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9 条记录 (耗时 0.058 秒)

    Fluoro-and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof
    1.
    发明申请
    Fluoro-and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof 失效
    含有氟和三氟烷基的杂环磺酰胺抑制剂β淀粉样蛋白产生及其衍生物

    公开(公告)号：US20070254929A1

    公开(公告)日：2007-11-01

    申请号：US11818630

    申请日：2007-06-15

    申请人： Anthony Kreft ,  Lynn Resnick ,  Scott Mayer ,  George Diamantidis ,  Derek Cole ,  Boyd Harrison ,  Minsheng Zhang ,  Molly Hoke ,  Tingzhong Wang ,  Rocco Galante

    发明人： Anthony Kreft ,  Lynn Resnick ,  Scott Mayer ,  George Diamantidis ,  Derek Cole ,  Boyd Harrison ,  Minsheng Zhang ,  Molly Hoke ,  Tingzhong Wang ,  Rocco Galante

    IPC分类号： A61K31/433 ,  A61P25/00 ,  C07D285/08

    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，COR 8或C（OH）R 1 R 2 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。

    Acylated benzylmaltosides as inhibitors of smooth muscle cell proliferation
    6.
    发明申请
    Acylated benzylmaltosides as inhibitors of smooth muscle cell proliferation 有权

    公开(公告)号：US20050176652A1

    公开(公告)日：2005-08-11

    申请号：US10699233

    申请日：2003-10-31

    申请人： Scott Mayer ,  Robert McDevitt ,  Paul Dollings

    发明人： Scott Mayer ,  Robert McDevitt ,  Paul Dollings

    IPC分类号： A61K31/704 ,  C07H5/06

    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 wherein R1, R2, R3, R4, and R5 are each, independently, hydrogen, acyl of 2-7 carbon atoms, haloacyl of 2-7 carbon atoms, nitroacyl of 2-7 carbon atoms, cyanoacyl of 2-7 carbon atoms, trifluoromethylacyl of 3-8 carbon atoms, or benzoyl in which the phenyl moiety is substituted with R8; R6 and R7 are each, independently, —OH, —OR9, O-tert-butyldimethylsilyl, O-trialkylsilyl of 1-6 carbon atoms per alkyl moiety, O-triphenylsilyl, R8, R10, R11, and R12 are each, independently, hydrogen, —CN, —NO2, halogen, CF3, alkyl of 1-6 carbon atoms, acetyl, benzoyl, or alkoxy of 1-6 carbon atoms; R9 is acyl of 2-7 carbon atoms, haloacyl of 2-7 carbon atoms, nitroacyl of 2-7 carbon atoms, cyanoacyl of 2-7 carbon atoms, trifluoromethylacyl of 3-8 carbon atoms, or benzoyl in which the phenyl moiety is substituted with R8; Y is O, S, NH, NMe, or CH2; W is halogen, —CN, CF3, alkyl of 1-6 carbon atoms, haloalkyl of 1-6 carbon atoms, nitroalkyl of 1-6 carbon atoms, cyanoalkyl of 1-6 carbon atoms, alkoxyalkyl of 2-12 carbon atoms, alkoxy of 1-6 carbon atoms, or phenyl mono-, di-, or tri-substituted with R8; Z is —NO2, —NH2, —NHR13, or —NHCO-Het; R13 is acyl of 2-7 carbon atoms, haloacyl of 2-7 carbon atoms, nitroacyl of 2-7 carbon atoms, cyanoacyl of 2-7 carbon atoms, trifluoromethylacyl of 3-8 carbon atoms, benzoyl in which the phenyl moiety is substituted with R8, or R13 is an α-amino acid in which the a carboxyl group forms an amide with the nitrogen of Z, wherein if said amino acid is glutamic acid or aspartic acid, the non-α carboxylic acid is an alkyl ester in which the alkyl moiety contains from 1-6 carbon atoms; Het is pyridyl substituted with R8, thienyl substituted with R8, furyl substituted with R8, oxazolyl substituted with R8, pyrazinyl substituted with R8, pyrimidinyl substituted with R8, or thiazolyl substituted with R8; R14 is R8, —NH2, —CO2H, or —NH-acyl of 2-7 carbon atoms; n=0-3; with the proviso that when Z is —NHR13 and Y is O, at least one of R1, R2, R3, R4, and R5 is hydrogen, or at least one of R6 and R7 is OH, or a pharmaceutically acceptable salt thereof.

    Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1)
    8.
    发明申请
    Substituted naphthyl indole derivatives as inhibitors of plasminogen activator inhibitor type-1 (PAI-1) 失效
    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：US20060014725A1

    公开(公告)日：2006-01-19

    申请号：US11158881

    申请日：2005-06-22

    申请人： Scott Mayer ,  Eric Gundersen ,  Hassan Elokdah ,  David Crandall

    发明人： Scott Mayer ,  Eric Gundersen ,  Hassan Elokdah ,  David Crandall

    IPC分类号： A61K31/415 ,  A61K31/404 ,  C07D403/02 ,  C07D209/12

    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 R8, 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：R 1，R 2，R 3和R 4 每个H，烷基，烷酰基，卤素，OH，任选被R 8 8，全氟烷基，烷氧基，氨基，烷基氨基，二烷基氨基，全氟烷氧基取代的芳基; R 5是H，烷基，全氟烷基，任选被R 8取代的芳基，烷酰基，任选被R 8取代的芳酰基; R 6是H，烷基，烷基芳基，任选被R 8取代的苄基，烷酰基，任选被R 8取代的芳酰基; R 7是H，烷基，烷芳基，任选被R 8取代的芳基; n为0-6; A是COOH或酸模拟物，例如四唑，SO 3 H，PO 3 H 2 H 2，次ronic酸等; R 8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。

    Acylated benzylmaltosides as inhibitors of smooth muscle cell proliferation
    9.
    发明申请
    Acylated benzylmaltosides as inhibitors of smooth muscle cell proliferation 失效

    公开(公告)号：US20060276429A1

    公开(公告)日：2006-12-07

    申请号：US11505543

    申请日：2006-08-17

    申请人： Scott Mayer ,  Robert McDevitt ,  Paul Dollings

    发明人： Scott Mayer ,  Robert McDevitt ,  Paul Dollings

    IPC分类号： A61K31/7052 ,  A61K31/7024 ,  C07H17/02

    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 wherein R1, R2, R3, R4, and R5 are each, independently, hydrogen, acyl of 2-7 carbon atoms, haloacyl of 2-7 carbon atoms, nitroacyl of 2-7 carbon atoms, cyanoacyl of 2-7 carbon atoms, trifluoromethylacyl of 3-8 carbon atoms, or benzoyl in which the phenyl moiety is substituted with R8; R6 and R7 are each, independently, —OH, —OR9, O-tert-butyldimethylsilyl, O-trialkylsilyl of 1-6 carbon atoms per alkyl moiety, O-triphenylsilyl, R8, R10, R11, and R12 are each, independently, hydrogen, —CN, —NO2, halogen, CF3, alkyl of 1-6 carbon atoms, acetyl, benzoyl, or alkoxy of 1-6 carbon atoms; R9 is acyl of 2-7 carbon atoms, haloacyl of 2-7 carbon atoms, nitroacyl of 2-7 carbon atoms, cyanoacyl of 2-7 carbon atoms, trifluoromethylacyl of 3-8 carbon atoms, or benzoyl in which the phenyl moiety is substituted with R8; Y is O, S, NH, NMe, or CH2; W is halogen, —CN, CF3, alkyl of 1-6 carbon atoms, haloalkyl of 1-6 carbon atoms, nitroalkyl of 1-6 carbon atoms, cyanoalkyl of 1-6 carbon atoms, alkoxyalkyl of 2-12 carbon atoms, alkoxy of 1-6 carbon atoms, or phenyl mono-, di-, or tri-substituted with R8; Z is —NO2, —NH2, —NHR13, or —NHCO-Het; R13 is acyl of 2-7 carbon atoms, haloacyl of 2-7 carbon atoms, nitroacyl of 2-7 carbon atoms, cyanoacyl of 2-7 carbon atoms, trifluoromethylacyl of 3-8 carbon atoms, benzoyl in which the phenyl moiety is substituted with R8, or R13 is an α-amino acid in which the α carboxyl group forms an amide with the nitrogen of Z, wherein if said amino acid is glutamic acid or aspartic acid, the non-α carboxylic acid is an alkyl ester in which the alkyl moiety contains from 1-6 carbon atoms; Het is pyridyl substituted with R8, thienyl substituted with R8, furyl substituted with R8, oxazolyl substituted with R8, pyrazinyl substituted with R8, pyrimidinyl substituted with R8, or thiazolyl substituted with R8; R14 is R8, —NH2, —CO2H, or —NH-acyl of 2-7 carbon atoms; n=0-3; with the proviso that when Z is —NHR13 and Y is O, at least one of R1, R2, R3, R4, and R5 is hydrogen, or at least one of R6 and R7 is OH, or a pharmaceutically acceptable salt thereof.