公开(公告)号：US10010587B2

公开(公告)日：2018-07-03

申请号：US15120214

申请日：2015-02-20

Applicant: Nektar Therapeutics ,  NEKTAR THERAPEUTICS (INDIA) PVT. LTD.

Inventor： Murali Krishna Addepalli ,  Deborah H. Charych ,  Seema Kantak ,  Steven Robert Lee

IPC: A61K38/20 ,  A61K39/395 ,  A61K47/48 ,  C07K16/28 ,  C07K16/30

CPC classification number: A61K38/2013 ,  A61K39/39541 ,  A61K39/39558 ,  A61K45/06 ,  A61K47/60 ,  A61K2039/505 ,  A61K2300/00 ,  C07K16/2815 ,  C07K16/2818 ,  C07K16/3015 ,  C07K16/3046 ,  C07K16/3084 ,  C07K2317/76

Abstract: The invention relates to (among other things) method of administering to a patient suffering from a cancer, the method comprising the steps of: (a) an IL-2Rβ-activating amount of a long acting, IL-2Rβ-selective agonist; and (b) a CTLA-4 pathway-inhibiting amount of an anti-CTLA-4 antibody or a PD-1 pathway-inhibiting amount of an anti-PD-1 antibody.

公开(公告)号：US09688638B2

公开(公告)日：2017-06-27

申请号：US15039686

申请日：2014-11-27

Applicant: NEKTAR THERAPEUTICS (INDIA) PVT.LTD. ,  NEKTAR THERAPEUTICS (Incorporated under the Laws of Delaware and domiclled in the State of California)

Inventor： Franco J. Duarte ,  Neel K. Anand ,  Pankaj Sharma ,  Devendrapratap Singh

IPC: C07D221/22 ,  C07D221/26 ,  C07D513/08 ,  C07D401/12

CPC classification number: C07D221/26 ,  C07D401/12 ,  C07D513/08

Abstract: 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.

公开(公告)号：US20170128539A1

公开(公告)日：2017-05-11

申请号：US15120214

申请日：2015-02-20

Applicant: NEKTAR THERAPEUTICS (INDIA) PVT. LTD. ,  Nektar Therapeutics

Inventor： Murali Krishna Addepalli ,  Deborah H. Charych ,  Seema Kantak ,  Steven Robert Lee

IPC: A61K38/20 ,  C07K16/28 ,  C07K16/30 ,  A61K39/395

CPC classification number: A61K38/2013 ,  A61K39/39558 ,  A61K45/06 ,  A61K47/60 ,  A61K2039/505 ,  A61K2300/00 ,  C07K16/2815 ,  C07K16/2818 ,  C07K16/3015 ,  C07K16/3046 ,  C07K16/3084 ,  C07K2317/76 ,  A61K39/39541

Abstract: The invention relates to (among other things) method of administering to a patient suffering from a cancer, the method comprising the steps of: (a) an IL-2Rβ-activating amount of a long acting, IL-2Rβ-selective agonist; and (b) a CTLA-4 pathway-inhibiting amount of an anti-CTLA-4 antibody or a PD-1 pathway-inhibiting amount of an anti-PD-1 antibody.

公开(公告)号：US20170022167A1

公开(公告)日：2017-01-26

申请号：US15039686

申请日：2014-11-27

Applicant: NEKTAR THERAPEUTICS (INDIA) PVT.LTD. ,  NEKTAR THERAPEUTICS (Incorporated Under the laws of Delaware and domiclled in the State of Ca.)

Inventor： Franco J. Duarte ,  Neel K. Anand ,  Pankaj Sharma ,  Devendrapratap Singh

IPC: C07D221/26 ,  C07D401/12 ,  C07D513/08

CPC classification number: C07D221/26 ,  C07D401/12 ,  C07D513/08

Abstract: 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.

Abstract translation: 提供的化合物包括式I化合物; 及其药学上可接受的盐和溶剂化物。 本文所述的化合物涉及（和其中）药物发现，药物治疗，生理学，有机化学和聚合物化学领域中和/或具有应用。

公开(公告)号：US12247059B2

公开(公告)日：2025-03-11

申请号：US17373665

申请日：2021-07-12

Applicant: Nektar Therapeutics

Inventor： Mary J. Bossard ,  Cherie F. Ali ,  Xiaofeng Liu ,  Deborah H. Charych ,  Yujun Wang

IPC: C07K14/55 ,  A61K38/20 ,  A61K47/60

Abstract: Conjugates of an interleukin-2 (“IL-2”) moiety and one or more nonpeptidic, water-soluble polymers are provided. Typically, the non-peptidic, water-soluble polymer is poly(ethylene glycol) or a derivative thereof. Also provided, among other things, are compositions comprising conjugates, methods of making conjugates, methods of administering compositions to an individual, nucleic acid sequences, expression systems, host cells, and methods for preparing IL-moieties.

公开(公告)号：US12214045B2

公开(公告)日：2025-02-04

申请号：US18221300

申请日：2023-07-12

Applicant: Nektar Therapeutics

Inventor： Zhongxu Ren ,  Neel K. Anand ,  Haiying Cai ,  Bo-Liang Deng ,  Bhalchandra V. Joshi ,  Jonathan Zalevsky ,  Takahiro Miyazaki ,  Saul Kivimae

IPC: A61K47/60 ,  A61K9/00 ,  A61K47/54 ,  A61K47/64 ,  A61P35/00

Abstract: 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 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-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.

公开(公告)号：US11813241B2

公开(公告)日：2023-11-14

申请号：US16125341

申请日：2018-09-07

Applicant: Nektar Therapeutics

Inventor： Antoni Kozlowski ,  Timothy A. Riley ,  Samuel P. McManus

IPC: A61K31/337 ,  A61K47/60 ,  C08G65/329 ,  C08G65/333 ,  C07D305/14

CPC classification number: A61K31/337 ,  A61K47/60 ,  C07D305/14 ,  C08G65/329 ,  C08G65/33337 ,  C08L2203/02

Abstract: Among other aspects, provided herein are multi-arm polymeric prodrug conjugates of taxane-based compounds and/or fluorinated forms thereof. Methods of preparing such conjugates as well as methods of administering the conjugates are also provided. Upon administration to a patient, release of the taxane-based compound is achieved.

公开(公告)号：US11672776B2

公开(公告)日：2023-06-13

申请号：US16026979

申请日：2018-07-03

Applicant: Nektar Therapeutics

Inventor： Antoni Kozlowski ,  Samuel P. McManus ,  Jennifer Riggs-Sauthier ,  Xiaoming Shen ,  Wen Zhang

IPC: A61K31/337 ,  A61K38/00 ,  A61K31/785 ,  C08G79/08 ,  A61K47/60 ,  A61K31/4745 ,  C08G65/332 ,  C08G65/333

CPC classification number: A61K31/337 ,  A61K31/4745 ,  A61K31/785 ,  A61K38/00 ,  A61K47/60 ,  C08G65/3328 ,  C08G65/33344 ,  C08G79/08

Abstract: Among other aspects, provided herein are multi-armed polymer conjugates comprising an alkanoate-linker, compositions comprising such conjugates, and related methods of making and administering the same. Methods of treatment employing such conjugates and related uses are also provided. The conjugates are prepared with high drug loading efficiencies.

公开(公告)号：US11406618B2

公开(公告)日：2022-08-09

申请号：US16243914

申请日：2019-01-09

Applicant: Nektar Therapeutics

Inventor： Antoni Kozlowski ,  Sean M. Culbertson ,  Xiaoming Shen ,  Samuel P. McManus ,  Mark A. Wilson

IPC: A61K31/404 ,  A61K47/60 ,  A61P35/00

Abstract: The invention relates to (among other things) polymer-des-ethyl sunitinib conjugates and related compounds. A compound of the invention, when administered by any of a number of administration routes, exhibits advantages over des-ethyl sunitinib in unconjugated form.

公开(公告)号：US20220079936A1

公开(公告)日：2022-03-17

申请号：US17535385

申请日：2021-11-24

Applicant: Nektar Therapeutics

Inventor： Xuan Zhao ,  Michael D. Bentley ,  Zhongxu Ren ,  Tacey X. Viegas

IPC: A61K31/4745 ,  C08G65/331 ,  C08G65/332 ,  C08G65/333 ,  C08G65/334 ,  A61K47/59 ,  A61K47/61 ,  A61K47/64 ,  A61K31/4709 ,  A61K47/60

Abstract: 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.