Cephalon, Inc.

Vertex Pharmaceuticals, Inc.

Nycomed Imaging As

Sanofi

Amersham Health As

Sanofi Winthrop Inc.

Jasbir Singh

Rabindranath Tripathy

Roland Ellwood Dolle

Robert L Hudkins

Prasad V Chaturvedula

Tina Morgan Ross

Stanley J Schmidt

Denton W Hoyer

Dandu R Reddy

Mohamed M Awad

Ted Underiner

John P Mallamo

Joseph M Salvino

Catherine P Prouty

James M Rinker

Theodore L Underiner

Mark A Ator

Irennegbe K Osifo

Shi-Bao Yu

Catherine Prouty

David A Whipple

Eric P Lodge

Edward R Bacon

Robert A Snow

Gregory L McIntire

Torgrim Engell

David L Ladd

Anne Kjersti Fahlvik

Anne Naevestad

Christopher Black

Vinay Chandrakant Desai

Wolfgang H Gunther

Kenneth Edmund Kellar

Dennis Fujii

Michel Gacek

Mohamed M A Awad

Jennifer Wellons

Gary Speier

Marshall Beeber

Brian Weekley

George Na

Barbara Yuan

Jack Stevens

The present invention is directed to cyclic substituted fused pyrrolocarbazoles and isoindolones. The invention also is directed to methods for making and using the cyclic substituted fused pyrrolocarbazoles and isoindolones.

Cyclic substituted fused pyrrolocarbazoles and isoindolones

The present invention is directed to novel heterocyclic substituted pyrazolones, including pharmaceutical compositions, diagnostic kits, assay standards or reagents containing the same, and methods of using the same as therapeutics. The invention is also directed to intermediates and processes for making these novel compounds.

Heterocyclic substituted pyrazolones

Disclosed are compounds, compositions, and methods for inhibiting interleukin-1&bgr; protease activity, wherein the compounds are &agr;-substituted methyl ketones having formula (I) as set forth herein. These compounds are inhibitors of IL-1&bgr; converting enzyme and as such are useful as therapeutic agents for certain infectious diseases.

Peptide analogs as irreversible interleukin-1&bgr; protease inhibitors

The invention relates to MR contrast media containing composite nanoparticles, preferably comprising a superparamagnetic iron oxide core provided with a coating comprising an oxidatively cleaved starch coating optionally together with a functionalized polyalkyleneoxide which serves to prolong blood residence.

Constrast media

The present invention is directed to novel fused aryl and heteroaryl bridged indenopyrrolocarbazoles which are useful, inter alia, as therapeutic agents. The invention is also directed to methods for making and using the bridged indenopyrrolocarbazoles.

Bridged indenopyrrolocarbazoles

Chelating agents

The invention provides a complexant compound of formula I

Disclosed are compounds, compositions and methods for inhi.beta.iting interleukin-1.beta. protease activity, the compounds .alpha.-substituted methyl ketones having the formula (I) set forth herein. These compounds are inhibitors of IL-1.beta. converting enzyme and as such are useful as therapeutic agents for certain infectious diseases.

Peptide analogs as irreversible interleukin-1.beta. protease inhibitors

Disclosed are compounds, compositions and methods for inhibiting interleukin -1.beta. protease activity, the compounds having the structure of formula (1) as described in the specification.

Peptidic phosphinyloxymethyl ketones as interleukin-1.beta.-converting

Compounds which Inhibit interleukin-1.beta. protease activity, pharmaceutical compositions containing the compounds and methods using the compounds are provided. The compounds have the formula ##STR1## wherein n is 0-2; each AA is Independently L-valine or L-alanine; R.sub.1 is selected from the group consisting of N-�4(N,N-dimethylaminomethyl)!benzoyl, N-benzoyloxycarbonyl, N-methyl-N-�4-(pyridyl)methyl!, N-�4-(pyddyl)methyl!carbonyl, N-3-(piperidinopropionyl), N-�4-(morpholinoethoxy)benzoyl, N-2-(quinuclidinyl)carbonyl, N-(3-pyridyl)methoxy carbonyl, N-(2-pyddyl)methoxy carbonyl, N-methyl-N-benzyl carbonyl, N-methyl-N-�2-(4-pyridyl)ethyl!carbonyl, and N-(N-phenylpiperazino) carbonyl; and R.sub.8, R.sub.9 and R.sub.10 are as defined below.

.alpha.-heteroaryloxymethyl ketones as interleukin - 1 .beta. converting

Compounds which inhibit interleukin-1.beta. protease activity, pharmaceutical compositions containing the compounds and methods using the compounds are provided. The compounds have the formula ##STR1## wherein n is 0-2; each AA is independently L-valine or L-alanine; R.sub.1 is selected from the group consisting of N-[4-(N,N-dimethylaminomethyl)]benzoyl, N-benzyloxycarbonyl, N-methyl-N-[4-(pyridyl)methyl], N-[4-(pyridyl)methyl]carbonyl, N-3-(piperidinopropionyl), N-[4-(morpholinoethoxy)benzoyl, N-2-(quinuclidinyl)carbonyl, N-(3-pyridyl)methoxy carbonyl, N-(2-pyridyl)methoxy carbonyl, N-methyl-N-benzyl carbonyl, N-methyl-N-[2-(4-pyridyl)ethyl]carbonyl, and N-(N-phenylpiperazino)carbonyl; and R.sub.8, R.sub.9, R.sub.10 are each independently hydrogen, lower alkyl, halo substituted methyl, carbalkoxy, benzyl, phenyl, or phenyl mono or disubstituted with fluoro, nitro, methoxy, chloro, trifluoromethyl or methanesulfonyl.

Heteroaryloxymethyl ketones as interleukin-1.beta.converting enzyme

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Gilbertsville, PA, United States of America

Jasbir Singh