American Home Products Corporation

Wyeth

Viropharma Incorporated

Wyeth, Five Giralda Farms

John W Ellingboe

Jehan F Bagli

Thomas R Alessi

Zhilian Tang

Chingfan Chiu

Madelene Nikaido

John Anthony Butera

Ariamala Gopalsamy

Tarek Suhayl Mansour

Thomas T Nguyen

Richard Eric Mewshaw

Christopher J Burns

Richard M Soll

Derek Cecil Cole

Stephen M Condon

Michael David Collini

Louis John Lombardo

Ping Zhou

Matthew G Laporte

Michael W Winkley

Frank Eldridge Lovering

Magda Asselin

Eric Steven Manas

Koi Morris

Joseph Raymond Stock

Lee Dalton Jennings

William Jay Moore

James J Bicksler

Kaapjoo Park

Terence M Dolak

Jeffrey Scott Condon

Sarah Ta Novak

Dimitri Sarantakis

Mohani Nirmala Sukhdeo

Junjun Wu

Marc S Collett

The present invention provides an azolylacylquanidine 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.

Azolylacylguanidines as &#x3b2;-secretase inhibitors

The invention is directed to methods of treating, preventing, or inhibiting a Hepatitis C viral infection in a mammal comprising contacting the mammal with an effective amount of a compound of the formula: Wherein substitutions at R, R, R&#x2014;R, and Y are set forth in the specification.

Method for the use of pyranoindole derivatives to treat infection with Hepatitis C virus

The invention is directed to a compound and a pharmaceutical composition of the formula: Wherein substitutions at R, R, R-R, and Y are set forth in the specification.

R-enantiomers of pyranoindole derivatives and the use thereof for the treatment of hepatitis C virus infection or disease

2,4,6-trisubstituted pyridines with estrogenic activity and methods for the solid phase synthesis thereof

2,4,6-trisbstituted pyridines with estrogenic activity and methods for the solid phase synthesis thereof

2,4,6-trisubstituted pryridines with estrogenic activity and methods for the solid phase synthesis thereof

2,4,6-trisubstituted pyridines with estrogenic activity and methods for the solid phase synthesis

This invention provides novel compounds and pharmaceutical compositions and methods of using the compounds in the treatment of central nervous system disorders, such as anxiety and depression, the compounds having the formula I:

&lsqb;(Indol-3-yl)-cycloalkyl&rsqb;-3-substituted azetidines for the treatment of central nervous system disorders

The present invention relates to novel substituted indole compounds of formula (I) ##STR1## having pharmacological activity, to processes for their preparation, to solid phase methods for preparing libraries of the compounds, to utilizing libraries of the compounds for drug discovery, and to pharmaceutical compositions thereof.

Methods for the solid phase synthesis of substituted indole compounds

This invention relates to acylated benzylglycosides and a method for their use as smooth muscle cell proliferation inhibitors and as therapeutic compositions for treating diseases and conditions which are characterize by excessive smooth muscle proliferation, such as restenosis. The acylated benzylglycosides of this invention are those of formula I, below: ##STR1## wherein X is ##STR2## R.sup.1 is H, alkyl having 1 to 6 carbon atoms, chloro, bromo, or alkoxy having 1 to 6 carbon atoms;

Acylated benzylglycosides as inhibitors of smooth muscle cell

This invention relates to the use of polyanionic benzylglycosides as smooth muscle cell proliferation inhibitors and as therapeutic compositions for treating diseases and conditions which are characterized by excessive smooth muscle proliferation, such as restenosis. The compounds of this invention are those of formula I ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are, independently, H, SO.sub.3 M, or ##STR2## and each oligosaccharide group contains 1 to 3 sugar groups; M is lithium, sodium, potassium, or ammonium; n is 1 or 2; X is a halogen, lower alkyl having 1 to 6 carbon atoms, or lower alkoxy having 1 to 6 carbon atoms; Y is carbonyl or sulfonyl; Z is alkyl from 1 to 12 carbon atoms, ##STR3## and X is as defined above; or a pharmaceutically acceptable salt thereof.

Polyanionic benzylglycosides as inhibitors of smooth muscle cell

This invention relates to pyrrolo-, pyrido-, azepino-, and azocinopyrimidines of the general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently H, lower alkyl containing 1 to 6 carbon atoms, or perfluoroalkyl containing 1 to 6 carbon atoms; R.sup.5 is H or, when n is 1, R.sup.5 taken together with R.sup.3 comprises a double bond, n is 0 or 1, p is 0 to 2, m is 0 to 3; Ar.sup.1 is ##STR2## wherein W is H, lower alkyl containing 1 to 6 carbon atoms, halogen, hydroxy, or lower alkoxy containing 1 to 6 carbon atoms; and Ar.sup.2 is ##STR3## wherein X is ##STR4## wherein R.sup.6 is H, tert-butyl, tri-n-butylstannyl, or triphenylmethyl; and the pharmaceutically acceptable salts thereof, which compounds are useful in the treatment of hypertension and congestive heart failure.

Substituted pyrrolopyrimidines and pyridopyrimidines useful as

This invention relates to substituted pyridopyrimidinones of general formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are independently H, lower alkyl containing 1 to 6 carbon atoms, hydroxyalkyl containing 1 to 6 carbon atoms, formyl, carbonylalkyl containing 1 to 6 carbon atoms, carboxy, or carboxyalkyl containing 1 to 6 carbon atoms; R.sup.3 and R.sup.4 are independently H, lower alkyl containing 1 to 6 carbon atoms, hydroxy; R.sup.3a and R.sup.4a are H, and when taken together with R.sup.3 and R.sup.4 respectively comprise a carbonyl; with the proviso that at least one of the groups R1 and R.sup.2 must be hydroxyalkyl, formyl, carbonylalkyl containing 1 to 6 carbon atoms, carboxy, or carboxyalkyl containing 1 to 6 carbon atoms; or R.sup.3 and R.sup.4 must be hydroxy or taken together with R.sup.3a and R.sup.4a respectively must comprise a carbonyl; n is 0 to 3; Ar.sup.1 is ##STR2## wherein W is H, lower alkyl containing 1 to 6 carbon atoms, halogen, hydroxy, or lower alkoxy containing 1 to 6 carbon atoms; Ar.sup.2 is ##STR3## wherein X is CO.sub.2 H, CN, or ##STR4## wherein R.sup.5 is H, CH.sub.3, tert-butyl, tri-n-butylstannyl, or triphenylmethyl; and the pharmaceutically acceptable salts thereofuseful for treating hypertension and congestive heart failure, to pharmaceutical compositions, and to methods for production thereof.

Substituted pyridopyrimidines and antihypertensives

There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are defined in the specification; n is 1 to 3;

Substituted benzimidazoles and quinazolines as antihypertensives

This invention relates to substituted 4-aminopyrimidines, which by virtue of their ability to antagonize angiotensin II are useful for the treatment of hypertension, congestive heart failure, and restenosis. The compounds are also useful for reducing lipid levels in the blood plasma and are thus useful for treating hyperlipidemia and hypercholesterolemia. Also disclosed are processes for the production of said compounds and pharmaceutical compositions containing said compounds.

Substituted aminopyrimidines as antihypertensives

Growing community of inventors

Princeton, NJ, United States of America

John W Ellingboe