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1. 发明申请

US20080153853A1 USE OF MTKI 1 FOR TREATING OR PREVENTING BRAIN CANCER 审中-公开
标题翻译：使用MTKI 1治疗或预防脑癌
公开(公告)号：US20080153853A1
公开(公告)日：2008-06-26
申请号：US11875350
申请日：2007-10-19
申请人： Eddy Jean Edgard FREYNE , Michel Marie Francois Janicot , Martin John Page , Timothy Pietro Suren Perera
发明人： Eddy Jean Edgard FREYNE , Michel Marie Francois Janicot , Martin John Page , Timothy Pietro Suren Perera
IPC分类号： A61K31/519 , A61P35/00
CPC分类号： A61K31/519 , A61K31/4188 , A61K2300/00
摘要： The present invention is concerned with the finding that some the macrocyclic quinazoline derivative 4,6-ethanediylidenepyrimido[4,5-b][6,1,12]benzoxadiazacyclo-pentadecine, 17-bromo-8,9,10,11,12,13,14,19-octahydro-20-methoxy-13-methyl-, described as compound 22 in PCT publication W02004/105765, is useful in the manufacture of a medicament for the treatment or prevention of a primary brain cancer or brain metastasis. It accordingly provides methods for treating, preventing, delaying or mitigating brain cancer, or for preventing or slowing proliferation of cells of brain origin.
摘要翻译：本发明涉及一些大环喹唑啉衍生物4,6-乙二亚甲基嘧啶并[4,5-b] [6,1,12]苯并二氮杂环十五碳烯，17-溴-8,9,10,11,12 在PCT公开WO2004 / 105765中描述为化合物22的13,14,19-八氢-20-甲氧基-13-甲基，可用于制备用于治疗或预防原发性脑癌或脑转移的药物。因此，它提供了治疗，预防，延迟或减轻脑癌或预防或减缓脑源性细胞增殖的方法。

2. 发明申请

US20080219975A1 VEGFR3 INHIBITORS 审中-公开
标题翻译： VEGFR3抑制剂
公开(公告)号：US20080219975A1
公开(公告)日：2008-09-11
申请号：US11875288
申请日：2007-10-19
申请人： Timothy Pietro Suren PERERA , Matthias Luc A. Versele , Martin John Page
发明人： Timothy Pietro Suren PERERA , Matthias Luc A. Versele , Martin John Page
IPC分类号： A61K39/395 , A61K31/519 , A61P35/00 , A61K31/704
CPC分类号： A61K31/519 , A61K31/704
摘要： The present invention relates to the use of some of the macrocyclic quinazoline derivatives described in PCT publication WO2004/105765 as inhibitors of VEGFR3 mediated biological activities, especially those activities which are mediated by VEGFR3 ligands VEGF-C and/or VEGF-D.
摘要翻译：本发明涉及PCT公开WO2004 / 105765中描述的一些大环喹唑啉衍生物用作VEGFR3介导的生物活性的抑制剂，特别是由VEGFR3配体VEGF-C和/或VEGF-D介导的那些活性。

3. 发明申请

US20090312284A1 HISTONE DEACETYLASE INHIBITORS WITH COMBINED ACTIVITY ON CLASS-I AND CLASS-IIB HISTONE DEACETYLASES IN COMBINATION WITH PROTEASOME INHIBITORS 审中-公开
标题翻译：具有组合I和IIB类组合活性的组织脱乙酰壳多糖抑制剂与抗抑郁药组合
公开(公告)号：US20090312284A1
公开(公告)日：2009-12-17
申请号：US12441218
申请日：2007-09-11
申请人： Janine Arts , Peter Willem Jan Hellemans , Michel Marie Francois Janicot , Martin John Page
发明人： Janine Arts , Peter Willem Jan Hellemans , Michel Marie Francois Janicot , Martin John Page
IPC分类号： A61K31/69 , A61K31/506 , C12Q1/25 , A61P35/00
CPC分类号： A61K45/06 , A61K31/506 , A61K38/05 , A61K2300/00
摘要： The present invention is concerned with combinations of a proteasome inhibitor and a histone deacetylase inhibitor with combined activity on class-I and class-IIb histone deacetylases, for inhibiting the growth of tumor cells, useful in the treatment of cancer.
摘要翻译：本发明涉及蛋白酶体抑制剂和组蛋白脱乙酰酶抑制剂与I类和IIb组蛋白脱乙酰酶的组合活性的组合，用于抑制肿瘤细胞的生长，可用于治疗癌症。

4. 发明申请

US20090270419A1 COMBINATIONS OF CLASS-I SPECIFIC HISTONE DEACETYLASE INHIBITORS WITH PROTEASOME INHIBITORS 审中-公开
标题翻译：第一类特异性HISTONE脱乙酰壳多糖酶抑制剂与抗生素抑制剂的组合
公开(公告)号：US20090270419A1
公开(公告)日：2009-10-29
申请号：US12441236
申请日：2007-09-11
申请人： Janine Arts , Peter Willem Jan Hellemans , Michel Marie Francois Janicot , Martin John Page
发明人： Janine Arts , Peter Willem Jan Hellemans , Michel Marie Francois Janicot , Martin John Page
IPC分类号： A61K31/497 , C07D403/04 , A61P35/00
CPC分类号： A61K31/69 , A61K31/506 , A61K38/05 , A61K45/06 , A61K2300/00
摘要： The present invention is concerned with combinations of a proteasome inhibitor and a class-I specific histone deacetylase inhibitor for inhibiting the growth of tumor cells, useful in the treatment of cancer.
摘要翻译：本发明涉及用于抑制肿瘤细胞生长的蛋白酶体抑制剂和I类特异性组蛋白脱乙酰酶抑制剂的组合，其可用于治疗癌症。

5. 发明授权

US06169091A Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors 失效
标题翻译：双环杂芳族化合物作为蛋白酪氨酸激酶抑制剂
公开(公告)号：US06169091A
公开(公告)日：2001-01-02
申请号：US09051324
申请日：1998-08-26
申请人： George Stuart Cockerill , Stephen Barry Guntrip , Stephen Carl McKeown , Martin John Page , Kathryn Jane Smith , Sadie Vile , Alan Thomas Hudson , Paul Barraclough , Karl Witold Franzmann
发明人： George Stuart Cockerill , Stephen Barry Guntrip , Stephen Carl McKeown , Martin John Page , Kathryn Jane Smith , Sadie Vile , Alan Thomas Hudson , Paul Barraclough , Karl Witold Franzmann
IPC分类号： C07D48704
CPC分类号： C07D471/04 , C07D495/04
摘要： Substituted heteroaromatic compounds of formula (A) wherein X is N or CH; in which (a) represents a fused 5, 6 or 7-membered heterocyclic ring and R3 is a group ZR4 wherein Z is joined to R4 through a (CH2)p group in which p is 0, 1, or 2 and Z represents a group V(CH2), V(CF2), (CH2)V, (CF2)V, V(CRR′), V(CHR) or V where R and R′ are each C1-4 alkyl and in which V is a hydrocarbyl group containing 0, 1 or 2 carbon atoms, carbonyl, dicarbonyl, CH(OH), CH(CN), sulphonamide, amide, O, S(O)m or NRb where Rb is hydrogen or Rb is C1-4 alkyl; and R4 is an optionally substituted C3-6 cycloalkyl or an optionally substituted 5, 6, 7, 8, 9 or 10-membered carbocyclic or heterocyclic moiety; or R3 is a group ZR4 in which Z is NRb, and NRb and R4 together form an optionally substituted 5, 6, 7, 8, 9 or 10-membered carbocyclic or heterocyclic moiety, are protein tyrosine kinase inhibitors. The compounds are described, as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of psoriasis, fibrosis, atherosclerosis, restenosis, auto-immune disease, allergy, asthma, transplantation rejection, inflammation, thrombosis, nervous system diseases, and cancer.
摘要翻译：取代的式（A）的杂芳族化合物，其中X是N或CH; 其中（a）表示稠合的5,6或7-元杂环，R3是基团ZR4，其中Z通过其中p为0,1或2的（CH 2）p基团连接到R 4，Z表示组V（CH 2），V（CF 2），（CH 2）V，（CF 2）V，V（CRR'），V（CHR）或V其中R和R'各自是C 1-4烷基，其中V是羰基，二羰基，CH（OH），CH（CN），磺酰胺，酰胺，O，S（O）m或NR b，其中R b是氢或R b是C 1-4烷基; 并且R 4是任选取代的C 3-6环烷基或任选取代的5,6,7,8,9或10元碳环或杂环部分; 或R3是Z Z4，其中Z是NRb，NRb和R4一起形成任选取代的5,6,7,8,9或10元碳环或杂环部分是蛋白质酪氨酸激酶抑制剂。描述了这些化合物，以及其制备方法，包括这些化合物的药物组合物及其在医学中的用途，例如治疗牛皮癣，纤维化，动脉粥样硬化，再狭窄，自身免疫疾病，变态反应，哮喘，移植排斥，炎症，血栓形成，神经系统疾病和癌症。

6. 发明授权

US6051221A BRK protein tyrosine kinase and encoding nucleic acid 失效
标题翻译： BRK蛋白酪氨酸激酶和编码核酸
公开(公告)号：US6051221A
公开(公告)日：2000-04-18
申请号：US591474
申请日：1996-06-10
申请人： Barry Austin Gusterson , Mark Roger Crompton , Philip John Mitchell , Karen Tracey Barker , Taherah Kamalati , Martin John Page , Paul Spence
发明人： Barry Austin Gusterson , Mark Roger Crompton , Philip John Mitchell , Karen Tracey Barker , Taherah Kamalati , Martin John Page , Paul Spence
IPC分类号： A61K31/275 , A61K31/35 , A61K31/55 , A61K31/70 , A61K38/00 , A61K39/395 , A61K45/00 , A61K47/48 , A61K48/00 , A61P35/00 , C07H21/04 , C12N1/19 , C12N1/21 , C12N5/10 , C12N9/12 , C12N15/09 , C12N15/12 , C12N15/54 , C12Q1/48 , C12Q1/68 , C12R1/91 , G01N33/573 , A61K38/43 , C12N15/11
CPC分类号： A61K31/70 , A61K31/275 , A61K31/35 , A61K31/55 , A61K47/48238 , C12N9/1205 , C12Q1/48 , C12Q1/6886 , G01N33/573 , A61K38/00 , C12Q2600/136 , C12Q2600/158
摘要： The invention relates to a novel tyrosine kinase designated brk and the use of this tyrosine kinase in the development of diagnostic and therapeutic approaches to cancer. The novel tyrosine kinase was isolated from a human metastatic breast tumor using a PCR based differential screening approach and has the deduced amino acid sequence shown in SEQ ID NO:2.
摘要翻译： PCT No.PCT / GB94 / 01479 Sec。 371日期1996年6月10日 102（e）1996年6月10日PCT 1994年7月8日PCT公布。第WO95 / 02057号公报日期1995年1月19日本发明涉及一种新的酪氨酸激酶，指定为brk，以及该酪氨酸激酶在癌症诊断和治疗方法开发中的应用。使用基于PCR的差异筛选方法从人转移性乳腺肿瘤中分离出新的酪氨酸激酶，并且具有SEQ ID NO：2所示的推导的氨基酸序列。

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