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1. 发明申请

WO2009056886A1 PYRIMIDINE DERIVATIVES AND THEIR USE AS MODULATORS OF FGFR ACTIVITY 审中-公开
标题翻译：吡嗪衍生物及其用作FGFR活性的调节剂
公开(公告)号：WO2009056886A1
公开(公告)日：2009-05-07
申请号：PCT/GB2008/051018
申请日：2008-10-30
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , FOOTE, Kevin, Michael , THEOCLITOU, Maria-Elena
发明人： FOOTE, Kevin, Michael , THEOCLITOU, Maria-Elena
IPC分类号： C07D401/14 , A61K31/506 , A61P35/00
CPC分类号： C07D401/14
摘要： There is provided pyrimidine compounds of formula 1: or pharmaceutical salts thereof. There is al so provided processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy, for exampl e in the treatment of proliferative disease such as cancer and particular ly in disease mediated by a FGFR inhibitory effect.
摘要翻译：提供式1的嘧啶化合物或其药用盐。所提供的制备方法，含有它们的药物组合物，制备药物组合物的方法及其在治疗中的用途，用于治疗增殖性疾病如癌症，特别是由FGFR介导的疾病抑制作用。

2. 发明申请

WO2007083096A3 N- (2, 3-DIFLUOROPHENYL) -2- [4- ( {7-METHOXY-5- [ (2R) -PIPERIDIN. -2-YLMETHOXY] QUINAZOLI N-4-YL}AMINO) -LH-PYRAZOL-1-YL] ACETAMIDE AND N- (2, 3 -D I FLUORO PHENYL) -2- [4- ( {7-ETHOXY-5- [ (2R) -PIPERIDIN. -2-YLMETHOXY] QUINAZOLIN 审中-公开
公开(公告)号：WO2007083096A3
公开(公告)日：2007-07-26
申请号：PCT/GB2007/000119
申请日：2007-01-17
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , FOOTE, Kevin, Michael
发明人： FOOTE, Kevin, Michael
IPC分类号： C07D403/12 , A61K31/47
摘要： The invention provided a compound of formula (I) for use in the treatment of disease, in particular proliferative diseases such as cancer and for use in the preparation of medicaments for use in the treatment of proliferative diseases; the invention also processes for the preparation of such compounds, as well as pharmaceutical compositions containing them as active ingredient.

3. 发明申请

WO2006067391A1 PYRAZOLYLAMINO SUBSTITUTED QUINAZOLES FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的吡唑啉胺取代的喹诺酮
公开(公告)号：WO2006067391A1
公开(公告)日：2006-06-29
申请号：PCT/GB2005/004872
申请日：2005-12-16
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , FOOTE, Kevin, Michael
发明人： FOOTE, Kevin, Michael
IPC分类号： C07D401/12 , C07D403/14 , A61K31/517 , A61P35/00 , C07F9/09
CPC分类号： C07F9/65583 , C07D403/12 , C07D403/14
摘要： The invention provided a compound of formula: (I) for use in the treatment of disease, in particular proliferative diseases such as cancer and for use in the preparation of medicaments for use in the treatment of proliferative diseases; the invention also processes for the preparation of such compounds, as well as pharmaceutical compositions containing them as active ingredient.
摘要翻译：本发明提供了一种式（I）化合物，其用于治疗疾病，特别是增殖性疾病如癌症和用于制备用于治疗增殖性疾病的药物; 本发明还用于制备这些化合物以及含有它们作为活性成分的药物组合物。

4. 发明申请

WO2009153589A1 PYRIDINE COMPOUNDS 审中-公开
标题翻译：吡啶化合物
公开(公告)号：WO2009153589A1
公开(公告)日：2009-12-23
申请号：PCT/GB2009/050675
申请日：2009-06-15
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , BARLAAM, Bernard, Christophe , FOOTE, Kevin, Michael , PLE, Patrick
发明人： BARLAAM, Bernard, Christophe , FOOTE, Kevin, Michael , PLE, Patrick
IPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , A61K31/4439 , A61P35/00
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14
摘要： The present invention relates to compounds that inhibit of focal adhesion kinase 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 such as cancer.
摘要翻译：本发明涉及抑制粘着斑激酶功能的化合物，其制备方法，含有它们作为活性成分的药物组合物，作为药物的用途，以及它们在制备用于温热治疗的药物中的用途，血液动物如人类的疾病如癌症。

5. 发明申请

WO2007135398A1 INDOLE DERIVATIVES 审中-公开
标题翻译： INDOLE DORIVATIVES
公开(公告)号：WO2007135398A1
公开(公告)日：2007-11-29
申请号：PCT/GB2007/001858
申请日：2007-05-18
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , FOOTE, Kevin, Michael , GRIFFEN, Edward, Jolyon
发明人： FOOTE, Kevin, Michael , GRIFFEN, Edward, Jolyon
IPC分类号： C07D471/04 , A61K31/4162 , A61K31/437 , A61P31/00
CPC分类号： C07D471/04
摘要： The invention concerns indole derivatives of Formula (I) or pharmaceutically-acceptable salts thereof, wherein each of Ring A, m, R 1 , R 2 , n, R 3 and G 1 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of disease mediated by a PI3K enzyme and/or a mTOR kinase.
摘要翻译：本发明涉及式（I）的吲哚衍生物或其药学上可接受的盐，其中环A，m，R 1，R 2，n，R 0 > 3＆gt;和＆lt; 1＆gt;具有上文在描述中定义的任何含义; 其制备方法，含有它们的药物组合物及其在治疗中的用途，例如用于治疗由PI3K酶和/或mTOR激酶介导的疾病。

6. 发明申请

WO2007008143A1 HETEROCYCLIC SULFONAMIDE DERIVATIVES AS INHIBITORS OF FACTOR XA 审中-公开
标题翻译：作为因子XA的抑制剂的杂环磺酰胺衍生物
公开(公告)号：WO2007008143A1
公开(公告)日：2007-01-18
申请号：PCT/SE2006/000837
申请日：2006-07-05
申请人： ASTRAZENECA AB , ALSTERMARK, Christer , AMIN, Kosrat , ANDERSSON, Kjell , CHEN, Yantao , FAHLANDER, Ulf , FOOTE, Kevin, Michael , GRANBERG, Kenneth , HOVDAL, Daniel
发明人： ALSTERMARK, Christer , AMIN, Kosrat , ANDERSSON, Kjell , CHEN, Yantao , FAHLANDER, Ulf , FOOTE, Kevin, Michael , GRANBERG, Kenneth , HOVDAL, Daniel
IPC分类号： C07D401/14 , A61K31/497 , A61K31/501 , A61P7/02 , C07D401/12 , C07D403/14 , C07D409/14 , C07D413/14
CPC分类号： C07D409/14 , C07D401/04 , C07D401/14
摘要： The invention relates to compounds of formula (I), wherein R 1 and R 3 are independently selected from carbon and nitrogen; R 2 is oxo or thioxo; n is 0, 1 or 2; each R 10 is independently selected from hydrogen and C 1 - 3 alkyl; R 4 and R 5 are each selected from carbon and nitrogen, wherein at least one of R 4 and R 5 is nitrogen; R 6 is hydrogen or oxo; R 7 is an aliphatic, partially saturated or aromatic carbocyclic ring, said carbocyclic ring having 0, 1 or 2 hetero nitrogen; m is 0, 1 or 2; each R 11 is independently selected from hydrogen, hydroxy, oxo, C 1-5 alkyl, carboxy, hydroxyC 1-5 alkyl, carboxyC 1-5 alkyl, C 1-5 alkoxyoxoC 1-5 alkyl, carbamoyl, C 1-5 alkylcarbamoyl, di (C 1-5 alkyl)carbamoyl, carbamoylC 1-4 alkyl,C 1-5 alkylcarbamoylC 1-4 alkyl, di(C 1-5 alkyl)carbamoylC 1-4 alkyl, hydroxyC 1-5 alkylcarbamoyl, C 1-5 alkoxyC 1-5 alkylcarbamoyl, hydroxyC 1-5 alkylcarbamoylC 1-4 alkyl, C 1-5 alkoxyC 1-5 alkylcarbamoylC 1-4 alkyl, CONR 80 (CH 2 ) x S(O) p R90, CONH(CH 2 ) q NR 100 R 100 , -C 1-5 alkyl-Y 1 , -COOCHR 170 R 180 and -CON R 170 R 180 ; R 8 is a bond, C 1-4 alkylene or C 2-6 alkenylene; R 9 is an aromatic ring system having 0, 1 or 2 hetero atoms; wherein R 9 is substituted by 0 or 1 halogen; or a pharmaceutically acceptable salt thereof, said compounds possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the compounds, to their use, to pharmaceutical compositions comprising them, to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect, and to combinations comprising them.
摘要翻译：本发明涉及式（I）化合物，其中R 1和R 3独立地选自碳和氮; R 2是氧代或硫代; n为0,1或2; 每个R 10独立地选自氢和C 1 -C 3 - 烷基; R 4和R 5各自选自碳和氮，其中R 4和R 5中的至少一个 >是氮; R 6是氢或氧代; R 7是脂族，部分饱和或芳族碳环，所述碳环具有0,1或2个杂氮; m为0,1或2; 每个R 11独立地选自氢，羟基，氧代，C 1-5烷基，羧基，羟基C 1-5烷基，羧基C 1-4烷基， C 1-5烷基，C 1-5烷氧基氧基C 1-5烷基，氨基甲酰基，C 1-5烷基氨基甲酰基，二（C 1-5烷基）氨基甲酰基，氨基甲酰基C 1-4烷基，C 1-5烷基氨基甲酰基C 1-4 - 烷基，二（C 1-5烷基）氨基甲酰基C 1-4烷基，羟基C 1-5烷基氨基甲酰基，C 1 -5烷氧基C 1-5烷基氨基甲酰基，羟基C 1-5烷基氨基甲酰基C 1-4烷基，C 1-5 烷基C 1-4烷基氨基甲酰基C 1-4烷基，CONR 80（CH 2）

7. 发明申请

WO2003022849A1 CARBAZOLE DERIVATIVES AND THEIR USE AS NPY5 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：卡巴唑衍生物及其作为NPY5受体拮抗剂的用途
公开(公告)号：WO2003022849A1
公开(公告)日：2003-03-20
申请号：PCT/GB2002/004109
申请日：2002-09-09
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , FOOTE, Kevin, Michael , BLOCK, Michael, Howard , BRAILSFORD, Wayne
发明人： FOOTE, Kevin, Michael , BLOCK, Michael, Howard , BRAILSFORD, Wayne
IPC分类号： C07D487/04
CPC分类号： C07D471/04
摘要： The use of a compound of formula (I) in the manufacture of a medicament for the treatment, in a warm-blooded animal, of disorders mediated by the neuropeptide Y5 receptor (I), wherein: R 1 , R 2 , R 3 and X 1 -X 6 are as defined within or a pharmaceutically acceptable salt, prodrug or solvate thereof, is described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are also described.
摘要翻译：式（I）化合物在制备用于在温血动物中治疗由神经肽Y5受体（I）介导的病症的药物中的用途，其中：R1，R2，R3和X <1 > -X 6定义在其内或其药学上可接受的盐，前药或溶剂化物中。还描述了制备式（I）化合物的药物组合物，方法和方法。

8. 发明申请

WO2003047583A1 PHARMACEUTICAL COMPOSITIONS COMPRISING BENZOFURANYL SUBSTITUTED 3-CYANOQUINOLINE DERIVATIVES AND THEIR USE FOR THE TREATMENT OF SOLID TUMOURS 审中-公开
标题翻译：包含苯并呋喃取代的3-氰基喹啉衍生物的药物组合物及其用于治疗固体肿瘤的用途
公开(公告)号：WO2003047583A1
公开(公告)日：2003-06-12
申请号：PCT/GB2002/005497
申请日：2002-12-05
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , HENNEQUIN, Laurent, Francois, Andre , GIBSON, Keith, Hopkinson , FOOTE, Kevin, Michael
发明人： HENNEQUIN, Laurent, Francois, Andre , GIBSON, Keith, Hopkinson , FOOTE, Kevin, Michael
IPC分类号： A61K31/4709
CPC分类号： A61K31/4709
摘要： The invention concerns the use of quinoline derivatives of Formula (I) wherein each of Z, m, R 1 , n and R 3 have any of the meanings defined hereinbefore in the description in the manufacture of a medicament for use for use as an anti-proliferative agent in the containment and/or treatment of solid tumour disease.
摘要翻译：本发明涉及式（I）的喹啉衍生物的用途，其中Z，m，R 1，n和R 3中的每一个在制备用于制备在实体瘤疾病的遏制和/或治疗中用作抗增殖剂。

9. 发明申请

WO2009019518A1 PYRIMIDINE COMPOUNDS HAVING A FGFR INHIBITORY EFFECT 审中-公开
标题翻译：具有FGFR抑制作用的吡咯烷酮化合物
公开(公告)号：WO2009019518A1
公开(公告)日：2009-02-12
申请号：PCT/GB2008/050673
申请日：2008-08-07
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , FOOTE, Kevin, Michael , THEOCLITOU, Maria-Elena
发明人： FOOTE, Kevin, Michael , THEOCLITOU, Maria-Elena
IPC分类号： C07D413/14 , A61K31/506 , A61P35/00
CPC分类号： C07D413/14
摘要： There is provided pyrimidine compounds of formula (I): or pharmaceutical salts thereof. There is also provided processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy, for example in the treatment of proliferative disease such as cancer and particularly in disease mediated by a FGFR inhibitory effect.
摘要翻译：提供式（I）的嘧啶化合物：或其药学上可接受的盐。还提供了其制备方法，含有它们的药物组合物，制备药物组合物的方法及其在治疗中的用途，例如用于治疗增殖性疾病如癌症，特别是在由FGFR抑制作用介导的疾病中的治疗。

10. 发明申请

WO2007129052A1 PYRAZOLE DERIVATIVES AND THEIR USE AS PI3K INHIBITORS 审中-公开
标题翻译：吡唑衍生物及其作为PI3K抑制剂使用
公开(公告)号：WO2007129052A1
公开(公告)日：2007-11-15
申请号：PCT/GB2007/001619
申请日：2007-05-02
申请人： ASTRAZENECA AB , ASTRAZENECA UK LIMITED , DAVID, Laurent , FOOTE, Kevin, Michael , LISIUS, Annea
发明人： DAVID, Laurent , FOOTE, Kevin, Michael , LISIUS, Annea
IPC分类号： C07D401/04 , A61K31/44 , A61P35/00 , C07D417/14
CPC分类号： C07D401/04 , C07D417/14
摘要： The invention concerns pyrazole derivatives of Formula( I) or pharmaceutically-acceptable salts thereof, wherein each of R, Ring A, m, R 1 , R 2 and R 3 has any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in therapy, for example in the treatment of disease mediated by a PI3K enzyme and/or a mTOR kinase.
摘要翻译：本发明涉及式（I）的吡唑衍生物或其药学上可接受的盐，其中R，A，M，R 1，R 2和R 2中的每一个 > 3 具有上文在描述中定义的任何含义; 其制备方法，含有它们的药物组合物及其在治疗中的用途，例如用于治疗由PI3K酶和/或mTOR激酶介导的疾病。

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