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1. 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。

2. 发明授权

US07115740B2 Pyrimido compounds having antiproliferative activity 失效
标题翻译：具有抗增殖活性的嘧啶化合物
公开(公告)号：US07115740B2
公开(公告)日：2006-10-03
申请号：US10817697
申请日：2004-04-02
申请人： Yi Chen , Apostolos Dermatakis , Jin-Jun Liu , Kin-Chun Luk , Christophe Michoud , Pamela Loreen Rossman
发明人： Yi Chen , Apostolos Dermatakis , Jin-Jun Liu , Kin-Chun Luk , Christophe Michoud , Pamela Loreen Rossman
IPC分类号： C07D487/04 , C07D239/47 , C07D407/12 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR and FGFR kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer.
摘要翻译：公开了作为KDR和FGFR激酶的选择性抑制剂的新型嘧啶化合物。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，特别是乳腺癌，结肠癌，肺癌和前列腺肿瘤的抗增殖剂。还公开了含有这些化合物的药物组合物和治疗癌症的方法。

3. 发明授权

US06504034B2 Naphthostyrils 失效
公开(公告)号：US06504034B2
公开(公告)日：2003-01-07
申请号：US10043732
申请日：2002-01-10
申请人： Yi Chen , Apostolos Dermatakis , Frederick Martin Konzelmann , Jin-Jun Liu , Kin-Chun Luk
发明人： Yi Chen , Apostolos Dermatakis , Frederick Martin Konzelmann , Jin-Jun Liu , Kin-Chun Luk
IPC分类号： C07D40302
CPC分类号： C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14
摘要： Disclosed are novel naphthostyrils of formula These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts and esters are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing such compounds, methods for the treatment and/or prevention of cancer using such compositions, and intermediates useful in the preparation of the compounds of formula I.

4. 发明授权

US06307056B1 4-aryloxindoles 失效
标题翻译： 4-芳氧基吲哚
公开(公告)号：US06307056B1
公开(公告)日：2001-10-23
申请号：US09464466
申请日：1999-12-15
申请人： Wendy Lea Corbett , Kin-Chun Luk , Paige E. Mahaney
发明人： Wendy Lea Corbett , Kin-Chun Luk , Paige E. Mahaney
IPC分类号： C07D40302
CPC分类号： C07D409/14 , C07D403/06 , C07D403/14 , C07D405/14
摘要： Disclosed are 4-aryloxindoles that inhibit or modulate protein kinases, in particular JNK protein kinases. These compounds and their pharmaceutically acceptable salts, and prodrugs of said compounds, are useful as anti-inflammatory agents, particularly useful in the treatment of rheumatoid arthritis. Also disclosed are pharmaceutical compositions containing the foregoing compounds, as well as methods for the treatment and/or control of inflammation, particularly in the treatment or control of rheumatoid arthritis, using said compounds.
摘要翻译：公开了抑制或调节蛋白激酶，特别是JNK蛋白激酶的4-芳氧基吲哚。这些化合物及其药学上可接受的盐和所述化合物的前药可用作抗炎剂，特别可用于治疗类风湿性关节炎。还公开了含有前述化合物的药物组合物，以及使用所述化合物治疗和/或控制炎症，特别是治疗或控制类风湿性关节炎的方法。

5. 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。

6. 发明授权

US06313310B1 4-and 5-alkynyloxindoles and 4-and 5-alkenyloxindoles 失效
标题翻译： 4-和5-炔氧基吲哚和4-和5-烯氧基吲哚
公开(公告)号：US06313310B1
公开(公告)日：2001-11-06
申请号：US09464238
申请日：1999-12-15
申请人： Kin-Chun Luk , Paige E. Mahaney , Steven Gregory Mischke
发明人： Kin-Chun Luk , Paige E. Mahaney , Steven Gregory Mischke
IPC分类号： C07D40302
CPC分类号： C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14
摘要： Disclosed are 4- and 5-alkynyloxindoles as well as 4- and 5-alkenyloxindoles that inhibit or modulate protein kinases, in particular JNK protein kinases. The compounds of the invention and their pharmaceutically acceptable salts, and prodrugs of said compounds, are useful as anti-inflammatory agents, particularly useful in the treatment of rheumatoid arthritis. Also disclosed are pharmaceutical compositions containing the foregoing compounds, methods for the treatment and/or control of inflammation, particularly in the treatment or control of rheumatoid arthritis using these compounds, as well as intermediates useful in the preparation of compounds of the invention.
摘要翻译：公开了抑制或调节蛋白激酶，特别是JNK蛋白激酶的4-和5-炔氧基吲哚以及4-和5-链烯氧基吲哚。本发明的化合物及其药学上可接受的盐和所述化合物的前药可用作抗炎剂，特别可用于治疗类风湿性关节炎。还公开了含有前述化合物的药物组合物，用于治疗和/或控制炎症的方法，特别是在使用这些化合物治疗或控制类风湿性关节炎的药物组合物中，以及可用于制备本发明化合物的中间体。

7. 发明授权

US06531598B1 Naphthostyrils 失效
标题翻译：萘妥拉明
公开(公告)号：US06531598B1
公开(公告)日：2003-03-11
申请号：US10224022
申请日：2002-08-20
申请人： Apostolos Dermatakis , Jin-Jun Liu , Kin-Chun Luk
发明人： Apostolos Dermatakis , Jin-Jun Liu , Kin-Chun Luk
IPC分类号： C07D41314
CPC分类号： C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14
摘要： Disclosed are novel naphthostyrils of formula These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts and esters are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing such compounds, methods for the treatment and/or prevention of cancer using such compositions, and intermediates useful in the preparation of the compounds of formula I.
摘要翻译：公开了新颖的式萘普通抗坏血酸的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酯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。还公开了含有这些化合物的药物组合物，使用这种组合物治疗和/或预防癌症的方法，以及可用于制备式I化合物的中间体。

8. 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。

9. 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。

10. 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。

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