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1. 发明申请

US20140275133A1 MINERALOCORTICOID RECEPTOR ANTAGONISTS 有权
标题翻译：矿物胆碱受体拮抗剂
公开(公告)号：US20140275133A1
公开(公告)日：2014-09-18
申请号：US14350930
申请日：2012-10-08
申请人： Hong Shen , Jason M. Cox , Hong Dong Chu
发明人： Hong Shen , Jason M. Cox , Hong Dong Chu
IPC分类号： C07D413/04 , C07D413/14 , A61K31/4245 , A61K31/422 , A61K31/506 , A61K31/454
CPC分类号： C07D413/04 , A61K31/422 , A61K31/4245 , A61K31/4439 , A61K31/454 , A61K31/506 , C07D263/44 , C07D413/14
摘要： The present invention is directed to compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof that are possible useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the Formula (I), to their possible use for the treatment of the above mentioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula (I).
摘要翻译：本发明涉及可用于治疗醛固酮介导的疾病的式（I）化合物及其药学上可接受的盐。本发明还涉及制备式（I）化合物，其可能用于治疗上述疾病和为此目的制备药物的方法，以及包含式（I）化合物的药物组合物。

2. 发明申请

US20150274672A1 SUBSTITUTED SPIROPIPERIDINYL COMPOUNDS USEFUL AS GPR120 AGONISTS 有权
标题翻译：替代的螺旋磷酸化合物可用作GPR120激动剂
公开(公告)号：US20150274672A1
公开(公告)日：2015-10-01
申请号：US14434524
申请日：2013-10-11
申请人： Mariappan CHELLIAH , Hong Dong CHU , Jason M. COX , John S. DEBENHAM , Keith EAGEN , Ping LAN , Clare LONDON , Michael A. PLOTKIN , Unmesh SHAH , Christopher Joseph SINZ , Zhongxiang SUN , Henry M. VACCARO , Skikanth KATRAMAN , MERCK SHARP & DOHME CORP.
发明人： Mariappan Chelliah , Hong Dong Chu , Jason M. Cox , John S. Debenham , Keith Eagen , Ping Lan , Clare London , Michael A. Plotkin , Unmesh Shah , Christopher Joseph Sinz , Zhongxiang Sun , Henry M. Vaccaro , Srikanth Venkatraman
IPC分类号： C07D221/20 , C07D401/04 , C07D491/107 , C07D405/10
CPC分类号： C07D221/20 , C07D401/04 , C07D401/12 , C07D405/10 , C07D491/107
摘要： The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing diabetes, hyperlipidemia, obesity, inflammation related disorders, and related diseases and conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR120. Pharmaceutical compositions and methods of treatment are also included.
摘要翻译：本发明涉及由式（I）表示的化合物及其药学上可接受的盐，其可用于治疗或预防糖尿病，高脂血症，肥胖，炎症相关疾病及相关疾病和病症。该化合物可用作G蛋白偶联受体GPR120的激动剂。还包括药物组合物和治疗方法。

3. 发明授权

US08716482B2 Substituted aminopiperidines as dipeptidyl peptidase-IV inhibitors for the treatment of diabetes 有权
标题翻译：取代的氨基哌啶作为二肽基肽酶-IV抑制剂用于治疗糖尿病
公开(公告)号：US08716482B2
公开(公告)日：2014-05-06
申请号：US13390708
申请日：2010-09-15
申请人： Jason M. Cox , Tesfaye Biftu , Hong Dong Chu , Danqing Feng , Ann E. Weber
发明人： Jason M. Cox , Tesfaye Biftu , Hong Dong Chu , Danqing Feng , Ann E. Weber
IPC分类号： C07D211/32 , A61K31/00
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention is directed to novel substituted aminopiperidines of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-ÏV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译：本发明涉及结构式I的新型取代氨基哌啶，其是二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防涉及二肽基肽酶-κV酶的疾病，例如糖尿病，特别是 2型糖尿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二肽基肽酶-IV酶的疾病中的用途。

4. 发明申请

US20120149683A1 SUBSTITUTED AMINOPIPERIDINES AS DIPEPTIDYL PEPTIDASE-IV INHIBITORS FOR THE TREATMENT OF DIABETES 有权
标题翻译：替代的氨基磷酸酯作为用于治疗糖尿病的DIPEPTIDYL PEPTIDASE-IV抑制剂
公开(公告)号：US20120149683A1
公开(公告)日：2012-06-14
申请号：US13390708
申请日：2010-09-15
申请人： Jason M. Cox , Tesfaye Biftu , Hong Dong Chu , Danqing Feng , Ann E. Weber
发明人： Jason M. Cox , Tesfaye Biftu , Hong Dong Chu , Danqing Feng , Ann E. Weber
IPC分类号： A61K31/454 , C07D401/12 , A61K31/497 , C07D401/06 , A61P3/10 , C07D487/04 , A61K31/4985 , C07D413/06 , A61K31/5377 , C07D211/56 , A61K31/4545
CPC分类号： C07D487/04 , C07D519/00
摘要： The present invention is directed to novel substituted aminopiperidines of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-ÏV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译：本发明涉及结构式I的新型取代氨基哌啶，其是二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防涉及二肽基肽酶-κV酶的疾病，例如糖尿病，特别是 2型糖尿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二肽基肽酶-IV酶的疾病中的用途。

5. 发明授权

US09193717B2 Mineralocorticoid receptor antagonists 有权
标题翻译：盐皮质激素受体拮抗剂
公开(公告)号：US09193717B2
公开(公告)日：2015-11-24
申请号：US14350888
申请日：2012-10-08
申请人： Hong Shen , Christine Yang , Jason M. Cox , Kun Liu
发明人： Hong Shen , Christine Yang , Jason M. Cox , Kun Liu
IPC分类号： C07D413/04 , C07D413/14 , C07D403/04 , A61K31/422 , A61K31/4439 , A61K31/506 , A61K31/5377
CPC分类号： C07D413/04 , A61K31/422 , A61K31/4439 , A61K31/506 , A61K31/5377 , C07D403/04 , C07D413/14
摘要： The present invention is directed to compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof, that are aldosterone receptor antagonists which might be useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the Formula (I), to their possible use for the treatment of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula (I).
摘要翻译：本发明涉及可用于治疗醛固酮介导的疾病的醛固酮受体拮抗剂的式（I）化合物及其药学上可接受的盐。本发明还涉及制备式（I）化合物，其可能用于治疗上述疾病和为此目的制备药物的方法，以及包含式（I）化合物的药物组合物。

6. 发明授权

US09505730B2 Mineralocorticoid receptor antagonists 有权
标题翻译：盐皮质激素受体拮抗剂
公开(公告)号：US09505730B2
公开(公告)日：2016-11-29
申请号：US14351006
申请日：2012-10-08
申请人： Hong Shen , Jason M. Cox , Christine Yang , Zhicai Wu
发明人： Hong Shen , Jason M. Cox , Christine Yang , Zhicai Wu
IPC分类号： C07D263/44 , C07D413/12 , C07D413/06 , A61K31/422 , A61K31/4439 , A61K31/4725 , C07D401/06 , A61K31/421
CPC分类号： C07D263/44 , A61K31/421 , A61K31/422 , A61K31/4439 , A61K31/4725 , C07D401/06 , C07D413/06 , C07D413/12
摘要： The present invention is directed to compounds of the Formula I as well as pharmaceutically acceptable salts thereof, that are potentially useful for treating aldosterone-mediated diseases. The invention furthermore relates to processes for preparing compounds of the Formula I, to their possible use in the treatment of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and to pharmaceutical compositions which comprise compounds of the Formula I.

7. 发明授权

US08143289B2 Aminotetrahydropyrans as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes 有权
标题翻译：氨基四氢吡喃作为二肽基肽酶-IV抑制剂用于治疗或预防糖尿病
公开(公告)号：US08143289B2
公开(公告)日：2012-03-27
申请号：US12616831
申请日：2009-11-12
申请人： Tesfaye Biftu , Ping Chen , Jason M. Cox , Ann E. Weber
发明人： Tesfaye Biftu , Ping Chen , Jason M. Cox , Ann E. Weber
IPC分类号： A61K31/4439 , A61K31/4162 , A61P3/10 , C07D401/14 , C07D487/04
CPC分类号： C07D309/30 , A61K9/2054 , A61K31/4162 , A61K38/1709 , A61K38/26 , A61K45/06 , C07D487/04
摘要： The present invention is directed to novel substituted aminotetrahydropyrans of structural formula I which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译：本发明涉及结构式I的新型取代的氨基四氢吡喃，其是二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病，特别是 2型糖尿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二肽基肽酶-IV酶的疾病中的用途。

8. 发明申请

US20150069258A1 DIFFERENTIAL EXCITATION SPECTROSCOPY 有权
标题翻译：差异激发光谱
公开(公告)号：US20150069258A1
公开(公告)日：2015-03-12
申请号：US14473796
申请日：2014-08-29
申请人： Eugene W. Butler , Timothy M. Stratman , Boyd V. Hunter , Paul Harrison , Jason M. Cox
发明人： Eugene W. Butler , Timothy M. Stratman , Boyd V. Hunter , Paul Harrison , Jason M. Cox
IPC分类号： G01N21/62 , G01N22/00 , G01N21/27
CPC分类号： G01N21/35 , G01N21/031 , G01N21/27 , G01N21/3581 , G01N21/636 , G01N22/00 , G01N2021/3125
摘要： A new technique which uses a pump-probe methodology to place a molecule into one or more excited rotational and/or vibrational states. By evaluating spectral changes due to at least one discrete frequency of pump photons a multi-dimensional characterization of the molecule's excited state energy level results. This multi-dimensional characterization typically involves evaluating the changes between excited and unexcited state measurements. The differential nature of the evaluation makes the technique self-referencing and solves problems common to many spectroscopic techniques. The multi-dimensionality of the technique provides high specificity and immunity to interferents. The preferred embodiments involve excitation by using photons suited to pumping the rotational states and evaluating the effects by probing the energy levels of one of more vibrational states. The technique is capable of detecting bulk and trace concentrations of a molecule in gas, liquid and solid phases, both in pure form and in the presence of other molecules.
摘要翻译：一种使用泵浦探针方法将分子置于一个或多个激发的旋转和/或振动状态的新技术。通过评估由于至少一个离散频率的泵浦光子的光谱变化，可以得到分子激发态能级的多维表征。这种多维表征通常包括评估激发态和不精确状态测量之间的变化。评估的差异性使得技术自我参照并且解决了许多光谱技术常见的问题。该技术的多维度为干扰物提供了高度的特异性和免疫性。优选实施例涉及通过使用适于泵送旋转状态的光子并通过探测更多振动状态之一的能量水平来评估效果来激发。该技术能够检测气体，液体和固相中分子的体积和痕量浓度，无论是纯形式还是在其它分子存在下。

9. 发明授权

US07855206B2 Tricyclic heteroaromatic compounds as dipeptidyl peptidase-IV inhibitors for the treatment or prevention of diabetes 有权
标题翻译：三环杂芳族化合物作为二肽基肽酶-IV抑制剂用于治疗或预防糖尿病
公开(公告)号：US07855206B2
公开(公告)日：2010-12-21
申请号：US12513190
申请日：2007-11-09
申请人： Jason M. Cox , Hong Dong
发明人： Jason M. Cox , Hong Dong
IPC分类号： A01N43/54 , A01N43/66 , A01N43/58 , A01N43/60 , A01N43/64 , A61K31/50 , A61K31/505 , A61K31/495 , A61K31/53 , C07D471/00 , C07D487/00 , C07D251/00
CPC分类号： C07D487/14
摘要： The present invention is directed to novel substituted tricyclic heteroaromatic compounds of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.
摘要翻译：本发明涉及结构式（I）的新型取代三环杂芳族化合物，其为二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如作为糖尿病，特别是2型糖尿病。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二肽基肽酶-IV酶的疾病中的用途。

10. 发明申请

US20090233936A1 Fused Aminopiperidines as Dipeptidyl Peptidase-4 Inhibitors for the Treatment or Prevention of Diabetes 有权
标题翻译：融合氨基哌啶作为二肽基肽酶-4抑制剂治疗或预防糖尿病
公开(公告)号：US20090233936A1
公开(公告)日：2009-09-17
申请号：US12085797
申请日：2006-12-08
申请人： Jason M. Cox , Scott D. Edmondson , Anthony Mastracchio
发明人： Jason M. Cox , Scott D. Edmondson , Anthony Mastracchio
IPC分类号： A61K31/4985 , C07D471/12 , A61K31/4375 , C07D487/12 , A61K31/519 , A61K31/5025 , A61P3/10
CPC分类号： C07D471/14
摘要： The present invention is directed to novel substituted fused aminopiperidines of structural formula (I) which are inhibitors of the dipeptidyl peptidase-4 enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-4 enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-4 enzyme is involved.
摘要翻译：本发明涉及结构式（I）的新型取代的稠合氨基哌啶，其是二肽基肽酶-4酶的抑制剂，其可用于治疗或预防涉及二肽基肽酶-4酶的疾病，例如糖尿病，特别是2型糖尿病。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二肽基肽酶-4酶的疾病中的用途。

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