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公开(公告)号：US08063085B2
公开(公告)日：2011-11-22
申请号：US12331538
申请日：2008-12-10
IPC分类号： A01N43/50 , A61K31/415 , C07D407/00
CPC分类号： C07D233/74 , C07D233/78 , C07D417/14
摘要： The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.
摘要翻译： 本发明涉及其制备方法的化合物及其使用方法。 该化合物可用于治疗以MEK多动症为特征的疾病。 因此，该化合物可用于治疗诸如癌症，认知和CNS疾病以及炎性/自身免疫性疾病的疾病。
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公开(公告)号：US20090048452A1
公开(公告)日：2009-02-19
申请号：US12186648
申请日：2008-08-06
IPC分类号： C07D403/06 , C07D409/14
CPC分类号： C07D403/06
摘要： This invention relates to compounds of formula I: or pharmaceutically acceptable salts thereof,wherein R1, R2, R3, R4, R5, and R6 are described in this application. These compounds inhibit the enzymes MEK 1 and MEK2, protein kinases that are components of the MAP kinase signal transduction pathway and as such the compounds will have anti-hyperproliferative cellular activity.
摘要翻译： 本发明涉及式I化合物或其药学上可接受的盐，其中本申请中描述了R1，R2，R3，R4，R5和R6。 这些化合物抑制作为MAP激酶信号转导途径成分的蛋白激酶MEK1和MEK2，因此这些化合物将具有抗过度增殖的细胞活性。
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公开(公告)号：US07557221B2
公开(公告)日：2009-07-07
申请号：US12186648
申请日：2008-08-06
IPC分类号： A61K31/4184 , C07D403/06
CPC分类号： C07D403/06
摘要： This invention relates to compounds of formula I: or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, and R6 are described in this application. These compounds inhibit the enzymes MEK 1 and MEK2, protein kinases that are components of the MAP kinase signal transduction pathway and as such the compounds will have anti-hyperproliferative cellular activity.
摘要翻译： 本发明涉及式I化合物或其药学上可接受的盐，其中本申请中描述了R1，R2，R3，R4，R5和R6。 这些化合物抑制作为MAP激酶信号转导途径成分的蛋白激酶MEK1和MEK2，因此这些化合物将具有抗过度增殖的细胞活性。
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公开(公告)号：US07612212B2
公开(公告)日：2009-11-03
申请号：US11657800
申请日：2007-01-25
申请人： Shaoqing Chen , Nicholas J. S. Huby , Norman Kong , Steven Gregory Mischke , John Anthony Moliterni , Hong Wang , Zhuming Zhang
发明人： Shaoqing Chen , Nicholas J. S. Huby , Norman Kong , Steven Gregory Mischke , John Anthony Moliterni , Hong Wang , Zhuming Zhang
IPC分类号： C07D233/02 , A61K31/4166
CPC分类号： C07D233/76 , C07D233/78 , C07D401/04 , C07D401/06 , C07D403/06 , C07D405/04 , C07D405/12 , C07D407/04 , C07D407/12 , C07D409/04 , C07D409/06 , C07D417/06
摘要： The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.
摘要翻译： 本发明涉及其制备方法的化合物及其使用方法。 该化合物可用于治疗以MEK多动症为特征的疾病。 因此，该化合物可用于治疗诸如癌症，认知和CNS疾病以及炎性/自身免疫性疾病的疾病。
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公开(公告)号：US20070197617A1
公开(公告)日：2007-08-23
申请号：US11657800
申请日：2007-01-25
申请人： Shaoqing Chen , Nicholas J. S. Huby , Norman Kong , Steven Gregory Mischke , John Anthony Moliterni , Hong Wang , Zhuming Zhang
发明人： Shaoqing Chen , Nicholas J. S. Huby , Norman Kong , Steven Gregory Mischke , John Anthony Moliterni , Hong Wang , Zhuming Zhang
IPC分类号： A61K31/4178 , A61K31/4166 , C07D403/02
CPC分类号： C07D233/76 , C07D233/78 , C07D401/04 , C07D401/06 , C07D403/06 , C07D405/04 , C07D405/12 , C07D407/04 , C07D407/12 , C07D409/04 , C07D409/06 , C07D417/06
摘要： The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.
摘要翻译： 本发明涉及其制备方法的化合物及其使用方法。 该化合物可用于治疗以MEK多动症为特征的疾病。 因此，该化合物可用于治疗诸如癌症，认知和CNS疾病以及炎性/自身免疫性疾病的疾病。
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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：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：US07371869B2
公开(公告)日：2008-05-13
申请号：US11225950
申请日：2005-09-14
申请人： Robert Alan Goodnow, Jr. , Nicholas J. S. Huby , Norman Kong , Lee Apostle McDermott , John Anthony Moliterni , Zhuming Zhang
发明人： Robert Alan Goodnow, Jr. , Nicholas J. S. Huby , Norman Kong , Lee Apostle McDermott , John Anthony Moliterni , Zhuming Zhang
IPC分类号： A61K31/427 , C07D409/12
CPC分类号： C07D417/14 , C07D417/12
摘要： The present invention relates to compounds of the formula which are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as, cancer, cognative and CNS disorders and inflammatory/autoimmune diseases.
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