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1. 发明申请

WO2011144578A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2011144578A1
公开(公告)日：2011-11-24
申请号：PCT/EP2011/057902
申请日：2011-05-16
申请人： SENEXIS LIMITED , HORWELL, David Christopher , SCOPES, David Ian Carter
发明人： HORWELL, David Christopher , SCOPES, David Ian Carter
IPC分类号： C07D413/04 , C07D498/04 , A61K31/538 , A61K31/553 , A61P25/28
CPC分类号： C07D413/04 , C07D498/04
摘要： A compound of formula (I) or a pharmaceutically acceptable salt or prodrug thereof wherein X is N or CH; Q is NR 6 or O; A 1 and A 2 are independently hydrogen or C 1-6 alkyl or may together form a carbonyl group; R 1 and R 2 are independently hydrogen, halogen, CF 3 , CN, OR 7 , OR 8 , NR 8 R 9 , NR 8 COR 10 , NR 8 S0 2 R 10 , S0 2 NR 8 R 9 , SO 2 R 10 or C 1-6 alkyl optionally and independently substituted by one or more of hydroxyl, C 1-6 alkoxy, halogen or NR 8 R 9 ; R 3 is hydrogen, halogen, CF3 or OR 7; R4 is hydrogen, halogen, CF3, OR8, NR8R9, NR8COR10, NR8S02R10 or C1-6 alkyl optionally substituted by hydroxyl, C1-6 alkoxy or NR 8 R 9; or when R 3 and R 4 are positioned ortho and taken together form -0(CH 2 ) m O-, where m is 1-3; R 5 is hydrogen or C 1-6 alkyl optionally substituted by hydroxyl, C 1-6 alkoxy or NR 8 R 9 ; R 6 is hydrogen or C 1-6 alkyl; R 7 is hydrogen or C 1-6 alkyl optionally substituted by OR 8 or NR 8 R 9 ; R 8 is hydrogen, C 1-6 alkyl, optionally substituted by hydroxyl or C 1-6 alkoxy or C 1-3 alkylphenyl wherein said phenyl group is optionally substituted by one or more substituents selected from halogen, C 1-6 alkyl, CF 3 , OR 7 , NR 8 R 9 or OCF 3 ; or the groups R 8 and R 9 when they are attached to a nitrogen atom may together form a 5- or 6-membered ring which optionally contains one further heteroatom selected from NR 7 , S and O said 5 or 6 membered ring being optionally substituted by hydroxyl or C 1-6 alkoxy; or the groups R 8 and R 9 when they are attached to a nitrogen atom may together form an azetidinyl ring optionally substituted by hydroxyl or C 1-6 alkoxy; and R 10 is C 1-6 alkyl or a phenyl group optionally substituted by one or more substituents selected from halogen, C 1-6 alkyl, CF 3 , OCF 3 or OR 7 ; and n is 1 or 2. The use of the compounds in treating amyloid disease is also disclosed.
摘要翻译：式（I）化合物或其药学上可接受的盐或前药，其中X为N或CH; Q是NR6或O; A1和A2独立地是氢或C1-6烷基，或者可以一起形成羰基; R1和R2独立地是氢，卤素，CF3，CN，OR7，OR8，NR8R9，NR8COR10，NR8S02R10，SO2NR8R9，SO2R10或C1-6烷基，任选和独立地被一个或多个羟基，C 1-6烷氧基，卤素或NR 8取代 R9; R 3是氢，卤素，CF 3或OR 7; R4是氢，卤素，CF3，OR8，NR8R9，NR8COR10，NR8S02R10或任选被羟基，C 1-6烷氧基或NR 8 R 9取代的C 1-6烷基; 或当R3和R4相邻并且一起形成-O（CH 2）m O-时，其中m是1-3; R5是氢或任选被羟基取代的C 1-6烷基，C 1-6烷氧基或NR 8 R 9; R6是氢或C1-6烷基; R 7是氢或任选被OR 8或NR 8 R 9取代的C 1-6烷基; R 8是氢，任选地被羟基或C 1-6烷氧基取代的C 1-6烷基或C 1-3烷基苯基，其中所述苯基任选被一个或多个选自卤素，C 1-6烷基，CF 3，OR 7，NR 8 R 9或 OCF 3; 或基团R8和R9可以一起形成5-或6-元环，其任选地含有一个选自NR7，S和O的另外的杂原子，所述5或6元环任选地被羟基或 C 1-6烷氧基或者当基团R8和R9连接到氮原子时可以一起形成任选被羟基或C 1-6烷氧基取代的氮杂环丁烷基环; R 10是C 1-6烷基或任选被一个或多个选自卤素，C 1-6烷基，CF 3，OCF 3或OR 7的取代基取代的苯基; 并且n为1或2.还公开了化合物在治疗淀粉样蛋白病中的用途。

2. 发明申请

WO2005121149A1 FURANOPYRIMIDINE COMPOUNDS EFFECTIVE AS POTASSIUM CHANNEL INHIBITORS 审中-公开
标题翻译：作为钾通道抑制剂有效的氟脲嘧啶化合物
公开(公告)号：WO2005121149A1
公开(公告)日：2005-12-22
申请号：PCT/GB2005/002318
申请日：2005-06-10
申请人： XENTION DISCOVERY LIMITED , FORD, John , PALMER, Nicholas, John , ATHERALL, John, Frederick , MADGE, David, John
发明人： FORD, John , PALMER, Nicholas, John , ATHERALL, John, Frederick , MADGE, David, John
IPC分类号： C07D491/04
CPC分类号： C07D491/04
摘要： A compound of formula (I) wherein R1 is aryl, heteroaryl, cycloalkyl or alkyl; R2 is H, alkyl, nitro, -CO 2 R7, CONR4R5 or halo; R3 is H, NR4R5, NC(O)R8, halo, trifluoromethyl, alkyl, nitrile or alkoxy; R4 and R5 may be the same or different, and may be H, alkyl, aryl, heteroaryl or cycloalkyl; or R4 and R5 may together form a saturated, unsaturated or partially saturated 4 to 7 member ring, wherein said ring may optionally comprise one or more further heteroatoms selected from N, O or S; X is O, S or NR6; R6 is H or alkyl; R7 is hydrogen, methyl or ethyl; R8 is methyl or ethyl; Ll is (CH 2 ) n , where n is 1,2 or 3; and Y is aryl, a heterocyclic group, alkyl, alkenyl or cycloalkyl; together with pharmaceutically acceptable salts thereof. The use of these compounds as potassium channel inhibitors is also described.
摘要翻译：式（I）的化合物，其中R 1是芳基，杂芳基，环烷基或烷基; R2是H，烷基，硝基，-CO 2 R 7，CONR 4 R 5或卤素; R3是H，NR4R5，NC（O）R8，卤素，三氟甲基，烷基，腈或烷氧基; R 4和R 5可以相同或不同，并且可以是H，烷基，芳基，杂芳基或环烷基; 或R 4和R 5可以一起形成饱和的，不饱和的或部分饱和的4至7元环，其中所述环可任选地包含一个或多个选自N，O或S的其它杂原子; X是O，S或NR 6; R6是H或烷基; R7是氢，甲基或乙基; R8是甲基或乙基; L 1是（CH 2）n，其中n是1,2或3; Y为芳基，杂环基，烷基，链烯基或环烷基; 以及其药学上可接受的盐。还描述了这些化合物作为钾通道抑制剂的用途。

3. 发明申请

WO2005061611A1 COMPOSITIONS OF SEMI-INTERPENETRATING POLYMER NETWORK 审中-公开
标题翻译：半导体聚合物网络的组成
公开(公告)号：WO2005061611A1
公开(公告)日：2005-07-07
申请号：PCT/GB2004/005443
申请日：2004-12-22
申请人： INNOMED LIMITED , WHITE, Barry, James , RODDEN, Gillina, Isabella
发明人： WHITE, Barry, James , RODDEN, Gillina, Isabella
IPC分类号： C08L5/08
CPC分类号： A61L27/52 , C08B37/003 , C08J3/246 , C08J2303/02 , C08J2305/02 , C08J2305/04 , C08J2305/08 , C08L5/08 , C08L2203/02 , C08L2205/02 , C08L2205/04 , C08L2666/02 , C08L2666/26
摘要： Novel compositions consisting of semi-interpenetrating network of cross-linked water soluble derivatives of basic polysaccharides and a non-cross-linked component, which is an anionic polysaccharide are provided. Methods for the production of such compositions are also disclosed. Preferably the basic polysaccharide is chitosan or a derivative thereof and the anionic polysaccharide is hyaluronic acid. The compositions can be formed into gels or films, for example, and thus find use in a wide range of medical applications in the fields of dermatology, plastic surgery, urology and orthopaedics.
摘要翻译：提供由基础多糖的交联水溶性衍生物的半互穿网络和作为阴离子多糖的非交联成分组成的新型组合物。还公开了制备这种组合物的方法。碱性多糖优选为壳聚糖或其衍生物，阴离子多糖为透明质酸。组合物可以例如形成凝胶或膜，因此可用于皮肤病学，整形外科学，泌尿科和骨科学领域的广泛的医学应用。

4. 发明申请

WO2005054257A1 VANADIUM COMPOUNDS AS INHIBITORS OF PHOSPHATASES 审中-公开
标题翻译： VANADIUM化合物作为磷酸盐抑制剂
公开(公告)号：WO2005054257A1
公开(公告)日：2005-06-16
申请号：PCT/GB2004/005080
申请日：2004-12-06
申请人： IMPERIAL COLLEGE INNOVATIONS LIMITED , WOSCHOLSKI, Rudiger , ROSIVATZ, Erika , VILAR, Ramon
发明人： WOSCHOLSKI, Rudiger , ROSIVATZ, Erika , VILAR, Ramon
IPC分类号： C07F9/00
CPC分类号： C07F9/005
摘要： Novel Vanadium compounds are described as well as their use as inhibitors of phosphatases, particularly inositol phosphatases, The use of the compound in the treatment of nerodegenerative diseases is also described.
摘要翻译：描述了新的钒化合物以及它们作为磷酸酶抑制剂，特别是肌醇磷酸酶的用途。还描述了该化合物在治疗神经复发性疾病中的用途。

5. 发明申请

WO2005040425A2 PARALLEL POLYMER SEQUENCING METHODS 审中-公开
标题翻译：并行聚合物测序方法
公开(公告)号：WO2005040425A2
公开(公告)日：2005-05-06
申请号：PCT/GB2004/004432
申请日：2004-10-20
申请人： ISIS INNOVATION LTD , SHCHEPINOV, Mikhail, S. , MIR, Kalim
发明人： SHCHEPINOV, Mikhail, S. , MIR, Kalim
IPC分类号： C12Q1/68
CPC分类号： C12Q1/6874 , C12Q1/6818 , C12Q1/6869 , G01N21/6428 , G01N2021/6432 , G01N2021/6441 , C12Q2565/501 , C12Q2565/101 , C12Q2563/155 , C12Q2565/518 , C12Q2533/107 , C12Q2535/122 , C12Q2533/101 , C12Q2563/173 , C12Q2565/301 , C12Q2561/113
摘要： The present invention relates to a method of sequencing a target polynucleotide by enzymatic and/or chemical means. The sequencing method includes a method for characterizing multiple alleles in a sample, a method of calculating confidence levels in ascertained sequences, a method for comparing polynucleotide sequences and a method of resolving ambiguities in a polynucleotide sequence. It also provides methods for appropriately preparing samples, for immobilising template molecules, for organising the template molecules and to conduct the sequencing of many molecules in parallel. The method involves analysing molecules as members of an array. Many target polynucleotides or many segments of a single target polynucleotide can be sequenced simultaneously. In a preferred embodiment the method involves analysing individual molecules within an array and base calls are based on the signals from two or more molecules. A method to prevent non-specific signal in sequencing is also provided. The invention is readily automated, both for small-scale and large-scale operation and relevant algorithms and the composition of kits and systems are provided.
摘要翻译：本发明涉及通过酶和/或化学方法测序靶多核苷酸的方法。测序方法包括用于表征样品中多个等位基因的方法，计算确定序列中的置信水平的方法，用于比较多核苷酸序列的方法和解决多核苷酸序列中的模糊度的方法。它还提供了适当制备样品，固定模板分子，组织模板分子和并行进行许多分子测序的方法。该方法包括分析分子作为阵列的成员。单个靶多核苷酸的许多靶多核苷酸或许多片段可以同时测序。在优选实施方案中，该方法包括分析阵列内的各个分子，并且基于来自两个或更多个分子的信号进行碱基呼叫。还提供了一种在排序中防止非特异性信号的方法。本发明容易地自动化，用于小规模和大规模操作以及相关算法，并提供了套件和系统的组成。

6. 发明申请

WO2003004147A2 COMPOUND LIBRARIES 审中-公开
标题翻译：复合图书馆
公开(公告)号：WO2003004147A2
公开(公告)日：2003-01-16
申请号：PCT/GB2002/003094
申请日：2002-07-05
申请人： BIOFOCUS PLC , CROSSLEY, Roger , ROSE, Valerie, Sarah , STEVENS, Adrian, Philip
发明人： CROSSLEY, Roger , ROSE, Valerie, Sarah , STEVENS, Adrian, Philip
IPC分类号： B01J19/00
CPC分类号： C40B50/02 , B01J2219/007 , B01J2219/00725 , C07D261/16 , C40B40/10 , G06F19/16
摘要： The present invention provides methods for producing compound libraries. One such method involves a number of steps to generate a model of a biological target using sequence information of that target and then using the model to define microenvironments which are capable of interacting with a ligand. The microenvironments can then be used to define motifs which interact with the microenvironments, the motifs then being used to generate the compound library. An alternative method makes use of X-ray crystal structures of biological targets to produce compound libraries.
摘要翻译：本发明提供了制备化合物文库的方法。一种这样的方法包括使用该靶的序列信息生成生物靶的模型的许多步骤，然后使用该模型来定义能够与配体相互作用的微环境。然后可以使用微环境来定义与微环境相互作用的基序，然后用于产生化合物文库的基序。另一种方法是利用生物靶标的X射线晶体结构产生化合物文库。

7. 发明申请

WO2011144577A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2011144577A1
公开(公告)日：2011-11-24
申请号：PCT/EP2011/057900
申请日：2011-05-16
申请人： SENEXIS LIMITED , HORWELL, David , SCOPES, David
发明人： HORWELL, David , SCOPES, David
IPC分类号： C07D239/47 , A61K31/505 , A61P25/28
CPC分类号： C07D239/47
摘要： A compound of formula (I) or a pharmaceutically acceptable salt or prodrug thereof: wherein R 1 is CN; R 2 is H or F; R 3 and R 4 are independently hydrogen, fluorine, chlorine or OR 8 ; R 5 is hydrogen, C 1-6 alkyl, C 1-6 alkenyl or C 1-6 alkynyl; R 6 and R 7 are independently hydrogen, halogen, OR 8 or NR 9 R 10 ; R 8 is hydrogen or C 1-6 alkyl; R 9 and R 10 are independently hydrogen or C 1-6 alkyl; or the groups R 9 and R 10 when they are attached to a nitrogen atom may together form a 5- or 6-membered ring which optionally contains one further heteroatom selected from NR 8 , S and O said 5 or 6 membered ring being optionally substituted by hydroxyl or C 1-6 alkoxy; or the groups R 9 and R 10 when they are attached to a nitrogen atom may together form an azetidinyl ring optionally substituted by hydroxyl or C 1-6 alkoxy, is provided. The use of such compounds in treating amyloid-related disease is also disclosed.
摘要翻译：式（I）化合物或其药学上可接受的盐或前药：其中R1为CN; R2为H或F; R3和R4独立地是氢，氟，氯或OR8; R5是氢，C1-6烷基，C1-6链烯基或C1-6炔基; R6和R7独立地是氢，卤素，OR8或NR9R10; R8是氢或C1-6烷基; R9和R10独立地是氢或C1-6烷基; 或当基团连接到氮原子上时，基团R 9和R 10可以一起形成5-或6-元环，其任选地含有一个选自NR 8，S和O的另外的杂原子，所述5或6元环任选被羟基或 C 1-6烷氧基或者当它们连接到氮原子上时，基团R 9和R 10可以一起形成任选被羟基或C 1-6烷氧基取代的氮杂环丁烷基环。还公开了这些化合物在治疗淀粉样蛋白相关疾病中的用途。

8. 发明申请

WO2010139953A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2010139953A1
公开(公告)日：2010-12-09
申请号：PCT/GB2010/001092
申请日：2010-06-04
申请人： XENTION LIMITED , HAMLYN, Richard, John , MADGE, David , MULLA, Mushtaq
发明人： HAMLYN, Richard, John , MADGE, David , MULLA, Mushtaq
IPC分类号： C07D209/46 , C07D217/24 , C07D401/12 , C07D403/12
CPC分类号： C07D209/46 , C07D217/24 , C07D401/12 , C07D403/12
摘要： A compound of formula (I): or its salts or pharmaceutically acceptable derivatives thereof wherein; A represents a chemical moiety with the general formula (II): X is selected from a group consisting of CH 2 , C(=O), CH(R 5 ), C(R 5 )(R 6 ) or C(R 5 )(R 6 )CH 2 ; R 1 is selected from the group consisting of optionally substituted arylalkyl, and optionally substituted heteroarylalkyl; R 2 is selected from the group consisting of optionally substituted aryl or optionally substituted heteroaryl or NR 7 R 8 ; R 3 is selected from the group consisting of hydrogen, halogen, hydroxyl, alkoxy, aryloxy, optionally substituted alkyl, optionally substituted amino, optionally substituted amino sulfonyl or nitrile; R4 is selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted acyl, optionally substituted sulfonyl, optionally substituted sulfamoyl, optionally substituted aryl, optionally substituted arylalkyl, and optionally substituted heteroaryl; R 5 and R 6 for each occurrence is optionally substituted alkyl; R 7 and R 8 are the same or different and each represents hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted arylalkyl, optionally substituted aryl or optionally substituted heteroaryl; n = 1 or 2 is provided. Pharmaceutical compositions comprising the compounds are also provided. The compounds are useful in treating various conditions including arrhythmia.
摘要翻译：式（I）的化合物或其盐或药学上可接受的衍生物，其中： A表示具有通式（II）的化学部分：X选自CH 2，C（= O），CH（R 5），C（R 5）（R 6）或C（R 5）（R 6）CH 2 ; R 1选自任选取代的芳基烷基和任选取代的杂芳基烷基; R 2选自任选取代的芳基或任选取代的杂芳基或NR 7 R 8; R 3选自氢，卤素，羟基，烷氧基，芳氧基，任选取代的烷基，任选取代的氨基，任选取代的氨基磺酰基或腈; R 4选自氢，任选取代的烷基，任选取代的环烷基，任选取代的杂环烷基，任选取代的酰基，任选取代的磺酰基，任选取代的氨磺酰基，任选取代的芳基，任选取代的芳烷基和任选取代的杂芳基; R5和R6每次出现是任选取代的烷基; R 7和R 8相同或不同，各自表示氢，任选取代的烷基，任选取代的环烷基，任选取代的芳烷基，任选取代的芳基或任选取代的杂芳基; 提供n = 1或2。还提供了包含该化合物的药物组合物。该化合物可用于治疗各种病症，包括心律失常。

9. 发明申请

WO2006087536A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2006087536A1
公开(公告)日：2006-08-24
申请号：PCT/GB2006/000519
申请日：2006-02-15
申请人： ISIS INNOVATION LIMITED , JAMES, William , SPROAT, Brian, Stephen
发明人： JAMES, William , SPROAT, Brian, Stephen
IPC分类号： C12N15/11 , A61K31/713 , A61K31/7115
CPC分类号： C12N15/115 , C12N2310/16 , C12N2310/322
摘要： The present invention provides novel aptamer derivatives which are useful in binding to and neutralising viruses. Pharmaceutical formualtions comprising the aptamers and the use of the aptamers in screening for useful compounds are also provided.
摘要翻译：本发明提供了可用于结合和中和病毒的新的适体衍生物。还提供了包含适体和适配体在筛选有用化合物中的用途的药物制剂。

10. 发明申请

WO2005099752A2 ANTIGEN DELIVERY VECTORS AND CONSTRUCTS 审中-公开
标题翻译：抗原递送载体和构建体
公开(公告)号：WO2005099752A2
公开(公告)日：2005-10-27
申请号：PCT/GB2005/001279
申请日：2005-04-01
申请人： IMMUNE TARGETING SYSTEMS , BONNET, Dominique , BROWN, Carlton, B. , GEORGES, Bertrand , SIZER, Philip, J.
发明人： BONNET, Dominique , BROWN, Carlton, B. , GEORGES, Bertrand , SIZER, Philip, J.
IPC分类号： A61K39/385
CPC分类号： A61K47/48023 , A61K31/02 , A61K38/02 , A61K39/00 , A61K39/12 , A61K39/21 , A61K39/385 , A61K47/54 , A61K2039/54 , A61K2039/543 , A61K2039/545 , A61K2039/55511 , A61K2039/5555 , A61K2039/55566 , A61K2039/60 , A61K2039/6018 , C07C19/08 , C07C57/52 , C07K2/00 , C07K14/005 , C12N7/00 , C12N2740/16022 , C12N2740/16034 , C12N2740/16122 , C12N2740/16134 , C12N2740/16322
摘要： The present invention relates to fluorocarbon vectors for the delivery of antigens to immunoresponsive target cells. It further relates to fluorocarbon vector-antigen constructs and the use of such vectors associated with antigens as vaccines and immunotherapeutics in animals.
摘要翻译：本发明涉及用于将抗原递送至免疫应答性靶细胞的碳氟化合物载体。它进一步涉及氟碳载体 - 抗原构建体以及与抗原相关的载体在动物中作为疫苗和免疫治疗剂的用途。

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