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61. 发明公开

EP1756098A2 2-SUBSTITUTED-4-HETEROARYL-PYRIMIDINES USEFUL FOR THE TREATMENT OF PROLIFERATIVE DISORDERS 审中-公开
标题翻译：对于增殖病症的治疗合适的2-取代的-4-芳基 - 嘧啶
公开(公告)号：EP1756098A2
公开(公告)日：2007-02-28
申请号：EP05748147.5
申请日：2005-05-26
申请人： Cyclacel Limited
发明人： WANG, Shudong , WOOD, Gavin , DUNCAN, Kenneth , MEADES, Christopher , GIBSON, Darron , MCLACHLAN, Janice , FISCHER, Peter
IPC分类号： C07D417/04
CPC分类号： C07D417/04 , C07D417/14
摘要： The present invention relates to selected substituted pyrimidines their preparation, pharmaceutical compositions containing them and their use as inhibitors of one or more protein kinases, and hence their use in the treatment of proliferative disorders, viral disorders and/or other disorders.

62. 发明公开

EP1734962A2 COMPOSITIONS AND METHODS FOR MODULATING GATED ION CHANNELS 审中-公开
标题翻译：组合物和方法调制来控制离子通道
公开(公告)号：EP1734962A2
公开(公告)日：2006-12-27
申请号：EP05805035.2
申请日：2005-03-30
申请人： PainCeptor Pharma Corp.
发明人： BABINSKI, Kazimierz , SZAREK, Walter A. , VOHRA, Rahul , VARMING, Thomas , AHRING, Philip, K. , DYHRING JOERGENSEN, Tino , BLACKBURN-MUNRO, Gordon, John
IPC分类号： A61K31/4709 , A61P25/00 , A61P29/00 , A61K31/49
CPC分类号： A61K31/4709 , A61K31/49 , A61K31/496 , A61K31/5377 , A61K31/675
摘要： The present application relates to compositions which modulate the activity of gated ion channels. This provide an effect in the treatment of pain, inflammatory disorders and neurological disorders. Preferred compounds include quinine or quinidine derivatives with the hydroxyl at the nine position being esterified with an aliphatic carboxylic acid, optionally bearing an additional cycloalkyl ring on the chain. The gated ion channels modulated include homomultimeric and heteromultimeric gates.

63. 发明公开

EP1683056A2 METHOD FOR IDENTIFYING INHIBITORS USING A HOMOLOGY MODEL OF POLO-LIKE KINASE 1 审中-公开
标题翻译：一种用于识别抑制剂，通过使用POLO样激酶1的同源模型
公开(公告)号：EP1683056A2
公开(公告)日：2006-07-26
申请号：EP04798485.1
申请日：2004-11-12
申请人： Cyclacel Limited
发明人： MCINNES, Campbell , MCLACHLAN, Janice , MEZNA, Mokdad , FISCHER, Peter
IPC分类号： G06F17/50
CPC分类号： C07D493/06 , C07D311/22 , C07D417/04 , C07D473/16 , C07K2299/00 , C12N9/1205 , G01N2333/9121 , G01N2500/02 , Y02A90/24 , Y02A90/26
摘要： The present invention relates to a homology model for PLK, and the use thereof in assays for the identification of small molecule PLK modulators. The invention further relates to PLK modulators identified by said assays, and their use in the treatment of PLK-related disorders such as proliferative disorders.

64. 发明公开

EP1678171A1 PYRIMIDIN-4-YL-3,4-THIONE COMPOUNDS AND THEIR USE IN THERAPY 有权
标题翻译： 2-氨基-4-噻唑烷 - 吡啶衍生物ALS蛋白激酶
公开(公告)号：EP1678171A1
公开(公告)日：2006-07-12
申请号：EP04768981.5
申请日：2004-10-21
申请人： Cyclacel Limited
发明人： WANG, Shudong , WOOD, Gavin , DUNCAN, Kenneth W. , MEADES, Christopher , GIBSON, Darren , MCLACHLAN, Janice, C. , PERRY, Alex , BLAKE, David , ZHELEVA, Daniella I. , FISCHER, Peter M.
IPC分类号： C07D417/14 , C07D417/04 , A61K31/506
CPC分类号： C07D417/04 , C07D417/14
摘要： The present invention relates to compounds of formula: (I), or pharmaceutically acceptable salts thereof, wherein R1 and R5 are each independently H, C(ORj’) or a hydrocarbyl group optionally substituted by one or more R6 groups; R2, R3, and R4 are each independently H, alkyl or alkenyl, each of which may be optionally substituted with one or more R7 groups; R6 and R7 are each independently halogen, NO2, CN, (CH2)mORa, O(CH2)nORb, (CH2)pNRcRd, CF3, COORe, CONRfRg, CORh, SO3H, SO2Ri, SO2NRjRk, (CH2)qNRa’CORg’, Rf’, (CH2)rNRb’SO2Rh’, SO2NRd’Ri’, SO2NRe'(CH2)s,ORc', heterocycloalkyl or heteroaryl, wherein said heterocycloalkyl and heteroaryl may be optionally substituted by one or more substituents selected from aralkyl, sulfonyl, Rm and CORn; Rg', Rh', Ri' and Rj' are each independently selected from alkyl, aryl, aralkyl and heteroaryl, each of which may be optionally substituted with one or more substituents selected from halogen, OH, NO2, NH2 CF3 and COOH; m, p, q and r are each independently 0, 1, 2 or 3; n and s are each independently 1, 2, or 3; and Ra-n and Ra'-f' are each independently H or alkyl. Further aspects of the invention relate to pharmaceutical compositions comprising such compounds, and their use in the preparation of a medicament for treating one or more of the following: a proliferative disorder, a viral disorder, a CNS disorder, a stroke, alopecia and diabetes.

65. 发明公开

EP1671980A2 Avermectin derivatives 失效
标题翻译：阿维菌素衍生物
公开(公告)号：EP1671980A2
公开(公告)日：2006-06-21
申请号：EP06004047.4
申请日：1990-01-17
申请人： Merial Limited
发明人： Fisher, Michael H. , Mrozik, Helmut
IPC分类号： C07H19/01 , A61K31/70 , A61P33/00
CPC分类号： C07H19/01 , C07H17/08
摘要： Novel avermectin derivatives are disclosed, wherein the 5-hydroxy group is replaced by an oxime group. The avermectin-5-oximes can further be derivatized at the 4"- or 4'-positions as amino, substituted amino, acylhydrazone, semicarbazone, or substituted semicarbazone analogues. The avermectin-5-oximes are prepared by the oxidation of the 5-hydroxy compounds with manganese dioxide or with pyridinium dichromate to the known 5-oxo analogues, and these are then reacted with a hydroxylamine salt. The new compounds are potent anti-parasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.
摘要翻译：公开了新的阿维菌素衍生物，其中5-羟基被肟基替代。阿维菌素-5-肟可以进一步在4“ - 或4'-位被衍生为氨基，取代的氨基，酰腙，缩氨基脲或取代的缩氨基脲类似物，阿维菌素-5-肟通过氧化5- 羟基化合物与二氧化锰或与重铬酸吡啶鎓转化成已知的5-氧代类似物，然后将它们与羟胺盐反应，新化合物是有效的抗寄生虫剂，特别是该化合物是驱虫剂，杀虫剂和杀螨剂。

66. 发明公开

EP1572676A2 HIGH SPECIFICITY ANTICANCER PHARMACOLOGICAL DRUG SYSTEM, DRUG SYNTHESIS, AND DRUG DEVELOPMENT PROCESS 审中-公开
标题翻译：随着对医药品的开发抗癌作用药物合成和方法HIGH特定药理学药物制度
公开(公告)号：EP1572676A2
公开(公告)日：2005-09-14
申请号：EP03814041.4
申请日：2003-12-15
申请人： Walker Cancer Research Institute, Inc.
发明人： WALKER, Evan, Harris , PALOMINO, Eduardo , BLUMENTHAL, Steven, L.
IPC分类号： C07D327/00 , A61K31/38
CPC分类号： C07D409/04 , A61K31/382 , A61K31/385 , A61K47/54 , A61K47/545 , A61K47/555 , C07D335/16 , C07D409/12
摘要： A process for producing new anticancer drugs such that the drugs can be administered in a nontoxic, proto-drug form and, subsequent to a time delay which allows for differential concentration in the target cancer or invasive tissues or cells, the non-toxic drug is then modified by an activation drug to selectively provide toxic levels of a pharmacologically active agent to the target issue.

67. 发明公开

EP1558239A1 COMBINATION COMPRISING A CDK INHIBITOR AND CISPLATIN 审中-公开
标题翻译：组合CDK抑制剂联合顺铂
公开(公告)号：EP1558239A1
公开(公告)日：2005-08-03
申请号：EP03810525.0
申请日：2003-11-05
申请人： Cyclacel Limited
发明人： GIANNELLA-BORRADORI, Athos
IPC分类号： A61K31/282 , A61K31/52 , A61P35/00
CPC分类号： A61K31/282 , A61K31/52 , A61K33/24 , A61K2300/00
摘要： A first aspect of the invention relates to a combination comprising a CDK inhibitor and cisplatin. A second aspect of the invention relates to a pharmaceutical product comprising a CDK inhibitor and cisplatin as a combined preparation for simultaneous, sequential or separate use in therapy. A third aspect of the invention relates to a method of treating a proliferative disorder, said method comprising simultaneously, sequentially or separately administering a CDK inhibitor and cisplatin to a subject.

68. 发明公开

EP1487495A1 COMBINATION COMPRISING A CDK INHIBITOR AND DOXORUBICIN 审中-公开
标题翻译：组合中包含CDK抑制剂和阿霉素
公开(公告)号：EP1487495A1
公开(公告)日：2004-12-22
申请号：EP03712412.0
申请日：2003-03-25
申请人： Cyclacel Limited
发明人： SLEIGH, Roger Neil , BERNS, Anton , COLEY, Helen Mary , LYONS, Scott
IPC分类号： A61K45/06 , A61K31/704 , A61P35/00
CPC分类号： A61K45/06 , A61K31/704 , Y02A50/411 , A61K2300/00
摘要： A first aspect of the invention relates to a combination comprising a CDK inhibitor and doxorubicin. A second aspect of the invention relates to a pharmaceutical product comprising a CDK inhibitor and doxorubicin as a combined preparation for simultaneous, sequential or separate use in therapy. A third aspect of the invention relates to a method of treating a proliferative disorder, said method comprising simultaneously, sequentially or separately administering a CDK inhibitor and doxorubicin to a subject.

69. 发明公开

EP1487416A2 DRUG MICROPARTICLES 有权
标题翻译：中药微粒
公开(公告)号：EP1487416A2
公开(公告)日：2004-12-22
申请号：EP03745623.3
申请日：2003-03-25
申请人： TEVA PHARMACEUTICAL INDUSTRIES LTD.
发明人： LERNER, Itzhak, E. , ROSENBERGER, Vered , FLASHNER-BARAK, Moshe , DRABKIN, Anna , MOLDAVSKI, Naomi
IPC分类号： A61K9/14
CPC分类号： A61K9/1682 , A61K9/167 , A61K9/1676 , A61K9/1694 , A61K31/519 , B01J13/02 , B01J13/125
摘要： Provided are microparticles of active pharmaceutical ingredients, drug delivery vehicles comprising same, and methods for making them.

70. 发明公开

EP1465887A1 NOVEL CRYSTAL FORMS OF ONDANSETRON, PROCESSES FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS CONTAINING THE NOVEL FORMS AND METHODS FOR TREATING NAUSEA USING THEM 审中-公开
标题翻译：昂丹司琼FOR治疗恶心，以便新的晶体形式中，METHOD FOR THE PRODUCTION，含药物和方法¬1983/ 18
公开(公告)号：EP1465887A1
公开(公告)日：2004-10-13
申请号：EP03719967.6
申请日：2003-04-29
申请人： BIOGAL GYOGYSZERGYAR RT.
发明人： ARONHIME, Judith , MOLNAR, Sandor , SZABO, Csaba , MESZAROS SOS, Erzsebet , SALYI, SzabolcsDerek ut. , TAMAS, Tivadar
IPC分类号： C07D401/06 , A61K31/473
CPC分类号： C07D403/06
摘要： Ondansetron crystalline Forms A and B are useful in the treatment of nausea and vomiting. Form B has uniquely high melting point of about 244 °C and both forms are stable against thermally induced polymorphic transition from 30 °C up to their melting points.

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