This invention describes an ICE inhibitor prodrug (I) having good bioavailability.

##STR00001##

Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.

This invention describes an ICE inhibitor prodrug (I) having good bioavailability.

##STR00001##

Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.

The present invention is aimed to provide an industrially advantageous method for producing a furan compound, in which a furan compound can be efficiently obtained in a high selectivity from a furfural compound. The present invention is concerned with a method for producing a furan compound including feeding, as a raw material, a furfural composition containing a furfural compound into a reactor and subjecting to a decarbonylation reaction in the presence of a catalyst to obtain a furan compound as a product, wherein a furfural dimer concentration in the furfural composition is 1,000 ppm by weight or less, and a peroxide value in the furfural composition is 0.01 mEq/kg or more and 1.0 mEq/kg or less.

Dialkyil esters of 2,5-furandicarboxylic acid are prepared in a process including: contacting an acid starting composition having 2,5-furandicarboxylic acid with an excess of alkanol to form an esterification product having the dialkyil ester of 2,5-furan dicarboxylic acid, water and unreacted alkanol; separating at least part of the unreacted alkanol and water from the esterification product to yield a solid crude product composition having the dialkyil ester of 2,5-furandicarboxylic acid; and subjecting at least part of the solid crude product composition to an evaporation step, where the dialkyil ester of 2,5-furandicarboxylic acid is evaporated and subsequently condensed to yield purified dialkyil ester of 2,5-furandicarboxylic acid.

A supported catalyst for aldehyde coupling reaction, comprising a carrier having supported thereon a catalyst comprising at least one azolium compound selected from the group consisting of a thiazolium salt, an imidazolium salt, a benzimidazolium salt and a triazolium salt, the azolium compound having, at a nitrogen atom thereof, a substituent selected from the group consisting of an aliphatic group having 6 or more carbon atoms and an aromatic group having 6 or more carbon atoms.

Dialkyl esters of 2,5-furandicarboxylic acid are prepared from a 2,5-furandicarboxylic acid-containing starting material in a process, which includes: contacting a vaporous stream of an alkanol countercurrently with the at least partially liquid starting material having the 2,5-furandicarboxylic acid, in a reaction zone to conduct an esterification reaction to yield the dialkyl ester of 2,5-furandicarboxylic acid and water; withdrawing a reaction vapor comprising the alkanol and water from the reaction zone; and discharging a liquid phase having at least the dialkyl ester of 2,5-furandicarboxylic acid, from the bottom part of the reaction zone, to obtain the dialkyl ester of 2,5-furandicarboxylic acid.

A hydrogenation catalyst, preferably palladium on a support, preferably alumina or activated charcoal support, is used in the presence of lithium salts, with salts such as the borates being preferred. This provides hydrogenation of precursors to give rise to a stereoselective, such as diastereoselective bias in the product of alkene hydrogenation using the catalyst.

This invention describes an ICE inhibitor prodrug (I) having good bioavailability. ##STR00001##
Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.

This invention describes an ICE inhibitor prodrug (I) having good bioavailability. ##STR00001##
Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.

The present invention relates to a process for preparing an ester having formula RCOOR (I), wherein R represents a group selected from: (i) a linear or branched alkyl, containing from 1 to 20 carbon atoms, (ii) an aryl containing from 6 to 12 carbon atoms, (iii) a heterocycle with 4 to 12 carbon atoms containing at least one heteroatom selected from O, N, P and S, R represents a linear or branched alkyl containing from 1 to 12 carbon atoms, said process comprising at least a phase of reacting a reaction mixture comprising at least one aldehyde having formula RCHO (II), wherein R has the meanings defined above, and at least one alcohol having general formula ROH (III), wherein R has the meanings defined above, in the presence of at least one solid basic catalyst, at a temperature within the range of 120 C.-300 C., obtaining said ester having formula (I).