Sterling Winthrop Inc.

Janssen Pharmaceutica Nv

Wyeth

Nycomed Imaging As

Viropharma Incorporated

Other

Sanofi

Sanofi Sa

Ashis Kumar Saha

Robert A Snow

Li Liu

Henry Joseph Breslin

David William End

Daniel J Delecki

Bart Lieven Daniel De Corte

Thomas R Bailey

Christopher J Burns

Theodore John Nitz

Bruce Edward Tomczuk

Hao Feng

Susan R Rippin

Yijun Deng

David J Rys

Thomas A Lessen

Thomas Faitg

Robert C Wahl

Alfred Michael Del Vecchio

John Swestock

Madhusudhan R Gowravaram

Jeffrey Johnson

Ewell R Cook

Alan M Mathiowetz

Jason A Reinhardt

Bheemashankar A Kulkarni

Charles W Blackledge

Frederick H Hausheer

Patrick René Angibaud

Marc Gaston Venet

John L Toner

Prasad V Chaturvedula

Laurence Anne Mevellec

Alexander L Weis

Bruce J Murray

David A Hilborn

Timothy Z Hossain

Chandra R Shah

Clyde W Shearman

Richard Philion

The present invention relates to benzofuran derivatives and analogs, as well as compositions containing the same and to the use thereof for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the hepatitis C virus.

Benzofuran compounds, compositions and methods for treatment and prophylaxis of hepatitis C viral infections and associated diseases

a prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein Land Lare R&#x2014;Y&#x2014; wherein each (R&#x2014;Y)&#x2014; substituent is defined independently of the other; Y is Calkanediyl, Calkenediyl, Calkynediyl, C(&#x2550;O), or a direct bond; Ris hydrogen, cyano, aryl or a substituted or unsubstituted Cheterocycle; &#x2550;Z&#x2014;Z&#x2550;Z&#x2014; represents a radical of formula &#x2550;N&#x2014;N&#x2550;CH&#x2014; (a-1), &#x2550;N&#x2014;CH&#x2550;N&#x2014; (a-2), &#x2550;CH&#x2014;N&#x2550;N&#x2014; (a-3); X is SO, (CH), wherein n is 1 to 4, C(&#x2550;O), C(&#x2550;S), or a direct bond; Ris aryl, Ccycloalkyl, Ccycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted Cheterocycle, Ccycloalkyl, hydroxycarbonyl, Calkyloxycarbonyl, hydroxyCalkyl, hydroxyCalkyloxy, hydroxyCalkylthio and arylCalkylthio, Calkyl or Calkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted Cheterocycle, Ccycloalkyl, hydroxycarbonyl, Calkyloxycarbonyl, hydroxyCalkyl, hydroxyCalkyloxy, hydroxyCalkylthio and arylCalkylthio; Ris aryl, &#x2014;NRR, a substituted or unsubstituted Cheterocycle, or Calkenediyl substituted with a substituted or unsubstituted Cheterocycle or aryl; Ris hydrogen, aryl, Ccycloalkyl, Calkyl or Calkyl substituted with Ccycloalkyl, hydroxycarbonyl, Calkyloxycarbonyl or aryl; Rand Rare each independently selected from hydrogen, a substituted or unsubstituted Cheterocycle, aryl, Calkyl and Calkyl substituted with one or more substituents selected from hydroxy, aryl, aryloxy or a substituted or unsubstituted Cheterocycle.

Triazoles as farnesyl transferase inhibitors

A prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein Land Lare R&#x2014;Y&#x2014; wherein each (R&#x2014;Y)&#x2014; substituent is defined independently of the other; Y is Calkanediyl, Calkenediyl, Calkynediyl, C(&#x2550;O), or a direct bond; Ris hydrogen, cyano, aryl or a substituted or unsubstituted Cheterocycle; =Z-Z=Z- represents a radical of formula &#x2550;N&#x2014;N&#x2550;CH&#x2014; (a-1), &#x2550;N&#x2014;CH&#x2550;N&#x2014; (a-2), &#x2550;CH&#x2014;N&#x2550;N&#x2014; (a-3); X is SO, (CH)wherein n is 1 to 4, C(&#x2550;O), C(&#x2550;S), or a direct bond; Ris aryl, Ccycloalkyl, Ccycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted Cheterocycle, Ccycloalkyl, hydroxycarbonyl, Calkyloxycarbonyl, hydroxyCalkyl, hydroxyCalkyloxy, hydroxyCalkylthio and arylCalkylthio, Calkyl or Calkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted Cheterocycle, Ccycloalkyl, hydroxycarbonyl, Calkyloxycarbonyl, hydroxyCalkyl, hydroxyCalkyloxy, hydroxyCalkylthio and arylCalkylthio; Ris aryl, &#x2014;NRR, a substituted or unsubstituted Cheterocycle, or Calkenediyl substituted with a substituted or unsubstituted Cheterocycle or aryl; Ris hydrogen, aryl, Ccycloalkyl, Calkyl or Calkyl substituted with Ccycloalkyl, hydroxycarbonyl, Calkyloxycarbonyl or aryl; Rand Rare each independently selected from hydrogen, a substituted or unsubstituted Cheterocycle, aryl, Calkyl and Calkyl substituted with one or more substituents selected from hydroxy, aryl, aryloxy or a substituted or unsubstituted Cheterocycle. 

The present invention relates to novel benzofuran derivatives and analogs, as well as compositions containing the same and to the use thereof for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the hepatitis C virus.

This invention comprises the compounds of formula (I): wherein r, s, t, Y&#x2013;Y, R, R, R, R, R, Rand Rhave defined meanings, having farnesyl transferase inhibiting activity; their preparation, compositions containing them and their use as a medicine.

Farnesyl transferase inhibiting 6-[(substituted phenyl)methyl]-quinoline and quinazoline derinazoline derivatives

a prodrug, N-oxide, addition salt, quaternary amine or stereochemically isomeric form thereof, wherein Land Lare R&#x2014;Y&#x2014; wherein each (R&#x2014;Y)&#x2014; substituent is defined independently of the other; Y is Calkanediyl, Calkenediyl, Calkynediyl, C(&#x2550;O), or a direct bond; Ris hydrogen, cyano, aryl or a substituted or unsubstituted Cheterocycle; &#x2550;Z&#x2014;Z&#x2550;Z&#x2014; represents a radical of formula &#x2550;N&#x2014;N&#x2550;CH&#x2014; (a-1), &#x2550;N&#x2014;CH&#x2550;N&#x2014; (a-2), &#x2550;CH&#x2014;N&#x2550;N&#x2014; (a-3); X is SO, (CH)wherein n is 1 to 4, C(&#x2550;O), C(&#x2550;S), or a direct bond, Ris aryl, Ccycloalkyl, Ccycloalkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted Cheterocycle, Ccycloalkyl, hydroxycarbonyl, Calkyloxycarbonyl, hydroxyCalkyl, hydroxyCalkyloxy, hydroxyCalkylthio and arylCalkylthio, Calkyl or Calkyl substituted with one or more substituents independently selected from hydroxy, aryl, aryloxy, a substituted or unsubstituted Cheterocycle, Ccycloalkyl, hydroxycarbonyl, Calkyloxycarbonyl, hydroxyCalkyl, hydroxyCalkyloxy, hydroxyCalkylthio and arylCalkylthio; Ris aryl, &#x2014;NRR, a substituted or unsubstituted Cheterocycle, or Calkenediyl substituted with a substituted or unsubstituted Cheterocycle or aryl; Ris hydrogen, aryl, Ccycloalkyl, Calkyl or Calkyl substituted with Ccycloalkyl, hydroxycarbonyl, Calkyloxycarbonyl or aryl; Rand Rare each independently selected from hydrogen, a substituted or unsubstituted Cheterocycle, aryl, Calkyl and Calkyl substituted with one or more substituents selected from hydroxy, aryl, aryloxy or a substituted or unsubstituted Cheterocycle.

A method for diagnostic imaging a site in a patient. The method involves the use of an immunoreactive group which is linked to an unsymmetrical oligo-2,6-pyrimidine complexing agent.

Unsymmetrical complexing agents and targeting immunoreagents useful in therapeutic and diagnostic compositions and methods

Disclosed are novel bifunctional nucleoside analogs and oligonucleosides of 3-4 bases (trimers and tetramers) and longer containing at least two consecutive internucleoside linkages of two carbon-one nitrogen atom or two carbon-one oxygen atom (3'-NCC-5', 3'-CNC-5', 3'-OCC-5') internucleoside linkages. The bifunctional nucleosides are useful for preparing the trimers and tetramers, which, in turn, are useful, together with the nucleosides, in preparing oligonucleosides as well as chimeric oligonucleotide analogs, preferably antisense oligonucleosides and oligonucleotide analogs, of 6 to about 60 bases having at least two consecutive internucleoside linkages of two carbon atoms and one nitrogen atom or 2 carbon atoms and one oxygen atom in the oligonucleoside backbone.

Bifunctional nucleosides, oligomers thereof, and methods of making and

Described are novel, unsymmetrical oligo-2,6-pyridine complexing agents. Also described are metal chelates and targeting immunoreagents containing such completing agents as well as diagnostic and therapeutic compositions containing such immunoreagents and diagnostic and therapeutic methods of using the immunoreagents.

Unsymmetrical complexing agents and targeting immunoreagents useful in

The invention provides targeting radioactive immunoreagents comprising a metal radionuclide ion, a complexing agent having structure A-I, as defined in the specification, and an immunoreactive group covalently bonded to the complexing agent. The present invention also provides novel complexing agents having the structure A-I, as defined in the specification. The targeting radioactive immunoreagents are particularly useful in therapeutic and diagnostic imaging compositions and methods.

Pyridine complexing agents and targeting immunoreagents useful in

This disclosure relates to a novel class of hydroxamic and carboxylic acid based matrix metalloproteinase inhibitor derivatives. The disclosure further relates to pharmaceutical compositions containing such compounds and to the use of such compounds and compositions in the treatment of matrix metalloproteinase induced diseases.

Hydroxamic acid and carboxylic acid derivatives, process for their

##STR1## Unsymmetrical oligo-2,6-pyridine complexing agents, metal chelates and targeting immunoreagents containing such complexing agents are provided, as well as diagnostic and therapeutic compositions containing such immunoreagents and diagnostic and therapeutic methods of using the immunoreagents.

A method of linking nucleosides with a siloxane bridge comprising reacting a 3'-silylated-5'-protected nucleoside with an unprotected nucleoside is disclosed. The silylated and unprotected nucleosides may be either monomeric nucleosides or the terminal nucleosides of an oligonucleotide or oligonucleotide analog. A method of synthesizing an oligonucleotide analog having siloxane internucleoside linkages is also disclosed. The method of synthesis comprises silylating a 5'-protected nucleoside with a bifunctional silylating reagent to form a 3'-silylated nucleoside, reacting the silylated nucleoside with an unprotected nucleoside in the presence of a base catalyst and repeating these steps to form an oligonucleotide analog. A modified solid phase synthesis method for preparing an oligonucleotide analog having siloxane internucleoside linkages is also disclosed.

Process of linking nucleosides with a siloxane bridge

Growing community of inventors

Harleysville, PA, United States of America

Ashis Kumar Saha