公开(公告)号：US11485710B2

公开(公告)日：2022-11-01

申请号：US17156478

申请日：2021-01-22

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

Inventor： Niall Andrew Anderson ,  Deepak Bandyopadhyay ,  Alain Claude-Marie Daugan ,  Frederic G. Donche ,  Patrick M. Eidam ,  Nicolas Eric Faucher ,  Nicolas S. George ,  Philip Anthony Harris ,  Jae U. Jeong ,  Bryan W. King ,  Clark A. Sehon ,  Gemma Victoria White ,  David Duff Wisnoski

IPC: A61K31/415 ,  C07D231/06 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/04 ,  C07D401/06 ,  C07D405/04 ,  C07D405/06 ,  C07D409/14 ,  C07D417/14 ,  C07D403/04 ,  C07D487/04 ,  A61P21/00 ,  A61K31/422 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/506 ,  A61K31/5377 ,  C07D403/06 ,  C07D409/06 ,  C07D413/04

Abstract: Disclosed are compounds having the formula: wherein R1, R2, and R3 are as defined herein, and methods of making and using the same.

公开(公告)号：US20220315556A1

公开(公告)日：2022-10-06

申请号：US17054491

申请日：2019-05-10

Applicant: Glaxosmithkline Intellectual Property Development Limited

Inventor： Jeffrey Michael Axten ,  Mui Cheung ,  Michael P. Demartino ,  Huiping Amy Guan ,  Yan Hu ,  Aaron Bayne Miller ,  Donghui Qin ,  Chengde Wu ,  Zhiliu Zhang ,  Xiaojuan Lin

IPC: C07D401/14 ,  A61P11/00 ,  C07D401/12 ,  C07D211/26 ,  C07D487/08

Abstract: This invention relates to novel compounds according to Formula (I) which are inhibitors of furin, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of fibrotic diseases, including pulmonary fibrosis, renal fibrosis, liver fibrosis, skin fibrosis, ocular fibrosis, cardiac fibrosis, and other miscellaneous fibrotic conditions. The disclosed compounds may also be useful for treating other furin-mediated conditions, including but not limited to, hypertension, cancer, infectious diseases, and genetic disorders (e.g., cystic fibrosis (CF)), and neurodegenerative disorders.

公开(公告)号：US20220306623A1

公开(公告)日：2022-09-29

申请号：US17617898

申请日：2020-06-11

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

Inventor： Sophie Marie BERTRAND ,  Heather HOBBS ,  Simon Marc NICOLLE ,  Sandeep PAL ,  Simon PEACE ,  Margarita PUENTE-FELIPE

IPC: C07D471/04

Abstract: The invention relates to compounds or pharmaceutically acceptable salts thereof of formula (I): wherein R1, R2, R3, R4, R4′ and R5 are as defined in the description and claims; and compounds or pharmaceutically acceptable salts thereof of formulas (II), (IIa), (IIb), (IIc), and (III) having mTOR kinase inhibitor activity. The invention also relates to pharmaceutical compositions which include a compound of formula (I), (II), (IIa), (IIb), (IIc), or (III) or a pharmaceutically acceptable salt thereof, and to the use of a compound of formula (I), (II), (IIa), (IIb), (IIc), or (III), or a pharmaceutically acceptable salt thereof in therapy, including in the treatment of a disease or condition for which an mTOR kinase inhibitor activity is indicated, and in particular the treatment of idiopathic pulmonary fibrosis.

公开(公告)号：US20220204526A1

公开(公告)日：2022-06-30

申请号：US17429088

申请日：2020-02-11

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

Inventor： Mark ELBAN ,  Michal Pawel GLOGOWSKI ,  Michael Clinton KOETTING ,  Brian Griffin LAWHORN ,  Jay M. MATTHEWS ,  Jaclyn Renee PATTERSON

IPC: C07D498/04 ,  C07D498/10

Abstract: The present invention relates hydroxypyridoxazepine compounds, methods of making them, pharmaceutical compositions containing them and their use as Nrf2 activators. In particular, the invention relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof, or a tautomer thereof, or a hydrate thereof.

公开(公告)号：US20220177517A1

公开(公告)日：2022-06-09

申请号：US17600276

申请日：2020-04-03

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： Daniel GIBSON ,  Richard KUCIA-TRAN ,  Nehal PATEL ,  Trevor WILEY

IPC: C07K1/22 ,  C07K16/06 ,  C07K1/16 ,  C07K1/18 ,  C07K1/20

Abstract: The present invention is directed to a novel process for purifying a recombinant polypeptide from a solution comprising one or more impurities, wherein the process is a chromatography process which uses saccharin. The present invention also provides the use of saccharin in a process for purifying a recombinant polypeptide from a solution comprising one or more impurities, wherein the process is a chromatography process. The invention further provides a wash buffer for purifying using chromatography a recombinant polypeptide from a solution comprising one or more impurities, wherein the wash buffer comprises saccharin.

公开(公告)号：US20220144834A1

公开(公告)日：2022-05-12

申请号：US17509769

申请日：2021-10-25

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED

Inventor： John G. CATALANO ,  Pek Yoke CHONG ,  Hamilton D. DICKSON ,  Martin R. LEIVERS ,  Jason Gordon WEATHERHEAD

IPC: C07D471/14 ,  A61P31/20 ,  C07D471/20

Abstract: Compounds, specifically hepatitis B virus and/or hepatitis D virus inhibitors, more specifically compounds that inhibit HBe antigen and HBs antigen in a subject, for the treatment of viral infections, and methods of preparing and using such compounds.

公开(公告)号：US20220098303A1

公开(公告)日：2022-03-31

申请号：US17426695

申请日：2020-01-31

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： Swethajit Biswas ,  Nicola A. JACKSON ,  Elaine Marie PAUL ,  Herbert STRUEMPER ,  Joanna OPALINSKA

IPC: C07K16/28 ,  A61K47/68 ,  A61P35/00

Abstract: Disclosed herein are combinations of an antigen binding protein that binds BCMA with an antigen binding protein that bind to an immunomodulatory agent, such as PD-1 or OX40, pharmaceutical compositions thereof, uses thereof, and methods of treatment comprising administering said combinations, including uses in cancer.

公开(公告)号：US11254753B2

公开(公告)日：2022-02-22

申请号：US16339027

申请日：2017-10-03

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： Hella Bosteels ,  Shugui Chen ,  Kayeleigh Farrow ,  Richard Kucia-Tran ,  William John Kenneth Lewis ,  Andrew S. Thomson ,  Mark Uden

IPC: C07K16/40 ,  C07K16/00

Abstract: The present invention relates to variant antibodies and methods of generating said antibodies with a reduced level of binding to process impurities. In particular, the invention describes variant IgG4 antibodies which have been modified in the heavy chain constant region at any one or a combination of amino acids in the region between Kabat residues 203 and 256, wherein the variant IgG4 antibody has a reduced level of binding to host cell protein (HCP), compared to an unmodified IgG4 antibody. The invention also relates to compositions comprising said variant IgG4 antibodies.

公开(公告)号：US11253499B2

公开(公告)日：2022-02-22

申请号：US16639292

申请日：2018-08-15

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED ,  BIOVERSYS AG

Inventor： Esther Porras De Francisco ,  Modesto Jesús Remuiñan-Blanco ,  Marilyne Bourotte ,  Benoit Deprez ,  Geoffroy Dequirez ,  Nicolas Willand

IPC: A61K31/397 ,  A61P31/06 ,  A61K31/4427 ,  A61K45/06 ,  C07D205/04 ,  C07D401/04 ,  C07D405/04

Abstract: The invention relates to compounds of Formula (I) and their use in therapy, for example in the treatment of mycobacterial infections or in the treatment of diseases caused by Mycobacterium, such as tuberculosis.

公开(公告)号：US11229646B2

公开(公告)日：2022-01-25

申请号：US16918084

申请日：2020-07-01

Applicant: GlaxoSmithKline Intellectual Property Development Limited

Inventor： Katherine Louisa Widdowson

IPC: C07D471/16 ,  C07D487/06 ,  A61K31/4985 ,  A61K31/538 ,  A61K31/5383 ,  A61K31/542 ,  A61K31/554 ,  A61K31/5415 ,  A61K31/4375 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/5377

Abstract: The present invention relates to methods for treating Neisseria gonorrhoeae infection which comprises administering to a subject in need thereof novel Tricyclic nitrogen containing compounds and corresponding pharmaceutical compositions as described herein.