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1. 发明申请

WO2012175991A1 FUSED PENTACYCLIC ANTI - PROLIFERATIVE COMPOUNDS 审中-公开
标题翻译： FUSED PENTACYCLIC ANTI - PROLIFERATIVE COMPOUNDS
公开(公告)号：WO2012175991A1
公开(公告)日：2012-12-27
申请号：PCT/GB2012/051467
申请日：2012-06-22
申请人： PHARMINOX LIMITED , COUSIN, David , FRIGERIO, Mark , HUMMERSONE, Marc Geoffery
发明人： COUSIN, David , FRIGERIO, Mark , HUMMERSONE, Marc Geoffery
IPC分类号： C07D491/06 , C07D495/06 , A61K31/436 , A61K31/4365 , A61P35/00
CPC分类号： C07D495/06 , C07D491/06
摘要： The present invention relates to novel compounds of formula (I) wherein X, Q, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , R 21 , R2 2 and R 23 are as defined herein. The compounds of formula (I) are inhibitors of telomerase enzyme function and are accordingly useful for the treatment cellular proliferation disorders, such as cancer.
摘要翻译：本发明涉及新的式（I）化合物，其中X，Q，R 1，R 2，R 3，R 4，R 5，R 6，R 7，R 8，R 21，R 22和R 23如本文所定义。式（I）化合物是端粒酶功能的抑制剂，因此可用于治疗细胞增殖紊乱，如癌症。

2. 发明申请

WO2012042265A1 NOVEL ACRIDINE DERIVATIVES 审中-公开
标题翻译：新型吡啶衍生物
公开(公告)号：WO2012042265A1
公开(公告)日：2012-04-05
申请号：PCT/GB2011/051845
申请日：2011-09-29
申请人： PHARMINOX LIMITED , HUMMERSONE, Marc Geoffery , COUSIN, David , FRIGERIO, Mark
发明人： HUMMERSONE, Marc Geoffery , COUSIN, David , FRIGERIO, Mark
IPC分类号： C07D491/04 , C07D495/04 , A61K31/4741 , A61K31/4743 , A61P35/00
CPC分类号： C07D495/04 , C07D491/04 , C07D491/052
摘要： The present invention relates to novel acridine derivatives of formula (I), or pharmaceutically acceptable salts thereof, which are inhibitors of the telomerase enzyme function. These compounds are useful for the treatment cellular proliferation disorders, such as cancer.
摘要翻译：本发明涉及作为端粒酶功能抑制剂的式（I）的新型吖啶衍生物或其药学上可接受的盐。这些化合物可用于治疗细胞增殖紊乱，例如癌症。

3. 发明申请

WO2009077741A2 3-SUBSTITUTED-4-OXO-3,4-DIHYDRO-IMIDAZO-[5,1-D][1,2,3,5-TETRAZINE-8-CARBOXYLIC ACID AMIDES AND THEIR USE 审中-公开
标题翻译： 3-取代-4-氧代-3,4-二氢-1H-咪唑并[5,1-D] [1,2,3,5-四唑-8-羧酸酰胺及其用途
公开(公告)号：WO2009077741A2
公开(公告)日：2009-06-25
申请号：PCT/GB2008/004140
申请日：2008-12-16
申请人： PHARMINOX LIMITED , STEVENS, Malcolm, Francis, Graham , COUSIN, David , JENNINGS, Sharon , MCCARROLL, Andrew, James , WILLIAMS, John, Gareth , HUMMERSONE, Marc, Geoffery , ZHANG, Jihong
发明人： STEVENS, Malcolm, Francis, Graham , COUSIN, David , JENNINGS, Sharon , MCCARROLL, Andrew, James , WILLIAMS, John, Gareth , HUMMERSONE, Marc, Geoffery , ZHANG, Jihong
IPC分类号： C07D487/04 , C07D519/00 , C07F7/10 , C07F9/141 , A61K31/395 , A61K31/4188 , A61P35/00
CPC分类号： C07D487/04 , C07D519/00 , C07F7/10 , C07F7/1856 , C07F9/6561
摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain 3-substituted-4-oxo-3,4-dihydro-imidazo[5,1-d][1,2,3,5]tetrazine-8-carboxylic acid amide (collectively referred to herein as 3TM compounds). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo , to inhibit cell proliferation, and in the treatment of proliferative disorders such as cancer, etc., and methods of preparing such compounds.
摘要翻译：本发明一般涉及治疗化合物领域，更具体地涉及某些3-取代-4-氧代-3,4-二氢 - 咪唑并[5,1-d] [1,2,3,5]四嗪 - 8-羧酸酰胺（本文统称为3TM化合物）。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内都用于抑制细胞增殖以及治疗增殖性疾病例如癌症等的用途，以及制备此类化合物。

4. 发明申请

WO2012085501A1 8 - SULFO - IMIDAZOTETRAZIN- 4 - ONE COMPOUNDS AND THEIR USE AS ANTICANCER DRUG 审中-公开
标题翻译： 8 - SULFO - 咪达唑他丁-4 - 一种化合物及其作为抗药剂的用途
公开(公告)号：WO2012085501A1
公开(公告)日：2012-06-28
申请号：PCT/GB2011/001739
申请日：2011-12-19
申请人： PHARMINOX LIMITED , HUMMERSONE, Marc, Geoffery , COUSIN, David
发明人： HUMMERSONE, Marc, Geoffery , COUSIN, David
IPC分类号： C07D487/04 , A61K31/4188 , A61P35/00
CPC分类号： C07D487/04
摘要： Compounds of formula (I) and pharmaceutically acceptable salts, hydrates or solvates thereof are provided (I) wherein B, X, and Y are as defined herein. The compounds are of use in methods of regulating cell proliferation, inhibiting cell cycle progression, and/or promoting apoptosis, and in the treatment of proliferative disorders.
摘要翻译：提供式（I）化合物及其药学上可接受的盐，水合物或溶剂合物（I）其中B，X和Y如本文所定义。这些化合物可用于调节细胞增殖，抑制细胞周期进程和/或促进细胞凋亡的方法，以及治疗增殖性疾病。

5. 发明申请

WO2010149968A1 3-SUBSTITUTED-8-SUBSTITUTED-3H IMIDAZO[5,1-D][1,2,3,5-TETRAZIN-4-ONE COMPOUNDS AND THEIR USE 审中-公开
标题翻译： 3-取代-8-取代-3H-咪唑并[5,1-D] [1,2,3,5-四乙基-4-酮化合物及其用途
公开(公告)号：WO2010149968A1
公开(公告)日：2010-12-29
申请号：PCT/GB2010/001233
申请日：2010-06-23
申请人： PHARMINOX LIMITED , HUMMERSONE, Marc, Geoffery , STEVENS, Malcolm, Francis, Graham , COUSIN, David
发明人： HUMMERSONE, Marc, Geoffery , STEVENS, Malcolm, Francis, Graham , COUSIN, David
IPC分类号： C07D487/04 , A61P35/00 , A61K31/4188 , A61K31/427
CPC分类号： C07D487/04 , C07C2601/02
摘要： The present invention pertains generally to the field of therapeutic compounds, and more specifically to 3-substituted-8-substituted-3H-imidazo[5,1-d][1,2,3,5]tetrazin-4-one compounds of the following formula, wherein -A and -B are as defined herein (collectively referred to herein as 38TM compounds): (1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo , to inhibit cell proliferation, and in the treatment of proliferative disorders such as cancer, etc., and methods of preparing such compounds.
摘要翻译：本发明一般涉及治疗化合物领域，更具体地涉及3-取代-8-取代-3H-咪唑并[5,1-d] [1,2,3,5]四嗪-4-酮化合物其中-A和-B如本文所定义（在本文中统称为38TM化合物）：（1）。本发明还涉及包含这些化合物的药物组合物，以及这些化合物和组合物在体外和体内都用于抑制细胞增殖以及治疗增殖性疾病例如癌症等的用途，以及制备此类化合物。

6. 发明申请

WO2011107726A1 METHODS AND INTERMEDIATES FOR THE SYNTHESIS OF 4-OXO-3,4-DIHYDRO-IMIDAZO[5,1-D][1,2,3,5]TETRAZINES 审中-公开
标题翻译：合成4-氧代-3,4-二氢-1H-咪唑并[5,1-D] [1,2,3,5]四氢噻吩的方法和中间体
公开(公告)号：WO2011107726A1
公开(公告)日：2011-09-09
申请号：PCT/GB2011/000266
申请日：2011-02-25
申请人： PHARMINOX LTD , HUMMERSONE, Marc, Geoffery , COUSIN, David
发明人： HUMMERSONE, Marc, Geoffery , COUSIN, David
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides a compound of general formula (II), or a salt or solvate thereof wherein A is independently -A 1 , -A 2 , -A 3 , -A 4 , -A 5 , -A 6 , or -A 7 , wherein: -A 1 is independently C 5-12 heteroaryl, and is optionally substituted; -A 2 is independently thioamido or substituted thioamido; -A 3 is independently imidamido, substituted imidamido, N-hydroxyimidamido, or substituted N-hydroxyimidamido; -A 4 is independently hydroxamic acid or hydroxamate; -A 5 is independently carboxamide or substituted carboxamide; -A 6 is independently aliphatic C 2-6 alkenyl, and is optionally substituted; and -A 7 is independently carboxy or C 1-4 alkyl-carboxylate; and its use in the synthesis of temozolomide and analogues thereof.
摘要翻译：本发明提供通式（II）的化合物或其盐或溶剂合物，其中A独立地为-A1，-A2，-A3，-A4，-A5，-A6或-A7，其中：-A1为独立地是C 5-12杂芳基，并且是任选被取代的; -A2独立地是硫代酰氨基或取代的硫代酰氨基; -A3独立地是亚氨基酰胺基，取代的亚胺酰氨基，N-羟基亚氨基酰胺基或取代的N-羟基亚氨基酰胺基; -A4独立地是异羟肟酸或异羟肟酸盐; -A5独立地是甲酰胺或取代的甲酰胺; -A6独立地是脂族C 2-6烯基，并且任选被取代; -A7独立地是羧基或C1-4烷基 - 羧酸酯; 及其在替莫唑胺及其类似物合成中的应用。

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