公开(公告)号：US20180186770A1

公开(公告)日：2018-07-05

申请号：US15736925

申请日：2016-06-15

申请人： Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Andriana Jouk ,  Rajesh Karki ,  Matthew J. LaMarche ,  Gang Liu ,  Mark G. Palermo ,  Lawrence Blas Perez ,  Patrick James Sarver ,  Michael David Shultz ,  Martin Sendzik ,  Bakary-Barry Toure ,  Bing Yu

发明人： Zhuoliang Chen ,  Jorge Garcia Fortanet ,  Andriana Jouk ,  Rajesh Karki ,  Matthew J. LaMarche ,  Gang Liu ,  Mark G. Palermo ,  Lawrence Blas Perez ,  Patrick James Sarver ,  Michael David Shultz ,  Martin Sendzik ,  Bakary-Barry Toure ,  Bing Yu

IPC分类号： C07D401/14 ,  C07D491/107 ,  C07D498/10 ,  C07D471/10 ,  C07D401/04

CPC分类号： C07D401/14 ,  C07D401/04 ,  C07D471/10 ,  C07D491/107 ,  C07D498/10

摘要： The present invention relates to compounds of formula I: in which Y1, Y2, Y3, R1, R2, R4a, R5b, R5a, R5b, R6a and R6b are defined in the Summary of the Invention; capable of inhibiting the activity of SHP2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with the aberrant activity of SHP2.

公开(公告)号：US20160318915A1

公开(公告)日：2016-11-03

申请号：US15209731

申请日：2016-07-13

申请人： Thomas Raymond CAFERRO ,  Zhuoliang CHEN ,  Young Shin CHO ,  Abran Q. COSTALES ,  Julian Roy LEVELL ,  Gang LIU ,  James R. MANNING ,  Martin SENDZIK ,  Cynthia SHAFER ,  Michael David SHULTZ ,  James Clifford SUTTON ,  Yaping WANG ,  Qian ZHAO

发明人： Thomas Raymond CAFERRO ,  Zhuoliang CHEN ,  Young Shin CHO ,  Abran Q. COSTALES ,  Julian Roy LEVELL ,  Gang LIU ,  James R. MANNING ,  Martin SENDZIK ,  Cynthia SHAFER ,  Michael David SHULTZ ,  James Clifford SUTTON ,  Yaping WANG ,  Qian ZHAO

IPC分类号： C07D413/14 ,  C07D413/04 ,  C07D417/14

CPC分类号： C07D413/14 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/04 ,  C07D417/14

摘要： The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.

摘要翻译： 或其药学上可接受的盐，其中R1，R2a，R2b和R3-R7为本文。 本发明还涉及含有式（I）化合物的组合物以及这些化合物在抑制具有新形态活性的突变体IDH蛋白质中的用途。 本发明还涉及式（I）化合物在治疗与这种突变体IDH蛋白相关的疾病或病症中的用途，包括但不限于细胞增殖病症如癌症。

公开(公告)号：US20150126513A1

公开(公告)日：2015-05-07

申请号：US14154173

申请日：2012-07-13

申请人： Christine Hiu-Tung Chen ,  Donovan Noel Chin ,  Lucian V. DiPietro ,  Jianmei Fan ,  Mark G. Palermo ,  Michael David Shultz ,  Bakary-Barry Toure

发明人： Christine Hiu-Tung Chen ,  Donovan Noel Chin ,  Lucian V. DiPietro ,  Jianmei Fan ,  Mark G. Palermo ,  Michael David Shultz ,  Bakary-Barry Toure

IPC分类号： C07D401/04 ,  C07D487/04 ,  C07D498/04 ,  C07D401/14 ,  C07D513/04 ,  C07D471/04 ,  C07D491/052 ,  C07D495/04

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/052 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

摘要： The present invention provides for compounds of formula (I): wherein R1-R4 and n are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.

摘要翻译： 本发明提供式（I）化合物：其中R 1 -R 4和n如本文所定义。 本发明还提供药物组合物和组合物，其包含式（I）化合物以及使用这些化合物作为阻断酶抑制剂和用于治疗Wnt信号传导和阻断酶1和2信号传导相关疾病，其包括但是是 不限于癌症。

公开(公告)号：US20150025070A1

公开(公告)日：2015-01-22

申请号：US14154161

申请日：2012-07-13

申请人： Atwood Kim Cheung ,  Donovan Noel Chin ,  Jianmei Fan ,  Karen Marie Miller-Moslin ,  Michael David Shultz ,  Troy D. Smith ,  Ronald Charles Tomlinson ,  Bakary-Barry Toure ,  Michael Scott Visser

发明人： Atwood Kim Cheung ,  Donovan Noel Chin ,  Jianmei Fan ,  Karen Marie Miller-Moslin ,  Michael David Shultz ,  Troy D. Smith ,  Ronald Charles Tomlinson ,  Bakary-Barry Toure ,  Michael Scott Visser

IPC分类号： C07D491/052 ,  C07D493/04 ,  C07D401/12

CPC分类号： C07D491/052 ,  A61K31/453 ,  A61K31/4545 ,  C07D401/12 ,  C07D409/14 ,  C07D493/04

摘要： The present invention provides for compounds of formula (I): wherein R1-R5 and L are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.

摘要翻译： 本发明提供式（I）化合物：其中R1-R5和L在本文中定义。 本发明还提供药物组合物和组合物，其包含式（I）化合物以及使用这些化合物作为阻断酶抑制剂和用于治疗Wnt信号传导和阻断酶1和2信号传导相关疾病，其包括但是是 不限于癌症。

公开(公告)号：US20140275083A1

公开(公告)日：2014-09-18

申请号：US14208015

申请日：2014-03-13

申请人： Thomas Raymond CAFERRO ,  Zhuoliang CHEN ,  Young Shin CHO ,  Abran Q. COSTALES ,  Julian Roy LEVELL ,  Gang LIU ,  James R. MANNING ,  Martin SENDZIK ,  Cynthia SHAFER ,  Michael David SHULTZ ,  James SUTTON ,  Yaping WANG ,  Qian ZHAO

发明人： Thomas Raymond CAFERRO ,  Zhuoliang CHEN ,  Young Shin CHO ,  Abran Q. COSTALES ,  Julian Roy LEVELL ,  Gang LIU ,  James R. MANNING ,  Martin SENDZIK ,  Cynthia SHAFER ,  Michael David SHULTZ ,  James SUTTON ,  Yaping WANG ,  Qian ZHAO

IPC分类号： C07D413/04 ,  A61K31/5377 ,  C07D417/14 ,  C07D413/14 ,  A61K31/506

CPC分类号： C07D413/14 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/04 ,  C07D417/14

摘要： The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.

摘要翻译： 本发明涉及式（I）：或其药学上可接受的盐，其中R1，R2a，R2b和R3-R7为本文。 本发明还涉及含有式（I）化合物的组合物以及这些化合物在抑制具有新形态活性的突变体IDH蛋白质中的用途。 本发明还涉及式（I）化合物在治疗与这种突变体IDH蛋白相关的疾病或病症中的用途，包括但不限于细胞增殖病症如癌症。

公开(公告)号：US09434719B2

公开(公告)日：2016-09-06

申请号：US14408418

申请日：2014-03-12

申请人： Thomas Raymond Caferro ,  Zhuoliang Chen ,  Young Shin Cho ,  Abran Q. Costales ,  Julian Roy Levell ,  Gang Liu ,  James R. Manning ,  Martin Sendzik ,  Cynthia Shafer ,  Michael David Shultz ,  James Sutton ,  Yaping Wang ,  Qian Zhao

发明人： Thomas Raymond Caferro ,  Zhuoliang Chen ,  Young Shin Cho ,  Abran Q. Costales ,  Julian Roy Levell ,  Gang Liu ,  James R. Manning ,  Martin Sendzik ,  Cynthia Shafer ,  Michael David Shultz ,  James Sutton ,  Yaping Wang ,  Qian Zhao

IPC分类号： C07D413/04 ,  A61K31/506 ,  C07D413/14 ,  C07D417/14 ,  A61K31/5377

CPC分类号： C07D413/14 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/04 ,  C07D417/14

摘要： The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.

公开(公告)号：US09181266B2

公开(公告)日：2015-11-10

申请号：US14154161

申请日：2012-07-13

申请人： Atwood Kim Cheung ,  Donovan Noel Chin ,  Jianmei Fan ,  Karen Marie Miller-Moslin ,  Michael David Shultz ,  Troy D Smith ,  Ronald Charles Tomlinson ,  Bakary-Barry Toure ,  Michael Scott Visser ,  Zhuoliang Chen

发明人： Atwood Kim Cheung ,  Donovan Noel Chin ,  Jianmei Fan ,  Karen Marie Miller-Moslin ,  Michael David Shultz ,  Troy D Smith ,  Ronald Charles Tomlinson ,  Bakary-Barry Toure ,  Michael Scott Visser ,  Zhuoliang Chen

IPC分类号： C07D401/12 ,  C07D409/14 ,  A61K31/453 ,  A61K31/4545 ,  C07D491/052 ,  C07D493/04

CPC分类号： C07D491/052 ,  A61K31/453 ,  A61K31/4545 ,  C07D401/12 ,  C07D409/14 ,  C07D493/04

摘要： The present invention provides for compounds of formula (I): wherein R1-R5 and L are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.

摘要翻译： 本发明提供式（I）化合物：其中R1-R5和L在本文中定义。 本发明还提供药物组合物和组合物，其包含式（I）化合物以及使用这些化合物作为阻断酶抑制剂和用于治疗Wnt信号传导和阻断酶1和2信号传导相关疾病，其包括但是是 不限于癌症。

公开(公告)号：US20160039802A1

公开(公告)日：2016-02-11

申请号：US14774741

申请日：2014-03-13

申请人： Young Shin CHO ,  Julian Roy LEVELL ,  Gang LIU ,  Michael David SHULTZ ,  Simon Cornelis VAN DER PLAS ,  NOVARTIS AG

发明人： Young Shin CHO ,  Julian Roy LEVELL ,  Gang LIU ,  Michael David SHULTZ ,  Simon Cornelis VAN DER PLAS

IPC分类号： C07D413/04 ,  C07D487/08 ,  C07D417/14 ,  A61K31/5377 ,  A61K31/506 ,  C07D413/14

CPC分类号： C07D413/04 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/14 ,  C07D417/14 ,  C07D487/08 ,  A61K2300/00

摘要： The invention is directed to a formula (I): or a pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are described herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant I DH proteins including, but not limited to, cell-proliferation disorders, such as cancer.

摘要翻译： 本发明涉及式（I）：或其药学上可接受的盐，其中R1，R2a，R2b和R3-R7如本文所述。 本发明还涉及含有式（I）化合物的组合物以及这些化合物在抑制具有新形态活性的突变体IDH蛋白质中的用途。 本发明还涉及式（I）化合物在治疗与这种突变体I DH蛋白相关的疾病或病症中的应用，包括但不限于细胞增殖病症如癌症。

公开(公告)号：US09227982B2

公开(公告)日：2016-01-05

申请号：US14154170

申请日：2012-07-13

申请人： Atwood Kim Cheung ,  Donovan Noel Chin ,  Jianmei Fan ,  Michael David Shultz ,  Ronald Charles Tomlinson

发明人： Atwood Kim Cheung ,  Donovan Noel Chin ,  Jianmei Fan ,  Michael David Shultz ,  Ronald Charles Tomlinson

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D491/00 ,  C07D495/00 ,  C07D491/052

CPC分类号： C07D491/052 ,  A61K31/519

摘要： The present invention provides for compounds of formula (I) wherein R1 and R2 are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.

摘要翻译： 本发明提供式（I）化合物，其中R 1和R 2在本文中定义。 本发明还提供药物组合物和组合物，其包含式（I）化合物以及使用这些化合物作为阻断酶抑制剂和用于治疗Wnt信号传导和阻断酶1和2信号传导相关疾病，其包括但是是 不限于癌症。

公开(公告)号：US09163003B2

公开(公告)日：2015-10-20

申请号：US14154173

申请日：2012-07-13

申请人： Christine Hiu-Tung Chen ,  Donovan Noel Chin ,  Lucien V. DiPietro ,  Jianmei Fan ,  Mark G. Palermo ,  Michael David Shultz ,  Bakary-Barry Toure

发明人： Christine Hiu-Tung Chen ,  Donovan Noel Chin ,  Lucien V. DiPietro ,  Jianmei Fan ,  Mark G. Palermo ,  Michael David Shultz ,  Bakary-Barry Toure

IPC分类号： C07D491/052 ,  C07D493/04 ,  C07D401/12 ,  C07D401/04 ,  C07D401/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/052 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04

摘要： The present invention provides for compounds of formula (I): wherein R1-R4 and n are defined herein. The present invention also provides for pharmaceutical compositions and combinations comprising a compound of formula (I) as well as for the use of such compounds as tankyrase inhibitors and in the treatment of Wnt signaling and tankyrase 1 and 2 signaling related disorders which include, but are not limited to, cancer.

摘要翻译： 本发明提供式（I）化合物：其中R 1 -R 4和n如本文所定义。 本发明还提供药物组合物和组合物，其包含式（I）化合物以及使用这些化合物作为阻断酶抑制剂和用于治疗Wnt信号传导和阻断酶1和2信号传导相关疾病，其包括但是是 不限于癌症。