公开(公告)号：US20160312311A1

公开(公告)日：2016-10-27

申请号：US14772976

申请日：2014-02-24

申请人： Fallon LIN ,  Young Shin CHO ,  Julian Roy LEVELL ,  Margaret Elise MCLAUGHLIN ,  Ronald MEYER ,  Raymond PAGLIARINI ,  Veronica SAENZ-VASH ,  Olga SHEBANOVA ,  Huili ZHAI

发明人： Young Shin Cho ,  Julian Roy Levell ,  Fallon Lin ,  Margaret Elise McLaughlin ,  Ronald Meyer ,  Raymond Pagliarini ,  Veronica Saenz-Vash ,  Olga Shebanova ,  Huili Zhai

IPC分类号： C12Q1/68 ,  G01N33/68

CPC分类号： C12Q1/6888 ,  C12Q1/6886 ,  C12Q2600/106 ,  C12Q2600/154 ,  C12Q2600/156 ,  C12Q2600/158 ,  G01N33/6848 ,  G01N33/6875 ,  G01N2333/47 ,  G01N2333/904 ,  G01N2800/52 ,  G01N2800/7028

摘要： The invention provides methods of detecting cancer and detecting activity of IDH inhibitors, and methods of screening for IDH inhibitors by detecting levels of H3K9me2.

摘要翻译： 本发明提供了检测癌症和检测IDH抑制剂的活性的方法，以及通过检测H3K9me2的水平来筛选IDH抑制剂的方法。

公开(公告)号：US08957068B2

公开(公告)日：2015-02-17

申请号：US14347481

申请日：2012-09-26

申请人： Thomas Raymond Caferro ,  Young Shin Cho ,  Abran Q. Costales ,  Huangshu Lei ,  Francois Lenoir ,  Julian Roy Levell ,  Gang Liu ,  Mark G. Palermo ,  Keith Bruce Pfister ,  Martin Sendzik ,  Cynthia Shafer ,  Michael David Shultz ,  Troy Smith ,  James Clifford Sutton ,  Bakary-Barry Toure ,  Fan Yang ,  Qian Zhao

发明人： Thomas Raymond Caferro ,  Young Shin Cho ,  Abran Q. Costales ,  Huangshu Lei ,  Francois Lenoir ,  Julian Roy Levell ,  Gang Liu ,  Mark G. Palermo ,  Keith Bruce Pfister ,  Martin Sendzik ,  Cynthia Shafer ,  Michael David Shultz ,  Troy Smith ,  James Clifford Sutton ,  Bakary-Barry Toure ,  Fan Yang ,  Qian Zhao

IPC分类号： C07D413/04 ,  C07D413/14 ,  A61K31/506 ,  C07D487/04 ,  C07D471/04 ,  C07D487/08 ,  C07D417/14 ,  C07D498/10

CPC分类号： C07D413/14 ,  C07D413/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D487/08 ,  C07D498/10 ,  C07D513/04

摘要： The invention is directed to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1-R6 are defined 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）化合物或其药学上可接受的盐，其中R 1 -R 6在本文中定义。 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：US09309252B2

公开(公告)日：2016-04-12

申请号：US14568410

申请日：2014-12-12

申请人： Christopher Thomas Brain ,  Young Shin Cho ,  John William Giraldes ,  Bharat Lagu ,  Julian Roy Levell ,  Michael Joseph Luzzio ,  Lawrence Blas Perez ,  Yaping Wang ,  Fan Yang

发明人： Christopher Thomas Brain ,  Young Shin Cho ,  John William Giraldes ,  Bharat Lagu ,  Julian Roy Levell ,  Michael Joseph Luzzio ,  Lawrence Blas Perez ,  Yaping Wang ,  Fan Yang

IPC分类号： A01N43/90 ,  A61K31/519 ,  C07D487/04 ,  C07D519/00 ,  C07D471/08 ,  C07D471/10 ,  C07D487/08 ,  C07D498/08 ,  C07D498/20 ,  C07D487/10 ,  C07D498/10

CPC分类号： C07D487/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/08 ,  C07D487/10 ,  C07D498/08 ,  C07D498/10 ,  C07D498/20 ,  C07D519/00

摘要： The invention is directed to novel pyrrolopyrimidine compounds of formula (1) wherein R1, R2y, R4, R8-R11, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

摘要翻译： 本发明涉及式（1）的新颖的吡咯并嘧啶化合物，其中R 1，R 2y，R 4，R 8 -R 11，A和L在本文中定义，并且包括其药学上可接受的盐。 本发明的化合物是CDK4 / 6抑制剂，可用于治疗由CDK4 / 6介导的疾病和病症，如癌症，包括外套细胞淋巴瘤，脂肪肉瘤，非小细胞肺癌，黑素瘤，鳞状细胞食管癌 癌症和乳腺癌。 本发明还涉及包含本发明化合物的药物组合物。 本发明还涉及抑制CDK4 / 6活性的方法以及使用本发明化合物或包含本发明化合物的药物组合物治疗与之相关的病症。

公开(公告)号：US08957074B2

公开(公告)日：2015-02-17

申请号：US13579359

申请日：2011-02-17

申请人： Christopher Thomas Brain ,  Young Shin Cho ,  John William Giraldes ,  Bharat Lagu ,  Julian Roy Levell ,  Michael J. Luzzio ,  Lawrence Blas Perez ,  Yaping Wang ,  Fan Yang

发明人： Christopher Thomas Brain ,  Young Shin Cho ,  John William Giraldes ,  Bharat Lagu ,  Julian Roy Levell ,  Michael J. Luzzio ,  Lawrence Blas Perez ,  Yaping Wang ,  Fan Yang

IPC分类号： A61K31/50 ,  A61K31/501 ,  C07D401/00 ,  C07D403/00 ,  C07D405/00 ,  C07D409/00 ,  A01N43/90 ,  A61K31/519 ,  C07D487/00 ,  C07D498/20 ,  C07D487/04 ,  C07D519/00 ,  C07D471/08 ,  C07D471/10 ,  C07D487/08 ,  C07D498/08

CPC分类号： C07D487/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/08 ,  C07D487/10 ,  C07D498/08 ,  C07D498/10 ,  C07D498/20 ,  C07D519/00

摘要： The invention is directed to novel pyrrolopyrimidine compounds of formula (I) wherein R1, R2Y, R4, R8-R11, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

摘要翻译： 本发明涉及新的式（I）吡咯并嘧啶化合物，其中R 1，R 2 Y，R 4，R 8 -R 11，A和L在本文中定义，并且包括其药学上可接受的盐。 本发明的化合物是CDK4 / 6抑制剂，可用于治疗由CDK4 / 6介导的疾病和病症，如癌症，包括外套细胞淋巴瘤，脂肪肉瘤，非小细胞肺癌，黑素瘤，鳞状细胞食管癌 癌症和乳腺癌。 本发明还涉及包含本发明化合物的药物组合物。 本发明还涉及抑制CDK4 / 6活性的方法以及使用本发明化合物或包含本发明化合物的药物组合物治疗与之相关的病症。

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：US20130150342A1

公开(公告)日：2013-06-13

申请号：US13579359

申请日：2011-02-17

申请人： Christopher Thomas Brain ,  Young Shin Cho ,  John William Giraldes ,  Bharat Lagu ,  Julian Roy Levell ,  Michael J. Luzzio ,  Lawrence Blas Perez ,  Yaping Wang ,  Fan Yang

发明人： Christopher Thomas Brain ,  Young Shin Cho ,  John William Giraldes ,  Bharat Lagu ,  Julian Roy Levell ,  Michael J. Luzzio ,  Lawrence Blas Perez ,  Yaping Wang ,  Fan Yang

IPC分类号： C07D498/20 ,  C07D498/08 ,  C07D471/10 ,  C07D487/04 ,  C07D471/08 ,  C07D487/08

CPC分类号： C07D487/04 ,  C07D471/08 ,  C07D471/10 ,  C07D487/08 ,  C07D487/10 ,  C07D498/08 ,  C07D498/10 ,  C07D498/20 ,  C07D519/00

摘要： The invention is directed to novel pyrrolopyrimidine compounds of formula (I) wherein R1, R2Y, R4, R8-R11, A and L are defined herein and to salts, including pharmaceutically acceptable salts thereof. The compounds of the present invention are CDK4/6 inhibitors and could be useful in the treatment of diseases and disorders mediated by CDK4/6, such as cancer, including mantle cell lymphoma, liposarcoma, non small cell lung cancer, melanoma, squamous cell esophageal cancer and breast cancer. The invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting CDK4/6 activity and to the treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.

摘要翻译： 本发明涉及新的式（I）吡咯并嘧啶化合物，其中R 1，R 2 Y，R 4，R 8 -R 11，A和L在本文中定义，并且包括其药学上可接受的盐。 本发明的化合物是CDK4 / 6抑制剂，可用于治疗由CDK4 / 6介导的疾病和病症，如癌症，包括外套细胞淋巴瘤，脂肪肉瘤，非小细胞肺癌，黑素瘤，鳞状细胞食管癌 癌症和乳腺癌。 本发明还涉及包含本发明化合物的药物组合物。 本发明还涉及抑制CDK4 / 6活性的方法以及使用本发明化合物或包含本发明化合物的药物组合物治疗与之相关的病症。