Paul E Greenspan, 68Branford, CT

6812237, Nov 2, 2004

Nov 7, 2002

10/275583

Scott Douglas Cowen - Longport CO
Paul David Greenspan - New Providence NJ
Leslie Wighton McQuire - Warren NJ
Ruben Alberto Tommasi - Whitehouse Station NJ
John Henry Van Duzer - Georgetown MA

Novartis AG - Basel

A61K 31445

514320, 514343, 514381, 514391, 514466, 5483381, 548252, 548222, 548253, 548472, 548477, 546113, 546326, 549484, 549466, 549 72, 549304, 558392

Compounds of the formula (I), wherein R is aryl or biaryl; R is aryl-lower alkyl, biaryl-lower alkyl, benzo-fused cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, aryloxy-lower alkyl, or aryl-C -C -alkyl in which C -C -alkyl is interrupted by Y; Y is O, S, SO, SO , CO or NR ; R is hydrogen or lower alkyl; or R and R combined are C -C -alkylene or C -C -alkylene interrupted by Y; R is hydrogen or lower alkyl; R is hydrogen, optionally substituted lower alkyl, aryl-lower alkyl, biaryl-lower alkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, aryloxy-lower alkyl, or aryl-C -C -alkyl in which C -C -alkyl is interrupted by Y; R is hydrogen, lower alkyl or aryl-lower alkyl; and pharmaceutically acceptable salts thereof, which are useful as cysteine cathepsin inhibitors.

6291530, Sep 18, 2001

Mar 23, 1999

9/269251

Paul David Greenspan - New Providence NJ
Roger Aki Fujimoto - Morristown NJ

Novartis AG - Basel

A61K 31165
A61K 31445
A61K 3140
A61K 31535
A61K 3141

514617

##STR1## Disclosed are compounds of formula (I) wherein W is CH or N; R is (mono- or di cabocyclic or heterocyclic aryl)-lower alkyl; R. sup. 1 is hydrogen or lower alkyl; R. sup. 2 and R. sup. 3 are hydrogen, lower alkyl, lower alkoxy-lower alkyl or aryl-lower alkyl; or R. sup. 2 and R. sup. 3 joined together represent lower alkylene optionally interrupted by O, NH, N-lower alkyl or S so as to form a ring with the amide nitrogen; X is O, S, SO, S. sub. 2 or a direct bond; X. sup. 1 is O, S, SO, SO. sub. 2 or a direct bond; Y is a direct bond, lower alkylene or lower alkylidene; and Z is carboxyl, 5-tetrazolyl,, hydroxymethyl or carboxyl derivatized in the form of a pharmaceutically acceptable ester, and pharmaceutically acceptable salts thereof; which arm useful as LTB-4 antagonists.