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: 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:
Grant
Filed:
January 23, 2017
Date of Patent:
July 2, 2019
Assignee:
ONO PHARMACEUTICAL CO., LTD.
Inventors:
Akira Imagawa, Takashi Kondo, Taihei Nishiyama, Steve Courtney, Chris Yarnold, Osamu Ichihara, Stuart Flanagan
Abstract: Inhibitors for Bruton's Tyrosine Kinase (BTK) are disclosed as are compositions thereof, methods for their preparation, and methods for their use.
Type:
Grant
Filed:
February 23, 2018
Date of Patent:
June 11, 2019
Assignees:
GILEAD SCIENCES, INC., ONO PHARMACEUTICAL CO., LTD.
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: 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 26, 2018
Date of Patent:
May 28, 2019
Assignees:
ONO PHARMACEUTICAL CO., LTD, HELSINN HEALTHCARE SA
Inventors:
Shin-itsu Kuwabe, Takehiko Yanagimachi, Hideyuki Yoshiyama, Seemon Pines, Eleanor de Groot, Silvina Garcia Rubio, Peter Manini
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:
Application
Filed:
December 31, 2018
Publication date:
May 9, 2019
Applicant:
ONO PHARMACEUTICAL CO., LTD.
Inventors:
Takayuki Inukai, Jun Takeuchi, Tomoko Yasuhiro
Abstract: Crystal polymorphism may exist in a crystalline compound. In the case where crystal polymorphism exists, depending on the crystal form, solubility, dissolution rate, stability against heat, light, humidity, etc. or the like is different. Accordingly, in the production of a pharmaceutical product, it is a very important task to select a crystal form of a drug substance most suitable for a disease indication and a dosage form. The present invention relates to novel crystal forms (A crystal, W crystal, and a hydrate crystal (H crystal)) of a compound I having a strong opening action with respect to KCNQ2-5 channels.
Abstract: Disclosed are a method for treating brain tumors, as well as a medicament for treating brain tumors. Provided is a medicament for treating brain tumors, the medicament containing a combination of 4-[4-cyano-2-({[(2?R,4S)-6-(isopropylcarbamoyl)-2,3-dihydrospiro[chromene-4,1?-cyclopropan]-2?-yl]carbonyl}amino)phenyl]butanoic acid or a pharmaceutically acceptable salt thereof, and an anti-PD-1 antibody. The combination exhibits an excellent effect for treating brain tumors, and is thus useful to treat brain tumors.
Type:
Application
Filed:
October 31, 2018
Publication date:
May 2, 2019
Applicants:
ONO PHARMACEUTICAL CO., LTD., The Regents of The University of California
Abstract: An object of the present invention is to provide a novel compound having a strong opening action with respect to KCNQ2-5 channels. A compound represented by the general formula (1) (wherein the definition of each group is as described in the specification) is provided. The compound represented by the general formula (1) has a strong opening action with respect to KCNQ2-5 channels, and therefore is useful as a prophylactic and/or therapeutic agent for a KCNQ2-5 channel-related disease (for example, dysuria, overactive bladder, or the like).
Type:
Application
Filed:
April 21, 2017
Publication date:
May 2, 2019
Applicant:
ONO PHARMACEUTICAL CO., LTD.
Inventors:
Kentaro YASHIRO, Masashi KATO, Tetsuji SAITO, Takuya OKADA, Daisuke WAKAMATSU, Adam James DAVENPORT, Christopher Charles STIMSON
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 drug for cancer therapy characterized in that an Axl inhibitor and an immune checkpoint inhibitor (for example, an anti-PD-1 antibody) are administered in combination, wherein the Axl inhibitor is a compound represented by the general formula (I): (wherein in the formula, all of the symbols have the same meanings as defined in the specification), a salt thereof, a solvate thereof, an N-oxide thereof, or a prodrug thereof, and the combination exhibits a strong anti-tumor effect and, therefore, is useful for cancer therapy.
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: 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: 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: To provide a medicament which shows more remarkable effect in treatment of activated B-cell like diffuse large B-cell lymphoma (ABC-CLBCL) than the existing Btk inhibitor, and is excellent in safety. The present compound exhibits more remarkable effect in treatment of activated B-cell like diffuse large B-cell lymphoma (ABC-DLBCL) patients, inter alia, ABC-DLBCL patients having CD79B wild-type gene background than the existing Btk inhibitor, and therefore, it can attain the object of the present invention.
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:
May 10, 2018
Date of Patent:
February 19, 2019
Assignee:
ONO PHARMACEUTICAL CO., LTD.
Inventors:
Takayuki Inukai, Jun Takeuchi, Tomoko Yasuhiro
Abstract: A compound represented by general formula (I) and having a quinoline skeleton has a strong Axl inhibitory activity, and therefore the compound can be an agent for treating Axl-related diseases, for example, cancer such as acute myeloid leukemia, chronic myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glioma, kidney diseases, immune system diseases, and circulatory system diseases.
Type:
Grant
Filed:
December 24, 2015
Date of Patent:
February 19, 2019
Assignee:
ONO PHARMACEUTICAL CO., LTD.
Inventors:
Takayuki Inukai, Jun Takeuchi, Tomoko Yasuhiro
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 a compound represented by the general formula (I) (wherein the definition of each group has the same meaning as described in the specification). The compound is useful as preventive and/or therapeutic agent for KCNQ2-5 channel-related diseases.