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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:US07615634B2
公开(公告)日:2009-11-10
申请号:US11471001
申请日:2006-06-20
申请人: David Joseph Bartkovitz , Xin-Jie Chu , Qingjie Ding , Nan Jiang , Allen John Lovey , John Anthony Moliterni , John Guilfoyle Mullin, Jr. , Binh Thanh Vu , Peter Michael Wovkulich
发明人: David Joseph Bartkovitz , Xin-Jie Chu , Qingjie Ding , Nan Jiang , Allen John Lovey , John Anthony Moliterni , John Guilfoyle Mullin, Jr. , Binh Thanh Vu , Peter Michael Wovkulich
IPC分类号: C07D239/47 , C07D239/48
CPC分类号: C07D239/47 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/14
摘要: Novel intermediate compounds are disclosed. These compounds are useful in the synthesis of 4-aminopyrimidine-5-one derivatives that inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). The 4-aminopyrimidine-5-one derivatives and their pharmaceutically acceptable salts have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors.
摘要翻译: 公开了新的中间体化合物。 这些化合物可用于合成抑制细胞周期蛋白依赖性激酶,特别是细胞周期蛋白依赖性激酶4(Cdk4)的4-氨基嘧啶-5-酮衍生物。 4-氨基嘧啶-5-酮衍生物及其药学上可接受的盐具有抗增殖活性,并且可用于治疗或控制癌症,特别是实体瘤。
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公开(公告)号:US07157455B2
公开(公告)日:2007-01-02
申请号:US10770379
申请日:2004-02-02
申请人: David Joseph Bartkovitz , Xin-Jie Chu , Qingjie Ding , Nan Jiang , Allen John Lovey , John Anthony Moliterni , John Guilfoyle Mullin, Jr. , Binh Thanh Vu , Peter Michael Wovkulich
发明人: David Joseph Bartkovitz , Xin-Jie Chu , Qingjie Ding , Nan Jiang , Allen John Lovey , John Anthony Moliterni , John Guilfoyle Mullin, Jr. , Binh Thanh Vu , Peter Michael Wovkulich
IPC分类号: C07D401/12 , C07D403/12 , C07D413/12 , A61K31/4468 , C07D239/42
CPC分类号: C07D239/47 , C07D239/48 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/14
摘要: Novel 4-aminopyrimidine-5-one derivatives are disclosed. These compounds inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). 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 4-aminopyrimidine-5-one derivatives.
摘要翻译: 公开了新的4-氨基嘧啶-5-酮衍生物。 这些化合物抑制细胞周期蛋白依赖性激酶,特别是细胞周期蛋白依赖性激酶4(Cdk4)。 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4-氨基嘧啶-5-酮衍生物的中间体。
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公开(公告)号:US20090111789A1
公开(公告)日:2009-04-30
申请号:US12248095
申请日:2008-10-09
申请人: David Joseph Bartkovitz , Jianping Cai , Xin-Jie Chu , Hongju Li , Allen John Lovey , Binh Thanh Vu , Chunlin Zhao
发明人: David Joseph Bartkovitz , Jianping Cai , Xin-Jie Chu , Hongju Li , Allen John Lovey , Binh Thanh Vu , Chunlin Zhao
IPC分类号: C07D401/14 , C07D401/04 , C07D403/02 , C07D403/14 , C07D411/14 , C07D413/14 , C07D417/14 , A61K31/5513 , A61K31/551 , A61K31/5395 , A61K31/5377 , A61K31/445 , A61K31/444 , A61K31/496
CPC分类号: C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/10
摘要: There are provided compounds of the formula or the pharmaceutically acceptable salts thereof, wherein X, Y, Z, V1, V2, R1, R2, R3, R4 and R5 are herein described. These compounds are useful as anticancer agents.
摘要翻译: 提供下式的化合物或其药学上可接受的盐,其中本文描述了X,Y,Z,V1,V2,R 1,R 2,R 3,R 4和R 5。 这些化合物可用作抗癌剂。
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公开(公告)号:US08513239B2
公开(公告)日:2013-08-20
申请号:US12248095
申请日:2008-10-09
申请人: David Joseph Bartkovitz , Jianping Cai , Xin-Jie Chu , Hongju Li , Allen John Lovey , Binh Thanh Vu , Chunlin Zhao
发明人: David Joseph Bartkovitz , Jianping Cai , Xin-Jie Chu , Hongju Li , Allen John Lovey , Binh Thanh Vu , Chunlin Zhao
IPC分类号: A61K31/55 , A61K31/03 , A61K31/44 , A61K31/535 , A61K31/505 , C07D243/06 , C07D243/14 , C07D279/10 , C07D413/08 , C07D403/08 , C07D239/02 , C07D215/02
CPC分类号: C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D417/14 , C07D471/10
摘要: There are provided compounds of the formula or the pharmaceutically acceptable salts thereof, wherein X, Y, Z, V1, V2, R1, R2, R3, R4 and R5 are herein described. These compounds are useful as anticancer agents.
摘要翻译: 提供下式的化合物或其药学上可接受的盐,其中本文描述了X,Y,Z,V1,V2,R 1,R 2,R 3,R 4和R 5。 这些化合物可用作抗癌药。
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公开(公告)号:US06818663B2
公开(公告)日:2004-11-16
申请号:US10429551
申请日:2003-05-05
申请人: Xin-Jie Chu , Qingjie Ding , Nan Jiang , Kyungjin Kim , Allen John Lovey , Warren William McComas , John Guifoyle Mullin, Jr. , Jefferson Wright Tilley
发明人: Xin-Jie Chu , Qingjie Ding , Nan Jiang , Kyungjin Kim , Allen John Lovey , Warren William McComas , John Guifoyle Mullin, Jr. , Jefferson Wright Tilley
IPC分类号: C07D27742
CPC分类号: C07D417/06 , C07D277/42 , C07D417/12 , C07D417/14
摘要: The present invention is directed to novel diaminothiazoles of formula These compounds inhibit cyclin-dependent kinase 4 (Cdk4) and are selective against Cdk2 and Cdk1. 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 and colon and prostate tumors.
摘要翻译: 本发明涉及新型式的二氨基噻唑,这些化合物抑制细胞周期蛋白依赖性激酶4(Cdk4),并且对Cdk2和Cdk1具有选择性。 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,肺癌和结肠癌和前列腺肿瘤的治疗或控制。
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公开(公告)号:US07423053B2
公开(公告)日:2008-09-09
申请号:US11170636
申请日:2005-06-29
申请人: Li Chen , Xin-Jie Chu , Allen John Lovey , Chunlin Zhao
发明人: Li Chen , Xin-Jie Chu , Allen John Lovey , Chunlin Zhao
IPC分类号: A61K31/4523 , C07D417/02
CPC分类号: C07D277/20 , C07D277/42 , C07D417/12
摘要: Novel 4-aminothiazole derivatives 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 4-aminothiazole derivatives.
摘要翻译: 公开了新的4-氨基噻唑衍生物。 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4-氨基噻唑衍生物的中间体。
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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:US20130059834A1
公开(公告)日:2013-03-07
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: A61K31/4985 , C07D491/107 , A61K31/5377 , C07D471/04 , C07D495/04 , A61P29/00 , A61P31/00 , A61P37/02 , A61P37/06 , A61P9/00 , A61P3/10 , A61P19/02 , A61P11/06 , A61P25/00 , A61P25/28 , A61P17/06 , A61P17/00 , A61P35/00 , A61P35/02 , A61P1/04 , C07D487/04
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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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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