Roland E. Dolle - King of Prussia PA Irennegbe K. Osifo - W. Norriton PA Stanley J. Schmidt - Chester Springs PA Denton W. Hoyer - Exton PA Tina Morgan Ross - Audubon PA Prasad V. Chaturvedula - Cheshire CT Catherine P. Prouty - Doylestown PA Mohamed M. A. Awad - Westerly RI Joseph M. Salvino - Schwenksville PA James M. Rinker - Hamden CT Eric P. Lodge - Glendale AZ Jasbir Singh - Gilbertsville PA Mark A. Ator - Paoli PA
Assignee:
Vertex Pharmaceuticals Incorporated - Cambridge MA
International Classification:
C07K 506
US Classification:
514 19, 514 17, 514 18, 530330, 530331, 562571
Abstract:
Disclosed are compounds, compositions, and methods for inhibiting interleukin-1 protease activity, wherein the compounds are -substituted methyl ketones having formula (I) as set forth herein. These compounds are inhibitors of IL-1 converting enzyme and as such are useful as therapeutic agents for certain infectious diseases.
Pyridazines As Interleukin-1 Converting Enzyme Inhibitors
Roland E. Dolle - King of Prussia PA Denton W. Hoyer - Exton PA Tina Morgan Ross - Audubon PA James M. Rinker - Reading PA Stanley J. Schmidt - Chester Springs PA Mark A. Ator - Paoli PA
Assignee:
Vertex Pharmaceuticals Incorporated - Cambridge MA
Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof: wherein R is a halogen, or an oxygen linked leaving group including an aromatic ether, an alkyl sulfonate, an aryl sulfonate, an alkyl phosphonate, an aryl phosphonate, an alkyl phosphate or aryl phosphate; R is COOR , C( O)NH(CHR ) âCOOR , NH(CHR ) CON(R )R , C( O)N(R )R or NH(CHR ) OH; R is H or alkyl; R is H, sybstituted or unsubstituted aryl, heteroaryl or alkyl; R and R are independently H, lower alkyl, aryl, hydroxy alkyl, amino alkyl, heteroaryl, lower alkylene-aryl, lower alkylene-heteroaryl or lower cycloalkyl; and m=0-6; pharmaceutical compositions containing the compounds; and a method for inhibiting interleukin-1 protease activity in a mammal utilizing the compounds and compositions.
Substituted Diphenyloxazoles, The Synthesis Thereof, And The Use Thereof As Fluorescence Probes
The present invention is directed to a compound of Formula I: wherein A, R , and R are defined herein. The present invention is also directed to compositions comprising compounds of Formula I, methods of using compounds of Formula I, and methods of making compounds of Formula I.
4-Pyridazinecarboxamides And Esters As Interleukin-1Β Converting Enzyme Inhibitors
Roland E. Dolle - King of Prussia PA, US Denton W. Hoyer - Exton PA, US Tina Morgan Ross - Audubon PA, US James M. Rinker - Reading PA, US Stanley J. Schmidt - Chester Springs PA, US Mark A. Ator - Paoli PA, US
Assignee:
Vertex Pharmaceuticals Incorporated - Cambridge MA
Werner Mederski - Zwingenberg, DE Ralf Devant - Darmstadt, DE Gerhard Barnickel - Darmstadt, DE Sabine Bernotat-Danielowski - Bad Nauheim, DE Guido Melzer - Hofheim/Taunus, DE Bertram Cezanne - Mörfelden-Walldorf, DE Daljit Dhanoa - Del Mar CA, US James Rinker - Kenhorst PA, US Mark Player - Phoenixville PA, US Richard Soll - Lawrencehill NJ, US
Assignee:
3-Dimensional Pharmaceuticals, Inc. - Exton PA
International Classification:
C07D 239/91 A61K 31/517 A61P 9/10
US Classification:
51426631, 544287
Abstract:
Quinazolinones of formula (I) in which R, R, R, R, R, Y, n and m have the meaning indicated in Patent claim 1, and their salts or solvates as glycoprotein IbIX antagonists.
Substituted Diphenyloxazoles, The Synthesis Thereof, And The Use Thereof As Fluorescence Probes
Charles L. Cywin - Bethel CT, US Scott E. Jakes - Southbury CT, US Joachim Heider - Warthausen, DE Mark A. Bobko - Exton PA, US Renee L. Des Jarlais - St. Davids PA, US Mark Player - Phoenixville PA, US James Rinker - Reading PA, US Michael Winters - Lancaster PA, US
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc. - Ridgefield CT
International Classification:
C07D 471/02
US Classification:
546122
Abstract:
Disclosed are compounds of formula (I):.
1,6 Naphthyridines Useful As Inhibitors Of Syk Kinase
Charles L. Cywin - Bethel CT, US Scott E. Jakes - Southbury CT, US Joachim Heider - Warthausen, DE Mark A. Bobko - Exton PA, US Renee L. Des Jarlais - St. Davids PA, US Mark Player - Phoenixville PA, US James Rinker - Reading PA, US Michael Winters - Lancaster PA, US
Assignee:
Boehringer Ingelheim Pharmaceuticals, Inc. - Ridgefield CT