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
Roland Dolle - King of Prussia PA, US Irennegbe Osifo - West Chester PA, US Stanley Schmidt - Chester Springs PA, US Denton Hoyer - Exton PA, US Tina Ross - Audubon PA, US Prasad Chaturvedula - Exton PA, US Catherine Prouty - Wayne PA, US Mohamed Awad - Frazer PA, US Joseph Salvino - Schwenksville PA, US James Rinker - Schwenksville PA, US Eric Lodge - Pottstown PA, US Jasbir Singh - Gilbertsville PA, US Mark Ator - Paoli PA, US
Mark Player - Phoenixville PA, US William Parsons - Belle Mead NJ, US Hui Huang - Monroe Twp. NJ, US Daniel Hutta - Belle Mead NJ, US Huaping Hu - Pennington NJ, US James Rinker - Reading PA, US
The invention addresses the current need for selective and potent protein tyrosine kinase inhibitors by providing potent inhibitors of c-fms kinase. The invention is directed to the novel compounds of Formula I: or a salt, stereoisomer, tautomer, crystalline, polymorph, amorphous, solvate, hydrate, ester, prodrug or metabolite form thereof, wherein A, Y, Z, Rand Rare described in the specification.
Halomethyl Amides As Il-1.Beta. Protease Inhibitors
Roland E. Dolle - King of Prussia PA James M. Rinker - Reading PA
Assignee:
Vertex Pharmaceuticals, Incorporated - Cambridge MA
International Classification:
A61K 3116
US Classification:
514629
Abstract:
Disclosed are compounds, compositions and methods for inhibiting interleukin-1. beta. protease activity, the compounds having the formula A described herein.