Kosan Biosciences Incorporated

Prolynx LLC

Northwestern University

Other

Leland Stanford Junior University

Ortho-mcneil Pharmaceutical Corp.

Gary W Ashley

Daniel V Santi

Robert C MacDonald

Miho Shida

Brian Walter Metcalf

Robert G McDaniel

Li Tang

Mark A Burlingame

Eric L Schneider

Jeffrey C Henise

Chaitan Khosla

Camilla M Kao

Rainer Ziermann

Mary C Betlach

Daniel T Chu

Philip J Barr

Brian R Hearn

John R Carney

Melanie C Betlach

Christopher Carreras

Daniel T W Chu

Simon James Shaw

Qun Xue

Isaac C Chan-Kai

Claes Gustafsson

Guanglin Luo

Yandong Li

Leonard Katz

David C Myles

Dennis J Hlasta

Janice Lau Wee

Hong Fu

Bryan Julien

Rembert Pieper

David E Cane

Todd C Henninger

Eugene B Grant

Robert L Arslanian

Shaun Fontaine

Chaitin Khosla

Hugo Menzella

Provided are β-eliminative linkers suitable for the conjugation of small molecule, peptide, and protein and compounds comprising the linkers.

Conjugation linkers

Hydrogels that degrade under appropriate conditions of pH and temperature by virtue of crosslinking compounds that cleave through an elimination reaction are described. The hydrogels may be used for delivery of various agents, such as pharmaceuticals.

Hydrogels with biodegradable crosslinking

Conjugates of carriers and hydrogels for controlling the biological half-life of somatostatin and its analogs are disclosed.

Conjugates of somatostatin analogues

Conjugates of SN-38 that provide optimal drug release rates and minimize the formation of the corresponding glucuronate are described. The conjugates release SN-38 from a polyethylene glycol through a &#x3b2;-elimination mechanism.

Slow-release conjugates of SN-38

Hydrogels that degrade under appropriate conditions of pH and temperature by virtue of crosslinking compounds that cleave through an elimination reaction are described. The hydrogels may be used for delivery of various agents, such as pharmaceuticals. This invention provides hydrogels that degrade to smaller, soluble components in a non-enzymatic process upon exposure to physiological conditions and to methods to prepare them. The hydrogels are prepared from crosslinking agents that undergo elimination reactions under physiological conditions, thus cleaving the crosslinking agent from the backbone of the hydrogel. The invention also relates to the crosslinking agents themselves and intermediates in forming the hydro gels of the invention. The biodegradable hydro gels prepared according to the methods of the invention may be of use in diverse fields, including biomedical engineering, absorbent materials, and as carriers for drug delivery.

The present invention provides methods and compositions that permit controlled and prolonged drug release in vivo. The compounds are either prodrugs with tunable rates of release, or conjugates of the drug with macromolecules which exhibit tunable controlled rates of release.

Prodrugs and drug-macromolecule conjugates having controlled drug release rates

The invention relates to solid supports useful in medical applications that provide controlled release of drugs, such as peptides, nucleic acids and small molecules. The drugs are covalently coupled to the solid support through a linkage that releases the drug or a prodrug through controlled beta elimination.

Controlled release from solid supports

The invention relates to conjugates of macromolecular carriers and drugs comprising linkers that release the drug or a prodrug through rate-controlled beta-elimination, and methods of making and using the conjugates.

Controlled release from macromolecular conjugates

The invention relates to compositions that comprise dendrimers useful in medical and veterinary applications that provide controlled release of drugs, such as peptides, nucleic acids and small molecules. The drugs are covalently coupled to the dendrimer through a linkage that releases the drug or a prodrug through controlled beta elimination.

Controlled drug release from dendrimers

Growing community of inventors

Alameda, CA, United States of America

Gary W Ashley