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1.发明授权Cycloalkyl lactam derivatives as inhibitors of 11-beta-hydroxysteroid dehydrogenase 1 失效环烷基内酰胺衍生物作为11-β-羟基类固醇脱氢酶1的抑制剂公开(公告)号：US07713979B2
公开(公告)日：2010-05-11
申请号：US11718111
申请日：2005-10-26
申请人： Thomas Daniel Aicher , Mark Joseph Chicarelli , Ronald Jay Hinklin , Hongqi Tian , Owen Brendan Wallace , John Gordon Allen , Zhaogen Chen , Thomas Edward Mabry , Jefferson Ray McCowan , Nancy June Snyder , Leonard Larry Winneroski, Jr.
发明人： Thomas Daniel Aicher , Mark Joseph Chicarelli , Ronald Jay Hinklin , Hongqi Tian , Owen Brendan Wallace , John Gordon Allen , Zhaogen Chen , Thomas Edward Mabry , Jefferson Ray McCowan , Nancy June Snyder , Leonard Larry Winneroski, Jr.
IPC分类号： C07D207/00 , A61K31/40 , A61K31/497 , A61K31/445 , C07D211/06 , C07D403/00
CPC分类号： C07D403/12 , C07D207/26 , C07D207/267 , C07D207/273 , C07D211/76 , C07D401/10 , C07D401/12 , C07D403/10 , C07D405/04 , C07D409/04 , C07D409/10
摘要： The present invention discloses compounds of Formula I: (I) having 11beta-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 the use of the Formula I and compositions as medicaments to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, Syndrome X, and other conditions associated with hyperglycemia.
摘要翻译： 本发明公开了具有11β-HSD 1型拮抗剂活性的式I化合物：（I），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，以及式I和组合物作为药物用于治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，综合征X和与高血糖相关的其它病症的用途。
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公开(公告)号：US20100222339A1
公开(公告)日：2010-09-02
申请号：US12377733
申请日：2007-09-17
申请人： Zhaogen Chen , Chafiq Hamdouchi Hamdouchi , Erik James Hembre , Philip Arthur Hipskind , Jason Kenneth Myers , Takako Takakuwa , James Lee Toth
发明人： Zhaogen Chen , Chafiq Hamdouchi Hamdouchi , Erik James Hembre , Philip Arthur Hipskind , Jason Kenneth Myers , Takako Takakuwa , James Lee Toth
IPC分类号： A61K31/5377 , C07D471/04 , A61K31/437 , C07D417/14 , A61P25/30 , A61P25/32
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of Formula (I), pharmaceutical compositions thereof, and use thereof as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric and neuroendocrine disorders, neurological diseases, and metabolic syndrome.
摘要翻译： 本发明涉及式（I）的化合物，其药物组合物及其作为促肾上腺皮质激素释放因子1（CRF1）受体拮抗剂在治疗精神和神经内分泌障碍，神经系统疾病和代谢综合征中的用途。
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公开(公告)号：US07384934B2
公开(公告)日：2008-06-10
申请号：US10523147
申请日：2003-07-28
申请人： Thomas Daniel Aicher , Zhaogen Chen , Yvan LeHuerou , Fionna Mitchell Martin , Marta Maria Pineiro-Nunez , Vincent Patrick Rocco , Kevin Michael Ruley , John Mehnert Schaus , Patrick Gianpietro Spinazze , David Edward Tupper
发明人： Thomas Daniel Aicher , Zhaogen Chen , Yvan LeHuerou , Fionna Mitchell Martin , Marta Maria Pineiro-Nunez , Vincent Patrick Rocco , Kevin Michael Ruley , John Mehnert Schaus , Patrick Gianpietro Spinazze , David Edward Tupper
IPC分类号： C07D403/04 , C07D495/04 , C07D513/04 , A61K31/55 , A61P25/18
CPC分类号： C07D403/04 , C07D495/04 , C07D513/04
摘要： Described herein are compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, S, and O; Alk is (C1-4) alkylene or hydroxy substituted (C1-4) alkylene; X is oxygen or sulfur; R1 is hydrogen, (C1-6) fluroalkyl, (C3-6) cycloalkyl, or (C1-4) alkyl, wherein the (C1-4) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCH2CH2OH, or —CN; R2 is H, halogen, (C1-6) fluoroalkyl, (C1-6) cycloalkyl, OR4, SR4, NO2, CN, COR4, C(O)OR4, CONR5R6, NR5R6, SO2NR5R6, NR5COR4, NR5SO2R4, optionally substituted aromatic, or (C1-6) alkyl, wherein (C1-6) alkyl is unsubstituted or substituted with a hydroxy group; R3 is hydrogen (C1-6) fluoroalkyl, (C2-6) alkenyl, Ar, (C1-4)alkyl-Ar, or (C1-4) alkyl wherein (C1-4) alkyly is unsubstituted or substituted with a phenyl; R4 is hydrogen, (C1-6) alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R5 and R6 are independently hydrogen, (C1-6) alkyl, or optionally substituted aromatic, R7 is hydrogen, (C1-6) alkyl, (C1-6) fluoroalkyl, or optionally substituted aromatic; R8 and R9 are independently hydrogen, (C1-6) alkyl, or optionally substituted aromatic; Ar is optionally substituted phenyl, napthyl, monocyclic heteroaromatic or bicyclic heteroaromatic; Z1 and Z2 are independently selected from hydrogen, halogen, (C1-6) alkyl, (C1-6) fluoroalkyl, OR7, SR7, NO2, CN, COR7, CONR8R9, NR8R9, and optionally substituted aromatic; and all salts, solvates, optical and geometric isomers, and crystalline forms thereof. Also, described are the use of the compounds of formula (I) as antagonists of the dopamine D2 receptor and as agents for the treatment of psychosis and bipolar disorders, and pharmaceutical formulations of the compounds of formula (I)
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4.发明申请公开(公告)号：US20070099909A1
公开(公告)日：2007-05-03
申请号：US11608922
申请日：2006-12-11
申请人： Zhaogen Chen , Michael Cohen , Matthew Fisher , Bruno Giethlen , James Gillig , Jefferson McCowan , Shawn Miller , John Schaus
发明人： Zhaogen Chen , Michael Cohen , Matthew Fisher , Bruno Giethlen , James Gillig , Jefferson McCowan , Shawn Miller , John Schaus
IPC分类号： A61K31/54 , A61K31/5375 , A61K31/405 , A61K31/495 , A61K31/426 , A61K31/421 , A61K31/4172 , A61K31/445 , A61K31/137
CPC分类号： C07D213/64 , C07C211/52 , C07C211/56 , C07C217/58 , C07C217/60 , C07C225/16 , C07C311/37 , C07C317/34 , C07C323/32 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/86 , C07D213/38 , C07D213/65 , C07D213/68 , C07D213/74 , C07D233/24 , C07D239/34 , C07D277/34 , C07D307/91 , C07D333/20 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D417/12 , C07D471/04 , C07F7/0812
摘要： The present invention provides compounds of formula (I), which are antagonists of the 5-HT6 receptor.
摘要翻译： 本发明提供作为5-HT 6受体的拮抗剂的式（I）化合物。
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公开(公告)号：US08030304B2
公开(公告)日：2011-10-04
申请号：US12377733
申请日：2007-09-17
申请人： Zhaogen Chen , Chafiq Hamdouchi Hamdouchi , Erik James Hembre , Philip Arthur Hipskind , Jason Kenneth Myers , Takako Takakuwa , James Lee Toth
发明人： Zhaogen Chen , Chafiq Hamdouchi Hamdouchi , Erik James Hembre , Philip Arthur Hipskind , Jason Kenneth Myers , Takako Takakuwa , James Lee Toth
IPC分类号： A01N43/58 , A01N43/54 , A01N43/64 , A01N43/78 , A01N43/56 , A61K31/50 , A61K31/505 , A61K31/41 , A61K31/425 , A61K31/415 , C07D239/42 , C07D401/04 , C07D471/04 , C07D471/22 , C07D487/04
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of Formula (I), pharmaceutical compositions thereof, and use thereof as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric and neuroendocrine disorders, neurological diseases, and metabolic syndrome.
摘要翻译： 本发明涉及式（I）的化合物，其药物组合物及其作为促肾上腺皮质激素释放因子1（CRF1）受体拮抗剂在治疗精神和神经内分泌障碍，神经系统疾病和代谢综合征中的用途。
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6.发明申请Cycloalkyl Lactam Derivatives as Inhibitors of 11-Beta-Hydroxysteroid Dehydrogenase 1 失效环烷基内酰胺衍生物作为11-β-羟基类固醇脱氢酶抑制剂1公开(公告)号：US20080275043A1
公开(公告)日：2008-11-06
申请号：US11718111
申请日：2005-10-26
申请人： Thomas Daniel Aicher , Mark Joseph Chicarelli , Ronald Jay Hinklin , Hongqi Tian , Owen Brendan Wallace , John Gordon Allen , Zhaogen Chen , Thomas Edward Mabry , Jefferson Ray McCowan , Nancy June Snyder , Leonard Larry Winneroski
发明人： Thomas Daniel Aicher , Mark Joseph Chicarelli , Ronald Jay Hinklin , Hongqi Tian , Owen Brendan Wallace , John Gordon Allen , Zhaogen Chen , Thomas Edward Mabry , Jefferson Ray McCowan , Nancy June Snyder , Leonard Larry Winneroski
IPC分类号： A61K31/5377 , C07D207/12 , A61K31/4015 , C07D403/08 , C07D413/12 , A61P3/10 , A61K31/496 , A61K31/4439 , C07D401/08
CPC分类号： C07D403/12 , C07D207/26 , C07D207/267 , C07D207/273 , C07D211/76 , C07D401/10 , C07D401/12 , C07D403/10 , C07D405/04 , C07D409/04 , C07D409/10
摘要： The present invention discloses compounds of Formula I: (I) having 11beta-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 the use of the Fomula I and compositions as medicaments to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, Syndrome X, and other conditions associated with hyperglycemia.
摘要翻译： 本发明公开了具有11β-HSD 1型拮抗剂活性的式I化合物：（I），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，以及作为药物用于治疗糖尿病，高血糖症，肥胖症，高血压，高脂血症，综合征X和与高血糖相关的其它病症的组合物I和组合物的用途。
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7.发明申请公开(公告)号：US20060009511A9
公开(公告)日：2006-01-12
申请号：US10472741
申请日：2002-03-15
申请人： Zhaogen Chen , Michael Cohen , Matthew Fisher , Bruno Giethlen , James Gillig , Jefferson McCowan , Shawn Miller , John Schaus
发明人： Zhaogen Chen , Michael Cohen , Matthew Fisher , Bruno Giethlen , James Gillig , Jefferson McCowan , Shawn Miller , John Schaus
IPC分类号： C07D209/04 , A61K31/404
CPC分类号： C07D213/64 , C07C211/52 , C07C211/56 , C07C217/58 , C07C217/60 , C07C225/16 , C07C311/37 , C07C317/34 , C07C323/32 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/86 , C07D213/38 , C07D213/65 , C07D213/68 , C07D213/74 , C07D233/24 , C07D239/34 , C07D277/34 , C07D307/91 , C07D333/20 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D417/12 , C07D471/04 , C07F7/0812
摘要： The present invention provides compounds of formula (I), which are antagonists of the 5-HT6 receptor.
摘要翻译： 本发明提供作为5-HT 6受体的拮抗剂的式（I）化合物。
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8.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：US20100022560A1
公开(公告)日：2010-01-28
申请号：US12438953
申请日：2007-09-13
申请人： Zhaogen Chen , Chafiq Hamdouchi Hamdouchi , Erik James Hembre , Philip Arthur Hipskind , Shaojuan Jia , James Lee Toth
发明人： Zhaogen Chen , Chafiq Hamdouchi Hamdouchi , Erik James Hembre , Philip Arthur Hipskind , Shaojuan Jia , James Lee Toth
IPC分类号： A61K31/519 , C07D487/04 , A61P25/24 , A61P25/22
CPC分类号： C07D487/04
摘要： The present invention relates to compounds of Formula (I), pharmaceutical compositions thereof, and the use of such compounds as corticotropin releasing factor 1 (CRF1) receptor antagonists in the treatment of psychiatric and neuroendocrine disorders, neurological diseases, and metabolic syndrome.
摘要翻译： 本发明涉及式（I）的化合物，其药物组合物，以及这些化合物作为促肾上腺皮质激素释放因子1（CRF1）受体拮抗剂在治疗精神和神经内分泌障碍，神经系统疾病和代谢综合征中的用途。
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10.发明申请公开(公告)号：US20090306110A1
公开(公告)日：2009-12-10
申请号：US12504242
申请日：2009-07-16
申请人： Zhaogen Chen , Michael Philip Cohen , Matthew Joseph Fisher , Bruno Giethlen , James Ronald Gillig , Jefferson Ray McCowan , Shawn Christopher Miller , John Mehnert Schaus
发明人： Zhaogen Chen , Michael Philip Cohen , Matthew Joseph Fisher , Bruno Giethlen , James Ronald Gillig , Jefferson Ray McCowan , Shawn Christopher Miller , John Mehnert Schaus
IPC分类号： A61K31/404 , A61K31/506 , A61K31/435 , A61K31/445 , A61P25/28
CPC分类号： C07D213/64 , C07C211/52 , C07C211/56 , C07C217/58 , C07C217/60 , C07C225/16 , C07C311/37 , C07C317/34 , C07C323/32 , C07D209/08 , C07D209/14 , C07D209/16 , C07D209/86 , C07D213/38 , C07D213/65 , C07D213/68 , C07D213/74 , C07D233/24 , C07D239/34 , C07D277/34 , C07D307/91 , C07D333/20 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D417/12 , C07D471/04 , C07F7/0812
摘要： The present invention provides compounds of formula (I), which are antagonists of the 5-HT6 receptor.
摘要翻译： 本发明提供作为5-HT 6受体拮抗剂的式（I）化合物。
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