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1. 发明申请

WO2008068507A3 2 -PHENYLAMINO, 6- (PYRID-3-YL) QUINAZOLINE DERIVATIVES AS RAF-PROTEIN KINASE INHIBITORS IN CANCER TREATMENT 审中-公开
公开(公告)号：WO2008068507A3
公开(公告)日：2008-06-12
申请号：PCT/GB2007/004697
申请日：2007-12-07
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , AQUILA, Brian , COOK, Donald, James , JOHNSTONE, Craig , LEE, Stephen , LYNE, Paul , RUDGE, David, Alan , VASBINDER, Melissa , WANG, Haixia
发明人： AQUILA, Brian , COOK, Donald, James , JOHNSTONE, Craig , LEE, Stephen , LYNE, Paul , RUDGE, David, Alan , VASBINDER, Melissa , WANG, Haixia
IPC分类号： C07D401/04 , A61K31/472 , A61P35/00
摘要： The invention relates to chemical compounds of the formula (I): or pharmaceutically or pharmaceutically acceptable salts thereof, which possess B-Raf inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.

2. 发明申请

WO2008003958A3 FUSED PYRIMIDO COMPOUNDS 审中-公开
标题翻译：熔化的吡咯烷酮化合物
公开(公告)号：WO2008003958A3
公开(公告)日：2008-03-06
申请号：PCT/GB2007002490
申请日：2007-07-05
申请人： ASTRAZENECA AB , ASTRAZENECA UK LTD , HALSALL CHRISTOPHER THOMAS , RUDGE DAVID ALAN , SIMPSON IAIN , WARD RICHARD ANDREW
发明人： HALSALL CHRISTOPHER THOMAS , RUDGE DAVID ALAN , SIMPSON IAIN , WARD RICHARD ANDREW
IPC分类号： C07D487/04 , A61K31/522
CPC分类号： C07D487/04 , C07D519/00
摘要： There is provided a compound of formula (I):processes for the manufacure thereof, pharmaceutical compoitions thereof and uses in therapy.
摘要翻译：提供了式（I）化合物：其制备方法，药物组合物和治疗用途。

3. 发明申请

WO2009093032A1 PHTHALAZINONE DERIVATIVES 审中-公开
标题翻译：苯乙烯酮衍生物
公开(公告)号：WO2009093032A1
公开(公告)日：2009-07-30
申请号：PCT/GB2009/000181
申请日：2009-01-23
申请人： ASTRAZENECA AB , MENEAR, Keith, Allan , JAVAID, Muhammad, Hashim , GOMEZ, Sylvie , HUMMERSONE, Marc, Geoffrey , LENCE, Carlos, Fenandez , MARTIN, Niall, Morrison, Barr , RUDGE, David, Alan , ROBERTS, Craig, Anthony , BLADES, Kevin
发明人： MENEAR, Keith, Allan , JAVAID, Muhammad, Hashim , GOMEZ, Sylvie , HUMMERSONE, Marc, Geoffrey , LENCE, Carlos, Fenandez , MARTIN, Niall, Morrison, Barr , RUDGE, David, Alan , ROBERTS, Craig, Anthony , BLADES, Kevin
IPC分类号： C07D401/10 , C07D401/14 , C07D405/14 , C07D487/04 , C07D491/10 , A61K31/502 , A61K31/5025 , A61P35/00
CPC分类号： C07D401/10 , C07D401/14 , C07D405/14 , C07D487/04 , C07D491/10
摘要： A compound of the formula (I): wherein: A and B together represent an optionally substituted, fused aromatic ring; X and Y are selected from CH and CH, CF and CH, CH and CF and N and CH respectively; R c is selected from H, C 1.4 alkyl; and R 1 is selected from C 1-7 alkyI, C 3-20 heterocydyl and C 5-20 aryl, which groups are optionally substituted; or R c and R 1 together with the carbon and oxygen atoms to which they are attached form a spiro-C 5-7 oxygen-containing heterocyclic group, which is optionally substituted or fused to a C 5-7 aromatic ring. These compounds are useful in the preparation of a medicament for inhibiting the activity of PARP for the treatment of : vascular disease; septic shock;ischaemic injury;neurotoxicity;haemorraghic shock;viral infection; or for use as an adjunct in cancer therapy or for potentiating tumour cells for treatment with ionizing radiation or chemotherapeutic agents.
摘要翻译：式（I）的化合物：其中：A和B一起表示任选取代的稠合芳环; X和Y分别选自CH和CH，CF和CH，CH和CF以及N和CH; Rc选自H，C 1-4烷基; 并且R 1选自C 1-7烷基，C 3-20杂环基和C 5-20芳基，该基团任选被取代; 或Rc和R 1与它们所连接的碳原子和氧原子一起形成一个含C 5-7的含氧杂环基团，该杂环基团任选被取代或稠合至C5-7芳环。这些化合物可用于制备用于抑制PARP的活性用于治疗血管疾病的药物; 败血性休克;缺血性损伤;神经毒性;血肿性休克;病毒感染; 或用作癌症治疗中的辅助剂或用于增强肿瘤细胞以用电离辐射或化学治疗剂治疗。

4. 发明申请

WO2008003958A2 NOVEL COMPOUNDS 审中-公开
标题翻译：新型化合物
公开(公告)号：WO2008003958A2
公开(公告)日：2008-01-10
申请号：PCT/GB2007/002490
申请日：2007-07-05
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , HALSALL, Christopher, Thomas , RUDGE, David, Alan , SIMPSON, Iain , WARD, Richard, Andrew
发明人： HALSALL, Christopher, Thomas , RUDGE, David, Alan , SIMPSON, Iain , WARD, Richard, Andrew
CPC分类号： C07D487/04 , C07D519/00
摘要： There is provided a compound of formula (I):processes for the manufacure thereof, pharmaceutical compoitions thereof and uses in therapy.
摘要翻译：提供了式（I）化合物：其制备方法，药物组合物和治疗用途。

5. 发明申请

WO2007060408A3 L-PHENYLALANINE DERIVATIVES AND THEIR USE AS INTEGRIN ANTAGONISTS 审中-公开
标题翻译： L-苯丙氨酸衍生物及其作为整合拮抗剂的用途
公开(公告)号：WO2007060408A3
公开(公告)日：2007-08-02
申请号：PCT/GB2006004337
申请日：2006-11-22
申请人： ASTRAZENECA AB , ASTRAZENECA UK LTD , KETTLE JASON GRANT , BARRY SIMON THOMAS , RUDGE DAVID ALAN
发明人： KETTLE JASON GRANT , BARRY SIMON THOMAS , RUDGE DAVID ALAN
IPC分类号： C07D211/34 , C07D211/70 , C07D309/04 , C07D309/20 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/06
CPC分类号： C07D309/20 , C07C309/65 , C07D211/34 , C07D211/70 , C07D309/04 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06 , C07D409/12 , C07D413/06 , C07D417/06
摘要： The present invention relates to compounds that inhibit of a5b1 function, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment in warm blooded animals such as humans of diseases that have a significant angiogenesis or vascular component such as for treatment of solid tumours. The present invention also relates to compounds that inhibit a5b1, and also that exhibit appropriate selectivity profile(s) against other integrins.
摘要翻译：本发明涉及抑制a5b1功能的化合物，其制备方法，含有它们作为活性成分的药物组合物，其作为药物的用途及其在制备用于治疗温血动物的药物中的用途，例如作为具有显着血管生成或血管成分的疾病的人，例如用于治疗实体瘤。本发明还涉及抑制αb1的化合物，并且还表现出对其他整联蛋白的适当选择性分布。

6. 发明申请

WO2008020203A1 PYRIDINYLQUINAZ0LINAMINE DERIVATIVES AND THEIR USE AS B-RAF INHIBITORS 审中-公开
标题翻译：吡啶并噻唑啉衍生物及其作为B-RAF抑制剂的用途
公开(公告)号：WO2008020203A1
公开(公告)日：2008-02-21
申请号：PCT/GB2007/003111
申请日：2007-08-15
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , AQUILA, Brian , COOK, Donald, J. , JOHNSTONE, Craig , LEE, Stephen , LYNE, Paul , RUDGE, David, Alan , VASBINDER, Melissa , WANG, Haixia
发明人： AQUILA, Brian , COOK, Donald, J. , JOHNSTONE, Craig , LEE, Stephen , LYNE, Paul , RUDGE, David, Alan , VASBINDER, Melissa , WANG, Haixia
IPC分类号： C07D401/04 , C07D405/12 , C07D401/12 , A61P35/00 , A61K31/517
CPC分类号： C07D401/04 , C07D401/12 , C07D405/12
摘要： The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess B-Raf inhibitory activity and are accordingly useful for their anti cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm blooded animal such as man.
摘要翻译：本发明涉及具有B-Raf抑制活性的式（I）化合物或其药学上可接受的盐，因此可用于其抗癌活性，因此可用于治疗人或动物体的方法。本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在制备用于在温血动物例如人中产生抗癌作用的药物中的用途。

7. 发明申请

WO2009022171A1 PYRIDINYIIOXY PYRIDINES AS ALK5 INHIBITORS 审中-公开
标题翻译：吡啶二氧基吡啶作为ALK5抑制剂
公开(公告)号：WO2009022171A1
公开(公告)日：2009-02-19
申请号：PCT/GB2008/050689
申请日：2008-08-11
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , FINLAY, Maurice, Raymond, Verschoyle , GOLDBERG, Frederick, Woolf , ROBERTS, Craig, Anthony , ROBERTS, Nicola, Jane , RUDGE, David, Alan
发明人： FINLAY, Maurice, Raymond, Verschoyle , GOLDBERG, Frederick, Woolf , ROBERTS, Craig, Anthony , ROBERTS, Nicola, Jane , RUDGE, David, Alan
IPC分类号： C07D401/12 , C07D401/14 , C07D407/14 , C07D417/14 , C07D405/14 , A61K31/444 , A61P35/00
CPC分类号： C07D213/74 , C07D401/14 , C07D409/14 , C07D417/14
摘要： The invention relates to chemical compounds of the formula (I) or pharmaceutically acceptable salts thereof, which possess ALK5 (TGFβRl) inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an anti¬ cancer effect in a warm-blooded animal such as man.
摘要翻译：本发明涉及具有ALK5（TGFβR1）抑制活性的式（I）化合物或其药学上可接受的盐，因此可用于其抗癌活性，因此可用于治疗人或动物体的方法。本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在制造用于在温血动物如人中产生抗癌作用的药物中的用途。

8. 发明申请

WO2008001070A1 PYRIMIDINE DERIVATIVES USEFUL IN THE TREATMENT OF CANCER 审中-公开
标题翻译：吡嗪衍生物可用于治疗癌症
公开(公告)号：WO2008001070A1
公开(公告)日：2008-01-03
申请号：PCT/GB2007/002381
申请日：2007-06-27
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BUTTAR, David , FOOTE, Kevin, Michael , NOWAK, Thorsten , RUDGE, David, Alan , THEOCLITOU, Maria-Elena , THOMAS, Andrew, Peter
发明人： BUTTAR, David , FOOTE, Kevin, Michael , NOWAK, Thorsten , RUDGE, David, Alan , THEOCLITOU, Maria-Elena , THOMAS, Andrew, Peter
IPC分类号： C07D413/14 , A61K31/506 , A61P35/00
CPC分类号： C07D413/14
摘要： There is provided a compound of formula (I): processes for the manufacture thereof, pharmaceutical compositions thereof and uses in therapy.
摘要翻译：提供式（I）的化合物：其制备方法，其药物组合物和治疗用途。

9. 发明申请

WO2009004356A1 PHTHALAZINONE DERIVATIVES AS INHIBITORS OF PARP-1 审中-公开
标题翻译：作为PARP-1的抑制剂的苯乙烯酮衍生物
公开(公告)号：WO2009004356A1
公开(公告)日：2009-01-08
申请号：PCT/GB2008/002318
申请日：2008-07-04
申请人： ASTRAZENECA AB , JAVAID, Muhammad, Hashim , MENEAR, Keith, Allan , MARTIN, Niall, Morrison, Barr , SMITH, Graeme, Cameron, Murray , RUDGE, David, Alan , ROBERTS, Craig, Anthony
发明人： JAVAID, Muhammad, Hashim , MENEAR, Keith, Allan , MARTIN, Niall, Morrison, Barr , SMITH, Graeme, Cameron, Murray , RUDGE, David, Alan , ROBERTS, Craig, Anthony
IPC分类号： C07D237/32 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , A61K31/502 , A61P35/00
CPC分类号： C07D237/32 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12
摘要： A compound of the formula (I): wherein: R represents one or more optional substituents on the fused cyclohexene ring; X can be NR X or CR X R Y ; if X = NR X then n is 1 or 2 and if X = CR X R Y then n is 1; if X = NR X , then R X is selected from the group consisting of H, optionally substituted C 1-20 alkyl, optionally substituted C 5-20 aryl, optionally substituted C 3-20 heterocyclyl, optionally substituted amido, optionally substituted thioamido, optionally substituted ester, optionally substituted acyl, and optionally substituted sulfonyl groups; if X = CR X R Y then R x is selected from the group consisting of H, optionally substituted C 1-20 alkyl, optionally substituted C 5-20 aryl, optionally substituted C 3-20 heterocyclyl, optionally substituted amido, optionally substituted thioamido, optionally substituted sulfonamino, optionally substituted ether, optionally substituted ester, optionally substituted acyl, optionally substituted acylamido, and optionally substituted sulfonyl groups and Rγ is selected from H, hydroxy, optionally substituted amino, or R x and R γ may together form an optionally substituted spiro-C 3-7 cycloalkyl or heterocyclyl group; R C1 and R C2 are both hydrogen, or when X is CR X R Y , R C1 , R C2 , R x and R y , together with the carbon atoms to which they are attached, may form an optionally substituted fused aromatic ring; and R 1 is selected from H and halo. The compounds act as inhibitors of poly(APD-ribose)synthase, PARP-1.
摘要翻译：式（I）的化合物：其中：R表示稠合环己烯环上的一个或多个任选的取代基; X可以是NRX或CRXRY; 如果X = NRX，则n为1或2，如果X = CRXRY，则n为1; 如果X = NRX，则RX选自H，任选取代的C 1-20烷基，任选取代的C 5-20芳基，任选取代的C 3-20杂环基，任选取代的酰胺基，任选取代的硫代酰氨基，任选取代的酯，任选地取代的酰基和任选取代的磺酰基; 如果X = CRXRY，则Rx选自H，任选取代的C 1-20烷基，任选取代的C 5-20芳基，任选取代的C 3-20杂环基，任选取代的酰胺基，任选取代的硫代酰氨基，任选取代的磺酰氨基，任选取代的醚，任选取代的酯，任选取代的酰基，任选取代的酰基酰氨基和任选取代的磺酰基，选自H，羟基，任选取代的氨基，或R x和R' 可以一起形成任选取代的螺C3-7环烷基或杂环基; RC1和RC2均为氢，或当X为CRXRY时，RC1，RC2，Rx和Ry与它们所连接的碳原子一起形成任选取代的稠合芳环; 并且R 1选自H和卤素。该化合物作为聚（APD-核糖）合酶PARP-1的抑制剂。

10. 发明申请

WO2008068507A2 CHEMICAL COMPOUNDS-576 审中-公开
标题翻译：化学化合物-576
公开(公告)号：WO2008068507A2
公开(公告)日：2008-06-12
申请号：PCT/GB2007004697
申请日：2007-12-07
申请人： ASTRAZENECA AB , ASTRAZENECA UK LTD , AQUILA BRIAN , COOK DONALD JAMES , JOHNSTONE CRAIG , LEE STEPHEN , LYNE PAUL , RUDGE DAVID ALAN , VASBINDER MELISSA , WANG HAIXIA
发明人： AQUILA BRIAN , COOK DONALD JAMES , JOHNSTONE CRAIG , LEE STEPHEN , LYNE PAUL , RUDGE DAVID ALAN , VASBINDER MELISSA , WANG HAIXIA
IPC分类号： C07D401/04 , A61K31/472 , A61P35/00
CPC分类号： C07D401/04
摘要： The invention relates to chemical compounds of the formula (I): or pharmaceutically or pharmaceutically acceptable salts thereof, which possess B-Raf inhibitory activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments of use in the production of an anti-cancer effect in a warm-blooded animal such as man.
摘要翻译：本发明涉及具有B-Raf抑制活性的式（I）化合物或其药学上可接受的盐，因此可用于其抗癌活性，因此可用于治疗人或动物体的方法。本发明还涉及制备所述化合物的方法，含有它们的药物组合物及其在制造用于在温血动物如人中产生抗癌作用的药物中的用途。

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