公开(公告)号：US09283225B2

公开(公告)日：2016-03-15

申请号：US14234356

申请日：2012-06-15

Applicant: Wolfgang Staehle ,  Oliver Schadt ,  Christine Knuehl ,  Manja Friese-Hamim ,  Bayard R. Huck ,  Andreas Goutopoulos ,  Nadia Brugger

Inventor： Wolfgang Staehle ,  Oliver Schadt ,  Christine Knuehl ,  Manja Friese-Hamim ,  Bayard R. Huck ,  Andreas Goutopoulos ,  Nadia Brugger

IPC: C07D487/04 ,  A61K31/519 ,  A61K45/06 ,  C07D471/04 ,  A61P35/00 ,  A61P37/00 ,  A61P9/10 ,  A61P25/28 ,  A61P27/06

CPC classification number: A61K31/519 ,  A61K45/06 ,  C07D471/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US08946247B2

公开(公告)日：2015-02-03

申请号：US13989199

申请日：2011-11-11

Applicant: Bayard R. Huck ,  Reinaldo Jones ,  Yufang Xiao ,  Constantin Neagu ,  Donald Bankston ,  Andreas Goutopoulos

Inventor： Bayard R. Huck ,  Reinaldo Jones ,  Yufang Xiao ,  Constantin Neagu ,  Donald Bankston ,  Andreas Goutopoulos

IPC: A61K31/517 ,  C07D239/72

CPC classification number: C07D403/12 ,  A61K31/517 ,  A61K45/06

Abstract: The invention provides novel quinazoline carboxamide azetidine compounds according to Formula (I) and use for the treatment of hyperproliferative diseases, such as cancer.

Abstract translation: 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。

公开(公告)号：US20140228379A1

公开(公告)日：2014-08-14

申请号：US14234356

申请日：2012-06-15

Applicant: Wolfgang Stahle ,  Oliver Schadt ,  Christine Knuehl ,  Manja Friese-Hamim ,  Bayard Huck ,  Andreas Goutopoulos ,  Nadia Brugger

Inventor： Wolfgang Stahle ,  Oliver Schadt ,  Christine Knuehl ,  Manja Friese-Hamim ,  Bayard Huck ,  Andreas Goutopoulos ,  Nadia Brugger

IPC: A61K31/519 ,  A61K45/06 ,  C07D471/04

CPC classification number: A61K31/519 ,  A61K45/06 ,  C07D471/04

Abstract: 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

Abstract translation: 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

公开(公告)号：US20130184314A1

公开(公告)日：2013-07-18

申请号：US13785120

申请日：2013-03-05

Applicant: Andreas Goutopoulos ,  Henry YU ,  Benny C. Askew, JR. ,  Lesley Liu-Bujalski

Inventor： Andreas Goutopoulos ,  Henry YU ,  Benny C. Askew, JR. ,  Lesley Liu-Bujalski

IPC: C07D213/82

CPC classification number: C07D213/82 ,  C07D213/79 ,  C07D213/81

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20160016936A1

公开(公告)日：2016-01-21

申请号：US14775205

申请日：2014-03-10

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

Inventor： Ruoxi LAN ,  Xiaoling CHEN ,  Yufang XIAO ,  Bayard R. HUCK ,  Andreas GOUTOPOULOS

IPC: C07D401/14 ,  C07D487/04 ,  A61K31/519 ,  A61K31/506

CPC classification number: A61K31/519 ,  A61K31/506 ,  C07D401/14 ,  C07D487/04

Abstract: The invention provides novel heterocyclic amines 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）的新型杂环胺，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：US09073947B2

公开(公告)日：2015-07-07

申请号：US14112428

申请日：2012-06-10

Applicant: Brian L. Hodous ,  Lesley Liu-Bujalski ,  Reinaldo Jones ,  Donald Bankston ,  Theresa L. Johnson ,  Igor Mochalkin ,  Ngan Nguyen ,  Hui Qiu ,  Andreas Goutopoulos ,  Nadia Brugger

Inventor： Brian L. Hodous ,  Lesley Liu-Bujalski ,  Reinaldo Jones ,  Donald Bankston ,  Theresa L. Johnson ,  Igor Mochalkin ,  Ngan Nguyen ,  Hui Qiu ,  Andreas Goutopoulos ,  Nadia Brugger

IPC: A61K31/506 ,  C07D401/12 ,  C07F5/02 ,  C07D213/68 ,  C07D213/73 ,  C07D213/74 ,  C07D239/47 ,  C07D239/48 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07D413/14 ,  C07D495/04 ,  C07D405/14 ,  C07D451/02 ,  C07D471/10

CPC classification number: A61K31/69 ,  A61K31/44 ,  A61K31/4545 ,  A61K31/505 ,  A61K31/506 ,  A61K31/513 ,  A61K31/5377 ,  A61K31/55 ,  C07D213/68 ,  C07D213/73 ,  C07D213/74 ,  C07D239/47 ,  C07D239/48 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/12 ,  C07D413/14 ,  C07D451/02 ,  C07D471/10 ,  C07D495/04 ,  C07F5/022

Abstract: The present invention provides novel pyrimidine and pyridine compounds according to Formula (I), Formula (II), Formula (III), Formula (IV) and Formula (V) their manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren's disease and rheumatoid arthritis. In preferred embodiments, the present invention describes irreversible kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase.

Abstract translation: 本发明提供了式（I），式（II），式（III），式（IV）和式（V））的新型嘧啶和吡啶化合物用于治疗过度增殖性疾病的制造和用途，包括但不限于 癌症，狼疮，过敏性疾病，干燥病和类风湿性关节炎。 在优选的实施方案中，本发明描述不可逆激酶抑制剂，包括但不限于Bruton酪氨酸激酶的抑制剂。

公开(公告)号：US08889719B2

公开(公告)日：2014-11-18

申请号：US13785120

申请日：2013-03-05

Applicant: Andreas Goutopoulos ,  Henry Yu ,  Benny C. Askew, Jr. ,  Lesley Liu-Bujalski

Inventor： Andreas Goutopoulos ,  Henry Yu ,  Benny C. Askew, Jr. ,  Lesley Liu-Bujalski

IPC: A61K31/455 ,  C07D213/46 ,  C07D213/82 ,  C07D213/79 ,  C07D213/81

CPC classification number: C07D213/82 ,  C07D213/79 ,  C07D213/81

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US08637532B2

公开(公告)日：2014-01-28

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 ,  Yufang Xiao ,  Lesley Liu-Bujalski ,  Andreas Goutopoulos ,  Frank Stieber ,  Brian L. Hodous ,  Hui Qiu ,  Reinaldo 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 ,  Yufang Xiao ,  Lesley Liu-Bujalski ,  Andreas Goutopoulos ,  Frank Stieber ,  Brian L. Hodous ,  Hui Qiu ,  Reinaldo Jones ,  Brian H. Heasley

IPC: A01N43/54 ,  A61K31/517 ,  C07D239/72 ,  C07D401/00

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：US08404725B2

公开(公告)日：2013-03-26

申请号：US13057052

申请日：2009-07-27

Applicant: Andreas Goutopoulos ,  Henry Yu ,  Benny C. Askew, Jr. ,  Lesley Liu-Bujalski

Inventor： Andreas Goutopoulos ,  Henry Yu ,  Benny C. Askew, Jr. ,  Lesley Liu-Bujalski

IPC: A61K31/455 ,  C07D213/46

CPC classification number: C07D213/82 ,  C07D213/79 ,  C07D213/81

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20130023522A1

公开(公告)日：2013-01-24

申请号：US13551072

申请日：2012-07-17

Applicant: Henry YU ,  Jiezhen LI ,  Thomas E. RICHARDSON ,  Pandi BHARATHI ,  Brian H. HEASLEY ,  Andreas GOUTOPOULOS

Inventor： Henry YU ,  Jiezhen LI ,  Thomas E. RICHARDSON ,  Pandi BHARATHI ,  Brian H. HEASLEY ,  Andreas GOUTOPOULOS

IPC: A61K31/496 ,  C07D405/12 ,  C07D405/14 ,  C07D413/14 ,  C07D413/12 ,  C07D417/14 ,  A61K31/541 ,  C07D409/14 ,  C07D403/12 ,  C07D401/14 ,  C07D403/14 ,  A61K31/506 ,  A61K31/454 ,  A61K31/551 ,  C12N5/071 ,  A61P15/08

CPC classification number: C07D417/12 ,  A61K31/454 ,  A61K31/496 ,  A61K31/498 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  C07D233/64 ,  C07D263/34 ,  C07D307/68 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/10 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14

Abstract: Novel benzamide derivatives of formula (I) wherein W1, W2, R1 to R7, R8, X and Y have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.

Abstract translation: 其中W 1，W 2，R 1至R 7，R 8，X和Y具有根据权利要求的含义的式（I）的新型苯甲酰胺衍生物是FSH受体的正变构调节剂，并且可以用于治疗 的生育障碍。