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公开(公告)号：US09879001B2
公开(公告)日：2018-01-30
申请号：US14775134
申请日：2014-03-10
申请人： Merck Patent GmbH
IPC分类号： C07D417/06 , C07D413/06 , C07D417/14 , C07D277/46 , G01N33/68 , A61K31/426 , A61K31/427 , A61K31/454 , A61K31/496 , A61K31/498
CPC分类号： C07D417/06 , A61K31/426 , A61K31/427 , A61K31/454 , A61K31/496 , A61K31/498 , C07D277/46 , C07D413/06 , C07D417/14 , G01N33/6893
摘要： Compounds of formula (I) wherein X1, X2, W, R1 to R5, L and m have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.
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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：US08710044B2
公开(公告)日：2014-04-29
申请号：US13703276
申请日：2011-07-01
申请人： Bayard R. Huck , Constantin Neagu , Reinaldo Jones , Lizbeth Celeste DeSelm , Yufang Xiao , Srinivasa R. Karra , Ruoxi Lan , Igor Mochalkin , Amanda E. Sutton , Thomas E. Richardson
发明人： Bayard R. Huck , Constantin Neagu , Reinaldo Jones , Lizbeth Celeste DeSelm , Yufang Xiao , Srinivasa R. Karra , Ruoxi Lan , Igor Mochalkin , Amanda E. Sutton , Thomas E. Richardson
IPC分类号： A61K31/00 , A61K31/519 , C07D239/72
CPC分类号： C07D239/94 , A61K31/517 , A61K45/06 , C07D239/74 , C07D403/12
摘要： The invention provides novel bicyclic azaheterocyclic carboxamide compounds according to Formula (I), their manufacture 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）的新型双环氮杂杂环甲酰胺化合物，其用于治疗过度增殖性疾病如癌症的制备和用途。
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公开(公告)号：US08637532B2
公开(公告)日：2014-01-28
申请号：US13148903
申请日：2010-02-04
申请人： Amanda E. Sutton , Ruoxi Lan , Thomas E. Richardson , David Perrey , Harold George Vandeveer , Bayard R. Huck , Srinivasa R. Karra , Xiaoling Chen , Yufang Xiao , Lesley Liu-Bujalski , Andreas Goutopoulos , Frank Stieber , Brian L. Hodous , Hui Qiu , Reinaldo Jones , Brian H. Heasley
发明人： Amanda E. Sutton , Ruoxi Lan , Thomas E. Richardson , David Perrey , Harold George Vandeveer , Bayard R. Huck , Srinivasa R. Karra , Xiaoling Chen , Yufang Xiao , Lesley Liu-Bujalski , Andreas Goutopoulos , Frank Stieber , Brian L. Hodous , Hui Qiu , Reinaldo Jones , Brian H. Heasley
IPC分类号： A01N43/54 , A61K31/517 , C07D239/72 , C07D401/00
CPC分类号： C07D215/04 , A61K31/47 , C07D239/94 , C07D401/04 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/04 , C07D409/12 , C07D413/04
摘要： The invention provides novel substituted amino azaheterocyclic carboxamide compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
摘要翻译： 本发明提供根据式（I）的新型取代的氨基氮杂环甲酰胺化合物，其用于治疗过度增殖性疾病如癌症的制备和用途。
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公开(公告)号：US10301299B2
公开(公告)日：2019-05-28
申请号：US15830675
申请日：2017-12-04
申请人： Merck Patent GmbH
IPC分类号： C07D417/06 , C07D413/06 , C07D417/14 , C07D277/46 , G01N33/68 , A61K31/426 , A61K31/427 , A61K31/454 , A61K31/496 , A61K31/498
摘要： Compounds of formula (I) wherein X1, X2, W, R1 to R5, L and m have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.
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公开(公告)号：US09469657B2
公开(公告)日：2016-10-18
申请号：US14502213
申请日：2014-09-30
申请人： Merck Patent GmbH
IPC分类号： A61K31/429 , C07D513/04 , A61K31/4439 , A61K31/454
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.
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公开(公告)号：US08236963B2
公开(公告)日：2012-08-07
申请号：US11919471
申请日：2006-05-23
申请人： Matthias Schwarz , Eric Sebille , Christophe Cleva , Cedric Merlot , Dennis Church , Patrick Page , Jacqueline A. Macritchie , John Frederick Atherall , Stefano Crosignani , Doris Pupowicz
发明人： Matthias Schwarz , Eric Sebille , Christophe Cleva , Cedric Merlot , Dennis Church , Patrick Page , Jacqueline A. Macritchie , John Frederick Atherall , Stefano Crosignani , Doris Pupowicz
IPC分类号： C07D277/20 , C07D271/06 , C07D417/14 , C07D487/10 , C07D261/06 , A61K31/44 , A61K31/431 , A61K31/4184 , A61K31/4196 , A61K31/41
CPC分类号： C07D487/10
摘要： The present invention is related to the use of spiro derivatives of Formula (I) for the treatment and/or prevention of allergic diseases, inflammatory dermatoses and other diseases with an inflammatory component. Specifically, the present invention is related to the use of spiro derivatives for the modulation of CRTH2 activity.
摘要翻译： 本发明涉及式（I）的螺衍生物用于治疗和/或预防具有炎性成分的过敏性疾病，炎性皮肤病和其它疾病的用途。 具体地说，本发明涉及螺衍生物用于调节CRTH2活性的用途。
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8.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：US09273029B2
公开(公告)日：2016-03-01
申请号：US14118845
申请日：2012-04-11
IPC分类号： C07D401/12 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D471/04 , C07D491/048 , C07D409/04
CPC分类号： C07D401/12 , A61K31/444 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D471/04 , C07D491/048
摘要： Compounds of the formula (I) in which R, R1 and X have the meanings indicated in claim 1, are inhibitors of TBK1 and IKKε and can be employed, inter alia, for the treatment of cancer and inflammatory diseases
摘要翻译： 其中R，R 1和X具有权利要求1所示含义的式（I）化合物是TBK1和IKK的抑制剂; 并且可以用于治疗癌症和炎性疾病
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![Hetaryl-[1,8]naphthyridine derivatives](/abs-image/US/2013/12/24/US08614226B2/abs.jpg.150x150.jpg)
公开(公告)号：US08614226B2
公开(公告)日：2013-12-24
申请号：US13574282
申请日：2010-12-17
IPC分类号： A01N43/42 , A61K31/44 , C07D471/02
CPC分类号： C07D471/04 , A61K31/4375 , C07D401/14 , C07D413/14 , C07D519/00
摘要： Novel hetaryl-[1,8]naphthyridine derivatives of formula (I) wherein R1, R2, W1, W3, W5 and W6 have the meaning according to claim 1, are inhibitors of ATP consuming proteins, and can be employed, inter alia, for the treatment of tumors.
摘要翻译： 其中R 1，R 2，W 1，W 3，W 5和W 6具有权利要求1的含义的式（I）的新型杂芳基 - [1,8]二氮杂萘衍生物是ATP消耗蛋白质的抑制剂， 用于治疗肿瘤。
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