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7405307 |
Biphenylcarboxamides useful as lipid lowering agents
Biphenylcarboxamide compounds of formula (I)
methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for...
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7385080 |
Method for producing optically active β-phenylalanine compounds
Optically active β-phenylalanine compound may be prepared in an industrially advantageous manner by reacting an N-acyl-β-phenylalanine compound with a specific optically resolving agent to effect...
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7384982 |
Disodium salts, monohydrates, and ethanol solvates for delivering active agents
The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore,...
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7378446 |
Compound having anti-HCV activity and process for producing the same
The object of the present invention is to provide a compound useful for the prevention and treatment of viral infectious diseases, and particularly liver diseases caused by HCV infection due to its...
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7371867 |
Non-racemic trifluoroleucine, and methods of making and using
One aspect of the invention relates to hexafluoroleucine and congeners thereof, and methods of making the compounds. Another aspect of the invention relates to the synthesis of protein cores...
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7358390 |
Polymorphic forms of nateglinide
Provides are crystalline forms of nateglinide, labeled Forms A, C, D, F, G, I, J, K, L, M, N, O, P, Q, T, U, V, Y, α, β, γ, δ, ε, σ, θ and Ω, processes for their preparation and processes...
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7355069 |
Ortho-substituted benzoic acid derivatives for the treatment of insulin resistance
The present invention provides a compound of formula (I), wherein n is 0, 1 or 2 and R 1 represents halo, a C 1-4 alkyl group which is optionally substituted by one or more fluoro, a C 1-4 alkoxy...
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7351858 |
Ortho-substituted benzoic acid derivatives for the treatment of insulin resistance
The present invention provides a compound of formula (I), wherein n is 0, 1 or 2; R 1 represents halo, a C 1-4 alkyl group which is optionally substituted by one or more fluoro, a C 1-4 alkoxy...
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7351855 |
Chemically defined non-polymeric valency platform molecules and conjugates thereof
Chemically-defined, non-polymeric valency platform molecules and conjugates comprising chemically-defined valency platform molecules and biological or chemical molecules including polynucleotide...
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7351741 |
Compounds and compositions for delivering active agents
Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provide as well.
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7342126 |
Process for the preparation of 4-oxo-4-((4-(phenylamino)phenyl)amino)-2-butenoic acid
A process for the preparation of 4-oxo-4-((4-(phenylamino)phenyl)amino)-2-butenoic acid includes reacting p-aminodiphenyl amine and maleic anhydride in a reaction first mixture containing a...
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7321056 |
Selective peroxisome proliferator activated receptor modulators
The present invention is directed to a novel compound, its composition and use of a compound having a structural formula (I), or a pharmaceutically acceptable salt, solvate, hydrate or...
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7314955 |
Form of N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine
The present invention relates to a novel crystalline form of N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine and methods for preparing the same.
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7312353 |
Cathespin cysteine protease inhibitors
This invention relates to a novel class of compounds, represented by the formula below, wherein the meanings of G, E, E, n, R 1 , R 2 , R 3 et R 4 are indicated therein, which are cysteine...
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7307187 |
Process for converting primary amidoalcohols to amidocarboxylic acids in high yield
The invention relates to an improved process for oxidizing a primary amidoalcohol to the corresponding amidocarboxylic acid in high yield.
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7304167 |
Biphenylcarboxamides useful as lipid lowering agents
Biphenylcarboxamide compounds of formula (I)
methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for...
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7273951 |
Polyhydroxy phenols and their use in binding p-selectin
Polyhydroxy phenols, which are non-peptidic mimetics of galloyl peptides, and a process for the preparation of gallic acid derivatives using a gallic-acid providing moiety are provided as well as...
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7259276 |
Polyenecarboxylic acid derivatives, processes for preparing them, and their use
The present invention relates to novel compounds, termed serpentemycins, of the formula (I)
in which Y, R, R 2 , R 3 , R 4 , X, X 2 , X 3 , n, m and o are as defined in the specification, which...
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7250439 |
Matrix metalloproteinase inhibitors
Compounds of formula (I):
wherein:
Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents O, S, NR 5 or CR 6 R 7 ; Y represents CHOH, CHSH, NOR 8...
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7247746 |
Crystal forms of N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine
New crystal forms of N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine, also known asnateglinide, may be produced by dissolving nateglinide in any of its forms, including solvates, in an...
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7247736 |
Method of identifying inhibitors of DHODH
The present invention provides a compound capable of binding to the ubiquinone binding site of DHODH which contains a non-aromatic ring system as a core structure, a group capable of interacting...
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7238834 |
Piperidine derivatives and process for their production
The present invention relates to substantially pure piperidine derivative compounds of the formulae:
wherein
R 1 is hydrogen or hydroxy; R 2 is hydrogen; or R 1 and R 2 taken...
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7227033 |
Polymorphs of sodium 4-[(4-chloro-2-hydroxybenzoyl) amino] butanoate
The present invention relates to amorphous and polymorphic forms of sodium 4-[(4-chloro-2-hydroxybenzoyl)amino]butanoate and their use for facilitating the delivery of active agents, such as...
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7214712 |
Isophthalic acid derivatives as matrix metalloproteinase inhibitors
Selective MMP-13 inhibitors are isophthalic acid derivatives of the formula
wherein:
R 1 , R 2 , and R 3 independently are hydrogen, halo, hydroxy, C 1 –C 6 alkyl, C 1 –C 6 ...
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7208622 |
Methods for producing nateglinide crystals
There is provided methods for producing nateglinide crystals, which comprises the steps of adding an acid(s) to a reaction mixture containing nateglinide to make it acidic, the reaction mixture...
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7208178 |
Polymorphs of sodium 4-[(4-chloro-2-hydroxybenzoyl) amino] butanoate
The present invention relates to amorphous and polymorphic forms of sodium 4-[(4-chloro-2-hydroxybenzoyl)amino]butanoate and their use for facilitating the delivery of active agents, such as...
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7193108 |
Phenylpropionic acid derivatives
Specified phenylpropionic acid derivatives and analogues thereof have an antagonistic activity to α 4 integrin. They are used as therapeutic agents or preventive agents for various diseases...
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7183317 |
Compounds and methods to increase plasma HDL cholesterol levels and improve HDL functionality
It has been discovered that certain selected ethers of probucol, and their pharmaceutically acceptable salts or prodrugs, are useful for increasing circulating HDL cholesterol. These compounds may...
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7148376 |
Polymorphic forms of nateglinide
Provides are crystalline forms of nateglinide, labeled Forms A, C, D, F, G, I, J, K, L, M, N, O, P, Q, T, U, V, Y, α, β, γ, δ, ε, σ, θ and Ω, processes for their preparation and processes...
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7084176 |
N-arylphenylacetamide derivatives and medicinal compositions containing the same
N-Arylphenylacetamide derivatives represented by the following formula [I]:
(wherein R 1 is C 1-6 alkoxy, etc.; R 2 is hydrogen, —(CH 2 ) m —N(R 6 )(R 7 ) (m is an integer of from 1 to...
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7064229 |
Succinic acid derivatives
The present invention relates to compounds of the general formula (I), processes for their preparation, pharmaceutical compositions containing them as well as their use for the production of...
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7056707 |
Bioactive compound and its isolation and method of treatment for lipoxygenase inhibition and as free radical scavenging agent
The present invention relates to a novel compound having a molecular formula C 13 H 15 NO 5 having molecular structure of Formula I and a process for the isolation of said compound. The present...
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7049342 |
Substituted phenylpropionic acid derivatives
The invention provides novel substituted phenylpropionic acid derivatives that bind to the receptor as ligands of human peroxisome proliferator-activated receptor α (PPARα) to activate and...
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7045653 |
Pharmaceuticals
The invention relates to NEP inhibitors for treating cardiovascular disorders. Preferred NEP inhibitors are compounds of formula (I) wherein R 1 is C 1 –C 6 alkyl, C 1 –C 6 alkoxyC 1 –C 3...
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7030268 |
Methods for producing acylphenylalanine
There is provided a method for producing easily highly-purified acylphenylalanine that is useful as a raw material of pharmaceutical products and the like, which comprises the step of reacting an...
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7026501 |
Inhibitors of α4 mediated cell adhesion
The present invention relates to a phenylalanine derivative of Formula (I) wherein X 1 is a halogen atom, X 2 is a halogen atom, Q is a CH 2 R— is a carboxyl group which may be esterified; or a...
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6992207 |
Melphalan derivatives and their use as cancer chemotherapeutic drugs
The invention refers to new alkylating di- and tripeptides based on a melphalan unit, and one or two additional amino acids or amino acid derivatives, which can be used in the treatment of...
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6962899 |
Method for reducing the inflammation and inducing an analgesic effect and compounds thereof
Pharmaceutically acceptable compounds for administering to a subject, comprising the general structure II:
wherein R 1 is an L-amino acid or salt or ester thereof, or an L-amino acid...
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6939889 |
Quarternary ammonium compounds
Novel compounds and pharmaceutical compositions containing such compounds and possessing anti-tussive activity, and a method of administering the same to warm-blooded animals, including humans.
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6936597 |
Prodrugs of anticancer agents employing substituted aromatic acids
Polymeric prodrugs of the formula:
wherein
B is selected from the group consisting of OH, leaving groups, residues of amine-containing moieties and a residues of hydroxyl-containing...
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6930106 |
Inhibitors of HCV NS5B polymerase
The present invention provides compounds of Formula I, compositions and methods that are useful for treating viral infections and associated diseases, particularly HCV infections and associated...
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6903232 |
Process for the preparation of a highly pure pharmaceutical intermediate, 4-(cyclopropylcarbonyl)-α, α-dimethylphenylacetic acid
This invention relates to a novel process to obtain highly pure 4-(cyclopropylcarbonyl)-α,α-dimethylphenylacetic acid of Formula I through crystallization from a mixture of para and meta...
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6900344 |
Method of preparing alkylated salicylamides via a dicarboxylate intermediate
The present invention relates to a method of preparing an alkylated salicylamide from a protected and activated salicylamide via a dicarboxylated salicylamide intermediate. The present invention...
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6887877 |
Compounds and methods for the treatment or prevention of Flavivirus infections
The present invention provides novel compounds represented by formula I:
or pharmaceutically acceptable salts thereof useful for treating Flaviviridae viral infection.
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6861553 |
Process for preparing nateglinide and intermediates thereof
Provided is a process for preparation of an intermediate in the synthesis of nateglinide. Trans-4-isopropylcyclohexane acid chloride is formed by reacting 4-isopropylcyclohexanecarboxyl acid with...
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6849649 |
N-phenpropylcyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase
The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R 1 is optionally substituted C 1-6 alkyl, optionally substituted carbocyclyl, optionally...
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6849648 |
Phenylene alkyne matrix metalloproteinase inhibitors
A compound of Formula I
or a pharmaceutically acceptable salt thereof, or a tautomer thereof, wherein G 1 , G 2 , and B are as defined in the application, are selective inhibitors of...
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6831193 |
Trisubstituted-N-&lsqb (1S)-1,2,3,4-Tetrahydro-1-naphthalenyl&rsqb benzamides which inhibit P2X3 and P2X2/3 containing receptors
Compounds of formula (I) are novel P2X 3 and P2X 2 /P2X 3 antagonists which are useful in treating pain, urinary incontinence and bladder overactivity.
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6803383 |
Inhibition of angiogenesis and tumor growth
Compounds which inhibit tumor growth and angiogenesis, of general formula (II) are provided. These compounds include glycyl lysine derivatives bound to a central aromatic linking core.
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6770778 |
N-(4-substituted phenyl)-anthranilic acid hydroxamate esters
The present invention relates to oxygenated esters of 4-substituted-phenylamino benzhydroxamic acid derivatives, pharmaceutical compositions, and methods of use thereof.
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