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：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：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：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：US20060122234A1

公开(公告)日：2006-06-08

申请号：US10522873

申请日：2003-07-24

申请人： Janet Archer ,  Walter Bordogna ,  Richard Bull ,  David Clark ,  Hazel Dyke ,  Matthew Gill ,  Neil Harris ,  Marco Van Den Heuvel ,  Stephen Price

发明人： Janet Archer ,  Walter Bordogna ,  Richard Bull ,  David Clark ,  Hazel Dyke ,  Matthew Gill ,  Neil Harris ,  Marco Van Den Heuvel ,  Stephen Price

IPC分类号： A61K31/4436 ,  A61K31/433 ,  A61K31/4245 ,  A61K31/4178 ,  A61K31/416 ,  C07D409/02

CPC分类号： C07D409/04 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/14

摘要： A compound of formula (I): which can be used in the treatment of diseases associated with histone deacetylase enzymatic activity.

摘要翻译： 式（I）化合物：其可用于治疗与组蛋白脱乙酰酶酶活性相关的疾病。

公开(公告)号：US20060029240A1

公开(公告)日：2006-02-09

申请号：US11244230

申请日：2005-10-06

申请人： Graham Bank ,  Neil Harris ,  Denis Morecroft

发明人： Graham Bank ,  Neil Harris ,  Denis Morecroft

IPC分类号： H04R25/00

CPC分类号： H04R9/025 ,  H04R1/227 ,  H04R7/045 ,  H04R9/06 ,  H04R9/066 ,  H04R17/00 ,  H04R2440/05 ,  H04R2499/15

摘要： A loudspeaker comprising a resonant panel-form member adapted to produce an acoustic output and a vibration exciting system on the panel-form member and adapted to apply bending wave energy thereto, characterised in that the vibration exciting system is adapted to apply a bending couple to the panel-form member.

摘要翻译： 一种扬声器，包括适于在所述面板构件上产生声输出和振动激励系统的谐振板形构件，并且适于向其施加弯曲波能，其特征在于，所述振动激励系统适于将弯曲耦合施加到 面板成员。

公开(公告)号：US06389935B1

公开(公告)日：2002-05-21

申请号：US09029056

申请日：1998-07-08

申请人： Henry Azima ,  Martin Colloms ,  Neil Harris

发明人： Henry Azima ,  Martin Colloms ,  Neil Harris

IPC分类号： H04R2500

CPC分类号： H04R7/06 ,  G07F9/02 ,  H04R5/02 ,  H04R7/045 ,  H04R2307/029 ,  H04R2499/15

摘要： A display screen (32), e.g., a projection screen comprising a panel having a light reflective surface, characterised in that the screen is a distributed mode acoustic radiator loudspeaker having a transducer (9) mounted wholly and exclusively thereon to vibrate the radiator to cause it to resonate to provide an acoustic output.

摘要翻译： 显示屏（32），例如包括具有光反射表面的面板的投影屏幕，其特征在于，所述屏幕是分布式模式声辐射扬声器，其具有完全和专门地安装在其上的振动器（9），以使散热器振动， 它共鸣提供声输出。

公开(公告)号：US06320967B1

公开(公告)日：2001-11-20

申请号：US09029349

申请日：1998-08-24

申请人： Henry Azima ,  Martin Colloms ,  Neil Harris

发明人： Henry Azima ,  Martin Colloms ,  Neil Harris

IPC分类号： H04R2500

CPC分类号： B42D15/022 ,  B60R11/0217 ,  G06F1/1605 ,  G06F1/1616 ,  G06F1/1688 ,  G06F9/02 ,  G07F9/02 ,  H04R1/021 ,  H04R1/025 ,  H04R1/028 ,  H04R1/24 ,  H04R1/26 ,  H04R1/2811 ,  H04R3/04 ,  H04R5/02 ,  H04R5/027 ,  H04R7/045 ,  H04R7/06 ,  H04R7/08 ,  H04R9/025 ,  H04R9/045 ,  H04R9/066 ,  H04R17/00 ,  H04R2201/021 ,  H04R2307/029 ,  H04R2440/07 ,  H04R2499/13 ,  H04R2499/15

摘要： A vehicle having a passenger compartment (102) characterised by a loudspeaker (81) in the passenger compartment comprising a distributed mode acoustic radiator (2) and a transducer (9) mounted wholly and exclusively on the radiator to vibrate the radiator to cause it to resonate.

摘要翻译： 一种具有乘客舱（102）的车辆，其特征在于乘客舱中的扬声器（81），包括分布式声辐射器（2）和传感器（9），传感器全部和全部安装在散热器上以使散热器振动 谐振。