Abstract: The present invention relates to a compound represented by general formula (I) (wherein, all symbols represent the same meanings as the symbols set forth in the specification), a salt thereof, a solvate thereof an N-oxide thereof, or a prodrug of any of these. Since the compound has a Brk inhibitory activity, the compound is useful as a drug ingredient for the prevention and/or treatment of Brk-related diseases such as cancer, for example.
Abstract: (1S)-2-acetyl-1-(4-chloro-2-methoxyphenyl)-5-fluoro-1,2,3,9-tetrahydrospiro[?-carboline-4,1?-cyclopropane] can significantly suppress a decrease of a pain threshold compared to well-known TSPO antagonists, and thus can be an excellent prophylactic and/or therapeutic agent for fibromyalgia, fibromyalgia-associated diseases, and fibromyalgia-associated symptoms.
Abstract: Compounds represented by general formula (I) (all of the symbols in the formula conform to the definitions in the Description) are compounds that, in addition to having a Btk-selective inhibitory activity, exhibit an excellent metabolic stability and can avoid hepatotoxicity or the like, and as a consequence can provide safe therapeutic agents for diseases in which B cells or mast cells participate.
Abstract: The present invention provides a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy for Trk-related diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I), wherein all symbols represent the same meanings as described in the specification, a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.
Abstract: A compound represented by general formula (I) has a strong Axl inhibitory activity by introducing a distinctive bicyclic structure in which a saturated carbon ring is fused to a pyridone ring, and can be a therapeutic agent for Axl-related diseases, for example, cancer such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glioma, kidney diseases, immune system diseases, and circulatory system diseases
Type:
Grant
Filed:
December 8, 2016
Date of Patent:
June 12, 2018
Assignee:
ONO PHARMACEUTICAL CO., LTD.
Inventors:
Takayuki Inukai, Jun Takeuchi, Tomoko Yasuhiro
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: 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:
April 21, 2016
Date of Patent:
May 29, 2018
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: An object of the present invention is to provide a drug having the inhibitory activity on ENPP2 which is a different target from that of the existing drug, as a medicament useful in a urinary excretion disorder patient for whom the existing drug has the insufficient effect. The present invention provides a compound represented by the general formula (I): (wherein definition of each group is as defined in the description) having the ENPP2 inhibitory activity, a salt thereof or a solvate thereof or a prodrug thereof, and an agent for preventing or treating urinary excretion disorder and/or improving symptoms thereof, containing them as an active ingredient.
Abstract: Provision of orally-available and low-toxic somatostatin receptor subtype 2 agonist. Since the compound represented by the general formula (I): wherein all symbols represent the same meanings as those described in the description, a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof is non-peptidic low-molecular compound which has strong somatostatin receptor subtype 2 agonist activity, the compound is orally-available. Additionally, since the compound is low-toxic, the compound is useful for the prevention and/or treatment of the somatostatin related diseases such as acromegaly or gastrointestinal obstruction.
Abstract: The present invention provides a drug-eluting stent graft for preventing stent graft-related complications as well as treating aneurysm. Specifically, the present invention relates to a drug-eluting stent graft comprising a drug, a drug-retaining agent and a stent graft, and a method for therapy of aneurysm including the use of the drug-eluting stent graft.
Type:
Grant
Filed:
September 10, 2014
Date of Patent:
May 15, 2018
Assignees:
ONO PHARMACEUTICAL CO., LTD., OSAKA UNIVERSITY
Abstract: The present invention relates to use of an antagonist of BIR1 (B cell immunoglobulin receptor 1) related to the present invention, a method for screening the antagonist, in addition to subtype polypeptides of BIR1, the polynucleotide encoding them and antibodies for the polypeptides. BIR1 functions as an immunosuppressive receptor, and the antagonist of BIR1 has immunopotentive activity, which is able to use for preventing and/or treating a cancer, an immunodeficiency disease or an infectious disease.
Type:
Application
Filed:
November 22, 2017
Publication date:
May 3, 2018
Applicant:
ONO PHARMACEUTICAL CO., LTD.
Inventors:
Tomoyuki ODANI, Hideaki TADA, Kimiho YAMADA
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:
April 21, 2016
Date of Patent:
May 1, 2018
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 extracting a lead compound from a plurality of compounds against a drug discovery target, includes the steps of creating a scatter diagram for a plurality of compounds by disposing symbols representing the compounds according to a plurality of features of the compounds and extracting a lead compound from the compounds represented by the symbols disposed in a predetermined region of the scatter diagram. The locations of the symbols to be disposed on the scatter diagram are determined according to first and second features (for example, selectivity and activity) of the respective compounds, and attributes (for example, color and size) of the symbols are determined according to third and fourth features (for example, molecular weight and ligand efficiency) of the respective compounds.
Type:
Application
Filed:
April 21, 2016
Publication date:
March 29, 2018
Applicant:
ONO PHARMACEUTICAL CO., LTD.
Inventors:
Masakuni KURONO, Hiromu EGASHIRA, Jun TAKEUCHI
Abstract: Compounds represented by general formula (I) (all of the symbols in the formula conform to the definitions in the Description) are compounds that, in addition to having a Btk-selective inhibitory activity, exhibit an excellent metabolic stability and can avoid hepatotoxicity or the like, and as a consequence can provide safe therapeutic agents for diseases in which B cells or mast cells participate.
Abstract: According to the present invention, differently from well-known production methods, with the use of a different starting material, Ullmann condensation which may decrease the yield with an increase of a production scale can be avoided and thus 6-amino-9-[(3R)-1-(2-butynoyl)-3-pyrrolidinyl]-7-(4-phenoxyphenyl)-7,9-dihydro-8H-purin-8-one can be provided safely and stably with high reaction yield.
Abstract: To produce and/or maintain naïve pluripotent stem cells capable of highly expressing genes important for maintaining an undifferentiated state, which could not be achieved by known methods for producing pluripotent stem cells. The present invention can produce naïve pluripotent stem cells capable of maintaining an undifferentiated state by introducing and allowing transient expression of six genes (Oct3/4, Klf4, c-Myc, Sox2, Nanog, and Klf2) among the so-called initializing factors, and further performing culturing in a medium containing LIF, an MEK inhibitor, a GSK3 inhibitor, a cAMP production promoter, a TGF-? inhibitor and a PKC inhibitor. Thus, the problem of the present invention can be solved.
Type:
Application
Filed:
March 17, 2016
Publication date:
March 22, 2018
Applicants:
ONO PHARMACEUTICAL CO., LTD., KEIO UNIVERSITY
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: The compound of the formula (I-1): wherein all the symbols have the same meanings as described in the specification, has two cyclic groups, particularly phenoxy groups at specific substitution positions and thus has high human S1P2 antagonistic activity. The compound may therefore be used as a therapeutic agent for S1P2-mediated diseases such as diseases resulting from vascular constriction, fibrosis, and respiratory 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.