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11. 发明申请

WO2009120094A2 SUBSTITUTED PYRIMIDINES AND TRIAZINES AND THEIR USE IN CANCER THERAPY 审中-公开
标题翻译：替代吡嘧啶和三氮唑及其在癌症治疗中的应用
公开(公告)号：WO2009120094A2
公开(公告)日：2009-10-01
申请号：PCT/NZ2009000038
申请日：2009-03-26
申请人： AUCKLAND UNISERVICES LTD , REWCASTLE GORDON WILLIAM , SHEPHERD PETER ROBIN , CHAUSSADE CLAIRE , DENNY WILLIAM ALEXANDER , GAMAGE SWARNALATHA AKURATIYA
发明人： REWCASTLE GORDON WILLIAM , SHEPHERD PETER ROBIN , CHAUSSADE CLAIRE , DENNY WILLIAM ALEXANDER , GAMAGE SWARNALATHA AKURATIYA
IPC分类号： C07D251/48 , A61K31/53 , A61P35/00 , C07D251/18 , C07D401/12 , C07D403/12 , C07D487/04
CPC分类号： C07D251/18 , C07D401/12 , C07D403/12 , C07D487/04
摘要： Provided herein are substituted pyrimidine and triazine derivatives, including bicyclic pyrimidine derivatives, their pharmaceutical compositions, their preparation, and their use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs. In one embodiment, the pyrimidine and triazine derivatives are morpholino-pyrimidine, morpholino-triazine, pyridyl-pyrimidine, and pyridyl-triazine derivatives which are selective irreversible inhibitors of the p110a isoform of PI3K.
摘要翻译：本文提供了取代的嘧啶和三嗪衍生物，包括双环嘧啶衍生物，它们的药物组合物，它们的制备及其用作癌症治疗的药物或药物，单独或与辐射和/或其它抗癌药物组合。在一个实施方案中，嘧啶和三嗪衍生物是作为PI3K的p110a同种型的选择性不可逆抑制剂的吗啉代 - 嘧啶，吗啉代 - 三嗪，吡啶基 - 嘧啶和吡啶基 - 三嗪衍生物。

12. 发明申请

WO2010110685A3 PYRIMIDINYL AND 1,3,5-TRIAZINYL BENZIMIDAZOLE SULFONAMIDES AND THEIR USE IN CANCER THERAPY 审中-公开
标题翻译：嘧啶基和1,3,5-三氮嗪基苯并咪唑磺酰胺及其在癌症治疗中的应用
公开(公告)号：WO2010110685A3
公开(公告)日：2011-05-05
申请号：PCT/NZ2010000060
申请日：2010-03-26
申请人： PATHWAY THERAPEUTICS INC , REWCASTLE GORDON WILLIAM , GAMAGE SWARNALATHA AKURATIYA , FLANAGAN JACK URQUHART , GIDDENS ANNA CLAIRE , TSANG KIT YEE
发明人： REWCASTLE GORDON WILLIAM , GAMAGE SWARNALATHA AKURATIYA , FLANAGAN JACK URQUHART , GIDDENS ANNA CLAIRE , TSANG KIT YEE
IPC分类号： C07D413/14 , A61K31/53 , A61P35/00 , C07D473/34 , C07D487/04 , C07D498/08
CPC分类号： C07D491/08 , A61K31/5355 , A61K31/541 , A61K45/06 , C07D403/04 , C07D403/14 , C07D413/14 , C07D473/34 , C07D487/04 , C07D498/08
摘要： Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides, e.g., compounds of Formulae (IA), (IB), and (IC), and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.
摘要翻译：本文提供嘧啶基和1,3,5-三嗪基苯并咪唑磺酰胺，例如式（IA），（IB）和（IC）的化合物及其药物组合物，制剂和用作癌症治疗的药剂或药物的用途，单独或与放射和/或其他抗癌药物组合。

13. 发明申请

WO2011005119A1 PYRIMIDINYL AND 1,3,5-TRIAZINYL BENZIMIDAZOLES AND THEIR USE IN CANCER THERAPY 审中-公开
标题翻译：吡嗪二酮和1,3,5-三嗪基苯并咪唑及其在癌症治疗中的应用
公开(公告)号：WO2011005119A1
公开(公告)日：2011-01-13
申请号：PCT/NZ2010/000139
申请日：2010-07-06
申请人： PATHWAY THERAPEUTICS LIMITED , REWCASTLE, Gordon, William , TSANG, Kit, Yee , GAMAGE, Swarnalatha, Akuratiya , GIDDENS, Anna, Claire
发明人： REWCASTLE, Gordon, William , TSANG, Kit, Yee , GAMAGE, Swarnalatha, Akuratiya , GIDDENS, Anna, Claire
IPC分类号： C07D401/14 , C07D403/04 , C07D403/14 , C07D487/04 , A61K31/53
CPC分类号： C07D487/04 , C07D401/14 , C07D403/04 , C07D403/14
摘要： Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazoles of Formula (I), (1A), (1B) and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.
摘要翻译：本文提供式（I），（1A），（1B）的嘧啶基和1,3,5-三嗪基苯并咪唑及其药物组合物，制剂和用作癌症治疗的药物或药物，单独或与辐射组合和/或其他抗癌药物。

14. 发明申请

WO2010110685A8 PYRIMIDINYL AND 1,3,5-TRIAZINYL BENZIMIDAZOLE SULFONAMIDES AND THEIR USE IN CANCER THERAPY 审中-公开
标题翻译：吡嗪二酮和1,3,5-三嗪基苯并咪唑磺酰胺及其在癌症治疗中的应用
公开(公告)号：WO2010110685A8
公开(公告)日：2010-11-18
申请号：PCT/NZ2010000060
申请日：2010-03-26
申请人： PATHWAY THERAPEUTICS LTD , REWCASTLE GORDON WILLIAM , GAMAGE SWARNALATHA AKURATIYA , FLANAGAN JACK URQUHART , GIDDENS ANNA CLAIRE , TSANG KIT YEE
发明人： REWCASTLE GORDON WILLIAM , GAMAGE SWARNALATHA AKURATIYA , FLANAGAN JACK URQUHART , GIDDENS ANNA CLAIRE , TSANG KIT YEE
IPC分类号： C07D413/14
CPC分类号： C07D491/08 , A61K31/5355 , A61K31/541 , A61K45/06 , C07D403/04 , C07D403/14 , C07D413/14 , C07D473/34 , C07D487/04 , C07D498/08
摘要： Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides, e.g., compounds of Formulae (IA), (IB), and (IC), and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.
摘要翻译：本文提供了嘧啶基和1,3,5-三嗪基苯并咪唑磺酰胺，例如式（IA），（IB）和（IC）的化合物及其药物组合物，制剂和用作癌症治疗的药剂或药物，单独或与辐射和/或其他抗癌药物组合。

15. 发明申请

WO2010110686A1 PYRIMIDINYL AND 1,3,5 TRIAZINYL BENZIMIDAZOLES AND THEIR USE IN CANCER THERAPY 审中-公开
标题翻译：吡嗪二酮和1,3,5-二苯乙烯苯并咪唑及其在癌症治疗中的应用
公开(公告)号：WO2010110686A1
公开(公告)日：2010-09-30
申请号：PCT/NZ2010/000061
申请日：2010-03-26
申请人： PATHWAY THERAPEUTICS LIMITED , REWCASTLE, Gordon, William , GAMAGE, Swarnalatha, Akuratiya
发明人： REWCASTLE, Gordon, William , GAMAGE, Swarnalatha, Akuratiya
IPC分类号： C07D413/14 , A61K31/53 , A61P35/00
CPC分类号： C07D413/14
摘要： Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazoles, and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.
摘要翻译：本文提供了嘧啶基和1,3,5-三嗪基苯并咪唑，以及它们的药物组合物，制剂和用作癌症治疗的药物或药物，单独或与辐射和/或其它抗癌药物组合。

16. 发明申请

WO2010110685A4 PYRIMIDINYL AND 1,3,5-TRIAZINYL BENZIMIDAZOLE SULFONAMIDES AND THEIR USE IN CANCER THERAPY 审中-公开
公开(公告)号：WO2010110685A4
公开(公告)日：2010-09-30
申请号：PCT/NZ2010/000060
申请日：2010-03-26
申请人： PATHWAY THERAPEUTICS, INC. , REWCASTLE, Gordon William , GAMAGE, Swarnalatha Akuratiya , FLANAGAN, Jack Urquhart , GIDDENS, Anna Claire , TSANG, Kit Yee
发明人： REWCASTLE, Gordon William , GAMAGE, Swarnalatha Akuratiya , FLANAGAN, Jack Urquhart , GIDDENS, Anna Claire , TSANG, Kit Yee
IPC分类号： C07D413/14 , C07D473/34 , C07D487/04 , C07D498/08 , A61K31/53 , A61P35/00
摘要： Provided herein are pyrimidinyl and 1,3,5-triazinyl benzimidazole sulfonamides, e.g. , compounds of Formulae (IA), (IB), and (IC), and their pharmaceutical compositions, preparation, and use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs.

17. 发明申请

WO1998017649A1 PROCESS FOR THE PREPARATION OF N-[2-(DIMETHYLAMINO)ETHYL]ACRIDINE-4-CARBOXAMIDE 审中-公开
标题翻译：制备N- [2-（二甲基氨基）乙基]亚胺-4-羧酰胺的方法
公开(公告)号：WO1998017649A1
公开(公告)日：1998-04-30
申请号：PCT/GB1997002884
申请日：1997-10-17
申请人： XENOVA LIMITED , DENNY, William, Alexander , GAMAGE, Swarnalatha, Akuratiya , SPICER, Julie, Ann , WRIGHT, Michael , HAYMAN, David, Frank
发明人： XENOVA LIMITED
IPC分类号： C07D219/04
CPC分类号： C07D219/04 , C07C227/18 , C07C229/58
摘要： A process for producing an acridine carboxamide of formula (I) wherein each of R , R , R and R , which may be the same or different, is hydrogen or an organic substituent, x is an integer of 1 to 6 and Y is N(R)2 wherein R is C1-C6 alkyl, or a pharmaceutically acceptable salt thereof, which process comprises: (a) cyclising a compound of formula (II) wherein R , R , R and R are as defined above and R is C1-C6 alkyl, aryl or aryl-C1-C3 alkyl, by treatment with a Lewis acid in an organic solvent, to obtain a compound of formula (III) wherein R , R , R , R and R are as defined above; (b) treating either (i) the compound of formula (III) as defined above with a primary alkylamine of the formula (IV): NH2(CH2)xY, wherein x and Y are as defined above; or (ii) the carboxylic acid, obtainable by hydrolysing the compound of formula (III) as defined above under basic conditions, with a primary alkyl amine of formula the (IV) as defined above in the presence of a suitable coupling agent to obtain a compound of formula (I) as defined above; and (c) if desired, converting one compound of formula (I) into another compound of formula (I), and/or converting a compound of formula (I) into a pharmaceutically acceptable salt thereof. The aldehyde of formula (II) is obtained by oxidation of the corresponding alcohol, which in turn is produced by mild reduction of the corresponding carboxylic acid via an immidazolide intermediate.
摘要翻译：制备式（I）的吖啶甲酰胺的方法，其中R 1，R 2，R 5和R 6各自可以相同或不同，是氢或有机取代基， x是1至6的整数，Y是N（R）2，其中R是C 1 -C 6烷基或其药学上可接受的盐，该方法包括：（a）使式（II）的化合物环化，其中R 1 >，R 2，R 5和R 6如上所定义，R 3是C 1 -C 6烷基，芳基或芳基-C 1 -C 3烷基，通过在有机溶剂中用路易斯酸处理，得到其中R 1，R 2，R 3，R 5和R 6如上定义的式（III）化合物; （b）用式（IV）的伯烷基胺：NH 2（CH 2）x Y（其中x和Y如上定义）处理（i）如上定义的式（III）化合物; 或（ii）通过在碱性条件下水解上述式（III）化合物而得到的羧酸与式（IV）的伯烷基胺在合适的偶联剂存在下水解，得到如上定义的式（I）化合物; 和（c）如果需要，将一种式（I）化合物转化为另一种式（I）化合物，和/或将式（I）化合物转化为其药学上可接受的盐。通过氧化相应的醇获得式（II）的醛，其依次通过咪唑啉中间体温和还原相应的羧酸而产生。

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