Nektar Therapeutics

Other

Nektar Therapeutics Al, Corporation

Zhongxu Ren

Xuan Zhao

Jennifer A Riggs-Sauthier

Michael David Bentley

Neel Kumar Anand

Bo-Liang Deng

Tacey Viegas

Haiying Cai

Timothy A Riley

Wen Zhang

Bhalchandra V Joshi

Saul Kivimae

Franco J Duarte

Natalia Aurrecoechea

Donogh John Roger O'Mahony

Kazunori Emoto

Antoni Kozlowski

YongQi Mu

Xiaoming Shen

Pankaj Sharma

Xuyuan Gu

Aaron S Hammons

Micah Brandon Harvey

Laurie A VanderVeen

Yuan Song

Xuejun Yuan

Aleksandrs Odinecs

Vijay Kumar Khatri

Takahiro Miyazaki

Michael Lixin Shen

Jonathan Zalevsky

Lin Cheng

Mary Tagliaferri

Anthony James Brockway

Marlene Hennessy

Rhoneil L Pena

Werner Rubas

Xuan S Zhao

The instant disclosure provides novel adenosine receptor antagonist compounds, compositions, methods of making and methods of using. In a further aspect, a method of treating a subject in need thereof, comprising administering a therapeutically effective amount of any one or more of the compounds described herein. In some embodiments, the subject has cancer and the method is a method of treating cancer.

Adenosine 2 receptor antagonists

Provided are multi-arm polymer conjugates of Toll-Like Receptor (“TLR”) agonists such as TLR 7/8 agonists, as well as related compositions, and methods of making and using such conjugates. Exemplary conjugates are encompassed by Formula I: or a pharmaceutically acceptable salt form thereof, where R, taken together with each Q, is a residue of a polyol, polythiol, or polyamine bearing from 3 to about 50 hydroxyl, thiol, or amino groups; each Q is a linker selected from oxygen, sulfur and —NH; each POLY is independently a water-soluble, non-peptidic polymer; each Xis independently a linkage-containing spacer moiety; q is a positive integer from 3 to about 50; and each TLR 7/8 AG is a Toll-like receptor 7/8 agonist. Also provided is a method of administering to a patient having cancer (a) an IL-2Rβ-activating amount of a long-acting, IL-2Rβ-selective agonist; and (b) a Toll-like receptor agonist such as a conjugate as described above, as well as related compositions, kits and methods.

Multi-arm polymer conjugates of TLR agonist compounds and related immunotherapeutic treatment methods

Provided is a method of administering to a patient having cancer: (a) a 4-1BB agonist; (b) an IL-2Rβ-activating amount of a long-acting, IL-2Rβ-selective agonist; and/or (c) a toll-like receptor agonist, as well as related compositions, kits and compositions.

Immunotherapeutic tumor treatment method

Disclosed herein are methods in the field of cancer immunotherapy that involve the treatment of a subject having cancer by administering to the subject a toll-like receptor 7/8 (TLR7/8) agonist in combination with a long-acting IL-2Rβ-biased agonist and a programmed cell death protein 1 (PD-1)/programmed cell death protein ligand 1 (PD-L1) axis inhibitor, and related compositions, dosage forms, and kits.

Provided are multi-arm polymer conjugates of Toll-Like Receptor ('TLR') agonists such as TLR 7/8 agonists, as well as related compositions, and methods of making and using such conjugates. Exemplary conjugates are encompassed by Formula I: (I) or a pharmaceutically acceptable salt form thereof, where R, taken together with each Q, is a residue of a polyol, polythiol, or polyamine bearing from 3 to about 50 hydroxyl, thiol, or amino groups; each Q is a linker selected from oxygen, sulfur and &#x2014;NH; each POLY is independently a water-soluble, non-peptidic polymer; each Xr is independently a linkage-containing spacer moiety; q is a positive integer from 3 to about 50; and each TLR 7/8 AG is a Toll-like receptor 7/8 agonist. Also provided is a method of administering to a patient having cancer (a) an IL-2R&#x3b2;-activating amount of a long-acting, IL-2R&#x3b2;-selective agonist; and (b) a Toll-like receptor agonist such as a conjugate as described above, as well as related compositions, kits and methods.RQ-POLY-Xr-TLR7/8 AG)&#x2003;&#x2003;(I)

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 instant disclosure relates to (among other things) compounds that are derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5-amine. The compounds provided possess unique effects and differences over other phenyltriazines known in the art.

Derivatives of 6-(2,3-dichlorophenyl)-1,2,4-triazin-5-amine

Provided herein are water-soluble prodrugs, compositions comprising such prodrugs, and related methods of making and administering the same. The prodrugs of the invention comprise a water-soluble polymer having three or more arms, at least three of which are typically covalently attached to an active agent, e.g., a small molecule. The conjugates of the invention provide an optimal balance of polymer size and structure for achieving improved drug loading, since the conjugates of the invention possess three or more active agents releasably attached to a multi-armed water-soluble polymer. The prodrugs of the invention are therapeutically effective, and exhibit improved properties in-vivo when compared to unmodified parent drug.

Multi-arm polymer prodrugs

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.

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 small molecule drugs that are chemically modified by covalent attachment of a water soluble, non-peptidic oligomer. The conjugates of the invention, when administered by any of a number administration routes, exhibits advantages over previously administered compounds.

Oligomer-nucleoside phosphate conjugates

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

Oligomer-diarylpiperazine conjugates

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Foster City, CA, United States of America

Zhongxu Ren