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11. 发明申请

US20050277655A1 Pyrazolopyrimidines 失效
标题翻译：吡唑并嘧啶
公开(公告)号：US20050277655A1
公开(公告)日：2005-12-15
申请号：US11136023
申请日：2005-05-24
申请人： Qingjie Ding , Nan Jiang , John Roberts
发明人： Qingjie Ding , Nan Jiang , John Roberts
IPC分类号： A61K31/4162 , A61K31/519 , C07D239/70 , C07D487/02 , C07D487/04
CPC分类号： C07D487/04
摘要： Novel pyrazolopyrimidines of formula (I): are discussed. These pyrazolopyrimidines are capable of inhibiting the activity of cyclin-dependent kinases, most particularly cyclin-dependent kinase 1 (Cdk1), cyclin-dependent kinase 2 (Cdk2), and cyclin-dependent kinase 4 (Cdk4) and are thus useful, inter alia, in the treatment or control of cancer, in particular solid tumors. This invention also provides pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment or control of breast, lung, colon and prostate tumors.
摘要翻译：讨论式（I）的新型吡唑并嘧啶：。这些吡唑并嘧啶能够抑制细胞周期蛋白依赖性激酶的活性，特别是细胞周期蛋白依赖性激酶1（Cdk1），细胞周期蛋白依赖性激酶2（Cdk2）和细胞周期蛋白依赖性激酶4（Cdk4）的活性，因此尤其有用，治疗或控制癌症，特别是实体瘤。本发明还提供含有这些化合物的药物组合物以及治疗或控制癌症的方法，特别是治疗或控制乳腺癌，肺癌，结肠癌和前列腺肿瘤的方法。

12. 发明申请

US20110269809A1 SPIROINDOLINONE PYRROLIDINES 失效
标题翻译：螺吲哚啉酮吡咯烷酮
公开(公告)号：US20110269809A1
公开(公告)日：2011-11-03
申请号：US13072872
申请日：2011-03-28
申请人： Xin-Jie Chu , Qingjie Ding , Nan Jiang , Jing Zhang , Zhuming Zhang
发明人： Xin-Jie Chu , Qingjie Ding , Nan Jiang , Jing Zhang , Zhuming Zhang
IPC分类号： A61K31/407 , A61P35/00 , C07D487/10
CPC分类号： C07D487/10
摘要： There are provided compounds of the formula wherein X, Y and R1 to R8 are as described herein and the enantiomers and pharmaceutically acceptable salts and esters thereof which compounds have anticancer activity.
摘要翻译：提供下式的化合物其中X，Y和R 1至R 8如本文所述，其化合物具有抗癌活性的对映异构体和药学上可接受的盐和酯。

13. 发明授权

US07705009B2 4-aminopyrimidine-5-thione derivatives 失效
标题翻译： 4-氨基嘧啶-5-硫酮衍生物
公开(公告)号：US07705009B2
公开(公告)日：2010-04-27
申请号：US11581529
申请日：2006-10-16
申请人： Qingjie Ding , Nan Jiang , Allen John Lovey
发明人： Qingjie Ding , Nan Jiang , Allen John Lovey
IPC分类号： C07D239/48 , C07D405/14 , C07D413/14 , A61K31/506
CPC分类号： C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D409/14 , C07D413/14
摘要： Novel 4-aminopyrimidine-5-thione derivatives are disclosed. These compounds inhibit cyclin-dependent kinases, in particular Cdk1, Cdk2 and Cdk4. These compounds and their pharmaceutically acceptable salts have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors. This invention is also directed to pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment or control of breast, lung, colon and prostate tumors.
摘要翻译：公开了新的4-氨基嘧啶-5-硫酮衍生物。这些化合物抑制细胞周期蛋白依赖性激酶，特别是Cdk1，Cdk2和Cdk4。这些化合物及其药学上可接受的盐具有抗增殖活性，并且可用于治疗或控制癌症，特别是实体瘤。本发明还涉及含有这些化合物的药物组合物以及治疗或控制癌症的方法，特别是乳腺癌，肺癌，结肠癌和前列腺肿瘤的治疗或控制。

14. 发明授权

US07405220B2 Pyrazolopyrimidines 失效
标题翻译：吡唑并嘧啶
公开(公告)号：US07405220B2
公开(公告)日：2008-07-29
申请号：US11136023
申请日：2005-05-24
申请人： Qingjie Ding , Nan Jiang , John Lawson Roberts
发明人： Qingjie Ding , Nan Jiang , John Lawson Roberts
IPC分类号： C07D239/70 , A61K31/4162
CPC分类号： C07D487/04
摘要： Novel pyrazolopyrimidines of formula (I): are discussed. These pyrazolopyrimidines are capable of inhibiting the activity of cyclin-dependent kinases, most particularly cyclin-dependent kinase 1 (Cdk1), cyclin-dependent kinase 2 (Cdk2), and cyclin-dependent kinase 4 (Cdk4) and are thus useful, inter alia, in the treatment or control of cancer, in particular solid tumors. This invention also provides pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment or control of breast, lung, colon and prostate tumors.
摘要翻译：讨论式（I）的新型吡唑并嘧啶：。这些吡唑并嘧啶能够抑制细胞周期蛋白依赖性激酶的活性，特别是细胞周期蛋白依赖性激酶1（Cdk1），细胞周期蛋白依赖性激酶2（Cdk2）和细胞周期蛋白依赖性激酶4（Cdk4）的活性，因此尤其有用，治疗或控制癌症，特别是实体瘤。本发明还提供含有这些化合物的药物组合物以及治疗或控制癌症的方法，特别是治疗或控制乳腺癌，肺癌，结肠癌和前列腺肿瘤的方法。

15. 发明授权

US08217044B2 Spiroindolinone pyrrolidines 失效
标题翻译：螺吲哚啉酮吡咯烷
公开(公告)号：US08217044B2
公开(公告)日：2012-07-10
申请号：US13072872
申请日：2011-03-28
申请人： Xin-Jie Chu , Qingjie Ding , Nan Jiang , Jing Zhang , Zhuming Zhang
发明人： Xin-Jie Chu , Qingjie Ding , Nan Jiang , Jing Zhang , Zhuming Zhang
IPC分类号： A61K31/4025 , A61K31/407 , A61K31/4155 , A61K31/4178 , A61K31/427 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , C07D209/54 , C07D401/14 , C07D403/14 , C07D405/14 , C07D417/14
CPC分类号： C07D487/10
摘要： There are provided compounds of the formula wherein X, Y and R1 to R8 are as described herein and the enantiomers and pharmaceutically acceptable salts and esters thereof which compounds have anticancer activity.
摘要翻译：提供下式的化合物其中X，Y和R 1至R 8如本文所述，其化合物具有抗癌活性的对映异构体和药学上可接受的盐和酯。

16. 发明授权

US08134001B2 Spiroindolinone derivatives 失效
标题翻译：螺吲哚啉酮衍生物
公开(公告)号：US08134001B2
公开(公告)日：2012-03-13
申请号：US12272870
申请日：2008-11-18
申请人： Qingjie Ding , Nan Jiang , Song Yang , Jing Zhang , Zhuming Zhang
发明人： Qingjie Ding , Nan Jiang , Song Yang , Jing Zhang , Zhuming Zhang
IPC分类号： C07D471/10 , A61K31/44
CPC分类号： C07D471/10
摘要： There are provided compounds of the formula and pharmaceutically acceptable salts and esters thereof wherein W, V, X, Y, A, R and R′ are as described herein. The compounds are useful as anticancer agents.
摘要翻译：提供下式的化合物及其药学上可接受的盐和酯，其中W，V，X，Y，A，R和R'如本文所述。这些化合物可用作抗癌剂。

17. 发明申请

US20110130398A1 SPIROINDOLINONE PYRROLIDINES 有权
标题翻译：螺吲哚啉酮吡咯烷酮
公开(公告)号：US20110130398A1
公开(公告)日：2011-06-02
申请号：US12939234
申请日：2010-11-04
申请人： David Joseph Bartkovitz , Xin-Jie Chu , Qingjie Ding , Bradford James Graves , Nan Jiang , Jing Zhang , Zhuming Zhang
发明人： David Joseph Bartkovitz , Xin-Jie Chu , Qingjie Ding , Bradford James Graves , Nan Jiang , Jing Zhang , Zhuming Zhang
IPC分类号： A61K31/5377 , C07D487/10 , A61K31/4045 , C07D401/14 , A61K31/4439 , C07D417/14 , A61K31/427 , C07D403/14 , A61K31/506 , C07D413/14 , A61K31/41 , A61K31/4155 , A61P35/00
CPC分类号： C07D487/10
摘要： There are provided compounds of the formula wherein X, Y and R1 to R8 are described herein along with the enantiomers, pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.
摘要翻译：提供下式的化合物其中X，Y和R 1至R 8与本文所述的对映异构体，其药学上可接受的盐和酯一起描述。这些化合物可用作抗癌剂。

18. 发明授权

US07615634B2 4-aminopyrimidine-5-one derivatives 失效
标题翻译： 4-氨基嘧啶-5-酮衍生物
公开(公告)号：US07615634B2
公开(公告)日：2009-11-10
申请号：US11471001
申请日：2006-06-20
申请人： David Joseph Bartkovitz , Xin-Jie Chu , Qingjie Ding , Nan Jiang , Allen John Lovey , John Anthony Moliterni , John Guilfoyle Mullin, Jr. , Binh Thanh Vu , Peter Michael Wovkulich
发明人： David Joseph Bartkovitz , Xin-Jie Chu , Qingjie Ding , Nan Jiang , Allen John Lovey , John Anthony Moliterni , John Guilfoyle Mullin, Jr. , Binh Thanh Vu , Peter Michael Wovkulich
IPC分类号： C07D239/47 , C07D239/48
CPC分类号： C07D239/47 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/14
摘要： Novel intermediate compounds are disclosed. These compounds are useful in the synthesis of 4-aminopyrimidine-5-one derivatives that inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). The 4-aminopyrimidine-5-one derivatives and their pharmaceutically acceptable salts have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors.
摘要翻译：公开了新的中间体化合物。这些化合物可用于合成抑制细胞周期蛋白依赖性激酶，特别是细胞周期蛋白依赖性激酶4（Cdk4）的4-氨基嘧啶-5-酮衍生物。 4-氨基嘧啶-5-酮衍生物及其药学上可接受的盐具有抗增殖活性，并且可用于治疗或控制癌症，特别是实体瘤。

19. 发明授权

US06818663B2 Diaminothiazoles 失效
标题翻译：二氨基噻唑
公开(公告)号：US06818663B2
公开(公告)日：2004-11-16
申请号：US10429551
申请日：2003-05-05
申请人： Xin-Jie Chu , Qingjie Ding , Nan Jiang , Kyungjin Kim , Allen John Lovey , Warren William McComas , John Guifoyle Mullin, Jr. , Jefferson Wright Tilley
发明人： Xin-Jie Chu , Qingjie Ding , Nan Jiang , Kyungjin Kim , Allen John Lovey , Warren William McComas , John Guifoyle Mullin, Jr. , Jefferson Wright Tilley
IPC分类号： C07D27742
CPC分类号： C07D417/06 , C07D277/42 , C07D417/12 , C07D417/14
摘要： The present invention is directed to novel diaminothiazoles of formula These compounds inhibit cyclin-dependent kinase 4 (Cdk4) and are selective against Cdk2 and Cdk1. These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors. This invention is also directed to pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment or control of breast, lung and colon and prostate tumors.
摘要翻译：本发明涉及新型式的二氨基噻唑，这些化合物抑制细胞周期蛋白依赖性激酶4（Cdk4），并且对Cdk2和Cdk1具有选择性。这些化合物及其药学上可接受的盐和酯具有抗增殖活性，并且可用于治疗或控制癌症，特别是实体瘤。本发明还涉及含有这些化合物的药物组合物以及治疗或控制癌症的方法，特别是乳腺癌，肺癌和结肠癌和前列腺肿瘤的治疗或控制。

20. 发明授权

US08354444B2 Substituted pyrrolidine-2-carboxamides 有权
标题翻译：取代的吡咯烷-2-甲酰胺
公开(公告)号：US08354444B2
公开(公告)日：2013-01-15
申请号：US12702402
申请日：2010-02-09
申请人： David Joseph Bartkovitz , Xin-Jie Chu , Qingjie Ding , Nan Jiang , Jin-Jun Liu , Tina Morgan Ross , Jing Zhang , Zhuming Zhang
发明人： David Joseph Bartkovitz , Xin-Jie Chu , Qingjie Ding , Nan Jiang , Jin-Jun Liu , Tina Morgan Ross , Jing Zhang , Zhuming Zhang
IPC分类号： A61K31/40 , C07D207/04
CPC分类号： C07D207/16 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/12 , C07D413/12 , C07D417/12
摘要： There are provided compounds of the formula wherein X, Y, R1, R2, R3, R3, R4, R5, R6 and R7 are as described herein and enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.
摘要翻译：提供下式的化合物其中X，Y，R 1，R 2，R 3，R 3，R 4，R 5，R 6和R 7如本文所述，其对映异构体及其药学上可接受的盐和酯。这些化合物可用作抗癌剂。

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