Abstract: A bispecific antibody which is capable of specifically binding to PD-1 and CD3 is disclosed. The bispecific antibody is suitable for preventing, suppressing symptom progression or recurrence of, and/or treating autoimmune diseases. Also disclosed is a formulation which can reduce occurrence of adverse infusion reactions or adverse reaction called cytokine release syndrome. The bispecific antibody has the feature to allow interaction between PD-1 and PD-L1 as its ligand, contributes enhancement or duration of its effects.
Type:
Grant
Filed:
February 8, 2019
Date of Patent:
August 17, 2021
Assignee:
ONO PHARMACEUTICAL CO., LTD.
Inventors:
Shiro Shibayama, Takuya Shimbo, Tomoya Tezuka, Mark Throsby, Cornelis Adriaan de Kruif, Pieter Fokko van Loo, Rinse Klooster
Abstract: An object of the present disclosure is to provide a novel therapeutic agent for a cartilage-related disease, having cartilage regenerating action. Since a substance having SIK2 inhibitory action has chondrocyte differentiation promoting action, a therapeutic agent containing a substance having SIK2 inhibitory action is useful as a therapeutic agent having cartilage regenerating action for cartilage-related diseases such as cartilage damage or osteoarthritis.
Abstract: A medicament comprising a combination of a compound represented by formula (I), a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug of any of these and an immune checkpoint inhibitor (such as an anti-PD-1 antibody), which exhibits a strong anti-tumor effect and thus is useful for the treatment of cancer.
Abstract: A bispecific antibody which is capable of specifically binding to PD-1 and CD3 is disclosed. The bispecific antibody is suitable for preventing, suppressing symptom progression or recurrence of, and/or treating autoimmune diseases. Also disclosed is a formulation which can reduce occurrence of adverse infusion reactions or adverse reaction called cytokine release syndrome. The bispecific antibody has the feature to allow interaction between PD-1 and PD-L1 as its ligand, contributes enhancement or duration of its effects.
Type:
Application
Filed:
February 8, 2019
Publication date:
July 15, 2021
Applicant:
ONO PHARMACEUTICAL CO., LTD.
Inventors:
Shiro SHIBAYAMA, Takuya SHIMBO, Tomoya TEZUKA, Mark THROSBY, Cornelis Adriaan de KRUIF, Pieter Fokko van LOO, Rinse KLOOSTER
Abstract: The present invention relates to a Brk inhibitory compound represented by general formula (I) (wherein, all symbols represent the same meanings as the symbols set forth in the specification), a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug of any of these.
Abstract: The object of the present invention is to provide a method for identifying a patient with malignant tumor on which the effect of an immune checkpoint inhibitor can be more expected, and agents for suppressing the progression of, suppressing the recurrence of, and/or treating malignant tumor, characterized by prescriptions based on those. The present invention can provide agents for suppressing the progression of, suppressing the recurrence of, and/or treating malignant tumor, characterized by prescriptions based on identifying a patient with a malignant tumor on which the effect of an immune checkpoint inhibitor can be more expected, by analyzing the evaluation items consisting of combinations such as the PD-1 expression intensity, the percentage of the number of PD-1 expressing cells and the like in Treg cells and CD8+ T cells in tumor tissue or blood.
Type:
Application
Filed:
May 30, 2019
Publication date:
July 1, 2021
Applicants:
ONO PHARMACEUTICAL CO., LTD., NATIONAL CANCER CENTER
Abstract: Disclosed is a compound of formula (I): wherein all symbols are defined in the description. Also disclosed are pharmaceutical compositions comprising the compounds, methods of making the compounds, kits comprising the compounds, and methods of using the compounds, compositions and kits for treatment of disorders associated with TREK-1, TREK-2 or both TREK-1 and TREK-2 dysfunction in a mammal.
Type:
Grant
Filed:
December 14, 2017
Date of Patent:
June 29, 2021
Assignees:
ONO PHARMACEUTICAL CO., LTD., VANDERBILT UNIVERSITY
Inventors:
Craig W Lindsley, Joshua M. Wieting, Kevin M. McGowan, Jerod S. Denton, Kentaro Yashiro, Haruto Kurata, Yoko Sekioka, Takahiro Mori, Yuzo Iwaki
Abstract: Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
Abstract: A compound represented by general formula (I): (wherein in the formula, all the symbols have the same meanings as those described in the specification), or a pharmaceutically acceptable salt thereof is useful as a medicament's active ingredient having an EP4 receptor antagonistic activity, in preventing and/or treating disease caused by activation of an EP4 receptor.
Abstract: COMPOUNDS The present invention provides compounds of the general formula (I), their salts and N-oxides, and solvates and prodrugs thereof (wherein the substituents are as defined in the description). The compounds of the general formula (I) are inhibitors of factor XIa, and are useful in the prevention of and/or therapy for thromboembolic diseases.
Type:
Application
Filed:
November 24, 2020
Publication date:
May 20, 2021
Applicant:
ONO PHARMACEUTICAL CO., LTD.
Inventors:
Akira IMAGAWA, Takashi KONDO, Taihei NISHIYAMA, Steve COURTNEY, Chris YARNOLD, Osamu ICHIHARA, Stuart FLANAGAN
Abstract: The problem of the present invention is to find an effective preventive and/or therapeutic agent for an autoimmune disease, in particular, pemphigus, pemphigoid, ANCA-related angiitis and to provide the same as a medicine. The compounds having a Btk inhibitory activity to be used in the present invention inhibits antibody production from B cells and, moreover, inhibits the formation of neutrophil extracellular traps (NETs).
Abstract: A combination of the present invention is an effective therapy for glaucoma, in particular a combination of 2-propanyl 4-{(3S,5aR,6R,7R,8aS)-6-[(1E,3R)-4-(2,5-difluorophenoxy)-3-hydroxy-1-buten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoate and a ?-blocker, is useful as an agent for treating glaucoma since the combination enhances intraocular pressure lowering action compared to a single administration of each drug and has an effect of maintaining intraocular pressure lowering action.
Abstract: A compound represented by the general formula (V) wherein all the symbols are as defined in the specification, has an improved balance of the agonist activity against the S1P5 receptor relative to the S1P1 receptor, and can thus serve as a therapeutic agent for S1P5-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases.
Abstract: Since a compound represented by the general formula (I) (wherein definition of each group is as described in the specification), a salt thereof, a solvate thereof, or a prodrug thereof has strong and sustaining intraocular pressure lowering activity and, further, has no side effect on eyes such as ocular stimulating property (hyperemia, corneal clouding etc.), aqueous humor protein rise etc., it has high safety, and can be an excellent agent for preventing and/or treating glaucoma etc.
Abstract: The present invention relates to particulate forms of anamorelin monohydrochloride or a composition comprising anamorelin monohydrochloride having controlled chloride content, preferably isolated in an amorphous and/or fine particulate state, processes for making the particulate forms, and pharmaceutical compositions comprising the particulate forms.
Type:
Grant
Filed:
January 24, 2020
Date of Patent:
February 2, 2021
Assignees:
Helsinn Healthcare SA, Ono Pharmaceutical Co., Ltd.
Inventors:
Shin-itsu Kuwabe, Takehiko Yanagimachi, Hideyuki Yoshiyama, Seemon Pines, Eleanor de Groot, Silvina Garcia Rubio, Peter Manini
Abstract: A method for producing a compound, such as 2-propanyl 4-{(3S,5aR,6R,7R,8aS)-6-[(1E,3R)-4-(2,5-difluorophenoxy)-3-hydroxy-1-buten-1-yl]-7-hydroxyoctahydro-2H-cyclopenta[b]oxepin-3-yl}butanoate, and a novel intermediate suitable for the method, whereby the compound can be stably supplied with a high total reaction yield, by changing the starting material and improving the metathesis reaction, asymmetric reduction reaction and the like.
Abstract: The purinone derivative 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one hydrochloride has Btk-selective inhibitory activity and, in addition to having excellent metabolic stability, it is a compound that exhibits a high level of solubility and absorption with respect to the free base and can be crystallized, hence it can serve as a therapeutic agent for diseases involving B cells and mast cells.
Abstract: A compound represented by general formula (I) (wherein all symbols are as defined in the description) or a salt, solvate, N-oxide form or prodrug thereof is a potent FXIa inhibitor, has excellent oral absorption properties and kinetics in blood, can exert a potent anti-coagulation activity over a long period of time after being administered orally, and has a discrepancy between the anti-coagulation activity thereof and the CYP-inhibiting activity thereof. Therefore, the compound or the salt, solvate, N-oxide form or prodrug thereof can be used as an efficient prophylactic and/or therapeutic agent for vascular occlusive diseases.
Abstract: An object of the present invention is to provide a combination therapy in which an antitumor effect is enhanced as compared to when a Trk inhibitor or any of various kinase inhibitors is administered alone. A Trk inhibitor, particularly, a compound represented by General Formula (I): wherein all symbols have the same meanings as symbols described in this specification, a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof is useful as an active ingredient of a cancer therapeutic agent used in combination with one or more drugs selected from the group consisting of an MEK inhibitor, a CDK4/6 inhibitor, an EGFR inhibitor and a JAK1/2 inhibitor.
Abstract: Disclosed is a method for assisting a determination of an efficacy of an immune checkpoint inhibitor, the method comprising: measuring a free protein marker in a liquid sample collected from a subject; and determining the efficacy of the immune checkpoint inhibitor in the subject based on a result of the measurement, wherein the free protein marker is at least one selected from free Cytotoxic T lymphocyte antigen-4 (CTLA-4), free Programmed cell death-1 (PD-1) and free Programmed cell death-ligand 1 (PD-L1).