公开(公告)号：US09586938B2

公开(公告)日：2017-03-07

申请号：US13810860

申请日：2011-07-28

Applicant: Bayard R. Huck ,  Xiaoling Chen ,  Constantin Neagu ,  Reinaldo Jones ,  Yufang Xiao ,  Igor Mochalkin

Inventor： Bayard R. Huck ,  Xiaoling Chen ,  Constantin Neagu ,  Reinaldo Jones ,  Yufang Xiao ,  Igor Mochalkin

IPC: A01N43/54 ,  C07D239/42 ,  C07D401/04 ,  A01N43/42 ,  A61K31/47 ,  C07D403/12 ,  C07D233/90 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D405/12 ,  C07D405/14 ,  A61K31/4709 ,  A61K31/517 ,  A61K45/06 ,  C07D403/14

CPC classification number: C07D403/12 ,  A61K31/4709 ,  A61K31/517 ,  A61K45/06 ,  C07D233/90 ,  C07D401/04 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14

Abstract: The invention provides novel cyclic amine azaheterocyclic carboxamide according to Formula (I), Formula (II) and Formula (III) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.

Abstract translation: 本发明提供了式（I），式（II）和式（III）的新型环胺氮杂环甲酰胺，其用于治疗过度增殖性疾病如癌症的制备和用途。

公开(公告)号：US09321760B2

公开(公告)日：2016-04-26

申请号：US14236405

申请日：2012-09-12

Applicant: Ruoxi Lan ,  Bayard R. Huck ,  Xiaoling Chen ,  Lizbeth Celeste Deselm ,  Hui Qiu ,  Yufang Xiao ,  Constantin Neagu ,  Igor Mochalkin ,  Theresa L. Johnson

Inventor： Ruoxi Lan ,  Bayard R. Huck ,  Xiaoling Chen ,  Lizbeth Celeste Deselm ,  Hui Qiu ,  Yufang Xiao ,  Constantin Neagu ,  Igor Mochalkin ,  Theresa L. Johnson

IPC: A61K31/506 ,  C07D417/12 ,  C07D403/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/06 ,  C07D239/48 ,  C07D413/04 ,  C07D417/14 ,  C07D405/12

CPC classification number: A61K31/506 ,  C07D239/48 ,  C07D239/49 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/06 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D413/04 ,  C07D413/06 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14

Abstract: The invention provides novel heterocyclic amine compounds according to Formula (I) and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.

Abstract translation: 本发明提供了式（I）的新型杂环胺化合物及其制备和用于治疗过度增殖性疾病如癌症的用途。

公开(公告)号：US20150274750A1

公开(公告)日：2015-10-01

申请号：US14432316

申请日：2013-11-15

Applicant: Ruoxi LAN ,  Bayard R. HUCK ,  Xiaoling CHEN ,  Yufang XIAO ,  MERCK PATENT GMBH

Inventor： Ruoxi Lan ,  Bayard R. Huck ,  Xiaoling Chen ,  Yufang Xiao

IPC: C07D498/04 ,  A61K31/496 ,  C07D487/04 ,  A61N5/10 ,  C07D239/70 ,  A61K31/517 ,  A61K31/5383 ,  A61K45/06 ,  C07D471/04 ,  A61K31/519

CPC classification number: C07D498/04 ,  A61K31/496 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5383 ,  A61K45/06 ,  A61N5/10 ,  A61N2005/1098 ,  C07D239/70 ,  C07D471/04 ,  C07D475/06 ,  C07D487/04

Abstract: The invention provides novel imidazol-piperidinyl derivatives of the formula (I) in which R1, R2, W, X1, X2, X3, X4 and n have the meanings indicated in formula I, and their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.

Abstract translation: 本发明提供式（I）的新型咪唑 - 哌啶基衍生物，其中R1，R2，W，X1，X2，X3，X4和n具有式I所示的含义及其制备和用于治疗过度增殖性疾病 ，如癌症。

公开(公告)号：US08569295B2

公开(公告)日：2013-10-29

申请号：US13388952

申请日：2010-07-28

Applicant: Xiaoling Chen ,  Srinivasa R. Karra ,  Bayard R. Huck ,  Ruoxi Lan ,  Amanda E. Sutton ,  Andreas Goutopoulos ,  Brian L. Hodous ,  Reinaldo Jones

Inventor： Xiaoling Chen ,  Srinivasa R. Karra ,  Bayard R. Huck ,  Ruoxi Lan ,  Amanda E. Sutton ,  Andreas Goutopoulos ,  Brian L. Hodous ,  Reinaldo Jones

IPC: C07D471/04 ,  C07D498/14 ,  A61K31/519

CPC classification number: C07D471/04 ,  C07D498/14

Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.

Abstract translation: 本发明提供根据式（I）的新型取代的氮杂环化合物，其用于治疗过度增殖性疾病如癌症的制备和用途。

公开(公告)号：US20120190654A1

公开(公告)日：2012-07-26

申请号：US13388952

申请日：2010-07-28

Applicant: Xiaoling Chen ,  Srinivasa R. Karra ,  Bayard R. Huck ,  Ruoxi Lan ,  Amanda E. Sutton ,  Andreas Goutopoulos ,  Brian L. Hodous ,  Reinaldo Jones

Inventor： Xiaoling Chen ,  Srinivasa R. Karra ,  Bayard R. Huck ,  Ruoxi Lan ,  Amanda E. Sutton ,  Andreas Goutopoulos ,  Brian L. Hodous ,  Reinaldo Jones

IPC: A61K31/519 ,  C07D498/14 ,  A61K31/5365 ,  C07D471/14 ,  A61K31/5377 ,  A61K31/635 ,  A61P35/00 ,  A61P29/00 ,  A61P1/18 ,  A61P13/12 ,  A61P13/08 ,  A61P9/00 ,  A61P17/06 ,  A61P17/04 ,  A61P17/00 ,  A61P3/10 ,  A61P27/02 ,  C07D519/00 ,  C07D471/04

CPC classification number: C07D471/04 ,  C07D498/14

Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.

Abstract translation: 本发明提供根据式（I）的新型取代的氮杂环化合物，其用于治疗过度增殖性疾病如癌症的制备和用途。

公开(公告)号：US20120046269A1

公开(公告)日：2012-02-23

申请号：US13148903

申请日：2010-02-04

Applicant: Amanda E. Sutton ,  Ruoxi Lan ,  Thomas E. Richardson ,  David Perrey ,  Harold George Vandeveer ,  Bayard R. Huck ,  Srinivasa R. Karra ,  Xiaoling Chen ,  Lesley Liu-Bujalski ,  Andreas Goutopoulos ,  Frank Steiber ,  Brian L. Hodous ,  Hui Qiu ,  Reinaldo C. Jones ,  Brian H. Heasley

Inventor： Amanda E. Sutton ,  Ruoxi Lan ,  Thomas E. Richardson ,  David Perrey ,  Harold George Vandeveer ,  Bayard R. Huck ,  Srinivasa R. Karra ,  Xiaoling Chen ,  Lesley Liu-Bujalski ,  Andreas Goutopoulos ,  Frank Steiber ,  Brian L. Hodous ,  Hui Qiu ,  Reinaldo C. Jones ,  Brian H. Heasley

IPC: A61K31/517 ,  C07D401/12 ,  A61K31/4709 ,  C07D405/12 ,  C07D409/12 ,  C07D403/12 ,  C07D401/04 ,  C07D413/12 ,  A61K31/5377 ,  C07D413/04 ,  C07D401/14 ,  C07D417/12 ,  C07D413/14 ,  C07D409/10 ,  C07D471/04 ,  A61P35/00 ,  A61P29/00 ,  A61P1/18 ,  A61P13/12 ,  A61P17/00 ,  A61P9/00 ,  A61P17/06 ,  A61P3/10 ,  A61P27/02 ,  C07D239/94

CPC classification number: C07D215/04 ,  A61K31/47 ,  C07D239/94 ,  C07D401/04 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D413/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20070287737A1

公开(公告)日：2007-12-13

申请号：US11788032

申请日：2007-04-18

Applicant: Andreas Goutopoulos ,  Benny Askew ,  Xiaoling Chen ,  Srinivasa Karra ,  Yufang Xiao ,  Henry Yu

Inventor： Andreas Goutopoulos ,  Benny Askew ,  Xiaoling Chen ,  Srinivasa Karra ,  Yufang Xiao ,  Henry Yu

IPC: A61K31/44 ,  A61P35/00 ,  C07D401/00 ,  C07D417/00

CPC classification number: C07D213/79 ,  C07D213/81 ,  C07D403/04 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04

Abstract: 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.

Abstract translation: 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。