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1.发明授权Biphenyl amide lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 有权联苯酰胺内酰胺衍生物作为11-β-羟基类固醇脱氢酶的抑制剂1公开(公告)号：US08088776B2
公开(公告)日：2012-01-03
申请号：US12297349
申请日：2007-04-19
申请人： Thomas Daniel Aicher , Zhaogen Chen , Ronald Jay Hinklin , Gary Alan Hite , Alexei Pavlovych Krasutsky , Renhua Li , Jefferson Ray McCowan , Ashraf Saeed , Nancy June Snyder , James Lee Toth , Owen Brendan Wallace , Leonard Larry Winneroski, Jr. , Yanping Xu , Jeremy Schulenburg York
发明人： Thomas Daniel Aicher , Zhaogen Chen , Ronald Jay Hinklin , Gary Alan Hite , Alexei Pavlovych Krasutsky , Renhua Li , Jefferson Ray McCowan , Ashraf Saeed , Nancy June Snyder , James Lee Toth , Owen Brendan Wallace , Leonard Larry Winneroski, Jr. , Yanping Xu , Jeremy Schulenburg York
IPC分类号： A61K31/496 , A61K31/453 , C07D403/02 , C07D405/14
CPC分类号： C07D207/12 , C07D401/10 , C07D401/12 , C07D403/10 , C07D405/14 , C07D413/10 , C07D417/10 , C07D417/14 , C07D471/04 , C07D487/04 , C07D487/08 , C07D491/08 , C07D491/10
摘要： The present invention discloses novel compounds of Formula I: possessing 11 β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, cognitive disorders, and other conditions associated with 11 β-HSD type 1 activity.
摘要翻译： 本发明公开了具有11＆amp; b -HSD 1型拮抗剂活性的式I化合物，以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式I化合物的药物组合物，以及使用化合物和组合物治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，代谢综合征，认知障碍以及与其相关的其它病症的方法 ; -HSD 1型活动。
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公开(公告)号：US07968585B2
公开(公告)日：2011-06-28
申请号：US12297906
申请日：2007-04-25
申请人： Thomas Edward Mabry , Owen Brendan Wallace , Yanping Xu , Nancy June Snyder , Leonard Larry Winneroski, Jr.
发明人： Thomas Edward Mabry , Owen Brendan Wallace , Yanping Xu , Nancy June Snyder , Leonard Larry Winneroski, Jr.
IPC分类号： A01N43/38 , A01N43/36 , A61K31/40 , C07D209/54 , C07D209/96 , C07D207/00
CPC分类号： C07D209/44 , C07D401/10 , C07D403/10 , C07D487/10
摘要： The present invention discloses novel compounds of Formula (I): having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11β-HSD type 1 activity.
摘要翻译： 本发明公开了具有11＆amp; b -HSD 1拮抗剂活性的式（I）的新化合物，以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式I化合物的药物组合物，以及使用化合物和组合物治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，代谢综合征以及与其相关的其它病症的方法。 1活动。
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3.发明授权Multicyclic compounds for use as melanin concentrating hormone antagonists in the treatment of obesity and diabetes 失效用作黑色素浓缩激素拮抗剂治疗肥胖和糖尿病的多环化合物公开(公告)号：US07229987B2
公开(公告)日：2007-06-12
申请号：US10512986
申请日：2003-05-06
申请人： Jochen Ammenn , James Ronald Gillig , Lawrence Joseph Heinz , Philip Arthur Hipskind , Michael Dean Kinnick , Yen-Shi Lai , John Michael Morin, Jr. , James Arthur Nixon , Carsten Ott , Kenneth Allen Savin , Theo Schotten , Lawrence John Slieker , Nancy June Snyder , Michael Alan Robertson
发明人： Jochen Ammenn , James Ronald Gillig , Lawrence Joseph Heinz , Philip Arthur Hipskind , Michael Dean Kinnick , Yen-Shi Lai , John Michael Morin, Jr. , James Arthur Nixon , Carsten Ott , Kenneth Allen Savin , Theo Schotten , Lawrence John Slieker , Nancy June Snyder , Michael Alan Robertson
IPC分类号： A61K31/5355 , A61K31/454 , C07D401/12 , C07D403/12 , C07D263/32
CPC分类号： C07D249/08 , C07D261/08 , C07D263/32 , C07D271/06 , C07D271/10 , C07D271/107 , C07D277/26 , C07D333/18 , C07D413/04 , C07D413/06 , C07D413/10 , C07D413/12 , C07D413/14 , C07D417/12
摘要： The present invention relates to a melanin concentrating hormone antagonist compound of formula I: (I); or a pharmaceutically acceptable salt, solvate, enantiomer or prodrug thereof useful in the treatment, prevention or amelioration of symptoms associated with obesity and related diseases.
摘要翻译： 本发明涉及式I的黑色素浓缩激素拮抗剂化合物：（I）; 或其药学上可接受的盐，溶剂化物，对映异构体或前药，用于治疗，预防或改善与肥胖症和相关疾病相关的症状。
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公开(公告)号：US08252923B2
公开(公告)日：2012-08-28
申请号：US12231982
申请日：2008-09-08
申请人： Robert Edward Babine , Shu-Hui Chen , Jason Eric Lamar , Nancy June Snyder , Xicheng Sun , Mark Joseph Tebbe , Frantz Victor , Q. May Wang , Yvonne Yee Mai Yip , Ivan Collado , Cristina Garcia-Paredes , Raymond Samuel Parker, III , Ling Jin , Deqi Guo , John Irvin Glass
发明人： Robert Edward Babine , Shu-Hui Chen , Jason Eric Lamar , Nancy June Snyder , Xicheng Sun , Mark Joseph Tebbe , Frantz Victor , Q. May Wang , Yvonne Yee Mai Yip , Ivan Collado , Cristina Garcia-Paredes , Raymond Samuel Parker, III , Ling Jin , Deqi Guo , John Irvin Glass
IPC分类号： C07D265/34 , C07D241/08 , C07D275/06 , C07D417/02 , C07D233/32 , C07D403/02 , C07D207/08 , C07D493/14 , C07C229/00
CPC分类号： C07K7/02 , A61K38/07 , A61K38/08 , A61K38/21 , A61K38/212 , A61K38/215 , A61K45/06 , C07D209/02 , C07D209/52 , C07K5/0202 , C07K5/0205 , C07K5/06052 , C07K5/0808 , C07K5/101 , C07K5/1016 , C07K7/06 , C07K14/005 , C12N2770/24222 , Y02P20/55 , A61K2300/00
摘要： The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.
摘要翻译： 本发明涉及可用作蛋白酶抑制剂的肽模拟化合物，特别是作为丝氨酸蛋白酶抑制剂，更具体地，涉及丙型肝炎NS3蛋白酶抑制剂; 中间体; 它们的制备方法包括对中间体的新型置换步骤。 本发明还涉及药物组合物和使用该化合物抑制HCV蛋白酶或治疗患有HCV感染或与感染有关的生理病症的患者的方法。 还提供了药物组合，除一种或多种HCV丝氨酸蛋白酶抑制剂外还包含一种或多种表现出抗HCV活性的干扰素和/或一种或多种具有抗HCV活性的化合物和药学上可接受的载体，以及用于治疗或预防的方法 使用该组合物的患者中的HCV感染。 本发明还涉及用于治疗或预防患者HCV感染的试剂盒或药物包装。
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公开(公告)号：US20120064034A1
公开(公告)日：2012-03-15
申请号：US13293812
申请日：2011-11-10
申请人： ROBERT EDWARD BABINE , SHU HUI CHEN , IVAN COLLADO , CRISTINA GARCIA-PAREDES , JOHN IRVIN GLASS , DEQI GUO , LING JIN , JASON ERIC LAMAR , RAYMOND SAMUEL PARKER, III , NANCY JUNE SNYDER , XICHENG DAVID SUN , YVONNE YEE MAI YIP , Q. MAY WANG , FRANTZ VICTOR , MARK JOSEPH TEBBE , ROBERT B. PERNI , LUC FARMER
发明人： ROBERT EDWARD BABINE , SHU HUI CHEN , IVAN COLLADO , CRISTINA GARCIA-PAREDES , JOHN IRVIN GLASS , DEQI GUO , LING JIN , JASON ERIC LAMAR , RAYMOND SAMUEL PARKER, III , NANCY JUNE SNYDER , XICHENG DAVID SUN , YVONNE YEE MAI YIP , Q. MAY WANG , FRANTZ VICTOR , MARK JOSEPH TEBBE , ROBERT B. PERNI , LUC FARMER
IPC分类号： A61K38/08 , C07K5/037 , A61K38/21 , C12N5/071 , C07C229/42 , C07D209/52 , C12N9/99 , C07K7/06 , A61K38/20
CPC分类号： C07K7/02 , A61K38/07 , A61K38/08 , A61K38/21 , A61K38/212 , A61K38/215 , A61K45/06 , C07D209/02 , C07D209/52 , C07K5/0202 , C07K5/0205 , C07K5/06052 , C07K5/0808 , C07K5/101 , C07K5/1016 , C07K7/06 , C07K14/005 , C12N2770/24222 , Y02P20/55 , A61K2300/00
摘要： The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.
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6.发明授权Cyclohexyl substituted pyrrolidinones as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 有权环己基取代的吡咯烷酮作为11-β-羟基类固醇脱氢酶的抑制剂1公开(公告)号：US07998999B2
公开(公告)日：2011-08-16
申请号：US12297877
申请日：2007-04-24
申请人： Owen Brendan Wallace , Yanping Xu , Nancy June Snyder , Jeremy Schulenburg York , Alexei Pavlovych Krasutsky
发明人： Owen Brendan Wallace , Yanping Xu , Nancy June Snyder , Jeremy Schulenburg York , Alexei Pavlovych Krasutsky
IPC分类号： A61K31/4015 , C07D207/26
CPC分类号： C07D207/26 , C07D401/10 , C07D403/10
摘要： The present invention discloses novel compounds of Formula I: having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11β-HSD type 1 activity.
摘要翻译： 本发明公开了具有11＆amp; b -HSD 1型拮抗剂活性的新颖的式I化合物，以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式I化合物的药物组合物，以及使用化合物和组合物治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，代谢综合征以及与其相关的其它病症的方法。 1活动。
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7.发明授权Cyclohexylpyrazole-lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 有权环己基吡唑 - 内酰胺衍生物作为11-β-羟基类固醇脱氢酶1的抑制剂公开(公告)号：US07981918B2
公开(公告)日：2011-07-19
申请号：US12297375
申请日：2007-04-05
申请人： Thomas Daniel Aicher , Peter Biagio Anzeveno , Renhua Li , Alexei Pavlovych Krasutsky , Thomas Edward Mabry , Ashraf Saeed , Nancy June Snyder , Hongqi Tian , Owen Brendan Wallace , Leonard Larry Winneroski , Yanping Xu
发明人： Thomas Daniel Aicher , Peter Biagio Anzeveno , Renhua Li , Alexei Pavlovych Krasutsky , Thomas Edward Mabry , Ashraf Saeed , Nancy June Snyder , Hongqi Tian , Owen Brendan Wallace , Leonard Larry Winneroski , Yanping Xu
IPC分类号： A61K31/416 , C07D231/56
CPC分类号： C07D403/04
摘要： The present invention discloses novel compounds of Formula (I): having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I), as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11β-HSD type 1 activity.
摘要翻译： 本发明公开了具有11＆amp; b -HSD 1拮抗剂活性的式（I）的新化合物，以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式（I）化合物的药物组合物，以及使用化合物和组合物治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，代谢综合征以及与其相关的其它病症的方法。 HSD 1型活动。
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公开(公告)号：US20100137583A1
公开(公告)日：2010-06-03
申请号：US12231982
申请日：2008-09-08
申请人： Robert Edward Babine , Shu-Hui Chen , Jason Eric Lamar , Nancy June Snyder , Xicheng Sun , Mark Joseph Tebbe , Frantz Victor , Q. May Wang , Yvonne Yee Mai Yip , Ivan Collado , Cristina Garcia-Paredes , Raymond Samuel Parker, III , Ling Jin , Deqi Guo , John Irvin Glass
发明人： Robert Edward Babine , Shu-Hui Chen , Jason Eric Lamar , Nancy June Snyder , Xicheng Sun , Mark Joseph Tebbe , Frantz Victor , Q. May Wang , Yvonne Yee Mai Yip , Ivan Collado , Cristina Garcia-Paredes , Raymond Samuel Parker, III , Ling Jin , Deqi Guo , John Irvin Glass
IPC分类号： C07D265/34 , C07D265/32 , C07D241/08 , C07D275/06 , C07D417/02 , C07D233/32 , C07D403/02 , C07D207/08 , C07D493/14 , C07C229/00
CPC分类号： C07K7/02 , A61K38/07 , A61K38/08 , A61K38/21 , A61K38/212 , A61K38/215 , A61K45/06 , C07D209/02 , C07D209/52 , C07K5/0202 , C07K5/0205 , C07K5/06052 , C07K5/0808 , C07K5/101 , C07K5/1016 , C07K7/06 , C07K14/005 , C12N2770/24222 , Y02P20/55 , A61K2300/00
摘要： The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.
摘要翻译： 本发明涉及可用作蛋白酶抑制剂的肽模拟化合物，特别是作为丝氨酸蛋白酶抑制剂，更具体地，涉及丙型肝炎NS3蛋白酶抑制剂; 中间体; 它们的制备方法包括对中间体的新型置换步骤。 本发明还涉及药物组合物和使用该化合物抑制HCV蛋白酶或治疗患有HCV感染或与感染有关的生理病症的患者的方法。 还提供了药物组合，除一种或多种HCV丝氨酸蛋白酶抑制剂外还包含一种或多种表现出抗HCV活性的干扰素和/或一种或多种具有抗HCV活性的化合物和药学上可接受的载体，以及用于治疗或预防的方法 使用该组合物的患者中的HCV感染。 本发明还涉及用于治疗或预防患者HCV感染的试剂盒或药物包装。
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公开(公告)号：US20090099180A1
公开(公告)日：2009-04-16
申请号：US12297906
申请日：2007-04-25
申请人： Thomas Edward Mabry , Owen Brendan Wallace , Yanping Xu , Nancy June Snyder , Leonard Larry Winneroski, JR.
发明人： Thomas Edward Mabry , Owen Brendan Wallace , Yanping Xu , Nancy June Snyder , Leonard Larry Winneroski, JR.
IPC分类号： A61K31/403 , C07D209/54 , C07D401/10 , C07D403/10 , C07D413/10 , A61P3/10 , A61K31/496 , A61K31/5377 , A61K31/454
CPC分类号： C07D209/44 , C07D401/10 , C07D403/10 , C07D487/10
摘要： The present invention discloses novel compounds of Formula (I): having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11β-HSD type 1 activity.
摘要翻译： 本发明公开了具有11β-HSD 1型拮抗剂活性的式（I）的新化合物，以及制备这些化合物的方法。 在另一个实施方案中，本发明公开了包含式I化合物的药物组合物，以及使用化合物和组合物治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，代谢综合征和与11beta-HSD 1型相关的其它病症的方法 活动。
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公开(公告)号：US5916873A
公开(公告)日：1999-06-29
申请号：US53848
申请日：1998-04-01
摘要： The present invention is directed to teicoplanin derivatives of the following general formula, wherein R.sup.1 and R.sup.2 are as defined in the specification. ##STR1## These derivatives are useful as antibiotics for the control of gram-positive bacteria.
摘要翻译： 本发明涉及以下通式的替考拉宁衍生物，其中R1和R2如说明书中所定义。 这些衍生物可用作控制革兰氏阳性细菌的抗生素。
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