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1. 发明专利

IL213325A Use of imidazole compounds in the manufacture of a medicament for selectively treating an infection with clostridium difficile or a clostridium difficile-associated disease 未知
公开(公告)号：IL213325A
公开(公告)日：2016-02-29
申请号：IL21332511
申请日：2011-06-02
申请人： SUMMIT CORP PLC , FRANCIS XAVIER WILSON , PETER DAVID JOHNSON , RICHARD VICKERS , RICHARD STORER , GRAHAM MICHAEL WYNNE , ALAN GEOFFREY ROACH , OLIVIER DE MOOR , COLIN RICHARD DORGAN , PAUL JAMES DAVIS
发明人： FRANCIS XAVIER WILSON , PETER DAVID JOHNSON , RICHARD VICKERS , RICHARD STORER , GRAHAM MICHAEL WYNNE , ALAN GEOFFREY ROACH , OLIVIER DE MOOR , COLIN RICHARD DORGAN , PAUL JAMES DAVIS
摘要： Disclosed are pharmaceutical compositions comprising the compound 2,2'-di(pyridin-4-yl)-1H,1'H-5,5'-bibenzo[d]imidazole, or a pharmaceutically acceptable N-oxide, salt, hydrate or solvate thereof, and a pharmaceutically acceptable excipient. The compositions find application in methods of treating infection with Clostridium difficile and in methods of treating Clostridium difficile -associated disease (CDAD).

2. 发明专利

IL213325D0 ANTIBACTERIAL COMPOUNDS 未知
公开(公告)号：IL213325D0
公开(公告)日：2011-07-31
申请号：IL21332511
申请日：2011-06-02
申请人： DAVEY PAUL JAMES , SUMMIT CORP PLC , FRANCIS XAVIER WILSON , PETER DAVID JOHNSON , RICHARD VICKERS , RICHARD STORER , GRAHAM MICHAEL WYNNE , ALAN GEOFFREY ROACH , OLIVIER DE MOOR , COLIN RICHARD DORGAN
IPC分类号： C07D20060101
摘要： Disclosed are pharmaceutical compositions comprising the compound 2,2'-di(pyridin-4-yl)-1H,1'H-5,5'-bibenzo[d]imidazole, or a pharmaceutically acceptable N-oxide, salt, hydrate or solvate thereof, and a pharmaceutically acceptable excipient. The compositions find application in methods of treating infection with Clostridium difficile and in methods of treating Clostridium difficile -associated disease (CDAD).

3. 发明授权

US08975416B2 Antibacterial compounds 有权
标题翻译：抗菌化合物
公开(公告)号：US08975416B2
公开(公告)日：2015-03-10
申请号：US13131469
申请日：2009-12-01
申请人： Paul James Davis , Olivier De Moor , Colin Richard Dorgan , Peter David Johnson , Alan Geoffrey Roach , Richard Storer , Richard John Vickers , Francis Xavier Wilson , Graham Michael Wynne
发明人： Paul James Davis , Olivier De Moor , Colin Richard Dorgan , Peter David Johnson , Alan Geoffrey Roach , Richard Storer , Richard John Vickers , Francis Xavier Wilson , Graham Michael Wynne
IPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , A61K31/4184 , A61K31/4439 , C07D235/18
CPC分类号： A61K31/444 , A61K31/4439 , C07D235/18 , C07D401/14 , Y02A50/473
摘要： Disclosed are compounds of formula (I), which are of use in the treatment of bacterial diseases and infections, to compositions containing those compounds and to methods of treating bacterial diseases and infections using the compounds. In particular, the compounds are useful for the treatment of infection with, and diseases caused by, Clostridium difficile.
摘要翻译：公开了用于治疗细菌性疾病和感染的式（I）化合物，含有这些化合物的组合物以及使用该化合物治疗细菌性疾病和感染的方法。特别地，这些化合物可用于治疗由艰难梭菌引起的感染和疾病。

4. 发明授权

US08518980B2 Treatment of Duchenne muscular dystrophy 有权
标题翻译：杜氏肌营养不良症的治疗
公开(公告)号：US08518980B2
公开(公告)日：2013-08-27
申请号：US12278769
申请日：2007-02-09
申请人： Graham Michael Wynne , Stephen Paul Wren , Peter David Johnson , Paul Damien Price , Olivier De Moor , Gary Nugent , Richard Storer , Richard Joseph Pye , Colin Richard Dorgan
发明人： Graham Michael Wynne , Stephen Paul Wren , Peter David Johnson , Paul Damien Price , Olivier De Moor , Gary Nugent , Richard Storer , Richard Joseph Pye , Colin Richard Dorgan
IPC分类号： A61K31/42 , A01N43/76 , C07D263/57
CPC分类号： C07F9/4003 , A61K31/343 , A61K31/404 , A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/423 , A61K31/4245 , A61K31/426 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/4439 , A61K31/4525 , A61K31/454 , A61K31/4709 , A61K31/496 , A61K31/506 , A61K31/517 , A61K31/5377
摘要： There are disclosed compound of Formula (1): A1, A2, A3 and A4 which may be the same or different, represent N or CR1, X is a divalent group selected from O, S(O)n, C═W, NR4, NC(═O)R5 and CR6R7, W is O, S, NR20, Y is N or CR8, one of R4, R5, R6, R8, R9 and NR20 represents -L-R3, in which L is a single bond or a linker group, additionally, R1, R3-R9, which may be the same or different, independently represent hydrogen or a substituent and R20 represents hydrogen, hydroxyl, alkyl optionally substituted by aryl, alkoxy optionally substituted by aryl, aryl, CN, optionally substituted alkoxy, optionally substituted aryloxy, optionally substitute alkanoyl, optionally substituted aroyl, NO2, NR30R31, in which R30 and R31, which may be the same or different, represent hydrogen, optionally substituted alkyl or optionally substituted aryl; additionally, one of R30 and R31 may represent optionally substituted alkanoyl or optionally substituted aroyl, n represents an integer from 0 to 2, in addition, when an adjacent pair of A1-A4 each represent CR1, then the adjacent carbon atoms, together with their substituents may form a ring B, when X is CR6R7, R6 and R7, together with the carbon atom to which they are attached may form a ring C, or a pharmaceutically acceptable salt thereof, in the manufacture of a medicament for the therapeutic and/or prophylactic treatment of Duchenne muscular dystrophy, Becker muscular dystrophy or cachexia.
摘要翻译：公开了式（1）的化合物：A1，A2，A3和A4可以相同或不同，表示N或CR1，X是选自O，S（O）n，C = W，NR4的二价基团，NC（= O）R5和CR6R7，W是O，S，NR20，Y是N或CR8，R4，R5，R6，R8，R9和NR20之一表示-L-R3，其中L是单键或连接基团，另外，可以相同或不同的R 1，R 3 -R 9独立地表示氢或取代基，R 20表示氢，羟基，任选被芳基取代的烷基，任选被芳基，芳基，CN，任选取代的烷氧基，任选取代的芳氧基，任选取代的烷酰基，任选取代的芳酰基，NO 2，NR 30 R 31，其中R 30和R 31可以相同或不同，表示氢，任选取代的烷基或任选取代的芳基; 此外，R30和R31中的一个可以表示任选取代的烷酰基或任选取代的芳酰基，n表示0至2的整数，此外，当相邻的一对A1-A4各自表示CR1时，则相邻的碳原子连同它们取代基可以形成环B，当X是CR 6 R 7，R 6和R 7时，连同它们所连接的碳原子一起形成环C或其药学上可接受的盐在制备用于治疗和/ 或预防性治疗杜氏肌营养不良症，贝克肌营养不良症或恶病质。

5. 发明授权

US08138351B2 Treatment of duchenne muscular dystrophy 有权
标题翻译：杜氏肌营养不良症的治疗
公开(公告)号：US08138351B2
公开(公告)日：2012-03-20
申请号：US12599970
申请日：2008-08-14
申请人： Graham Michael Wynne , Alexander Charles Weymouth-Wilson , Robert Clarkson , Renate Van Well , Stephen Paul Wren , Olivier De Moor
发明人： Graham Michael Wynne , Alexander Charles Weymouth-Wilson , Robert Clarkson , Renate Van Well , Stephen Paul Wren , Olivier De Moor
IPC分类号： C07D263/57
CPC分类号： C07D263/57
摘要： Provided is a process for the preparation of 5-(ethylsulfonyl)-2-(naphthalen-2-yl) benzo[d] oxazole useful in the treatment of Duchenne muscular dystrophy.
摘要翻译：提供了一种制备可用于治疗杜氏肌营养不良症的5-（乙基磺酰基）-2-（萘-2-基）苯并[d]恶唑的方法。

6. 发明申请

US20090192195A1 Compounds Having CRTH2 Antagonist Activity 有权
标题翻译：具有CRTH2拮抗作用的化合物
公开(公告)号：US20090192195A1
公开(公告)日：2009-07-30
申请号：US12357821
申请日：2009-01-22
申请人： Richard Edward Armer , Carole Eliane Andree Maillol , Colin Richard Dorgan , Graham Michael Wynne , Julia Vile
发明人： Richard Edward Armer , Carole Eliane Andree Maillol , Colin Richard Dorgan , Graham Michael Wynne , Julia Vile
IPC分类号： A61K31/404 , C07D209/10 , C07D401/12 , A61K31/454 , A61P31/16 , A61P37/00
CPC分类号： C07D209/10
摘要： Compounds of general formula (I) wherein W is chloro or fluoro; Z is a group SO2R1; wherein R1 is —C3-C8 cycloalkyl or heterocyclyl optionally substituted with one or more substituents chosen from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, and —O(CH2)p—O—(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
摘要翻译：通式（I）的化合物，其中W是氯或氟; Z是SO2R1基团; 其中R 1为-C 3 -C 8环烷基或任选被一个或多个选自卤素，-CN，-C 1 -C 6烷基，-SOR 3，-SO 2 R 3，-SO 2 N（R 2）2，-N（R 2）2， -NR 2 C（O）R 3，-CO 2 R 2，-CONR 2 R 3，-NO 2，-OR 2，-SR 2，-O（CH 2）pOR 2和-O（CH 2）p O-（CH 2）q OR 2，其中每个R 2独立地是氢， -C6烷基，-C3-C8环烷基，芳基或杂芳基; 每个R 3独立地是-C 1 -C 6烷基，-C 3 -C 8环烷基，芳基或杂芳基; p和q各自独立地为1至3的整数; 其药学上可接受的盐，水合物，溶剂合物，复合物或前药可用于口服给药的组合物中，用于治疗过敏性疾病如哮喘，过敏性鼻炎和特应性皮炎。

7. 发明授权

US06504037B2 Process for preparing resorcinol derivatives 失效
公开(公告)号：US06504037B2
公开(公告)日：2003-01-07
申请号：US09801999
申请日：2001-03-08
申请人： Stuart Edward Bradley , John Kitchin , Graham Michael Wynne
发明人： Stuart Edward Bradley , John Kitchin , Graham Michael Wynne
IPC分类号： C07D31100
CPC分类号： C07D317/72 , C07C37/07 , C07C45/59 , C07C45/71 , C07C49/747 , C07C2601/14 , C07C2601/18 , Y02P20/55 , Y10S977/926 , C07C49/753 , C07C39/17
摘要： The present invention relates to an improved process for preparing 4-substituted resorcinol derivatives, and intermediate compounds useful in the preparation of such resorcinol derivatives.

8. 发明申请

US20110142855A1 Compounds Having CRTH2 Antagonist Activity 有权
标题翻译：具有CRTH2拮抗作用的化合物
公开(公告)号：US20110142855A1
公开(公告)日：2011-06-16
申请号：US13014314
申请日：2011-01-26
申请人： Richard Edward Armer , Eric Roy Pettipher , Mark Whittaker , Graham Michael Wynne , Julia Vile , Frank Schroer
发明人： Richard Edward Armer , Eric Roy Pettipher , Mark Whittaker , Graham Michael Wynne , Julia Vile , Frank Schroer
IPC分类号： A61K39/395 , A61K31/4439 , A61K31/47 , A61K31/573 , A61K31/519 , A61K31/58 , A61K31/7135 , A61K33/24 , A61P31/12 , A61P31/00 , A61P37/02 , A61P11/06
CPC分类号： A61K31/4439 , A61K31/47 , A61K45/06 , C07D401/06
摘要： Compounds of general formula (I) wherein W is chloro or fluoro; R1 is phenyl optionally substituted with one or more substituents, selected from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, or —O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and R4 is hydrogen, C1-C6 alkyl, C1-C6 alkyl substituted with aryl, aryl, (CH2)mOC(═O)C1-C6alkyl, ((CH2)mO)nCH2CH2X, (CH2)mN(R5)2 or CH((CH2)mO(C═O)R6)2; m is 1 or 2; n is 1-4; X is OR5 or N(R5)2; R5 is hydrogen or methyl; and R6 is C1-C18 alkyl; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
摘要翻译：通式（I）的化合物，其中W是氯或氟; R 1是任选被一个或多个选自卤素，-CN，-C 1 -C 6烷基，-SOR 3，-SO 2 R 3，-SO 2 N（R 2）2，-N（R 2）2，-NR 2 C（O）R 3 ，-CO 2 R 2，-CONR 2 R 3，-NO 2，-OR 2，-SR 2，-O（CH 2）pOR 2或-O（CH 2）p O（CH 2）q OR 2，其中每个R 2独立地是氢，-C 1 -C 6烷基， C8环烷基，芳基或杂芳基; 每个R 3独立地是-C 1 -C 6烷基，-C 3 -C 8环烷基，芳基或杂芳基; p和q各自独立地为1至3的整数; 芳基，（CH2）mOC（= O）C1-C6烷基，（（CH2）mO）nCH2CH2X，（CH2）mN（R5）2或CH （（CH 2）m O（C = O）R 6）2; m为1或2; n为1-4; X为OR 5或N（R 5）2; R5是氢或甲基; R6为C1-C18烷基; 其药学上可接受的盐，水合物，溶剂合物，复合物或前药可用于口服给药的组合物中，用于治疗过敏性疾病如哮喘，过敏性鼻炎和特应性皮炎。

9. 发明授权

US07919512B2 Compounds having CRTH2 antagonist activity 有权
标题翻译：具有CRTH2拮抗活性的化合物
公开(公告)号：US07919512B2
公开(公告)日：2011-04-05
申请号：US12828800
申请日：2010-07-01
申请人： Richard Edward Armer , Eric Roy Pettipher , Mark Whittaker , Graham Michael Wynne , Julia Vile , Frank Schroer
发明人： Richard Edward Armer , Eric Roy Pettipher , Mark Whittaker , Graham Michael Wynne , Julia Vile , Frank Schroer
IPC分类号： A61K31/44 , C07D401/00
CPC分类号： A61K31/4439 , A61K31/47 , A61K45/06 , C07D401/06
摘要： Compounds of general formula (II) wherein W is chloro or fluoro; R1 is phenyl optionally substituted with one or more substituents, selected from halo, —CN, —C1-C6 alkyl, —SOR3, —SO2R3, —SO2N(R2)2, —N(R2)2, —NR2C(O)R3, —CO2R2, —CONR2R3, —NO2, —OR2, —SR2, —O(CH2)pOR2, or —O(CH2)pO(CH2)qOR2 wherein each R2 is independently hydrogen, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; each R3 is independently, —C1-C6 alkyl, —C3-C8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; and R4 is hydrogen, C1-C6 alkyl, C1-C6 alkyl substituted with aryl, aryl, (CH2)mOC(═O)C1-C6alkyl, ((CH2)mO)nCH2CH2X, (CH2)mN(R5)2 or CH((CH2)mO(C═O)R6)2; m is 1 or 2; n is 1-4; X is OR5 or N(R5)2; R5 is hydrogen or methyl; and R6 is C1-C18 alkyl; and their pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs are useful in orally administrable compositions for the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
摘要翻译：通式（II）的化合物，其中W是氯或氟; R 1是任选被一个或多个选自卤素，-CN，-C 1 -C 6烷基，-SOR 3，-SO 2 R 3，-SO 2 N（R 2）2，-N（R 2）2，-NR 2 C（O）R 3 ，-CO 2 R 2，-CONR 2 R 3，-NO 2，-OR 2，-SR 2，-O（CH 2）pOR 2或-O（CH 2）p O（CH 2）q OR 2，其中每个R 2独立地是氢，-C 1 -C 6烷基， C8环烷基，芳基或杂芳基; 每个R 3独立地是-C 1 -C 6烷基，-C 3 -C 8环烷基，芳基或杂芳基; p和q各自独立地为1至3的整数; 芳基，（CH2）mOC（= O）C1-C6烷基，（（CH2）mO）nCH2CH2X，（CH2）mN（R5）2或CH （（CH 2）m O（C = O）R 6）2; m为1或2; n为1-4; X为OR 5或N（R 5）2; R5是氢或甲基; R6为C1-C18烷基; 其药学上可接受的盐，水合物，溶剂合物，复合物或前药可用于口服给药的组合物中，用于治疗过敏性疾病如哮喘，过敏性鼻炎和特应性皮炎。

10. 发明申请

US20100305120A1 COMPOUNDS FOR TREATING MUSCULAR DYSTROPHY 审中-公开
标题翻译：用于治疗肌肉晶状体的化合物
公开(公告)号：US20100305120A1
公开(公告)日：2010-12-02
申请号：US12599963
申请日：2009-04-03
申请人： Graham Michael Wynne , Stephen Paul Wren , Renate Maria Van Well , Daniel Robert Chancellor , Frank Schroer , Francis Xavier Wilson
发明人： Graham Michael Wynne , Stephen Paul Wren , Renate Maria Van Well , Daniel Robert Chancellor , Frank Schroer , Francis Xavier Wilson
IPC分类号： A61K31/5377 , A61K31/498 , A61K31/4709 , A61K31/454 , A61K31/4439 , A61K31/433 , A61K31/4245 , A61K31/428 , A61K31/427 , A61K31/423 , A61K31/422 , A61K31/416 , C07D413/10 , C07D231/56 , A61P21/00
CPC分类号： A61K31/428 , A61K31/404 , A61K31/415 , A61K31/4155 , A61K31/416 , A61K31/422 , A61K31/423 , A61K31/4245 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/454 , A61K31/4709 , A61K31/498 , A61K31/5377 , C07D231/56 , C07D405/12
摘要： Compounds of formula (I): wherein X, L1, R1, L2, R2, R3, and R4 are as defined herein, are useful in the treatment or prophylaxis of Duchenne muscular dystrophy, Becker muscular dystrophy, or cachexia.
摘要翻译：式（I）化合物：其中X，L1，R1，L2，R2，R3和R4如本文所定义，可用于治疗或预防杜氏肌营养不良症，贝克肌营养不良症或恶病质。

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