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公开(公告)号:US20110071147A1
公开(公告)日:2011-03-24
申请号:US12952251
申请日:2010-11-23
申请人: Kin-Chun Luk , Lee Apostle McDermott , Pamela Loreen Rossman , Peter Michael Wovkulich , Zhuming Zhang
发明人: Kin-Chun Luk , Lee Apostle McDermott , Pamela Loreen Rossman , Peter Michael Wovkulich , Zhuming Zhang
IPC分类号: A61K31/5355 , C07D471/04 , C07D413/14 , A61K31/4375 , A61P35/00
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。
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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。
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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: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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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。
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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。
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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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公开(公告)号:US08481540B2
公开(公告)日:2013-07-09
申请号:US13207481
申请日:2011-08-11
申请人: Steven Joseph Berthel , Roland Joseph Billedeau , Christine E. Brotherton-Pleiss , Fariborz Firooznia , Stephen Deems Gabriel , Xiaochun Han , Ramona Hilgenkamp , Saul Jaime-Figueroa , Buelent Kocer , Francisco Javier Lopez-Tapia , Yan Lou , Lucja Orzechowski , Timothy D. Owens , Jenny Tan , Peter Michael Wovkulich
发明人: Steven Joseph Berthel , Roland Joseph Billedeau , Christine E. Brotherton-Pleiss , Fariborz Firooznia , Stephen Deems Gabriel , Xiaochun Han , Ramona Hilgenkamp , Saul Jaime-Figueroa , Buelent Kocer , Francisco Javier Lopez-Tapia , Yan Lou , Lucja Orzechowski , Timothy D. Owens , Jenny Tan , Peter Michael Wovkulich
IPC分类号: A01N43/58 , A61K31/50 , C07D237/00
CPC分类号: C07D401/14 , C07D403/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D487/04 , C07D487/08 , C07D487/10 , C07D491/107
摘要: This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula I: wherein, variables X, R, and Y4, are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.
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公开(公告)号:US07423051B2
公开(公告)日:2008-09-09
申请号:US11165912
申请日:2005-06-24
IPC分类号: A61K31/4545 , C07D401/12
CPC分类号: C07D213/73
摘要: Novel 2,6-diaminopyridine derivatives of formula wherein R1 and R2 are as defined below, are disclosed. These compounds inhibit cyclin-dependent kinases. 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, colon and prostate tumors. Also disclosed are intermediates useful in the preparation of these novel 2,6-diaminopyridine derivatives.
摘要翻译: 公开了下述新的2,6-二氨基吡啶衍生物,其中R 1和R 2定义如下。 这些化合物抑制细胞周期蛋白依赖性激酶。 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,结肠癌和前列腺肿瘤的治疗或控制。 还公开了可用于制备这些新型2,6-二氨基吡啶衍生物的中间体。
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公开(公告)号:US08658646B2
公开(公告)日:2014-02-25
申请号:US13600863
申请日:2012-08-31
申请人: Shaoqing Chen , Javier de Vicente Fidalgo , Matthew Michael Hamilton , Johannes Cornelius Hermann , Joshua Kennedy-Smith , Hongju Li , Allen John Lovey , Matthew C. Lucas , Kin-Chun Thomas Luk , Stephen M. Lynch , Counde O'yang , Fernando Padilla , Ryan Craig Schoenfeld , Achyutharao Sidduri , Michael Soth , Ce Wang , Peter Michael Wovkulich , Xiaohu Zhang
发明人: Shaoqing Chen , Javier de Vicente Fidalgo , Matthew Michael Hamilton , Johannes Cornelius Hermann , Joshua Kennedy-Smith , Hongju Li , Allen John Lovey , Matthew C. Lucas , Kin-Chun Thomas Luk , Stephen M. Lynch , Counde O'yang , Fernando Padilla , Ryan Craig Schoenfeld , Achyutharao Sidduri , Michael Soth , Ce Wang , Peter Michael Wovkulich , Xiaohu Zhang
IPC分类号: A61K31/495
CPC分类号: C07D487/04
摘要: The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.
摘要翻译: 本发明涉及式I的新型吡咯并吡嗪衍生物的用途,其中所述变量如本文所述定义,其抑制JAK和SYK并且可用于治疗自身免疫和炎性疾病。
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