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公开(公告)号：US07485649B2
公开(公告)日：2009-02-03
申请号：US11794861
申请日：2006-01-05
IPC分类号： A61K31/4745 , C07D471/06
CPC分类号： A61K31/00
摘要： The instant invention provides for compounds which comprise fused pyrazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译： 本发明提供了包含抑制CHK1活性的稠合吡唑的化合物。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制CHK1活性的方法。
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公开(公告)号：US20090023767A1
公开(公告)日：2009-01-22
申请号：US12087375
申请日：2006-12-29
申请人： Edward J. Brnardic , Mark E. Fraley
发明人： Edward J. Brnardic , Mark E. Fraley
IPC分类号： A61K31/4745 , C07D471/02 , A61P35/00
CPC分类号： C07D471/04
摘要： The instant invention provides for compounds which comprise fused pyrazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译： 本发明提供了包含抑制CHK1活性的稠合吡唑的化合物。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制CHK1活性的方法。
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公开(公告)号：US20080280902A1
公开(公告)日：2008-11-13
申请号：US11795005
申请日：2006-01-24
IPC分类号： A61K31/5377 , C07D401/04 , A61K31/497 , C07D401/14 , A61P35/00 , C07D413/14 , A61K31/4709
CPC分类号： C07D401/14 , C07D401/04
摘要： The instant invention provides for compounds which comprise substituted quinolinones that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译： 本发明提供了包含抑制CHK1活性的取代的喹啉酮的化合物。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制CHK1活性的方法。
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公开(公告)号：US20080214594A1
公开(公告)日：2008-09-04
申请号：US11794861
申请日：2006-01-05
IPC分类号： A61K31/437 , C07D471/04 , A61P35/04
CPC分类号： A61K31/00
摘要： The instant invention provides for compounds which comprise fused pyrazoles that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译： 本发明提供了包含抑制CHK1活性的稠合吡唑的化合物。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制CHK1活性的方法。
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公开(公告)号：US07301028B2
公开(公告)日：2007-11-27
申请号：US10517576
申请日：2003-06-12
IPC分类号： C07D401/02 , C07D293/10 , C07D291/00 , C07D265/00 , C07D257/12 , C07D251/00 , C07D213/00 , C07D221/02 , C07D211/00 , C07D421/00 , C07D271/00 , C07D277/04 , C07D513/00 , A01N43/00 , A01N43/62 , A01N43/66 , A01N43/58 , A01N43/40 , A01N43/64 , A61K31/54 , A61K31/535 , A61K31/40
CPC分类号： C07D207/27 , C07D207/20
摘要： The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
摘要翻译： 本发明涉及可用于治疗细胞增殖性疾病，治疗与KSP驱动蛋白活性相关的疾病和用于抑制KSP驱动蛋白的二氢吡唑化合物。 本发明还涉及包含这些化合物的组合物，以及使用它们治疗哺乳动物癌症的方法。
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公开(公告)号：US20070254879A1
公开(公告)日：2007-11-01
申请号：US11789288
申请日：2007-04-24
申请人： Kenneth L. Arrington , Edward J. Brnardic , Vadim Y. Dudkin , Mark E. Fraley , Shaei Y. Huang , Cheng Wang
发明人： Kenneth L. Arrington , Edward J. Brnardic , Vadim Y. Dudkin , Mark E. Fraley , Shaei Y. Huang , Cheng Wang
IPC分类号： A61K31/5377 , A61K31/506 , A61K31/4745 , C07D471/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The instant invention provides for compounds which comprise substituted triazoloquinazolinones that inhibit CHK1 activity. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting CHK1 activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译： 本发明提供了包含抑制CHK1活性的取代的三唑并喹唑啉酮的化合物。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制CHK1活性的方法。
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公开(公告)号：US20170158698A1
公开(公告)日：2017-06-08
申请号：US15128782
申请日：2015-03-23
申请人： Helen MITCHELL , Mark E. FRALEY , Andrew J. COOKE , Craig A. STUMP , Xu-Fang ZHANG , Casey C. MCCOMAS , Kathy SCHIRRIPA , Melody MCWHERTER , Ping LIU , Dann PARKER , Chun Sing LI , Qinghua MAO , Merck Sharp & Dohme Corp.
发明人： Helen Mitchell , Mark E. Fraley , Andrew J. Cooke , Craig A. Stump , Xu-Fang Zhang , Casey C. McComas , Kathy Schirripa , Melody McWherter , Ping Liu , Dann Parker , Chun Sing Li , Qinghua Mao
IPC分类号： C07D487/04 , C07D231/40 , C07D417/12 , C07D401/04 , C07D417/14 , C07D471/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D413/12 , C07D413/14 , C07D277/46 , C07D403/14
CPC分类号： C07D487/04 , C07D231/40 , C07D277/46 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The present invention is directed to substituted five membered heteroaryl benzamide compounds of formula (I) (Formula (I)) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
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公开(公告)号：US20170114056A1
公开(公告)日：2017-04-27
申请号：US15129206
申请日：2015-03-23
申请人： Helen MITCHELL , Mark E. FRALEY , Andrew J. COOKE , Craig A. STUMP , Yi Heng CHEN , Douglas C. BESHORE , Xu-Fank ZHANG , Casey C. MCCOMAS , Kathy SCHIRRIPA , Melody MCWHERTER , Swati P. MERCER , Keith P. MOORE , Ping LIU , Harold B. WOOD , Chun Sing LI , Qinghua MAO , Merck Sharp & Dohme Corp.
发明人： Helen Mitchell , Mark E. Fraley , Andrew J. Cooke , Craig A. Stump , Yi- Heng Chen , Xu-Fang Zhang , Casey C. McComas , Kathy Schirripa , Melody McWherter , Swati P. Mercer , Keith P. Moore , Ping Liu , Harold B. Wood , Chun Sing Li , Qinghua Mao , Douglas C. Beshore
IPC分类号： C07D471/04 , C07D513/04
CPC分类号： C07D403/12 , C07D401/12 , C07D403/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention is directed to a bicyclic heteroaryl benzamide compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
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公开(公告)号：US20120149677A1
公开(公告)日：2012-06-14
申请号：US13391315
申请日：2010-08-16
申请人： Vadim Y. Dudkin , Mark E. Fraley , Cheng Wang , Robert M. Garbaccio , Douglas C. Beshore , Scott K. Kuduk , Jason W. Skudlarek
发明人： Vadim Y. Dudkin , Mark E. Fraley , Cheng Wang , Robert M. Garbaccio , Douglas C. Beshore , Scott K. Kuduk , Jason W. Skudlarek
IPC分类号： A61K31/4439 , C07D403/12 , C07D495/04 , C07D403/14 , C07D401/14 , C07D417/14 , A61K31/497 , A61K31/4709 , A61K31/506 , A61K31/519 , A61K31/444 , A61K31/541 , A61K31/438 , A61P25/00 , A61P25/18 , C07D401/12
CPC分类号： C07D417/14 , A61K31/4192 , A61K31/4439 , A61K31/444 , A61K31/454 , A61K31/4545 , A61K31/496 , A61K31/497 , A61K31/506 , C07D249/18 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/12 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/08 , C07D487/10 , C07D495/04 , C07D498/04
摘要： The present invention is directed to ether benzotriazole derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
摘要翻译： 本发明涉及作为代谢型谷氨酸受体，特别是mGluR2受体的增强剂的醚苯并三唑衍生物，其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及涉及代谢型谷氨酸受体的疾病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。
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公开(公告)号：US20120122911A1
公开(公告)日：2012-05-17
申请号：US13293186
申请日：2011-11-10
申请人： Ian M. Bell , Mark E. Fraley
发明人： Ian M. Bell , Mark E. Fraley
IPC分类号： A61K31/438 , A61P25/06 , C07D471/20
CPC分类号： A61K31/4545 , A61K31/435 , A61K31/438 , C07D471/10 , C07D471/20
摘要： The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
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