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11. 发明授权

US06252086B1 4-alkenyl-and 4-alkynyloxindoles 失效
标题翻译： 4-链烯基和4-炔氧基吲哚
公开(公告)号：US06252086B1
公开(公告)日：2001-06-26
申请号：US09549864
申请日：2000-04-14
申请人： Yi Chen , Apostolos Dermatakis , Kin-Chun Luk
发明人： Yi Chen , Apostolos Dermatakis , Kin-Chun Luk
IPC分类号： C07D40306
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14
摘要： Disclosed are novel 4-alkenyl- and 4-alkynyl oxindoles having the formula and the pharmaceutically acceptable salts thereof. These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. 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, more particularly, the treatment or control of breast and colon tumors. Also disclosed are pharmaceutical compositions containing the compounds of formula I and II as well as intermediates useful in the preparation of the compounds of formula I and II.
摘要翻译：公开了具有下式的新的4-烯基 - 和4-炔基羟基吲哚及其药学上可接受的盐。这些化合物抑制细胞周期蛋白依赖性激酶（CDK），特别是CDK2。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，更具体地，涉及乳腺癌和结肠肿瘤的治疗或控制。还公开了含有式I和II化合物的药物组合物以及可用于制备式I和II化合物的中间体。

12. 发明授权

US06303793B1 4-alkenyl-and 4-alkynyloxindoles 失效
标题翻译： 4-链烯基和4-炔氧基吲哚
公开(公告)号：US06303793B1
公开(公告)日：2001-10-16
申请号：US09566054
申请日：2000-05-05
申请人： Yi Chen , Apostolos Dermatakis , Jin-Jun Liu , Kin-Chun Luk
发明人： Yi Chen , Apostolos Dermatakis , Jin-Jun Liu , Kin-Chun Luk
IPC分类号： C07D20934
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14
摘要： Disclosed are novel 4-alkenyl- and 4-alkynyl oxindoles having the formula and the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, a, b, and X are as defined herein. These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. 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, more particularly, the treatment or control of breast and colon tumors. Also disclosed are pharmaceutical compositions containing the compounds of formula I and II as well as intermediates useful in the preparation of the compounds of formula I and II.
摘要翻译：公开了具有下式的新的4-烯基 - 和4-炔基羟基吲哚及其药学上可接受的盐，其中R1，R2，R3，a，b和X如本文所定义。这些化合物抑制细胞周期蛋白依赖性激酶（CDK），特别是CDK2。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，更具体地，涉及乳腺癌和结肠肿瘤的治疗或控制。还公开了含有式I和II化合物的药物组合物以及可用于制备式I和II化合物的中间体。

13. 发明授权

US6130239A 4-Alkenyl- and 4-alkynyloxindoles 失效
标题翻译： 4-烯基和4-炔氧基吲哚
公开(公告)号：US6130239A
公开(公告)日：2000-10-10
申请号：US464502
申请日：1999-12-15
申请人： Yi Chen , Wendy Lea Corbett , Apostolos Dermatakis , Jin-Jun Liu , Kin-Chun Luk , Paige E. Mahaney , Steven Gregory Mischke
发明人： Yi Chen , Wendy Lea Corbett , Apostolos Dermatakis , Jin-Jun Liu , Kin-Chun Luk , Paige E. Mahaney , Steven Gregory Mischke
IPC分类号： A61K31/404 , A61K31/4178 , A61K31/4409 , A61K31/454 , A61K31/5377 , A61P35/00 , A61P43/00 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D209/34
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14
摘要： Disclosed are novel 4-alkenyl- and 4-alkynyl oxindoles having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R.sup.1, R.sup.2, R.sup.3, a, b, and X are as defined herein. These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. 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, more particularly, the treatment or control of breast and colon tumors. Also disclosed are pharmaceutical compositions containing the compounds of formula I and II as well as intermediates useful in the preparation of the compounds of formula I and II.
摘要翻译：公开了具有下式的新的4-烯基 - 和4-炔基羟基吲哚及其药学上可接受的盐，其中R1，R2，R3，a，b和X如本文所定义。这些化合物抑制细胞周期蛋白依赖性激酶（CDK），特别是CDK2。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可用于治疗或控制细胞增殖性疾病，特别是癌症的抗增殖剂，更特别是乳腺癌和结肠肿瘤的治疗或控制。还公开了含有式I和II化合物的药物组合物以及可用于制备式I和II化合物的中间体。

14. 发明申请

US20050256154A1 4-Amino-thieno[3,2-c]pyridine-7-carboxylic acid amides 审中-公开
标题翻译： 4-氨基 - 噻吩并[3,2-c]吡啶-7-羧酸酰胺
公开(公告)号：US20050256154A1
公开(公告)日：2005-11-17
申请号：US11110614
申请日：2005-04-20
申请人： Kin-Chun Luk , Lee McDermott , Pamela Rossman , Peter Wovkulich , Zhuming Zhang
发明人： Kin-Chun Luk , Lee McDermott , Pamela Rossman , Peter Wovkulich , Zhuming Zhang
IPC分类号： A61K31/4743 , C07D498/02
CPC分类号： C07D495/04
摘要： Disclosed are novel 4-amino-thieno[3,2-c]pyridine-7-carboxylic acid amides, and their pharmaceutically acceptable salts and esters, that are selective inhibitors of KDR and/or FGFR kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular solid cancerous tumors of the breast, colon, lung and prostate. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer using these compounds.
摘要翻译：公开了新的4-氨基 - 噻吩并[3,2-c]吡啶-7-羧酸酰胺及其药学上可接受的盐和酯，其是KDR和/或FGFR激酶的选择性抑制剂。这些化合物及其药学上可接受的盐是可用于治疗或控制实体瘤，特别是乳腺，结肠，肺和前列腺的固体癌性肿瘤的抗增殖剂。还公开了含有这些化合物的药物组合物和使用这些化合物治疗癌症的方法。

15. 发明授权

US08673905B2 Imidazo pyrazines 有权
标题翻译：咪唑吡嗪
公开(公告)号：US08673905B2
公开(公告)日：2014-03-18
申请号：US13415868
申请日：2012-03-09
申请人： Kin-Chun Luk , Michael Soth
发明人： Kin-Chun Luk , Michael Soth
IPC分类号： A61K31/535 , A61K31/50 , C07D403/04 , C07D413/04 , C07D491/04
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/506
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 AML.
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AML的用途。

16. 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。

17. 发明申请

US20120238564A1 IMIDAZO PYRAZINES 有权
标题翻译：咪唑啉吡啶
公开(公告)号：US20120238564A1
公开(公告)日：2012-09-20
申请号：US13415868
申请日：2012-03-09
申请人： Kin-Chun Luk , Michael Soth
发明人： Kin-Chun Luk , Michael Soth
IPC分类号： A61K31/506 , A61K31/4985 , A61P35/00 , A61P35/02 , C07D487/04 , A61K31/5377
CPC分类号： C07D487/04 , A61K31/4985 , A61K31/506
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 AML.
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AML的用途。

18. 发明申请

US20120184508A1 PYRAZOLO PYRIMIDINES 失效
标题翻译：吡唑并吡啶
公开(公告)号：US20120184508A1
公开(公告)日：2012-07-19
申请号：US13347718
申请日：2012-01-11
申请人： Wenjian Liu , Kin-Chun Luk , Xiaohu Zhang
发明人： Wenjian Liu , Kin-Chun Luk , Xiaohu Zhang
IPC分类号： A61K31/695 , C07D487/04 , C07F7/10 , A61K31/5377 , A61K31/519
CPC分类号： C07D487/04
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。

19. 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。

20. 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。

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