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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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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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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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4.发明授权Imidazole derivatives and their use as modulators of cyclin dependent kinases 失效咪唑衍生物及其作为细胞周期蛋白依赖性激酶的调节剂的用途公开(公告)号：US08598217B2
公开(公告)日：2013-12-03
申请号：US13266976
申请日：2010-04-30
申请人： Steven Howard , Paul Neil Mortenson , Steven Douglas Hiscock , Alison Jo-Anne Woolford , Andrew James Woodhead , Gianni Chessari , Marc O'Reilly , Miles Stuart Congreve , Claudio Dagostin , Young Shin Cho , Fan Yang , Christine Hiu-Tung Chen , Christopher Thomas Brain , Bharat Lagu , Yaping Wang , Sunkyu Kim , John Giraldes , Michael Joseph Luzzio , Lawrence Blas Perez
发明人： Steven Howard , Paul Neil Mortenson , Steven Douglas Hiscock , Alison Jo-Anne Woolford , Andrew James Woodhead , Gianni Chessari , Marc O'Reilly , Miles Stuart Congreve , Claudio Dagostin , Young Shin Cho , Fan Yang , Christine Hiu-Tung Chen , Christopher Thomas Brain , Bharat Lagu , Yaping Wang , Sunkyu Kim , John Giraldes , Michael Joseph Luzzio , Lawrence Blas Perez
IPC分类号： A61K31/496 , A61K31/4545 , A61K31/4439 , A61K31/4725 , A61K31/4353 , A61K31/4178 , A61K31/4184 , A61P35/00 , C07D471/04 , C07D401/06 , C07D417/10 , C07D413/06 , C07D403/10
CPC分类号： C07D471/04 , C07D233/22 , C07D233/24 , C07D235/12 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D487/04 , C07D519/00
摘要： The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+—O− or CR3; Y is N, N+—O− or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.
摘要翻译： 本发明提供式（I）化合物及其盐，互变异构体，溶剂化物和N-氧化物; 其中Q是CH或N; X是N，N + -O-或CR 3; Y是N，N + -O-或CR3a; R1和R2独立地选自氢和权利要求中定义的各种取代基; 或R 1和R 2与它们所连接的原子一起连接以形成任选取代的4至7个成员的碳环或杂环芳族或非芳族环; R3选自氢和各种取代基; 并且R 3a选自氢和权利要求中定义的各种取代基。 还提供含有式（I）化合物，制备化合物的方法和化合物的医疗用途的药物组合物。 式（I）化合物具有作为CDK激酶抑制剂的活性，并且可用于治疗尤其是增殖性疾病如癌症。
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5.发明申请IMIDAZOLE DERIVATIVES AND THEIR USE AS MODULATORS OF CYCLIN DEPENDENT KINASES 失效咪唑衍生物及其作为细胞周期调节因子的调节剂公开(公告)号：US20120101064A1
公开(公告)日：2012-04-26
申请号：US13266976
申请日：2010-04-30
申请人： Steven Howard , Paul Neil Mortenson , Steven Douglas Hiscock , Alison Jo-Anne Woolford , Andrew James Woodhead , Gianni Chessari , Marc O'reilly , Miles Stuart Congreve , Claudio Dagostin , Young Shin Cho , Fan Yang , Christine Hiu-Tung Chen , Christopher Thomas Brain , Bharat Lagu , Yaping Wang , Sunkyu Kim , John Grialdes , Michael Joseph Luzzio , Lawrence Blas Perez
发明人： Steven Howard , Paul Neil Mortenson , Steven Douglas Hiscock , Alison Jo-Anne Woolford , Andrew James Woodhead , Gianni Chessari , Marc O'reilly , Miles Stuart Congreve , Claudio Dagostin , Young Shin Cho , Fan Yang , Christine Hiu-Tung Chen , Christopher Thomas Brain , Bharat Lagu , Yaping Wang , Sunkyu Kim , John Grialdes , Michael Joseph Luzzio , Lawrence Blas Perez
IPC分类号： A61K31/675 , A61K31/4439 , A61K31/496 , A61K31/4545 , C07D413/06 , A61K31/5377 , C07D417/10 , A61K31/427 , C07D403/10 , A61K31/4178 , C07D409/10 , C07D401/06 , A61K31/4725 , A61K31/551 , C07D471/04 , A61K31/437 , C07F9/6561 , A61P35/00 , A61P35/02 , C07D401/14
CPC分类号： C07D471/04 , C07D233/22 , C07D233/24 , C07D235/12 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D403/10 , C07D405/14 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/14 , C07D417/10 , C07D417/14 , C07D487/04 , C07D519/00
摘要： The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+—O− or CR3; Y is N, N+—O− or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.
摘要翻译： 本发明提供式（I）化合物及其盐，互变异构体，溶剂化物和N-氧化物; 其中Q是CH或N; X是N，N + -O-或CR 3; Y是N，N + -O-或CR3a; R1和R2独立地选自氢和权利要求中定义的各种取代基; 或R 1和R 2与它们所连接的原子一起连接以形成任选取代的4至7个成员的碳环或杂环芳族或非芳族环; R3选自氢和各种取代基; 并且R 3a选自氢和权利要求中定义的各种取代基。 还提供含有式（I）化合物，制备化合物的方法和化合物的医疗用途的药物组合物。 式（I）化合物具有作为CDK激酶抑制剂的活性，并且可用于治疗尤其是增殖性疾病如癌症。
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6.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：US20050234042A1
公开(公告)日：2005-10-20
申请号：US11099941
申请日：2005-04-06
申请人： Mark Palermo , Sushil Sharma , Christopher Straub , Run-Ming Wang , Leigh Zawel , Yanlin Zhang , Zhuoliang Chen , Yaping Wang , Fan Yang , Wojciech Wrona , Gang Liu , Mark Charest , Feng He
发明人： Mark Palermo , Sushil Sharma , Christopher Straub , Run-Ming Wang , Leigh Zawel , Yanlin Zhang , Zhuoliang Chen , Yaping Wang , Fan Yang , Wojciech Wrona , Gang Liu , Mark Charest , Feng He
IPC分类号： A61K31/40 , A61K31/4025 , A61K31/437 , A61K31/4745 , A61K31/55 , C07D207/06 , C07D207/08 , C07D207/09 , C07D207/16 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/10 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/02 , C07D471/04 , C07D487/04
CPC分类号： C07D207/16 , C07D207/06 , C07D207/08 , C07D207/09 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/10 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
摘要： Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula I
摘要翻译： 抑制Smac蛋白与抑制凋亡蛋白抑制剂（IAP）的新型化合物
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公开(公告)号：US20080242658A1
公开(公告)日：2008-10-02
申请号：US10594413
申请日：2005-04-06
申请人： Mark G Palermo , Sushil Kumar Sharma , Christopher Straub , Run-Ming Wang , Leigh Zawel , Yanlin Zhang , Zhuoliang Chen , Yaping Wang , Fan Yang , Wojciech Wrona , Gang Liu , Mark G. Charest , Feng He
发明人： Mark G Palermo , Sushil Kumar Sharma , Christopher Straub , Run-Ming Wang , Leigh Zawel , Yanlin Zhang , Zhuoliang Chen , Yaping Wang , Fan Yang , Wojciech Wrona , Gang Liu , Mark G. Charest , Feng He
IPC分类号： A61K31/407 , C07D471/04 , C07D207/08 , C07D487/04 , C07D207/32 , A61P35/00 , A61K31/4439 , A61K31/422 , A61K31/41 , A61K31/506 , C07D401/04 , C07D403/12 , A61K31/437 , A61K31/55 , A61K31/40
CPC分类号： C07D207/16 , C07D207/06 , C07D207/08 , C07D207/09 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/10 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
摘要： Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula I
摘要翻译： 抑制Smac蛋白与抑制凋亡蛋白抑制剂（IAP）的新型化合物
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公开(公告)号：US07419975B2
公开(公告)日：2008-09-02
申请号：US11099941
申请日：2005-04-06
申请人： Mark Gabriel Palermo , Sushil Kumar Sharma , Christopher Straub , Run-Ming Wang , Leigh Scott Zawel , Yanlin Zhang , Zhuoliang Chen , Yaping Wang , Fan Yang , Wojciech Wrona , Gang Liu , Mark G. Charest , Feng He
发明人： Mark Gabriel Palermo , Sushil Kumar Sharma , Christopher Straub , Run-Ming Wang , Leigh Scott Zawel , Yanlin Zhang , Zhuoliang Chen , Yaping Wang , Fan Yang , Wojciech Wrona , Gang Liu , Mark G. Charest , Feng He
IPC分类号： A61K31/407 , A61K31/437 , A61K31/55 , C07D487/04 , C07D471/04
CPC分类号： C07D207/16 , C07D207/06 , C07D207/08 , C07D207/09 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/10 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
摘要： Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula I
摘要翻译： 抑制Smac蛋白与抑制凋亡蛋白抑制剂（IAP）的新型化合物
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公开(公告)号：US08338440B2
公开(公告)日：2012-12-25
申请号：US13456274
申请日：2012-04-26
申请人： Mark G. Palermo , Sushil Kumar Sharma , Christopher Sean Straub , Run-Ming Wang , Leigh Zawel , Yanlin Zhang , Zhuoliang Chen , Yaping Wang , Fan Yang , Wojciech Wrona , Gang Liu , Mark G. Charest , Feng He
发明人： Mark G. Palermo , Sushil Kumar Sharma , Christopher Sean Straub , Run-Ming Wang , Leigh Zawel , Yanlin Zhang , Zhuoliang Chen , Yaping Wang , Fan Yang , Wojciech Wrona , Gang Liu , Mark G. Charest , Feng He
IPC分类号： A61K31/427 , A61K31/4245 , A61K31/422 , A61K31/435 , A61K31/40 , A61K31/506 , A61K31/41
CPC分类号： C07D207/16 , C07D207/06 , C07D207/08 , C07D207/09 , C07D401/04 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/10 , C07D405/12 , C07D409/12 , C07D413/04 , C07D413/14 , C07D417/04 , C07D471/04 , C07D487/04
摘要： Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).
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