Abstract: The present invention provides a pharmaceutical composition for use in treating acute myeloid leukemia (AML) and a method of treating AML in a patient in need thereof. The present invention also provides a method for predicting the sensitivity to the treatment in the patient using gene expression signature.
Type:
Application
Filed:
October 21, 2016
Publication date:
October 25, 2018
Applicants:
DAIICHI SANKYO COMPANY, LIMITED, BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM
Inventors:
Kenji NAKAMARU, Koichi TAZAKI, Takahiko SEKI, Ngai-chiu Archie TSE, Michael ANDREEFF, Jo ISHIZAWA
Abstract: The present invention provides a method for treating a cancer in a subject in need thereof, comprising administering a specific MDM2 inhibitor to the subject according to a specific dosage regimen and a pharmaceutical composition for use in treating a cancer according to the dosage regimen. The present invention also provides a method for treating liposarcoma in a subject in need thereof, comprising administering a specific MDM2 inhibitor to the subject and a pharmaceutical composition for use in treating liposarcoma, comprising the MDM2 inhibitor.
Abstract: The present invention provides a compound having a particular chemical structure or a pharmacologically acceptable salt thereof which has an excellent inhibitory effect on EZH1 and/or EZH2 activity. The present invention provides a compound having a 1,3-benzodioxole structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, or a pharmaceutical composition comprising the compound (wherein R1, R2, R3, R4, R5, R6, and V in the formula (I) are each as defined in the present specification).
Abstract: The present invention relates to an antibody that binds to GARP and is useful as a therapeutic agent for a tumor, and a method for treating a tumor using the aforementioned antibody. It is an object of the present invention to provide an antibody, which inhibits the function of Treg in a tumor and is thereby used as a pharmaceutical product having therapeutic effects, a method for treating a tumor using the aforementioned antibody, and the like. An anti-GARP antibody that binds to GARP and exhibits inhibitory activity to Treg function and exhibits ADCC activity is obtained, and moreover a pharmaceutical composition for use in tumor therapy, comprising the aforementioned antibody, etc. is obtained.
Abstract: Provided is a test method for discriminating a liver injury type using as an indicator a level of lithocholic acid (hereinafter abbreviated as LCA) in a biological sample of a subject. That is, provided is a test method comprising measuring a level of LCA in a biological sample collected from a subject, and discriminating a liver injury type as hepatocellular injury type, cholestasis type, or a mixed type thereof using the measured level of LCA as an indicator.
Abstract: A method of producing a tablet in which an uncoated tablet is coated by a coating agent, the method including: a coating process of coating uncoated tablets with a coating agent by spray coating the coating agent onto tablets that are churned and tumbled inside a container, and drying the tablets inside the container by supplying drying air into the container and exhausting air from the container, wherein spray coating conditions, including air supply temperature, air supply rate, and spray speed, are controlled according to the weight of the coating agent with which the uncoated tablets are coated, such that the humidity of air exhausted during spray coating is within a range of from 14% RH to 30% RH.
Abstract: In a method for producing a de-dimethoxybenzylated compound by removing a dimethoxybenzyl group from a compound containing a dimethoxybenzyl group bonded to a nitrogen atom in the presence of an acid, the de-dimethoxybenzylated compound is obtained by removing the dimethoxybenzyl group without forming a poorly soluble product resulting from the removed dimethoxybenzyl group. The de-dimethoxybenzylation reaction is carried out in the presence of triphenylphosphine or diethylthiourea.
Abstract: It is an object of the present invention to provide a medicament for preventing or treating hyperphosphatemia. The solution is crystals, or hydrate thereof, of a salt of a compound represented by formula (I).
Type:
Grant
Filed:
September 18, 2015
Date of Patent:
August 21, 2018
Assignee:
DAIICHI SANKYO COMPANY, LIMITED
Inventors:
Mizuka Yokoyama, Yasusi Ueda, Daisuke Fukatsu, Yuichi Aki
Abstract: The present invention provides a method for producing an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, and an intermediate thereof. A method for producing an atropisomer of a pyrrole derivative using a compound represented by (B) [wherein R1 represents a C1-C4 alkyl group, and R2 represents a 2-hydroxyethyl group or a carboxymethyl group] as a production intermediate.
Type:
Application
Filed:
April 11, 2018
Publication date:
August 16, 2018
Applicant:
Daiichi Sankyo Company, Limited
Inventors:
Masashi Watanabe, Hiroshi Nagasawa, Noritada Sato
Abstract: The present disclosure provides processes for the preparation of a compound of formula I: or a salt thereof, active on the receptor protein kinases c-Kit and/or c-Fms and/or Flt3. The disclosure also provides compounds and processes for the preparation of the compounds that are synthetic intermediates to the compound of formula I.
Abstract: It has been found that a compound of the general formula (I) having an isoxazole skeleton has excellent inhibitory activity against mutant IDH1 protein and inhibits the production of 2-HG by this protein, while the compound is also capable of effectively inhibiting the growth of various tumors expressing the protein. In the formula, R1, R2, R3, Y, and Z are as defined in claim 1.
Type:
Grant
Filed:
October 1, 2015
Date of Patent:
August 7, 2018
Assignees:
Daiichi Sankyo Company, Limited, National Cancer Center
Abstract: An object is to provide a solid composition of stabilized pyrrole carboxamide. A means for achieving the object is a solid composition for medical use containing (S)-1-(2-hydroxyethyl)-4-methyl-N-[4-(methylsulfonyl)phenyl]-5-[2-(trifluoromethyl)phenyl]-1H-pyrrole-3-carboxamide and an appropriate additive.
Abstract: The present invention provides an EndoS mutant enzyme having an amino acid sequence of EndoS D233Q and further having a particular additional mutation and exhibiting a reduced hydrolysis activity, in comparison with the activity of EndoS D233Q, to an N-linked sugar chain (N297-linked sugar chain) linked to Asn at position 297 in IgG and a gene encoding the same.
Abstract: The present disclosure provides a method for efficiently producing and providing compounds having a spirooxindole skeleton, for example compounds having a spirooxindole skeleton and having antitumor activity that inhibit the interaction between Mdm2 protein and p53 protein, or intermediates thereof, using an asymmetric catalyst. Compounds having optically active tricyclic dispiroindole skeletons are obtained through catalytic asymmetric 1,3-dipolar cycloaddition reactions using ketimine as a reaction substrate and using a chiral ligand and a Lewis acid.
Abstract: Crystals of a dispiropyrrolidine compound or a salt thereof which inhibits the action of Mdm2 are provided. The present invention provides crystals of (3?R,4?S,5?R)—N-[(3R,6S)-6-carbamoyltetrahydro-2H-pyran-3-yl]-6?-chloro-4?-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2?-oxo-1?,2?-dihydrodispiro[cyclohexane-1,2?-pyrrolidine-3?,3?-indole]-5?-carboxamide or a salt thereof which inhibits Mdm2 and has anti-tumor activity. The present invention also provides a medicament comprising the same.
Abstract: The present invention provides an agent for treating and/or preventing adult T cell leukemia/lymphoma containing a compound having a specific chemical structure or a pharmaceutically acceptable salt thereof. Specifically, the present invention provides an agent for treating and/or preventing adult T cell leukemia/lymphoma containing, as an active ingredient, 7-chloro-2-[trans-4-(dimethylamino)cyclohexyl]-N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-2,4-dimethyl-1,3-benzodioxole-5-carboxamide or a pharmaceutically acceptable salt thereof, or 7-bromo-2-[trans-4-(dimethylamino)cyclohexyl]-N-[(4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl]-2,4-dimethyl-1,3-benzodioxole-5-carboxamide or a pharmaceutically acceptable salt thereof.
Type:
Application
Filed:
July 29, 2016
Publication date:
July 19, 2018
Applicants:
DAIICHI SANKYO COMPANY, LIMITED, THE UNIVERSITY OF TOKYO
Abstract: Crystals of a dispiropyrrolidine compound or a salt thereof which inhibits the action of Mdm2 are provided. The present invention provides crystals of (3?R,4?S,5?R)—N-[(3R,6S)-6-carbamoyltetrahydro-2H-pyran-3-yl]-6?-chloro-4?-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2?-oxo-1?,2?-dihydrodispiro[cyclohexane-1,2?-pyrrolidine-3?,3?-indole]-5?-carboxamide or a salt thereof which inhibits Mdm2 and has anti-tumor activity. The present invention also provides a medicament comprising the same.
Abstract: The present invention provides a compound having a particular chemical structure or a pharmacologically acceptable salt thereof which has an excellent inhibitory effect on EZH1 and/or EZH2 activity. The present invention provides a compound having a 1,3-benzodioxole structure represented by the general formula (I) or a pharmacologically acceptable salt thereof, or a pharmaceutical composition comprising the compound (wherein R1, R2, R3, R4, R5, R6, and V in the formula (I) are each as defined in the present specification).
Abstract: The present invention provides a method for producing an atropisomer of a pyrrole derivative having excellent mineralocorticoid receptor antagonistic activity, and an intermediate thereof. A method for producing an atropisomer of a pyrrole derivative using a compound represented by (B) [wherein R1 represents a C1-C4 alkyl group, and R2 represents a 2-hydroxyethyl group or a carboxymethyl group] as a production intermediate.
Type:
Grant
Filed:
September 8, 2017
Date of Patent:
June 26, 2018
Assignee:
Daiichi Sankyo Company, Limited
Inventors:
Masashi Watanabe, Hiroshi Nagasawa, Noritada Sato
Abstract: A crystal of a compound represented by the general formula (I) or a pharmacologically acceptable salt thereof has an excellent LCAT-activating effect and is useful as an active ingredient in a therapeutic or prophylactic agent for arteriosclerosis, arteriosclerotic heart disease, coronary heart disease (including heart failure, myocardial infarction, angina pectoris, cardiac ischemia, cardiovascular disturbance, and restenosis caused by angiogenesis), cerebrovascular disease (including stroke and cerebral infarction), peripheral vascular disease (including diabetic vascular complications), dyslipidemia, hypo-HDL-cholesterolemia, or renal disease, particularly, an anti-arteriosclerotic agent, wherein R1 is a hydrogen atom or a hydroxy group, and R is a 2-(trifluoromethyl)pyrimidin-5-yl group or a 5-(trifluoromethyl)pyrazin-2-yl group.