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11. 发明授权

US08236963B2 Tricyclic spiro derivatives as CRTH2 modulators 失效
标题翻译：三环螺衍生物作为CRTH2调节剂
公开(公告)号：US08236963B2
公开(公告)日：2012-08-07
申请号：US11919471
申请日：2006-05-23
申请人： Matthias Schwarz , Eric Sebille , Christophe Cleva , Cedric Merlot , Dennis Church , Patrick Page , Jacqueline A. Macritchie , John Frederick Atherall , Stefano Crosignani , Doris Pupowicz
发明人： Matthias Schwarz , Eric Sebille , Christophe Cleva , Cedric Merlot , Dennis Church , Patrick Page , Jacqueline A. Macritchie , John Frederick Atherall , Stefano Crosignani , Doris Pupowicz
IPC分类号： C07D277/20 , C07D271/06 , C07D417/14 , C07D487/10 , C07D261/06 , A61K31/44 , A61K31/431 , A61K31/4184 , A61K31/4196 , A61K31/41
CPC分类号： C07D487/10
摘要： The present invention is related to the use of spiro derivatives of Formula (I) for the treatment and/or prevention of allergic diseases, inflammatory dermatoses and other diseases with an inflammatory component. Specifically, the present invention is related to the use of spiro derivatives for the modulation of CRTH2 activity.
摘要翻译：本发明涉及式（I）的螺衍生物用于治疗和/或预防具有炎性成分的过敏性疾病，炎性皮肤病和其它疾病的用途。具体地说，本发明涉及螺衍生物用于调节CRTH2活性的用途。

12. 发明授权

US08193215B2 Thieno[2 3-b]pyridines as potassium channel inhibitors 有权
标题翻译：噻吩并[2,3-b]吡啶作为钾通道抑制剂
公开(公告)号：US08193215B2
公开(公告)日：2012-06-05
申请号：US12543151
申请日：2009-08-18
申请人： John Ford , Nicholas John Palmer , John Frederick Atherall , David John Madge , Derek John
发明人： John Ford , Nicholas John Palmer , John Frederick Atherall , David John Madge , Derek John
IPC分类号： A01N43/42
CPC分类号： C07D495/04 , C07D333/36 , C07D333/38 , C07D409/12
摘要： The invention provides compounds of the formula: wherein R1 is aryl, heteroaryl, cycloalkyl or alkyl; R2 is H, alkyl, nitro, CO2R7, CONR5R6 or halo; R3 and R4 are H, NR5R6, NC(O)R7, halo, trifluromethyl, alkyl, CONR5R6, CO2R7, nitrile or alkoxy; R5 and R6 may be the same or different and may be H, alkyl, aryl, heteroaryl or cycloalkyl; or R5 and R6 may together form a saturated, unsaturated or partially saturated 4 to 7 member ring, wherein said ring may optionally comprise one or more further heteroatoms selected from N, O or S; R7 is H or alkyl; A is H, halo, or a group of formula X-L-Y; X is O, S or NR8; R8 is H or alkyl; L is (CH2)n, where n is 0, 1, 2, 3 or 4; and Y is aryl, a heterocyclic group, alkyl, alkenyl or cycloalkyl; the products of mono- and di-oxidation of sulphur and/or mono-oxidation of nitrogen moieties in compounds of formula I; or a pharmaceutically acceptable salt thereof. These compounds find use as inhibitors of potassium ion channels and thus are useful in the treatment of various conditions including arrhythmia and type-2 diabetes mellitus.
摘要翻译：本发明提供下式的化合物：其中R1是芳基，杂芳基，环烷基或烷基; R2是H，烷基，硝基，CO 2 R 7，CONR 5 R 6或卤素; R3和R4是H，NR5R6，NC（O）R7，卤素，三氟甲基，烷基，CONR5R6，CO2R7，腈或烷氧基; R5和R6可以相同或不同，可以是H，烷基，芳基，杂芳基或环烷基; 或R 5和R 6可以一起形成饱和的，不饱和的或部分饱和的4至7元环，其中所述环可任选地包含一个或多个选自N，O或S的其它杂原子; R7是H或烷基; A是H，卤素或式X-L-Y基团; X是O，S或NR8; R8是H或烷基; L是（CH 2）n，其中n是0,1,2,3或4; Y为芳基，杂环基，烷基，链烯基或环烷基; 式I化合物中硫的单和二氧化和/或氮部分的单氧化的产物; 或其药学上可接受的盐。这些化合物可用作钾离子通道的抑制剂，因此可用于治疗各种病症，包括心律失常和2型糖尿病。

13. 发明申请

US20110263590A1 Antibacterial Compositions 有权
标题翻译：抗菌组合物
公开(公告)号：US20110263590A1
公开(公告)日：2011-10-27
申请号：US13154592
申请日：2011-06-07
申请人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
发明人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
IPC分类号： A61K31/4439 , A61K31/428 , A61K31/497 , A61K31/496 , A61P31/04 , A61K31/506 , A61K31/501 , A61K31/5383 , A61K31/519 , A61K31/444 , A61K31/5377
CPC分类号： C07D417/04 , C07D417/14 , Y02P20/582
摘要： Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; Alk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(═O)NR6—, —S(O)NR6—, —C(═O)O— or —S(═O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N or CH, or CF; R2 and R3 are as defined in the description.
摘要翻译：式（I）化合物具有抗菌活性：其中：m为0或1; Q是氢或环丙基; Alk是可以含有醚（-O-），硫醚（-S-）或氨基（-NR） - 连接的任意取代的二价C1-C6亚烷基，亚烯基或亚炔基，其中R是氢，-CN或 C1-C3烷基; X是-C（= O）NR 6 - ， - S（O）NR 6 - ， - C（= O）O-或-S（= O）O-，其中R 6是氢，任选取代的C 1 -C 6烷基， C6链烯基，C2-C6炔基，-Cyc或 - （C1-C3烷基）-Cyc，其中Cyc是具有3-7个环原子的任选取代的单环碳环或杂环; Z是N或CH，或CF; R2和R3如说明书中所定义。

14. 发明授权

US08022076B2 Substituted thieno[2,3-d]pyrimidines as potassium channel inhibitors 有权
标题翻译：取代噻吩并[2,3-d]嘧啶作为钾通道抑制剂
公开(公告)号：US08022076B2
公开(公告)日：2011-09-20
申请号：US10864771
申请日：2004-06-10
申请人： John Ford , Nicholas John Palmer , John Frederick Atherall , David John Madge , Brad Sherborne , Mark Bushfield , Edward Benedict Stevens
发明人： John Ford , Nicholas John Palmer , John Frederick Atherall , David John Madge , Brad Sherborne , Mark Bushfield , Edward Benedict Stevens
IPC分类号： C07D495/04 , A61K31/519 , A61P9/06
CPC分类号： A61K31/495 , C07D495/04
摘要： This invention relates to novel compound of formula (I) or pharmaceutically acceptable salts thereof. The invention is also directed to the uses of compounds having formula (I) in the treatment or prevention of diseases or disorders which requires potassium channel inhibition to an animal, mammal or human in need thereof. The invention is also directed to the use of compounds having formula (I) in the treatment or prevention of arrhythmia to an animal, mammal or human in need thereof.
摘要翻译：本发明涉及新的式（I）化合物或其药学上可接受的盐。本发明还涉及具有式（I）的化合物在治疗或预防需要钾通道抑制的疾病或病症中对于有需要的动物，哺乳动物或人的用途。本发明还涉及具有式（I）的化合物在治疗或预防心律失常的用途对于有需要的动物，哺乳动物或人类的用途。

15. 发明申请

US20090197877A1 Antibacterial Compositions 有权
标题翻译：抗菌组合物
公开(公告)号：US20090197877A1
公开(公告)日：2009-08-06
申请号：US12304303
申请日：2007-06-21
申请人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
发明人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
IPC分类号： A61K31/5383 , C07D417/10 , A61K31/4439 , A61K31/496 , C07D417/14 , C07D498/04 , A61P31/04
CPC分类号： C07D417/04 , C07D417/14 , Y02P20/582
摘要： Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(═O)NR6—, —S(O)NR6—, —C(═O)O— or —S(═O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N or CH, or CF; R2 and R3 are as defined in the description.
摘要翻译：式（I）化合物具有抗菌活性：其中：m为0或1; Q是氢或环丙基; Alk是可以含有醚（-O-），硫醚（-S-）或氨基（-NR） - 连接的任意取代的二价C 1 -C 6亚烷基，亚烯基或亚炔基，其中R是氢，-CN或 C1-C3烷基; X是-C（-O）NR 6 - ， - S（O）NR 6 - ， - C（-O）O-或-S（-O）O-，其中R 6是氢，任选取代的C 1 -C 6烷基， C6链烯基，C2-C6炔基，-Cyc或 - （C1-C3烷基）-Cyc，其中Cyc是具有3-7个环原子的任选取代的单环碳环或杂环; Z是N或CH，或CF; R2和R3如说明书中所定义。

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