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1.发明授权Substituted pyrazin-2-yl-sulphonamide (-3-pyridyl) compounds and uses thereof 有权取代的吡嗪-2-基 - 磺酰胺（-3-吡啶基）化合物及其用途公开(公告)号：US06258817B1
公开(公告)日：2001-07-10
申请号：US09504364
申请日：2000-02-15
IPC分类号： A01N4360
CPC分类号： C07D401/12 , C07D401/14 , C07D413/14
摘要： The invention concerns pharmaceutically useful compounds of the formula I, in which A1, A2, A3, A4, B1, m, Ar, W, X, Y, Z and R1 have any of the meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.
摘要翻译： 本发明涉及药学上有用的式I化合物，其中A1，A2，A3，A4，B1，m，Ar，W，X，Y，Z和R1具有本文定义的任何含义及其药学上可接受的盐， 和含有它们的药物组合物。 新型化合物具有内皮素受体拮抗剂活性，并且可用于例如治疗疾病或医学病症，其中升高或异常水平的内皮素起重要作用。 本发明还涉及制备新化合物的方法和该化合物在医疗中的用途。
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公开(公告)号：US5866568A
公开(公告)日：1999-02-02
申请号：US658969
申请日：1996-06-04
IPC分类号： A61K31/495 , A61K31/497 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/5377 , A61P1/00 , A61P3/00 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/02 , A61P15/00 , A61P19/00 , A61P35/00 , A61P43/00 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , A61N31/54 , A01N43/66 , C07D401/00 , C07D417/00
CPC分类号： C07D401/12 , C07D401/14 , C07D413/14
摘要： The invention concerns pharmaceutically useful compounds of the formula I, in which A.sup.1, A.sup.2, A.sup.3, A.sup.4, B.sup.1, m, Ar, W, X, Y, Z and R.sup.1 have any of the meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.
摘要翻译： 本发明涉及药学上有用的式I化合物，其中A1，A2，A3，A4，B1，m，Ar，W，X，Y，Z和R1具有本文定义的任何含义及其药学上可接受的盐， 和含有它们的药物组合物。 新型化合物具有内皮素受体拮抗剂活性，并且可用于例如治疗疾病或医学病症，其中升高或异常水平的内皮素起重要作用。 本发明还涉及制备新化合物的方法和该化合物在医疗中的用途。
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3.发明授权Substituted pyrazin-2-yl-sulphonamide-(3-pyridyl) compounds and uses thereof 有权取代的吡嗪-2-基 - 磺酰胺 - （3-吡啶基）化合物及其用途
公开(公告)号：US6060475A
公开(公告)日：2000-05-09
申请号：US211483
申请日：1998-12-14
IPC分类号： A61K31/495 , A61K31/497 , A61K31/505 , A61K31/506 , A61K31/535 , A61K31/5377 , A61P1/00 , A61P3/00 , A61P9/00 , A61P9/10 , A61P9/12 , A61P11/00 , A61P13/02 , A61P15/00 , A61P19/00 , A61P35/00 , A61P43/00 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , A01N43/60 , A61K31/445 , C07D241/04 , C07D401/00 , C07D413/00
CPC分类号： C07D401/12 , C07D401/14 , C07D413/14
摘要： The invention concerns pharmaceutically useful compounds of the formula I, in which A.sup.1, A.sup.2, A.sup.3, A.sup.4, B.sup.1, m, Ar, W, X, Y, Z and R.sup.1 have any of the meanings defined herein, and their pharmaceutically acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processes for the manufacture of the novel compounds and the use of the compounds in medical treatment.
摘要翻译： 本发明涉及药学上有用的式I化合物，其中A1，A2，A3，A4，B1，m，Ar，W，X，Y，Z和R1具有本文定义的任何含义及其药学上可接受的盐， 和含有它们的药物组合物。 新型化合物具有内皮素受体拮抗剂活性，并且可用于例如治疗疾病或医学病症，其中升高或异常水平的内皮素起重要作用。 本发明还涉及制备新化合物的方法和该化合物在医疗中的用途。
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公开(公告)号：US5668137A
公开(公告)日：1997-09-16
申请号：US667131
申请日：1996-06-20
IPC分类号： A61K31/41 , A61K31/42 , A61K31/433 , A61K31/495 , A61K31/496 , A61K31/50 , A61K31/505 , A61P1/00 , A61P1/16 , A61P3/06 , A61P9/00 , A61P9/04 , A61P9/08 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/08 , A61P13/02 , A61P15/00 , A61P43/00 , C07D237/20 , C07D239/69 , C07D241/22 , C07D261/16 , C07D285/12 , C07D285/135 , C07D241/00 , A61K31/54
CPC分类号： C07D285/135 , C07D237/20 , C07D239/69 , C07D241/22 , C07D261/16
摘要： The invention concerns pharmaceutically useful compounds of the formula I, in which R.sup.1, R.sup.2, R.sup.3, n, m and Het have any of the meanings defined herein, and their pharmaceutically-acceptable salts, and pharmaceutical compositions containing them. The novel compounds possess endothelin receptor antagonist activity and are useful, for example, in the treatment of diseases or medical conditions in which elevated or abnormal levels of endothelin play a significant causative role. The invention further concerns processess for the manufacture of the novel compounds and the use of the compounds in medical treatment.
摘要翻译： 本发明涉及药学上有用的式I化合物，其中R 1，R 2，R 3，n，m和Het具有本文定义的任何含义及其药学上可接受的盐和含有它们的药物组合物。 新型化合物具有内皮素受体拮抗剂活性，并且可用于例如治疗疾病或医学病症，其中升高或异常水平的内皮素起重要作用。 本发明还涉及用于制备新化合物的方法和该化合物在医疗中的用途。
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公开(公告)号：US20120329795A1
公开(公告)日：2012-12-27
申请号：US13607999
申请日：2012-09-10
IPC分类号： A61K31/517 , A61P35/00 , A61K31/5377
CPC分类号： C04B35/632 , C07D401/12
摘要： The invention concerns quinazoline derivatives of Formula I: wherein each of R1, X1, R2, R3, R5, n 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R1，X1，R2，R3，R5，n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：US20100292222A1
公开(公告)日：2010-11-18
申请号：US12776970
申请日：2010-05-10
IPC分类号： A61K31/551 , C07D487/04 , A61K31/5025 , C07D243/08 , A61P35/00
CPC分类号： C07D487/04
摘要： The invention concerns bicyclic compounds of Formula (I) wherein, R1, R2, R3, R4, R5, X1, X2, Y, k, m, n and p are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of androgen-receptor associated conditions, particularly prostate cancer.
摘要翻译： 本发明涉及式（I）的双环化合物，其中R1，R2，R3，R4，R5，X1，X2，Y，k，m，n和p如说明书中所定义。 本发明还涉及制备这些化合物的方法，含有它们的药物组合物及其在治疗雄激素受体相关病症，特别是前列腺癌中的用途。
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公开(公告)号：US20100267699A1
公开(公告)日：2010-10-21
申请号：US12702603
申请日：2010-02-09
申请人： Robert Hugh Bradbury , Gregory Richard Carr , Alfred Arthur Rabow , Srinivasa Rao Korupoju , Harikrishna Tumma
发明人： Robert Hugh Bradbury , Gregory Richard Carr , Alfred Arthur Rabow , Srinivasa Rao Korupoju , Harikrishna Tumma
IPC分类号： A61K31/551 , C07D487/04 , A61K31/5025 , C07D243/08 , A61P35/00
CPC分类号： A61K31/5025 , A61K31/551 , A61K31/58 , C07D471/04 , C07D487/04
摘要： The invention concerns bicyclic compounds of Formula I wherein , R1, R2, L1, L2, J, Y, k, n, p and r are as defined in the description. The present invention also relates to processes for the preparation of such compounds, pharmaceutical compositions containing them and their use in the treatment of androgen-receptor associated conditions, particularly prostate cancer.
摘要翻译： 本发明涉及式I的双环化合物，其中R1，R2，L1，L2，J，Y，k，n，p和r如说明书中所定义。 本发明还涉及制备这些化合物的方法，含有它们的药物组合物及其在治疗雄激素受体相关病症，特别是前列腺癌中的用途。
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公开(公告)号：US20080096881A1
公开(公告)日：2008-04-24
申请号：US10571991
申请日：2004-09-15
IPC分类号： A61K31/517 , A61K31/496 , A61K31/5377 , A61P35/00 , C07D401/12 , C07D401/14 , C07D413/14
CPC分类号： C04B35/632 , C07D401/12
摘要： The invention concerns quinazoline derivatives of Formula (I): wherein each of R1, X1, R2, R3, R5, n 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，X 1，R 2，R 3， R 5，n和m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：US20100029696A1
公开(公告)日：2010-02-04
申请号：US11817391
申请日：2006-02-28
申请人： Robert Hugh Bradbury
发明人： Robert Hugh Bradbury
IPC分类号： A61K31/517 , C07D401/14 , A61P35/00
CPC分类号： 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例如人中抑制erbB2受体酪氨酸激酶产生 。
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10.发明申请公开(公告)号：US20090029968A1
公开(公告)日：2009-01-29
申请号：US12095659
申请日：2006-11-29
IPC分类号： A61K31/517 , C07D455/02 , A61P35/00 , A61K31/55
CPC分类号： C07D239/94
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中抑制erbB2受体酪氨酸激酶产生，例如 人。
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