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JP5544358B2 |
The invention relates to bicyclic heterocycles of formulae I and II with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for ...
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JP5498524B2 |
Processes and intermediates for the preparation of compounds of the Formula I and the pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, wherein R1, R2, and R3 have the definitions provided herein.
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JP5490481B2 |
Compounds having formula (I) or a pharmaceutically acceptable salt thereof wherein R1 is (a) hydrogen, (b) loweralkyl, (c) alkenyl, (d) alkoxy, (e) thioalkoxy, (f) halo, (g) haloalkyl, (h) aryl-L2-, and (i) heterocyclic -L2-; R2 is selec...
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JP5466759B2 |
The present invention provides a compound of formula I'; or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , X and n are defined herein. The invention also relates to a method for manufacturing the compounds of the i...
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JP5455916B2 |
The present application provides a process for continuously producing 3-isothiazolinone derivatives and intermediate products thereof, comprising continuously carrying out four steps, i.e ., sulfuration, purification, amination and chlor...
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JP5444077B2 |
An object of the present invention is to provide a compound represented by Formula (1): wherein A 1 , A 2 , A 3 and A 4 each represent a carbon atom, a nitrogen atom or an oxidized nitrogen atom; R 1 and R 2 each represent a hydrogen ato...
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JP5430881B2 |
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JP5428274B2 |
To provide a nonaqueous electrolyte providing excellent battery characteristics such as storage characteristics of a primary battery, and high-temperature cycling characteristics when a secondary battery is used at a high voltage, and to...
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JP5420761B2 |
The present invention provides a compound of formula I'; or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 5 , B 1 , X and n are defined herein. The invention also relates a method for manufacturing the compounds...
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JP2014503528A |
The invention relates to pharmaceutical compositions comprising casein kinase 1 delta (CK1´) inhibitors and to the use of said inhibitors in the treatment of neurodegenerative disorders such as Alzheimer's disease.
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JP2014501705A |
The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making su...
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JP5392917B2 |
This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R 1 is optionally substituted lower alkyl, Y is -S(O)n- wherein n is 1 or 2, or -CO-, R 2 is hydrogen or lower alkyl, R...
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JP5390384B2 |
A method for reducing irritation caused by an isothiazolone compound represented by formula (1) by converting the isothiazolone compound represented by formula (1) into a zinc salt.
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JP5364875B2 |
Compounds that inhibit Aurora-kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed.
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JP2013542201A |
A compound of Formula I is set forth, including pharmaceutically acceptable salts thereof: wherein Het is a 5 or 6-membered heterocycle with —N, —O, or —S adjacent to the —Ar substituent or adjacent to the point of attachment for...
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JP5344923B2 |
The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/o...
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JP5340745B2 |
Compounds of formula I processes for their preparation, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
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JP5336461B2 |
Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.
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JP5327794B2 |
To provide an industrially advantageous method for safely producing a 1,2-benzoisothiazolin-3-one compound of a useful compound as an industrial antimicrobial agent or the like without using a harmful reagent in good yield. The method fo...
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JP5314037B2 |
The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal plasma uric acid level and the like. The present invention relates to fused ring derivatives represented by t...
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JP5311072B2 |
Heterocyclic amine derivatives represented by general formula (I): wherein R<1>, R<2> and R<3> represent each H, optionally halogenated C3-6 cycloalkyl, etc.; Q represents an optionally substituted heterocycle containing O, S or N; X rep...
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JP5291994B2 |
To provide an active ingredient expressing excellent controlling effects to harmful microorganisms such as bacteria, fungi, yeasts, algae, etc., and an industrial bactericidal composition containing the same. This industrial bactericidal...
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JP5289308B2 |
The present invention provides a compound represented by the formula wherein R 1 is a hydrocarbon group optionally having substituent(s), amino optionally having substituent(s), hydroxy optionally having a substituent or a heterocyclic g...
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JP2013532643A |
The present invention relates to hetaryl (thio)carboxamide compounds of formula I, to the tautomers and N-oxides thereof and to the salts thereof: wherein X, R1 and A are as defined in the description. The present invention further relat...
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JP5248327B2 |
A compound represented by the following formula (1): (wherein the carbon atom denoted by * is in the R-configuration; R 1 and R 2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino gr...
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JP5218788B2 |
A retroviral protease inhibiting compound of formula (A) is disclosed for use in combination with other active pharmaceutical agents for treating a human infected by HIV. Intermediates and processes useful in the manufacture of compounds...
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JP2013519716A |
The invention relates to compounds of formula (I), useful for treating disorders mediated by the 5-hydroxytryptamine (serotonin) receptor IB (5-HT1B), e.g. vascular disorders, cancer and CNS disorders. The invention also provides methods...
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JP5175052B2 |
Soluble polymers and methods for the preparation thereof, wherein the polymers of the present invention have pendant acylsulfonamide amine-reactive groups that can be used for the capture of amine containing materials.
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JP2013056894A |
To provide novel anthranilamide and 2-amino-heteroarene carboxamide derivatives useful as cholesteryl ester transfer protein (CETP) inhibitors; methods for producing the same; use thereof as pharmaceuticals; and pharmaceutical compositio...
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JP5173193B2 |
Compounds having two reactive functional groups are described that can be used to provide a connector group between a substrate and an amine-containing material. The first reactive functional group can be used to provide attachment to a ...
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JP5173126B2 |
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JP5166269B2 |
Crosslinked polymeric materials are described that contain pendant amine capture groups. The amine capture groups include N-sulfonylaminocarbonyl groups that can react with amine-containing materials by a nucleophilic displacement reacti...
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JP5159623B2 |
3,4-Dichloro-N-(2-cyanophenyl)-5-isothiazole-carboxamide (I) is prepared by (a) reacting 3,4-isothiazole-5-carbonyl chloride (II) with anthanilamide (III) and (b) dehydrating the obtained amide (IV), where (i) at least step (a) is carrie...
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JP2013043882A |
To obtain a 1,2-benzisothiazolin-3-one compound from a reaction liquid obtained by making a 2-(alkylthio)benzonitrile compound and a halogenating agent react with each other in the presence of water, with high purity and with a high yiel...
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JP2013040240A |
To provide an azo compound and an azo pigment that excel in solidity such as light resistance and heat resistance, and that can express excellent dispersion stability when being contained in liquid, and to provide a pigment dispersion, a...
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JP5112315B2 |
[Task] The present invention is to provide a 3,4-dihalogenoisothiazole derivative or a salt thereof which is not harmful to a crop and is remarkably effective on an agricultural or horticultural plant disease such as rice blast disease, ...
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JP5108878B2 |
This application relates to a substituted carboxamide compound of formula I, or a pharmaceutically acceptable salt thereof, as defined herein, a pharmaceutical composition thereof, and its use in treating pain.
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JP5100390B2 |
Processes and intermediates for the preparation of compounds of the Formula I and the pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, wherein R1, R2, and R3 have the definitions provided herein.
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JP5089581B2 |
[Task] The present invention is to provide a 1,2-benzoisothiazole derivative or a salt thereof which is not harmful to a crop and is remarkably effective on an agricultural or horticultural plant disease such as Pyricularia oryzae, Septo...
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JP5084839B2 |
Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is a group of formula A or formula B, and X, R2, R3, R4, R5, R6, Ra and Rb are as defined herein. Also provided are methods of using the compounds for...
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JP5075554B2 |
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JP5078337B2 |
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JP2012214427A |
To provide a method for producing an aqueous composition containing 1,2-benzisothiazolin-3-one simply and economically which does not require removal by such as filtration of insoluble by-products.The method for producing an aqueous comp...
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JP2012214405A |
To provide a novel N,N'-methylenebis(1,2-benzisothiazolin-3-one) compound having a 1,2-benzisothiazolin-3-one frame and being useful as antibiotics, antifungal agents and the like.The N,N'-methylenebis(1,2-benzisothiazolin-3-one) compoun...
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JP5064503B2 |
The present invention relates to compounds of formula I wherein R1, R2, R3, R4, R5, X, and n are as defined herein and the dotted line denotes an optional bond and pharmaceutically acceptable acid addition salts thereof. The compounds ar...
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JPWO2010122968A1 |
To provide a compound useful as an anti-obesity drug. The present inventors have investigated a compound having a DGAT1 inhibitory action, which is promising as an active ingredient of a pharmaceutical composition for treating obesity, t...
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JP5048017B2 |
A compound represented by the formula (I) or a salt thereof wherein n represents an integer of 1 to 3, R represents an alkyl group having 3 to 8 carbon atoms, a group represented by the following formula: R<1>(CH2)k- (wherein k represent...
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JP5052531B2 |
The present invention relates to N-cycloalkyl-benzyl-amide derivatives of formula (I) wherein the substituents are as in the description, their process of preparation, their use as fungicide active agents, particularly in the form of fun...
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JP5053459B2 |
The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing su...
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JP5047801B2 |
The present invention relates to compounds of formula (I): in which R 1 , R 2 , R 3 , X, Y and A are as defined in the specification. The compounds are modulators of the estrogen receptors.
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