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公开(公告)号:US20070232607A1
公开(公告)日:2007-10-04
申请号:US11628011
申请日:2005-06-02
申请人: Robert Bradbury , Jason Kettle , James Scott , Bernard Barlaam
发明人: Robert Bradbury , Jason Kettle , James Scott , Bernard Barlaam
IPC分类号: A61K31/517 , A61K31/496 , A61K31/5377 , C07D239/72 , C07D401/00 , C07D413/14
CPC分类号: C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14
摘要: The invention concerns quinazoline derivatives of the formula (I), wherein each of R1, R2, R3, R4, R5, R6, R7, X1, Q1, m and n 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 1,R 2,R 3,R 4, R 5,R 6,R 7,X 1,X 1,..., m和n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:US20070037837A1
公开(公告)日:2007-02-15
申请号:US10572048
申请日:2004-09-15
IPC分类号: A61K31/517
CPC分类号: C04B35/632 , A61K31/517 , C07D401/12
摘要: The invention concerns quinazoline derivatives of Formula (I): wherein each of R1, R2, X1, R5 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 as an antiproliferative agent in the prevention or treatment of tumours which are sensitive to inhibition of EGF and 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 1,R 2,X 1,R 5, / SUP>和m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EGF和erbB受体酪氨酸激酶的抑制敏感的肿瘤中作为抗增殖剂的药物中的用途。
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公开(公告)号:US20090131463A1
公开(公告)日:2009-05-21
申请号:US12359541
申请日:2009-01-26
申请人: Bernard Barlaam , Andrew Pape , Andrew Thomas
发明人: Bernard Barlaam , Andrew Pape , Andrew Thomas
IPC分类号: A61K31/506 , C07D401/02 , A61P35/00
CPC分类号: C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14
摘要: The invention provides compounds of formula in which R1, R2, R3 and R4 have the meanings defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.
摘要翻译: 本发明提供式R1化合物,其中R1,R2,R3和R4具有本说明书中定义的含义; 其准备过程; 含有它们的药物组合物; 制备药物组合物的方法; 及其在治疗中的应用。
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公开(公告)号:US20120095011A1
公开(公告)日:2012-04-19
申请号:US13313097
申请日:2011-12-07
申请人: Bernard Barlaam , Andrew Pape , Andrew Thomas
发明人: Bernard Barlaam , Andrew Pape , Andrew Thomas
IPC分类号: A61K31/506 , A61P35/00 , A61P35/02 , C07D403/12
CPC分类号: C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14
摘要: The invention provides compounds of formula in which R1, R2, R3 and R4 have the meanings defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.
摘要翻译: 本发明提供式R1化合物,其中R1,R2,R3和R4具有本说明书中定义的含义; 其准备过程; 含有它们的药物组合物; 制备药物组合物的方法; 及其在治疗中的应用。
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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:US07045539B2
公开(公告)日:2006-05-16
申请号:US10450927
申请日:2001-12-19
申请人: Bernard Barlaam , Peter Bernstein , Cathy Dantzman , Paul Warwick
发明人: Bernard Barlaam , Peter Bernstein , Cathy Dantzman , Paul Warwick
IPC分类号: A61K31/425 , C07D277/62 , A61P25/00
CPC分类号: C07D263/57 , C07D277/66 , C07D413/04 , C07D417/04
摘要: Compounds of the formula (I) for use as an estrogen receptor-β-selective ligand are described wherein: X is O or S; and R1, R3 R6 are as described in the specification. The use of these compounds in treating Alzheimer's disease, anxiety disorders, depressive disorders, osteoporosis, cardiovascular disease, rheumatoid arthritis and prostate cancer is described; as are processes for making them.
摘要翻译: 描述了用作雌激素受体-β-选择性配体的式(I)化合物,其中:X为O或S; 和R 1,R 3,R 6和S 6如说明书中所述。 描述了这些化合物在治疗阿尔茨海默病,焦虑障碍,抑郁障碍,骨质疏松症,心血管疾病,类风湿性关节炎和前列腺癌中的用途。 制作它们的过程也是如此。
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公开(公告)号:US20070208066A1
公开(公告)日:2007-09-06
申请号:US11247537
申请日:2005-10-11
申请人: Bernard Barlaam , Peter Bernstein , Cathy Dantzman , Paul Warwick
发明人: Bernard Barlaam , Peter Bernstein , Cathy Dantzman , Paul Warwick
IPC分类号: A61K31/41 , A61K31/423 , A61K31/428 , C07D263/52 , C07D277/60
CPC分类号: C07D263/57 , C07D277/66 , C07D413/04 , C07D417/04
摘要: Compounds of the formula (I) for use as an estrogen receptor -β-selective ligand are described wherein: X is O or S; and R1, R3-R6 are as described in the specification. The use of these compounds in treating Alzheimer's disease, anxiety disorders, depressive disorders, osteoporosis, cardiovascular disease, rheumatoid arthritis and prostate cancer is described; as are processes for making them.
摘要翻译: 描述了用作雌激素受体 - 选择性配体的式(I)化合物,其中:X为O或S; R 1,R 3,R 6和R 6如说明书中所述。 描述了这些化合物在治疗阿尔茨海默病,焦虑障碍,抑郁障碍,骨质疏松症,心血管疾病,类风湿性关节炎和前列腺癌中的用途。 制作它们的过程也是如此。
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公开(公告)号:US20060111408A1
公开(公告)日:2006-05-25
申请号:US11246663
申请日:2006-01-03
申请人: Bernard Barlaam , Peter Bernstein , Cathy Dantzman , Paul Warwick
发明人: Bernard Barlaam , Peter Bernstein , Cathy Dantzman , Paul Warwick
IPC分类号: A61K31/428 , C07D417/02 , C07D277/60
CPC分类号: C07D263/57 , C07D277/66 , C07D413/04 , C07D417/04
摘要: Compounds of the formula (I) for use as an estrogen receptor -β-selective ligand are described wherein: X is O or S; and R1, R3-R6 are as described in the specification. The use of these compounds in treating Alzheimer's disease, anxiety disorders, depressive disorders, osteoporosis, cardiovascular disease, rheumatoid arthritis and prostate cancer is described; as are processes for making them.
摘要翻译: 描述了用作雌激素受体 - 选择性配体的式(I)化合物,其中:X为O或S; R 1,R 3,R 6和R 6如说明书中所述。 描述了这些化合物在治疗阿尔茨海默病,焦虑障碍,抑郁障碍,骨质疏松症,心血管疾病,类风湿性关节炎和前列腺癌中的用途。 制作它们的过程也是如此。
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公开(公告)号:US20050043350A9
公开(公告)日:2005-02-24
申请号:US10399010
申请日:2001-10-10
申请人: Bernard Barlaam , James Folmer , Timothy Piser
发明人: Bernard Barlaam , James Folmer , Timothy Piser
IPC分类号: A61K31/00 , A61K31/352 , A61K31/353 , A61K31/37 , A61P5/24 , A61P9/10 , A61P13/08 , A61P19/02 , A61P19/10 , A61P25/22 , A61P25/24 , A61P25/28 , A61P29/00 , A61P35/00 , A61P43/00 , C07D311/18 , C07D311/36 , C07D311/58 , A61K31/47 , A61K31/385
CPC分类号: C07D311/36 , A61K31/00 , A61K31/352
摘要: A method for treating a disease associated with the estrogen receptor-β, comprising the step of administiering a therapeutically-effective amount of a compound that satifies the equation: KiαA/KiβA>25, optionally having general structure (I).
摘要翻译: 一种用于治疗与雌激素受体-β相关的疾病的方法,包括给予治疗有效量的饱和以下方程式的化合物的步骤:KialphaA / KibetaA 25,任选具有通式结构(I)。
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