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公开(公告)号：US20070099872A1
公开(公告)日：2007-05-03
申请号：US11508458
申请日：2006-08-23
申请人： Kevin McCormick , Christopher Boyce , Robert Aslanian , Neng-Yang Shih , Salem Fevrier , Pietro Mangiaracina , Chia-Yu Huang , Bo Liang , Rong-Qiang Liu , Huagang Lu
发明人： Kevin McCormick , Christopher Boyce , Robert Aslanian , Neng-Yang Shih , Salem Fevrier , Pietro Mangiaracina , Chia-Yu Huang , Bo Liang , Rong-Qiang Liu , Huagang Lu
IPC分类号： A61K31/675 , A61K31/4709 , A61K31/4178 , C07D403/02
CPC分类号： C07D403/02 , C07D401/06 , C07D403/06
摘要： In its many embodiments, the present invention provides a novel class of indolines as inhibitors of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.
摘要翻译： 在其许多实施方案中，本发明提供了作为α2C肾上腺素能受体激动剂抑制剂的新一类中和体，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种此类化合物的药物制剂的方法，以及 使用这些化合物或药物组合物治疗，预防，抑制或改善与α2C肾上腺素能受体相关的一种或多种病症的方法。
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公开(公告)号：US20080027100A1
公开(公告)日：2008-01-31
申请号：US11705683
申请日：2007-02-13
申请人： Kevin McCormick , Christopher Boyce , Neng-Yang Shih , Chia-Yu Huang , Robert Aslanian , Jianhua Chao , Salem Fevrier , Bo Liang , Huagang Lu , Pietro Mangiaracina , Rong-Qiang Liu , Younong Yu
发明人： Kevin McCormick , Christopher Boyce , Neng-Yang Shih , Chia-Yu Huang , Robert Aslanian , Jianhua Chao , Salem Fevrier , Bo Liang , Huagang Lu , Pietro Mangiaracina , Rong-Qiang Liu , Younong Yu
IPC分类号： A61K31/4178 , A61K31/4709 , A61P1/12 , A61P13/00 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/24 , A61P27/14 , A61P37/00 , A61P9/00 , C07D215/00 , C07D403/06 , C12N5/00
CPC分类号： C07D403/02 , C07D401/14 , C07D403/06 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： In its many embodiments, the present invention provides a novel class of indolines as inhibitors of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.
摘要翻译： 在其许多实施方案中，本发明提供了作为α2C肾上腺素能受体激动剂抑制剂的新一类中和体，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种此类化合物的药物制剂的方法，以及 使用这些化合物或药物组合物治疗，预防，抑制或改善与α2C肾上腺素能受体相关的一种或多种病症的方法。
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公开(公告)号：US20080039439A1
公开(公告)日：2008-02-14
申请号：US11705673
申请日：2007-02-13
申请人： Kevin McCormick , Christopher Boyce , Neng-Yang Shih , Chia-Yu Huang , Robert Aslanian , Salem Fevrier , Bo Liang , Rong-qiang Liu , Ruiyan Liu , Pietro Mangiaracina , Manuel de Lera Ruiz , Younong Yu , Lisa Guise-Zawacki , Junying Zheng
发明人： Kevin McCormick , Christopher Boyce , Neng-Yang Shih , Chia-Yu Huang , Robert Aslanian , Salem Fevrier , Bo Liang , Rong-qiang Liu , Ruiyan Liu , Pietro Mangiaracina , Manuel de Lera Ruiz , Younong Yu , Lisa Guise-Zawacki , Junying Zheng
IPC分类号： A61K31/535 , A61K31/502 , A61K31/54 , A61K31/553 , A61P1/00 , A61P25/00 , A61P37/00 , A61P9/00 , C07D241/36 , C07D279/06 , C07D498/04 , C12N5/06
CPC分类号： C07D413/14 , C07D241/36 , C07D279/06 , C07D403/06 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04 , C07D498/04
摘要： In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as α2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the α2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.
摘要翻译： 在其许多实施方案中，本发明涉及可用作α2C肾上腺素能受体激动剂的新型苯基吗啉和苯硫基吗啉化合物，含有该化合物的药物组合物，以及治疗，预防，抑制或改善一种或多种与 α2C肾上腺素能受体激动剂，使用这些化合物或药物组合物。
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公开(公告)号：US20070093477A1
公开(公告)日：2007-04-26
申请号：US11508467
申请日：2006-08-23
申请人： Kevin McCormick , Christopher Boyce , Neng-Yang Shih , Robert Aslanian , Pietro Mangiaracina , Manuel de Lera Ruiz , Younong Yu , Purakkattle Biju , Chia-Yu Huang , Bo Liang , Ruiyan Liu , Rong-Qiang Liu , Lisa Guise-Zawacki
发明人： Kevin McCormick , Christopher Boyce , Neng-Yang Shih , Robert Aslanian , Pietro Mangiaracina , Manuel de Lera Ruiz , Younong Yu , Purakkattle Biju , Chia-Yu Huang , Bo Liang , Ruiyan Liu , Rong-Qiang Liu , Lisa Guise-Zawacki
IPC分类号： A61K31/5415 , A61K31/538 , A61K31/498 , C07D413/02 , C07D417/02
CPC分类号： C07D413/06 , C07D403/06 , C07D413/04 , C07D413/14 , C07D417/06 , C07D471/04 , C07D487/04 , C07D498/04
摘要： In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as α2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the α2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.
摘要翻译： 在其许多实施方案中，本发明涉及可用作α2C肾上腺素能受体激动剂的新型苯基吗啉和苯硫基吗啉化合物，含有该化合物的药物组合物，以及治疗，预防，抑制或改善一种或多种与 α2C肾上腺素能受体激动剂，使用这些化合物或药物组合物。
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公开(公告)号：US07803828B2
公开(公告)日：2010-09-28
申请号：US11508458
申请日：2006-08-23
申请人： Kevin D. McCormick , Christopher W. Boyce , Robert G. Aslanian , Neng-Yang Shih , Salem Fevrier , Pietro Mangiaracina , Chia-Yu Huang , Bo Liang , Rong-Qiang Liu , Huagang Lu
发明人： Kevin D. McCormick , Christopher W. Boyce , Robert G. Aslanian , Neng-Yang Shih , Salem Fevrier , Pietro Mangiaracina , Chia-Yu Huang , Bo Liang , Rong-Qiang Liu , Huagang Lu
IPC分类号： A01N43/50 , C07D233/00
CPC分类号： C07D403/02 , C07D401/06 , C07D403/06
摘要： In its many embodiments, the present invention provides a novel class of indolines as inhibitors of α2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the α2C adrenergic receptors using such compounds or pharmaceutical compositions.
摘要翻译： 在其许多实施方案中，本发明提供了作为α2C肾上腺素能受体激动剂抑制剂的新一类中和体，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种此类化合物的药物制剂的方法，以及 使用这些化合物或药物组合物治疗，预防，抑制或改善与α2C肾上腺素能受体相关的一种或多种病症的方法。
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公开(公告)号：US07700592B2
公开(公告)日：2010-04-20
申请号：US11705673
申请日：2007-02-13
申请人： Kevin D. McCormick , Christopher W. Boyce , Neng-Yang Shih , Chia-Yu Huang , Robert G. Aslanian , Salem Fevrier , Bo Liang , Rong-qiang Liu , Ruiyan Liu , Pietro Mangiaracina , Manuel de Lera Ruiz , Younong Yu , Lisa Guise-Zawacki , Junying Zheng
发明人： Kevin D. McCormick , Christopher W. Boyce , Neng-Yang Shih , Chia-Yu Huang , Robert G. Aslanian , Salem Fevrier , Bo Liang , Rong-qiang Liu , Ruiyan Liu , Pietro Mangiaracina , Manuel de Lera Ruiz , Younong Yu , Lisa Guise-Zawacki , Junying Zheng
IPC分类号： C07D498/04 , A61K31/538
CPC分类号： C07D413/14 , C07D241/36 , C07D279/06 , C07D403/06 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04 , C07D498/04
摘要： In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as α2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the α2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.
摘要翻译： 在其许多实施方案中，本发明涉及可用作α2C肾上腺素能受体激动剂的新一类苯基吗啉和苯硫基吗啉化合物，含有该化合物的药物组合物，以及治疗，预防，抑制或改善一种或多种与 α2C肾上腺素能受体激动剂，使用这些化合物或药物组合物。
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公开(公告)号：US07985748B2
公开(公告)日：2011-07-26
申请号：US12722879
申请日：2010-03-12
申请人： Kevin D. McCormick , Christopher W. Boyce , Neng-Yang Shih , Robert G. Aslanian , Pietro Mangiaracina , Manuel de Lera Ruiz , Younong Yu , Purakkattle Biju , Chia-Yu Huang , Bo Liang , Ruiyan Liu , Rong-Qiang Liu , Lisa Guise-Zawacki
发明人： Kevin D. McCormick , Christopher W. Boyce , Neng-Yang Shih , Robert G. Aslanian , Pietro Mangiaracina , Manuel de Lera Ruiz , Younong Yu , Purakkattle Biju , Chia-Yu Huang , Bo Liang , Ruiyan Liu , Rong-Qiang Liu , Lisa Guise-Zawacki
IPC分类号： C07D413/06 , A61K31/538
CPC分类号： C07D413/06 , C07D403/06 , C07D413/04 , C07D413/14 , C07D417/06 , C07D471/04 , C07D487/04 , C07D498/04
摘要： In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as α2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the α2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.
摘要翻译： 在其许多实施方案中，本发明涉及可用作α2C肾上腺素能受体激动剂的新一类苯基吗啉和苯硫基吗啉化合物，含有该化合物的药物组合物，以及治疗，预防，抑制或改善一种或多种与 α2C肾上腺素能受体激动剂，使用这些化合物或药物组合物。
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公开(公告)号：US20100173823A1
公开(公告)日：2010-07-08
申请号：US12722879
申请日：2010-03-12
申请人： Kevin D. McCormick , Christopher W. Boyce , Neng-Yang Shih , Robert G. Aslanian , Pietro Mangiaracina , Manuel de Lera Ruiz , Younong Yu , Purakkattle Biju , Chia-Yu Huang , Bo Liang , Ruiyan Liu , Rong-Qiang Liu , Lisa Guise-Zawacki
发明人： Kevin D. McCormick , Christopher W. Boyce , Neng-Yang Shih , Robert G. Aslanian , Pietro Mangiaracina , Manuel de Lera Ruiz , Younong Yu , Purakkattle Biju , Chia-Yu Huang , Bo Liang , Ruiyan Liu , Rong-Qiang Liu , Lisa Guise-Zawacki
IPC分类号： A61K31/553 , C07D265/36 , A61K31/538 , C12N5/00 , C07D279/16 , A61K31/5415 , C07D241/36 , A61K31/498 , C07D267/14 , C07D471/04 , A61K31/56 , A61K38/02 , A61P11/00 , A61P37/08 , A61P9/00 , A61P25/00 , A61P29/00 , A61P13/00
CPC分类号： C07D413/06 , C07D403/06 , C07D413/04 , C07D413/14 , C07D417/06 , C07D471/04 , C07D487/04 , C07D498/04
摘要： In its many embodiments, the present invention relates to a novel class of phenylmorpholine and phenylthiomorpholine compounds useful as α2C adrenergic receptor agonists, pharmaceutical compositions containing the compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the α2C adrenergic receptor agonists using such compounds or pharmaceutical compositions.
摘要翻译： 在其许多实施方案中，本发明涉及可用作α2C肾上腺素能受体激动剂的新一类苯基吗啉和苯硫基吗啉化合物，含有该化合物的药物组合物，以及治疗，预防，抑制或改善一种或多种与 α2C肾上腺素能受体激动剂，使用这些化合物或药物组合物。
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9.发明申请Heteroatom-linked substituted piperidines and derivatives thereof useful as histamine H3 antagonists 失效杂原子取代的哌啶及其衍生物可用作组胺H3拮抗剂公开(公告)号：US20070015807A1
公开(公告)日：2007-01-18
申请号：US11455625
申请日：2006-06-19
申请人： Robert Aslanian , Michael Berlin , Christopher Boyce , Jianhua Chao , Manuel de Lera Ruiz , Pietro Mangiaracina , Kevin McCormick , Mwangi Mutahi , Stuart Rosenblum , Neng-Yang Shih , Daniel Solomon , Wing Tom , Henry Vaccaro , Junying Zheng , Xiaohong Zhu
发明人： Robert Aslanian , Michael Berlin , Christopher Boyce , Jianhua Chao , Manuel de Lera Ruiz , Pietro Mangiaracina , Kevin McCormick , Mwangi Mutahi , Stuart Rosenblum , Neng-Yang Shih , Daniel Solomon , Wing Tom , Henry Vaccaro , Junying Zheng , Xiaohong Zhu
IPC分类号： C07D403/02 , A61K31/4178 , A61K31/4025
CPC分类号： C07D295/185 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , Y02P20/582
摘要： Disclosed are novel compounds of the formula or a pharmaceutically acceptable salt thereof, wherein: M1 and M3 are CH or N; M2 is CH, CF or N; Y is —C(═O)—, —C(═S)—, —(CH2)q—, —C(═NOR7)— or —SO1-2—; Z is a bond or optionally substituted alkylene or alkenylene; R1 is H, or alkyl, cycloalkyl, aryl, heteroaryl, heterocycloalkyl, all optionally substituted, or a group of the formula: where ring A is a heteroaryl ring; R2 is optionally substituted alkyl, alkenyl, aryl, heteroaryl, cycloalkyl or heterocycloalkyl; R3 is H, —C(O)NH2, or alkyl, aryl, cycloalkyl, heterocycloalkyl or heteroaryl, all optionally substituted; and the remaining variables are as defined in the specification; compositions and methods of treating allergy-induced airway responses, congestion, obesity, metabolic syndrome, alcoholic fatty liver disease, hepatic steatosis, nonalcoholic steatohepatitis, cirrhosis, hepatacellular carcinoma and cognition deficit disorders using said compounds, alone or in combination with other agents.
摘要翻译： 公开了下式的新化合物或其药学上可接受的盐，其中：M 1和M 3是CH或N; M 2是CH，CF或N; Y是-C（-O） - ， - C（-S） - ， - （CH 2 CH 2）q - ， - C（-NOR 7） / SO 2 - ） - 或-SO 2 1-2。 Z是键或任选取代的亚烷基或亚烯基; R 1是H或烷基，环烷基，芳基，杂芳基，杂环烷基，全部是任选取代的，或下式的基团：其中环A是杂芳基环; R 2是任选取代的烷基，烯基，芳基，杂芳基，环烷基或杂环烷基; R 3是H，-C（O）NH 2或烷基，芳基，环烷基，杂环烷基或杂芳基，全部任选被取代; 剩余的变量如规范中所定义; 使用所述化合物单独或与其它试剂组合治疗过敏引起的气道反应，充血，肥胖，代谢综合征，酒精性脂肪肝疾病，肝脂肪变性，非酒精性脂肪性肝炎，肝硬化，肝细胞癌和认知缺陷障碍的组合物和方法。
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10.发明申请公开(公告)号：US20100197562A1
公开(公告)日：2010-08-05
申请号：US12525641
申请日：2008-02-11
申请人： Manuel De lera Ruiz , Kevin D. McCormick , Christopher W. Boyce , Robert G. Aslanian , Younong Yu , Pietro Mangiaracina , Junying Zheng , Michael Y. Berlin , Stephanie L. Ciesla , Chia-yu Huang , Bo Liang
发明人： Manuel De lera Ruiz , Kevin D. McCormick , Christopher W. Boyce , Robert G. Aslanian , Younong Yu , Pietro Mangiaracina , Junying Zheng , Michael Y. Berlin , Stephanie L. Ciesla , Chia-yu Huang , Bo Liang
IPC分类号： A61K31/506 , C07D403/14 , A61K31/4178 , C07D401/10 , C07D487/04 , A61K31/519 , C07D401/14 , A61K31/4439 , A61K31/56 , A61K38/02 , A61P11/00 , A61P29/00 , A61P1/12 , A61P9/00 , A61P25/00 , A61P25/24 , A61P25/22 , A61P25/18 , A61P3/10 , A61P19/02
CPC分类号： C07D403/14 , C07D233/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D405/14 , C07D407/14 , C07D409/14 , C07D413/14
摘要： In its many embodiments, the present invention provides a novel class of biaryl compounds as inhibitors of ÿ2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ÿ2C adrenergic receptors using such compounds or pharmaceutical compositions.
摘要翻译： 在其许多实施方案中，本发明提供了一类新颖的联芳基化合物作为ÿ2C肾上腺素能受体激动剂的抑制剂，制备此类化合物的方法，含有一种或多种此类化合物的药物组合物，制备包含一种或多种此类化合物的药物制剂的方法， 以及使用这些化合物或药物组合物治疗，预防，抑制或改善与ÿ2C肾上腺素能受体相关的一种或多种病症的方法。
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