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公开(公告)号：US08889719B2
公开(公告)日：2014-11-18
申请号：US13785120
申请日：2013-03-05
IPC分类号： A61K31/455 , C07D213/46 , C07D213/82 , C07D213/79 , C07D213/81
CPC分类号： C07D213/82 , C07D213/79 , C07D213/81
摘要： The invention provides novel compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation.
摘要翻译： 本发明提供根据式（I）的新化合物，其用于治疗过度增生性疾病如癌症，再狭窄和炎症的制备和用途。
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公开(公告)号：US08404725B2
公开(公告)日：2013-03-26
申请号：US13057052
申请日：2009-07-27
IPC分类号： A61K31/455 , C07D213/46
CPC分类号： C07D213/82 , C07D213/79 , C07D213/81
摘要： The invention provides novel substituted phenylamino isonicotinamide compounds (I), pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein X, R1, R2, R3, R4, R5 and R6 are as defined in the specification. Said compounds are MEK inhibitors useful in the treatment of hyperproliferative diseases related to the hyperactivity of MEK, such as restenosis, as well as diseases modulated by the MEK cascade, such as cancer 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苯基氨基异烟酰胺化合物（I），其药学上可接受的盐，溶剂合物或前药，其中X，R 1，R 2，R 3，R 4，R 5和R 6如说明书中所定义。 所述化合物是可用于治疗与MEK的多动症相关的过度增生性疾病的MEK抑制剂，例如再狭窄，以及由MEK级联调节的疾病，例如癌症和炎症。 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：US20110184032A1
公开(公告)日：2011-07-28
申请号：US13057052
申请日：2009-07-27
IPC分类号： A61K31/44 , C07D213/74 , A61P35/00 , A61P29/00 , A61P1/18 , A61P13/12 , A61P9/00 , A61P17/06 , A61P17/00 , A61P3/10 , A61P27/02 , A61P35/02
CPC分类号： C07D213/82 , C07D213/79 , C07D213/81
摘要： The invention provides novel compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer, restenosis and inflammation.
摘要翻译： 本发明提供根据式（I）的新化合物，其用于治疗过度增生性疾病如癌症，再狭窄和炎症的制备和用途。
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公开(公告)号：US08815872B2
公开(公告)日：2014-08-26
申请号：US13062413
申请日：2009-09-03
申请人： Henry Yu , Lizbeth Celeste De Selm , Xuliang Jiang , Benny C. Askew, Jr. , Srinivasa R. Karra , Andreas Goutopoulos
发明人： Henry Yu , Lizbeth Celeste De Selm , Xuliang Jiang , Benny C. Askew, Jr. , Srinivasa R. Karra , Andreas Goutopoulos
IPC分类号： A61K31/529 , C07D239/42 , C07D487/08 , C07D487/18 , C07D498/08 , C07D498/18 , C07D513/08 , C07D513/18 , C07D515/08
CPC分类号： C07D498/08 , C07D487/08 , C07D487/18 , C07D498/18 , C07D513/08 , C07D513/18 , C07D515/08
摘要： Macrocyclic derivative compounds that inhibit protein kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed kinase activity such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.
摘要翻译： 公开了抑制蛋白激酶的大环衍生物化合物以及包含这些化合物的药物组合物及其合成方法。 这些化合物可用于治疗由不稳定和/或受干扰的激酶活性如癌症，牛皮癣，病毒和细菌感染，炎性和自身免疫性疾病引起的增殖性疾病。
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公开(公告)号：US08802703B2
公开(公告)日：2014-08-12
申请号：US12815071
申请日：2010-06-14
申请人： Andreas Goutopoulos , Benny C. Askew, Jr. , Nhut Kiet Diep , Srinivasa R. Karra , Matthias Schwarz , Henry Yu
发明人： Andreas Goutopoulos , Benny C. Askew, Jr. , Nhut Kiet Diep , Srinivasa R. Karra , Matthias Schwarz , Henry Yu
IPC分类号： A61K31/465 , A61K31/4412 , A61K31/44 , C07D213/81 , C07D213/80 , C07D213/82 , C07D405/12 , C07D213/84 , C07D237/24 , C07D213/79 , A61P35/00 , A61P29/00
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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6.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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7.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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![Pyrano [3,2-D][1,3]thiazole as glycosidase inhibitors](/abs-image/US/2014/11/11/US08884023B2/abs.jpg.150x150.jpg)
公开(公告)号：US08884023B2
公开(公告)日：2014-11-11
申请号：US14131471
申请日：2012-08-22
IPC分类号： C07D513/04 , A61K31/429 , A61K31/454 , A61K31/4439
CPC分类号： C07D513/04 , A61K31/429 , A61K31/4439 , A61K31/454
摘要： Novel compounds of formula (I) wherein R1 to R4 and X have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.
摘要翻译： 式（I）的新化合物，其中R 1至R 4和X具有权利要求所述的含义，其为葡糖苷酶抑制剂，并且可用于治疗阿尔茨海默氏病。
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![Pyrano[3,2-D][1,3]thiazole as glycosidase inhibitors](/abs-image/US/2014/08/28/US20140243370A1/abs.jpg.150x150.jpg)
公开(公告)号：US20140243370A1
公开(公告)日：2014-08-28
申请号：US14131471
申请日：2012-08-22
IPC分类号： A61K31/4439 , A61K31/429 , A61K31/454 , C07D513/04
CPC分类号： C07D513/04 , A61K31/429 , A61K31/4439 , A61K31/454
摘要： Novel compounds of formula (I) wherein R1 to R4 and X have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.
摘要翻译： 式（I）的新化合物，其中R 1至R 4和X具有权利要求所述的含义，其为葡糖苷酶抑制剂，并且可用于治疗阿尔茨海默氏病。
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10.发明申请公开(公告)号：US20110294801A1
公开(公告)日：2011-12-01
申请号：US13062413
申请日：2009-09-03
申请人： Henry Yu , Lizbeth Celeste De Selm , Xuliang Jiang , Benny C. Askew, Jr. , Srinivasa R. Karra , Andreas Goutopoulos
发明人： Henry Yu , Lizbeth Celeste De Selm , Xuliang Jiang , Benny C. Askew, Jr. , Srinivasa R. Karra , Andreas Goutopoulos
IPC分类号： A61K31/519 , C07D487/06 , C07D487/16 , A61P31/00 , A61K31/5377 , A61P35/00 , A61P37/00 , A61P29/00 , C07D498/06 , C07D498/16
CPC分类号： C07D498/08 , C07D487/08 , C07D487/18 , C07D498/18 , C07D513/08 , C07D513/18 , C07D515/08
摘要： Macrocyclic derivative compounds that inhibit protein kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed kinase activity such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.
摘要翻译： 公开了抑制蛋白激酶的大环衍生物化合物以及包含这些化合物的药物组合物及其合成方法。 这些化合物可用于治疗由不稳定和/或受干扰的激酶活性如癌症，牛皮癣，病毒和细菌感染，炎性和自身免疫性疾病引起的增殖性疾病。
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