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1. 发明申请

US20060009517A1 Tricyclic inhibitors of poly(ADP-ribose) polymerases 有权
公开(公告)号：US20060009517A1
公开(公告)日：2006-01-12
申请号：US11221245
申请日：2005-09-06
申请人： Stephen Webber , Stacie Canan-Koch , Jayashree Tikhe , Lars Thoresen
发明人： Stephen Webber , Stacie Canan-Koch , Jayashree Tikhe , Lars Thoresen
IPC分类号： A61K31/277
CPC分类号： C07D471/06 , A61K31/277 , A61K31/4375 , C07D487/06
摘要： Compounds of the formula below are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapeutics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and neurodegenerative disease. As cancer therapeutics, the compounds of the invention may be used, e.g., in combination with cytotoxic agents and/or radiation.

2. 发明授权

US06852755B1 Nitrogen mustard compounds and prodrugs therefor 有权
标题翻译：氮芥化合物及其前药
公开(公告)号：US06852755B1
公开(公告)日：2005-02-08
申请号：US09937714
申请日：2000-03-29
申请人： Caroline J. Springer , Lawrence C. Davies
发明人： Caroline J. Springer , Lawrence C. Davies
IPC分类号： A61K48/00 , A61K31/606 , A61K31/609 , A61K38/46 , A61K47/48 , A61P35/00 , A61P43/00 , C07C229/60 , C07C237/36 , A61K31/235 , A61K31/255 , C07C229/14 , C07C303/00 , C07C313/00
CPC分类号： B82Y5/00 , A61K47/6899 , A61K47/6957 , C07C229/60 , C07C237/36
摘要： This invention pertains to nitrogen mustard compounds (Formula (II)) and prodrugs therefor (Formula (I)), methods for their preparation, pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in therapy and treatment, for example, of cancer, wherein: R1 and R2 are independently —Cl, —Br, —I, —OSO2CH3, or —OSO2Ph; R1a, R2a, R1b, and R2b are independently —H, a C1-4alkyl group, or a C1-4haloalkyl group; R3 is —F, —Cl, —Br, —I, —OCHF2, —C≡CH, —OCF3, —CH3, —CF3, —SF5, —SCF3, or —CF2CF3; R4 is —H or as defined for R3−, R5 is —H or —F; R7 is —H, —C(CH3)3, or —CH2—CH—CH2; Z is —CH2—T—W; T is —CH2—, —O—, —S—, —(S═O)—, or —(SO2)—; W is one of: (1) —COOH; (2)—(C═O)OR8; (3) —(C═O)NR9R9; (4) —SO2NHR10−, (5) SO2OR11; (6)—PO3R11R11; (7) a tetrazol-5-yl group; (8) —CONH—SO2R12; and, (9)-M-Het.
摘要翻译：本发明涉及氮芥化合物（式（II））及其前药（式（I）），其制备方法，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，在治疗和治疗中，例如癌症，其中：R 1和R 2独立地是-Cl，-Br，-I，-OSO 2 CH 3或-OSO 2 Ph; R 1a，R 2a，R 1b和R 2b独立地是-H，C 1-4烷基或C 1-4卤代烷基; R 3是-F，-Cl，-Br，-I，-OCHF 2，-C = CH，-OCF 3，-CH 3，-CF 3，-SF 5，-SCF 3或-CF 2 CF 3; R 4是-H或如对R 3-3所定义，R 5是-H或-F; R 7是-H，-C（CH 3）3或-CH 2 -CH-CH 2; Z是-CH 2 -T-W; T是-CH 2 - ， - O - ， - S - ， - （S = O） - 或 - （SO 2） - ; W是以下之一：（1）-COOH; （2） - （C = O）OR 8; （3） - （C = O）NR 9 R 9; （4）-SO 2 NHR 10，（5）SO 2 OR 11; （6）-PO 3 R 11 R 11; （7）四唑-5-基; （8）-CONH-SO 2 R 12; 和（9）-M-Het。

3. 发明授权

US6165715A Expression systems 失效
标题翻译：表达系统
公开(公告)号：US6165715A
公开(公告)日：2000-12-26
申请号：US11745
申请日：1998-06-22
申请人： Mary Katherine Levinge Collins , Robin Anthony Weiss , Yasuhiro Takeuchi , Francois-Lois Cosset
发明人： Mary Katherine Levinge Collins , Robin Anthony Weiss , Yasuhiro Takeuchi , Francois-Lois Cosset
IPC分类号： C12N15/67 , C12N15/867 , C12Q1/68 , C12N5/10 , C12N15/63 , C12N15/86
CPC分类号： C12N15/86 , C12N15/67 , C12N2740/13043
摘要： The invention relates to new expression systems and in particular to an expression system in which a gene of interest is expressed at an optimal level. The invention provides a recombinant expression vector comprising a gene of interest and a selectable marker gene, wherein the selectable marker gene is arranged downstream of the gene of interest and a stop codon associated with the gene of interest is spaced from a start codon of said selectable marker gene at a distance which is sufficient to ensure that translation reinitiation is required before said selectable marker protein is expressed from the corresponding mRNA. Examples of such expression systems are vector viral packaging cell lines and a number of preferred cell lines have been identified.
摘要翻译： PCT No.PCT / GB96 / 02061 Sec。 371日期：1998年6月22日 102（e）日期1998年6月22日PCT提交1996年8月23日PCT公布。公开号WO97 / 08330 日期1997年3月6日本发明涉及新的表达系统，特别涉及其中目标基因以最佳水平表达的表达系统。本发明提供了包含感兴趣的基因和选择性标记基因的重组表达载体，其中所述选择性标记基因设置在感兴趣的基因的下游，并且与感兴趣的基因相关的终止密码子与所述可选择的基因的起始密码子间隔开标记基因，其距离足以确保在从相应mRNA表达所述可选择标记蛋白之前需要翻译重新启动。这种表达系统的实例是载体病毒包装细胞系，并且已经鉴定了许多优选的细胞系。

4. 发明授权

US6045997A Materials and methods relating to the identification and sequencing of the BRCA2 cancer susceptibility gene and uses thereof 失效
标题翻译：与BRCA2癌症易感性基因的鉴定和测序相关的材料和方法及其用途
公开(公告)号：US6045997A
公开(公告)日：2000-04-04
申请号：US755587
申请日：1996-11-25
申请人： Phillip Andrew Futreal , Richard Francis Wooster , Alan Ashworth , Michael Rudolf Stratton
发明人： Phillip Andrew Futreal , Richard Francis Wooster , Alan Ashworth , Michael Rudolf Stratton
IPC分类号： A01K67/027 , A61K35/76 , A61K38/00 , A61K48/00 , A61P35/00 , A61P43/00 , C07K14/47 , C07K14/82 , C07K16/32 , C12N1/15 , C12N1/19 , C12N1/21 , C12N5/10 , C12N15/09 , C12P21/02 , C12P21/08 , C12Q1/68 , G01N33/15 , G01N33/50 , G01N33/53 , C07H21/02 , C07H21/04
CPC分类号： C07K14/4703 , A01K2217/05 , A61K38/00 , A61K48/00
摘要： The identification and sequencing of the BRCA2 gene is disclosed as well as the amino acid sequence of the corresponding BRCA2 polypeptides. BRCA2 alleles including those with mutations in the BRCA2 gene which are associated with a predisposition to develop cancer, especially breast and ovarian cancer are also disclosed. The present invention further relates to polypeptides encoded by the above nucleic acid. The present invention further relates to uses of much BRCA2 nucleic acid and BRCA2 polypeptides, in particular in the diagnostic, prognostic or therapeutic treatment of cancer.
摘要翻译：公开了BRCA2基因的鉴定和测序以及相应BRCA2多肽的氨基酸序列。还公开了BRCA2等位基因，包括与BRCA2基因突变相关的BRCA2等位基因，其与发生癌症的倾向相关，特别是乳腺癌和卵巢癌。本发明还涉及由上述核酸编码的多肽。本发明还涉及多个BRCA2核酸和BRCA2多肽的用途，特别是癌症的诊断，预后或治疗性治疗。

5. 发明授权

US5977065A Bacterial nitroreductase for the reduction of CB1954 and analogues thereof to a cytotoxic form 失效
标题翻译：用于将CB1954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：US5977065A
公开(公告)日：1999-11-02
申请号：US87855
申请日：1998-06-01
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 , A61K38/12 , C07K5/00 , C07K7/00
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.sup.1 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.2 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R1是使化合物R1NH2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 2 是化合物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。

6. 发明授权

US5958971A Chemical compounds 失效
公开(公告)号：US5958971A
公开(公告)日：1999-09-28
申请号：US956008
申请日：1997-10-22
申请人： Philip John Burke , Robert Ian Dowell , Anthony Brian Mauger , Caroline Joy Springer
发明人： Philip John Burke , Robert Ian Dowell , Anthony Brian Mauger , Caroline Joy Springer
IPC分类号： A61K31/17 , A61K31/195 , A61K31/27 , A61K31/41 , A61K39/395 , A61K45/00 , A61K47/48 , A61P35/00 , A61P43/00 , C07C237/20 , C07C237/40 , C07C269/04 , C07C271/54 , C07C275/24 , C07C275/40 , C07C275/42 , C07C309/66 , C07C309/69 , C07C309/72 , C07C311/51 , C07C317/50 , C07C323/58 , C07D257/04 , A01N47/10
CPC分类号： C07D257/04 , A61K47/48761 , B82Y5/00 , C07C237/20 , C07C271/54 , C07C275/24 , C07C275/40 , C07C309/66 , C07C311/51
摘要： Prodrugs, of generic formula I, are disclosed for use in antibody directed enzyme prodrug therapy (ADEPT). The prodrugs are substrates for carboxypeptidase G2 (CPG2) and yield more active cytotoxic drugs than known products of CPG2 catalyzed reactions.

7. 发明授权

US5281620A Compounds having antitumor and antibacterial properties 失效
标题翻译：具有抗肿瘤和抗菌特性的化合物
公开(公告)号：US5281620A
公开(公告)日：1994-01-25
申请号：US912466
申请日：1992-07-13
申请人： William A. Denny , Bruce C. Baguley , Graham J. Atwell , Gordon W. Rewcastle
发明人： William A. Denny , Bruce C. Baguley , Graham J. Atwell , Gordon W. Rewcastle
IPC分类号： C07D311/78 , C07D311/86 , C07D491/04 , A61K31/335
CPC分类号： C07D491/04 , C07D311/78 , C07D311/86
摘要： The novel class of xanthenone-4-acetic acids represented by the general formula (I) ##STR1## where R.sub.1 represents up to two of the groups lower alkyl, halogen, CF.sub.3, CN, NO.sub.2, NH.sub.2, CH.sub.2 COOH, OR.sub.2, OH, NHCOR.sub.2, NHSO.sub.2 R.sub.2, SR.sub.2, SO.sub.2 R.sub.2, CH.sub.2 CONHR.sub.2 or NHR.sub.2 (where R.sub.2 is lower alkyl optionally substituted with hydroxy, amino or methoxy functions), at any of the positions 1-8 which are available, R.sub.1 may also represent the substitution of an aza (--N.dbd.) group for one or two of the methine (--CH.dbd.) groups in the carbocyclic rings and two of R.sub.1 on any two available adjacent positions may also represent the grouping --CH.dbd.CH--CH.dbd.CH-- to form an additional fused benzene ring;and basic addition salts thereof, possess antitumour and antibacterial properties.
摘要翻译：由通式（I）表示的呫吨酮-4-乙酸的新型类别（I）其中R1代表至少两个低级烷基，卤素，CF 3，CN，NO 2，NH 2，CH 2 COOH，OR 2， OH，NHCOR 2，NHSO 2 R 2，SR 2，SO 2 R 2，CH 2 CONHR 2或NHR 2（其中R 2是任选被羟基，氨基或甲氧基官能团取代的低级烷基），在任何可用的位置1-8，R 1还可以代表碳环中的一个或两个次甲基（-CH =）基团和任何两个可用相邻位置上的两个R1中的氮杂（-N =）基团也可以表示组-CH = CH-CH = CH-以形成一个额外的稠合苯环; 及其碱式加成盐，具有抗肿瘤和抗菌的特性。

8. 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。

9. 发明授权

US07429578B2 Tricyclic inhibitors of poly(ADP-ribose) polymerases 有权
标题翻译：聚（ADP-核糖）聚合酶的三环抑制剂
公开(公告)号：US07429578B2
公开(公告)日：2008-09-30
申请号：US11221245
申请日：2005-09-06
申请人： Stephen Evan Webber , Stacie S. Canan-Koch , Jayashree Tikhe , Lars Henrik Thoresen
发明人： Stephen Evan Webber , Stacie S. Canan-Koch , Jayashree Tikhe , Lars Henrik Thoresen
IPC分类号： A61P35/00 , A61P43/00
CPC分类号： C07D471/06 , A61K31/277 , A61K31/4375 , C07D487/06
摘要： Compounds of the formula below are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapeutics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and neurodegenerative disease. As cancer therapeutics, the compounds of the invention may be used, e.g., in combination with cytotoxic agents and/or radiation.
摘要翻译：下式的化合物是聚（ADP-核糖基）转移酶（PARP）抑制剂，并且可用作治疗癌症和改善中风，头部创伤和神经变性疾病的作用的治疗剂。作为癌症治疗剂，可以使用本发明的化合物，例如与细胞毒性剂和/或辐射组合使用。

10. 发明授权

US06977298B2 Tricyclic inhibitors of poly(ADP-ribose) polymerases 有权
公开(公告)号：US06977298B2
公开(公告)日：2005-12-20
申请号：US11004261
申请日：2004-12-03
申请人： Stephen Evan Webber , Stacie S. Canan-Koch , Jayashree Tikhe , Lars Henrik Thoresen
发明人： Stephen Evan Webber , Stacie S. Canan-Koch , Jayashree Tikhe , Lars Henrik Thoresen
IPC分类号： A61K20060101 , A61K31/437 , A61K31/4375 , A61K31/55 , A61K31/551 , A61P20060101 , A61P3/10 , A61P9/10 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , C07D20060101 , C07D209/00 , C07D221/00 , C07D223/00 , C07D243/00 , C07D471/06 , C07D487/00 , C07D487/06 , C07D519/00 , C07D481/00
CPC分类号： C07D471/06 , A61K31/277 , A61K31/4375 , C07D487/06
摘要： Compounds of the formula below are poly(ADP-ribosyl)transferase (PARP) inhibitors, and are useful as therapeutics in treatment of cancers and the amelioration of the effects of stroke, head trauma, and neurodegenerative disease. As cancer therapeutics, the compounds of the invention may be used, e.g., in combination with cytotoxic agents and/or radiation.

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