Hoffmann-la Roche Inc.

Syntex (u.s.a.) Inc.

Roche Palo Alto LLC

Syntex LLC

Hans Maag

Perry Rosen

George W Holland

David Bruce Repke

Ralph New Harris, Iii

Lawrence Emerson Fisher

Russell Stephen Stabler

Charles Alois Dvorak

Anthony Prince

Keena Lynn Green

Samuel J Rose

Ivan Kompis

John J Nestor

John J Nestor, Jr

Daisy Joe Du Bois

Beat Schmidt

Rita Locher

Scott William Womble

David Bernard Smith

Robin D Clark

Michael Patrick Dillon

Shu-Hai Zhao

Ernest J Prisbe

Todd Richard Elworthy

David Garrett Loughhead

Clara Jeou Jen Lin

Julien P Verheyden

David Nigel Hurst

Joan Marie Caroon

Ferdinand K Lee

Meng Sui

Jason Manka

Sharathchandra Surendra Hegde

Sunil Sahdeo

Compounds of the formula: wherein R, R, Ar, Ar, and n are as defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the subject compounds.

Tetrazole-substituted aryl amide derivatives and uses thereof

Compounds of the formula: wherein Ar, Ar, Rand Rare as defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the subject compounds.

Cyclopropyl aryl amide derivatives and uses thereof

This invention relates to compounds which are generally muscarinic M2/M3 receptor antagonists and which are represented by Formula I: wherein X, Y, and Z are O, S or NR, and the other substituents are as defined in the specification; and prodrugs, individual isomers, racemic or non-racemic mixtures of isomers, and pharmaceutically acceptable salts or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and methods for their use as therapeutic agents.

Heterocyclylakylamines as muscarinic receptor antagonists

Compound of the Formula: and pharmaceutically acceptable salts or prodrugs thereof, wherein: X is CH or N, Y is C or S, Z is &#x2014;SO&#x2014; or &#x2014;(CRR)&#x2014;, n is 1 or 2, Ris aryl or heteroaryl, and R, R, R, R, R, R, R, R, R, R, m, p, q and r, are as defined herein. The compounds are modulators of the 5-HT6 receptor and are useful for treatment of central nervous system disorders. Also provided are methods for preparing, compositions comprising, and methods for using Compounds of Formula I.

Substituted benzoxazinones and uses thereof

Heterocyclylalkylamines as muscarinic receptor antagonists

This invention relates to muscarinic receptor antagonist compounds selected from the group of compounds represented by Formula I:

2-arylethyl-(piperidin-4-ylmethyl)amine derivatives

The L-monovaline ester derived from 2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol and its pharmaceutically acceptable salts are of value as antiviral agents with improved absorption.

2- (2-amino-1,6-dihydro-6-oxo-purin-9-yl) methoxy-1,3- propanediol

2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl)methoxy-1,3-propanediol

2-(2-amino-1,6-dihydro-6-oxo-purin-9-yl) methoxy-1,3-propanediol

This invention relates to use of oligonucleotides having at least one nucleotide that is substituted at the 4'-position of the sugar moiety with a substituent other than hydrogen as nucleotide probes in methods for detecting the presence or amount of a polynucleotide analyte in a sample suspected of containing the polynucleotide analyte. These oligonucleotides can also be packaged in diagnostic assay kits.

Methods of detecting nucleic acids with nucleotide probes containing

Compounds of the Formula I ##STR1## wherein X is hydrogen, chloro, amino or hydroxy; R.sup.1 is an achiral amino acid acyl residue with a tertiary .alpha.-carbon atom. Preferred achiral amino acid acyl residues have the formula ##STR2## wherein each R.sup.2 is alkyl with 1 to 6 carbon atoms, cycloalkyl with 3 to 5 carbon atoms, or benzyl; or the two R.sup.2 groups link together to form a polymethylene group with 3 to 9 carbon atoms, and pharmaceutically acceptable salts thereof are antiviral agents with improved absorption. Intermediates for the preparation of the compounds of Formula I are also described.

Achiral amino acid acyl esters of ganciclovir and its derivatives

Nucleoside compounds of the formula ##STR1## wherein: B is a purine or a pyrimidine; X and X' are H, OH or F, provided that at least one is H; Y and Y' are H, OH, OCH.sub.3 or F, provided that at least one is H; Y' and Z together form a cyclic phosphate ester, provided that Y is H; or Z is ##STR2## where n is zero, one, two or three; and Z' is N.sub.3 or OCH.sub.3 ; provided that when X' and Y' are OH and Z' is N.sub.3, B is not cytosine, and when X' and Y' are OH and Z' is OCH.sub.3, B is not uracil, adenine or cytosine; and the pharmaceutically acceptable esters, ethers and salts thereof, have been found to have potent antiviral activity with a high therapeutic ratio.

Antiviral agents

This invention relates to oligonucleotides having at least one nucleotide that is substituted at the 4' position of the sugar moiety with a substituent other than hydrogen. These oligonucleotides are useful in hybridization assays and as therapeutic agents.

Oligonucleotides containing 4'-substituted nucleotides

16-Cycloalkyl-7-fluoro prostacyclins having a 16 lower alkyl or fluoro substituent useful as blood platelet anti-aggregating agent, vasodilators, cyto protective lowering agents, anti-ulcerogenic agent and for treating peripheral vascular diseases such as schleroderma.

16-cycloalkyl-7-fluoro-prostacyclins

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Menlo Park, CA, United States of America

Hans Maag