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。

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：US09555003B2

公开(公告)日：2017-01-31

申请号：US14111323

申请日：2012-04-10

申请人： Maojian Gu ,  Qilan Zheng ,  Chao Xu ,  Ning Li ,  Guixian Chen ,  Lan Zheng ,  Min Wang ,  Lintao Jiang

发明人： Maojian Gu ,  Qilan Zheng ,  Chao Xu ,  Ning Li ,  Guixian Chen ,  Lan Zheng ,  Min Wang ,  Lintao Jiang

IPC分类号： A61K9/28 ,  A61K31/133 ,  A61K31/4965 ,  A61K31/496 ,  A61K31/4409 ,  A61K9/20 ,  A61K9/24

CPC分类号： A61K9/286 ,  A61K9/2086 ,  A61K9/209 ,  A61K9/28 ,  A61K9/284 ,  A61K9/2866 ,  A61K9/2886 ,  A61K31/133 ,  A61K31/4409 ,  A61K31/496 ,  A61K31/4965 ,  A61K2300/00

摘要： Provided is an oral solid preparation of a compound anti-tubercular drug, wherein the active ingredients are rifampicin, isoniazid, pyrazinamide and ethambutol hydrochloride. The compound oral solid preparation is a coated tablet with coated core or a coated three-layer tablet, wherein the two active ingredients rifampicin and isoniazid do not come to contact with each other directly. The compound oral solid preparation not only improves the stability of the compound preparation, but also improves the bioavailability of rifampicin.

摘要翻译： 本发明提供化合物抗结核药物的口服固体制剂，其中活性成分为利福平，异烟肼，吡嗪酰胺和盐酸乙胺丁醇。 复合口服固体制剂是具有包衣核心或涂覆的三层片剂的包衣片剂，其中两种活性成分利福平和异烟肼不直接相互接触。 复方口服固体制剂不仅提高了化合物制剂的稳定性，而且提高了利福平的生物利用度。

公开(公告)号：US20140127294A1

公开(公告)日：2014-05-08

申请号：US14111323

申请日：2012-04-10

申请人： Maojian Gu ,  Qilan Zheng ,  Chao Xu ,  Ning Li ,  Guixian Chen ,  Lan Zheng ,  Min Wang ,  Lintao Jiang

发明人： Maojian Gu ,  Qilan Zheng ,  Chao Xu ,  Ning Li ,  Guixian Chen ,  Lan Zheng ,  Min Wang ,  Lintao Jiang

IPC分类号： A61K9/28 ,  A61K31/133 ,  A61K31/4965 ,  A61K31/496 ,  A61K31/4409

CPC分类号： A61K9/286 ,  A61K9/2086 ,  A61K9/209 ,  A61K9/28 ,  A61K9/284 ,  A61K9/2866 ,  A61K9/2886 ,  A61K31/133 ,  A61K31/4409 ,  A61K31/496 ,  A61K31/4965 ,  A61K2300/00

摘要： Provided is an oral solid preparation of a compound anti-tubercular drug, wherein the active ingredients are rifampicin, isoniazid, pyrazinamide and ethambutol hydrochloride. The compound oral solid preparation is a coated tablet with coated core or a coated three-layer tablet, wherein the two active ingredients rifampicin and isoniazid do not contact directly. The compound oral solid preparation not only improves the stability of the compound preparation, but also improves the bioavailability of rifampicin.

摘要翻译： 本发明提供化合物抗结核药物的口服固体制剂，其中活性成分为利福平，异烟肼，吡嗪酰胺和盐酸乙胺丁醇。 复合口服固体制剂是具有包衣核心或涂层三层片剂的包衣片剂，其中两种活性成分利福平和异烟肼不直接接触。 复方口服固体制剂不仅提高了化合物制剂的稳定性，而且提高了利福平的生物利用度。