Abstract: A method for preparing a compound represented by general formula I: or a salt thereof includes a step of reacting a compound represented by formula II: with a reducing agent to cleave an oxazolidine ring fused to a cycle A?. The reducing agent includes at least one of phosphines, metal hydrides, or transition metal catalysts in the presence of hydrogen gas.
Type:
Grant
Filed:
September 20, 2016
Date of Patent:
March 30, 2021
Assignees:
MITSUBISHI TANABE PHARMA CORPORATION, OSAKA UNIVERSITY
Abstract: This method of analyzing the phenylhydrazine content in a 3-methyl-1-phenyl-2-pyrazolin-5-one bulk drug involves: obtaining a first measured value by measuring the phenylhydrazine content of a standard solution that contains phenylhydrazine or a salt thereof, a first acidic water and a first water-soluble organic solvent, and that exhibits a phenylhydrazine concentration of 0.01 ?g/mL to 10 ?g/mL; obtaining a second measured value by measuring the phenylhydrazine content in a sample solution that contains a 3-methyl-1-phenyl-2-pyrazolin-5-one bulk drug, a second acidic water and a second water-soluble organic solvent; and detecting the phenylhydrazine content in the 3-methyl-1-phenyl-2-pyrazolin-5-one bulk drug on the basis of the first measured value and the second measured value.
Abstract: The present disclosure is directed to compositions comprising as an active ingredient, a lower dose of 4-({(1-cyclopropy-lisoquinolm-3-yl)[4-(trifluoromethoxy)benzyl]amino}sulfonyl)benzoic acid or a pharmaceutically acceptable salt thereof for treating or preventing vasomotor symptoms in a subject, and methods which comprises administering the said compound or the pharmaceutically acceptable salt thereof at a lower dose, respectively.
Abstract: Provided are a novel compound having a superior inhibitory action on KAT-II, a production method thereof, use thereof, and a pharmaceutical composition containing the aforementioned compound and the like. A compound represented by the formula (I) or a pharmacologically acceptable salt thereof. wherein each symbol is as defined in the DESCRIPTION.
Abstract: The present invention provides a drug for treating cocaine addiction or preventing the relapse of the same. Specifically, the present invention provides a drug for treating cocaine addiction or preventing the relapse of the same containing (R)-2-{3-[1-(5-methyl-1,2,3,4-tetrahydronaphthalen-1-yl)piperidin-4-yl]-2,3-dihydro-2-oxo-benzimidazol-1-yl}-N-methylacetamide or a pharmaceutically acceptable salt thereof.
Abstract: The present invention relates to a production method of 4-alkoxy-3-trifluoromethylbenzyl alcohol at a high conversion ratio, which can strictly suppress production of a byproduct by using DIBAL as a reducing agent.
Abstract: The present invention provides: a methyl 1-{2-[(3S,4R)-1-[(3R,4R)-1-cyclopentyl-3-fluoro-4-(4-methoxyphenyl) pyrrolidine-3-carbonyl]-4-(methoxymethyl)pyrrolidin-3-yl]-5-(trifluoromethyl) phenyl}piperidine-4-carboxylate 1/2 ethane-1,2-disulfonic acid which is represented by formula (1) and is excellent in crystallinity; and a method for producing the same; and a production intermediate thereof; and a production method using this compound.
Abstract: A compound represented by general formula [I] wherein X represents N or the like, Y represents CH or the like; RA represents a cycloalkyl group which may be substituted or the like, R1 represents an alkyl group or the like, R2 represents an alkyl group which may be substituted or the like, R3 represents a hydrogen atom or an alkyl group, or a pharmaceutically acceptable salt thereof has an inhibitory activity on aldosterone synthetase, and is useful as a prophylactic and/or therapeutic agent for various diseases or symptoms associated with aldosterone.
Abstract: The present invention provides a process for preparing a compound represented by formula (VII), which comprises reacting a compound represented by formula (VI) with a malonic acid derivative in the presence of a base and an asymmetric catalyst in a two layer solvent system of hydrophobic solvent and water.
Abstract: The present invention relates to a novel imidazole compound or a pharmaceutically acceptable salt thereof having a melanocortin receptor agonistic activity, and medical use thereof. The present invention relates to an imidazole compound represented by general formula [I] [wherein: Ring A represents an optionally substituted aryl group or the like; R1 represents a hydrogen atom, an optionally substituted alkyl group, or the like; R2 represents a hydrogen atom, a halogen atom, or the like; and R3 represents an optionally substituted alkyl group] or a pharmaceutically acceptable salt thereof.
Abstract: A method of producing a rotavirus-like particle (RLP) in a plant is provided. The method comprises expressing within a host or host cell for example a plant, portion of a plant or plant cell one or more nucleic acid comprising one or more regulatory region operatively linked to a first, second and third nucleotide sequence, the regulatory region active in the host or host cell. The first nucleotide sequence encoding a first rotavirus protein, the second nucleotide sequence encoding a second rotavirus protein and the third nucleotide sequence encoding a third rotavirus protein. The first, second and third encode rotavirus protein NSP4 and VP2 or VP6 and VP4 or VP7. The host or host cell is incubated under conditions that permit the expression of the nucleic acids, so that NSP4 and either VP2 of VP6 and VP4 or VP7 are expressed, thereby producing the RLP. Hosts comprising the RLP, compositions comprising the RLP and method for using the composition are also provided.
Abstract: Provided is a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2. The present invention relates to a compound represented by the following formula (I): wherein each symbol is as described in the DESCRIPTION. The compound has a selective MMP-9 production suppressive action, and is useful as a drug for the prophylaxis and/or treatment of autoimmune diseases such as rheumatoid arthritis and the like, inflammatory bowel diseases (ulcerative colitis, Crohn's disease) or osteoarthritis.
Abstract: The present invention aims to obtain an anti-repulsive guidance molecule a (RGMa) antibody having a high binding activity and few side effects which can be used as a medicine for preventing, treating, or preventing the relapse of neurological or immunological diseases. The problem is solved by providing an isolated RGMa binding protein which does not inhibit binding between RGMa and neogenin but neutralizes the neurite outgrowth inhibiting activity of RGMa, preferably by providing an anti-RGMa antibody which has complementarity determining regions having amino acid sequences of SEQ ID NOS: 30-35 or SEQ ID NOS: 36-40 in Sequence Listing, and SFG.
Type:
Application
Filed:
March 19, 2019
Publication date:
September 5, 2019
Applicants:
MITSUBISHI TANABE PHARMA CORPORATION, OSAKA UNIVERSITY, NATIONAL UNIVERSITY CORPORATION CHIBA UNIVERSITY
Abstract: Provided are a novel compound having a superior inhibitory action on KAT-II, a production method thereof, use thereof, and a pharmaceutical composition containing the aforementioned compound and the like. A compound represented by the formula (I) or a pharmacologically acceptable salt thereof. wherein each symbol is as defined in the DESCRIPTION.
Abstract: This invention provides a novel disubstituted 1,2,4-triazine compound or a pharmaceutically acceptable salt thereof, which has an aldosterone synthetase inhibitory activity and is useful for preventing and/or treating various diseases or conditions associated with aldosterone; a method for preparing it; use of it; as well as a pharmaceutical composition comprising it as an active ingredient. A compound of the general formula [I]: wherein RA is, for example, a group of the following formula (A-1): wherein ring A1 is, for example, a cycloalkyl group which may be substituted, and RB is, for example, a monocyclic cycloalkyl group, or a pharmaceutically acceptable salt thereof.
Abstract: The present invention provides: a novel use of a specific bicyclic nitrogen-containing heterocyclic compound as a PDE7 inhibitor; a novel bicyclic nitrogen-containing heterocyclic compound having a PDE7 inhibitory effect, a method for producing the compound, a use of the compound, and a pharmaceutical composition containing the PDE7 inhibitor or the compound; and others. More specifically, the present invention provides a PDE7 inhibitor containing the compound represented by the formula (I): [wherein the symbols have the same meanings as those described in the description] or a pharmaceutically acceptable salt thereof as an active ingredient.
Abstract: Provided is a bi-specific fusion polypeptide comprising a fynomer sequence that binds to interleukin-17a (IL-17a) and is conjugated to an antibody or subsequence thereof that binds to interleukin-6 receptor (IL-6R). The fusion polypeptide can bind to both IL-17a and IL-6R thereby suppresses, reduces, decreases, inhibits or blocks both IL-17a and IL-6R activities.
Type:
Grant
Filed:
March 16, 2015
Date of Patent:
June 18, 2019
Assignee:
MITSUBISHI TANABE PHARMA CORPORATION
Inventors:
Roland Newman, Steve Granger, Michael Lyman, Dragan Grabulovski, Richard Woods, Michela Silacci, Wenjuan Zha, Isabella Attinger-Toller
Abstract: The compound represented by the general formula: wherein ring A is benzene which may be substituted and the like; ring B is benzene which may be substituted and the like; X is a single bond and the like; Y is alkyl which may be substituted and the like; Z is CR1 or nitrogen atom; R1 is hydrogen and the like; R2 is alkyl which may be substituted and the like or a pharmaceutically acceptable salt thereof is useful as a prevention/treatment agent of obesity, diabetes, and the like.