专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

21. 发明授权

US5696131A Treatment of cancers 失效
标题翻译：癌症治疗
公开(公告)号：US5696131A
公开(公告)日：1997-12-09
申请号：US387565
申请日：1995-02-13
申请人： Bruce Charles Baguley , Graham John Atwell , William Alexander Denny , Graeme John Finlay , Gordon William Rewcastle
发明人： Bruce Charles Baguley , Graham John Atwell , William Alexander Denny , Graeme John Finlay , Gordon William Rewcastle
IPC分类号： A61K31/473 , A61K31/165
CPC分类号： A61K31/00 , A61K31/473
摘要： A new treatment schedule for administration of N-�2-(dimethylamino)ethyl!acridine-4-carboxamide and other related carboxamide anticancer drugs in which the drug is administered in a divided-dose schedule comprising two or more administrations at frequent intervals, for example every hour. Schedules to produce cyclic peaks/troughs in plasma levels are mentioned. The compounds can be used for circumventing multidrug resistance in cancers and may, for example, be used in combination with other cytotoxic drugs, especially non-topo II inhibitors. Treatment of melanoma and advanced colon cancer is included.
摘要翻译：用于施用N- [2-（二甲基氨基）乙基]吖啶-4-甲酰胺和其它相关的羧酰胺抗癌药物的新的治疗方案，其中药物以分次给药方案施用，其包含频繁间隔的两次或更多次给药，用于例如每小时。提及产生血浆水平的循环峰/谷的时间表。该化合物可用于规避癌症中的多药耐药性，并且可以例如与其它细胞毒性药物，特别是非地头性II抑制剂组合使用。包括黑色素瘤和晚期结肠癌的治疗。

22. 发明授权

US07816521B2 1,2,4-benzotriazine-1,4-dioxides 有权
标题翻译： 1,2,4-苯并三嗪-1,4-二氧化物
公开(公告)号：US07816521B2
公开(公告)日：2010-10-19
申请号：US10590796
申请日：2005-03-01
申请人： William Alexander Denny , Michael Patrick Hay , Kevin Owen Hicks , Frederik Pruijn , William Robert Wilson , Karin Pchalek
发明人： William Alexander Denny , Michael Patrick Hay , Kevin Owen Hicks , Frederik Pruijn , William Robert Wilson , Karin Pchalek
IPC分类号： C07D253/10 , C07D413/12 , A61K31/53 , A61P35/00
CPC分类号： C07D253/10 , C07D253/08 , C07D401/12
摘要： The compound 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide and pharmacologically acceptable salts thereof. A method of treating cancer in a subject is also described in which 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof is administered to tumor cells in a hypoxic environment. Also described is a method of radiosensitising in a subject tumor cells of solid tumors in hypoxic conditions by administering to the subject a pharmaceutical composition containing 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof in an amount sufficient to produce radiosensitivity in the tumor cells, and subjecting the tumor cells to radiation. A pharmaceutical composition is additionally provided containing a therapeutically effective amount of 3-ethyl-6-[3-(4-morpholinyl)propoxy]-1,2,4-benzotriazine 1,4-dioxide or a pharmacologically acceptable salt thereof and a pharmaceutically acceptable excipient, adjuvant, carrier, buffer or stabiliser.
摘要翻译：化合物3-乙基-6- [3-（4-吗啉基）丙氧基] -1,2,4-苯并三嗪1,4-二氧化物及其药理学上可接受的盐。还描述了在受试者中治疗癌症的方法，其中给予3-乙基-6- [3-（4-吗啉基）丙氧基] -1,2,4-苯并三嗪1,4-二氧化物或其药理学上可接受的盐到缺氧环境中的肿瘤细胞。还描述了通过向受试者施用含有3-乙基-6- [3-（4-吗啉基）丙氧基] -1,2,4-恶二唑的药物组合物，在缺氧条件下的实体瘤的受试肿瘤细胞中放射增敏的方法，苯并三嗪1,4-二氧化物或其药理学上可接受的盐，其量足以在肿瘤细胞中产生放射敏感性，并对肿瘤细胞进行辐射。另外提供含有治疗有效量的3-乙基-6- [3-（4-吗啉基）丙氧基] -1,2,4-苯并三嗪1,4-二氧化物或其药学上可接受的盐和药学上可接受的盐的药物组合物可接受的赋形剂，佐剂，载体，缓冲液或稳定剂。

23. 发明授权

US6124310A Enediyne compounds 失效
标题翻译：恩二炔化合物
公开(公告)号：US6124310A
公开(公告)日：2000-09-26
申请号：US11644
申请日：1998-04-17
申请人： William Alexander Denny , Michael Patrick Hay , William Robert Wilson
发明人： William Alexander Denny , Michael Patrick Hay , William Robert Wilson
IPC分类号： C12N9/06 , A61K31/00 , A61K31/445 , A61K39/395 , A61K47/48 , A61K48/00 , A61P35/00 , C07D491/08 , C07G491/08 , A61K31/435
CPC分类号： C07D491/08 , A61K47/48761 , B82Y5/00
摘要： The present invention provides compounds of formulae (I) and (II), where X in formula (I) represents a group cleavable by a nitroreductase or carboxypeptidase enzyme. Enzymatic activation of the compounds provide pharmaceutical compounds which may be used for the treatment of neoplastic disease. ##STR1##
摘要翻译： PCT No.PCT / NZ96 / 00084 Sec。 371日期：1998年4月17日 102（e）日期1998年4月17日PCT PCT 1996年8月19日PCT公布。出版物WO97 / 07118 日期1997年2月27日本发明提供式（I）和（II）的化合物，其中式（I）中的X表示可被硝基还原酶或羧肽酶切割的基团。化合物的酶促活化提供可用于治疗肿瘤性疾病的药物化合物。

24. 发明授权

US5750782A Nitroaniline derivatives and their use as anti-tumour agents 失效
标题翻译：硝基苯胺衍生物及其作为抗肿瘤剂的用途
公开(公告)号：US5750782A
公开(公告)日：1998-05-12
申请号：US685079
申请日：1996-07-23
申请人： William Alexander Denny , Brian Desmond Palmer , William Robert Wilson
发明人： William Alexander Denny , Brian Desmond Palmer , William Robert Wilson
IPC分类号： C07C237/34 , C07C233/65
CPC分类号： C07C237/34
摘要： The invention provides nitroaniline derivatives represented by general formula (1) where the nitro group is substituted at any one of the available benzene positions 2-6; where R and A separately represent the groups NO.sub.2, CN,COOR.sup.1, CONR.sup.1 R.sup.2, CSNR.sup.1 R.sup.2 or SO.sub.2 NR.sup.1 R.sup.2 and A is substituted at any one of the available benzene positions 2-6; where B represents N(CH.sub.2 CH.sub.2 halogen).sub.2 or N(CH.sub.2 CH.sub.2 OSO.sub.2 R.sup.3).sub.2 substituted at any one of the available benzene positions; and where R.sup.1, R.sup.2 and R.sup.3 separately represent H, or lower alkyl optionally substituted with hydroxyl, ether, carboxy or amino functions, including cyclic structures, or R.sup.1 and R.sup.2 together with the nitrogen form a heterocyclic structure, and pharmaceutical preparations containing them. These compounds have activity as hypoxia-selective cytotoxins, reductively-activated prodrugs for cytotoxins, hypoxic cell radiosensitisers, and anticancer agents. ##STR1##
摘要翻译：本发明提供了通式（1）表示的硝基苯胺衍生物，其中硝基在任何一个可用苯位置2-6取代; 其中R和A分别代表基团NO2，CN，COOR1，CONR1R2，CSNR1R2或SO2NR1R2，A在任何一个可用的苯位置2-6取代; 其中B表示在任何一个可用苯位置取代的N（CH 2 CH 2卤素）2或N（CH 2 CH 2 OSO 2 R 3）2）并且其中R 1，R 2和R 3分别代表H，或任选被羟基，醚，羧基或氨基官能团取代的低级烷基，包括环状结构，或者R 1和R 2与氮一起形成杂环结构，以及含有它们的药物制剂。这些化合物具有作为缺氧选择性细胞毒素，用于细胞毒素的还原活化前药，缺氧细胞放射增敏剂和抗癌剂的活性。

25. 发明授权

US07666864B2 Bicyclic nitroimidazole-substituted phenyl oxazolidinones 有权
标题翻译：双环硝基咪唑取代的苯基恶唑烷酮
公开(公告)号：US07666864B2
公开(公告)日：2010-02-23
申请号：US12411220
申请日：2009-03-25
申请人： Charles Z. Ding , Genliang Lu , Keith Combrink , Dianjun D. Chen , Minsoo Song , Jiancheng Wang , Zhenkun Ma , Brian Desmond Palmer , Adrian Blaser , Andrew M. Thompson , Iveta Kmentova , Hamish Scott Sutherland , William Alexander Denny
发明人： Charles Z. Ding , Genliang Lu , Keith Combrink , Dianjun D. Chen , Minsoo Song , Jiancheng Wang , Zhenkun Ma , Brian Desmond Palmer , Adrian Blaser , Andrew M. Thompson , Iveta Kmentova , Hamish Scott Sutherland , William Alexander Denny
IPC分类号： C07D498/04 , A61K31/424 , A61K31/5365 , A61K31/553
CPC分类号： C07D498/04
摘要： The current invention provides a series of bicyclic nitroimidazole-substituted phenyl oxazolidinones in which a bicyclic nitroimidazole pharmacophore is covalently bonded to a phenyl oxazolidinone, their pharmaceutical compositions, and the method of use of the compositions for prevention and treatment of bacterial infections. The bicyclic nitroimidazole-substituted phenyl oxazolidinones possess surprising antibacterial activity against wild-type and resistant strains of pathogens, and are therefore useful for the prevention, control and treatment of a number of human and veterinary bacterial infections caused by these pathogens, such as Mycobacterium tuberculosis.
摘要翻译：本发明提供了一系列双环硝基咪唑取代的苯基恶唑烷酮，其中双环硝基咪唑药效团与苯基恶唑烷酮共价键合，其药物组合物，以及组合物用于预防和治疗细菌感染的方法。双环硝基咪唑取代的苯基恶唑烷酮对于野生型和抗性病原体菌株具有惊人的抗菌活性，因此可用于预防，控制和治疗由这些病原体引起的许多人和兽医细菌感染如结核分枝杆菌。

26. 发明授权

US07094798B1 Inhibitors of checkpoint kinases (Wee1 and Chk1) 有权
标题翻译：检测点激酶抑制剂（Wee1和Chk1）
公开(公告)号：US07094798B1
公开(公告)日：2006-08-22
申请号：US10424228
申请日：2003-04-25
申请人： Richard John Booth , Ellen Myra Dobrusin , Alan Kraker , Lorna Helen Mitchell , William Alexander Denny , Jeffrey Bruce Smaill , Andrew Mark Thompson , Florence Oliver Joseph McCarthy , Ho Huat Lee , Brian Desmond Palmer
发明人： Richard John Booth , Ellen Myra Dobrusin , Alan Kraker , Lorna Helen Mitchell , William Alexander Denny , Jeffrey Bruce Smaill , Andrew Mark Thompson , Florence Oliver Joseph McCarthy , Ho Huat Lee , Brian Desmond Palmer
IPC分类号： A61K31/403 , C07D209/88
CPC分类号： C07D487/04 , C07D209/88 , C07D491/04
摘要： This invention relates to pyrrolocarbazole derivatives according formula I wherein R1, R2, R7, R8, R9, X and Y are as defined in the specification wherein said derivatives specifically inhibit one or both of the checkpoint kinases Wee1 and Chk1
摘要翻译：本发明涉及式I的吡咯并咔唑衍生物，其中R 1，R 2，R 7，R 8， R 9，X和Y如说明书中所定义，其中所述衍生物特异性抑制检查点激酶Wee1和Chk1中的一个或两个

27. 发明授权

US06713484B2 Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family 失效
标题翻译：能够抑制表皮生长因子受体家族酪氨酸激酶的双环化合物
公开(公告)号：US06713484B2
公开(公告)日：2004-03-30
申请号：US10201808
申请日：2002-07-24
申请人： Alexander James Bridges , William Alexander Denny , David Fry , Gordon William Rewcastle
发明人： Alexander James Bridges , William Alexander Denny , David Fry , Gordon William Rewcastle
IPC分类号： A61K31519
CPC分类号： C07D471/04 , A61K31/4985 , A61K31/519 , C07D473/34 , C07D495/04
摘要： Described are heterocyclic pyrimidine derivatives and a method of inhibiting epidermal growth factor by treating, with an effective inhibiting amount, a mammal, in need thereof, a compound of the formula: where: at least two of A-E are nitrogen, with the remaining atom(s) carbon; X=NH or NR7, such that R7=lower alkyl (1-4 carbon atoms), OH, NH2, lower alkoxy (1-4 carbon atoms) or lower monoalkylamino (1-4 carbon atoms); n=0, 1, 2. The remaining substituents are described in detail in the specification.
摘要翻译：描述的是杂环嘧啶衍生物和抑制表皮生长因子的方法，其中：有效抑制量的哺乳动物，有需要的下列化合物：其中：至少两个AE是氮，剩余的原子（ s）碳; X = NH或NR 7，使得R 7 =低级烷基（1-4个碳原子），OH，NH 2，低级烷氧基（1-4个碳原子）或低级单烷基氨基（1-4 碳原子）; n = 0,1,2。其余取代基在说明书中详细描述。

28. 发明授权

US06552021B2 Pharmaceutical compounds 失效
标题翻译：药物化合物
公开(公告)号：US06552021B2
公开(公告)日：2003-04-22
申请号：US09797902
申请日：2001-03-05
申请人： John Milton , Nigel Vicker , William Alexander Denny , Swarnalatha Akuratiya Gamage , Julie Ann Spicer
发明人： John Milton , Nigel Vicker , William Alexander Denny , Swarnalatha Akuratiya Gamage , Julie Ann Spicer
IPC分类号： C07D47104
CPC分类号： C07D471/04 , C07D487/04
摘要： A compound which is a heteroaromatic[a]phenazine carboxamide derivative of formula (I) wherein X is a five- or six-membered heteroaromatic ring which contains one or two nitrogen atoms and which is unsubstituted or substituted by C1-C6 alkyl, hydroxyl or C1-C6 alkoxy; Q is C1-C6 alkylene which is unsubstituted or substituted by C1-C6 alkyl which is unsubstituted or substituted by a hydroxy group; and R1 and R2 which are the same or different are each C1-C6 alkyl; or a pharmaceutically acceptable salt thereof. These compounds are inhibitors of topoisomerase I and II and can be used to treat tumours, including tumours which express MDR.
摘要翻译：一种化合物，其是式（I）的杂芳族[a]吩嗪甲酰胺衍生物，其中X是含有一个或两个氮原子且未被取代或被C 1 -C 6烷基取代的五元或六元杂芳环，羟基或 C 1 -C 6烷氧基; Q是未被取代或被未取代或被羟基取代的C1-C6烷基取代的C1-C6亚烷基; 和相同或不同的R 1和R 2各自为C 1 -C 6烷基;或其药学上可接受的盐。这些化合物是拓扑异构酶I和II的抑制剂，可用于治疗肿瘤，包括表达MDR的肿瘤。

29. 发明授权

US06521620B1 Bicyclic compounds capable of inhibiting tyrosine kinases of the epidermal growth factor receptor family 失效
标题翻译：能够抑制表皮生长因子受体家族酪氨酸激酶的双环化合物
公开(公告)号：US06521620B1
公开(公告)日：2003-02-18
申请号：US09183190
申请日：1998-10-30
申请人： Alexander James Bridges , William Alexander Denny , David Fry , Gordon William Rewcastle
发明人： Alexander James Bridges , William Alexander Denny , David Fry , Gordon William Rewcastle
IPC分类号： A61K314985
CPC分类号： C07D471/04 , A61K31/4985 , A61K31/519 , C07D473/34 , C07D495/04
摘要： Described are heterocyclic pyrimidine derivatives and a method of inhibiting epidermal growth factor by treating, with an effective inhibiting amount, a mammal, in need thereof, a compound of the formula: where: at least two of A-E are nitrogen, with the remaining atom(s) carbon; X=NH or NR7, such that R7=lower alkyl (1-4 carbon atoms), OH, NH2, lower alkoxy (1-4 carbon atoms) or lower monoalkylamino (1-4 carbon atoms); n=0, 1, 2. The remaining substituents are described in detail in the specification.
摘要翻译：描述的是杂环嘧啶衍生物和抑制表皮生长因子的方法，其中：有效抑制量的哺乳动物，有需要的下列化合物：其中：至少两个AE是氮，剩余的原子（ X = NH或NR7，使得R7 =低级烷基（1-4个碳原子），OH，NH2，低级烷氧基（1-4个碳原子）或低级单烷基氨基（1-4个碳原子）; n = 剩余的取代基在说明书中详细描述。

30. 发明申请

US20110028466A1 NITROIMIDAZOOXAZINE AND NITROIMIDAZOOXAZOLE ANALOGUES AND THEIR USES 有权
标题翻译： NITROIMIDAZOOXAZINE和NITROIMIDAZOOXAZOLE ANALOGUES及其用途
公开(公告)号：US20110028466A1
公开(公告)日：2011-02-03
申请号：US12847459
申请日：2010-07-30
申请人： Andrew Mark Thompson , William Alexander Denny , Adrian Blaser , Zhenkun Ma
发明人： Andrew Mark Thompson , William Alexander Denny , Adrian Blaser , Zhenkun Ma
IPC分类号： A61K31/5365 , A61K31/4965 , A61K31/506 , A61K31/4439 , A61K31/424 , C07D498/04 , A61P31/04
CPC分类号： C07D498/04
摘要： The current invention pertains to nitroimidazooxazine and nitroimidazooxazole analogues, their methods of preparation, and uses of the compounds as treatment for Mycobacterium tuberculosis, for use as anti-tubercular drugs, for use as anti-protozoal agents with unexpectedly high potency against Trypanosoma cruzi or Leishmania donovani, and for the treatment of other microbial infections.
摘要翻译：本发明涉及硝基咪唑并恶嗪和硝基咪唑并恶唑类似物，其制备方法，以及该化合物作为结核分枝杆菌治疗的用途，用作抗结核药物，用作对克氏锥虫或利什曼原虫具有意想不到的高效力的抗原生动物 donovani和治疗其他微生物感染。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式