Wei Yuan Zhang - Collegeville PA Alan L. Maycock - Malvern PA Michael Anthony Marella - Exton PA Virendra Kumar - Paoli PA Forrest Gaul - Glen Moore PA An-Chih Chang - Rochester MN Deqi Guo - Phoenixville PA
Assignee:
Adolor Corporation - Exton PA
International Classification:
A61K 3140
US Classification:
514429, 514 91, 548413, 548578
Abstract:
Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compounds of formulae I, II, IIA, III, IIIA, IV and IVA have the structure: wherein R , R , R , R ; and X, X , X , X , X ; Y, Z and n are as described in the specification.
Kappa Agonist Compounds, Pharmaceutical Formulations And Method Of Prevention And Treatment Of Pruritus Therewith
Wei Yuan Zhang - Collegeville PA Alan L. Maycock - Malvern PA Anthony Michael Marella - Exton PA Virendra Kumar - Paoli PA Forrest Gaul - Glen Moore PA Deqi Guo - Phoenixville PA
Method for the prevention or treatment of pruritus with anti-pruritic compounds is provided. The compounds of formulae I, II, IIA, III, IIIA, IV and IVA have the structure: wherein R , R , R , R ; and X, X , X , X , X ; Y, Z and n are as described in the specification.
Kappa Agonist Compounds, Pharmaceutical Formulations And Method Of Prevention And Treatment Of Pruritus Therewith
Wei Yuan Zhang - Collegeville PA Alan L. Maycock - Malvern PA Michael Anthony Marella - Exton PA Virendra Kumar - Paoli PA Forrest Gaul - Glen Moore PA Deqi Guo - Phoenixville PA
Wei Yuan Zhang - Collegeville PA Alan L. Maycock - Malvern PA Michael Anthony Marella - Exton PA Virendra Kumar - Paoli PA Forrest Gaul - Glen Moore PA Deqi Guo - Phoenixville PA
Assignee:
Adolor Corporation - Exton PA
International Classification:
C07F 9547
US Classification:
514 91, 548413
Abstract:
The compounds of formulae IIA, the structure: wherein R , R , and X , X , n are as described in the specification.
Kappa Agonist Compounds And Pharmaceutical Formulations Thereof
Virendra Kumar - Berwyn PA Deqi Guo - Carmel IN Michael Anthony Marella - Exton PA Alan L. Maycock - Malvern PA
Assignee:
Adolor Corporation - Exton PA
International Classification:
A61K 3144
US Classification:
5142355, 51425402, 514428, 544111, 544372, 548579
Abstract:
Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics are provided. The compounds of formula IIIB have the structure: wherein R , R , R, Ar and n are as described in the specification.
Robert Edward Babine - Carlsbad CA, US Shu Hui Chen - Thousand Oaks CA, US Ivan Collado - Madrid, ES Cristina Garcia-Paredes - Madrid, ES John Irvin Glass - Germantown MD, US Deqi Guo - Carmel IN, US Ling Jin - Indianapolis IN, US Jason Eric Lamar - Indianapolis IN, US Nancy June Snyder - Lizton IN, US Xicheng David Sun - Broumfied CO, US Mark Joseph Tebbe - Zionsville IN, US Frantz Victor - Indianapolis IN, US Yvonne Yee Mai Yip - Indianapolis IN, US Robert B. Perni - Marlborough MA, US Luc Farmer - Foxborough MA, US
Assignee:
Vertex Pharmaceuticals Incorporated - Cambridge MA
International Classification:
A61K 31/497 C07D 241/02
US Classification:
5142521, 544406
Abstract:
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.
Robert Edward Babine - Franklin MA, US Shu-Hui Chen - Carmel IN, US Jason Eric Lamar - Indianapolis IN, US Nancy June Snyder - Lizton IN, US Xicheng Sun - Superior CO, US Mark Joseph Tebbe - Hamburg, DE Frantz Victor - Indianapolis IN, US Yvonne Yee Mai Yip - Indianapolis IN, US Ivan Collado - Madrid, ES Cristina Garcia-Paredes - Madrid, ES Ling Jin - Carmel IN, US Deqi Guo - Carmel IN, US John Irvin Glass - Indianapolis IN, US
Assignee:
Vertex Pharmaceuticals Incorporated - Cambridge MA
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.
Robert Edward Babine - Franklin MA, US Shu Hui Chen - Carmel IN, US Ivan Collado - Madrid, ES Cristina Garcia-Paredes - Madrid, ES John Irvin Glass - Indianapolis IN, US Ling Jin - Carmel IN, US Jason Eric Lamar - Indianapolis IN, US Nancy June Snyder - Lizton IN, US Xicheng David Sun - Superior CO, US Deqi Guo - Carmel IN, US Yvonne Yee Mai Yip - Indianapolis IN, US Frantz Victor - Indianapolis IN, US Mark Joseph Tebbe - Hamburg, DE Robert B. Perni - Marlborough MA, US Luc Farmer - Montreal, CA
Assignee:
Vertex Pharmaceuticals Incorporated - Cambridge MA
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.
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