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21. 发明授权

US06825204B2 N-substituted 3-hydroxy-4-pyridinones and pharmaceuticals containing thereof 失效
标题翻译： N-取代的3-羟基-4-吡啶酮和含有它们的药物
公开(公告)号：US06825204B2
公开(公告)日：2004-11-30
申请号：US10358835
申请日：2003-02-05
申请人： Shuang Liu
发明人： Shuang Liu
IPC分类号： A61K3144
CPC分类号： C07D213/89 , A61K51/0476 , C07B2200/05 , C07D401/12 , C07D409/12
摘要： N-substituted 3-hydroxy-4-pyridinones and metal chelates, methods of preparing N-substituted 3-hydroxy-4-pyridinones and metal chelates, and pharmaceutical compositions containing new N-substituted 3-hydroxy-4-pyridinones and/or their metal chelates. Use of N-substituted 3-hydroxy-4-pyridinones and their metal chelates as pharmaceutical agents for the treatment of diseases, such as parasitic and viral infections, conditions associated with inflammation and infection, and conditions mediated by cell-proliferation or collagen formation.
摘要翻译： N-取代的3-羟基-4-吡啶酮和金属螯合物，N-取代的3-羟基-4-吡啶酮和金属螯合物的制备方法，以及含有新的N-取代的3-羟基-4-吡啶酮和/或它们的N- 金属螯合物。 N-取代的3-羟基-4-吡啶酮及其金属螯合物作为用于治疗疾病如寄生虫病毒和病毒感染，与炎症和感染相关的疾病以及由细胞增殖或胶原形成介导的病症的药物的用途。

22. 发明授权

US5879659A Ternary radiopharmaceutical complexes 失效
标题翻译：三元放射性药物复合物
公开(公告)号：US5879659A
公开(公告)日：1999-03-09
申请号：US808699
申请日：1997-02-28
申请人： David Scott Edwards , Shuang Liu
发明人： David Scott Edwards , Shuang Liu
IPC分类号： A61B20060101 , A61K20060101 , A61K51/08 , A61M20060101 , A61N20060101 , A61K51/00 , A61K38/12 , A61M36/14 , C07F5/00
CPC分类号： A61K51/088 , A61K51/082 , A61K2123/00
摘要： This invention relates to novel radiopharmaceuticals which are useful as imaging agents for the diagnosis of cardiovascular disorders, infectious disease and cancer, and to kits useful for their preparation. The radiopharmaceuticals of this invention are comprised of a transition metal radionuclide, a transition metal chelator, a biologically active group connected to said chelator, a first ancillary ligand, a second ancillary ligand capable of stabilizing the radiopharmaceutical, optionally having a linking group between said chelator and said biologically active group. Preferred radiopharmaceuticals of this invention have the formula:�(Q).sub.d' L.sub.n --C.sub.h' !.sub.x --M.sub.t (A.sub.L1).sub.y (A.sub.L2).sub.z,wherein the shown variables are as defined herein.
摘要翻译：本发明涉及可用作诊断心血管疾病，感染性疾病和癌症的成像剂的新型放射性药物，以及可用于其制备的试剂盒。本发明的放射性药物包括过渡金属放射性核素，过渡金属螯合剂，与所述螯合剂连接的生物活性基团，第一辅助配体，能稳定放射性药物的第二辅助配体，任选地在所述螯合剂之间具有连接基团并表示生物活性组。本发明优选的放射性药物具有下式：[（Q）d'Ln-Ch'] x-Mt（AL1）y（AL2）z，其中所示变量如本文所定义。

23. 发明授权

US08575114B2 SGLT-2 inhibitors, methods of making them, and uses thereof 失效
标题翻译： SGLT-2抑制剂，其制备方法及其应用
公开(公告)号：US08575114B2
公开(公告)日：2013-11-05
申请号：US13052171
申请日：2011-03-21
申请人： Shuang Liu , Cheng Guo
发明人： Shuang Liu , Cheng Guo
IPC分类号： A01N43/04 , A61K31/70 , C07H5/04 , C07H5/06
CPC分类号： A61K31/706
摘要： The present invention relates to compounds which are inhibitors of sodium dependent glucose co-transporter-2 (SGLT-2). These compounds are used in the treatment of various disorders, including diabetes, impaired glucose tolerance, insulin resistance, retinopathy, nephropathy, neuropathy, cataracts, hyperglycemia, hyperinsulinemia, hyperchlolesterolemia, elevated blood level of free fatty acids or glycerol, hyperlipidemia, hypertriglyceridemia, obesity, wound healing, tissue ischemia, atherosclerosis, and hypertension. These compounds and compositions are also useful for treating and preventing kidney stones, hyperuricemia, gout, and hyponatremia. Methods of making these compounds are also described in the present invention.
摘要翻译：本发明涉及作为钠依赖性葡萄糖共转运体-2（SGLT-2）抑制剂的化合物。这些化合物用于治疗各种疾病，包括糖尿病，葡萄糖耐量降低，胰岛素抵抗，视网膜病变，肾病，神经病，白内障，高血糖症，高胰岛素血症，高胆固醇血症，游离脂肪酸或甘油血液水平升高，高脂血症，高甘油三酯血症，肥胖伤口愈合，组织缺血，动脉粥样硬化和高血压。这些化合物和组合物还可用于治疗和预防肾结石，高尿酸血症，痛风和低钠血症。制备这些化合物的方法也在本发明中描述。

24. 发明授权

US07956050B2 Aryl- and heteroaryl-substituted tetrahydrobenzazepines and use thereof to block reuptake of norepinephrine, dopamine, and serotonin 有权
标题翻译：芳基和杂芳基取代的四氢苯并氮杂及其用于阻断去甲肾上腺素，多巴胺和5-羟色胺的再摄取
公开(公告)号：US07956050B2
公开(公告)日：2011-06-07
申请号：US11487884
申请日：2006-07-17
申请人： Bruce F. Molino , Shuang Liu , Aruna Sambandam , Peter R. Guzzo , Min Hu , Congxiang Zha , Kassoum Nacro , David D. Manning , Matthew L. Isherwood , Kristen N. Fleming , Wenge Cui , Richard E. Olson
发明人： Bruce F. Molino , Shuang Liu , Aruna Sambandam , Peter R. Guzzo , Min Hu , Congxiang Zha , Kassoum Nacro , David D. Manning , Matthew L. Isherwood , Kristen N. Fleming , Wenge Cui , Richard E. Olson
IPC分类号： A61P25/00 , A61K31/55 , C07D223/16
CPC分类号： C07D223/16 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D409/04 , C07D409/14 , C07D413/04 , C07D413/14 , C07D471/04 , C07D487/04
摘要： The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II): where the carbon atom designated * is in the R or S configuration, and the substituents X and R1-R9 are as defined herein.
摘要翻译：本发明的化合物由以下芳基 - 和杂芳基取代的四氢苯并吖庚因和具有式I（AE）和式（II）的二氢苯并氮杂衍生物表示：其中指定为*的碳原子为R或S构型， X和R 1 -R 9如本文所定义。

25. 发明申请

US20100292242A1 ARYL, HETEROARYL, AND HETEROCYCLE SUBSTITUTED TETRAHYDROISOQUINOLINES AND USE THEREOF 有权
标题翻译： ARYL，HETEROARYL和HETEROCYCLE取代的四氢喹啉和其用途
公开(公告)号：US20100292242A1
公开(公告)日：2010-11-18
申请号：US12777728
申请日：2010-05-11
申请人： Shuang Liu , Bruce F. Molino , Kassoum Nacro
发明人： Shuang Liu , Bruce F. Molino , Kassoum Nacro
IPC分类号： A61K31/472 , C07D401/10 , A61K31/501 , A61K31/497 , C07D217/14 , A61K31/4725 , C07D471/04 , A61P25/00 , A61P25/24 , A61P15/00
CPC分类号： C07D401/04 , C07D217/02 , C07D217/12 , C07D217/14 , C07D413/04 , C07D471/04
摘要： Novel aryl, heteroaryl, and non-aromatic heterocyle substituted tetrahydroisoquinolines are described in the present invention. These compounds are used in the treatment of various neurological and physiological disorders. Methods of making these compounds are also described in the present invention.
摘要翻译：本发明描述了新的芳基，杂芳基和非芳族杂环取代的四氢异喹啉。这些化合物用于治疗各种神经和生理疾病。制备这些化合物的方法也在本发明中描述。

26. 发明申请

US20100137287A1 ARYL-AND HETEROARYL-SUBSTITUTED TETRAHYDROBENZO-1,4-DIAZEPINES AND USE THEREOF TO BLOCK REUPTAKE OF NOREPINEPHRINE, DOPAMINE, AND SEROTONIN 有权
标题翻译：芳基取代四氢呋喃-1,4-二氮杂萘并用于阻断肾上腺素，多巴胺和丝氨酸蛋白酶
公开(公告)号：US20100137287A1
公开(公告)日：2010-06-03
申请号：US12598882
申请日：2008-05-08
申请人： Peter R. Guzzo , Bruce F. Molino , Wenge Cui , Shuang Liu , Richard E. Olson
发明人： Peter R. Guzzo , Bruce F. Molino , Wenge Cui , Shuang Liu , Richard E. Olson
IPC分类号： A61K31/5513 , C07D243/14 , A61P25/00
CPC分类号： C07D243/14 , C07D401/04 , C07D403/04 , C07D403/12 , C07D405/14 , C07D471/04
摘要： The aryl- and heteroaryl-substituted tetrahydrobenzo-1,4-diazepine derivative compounds of the present invention are represented by formulae 1(A-D) having the following structure: where the substituents X and R1-R8 are as defined herein.
摘要翻译：本发明的芳基 - 和杂芳基取代的四氢苯并-1,4-二氮杂衍生物化合物由具有以下结构的式1（A-D）表示：其中取代基X和R 1 -R 8如本文所定义。

27. 发明授权

US07629363B2 Diaryl substituted pyridinones 失效
标题翻译：二芳基取代的吡啶酮
公开(公告)号：US07629363B2
公开(公告)日：2009-12-08
申请号：US11226556
申请日：2005-09-14
申请人： Balekudru Devadas , John Walker , Shaun R. Selness , Terri L. Boehm , Richard C. Durley , Rajesh Devraj , Brian S. Hickory , Paul V. Rucker , Kevin D. Jerome , Heather M. Madsen , Edgardo Alvira , Michele A. Promo , Radhika M. Blevis-Bal , Laura D. Marruto , Jeff Hitchcock , Thomas Owen , Win Naing , Li Xing , Huey S. Shieh , Aruna Sambandam , Shuang Liu , Ian L. Scott , Kevin F. McGee
发明人： Balekudru Devadas , John Walker , Shaun R. Selness , Terri L. Boehm , Richard C. Durley , Rajesh Devraj , Brian S. Hickory , Paul V. Rucker , Kevin D. Jerome , Heather M. Madsen , Edgardo Alvira , Michele A. Promo , Radhika M. Blevis-Bal , Laura D. Marruto , Jeff Hitchcock , Thomas Owen , Win Naing , Li Xing , Huey S. Shieh , Aruna Sambandam , Shuang Liu , Ian L. Scott , Kevin F. McGee
IPC分类号： A61K31/44 , C07D211/02
CPC分类号： C07D213/64 , C07D213/69 , C07D213/70 , C07D213/74 , C07D213/75 , C07D213/79 , C07D213/84 , C07D213/85 , C07D215/22 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/06 , C07D405/12 , C07D405/14 , C07D409/06 , C07D409/14 , C07D413/10
摘要： Disclosed are compounds Formula I and pharmaceutically acceptable salts thereof, wherein R1, R2, R3/R4, and R5 are defined herein. These compounds are useful for treating diseases and conditions caused or exacerbated by unregulated p38 MAP Kinase and/or TNF activity. Pharmaceutical compositions containing the compounds, methods of preparing the compounds and methods of treatment using the compounds are also disclosed.
摘要翻译：公开了式I化合物及其药学上可接受的盐，其中R 1，R 2，R 3 / R 4和R 5在本文中定义。这些化合物可用于治疗由不受调节的p38 MAP激酶和/或TNF活性引起或加重的疾病和病症。还公开了含有化合物的药物组合物，制备化合物的方法和使用该化合物的治疗方法。

28. 发明申请

US20080124273A1 Novel cationic metal complex radiopharmaceuticals 审中-公开
标题翻译：新型阳离子金属络合物放射性药物
公开(公告)号：US20080124273A1
公开(公告)日：2008-05-29
申请号：US11811064
申请日：2007-06-08
申请人： Shuang Liu , Zhengjie He
发明人： Shuang Liu , Zhengjie He
IPC分类号： A61K51/04 , C07F13/00
CPC分类号： C07F13/005
摘要： This invention relates to novel cationic crown-ether containing metal complexes, methods of preparing the cationic crown-ether containing metal complexes, and radiopharmaceutical compositions comprising the cationic crown-ether containing metal complexes. This invention relates particularly to cationic crown-ether containing 99mTc complex radiopharmaceuticals for diagnosis of cardiovascular disorders and cancer. This invention further relates to cationic crown-ether containing 186/188Re complex radiopharmaceuticals for radiotherapy of cardiovascular disorders and cancer.
摘要翻译：本发明涉及新型含阳离子冠醚的金属络合物，制备含阳离子冠醚的金属络合物的方法，以及包含阳离子冠醚的金属络合物的放射性药物组合物。本发明特别涉及用于诊断心血管疾病和癌症的含有99m Tc复合物放射性药物的阳离子冠醚。本发明还涉及含有用于放射治疗心血管疾病和癌症的阳离子冠醚，其包含用于放射治疗心血管疾病和癌症的146复方放射性药物。

29. 发明授权

US07319149B2 Chelants and macrocyclic metal complex radiopharmaceuticals thereof 失效
标题翻译：螯合剂及其大环金属络合物放射性药物
公开(公告)号：US07319149B2
公开(公告)日：2008-01-15
申请号：US10864792
申请日：2004-06-09
申请人： Shuang Liu
发明人： Shuang Liu
IPC分类号： C07D401/02
CPC分类号： C07F13/005 , A61K51/0478 , A61K51/0482 , C07D213/81 , C07D213/82 , C07F9/58
摘要： Chelants and macrocyclic metal complexes thereof, methods of preparing the chelants and macrocyclic metal complexes, and radiopharmaceutical compositions comprising the macrocyclic metal complexes are disclosed. Methods of using the macrocyclic metal complexes as radiopharmaceuticals for the diagnosis of cardiovascular disorders, infectious diseases and cancer are also disclosed. Chelants as bifunctional chelators (BFCs) for the radiolabeling of target-specific biomolecules, such as proteins, peptides, peptidomimetics, non-peptide receptor ligands, enzyme inhibitors, and enzyme substrates are disclosed. Methods of using macrocyclic metal complexes containing the chelant-biomolecule conjugates as target-specific diagnostic radiopharmaceuticals that selectively localize at sites of disease and allow an image to be obtained of the loci using gamma scintigraphy are disclosed. Methods of use of the radiopharmaceuticals as imaging agents for the diagnosis of cardiovascular disorders, such as thromboembolic disease or atherosclerosis, infectious disease and cancer are further disclosed.
摘要翻译：公开了螯合剂及其大环金属络合物，制备螯合剂和大环金属配合物的方法，以及包含大环金属络合物的放射性药物组合物。还公开了将大环金属络合物用作放射性药物用于诊断心血管疾病，感染性疾病和癌症的方法。公开了用于靶标特异性生物分子例如蛋白质，肽，肽模拟物，非肽受体配体，酶抑制剂和酶底物的放射性标记的双功能螯合剂（BFC）的螯合剂。公开了使用含有螯合剂 - 生物分子共轭物的大环金属络合物作为靶向特异性诊断放射性药物的方法，其在疾病部位选择性定位并允许使用γ闪烁扫描获得基因座的图像。进一步公开了使用放射性药物作为诊断心血管疾病如血栓栓塞性疾病或动脉粥样硬化，感染性疾病和癌症的显像剂的方法。

30. 发明申请

US20070166227A1 Crowned dithiocarbamate metal complexes and methods for their use 审中-公开
标题翻译：冠状二硫代氨基甲酸金属络合物及其使用方法
公开(公告)号：US20070166227A1
公开(公告)日：2007-07-19
申请号：US10588343
申请日：2005-02-10
申请人： Shuang Liu , Zhengjie He
发明人： Shuang Liu , Zhengjie He
IPC分类号： A61K51/00 , C07F13/00
CPC分类号： A61K51/0478 , A61K51/0423 , A61K51/044 , A61K51/0476 , C07F13/005
摘要： Compositions containing crowned dithiocarbamate metal complexes and methods of using these compositions; neutral and cationic radioactive metal-nitrido complexes of crowned dithiocarbamates (DTCs) and methods of using these complexes as radiopharmaceuticals for diagnosis and treatment of cardiovascular disorders, infectious diseases, and cancer; tripodal chelatormetal complexes of crowned DTCs and methods of using these complexes for treating diseases such as those characterized by nitric oxide overproduction; and methods of using crowned DTCs for heavy metal detoxification are described.
摘要翻译：含有二硫代氨基甲酸金属络合物的组合物和使用这些组合物的方法; 中性和阳离子放射性金属 - 氮化复合物的冠状二硫代氨基甲酸盐（DTC）和使用这些复合物作为放射性药物用于诊断和治疗心血管疾病，传染病和癌症的方法; 冠状DTC的三峰螯合物复合物和使用这些复合物治疗诸如以一氧化氮过量产生为特征的疾病的方法; 并描述了使用加冠DTC用于重金属解毒的方法。

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