Wyeth

Molly Hoke

Boyd Lynn Harrison

Anthony Frank Kreft

Scott Christian Mayer

George Diamantidis

Derek Cecil Cole

Minsheng Zhang

Lynn Resnick

Rocco John Galante

Tingzhong Wang

Amedeo A Failli

Mark Anthony Ashwell

Thomas Joseph Caggiano

Dennis Michael Kubrak

Madelene M Antane

William Ronald Solvibile

Koi Morris

William Jay Moore

Brian Hugh Ridgway

Charles William Mann

Diane Barbara Hauze

Alexander Michael Porte

Amy Tsai-Ting Lee

Compounds of Formula (I), are provided where T is CHO, COR, or C(OH)RR; Rand Rare hydrogen, optionally substituted lower alkyl, CF, optionally substituted alkenyl, or optionally substituted alkynyl; Ris hydrogen or optionally substituted lower alkyl; Ris (CF)alkyl, (CF)(substitutedalkyl), (CF)alkylphenyl, (CF)alkyl(substitutedphenyl), or (F)cycloalkyl; n=1-3; Ris hydrogen, halogen, CF, diene fused to Y when Y=C, or substituted diene fused to Y when Y=C; W, Y and Z are C, CRor N where at least one of W, Y or Z are C; Ris hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO, or NR; Ris hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and Ris lower alkyl, CF, 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.

Fluoro- and trifluoroalkyl-containing heterocyclic sulfonamide inhibitors of beta amyloid production and derivatives thereof

A compound of Formula (I), or pharmaceutically acceptable salts and/or hydrates or prodrugs thereof, wherein Formula (I) has the structure: is provided, wherein R-Rare defined herein. These compounds are useful in medicaments for treating a disease selected from the group consisting of Alzheimer's Disease, amyloid angiopathy, cerebral amyloid angiopathy, systemic amyloidosis, hereditary cerebral hemorrhage with amyloidosis of the Dutch type, inclusion body myositis, mild cognitive impairment (MCI) and Down's syndrome, in a subject.

Trifluoromethyl-containing phenylsulfonamide beta amyloid inhibitors

Compounds of Formula (I), are provided where T is CHO, COR, or C(OH)RR; Rand Rare hydrogen, optionally substituted lower alkyl, CF, optionally substituted alkenyl, or optionally substituted alkynyl; Ris hydrogen or optionally substituted lower alkyl; Ris (CF)alkyl, (CF)(substituted alkyl), (CF)alkylphenyl, (CF)alkyl(substituted phenyl), or (F)cycloalkyl; n=1-3; Ris hydrogen, halogen, CF, diene fused to Y when Y&#x2550;C, or substituted diene fused to Y when Y&#x2550;C; W, Y and Z are C, CRor N where at least one of W, Y or Z are C; Ris hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO, or NR; Ris hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and Ris lower alkyl, CF, 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.

Synthetic methods are provided for production of compounds of the formula: where R, R, R, R, R, R, R, R, R, R, R, R, Rand Rare as defined in the specification.

Processes for preparing 6-alkyl-5-arylsulfonyl-dihydrophenanthridines

Compounds of Formula (I), are provided where T is CHO, CON, or C(OH)RR; Rand Rare hydrogen, optionally substituted lower alkyl, CF, optionally substituted alkenyl, or optionally substituted alkynyl; Ris hydrogen or optionally substituted lower alkyl; Ris (CF)alkyl, (CF)(substitutedalkyl), (CF)alkylphenyl, (CF)alkyl(substitutedphenyl), or (F)cycloalkyl; n=1-3; Ris hydrogen, halogen, CF, diene fused to Y when Y&#x2550;C, or substituted diene fused to Y when Y&#x2550;C; W, Y and Z are C, CRor N where at least one of W, Y or Z are C; Ris hydrogen, halogen, or optionally substituted lower alkyl; X is O, S, SO, or NR; Ris hydrogen, optionally substituted lower alkyl, optionally substituted benzyl, or optionally substituted phenyl; and Ris lower alkyl, CF, 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.

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Hightstown, NJ, United States of America

Molly Hoke