PATENTSCOPE: EN_ALL:nmr AND PA:otsuka

INDUSTRIAL PROCESS OF MONO-ALKYLATING A PIPERIDINE NITROGEN IN PIPERIDINE DERIVATIVES WITH DEUTERATED-ALKYL (Fri, 15 Mar 2019)
The present invention relates to a method of mono-alkylating a piperidine nitrogen in a piperidine derivative with a deuterated lower-alkyl, which comprises protecting the piperidine nitrogen with an aralkyl protective group, lower-alkylating the piperidine nitrogen with a deuterated-lower-alkylating agent under neutral or basic condition, and then deprotecting the aralkyl protective group.
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BENZAZEPINE DERIVATIVES (Fri, 04 Jan 2019)
The present invention provides novel benzazepine compounds of Formula (1), or salts thereof, having vasopressin V1a and V2 antagonisms, and medical uses thereof. In the formula, R1 is optionally substituted C1-6 alkyl, etc.; L is -C(=O)-NH-, etc.; Ring A1 is a hydrocarbon ring, etc.; Ring A2 is a hydrocarbon ring, etc.; and each of Rings A1 and A2 may have at least one substituent.
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PYRIMIDINE COMPOUND (Fri, 07 Dec 2018)
The present invention provides a novel pyrimidine compound represented by Formula [I] and a salt thereof: [in the formula, the symbols are as defined in the specification], which is useful for treating, preventing and/or diagnosing seizure and the like in disease involving epileptic seizure or convulsive seizure (including multiple drug resistant seizure, refractory seizure, acute symptomatic seizure, febrile seizure and status epilepticus), as well as a medical use therefor.
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PROCESS OF PREPARING IOSIMENOL (Fri, 09 Nov 2018)
The present invention relates to a 5-step process for preparing iosimenol starting from ammonium 3-amino-5-(aminocarbonyl)benzoate which is first converted to 3-amino-5-(aminocarbonyl)-2,4,6-triiodobenzoic acid using sodium iodine dichloride (NaICl2). The present invention further relates to processes for purifying iosimenol.
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6-PYRIMIDIN-ISOINDOLE DERIVATIVE AS ERK1/2 INHIBITOR (Fri, 26 Oct 2018)
This invention relates to the compound (2R)-2-(6-{5-chloro-2-[(oxan-4-yl)amino]pyrimidin-4-yl}-1 -oxo-2,3-dihydro-1 H-isoindol-2-yl)-N-[(1 S)-1-(3-fluoro-5-methoxyphenyl)-2-hydroxyethyl]propanamide, and in particular to novel physical forms of the compound, a process for preparing the compound and synthetic intermediates for use in the process, and novel formulations containing the compound, as well as therapeutic uses of the compound.
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CLIPTAC COMPOSITION (Fri, 15 Dec 2017)
This invention relates to proteolysis targeting chimeric molecules formed from the intracellular self-assembly of precursors via bioorthogonal click chemistry (CLIPTACs), as well as related precursor compositions, methods and therapeutic applications.
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5-METHYL-6-PHENYL-4,5-DIHYDRO-2H-PYRIDAZIN-3-ONE DERIVATIVE (Sat, 09 Sep 2017)
The present invention provides an agent for treating malignant tumor, comprising a compound of formula (1): wherein R1 to R4 are hydrogen atom, halogen, or etc., Y is optionally-substituted alkylene group or etc.
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OINTMENT (Fri, 07 Jul 2017)
An ointment is provided. The ointment stably comprises an oxazole compound that has specific inhibitory activity against PDE4 and that is represented by the following formula (11). The ointment can be efficiently absorbed into the skin.
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BENZOLACTAM COMPOUNDS AS PROTEIN KINASE INHIBITORS (Fri, 28 Apr 2017)
The invention provides a compound of formula (0): or a pharmaceutically acceptable salt, N-oxide or tautomer thereof. The compounds are inhibitors of ERK 1/2 kinases and will be useful in the treatment of ERKl/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.
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HETEROBICYCLIC COMPOUNDS AND THEIR USE FOR THE TREATMENT OF TUBERCULOSIS (Fri, 04 Mar 2016)
It is an object of the present invention to provide a compound having an excellent antibacterial activity against tuberculosis bacteria, multidrug-resistant tuberculosis bacteria and/or non-tuberculous mycobacteria. Disclosed is a compound of the general formula (1): wherein each symbol is defined as described in the attached specification, or a salt thereof.
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PHARMACEUTICAL FORMULATION COMPRISING A SUBSTITUED PHENYL- (1, 3-DIHYDRO-ISOINDOL-2-YL) -METHANONE (Fri, 25 Sep 2015)
Provided herein are formulations of (2,4-dihydroxy-5-isopropyl-phenyl)-[5-(4- methyl-piperazin-1-ylmethyl)-1,3-dihydro-isoindol-2-yl]-methanone of formula (I), or a L- lactate salt thereof, in a phosphate or succinate buffer.
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CYANOTRIAZOLE COMPOUNDS (Fri, 23 Jan 2015)
This invention relates to a cyanotriazole compound represented by the formula (1):, wherein each symbols are defined in the specification, or a salt thereof. The compound or a salt thereof stimulates the citric acid cycle activity and/or improves hyperglycemia with less side effects, and excellent safety, and therefore, it is useful for treating and/or preventing diseases or disorders on which citric acid cycle activation and/or improvement of hyperglycemia has a prophylactic and/or therapeutic effect, for example, diabetes, impaired glucose tolerance, insulin resistance, diabetic complications, obesity, dyslipidemia, hepatic steatosis, atherosclerosis and/or cardiovascular disease, as well as diseases or disorders that would benefit from stimulating energy expenditure.
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METHOD FOR PRODUCING OXAZOLE COMPOUND (Fri, 07 Mar 2014)
An object of the present invention is to provide a novel method for producing an oxazole compound. The invention relates to a method for producing a compound represented by formula (1): wherein R1 is lower alkyl group or halogen substituted lower alkyl group, R2 is lower alkyl group, R5 is lower alkyl group, R11 is lower alkyl group, halogen substituted lower alkyl group or a group represented by formula: -CY2COOR12, wherein Y is a halogen atom, R12 is an alkali metal atom or lower alkyl group, Ar1 is phenyl group substituted with lower alkyl group, etc., or pyridyl group substituted with lower alkyl group, etc., X2, X3 and X9 are the same or different and are halogen atoms, X4 is a leaving group, and M is an alkali metal atom.
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DIHYDRATE OF BENZOTHIOPHENE COMPOUND OR OF A SALT THEREOF, AND PROCESS FOR PRODUCING THE SAME (Fri, 01 Nov 2013)
An object of the present invention is to provide a compound that can be used as a more superior therapeutic agent for central nervous system diseases. The present invention provides a dihydrate of 7-[4-(4-benzo[b]thiophen-4-y1-piperazin-1-y1)butoxy]-1H-quinolin-2-one or of a salt thereof, and a process for producing the same.
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DECAHYDROQUINOXALINE DERIVATIVES AND ANALOGS THEREOF (Fri, 20 Sep 2013)
A heterocyclic compound represented by the general formula (1) or a salt thereof: wherein m, l, and n respectively represent an integer of 1 or 2; X represents -O- or -CH2-; R1 represents hydrogen, a lower alkyl group, a hydroxy-lower alkyl group, a protecting group, or a tri-lower alkylsilyloxy-lower alkyl group; R2 and R3, which are the same or different, each independently represent hydrogen or a lower alkyl group; or R2 and R3 are bonded to form a cyclo-C3-C8 alkyl group; and R4 represents an aromatic group or a heterocyclic group, wherein the aromatic or heterocyclic group may have one or more arbitrary substituent(s).
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PIPERAZINE- SUBSTITUTED BENZOTHIOPHENE DERIVATIVES AS ANTIPSYCHOTIC AGENTS (Fri, 15 Mar 2013)
Provided is a superior, novel heterocyclic compound with improved solubility in oil such as sesame oil and benzyl benzoate, which has a broader treatment spectrum, causes less side effects, and is superior in tolerability and safety, and use thereof. A heterocyclic compound represented by the formula (I) wherein each symbol is as defined in the specification, or a salt thereof.
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QUINOLONE COMPOUND (Fri, 08 Mar 2013)
The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile- associated diarrhea.
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COMBINATION DRUG OF ANTIBODY AGAINST LIPOPOLYSACCHARIDE OF PSEUDOMONAS AERUGINOSA AND ANTIBACTERIAL AGENT (Fri, 22 Feb 2013)
A problem was to provide a combination an antibody against lipopolysaccharide of P. aeruginosa and an antibacterial agent, having an excellent antibacterial activity against P. aeruginosa. To solve the problem, by using plasmablasts obtained from cystic fibrosis patients with chronic P. aeruginosa pulmonary infection as starting materials, antibodies which bind to LPS of P. aeruginosa strains of a wide range of serotypes and which have excellent antibacterial activities in vitro and in vivo were successfully obtained. Moreover, it is also found out that a combined use of the antibody and an antibacterial agent enhance an effect on a protective activity against P. aeruginosa infections.
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METHOD FOR PRODUCING BENZO[B]THIOPHENE COMPOUND (Fri, 01 Feb 2013)
The present invention provides a method for producing a compound of Formula (4): wherein R1 is a hydrogen atom etc. by reacting a compound of Formula (2): wherein X1 is a leaving group, with a compound of Formula (3): wherein R1 is as defined above, in the presence of (a) a palladium compound and a tertiary phosphine or (b) a palladium carbene complex, in an inert solvent or without a solvent. The present invention can produce the compound of Formula (4), with high purity and high yield, and by a simple operation.
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METHOD FOR PRODUCING FINE PARTICLES OF ARIPIPRAZOLE ANHYDRIDE CRYSTALS B (Fri, 04 Jan 2013)
The present invention provides a novel method for producing fine particles of aripiprazole anhydride crystals B. The method for producing fine particles of aripiprazole anhydride crystals B comprises the steps of: (1) heating and dissolving crude aripiprazole in a lower alcohol, and subsequently cooling the resulting mixture to precipitate crystals to obtain crystals of aripiprazole lower alcohol solvate; (2) subjecting the crystals of aripiprazole lower alcohol solvate to wet-milling in the form of a slurry containing the lower alcohol; and (3) subjecting the dispersion of the wet-milled crystals to solid-liquid separation to obtain the crystals, and heating the crystals.
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