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1. 发明授权

US07858658B2 Fluoro- and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof 失效
标题翻译： β-淀粉样蛋白产生的含氟和三氟烷基的杂环磺酰胺抑制剂及其衍生物
公开(公告)号：US07858658B2
公开(公告)日：2010-12-28
申请号：US12435442
申请日：2009-05-05
申请人： Anthony Frank Kreft , Lynn Resnick , Scott Christian Mayer , George Diamantidis , Derek Cecil Cole , Boyd Lynn Harrison , Minsheng Zhang , Molly Hoke , Tingzhong Wang , Rocco John Galante
发明人： Anthony Frank Kreft , Lynn Resnick , Scott Christian Mayer , George Diamantidis , Derek Cecil Cole , Boyd Lynn Harrison , Minsheng Zhang , Molly Hoke , Tingzhong Wang , Rocco John Galante
IPC分类号： A61K31/381 , C07D333/34
CPC分类号： C07D333/62 , C07D231/18 , C07D333/34
摘要： Compounds of Formula (I), are provided where T is CHO, COR8, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substitutedalkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substitutedphenyl), or (F)ncycloalkyl; n=1-3; R5 is hydrogen, halogen, CF3, diene fused to Y when Y=C, or substituted diene fused to Y when Y=C; W, Y and Z are C, CR6 or N where at least one of W, Y or Z are C; R6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO2, or NR7; R7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R8 is lower alkyl, CF3, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.
摘要翻译：提供式（I）化合物，其中T是CHO，COR8或C（OH）R 1 R 2; R 1和R 2是氢，任选取代的低级烷基，CF 3，任选取代的烯基或任选取代的炔基; R3是氢或任选取代的低级烷基; R4是（CF3）n烷基，（CF3）n（取代烷基），（CF3）n烷基苯基，（CF3）n烷基（取代苯基）或（F）n环烷基; n = 1-3; 当Y = C时，R 5为氢，卤素，CF 3，与Y稠合的二烯，或Y = C时与Y稠合的取代二烯; W，Y和Z是C，CR 6或N，其中W，Y或Z中的至少一个是C; R6是氢，卤素或任选取代的低级烷基; X是O，S，SO 2或NR 7; R 7是氢，任选取代的低级烷基，任选取代的苄基或任选取代的苯基; 且R 8为低级烷基，CF 3或任选取代的苯基。还描述了制备和使用这些化合物抑制β-淀粉样蛋白产生和治疗阿尔茨海默病和唐氏综合征的方法。

2. 发明申请

US20090227667A1 FLUORO- AND TRIFLUOROALKYL-CONTAINING HETEROCYCLIC SULFONAMIDE INHIBITORS OF BETA AMYLOID PRODUCTION AND DERIVATIVES THEREOF 失效
标题翻译：含氟和含三氟甲磺酸的苯甲酰胺酰胺抑制剂的制备及其衍生物
公开(公告)号：US20090227667A1
公开(公告)日：2009-09-10
申请号：US12435442
申请日：2009-05-05
申请人： Anthony Frank Kreft , Lynn Resnick , Scott Christian Mayer , George Diamantidis , Derek Cecil Cole , Boyd Lynn Harrison , Minsheng Zhang , Molly Hoke , Tingzhong Wang , Rocco John Galante
发明人： Anthony Frank Kreft , Lynn Resnick , Scott Christian Mayer , George Diamantidis , Derek Cecil Cole , Boyd Lynn Harrison , Minsheng Zhang , Molly Hoke , Tingzhong Wang , Rocco John Galante
IPC分类号： A61K31/381 , C07D333/34 , C07D333/62
CPC分类号： C07D333/62 , C07D231/18 , C07D333/34
摘要： Compounds of Formula (I), are provided where T is CHO, COR8, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substitutedalkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substitutedphenyl), or (F)ncycloalkyl; n=1-3; R5 is hydrogen, halogen, CF3, diene fused to Y when Y=C, or substituted diene fused to Y when Y=C; W, Y and Z are C, CR6 or N where at least one of W, Y or Z are C; R6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO2, or NR7; R7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R8 is lower alkyl, CF3, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.
摘要翻译：提供式（I）化合物，其中T是CHO，COR8或C（OH）R 1 R 2; R 1和R 2是氢，任选取代的低级烷基，CF 3，任选取代的烯基或任选取代的炔基; R3是氢或任选取代的低级烷基; R4是（CF3）n烷基，（CF3）n（取代烷基），（CF3）n烷基苯基，（CF3）n烷基（取代苯基）或（F）n环烷基; n = 1-3; 当Y = C时，R 5为氢，卤素，CF 3，与Y稠合的二烯，或Y = C时与Y稠合的取代二烯; W，Y和Z是C，CR 6或N，其中W，Y或Z中的至少一个是C; R6是氢，卤素或任选取代的低级烷基; X是O，S，SO 2或NR 7; R 7是氢，任选取代的低级烷基，任选取代的苄基或任选取代的苯基; 且R 8为低级烷基，CF 3或任选取代的苯基。还描述了制备和使用这些化合物抑制β-淀粉样蛋白产生和治疗阿尔茨海默病和唐氏综合征的方法。

3. 发明授权

US07547725B2 Fluoro- and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof 失效
标题翻译： β-淀粉样蛋白产生的含氟和三氟烷基的杂环磺酰胺抑制剂及其衍生物
公开(公告)号：US07547725B2
公开(公告)日：2009-06-16
申请号：US11818630
申请日：2007-06-15
申请人： Anthony Frank Kreft , Lynn Resnick , Scott Christian Mayer , George Diamantidis , Derek Cecil Cole , Boyd Lynn Harrison , Minsheng Zhang , Molly Hoke , Tingzhong Wang , Rocco John Galante
发明人： Anthony Frank Kreft , Lynn Resnick , Scott Christian Mayer , George Diamantidis , Derek Cecil Cole , Boyd Lynn Harrison , Minsheng Zhang , Molly Hoke , Tingzhong Wang , Rocco John Galante
IPC分类号： A61K31/381 , C07D333/10 , C07D333/34
CPC分类号： C07D333/62 , C07D231/18 , C07D333/34
摘要： Compounds of Formula (I), are provided where T is CHO, COR8, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substituted alkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substituted phenyl), or (F)ncycloalkyl; n=1-3; R5 is hydrogen, halogen, CF3, diene fused to Y when Y═C, or substituted diene fused to Y when Y═C; W, Y and Z are C, CR6 or N where at least one of W, Y or Z are C; R6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO2, or NR7; R7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R8 is lower alkyl, CF3, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.
摘要翻译：提供式（I）化合物，其中T是CHO，COR8或C（OH）R 1 R 2; R 1和R 2是氢，任选取代的低级烷基，CF 3，任选取代的烯基或任选取代的炔基; R3是氢或任选取代的低级烷基; R4是（CF3）n烷基，（CF3）n（取代烷基），（CF3）n烷基苯基，（CF3）n烷基（取代苯基）或（F） n = 1-3; 当Y-C或Y-C与Y稠合时，R 5为氢，卤素，CF 3，二烯稠合至Y; W，Y和Z是C，CR 6或N，其中W，Y或Z中的至少一个是C; R6是氢，卤素或任选取代的低级烷基; X是O，S，SO 2或NR 7; R 7是氢，任选取代的低级烷基，任选取代的苄基或任选取代的苯基; 且R 8为低级烷基，CF 3或任选取代的苯基。还描述了制备和使用这些化合物抑制β-淀粉样蛋白产生和治疗阿尔茨海默病和唐氏综合征的方法。

4. 发明授权

US07300951B2 Fluoro- and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof 失效
标题翻译： β-淀粉样蛋白产生的含氟和三氟烷基的杂环磺酰胺抑制剂及其衍生物
公开(公告)号：US07300951B2
公开(公告)日：2007-11-27
申请号：US10810517
申请日：2004-03-26
申请人： Anthony Frank Kreft , Lynn Resnick , Scott Christian Mayer , George Diamantidis , Derek Cecil Cole , Boyd Lynn Harrison , Minsheng Zhang , Molly Hoke , Tingzhong Wang , Rocco John Galante
发明人： Anthony Frank Kreft , Lynn Resnick , Scott Christian Mayer , George Diamantidis , Derek Cecil Cole , Boyd Lynn Harrison , Minsheng Zhang , Molly Hoke , Tingzhong Wang , Rocco John Galante
IPC分类号： A61K31/381 , C07D333/10 , C07D333/34
CPC分类号： C07D333/62 , C07D231/18 , C07D333/34
摘要： Compounds of Formula (I), are provided where T is CHO, CON, or C(OH)R1R2; R1 and R2 are hydrogen, optionally substituted lower alkyl, CF3, optionally substituted alkenyl, or optionally substituted alkynyl; R3 is hydrogen or optionally substituted lower alkyl; R4 is (CF3)nalkyl, (CF3)n(substitutedalkyl), (CF3)nalkylphenyl, (CF3)nalkyl(substitutedphenyl), or (F)ncycloalkyl; n=1-3; R5 is hydrogen, halogen, CF3, diene fused to Y when Y═C, or substituted diene fused to Y when Y═C; W, Y and Z are C, CR6 or N where at least one of W, Y or Z are C; R6 is hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO2, or NR7; R7 is hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and R8 is lower alkyl, CF3, or optionally substituted phenyl. Methods of preparing and using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's Disease and Down's syndrome are also described.
摘要翻译：提供式（I）的化合物，其中T是CHO，CON或C（OH）R 1 R 2 R 2; R 1和R 2均为氢，任选取代的低级烷基，CF 3，任选取代的烯基或任选取代的炔基; R 3是氢或任选取代的低级烷基; R 4是（CF 3）n烷基，（CF 3 N）N（S）（取代的烷基），（CF 3）n烷基苯基，（CF 3）n烷基（取代的苯基）或（C 3 -C 6）烷基（F）环烷基; n = 1-3; 当Y-C时，R 5是氢，卤素，CF 3 O，与Y稠合的二烯，或Y-C时与Y稠合的取代的二烯; W，Y和Z是C，CR 6或N，其中W，Y或Z中的至少一个是C; R 6是氢，卤素或任选取代的低级烷基; X是O，S，SO 2或NR 7; R 7是氢，任选取代的低级烷基，任选取代的苄基或任选取代的苯基; 和R 8是低级烷基，CF 3或任选取代的苯基。还描述了制备和使用这些化合物抑制β-淀粉样蛋白产生和治疗阿尔茨海默病和唐氏综合征的方法。

5. 发明授权

US07629377B2 Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1) 失效
标题翻译：取代的萘基吲哚衍生物作为纤溶酶原激活物抑制剂1型（PAI-1）的抑制剂
公开(公告)号：US07629377B2
公开(公告)日：2009-12-08
申请号：US12026272
申请日：2008-02-05
申请人： David LeRoy Crandall , Scott Christian Mayer , Eric Gould Gundersen , Hassan Mahmoud Elokdah
发明人： David LeRoy Crandall , Scott Christian Mayer , Eric Gould Gundersen , Hassan Mahmoud Elokdah
IPC分类号： A61K31/404 , C07D209/04
CPC分类号： C07D403/12 , C07D209/12
摘要： This invention provides PAI-1 inhibiting compounds of Formula I: wherein: R1, R2, R3, and R4 are each H, alkyl, alkanoyl, halo, OH, aryl optionally substituted with R8, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; R5 is H, alkyl, perfluoroalkyl, aryl optionally substituted with R5, alkanoyl, aroyl optionally substituted with R8; R6 is H, alkyl, alkylaryl, benzyl optionally substituted with R8, alkanoyl, aroyl optionally substituted with R8; R7 is H, alkyl, alkylaryl, aryl optionally substituted with R8; n is 0-6; A is COOH, or an acid mimic such as tetraazole, SO3H, PO3H2, tetronic acid, etc.; R8 is H, alkyl, cycloalkyl, alkanoyl, halo, OH, perfluoroalkyl, alkoxy, amino, alkylamino, dialkylamino, perfluoroalkoxy; or a pharmaceutically acceptable salt thereof; as well as pharmaceutical compositions and methods of treatment using these compounds.
摘要翻译：本发明提供了PAI-1抑制式I化合物：其中：R1，R2，R3和R4分别为H，烷基，烷酰基，卤素，OH，任选被R8，全氟烷基，烷氧基，氨基，烷基氨基，二烷基氨基，全氟烷氧基 R5是H，烷基，全氟烷基，任选被R 5取代的芳基，烷酰基，任选被R 8取代的芳酰基; R6是H，烷基，烷芳基，任选被R8，烷酰基取代的苄基，任选被R8取代的芳酰基; R7是H，烷基，烷芳基，任选被R8取代的芳基; n为0-6; A是COOH，或酸性模拟物如四唑，SO 3 H，PO 3 H 2，四氢萘等; R8是H，烷基，环烷基，烷酰基，卤素，OH，全氟烷基，烷氧基，氨基，烷基氨基，二烷基氨基，全氟烷氧基; 或其药学上可接受的盐; 以及使用这些化合物的药物组合物和治疗方法。

6. 发明授权

US07713994B2 Substituted isoquinoline-1,3(2H,4H)-diones, 1-thioxo,1,4-dihydro-2H-isoquinoline-3-ones and 1,4-dihyro-3 (2H)-isoquinolones and methods of use thereof 失效
标题翻译：取代的异喹啉-1,3（2H，4H） - 二酮，1-硫代，1,4-二氢-2H-异喹啉-3-酮和1,4-二羟基-3（2H） - 异喹诺酮及其使用方法
公开(公告)号：US07713994B2
公开(公告)日：2010-05-11
申请号：US11728897
申请日：2007-03-26
申请人： Hwei-Ru Tsou , Semiramis Ayral-Kaloustian , Gary Harold Birnberg , Middleton Brawner Floyd , Joshua Kaplan , Kristina M. Kutterer , Xiaoxiang Liu , Ramaswamy Nilakantan , Mercy Adufa Otteng , Zhilian Tang , Arie Zask , Tritin Tran , Scott Christian Mayer , Annette L. Banker , Marvin Reich
发明人： Hwei-Ru Tsou , Semiramis Ayral-Kaloustian , Gary Harold Birnberg , Middleton Brawner Floyd , Joshua Kaplan , Kristina M. Kutterer , Xiaoxiang Liu , Ramaswamy Nilakantan , Mercy Adufa Otteng , Zhilian Tang , Arie Zask , Tritin Tran , Scott Christian Mayer , Annette L. Banker , Marvin Reich
IPC分类号： A61K31/47 , C07D217/08
CPC分类号： C07D217/24 , C07D237/28 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/04 , C07D405/12 , C07D405/14 , C07D409/04 , C07D409/06 , C07D409/12 , C07D409/14 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07D487/04
摘要： This invention provides compounds of Formula (I), having the structure where G1, G2, G3, G4, A1, A2, Y1, Y2, L1, Z, e and f are defined herein, or a pharmaceutically acceptable salt thereof, which are useful for treating or preventing cancer.
摘要翻译：本发明提供具有本文定义的G1，G2，G3，G4，A1，A2，Y1，Y2，L1，Z，e和f的结构的式（I）化合物或其药学上可接受的盐，可用于治疗或预防癌症。

7. 发明授权

US07132402B2 Acylated benzylmaltosides as inhibitors of smooth muscle cell proliferation 有权
标题翻译：作为平滑肌细胞增殖的抑制剂的酰化苄基甲基卤化物
公开(公告)号：US07132402B2
公开(公告)日：2006-11-07
申请号：US10699233
申请日：2003-10-31
申请人： Scott Christian Mayer , Robert E. McDevitt , Paul J. Dollings
发明人： Scott Christian Mayer , Robert E. McDevitt , Paul J. Dollings
IPC分类号： A61K31/7036
CPC分类号： C07H17/02 , A61K31/704 , C07H5/06
摘要： This invention provides smooth muscle cell proliferation inhibitors of formula I having the structure
摘要翻译：本发明提供具有该结构的式I的平滑肌细胞增殖抑制剂

8. 发明申请

US20090264427A1 3-Cyanoquinolines, Methods for Preparation and Use as Insulin-like Growth Factor Inhibitors 审中-公开
标题翻译： 3-氰基喹啉，制备和用作胰岛素样生长因子抑制剂的方法
公开(公告)号：US20090264427A1
公开(公告)日：2009-10-22
申请号：US12423096
申请日：2009-04-14
申请人： Scott Christian Mayer , Lori Michelle Miller
发明人： Scott Christian Mayer , Lori Michelle Miller
IPC分类号： A61K31/4709 , C07D401/12 , C07D413/14 , C07D401/14 , A61K31/5377 , A61K31/496 , A61P29/00 , A61P35/00
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14
摘要： Imidazole-substituted 4-anilino-3-cyanoquinolines are described, which selectively inhibit IFGR kinase activity and are useful for treating disorders associated with IGFR kinases.
摘要翻译：描述了咪唑取代的4-苯胺基-3-氰基喹啉，其选择性地抑制IFGR激酶活性并且可用于治疗与IGFR激酶相关的疾病。

9. 发明授权

US06849761B2 Substituted naphthoic acid derivatives useful in the treatment of insulin resistance and hyperglycemia 失效
标题翻译：用于治疗胰岛素抵抗和高血糖症的取代萘甲酸衍生物
公开(公告)号：US06849761B2
公开(公告)日：2005-02-01
申请号：US10656981
申请日：2003-09-05
申请人： Scott Christian Mayer , Alan Howard Katz
发明人： Scott Christian Mayer , Alan Howard Katz
IPC分类号： C07C229/38 , C07C311/37 , C07C229/00
CPC分类号： C07C229/38 , C07C311/37
摘要： This invention provides compounds of Formula I having the structure wherein: R1 is hydroxyl, alkoxy of 1-4 carbons or —O(CH2)nX; n is an integer of 1-13; X is CONHR6 or CO2R6; R2 is hydrogen, halogen, hydroxyl, alkyl of 1-4 carbons, alkoxy of 1-4 carbons or acyl of 1-4 carbons; R3, R4 and R5 are each independently, hydrogen, halogen, hydroxyl, alkyl of 1-4 carbons, alkoxy of 1-4 carbons, acyl of 1-4 carbons, CF3, OCF3, SO2NHR6, NR6R7 or CO2R6; R6, and R7 are each independently, hydrogen, alkyl of 1-4 carbons, or alkylaryl where the aryl group is substituted with R2; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.
摘要翻译：本发明提供具有以下结构的式I化合物，其中R1为羟基，1-4个碳原子的烷氧基或-O（CH2）nX; n为1-13的整数; X为CONHR6或CO2R6; R2为氢，卤素，羟基，1-4个碳的烷基，1-4个碳的烷氧基或1-4个碳的酰基; R3，R4和R5各自独立地为氢，卤素，羟基，1-4个碳的烷基，1-4个碳原子的烷氧基碳原子，1-4个碳的酰基，CF 3，OCF 3，SO 2 NHR 6，NR 6 R 7或CO 2 R 6; R 6和R 7各自独立地为氢，1-4个碳的烷基或芳基被R 2取代的烷基芳基; 其可用的盐可用于治疗与胰岛素抵抗或高血糖相关的代谢紊乱。

10. 发明授权

US07446201B2 Substituted heteroaryl benzofuran acids 失效
标题翻译：取代的杂芳基苯并呋喃酸
公开(公告)号：US07446201B2
公开(公告)日：2008-11-04
申请号：US10947840
申请日：2004-09-23
申请人： Hassan Mahmoud Elokdah , Geraldine Ruth McFarlane , Scott Christian Mayer
发明人： Hassan Mahmoud Elokdah , Geraldine Ruth McFarlane , Scott Christian Mayer
IPC分类号： C07D215/38
CPC分类号： C07D405/14
摘要： The present invention relates generally to substituted heteroaryl benzofuran acids and methods of using them.
摘要翻译：本发明一般涉及取代的杂芳基苯并呋喃酸及其使用方法。

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