Wyeth

Arqule, Inc.

Other

George Diamantidis

Derek Cecil Cole

Anthony Frank Kreft

Dennis Michael Kubrak

Boyd Lynn Harrison

David S Casebier

Kevin R Woller

Scott Christian Mayer

Joseph Raymond Stock

William Jay Moore

Lynn Resnick

Kristina Martha Kutterer

Molly Hoke

Minsheng Zhang

Rocco John Galante

Tingzhong Wang

Jeremy Ian Levin

Yang-I Lin

Jerauld S Skotnicki

Anthony F Kreft, Iii

Thomas Joseph Caggiano

Frank Eldridge Lovering

Koi Morris

Charles William Mann

Zhong Li

Kaapjoo Park

Diane Barbara Hauze

Jeffrey Scott Condon

Weiheng Wang

Alexander Michael Porte

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

Compounds of Formula (I), wherein R, R, R, R, R, R, 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.

Heterocyclic sulfonamide inhibitors of beta amyloid production

Compounds of Formula (I), wherein R, R, R, R, R, R, 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 &#x3b2;-amyloid levels in a subject are described.

Heterocyclic sulfonamide inhibitors of &#x3b2; amyloid production

This invention provides compounds of Formula I, having the structure: that are useful in treating diseases or disorders mediated by TNF-&#x3b1;, such as arthritis (rheumatoid arthritis (RA), juvenile RA, psoriatic arthritis, osteoarthritis etc), tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection, ankylosing spondylitis, psoriasis, sepsis, multiple sclerosis, Crohn's disease, degenerative cartilage loss, asthma, idiopathic pulmonary fibrosis, vasculitis, systemic lupus erythematosus, irritable bowel syndrome, acute coronary syndrome, hepatitis C, cachexia, COPD, stroke or type 2 diabetes, and for alleviation of symptoms thereof. The invention further provides methods for use of the compounds.

Beta-sulfonamide hydroxamic acid inhibitors of tace/matrix metalloproteinase

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.

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.

Compounds of Formula (I),wherein R, R, R, R, R, R, 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

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Randolph, NJ, United States of America

George Diamantidis