Nektar Therapeutics

Franco J Duarte

Neel Kumar Anand

Wen Zhang

Jennifer A Riggs-Sauthier

Pankaj Sharma

Devendrapratap Singh

Zhongxu Ren

Aaron S Hammons

Lin Cheng

Tacey Viegas

Xuyuan Gu

Jennifer Riggs-Sauthier

Tacey X Viegas

Compounds and pharmaceutically acceptable salts and solvates thereof are described. The compounds relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology and organic chemistry.

N-methyl-N-(1-phenyl-2-(1-pyrrolidinyl)ethyl)-2-aminophenylacetamide derivatives agonists for the &#x3ba; opioid receptor

Provided are compounds of Formula I; and pharmaceutically acceptable salts and solvates thereof:  The compounds of Formula I described herein relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology, organic chemistry and polymer chemistry.

Kappa opioid agonists and uses thereof

The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits a different biological membrane crossing rate as compared to the biological membrane crossing rate of the small molecule drug not attached to the water-soluble oligomer.

Oligomer-beta blocker conjugates

Provided are compounds, including those of Formula I; and pharmaceutically acceptable salts and solvates thereof. The compounds described herein relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology, organic chemistry and polymer chemistry.

Opioid agonists and uses thereof

Provided are compounds of Formula I: and pharmaceutically acceptable salts and solvates thereof, wherein R, R, R, R, R, and Rare as described herein. The compounds of Formula I are agonists of the kappa opioid receptor and relate to and/or have application(s) in (among others) the fields of drug discovery, pharmacotherapy, physiology, organic chemistry and polymer chemistry.

N-methyl-N-(1-phenyl-2-(1-pyrrolidinyl)ethyl)-2-aminophenylacetamide derivatives agonists for the kappa opioid receptor

Provided are compounds of Formula I; and pharmaceutically acceptable salts and solvates thereof.  The present disclosure relates to novel compounds and to their use as agonists of the kappa opioid receptor. The disclosure also relates to methods for preparation of the compounds and to pharmaceutical compositions containing such compounds. Kappa opioid agonists that exhibit full agonist properties at the kappa opioid receptor have been widely shown to be efficacious in preclinical models of pain, particularly visceral pain.

The invention provides water-soluble oligomer-beta blocker drug conjugates. A drug conjugate of the invention can be administered by any of a number of administration routes and exhibits properties that are different from the corresponding beta blocker not attached to the water-soluble oligomer.

The invention relates to (among other things) oligomer-aryloxy-substituted propanamine conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over un-conjugated aryloxy-substituted propanamine compounds.

Oligomer-aryloxy-substituted propanamine conjugates

The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the small molecule drug not attached to the water-soluble oligomer.

Oligomer-protease inhibitor conjugates

Oligomeric reagents are provided comprising a moiety of atoms arranged in a specific order, wherein the moiety is positioned between a water-soluble, non-peptidic oligomer and a pharmaceutically active agent. The oligomeric reagents are useful for, among other things, forming oligomer active agent conjugates. Related methods, compositions, preparations, and so forth are also provided.

Reagents

The invention provides protease inhibitors that are chemically modified by covalent attachment of a water-soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the protease inhibitors not attached to the water-soluble oligomer.

Growing community of inventors

Walnut Creek, CA, United States of America

Franco J Duarte