American Home Products Corporation

Wyeth

William Floyd Fobare

Donald P Strike

Michael Sotirios Malamas

William Ronald Solvibile

Dominick Anthony Quagliato

Richard Dale Coghlan

James Joseph Erdei

Albert Jean Robichaud

Ping Zhou

Iwan Suwandi Gunawan

Yinfa Yan

Patrick Michael Andrae

Jill Freymuller

Eugene John Trybulski

James C Keith, Jr

Frank Eldridge Lovering

Heather Anne Harris

Leo M Albert

Schuyler Adam Antane

Jeffrey Scott Condon

Patrick M Andrae

The present invention provides an amino-pyridine compound of formula I  The present invention also provides methods for the use thereof to inhibit &#x3b2;-secretase (BACE) and treat &#x3b2;-amyloid deposits and neurofibrillary tangles.

Amino-pyridines as inhibitors of &#x3b2;-secretase

The present invention provides a 2-amino-5-heteroaryl-5-phenylimidazolone compound of formula I  The present invention also provides methods for the use thereof to inhibit &#x3b2;-secretase (BACE) and treat &#x3b2;-amyloid deposits and neurofibrillary tangles.

Amino-5-(5-membered)hetero-arylimidazolone compounds and the use thereof for &#x3b2;-secretase modulation

This invention provides estrogen receptor modulators having the structure: wherein Rto Rare as defined in the specification; or a pharmaceutically acceptable salt thereof.

Thienoisoquinoline-phenylsulfonamides and their use as ER-NF&#x3ba;B inhibitors

The present invention provides a substituted thienyl or furyl acylguanidine compound of formula I The present invention also provides methods for the inhibition of &#x3b2;-secretase (BACE) and for the treatment of &#x3b2;-amyloid deposits and neurofibrillary tangles.

Substituted thienyl and furyl acylguanidines and methods of their use as beta-secretase modulators

The present invention provides a 2-amino-5-[4-(difluoromethoxy)phenyl]-5-phenylimidazolone compound of formula I  The present invention also provides methods for the use thereof to inhibit &#x3b2;-secretase (BACE) and treat &#x3b2;-amyloid deposits and neurofibrillary tangles.

Amino-5-[4-(difluoromethoxy)phenyl]-5-phenylimidazolone compounds for the inhibition of &#x3b2;-secretase

Phenyl substituted thiophenes as estrogenic agents

Phenyl-oxo-tetrahydroquinolin-3-yl beta-3 adrenergic receptor agonists

Piperidino-phenyl amino squarate and thiadiazole dioxide beta-3 adrenergic receptor agonists

Phenyl amino squarate and thiadiazole dioxide beta-3 adrenergic receptor agonists

The compounds of the formula: ##STR1## in which X, Y and Z are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino, dialkylamino, alkyl, alkoxy or phenylalkyloxy; R.sub.1 is thienyl, imidazolyl, thiazolyl, pyridinyl, quinolinyl, pyrimidinyl, pyrazinyl, benzamidazolyl, phenylalkylpiperidinyl or morpholino or athaae analogous hetercyclic groups with from one to three substituents selected from halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino of 1 to 6 carbon atoms, dialkylamino in which each alkyl group has 1 to 6 carbon atoms, alkyl of 1 to 6 carbon atoms, or alkoxy of 1 to 6 carbon atoms; R.sub.2 is hydrogen, alkyl, cycloalkyl, phenyl, benzyl or substituted phenyl or benzyl in which said substituent is alkyl, alkoxy, halogen, cyano, trifluoromethyl amino, nitro, alkylamino or dialkylamino; and a pharmaceutically acceptable salt thereof; are ACAT inhibitors, some of which possess antioxidant properties.

N,N',N'-trisubstituted-5-bisaminomethylene-1,3-dioxane-4,6-dione

The compounds of the formula: ##STR1## in which X, Y and Z are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino, dialkylamino, alkyl, alkoxy or phenylalkyloxy; R.sub.1 is thienyl, imidazolyl, thiazolyl, pyridinyl, quinolinyl, pyrimidinyl, pyrazinyl, benzamidazolyl, phenylalkylpiperidinyl or morpholino or athaae analogous hetercyclic groups with from one to tahree substituents selected from halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino of 1 to 6 carbon atoms, dialkylamino in which each alkyl group has 1 to 6 carbon atoms, alkyl of 1 to 6 carbon atoms, or alkoxy of 1 to 6 carbon atoms; R.sub.2 is hydrogen, alkyl, cycloalkyl, phenyl, benzyl or substituted phenyl or benzyl in which said substituent is alkyl, alkoxy, halogen, cyano, trifluoromethyl amino, nitro, alkylamino or dialkylamino; and a pharmaceutically acceptable salt thereof; are ACAT inhibitors, some of which possess antioxidant properties.

A compound of the formula: ##STR1## in which X, Y and Z are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino, dialkylamino, alkyl or alkoxy; R.sub.1 is hydrogen, alkyl, alkenyl, cycloalkyl, phenyl, benzyl or substituted phenyl or benzyl or alkoxy; or a pharmaceutically acceptable salt thereof are ACAT inhibitors.

N-phenyl-N'-benzothienylmethyl-bis-diamino-5-methylene-1,3-diox

The compounds of the formula: ##STR1## in which X, Y and Z are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino, dialkylamino, alkyl, alkoxy or phenylalkyloxy; R.sub.1 is alkyl, hydroxyalkyl, alkenyl, cycloalkyl, phenylcycloalkyl, 1-hydroxymethylphenethyl, 1-(t-butyl)dimethylsilyloxymethyl-phenethyl, 1-(t-butyl)dimethylsilyloxymethylisopentyl, 1-hydroxymethylisopentyl, phenyl, benzyl or substituted phenyl or benzyl, where the substituents are alkyl, alkoxy, halogen, cyano, trifluoromethyl, amino, alkylamino, dialkylamino, nitro or phenyl, benzyl, phenethyl or R.sub.1 is thienyl, imidazolyl, thiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, benzamidazolyl, phenylalkylpiperidinyl or morpholino; R.sub.2 is alkyl, cycloalkyl, phenyl, benzyl or substituted phenyl or benzyl in which said substituent is alkyl, alkoxy, halogen, cyano, trifluoromethyl amino, nitro, alkylamino or dialkylamino; and a pharmaceutically acceptable salt thereof; are ACAT inhibitors, some of which possess antioxidant properties.

Growing community of inventors

Lawrenceville, NJ, United States of America

William Floyd Fobare