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JP4342178B2 |
Compounds of formula (I) are useful as inhibitors of trypsin like serine protease enzymes such as thrombin, factor VIIa, factor Xa, TF/FVIIa, and trypsin. These compounds could be useful to treat and/or prevent clotting disorders, and as...
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JP2009221232A |
To provide useful compounds for treatments of various metabolic disturbances (for example, insulin resistant syndromes, diabetes mellitus, hyperlipidemia, fatty liver diseases, cachexia, obesity, atherosclerosis and arterial sclerosis).B...
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JP4324324B2 |
2(R or S)-[2R-(S-Hydroxy-hydroxycarbamoyl-methyl)-4-methyl-pentanoy
laminel]-2 -phenyl-ethanoic acid cyclopenty ester' 2(R or S)-(3S-Hydroxycarbamoyl-2R-isobutyl-hex-5-enoylamino)-2-phen
ylethanoic acid isopropyl ester; 2(R or S)-[2R-(S-...
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JP4320260B2 |
Arylamide derivatives (I) are new. Arylamide derivatives of formula (I) and their salts are new. [Image] X : optionally substituted lower alkylene or alkenylene; G 1O, S or NH; G 2C or N; R aH, halo or optionally substituted alkyl, cyclo...
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JP2009521424A |
The present invention relates to compositions and methods to selectively treat fungal infection. More particularly, this invention relates to compositions and methods for selectively enhancing fungal sensitivity to antifungal compounds.
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JP4271657B2 |
The invention is concerned with novel mandelic acid derivatives of formula (I) wherein R1 to R10, X and Y are as defined in the description and in the claims, as well as pharmaceutically acceptable salts thereof. These compounds inhibit ...
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JP4270522B2 |
Boron compound complexing reagents and methods of synthesizing these reagents are disclosed. These reagents, including those shown as General Formula (I) and General Formula (II) may be used, after further reactions described herein, to ...
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JP2009520695A |
Described herein are N-hydroxyamide antibacterial compounds, methods for making the compounds, pharmaceutical compositions containing the compounds and methods of treating bacterial infections utilizing the compounds and pharmaceutical c...
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JP2009108048A |
To provide a new hydroxylamine derivative falling within the scope of formula (I) or (II) for increasing expression of a molecular chaperon by a cell and/or enhancing the activity of a molecular chaperon in cells as well as a pharmaceuti...
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JP4266638B2 |
Novel PDF inhibitors and novel methods for their use are provided.
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JP4266815B2 |
Novel PDF inhibitors and novel methods for their use are provided.
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JP2009096717A |
To obtain a new compound that reduces an amount of an IAP family protein in cells and inhibits IAP family activity, to provide a method for producing the same and to obtain an IAP inhibitor or apoptosis inducer or enhancer comprising the...
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JP4257205B2 |
There are described derivatives of benzoylcyclohexanediones of the formula (I) and their use as herbicides.In this formula (I), R<1a>, R<1b>, R<1c>, R<2>, R<3>, R<4 >and R<5 >are various radicals, X<1 >is a bridging atom, X<2 >a carbon c...
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JP2009513697A |
This invention discloses a novel alkylcarbamoyl naphthalenyloxy octenoylhydroxyamide derivative of formula (1) useful for inhibiting the enzyme activity of histone deacetylase, which leads to effective suppression of the cancer cell prol...
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JP4243628B2 |
The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associ...
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JP4238334B2 |
Compounds of formula I are disclosedwherein R4 is an ester or thioester group, and R, R1, R2, and R3 are as defined in the specification are inhibitors of rapidly dividing tumor cells.
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JP4223003B2 |
This invention relates to N-acylamino aryl derivatives of the formula where R1, R21, R22, R23, R24, R3, R4, R5, R6, R7, R8, R, and n are as defined herein and where X is -CHRO, -OCHR-, -CH2S-, -SCH2-, -CH2CH2-, -CH-CH- or -C≡C-. The co...
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JP4220377B2 |
PDF inhibitors and novel methods for their use are provided.
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JP4208174B2 |
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JP2009500350A |
Novel amino acid derivatives are provided that are useful for management of disorders such as obesity and immunological diseases. The derivatives are also useful in lowering blood glucose levels in hyperglycemic disorders and for treatin...
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JP2009500343A |
Novel hydroxamic acid containing amino acid derivatives are provided that are useful for treatment of inflammation, inflammatory and immunological diseases; lowering blood glucose, serum insulin, free fatty acids, cholesterol and triglyc...
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JP4201716B2 |
This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bo...
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JP4197818B2 |
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JP4195377B2 |
Compounds of formula I wherein A, R<1 >and R<2 >are defined in the specification. These compounds are useful as HDAC inhibitors. Also disclosed are methods of making and using said compounds.
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JP2008542196A |
Covalent conjugation of an alpha amino acid ester to a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by intracellular carboxylesterase enzyme hCE1 and not...
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JP4183813B2 |
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JP4184435B2 |
Inhibitors of oleamide hydrolase, responsible for the hydrolysis of an endogenous sleep-inducing lipid (1, cis-9-octadecenamide) were designed and synthesized. The most potent inhibitors possess an electrophilic carbonyl group capable of...
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JP2008539227A |
The present invention provides hydroxamic acid derivatives represented by the formula, having antioxidation, collagen biosynthesis promotion and skin pore contraction effects, and a method for preparation thereof. Further, the present in...
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JP4176153B2 |
This invention is directed to polymeric hydroxylamine resin compounds and to processes for the solid-phase synthesis of aldehydes, ketones, oximes, amines and hydroxamic acid compounds useful thereof.
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JP2004509099A5 |
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JP2008253987A |
To provide a technique for manufacturing an optically active -amino acid derivative, which does not require external addition of a base.A catalyst for producing the optically active -amino acid derivative has M(OR1)2 (M represents an alk...
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JP2008201783A |
To provide a class of chemical compounds useful as efficacious drugs in the treatment of sickle cell disease and diseases characterized by unwanted or abnormal cell proliferation.The active compounds are substituted triaryl methane compo...
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JP4142453B2 |
Compounds of formula Iwherein R1, R2, A, X, Y and Z have the meanings provided in the specification, and their enantiomers, diastereoisomers, racemates, pharmaceutically acceptable salts and mixtures thereof. These compounds have HDAC in...
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JP2008531525A |
The invention relates to novel compounds with formula (I) and their use in stabilization of Factor VIIa or other Factor VII polypeptides, particularly in aqueous liquid compositions thereof.
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JP2008531535A |
A process for preparing a protected amidine group of formula (I): wherein R6 represents, for example, C1-10 alkyl (optionally substituted), aryl, C1-3 alkylaryl or C1-3 alkyloxyaryl; which comprises reacting a nitrile containing compound...
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JP4131698B2 |
The present invention provides a novel carboxylic acid compound, a salt thereof or a hydrate of them useful as an insulin sensitizer, and a medicament comprising the compound as an active ingredient. That is, the present invention provid...
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JP2008529962A |
Compounds of formula wherein A 0 , A 1 and A 2 are each independently of the others a bond or a C 1 -C 6 alkylene bridge; A 3 is a C 1 -C 6 alkylene bridge which is unsubstituted or substituted by from one to six identical or different s...
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JP4129993B2 |
Novel compounds are provided which are inhibitors of MTP and thus are useful for lowering serum lipids and treating atherosclerosis and related diseases, and have the structure (I) or (IA) or (IB) including pharmaceutically acceptable sa...
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JP4125868B2 |
Novel compounds represented by general formula (I) which do not act on normal cells but detransform specifically cells transformed by various oncogenes, salts thereof, or hydrates of the same, wherein G1 represents OR<1> or NR<2>R<3> (wh...
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JP4125912B2 |
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JP4120401B2 |
A hydroxyformamidine compound represented by the following formula or a pharmaceutically acceptable salt thereof. Äwherein R<1> represents a substituted morpholino group, a substituted piperidino group, a piperazin-1-yl group, a substit...
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JP4107687B2 |
The compounds according to the invention are substituted N-[(aminoiminomethyl or aminomethyl)phenyl]propyl amides of formula I herein which exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical comp...
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JP4106337B2 |
Amino acid amide compounds (I), are new. Amino acid amide compounds of formula (I), their optical isomers and acid addition salts are new. R1 = aryl, heteroaryl, 1-6C alkyl (optionally substituted by at least one aryl or heteroaryl), or ...
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JP4108127B2 |
Amide compounds of formula (I) are new. R' = H or 1-4C alkyl; A = adamantyl or a mono-, bi-or tri-cyclic radial optionally partially or totally unsaturated, which can contain one or more heteroatoms selected from N,S and O and optionally...
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JP2008518957A |
The present invention relates to niacin receptor agonists of formula: (I); as well as pharmaceutically acceptable salts and solvates. The compounds are useful for treating dyslipidemias, and in particular, reducing serum LDL, VLDL and tr...
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JP4096878B2 |
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JP2008518035A |
The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms...
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JP4090070B2 |
An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases. The ...
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JP4091431B2 |
The present invention provides compounds of formula I and pharmaceutically acceptable salts, wherein R1, R2, R3, R4, R5, X and Y have the meanings defined in the specification. The compounds have histone deacetylase (HDAC) inhibitory act...
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JP2008512364A |
The invention is concerned with novel 4-aminomethyl benzamidine derivatives of formula (I) wherein Ar and X are as defined in the description and in the claims, as well as prodrugs and pharmaceutically acceptable salts thereof These comp...
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