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41. 发明申请

WO2005074677A1 TRANSGENIC ANIMALS FOR ASSESSING DRUG METABOLISM AND TOXICITY IN MAN 审中-公开
标题翻译：用于评估人体中药物代谢和毒性的转基因动物
公开(公告)号：WO2005074677A1
公开(公告)日：2005-08-18
申请号：PCT/GB2005/000382
申请日：2005-02-03
申请人： IMPERIAL CANCER RESEARCH TECHNOLOGY LIMITED , WOLF, Charles, Roland , HENDERSON, Colin, J
发明人： WOLF, Charles, Roland , HENDERSON, Colin, J
IPC分类号： A01K67/027
CPC分类号： A01K67/0278 , A01K2207/15 , A01K2217/00 , A01K2227/105 , A01K2267/03 , C07K14/80 , C07K2319/00 , C12N9/0042 , C12N2800/30
摘要： A method of introducing at least one human cytochrome P450 into a non-human animal c ell in which corresponding endogenous P450 enzyme activities have been disabled, thus the method provides a way of using a non-human animal cell to make predictions regarding P450-mediated metabolism in a human. The present invention also provides transgenic non-human animals produced by the method of the invention and uses therefor, especially in assessing xenobiotic/drug metabolism and toxicity.
摘要翻译：将至少一种人细胞色素P450引入非活性动物体内的方法，其中相应的内源性P450酶活性已被禁用，因此该方法提供了使用非人类动物细胞对P450介导的预测方法人类的新陈代谢本发明还提供了通过本发明的方法生产的转基因非人动物，并且用于此，特别是在评估异生物/药物代谢和毒性方面。

42. 发明申请

WO2005061463A1 PYRAZOLE DERIVATIVES AS PROTEIN KINASE MODULATORS 审中-公开
标题翻译：作为蛋白激酶调节剂的吡唑衍生物
公开(公告)号：WO2005061463A1
公开(公告)日：2005-07-07
申请号：PCT/GB2004/005464
申请日：2004-12-23
申请人： ASTEX TECHNOLOGY LIMITED , CANCER RESEARCH TECHNOLOGY LIMITED , THE INSTITUTE OF CANCER RESEARCH: ROYAL CANCER HOSPITAL , BERDINI, Valerio , SAXTY, Gordon , VERDONK, Marinus, Leendert , WOODHEAD, Steven, John , WYATT, Paul, Graham , BOYLE, Robert, George , SORE, Hannah, Fiona , WALKER, David, Winter , COLLINS, Ian , DOWNHAM, Robert , CARR, Robin, Arthur, Ellis
发明人： BERDINI, Valerio , SAXTY, Gordon , VERDONK, Marinus, Leendert , WOODHEAD, Steven, John , WYATT, Paul, Graham , BOYLE, Robert, George , SORE, Hannah, Fiona , WALKER, David, Winter , COLLINS, Ian , DOWNHAM, Robert , CARR, Robin, Arthur, Ellis
IPC分类号： C07D231/12
CPC分类号： A61K31/415 , A61K9/0019 , A61K9/20 , A61K9/48 , A61K31/4155 , A61K31/4178 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/5377 , A61K31/551 , A61K45/06 , C07D231/12 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/10 , C07D403/12 , C07D405/04 , C07D413/10
摘要： The invention provides compounds of the formula: (I) having protein kinase B inhibiting activity: wherein A is a saturated hydrocarbon linker group containing from 1 to 7 carbon atoms, the linker group having a maximum chain length of 5 atoms extending between R l and NR 2 R 3 and a maximum chain length of 4 atoms extending between E and NR 2 R 3 , wherein one of the carbon atoms in the linker group may optionally be replaced by an oxygen or nitrogen atom; and wherein the carbon atoms of the inker group A may optionally bear one or more substituents selected from oxo, fluorine and hydroxy, provided that the hydroxy group when present is not located at a carbon atom a with respect to the NR 2 R 3 group and provided that the oxo group when present is located at a carbon atom a with respect to the NR 2 R 3 group; E is a monocyclic or bicyclic carbocyclic or heterocyclic group; R l is an aryl or heteroaryl group; and R 2 , R 3 , R 4 and R 5 are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, methods for preparing the compounds and their use as anticancer agents.
摘要翻译：本发明提供下式的化合物：（I）具有蛋白激酶B抑制活性：其中A是含有1至7个碳原子的饱和烃连接基团，该连接基团的最大链长度在R 1之间延伸 >和NR 2 R 3，并且在E和NR 2 R 3之间延伸的4个原子的最大链长度，其中连接基团中的一个碳原子可以任选地被氧或氮代替原子; 并且其中，墨水基团A的碳原子可以任选地具有一个或多个选自氧代，氟和羟基的取代基，条件是当存在的羟基不相对于NR 2 R'位于碳原子a时，并且条件是当存在的氧代基位于相对于NR 2 R 3基团的碳原子a时; E是单环或双环碳环或杂环基; R 1是芳基或杂芳基; R 2，R 3，R 4和R 5如权利要求中所定义。还提供含有化合物的药物组合物，制备化合物的方法及其作为抗癌剂的用途。

43. 发明申请

WO2005012305A2 THERAPEUTIC COMPOUNDS 审中-公开
标题翻译：治疗化合物
公开(公告)号：WO2005012305A2
公开(公告)日：2005-02-10
申请号：PCT/GB2004/003183
申请日：2004-07-23
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , HELLEDAY, Thomas , CURTIN, Nicola
发明人： HELLEDAY, Thomas , CURTIN, Nicola
IPC分类号： C07D487/00
CPC分类号： C07D487/06 , A61K31/5517 , A61K38/005 , C12N15/1137 , C12N2310/14 , C12Y204/0203
摘要： The invention relates to trycyclic lactam indole derivatives and triacyclic lactam benzimodole derivatives and their use in inhibiting the activity of PARP enzyme. The invention also relates to the use of these compounds in the preparation of medicaments.
摘要翻译：本发明涉及三环内酰胺衍生物和三环内酰胺苯并三唑衍生物及其在抑制PARP酶活性中的应用。本发明还涉及这些化合物在制备药物中的用途。

44. 发明申请

WO2004087955A1 MARKERS FOR ROSCOVITINE 审中-公开
标题翻译： ROSCOVITINE的标志
公开(公告)号：WO2004087955A1
公开(公告)日：2004-10-14
申请号：PCT/GB2004/001337
申请日：2004-03-26
申请人： CYCLACEL LIMITED , CANCER RESEARCH TECHNOLOGY LIMITED , GREEN, Simon, R. , WORKMAN, Paul , WHITTAKER, Steven, R.
发明人： GREEN, Simon, R. , WORKMAN, Paul , WHITTAKER, Steven, R.
IPC分类号： C12Q1/68
CPC分类号： G01N33/5023 , C12Q1/6809 , G01N33/5008
摘要： The present invention relates to pharmacodynamic markers for CDKIs including the candidate 2, 6, 9-tri-substituted purine known as roscovitine. The identity of these markers facilitates the convenient identification of roscovitine-like activity both in vitro and in vivo .
摘要翻译：本发明涉及用于CDKI的药效学标志物，其包括称为roscovitine的候选2,6,9-三取代的嘌呤。这些标记的身份有助于方便地鉴定体内和体外的罗可嘌呤样活性。

45. 发明申请

WO2003074059A3 MATERIALS AND METHODS RELATING TO THE TREATMENT OF LYMPHOMA 审中-公开
公开(公告)号：WO2003074059A3
公开(公告)日：2003-09-12
申请号：PCT/GB2003/000783
申请日：2003-02-24
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , ZHU, Delin , STEVENSON, Freda
发明人： ZHU, Delin , STEVENSON, Freda
IPC分类号： A61K31/70
摘要： The invention provides materials and methods for diagnosing and treating non-Hodgkins lymphoma, particularly follicular lymphoma and Burkitt's lymphoma, based on the abnormal glycosylation status of the immunoglobulins on B lymphocytes.

46. 发明申请

WO2003059885A1 THERAPEUTIC ACRIDONE AND ACRIDINE COMPOUNDS 审中-公开
标题翻译：治疗阿司匹林和阿司匹林化合物
公开(公告)号：WO2003059885A1
公开(公告)日：2003-07-24
申请号：PCT/GB2003/000102
申请日：2003-01-14
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , NEIDLE, Stephen , HARRISON, Richard, John , KELLAND, Lloyd, Royston , GOWAN, Sharon, Michele , READ, Martin, Anthony , RESZKA, Anthony
发明人： NEIDLE, Stephen , HARRISON, Richard, John , KELLAND, Lloyd, Royston , GOWAN, Sharon, Michele , READ, Martin, Anthony , RESZKA, Anthony
IPC分类号： C07D219/08
CPC分类号： C07D219/08 , C07D219/10
摘要： This invention pertains to certain acridone and acridine compounds of the formula (1) which inhibit telomerase, regulate cell proliferation, etc., and/or treat cancer, proliferative conditions, etc.: wherein either: (a) K is =O, L is -H, alpha single bond, beta is a double bond, gamma is a single bond (acridones); or, (b) K is a 9-substituent, L is absent, alpha is a double bond, beta is a single bond, gamma is a double bond (acridines); and wherein: J 1 is a 2- or 3-substituent; J 2 is a 6- or 7-substituent; J 1 and J 2 are each a group of the formula -N(R N )-W, wherein: R N is a nitrogen substituent and is hydrogen, C 1-7 alkyl, C 3-20 heterocyclyl, or C 5-20 aryl, and is optionally substituted; and, W is C 1-7 alkyl, C 3-20 heterocyclyl, or C 5-20 aryl, and is optionally substituted; and, wherein, when K is a 9-substituent, K is a group of the formula -N(R N )-Q, wherein: R N is an amino substituent and is hydrogen, C 1-7 alkyl, C 3-20 heterocyclyl, or C 5-20 aryl; and, Q is C 1-7 alkyl, C 3-20 heterocyclyl, or C 5-20 aryl, and is optionally substituted; and pharmaceutically acceptable salts, esters, amides, solvates, hydrates, and protected forms thereof. 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, etc., and/or in the treatment of cancer, proliferative conditions, etc.
摘要翻译：本发明涉及抑制端粒酶，调节细胞增殖等，和/或治疗癌症，增殖病症等的式（1）的某些吖啶酮和吖啶化合物，其中：（a）K = O，L 是-H，α单键，β是双键，γ是单键（吖啶酮）; 或（b）K是9取代基，L不存在，α是双键，β是单键，γ是双键（吖啶）; 并且其中：J 1是2-或3-取代基; J 2是6-或7-取代基; J 1和J 2各自是式-N（R N）-W的基团，其中：R N是氮取代基，并且是氢，C 1-7烷基，C 3-20杂环基或 C5-20芳基，并且任选被取代; 并且W是C 1-7烷基，C 3-20杂环基或C 5-20芳基，并且任选被取代; 并且其中，当K为9-取代基时，K为式-N（R N）-Q的基团，其中：R N为氨基取代基，为氢，C 1-7烷基， 20杂环基或C5-20芳基; 且Q为C 1-7烷基，C 3-20杂环基或C 5-20芳基，并且任选被取代; 和其药学上可接受的盐，酯，酰胺，溶剂合物，水合物及其保护形式。本发明还涉及包含这种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，调节细胞增殖等，和/或治疗癌症，增殖性条件等

47. 发明申请

WO2003029176A1 4-(C2-6ALKOXY)-SUBSTITUTED CHALCONES AS THERAPEUTIC AGENTS 审中-公开
标题翻译：作为治疗药物的4-C2-6烷氧基取代的中间体
公开(公告)号：WO2003029176A1
公开(公告)日：2003-04-10
申请号：PCT/GB2002/004462
申请日：2002-09-30
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , POTTER, Gerard, Andrew , IJAZ, Taeeba,
发明人： POTTER, Gerard, Andrew , IJAZ, Taeeba,
IPC分类号： C07C49/84
CPC分类号： C07C49/84 , A61K31/12 , C07C45/29 , C07C45/71 , C07C45/74 , C07C47/575
摘要： The present invention pertains to compounds of the following formula: (1) wherein: R ALK is primary or secondary aliphatic saturated C 2-6 alkyl; each of R B2 , R B3 , R B4 , and R B5 is independently -H, -OH, or -OMe; each of R 1 and R 2 is independently: -H, optionally substituted C 1-4 alkyl, or optionally substituted C 5-20 aryl; R A3 is -H, -OH, -OC(=O)R E , -OS(=O) 2 OH, or -OP(=O)(OH) 2 ; R E is : -H, optionally substituted C 1-6 alkyl, optionally substituted C 3-20 heterocyclyl, or optionally substituted C 5-20 aryl; or a pharmaceutically acceptable salt, solvate, amide, ester, ether, chemically protected form, or prodrug thereof. 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, for both diagnosis and treatment of, for example, proliferative conditions, such as cancer, and inflammatory conditions.
摘要翻译：本发明涉及以下化学式的化合物：（1）其中：R a是烷基或仲脂族饱和C 2-6烷基; R“，B”，R“”“”和“B”中的每一个独立地是-H，-OH，或-OMe; R 1和R 2各自独立地为：-H，任选取代的C 1-4烷基或任选取代的C 15烷基 -20 芳基; R 3是-H，-OH，-OC（= O）R e，-OS（= O）2 s OH，或 - OP（= O）（OH） 2 ; R e是：-H，任选取代的C 1-6烷基，任选取代的C 3-20杂环基，或任选取代的C s > 5-20 芳基; 或其药学上可接受的盐，溶剂化物，酰胺，酯，醚，化学保护形式或前药。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用于诊断和治疗例如增生性疾病如癌症和炎性病症的用途。

48. 发明申请

WO2003028713A3 3,4-METHYLENEDIOXY-SUBSTITUTED CHALCONES AS THERAPEUTIC AGENTS 审中-公开
公开(公告)号：WO2003028713A3
公开(公告)日：2003-04-10
申请号：PCT/GB2002/004406
申请日：2002-09-30
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , POTTER, Gerard, Andrew , BUTLER, Paul, Crispin
发明人： POTTER, Gerard, Andrew , BUTLER, Paul, Crispin
IPC分类号： A61K31/36
摘要： The present invention pertains to the use of a compound for the manufacture of a medicament for use in the treatment of a proliferative condition, wherein the compounds have the following formula (1): wherein: each of R B2 , R B3 , R B4 , and R B5 is independently -H, -OH, or -OMe; each of R 1 and R 2 is independently: -H, optionally substituted C 1-4 alkyl, or optionally substituted C 5-20 aryl; R A3 is -H, -OH, -OC(=O)R E , -OS(=O) 2 OH, or -OP(=O)(OH) 2 ; R E is: -H, optionally substituted C 1-6 alkyl, optionally substituted C 3-20 heterocyclyl, or optionally substituted C 5-20 aryl; or a pharmaceutically acceptable salt, solvate, amide, ester, ether, chemically protected form, or prodrug thereof. The present invention also pertains to such compounds, pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo , for both diagnosis and treatment of, for example, proliferative conditions, such as cancer, and inflammatory conditions.

49. 发明申请

WO2003007955A2 NEW USE 审中-公开
标题翻译：新用途
公开(公告)号：WO2003007955A2
公开(公告)日：2003-01-30
申请号：PCT/GB2002/003342
申请日：2002-07-22
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , HICKSON, Ian , David , HAMMONDS, Timothy, Robin
发明人： HICKSON, Ian , David , HAMMONDS, Timothy, Robin
IPC分类号： A61K31/4545
CPC分类号： A61K45/06 , A61K31/00 , A61K31/085 , A61K31/235 , A61K31/255 , A61K31/26 , A61K31/265 , A61K31/27 , A61K31/343 , A61K31/381 , A61K31/385 , A61K31/4025 , A61K31/404 , A61K31/44 , A61K31/4545 , A61K31/47 , A61K31/517 , A61K31/536 , A61K31/655 , A61K2300/00
摘要： The present invention provides the use of a low molecular weight mammalian AP endonuclease inhibitor for the preparation of a medicament for the treatment of cancer.
摘要翻译：本发明提供了低分子量哺乳动物AP内切核酸酶抑制剂在制备用于治疗癌症的药物中的用途。

50. 发明申请

WO2003004479A1 4-ARYL QUINOLS AND ANALOGS THEREOF AS THERAPEUTIC AGENTS 审中-公开
标题翻译： 4-ARYL QUINOLS及其类似物作为治疗剂
公开(公告)号：WO2003004479A1
公开(公告)日：2003-01-16
申请号：PCT/GB2002/003097
申请日：2002-07-05
申请人： CANCER RESEARCH TECHNOLOGY LIMITED , STEVENS, Malcolm, Francis, Graham , WELLS, Geoffrey , WESTWELL, Andrew, David , POOLE, Tracey, Dawn
发明人： STEVENS, Malcolm, Francis, Graham , WELLS, Geoffrey , WESTWELL, Andrew, David , POOLE, Tracey, Dawn
IPC分类号： C07D277/64
CPC分类号： C07D263/56 , C07C45/30 , C07C45/511 , C07C45/513 , C07C49/747 , C07C49/753 , C07C323/22 , C07C323/59 , C07C2601/14 , C07D209/12 , C07D215/14 , C07D235/12 , C07D277/64 , C07D307/80 , C07D333/54
摘要： The present invention pertains to compounds of the formula (1), which are, inter alia, antiproliferative agents, anticancer agents, antimycobacterial agents, antituberculosis agents, and/or thioredoxin/thioredoxin reductase inhibitors: wherein: Q is =O or =N-S(=O) 2 -R Q ;R Q is -H or optionally substituted C 1-7 alkyl, C 3-20 heterocyclyl, or C 5-20 aryl; Ar is optionally substituted C 5-20 aryl; R o is an oxy substituent; the bond marked α is a single bond or a double bond; the bond marked ß is a single bond or a double bond; R 3 and R 5 are each independently ring substituents; R 2 and R 6 are each independently ring substituents; and pharmaceutically acceptable salts, esters, amides, solvates, hydrates, and protected forms thereof. 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, for example, in the treatment of proliferative conditions, (e.g., cancer), mycobacterial infections (e.g., tuberculosis), and/or conditions mediated by thioredoxin/thioredoxin reductase.
摘要翻译：本发明涉及式（1）的化合物，其特别是抗增殖剂，抗癌剂，抗分枝杆菌药，抗结核药物和/或硫氧还蛋白/硫氧还蛋白还原酶抑制剂：其中：Q = = O）2-R Q; R Q是-H或任选取代的C 1-7烷基，C 3-20杂环基或C 5-20芳基; Ar是任选取代的C 5-20芳基; R o是氧取代基; 标记为α的键是单键或双键; 标记为ss的键是单键或双键; R 3和R 5各自独立地为环取代基; R 2和R 6各自独立地为环取代基; 和其药学上可接受的盐，酯，酰胺，溶剂合物，水合物及其保护形式。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，例如用于治疗增殖性疾病（例如癌症），分枝杆菌感染（例如，结核病））和/或由硫氧还蛋白/硫氧还蛋白还原酶介导的条件。

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