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1. 发明授权

US07842718B2 Heterocyclic sulfonamide inhibitors of beta amyloid production 失效
标题翻译： β-淀粉样蛋白生成的杂环磺酰胺抑制剂
公开(公告)号：US07842718B2
公开(公告)日：2010-11-30
申请号：US12576513
申请日：2009-10-09
申请人： Anthony Frank Kreft , Derek Cecil Cole , Kevin R. Woller , Joseph Raymond Stock , George Diamantidis , Dennis Michael Kubrak , Kristina Martha Kutterer , William J. Moore , David S. Casebier
发明人： Anthony Frank Kreft , Derek Cecil Cole , Kevin R. Woller , Joseph Raymond Stock , George Diamantidis , Dennis Michael Kubrak , Kristina Martha Kutterer , William J. Moore , David S. Casebier
IPC分类号： A61K31/381 , C07D333/34
CPC分类号： C07D409/12 , C07D307/64 , C07D333/34
摘要： Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt, hydrates and/or prodrugs thereof. Methods of using these compounds for inhibiting beta amyloid production and for treatment of Alzheimer's disease and Down's syndrome are described.
摘要翻译：提供其中R1，R2，R3，R4，R5，R6，T，W，X，Y和Z如本文所定义的式（I）化合物及其药学上可接受的盐，水合物和/或前药。描述了使用这些化合物抑制β淀粉样蛋白生成和治疗阿尔茨海默病和唐氏综合征的方法。

2. 发明授权

US07671075B2 Substituted phenylsulfonamide inhibitors of beta amyloid production 失效
标题翻译： β-淀粉样蛋白生成的取代苯磺酰胺抑制剂
公开(公告)号：US07671075B2
公开(公告)日：2010-03-02
申请号：US11528001
申请日：2006-09-27
申请人： Anthony Frank Kreft , Derek Cecil Cole , Kevin Roger Woller , Joseph Raymond Stock , Kristina Martha Kutterer , Dennis Martin Kubrak , Charles William Mann , William Jay Moore , David Scott Casebier
发明人： Anthony Frank Kreft , Derek Cecil Cole , Kevin Roger Woller , Joseph Raymond Stock , Kristina Martha Kutterer , Dennis Martin Kubrak , Charles William Mann , William Jay Moore , David Scott Casebier
IPC分类号： A61K31/18 , A61K31/34 , A61K31/357 , A61K31/4245 , C07C311/17 , C07D209/14 , C07D271/12 , C07D307/52 , C07D317/08
CPC分类号： C07C311/40 , A61K31/18 , A61K31/335 , A61K31/34 , A61K31/357 , A61K31/4245 , A61K31/655 , C07C311/17 , C07C311/18 , C07C311/20 , C07C311/29 , C07C323/49 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/42 , C07D209/16 , C07D307/52 , C07D319/06
摘要： Compounds of Formula I, wherein R1-R8 are defined herein are provided, together with pharmaceutically acceptable salts, hydrates, metabolites, and/or prodrugs thereof. Uses of these compounds for inhibiting beta amyloid production and for the prevention and treatment of Alzheimer's Disease and Down's syndrome are also described.
摘要翻译：提供其中R 1 -R 8在本文中定义的式I化合物及其药学上可接受的盐，水合物，代谢物和/或前药。还描述了这些化合物用于抑制β淀粉样蛋白生成和预防和治疗阿尔茨海默病和唐氏综合征的用途。

3. 发明申请

US20100120725A1 Substituted Phenylsulfonamide Inhibitors of Beta Amyloid Production 审中-公开
标题翻译： β淀粉样蛋白生成的取代苯磺酰胺抑制剂
公开(公告)号：US20100120725A1
公开(公告)日：2010-05-13
申请号：US12691193
申请日：2010-01-21
申请人： Anthony Frank Kreft , Derek Cecil Cole , Kevin Roger Woller , Joseph Raymond Stock , Kristina Martha Kutterer , Dennis Martin Kubrak , Charles William Mann , William Jay Moore , David Scott Casebier
发明人： Anthony Frank Kreft , Derek Cecil Cole , Kevin Roger Woller , Joseph Raymond Stock , Kristina Martha Kutterer , Dennis Martin Kubrak , Charles William Mann , William Jay Moore , David Scott Casebier
IPC分类号： A61K31/655 , A61K31/18 , G01N33/53 , C07C303/00 , C09B29/00
CPC分类号： C07C311/40 , A61K31/18 , A61K31/335 , A61K31/34 , A61K31/357 , A61K31/4245 , A61K31/655 , C07C311/17 , C07C311/18 , C07C311/20 , C07C311/29 , C07C323/49 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/42 , C07D209/16 , C07D307/52 , C07D319/06
摘要： Compounds of Formula I, wherein R1-R8 are defined herein are provided, together with pharmaceutically acceptable salts, hydrates, metabolites, and/or prodrugs thereof. Uses of these compounds for inhibiting beta amyloid production and for the prevention and treatment of Alzheimer's disease and Down's syndrome are also described.
摘要翻译：提供其中R 1 -R 8在本文中定义的式I化合物及其药学上可接受的盐，水合物，代谢物和/或前药。还描述了这些化合物用于抑制β淀粉样蛋白生成和预防和治疗阿尔茨海默氏病和唐氏综合征的用途。

4. 发明授权

US07166622B2 Substituted phenylsulfonamide inhibitors of beta amyloid production 失效
标题翻译： β-淀粉样蛋白生成的取代苯磺酰胺抑制剂
公开(公告)号：US07166622B2
公开(公告)日：2007-01-23
申请号：US10457641
申请日：2003-06-09
申请人： Anthony Frank Kreft , Derek Cecil Cole , Kevin Roger Woller , Joseph Raymond Stock , Kristina Martha Kutterer , Dennis Martin Kubrak , Charles William Mann , William Jay Moore , David Scott Casebier
发明人： Anthony Frank Kreft , Derek Cecil Cole , Kevin Roger Woller , Joseph Raymond Stock , Kristina Martha Kutterer , Dennis Martin Kubrak , Charles William Mann , William Jay Moore , David Scott Casebier
IPC分类号： C07C311/17 , C07D209/14 , C07D271/12 , C07D307/52 , C07D317/08 , A61K31/18 , A61K31/34 , A61K31/357 , A61K31/4245
CPC分类号： C07C311/40 , A61K31/18 , A61K31/335 , A61K31/34 , A61K31/357 , A61K31/4245 , A61K31/655 , C07C311/17 , C07C311/18 , C07C311/20 , C07C311/29 , C07C323/49 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07C2602/42 , C07D209/16 , C07D307/52 , C07D319/06
摘要： Compounds of Formula I, wherein R1–R8 are defined herein are provided, together with pharmaceutically acceptable salts, hydrates, metabolites, and/or prodrugs thereof. Uses of these compounds for inhibiting beta amyloid production and for the prevention and treatment of Alzheimer's Disease and Down's syndrome are described.
摘要翻译：提供了其中R 1 -R 8 - 8的式I化合物及其药学上可接受的盐，水合物，代谢物和/或前药。描述了这些化合物用于抑制β淀粉样蛋白生成和预防和治疗阿尔茨海默病和唐氏综合征的用途。

5. 发明授权

US07691884B2 Heterocyclic sulfonamide inhibitors of β amyloid production 失效
标题翻译：杂环磺酰胺抑制剂淀粉样蛋白生成
公开(公告)号：US07691884B2
公开(公告)日：2010-04-06
申请号：US11081784
申请日：2005-03-16
申请人： Anthony Frank Kreft , Derek C. Cole , Kevin R. Woller , Joseph R. Stock , George Diamantidis , Dennis M. Kubrak , Kristina M. Kutterer , William J. Moore , David S. Casebier
发明人： Anthony Frank Kreft , Derek C. Cole , Kevin R. Woller , Joseph R. Stock , George Diamantidis , Dennis M. Kubrak , Kristina M. Kutterer , William J. Moore , David S. Casebier
IPC分类号： A61K31/44 , A61K31/38 , A61K31/335 , A61K31/34 , C07D409/12 , C07D333/34 , C07D407/12 , C07D307/34
CPC分类号： C07D409/12 , C07D307/64 , C07D333/34
摘要： Compounds of Formula (I), wherein R1, R2, R3, R4, R5, R6, T, W, X, Y and Z are as defined herein are provided, together with pharmaceutically acceptable salt, hydrates and/or prodrugs thereof. Methods of using these compounds for determining β-amyloid levels in a subject are described.
摘要翻译：提供其中R1，R2，R3，R4，R5，R6，T，W，X，Y和Z如本文所定义的式（I）化合物及其药学上可接受的盐，水合物和/或前药。描述了使用这些化合物来测定受试者中的β-淀粉样蛋白水平的方法。

6. 发明授权

US06800764B2 Process for the synthesis of chirally pure beta-amino-alcohols 失效
标题翻译：手性纯合β-氨基醇的合成方法
公开(公告)号：US06800764B2
公开(公告)日：2004-10-05
申请号：US10304322
申请日：2002-11-26
申请人： Anthony Frank Kreft , Madelene Miyoko Antane , Derek Cecil Cole , Dennis Martin Kubrak , Lynn Resnick , Joseph Raymond Stock , Zheng Wang
发明人： Anthony Frank Kreft , Madelene Miyoko Antane , Derek Cecil Cole , Dennis Martin Kubrak , Lynn Resnick , Joseph Raymond Stock , Zheng Wang
IPC分类号： C07D33332
CPC分类号： C07C215/20 , C07B2200/07 , C07C215/08 , C07C215/24 , C07C215/28 , C07C215/56 , C07C229/08 , C07C229/28 , C07C229/30 , C07C229/36 , C07C247/12 , C07C323/63 , C07D263/26 , C07D333/34
摘要： A process is provided for preparing chirally pure S-enantiomers of &agr;-amino acids comprising the steps of: a) preparing an organometallic reagent from an alkyl halide of the formula (R)2CH(CH2)nCH2X; b) adding the organometallic reagent to carbon dioxide to afford a carboxylic acid; c) activating the carboxylic acid with an acid chloride, phosphorus trichloride, acid anhydride, or thionyl chloride in the presence of a tertiary amine base; d) reacting the product of step c) with an alkali metal salt of S-4-benzyl-2-oxazolidinone; e) treating the product of step d) with a strong non-nucleophilic base to form an enolate anion; f) trapping the enolate anion with 2,4,6-triisopropylbenzenesulfonyl azide to afford an oxazolidinone azide; g) hydrolyzing the oxazolidinone azide with an aqueous base to afford an &agr;-azido acid; h) reducing the &agr;-azido acid to the &agr;-amino acid; and i) recrystallizing the &agr;-amino acid to the chirally pure &agr;-amino acid. A process is also provided for preparing chirally pure S-enantiomers of &bgr;-amino alcohols further comprising the steps of reducing the crude &agr;-amino acid to the &bgr;-amino alcohol and recrystallizing the &bgr;-amino alcohol to the chirally pure &bgr;-amino alcohol. A process is further provided for preparing chirally pure S enantiomers of N-sulfonyl &bgr;-amino alcohols further comprising the steps of sulfonylating the &bgr;-amino alcohol with 5-chloro-thiophene-2-sulfonyl halide; and recrystallizing to afford the chirally pure N-sulfonyl &bgr;-amino alcohols.
摘要翻译：提供了一种用于制备α-氨基酸的手性纯的S-对映异构体的方法，包括以下步骤：a）由式（R）2CH（CH 2）n CH 2 X的烷基卤制备有机金属试剂; b）将有机金属试剂加入到二氧化碳中，得到羧酸; c）在叔胺碱存在下用酰氯，三氯化磷，酸酐或亚硫酰氯活化羧酸; d）使步骤c）的产物与S-4-苄基-2-恶唑烷酮的碱金属盐反应; e）用强非亲核碱处理步骤d）的产物以形成烯醇化物阴离子; f）用2,4,6-三异丙基苯磺酰叠氮化物捕获烯醇化阴离子，得到恶唑烷酮叠氮化物; g）用碱水溶液水解恶唑烷酮叠氮化物，得到α-叠氮基; h）将α-叠氮基还原成α-氨基酸; 和i）将α-氨基酸重结晶至手性纯的α-氨基酸。还提供了制备β-氨基醇的手性纯的S-对映异构体的方法，该方法还包括将β-氨基酸的粗α-氨基酸还原成β-氨基醇，并将β-氨基醇重结晶至手性纯的β-氨基醇。还提供了制备N-磺酰基β-氨基醇的手性纯S对映异构体的方法，其还包括用5-氯 - 噻吩-2-磺酰卤磺酰化β-氨基醇的步骤; 并重结晶得到手性纯的N-磺酰基β-氨基醇。

7. 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。

8. 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。

9. 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。

10. 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。

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