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1. 发明授权

US5260291A Tetrazine derivatives 失效
标题翻译：四氮唑衍生物
公开(公告)号：US5260291A
公开(公告)日：1993-11-09
申请号：US781020
申请日：1991-10-18
申请人： Edward Lunt , Malcolm F. G. Stevens , Robert Stone , Kenneth R. H. Wooldridge , Edward S. Newlands
发明人： Edward Lunt , Malcolm F. G. Stevens , Robert Stone , Kenneth R. H. Wooldridge , Edward S. Newlands
IPC分类号： A61K31/52 , C07D487/04 , A61K31/415 , C07P487/04
CPC分类号： C07D487/04 , A61K31/52
摘要： [ 3H]-Imidazo[ 5,1-d] -1,2,3,5-tetrazin-4-one derivatives of the formula: ##STR1## wherein R.sup.1 represents hydrogen, or an alkyl, alkenyl or alkynyl group containing up to 6 carbon atoms, each such group being unsubstituted or substituted by from one to three substituents selected from halogen atoms, alkoxy, alkylthio, alkylsulphinyl and alkylsulphonyl groups containing up to 4 carbon atoms, and optionally substituted phenyl groups, or R.sup.1 represents a cycloalkyl group containing from 3 to 8 carbon atoms, and R.sup.2 represents a carbamoyl group optionally N-substituted by one or two groups selected ftom alkyl and alkenyl groups containing up to 4 carbon atoms, and cycloalkyl groups containing 3 to 8 carbon atoms, are new therapeutically useful compounds possessing antineoplastic and immunomodulatory activity.
摘要翻译： [3 H] - 咪唑并[5,1-d] -1,2,3,5-四嗪-4-酮衍生物，其结构式如下：其中R 1表示氢，或烷基，烯基或炔基， 6个碳原子，每个这样的基团是未取代的或被1至3个选自卤素原子，烷氧基，烷硫基，烷基亚磺酰基和含有至多4个碳原子的烷基磺酰基的取代基取代，和任选取代的苯基，或者R1代表含有 3至8个碳原子，R 2表示任选被一个或两个选自具有至多4个碳原子的烷基和烯基的基团N-取代的氨基甲酰基和含有3至8个碳原子的环烷基，是新的治疗上有用的化合物具有抗肿瘤和免疫调节活性。

2. 发明授权

US07115619B2 N8, N13 -disubstituted quino[4,3,2-kl]acridinium salts as therapeutic agents 失效
标题翻译： N8，N13-二取代喹啉[4,3,2-kl]吖啶鎓盐作为治疗剂
公开(公告)号：US07115619B2
公开(公告)日：2006-10-03
申请号：US10398767
申请日：2001-10-12
申请人： Malcolm F. G. Stevens , Lloyd R Kelland , Robert A Heald
发明人： Malcolm F. G. Stevens , Lloyd R Kelland , Robert A Heald
IPC分类号： A61K31/4745 , C07D471/02
CPC分类号： C07D471/06
摘要： The present invention pertains to certain N8,N13-disubstituted quino[4,3,2-kl]acridinium salts of formula (Q−) which inhibit telomerase wherein: p is an integer from 0 to 4; q is an integer from 0 to 3; r is an integer from 0 to 4; each RA is —H or a ring substituent; each RB is —H or a ring substituent; each RC is —H or a ring substituent; RN8 is a nitrogen substituent; RN13 is a nitrogen substituent; and, Q is an anion. 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 telomerase, to regulate cell proliferation, and in the treatment of proliferative conditions, such as cancer.
摘要翻译：本发明涉及某些式（Q-O-SO 2）n N，N 13 - 二取代的喹啉并[4,3,2-k]吖啶鎓盐 >），其抑制端粒酶，其中：p为0至4的整数; q是0至3的整数; r为0〜4的整数; 每个R A A是-H或环取代基; 每个R B是-H或环取代基; 每个R O是-H或环取代基; R N8是氮取代基; R 13是氮取代基; 而Q是阴离子。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的用途，以抑制端粒酶，调节细胞增殖以及治疗增殖性疾病如癌症。

3. 发明授权

US06858633B1 Substituted 2-arylbenzazole compounds and their use as antitumour agents 失效
标题翻译：取代的2-芳基吲唑化合物及其作为抗肿瘤剂的用途
公开(公告)号：US06858633B1
公开(公告)日：2005-02-22
申请号：US10069018
申请日：2000-08-21
申请人： Malcolm F. G. Stevens , Andrew D. Westwell , Mei-Sze Chua , Tracey D. Poole , Ian P. Hutchinson
发明人： Malcolm F. G. Stevens , Andrew D. Westwell , Mei-Sze Chua , Tracey D. Poole , Ian P. Hutchinson
IPC分类号： A61K31/428 , A61K51/04 , A61P35/00 , C07D277/66 , C07F7/22 , A61K31/421 , A61K31/426 , C07D263/57 , C07D498/00
CPC分类号： C07D277/66 , A61K51/0453 , C07F7/2208
摘要： Substituted 2-phenylbenzazole compounds of formula (I) wherein X represents S or O and Q represents a direct bond, —CH2— or —CH═Ch—, exhibt selective antiproliferactive activity in respect of mammalian tumour cells. At least in preferred enbodiments the benzene ring of the benzazole nucleus has a halogen substituent, preferably flourine, and the 2-phenyl group has a 4′-amino substituent which may be conjugated with an amino acid to provide a water soluble amino acid amide prodrug or salt thereof.
摘要翻译：取代的式（I）的2-苯基吲唑化合物，其中X表示S或O，Q表示直接键，-CH 2 - 或-CH = CH-表示哺乳动物肿瘤细胞的选择性抗增殖活性。至少在优选的实施方案中，苯唑环的苯环具有卤素取代基，优选为氟，2-苯基具有可以与氨基酸缀合的4'-氨基取代基，以提供水溶性氨基酰胺前体药物或其盐。

4. 发明授权

US4992444A Antifolate agents 失效
标题翻译：防腐剂
公开(公告)号：US4992444A
公开(公告)日：1991-02-12
申请号：US127452
申请日：1987-12-02
申请人： Malcolm F. G. Stevens , Roger J. Griffin , Michelle A. Meek
发明人： Malcolm F. G. Stevens , Roger J. Griffin , Michelle A. Meek
IPC分类号： A61K31/505 , A61P17/00 , A61P31/04 , A61P33/02 , A61P35/00 , A61P43/00 , C07D239/48
CPC分类号： C07D239/48
摘要： 2,4-Diamino-5-phenylpyrimidines in the form of the free base or an acid addition salt thereof are provided having the structural formula (I): ##STR1## wherein R.sup.1 is an alkoxy, aralkoxy or a mono-substituted or disubstituted amino group, R.sup.2 is a nitro group, and R.sup.3 is an alkyl group. The compounds act as antifolate agents and are useful for therapeutic treatment, for example as antitumour agents, antipsoriatic agents, antibacterial agents, antitrypanosomal agents and antimalarial agents. Pharmaceutical preparations comprising these compounds for administration to mammals, and methods for preparing the compounds, are disclosed. Particularly useful new compounds, especially for antitumour therapy, have the structural formula IA: ##STR2## in which formula IA: n is 1-6; R.sub.1 represents hydrogen or alkyl; R.sup.4, R.sup.5 and R.sup.6, which may be identical or different, each represnt hydrogen, alkyl, alkoxy, halo, nitro, perfluoroalkyl, a group of formula --CO.sub.2 R.sup.a wherein R.sup.a represents hydrogen, alkyl or alkoxyalkyl, or a group of formula --COBR.sup.b R.sup.c wherein R.sup.b and R.sup.c which may be identical or different each represent alkyl; and R.sup.3 represents alkyl.
摘要翻译：提供游离碱形式的2,4-二氨基-5-苯基嘧啶或其酸加成盐，其具有结构式（I）：其中R 1是烷氧基，芳烷氧基或单取代或双取代氨基，R2为硝基，R3为烷基。化合物作为抗叶酸剂，可用于治疗性治疗，例如作为抗肿瘤剂，抗牛皮癣药，抗菌剂，抗睾丸激素和抗疟药。公开了包含用于给予哺乳动物的这些化合物的药物制剂及其制备方法。特别有用的新化合物，特别是用于抗肿瘤治疗，具有结构式IA：其中式IA：n为1-6; R1代表氢或烷基; R 4，R 5和R 6可以相同或不同，各自表示氢，烷基，烷氧基，卤素，硝基，全氟烷基，式-CO 2 R a基团，其中R a表示氢，烷基或烷氧基烷基或式-COBR b R c基团，其中可以相同或不同的R b和R c表示烷基; 并且R 3表示烷基。

5. 发明授权

US5618928A Triazenyl-substituted phenyl pyrimidines and their use in therapy 失效
标题翻译：三氮烯基取代的苯基嘧啶及其在治疗中的应用
公开(公告)号：US5618928A
公开(公告)日：1997-04-08
申请号：US374508
申请日：1995-01-13
申请人： Malcolm F. G. Stevens , Daniel L. Rathbone , Dennis M. O'Shea
发明人： Malcolm F. G. Stevens , Daniel L. Rathbone , Dennis M. O'Shea
IPC分类号： A61K31/505 , A61P31/04 , A61P31/12 , A61P33/00 , C07D239/48 , C07D401/12 , C07C245/24 , A01N33/26
CPC分类号： C07D239/48 , C07D401/12
摘要： Compounds of formula I: ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each independently hydrogen, alkyl or acyl, R.sup.5 is alkyl, X represents a hydrophobic substituent and n is an integer from 1 to 3, and R.sup.6 and R.sup.7 each represent alkyl, cycloalkyl, or aralkyl, or R.sup.6 and R.sup.7 together with the nitrogen to which they are attached form a heterocyclic ring, with the proviso that one or both of R.sup.6 and R.sup.7, or the heterocyclic ring including R.sup.6 and R.sup.7, carries and/or includes at least one oxygen or sulphur atom, or a salt or N-oxide thereof may be used in the treatment of P. carinii infections.
摘要翻译： PCT No.PCT / GB93 / 01381 Sec。 371日期1995年1月13日 102（e）日期1995年1月13日PCT提交1993年7月1日PCT公布。出版物WO94 / 02469 日期：2月3日，1994年2月3日，式I化合物：其中R 1，R 2，R 3和R 4各自独立地为氢，烷基或酰基，R 5为烷基，X为疏水性取代基，n为1〜 3，R6和R7各自表示烷基，环烷基或芳烷基，或R6和R7与它们所连接的氮一起形成杂环，条件是R6和R7之一或两者或杂环包括 R6和R7携带和/或包含至少一个氧原子或硫原子，或其盐或N-氧化物可用于处理卡氏肺囊虫感染。

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