Nektar Therapeutics

Inheris Pharmaceuticals, Inc.

Bo-Liang Deng

Jennifer A Riggs-Sauthier

Timothy A Riley

Zhongxu Ren

Neel Kumar Anand

Haiying Cai

Natalia Aurrecoechea

Donogh John Roger O'Mahony

Bhalchandra V Joshi

Saul Kivimae

YongQi Mu

Antoni Kozlowski

Xiaoming Shen

Lin Cheng

Pankaj Sharma

Xuyuan Gu

Micah Brandon Harvey

Yuan Song

Xuejun Yuan

Vijay Kumar Khatri

Michael Lixin Shen

Takahiro Miyazaki

Aleksandrs Odinecs

Jonathan Zalevsky

Wen Zhang

Hema Gursahani

Mary Tagliaferri

Werner Rubas

Erik Krogh-Jespersen

Anthony James Brockway

Marlene Hennessy

Rhoneil L Pena

Timothy Andrew Riley

Donogh O'MAHONY

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)

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

The present invention relates to compounds and their use as ligands for mu opioid receptors. Also included are methods for preparing the compounds and pharmaceutical compositions containing the compounds. In one or more embodiments of the invention, a compound according to Formula I is provided: and pharmaceutically acceptable salts thereof, wherein R-Rare as described herein. 

Morphinan derivatives for the treatment of neuropathic pain

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

Oligomer-opioid agonist conjugates

The invention provides compounds that are chemically modified by covalent attachment of a water&#x2014;soluble oligomer. A compound of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from those of the compound not attached to the water&#x2014;soluble oligomer.

The invention relates to (among other things) methods for treatment comprising administering oligomer-containing substituted aromatic triazine compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer.

Oligomer-containing substituted aromatic triazine compounds

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San Ramon, CA, United States of America

Bo-Liang Deng