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公开(公告)号：US07772233B2
公开(公告)日：2010-08-10
申请号：US11788028
申请日：2007-04-18
申请人： Andreas Goutopoulos , Benny C. Askew, Jr. , Nhut Kiet Diep , Srinivasa Karra , Matthias Schwarz , Henry Yu
发明人： Andreas Goutopoulos , Benny C. Askew, Jr. , Nhut Kiet Diep , Srinivasa Karra , Matthias Schwarz , Henry Yu
IPC分类号： C07D237/12 , C07D413/04 , A61K31/50 , A61K31/5355 , A61P35/00 , A61P29/00 , C07D213/74 , C07D405/12 , C07D213/57
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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2.发明申请公开(公告)号：US20100256149A1
公开(公告)日：2010-10-07
申请号：US12815071
申请日：2010-06-14
申请人： Andreas Goutopoulos , Benny C. Askew, JR. , Nhut Kiet Diep , Srinivasa Karra , Matthias Schwarz , Henry Yu
发明人： Andreas Goutopoulos , Benny C. Askew, JR. , Nhut Kiet Diep , Srinivasa Karra , Matthias Schwarz , Henry Yu
IPC分类号： A61K31/5377 , C07D213/90 , A61K31/44 , A61K31/455 , C07D237/24 , A61K31/50 , C07D413/04 , C07D403/12 , A61K31/501 , A61P29/00 , A61P35/00
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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3.发明授权公开(公告)号：US08076486B2
公开(公告)日：2011-12-13
申请号：US11788032
申请日：2007-04-18
IPC分类号： C07D417/00 , C07D413/04 , C07D401/00
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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5.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：US07276531B2
公开(公告)日：2007-10-02
申请号：US10547676
申请日：2004-03-02
申请人： Gian Luca Araldi , Srinivasa Karra , Zhong Zhao , Nadia Brugger
发明人： Gian Luca Araldi , Srinivasa Karra , Zhong Zhao , Nadia Brugger
IPC分类号： A61K31/4015 , C07D405/06 , C07D401/06 , C07D409/06 , C07D207/08
CPC分类号： C07D207/267 , C07D401/06 , C07D405/06 , C07D409/06
摘要： A gamma-lactam diene of Formula I: which is particularly useful as a medicament for the treatment of various disorders such as asthma, hypertension, osteoporosis, sexual dysfunction and fertility disorders.
摘要翻译： 式I的γ-内酰胺二烯：其特别可用作治疗各种疾病如哮喘，高血压，骨质疏松症，性功能障碍和生育障碍的药物。
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公开(公告)号：US20060194865A1
公开(公告)日：2006-08-31
申请号：US10547676
申请日：2004-03-02
申请人： Gian Araldi , Srinivasa Karra , Zhong Zhao , Nadia Brugger
发明人： Gian Araldi , Srinivasa Karra , Zhong Zhao , Nadia Brugger
IPC分类号： A61K31/558 , C07D403/02 , C07D207/24
CPC分类号： C07D207/267 , C07D401/06 , C07D405/06 , C07D409/06
摘要： The present invention relates γ-lactam derivatives, in particular for use as medicaments, as well as pharmaceutical formulations containing such γ-lactam derivatives. Said γ-lactam derivatives are useful in the treatment and/or prevention of asthma, hypertension, osteoporosis, sexual dysfunction and fertility disorders.
摘要翻译： 本发明涉及特别用作药物的γ-内酰胺衍生物，以及含有γ-内酰胺衍生物的药物制剂。 所述γ-内酰胺衍生物可用于治疗和/或预防哮喘，高血压，骨质疏松症，性功能障碍和生育障碍。
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公开(公告)号：US06458816B1
公开(公告)日：2002-10-01
申请号：US09977659
申请日：2001-10-15
申请人： Terrence W. Doyle , Srinivasa Karra , Zujin Li , Xu Lin , John Mao , Qi Qiao , Yang Xu
发明人： Terrence W. Doyle , Srinivasa Karra , Zujin Li , Xu Lin , John Mao , Qi Qiao , Yang Xu
IPC分类号： C07D21302
CPC分类号： C07D213/75 , A61K31/407 , A61K31/44 , A61K31/47 , A61K31/675 , A61K31/70 , A61K31/704 , A61K31/7068 , A61K33/24 , A61K45/06 , A61K47/52 , C07F9/58 , A61K31/195 , A61K2300/00
摘要： The present invention relates to compounds according to the structure: Where R is H or CH3; R2 is phosphate which can be free acid or salt; R3 is H, F, Cl, Br, I, OCH3, OCF3 , CF3 or a C1-C3 alkyl group; R4 is H, F, Cl, Br, I, OCH3, OCF3 or CF3; and R5 and R6 are each independently H, F, Cl, Br, I, OCH3, OCF3 or CF3, with the proviso that when any two of R3, R4, R5 or R6 are other than H, the other two of R3, R4, R5 or R6 are H which may be used to treat neoplasia, including cancer.
摘要翻译： 本发明涉及以下结构的化合物：其中R是H或CH 3; R 2是可以是游离酸或盐的磷酸酯; R 3是H，F，Cl，Br，I，OCH 3，OCF 3，CF 3或C 1 -C 3 烷基; R 4是H，F，Cl，Br，I，OCH 3，OCF 3或CF 3; R 5和R 6各自独立地为H，F，Cl，Br，I，OCH 3，OCF 3或CF 3，条件是当R 3，R 4，R 5或R 6中的任何两个不同于H时， R5或R6是H，其可以用于治疗包括癌症在内的肿瘤。
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