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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：US08501747B2
公开(公告)日：2013-08-06
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 Louise 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 Louise Ciesla , Chia-Yu Huang , Bo Liang
IPC分类号： A61K31/404 , A61K31/4025 , A61K31/4178 , A61K31/4439 , A61K31/4709 , A61K31/506 , C07D401/04 , C07D401/14 , C07D403/02 , C07D403/14
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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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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4.发明授权公开(公告)号：US07638531B2
公开(公告)日：2009-12-29
申请号：US11641175
申请日：2006-12-19
申请人： Mwangi W. Mutahi , Robert G. Aslanian , Michael Y. Berlin , Christopher W. Boyce , Manuel de Lera Ruiz , Kevin D. McCormick , Daniel M. Solomon , Henry A. Vaccaro , Junying Zheng , Purakkattle Biju , Younong Yu , Wei Zhou , Xiaohong Zhu
发明人： Mwangi W. Mutahi , Robert G. Aslanian , Michael Y. Berlin , Christopher W. Boyce , Manuel de Lera Ruiz , Kevin D. McCormick , Daniel M. Solomon , Henry A. Vaccaro , Junying Zheng , Purakkattle Biju , Younong Yu , Wei Zhou , Xiaohong Zhu
IPC分类号： A01N43/42 , A61K31/44 , A01N43/40 , C07D471/02 , C07D491/02 , C07D498/02 , C07D211/68 , C07D211/80 , C07D213/02
CPC分类号： C07D471/04 , C07D213/38 , C07D213/73 , C07D277/40 , C07D401/06 , C07D401/12 , C07D401/14 , C07D409/12 , C07D417/06 , C07D417/14 , C07D473/00
摘要： Disclosed are compounds of the formula or a pharmaceutically acceptable salt or solvate thereof, wherein: M is CH or N; U and W are each CH, or one of U and W is CH and the other is N; X is a bond, alkylene, —C(O)—, —C(N—OR5)—, —C(N—OR5)—CH(R6)—, —CH(R6)—C(N—OR5)—, —O—, —OCH2—, —CH2O— or —S(O)0-2—; Y is —O—, —(CH2)2—, —C(═O)—, —C(═NOR7)— or —SO0-2—; Z is a bond, optionally substituted alkylene or alkylene interrupted by a heteroatom or heterocyclic group; R1 is optionally substituted alkyl, cycloalkyl, aryl, arylalkyl, heteroaryl, heterocycloalkyl, or benzimidazolyl or a derivative thereof; R2 is optionally substituted alkyl, alkenyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl or heterocycloalkyl; and the remaining variables are as defined in the specification; compositions and methods for treating an allergy-induced airway response, congestion, diabetes, obesity, an obesity-related disorder, metabolic syndrome and a cognition deficit disorder using said compounds, alone or in combination with other agents.
摘要翻译： 公开了下式的化合物或其药学上可接受的盐或溶剂化物，其中：M是CH或N; U和W各自为CH，或U和W中的一个为CH，另一个为N; X是键，亚烷基，-C（O） - ， - C（N-OR 5） - ， - C（N-OR 5）-CH（R 6） - ， - CH（R 6）-C（N-OR 5） ，-O - ， - OCH 2 - ， - CH 2 O-或-S（O）0-2-; Y是-O - ， - （CH 2）2 - ， - C（-O） - ， - C（-NOR 7） - 或-SOO 2 - ; Z是一个键，任选取代的被杂原子或杂环基中断的亚烷基或亚烷基; R1是任选取代的烷基，环烷基，芳基，芳烷基，杂芳基，杂环烷基或苯并咪唑基或其衍生物; R 2是任选取代的烷基，烯基，芳基，芳基烷基，杂芳基，杂芳基烷基，环烷基或杂环烷基; 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，糖尿病，肥胖，肥胖相关病症，代谢综合征和认知缺陷障碍的组合物和方法。
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5.发明申请BIARYL-SPIROAMINOOXAZOLINE ANALOGUES AS ALPHA 2C ADRENERGIC RECEPTOR MODULATORS 失效作为ALPHA 2C ADRENERGIC受体调节剂的BIARYL-SPIROAMINOOXAZOLINE ANALOGUES公开(公告)号：US20110251207A1
公开(公告)日：2011-10-13
申请号：US13122679
申请日：2009-10-06
申请人： Kevin D. McCormick , Li Dong , Christopher W. Boyce , Manuel de Lera Ruiz , Salem Fevrier , Jie Wu , Junying Zheng , Younong Yu , Jianhua Chao , Walter S. Won , Ashwin U. Rao , Rongze Kuang , Pauline C. Ting , Xianhai Huang , Ning Shao , Adandan Palani , Michael Y. Berlin , Robert G. Aslanian
发明人： Kevin D. McCormick , Li Dong , Christopher W. Boyce , Manuel de Lera Ruiz , Salem Fevrier , Jie Wu , Junying Zheng , Younong Yu , Jianhua Chao , Walter S. Won , Ashwin U. Rao , Rongze Kuang , Pauline C. Ting , Xianhai Huang , Ning Shao , Adandan Palani , Michael Y. Berlin , Robert G. Aslanian
IPC分类号： A61K31/501 , A61K31/506 , A61K31/4439 , A61K31/427 , A61K31/497 , C07D263/52 , A61K31/423 , C07D235/02 , A61K31/4184 , C07D405/10 , C07D409/10 , A61K31/422 , C07D403/10 , A61P27/06 , A61P25/22 , A61P21/02 , A61P9/00 , A61P25/18 , A61P25/06 , A61P25/28 , A61P3/10 , A61P11/02 , C07D413/10
CPC分类号： A61K31/5377 , A61K31/437 , A61K31/501 , A61K31/506 , A61K31/537 , C07D235/02 , C07D263/52 , C07D401/10 , C07D403/10 , C07D405/10 , C07D409/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D471/04 , C07D498/10 , C07D519/00
摘要： In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators 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，本发明提供了一类新颖的作为α2C肾上腺素能受体激动剂的调节剂的生物二螺吡喃恶唑啉类似物，制备这些化合物的方法，含有一种或多种这类化合物的药物组合物，制备包含一种或多种这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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6.发明申请CYCLOPROPYLCHROMENE DERIVATIVES AS MODULATORS OF THE ALPHA-2C RECEPTOR 审中-公开作为ALPHA-2C受体的调节剂的环丙基胆碱衍生物公开(公告)号：US20110190247A1
公开(公告)日：2011-08-04
申请号：US13057376
申请日：2009-08-03
IPC分类号： A61K31/422 , A61K31/56 , A61K31/506 , A61K31/4178 , C07D405/10 , C07D413/14 , C07D405/08 , A61P25/24 , A61P11/02 , A61P29/00 , A61P25/28 , A61P25/18 , A61P25/06 , A61P25/22 , A61P27/06 , A61P9/10 , A61P9/04 , A61P3/10
CPC分类号： C07D405/04 , C07D405/14 , C07D413/14
摘要： In its many embodiments, the present invention provides a novel class of cyclopropylchromene derivatives as modulators of a2C adrenergic receptor, 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 a2C 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环丙烯基衍生物作为α2C肾上腺素能受体的调节剂，制备这些化合物的方法，含有一种或多种这类化合物的药物组合物，制备包含一种或多种这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α2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：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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8.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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9.发明申请REVERSED BIARYL SPIROAMINOOXAZOLINE ANALOGUES AS ALPHA2C ADRENERGIC RECEPTOR MODULATORS 审中-公开作为ALPHA2C ADRENERGIC受体调节剂的反相BIARYL SPIROAMINOOXAZOLINE ANALOGUES公开(公告)号：US20130079271A1
公开(公告)日：2013-03-28
申请号：US13499071
申请日：2010-09-22
申请人： Kevin D. McCormick , Ning Shao , Younong Yu , Xianhai Huang , Manuel De Lera Ruiz , Anandan Palani , Junying Zheng , Christopher W. Boyce , Robert G. Aslanian , Jianhua Chao
发明人： Kevin D. McCormick , Ning Shao , Younong Yu , Xianhai Huang , Manuel De Lera Ruiz , Anandan Palani , Junying Zheng , Christopher W. Boyce , Robert G. Aslanian , Jianhua Chao
IPC分类号： C07D413/10 , A61K31/537 , A61K31/4245 , A61K38/02 , A61K31/423 , A61K31/4439 , A61K31/56 , A61K31/506 , C07D263/52
CPC分类号： C07D413/10 , A61K31/42 , A61K31/423 , A61K31/4245 , A61K31/4439 , A61K31/506 , A61K31/537 , A61K31/56 , A61K38/02 , A61K45/06 , C07D263/52 , C07D413/04 , C07D417/04 , A61K2300/00
摘要： In its many embodiments, the present invention provides a novel class of biaryl spiroaminooxazoline analogues as modulators 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，本发明提供了一类新颖的联芳基螺氨基恶唑啉类似物作为α2C肾上腺素能受体激动剂的调节剂，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这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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10.发明授权Biaryl-spiroaminooxazoline analogues as alpha 2C adrenergic receptor modulators 失效双芳基 - 螺氨基恶唑啉类似物作为α2C肾上腺素能受体调节剂公开(公告)号：US08324213B2
公开(公告)日：2012-12-04
申请号：US13122679
申请日：2009-10-06
申请人： Kevin D. McCormick , Li Dong , Christopher W. Boyce , Manuel de Lera Ruiz , Salem Fevrier , Jie Wu , Junying Zheng , Youngong Yu , Jianhua Chao , Walter S. Won , Ashwin U. Rao , Rongze Kuang , Pauline C. Ting , Xianhai Huang , Ning Shao , Anandan Palani , Michael Y. Berlin , Robert G. Aslanian
发明人： Kevin D. McCormick , Li Dong , Christopher W. Boyce , Manuel de Lera Ruiz , Salem Fevrier , Jie Wu , Junying Zheng , Youngong Yu , Jianhua Chao , Walter S. Won , Ashwin U. Rao , Rongze Kuang , Pauline C. Ting , Xianhai Huang , Ning Shao , Anandan Palani , Michael Y. Berlin , Robert G. Aslanian
IPC分类号： A61K31/501 , A61K31/497 , A61K31/506 , A61K31/4439 , A61K31/427 , A61K31/423 , C07D235/02 , C07D405/02 , C07D409/02 , C07D413/02 , C07D263/52
CPC分类号： A61K31/5377 , A61K31/437 , A61K31/501 , A61K31/506 , A61K31/537 , C07D235/02 , C07D263/52 , C07D401/10 , C07D403/10 , C07D405/10 , C07D409/10 , C07D413/10 , C07D413/14 , C07D417/10 , C07D471/04 , C07D498/10 , C07D519/00
摘要： In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators 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，本发明提供了一类新颖的作为α2C肾上腺素能受体激动剂的调节剂的生物二螺吡喃恶唑啉类似物，制备这些化合物的方法，含有一种或多种这类化合物的药物组合物，制备包含一种或多种这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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