公开(公告)号：US11266746B2

公开(公告)日：2022-03-08

申请号：US16313454

申请日：2017-02-24

申请人： THE UNITED STATES OF AMERICA, as represented by the Secretary, Department of Health and Human Services

发明人： Joost J. Oppenheim ,  De Yang ,  Zhen Han ,  Joseph John Barchi, Jr. ,  Michael Bustin

IPC分类号： A61K47/69 ,  A61K9/51 ,  A61K39/395 ,  C07K16/28 ,  A61K31/664 ,  C07D215/00 ,  A61K45/06 ,  A61K38/17 ,  A61P35/00 ,  A61K9/00 ,  A61K31/4745 ,  A61K47/02 ,  B82Y5/00

摘要： Methods of treating cancer or reducing the incidence of relapse of a cancer in a subject comprising co-administration of Toll-like receptor (TLR) 4 ligand, such as an HMGN1 protein, and a TLR 7 or 8 ligand, and optionally an immune checkpoint inhibitor, to the subject in need of such therapy. The TLR4-mediated immune-stimulating effect is synergistically enhanced by ligands of TLR7 or 8, and the immune checkpoint inhibitor. Also described here is a nanoparticle delivery platform for the co-administration of the TLR 4 ligand and the TLR 7 or 8 ligand.

公开(公告)号：US20210308053A1

公开(公告)日：2021-10-07

申请号：US17204679

申请日：2021-03-17

申请人： Vertex Pharmaceuticals Incorporated

发明人： Brian Dean Phenix ,  Laurent Jean-Claude Bagnol ,  Geoffrey Glen Brodeur ,  Sachin Chandran ,  Eleni Dokou ,  Lori Ann Ferris ,  Dragutin Knezic ,  Katie Lynn McCarty ,  Ales Medek ,  Sara A. Waggener

IPC分类号： A61K9/14 ,  A61K9/16 ,  A61K45/06 ,  A61K9/20 ,  A61K31/404 ,  A61K31/47 ,  C07D215/00 ,  C07D209/04 ,  C07D215/56 ,  C07D405/12 ,  A61K31/443 ,  A61K31/4709 ,  A61K31/4725

摘要： The present invention features compositions comprising a plurality of therapeutic agents wherein the presence of one therapeutic agent enhances the properties of at least one other therapeutic agent. In one embodiment, the therapeutic agents are cystic fibrosis transmembrane conductance regulators (CFTR) such as a CFTR corrector or CFTR potentiator for the treatment of CFTR mediated diseases such as cystic fibrosis. Methods and kits thereof are also disclosed.

公开(公告)号：US10980746B2

公开(公告)日：2021-04-20

申请号：US16232540

申请日：2018-12-26

申请人： Vertex Pharmaceuticals Incorporated

发明人： Brian Dean Phenix ,  Laurent Jean-Claude Bagnol ,  Geoffrey Glen Brodeur ,  Sachin Chandran ,  Eleni Dokou ,  Lori Ann Ferris ,  Dragutin Knezic ,  Katie Lynn McCarty ,  Ales Medek ,  Sara A. Waggener

IPC分类号： A61K31/404 ,  A61K31/443 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61K9/14 ,  A61K9/16 ,  A61K45/06 ,  A61K9/20 ,  C07D215/00 ,  C07D209/04 ,  C07D215/56 ,  C07D405/12

摘要： The present invention features compositions comprising a plurality of therapeutic agents wherein the presence of one therapeutic agent enhances the properties of at least one other therapeutic agent. In one embodiment, the therapeutic agents are cystic fibrosis transmembrane conductance regulators (CFTR) such as a CFTR corrector or CFTR potentiator for the treatment of CFTR mediated diseases such as cystic fibrosis. Methods and kits thereof are also disclosed.

公开(公告)号：US10723728B2

公开(公告)日：2020-07-28

申请号：US16540802

申请日：2019-08-14

申请人： ALKERMES PHARMA IRELAND LIMITED

发明人： Laura Cook Blumberg ,  Julius F. Remenar ,  Orn Almarsson ,  Tarek A. Zeidan

IPC分类号： C07D417/12 ,  C07D215/22 ,  C07D263/58 ,  C07D401/12 ,  C07D471/14 ,  C07F9/6558 ,  A61K31/496 ,  A61K31/554 ,  C07D471/04 ,  C07D215/14 ,  C07D401/04 ,  C07D401/14 ,  C07D239/553 ,  C07D239/56 ,  C07H19/06 ,  C07D215/00

摘要： The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.

公开(公告)号：US10196394B2

公开(公告)日：2019-02-05

申请号：US14683871

申请日：2015-04-10

申请人： OPKO HEALTH, INC.

发明人： Mengwei Hu ,  Sunil Paliwal ,  Neng-Yang Shih ,  Frank Bruno Guenter ,  Ingrid Mergelsberg

IPC分类号： A01N43/42 ,  A61K31/44 ,  C07D215/00 ,  C07D217/00 ,  C07D219/00 ,  C07D221/00 ,  C07D471/10 ,  A61K31/435 ,  A61K31/495 ,  A61K45/06

摘要： Disclosed are hydrochloride and tosylate crystalline salt forms of (5S,8S)-8-[{(1R)-1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diazaspiro[4.5]decan-2-one, represented by Formula I and methods of preparing the same.

公开(公告)号：US09856219B2

公开(公告)日：2018-01-02

申请号：US15228088

申请日：2016-08-04

申请人： Nivalis Therapeutics, Inc.

发明人： Xicheng Sun ,  Jian Qiu ,  Adam Stout

IPC分类号： C07D215/20 ,  C07D215/46 ,  C07D215/00 ,  C07D215/42 ,  C07D215/54 ,  C07D215/60 ,  C07D401/04 ,  C07D401/10 ,  C07D409/04 ,  C07D409/14 ,  C07D413/10 ,  C07D417/10 ,  A61K31/47 ,  A61K31/4706 ,  A61K31/4709

CPC分类号： C07D215/20 ,  A61K31/47 ,  A61K31/4706 ,  A61K31/4709 ,  C07D215/00 ,  C07D215/42 ,  C07D215/46 ,  C07D215/54 ,  C07D215/60 ,  C07D401/04 ,  C07D401/10 ,  C07D409/04 ,  C07D409/14 ,  C07D413/10 ,  C07D417/10

摘要： The present invention is directed to novel quinoline compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors, pharmaceutical compositions comprising such compounds, and methods of making and using the same.

公开(公告)号：US09802935B2

公开(公告)日：2017-10-31

申请号：US15336880

申请日：2016-10-28

申请人： Heptares Therapeutics Limited

发明人： John Andrew Christopher ,  Miles Stuart Congreve ,  Sarah Joanne Bucknell ,  Francesca Deflorian ,  Mark Pickworth ,  Jonathan Stephen Mason

IPC分类号： C07D215/00 ,  C07D471/10

CPC分类号： C07D471/10

摘要： The disclosures herein relate to novel compounds of formula wherein R1, R2 and R3 are as defined herein, and their use in treating, preventing, ameliorating, controlling or reducing cerebrovascular or vascular disorders associated with CGRP receptor function.

公开(公告)号：US09764046B2

公开(公告)日：2017-09-19

申请号：US14601480

申请日：2015-01-21

申请人： CANON KABUSHIKI KAISHA

发明人： Kohei Watanabe ,  Taichi Shintou ,  Tsuyoshi Nomoto ,  Takeshi Miyazaki ,  Toshio Tanaka ,  Yuhei Nishimura ,  Yasuhito Shimada ,  Norihiro Nishimura

IPC分类号： A61K49/00 ,  C07D221/18 ,  C07D235/02 ,  C07D277/08 ,  C07D277/62 ,  C07D263/54 ,  C07D209/70 ,  C07D209/96 ,  C07D215/00 ,  C07D221/14 ,  C07D277/34 ,  C07D277/36 ,  C07D277/64 ,  C07D311/82 ,  C07D311/86 ,  C07D405/04 ,  C07D405/06 ,  C07D413/04 ,  C07D413/06 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14 ,  C07D491/052 ,  C07D491/12 ,  C07D497/10 ,  G01N33/50 ,  G01N33/58

CPC分类号： A61K49/0021 ,  A61K49/0002 ,  A61K49/0039 ,  A61K49/0041 ,  A61K49/006 ,  C07D209/70 ,  C07D209/96 ,  C07D215/00 ,  C07D221/14 ,  C07D221/18 ,  C07D263/54 ,  C07D277/34 ,  C07D277/36 ,  C07D277/64 ,  C07D311/82 ,  C07D311/86 ,  C07D405/04 ,  C07D405/06 ,  C07D413/04 ,  C07D413/06 ,  C07D417/04 ,  C07D417/06 ,  C07D417/14 ,  C07D491/052 ,  C07D491/12 ,  C07D497/10 ,  G01N33/5088 ,  G01N33/582 ,  G01N2333/4603

摘要： The invention provides a labeling composition for an intraocular tissue of a living individual, which specifically labels the intraocular tissue without need of an invasive operation such as exposure of an ocular tissue or injection of a staining agent into the ocular tissue or a nerve tissue linking to the ocular tissue, a method of noninvasively labeling an intraocular tissue of a living individual, and a screening method using the labeling composition for the intraocular tissues. The composition contains a compound capable of labeling at least a photoreceptor cell layer of a retina, wherein the compound is a staining compound having a particular structure as a partial structure thereof.

公开(公告)号：US09630924B2

公开(公告)日：2017-04-25

申请号：US15055108

申请日：2016-02-26

申请人： Takeda Pharmaceutical Company Limited

发明人： Satoshi Yamamoto ,  Junya Shirai ,  Tsuneo Oda ,  Mitsunori Kono ,  Atsuko Ochida ,  Takashi Imada ,  Hidekazu Tokuhara ,  Yoshihide Tomata ,  Naoki Ishii ,  Michiko Tawada ,  Yoshiyuki Fukase ,  Tomoya Yukawa ,  Shoji Fukumoto

IPC分类号： C07D471/04 ,  C07D215/00 ,  C07D217/26 ,  C07F7/08 ,  C07D491/048 ,  C07D491/056 ,  A61K31/4375 ,  A61K31/472 ,  A61K31/4741 ,  C07D217/14 ,  C07D491/14

CPC分类号： C07D217/26 ,  A61K31/4375 ,  A61K31/472 ,  A61K31/4741 ,  C07D217/14 ,  C07D471/04 ,  C07D491/048 ,  C07D491/056 ,  C07D491/14 ,  C07F7/0812

摘要： The present invention provides a heterocyclic compound having a RORγt inhibitory action.The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification. or a salt thereof.

公开(公告)号：US09346794B1

公开(公告)日：2016-05-24

申请号：US14981999

申请日：2015-12-29

申请人： Boehringer Ingelheim International GmbH

发明人： Thorsten Oost ,  Dennis Fiegen ,  Christian Gnamm

IPC分类号： A61K31/54 ,  A61K31/50 ,  A61K31/501 ,  A61K38/00 ,  A61P11/06 ,  A61P17/00 ,  A61P29/00 ,  C07D215/00 ,  C07D213/62 ,  C07D417/04 ,  C07D213/82 ,  C07D401/04 ,  C07D413/04 ,  C07D405/04

CPC分类号： C07D417/04 ,  C07D213/82 ,  C07D401/04 ,  C07D405/04 ,  C07D413/04

摘要： This invention relates to substituted 4-pyridones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other auto-immune and allergic disorders, allograft rejection, and oncological diseases.