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公开(公告)号：US20030220495A1
公开(公告)日：2003-11-27
申请号：US10071098
申请日：2002-02-11
IPC分类号： C07D265/30
CPC分类号： C07D233/64 , C07D231/12 , C07D233/56 , C07D249/08
摘要： The present invention relates to inhibitors of ras farnesylation of Formula (1), wherein T is of Formula (1) or (2) or (3), A is aryl or heteroaryl; B is aryl or heteroaryl; X and Y represent hydrogen, or both X and Y can represent a single bond (so as to form a double bond); R1 represents a group of Formula (II) or (III), the group of Formula (II) or Formula (III) (having L or D configuration at the chiral alpha carbon in the corresponding free amino acid); R2 represents hydrogen, aryl or heteroaryl; Z represents a direct bond, methylene, ethylene, vinylene, oxy, nullCH2nullOnull or nullOnullCH2null; and R3nullR4, p and r are as defined in the specification or a pharmaceutically-acceptable salt, prodrug or solvate thereof. Processes for their preparation, their use as therapeutic agents and pharmaceutical compositions containing them. A particular use is in cancer therapy.
摘要翻译： 本发明涉及式（1）的ras法呢基化抑制剂，其中T为式（1）或（2）或（3），A为芳基或杂芳基; B是芳基或杂芳基; X和Y表示氢，或者X和Y可以表示单键（从而形成双键）; R 1表示式（II）或（III）的基团，式（II）或式（III）的基团（在相应的游离氨基酸中的手性α碳处具有L或D构型）; R 2表示氢，芳基或杂芳基; Z表示直接键，亚甲基，亚乙基，亚乙烯基，氧基，-CH 2 -O-或-O-CH 2 - ; 和R 3 -R 4，p和r如说明书中所定义或其药学上可接受的盐，前药或溶剂化物。 其制备方法，用作治疗剂和含有它们的药物组合物。 一个特别的用途是癌症治疗。
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公开(公告)号：US20030018029A1
公开(公告)日：2003-01-23
申请号：US10136276
申请日：2002-05-02
申请人： ZENECA LIMITED
IPC分类号： C07D413/02 , C07D43/02 , A61K031/5377 , A61K031/517
CPC分类号： C07D231/12 , C07D233/56 , C07D239/94 , C07D249/08 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/04 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04 , C07D413/12 , C07D413/14
摘要： The invention concerns quinazoline derivatives of the formula I 1 wherein X1 is a direct link or a group such as CO, C(R2)2 and CH(OR2); wherein Q1 is phenyl, naphthyl or a 5- or 6-membered heteroaryl moiety and Q1 optionally bears up to 3 substituents; wherein m is 1 or 2 and each R1 may be a group such as hydrogen, halogeno and trifluoromethyl; and wherein Q2 may be phenyl or a 9- or 10-membered bicyclic heterocyclic moiety and Q2 optionally bears up to 3 substituents; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and the use of their receptor tyrosine kinase inhibitory properties in the treatment of proliferative disease such as cancer.
摘要翻译： 本发明涉及式I的喹唑啉衍生物，其中X 1是直接键或诸如CO，C（R 2）2和CH（OR 2）的基团。 其中Q1是苯基，萘基或5-或6-元杂芳基部分，并且Q1任选地带有至多3个取代基; 其中m为1或2，并且每个R 1可以为诸如氢，卤代和三氟甲基的基团; 并且其中Q2可以是苯基或9-或10-元双环杂环部分，Q2任选地带有多达3个取代基; 或其药学上可接受的盐; 其制备方法，含有它们的药物组合物及其受体酪氨酸激酶抑制性质在治疗增殖性疾病如癌症中的用途
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公开(公告)号：US20030119830A1
公开(公告)日：2003-06-26
申请号：US10194969
申请日：2002-07-15
申请人： ZENECA LIMITED
IPC分类号： A61K031/5377 , A61K031/496 , A61K031/42 , A61K031/405 , A61K031/4439 , C07D413/02
CPC分类号： A61K31/00
摘要： The invention concerns the use of a compound of formula (I), in which Z, X, T, A, R1, R2, p and q have any of the meanings defined herein, and their pharmaceutically acceptable salts or in vivo hydrolysable esters, in the treatment of a disease or condition mediated by monocyte chemoattractant protein-1 (MCP-1). Certain of the components of formula (I) are novel and are provided, together with pharmaceutical compositions thereof, as further features of the invention.
摘要翻译： 本发明涉及式（I）化合物的用途，其中Z，X，T，A，R 1，R 2，p和q具有本文定义的任何含义及其药学上可接受的盐或体内可水解的酯， 在治疗由单核细胞趋化蛋白-1（MCP-1）介导的疾病或病症。 式（I）的某些组分是新的，并且与其药物组合物一起提供作为本发明的进一步特征。
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公开(公告)号：US20030087240A1
公开(公告)日：2003-05-08
申请号：US09974870
申请日：2001-10-12
申请人： Zeneca Limited
IPC分类号： C12Q001/68 , C07H021/04 , C12P019/34
CPC分类号： C12Q1/6853 , C12Q1/6818 , C12Q1/6823 , C12Q2531/113 , C12Q2525/186 , C12Q2525/161 , C12Q2565/1025 , C12Q2561/119 , C12Q2525/301
摘要： A method for the detection of a target nucleic acid, which method comprises contacting template nucleic acid from a sample with (i) a signalling system and (ii) a tailed nucleic acid primer having a template binding region and the tail comprising a linker and a target binding region, in the presence of appropriate nucleoside triphosphates and an agent for polymerization thereof, under conditions such that the template binding region of the primer will hybridize to a complementary sequence in the template nucleic acid and be extended to form a primer extension product, separating any such product from the template whereupon the target binding region in the tail of the primer will hybridize to a sequence in the primer extension product corresponding to the target nucleic acid, and wherein any such target specific hybridization causes a detectable change in the signalling system, such that the presence or absence of the target nucleic acid in the sample is detected by reference to the presence or absence of a detectable change in the signalling system.
摘要翻译： 一种用于检测靶核酸的方法，所述方法包括使来自样品的模板核酸与（i）信号系统和（ii）具有模板结合区的尾部核酸引物接触，并且所述尾部包含接头和 在适当的核苷三磷酸和其聚合剂的存在下，在引物的模板结合区域将与模板核酸中的互补序列杂交并延伸以形成引物延伸产物的条件下， 将任何这样的产物与模板分离，因此引物尾部中的靶结合区域将与对应于靶核酸的引物延伸产物中的序列杂交，并且其中任何这样的靶特异性杂交引起信号系统中可检测的变化 ，使得通过参考前文检测样品中靶核酸的存在或不存在 信号系统中存在或不存在可检测的变化。
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公开(公告)号：US20020035738A1
公开(公告)日：2002-03-21
申请号：US09732561
申请日：2000-12-08
申请人： ZENECA Limited
发明人： Bart Pierre Helene Joseph Thomma , Franky Raymond Gerard Terras , Iris Anne Marie Armande Penninckx , John Michael Manners , Kemal Kazan , Willem Frans Broekaert
IPC分类号： A01H005/00
CPC分类号： A01N37/42 , A01N27/00 , A01N61/00 , C07K14/415 , C12N15/8237 , C12N15/8279
摘要： A method of protecting a plant against a pathogen is described, the method comprising inducing expression of a plant defensin gene by stimulating the jasmonate and/or ethylenc pathways. Also deseribed is a method of inducing expression of a plant defensin gene, a composition which is capable of inducing expression of a plant defensin gene and a method for screening compounds giving resistance-inducing activity. Preferably, the pathogen is a necrotrophic pathogen.
摘要翻译： 描述了保护植物免受病原体的方法，所述方法包括通过刺激茉莉酮酸和/或乙烯通路来诱导植物防御素基因的表达。 还可以诱导诱导植物防御素基因表达的方法，能够诱导植物防御素基因表达的组合物和筛选产生抗性诱导活性的化合物的方法。 优选地，病原体是坏死性病原体。
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公开(公告)号：US20010001101A1
公开(公告)日：2001-05-10
申请号：US09747254
申请日：2000-12-20
申请人： Zeneca Limited
IPC分类号： A61K031/4375 , C07D471/02
CPC分类号： C07D471/04 , A61K31/4745
摘要： The present invention provides a phenanthroline derivative of formula (I) 1 wherein, for example, R1 is hydrogen, carboxy, cyano, nitro, (1-4C)alkyl, (1-6C)alkoxycarbonyl, (1-4C)alkylamino, (2-4C)alkanoyl, (1-4C)alkoxy-(2-4C)alkoxy-(2-4C)alkoxycarbonyl or N-nullamino-(2-8C)alkylnullcarbamoyl; R2 is, for example, hydrogen, carboxy, (1-6C)alkoxycarbonyl, carbamoyl, N-(1-8C)alkylcarbamoyl, N,N-di-(1-8C)alkylcarbamoyl, N-(1-4C)alkylcyclohexylcarbamoyl, 1,2,3,4-tetrahydro-isoquinolin-2-ylcarbonyl or N,N-nulldi-(l -4C)alkylnullthiocarbamoyl; R3 and R4, which may be the same or different, are, for example, hydrogen or halo; and R5 is, for example, hydrogen, di-(1-4C)alkylamino or halo; or a pharmaceutically-acceptable salt thereof. The invention further provides pharmaceutical compositions comprising phenanthroline derivatives, processes for making the same and their use in producing an anti-fibroproliferative effect.
摘要翻译： 本发明提供式（I）的菲咯啉衍生物，其中例如R 1是氢，羧基，氰基，硝基，（1-4C）烷基，（1-6C）烷氧基羰基，（1-4C）烷基氨基，（2 -4C）烷酰基，（1-4C）烷氧基 - （2-4C）烷氧基 - （2-4C）烷氧基羰基或N- [氨基 - （2-8C）烷基]氨基甲酰基; R 2是例如氢，羧基，（1-6C）烷氧基羰基，氨基甲酰基，N-（1-8C）烷基氨基甲酰基，N，N-二（1-8C）烷基氨基甲酰基，N-（1-4C）烷基环己基氨基甲酰基， 1,2,3,4-四氢 - 异喹啉-2-基羰基或N，N- [二（1-4C）烷基]硫代氨基甲酰基; R 3和R 4可以相同或不同，例如是氢或卤素; 和R5是例如氢，二 - （1-4C）烷基氨基或卤素; 或其药学上可接受的盐。 本发明还提供了包含菲咯啉衍生物的药物组合物，其制备方法及其在产生抗纤维增生作用中的用途。
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公开(公告)号：US20020193375A1
公开(公告)日：2002-12-19
申请号：US10180337
申请日：2002-06-27
申请人： ZENECA LIMITED
发明人： Peter Warner , Roger James , Thorsten Nowak
IPC分类号： A61K031/53 , A61K031/513 , A61K031/501 , A61K031/497 , A61K031/444 , A61K031/4439
CPC分类号： C07D213/82
摘要： The invention relates to heterocyclic derivatives, or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The, invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, formula (I).
摘要翻译： 本发明涉及具有抗血栓形成和抗凝血性质的杂环衍生物或其药学上可接受的盐，因此可用于治疗人或动物的方法。 本发明还涉及制备杂环衍生物的方法，含有它们的药物组合物及其制备用于生产抗血栓形成或抗凝血作用的药物（式（I））的用途。
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公开(公告)号：US20020177169A1
公开(公告)日：2002-11-28
申请号：US10141833
申请日：2002-05-08
申请人： Zeneca Limited
IPC分类号： G01N033/53 , G01N033/543
CPC分类号： B01J19/0046 , B01J2219/00468 , B01J2219/005 , B01J2219/00502 , B01J2219/0054 , B01J2219/00547 , B01J2219/0059 , B01J2219/00592 , B01J2219/00596 , B01J2219/0072 , C40B70/00
摘要： A method for the preparation of a coded chemical library, which method comprises synthesising the chemical library on a plurality of synthesis particles and writing code on the synthesis particles using high-energy radiation during library synthesis, so as to provide the chemical library on a plurality of coded synthesis particles, and wherein the identity of library compounds associated with a synthesis particle is established by reference to its code.
摘要翻译： 一种制备编码化学文库的方法，该方法包括在文库合成期间使用高能量辐射在多个合成颗粒上合成化学文库并在合成颗粒上编写代码，以便提供多个化学文库 的编码合成颗粒，并且其中通过参考其代码确定与合成颗粒相关的文库化合物的身份。
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9.发明申请Crystalline dibenzothiazepine derivative and its use as an antipsychotic agent 审中-公开结晶二苯并硫氮杂衍生物及其作为抗精神病药的用途公开(公告)号：US20020147186A1
公开(公告)日：2002-10-10
申请号：US10101948
申请日：2002-03-21
申请人： Zeneca Limited
发明人： Evan William Snape
IPC分类号： A61K031/554 , C07D417/04
CPC分类号： C07D281/16
摘要： Crystalline 11-(4-null2-(2-hydroxyethoxy) ethylnull-1-piperazinyl)-dibenzonullb,fnull null1,4nullthiazepine (I) may be prepared by crystallising 11-(4-null2-(2-hydroxyethoxy) ethylnull-1-piperazinyl)-dibenzonullb,fnull null1,4nullthiazepine from a non-aromatic solvent such as ethyl acetate, isobutyl acetate, methyl iso-butylketone or methyl tert-butyl ether, preferably in the absence of water. The crystalline material produced may be converted into a pharmaceutically acceptable salt such as a fumarate. The crystalline 11-(4-null2-(2-hydroxyethoxy) ethylnull-1-piperazinyl)-dibenzo nullb,fnull null1,4nullthiazepine may be used to treat psychoses.
摘要翻译： 结晶的11-（4- [2-（2-羟基乙氧基）乙基] -1-哌嗪基） - 二苯并[b，f] [1,4]硫杂吗啉（I） （2-羟基乙氧基）乙基] -1-哌嗪基） - 二苯并[b，f] [1,4]硫杂吖庚因从非芳族溶剂如乙酸乙酯，异丁基乙酸酯，甲基异丁基酮或甲基叔丁基醚， 优选在没有水的情况下。 产生的结晶物质可以转化为药学上可接受的盐，例如富马酸盐。 结晶的11-（4- [2-（2-羟基乙氧基）乙基] -1-哌嗪基） - 二苯并[b，f] [1,4]硫氮杂菌可用于治疗精神病。
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公开(公告)号：US20020042408A1
公开(公告)日：2002-04-11
申请号：US09781556
申请日：2001-02-13
申请人： ZENECA LIMITED
IPC分类号： A61K031/397 , A61K031/407 , C07D498/08 , A61K031/403
CPC分类号： C07D477/20 , A61K31/40 , A61K31/407 , A61K31/41 , C07D207/16 , C07D403/12 , C07F9/568
摘要： The present invention relates to carbapenems and provides a compound of the formula (I): 1 or a pharmaceutically acceptable salt or in vivo hydrolysable ester thereof wherein: R1 is 1-hydroxyethyl, 1-fluoroethyl or hydroxymethyl; R2 is hydrogen or C1-4alkyl; R3 is hydrogen or C1-4alkyl; R4 and R5 are the same or different and are selected from hydrogen, halo, cyano, C1-4alkyl, nitro, hydroxy, carboxy, C1-4alkoxy, C1-4alkoxycarbonyl, aminosulphonyl, C1-4alkylaminosulphonyl, di-C1-4-alkylaminosulphonyl, carbamoyl, C1-4alkylcarbamoyl, di-C1-4 alkylcarbamoyl, trifluoromethyl, sulphonic acid, amino, C1-4alkylamino, di-C1-4alkylamino, C1-4alkanoylamino, C1-4alkanoyl(NnullC1-4alkyl)amino, C1-4alkanesulphonamido and C1-4alkylS(O)nnull wherein n is zero; one or two: with the proviso that there is no hydroxy or carboxy substituent in a position ortho to the link to nullNR3null. Processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.
摘要翻译： 本发明涉及碳青霉烯并提供式（I）化合物或其药学上可接受的盐或体内可水解的酯，其中：R1是1-羟乙基，1-氟乙基或羟甲基; R2是氢或C1-4烷基; R3是氢或C1-4烷基; R4和R5相同或不同，选自氢，卤素，氰基，C1-4烷基，硝基，羟基，羧基，C1-4烷氧基，C1-4烷氧基羰基，氨基磺酰基，C1-4烷基氨基磺酰基，二-C1-4烷基氨基磺酰基， 氨基甲酰基，C 1-4烷基氨基甲酰基，二-C 1-4烷基氨基甲酰基，三氟甲基，磺酸，氨基，C 1-4烷基氨基，二-C 1-4烷基氨基，C 1-4烷酰基氨基，C 1-4烷酰基（N-C 1-4烷基）氨基，C 1-4烷基磺酰胺基和 C 1-4烷基S（O）n - ，其中n为零; 一个或两个：条件是在与-NR 3 - 的连接相邻的位置处不存在羟基或羧基取代基。 其制备方法，制备中的中间体，其作为治疗剂的用途和含有它们的药物组合物。
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