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公开(公告)号:US07524840B2
公开(公告)日:2009-04-28
申请号:US11244251
申请日:2005-10-05
申请人: Jin-Jun Liu , Kin-Chun Luk , Giacomo Pizzolato , Yi Ren , Kshitij Chhabilbhai Thakkar , Peter Michael Wovkulich , Zhuming Zhang
发明人: Jin-Jun Liu , Kin-Chun Luk , Giacomo Pizzolato , Yi Ren , Kshitij Chhabilbhai Thakkar , Peter Michael Wovkulich , Zhuming Zhang
IPC分类号: A61P35/00 , A61K31/55 , C07D487/04
CPC分类号: C07D487/04
摘要: The present invention provides compounds of formula I wherein R1, R2, R3, R4, and R5are described herein. The invention also provides syntheses for preparation of such compounds and pharmaceutical compositions containing them. The invention further provides methods for inhibiting kinases, in particular CDK2, for inhibiting angiogenesis, and for treating cancers, in particular breast, colon, prostate, and lung cancer.
摘要翻译: 本发明提供式I化合物,其中R1,R2,R3,R4和R5如本文所述。 本发明还提供了用于制备这些化合物和含有它们的药物组合物的合成。 本发明进一步提供了用于抑制激酶,特别是CDK2抑制血管发生,以及用于治疗癌症,特别是乳腺癌,结肠癌,前列腺癌和肺癌的方法。
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公开(公告)号:US20060079511A1
公开(公告)日:2006-04-13
申请号:US11244251
申请日:2005-10-05
申请人: Jin-Jun Liu , Kin-Chun Luk , Giacomo Pizzolato , Yi Ren , Kshitij Thakkar , Peter Wovkulich , Zhuming Zhang
发明人: Jin-Jun Liu , Kin-Chun Luk , Giacomo Pizzolato , Yi Ren , Kshitij Thakkar , Peter Wovkulich , Zhuming Zhang
IPC分类号: A61K31/551 , C07D487/12
CPC分类号: C07D487/04
摘要: The present invention provides compounds of formula I wherein R1, R2, R3, R4, and R5 are described herein. The invention also provides syntheses for preparation of such compounds and pharmaceutical compositions containing them. The invention further provides methods for inhibiting kinases, in particular CDK2, for inhibiting angiogenesis, and for treating cancers, in particular breast, colon, prostate, and lung cancer.
摘要翻译: 本发明提供式I化合物,其中R 1,R 2,R 3,R 4和R 4, 本文描述了R 5。 本发明还提供了用于制备这些化合物和含有它们的药物组合物的合成。 本发明进一步提供了用于抑制激酶,特别是CDK2抑制血管发生,以及用于治疗癌症,特别是乳腺癌,结肠癌,前列腺癌和肺癌的方法。
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公开(公告)号:US06916923B2
公开(公告)日:2005-07-12
申请号:US10827667
申请日:2004-04-19
IPC分类号: A61K31/41 , A61K31/5517 , A61P1/00 , A61P11/00 , A61P13/08 , A61P35/00 , C07D243/22 , C07D487/04 , C07D243/10
CPC分类号: C07D487/04 , C07D243/22
摘要: Disclosed is a novel method for synthesizing pyrazolobenzodiazepines of formula I using intermediates of formula Pyrazolobenzodiazepines of formula I are useful in the treatment and control of solid tumors.
摘要翻译: 公开了一种使用式I的吡唑并苯并二氮杂的新型方法,其中式Ⅰ的吡唑并苯并二氮杂可用于治疗和控制实体瘤。
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公开(公告)号:US07851626B2
公开(公告)日:2010-12-14
申请号:US11604558
申请日:2006-11-27
申请人: Qingjie Ding , Bradford James Graves , Norman Kong , Jin-Jun Liu , Allen John Lovey , Giacomo Pizzolato , John Lawson Roberts , Sung-Sau So , Binh Thanh Vu , Peter Michael Wovkulich
发明人: Qingjie Ding , Bradford James Graves , Norman Kong , Jin-Jun Liu , Allen John Lovey , Giacomo Pizzolato , John Lawson Roberts , Sung-Sau So , Binh Thanh Vu , Peter Michael Wovkulich
IPC分类号: C07D403/02 , C07D233/06 , A61K31/497 , A01N43/50
CPC分类号: C07D233/22 , C07D233/26 , C07D401/06 , C07D401/12 , C07D403/06 , C07D405/06 , C07D407/12 , C07D409/12 , C07D417/12 , C07D471/04 , C07D487/04
摘要: There is provided a compound of formula I and the pharmaceutically acceptable salts and esters thereof wherein X1, X2, R1, R2, R3, R4, R5 and R6 are herein described. The compounds exhibit activity as anticancer agents.
摘要翻译: 提供式I化合物及其药学上可接受的盐和酯,其中本文描述了X1,X2,R1,R2,R3,R4,R5和R6。 化合物表现出抗癌作用。
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公开(公告)号:US06440959B1
公开(公告)日:2002-08-27
申请号:US09548091
申请日:2000-04-12
申请人: Qingjie Ding , Jin-Jun Liu , Vincent Stewart Madison , Giacomo Pizzolato , Chung-Chen Wei , Peter Michael Wovkulich
发明人: Qingjie Ding , Jin-Jun Liu , Vincent Stewart Madison , Giacomo Pizzolato , Chung-Chen Wei , Peter Michael Wovkulich
IPC分类号: A61K31551
CPC分类号: C07D487/04 , C07D243/22
摘要: Disclosed are novel pyrazolobenzodiazepines having the formula and the pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 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, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing the compounds of formula I as well as intermediates useful in the preparation of the compounds of formula I.
摘要翻译: 公开了具有下式的新的吡唑并苯并二氮杂类及其药学上可接受的盐,其中R 1,R 2,R 3和R 4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,更特别地,治疗或控制乳腺癌,结肠癌,肺癌和前列腺肿瘤 。 还公开了含有式I化合物的药物组合物以及可用于制备式I化合物的中间体。
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公开(公告)号:US06838558B2
公开(公告)日:2005-01-04
申请号:US10122559
申请日:2002-04-15
IPC分类号: A61K31/41 , A61K31/5517 , A61P1/00 , A61P11/00 , A61P13/08 , A61P35/00 , C07D243/22 , C07D487/04 , C07D243/18 , C07D243/10
CPC分类号: C07D487/04 , C07D243/22
摘要: Disclosed are novel pyrazolobenzodiazepines having the formula These compounds are useful in the preparation of the pyrazolobenzodiazepines of formula I, which are useful in the treatment and control of solid tumors.
摘要翻译: 公开了具有下式的新型吡唑并苯并二氮杂:这些化合物可用于制备式I的吡唑并苯并二氮杂,其可用于治疗和控制实体瘤。
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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。
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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。
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公开(公告)号:US06504034B2
公开(公告)日:2003-01-07
申请号:US10043732
申请日:2002-01-10
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.
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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。
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