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1.发明授权公开(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.
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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
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。
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3.发明申请3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES AS INHIBITORS OF MUTANT IDH 审中-公开3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES作为突变体IDH的抑制剂公开(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。
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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。
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5.发明授权公开(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。
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6.发明申请3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES AS INHIBITORS OF MUTANT IDH 有权3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES作为突变体IDH的抑制剂公开(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。
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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。
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8.发明申请3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES AS INHIBITORS OF MUTANT IDH 审中-公开3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES作为突变体IDH的抑制剂公开(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。
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公开(公告)号：US20150099737A1
公开(公告)日：2015-04-09
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： C07D487/04 , C07D487/08 , C07D498/10 , C07D498/08 , C07D487/10 , C07D471/08 , C07D471/10
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。
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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。
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