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公开(公告)号:US20060287295A1
公开(公告)日:2006-12-21
申请号:US10572794
申请日:2004-09-22
IPC分类号: A61K31/553 , A61K31/551 , A61K31/541 , A61K31/5377 , A61K31/517 , C07D417/02 , C07D413/02 , C07D403/02
CPC分类号: C07D413/14 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14
摘要: The invention concerns quinazoline derivatives of Formula (I), wherein each of R1a, R1b, R2, R3 and a have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosine kinases.
摘要翻译: 本发明涉及式(I)的喹唑啉衍生物,其中R 1a,R 1b,R 2,R 3, / SUP>和a具有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制备用于预防或治疗对erbB受体酪氨酸激酶抑制敏感的肿瘤中的抗增殖剂的药物中的用途。
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公开(公告)号:US20070032508A1
公开(公告)日:2007-02-08
申请号:US10571851
申请日:2004-09-14
IPC分类号: A61K31/517 , C07D403/02 , C07D417/02 , C07D413/02
CPC分类号: C04B35/632 , C07D401/12 , C07D401/14 , C07D417/14
摘要: A quinazoline derivative of the formula (I); wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm blooded animal such as man.
摘要翻译: 式(I)的喹唑啉衍生物; 其中取代基如用于产生抗增殖作用的文本中所定义,其作用单独或部分通过在温血动物如人中抑制erbB2受体酪氨酸激酶产生。
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公开(公告)号:US20070032513A1
公开(公告)日:2007-02-08
申请号:US10572261
申请日:2004-09-13
IPC分类号: A61K31/517 , C07D403/02
CPC分类号: C07D403/12 , C07D401/12 , C07D403/14
摘要: The invention concerns quinazoline derivatives of the Formula I: (A chemical formula should be inserted here—please see paper copy enclosed herewith) wherein each of R1, R2, W, X1, X2, Z, a and b are as defined in the description; processes for their preparation; pharmaceutical compositions containing them and their use in the manufacture of a medicament for providing an anti-proliferative effect. The quinazoline derivatives of Formula I are expected to be useful in the treatment of diseases such as certain cancers mediated by erbB receptor tyrosine kinases, particularly EGFR tyrosine kinase.
摘要翻译: 本发明涉及式I的喹唑啉衍生物:(化学式应在此插入,请参见随附的纸质复制品),其中R 1,R 2,W,X 1,X 2,Z,a和b各自如说明书中所定义 ; 其准备过程; 含有它们的药物组合物及其在制备用于提供抗增殖作用的药物中的用途。 预期式I的喹唑啉衍生物可用于治疗疾病,例如由erbB受体酪氨酸激酶,特别是EGFR酪氨酸激酶介导的某些癌症。
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公开(公告)号:US20070043010A1
公开(公告)日:2007-02-22
申请号:US10573352
申请日:2004-09-22
IPC分类号: A61K31/33
CPC分类号: C07D403/12 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14
摘要: The invention concerns a quinazoline derivative of the Formula (I): wherein each of the variables have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosine kinases.
摘要翻译: 本发明涉及式(I)的喹唑啉衍生物:其中每个变量具有说明书中定义的任何含义; 其制备方法,含有它们的药物组合物及其在制备用于预防或治疗对erbB受体酪氨酸激酶抑制敏感的肿瘤中的抗增殖剂的药物中的用途。
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公开(公告)号:US20070293490A1
公开(公告)日:2007-12-20
申请号:US10586965
申请日:2005-01-31
申请人: Benedicte Delouvrie , Craig Harris , Laurent Hennequin , Christopher Halsall , Janet Pease , Peter Smith
发明人: Benedicte Delouvrie , Craig Harris , Laurent Hennequin , Christopher Halsall , Janet Pease , Peter Smith
IPC分类号: A61K31/517 , A61K31/5377 , A61P35/00 , C07D239/94 , C07D413/12
CPC分类号: C07D239/42 , C07D401/12 , C07D403/12
摘要: A quinazoline derivative of the formula (I) wherein: R1, R2, R3, R3a, R4, R5, R5a R6, R7, a, m and p are as defined in the description. Also claimed are pharmaceutical compositions containing the quinazoline derivative, the use of the quinazoline derivatives as medicaments and processes for the preparation of the quinazoline derivative. The quinazoline derivatives of formula (I), are useful in the treatment of hyperproliferative disorders such as a cancer.
摘要翻译: 式(I)的喹唑啉衍生物其中:R 1,R 2,R 3,R 3, R 4,R 5,R 5,R 6,R 7,R 7, a,m和p如说明书中所定义。 还要求的是含有喹唑啉衍生物的药物组合物,喹唑啉衍生物作为药物的用途以及制备喹唑啉衍生物的方法。 式(I)的喹唑啉衍生物可用于治疗过度增殖性疾病如癌症。
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公开(公告)号:US20050054662A1
公开(公告)日:2005-03-10
申请号:US10494388
申请日:2002-10-31
申请人: Laurent Hennequin , Jason Kettle , Martin Pass , Robert Bradbury
发明人: Laurent Hennequin , Jason Kettle , Martin Pass , Robert Bradbury
IPC分类号: A61K31/517 , A61K31/5377 , A61P35/00 , A61P43/00 , C07D239/94 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D405/14 , C07D409/12 , C07D409/14 , C07D411/12 , C07D413/12 , C07D413/14 , C07D417/14
CPC分类号: C04B35/632 , C07D239/94 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要: The invention concerns quinazoline derivatives of Formula (I); wherein each of Q1, Q2, Z, R1, R2, R3, and m have any of the meanings defined in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of tumours which are sensitive to inhibition of erbB receptor tyrosin kinases.
摘要翻译: 本发明涉及式(I)的喹唑啉衍生物; 其中Q 1,Q 2,Z,R 1,R 2,R 3和m各自具有本说明书中定义的任何含义; 其制备方法,含有它们的药物组合物及其在制备用于预防或治疗对抑制erbB受体酪氨酸激酶敏感的肿瘤的药物中的用途。
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公开(公告)号:US20120197027A1
公开(公告)日:2012-08-02
申请号:US13090405
申请日:2011-04-20
IPC分类号: C07D209/04
CPC分类号: A61K31/505 , A61K31/517 , C07D231/12 , C07D233/56 , C07D239/88 , C07D239/94 , C07D249/08 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要: The invention relates to the use of compounds of formula (I) and salts thereof, in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm-blooded animals, processes for the preparation of such compounds, pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof as active ingredient and compounds of formula I. The compounds of formula I and the pharmaceutically acceptable salts thereof inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.
摘要翻译: 本发明涉及式(I)化合物及其盐在制备用于在温血动物中产生抗血管生成和/或血管通透性降低作用的药物中的用途,其制备方法 化合物,含有式I化合物的药物组合物或其药学上可接受的盐作为活性成分和式I化合物。式I化合物及其药学上可接受的盐抑制VEGF的作用,其在治疗中的价值性质 许多疾病状态包括癌症和类风湿性关节炎。
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公开(公告)号:US20050282856A1
公开(公告)日:2005-12-22
申请号:US10532958
申请日:2003-10-28
申请人: Laurent Hennequin
发明人: Laurent Hennequin
IPC分类号: A61P35/00 , C07D405/12 , A61K31/4709 , C07D45/02
CPC分类号: C07D405/12
摘要: The invention concerns quinoline derivatives of Formula (I) wherein each of Z1, m, R1, n, R3, Z2 and R14 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive or 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,其中Z 1,m,R 1,n,R 3,Z, > 2 SUP>和R 14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制备用于在实体瘤疾病的遏制和/或治疗中作为抗侵袭性或抗增殖剂的药物的用途。
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公开(公告)号:US20050085465A1
公开(公告)日:2005-04-21
申请号:US10502538
申请日:2003-01-28
申请人: Laurent Hennequin
发明人: Laurent Hennequin
IPC分类号: C07D491/113 , A61K31/517 , A61K31/519 , A61P9/00 , A61P35/00 , C07D401/14 , C07D403/12 , C07D403/14 , C07D471/04 , C07D491/04 , C07D519/00 , A61K31/541 , A61K31/5377
CPC分类号: C07D401/14 , C07D403/12 , C07D471/04 , C07D491/04
摘要: The invention relates to compounds of the formula (I): wherein ring C is as defined herein, for example indolyl, indazolyl or azaindolyl; Z is —O—, —NH— or —S—; n is 0-5; m is 0-3; R1 and R2 are defined herein including groups: (i) Q1X1 wherein Q1 and X1 are as defined herein; (ii) Q15W3 wherein Q15 and W3 are as defined herein, (iii) Q21W4C1-5alkylX1- wherein Q21, W4 and X1 are as defined herein, (iv) Q28C1-5alkylX1-, Q28C2-5alkenylX1- or Q28C2-5alkynylX1- wherein Q29 and X1 are as defined herein and (v) Q29C1-5alkylX1-, Q29C2-5alkenylX1- or Q29C2-5alkynylX1- wherein Q29 and X1 are as defined herein; R2 can also be 6,7-methylenedioxy or 6,7-ethylenedioxy; and salts thereof; their use in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm?blooded animals; processes for the preparation of such compounds; intermediates used in such processes; processes for making such intermediates; pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof and methods of treating disease states involving angiogenesis by administering a compound of formula I or a pharmaceutically acceptable salt thereof. The compounds of formula I inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.
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公开(公告)号:US20080027069A1
公开(公告)日:2008-01-31
申请号:US11705035
申请日:2007-02-12
申请人: Laurent Hennequin
发明人: Laurent Hennequin
IPC分类号: A61K31/517 , A61P35/00 , C07D401/14 , C07D471/04
CPC分类号: C07D401/14 , C07D403/12 , C07D471/04 , C07D491/04
摘要: The invention relates to compounds of the formula (I): wherein ring C is as defined herein, for example indolyl, indazolyl or azaindolyl; Z is —O—, —NH— or —S—; n is 0-5; m is 0-3; R1 and R2 are defined herein including groups: (i) Q1X1 wherein Q1 and X1 are as defined herein; (ii) Q15W3 wherein Q15 and W3 are as defined herein, (iii) Q21W4C1-5alkylX1— wherein Q21, W4 and X1 are as defined herein, (iv) Q28C1-5alkylX1—, Q28C2-5alkenylX1— or Q28C2-5alkynylX1— wherein Q28 and X1 are as defined herein and (v) Q29C1-5alkylX1—, Q29C2-5alkenylX1— or Q29C2-5alkynylX1— wherein Q29 and X1 are as defined herein; R2 can also be 6,7-methylenedioxy or 6,7-ethylenedioxy; and salts thereof; their use in the manufacture of a medicament for use in the production of an antiangiogenic and/or vascular permeability reducing effect in warm?blooded animals; processes for the preparation of such compounds; intermediates used in such processes; processes for making such intermediates; pharmaceutical compositions containing a compound of formula I or a pharmaceutically acceptable salt thereof and methods of treating disease states involving angiogenesis by administering a compound of formula I or a pharmaceutically acceptable salt thereof. The compounds of formula I inhibit the effects of VEGF, a property of value in the treatment of a number of disease states including cancer and rheumatoid arthritis.
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