 ,  C07D43/02

CPC分类号： C07D213/81 ,  C07C233/75 ,  C07C233/81 ,  C07C235/84 ,  C07D233/90 ,  C07D257/04 ,  C07D277/24 ,  C07D277/26 ,  C07D277/56 ,  C07D307/46 ,  C07D307/68 ,  C07D307/91 ,  C07D333/38 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/12

摘要： A compound of formula (I): or a salt, solvate and chemically protected form thereof, wherein: R5is an optionally substituted C5-20 aryl or C4-20 alkyl group; A is selected from the group consisting of: wherein X and Y are selected from the group consisiting of: O and CR3; S and CR3; NH and CR3; NH and N; O and N; S and N; N and S; and N and O., and where the dotted lines indicate a double bond in the appropriate location, and where Q is either N or CH; R3 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; R4 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; R6 is selected from H, F, Cl and optionally substituted C1-4 alkyl, C1-4 alkoxy, C5-7 aryl and C5-7 aryl-C1-4 alkyl groups; D is selected from: B is selected from the group consisting of: where RN′ is selected from H and C1-4 alkyl; where one of RP3 and RP4 is —Cm alkylene-R2 and the other of RP3 and RP4 is H, m and n can be 0 or 1, and m+n=1 or 2; and additionally when RP3 is —Cm alkylene-R2, m can also be 2 or 3, and m+n=1, 2, 3 or 4, and when R2 is tetrazol-5-yl, m+n may be 0; or where one of RP3 and RP4 is —O—CH2—R2, and the other of RP3 and RP4 is H, n is 0; RN is H or optionally substituted C1-4 alkyl; R2 is either: —CO2H (carboxy); —CONH2; —CH2-OH; or tetrazol-5-yl.

公开(公告)号：US20080039502A1

公开(公告)日：2008-02-14

申请号：US11889570

申请日：2007-08-14

申请人： Alexander Oxford ,  Richard Davis ,  Robert Coleman ,  Kenneth Clark ,  David Clark ,  Neil Harris ,  Garry Fenton ,  George Hynd ,  Keith Stuttle ,  Jonathan Sutton ,  Christopher Newton

发明人： Alexander Oxford ,  Richard Davis ,  Robert Coleman ,  Kenneth Clark ,  David Clark ,  Neil Harris ,  Garry Fenton ,  George Hynd ,  Keith Stuttle ,  Jonathan Sutton ,  Christopher Newton

IPC分类号： A61K31/34 ,  A61K31/341 ,  A61K31/4155 ,  A61K31/443 ,  A61P25/06 ,  C07D231/12 ,  C07D231/18 ,  C07D307/68 ,  C07D307/77 ,  C07D405/12 ,  C07D413/12

CPC分类号： C07D307/54 ,  A61K31/34 ,  A61K31/341 ,  A61K31/4155 ,  A61K31/443 ,  C07D307/64 ,  C07D307/68 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14

摘要： Compounds of formula (I): wherein: R2 is H or an optionally substituted C1-4 alkyl group; Y is either —(CH2)n—X—, where n is 1 or 2 and X is O, S, S(═O), S(═O)2, or NRN1, where RN1 is selected from H or optionally substituted C1-4 alkyl, or Y is —C(═O)NRN2—, where RN2 is selected from H, and optionally substituted C1-7 alkyl or C5-20 aryl; R3 is an optionally substituted C6 aryl group linked to a further optionally substituted C6 aryl group, wherein if both C6 aryl groups are benzene rings, there may be an oxygen bridge between the two rings, bound adjacent the link on both rings; A is a single bond or a C1-3 alkylene group; and R5 is either: (i) carboxy; (ii) a group of formula (II): (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; (iv) tetrazol-5-yl.

摘要翻译： 式（I）的化合物：其中：R 2是H或任选取代的C 1-4烷基; Y是 - （CH 2）n -X-，其中n是1或2，X是O，S，S（-O），S（-O ）N 2，或NR 11，其中R 0,1选自H或任选取代的C 1-4烷基 ，或Y是-C（-O）NR N2 - ，其中R N2选自H和任选取代的C 1-7 - 烷基或C 5-20-20芳基; R 3是与另外任选取代的C 6 -C 6芳基连接的任选取代的C 6-14芳基，其中如果两个C 6 芳基是苯环，两个环之间可能有一个氧桥，与两个环上的连接相邻; A是单键或C 1-3-3亚烷基; 和R 5是：（i）羧基; （ii）式（II）的基团：（iii）式（III）的基团：其中R是任选取代的C 1-7烷基，C 5〜20 其中R“N 3”和“R”N 4“独立地选自任选取代的C 1 -C 6烷基， 烷基; （ⅳ）四唑-5-基。

公开(公告)号：US20070135503A1

公开(公告)日：2007-06-14

申请号：US10576095

申请日：2004-10-15

申请人： David Clark ,  Neil Harris ,  Garry Fenton ,  George Hynd ,  Keith Stuttle ,  Jonathan Sutton ,  Alexander Oxford ,  Richard Davis ,  Robert Coleman ,  Kenneth Clark

发明人： David Clark ,  Neil Harris ,  Garry Fenton ,  George Hynd ,  Keith Stuttle ,  Jonathan Sutton ,  Alexander Oxford ,  Richard Davis ,  Robert Coleman ,  Kenneth Clark

IPC分类号： A61K31/41 ,  A61K31/34 ,  A61K31/405 ,  C07D307/02

CPC分类号： C07D307/68

摘要： A compound of formula (I): or a salt, solvate and chemically protected form thereof, wherein one of R2 and R5 is: (i) H or an optionally substituted C1-4 alkyl group; or (ii) an optionally substituted C5-7 aryl; and the other of R2 and R5 is the other group; m and n can be 0 or 1, and m+n=1 or 2 RN is H or optionally substituted C1-4 alkyl R3 is either: (i) carboxy; (ii) a group of formula (II): (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl, or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; or (iv) tetrazol-5-yl.

摘要翻译： 式（I）化合物或其盐，溶剂合物和化学保护形式，其中R 2和R 5中的一个为：（i）H或任选地 取代的C 1-4烷基; 或（ii）任选取代的C 5-7芳基; R 2和R 5中的另一个是另一个基团; m和n可以是0或1，m + n = 1或2 R N是H或任选取代的C 1-4烷基R 3， SUP>是：（i）羧基; （ii）式（II）的基团：（iii）式（III）的基团：其中R是任选取代的C 1-7烷基，C 5〜20 其中R 3，N 3和R 4各自独立地选自任选取代的C 1 -C 6芳基或NR N 3 N， 1-4个C 1-4烷基; 或（iv）四唑-5-基。

公开(公告)号：US20050124676A1

公开(公告)日：2005-06-09

申请号：US10964831

申请日：2004-10-15

申请人： David Clark ,  Neil Harris ,  Garry Fenton ,  George Hynd ,  Keith Stuttle ,  Jonathan Sutton ,  Alexander Oxford ,  Richard Davis ,  Robert Coleman ,  Kenneth Clark

发明人： David Clark ,  Neil Harris ,  Garry Fenton ,  George Hynd ,  Keith Stuttle ,  Jonathan Sutton ,  Alexander Oxford ,  Richard Davis ,  Robert Coleman ,  Kenneth Clark

IPC分类号： A61K31/34 ,  A61K31/41 ,  C07D307/68 ,  C07D45/02

CPC分类号： C07D307/68

摘要： A compound of formula (I): or a salt, solvate and chemically protected form thereof, wherein one of R2 and R5 is: (i) H or an optionally substituted C1-4 alkyl group; or (ii)an optionally substituted C5-7 aryl; and the other of R2 and R5 is the other group; m and n can be 0 or 1, and m+n=1 or 2 RN is H or optionally substituted C1-4 alkyl R3 is either: (i) carboxy; (ii) a group of formula (II): (iii) a group of formula (III): wherein R is optionally substituted C1-7 alkyl, C5-20 aryl, or NRN3RN4, where RN3 and RN4 are independently selected from optionally substituted C1-4 alkyl; or (iv) tetrazol-5-yl.

摘要翻译： 式（I）化合物或其盐，溶剂合物和化学保护形式，其中R 2和R 5中的一个为：（i）H或任选地 取代的C 1-4烷基; 或（ii）任选取代的C 5-7芳基; R 2和R 5中的另一个是另一个基团; m和n可以是0或1，m + n = 1或2 R N是H或任选取代的C 1-4烷基R 3， SUP>是：（i）羧基; （ii）式（II）的基团：（iii）式（III）的基团：其中R是任选取代的C 1-7烷基，C 5〜20 其中R 3，N 3和R 4各自独立地选自任选取代的C 1 -C 6芳基或NR N 3 N， 1-4个C 1-4烷基; 或（iv）四唑-5-基。

公开(公告)号：US20050209336A1

公开(公告)日：2005-09-22

申请号：US11019133

申请日：2004-12-22

申请人： Richard Borman ,  Robert Coleman ,  Kenneth Clark ,  Keith Mills ,  Alexander Oxford ,  Jian Zhang ,  Peter Duff

发明人： Richard Borman ,  Robert Coleman ,  Kenneth Clark ,  Keith Mills ,  Alexander Oxford ,  Jian Zhang ,  Peter Duff

IPC分类号： A61K31/192 ,  A61K31/557 ,  A61K31/5575 ,  C07C59/185 ,  C07C59/90 ,  C07C405/00

CPC分类号： C07C59/90 ,  C07C405/0025

摘要： A compound selected from one of the following: or a salt, solvate, chemically protected form or prodrug thereof, and its use in treating conditions alleviated by agonism of an EP2 receptor.

摘要翻译： 选自以下之一的化合物或其盐，溶剂合物，化学保护形式或前药，以及其用于治疗由受体受体拮抗剂缓解的病症的用途。

公开(公告)号：US20050154031A1

公开(公告)日：2005-07-14

申请号：US10504538

申请日：2003-02-11

申请人： Alexander Oxford ,  Richard Borman ,  Robert Coleman ,  Kenneth Clark

发明人： Alexander Oxford ,  Richard Borman ,  Robert Coleman ,  Kenneth Clark

IPC分类号： C07D277/20 ,  A61K31/425 ,  A61K31/426 ,  A61P1/00 ,  A61P43/00 ,  C07D277/40

CPC分类号： C07D277/40 ,  A61K31/425

摘要： The present invention concerns compounds of formula (I): wherein R1 is selected from the group consisting of H, and optionally substituted C1-6 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl-C1-4 alkyl, and phenyl-C1-4 alkyl; R2 and R3 are either: (i) independently selected from H, R, R′, SO2R, C(═O)R, (CH2)nNR5R6, where n is from 1 to 4 and R5 and R6 are independently selected from H and R, where R is optionally substituted C1-4 alkyl group, and R′ is an optionally substituted phenyl-C1-4 alkyl group, or (ii) together with the nitrogen atom to which they are attached, form an optionally substituted C5-7 heterocyclic group; R4 is an optionally substituted C9-14 aryl group; their use as pharmaceuticals, in particular for treating conditions alleviated by antagonism of a 5-HT2B receptor.

摘要翻译： 本发明涉及式（I）的化合物：其中R 1选自H和任选取代的C 1-6烷基，C 1 -C 6烷基， 3-7环烷基，C 3-7环烷基-C 1-4烷基和苯基-C 1-4烷基 ; R 2和R 3是：（i）独立地选自H，R，R'，SO 2 R，C（-O ）R，（CH 2）2 NR 6，其中n为1至4，R H和R 6独立地选自H和R，其中R是任选取代的C 1-4烷基，R'是 任选取代的苯基-C 1-4烷基，或（ii）与它们所连接的氮原子一起形成任选取代的C 5-7杂环基 ; R 4是任选取代的C 9-14芳基; 它们用作药物，特别是用于治疗通过拮抗5-HT 2B受体而减轻的病症。

公开(公告)号：US09227338B2

公开(公告)日：2016-01-05

申请号：US14527073

申请日：2014-10-29

申请人： Robert Coleman

发明人： Robert Coleman

IPC分类号： B27K3/52 ,  A01N59/14 ,  A01N59/20 ,  B27K3/02 ,  B27K3/04 ,  B27K3/08 ,  B27K3/16 ,  B27K3/36

CPC分类号： B27K3/52 ,  A01N59/14 ,  A01N59/20 ,  B27K3/0228 ,  B27K3/04 ,  B27K3/08 ,  B27K3/163 ,  B27K3/36 ,  Y10T428/31989 ,  Y10T428/662 ,  A01N37/02 ,  A01N2300/00

摘要： Wood preservatives, methods for protecting wood and wood-based products and/or structures utilizing the preservatives, and treated wood and wood-based articles and/or structures incorporating the preservatives are described. Methods are also provided for remediating structures already infected with mold. The subject wood preservative formulation includes a borate compound and a fatty acid. The addition of an emulsifier to the formulation further facilitates application of the treatment. The combination of a borate compound and fatty acid combination typically provide a synergistic effect compared to the additive result provided by the combination's individual components.

摘要翻译： 描述木材防腐剂，用于保护使用防腐剂的木材和木材产品和/或结构的方法，以及加入防腐剂的经处理的木材和木材制品和/或结构。 还提供了用于修复已经感染霉菌的结构的方法。 本发明的木材防腐剂配方包括硼酸盐化合物和脂肪酸。 向制剂中加入乳化剂进一步有利于处理的应用。 与组合的各个组分提供的添加剂结果相比，硼酸盐化合物和脂肪酸组合的组合通常提供协同效应。

公开(公告)号：US06969696B2

公开(公告)日：2005-11-29

申请号：US10346638

申请日：2003-01-17

申请人： Robert Coleman

发明人： Robert Coleman

IPC分类号： A01N37/04 ,  A01N63/00 ,  A01N37/00 ,  A01N37/08 ,  A01N57/00 ,  A01N59/00

CPC分类号： A01N37/04 ,  A01N57/20 ,  A01N37/06 ,  A01N37/02 ,  A01N2300/00

摘要： The invention provides, improved herbicide compositions, methods of making the compositions and methods of controlling plant growth. The subject invention relates to combining fatty acid based and other herbicides with succinic acid, succinic acid derivatives and other additives such as those having essentially no herbicidal activity to increase the activity of the herbicide and provide methods of controlling plant growth by applying a combination of a herbicidal fatty acid with succinic acid and/or succinic acid derivative chemicals and/or other additives. In addition to the use of succinic acid, combining other Krebs cycle acids with herbicides can also provide beneficial effects. Concentrations of herbicides and additives applied to plants in accordance with the invention can include compositions involving 0.1 to 30% herbicide, preferably 0.5 to 15% herbicide and additive and more preferably 1-8% herbicide. The ratio of herbicide, such as fatty acid herbicide to activity enhancing additives can be from 1:10 to 20:1, preferably 1:1 to 20:1, most preferably 1:1 to 5:1.

摘要翻译： 本发明提供了改进的除草剂组合物，制备组合物的方法和控制植物生长的方法。 本发明涉及将基于脂肪酸的和其它除草剂与琥珀酸，琥珀酸衍生物和其它添加剂组合，例如基本上没有除草活性的添加剂，以增加除草剂的活性，并提供通过应用 具有琥珀酸和/或琥珀酸衍生物化学品和/或其它添加剂的除草脂肪酸。 除了使用琥珀酸之外，将其他克雷伯循环酸与除草剂结合也可以提供有益效果。 根据本发明施用于植物的除草剂和添加剂的浓度可包括涉及0.1至30％除草剂，优选0.5至15％除草剂和添加剂，更优选1-8％除草剂的组合物。 除草剂如脂肪酸除草剂与活性增强添加剂的比例可以为1:10至20:1，优选1:1至20:1，最优选1:1至5:1。