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公开(公告)号:US08466165B2
公开(公告)日:2013-06-18
申请号:US12754556
申请日:2010-04-05
申请人: Stephen Alan Fakhoury , Helen Tsenwhei Lee , Jessica Elizabeth Reed , Kevin Matthew Schlosser , Karen Elaine Sexton , Haile Tecle , Roy Thomas Winters
发明人: Stephen Alan Fakhoury , Helen Tsenwhei Lee , Jessica Elizabeth Reed , Kevin Matthew Schlosser , Karen Elaine Sexton , Haile Tecle , Roy Thomas Winters
IPC分类号: A61K31/517 , A01N43/90 , C07D239/72
CPC分类号: C07D239/94 , C07D401/12 , C07D403/12
摘要: This invention provides quinazoline compounds of the formula: wherein: R1 is halo; R2 is H or halo; R3 is a) C1-C3 alkyl, optionally substituted by halo; or b) —(CH2)n-morpholino, —(CH2)n-piperidine, —(CH2)n-piperazine, —(CH2)n-piperazine-N(C1-C3 alkyl), —(CH2)n-pyrrolidine, or —(CH2)n-imidazole; n is 1 to 4; R4 is —(CH2)m-Het; Het is morpholine, piperidine, piperazine, piperazine-N(C1-C3 alkyl), imidazole, pyrrolidine, azepane, 3,4-dihydro-2H-pyridine, or 3,6-dihydro-2H-pyridine, each optionally substituted by alkyl, halo, OH, NH2, NH(C1-C3 alkyl) or N(C1-C3 alkyl)2; m is 1-3; and X is O, S or NH; or a pharmaceutically acceptable salt thereof, as well as processes and intermediate compounds for making them, useful pharmaceutical compositions and methods of using the compounds in the treatment of proliferative diseases.
摘要翻译: 本发明提供下式的喹唑啉化合物:其中:R1是卤素; R2是H或卤素; R3是a)任选被卤素取代的C 1 -C 3烷基; 或(b) - (CH 2)n - 吗啉代, - (CH 2)n - 哌啶, - (CH 2)n - 哌嗪, - (CH 2)n - 哌嗪-N(C 1 -C 3烷基), - (CH 2) ,或 - (CH 2)n - 咪唑; n为1〜4; R4是 - (CH2)m-Het; Het是吗啉,哌啶,哌嗪,哌嗪-N(C 1 -C 3烷基),咪唑,吡咯烷,氮杂环庚烷,3,4-二氢-2H-吡啶或3,6-二氢-2H-吡啶,各自任选被烷基 ,卤素,OH,NH 2,NH(C 1 -C 3烷基)或N(C 1 -C 3烷基)2; m为1-3; X为O,S或NH; 或其药学上可接受的盐,以及制备它们的方法和中间体化合物,有用的药物组合物和使用该化合物治疗增殖性疾病的方法。
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公开(公告)号:US07772243B2
公开(公告)日:2010-08-10
申请号:US11122345
申请日:2005-05-05
申请人: Stephen Alan Fakhoury , Helen Tsenwhei Lee , Jessica Elizabeth Reed , Kevin Matthew Schlosser , Karen Elaine Sexton , Haile Tecle , Roy Thomas Winters
发明人: Stephen Alan Fakhoury , Helen Tsenwhei Lee , Jessica Elizabeth Reed , Kevin Matthew Schlosser , Karen Elaine Sexton , Haile Tecle , Roy Thomas Winters
IPC分类号: A61K31/517 , C07D239/94 , C07D413/12
CPC分类号: C07D239/94 , C07D401/12 , C07D403/12
摘要: This invention provides quinazoline compounds of the formula: wherein: R1 is halo; R2 is H or halo; R3 is a) C1-C3 alkyl, optionally substituted by halo; or b) —(CH2)n-morpholino, —(CH2)n-piperidine, —(CH2)n-piperazine, —(CH2)n—-piperazine-N(C1-C3 alkyl), —(CH2)n-pyrrolidine, or —(CH2)n-imidazole; n is 1 to 4; R4 is —(CH2)m-Het; Het is morpholine, piperidine, piperazine, piperazine-N(C1-C3 alkyl), imidazole, pyrrolidine, azepane, 3,4-dihydro-2H-pyridine, or 3,6-dihydro-2H-pyridine, each optionally substituted by alkyl, halo, OH, NH2, NH(C1-C3 alkyl) or N (C1-C3 alkyl)2; m is 1-3; and X is O, S or NH; or a pharmaceutically acceptable salt thereof, as well as processes and intermediate compounds for making them, useful pharmaceutical compositions and methods of using the compounds in the treatment of proliferative diseases.
摘要翻译: 本发明提供下式的喹唑啉化合物:其中:R1是卤素; R2是H或卤素; R3是a)任选被卤素取代的C 1 -C 3烷基; 或(b) - (CH 2)n - 吗啉代, - (CH 2)n - 哌啶, - (CH 2)n - 哌嗪, - (CH 2)n - 哌嗪-N(C 1 -C 3烷基) 吡咯烷或 - (CH 2)n - 咪唑; n为1〜4; R4是 - (CH2)m-Het; Het是吗啉,哌啶,哌嗪,哌嗪-N(C 1 -C 3烷基),咪唑,吡咯烷,氮杂环庚烷,3,4-二氢-2H-吡啶或3,6-二氢-2H-吡啶,各自任选被烷基 ,卤素,OH,NH 2,NH(C 1 -C 3烷基)或N(C 1 -C 3烷基)2; m为1-3; X为O,S或NH; 或其药学上可接受的盐,以及制备它们的方法和中间体化合物,有用的药物组合物和使用该化合物治疗增殖性疾病的方法。
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公开(公告)号:US20100190977A1
公开(公告)日:2010-07-29
申请号:US12754556
申请日:2010-04-05
申请人: Stephen Alan Fakhoury , Helen Tsenwhei Lee , Jessica Elizabeth Reed , Kevin Matthew Schlosser , Karen Elaine Sexton , Haile Tecle , Roy Thomas Winters
发明人: Stephen Alan Fakhoury , Helen Tsenwhei Lee , Jessica Elizabeth Reed , Kevin Matthew Schlosser , Karen Elaine Sexton , Haile Tecle , Roy Thomas Winters
IPC分类号: C07D403/12 , C07D401/12 , C07D413/14
CPC分类号: C07D239/94 , C07D401/12 , C07D403/12
摘要: This invention provides quinazoline compounds of the formula: wherein: R1 is halo; R2 is H or halo; R3 is a) C1-C3 alkyl, optionally substituted by halo; or b) —(CH2)n-morpholino, —(CH2)n-piperidine, —(CH2)n-piperazine, —(CH2)n-piperazine-N(C1-C3 alkyl), —(CH2)n-pyrrolidine, or —(CH2)n-imidazole; n is 1 to 4; R4 is —(CH2)m-Het; Het is morpholine, piperidine, piperazine, piperazine-N(C1-C3 alkyl), imidazole, pyrrolidine, azepane, 3,4-dihydro-2H-pyridine, or 3,6-dihydro-2H-pyridine, each optionally substituted by alkyl, halo, OH, NH2, NH(C1-C3 alkyl) or N(C1-C3 alkyl)2; m is 1-3; and X is O, S or NH; or a pharmaceutically acceptable salt thereof, as well as processes and intermediate compounds for making them, useful pharmaceutical compositions and methods of using the compounds in the treatment of proliferative diseases.
摘要翻译: 本发明提供下式的喹唑啉化合物:其中:R1是卤素; R2是H或卤素; R3是a)任选被卤素取代的C 1 -C 3烷基; 或(b) - (CH 2)n - 吗啉代, - (CH 2)n - 哌啶, - (CH 2)n - 哌嗪, - (CH 2)n - 哌嗪-N(C 1 -C 3烷基), - (CH 2) ,或 - (CH 2)n - 咪唑; n为1〜4; R4是 - (CH2)m-Het; Het是吗啉,哌啶,哌嗪,哌嗪-N(C 1 -C 3烷基),咪唑,吡咯烷,氮杂环庚烷,3,4-二氢-2H-吡啶或3,6-二氢-2H-吡啶,各自任选被烷基 ,卤素,OH,NH 2,NH(C 1 -C 3烷基)或N(C 1 -C 3烷基)2; m为1-3; X为O,S或NH; 或其药学上可接受的盐,以及制备它们的方法和中间体化合物,有用的药物组合物和使用该化合物治疗增殖性疾病的方法。
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公开(公告)号:US20090170886A1
公开(公告)日:2009-07-02
申请号:US11997983
申请日:2006-07-07
申请人: Mark Laurence Boys , Michelle Marie Bruendl , Victoria Leigh Downs , Stephen Alan Fakhoury , William Glen Harter , Lain-Yen Hu , Sandra Marie Jennings , Bruce Allen Lefker , Lorna Helen Mitchell , Raj Kumar Raheja , Yvonne Dorothy Smith
发明人: Mark Laurence Boys , Michelle Marie Bruendl , Victoria Leigh Downs , Stephen Alan Fakhoury , William Glen Harter , Lain-Yen Hu , Sandra Marie Jennings , Bruce Allen Lefker , Lorna Helen Mitchell , Raj Kumar Raheja , Yvonne Dorothy Smith
IPC分类号: A61K31/435 , C07C43/20 , C07D213/02 , A61P35/00 , A61K31/08
CPC分类号: C07C255/54 , C07C2601/02 , C07D213/30 , C07D213/64 , C07D213/65 , C07D309/12 , C07D319/20
摘要: The present invention is directed to a new class of benzonitriles and to their use as androgen receptor modulators. Other aspects of the invention are directed to the use of these compounds to decrease excess sebum secretions and to stimulate hair growth.
摘要翻译: 本发明涉及一类新的苯腈和它们作为雄激素受体调节剂的用途。 本发明的其它方面涉及这些化合物用于减少过量的皮脂分泌和刺激毛发生长的用途。
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公开(公告)号:US20090131397A1
公开(公告)日:2009-05-21
申请号:US12262565
申请日:2008-10-31
申请人: Simon Bailey , Stephen Douglas Barrett , Larry Don Bratton , Stephen Alan Fakhoury , Sandra Marie Jennings , Lorna Helen Mitchell , Raj Kumar Raheja , Veerabahu Shanmugasundaram
发明人: Simon Bailey , Stephen Douglas Barrett , Larry Don Bratton , Stephen Alan Fakhoury , Sandra Marie Jennings , Lorna Helen Mitchell , Raj Kumar Raheja , Veerabahu Shanmugasundaram
IPC分类号: A61K31/397 , C07D261/06 , A61K31/42 , C07D413/02 , A61K31/4439 , A61K31/496 , A61P17/00 , A61K31/5377 , C07D417/02 , A61K31/541 , C07D487/12 , A61K31/506
CPC分类号: C07D261/08 , C07D261/18 , C07D413/08 , C07D413/12 , C07D413/14 , C07D417/08 , C07D471/04
摘要: The present application is directed to a new class of isoxazoles and their use as estrogen modulators.
摘要翻译: 本申请涉及一类新的异恶唑及其作为雌激素调节剂的用途。
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