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1. 发明申请

US20090318408A1 HALO-SUBSTITUTED PYRIMIDODIAZEPINES 失效
标题翻译： HALO取代的吡咯烷酮
公开(公告)号：US20090318408A1
公开(公告)日：2009-12-24
申请号：US12485108
申请日：2009-06-16
申请人： Jianping Cai , Shaoqing Chen , Xin-Jie Chu , Kin-Chun Luk , Steven Gregory Mischke , Hongmao Sun , Peter Michael Wovkulich
发明人： Jianping Cai , Shaoqing Chen , Xin-Jie Chu , Kin-Chun Luk , Steven Gregory Mischke , Hongmao Sun , Peter Michael Wovkulich
IPC分类号： A61K31/551 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides PLK1 inhibitor compounds of formula I: useful in the treatment or control of cell proliferative disorders, particularly oncological disorders. These compounds and formulations containing such compounds may be useful in the treatment or control of solid tumors, such as, for example, breast, colon, lung and prostate tumors and other oncological diseases such as non-Hodgkin's lymphomas. Also provided are intermediate compounds useful in the synthesis of compounds of formula I.
摘要翻译：本发明提供式I的PLK1抑制剂化合物：可用于治疗或控制细胞增殖性疾病，特别是肿瘤疾病。含有这些化合物的这些化合物和制剂可用于治疗或控制实体瘤，例如乳腺癌，结肠癌，肺癌和前列腺肿瘤以及其它肿瘤疾病如非霍奇金淋巴瘤。还提供了可用于合成式I化合物的中间体化合物。

2. 发明授权

US08003785B2 Halo-substituted pyrimidodiazepines 失效
标题翻译：卤代取代的嘧啶并二氮杂
公开(公告)号：US08003785B2
公开(公告)日：2011-08-23
申请号：US12485108
申请日：2009-06-16
申请人： Jianping Cai , Shaoqing Chen , Xin-Jie Chu , Kin-Chun Luk , Steven Gregory Mischke , Hongmao Sun , Peter Michael Wovkulich
发明人： Jianping Cai , Shaoqing Chen , Xin-Jie Chu , Kin-Chun Luk , Steven Gregory Mischke , Hongmao Sun , Peter Michael Wovkulich
IPC分类号： C07D487/04
CPC分类号： C07D487/04
摘要： The present invention provides PLK1 inhibitor compounds of formula I: useful in the treatment or control of cell proliferative disorders, particularly oncological disorders. These compounds and formulations containing such compounds may be useful in the treatment or control of solid tumors, such as, for example, breast, colon, lung and prostate tumors and other oncological diseases such as non-Hodgkin's lymphomas. Also provided are intermediate compounds useful in the synthesis of compounds of formula I.
摘要翻译：本发明提供式I的PLK1抑制剂化合物：可用于治疗或控制细胞增殖性疾病，特别是肿瘤疾病。含有这些化合物的这些化合物和制剂可用于治疗或控制实体瘤，例如乳腺癌，结肠癌，肺癌和前列腺肿瘤以及其它肿瘤疾病如非霍奇金淋巴瘤。还提供了可用于合成式I化合物的中间体化合物。

3. 发明授权

US08044213B2 Thiazolyl-benzimidazoles 失效
标题翻译：噻唑基 - 苯并咪唑
公开(公告)号：US08044213B2
公开(公告)日：2011-10-25
申请号：US12634771
申请日：2009-12-10
申请人： Jianping Cai , Shaoqing Chen , Yi Chen , Xin-Jie Chu , Robert Alan Goodnow, Jr. , Kang Le , Kin-Chun Luk , Steven Gregory Mischke , Peter Michael Wovkulich
发明人： Jianping Cai , Shaoqing Chen , Yi Chen , Xin-Jie Chu , Robert Alan Goodnow, Jr. , Kang Le , Kin-Chun Luk , Steven Gregory Mischke , Peter Michael Wovkulich
IPC分类号： A61K31/427 , C07D417/04 , C07D417/14
CPC分类号： C07D417/04 , C07D417/14
摘要： The invention is directed to compounds of formula (1) and pharmaceutically acceptable salts thereof, methods for the preparation thereof, and methods of use thereof.
摘要翻译：本发明涉及式（1）的化合物及其药学上可接受的盐，其制备方法及其使用方法。

4. 发明申请

US20100160308A1 Thiazolyl-Benzimidazoles 失效
标题翻译：噻唑基 - 苯并咪唑
公开(公告)号：US20100160308A1
公开(公告)日：2010-06-24
申请号：US12634771
申请日：2009-12-10
申请人： Jianping Cai , Shaoqing Chen , Yi Chen , Xin-Jie Chu , Robert Alan Goodnow, JR. , Kang Le , Kin-Chun Luk , Steven Gregory Mischke , Peter Michael Wovkulich
发明人： Jianping Cai , Shaoqing Chen , Yi Chen , Xin-Jie Chu , Robert Alan Goodnow, JR. , Kang Le , Kin-Chun Luk , Steven Gregory Mischke , Peter Michael Wovkulich
IPC分类号： A61K31/5377 , A61K31/496 , C07D413/14 , C07D417/14 , A61P35/00
CPC分类号： C07D417/04 , C07D417/14
摘要： The invention is directed to compounds of formula (1) and pharmaceutically acceptable salts thereof, methods for the preparation thereof, and methods of use thereof.
摘要翻译：本发明涉及式（1）的化合物及其药学上可接受的盐，其制备方法及其用途。

5. 发明申请

US20120184542A1 PYRIDO PYRIMIDINES 审中-公开
标题翻译：吡咯烷基吡啶
公开(公告)号：US20120184542A1
公开(公告)日：2012-07-19
申请号：US13348665
申请日：2012-01-12
申请人： Kevin Anderson , Yi Chen , Zhi Chen , Kin-Chun Luk , Pamela Loreen Rossman , Hongmao Sun , Peter Michael Wovkulich
发明人： Kevin Anderson , Yi Chen , Zhi Chen , Kin-Chun Luk , Pamela Loreen Rossman , Hongmao Sun , Peter Michael Wovkulich
IPC分类号： A61K31/519 , A61K31/5377 , A61P25/00 , A61K31/5386 , A61P35/00 , A61P25/28 , C07D471/04 , C07D519/00
CPC分类号： C07D471/04
摘要： Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of proliferative diseases, including cancer, Down syndrome or early onset Alzheimer's disease.
摘要翻译：本发明描述了式及其药学上可接受的盐的化合物，以及含有所述化合物及其药学上可接受的盐的药物组合物，以及所述化合物和药物组合物用于治疗，控制或改善增殖性疾病（包括癌症）Down 综合征或早发性阿尔茨海默氏病。

6. 发明申请

US20090048274A1 PYRAZOLO[3,4-d]PYRIMIDINE DERIVATIVES 有权
标题翻译：吡唑并[3,4-d]吡嗪衍生物
公开(公告)号：US20090048274A1
公开(公告)日：2009-02-19
申请号：US12175562
申请日：2008-07-18
申请人： David Joseph Bartkovitz , Xin-Jie Chu , Kin-Chun Luk
发明人： David Joseph Bartkovitz , Xin-Jie Chu , Kin-Chun Luk
IPC分类号： A61K31/519 , C07D487/04 , A61P35/00
CPC分类号： C07D487/04
摘要： Disclosed are novel pyrazolo[3,4-d]pyrimidine derivatives that are inhibitors of Raf kinase. These compounds and their pharmaceutically-acceptable salts and esters are anti-proliferative agents useful in the treatment or control of proliferative disorders such as solid tumors, in particular breast tumor, colon tumor, lung tumor, prostate tumor, and melanoma. Also disclosed are a composition and a unit dose formulation comprising such a compound, or a pharmaceutically-acceptable salt or ester thereof, methods for making such compounds, and methods for using such compounds, or their pharmaceutically-acceptable salts or esters, in the treatment of proliferative disorders.
摘要翻译：公开了作为Raf激酶抑制剂的新型吡唑并[3,4-d]嘧啶衍生物。这些化合物及其药学上可接受的盐和酯是可用于治疗或控制增殖性疾病如固体肿瘤，特别是乳腺肿瘤，结肠肿瘤，肺肿瘤，前列腺肿瘤和黑素瘤的抗增殖剂。还公开了包含这种化合物或其药学上可接受的盐或酯的组合物和单位剂量制剂，以及用于制备此类化合物的方法，以及在治疗中使用这些化合物或其药学上可接受的盐或酯的方法的增殖性疾病。

7. 发明申请

US20070060607A1 4-amino-thieno[3,2-c] pyridine-7-carboxylic acid derivatives 审中-公开
标题翻译： 4-氨基 - 噻吩并[3,2-c]吡啶-7-羧酸衍生物
公开(公告)号：US20070060607A1
公开(公告)日：2007-03-15
申请号：US11516905
申请日：2006-09-07
申请人： David Bartkovitz , Yi Chen , Xin-Jie Chu , Kin-Chun Luk , Pamela Rossman , Sung-Sau So
发明人： David Bartkovitz , Yi Chen , Xin-Jie Chu , Kin-Chun Luk , Pamela Rossman , Sung-Sau So
IPC分类号： A61K31/4743 , C07D498/02
CPC分类号： C07D495/04 , Y02P20/582
摘要： The present invention relates to compounds of the formula medicaments containing them and the use of these compounds as pharmaceutically active agents. The compounds exhibit activity as Raf kinase inhibitors and therefore may be useful for the treatment of diseases mediated by said kinases, especially as anticancer agents.
摘要翻译：本发明涉及含有它们的式药物的化合物以及这些化合物作为药物活性剂的用途。该化合物表现出作为Raf激酶抑制剂的活性，因此可用于治疗由所述激酶介导的疾病，特别是作为抗癌剂。

8. 发明授权

US07994321B2 Substituted thieno[3,2-C]pyridine-7-carboxylic acid derivatives 有权
标题翻译：取代的噻吩并[3,2-C]吡啶-7-羧酸衍生物
公开(公告)号：US07994321B2
公开(公告)日：2011-08-09
申请号：US11780603
申请日：2007-07-20
申请人： David Joseph Bartkovitz , Yi Chen , Xin-Jie Chu , Kin-Chun Luk
发明人： David Joseph Bartkovitz , Yi Chen , Xin-Jie Chu , Kin-Chun Luk
IPC分类号： C07D513/04 , A61K31/4365
CPC分类号： A61K31/4365 , C07D495/04
摘要： There are provided compounds of the formula wherein R1, R2, R3, X, Y, Q, Ring A and Ring B are as described. The compounds exhibit activity as anticancer agents.
摘要翻译：提供下式的化合物其中R1，R2，R3，X，Y，Q，环A和环B如上所述。化合物表现出抗癌作用。

9. 发明授权

US6153634A 4,5-azolo-oxindoles 失效
标题翻译： 4,5-azo-oxindoles
公开(公告)号：US6153634A
公开(公告)日：2000-11-28
申请号：US464507
申请日：1999-12-15
申请人： Kin-Chun Luk , Christophe Michoud , Steven Gregory Mischke
发明人： Kin-Chun Luk , Christophe Michoud , Steven Gregory Mischke
IPC分类号： C07D403/06 , C07D487/04 , C07D498/04 , C07D513/04 , A61K31/4188 , A61K31/424 , A61K31/429
CPC分类号： C07D403/06 , C07D487/04 , C07D513/04 , C09B23/04
摘要： Disclosed are novel 4,5-azolo-oxindoles having the formula ##STR1## These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. Thus, these compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing these compounds, and methods for the treatment and/or prevention of cancer, particularly in the treatment or control of solid tumors using these compounds, as well as intermediates useful in the preparation of compounds of formula I.
摘要翻译：公开了具有下式的新的4,5-azo-oxindoles这些化合物抑制细胞周期蛋白依赖性激酶（CDK），特别是CDK2。因此，这些化合物及其药学上可接受的盐和所述化合物的前药是用于治疗或控制细胞增殖性疾病，特别是癌症的抗增殖剂。还公开了含有这些化合物的药物组合物，以及用于治疗和/或预防癌症的方法，特别是使用这些化合物治疗或控制实体瘤的方法，以及可用于制备式I化合物的中间体。

10. 发明授权

US07968554B2 Pyrazolo[3,4-d]pyrimidine derivatives 有权
标题翻译：吡唑并[3,4-d]嘧啶衍生物
公开(公告)号：US07968554B2
公开(公告)日：2011-06-28
申请号：US12175562
申请日：2008-07-18
申请人： David Joseph Bartkovitz , Xin-Jie Chu , Kin-Chun Luk
发明人： David Joseph Bartkovitz , Xin-Jie Chu , Kin-Chun Luk
IPC分类号： C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： Disclosed are novel pyrazolo[3,4-d]pyrimidine derivatives that are inhibitors of Raf kinase. These compounds and their pharmaceutically-acceptable salts and esters are anti-proliferative agents useful in the treatment or control of proliferative disorders such as solid tumors, in particular breast tumor, colon tumor, lung tumor, prostate tumor, and melanoma. Also disclosed are a composition and a unit dose formulation comprising such a compound, or a pharmaceutically-acceptable salt or ester thereof, methods for making such compounds, and methods for using such compounds, or their pharmaceutically-acceptable salts or esters, in the treatment of proliferative disorders.
摘要翻译：公开了作为Raf激酶抑制剂的新型吡唑并[3,4-d]嘧啶衍生物。这些化合物及其药学上可接受的盐和酯是可用于治疗或控制增殖性疾病如固体肿瘤，特别是乳腺肿瘤，结肠肿瘤，肺肿瘤，前列腺肿瘤和黑素瘤的抗增殖剂。还公开了包含这种化合物或其药学上可接受的盐或酯的组合物和单位剂量制剂，以及用于制备这些化合物的方法，以及在治疗中使用这些化合物或其药学上可接受的盐或酯的方法的增殖性疾病。

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