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    Heterocyclic Sulfonamide Inhibitors of Beta Amyloid Production Containing an Azole
    3.
    发明申请
    Heterocyclic Sulfonamide Inhibitors of Beta Amyloid Production Containing an Azole 审中-公开
    包含唑类的β淀粉样蛋白的杂环磺酰胺抑制剂

    公开(公告)号：US20100144812A1

    公开(公告)日：2010-06-10

    申请号：US12708557

    申请日：2010-02-19

    申请人： Lynn Resnick ,  Donna M. Huryn ,  Joan E. Sabalski ,  Joshua D. Berkowitz ,  Anthony Frank Kreft ,  Dennis Martin Kubrak ,  Thomas Joseph Caggiano ,  Koi Michele Morris

    发明人： Lynn Resnick ,  Donna M. Huryn ,  Joan E. Sabalski ,  Joshua D. Berkowitz ,  Anthony Frank Kreft ,  Dennis Martin Kubrak ,  Thomas Joseph Caggiano ,  Koi Michele Morris

    IPC分类号： A61K31/4155 ,  A61K31/415 ,  A61K31/41 ,  A61K31/4178 ,  A61K31/4025 ,  A61P25/28 ,  A61P25/00 ,  C07D409/02 ,  C07D231/10

    CPC分类号： A61K31/416 ,  C07D231/12 ,  C07D409/12

    摘要： Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3 is hydrogen, lower alkyl, or substituted lower alkyl; R4 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6 is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7 or N; and R7 is hydrogen, halogen, lower alkyl, or substituted lower alkyl.

    摘要翻译： 提供了可用于降低β淀粉样蛋白水平的化合物。 所述化合物具有式Ia的结构：其中，R 1为低级烷基，取代的低级烷基，苯基，取代的苯基，苄基，取代的苄基，苄氧基，取代的苄氧基或SO 2 R 5; R5是苯基，取代的苯基，杂环，取代的杂环，烷基或取代的烷基; R2是低级烷基，取代的低级烷基，CF3，烯基，取代的烯基，炔基，取代的炔基，苯基，取代的苯基或环烷基; R3是氢，低级烷基或取代的低级烷基; R4是苯基，取代的苯基，杂环，取代的杂环，噻吩或取代的噻吩; R 6是氢，低级烷基，取代的低级烷基，CF 3，烯基，取代的烯基，炔基，取代的炔基，苯基，取代的苯基，环烷基或取代的环烷基; W，X和Y独立地为CR 7或N; 并且R 7是氢，卤素，低级烷基或取代的低级烷基。

    Heterocyclic sulfonamide inhibitors of beta amyloid production containing an azole
    4.
    发明授权
    Heterocyclic sulfonamide inhibitors of beta amyloid production containing an azole 失效
    含有唑类的β-淀粉样蛋白产生的杂环磺酰胺抑制剂

    公开(公告)号：US07674813B2

    公开(公告)日：2010-03-09

    申请号：US12142306

    申请日：2008-06-19

    申请人： Lynn Resnick ,  Donna M. Huryn ,  Joan E. Sabalski ,  Joshua D. Berkowitz ,  Anthony Frank Kreft ,  Dennis Martin Kubrak ,  Thomas Joseph Caggiano ,  Koi Michele Morris

    发明人： Lynn Resnick ,  Donna M. Huryn ,  Joan E. Sabalski ,  Joshua D. Berkowitz ,  Anthony Frank Kreft ,  Dennis Martin Kubrak ,  Thomas Joseph Caggiano ,  Koi Michele Morris

    IPC分类号： A01N43/50 ,  A01N43/56 ,  C07D231/00

    CPC分类号： A61K31/416 ,  C07D231/12 ,  C07D409/12

    摘要： Compounds useful for lowering beta amyloid levels are provided. The compounds have the structure of formula Ia: wherein, R1 is lower alkyl, substituted lower alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl, benzyloxy, substituted benzyloxy, or SO2R5; R5 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, alkyl, or substituted alkyl; R2 is lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, or cycloalkyl; R3 is hydrogen, lower alkyl, or substituted lower alkyl; R4 is phenyl, substituted phenyl, heterocycle, substituted heterocycle, thiophene, or substituted thiophene; R6 is hydrogen, lower alkyl, substituted lower alkyl, CF3, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, phenyl, substituted phenyl, cycloalkyl, or substituted cycloalkyl; W, X and Y are independently CR7 or N; and R7 is hydrogen, halogen, lower alkyl, or substituted lower alkyl.

    摘要翻译： 提供了可用于降低β淀粉样蛋白水平的化合物。 所述化合物具有式Ia的结构：其中，R 1为低级烷基，取代的低级烷基，苯基，取代的苯基，苄基，取代的苄基，苄氧基，取代的苄氧基或SO 2 R 5; R5是苯基，取代的苯基，杂环，取代的杂环，烷基或取代的烷基; R2是低级烷基，取代的低级烷基，CF3，烯基，取代的烯基，炔基，取代的炔基，苯基，取代的苯基或环烷基; R3是氢，低级烷基或取代的低级烷基; R4是苯基，取代的苯基，杂环，取代的杂环，噻吩或取代的噻吩; R 6是氢，低级烷基，取代的低级烷基，CF 3，烯基，取代的烯基，炔基，取代的炔基，苯基，取代的苯基，环烷基或取代的环烷基; W，X和Y独立地为CR 7或N; 并且R 7是氢，卤素，低级烷基或取代的低级烷基。

    Process for the synthesis of chirally pure beta-amino-alcohols
    5.
    发明授权
    Process for the synthesis of chirally pure beta-amino-alcohols 失效
    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。

    FLUORO- AND TRIFLUOROALKYL-CONTAINING HETEROCYCLIC SULFONAMIDE INHIBITORS OF BETA AMYLOID PRODUCTION AND DERIVATIVES THEREOF
    6.
    发明申请
    FLUORO- AND TRIFLUOROALKYL-CONTAINING HETEROCYCLIC SULFONAMIDE INHIBITORS OF BETA AMYLOID PRODUCTION AND DERIVATIVES THEREOF 失效
    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。

    Fluoro- and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof
    8.
    发明授权
    Fluoro- and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof 失效
    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。

    Fluoro- and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof
    9.
    发明授权
    Fluoro- and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof 失效
    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。