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1. 发明申请

WO2005040114A1 COMPOUNDS HAVING CRTH2 ANTAGONIST ACTIVITY 审中-公开
标题翻译：具有CRTH2拮抗剂活性的化合物
公开(公告)号：WO2005040114A1
公开(公告)日：2005-05-06
申请号：PCT/GB2004/004336
申请日：2004-10-13
申请人： OXAGEN LIMITED , MIDDLEMISS, David , ASHTON, Mark, Richard , BOYD, Edward, Andrew , BROOKFIELD, Frederick, Arthur , ARMER, Richard, Edward
发明人： MIDDLEMISS, David , ASHTON, Mark, Richard , BOYD, Edward, Andrew , BROOKFIELD, Frederick, Arthur , ARMER, Richard, Edward
IPC分类号： C07D209/30
CPC分类号： C04B35/632 , C07D209/30 , C07D401/12 , C07D403/12 , C07D417/12
摘要： Compounds of general formula (I) and their pharmaceutically acceptable salts, hydrates, solvates, complexes and prodrugs are useful in the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
摘要翻译：通式（I）化合物及其药学上可接受的盐，水合物，溶剂合物，复合物和前药可用于治疗过敏性疾病如哮喘，过敏性鼻炎和特应性皮炎。

2. 发明申请

WO2005040112A1 COMPOUNDS WITH PGD2 ANTAGONIST ACTIVITY 审中-公开
标题翻译：具有PGD2拮抗剂活性的化合物
公开(公告)号：WO2005040112A1
公开(公告)日：2005-05-06
申请号：PCT/GB2004/004337
申请日：2004-10-13
申请人： OXAGEN LIMITED , MIDDLEMISS, David , ASHTON, Mark, Richard , BOYD, Edward, Andrew , BROOKFIELD, Frederick, Arthur , ARMER, Richard, Edward
发明人： MIDDLEMISS, David , ASHTON, Mark, Richard , BOYD, Edward, Andrew , BROOKFIELD, Frederick, Arthur , ARMER, Richard, Edward
IPC分类号： C07D209/18
CPC分类号： C07D403/12 , C07D209/18
摘要： Compounds of general formula (I); wherein R 1 , R 2 , R 3 and R 4 are independently hydrogen, halo, -C 1 -C 6 alkyl, -O(C 1 -C 6 alkyl), -C 1 -C 6 alkyl(C 3 -C 7 cycloalkyl), -CON(R 9 ) 2 , -SOR 9 , -S0 2 R 9 . -S0 2 N(R 9 ) 2 , -N(R 9 ) 2 , -NR 9 OR 9 , -C0 2 R 9 , COR 9 , -SR 9 , -OH, -N0 2 or -CN; each R 9 independently hydrogen or C 1 -C 6 alkyl; R 5 and R 6 are each independently hydrogen, or C 1 -C 6 alkyl or together with the carbon atom to which they are attached form a C 3 -C 7 cycloalkyl. group; R 7 is hydrogen or C 1 -C 6 alkyl; R 8 is C 1 -C 6 alkyl, C 2 -C 6 alkenyl, C 2 -C 6 alkynyl or an aromatic moiety, any of which may optionally be substituted with one or more substituents selected from halo, -SOR 13 -S0 2 R 13 , -R 14 , -OR 14 , -CON(R 14 )2 -SOR 14 , -S0 2 R 14 , -S0 2 N(R 14 ) -SO 2 N(R 14 ) 2 , -N(R 14 )2, NR 14 COR 14 , -CO 2 R 14 , COR 14 , -SR 14 , -N0 2 or -CN; wherein R 13 is a 5 to 7 membered heterocyclic ring; and each R 14 is independently hydrogen, alkyl or aryl, the aryl being optionally substituted by -R 9 , -OR 9 , -CON(R 9 ) 2 , -SOR 9 -S0 2 R 9 , -S0 2 N(R 9 ) 2 , -N(R 9 ) 2 , NR9COR 9 , -C0 2 R 9 , -COR 9 , -SR 9 , halo, -N0 2 or -CN; wherein R 9 is as defined above; provided that when R 1 , R 3 and R 4 are hydrogen and R 2 is hydrogen, halogen or -O(C 1 -C 6 )alkyl, R 8 is not unsubstituted phenyl or phenyl substituted by halo, C 1 -C 6 alkyl, -O(C 1 -C 6 )alkyl, -S(C 1 -C 6 )alkyl or -CO(C 1 -C 6 )alkyl; or pharmaceutically acceptable salts, hydrates, solvates, compexes or prodrugs therof are useful in 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R 1，R 2，R 3和R 4独立地是氢，卤素，-C 1 -C 6烷基，-O（C 1 -C 6烷基），-C 1 -C 6烷基（C 3 -C 7 环烷基），-CON（R 9）2，-SOR 9，-SO 2 R 9。 -SO 2 N（R 9）2，-N（R 9）2，-NR 9 OR 9，-CO 2 R 9，COR 9，-SR 9，-OH， -NO 2或-CN; 每个R 9独立地是氢或C 1 -C 6烷基; R 5和R 6各自独立地为氢或C 1 -C 6烷基，或与它们所连接的碳原子一起形成C 3 -C 7环烷基。组; R 7是氢或C 1 -C 6烷基; R 8是C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基或芳族部分，其中任何一个可任选地被一个或多个选自卤素，-SOR 13 -SO 2 R 13，，-R 14，-OR 14，-CON（R 14）2 -SOR 14，-SO 2 R 14，-SO 2 N（R 14）-SO 2 N（R 14）2，-N（R COR 14，-C 14 R 14，COR 14，-SR 14，-NO 2或-CN; 其中R 13为5至7元杂环; 并且每个R 14独立地为氢，烷基或芳基，芳基任选被-R 9，-OR 9，-CON（R 9）2，-SOR 9 - （R 9）2，-N（R 9）2，NR 9 COR 9，-CO 2 R 9，-COR 9，-SR 9，卤素，-NO 2 或-CN; 其中R 9如上所定义; 条件是当R 1，R 3和R 4为氢且R 2为氢，卤素或-O（C 1 -C 6）烷基时，R 8为未取代的苯基或被卤素，C 1 -C 6烷基，-O（C 1 -C 6）烷基，-S（C 1 -C 6）烷基或-CO（C 1 -C 6）烷基; 或其药学上可接受的盐，水合物，溶剂合物，混合物或前药可用于治疗过敏性疾病如哮喘，过敏性鼻炎和特应性皮炎。

3. 发明申请

WO2005121141A1 PYRROLOPYRIDINE DERIVATIVES AND USE THEREOF FOR TREATING DISEASES MEDIATED BY PROSTAGLANDIN D2 (PGD2) 审中-公开
标题翻译：吡咯啉衍生物及其用于治疗PROSTAGLANDIN D2（PGD2）介导的疾病的用途
公开(公告)号：WO2005121141A1
公开(公告)日：2005-12-22
申请号：PCT/GB2005/002242
申请日：2005-06-07
申请人： OXAGEN LIMITED , ARMER, Richard, Edward , BOYD, Edward, Andrew , BROOKFIELD, Frederick, Arthur
发明人： ARMER, Richard, Edward , BOYD, Edward, Andrew , BROOKFIELD, Frederick, Arthur
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Compounds of formula (Ia) or (Ib): or pharmaceutically acceptable salts, hydrates, solvates, complexes or prodrugs thereof are useful in the treatment of allergic diseases such as asthma, allergic rhinitis and atopic dermatitis.
摘要翻译：式（Ia）或（Ib）化合物或其药学上可接受的盐，水合物，溶剂化物，复合物或前药可用于治疗过敏性疾病如哮喘，过敏性鼻炎和特应性皮炎。

4. 发明申请

WO2006095183A1 1-ACETIC ACID-INDOLE DERIVATIVES WITH PGD2 ANTAGONIST ACTIVITY 审中-公开
标题翻译：具有PGD2拮抗剂活性的1-乙酸内酯衍生物
公开(公告)号：WO2006095183A1
公开(公告)日：2006-09-14
申请号：PCT/GB2006/000851
申请日：2006-03-10
申请人： OXAGEN LIMITED , ARMER, Richard, Edward , BOYD, Edward, Andrew , HAY, Philip, Andrew
发明人： ARMER, Richard, Edward , BOYD, Edward, Andrew , HAY, Philip, Andrew
IPC分类号： C07D209/30 , C07D209/42 , A61K31/405 , A61P11/00 , A61P37/00
CPC分类号： C07D403/06
摘要： Compounds of general formula: (I) wherein R 1 is halo or cyano; R 2 is C 1 -C 4 alkyl; and R 3 is phenyl substituted with one or more substituents chosen from C 1 -C 6 alkyl, halo or -SO 2 (C 1 -C 6 alkyl); or a pharmaceutically acceptable salt, hydrate, solvate, complex or prodrug thereof; are useful in the treatment of diseases and conditions mediated by the action of PGD 2 at the CRTH2 receptor.
摘要翻译：通式（I）的化合物，其中R 1是卤素或氰基; R 2是C 1 -C 4烷基; R 2是C 1 -C 4烷基; R 3是被一个或多个选自C 1 -C 6烷基，卤素或-SO 2的取代基取代的苯基，（C 1 -C 6烷基）; 或其药学上可接受的盐，水合物，溶剂化物，复合物或前药; 可用于治疗由CRD2受体上的PGD 2 N 2的作用介导的疾病和病症。

5. 发明申请

WO2009093029A1 COMPOUNDS HAVING CRTH2 ANTAGONIST ACTIVITY 审中-公开
标题翻译：具有CRTH2拮抗剂活性的化合物
公开(公告)号：WO2009093029A1
公开(公告)日：2009-07-30
申请号：PCT/GB2009/000175
申请日：2009-01-22
申请人： OXAGEN LIMITED , ARMER, Richard, Edward , MAILLOL, Carole, Eliane, Andrée , DORGAN, Colin, Richard , WYNNE, Graham, Michael , VILE, Julia
发明人： ARMER, Richard, Edward , MAILLOL, Carole, Eliane, Andrée , DORGAN, Colin, Richard , WYNNE, Graham, Michael , VILE, Julia
IPC分类号： C07D209/10 , A61K31/404 , A61P11/06 , A61P17/06
CPC分类号： C07D209/10
摘要： Compounds of general formula (I): wherein W is chloro or fluoro; Z is a group SO 2 R 1 ; wherein R 1 is -C 3 -C 8 cycloalkyl or heterocyclyl optionally substituted with one or more substituents chosen from halo, -CN, -C 1 -C 6 alkyl, -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 ) P OR 2 , and - O(CH 2 ) p O(CH 2 ) q OR 2 wherein each R 2 is independently hydrogen, -C i -C 6 alkyl, -C 3 -C 8 cycloalkyl, aryl or heteroaryl; each R 3 is independently, -C 1 -C 6 alkyl, -C 3 -C 8 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。

6. 发明申请

WO2009093026A1 COMPOUNDS HAVING CRTH2 ANTAGONIST ACTIVITY 审中-公开
标题翻译：具有CRTH2拮抗剂活性的化合物
公开(公告)号：WO2009093026A1
公开(公告)日：2009-07-30
申请号：PCT/GB2009/000171
申请日：2009-01-22
申请人： OXAGEN LIMITED , ARMER, Richard, Edward , WYNNE, Graham, Michael
发明人： ARMER, Richard, Edward , WYNNE, Graham, Michael
IPC分类号： C07D209/10 , A61K31/404 , A61P11/06 , A61P17/06
CPC分类号： C07D209/10
摘要： Compounds of general formula (I) W is chloro or fluoro; Z is a -SO 2 YR 1 group wherein R 1 is C 3 -C 8 heterocyclyl, aryl or heteroaryl any of which may optionally be substituted with one or more substituents selected from halo, -CN, -C 1 -C 6 alkyl, -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 ) P OR 2 , and -O(CH 2 ) p O(CH 2 ) q OR 2 wherein each R 2 is independently hydrogen, -C 1 -C 6 alkyl, -C 3 -C 8 cycloalkyl, aryl or heteroaryl; each R 3 is independently, -C 1 -C 6 alkyl, -C 3 -C 8 cycloalkyl, aryl or heteroaryl; p and q are each independently an integer from 1 to 3; Y is a straight or branched C 1 -C 4 alkylene chain; 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W是氯或氟; Z是-SO 2 YR1基团，其中R 1是C 3 -C 8杂环基，芳基或杂芳基，其中任何一个可以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））qOR 2，其中每个R 2独立地是氢，-C 1 -C 6烷基，-C 3 -C 8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; Y是直链或支链C 1 -C 4亚烷基链; 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. 发明申请

WO2009090414A1 COMPOUNDS HAVING CRTH2 ANTAGONIST ACTIVITY 审中-公开
标题翻译：具有CRTH2拮抗剂活性的化合物
公开(公告)号：WO2009090414A1
公开(公告)日：2009-07-23
申请号：PCT/GB2009/000142
申请日：2009-01-19
申请人： OXAGEN LIMITED , ARMER, Richard, Edward , PETTIPHER, Eric, Roy , WHITTAKER, Mark , WYNNE, Graham, Michael , VILE, Julia , SCHROER, Frank
发明人： ARMER, Richard, Edward , PETTIPHER, Eric, Roy , WHITTAKER, Mark , WYNNE, Graham, Michael , VILE, Julia , SCHROER, Frank
IPC分类号： C07D401/06 , A61K31/4439 , A61P29/00
CPC分类号： C07D401/06
摘要： Compounds of general formula (I) wherein W is chloro or fluoro; R 1 is phenyl optionally substituted with one or more substituents selected from halo, -CN, -C 1 -C 6 alkyl, -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 ) P OR 2, and -O(CH 2 ) p O(CH 2 ) q OR 2 wherein each R 2 is independently hydrogen, -C 1 -C 6 alkyl, -C 3 -C 8 cycloalkyl, aryl or heteroaryl; each R 3 is independently, -C 1 -C 6 alkyl, -C 3 -C 8 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; 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） -CO 2 R 2，-OR 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，-C 1 -C 6烷基，-C 3 -C 8 环烷基，芳基或杂芳基; 每个R 3独立地为-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。

8. 发明申请

WO2008012511A1 COMPOUNDS HAVING CRTH2 ANTAGONIST ACTIVITY 审中-公开
标题翻译：具有CRTH2拮抗剂活性的化合物
公开(公告)号：WO2008012511A1
公开(公告)日：2008-01-31
申请号：PCT/GB2007/002761
申请日：2007-07-20
申请人： OXAGEN LIMITED , ARMER, Richard, Edward , WYNNE, Graham, Michael
发明人： ARMER, Richard, Edward , WYNNE, Graham, Michael
IPC分类号： C07D209/10 , A61K31/405
CPC分类号： C07D407/10
摘要： Compounds of general formula (I) wherein R is phenyl optionally substituted with one or more halo substituents ; 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R是任选被一个或多个卤素取代基取代的苯基; 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. 发明申请

WO2009133387A1 INDOLE- 3 -GLYOXYLAMIDE DERIVATIVES FOR USE AS CALCIUM ION CHANNEL MODULATORS 审中-公开
标题翻译：用作钙离子通道调节剂的吲哚-3-甲氧基酰胺衍生物
公开(公告)号：WO2009133387A1
公开(公告)日：2009-11-05
申请号：PCT/GB2009/050422
申请日：2009-04-24
申请人： LECTUS THERAPEUTICS LIMITED , KHAN, Nawaz, Mohammed , BURCKHARDT, Svenja , CANSFIELD, Julie, Elaine , BOFFEY, Raymond, John , ARMER, Richard, Edward , VO, Ngoc-Tri
发明人： KHAN, Nawaz, Mohammed , BURCKHARDT, Svenja , CANSFIELD, Julie, Elaine , BOFFEY, Raymond, John , ARMER, Richard, Edward , VO, Ngoc-Tri
IPC分类号： C07D209/12 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12 , A61K31/404 , A61P13/00
CPC分类号： C07D209/12 , C07D401/12 , C07D403/12 , C07D405/12 , C07D413/12
摘要： Compounds of formula (I) are of use in treating a range of conditions, including pain.
摘要翻译：式（I）化合物可用于治疗一系列病症，包括疼痛。

10. 发明公开

EP2240444A1 COMPOUNDS HAVING CRTH2 ANTAGONIST ACTIVITY 审中-公开
标题翻译：具有CRTH2拮抗剂活性的化合物
公开(公告)号：EP2240444A1
公开(公告)日：2010-10-20
申请号：EP09704001.8
申请日：2009-01-22
申请人： Oxagen Limited
发明人： ARMER, Richard, Edward , MAILLOL, Carole, Eliane, Andrée , DORGAN, Colin, Richard , WYNNE, Graham, Michael , VILE, Julia
IPC分类号： C07D209/10 , A61K31/404 , A61P11/06 , A61P17/06
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)pO(CH2)qOR2 wherein each R2 is independently hydrogen, -Ci-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，（O）R3，-CO2R2，-CONR2R3，-NO2，-OR2，-SR2，-O（CH2）POR2和-O（CH2）pO（CH2）qOR2，其中每个R2独立地为氢， C6烷基，-C3-C8环烷基，芳基或杂芳基; 每个R 3独立地为-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; 及其药学上可接受的盐，水合物，溶剂化物，复合物或前药可用于可口服给药的组合物，用于治疗变应性疾病，如哮喘，变应性鼻炎和特应性皮炎。

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