Eli Lilly and Company

Vertex Pharmaceuticals, Inc.

Frantz Victor

Mark Joseph Tebbe

Deyi Zhang

Wayne A Spitzer

Yao-Chang Xu

Daniel Timothy Kohlman

Bai-Ping Ying

Shawn Christopher Miller

Michael Philip Cohen

Xicheng David Sun

Deqi Guo

Nancy June Snyder

Karin Briner

John Irvin Glass

Roger Ryan Rothhaar

Q May Wang

Jason Eric Lamar

Cristina Garcia-Paredes

Yvonne Yee Mai Yip

Robert Edward Babine

Ivan Collado

Ling Jin

DeAnna Piatt Zacherl

Raymond Samuel Parker, Iii

Luc J Farmer

Robert B Perni

Michael J Rodriguez

Louis Nickolaus Jungheim

John Gordon Allen

Andrew Caerwyn Williams

Sidney Xi Liang

Christopher Stanley Galka

Maria Angeles Martinez-Grau

Michael Wade Tidwell

Michael Philip Mazanetz

Matthew Robert Reinhard

Joseph Chiou-Chung Tang

Joseph Matthew Colacino

Shu Hui Chen

Beverly Ann Heinz

Thomas R Sattelberg, Sr

Steven Armen Boyd

Sandra Ann Filla

Brian Michael Mathes

Ajay Singh

Vincent Mancuso

Maria-Jesus Blanco-Pillado

Kevin John Hudziak

Dana Rae Benesh

Anne Marie Camp

Sarah Lynne Hellman

Marie T Reamer

Shu-Hui Chen

Arundhati S Deo

Christopher Stephen Siedem

Alan Cornell

Wai-Man Lee

Deqi Duo

Samuel Raymond Iii Parker

Raymond Samuel Iii Parker

Michael Philip Eli Lilly And Company Limited Mazanetz

Richard Gerard Conway

Samuel Raymond Parker Iii

Mai Yee Yvonne Yip

Michael John Rodriguez

Deanna Piatt Zacherl

May Q Wang

The present invention relates to compounds of formula I: or pharmaceutically acceptable acid addition salts thereof, where;  The compounds of the present invention are useful for activating 5-HTreceptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. The present invention also relates to a process for the synthesis of intermediates in the synthesis of compounds of Formula I.

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The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HTreceptor agonists for the treatment of 5-HTassociated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: where:

The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel stereoselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.

Peptidomimetic protease inhibitors

The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel steroselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.

The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HTreceptor agonists for the treatment of 5-HTassociated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: 

The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula I as selective 5-HTreceptor agonists for the treatment of 5-HTassociated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: Formula (I) where: Ris selected from the group consisting of (a, b, c, d, e) and other substituents are as defined in the specification. 

The present invention relates to compounds of formula I: or pharmaceutically acceptable acid addition salts thereof, where; Ris C-Calkyl, substituted C-Calkyl, C-Ccycloalkyl, substituted C-Ccycloalkyl, C-Ccycloalkyl-C-Calkyl, substituted C-Ccycloalkyl-C-Calkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; Ris hydrogen, C-Calkyl, C-Ccycloalkyl-C-Calkyl, or a group of formula II  Ris hydrogen or C-Calkyl; Ris hydrogen, halo, or C-Calkyl; Ris hydrogen or C-Calkyl; Ris hydrogen or C-Calkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5-HTreceptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. The present invention also relates to a process for the synthesis of intermediates in the synthesis of compounds of Formula I.

The present invention relates to compounds of formula I: or a pharmaceutically acceptable acid addition salt thereof, where;

The present invention relates to compounds of formula I: (I) or a pharmaceutically acceptable acid addition salt thereof, where; X is C(R&#x2550; or N&#x2550;; Ris C&#x2013;Calkyl, substituted C&#x2013;Calkyl, C&#x2013;Ccycloalkyl, substituted C&#x2013;Ccycloalkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; Ris hydrogen, C&#x2013;Cn-alkyl, C&#x2013;Ccycloalkyl-C&#x2013;Calkyl, or a group of formula II (II) provided that when Ris C&#x2013;Calkyl or substituted C&#x2013;Calkyl, Ris hydrogen or methyl; R, R, and, when X is C(R)&#x2550;, R, are each independently hydrogen, fluoro, or methyl, provided that no more than one of R, R, and Rmay be other than hydrogen; Ris hydrogen or C&#x2013;Calkyl; Ris hydrogen, C&#x2013;Calkyl, or C&#x2013;Ccycloalkylcarbonyl, provided that when Ris other than hydrogen, Ris hydrogen; Ris hydrogen or C&#x2013;Calkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5-HTreceptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. 

A series of benzimidazole compounds having the following general structure are provided which inhibit the growth of picornaviruses (e.g., rhinoviruses, enteroviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus) and flaviviruses (e.g., hepatitis C and bovine diarrheal virus). ##STR1## A method for inhibiting picornaviruses and flaviviruses is also provided which includes administering to a host an effective amount of the inventive benzimidazole compounds.

Anti-viral compound

The present application provides a series of benzimidazole compounds which inhibit the growth of picornaviruses, such as rhinoviruses, enteroviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus and flaviviruses such as hepatitis C and bovine diarrheal virus.

Anti-viral compounds

Certain vinyl acetylene benzimidazole compounds which inhibit the growth of picornaviruses, such as rhinoviruses, enteroviruses, cardioviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus.

The present application provides a series of benzimidazole compounds which inhibit the growth of picornaviruses, such as rhinoviruses, enteroviruses, cardioviruses, polioviruses, coxsackieviruses of the A and B groups, echo virus and Mengo virus. Such compounds are also useful as intermediates for preparing additional benzimidazole antiviral compounds.

Ribosylated 2-amino-1,3,4-thiadiazoles having antiviral activity, methods of use and pharmaceutical formulations therefor.

Thiadiazole antiviral agents

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Indianapolis, IN, United States of America

Frantz Victor