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1. 发明申请

WO2010080357A1 SEROTONIN 5-HT2B RECEPTOR INHIBITORS 审中-公开
标题翻译： SEROTONIN 5-HT2B受体抑制剂
公开(公告)号：WO2010080357A1
公开(公告)日：2010-07-15
申请号：PCT/US2009/067865
申请日：2009-12-14
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , COGAN, Derek , MOSS, Neil , SARKO, Christopher Ronald , BAMFORD, Samantha Jayne , LOKE, Pui Leng , NAPIER, Spencer Charles, R. , TYE, Heather , WHITTAKER, Mark
发明人： COGAN, Derek , MOSS, Neil , SARKO, Christopher Ronald , BAMFORD, Samantha Jayne , LOKE, Pui Leng , NAPIER, Spencer Charles, R. , TYE, Heather , WHITTAKER, Mark
IPC分类号： C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D417/04 , A61K31/4178 , A61K31/4188 , A61P25/00
CPC分类号： C07D401/04 , C07D401/06 , C07D401/14 , C07D403/04 , C07D403/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： Disclosed are Serotonin 5-HT2B receptor inhibitors of the formula I. Also disclosed are methods of making and methods of using these compounds.
摘要翻译：公开了式I的5-羟色胺5-HT 2B受体抑制剂。还公开了制备方法和使用这些化合物的方法。

2. 发明申请

WO2009140089A2 SULFONE COMPOUNDS WHICH MODULATE THE CB2 RECEPTOR 审中-公开
标题翻译：调节CB2受体的SULFONE化合物
公开(公告)号：WO2009140089A2
公开(公告)日：2009-11-19
申请号：PCT/US2009/042665
申请日：2009-05-04
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG , HICKEY, Eugene, Richard , RIETHER, Doris , THOMSON, David, Smith , ZINDELL, Renee, M. , AMOUZEGH, Patricia , ERMANN, Monika , PALMER, Christopher, Francis , WHITTAKER, Mark
发明人： HICKEY, Eugene, Richard , RIETHER, Doris , THOMSON, David, Smith , ZINDELL, Renee, M. , AMOUZEGH, Patricia , ERMANN, Monika , PALMER, Christopher, Francis , WHITTAKER, Mark
IPC分类号： C07D271/10
CPC分类号： C07D413/04 , C07D271/06 , C07D403/04 , C07D405/14 , C07D413/14 , C07D417/04 , C07D417/14
摘要： Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
摘要翻译：公开了调节CB2受体的化合物。根据本发明的化合物与CB2受体结合并且是激动剂，并且可用于治疗炎症。作为激动剂的那些化合物另外可用于治疗疼痛。

3. 发明申请

WO2005095425A1 DITHIOPHOSPHATO-PLATINUM-COMPLEXES FOR THE TREATMENT OF CANCERS 审中-公开
标题翻译：用于治疗癌症的二磷脂 - 铂 - 复合物
公开(公告)号：WO2005095425A1
公开(公告)日：2005-10-13
申请号：PCT/GB2005/001251
申请日：2005-03-31
申请人： PHARMINOX LIMITED , LOWE, Anthony , WHITTAKER, Mark , DIETERICH, Petra , POLYWKA, Mario, Eugenio, Cosimino
发明人： LOWE, Anthony , WHITTAKER, Mark , DIETERICH, Petra , POLYWKA, Mario, Eugenio, Cosimino
IPC分类号： C07F15/00
CPC分类号： C07F15/0093 , A61K31/555
摘要： Complex of formulas: (I), (II) or (III): which are suitable for the treatment of tumors.
摘要翻译：式（I），（II）或（III）的配合物：适用于治疗肿瘤。

4. 发明申请

WO2010067067A1 COMPOUNDS FOR TREATING CANCER 审中-公开
标题翻译：化合物治疗癌症
公开(公告)号：WO2010067067A1
公开(公告)日：2010-06-17
申请号：PCT/GB2009/002848
申请日：2009-12-08
申请人： EVOTEC AG , EAST, Stephen, Peter , WHITTAKER, Mark , ICHIHARA, Osamu , KOTEY, Adrian, Kotei , BAMFORD, Jayne, Samantha
发明人： EAST, Stephen, Peter , WHITTAKER, Mark , ICHIHARA, Osamu , KOTEY, Adrian, Kotei , BAMFORD, Jayne, Samantha
IPC分类号： C07D235/06 , C07D235/12 , C07D401/06 , C07D407/06 , C07D417/06 , A61K31/4184 , A61P35/00
CPC分类号： C07D235/06 , C07D235/12 , C07D401/06 , C07D407/06 , C07D417/06
摘要： Compounds of general formula (I): wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X and Y are as defined herein are inhibitors of Bcl-2 and are useful for treating diseases characterised by abnormal cell growth and/or dysregulated apoptosis.
摘要翻译：通式（I）的化合物：其中R 1，R 2，R 3，R 4，R 5，R 6，X和Y如本文所定义，是Bcl-2的抑制剂，可用于治疗以异常细胞生长和/或失调凋亡为特征的疾病。

5. 发明申请

WO2004101506A1 GLYOXALASE INHIBITORS 审中-公开
标题翻译： GLYOXALASE抑制剂
公开(公告)号：WO2004101506A1
公开(公告)日：2004-11-25
申请号：PCT/GB2004/002101
申请日：2004-05-14
申请人： CHROMA THERAPEUTICS LIMITED , ASHTON, Mark , DAVIDSON, Alan , THOMAS, Russell , WHITTAKER, Mark
发明人： ASHTON, Mark , DAVIDSON, Alan , THOMAS, Russell , WHITTAKER, Mark
IPC分类号： C07C323/62
CPC分类号： C07D405/04 , A61K31/10 , A61K31/381 , A61K31/44 , A61K31/4436 , C07C323/62 , C07D213/85 , C07D217/26 , C07D409/04 , C07D409/14
摘要： This invention relates to compounds of formula (I) which are glyoxalase I inhibitors, pharmaceutical salts or compositions comprising such compounds, and the use of such compositions and compounds to treat various conditions alleviated by the inhibition of glyoxalase I. Wherein X is N or CH. R 2 is H, CF 3 ; or optionally substituted C 5-6 aryl, C 3-7 cycloalkyl, C 5-7 heterocyclyl. R 3 is H; or optionally substituted C 5-6 aryl, C 3-7 cycloalkyl, C 5-7 heterocyclyl. Alternatively R 2 and R 3 together form an optionally substituted C 3-4 alkylene group wherein L 3 and L 4 are single bonds thus forming a C 5-6 ring fused with the aromatic ring to which L 3 and L 4 are attached. L 3 and L 4 are independently selected from a single bond, optionally substituted C 1-4 alkylene, -L 9 YN(OH)C(=O)L 10 - and -L 9 C(=O)N(OH)YL 10 -, wherein L 9 and L 10 are independently selected from optionally substituted C 1-4 alkylene, C 5-6 arylene, C 1-4 alkylene-C 5-6 arylene and a single bond, wherein Y is NH or a single bond.
摘要翻译：本发明涉及作为乙二醛酶I抑制剂的式（I）化合物，包含这些化合物的药物盐或组合物，以及这些组合物和化合物用于治疗通过抑制乙二醛酶I减轻的各种病症的用途。其中X是N或CH 。 R 2是H，CF 3; 或任选取代的C 5-6芳基，C 3-7环烷基，C 5-7杂环基。 R 3为H; 或任选取代的C 5-6芳基，C 3-7环烷基，C 5-7杂环基。或者，R 2和R 3一起形成任选取代的C 3-4亚烷基，其中L 3和L 4是单键，从而形成与芳环稠合的C5-6环，其中L 3 >和L 4连接。 L 3和L 4独立地选自单键，任选取代的C 1-4亚烷基，-L 9 YN（OH）C（= O）L 10 - 和-L 9 C （= O）N（OH）YL 10 - ，其中L 9和L 10独立地选自任选取代的C 1-4亚烷基，C 5-6亚芳基，C 1-4亚烷基-C 5-6亚芳基和单键，其中Y是NH或单键。

6. 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。

7. 发明申请

WO2008142720A2 QUINAZOLIN-OXIME DERIVATIVES AS HSP90 INHIBITORS 审中-公开
标题翻译：喹诺酮衍生物作为HSP90抑制剂
公开(公告)号：WO2008142720A2
公开(公告)日：2008-11-27
申请号：PCT/IT2008/000326
申请日：2008-05-15
申请人： DAC SRL , COURTNEY, Stephen Martin , WHITTAKER, Mark , MATHER, Owen Clifford , YARNOLD, Christopher John , BARKER, Oliver Robin , MONTALBETTI, Christian Aldo Georges Napoleon , HESTERKAMP, Thomas , GARDINER, Mihaly Daniel
发明人： COURTNEY, Stephen Martin , WHITTAKER, Mark , MATHER, Owen Clifford , YARNOLD, Christopher John , BARKER, Oliver Robin , MONTALBETTI, Christian Aldo Georges Napoleon , HESTERKAMP, Thomas , GARDINER, Mihaly Daniel
CPC分类号： C07D239/84 , C07D401/04 , C07D403/10 , C07D405/04 , C07D409/04
摘要： Compounds of general formula (I); or a stereoisomers, tautomers, pharmaceutically acceptable salts, or prodrugs thereof, wherein R1, R2, R3, R4, R5, R6, R8 and R9 are as defined herein, are useful for the treatment of diseases and conditions which are mediated by excessive or inappropriate Hsp90 activity such as cancers, viral infection and inflammatory diseases or conditions.
摘要翻译：通式（I）的化合物; 或其立体异构体，互变异构体，药学上可接受的盐或前药，其中R 1，R 2，R 3，R 4，R 5，R 6，R 8和R 9如本文所定义，可用于治疗疾病和病症，不适当的Hsp90活动如癌症，病毒感染和炎性疾病或病症。

8. 发明申请

WO2004065372A1 TETRAZOLE-FUNCTIONALIZED AMINO ACIDS, THEIR PRODUCTION AND USE 审中-公开
标题翻译：四唑功能化氨基酸，其生产和使用
公开(公告)号：WO2004065372A1
公开(公告)日：2004-08-05
申请号：PCT/EP2004/000390
申请日：2004-01-20
申请人： MEDIGENE AKTIENGESELLSCHAFT , FUNK, Martin , KIRSCH, Thomas , RÖNICKE, Volker , LOPEZ-CALLE, Eloisa , SCHEEL, Andreas , WÖLCKE, Julian , SCHULZ, Astrid , KIRCHHOFF, Christian , GEMKOW, Mark , MÜLLER, Annett , KRAUSE, Ingo , WINKLER, Dirk , KLUMPP, Martin , UDDIN, Muhammed , BROWN, Christopher , MULLER, Christoph , ASHTON, Mark , WHITTAKER, Mark
发明人： FUNK, Martin , KIRSCH, Thomas , RÖNICKE, Volker , LOPEZ-CALLE, Eloisa , SCHEEL, Andreas , WÖLCKE, Julian , SCHULZ, Astrid , KIRCHHOFF, Christian , GEMKOW, Mark , MÜLLER, Annett , KRAUSE, Ingo , WINKLER, Dirk , KLUMPP, Martin , UDDIN, Muhammed , BROWN, Christopher , MULLER, Christoph , ASHTON, Mark , WHITTAKER, Mark
IPC分类号： C07D257/04
CPC分类号： C07D257/04
摘要： The present invention relates to novel tetrazole-functionalized amino acids of formula (I) and pharmaceutically acceptable salts thereof as well as their production and use.
摘要翻译：本发明涉及式（I）的新型四唑官能化氨基酸及其药学上可接受的盐及其生产和用途。

9. 发明申请

WO2004065350A1 TERTIARY AMINO ACIDS, THEIR PRODUCTION AND USE 审中-公开
标题翻译：临时氨基酸，其生产和使用
公开(公告)号：WO2004065350A1
公开(公告)日：2004-08-05
申请号：PCT/EP2004/000389
申请日：2004-01-20
申请人： MEDIGENE AKTIENGESELLSCHAFT , FUNK, Martin , KIRSCH, Thomas , RÖNICKE, Volker , LOPEZ-CALLE, Eloisa , SCHEEL, Andreas , WÖLCKE, Julian , SCHULZ, Astrid , KIRCHHOFF, Christian , GEMKOW, Mark , KRAUSE, Ingo , MÜLLER, Annett , WINKLER, Dirk , KLUMPP, Martin , UDDIN, Muhammed , BROWN, Christopher , MULLER, Christoph , ASHTON, Mark , WHITTAKER, Mark
发明人： FUNK, Martin , KIRSCH, Thomas , RÖNICKE, Volker , LOPEZ-CALLE, Eloisa , SCHEEL, Andreas , WÖLCKE, Julian , SCHULZ, Astrid , KIRCHHOFF, Christian , GEMKOW, Mark , KRAUSE, Ingo , MÜLLER, Annett , WINKLER, Dirk , KLUMPP, Martin , UDDIN, Muhammed , BROWN, Christopher , MULLER, Christoph , ASHTON, Mark , WHITTAKER, Mark
IPC分类号： C07C229/14
CPC分类号： C07C229/14 , C07C255/58
摘要： The present invention relates to novel tertiary amino acids and pharmaceutically acceptable salts thereof as well as their production and use.
摘要翻译：本发明涉及新型叔氨基酸及其药学上可接受的盐，以及它们的生产和用途。

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