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1. 发明授权

US5071857A 2,6-dioxopiperidine derivatives, their preparation and pharmaceutical compositions containing them 失效
标题翻译： 2,6-二氧代哌啶衍生物，其制备和含有它们的药物组合物
公开(公告)号：US5071857A
公开(公告)日：1991-12-10
申请号：US571830
申请日：1990-08-22
申请人： Allan B. Foster , Michael Jarman , Grahame N. Taylor , Chui-Sheung Kwan
发明人： Allan B. Foster , Michael Jarman , Grahame N. Taylor , Chui-Sheung Kwan
IPC分类号： C07D213/57 , C07D401/04
CPC分类号： C07D401/04 , C07D213/57
摘要： In the treatment of oestrogen-dependent tumors, it is desirable to improve the therapy obtainable from the compound aminoglutethimide. It has now been found that 3-ethyl-3-(4-pyridyl)glutarimide and derivatives thereof of formula ##STR1## wherein R represents a hydrogen atom or an alkyl group having 1 to 4 carbon atoms offers advantages over aminoglutethimide. 3-Ethyl-3-(4-pyridyl)glutarimide can be prepared by various ring-closing reactions, especially by heating 4-(4-pyridyl)-hexano-1,4-dinitrile with a strong mineral acid.
摘要翻译： PCT No.PCT / GB84 / 00425 Sec。 371日期：1985年7月16日 102（e）日期1985年7月16日PCT提交1984年12月10日PCT公布。出版物WO85 / 02618 1985年6月20日。在治疗雌激素依赖性肿瘤时，期望改善从化合物氨基丁二酰亚胺获得的治疗。现已发现3-氨基-3-（4-吡啶基）戊二酰亚胺及其衍生物，其中R表示氢原子或具有1-4个碳原子的烷基，具有优于氨基异丁酰亚胺的优点。 3-乙基-3-（4-吡啶基）戊二酰亚胺可以通过各种闭环反应制备，特别是通过用强无机酸加热4-（4-吡啶基） - 己酰-1,4-二腈。

2. 发明授权

US4668689A Glutarimide derivatives for treating oestrogen-dependent tumors 失效
标题翻译：用于治疗雌激素依赖性肿瘤的戊二酰亚胺衍生物
公开(公告)号：US4668689A
公开(公告)日：1987-05-26
申请号：US753878
申请日：1985-07-11
申请人： Allan B. Foster , Michael Jarman , Chui-Sheung Kwan
发明人： Allan B. Foster , Michael Jarman , Chui-Sheung Kwan
IPC分类号： C07D213/57 , A61K31/4409 , A61K31/4418 , A61K31/4427 , A61K31/445 , A61P35/00 , A61P43/00 , C07D401/04 , C12N9/99
CPC分类号： C07D401/04
摘要： In the treatment of oestrogen-dependent tumors, it is desirable to improve the therapy obtainable from the compound aminoglutethimide. It has now been found that 3-ethyl-3-(4-pyridyl)glutarimide derivatives of formula ##STR1## wherein: (a) R.sup.1 represents an ethyl group and R.sup.2 represents a methyl group, an alkyl or cycloalkyl group having 3 to 10 carbon atoms, or a fluoroalkyl group having 2 to 10 carbon atoms;(b) R.sup.1 represents an alkyl group having 3 to 10 carbon atoms or a fluoroalkyl group having 2 to 5 carbon atoms and R.sup.2 represents a hydrogen atom; or,(c) R.sup.1 represents an alkyl group having 3 to 8 carbon atoms or a fluoroalkyl group having 2 to 5 carbon atoms and R.sup.2 represents an alkyl or fluoroalkyl group having 2 to 8 carbon atoms, provided that the total number of carbon atoms in R.sup.1 and R.sup.2 is not more than 10;and therapeutically acceptable acid addition salts of the above compounds.
摘要翻译：在治疗雌激素依赖性肿瘤时，期望改善从化合物氨基丁二酰亚胺获得的治疗。现已发现式（2）的3-乙基-3-（4-吡啶基）戊二酰亚胺衍生物，其中：（a）R 1表示乙基，R 2表示甲基，烷基或环烷基具有 3〜10个碳原子，或2〜10个碳原子的氟烷基; （b）R1表示碳原子数3〜10的烷基或碳原子数2〜5的氟代烷基，R2表示氢原子。或者，（c）R1表示碳原子数3〜8的烷基或碳原子数2〜5的氟代烷基，R2表示碳原子数2〜8的烷基或氟代烷基，条件是碳原子数为 R1和R2不超过10; 和上述化合物的治疗上可接受的酸加成盐。

3. 发明授权

US5854244A Melamine derivatives for use in the treatment of cancer 失效
标题翻译：用于治疗癌症的三聚氰胺衍生物
公开(公告)号：US5854244A
公开(公告)日：1998-12-29
申请号：US631659
申请日：1996-04-02
申请人： Michael Jarman , Helen Mary Coley
发明人： Michael Jarman , Helen Mary Coley
IPC分类号： A61K31/53 , A61P35/00 , C07D251/70
CPC分类号： C07D251/70
摘要： The present invention provides compounds of the formula (I) wherein each R.sup.1, which may be the same or different, is hydrogen, C.sub.1-4 alkyl, or an electron withdrawing group selected from the group consisting of CF.sub.3 CH.sub.2 or CH.sub.2 C.tbd.CH, R.sup.2 is hydrogen, C.sub.1-4 alkyl, or an electron withdrawing group selected from the group consisting of CF.sub.3 CH.sub.2 or CH.sub.2 C.tbd.CH. The compounds are analogs of trimelamol which have comparable activity but enhanced stability, and are useful as anticancer agents, particularly against ovarian cancer.
摘要翻译：本发明提供式（I）化合物，其中每个可以相同或不同的R 1是氢，C 1-4烷基或选自CF 3 CH 2或CH 2 C 3 CH 2的吸电子基团，R 2是氢，C 1-4烷基或选自CF 3 CH 2或CH 2 C 3 CH 3的吸电子基团。这些化合物是具有相当活性但增强稳定性的三聚木酚类似物，并且可用作抗癌剂，特别是抗卵巢癌。

4. 发明授权

US5716990A Drug delivery systems 失效
标题翻译：药物输送系统
公开(公告)号：US5716990A
公开(公告)日：1998-02-10
申请号：US709740
申请日：1996-09-09
申请人： Kenneth D. Bagshawe , Michael Jarman , Caroline Joy Springer
发明人： Kenneth D. Bagshawe , Michael Jarman , Caroline Joy Springer
IPC分类号： A61K47/48 , A61K31/255 , C07C231/02 , C07C309/06
CPC分类号： B82Y5/00 , A61K47/48761
摘要： Nitrogen mustard pro-drugs of the formula ##STR1## are disclosed where R is the residue of an .alpha.-amino acid RNH.sub.2 and M is a disubstituted amino "mustard" group, useful in antibody directed enzyme pro-drug therapy in the treatment of cancer.
摘要翻译：公开了具有式“IMAGE”的氮芥前体药物，其中R是α-氨基酸RNH2的残基，M是二取代的氨基“芥子”基团，可用于治疗癌症中的抗体定向酶前药治疗。

5. 发明申请

US20120180110A1 Data Communication Authentication System and Method 有权
标题翻译：数据通信认证系统与方法
公开(公告)号：US20120180110A1
公开(公告)日：2012-07-12
申请号：US13389302
申请日：2010-08-09
申请人： Michael Jarman
发明人： Michael Jarman
IPC分类号： G06F21/00 , H04W12/06
CPC分类号： H04L63/126 , H04L63/08 , H04L63/107
摘要： A data communication authentication system (10) and method are described. One or more locator nodes (20) are installable at a location (30), the or each locator node (20) including an identifier (21) and a communication system (22) and being arranged to provide said identifier via said communication system (22). The communication authentication system (10) is arranged to generate an authentication code for the location (30) in dependence on identifiers (21) from the one or more locator nodes at the location and is arranged to provide said authentication code on demand for inclusion in a data communication originating locally to said location (30).
摘要翻译：描述了数据通信认证系统（10）和方法。一个或多个定位器节点（20）可安装在位置（30）处，所述或每个定位器节点（20）包括标识符（21）和通信系统（22），并且被布置成经由所述通信系统（ 22）。通信认证系统（10）被安排为根据来自该位置处的一个或多个定位器节点的标识符（21）生成位置（30）的认证码，并且被布置为根据需要提供所述认证码，以包括在本地发送到所述位置（30）的数据通信。

6. 发明授权

US5780585A Bacterial nitroreductase for the reduction of CB 1954 and analogues thereof to a cytotoxic form 失效
标题翻译：用于将CB 1954及其类似物还原成细胞毒性形式的细菌硝基还原酶
公开(公告)号：US5780585A
公开(公告)日：1998-07-14
申请号：US504047
申请日：1995-06-07
申请人： Gillian Anlezark , Roger Melton , Roger Sherwood , Thomas Connors , Frank Friedlos , Michael Jarman , Richard Knox , Anthony Mauger , Caroline Joy Springer
发明人： Gillian Anlezark , Roger Melton , Roger Sherwood , Thomas Connors , Frank Friedlos , Michael Jarman , Richard Knox , Anthony Mauger , Caroline Joy Springer
IPC分类号： C12N9/12 , A61K38/00 , C07C219/34 , C07C271/18 , C07D203/14 , C07D487/14 , C07H15/252 , C07H19/048 , C07K7/06 , C12N9/02 , C12N15/00 , C12N15/09 , C12N15/53 , C12P17/10 , C12P21/08 , C12R1/01 , C12R1/07 , C12R1/19 , G01N33/53 , G01N33/573 , C07K7/56 , C07C68/00 , C07C69/96 , C07C269/04 , C07C271/28 , C07H15/24
CPC分类号： C07D203/14 , C07C219/34 , C07C271/18 , C07D487/14 , C07H15/252 , C07H19/048 , C07K7/06 , C12N9/0036 , C12P17/10 , C12Y101/01284 , A61K38/00 , Y02E50/16
摘要： A prodrug of the formula (I): ##STR1## where R.sup.1 is a group such that the compound R--NH.sub.2 represents actinomycin D, doxorubicin, mitomycin C, or a nitrogen mustard of the formula (IV): ##STR2## a prodrug of the formula (II): ##STR3## where R.sup.1 is a group such that the compound R.sup.2 OH is a phenolic nitrogen mustard; and processes whereby the prodrugs shown above are made in which a prodrug precursor compound is reacted with 4-nitrobenzyl chloroformate under anhydrous conditions.
摘要翻译：式（I）的前药：其中R 1是使得化合物R-NH 2表示放线菌素D，多柔比星，丝裂霉素C或式（IV）的氮芥的基团：式（II）的前药：其中R 1是使化合物R 2 OH是酚氮芥的基团; 以及其中制备前述前药的方法，其中前药前体化合物与无水条件下的氯甲酸4-硝基苄酯反应。

7. 发明授权

US5618807A Method for preparing 17-substituted steroids useful in cancer treatment 失效
标题翻译：制备可用于癌症治疗的17-取代类固醇的方法
公开(公告)号：US5618807A
公开(公告)日：1997-04-08
申请号：US392178
申请日：1995-02-22
申请人： Susan E. Barrie , Michael Jarman , Gerard A. Potter , Ian R. Hardcastle
发明人： Susan E. Barrie , Michael Jarman , Gerard A. Potter , Ian R. Hardcastle
IPC分类号： C07J13/00 , C07J31/00 , C07J41/00 , C07J43/00 , C07J51/00 , A61K31/58
CPC分类号： C07J51/00 , C07J13/005 , C07J31/006 , C07J41/0005 , C07J43/003
摘要： Compounds of the general formula (1) ##STR1## wherein X represents the residue of the A, B and C rings of a asteroid, R represents a hydrogen atom or an alkyl group of 1 to 4 carbon atoms, R.sup.14 represents a hydrogen atom and R.sup.15 represents a hydrogen atom or an alkyl or alkoxy group of 1-4 carbon atoms, or a hydroxy or alkylcarbonyloxy group of 2 to 5 carbon atoms or R.sup.14 and R.sup.15 together represent a double bond, and R.sup.16 represents a hydrogen atom or an alkyl group of 1 to 4 carbon atoms, in the form of the free bases or pharmaceutically acceptable acid addition salts, are used for treatment of androgen-dependent disorders, especially prostatic cancer, and also oestrogen-dependent disorders such as breast cancer.
摘要翻译：通式（1）的化合物其中X表示小行星的A，B和C环的残基，R表示氢原子或1〜4个碳原子的烷基，R 14表示氢原子和R 15表示氢原子或1-4个碳原子的烷基或烷氧基，或2〜5个碳原子的羟基或烷基羰基氧基或R 14和R 15一起表示双键，R 16表示氢原子或使用游离碱或药学上可接受的酸加成盐形式的1至4个碳原子的烷基用于治疗雄激素依赖性疾病，特别是前列腺癌，以及雌激素依赖性疾病如乳腺癌。

8. 发明授权

US5589500A Substituted 1,1,2-triphenylbutenes and their use in the treatment of cancer 失效
标题翻译：取代的1,1,2-三苯基丁烯及其在治疗癌症中的应用
公开(公告)号：US5589500A
公开(公告)日：1996-12-31
申请号：US331582
申请日：1995-01-17
申请人： Karen J. Edwards , Michael Jarman , Charles A. Laughton , Stephen Neidle , Ian R. Hardcastle
发明人： Karen J. Edwards , Michael Jarman , Charles A. Laughton , Stephen Neidle , Ian R. Hardcastle
IPC分类号： C07D295/08 , A61K31/135 , A61K31/138 , A61K31/40 , A61K49/00 , A61K51/00 , A61P35/00 , C07C217/18 , C07D295/092 , C07D295/088
CPC分类号： C07D295/088 , C07C217/18
摘要： Compounds of the general formula (2) ##STR1## wherein n is an integer of from 3 to 10, the iodo substituent is in the 3- or 4-position and R.sup.1 and R.sup.2, which may be the same or different, represent C.sub.1-3 alkyl, especially methyl or ethyl, groups or R.sup.l represents a hydrogen atom and R.sup.2 a C.sub.1-3 alkyl group or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached represent a saturated heterocyclic group, especially a pyrrolidino group, in the form of their free bases or pharmaceutically acceptable acid addition salts are potent anti-oestrogenic compounds useful for treatment of oestrogen-dependent cancers, especially breast cancers. Compounds where the iodine atom is radioisotopic are useful in radiotherapy or gamma ray imaging of these cancers.
摘要翻译： PCT No.PCT / GB93 / 00889 Sec。 371日期1995年1月17日 102（e）日期1995年1月17日PCT提交1993年4月29日PCT公布。公开号WO93 / 22275 日期：1993年11月11日通式（2）（2）的化合物，其中n为3〜10的整数，碘取代基为3-或4-位，R1和R2可以是相同或不同，表示C1-3烷基，特别是甲基或乙基，或R1表示氢原子，R2表示C1-3烷基或R1和R2与它们所连接的氮原子一起表示饱和杂环基，特别是吡咯烷基，其游离碱或药学上可接受的酸加成盐的形式是有效的抗雌激素化合物，其可用于治疗雌激素依赖性癌症，特别是乳腺癌。碘原子是放射性同位素的化合物可用于这些癌症的放射治疗或γ射线成像。

9. 发明授权

US09178895B2 Data communication authentication system and method 有权
标题翻译：数据通信认证系统及方法
公开(公告)号：US09178895B2
公开(公告)日：2015-11-03
申请号：US13389302
申请日：2010-08-09
申请人： Michael Jarman
发明人： Michael Jarman
IPC分类号： H04L29/06
CPC分类号： H04L63/126 , H04L63/08 , H04L63/107
摘要： A data communication authentication system (10) and method are described. One or more locator nodes (20) are installable at a location (30), the or each locator node (20) including an identifier (21) and a communication system (22) and being arranged to provide said identifier via said communication system (22). The communication authentication system (10) is arranged to generate an authentication code for the location (30) in dependence on identifiers (21) from the one or more locator nodes at the location and is arranged to provide said authentication code on demand for inclusion in a data communication originating locally to said location (30).
摘要翻译：描述了数据通信认证系统（10）和方法。一个或多个定位器节点（20）可安装在位置（30）处，所述或每个定位器节点（20）包括标识符（21）和通信系统（22），并且被布置成经由所述通信系统（ 22）。通信认证系统（10）被安排为根据来自该位置处的一个或多个定位器节点的标识符（21）生成位置（30）的认证码，并且被布置为根据需要提供所述认证码，以包括在本地发送到所述位置（30）的数据通信。

10. 发明授权

US5633158A Bacterial nitroreductase for the reduction of CB 1954 and analogues thereof to a cytotoxic form 失效
标题翻译：用于将CB 1954及其类似物还原成细胞毒性形式的细菌硝基还原酶
公开(公告)号：US5633158A
公开(公告)日：1997-05-27
申请号：US232018
申请日：1994-07-27
申请人： Gillian Anlezark , Roger Melton , Roger Sherwood , Thomas Connors , Frank Friedlos , Michael Jarman , Richard Knox , Anthony Mauger
发明人： Gillian Anlezark , Roger Melton , Roger Sherwood , Thomas Connors , Frank Friedlos , Michael Jarman , Richard Knox , Anthony Mauger
IPC分类号： C12N9/12 , A61K38/00 , C07C219/34 , C07C271/18 , C07D203/14 , C07D487/14 , C07H15/252 , C07H19/048 , C07K7/06 , C12N9/02 , C12N15/00 , C12N15/09 , C12N15/53 , C12P17/10 , C12P21/08 , C12R1/01 , C12R1/07 , C12R1/19 , G01N33/53 , G01N33/573 , C07H21/04 , C12N1/20
CPC分类号： C07D203/14 , C07C219/34 , C07C271/18 , C07D487/14 , C07H15/252 , C07H19/048 , C07K7/06 , C12N9/0036 , C12P17/10 , C12Y101/01284 , A61K38/00 , Y02E50/16
摘要： The invention provides a nitroreductase, obtainable from a bacterium having the following characteristics as exemplified by examples isolated from Escherichia coli B and Bacillus amyloliquifaciens: 1) it is flavoprotein having a molecular weight in the range of 20-60 Kilodaltons; 2) it requires either NADH or NAD(P)H or analogues thereof as a cofactor; 3) it has a Km for NADH or NAD(P)H in the range of 1-100 .mu.M; and 4) it is capable of reducing either or both nitro groups of CB1954 and analogues thereof to a cytotoxic form e.g. the hydroxylamine. The sequence of one such nitroreductase is shown in Seq. ID No. 1. The nitroreductase may be conjugated to a tumor targeting agent such as a monoclonal antibody and used to convert prodrugs into active antitumor agents. Such prodrugs and drugs are also provided.
摘要翻译： PCT No.PCT / GB92 / 01947。 371日期：1994年7月27日 102（e）日期1994年7月27日PCT提交1992年10月23日PCT公布。公开号WO93 / 08288 日期：1993年04月29日本发明提供了可从具有以下特征的细菌获得的硝基还原酶，其特征如分离自大肠杆菌B和Bacillus amylolquifaciens的实施例所示：1）它是分子量在20-60千道尔顿范围内的黄素蛋白; 2）它需要NADH或NAD（P）H或其类似物作为辅因子; 3）其NADH或NAD（P）H的Km为1-100μM; 和4）它能够将CB1954的硝基和其类似物的一个或两个还原成细胞毒性形式，例如羟胺。一种这样的硝基还原酶的顺序示于Seq。硝基还原酶可以与肿瘤靶向剂如单克隆抗体缀合，并用于将前药转化为活性抗肿瘤剂。还提供了这些前药和药物。

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