公开(公告)号：US08822519B2

公开(公告)日：2014-09-02

申请号：US13057737

申请日：2009-08-07

申请人： Chunhua Jin ,  Xiaoyu Liu ,  Zhenliang Chen ,  Xiaohe Zheng ,  Shoufeng Ming

发明人： Chunhua Jin ,  Xiaoyu Liu ,  Zhenliang Chen ,  Xiaohe Zheng ,  Shoufeng Ming

IPC分类号： C07D249/12 ,  A61K31/4196 ,  A61P3/00 ,  A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  A61P25/28 ,  A61P5/48 ,  A61P35/00

CPC分类号： C07D249/12 ,  A61K31/4196

摘要： The present invention provides a novel compound of formula I, which has an agitation effect on the peroxisome proliferator-activated receptor subtype δ (PPARδ), to a pharmaceutical composition comprising the compound, to a process for preparation of the compound and to use of the compound in the manufacture of a medicament for treating or preventing a disease which could be treated or prevented by activating PPARδ thereof, said disease is one or more from the group comprising metabolic syndrome, obesity, dyslipidemia, pathoglycemia, insulin resistance, senile dementia and tumors. The present invention also relates to a new intermediate used in the preparation of the novel compound and a process for preparation of the intermediate.

摘要翻译： 本发明提供了一种新颖的式I化合物，其对过氧化物酶体增殖物激活受体亚型δ（PPARδ）具有搅拌作用，包含该化合物的药物组合物，该化合物的制备方法和 化合物在制备用于治疗或预防可通过激活其PPARδ而被治疗或预防的疾病的药物中，所述疾病是代谢综合征，肥胖症，血脂异常，病态血糖，胰岛素抵抗，老年痴呆和肿瘤中的一种或多种 。 本发明还涉及用于制备新化合物的新中间体和中间体的制备方法。

公开(公告)号：US08623855B2

公开(公告)日：2014-01-07

申请号：US13389932

申请日：2010-08-09

申请人： Hua Bai ,  Xuyang Zhao ,  Xiaojie Xu ,  Xiaoyu Liu ,  Yuncai Zhang ,  Ying Chen ,  Xiaohe Zheng ,  Maojian Gu ,  Qifeng Zhu ,  Yong Zhang ,  Hairong Luo

发明人： Hua Bai ,  Xuyang Zhao ,  Xiaojie Xu ,  Xiaoyu Liu ,  Yuncai Zhang ,  Ying Chen ,  Xiaohe Zheng ,  Maojian Gu ,  Qifeng Zhu ,  Yong Zhang ,  Hairong Luo

IPC分类号： A01N43/00 ,  C07D205/00

CPC分类号： A61K31/397 ,  C07D205/08 ,  C07D263/26

摘要： Preparation of azetidinone compounds and medical use thereof are provided by the present invention. More particularly, azetidionne compounds, shown as formula (I), wherein R1, R2, R3, R4, R5 and R6 are defined in description, and preparation methods thereof are provided by the present invention. The compounds of the present invention can reduce the levels of total cholesterol (TC) and low density lipoprotein cholesterol (LDL-C) in plasma, and can be used as medicaments for reducing cholesterol in blood. Therefore the compounds of the present invention can be used to treat or prevent diseases of atherosclerosis, cacergasia of blood vessel, cardiac failure, coronary artery disease, angiocardiopathy, myocardial, angina, hyperlipoidemia and hypercholesteremia and the like. Preparation method of compounds of formula (I) and intermediate compounds are also provided by the present invention.

摘要翻译： 氮杂环丁酮化合物的制备及其医疗用途由本发明提供。 更具体地，式（I）所示的氮杂环丁烷化合物，其中R 1，R 2，R 3，R 4，R 5和R 6在描述中定义，其制备方法由本发明提供。 本发明化合物可以降低血浆中总胆固醇（TC）和低密度脂蛋白胆固醇（LDL-C）的水平，可用作降低血液中胆固醇的药物。 因此，本发明的化合物可用于治疗或预防动脉粥样硬化，血管紧张素，心力衰竭，冠状动脉疾病，心血管病，心肌，心绞痛，高脂血症和高胆固醇血症等疾病。 式（I）化合物和中间体化合物的制备方法也由本发明提供。

公开(公告)号：US20130089613A1

公开(公告)日：2013-04-11

申请号：US13704281

申请日：2011-06-18

申请人： Yaping Wang ,  Guojun Zheng ,  Peng Sun ,  Yi Li ,  Yingqiu Wu ,  Bin Liu ,  Xiaoyu Liu ,  Hua Bai ,  Hongyan Li ,  Xiaohe Zheng

发明人： Yaping Wang ,  Guojun Zheng ,  Peng Sun ,  Yi Li ,  Yingqiu Wu ,  Bin Liu ,  Xiaoyu Liu ,  Hua Bai ,  Hongyan Li ,  Xiaohe Zheng

IPC分类号： C07D263/32 ,  C07D413/10

CPC分类号： C07D263/32 ,  A61K31/439 ,  C07D277/24 ,  C07D413/10

摘要： Phenyl propanoic acid compounds having activating effect on peroxisome proliferator-activated receptors (PPARα,δ,γ) and a preparation method and uses thereof are provided in the present invention. The compounds can be used for treating or preventing diseases associated with peroxisome proliferator-activated receptors (PPARα,δ,γ).

摘要翻译： 在本发明中提供了对过氧化物酶体增殖物激活受体（PPARα，δ，γ）具有活化作用的苯基丙酸化合物及其制备方法和用途。 该化合物可用于治疗或预防与过氧化物酶体增殖物激活受体（PPARα，δ，γ）相关的疾病。

公开(公告)号：US09346770B2

公开(公告)日：2016-05-24

申请号：US13704281

申请日：2011-06-18

申请人： Yaping Wang ,  Guojun Zheng ,  Peng Sun ,  Yi Li ,  Yingqiu Wu ,  Bin Liu ,  Xiaoyu Liu ,  Hua Bai ,  Hongyan Li ,  Xiaohe Zheng

发明人： Yaping Wang ,  Guojun Zheng ,  Peng Sun ,  Yi Li ,  Yingqiu Wu ,  Bin Liu ,  Xiaoyu Liu ,  Hua Bai ,  Hongyan Li ,  Xiaohe Zheng

IPC分类号： C07D263/32 ,  A61K31/421 ,  C07D413/10 ,  C07D277/24 ,  A61K31/439

CPC分类号： C07D263/32 ,  A61K31/439 ,  C07D277/24 ,  C07D413/10

摘要： Phenyl propanoic acid compounds having activating effect on peroxisome proliferator-activated receptors (PPARα,δ,γ) and a preparation method and uses thereof are provided in the present invention. The compounds can be used for treating or preventing diseases associated with peroxisome proliferator-activated receptors (PPARα,δ,γ).

摘要翻译： 在本发明中提供了对过氧化物酶体增殖物激活受体（PPARα，δ，γ）具有活化作用的苯基丙酸化合物及其制备方法和用途。 该化合物可用于治疗或预防与过氧化物酶体增殖物激活受体（PPARα，δ，γ）相关的疾病。

公开(公告)号：US20110319458A1

公开(公告)日：2011-12-29

申请号：US13057737

申请日：2009-08-07

申请人： Chunhua Jin ,  Xiaoyu Liu ,  Zhenliang Chen ,  Xiaohe Zheng ,  Shoufeng Ming

发明人： Chunhua Jin ,  Xiaoyu Liu ,  Zhenliang Chen ,  Xiaohe Zheng ,  Shoufeng Ming

IPC分类号： A61K31/4196 ,  A61P3/00 ,  A61P3/04 ,  A61P35/00 ,  A61P3/10 ,  A61P5/48 ,  A61P25/28 ,  C07D249/12 ,  A61P3/06

CPC分类号： C07D249/12 ,  A61K31/4196

摘要： The present invention provides a novel compound of formula I, which has an agitation effect on the peroxisome proliferator-activated receptor subtype δ (PPARδ), to a pharmaceutical composition comprising the compound, to a process for preparation of the compound and to use of the compound in the manufacture of a medicament for treating or preventing a disease which could be treated or prevented by activating PPARδ thereof, said disease is one or more from the group comprising metabolic syndrome, obesity, dyslipidemia, pathoglycemia, insulin resistance, senile dementia and tumors. The present invention also relates to a new intermediate used in the preparation of the novel compound and a process for preparation of the intermediate.

摘要翻译： 本发明提供了一种新颖的式I化合物，其对过氧化物酶体增殖物激活受体亚型δ（PPARδ）具有搅拌作用，包含该化合物的药物组合物，该化合物的制备方法和 化合物在制备用于治疗或预防可通过激活其PPARδ而被治疗或预防的疾病的药物中，所述疾病是代谢综合征，肥胖症，血脂异常，病态血糖，胰岛素抵抗，老年痴呆和肿瘤中的一种或多种 。 本发明还涉及用于制备新化合物的新中间体和中间体的制备方法。

公开(公告)号：US20120208994A1

公开(公告)日：2012-08-16

申请号：US13389932

申请日：2010-08-09

申请人： Hua Bai ,  Xuyang Zhao ,  Xiaojie Xu ,  Xiaoyu Liu ,  Yuncai Zhang ,  Ying Chen ,  Xiaohe Zheng ,  Maojian Gu ,  Qifeng Zhu ,  Yong Zhang ,  Hairong Luo

发明人： Hua Bai ,  Xuyang Zhao ,  Xiaojie Xu ,  Xiaoyu Liu ,  Yuncai Zhang ,  Ying Chen ,  Xiaohe Zheng ,  Maojian Gu ,  Qifeng Zhu ,  Yong Zhang ,  Hairong Luo

IPC分类号： C07D205/08 ,  C07D263/26

CPC分类号： A61K31/397 ,  C07D205/08 ,  C07D263/26

摘要： Preparation of azetidinone compounds and medical use thereof are provided by the present invention. More particularly, azetidionne compounds, shown as formula (I), wherein R1, R2, R3, R4, R5 and R6 are defined in description, and preparation methods thereof are provided by the present invention. The compounds of the present invention can reduce the levels of total cholesterol (TC) and low density lipoprotein cholesterol (LDL-C) in plasma, and can be used as medicaments for reducing cholesterol in blood. Therefore the compounds of the present invention can be used to treat or prevent diseases of atherosclerosis, cacergasia of blood vessel, cardiac failure, coronary artery disease, angiocardiopathy, myocardial, angina, hyperlipoidemia and hypercholesteremia and the like. Preparation method of compounds of formula (I) and intermediate compounds are also provided by the present invention.

摘要翻译： 氮杂环丁酮化合物的制备及其医疗用途由本发明提供。 更具体地，式（I）所示的氮杂环丁烷化合物，其中R 1，R 2，R 3，R 4，R 5和R 6在描述中定义，其制备方法由本发明提供。 本发明化合物可以降低血浆中总胆固醇（TC）和低密度脂蛋白胆固醇（LDL-C）的水平，可用作降低血液中胆固醇的药物。 因此，本发明的化合物可用于治疗或预防动脉粥样硬化，血管紧张素，心力衰竭，冠状动脉疾病，心血管病，心肌，心绞痛，高脂血症和高胆固醇血症等疾病。 式（I）化合物和中间体化合物的制备方法也由本发明提供。