Cetus Corporation

Glycomed, Inc.

Cetus Oncology Corporation

Margaret Moreland

Danute E Nitecki

Brian K Brandley

Michael Tiemeyer

Stuart J Swiedler

Hans Schweingruber

Lois Aldwin

David F Mark

Corey H Levenson

Irwin Braude

Henry Rapoport

Kirston E Koths

Nandini Katre

Paula J Shadle

Walter J Laird

Narasinga Rao

I Lawrence Greenfield

Henry Rapaport

John D Young

Ligands that bind to human selectin receptors are disclosed. The ligands are formulated with excipient carriers to form compositions which are administered to treated condition such as inflammation. The ligands have the structural formula III ##STR1## or molecules which have hydrogen bond donor groups equivalent to the circled groups with respect to their ability to form hydrogen bonds with a selectin under physiological conditions.

Methods of treating inflammation using selection binding compounds

Ligands in the form of N-acetyllactosamines which bind to endothelial leukocyte adhesion molecule-1 (ELAM-1) are disclosed. The ligand compounds can be formulated into pharmaceutical compositions and/or assay compositions used to alleviate inflammation and assay for the presence of (qualitative) and amount of (quantitative) ELAM-1 and thereby determine the presence, location and degree of inflammation.

Carbohydrate-based anti-inflammatory agents

Ligands in the form of N-acetyllactosamines which bind to endothelial leukocyte adhesion molecule-1 (ELAM-1) are disclosed. The ligand compounds can be formulated into pharmaceutical compositions and/or assay compositions used to alleviate inflammation and assay for the presence of (qualitative) and amount of (quantitative) ELAM-1 and thereby determine the presence, location and degree of inflammation. The ligands are encompassed by general structural formula I as follows: ##STR1## wherein one of F and G is hydrogen and one is an N-acetyl neuraminic acid residue on the terminal unit and are both hydrogen on any other unit; J is hydrogen, a lactosylceramide or a linking group and K is hydrogen or a fucose residue and n is an integer of from 1 to 10 (preferably 3 or 4) with the proviso that n and K are defined such that at least one K is a fucose residue.

Method of treating inflammation by blocking ELAM-1 receptor sites

Bifunctional chemicals useful for linking aldehyde containing moieties to moieties containing functionalities which are or can be reactive with sulfhydryl are claimed and have the formula:

Cross-linking agents

Succinylacetone derived or related medicaments and methods of synthesis of the same are shown wherein the medicaments consists of succinylacetonyl-proline-PEG, succinylacetonyl-NH-PEG, or compounds that have the formula: ##STR1## wherein n=1-6

Immunosuppressive analogues and derivatives of succinylacetone

This invention discloses heterobifunctional coupling agents for making a wide array of molecular conjugates. The agents contain a sterically hindered thiol, linked through a spacer arm to a second group reactive toward nucleophiles such as 1.degree. and 2.degree. amines or reactive thiols that are present on biological and organic materials. The coupling agents are useful for making conjugates containing a sterically hindered linkage.

Coupling agents and sterically hindered disulfide linked conjugates

Succinylacetone derived or related medicaments and methods of synthesis of the same are shown wherein the medicaments consists of succinylacetonyl-proline-PEG, succinylacetonyl-NH-PEG, or compounds that have the formula: ##STR1## and that have immunosuppressive activity both in vivo and in vitro based on their activities in cellular immunologic assays and adjuvant induced arthritis in rats, respectively.

Method of determining a cite of inflammation utilizing elam-1 ligands

Method of determining a site of inflammation utilizing ELAM-1 ligands

Conjugation of polymer to colony stimulating factor-1

Ligands in the form of N-acetyllactosamines which bind to endothelial leukocyte adhesion molecule-1 (ELAM-1) are disclosed. The ligand compounds can be formulated into pharmaceutical compositions and/or assay compositions used to alleviate inflammation and assay for the presence of (qualitative) and amount of (quantitative) ELAM-1 and thereby determine the presence, location and degree of inflammation. The ligands are encompassed by general structural formula I as follows: ##STR1## wherein one of A and B is hydrogen and one is an N-acetyl neuraminic acid residue; D and E are each independently hydrogen or a fucose residue; n is an integer of from 0 to 10 with the proviso that if n is 0, E is a fucose residue; F is hydrogen, a lactosylceramide residue or a linking group; and molecules equivalent to a compound of formula I regarding its ability to bind to an ELAM-1 receptor to the same degree as a compound of formula I.

Method of determining a site of inflammation utilizing elam-1 ligands

Novel cross-linking agents

Immunosupressive analogues and derivatives of succinylacetone

A biologically active CSF-1 protein is selectively conjugated via certain amino acid residues or carbohydrate moieties to a water-soluble polymer selected from polyethylene glycol or polypropylene glycol homopolymers, polyoxyethylated polyols, or polyvinyl alcohol. The resulting conjugated CSF-1 is biologically active and has increased circulating half-life in mammals, compared to that of the unconjugated protein. The conjugated CSF-1 may be used to stimulate the immune response or to provide more cells to be stimulated.

Growing community of inventors

Berkeley, CA, United States of America

Margaret Moreland