Publication number: 20070254929
Abstract: 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.
Type:
Application
Filed:
June 15, 2007
Publication date:
November 1, 2007
Applicant:
Wyeth
Inventors:
Anthony Kreft, Lynn Resnick, Scott Mayer, George Diamantidis, Derek Cole, Boyd Harrison, Minsheng Zhang, Molly Hoke, Tingzhong Wang, Rocco Galante
Publication number: 20060276429
Abstract: 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
Type:
Application
Filed:
August 17, 2006
Publication date:
December 7, 2006
Applicant:
Wyeth
Inventors:
Scott Mayer, Robert McDevitt, Paul Dollings
Publication number: 20060014725
Abstract: 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.
Type:
Application
Filed:
June 22, 2005
Publication date:
January 19, 2006
Applicant:
Wyeth
Inventors:
Scott Mayer, Eric Gundersen, Hassan Elokdah, David Crandall
Publication number: 20050176652
Abstract: 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
Type:
Application
Filed:
October 31, 2003
Publication date:
August 11, 2005
Applicant:
Wyeth
Inventors:
Scott Mayer, Robert McDevitt, Paul Dollings