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1. 发明申请

US20080262004A1 Tgf-Beta Inhibitors 失效
标题翻译： Tgf-β抑制剂
公开(公告)号：US20080262004A1
公开(公告)日：2008-10-23
申请号：US11577094
申请日：2005-11-02
申请人： Clive Gideon Diefenbacher , Thomas Albert Engler , Hong-Yu Li , Sushant Malhotra , Jason Scott Sawyer , Yan Wang
发明人： Clive Gideon Diefenbacher , Thomas Albert Engler , Hong-Yu Li , Sushant Malhotra , Jason Scott Sawyer , Yan Wang
IPC分类号： A61K31/519 , C07D471/04 , A61K31/437 , A61P25/28 , A61P35/00 , C07D487/04
CPC分类号： C07D487/04 , C07D471/04 , C07D519/00
摘要： The present invention is directed to inhibitors of TGF-β of Formula I:
摘要翻译：本发明涉及式I的TGF-β抑制剂：

2. 发明授权

US07405299B2 Compounds as pharmaceutical agents 失效
标题翻译：化合物作为药剂
公开(公告)号：US07405299B2
公开(公告)日：2008-07-29
申请号：US10535381
申请日：2003-11-24
申请人： Douglas Wade Beight , Timothy Paul Burkholder , Todd Vincent Decollo , Alexander Glenn Godfrey , Charles Raymond Heap , Chi-Hsin Richard King , Hong-Yu Li , William Thomas McMillen , Jason Scott Sawyer , Yan Wang , Clive Gideon Diefenbacher , Thomas Albert Engler , Sushant Malhotra , Sreenivasa Reedy Mundla
发明人： Douglas Wade Beight , Timothy Paul Burkholder , Todd Vincent Decollo , Alexander Glenn Godfrey , Charles Raymond Heap , Chi-Hsin Richard King , Hong-Yu Li , William Thomas McMillen , Jason Scott Sawyer , Yan Wang , Clive Gideon Diefenbacher , Thomas Albert Engler , Sushant Malhotra , Sreenivasa Reedy Mundla
IPC分类号： C07D241/36 , C07D217/00 , C07D401/00
CPC分类号： C07D487/04
摘要： The current invention relates to compounds of the formula: (Ia) and the pharmaceutically acceptable salts thereof and their use as TGF-beta signal transduction inhibitors for treating cancer and other diseases in a patient in need thereof by administration of said compounds.
摘要翻译：本发明涉及式（Ia）化合物及其药学上可接受的盐及其作为TGF-β信号转导抑制剂的用途，其用于通过施用所述化合物治疗有需要的患者中的癌症和其它疾病。

3. 发明授权

US07511056B2 TGF-β inhibitors 失效
标题翻译： TGF-β抑制剂
公开(公告)号：US07511056B2
公开(公告)日：2009-03-31
申请号：US11577094
申请日：2005-11-02
申请人： Clive Gideon Diefenbacher , Thomas Albert Engler , Hong-Yu Li , Sushant Malhotra , Jason Scott Sawyer , Yan Wang
发明人： Clive Gideon Diefenbacher , Thomas Albert Engler , Hong-Yu Li , Sushant Malhotra , Jason Scott Sawyer , Yan Wang
IPC分类号： A01N43/42 , A61K31/44 , C07D491/02 , C07D498/02 , C07D401/00
CPC分类号： C07D487/04 , C07D471/04 , C07D519/00
摘要： The present invention is directed to inhibitors of TGF-β of Formula I:
摘要翻译：本发明涉及式I的TGF-β抑制剂：

4. 发明申请

US20060058295A1 Novel compounds as pharmaceutical agents 失效
标题翻译：新型化合物作为药剂
公开(公告)号：US20060058295A1
公开(公告)日：2006-03-16
申请号：US10535381
申请日：2003-11-24
申请人： Douglas Beight , Timothy Burkholder , Todd Decollo , Alexander Godfrey , Charles Heap , Chi-Hsin King , Hong-Yu Li , William McMillen , Jason Sawyer , Yan Wang , Clive Diefenbacher , Thomas Engler , Sushant Malhotra , Sreenivasa Mundla
发明人： Douglas Beight , Timothy Burkholder , Todd Decollo , Alexander Godfrey , Charles Heap , Chi-Hsin King , Hong-Yu Li , William McMillen , Jason Sawyer , Yan Wang , Clive Diefenbacher , Thomas Engler , Sushant Malhotra , Sreenivasa Mundla
IPC分类号： A61K31/5377 , A61K31/519 , A61K31/4745 , C07D471/02
CPC分类号： C07D487/04
摘要： The current invention relates to compounds of the formula: (Ia) and the pharmaceutically acceptable salts thereof and their use as TGF-beta signal transduction inhibitors for treating cancer and other diseases in a patient in need thereof by administration of said compounds.
摘要翻译：本发明涉及式（Ia）化合物及其药学上可接受的盐及其作为TGF-β信号转导抑制剂的用途，其用于通过施用所述化合物治疗有需要的患者中的癌症和其它疾病。

5. 发明授权

US08063212B2 Imidazolidinonyl aminopyrimidine compounds for the treatment of cancer 失效
标题翻译：咪唑烷酰氨基嘧啶化合物治疗癌症
公开(公告)号：US08063212B2
公开(公告)日：2011-11-22
申请号：US12516251
申请日：2007-12-11
申请人： Harold Burns Brooks , Joyce Z. Crich , James Robert Henry , Hong-Yu Li , Jason Scott Sawyer , Yan Wang
发明人： Harold Burns Brooks , Joyce Z. Crich , James Robert Henry , Hong-Yu Li , Jason Scott Sawyer , Yan Wang
IPC分类号： C07D401/00
CPC分类号： C07D409/14
摘要： The present invention provides novel imidazolidinonyl aminopyrimidine compounds believed to have clinical use for treatment of cancer through inhibiting Plk1. Formula I wherein: R1 is aminomethyl, (C1-C3 alkyl)aminomethyl, di(C1-C2 alkyl)aminomethyl, N-ethyl-N-methyl-aminomethyl, 1-aminoethyl, 1-((C1-C2 alkyl)amino)-ethyl, 3,3,3-trifluoro-propylaminomethyl, ethynyl, 2-hydroxy-ethoxy, 2-hydroxyethylaminomethyl, 2-cyanoethylaminomethyl, morpholin-4-ylmethyl, methoxymethoxymethyl, cyclopropyl, 1-azetidinylmethyl, 1-pyrrolidinylmethyl, or 1,3-dioxolan-2-yl; R2 is hydrogen or halo; R3 is hydrogen or halo; provided that at least one of R2 and R3 is hydrogen; R4 is hydrogen, methyl, or halo; and is a single bond that is either present or absent, or pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了被认为具有通过抑制Plk1治疗癌症的临床用途的新型咪唑烷基氨基嘧啶化合物。式（I）其中：R1是氨基甲基，（C1-C3烷基）氨基甲基，二（C1-C2烷基）氨基甲基，N-乙基-N-甲基 - 氨基甲基，1-氨基乙基，1-（（C1-C2烷基）氨基）乙基，3,3,3-三氟 - 丙氨基甲基，乙炔基，2-羟基 - 乙氧基，2-羟乙基氨基甲基，2-氰乙基氨基甲基，吗啉-4-基甲基，甲氧基甲氧基甲基，环丙基，1-氮杂环丁基甲基，1-吡咯烷基甲基， 3-二氧戊环-2-基; R2是氢或卤素; R3是氢或卤素; R2和R3中的至少一个是氢; R4是氢，甲基或卤素; 并且是存在或不存在的单键或其药学上可接受的盐。

6. 发明授权

US08063035B2 Triazolyl aminopyrimidine compounds 失效
标题翻译：三唑基氨基嘧啶化合物
公开(公告)号：US08063035B2
公开(公告)日：2011-11-22
申请号：US12598926
申请日：2008-05-07
申请人： Joyce Z. Crich , James Robert Henry , Hong Hu , Delu Jiang , Hong-Yu Li , William Thomas McMillen , Jason Scott Sawyer , Melissa Kate Slater , Yan Wang
发明人： Joyce Z. Crich , James Robert Henry , Hong Hu , Delu Jiang , Hong-Yu Li , William Thomas McMillen , Jason Scott Sawyer , Melissa Kate Slater , Yan Wang
IPC分类号： A61K31/381 , C07D333/16 , C07D409/14
CPC分类号： C07D409/14
摘要： The present invention provides triazolyl aminopyrimidine compounds useful in the treatment of cancer.
摘要翻译：本发明提供可用于治疗癌症的三唑基氨基嘧啶化合物。

7. 发明申请

US20100081641A1 IMIDAZOLIDINONYL AMINOPYRIMIDINE COMPOUNDS FOR THE TREATMENT OF CANCER 失效
标题翻译：用于治疗癌症的咪达唑仑胺氨基嘧啶化合物
公开(公告)号：US20100081641A1
公开(公告)日：2010-04-01
申请号：US12516251
申请日：2007-12-11
申请人： Harold Burns Brooks , Joyce Z. Crich , James Robert Henry , Hong-Yu Li , Jason Scott Sawyer , Yan Wang
发明人： Harold Burns Brooks , Joyce Z. Crich , James Robert Henry , Hong-Yu Li , Jason Scott Sawyer , Yan Wang
IPC分类号： A61K31/397 , C07D403/14 , A61K31/506 , C07D413/14 , A61K31/5377 , A61P35/00
CPC分类号： C07D409/14
摘要： The present invention provides novel imidazolidinonyl aminopyrimidine compounds believed to have clinical use for treatment of cancer through inhibiting Plk1. Formula I wherein: R1 is aminomethyl, (C1-C3 alkyl)aminomethyl, di(C1-C2 alkyl)aminomethyl, N-ethyl-N-methyl-aminomethyl, 1-aminoethyl, 1-((C1-C2 alkyl)amino)-ethyl, 3,3,3-trifluoro-propylaminomethyl, ethynyl, 2-hydroxy-ethoxy, 2-hydroxyethylaminomethyl, 2-cyanoethylaminomethyl, mopholin-4-ylmethyl, methoxymethoxymethyl, cyclopropyl, 1-azetidinylmethyl, 1-pyrrolidinylmethyl, or 1,3-dioxolan-2-yl; R2 is hydrogen or halo; R3 is hydrogen or halo; provided that at least one of R2 and R3 is hydrogen; R4 is hydrogen, methyl, or halo; and is a single bond that is either present or absent, or pharmaceutically acceptable salt thereof.
摘要翻译：本发明提供了被认为具有通过抑制Plk1治疗癌症的临床用途的新型咪唑烷基氨基嘧啶化合物。式（I）其中：R1是氨基甲基，（C1-C3烷基）氨基甲基，二（C1-C2烷基）氨基甲基，N-乙基-N-甲基 - 氨基甲基，1-氨基乙基，1-（（C1-C2烷基）乙基，3,3,3-三氟 - 丙基氨基甲基，乙炔基，2-羟基 - 乙氧基，2-羟乙基氨基甲基，2-氰基乙基氨基甲基，吗啉-4-基甲基，甲氧基甲氧基甲基，环丙基，1-氮杂环丁基甲基，1-吡咯烷基甲基， 3-二氧戊环-2-基; R2为氢或卤素; R3是氢或卤素; R2和R3中的至少一个是氢; R4是氢，甲基或卤素; 并且是存在或不存在的单键或其药学上可接受的盐。

8. 发明授权

US08114872B2 Triazolyl aminopyrimidine compounds 失效
标题翻译：三唑基氨基嘧啶化合物
公开(公告)号：US08114872B2
公开(公告)日：2012-02-14
申请号：US12596957
申请日：2008-05-07
申请人： Joyce Z. Crich , Delu Jiang , Hong-Yu Li , William Thomas McMillen , Jason Scott Sawyer , Melissa Kate Slater , Yan Wang , James Robert Henry , Hong Hu , Sachin Govindlal Maniar
发明人： Joyce Z. Crich , Delu Jiang , Hong-Yu Li , William Thomas McMillen , Jason Scott Sawyer , Melissa Kate Slater , Yan Wang , James Robert Henry , Hong Hu , Sachin Govindlal Maniar
IPC分类号： C07D409/14 , A61K31/506
CPC分类号： C07D409/14
摘要： The present invention provides triazolyl aminopyrimidine compounds useful in the treatment of cancer.
摘要翻译：本发明提供可用于治疗癌症的三唑基氨基嘧啶化合物。

9. 发明申请

US20100087431A1 TRIAZOLYL AMINOPYRIMIDINE COMPOUNDS 失效
公开(公告)号：US20100087431A1
公开(公告)日：2010-04-08
申请号：US12598926
申请日：2008-05-07
申请人： Harold Burns Brooks , Joyce Z. Crich , James Robert Henry , Hong Hu , Delu Jiang , Hong-Yu Li , William Thomas McMillen , Jason Scott Sawyer , Melissa Kate Slater , Yan Wang
发明人： Harold Burns Brooks , Joyce Z. Crich , James Robert Henry , Hong Hu , Delu Jiang , Hong-Yu Li , William Thomas McMillen , Jason Scott Sawyer , Melissa Kate Slater , Yan Wang
IPC分类号： A61K31/506 , C07D409/14 , C07D413/14 , A61K31/5377 , A61P35/00
CPC分类号： C07D409/14
摘要： The present invention provides triazolyl aminopyrimidine compounds useful in the treatment of cancer.

10. 发明申请

US20100130466A1 TRIAZOLYL AMINOPYRIMIDINE COMPOUNDS 失效
标题翻译：三唑基氨基嘧啶化合物
公开(公告)号：US20100130466A1
公开(公告)日：2010-05-27
申请号：US12596957
申请日：2008-05-07
申请人： Harold Burns Brooks , Joyce Z. Crich , Delu Jiang , Hong-Yu Li , William Thomas McMillen , Jason Scott Sawyer , Melissa Kate Slater , Yan Wang , James Robert Henry , Hong Hu , Sachin Govindlal Maniar
发明人： Harold Burns Brooks , Joyce Z. Crich , Delu Jiang , Hong-Yu Li , William Thomas McMillen , Jason Scott Sawyer , Melissa Kate Slater , Yan Wang , James Robert Henry , Hong Hu , Sachin Govindlal Maniar
IPC分类号： A61K31/506 , C07D409/14 , A61P35/00 , C07D413/14 , A61K31/5377
CPC分类号： C07D409/14
摘要： The present invention provides triazolyl aminopyrimidine compounds useful in the treatment of cancer.
摘要翻译：本发明提供可用于治疗癌症的三唑基氨基嘧啶化合物。

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