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1. 发明申请

WO2011131741A1 HETEROCYCLIC CARBOXYLIC ACID AMIDES AS PDK1 INIHIBITORS 审中-公开
标题翻译：作为PDK1抑制剂的杂环羧酸酰胺
公开(公告)号：WO2011131741A1
公开(公告)日：2011-10-27
申请号：PCT/EP2011/056368
申请日：2011-04-20
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , ENGELHARDT, Harald , KOFINK, Christiane , MCCONNELL, Darryl
发明人： ENGELHARDT, Harald , KOFINK, Christiane , MCCONNELL, Darryl
IPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , A61K31/517 , A61K31/513 , A61K31/497 , A61K31/501 , A61K31/498 , A61K31/4709 , A61P35/00
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要： The present invention encompasses compounds of general formula (1) wherein the groups R 1 to R 4 , Q a , Q b , Q H , L and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.
摘要翻译：本发明包括通式（1）的化合物，其中基团R1至R4，Qa，Qb，QH，L和n如权利要求1中所定义，其适用于治疗以细胞增殖过度或异常为特征的疾病，含有这些化合物的药物制剂及其作为药物的用途。

2. 发明申请

WO2009112565A1 THIAZOLYL-DIHYDRO-INDAZOLES 审中-公开
标题翻译：噻唑基-1,3-二氢吲唑
公开(公告)号：WO2009112565A1
公开(公告)日：2009-09-17
申请号：PCT/EP2009/052959
申请日：2009-03-13
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , McCONNELL, Darryl , IMPAGNATIELLO, Maria , KESSLER, Dirk , KRAEMER, Oliver , SCHNEIDER, Siegfried , VAN DER VEEN, Lars , WEYER-CZERNILOFSKY, Ulrike , WUNBERG, Tobias
发明人： McCONNELL, Darryl , IMPAGNATIELLO, Maria , KESSLER, Dirk , KRAEMER, Oliver , SCHNEIDER, Siegfried , VAN DER VEEN, Lars , WEYER-CZERNILOFSKY, Ulrike , WUNBERG, Tobias
IPC分类号： C07D513/04 , A61K31/429 , A61P35/00
CPC分类号： C07D513/04
摘要： The present invention encompasses compounds of general formula (1) wherein R1 to R3 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.
摘要翻译：本发明包括通式（1）的化合物，其中R 1至R 3如权利要求1中所定义，其适用于治疗以细胞增殖过度或异常为特征的疾病，以及其用于制备具有上述特征的药物的用途，上述属性。

3. 发明申请

WO2006040281A1 THIAZOLYL-DIHYDRO-INDAZOLE 审中-公开
标题翻译：噻唑基二氢吲唑
公开(公告)号：WO2006040281A1
公开(公告)日：2006-04-20
申请号：PCT/EP2005/055021
申请日：2005-10-05
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , BOEHRINGER INGELHEIM PHARMA GmbH & Co. KG , BETZEMEIER, Bodo , BRANDL, Trixi , BREITFELDER, Steffen , BRUECKNER, Ralph , GERSTBERGER, Thomas , GMACHL, Michael , GRAUERT, Matthias , HILBERG, Frank , HOENKE, Christoph , HOFFMANN, Matthias , IMPAGNATIELLO, Maria , KESSLER, Dirk , KLEIN, Christian , KRIST, Bernd , MAIER, Udo , MCCONNELL, Darryl , REITHER, Charlotte , SCHEUERER, Stefan , SCHOOP, Andreas , SCHWEIFER, Norbert , SIMON, Oliver , STEEGMAIER, Martin , STEURER, Steffen , WAIZENEGGER, Irene , WEYER-CZERNILOFSKY, Ulrike , ZOEPHEL, Andreas
发明人： BETZEMEIER, Bodo , BRANDL, Trixi , BREITFELDER, Steffen , BRUECKNER, Ralph , GERSTBERGER, Thomas , GMACHL, Michael , GRAUERT, Matthias , HILBERG, Frank , HOENKE, Christoph , HOFFMANN, Matthias , IMPAGNATIELLO, Maria , KESSLER, Dirk , KLEIN, Christian , KRIST, Bernd , MAIER, Udo , MCCONNELL, Darryl , REITHER, Charlotte , SCHEUERER, Stefan , SCHOOP, Andreas , SCHWEIFER, Norbert , SIMON, Oliver , STEEGMAIER, Martin , STEURER, Steffen , WAIZENEGGER, Irene , WEYER-CZERNILOFSKY, Ulrike , ZOEPHEL, Andreas
IPC分类号： C07D513/04 , C07D417/06 , C07D277/82 , A61K31/429 , A61P35/00
CPC分类号： C07D513/04 , C07D277/82 , C07D277/84 , C07D417/06
摘要： Die vorliegende Erfindung umfasst Verbindungen der allgemeinen Formel (1) worin R1 bis R3 wie in Anspruch 1 definiert sind, welche zur Behandlung von Krankheiten, die durch exzessive oder anomale Zellproliferation charakterisiert sind, geeignet sind, sowie deren Verwendung zur Herstellung eines Arzneimittels mit den vorstehend genannten Eigenschaften.
摘要翻译：本发明包括通式（1）化合物其中R 1至R 3如权利要求1中所定义，其适合于治疗疾病为特征的过度或异常细胞增殖，以及它们对于具有上述制备的药物中的用途上述特性。

4. 发明申请

WO2010007114A3 HETEROCYCLYL CARBONIC ACID AMIDES AS ANTIPROLIFERATIVE AGENTS, PDKL INHIBITORS 审中-公开
标题翻译：作为抗增生剂的间苯二酚类碳酸钠，PDKL抑制剂
公开(公告)号：WO2010007114A3
公开(公告)日：2010-03-11
申请号：PCT/EP2009059112
申请日：2009-07-15
申请人： BOEHRINGER INGELHEIM INT , ENGELHARDT HARALD , BOEHMELT GUIDO , KOFINK CHRISTIANE , KUHN DANIEL , MCCONNELL DARRYL , STADTMUELLER HEINZ
发明人： ENGELHARDT HARALD , BOEHMELT GUIDO , KOFINK CHRISTIANE , KUHN DANIEL , MCCONNELL DARRYL , STADTMUELLER HEINZ
IPC分类号： C07D213/64 , A61K31/497 , A61P35/00 , C07D401/14 , C07D403/14 , C07D471/04
CPC分类号： C07D471/04 , C07D213/64 , C07D401/14 , C07D403/14
摘要： The present invention encompasses compounds of general formula (1) wherein the units W, A, L, Qa and QH are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use as medicaments having the above-mentioned properties.
摘要翻译：本发明包括通式（1）的化合物，其中单元W，A，L，Qa和QH如权利要求1中所定义，其适用于治疗以细胞增殖过度或异常为特征的疾病，其用途为具有上述特性的药物。

5. 发明申请

WO02051410A2 PHENYLTHIAZOLE AND THIAZOLINE DERIVATIVES AND THEIR USE AS ANTIPARASITICS 审中-公开
标题翻译：苯并噻唑衍生物及其作为抗菌剂的用途
公开(公告)号：WO02051410A2
公开(公告)日：2002-07-04
申请号：PCT/EP0115119
申请日：2001-12-19
申请人： AKZO NOBEL NV , FRUECHTEL JOERG , KOCH SANDRA , NEWTON TREVOR , MICULKA CHRISTIAN , MCCONNELL DARRYL , HOFMANN JOACHIM
发明人： FRUECHTEL JOERG , KOCH SANDRA , NEWTON TREVOR , MICULKA CHRISTIAN , MCCONNELL DARRYL , HOFMANN JOACHIM
IPC分类号： A61K31/351 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/4725 , A61K31/496 , A61K31/517 , A61K45/06 , A61P33/00 , A61P33/02 , C07D277/42 , C07D417/12
CPC分类号： C07D417/12 , A61K31/351 , A61K31/426 , A61K31/427 , A61K31/4439 , A61K31/4725 , A61K31/496 , A61K31/517 , A61K45/06 , C07D277/42 , A61K2300/00
摘要： The present invention provides a new class of antiparatisitcs. The compounds found with the present invention are substituted thiazole- and thiazoline derivatives. The present invention is based on the discovery that such compounds have been found to have antiparasitic activity. The present invention relates to 4-phenyl thiazole derivatives of the following general formula (I): X in formula (I) may be N-R or a bond. R in formula (I) may be (1-8C)alkyl, (2-8C)alkenyl, (2-8C)alkynyl, (3-8C)cycloalkyl, (2-7C)heterocycloalkyl, (6-14C)aryl, (3-13C)heteroaryl, (6-14C)aryl(1-8C)alkyl or (3-13C)heteroaryl(1-8C)alkyl. R in formula (I) may be SO2NR R , CONR R or NR R R and R in formula (I) may independently be selected from H, halogen, (1-8C)alkyl, hydroxy, (1-8) alkoxy, cyano, nitro, (1-8C) alkoxycarbonyl, (1-8C)(di)alkylamino and (6-14C)(di)arylamino, or R and R are joined together in a 5-7 membered carbocyclic or heterocyclic ring. R in formula (I) may be a halogen atom, (1-8C)alky, hydroxy, (1-8C)alkoxy, cyano, nitro, (1-8C)alkoxycarbonyl, (1-8C)(di)alkylamino or (6-14C)(di)arylamino. "n" may be 0-3. R in formula (I) may be H or (1-8C)alkyl, (2-8C)alkenyl, (2-8C)alkynyl, (3-8C)cycloalkyl, (2-7C)heterocycloalkyl, (6-14C)aryl, (3-13C)heteroaryl, (6-14C)aryl(1-8C)alkyl or (3-13C)heteroaryl(1-8C)alkyl. R and R in formula (I) may independently be selected from H, (1-8C)alkyl, (2-8C)alkenyl, (2-8C)alkynyl, (3-8C)cycloalkyl, (2-7C)heterocycloalkyl, (6-14C)aryl, (3-13C)heteroaryl, (6-14C)aryl(1-8C)alkyl and (3-13C)heteroaryl(1-8C)alkyl, or R and R are joined together in a (2-7C) heterocycloalkyl ring.
摘要翻译：本发明提供了一类新的反分类法。用本发明发现的化合物是取代的噻唑和噻唑啉衍生物。本发明是基于这样的发现，已经发现这些化合物具有抗寄生虫活性。本发明涉及以下通式（I）的4-苯基噻唑衍生物：式（I）中的X可以是N-R 6或键。式（I）中的R 1可以是（1-8C）烷基，（2-8C）烯基，（2-8C）炔基，（3-8C）环烷基，（2-7C）杂环烷基，（6-14C ）芳基，（3-13C）杂芳基，（6-14C）芳基（1-8C）烷基或（3-13C）杂芳基（1-8C）烷基。式（I）中的R 2可以是式（I）中的SO 2 NR 7 R 8，CONR 7 R 8或NR 7 R 8 R 3和R 4 可以独立地选自H，卤素，（1-8C）烷基，羟基，（1-8）烷氧基，氰基，硝基，（1-8C）烷氧基羰基，（1-8C）（二）烷基氨基和（6- 14C）（二）芳基氨基或R 3和R 4在5-7元碳环或杂环中连接在一起。式（I）中的R 5可以是卤素原子，（1-8C）烷基，羟基，（1-8C）烷氧基，氰基，硝基，（1-8C）烷氧基羰基，（1-8C）（二）（6-14C）（二）芳基氨基。 “n”可以是0-3。式（I）中的R 6可以是H或（1-8C）烷基，（2-8C）烯基，（2-8C）炔基，（3-8C）环烷基，（2-7C）杂环烷基，（6 -14C）芳基，（3-13C）杂芳基，（6-14C）芳基（1-8C）烷基或（3-13C）杂芳基（1-8C）烷基。式（I）中的R 7和R 8可以独立地选自H，（1-8C）烷基，（2-8C）烯基，（2-8C）炔基，（3-8C）环烷基，（（6-14C）芳基，（3-13C）杂芳基，（6-14C）芳基（1-8C）烷基和（3-13C）杂芳基（1-8C）烷基或R 7 >和R 8连接在一起（2-7C）杂环烷基环。

6. 发明申请

WO2011144622A1 1H - IMIDAZO [4, 5 - C] QUINOLINES 审中-公开
标题翻译： 1H-咪唑并[4,5-C]喹啉
公开(公告)号：WO2011144622A1
公开(公告)日：2011-11-24
申请号：PCT/EP2011/057985
申请日：2011-05-17
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , McCONNELL, Darryl , ENGELHARDT, Harald , KOFINK, Christiane
发明人： McCONNELL, Darryl , ENGELHARDT, Harald , KOFINK, Christiane
IPC分类号： C07D471/04 , A61K31/4745 , A61K31/497 , A61K31/501 , A61K31/506
CPC分类号： C07D471/04 , A61K31/444 , A61K31/4545 , A61K31/501 , A61K31/513 , A61K45/06
摘要： The present invention encompasses compounds of general formula (1), wherein the groups R 1 to R 7 , Q a , Q b , L, n and m are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations containing such compounds and their use as medicaments.
摘要翻译：本发明包括通式（1）的化合物，其中R1至R7，Qa，Qb，L，n和m基团如权利要求1中所定义，其适用于治疗以细胞增殖过度或异常为特征的疾病，含有这些化合物的药物制剂及其作为药物的用途。

7. 发明申请

WO2007113246A1 THIAZOLYLDIHYDROINDAZOL-DERIVATE ALS PROTEINKINASE- INHIBITOREN 审中-公开
标题翻译： THIAZOLYLDIHYDROINDAZOL衍生物作为蛋白激酶抑制剂
公开(公告)号：WO2007113246A1
公开(公告)日：2007-10-11
申请号：PCT/EP2007/053093
申请日：2007-03-30
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , MCCONNELL, Darryl , BETZEMEIER, Bodo , GERSTBERGER, Thomas , IMPAGNATIELLO, Maria , STEURER, Steffen , VAN DER VEEN, Lars , WEYER-CZERNILOFSKY, Ulrike
发明人： MCCONNELL, Darryl , BETZEMEIER, Bodo , GERSTBERGER, Thomas , IMPAGNATIELLO, Maria , STEURER, Steffen , VAN DER VEEN, Lars , WEYER-CZERNILOFSKY, Ulrike
IPC分类号： C07D513/04 , A61K31/41 , A61P35/00
CPC分类号： C07D513/04
摘要： Die vorliegende Erfindung umfasst Verbindungen der allgemeinen Formel (1) worin R 1 bis R 6 wie in Anspruch 1 definiert sind, welche zur Behandlung von Krankheiten, die durch exzessive oder anomale Zellproliferation charakterisiert sind, geeignet sind, sowie deren Verwendung zur Herstellung eines Arzneimittels mit den vorstehend genannten Eigenschaften.
摘要翻译：本发明包括通式（1）化合物，其中R ^{1 被定义于R ^{6 如权利要求1，用于治疗疾病的特征在于过度或异常细胞增殖的的特征在于，是合适的，以及它们对于具有上述特性的药物的制备中使用。}}

8. 发明申请

WO2006064044A1 INDOLINONES AND THEIR USE AS ANTIPROLIFERATIVE AGENTS 审中-公开
标题翻译：吲哚啉酮及其作为抗增生剂的用途
公开(公告)号：WO2006064044A1
公开(公告)日：2006-06-22
申请号：PCT/EP2005/056821
申请日：2005-12-15
申请人： BOEHRINGER INGELHEIM INTERNATIONAL GMBH , BOEHRINGER INGELHEIM PHARMA GMBH & CO. KG , MCCONNELL, Darryl , WEYER-CZERNILOFSKY, Ulrike , IMPAGNATIELLO, Maria , STEURER, Steffen , BRUECKNER, Ralph , KRIST, Bernd , BETZEMEIER, Bodo , HILBERG, Frank , HECKEL, Armin , ROTH, Gerald Juergen , KLEY, Joerg , LEHMANN-LINTZ, Thorsten
发明人： MCCONNELL, Darryl , WEYER-CZERNILOFSKY, Ulrike , IMPAGNATIELLO, Maria , STEURER, Steffen , BRUECKNER, Ralph , KRIST, Bernd , BETZEMEIER, Bodo , HILBERG, Frank , HECKEL, Armin , ROTH, Gerald Juergen , KLEY, Joerg , LEHMANN-LINTZ, Thorsten
IPC分类号： C07D209/34 , C07D405/06 , C07D403/12 , C07D413/04 , C07D401/10 , C07D405/10 , C07D403/04 , C07D401/14 , C07D409/04 , C07D401/04 , A61K31/4523 , A61P35/00
CPC分类号： C07D409/04 , C07D209/34 , C07D401/04 , C07D401/10 , C07D401/14 , C07D403/04 , C07D403/12 , C07D405/06 , C07D405/10 , C07D413/04
摘要： The invention relates to indolinone compounds of formula (I), wherein Y and R 1 to R 8 are defined as in claim 1, which are suitable for the treatment of diseases characterized by excessive or abnormal cell proliferation and the use thereof for preparing a pharmaceutical composition.
摘要翻译：本发明涉及式（I）的吲哚满酮化合物，其中Y和R 1至R 8定义如权利要求1，其适用于治疗特征性疾病通过过度或异常的细胞增殖及其用于制备药物组合物的用途。

9. 发明申请

WO2003040135A1 DIMERIC COMPOUNDS AND THEIR USE AS ANTI-VIRAL AGENTS 审中-公开
标题翻译：二元化合物及其用作反病毒剂
公开(公告)号：WO2003040135A1
公开(公告)日：2003-05-15
申请号：PCT/AU2002/001524
申请日：2002-11-08
申请人： BIOTA SCIENTIFIC MANAGEMENT PTY LTD , DOWLE, Michael, D. , JIN, Betty , MACDONALD, Simon, J., F. , MASON, Andrew, McM , MCCONNELL, Darryl , NGUYEN, Van, T., T. , SHANAHAN, Stephen, E. , WU, Wen-Yang
发明人： DOWLE, Michael, D. , JIN, Betty , MACDONALD, Simon, J., F. , MASON, Andrew, McM , MCCONNELL, Darryl , NGUYEN, Van, T., T. , SHANAHAN, Stephen, E. , WU, Wen-Yang
IPC分类号： C07D407/12
CPC分类号： C07D309/28
摘要： The invention relates to compounds of general formula (I); in which R is an amino or guanidino group; R 2 is acetyl or trifluoroacetyl; X is CONH, SO 2 NH, NHCO or NHCONH; m is either 0 or 1; n is an integer from 2 to 6; q is an integer from 0 to 3; and Y is hydrogen or an aromatic substituent, or a pharmaceutically acceptable derivative thereof; methods for their preparation, pharmaceutical formulations containing them or their use in the prevention or treatment of a viral infection.
摘要翻译：本发明涉及通式（I）的化合物; 其中R是氨基或胍基; R 2是乙酰基或三氟乙酰基; X是CONH，SO2NH，NHCO或NHCONH; m为0或1; n为2-6的整数; q是0至3的整数; Y为氢或芳香族取代基，或其药学上可接受的衍生物; 其制备方法，含有它们的药物制剂或其在预防或治疗病毒感染中的用途。

10. 发明申请

WO2002051410A3 PHENYLTHIAZOLE AND THIAZOLINE DERIVATIVES AND THEIR USE AS ANTIPARASITICS 审中-公开
公开(公告)号：WO2002051410A3
公开(公告)日：2002-07-04
申请号：PCT/EP2001/015119
申请日：2001-12-19
申请人： AKZO NOBEL N.V. , FRÜCHTEL, Jörg , KOCH, Sandra , NEWTON, Trevor , MICULKA, Christian , MCCONNELL, Darryl , HOFMANN, Joachim
发明人： FRÜCHTEL, Jörg , KOCH, Sandra , NEWTON, Trevor , MICULKA, Christian , MCCONNELL, Darryl , HOFMANN, Joachim
IPC分类号： A61K31/426
摘要： The present invention provides a new class of antiparatisitcs. The compounds found with the present invention are substituted thiazole- and thiazoline derivatives. The present invention is based on the discovery that such compounds have been found to have antiparasitic activity. The present invention relates to 4-phenyl thiazole derivatives of the following general formula (I): X in formula (I) may be N-R 6 or a bond. R 1 in formula (I) may be (1-8C)alkyl, (2-8C)alkenyl, (2-8C)alkynyl, (3-8C)cycloalkyl, (2-7C)heterocycloalkyl, (6-14C)aryl, (3-13C)heteroaryl, (6-14C)aryl(1-8C)alkyl or (3-13C)heteroaryl(1-8C)alkyl. R 2 in formula (I) may be SO 2 NR 7 R 8 , CONR 7 R 8 or NR 7 R 8 R 3 and R 4 in formula (I) may independently be selected from H, halogen, (1-8C)alkyl, hydroxy, (1-8) alkoxy, cyano, nitro, (1-8C) alkoxycarbonyl, (1-8C)(di)alkylamino and (6-14C)(di)arylamino, or R 3 and R 4 are joined together in a 5-7 membered carbocyclic or heterocyclic ring. R 5 in formula (I) may be a halogen atom, (1-8C)alky, hydroxy, (1-8C)alkoxy, cyano, nitro, (1-8C)alkoxycarbonyl, (1-8C)(di)alkylamino or (6-14C)(di)arylamino. "n" may be 0-3. R 6 in formula (I) may be H or (1-8C)alkyl, (2-8C)alkenyl, (2-8C)alkynyl, (3-8C)cycloalkyl, (2-7C)heterocycloalkyl, (6-14C)aryl, (3-13C)heteroaryl, (6-14C)aryl(1-8C)alkyl or (3-13C)heteroaryl(1-8C)alkyl. R 7 and R 8 in formula (I) may independently be selected from H, (1-8C)alkyl, (2-8C)alkenyl, (2-8C)alkynyl, (3-8C)cycloalkyl, (2-7C)heterocycloalkyl, (6-14C)aryl, (3-13C)heteroaryl, (6-14C)aryl(1-8C)alkyl and (3-13C)heteroaryl(1-8C)alkyl, or R 7 and R 8 are joined together in a (2-7C) heterocycloalkyl ring.

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