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21.发明申请Novel heteroaryl-substituted arylaminopyridine derivatives as MEK inhibitors 有权新的杂芳基取代的芳基氨基吡啶衍生物作为MEK抑制剂公开(公告)号：US20070287737A1
公开(公告)日：2007-12-13
申请号：US11788032
申请日：2007-04-18
申请人： Andreas Goutopoulos , Benny Askew , Xiaoling Chen , Srinivasa Karra , Yufang Xiao , Henry Yu
发明人： Andreas Goutopoulos , Benny Askew , Xiaoling Chen , Srinivasa Karra , Yufang Xiao , Henry Yu
IPC分类号： A61K31/44 , A61P35/00 , C07D401/00 , C07D417/00
CPC分类号： C07D213/79 , C07D213/81 , C07D403/04 , C07D413/04 , C07D413/14 , C07D417/04
摘要： The invention provides novel heteroaryl-substituted arylaminopyridine derivative MEK inhibitors of Formula (Ia) Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation. Also disclosed is the treatment of a hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds.
摘要翻译： 本发明提供式（Ia）的新型杂芳基取代的芳基氨基吡啶衍生物MEK抑制剂。这些化合物是可用于治疗过度增殖性疾病如癌症和炎症的MEK抑制剂。 还公开了哺乳动物中过度增殖性疾病的治疗，以及含有这些化合物的药物组合物。
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公开(公告)号：US20070287709A1
公开(公告)日：2007-12-13
申请号：US11788028
申请日：2007-04-18
申请人： Andreas Goutopoulos , Benny Askew , Nhut Diep , Srinivasa Karra , Matthias Schwarz , Henry Yu
发明人： Andreas Goutopoulos , Benny Askew , Nhut Diep , Srinivasa Karra , Matthias Schwarz , Henry Yu
IPC分类号： A61K31/44 , A61K31/50 , A61K31/535 , A61P43/00 , C07D211/70 , C07D211/72 , C07D237/02 , C07D401/00
CPC分类号： C07D213/84 , C07D213/79 , C07D213/80 , C07D213/81 , C07D213/82 , C07D237/24 , C07D405/12
摘要： The invention provides novel arylamino N-heteroaryl MEK inhibitors of Formula (I): Such compounds are MEK inhibitors that are useful in the treatment of hyperproliferative diseases, such as cancer and inflammation. Also disclosed is the treatment of a hyperproliferative disease in mammals, and pharmaceutical compositions containing such compounds.
摘要翻译： 本发明提供式（I）的新的芳基氨基N-杂芳基MEK抑制剂：这些化合物是可用于治疗过度增殖性疾病如癌症和炎症的MEK抑制剂。 还公开了哺乳动物中过度增殖性疾病的治疗，以及含有这些化合物的药物组合物。
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公开(公告)号：US09283225B2
公开(公告)日：2016-03-15
申请号：US14234356
申请日：2012-06-15
申请人： Wolfgang Staehle , Oliver Schadt , Christine Knuehl , Manja Friese-Hamim , Bayard R. Huck , Andreas Goutopoulos , Nadia Brugger
发明人： Wolfgang Staehle , Oliver Schadt , Christine Knuehl , Manja Friese-Hamim , Bayard R. Huck , Andreas Goutopoulos , Nadia Brugger
IPC分类号： C07D487/04 , A61K31/519 , A61K45/06 , C07D471/04 , A61P35/00 , A61P37/00 , A61P9/10 , A61P25/28 , A61P27/06
CPC分类号： A61K31/519 , A61K45/06 , C07D471/04
摘要： Compounds of the formula I in which Het, R3 and R4 have the meanings indicated in Claim 1, are inhibitors of RON and can be employed, for the treatment of cancer.
摘要翻译： 其中Het，R3和R4具有权利要求1所示含义的式I化合物是RON的抑制剂，可用于治疗癌症。
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公开(公告)号：US08946247B2
公开(公告)日：2015-02-03
申请号：US13989199
申请日：2011-11-11
申请人： Bayard R. Huck , Reinaldo Jones , Yufang Xiao , Constantin Neagu , Donald Bankston , Andreas Goutopoulos
发明人： Bayard R. Huck , Reinaldo Jones , Yufang Xiao , Constantin Neagu , Donald Bankston , Andreas Goutopoulos
IPC分类号： A61K31/517 , C07D239/72
CPC分类号： C07D403/12 , A61K31/517 , A61K45/06
摘要： The invention provides novel quinazoline carboxamide azetidine compounds according to Formula (I) and use for the treatment of hyperproliferative diseases, such as cancer.
摘要翻译： 本发明提供了根据式（I）的新型喹唑啉羧酰胺氮杂环丁烷化合物和用于治疗过度增殖性疾病如癌症的用途。
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公开(公告)号：US20140228379A1
公开(公告)日：2014-08-14
申请号：US14234356
申请日：2012-06-15
申请人： Wolfgang Stahle , Oliver Schadt , Christine Knuehl , Manja Friese-Hamim , Bayard Huck , Andreas Goutopoulos , Nadia Brugger
发明人： Wolfgang Stahle , Oliver Schadt , Christine Knuehl , Manja Friese-Hamim , Bayard Huck , Andreas Goutopoulos , Nadia Brugger
IPC分类号： A61K31/519 , A61K45/06 , C07D471/04
CPC分类号： A61K31/519 , A61K45/06 , C07D471/04
摘要： Compounds of the formula I in which Het, R3 and R4 have the meanings indicated in Claim 1, are inhibitors of RON and can be employed, for the treatment of cancer
摘要翻译： 其中Het，R3和R4具有权利要求1所示含义的式I化合物是RON的抑制剂，可用于治疗癌症
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公开(公告)号：US08946227B2
公开(公告)日：2015-02-03
申请号：US13754345
申请日：2013-01-30
IPC分类号： A61K31/4965 , C07D295/00 , C07D409/14 , A61K31/496 , C07D401/14 , C07D403/12 , C07D487/04 , C07D471/04
CPC分类号： C07D409/14 , A61K31/496 , C07D401/14 , C07D403/12 , C07D403/14 , C07D471/04 , C07D487/04
摘要： The invention provides 2-carboxamide piperazine compounds, and methods of treatment and pharmaceutical compositions that utilize or comprise one or more such compounds. Compounds of the invention are useful for the treatment of mammalian infertility.
摘要翻译： 本发明提供2-甲酰胺哌嗪化合物，以及使用或包含一种或多种这些化合物的治疗方法和药物组合物。 本发明的化合物可用于治疗哺乳动物不育症。
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公开(公告)号：US08198457B2
公开(公告)日：2012-06-12
申请号：US13112490
申请日：2011-05-20
申请人： Ulrich Abel , Holger Deppe , Achim Feurer , Ulrich Grädler , Kerstin Otte , Renate Sekul , Meinolf Thiemann , Andreas Goutopoulos , Matthias Schwarz , Xuliang Jiang
发明人： Ulrich Abel , Holger Deppe , Achim Feurer , Ulrich Grädler , Kerstin Otte , Renate Sekul , Meinolf Thiemann , Andreas Goutopoulos , Matthias Schwarz , Xuliang Jiang
IPC分类号： C07D213/72 , C07D211/70 , A01N43/58
CPC分类号： C07D405/12 , C07D213/79 , C07D213/81 , C07D213/89 , C07D295/125 , C07D295/13 , C07D295/32 , C07D401/12
摘要： The invention provides novel, substituted 3-arylamino pyridine compounds pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
摘要翻译： 本发明提供新的取代的3-芳基氨基吡啶化合物其药学上可接受的盐，溶剂合物和前药化合物，其中W，R 1，R 2，R 9，R 10，R 11，R 12，R 13，R 14如说明书中所定义。 这些化合物是MEK抑制剂，可用于治疗过度增殖性疾病，如癌症，再狭窄和炎症。 还公开了这样的化合物在哺乳动物，特别是人类中过度增殖性疾病的治疗和含有这些化合物的药物组合物中的应用。
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公开(公告)号：US07589220B2
公开(公告)日：2009-09-15
申请号：US10899191
申请日：2004-07-26
IPC分类号： C07C233/00
CPC分类号： C07C271/24 , A61K31/16 , A61K31/166 , A61K31/557 , C07B59/001 , C07C233/05 , C07C233/27 , C07C235/46 , C07C271/12 , C07C271/16 , C07C2601/02 , C07C2601/04 , C07C2601/14 , C07D213/75 , C07D277/18 , C07D277/46 , C07D277/82 , C07D285/08
摘要： Disclosed are compounds that are anandamide transport inhibitors and their pharmacological use.
摘要翻译： 公开了作为酰胺转运抑制剂及其药理学用途的化合物。
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公开(公告)号：US07161016B1
公开(公告)日：2007-01-09
申请号：US09600786
申请日：1999-11-24
IPC分类号： C07C231/00
CPC分类号： C07C233/13 , C07C233/09 , C07C235/06 , C07C247/04
摘要： Novel analogs of arachidonylethanolamide are presented which have higher affinities for the cannabinoid CB1 and/or CB2 receptor sites. Further, most of the analogs exhibit greater metabolic stability than arachidonylethanolamide. The improved receptor affinity and selectivity and/or greater metabolic stability make these analogs therapeutically useful as medications for relief of pain caused by cancer and nausea caused by chemotherapy, as well as for peripheral pain. The compounds may also be useful as oral and topical contraceptives, in suppression of the immune system, enhancement of appetite and in treatment of psychomotor disorders, multiple sclerosis and hypertension.
摘要翻译： 提出了对大麻素CB1和/或CB2受体位点具有较高亲和力的花生四烯乙醇酰胺的新型类似物。 此外，大多数类似物表现出比花生四烯酰乙酰胺更高的代谢稳定性。 改善的受体亲和力和选择性和/或更高的代谢稳定性使得这些类似物在治疗上作为缓解由化疗引起的癌症和恶心以及周围性疼痛引起的疼痛的药物治疗有用。 所述化合物还可用作口服和局部避孕药，抑制免疫系统，增强食欲和治疗精神运动障碍，多发性硬化和高血压。
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公开(公告)号：US07956191B2
公开(公告)日：2011-06-07
申请号：US11665651
申请日：2005-10-19
申请人： Ulrich Abel , Holger Deppe , Achim Feurer , Ulrich Grädler , Kerstin Otte , Renate Sekul , Meinolf Thiemann , Andreas Goutopoulos , Matthias Schwarz , Xuliang Jiang
发明人： Ulrich Abel , Holger Deppe , Achim Feurer , Ulrich Grädler , Kerstin Otte , Renate Sekul , Meinolf Thiemann , Andreas Goutopoulos , Matthias Schwarz , Xuliang Jiang
IPC分类号： C07D213/72 , C07D213/46
CPC分类号： C07D405/12 , C07D213/79 , C07D213/81 , C07D213/89 , C07D295/125 , C07D295/13 , C07D295/32 , C07D401/12
摘要： The invention provides novel, substituted 3-arylamino pyridine compounds (I) pharmaceutically acceptable salts, solvates and prodrug compounds thereof, wherein W, R1, R2, R9, R10, R11, R12, R13, R14 are as defined in the specification. Such compounds are MEK inhibitors and useful in the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation. Also disclosed is the use of such compounds in the treatment of hyperproliferative diseases in mammals, especially humans, and pharmaceutical compositions containing such compounds.
摘要翻译： 本发明提供新的取代的3-芳基氨基吡啶化合物（I）其药学上可接受的盐，溶剂合物和前药化合物，其中W，R 1，R 2，R 9，R 10，R 11，R 12，R 13，R 14如说明书中所定义。 这些化合物是MEK抑制剂，可用于治疗过度增殖性疾病，如癌症，再狭窄和炎症。 还公开了这样的化合物在哺乳动物，特别是人类中过度增殖性疾病的治疗和含有这些化合物的药物组合物中的应用。
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