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![Derivatives of 6[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one having antitumor activity](/abs-image/US/2013/08/06/US08501731B2/abs.jpg.150x150.jpg)
1.发明授权Derivatives of 6[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one having antitumor activity 有权具有抗肿瘤活性的6 [3-（三氟甲基）苯基]哒嗪-3（2H） - 酮的衍生物公开(公告)号：US08501731B2
公开(公告)日：2013-08-06
申请号：US12933104
申请日：2009-03-18
申请人： Youhong Hu , Liguang Lou , Shijun Lin , Hongbing Zhao , Zhende Liu , Yongping Xu , Bo Chao
发明人： Youhong Hu , Liguang Lou , Shijun Lin , Hongbing Zhao , Zhende Liu , Yongping Xu , Bo Chao
IPC分类号： C07D403/10 , C07D401/10 , C07D277/04 , C07D237/04 , C07D413/10 , A61K31/55 , A61K31/501 , A61P35/00
CPC分类号： C07D237/14 , C07D401/10 , C07D401/12 , C07D403/10 , C07D403/12 , C07D413/10 , C07D417/10 , Y02P20/582
摘要： The present invention relates to a class of pyridazinones of formula I, which comprises 6-[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one as a mother nucleus, the preparation method thereof and the use thereof in manufacturing medicaments against tumors, especially liver cancer.
摘要翻译： 本发明涉及一类式I的哒嗪酮，其包含作为母核的6- [3-（三氟甲基）苯基]哒嗪-3（2H） - 酮，其制备方法及其在制备药物中的用途 肿瘤，特别是肝癌。
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公开(公告)号：US20110112061A1
公开(公告)日：2011-05-12
申请号：US12933104
申请日：2009-03-18
申请人： Youhong Hu , Liguang Lou , Shijun Lin , Hongbing Zhao , Zhende Liu , Yongping Xu , Bo Chao
发明人： Youhong Hu , Liguang Lou , Shijun Lin , Hongbing Zhao , Zhende Liu , Yongping Xu , Bo Chao
IPC分类号： A61K31/501 , C07D403/10 , C07D413/10 , C07D237/14 , A61K31/55 , A61K31/5377 , A61K31/50 , A61P35/00
CPC分类号： C07D237/14 , C07D401/10 , C07D401/12 , C07D403/10 , C07D403/12 , C07D413/10 , C07D417/10 , Y02P20/582
摘要： The present invention relates to a class of pyridazinones of formula I, which comprises 6-[3-(trifluoromethyl)phenyl]pyridazin-3(2H)-one as a mother nucleus, the preparation method thereof and the use thereof in manufacturing medicaments against tumors, especially liver cancer.
摘要翻译： 本发明涉及一类式I的哒嗪酮，其包含作为母核的6- [3-（三氟甲基）苯基]哒嗪-3（2H） - 酮，其制备方法及其在制备药物中的用途 肿瘤，特别是肝癌。
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3.发明申请Substituted arylalcanoic acid derivatives as ppar pan agonists with potent antihyperglycemic and antihyperlipidemic activity 审中-公开取代的芳基烷酸衍生物作为具有有效的抗高血糖和抗高血脂活性的ppar pan激动剂公开(公告)号：US20080051321A1
公开(公告)日：2008-02-28
申请号：US11882417
申请日：2007-08-01
申请人： Xian-Ping Lu , Zhibin Li , Chenzhong Liao , Leming Shi , Zhende Liu , Baoshun Ma , Zhiqiang Ning , Song Shan , Tuo Deng
发明人： Xian-Ping Lu , Zhibin Li , Chenzhong Liao , Leming Shi , Zhende Liu , Baoshun Ma , Zhiqiang Ning , Song Shan , Tuo Deng
IPC分类号： A61K31/403 , A61K31/4439 , A61K38/28 , A61P3/00 , A61P3/10 , A61P7/12 , A61P9/00 , C07D209/56 , C07D401/12
CPC分类号： C07D401/12 , A61K31/185 , A61K31/335 , A61K31/403 , A61K31/422 , A61K31/426 , A61K31/538 , A61K31/5415 , A61K31/55 , C07D209/86 , C07D213/50
摘要： Disclosed is the preparation and pharmaceutical use of substituted arylalcanoic acid derivatives of Formula I, wherein ring A, ring B, R1, R2, R3, R4, R5, X, Alk1, Alk2, Ar1, and Ar2 are as defined in the specification. These compounds, as selective agonists activating peroxisome proliferator-activated receptors (PPAR), in particularly the RXR/PPARalpha, RXR/PPARgamma, and RXR/PPARdelta heterodimers, are useful in the treatment and/or prevention of type 2 diabetes and associated metabolic syndrome such as hypertension, obesity, insulin resistance, hyperlipidemia, hyperglycemia, hypercholesterolemia, atherosclerosis, coronary artery disease, and other cardiovascular disorders with improved side effects profile commonly associated with conventional PPARgamma agonists.
摘要翻译： 公开了式I的取代的芳基烷酸衍生物的制备和药物用途，其中环A，环B，R 1，R 2，R 3， R 4，R 4，R 5，X，Alk 1，Alk 2，Ar 1， ＆lt; / SUP＆gt;和Ar 2是如说明书中所定义的。 这些化合物作为激活过氧化物酶体增殖物激活受体（PPAR）的选择性激动剂，特别是RXR /PPARα，RXR /PPARγ和RXR /PPARδ异二聚体，可用于治疗和/或预防2型糖尿病和相关代谢综合征 例如高血压，肥胖症，胰岛素抵抗，高脂血症，高血糖症，高胆固醇血症，动脉粥样硬化，冠状动脉疾病和其它具有改善的与常规PPARγ激动剂相关的副作用的心血管疾病。
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4.发明授权Substituted arylalcanoic acid derivatives as PPAR pan agonists with potent antihyperglycemic and antihyperlipidemic activity 有权取代的芳基烷酸衍生物作为具有有效的抗高血糖和抗高血脂活性的PPAR泛激动剂公开(公告)号：US07268157B2
公开(公告)日：2007-09-11
申请号：US10715622
申请日：2003-11-18
申请人： Xian-Ping Lu , Zhibin Li , Chenzhong Liao , Leming Shi , Zhende Liu , Baoshun Ma , Zhiqiang Ning , Song Shan , Tuo Deng
发明人： Xian-Ping Lu , Zhibin Li , Chenzhong Liao , Leming Shi , Zhende Liu , Baoshun Ma , Zhiqiang Ning , Song Shan , Tuo Deng
IPC分类号： A61P3/00 , A61K31/403 , C07D209/82
CPC分类号： C07D401/12 , A61K31/185 , A61K31/335 , A61K31/403 , A61K31/422 , A61K31/426 , A61K31/538 , A61K31/5415 , A61K31/55 , C07D209/86 , C07D213/50
摘要： Disclosed is the preparation and pharmaceutical use of substituted arylalcanoic acid derivatives of Formula I, wherein ring A, ring B, R1, R2, R3, R4, R5, X, Alk1, Alk2, Ar1, and Ar2 are as defined in the specification. These compounds, as selective agonists activating peroxisome proliferator-activated receptors (PPAR), in particularly the RXR/PPARalpha, RXR/PPARgamma, and RXR/PPARdelta heterodimers, are useful in the treatment and/or prevention of type 2 diabetes and associated metabolic syndrome such as hypertension, obesity, insulin resistance, hyperlipidemia, hyperglycemia, hypercholesterolemia, atherosclerosis, coronary artery disease, and other cardiovascular disorders with improved side effects profile commonly associated with conventional PPARgamma agonists.
摘要翻译： 公开了式I的取代的芳基烷酸衍生物的制备和药物用途，其中环A，环B，R 1，R 2，R 3， R 4，R 4，R 5，X，Alk 1，Alk 2，Ar 1， ＆lt; / SUP＆gt;和Ar 2是如说明书中所定义的。 这些化合物作为激活过氧化物酶体增殖物激活受体（PPAR）的选择性激动剂，特别是RXR /PPARα，RXR /PPARγ和RXR /PPARδ异二聚体，可用于治疗和/或预防2型糖尿病和相关代谢综合征 例如高血压，肥胖症，胰岛素抵抗，高脂血症，高血糖症，高胆固醇血症，动脉粥样硬化，冠状动脉疾病和其它具有改善的与常规PPARγ激动剂相关的副作用的心血管疾病。
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5.发明申请Noncyclic 1,3-Dicarbonyl compounds as dual PPAR agonists with potent antihyperglycemic and antihyperlipidemic activity 审中-公开非环状1,3-二羰基化合物作为具有有效的抗高血糖和抗高血脂活性的双重PPAR激动剂公开(公告)号：US20070142427A1
公开(公告)日：2007-06-21
申请号：US11653385
申请日：2007-01-16
申请人： Xian-Ping Lu , Zhibin Li , Chenzhong Liao , Leming Shi , Zhende Liu , Zhiqiang Ning , Song Shan , Tuo Deng , Baoshun Ma
发明人： Xian-Ping Lu , Zhibin Li , Chenzhong Liao , Leming Shi , Zhende Liu , Zhiqiang Ning , Song Shan , Tuo Deng , Baoshun Ma
IPC分类号： A61K31/4745 , A61K31/4743 , A61K31/4741 , C07D471/02
CPC分类号： C07C59/68 , A61K31/185 , A61K31/335 , A61K31/403 , A61K31/422 , A61K31/426 , A61K31/538 , A61K31/5415 , A61K31/55 , C07C17/16 , C07C37/18 , C07C45/71 , C07C59/72 , C07C67/30 , C07C67/303 , C07C67/343 , C07C69/734 , C07C235/34 , C07C2602/10 , C07D215/20 , C07C19/01 , C07C47/575 , C07C39/17
摘要： Disclosed are the preparation and pharmaceutical use of novel noncyclic 1,3-dicarbonyl compounds of formula I, wherein ring A, ring B, R1, R2, R3, R4, R5, X, Y, Z, Q, Ar and n are as defined in the specification. These compounds, as peroxisome proliferator-activated receptor (PPAR) dual agonists for both RXR/PPARgamma and RXR/PPARalpha heterodimers, are useful in the treatment and/or prevention of type 2 diabetes and associated metabolic syndrome such as hypertension, obesity, insulin resistance, hyperlipidemia, hyperglycemia, hypercholesterolemia, atherosclerosis, coronary artery disease, and other cardiovascular disorders.
摘要翻译： 公开了式I的新型非环状1,3-二羰基化合物的制备和药物用途，其中环A，环B，R 1，R 2，R SUP R 3，R 4，R 5，X，Y，Z，Q，Ar和n如说明书中所定义。 这些化合物作为RXR /PPARγ和RXR /PPARα异源二聚体的过氧化物酶体增殖物激活受体（PPAR）双重激动剂，可用于治疗和/或预防2型糖尿病和相关的代谢综合征，如高血压，肥胖，胰岛素抵抗 ，高脂血症，高血糖症，高胆固醇血症，动脉粥样硬化，冠状动脉疾病和其他心血管疾病。
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6.发明授权Noncyclic 1,3-dicarbonyl compounds as dual PPAR agonists with potent antihyperglycemic and antihyperlipidemic activity 失效非环状1,3-二羰基化合物作为具有有效的抗高血糖和抗高脂血症活性的双重PPAR激动剂公开(公告)号：US07192970B2
公开(公告)日：2007-03-20
申请号：US10713722
申请日：2003-11-14
申请人： Xian-Ping Lu , Zhibin Li , Chenzhong Liao , Leming Shi , Zhende Liu , Zhiqiang Ning , Song Shan , Tuo Deng , Baoshun Ma
发明人： Xian-Ping Lu , Zhibin Li , Chenzhong Liao , Leming Shi , Zhende Liu , Zhiqiang Ning , Song Shan , Tuo Deng , Baoshun Ma
IPC分类号： A61K31/47 , C07D215/38 , C07D215/44
CPC分类号： C07C59/68 , A61K31/185 , A61K31/335 , A61K31/403 , A61K31/422 , A61K31/426 , A61K31/538 , A61K31/5415 , A61K31/55 , C07C17/16 , C07C37/18 , C07C45/71 , C07C59/72 , C07C67/30 , C07C67/303 , C07C67/343 , C07C69/734 , C07C235/34 , C07C2602/10 , C07D215/20 , C07C19/01 , C07C47/575 , C07C39/17
摘要： Disclosed are the preparation and pharmaceutical use of novel noncyclic 1,3-dicarbonyl compounds of formula I, wherein ring A, ring B, R1, R2, R3, R4, R5, X, Y, Z, Q, Ar and n are as defined in the specification. These compounds, as peroxisome proliferator-activated receptor (PPAR) dual agonists for both RXR/PPARgamma and RXR/PPARalpha heterodimers, are useful in the treatment and/or prevention of type 2 diabetes and associated metabolic syndrome such as hypertension, obesity, insulin resistance, hyperlipidemia, hyperglycemia, hypercholesterolemia, atherosclerosis, coronary artery disease, and other cardiovascular disorders
摘要翻译： 公开了式I的新型非环状1,3-二羰基化合物的制备和药物用途，其中环A，环B，R 1，R 2，R SUP R 3，R 4，R 5，X，Y，Z，Q，Ar和n如说明书中所定义。 这些化合物作为RXR /PPARγ和RXR /PPARα异源二聚体的过氧化物酶体增殖物激活受体（PPAR）双重激动剂，可用于治疗和/或预防2型糖尿病和相关的代谢综合征，如高血压，肥胖，胰岛素抵抗 ，高脂血症，高血糖症，高胆固醇血症，动脉粥样硬化，冠状动脉疾病和其他心血管疾病
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