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JP5525261B2 |
The present invention is concerned with novel tetrahydro-naphthalene-1-carboxylic acid derivatives having apoB secretion/MTP inhibiting activity and concomitant lipid lowering activity. The invention further relates to methods for prepar...
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JP5512202B2 |
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JP2014513145A |
The present invention relates to benzazepine derivatives of the formula (I) or a physiologically tolerated salt thereof. The present invention also relates to pharmaceutical compositions comprising such benzazepine derivatives, and the u...
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JP2014080395A |
To provide: compounds having voltage-dependent sodium channel Nav1.7 inhibitory action involved in acute pain, chronic pain, neuropathic pain, nociceptive pain including inflammatory pain, visceral pain and postoperative pain, cancer pai...
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JP5485346B2 |
The compounds of the present invention are represented by the following aryl- and heteroaryl-substituted tetrahydrobenzazepine and dihydrobenzazapine derivatives having formulae I(A-E) and formula (II): where the carbon atom designated *...
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JP5475813B2 |
Preparing ivabradine (I) comprises: reductive amination of aldehyde compound (VI) with N'-[[(8S)-3,4-dimethoxy-8-bicyclo[4.2.0]octa-1(6),2,4-trieny
l]methyl]-N'-methyl-propane-1,3-diamine (VII) in the presence of reducing agent to give (...
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JP5468900B2 |
The present invention relates to novel aniline derivatives and their use in therapy, in particular their use in the treatment of fungal infections.
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JP5442256B2 |
It is intended to obtain a new finding related to a mechanism of inducing differentiation of Th1/Th2/Th17 through dendritic cells, and to provide a pharmaceutical effective in an immunity-related disease by utilizing the finding, a scree...
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JP2014040476A |
To provide a method of manufacturing a chiral organic compound by an asymmetric contact with using an ionic catalyst containing a chiral catalytic anion.The method is suitable for performing reactions progressing through a cationic inter...
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JP2014037431A |
To provide a novel process for preparation of enantiomerically pure 7-amino-5H,7H-dibenzo [b,d]azepin-6-one.A process includes an optical resolution using chiral menthyl chloroformate of dibenzo [b,d]azepin-one derivative represented by ...
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JP5421311B2 |
The present invention provides processes and intermediates for the preparation of 3-benzazepines and salts thereof which can be useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disord...
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JP5415767B2 |
The present invention is based, in part, on our discovery that certain types of therapeutic agents can be used in combination to treat a variety of neuropsychiatric and related disorders, including addiction (e.g., to a substance or to a...
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JP5410996B2 |
Catalytic processes for preparing caprolactam, pipecolinic acid, and their derivatives, from lysine or alpha-amino-epsilon-caprolactam starting materials, and products produced thereby. A process for preparing caprolactam or a derivative...
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JP5404414B2 |
The present invention provides processes and intermediates for the preparation of (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine and salts thereof which are useful as serotonin-2C (5-HT2C) receptor agonists for the treatment o...
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JP5399383B2 |
A redox ammoximation process in which a ketone or aldehyde is reacted with ammonia and oxygen in the presence of a catalyst; wherein the catalyst is an aluminophosphate based redox catalyst having at least two different redox catalytic s...
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JP2014012684A |
To provide a method of rapidly and efficiently synthesizing positron emission tomography (PET) radiotracers including a radioisotope with a short half life used in the PET.One or more of the following steps are performed on a microfabric...
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JP5385299B2 |
The present invention is related to novel tricyclic compounds of formula (I) having TRPA1 receptor agonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their u...
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JP5385904B2 |
Compounds of formula (I), pharmaceutical compositions comprising them, and methods for their use are described.
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JP5379149B2 |
Provided is a method for producing a tetrafluoro nitrogen-containing heterocyclic compound such as tetrafluoropyrrolidine in good yield and at low cost. The method comprises the steps of: (A) reacting a compound represented by the formul...
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JP2013253102A |
To provide catalytic deamination for carprolactam production.There is provided: catalytic processes for preparing caprolactam, pipecolinic acid, and their derivatives, from lysine or alpha-amino-epsilon-caprolactam starting materials; an...
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JP5356687B2 |
The invention relates to the generation of a library of compounds enriched in agonist and antagonists for members of the G-protein coupled class of receptors (GPCRs). The library contains compounds of general formula (I) wherein y is any...
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JP5344523B2 |
According to the invention, a catalyst for a strecker reaction comprising a quaternary ammonium salt and a method for stereoselectively producing an a-aminonitrile derivative using the same are provided. By using the a-aminonitrile deriv...
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JP5345120B2 |
The present invention provides a method for separating an amide from an amino acid ionic liquid. The method includes the step of providing a polar solvent and an extracting agent to the amino acid ionic liquid, so as to separate the amid...
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JP5340269B2 |
The invention relates to a method of contacting a cyclic oxime with a Brønsted acidic ionic liquid having a sulfur atom in the anionic portion and/or the cationic portion further comprising mechanical stirring, microwave irradiation and...
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JP2013540719A |
The present disclosure relates to methods for weight management in an individual in need thereof by determining the level of renal sufficiency of the individual and prescribing or administering a therapeutically effective amount of (R)-8...
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JP2013539470A |
Salts of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine with optically active acids, and pharmaceutical compositions comprising them that are useful for, inter alia, weight management.
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JP5315299B2 |
The present invention relates to a compound which is 6-(3-cyclobutyl-2,3,4,5-tetrahydro-1 H -benzo[ d ]azepin-7-yloxy)- N -methyl-nicotinamide or a pharmaceutically acceptable salt thereof. This compound and its pharmaceutically acceptab...
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JP5312022B2 |
[PROBLEMS] To provide a novel compound having NMDA receptor channel blocking activity, and also a pharmaceutical agent comprising the compound. [MEANS FOR SOLVING PROBLEMS] A pharmaceutical agent for the treatment or prevention of a dise...
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JP5306387B2 |
Preparing ivabradine (I) comprises: subjecting N-{3-[((S)-3,4-dimethoxy-bicyclo[4.2.0]octa-1(6),2,4-trien-7
-ylmethyl)-methyl-amino]-propyl}-N-[2-(3,4-dimethoxy-phenyl)
-ethyl]-2-oxo-acetamide (VI) to the action of a thiol in an organic ...
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JP5306601B2 |
A compound represented by Formula 1 and an organic light emitting device including the same: where Ar is a substituted or unsubstituted C6-C26 aryl group; X is O, S, R1 and R2 are hydrogen, a halogen, a C1-C12 alkyl group, a C6-C26 aryl ...
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JP5302672B2 |
Lactams, in particular epsilon-caprolactam, are produced by the hydrolytic cyclization of aminonitriles, in particular 6-aminocapronitrile, in the vapor phase in a plurality of adiabatic fixed bed reaction zones arranged in succession wh...
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JP2013194012A |
To provide a method of producing lactam compounds and/or amide compounds in good yield.A lactone compound and ammonia or an amine compound are reacted with each other in the presence of a zeolite of an atomic ratio of silicon to aluminum...
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JP2013536859A |
Salts of the 5-HT2C-receptor agonist (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, and dosage forms comprising them that are useful for, inter alia, weight management.
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JP2013536858A |
Salts of the 5-HT2C-receptor agonist (R)-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine, and dosage forms comprising them that are useful for, inter alia, weight management.
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JP5296375B2 |
An optically active quaternary ammonium salt compound represented by formula (1), wherein R 1 represents a halogen, a C 1-8 alkyl which is optionally substituted and which is linear, branched, or cyclic, a C 2-8 alkenyl which is optional...
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JP5291623B2 |
Pyridine-piperazine-phenyl derivatives (I) or their enantiomers, diastereomers or salts, preferably salts with organic or inorganic acid or base, are new. Pyridin-piperazin-phenyl derivative (I) of formula (R 5>-A-R 4>-B 1>-R 3>-A-D-Y 1>...
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JP5295765B2 |
A process for preparing (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-car
boxamide or (R)-(-)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-car
boxamide, by reduction of oxcarbazepine in the presence of a catalyst and a hyd...
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JP5292432B2 |
A photoelectric conversion device comprising a transparent electrically conductive film, a photoelectric conversion film and an electrically conductive film in this order, wherein the photoelectric conversion film comprises a photoelectr...
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JP5292431B2 |
To provide a photoelectric conversion element that functions as a photoelectric conversion element and exhibits a low dark current when a compound having a specific structure is applied to the photoelectric conversion element, and that c...
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JP2013534819A |
Processes for producing caprolactam (CL) and derivatives thereof from adipic acid (AA) obtained from fermentation broths containing diammonium adipate (DAA) or monoammonium adipate (MAA).
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JP2013173764A |
To provide a process for asymmetric catalytic reduction of oxcarbazepine (10,11-dihydro-10-oxo-5H-dibenz/b,f/azepine-5-carboxamide).A
process for preparing (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-car
boxamide or (R)-(-)...
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JP5280252B2 |
A process for the preparation of 10,11-dihydro-10-oxo-5H-dibenz/b,f/azepine-5-carboxamide (2) from 10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide
(1), comprising oxidising 10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-c...
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JP5276579B2 |
Preparing ivabradine compounds (VI) comprises reacting 3,4-dimethoxy-bicyclo[4.2.0]octa-1,3,5-triene-7-carbaldehyde
(VII) with an amine (VIII) in the presence of a reducing agent. Preparing ivabradine compounds of formula (VI) comprises...
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JP5277130B2 |
Preparation of N-substituted tetrahydro-3-benzazepine derivatives (I) by catalytic hydrogenation of the corresponding dihydro compound (VI) at 40-80[deg]C, then filtering and crystallizing the product. Preparation of N-substituted 3-benz...
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JP2013533246A |
The invention relates to a method for preparing a lactam in a continuous process, comprising forming the lactam and ammonium sulphate by contacting a lactam sulphate contained in an acidic liquid with ammonia, during which forming of lac...
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JP5270167B2 |
The present invention is a process for preparing crystalline form of ( R )-8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride hemihydrate.
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JP5265913B2 |
The present invention relates to inhibitors of 11-² hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the ...
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JP5264704B2 |
A process for preparing an N-alkyllactam with improved color quality, wherein from 0.01 to 10% by weight of a C1-10-alcohol or a compound which releases from 0.01 to 10% by weight of a C1-10-alcohol is added to the N-alkyllactam. A mixtu...
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JP5264160B2 |
A compound comprising a substituent of the formula (II) is disclosed as an HIV protease inhibitor. Intermediates for making such compounds and processes for making such intermediates are also disclosed.
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JP2013151519A |
To provide new and improved drugs that target 11βHSD1 and/or MR.This invention relates to a compound represented by the following formula [I], wherein: Cy is aryl, heteroaryl, cycloalkyl or heterocycloalkyl, each optionally substituted ...
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