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JP5801011B2 |
The problem to be solved is to provide a method for efficiently producing compounds (1) and (1a) that are important intermediate compounds in the production of FXa inhibitors (X) and (X-a). The solutions thereto are a method for producin...
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JP5779142B2 |
The invention is directed to the cross-metathesis and ring-closing metathesis reactions between geminal disubstituted olefins and terminal olefins, wherein the reaction employs a Ruthenium or Osmium metal carbene complex. Specifically, t...
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JP2015510509A |
Methods and intermediates useful for preparing compounds of formula I and salts thereof. In the formula, R1aAnd R1bAre independently amine protecting groups or R1aIs an amine protecting group, R1bIs H and R1cIs -C (O) O (C1~ C6) Alkyl an...
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JP2015500905A |
The present invention relates to modifications of polymeric materials containing reactive carbon-carbon unsaturateds and amines containing aziridine used for such modifications. Polymeric materials containing carbon-carbon bonds can be m...
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JP5555919B2 |
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JP5550880B2 |
The present invention provides an agent for the prophylactic or treatment of diabetes, diabetic complications, insulin resistance syndrome, metabolic syndrome, hyperglycemia, dyslipidemia, atherosclerosis, cardiac failure, cardiomyopathy...
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JP5475863B2 |
The present invention relates to an improved method for preparing dipeptidyl peptidase-IV inhibitor which is able to reduce preparations costs by using low cost reagents in the reaction steps and is able to be used in mass production by ...
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JP5368803B2 |
There is provided 5-(aziridin-1-yl)-4-hydroxylamino-2-nitrobenzamide for various uses, as well as pharmaceutical compositions and devices comprising 5-(aziridin-1-yl)-4-hydroxylamino-2-nitrobenzamide. There is also provided a method for ...
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JP5268912B2 |
Novel compounds are provided which are 11-beta-hydroxysteroid dehydrogenase type I inhibitors. 11-Beta-hydroxysteroid dehydrogenase type I inhibitors are useful in treating, preventing, or slowing the progression of diseases requiring 11...
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JP2013107844A |
To provide a method that synthesizes an optical activity aziridine compound through one step, using a compound that has not optical activity as a raw material compound.The manufacturing method of a compound of formula (3) comprises as fo...
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JP2013075272A |
To provide a catalyst for producing an aziridine compound, which has specific composition and a specific ratio of the acid strength amount thereof to the base strength amount, and to provide a technique for producing the aziridine compou...
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JP5188706B2 |
There is provided a polydiacetylene supramolecule comprising diacetylene molecules, capable of immobilizing a receptor molecule having a thiol group. Since the polydiacetylene supramolecule has a receptor immobilized thereon having a thi...
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JP5122275B2 |
The invention provides novel inhibitors of IAP that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: X1 and X2 are independently O or S; L is a bond or -C(X3)-, -C(X3)NR12, -C(X...
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JP5086513B2 |
N-Benzoyl arylsulfonamides having the formula (I) are BCL-Xl inhibitors and are useful for promoting apoptosis. Also disclosed are BCL-Xl inhibiting compositions and methods of promoting apoptosis in a mammal.
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JP2012529473A |
The invention relates to nitrogen-containing inorganic carrier materials, more particularly to inorganic carrier materials containing organically bonded nitrogen, to their preparation and also to their use for stabilizing iodine-containi...
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JP2012192337A |
To provide a catalyst that can effectively produce an aziridine while maintaining performance even under such reaction conditions that water vapor is contained in reaction gas in particular regarding the catalyst for producing the azirid...
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JP4954378B2 |
The invention provides a multistep synthesis for the preparation of 4,5-diamino shikimic acid derivatives of formula starting from furan. 4,5-Diamino shikimic acid derivatives are potent inhibitors of viral neuraminidase.
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JP4896350B2 |
The invention concerns diamines of general formula (I), wherein: A represents a group A1 or A2 of general formula (II); B represents a group B1 or B2 of general formula (III); X represents a SO2, CH2, C-O or COO; YZ represents a group of...
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JP4860865B2 |
Described are new 1-aziridino-1-hydroxyiminomethyl derivatives with the general formula (I), wherein R is able to is a single bond or a linker moiety capable of covalently bonding two aziridine oxime groups, R1 and R2 independently of on...
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JP2012006921A |
To provide a new high-yield and practical chemical synthetic method of oseltamivir phosphate, with which the oseltamivir phosphate is obtained from an easily available raw material compound with high optical purity.In the new chemical sy...
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JP2011224551A |
To enhance an aziridine production efficiency, by restraining catalyst activity from getting low caused by selection of a carrier and a firing temperature.This catalyst is a catalyst for producing the aziridine compound by a gas-phase in...
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JP4767399B2 |
There is provided a method of efficiently removing polymer stuck to the inside and/or on the surface of packings of a distillation tower, when nitrogen-containing polymerizable monomers (for example, ethyleneimine) are distilled. Said me...
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JP4760712B2 |
The present invention relates to novel nitrophenyl mustard and nitrophenylaziridine alcohols, to their corresponding phosphates, to their use as targeted cytotoxic agents; as bioreductive drugs in hypoxic tumours, and to their use in cel...
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JP4759129B2 |
In order to carry out various vapor-phase reactions (e.g., the preparation of aziridine compounds by a vapor-phase intramolecular dehydration reaction) with industrial advantages, there is provided a process which can effectively prevent...
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JP2011512412A |
This invention is directed to a 3-(amido or sulphamido)-4-(4-substituted-azinyl)benzamide or benzsulphonamide compound as defined herein. The 3-(amido or sulphamido)-(4-substituted-azinyl)benzamide or benzsulphonamide compound is useful ...
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JP4619545B2 |
The invention concerns amide derivatives of Formula (Ia) wherein X is -NHCO- or -CONH-; m is 0-3; R1 is a group such as hydroxy, halogeno, trifluoromethyl, cyano, mercapto, nitro, amino, carboxy and carbamoyl; n is 0-2; R2 is a group suc...
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JP4594386B2 |
The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, to the preparation of such compounds and pharmaceutical compositions containing them. The compounds are useful for the treatment and/...
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JP4575666B2 |
The present invention provides a process for producing an aziridine-1-carboxamide of the formula:from an aziridine of the formula:and an isocyanate of the formula R5-N=C=O, where R1, R2, R3, R4 and R5 are those defined herein. In additio...
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JP4564010B2 |
This invention provides a method for producing an optically active aziridine compound or amine compound, which uses as a catalyst a Ru(salen)(CO) complex represented by the following formula (I) or its enantiomer having a high stability,...
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JP2010209090A |
To provide an immediate release pharmaceutical formulation that contains a pharmaceutically acceptable diluent or carrier and is useful for treatment of cardiovascular diseases. The immediate release pharmaceutical formulation contains a...
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JP2010530864A |
Preparation of N-unsubstituted aziridine (II) or N-substituted aziridine (III) comprises reacting an olefin compound (I) with ammonia or a primary amine compound (IV), in the presence of iodine or bromine, where the concentration of (IV)...
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JP2010522140A |
The present invention relates to novel compounds suitable for or already radiolabelled with 18F, methods of making such compounds and use of such compounds for diagnostic imaging.
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JP4476483B2 |
The present invention relates to 12,13-position modified epothilone derivatives, methods of preparation of the derivatives and intermediates therefor.
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JP4422895B2 |
Novel compounds of Formula (I) are described. R1, R2, R3, R4, R5 and R6 are described in this specification. Synthetic intermediates and pharmaceutical compositions comprising the inhibitors of the invention are also described. Methods o...
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JP4402462B2 |
The present invention relates to a process for the preparation of perfluoroalkanesulfonic acid esters and to the further conversion thereof into salts, and to the use of the resultant compounds in electrolytes and in batteries, capacitor...
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JP4374658B2 |
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JP4353901B2 |
The present invention relates to a composition comprising at least one polyfunctional aziridine compound and 1,4-diazabicyclo[2.2.2]octane. The present invention furthermore relates to the use of this composition as a curing component fo...
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JP2009167210A |
To provide a new synthetic method and a composition and to provide a new method for preparing an intermediate useful in the synthesis of neuraminidase inhibitor and to provide a composition useful as an intermediate that is itself useful...
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JP4237224B2 |
The invention provides a multi-step process for preparing 1,2-diamino compounds of formula wherein R1, R1', R2, R2', R3 and R4 have the meaning given in the specification and pharmaceutically acceptable addition salts thereof, from 1,2-e...
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JP4234917B2 |
Novel compounds are described. The compounds generally comprise an acidic group, a basic group, a substituted amino or N-acyl and a group having an optionally hydroxylated alkane moiety. Pharmaceutical compositions comprising the inhibit...
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JP4213435B2 |
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JP4205559B2 |
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JP4204069B2 |
PCT No. PCT/EP97/04166 Sec. 371 Date Jan. 29, 1999 Sec. 102(e) Date Jan. 29, 1999 PCT Filed Jul. 29, 1997 PCT Pub. No. WO98/05659 PCT Pub. Date Feb. 12, 1998Compounds of formula (3), and pharmaceutically acceptable salts and derivatives ...
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JP2008545706A |
One aspect of the present invention relates to an asymmetric catalytic nitroaldol (Henry) reaction with a ketone, which is an electrophilic component. In one embodiment, the invention relates to an asymmetric nitroaldol reaction with an ...
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JP2008542415A |
The invention related to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Aliskiren. Inter alia, the invention relates to a pr...
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JP2008273841A |
To provide an intermediate useful for producing a benzylamine derivative, and a method for producing the intermediate.The method for producing an ethylenediamine derivative represented by formula (6) is characterized by reacting an aziri...
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JP2008273948A |
To provide inhibition of viruses (especially influenza virus), especially, inhibition of glycolytic enzymes such as neuraminidase, and, especially, viral or bacterial neuraminidase inhibitors, to provide a method for synthesizing the inh...
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JP2008266336A |
To improve energy balance and a yield upon production of an alkylene imine by allowing a sulfate monoester of an aminoalkanol to react with an aqueous base at a temperature of 110C or higher and under pressure, reducing the pressure of t...
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JP4177483B2 |
Sulphonamide derivatives of formula (I) and their stereoisomers and salts are new. R1 = Ar or Het; Ar = phenyl (optionally substituted by 1 or 2 alkyl, 3-6C cycloalkyl, OH, alkyl-COO-, alkyl-O-, alkyl-O-(1-4C alkylene)-O-, halo, CF3, CN,...
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JP4163254B2 |
PCT No. PCT/EP96/05874 Sec. 371 Date Dec. 4, 1998 Sec. 102(e) Date Dec. 4, 1998 PCT Filed Dec. 19, 1996 PCT Pub. No. WO97/25309 PCT Pub. Date Jul. 17, 1997Derivatives of mutiline of formula (1A) and pharmaceutically acceptable salts and ...
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