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8076374 |
Glucagon receptor antagonists, preparation and therapeutic uses
The present invention discloses novel compounds of Formula (I), or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods...
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8026392 |
Crystalline forms of the di-sodium salt of N-(5-Chlorosalicyloyl)-8-aminocaprylic acid
The present invention relates to crystalline polymorphic forms of the di-sodium salt of N-(5-chlorosalicyloyl)-8-aminocaprylic acid, pharmaceutical compositions containing the same, methods of...
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8013184 |
Manufacture process of organic compounds
The present invention relates to a method of preparing N-substituted salicylamides or derivatives thereof and their derivatives, e.g. their salts. In particular, the present invention relates to a...
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8003819 |
Proteasome inhibitors
The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of...
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8003697 |
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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7998933 |
Process for treating the skin comprising applying to the skin at least one composition comprising at least one N-aminoacylamide
The invention concerns novel compounds of the N-acylamino-amide family, compositions, in particular cosmetic or pharmaceutical, containing them, and their use for treating body or face skin ageing,...
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7977506 |
Compounds and compositions for delivering active agents
Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.
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7939666 |
Enzyme inhibitors
Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers.
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7915314 |
***WITHDRAWN PATENT AS PER THE LATEST USPTO WITHDRAWN LIST*** 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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7893297 |
Amorphous 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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7863329 |
Glucagon receptor antagonists, preparation and therapeutic uses
The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods...
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7858665 |
Drugs for chronic pain
The present invention relates to nitrooxyderivatives or salts thereof having the following general formula (I): R—NR1c—(K)k0—(B)b0—(C)c0—NO2 (I) wherein c0, b0 and k0 are 0 or 1; R is the radical o...
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7816557 |
Glucagon receptor antagonists, preparation and therapeutic uses
The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods...
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7790770 |
Heterocyclic CETP inhibitors
Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.
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7781470 |
Aminodicarboxylic acid derivatives having pharmaceutical properties
The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, wherein the several variable groups are as defined in the specification and claims. Processes for making these...
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7767847 |
Process for the preparation of chirally pure N-(trans-4-is)
The invention relates to N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine (nateglinide) in the novel crystalline form “G” and a process for the preparation thereof. A process for the pre...
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7754897 |
Synthetic processes for the preparation of aminocyclohexyl ether compounds
This invention is directed to stereoselective synthesis of compounds of formula (I) or formula (II): or a pharmaceutically acceptable salt, ester, amide, complex, chelate, clathrate, solvate,...
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7750181 |
Antiproliferative agents
This invention relates to certain dioxodihydropyridine derivatives and certain methacrylic acid and furan derivative precursors thereof, processes for their preparation, pharmaceutical compositions...
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7745489 |
Compositions and methods for inhibition of phospholipase A2 mediated inflammation
Specific, highly potent 2-oxo-amide based inhibitors of phospholipase A2 (PLA2) activity are provided. A role for PLA2 activity in spinally mediated inflammatory processes is established, and a...
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7732492 |
Nateglinide-containing preparation
The present invention provides a small-sized preparation that is easy to take, containing 26% or more of nateglinide and 28% or more of at least one disintegrant selected from the group consisting...
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7696248 |
Glucagon receptor antagonists, preparation and therapeutic uses
The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods...
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7671090 |
Inhibitors of α4 mediated cell adhesion
The present invention relates to a phenylalanine derivative of Formula (I) wherein X1 is a halogen atom, X2 is a halogen atom, Q is a CH2R— is a carboxyl group which may be esterified; or a p...
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7662994 |
Method for the preparation of crystalline dexloxiglumide and products obtained
The present invention describes a novel method for the purification of dexloxiglumide by crystallization from isopropyl ether which permits the production, in a reproducible manner, of a product...
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7642289 |
Drugs for chronic pain
The present invention relates to nitrooxyderivatives or salts thereof having the following general formula (I): R—NR1c—(K)k0—(B)b0—(C)c0—NO2 (I) wherein c0, b0 and k0 are 0 or 1;R is the radical o...
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7605180 |
Nateglinide-containing preparation
The present invention discloses, as a immediate-release preparation useful as an antidiabetic, a nateglinide-containing preparation comprising nateglinide as an active ingredient wherein the...
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7569723 |
Benzoic acid derivatives as non nucleoside reverse-transcriptase inhibitors
Compounds of formula (I): wherein R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds are useful as reverse transcriptase inhibitors against HIV. In particular, the compounds are active...
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7553873 |
Glutamate aggrecanase inhibitors
The present invention relates to modulators of metalloproteinase activity.
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7544834 |
Methods for producing nateglinide B-type crystals
A method for producing B-type crystals of nateglinide substantially free of H-type crystals is provided, which comprises drying solvated wet crystals of nateglinide at a low temperature until no...
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7541485 |
Methods for preparing glutamic acid derivatives
The present invention relates to novel methods for the preparation of glutamic acid derivatives and intermediates thereof, and such compounds prepared by the novel methods.
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7534913 |
Crystalline form of nateglinide
Provided 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 for pre...
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7534914 |
Substituted methyl aryl or heteroaryl amide compounds
This invention provides a compound of the formula (I): wherein X represents a carbon atom or the like: Y represents imino, or the like: R1 represents an alkyl group having from 1 to 6 carbon atoms...
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7517896 |
Aminodicarboxylic acid derivatives having pharmaceutical properties
The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, wherein the several variable groups are as defined in the specification and claims. Processes for making these...
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7498460 |
Isophthalic acid derivatives
The present invention relates to isophthalic acid derivatives, to a process for their preparation and to their use for producing medicaments for the treatment and/or prophylaxis of diseases in...
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7495030 |
(5-(2-hydroxy-4-chlorobenzoyl) aminovaleric acid and salts thereof and compositions containing the same for delivering active agents
(5-(2-hydroxy-4-chlorobenzoyl) aminovaleric acid, salts thereof, and compositions containing the same for the delivery of active agents are provided. Methods of administration, treatment of disease...
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7482483 |
Growth factor-binding compounds and methods of use
Growth factor binding compounds having a plurality of acyclic isophthalic acid groups attached to a non-peptide organic scaffold and pharmaceutical compositions of the same are disclosed. Methods...
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7476759 |
Matrix metalloproteinase inhibitors
Compounds of Formula (I): wherein:R1 is optionally substituted —C4-12 alkyl, —C2-10alkylcycloalkyl, —C2-6alkylheterocycloalkyl, —C2-6alkylaryl, optionally substituted 5- or 6-membered aryl or hete...
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7476758 |
Process for preparing a phenylalanine derivative and intermediates thereof
The present invention provides a process for preparing a novel phenylalanine derivative of the formula (I): wherein X1 is a halogen atom, X2 is a halogen atom, Q is a group of the formula —CH2— or ...
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7465825 |
Phenyl substituted carboxylic acids
Disclosed are compounds and pharmaceutically acceptable salts of formula (A): which are useful in the treatment of metabolic disorders related to insulin resistance, leptin resistance, or...
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7462735 |
Amino acid diamides in non α position which are useful as adjuvants for administration of biological active agents
Amino acid diamides in non α position of formula (1), wherein R1 is selected from amongst the group consisting of the functional groups alkyl, halogen, NO2, OH, OCH3 alone or associated and R2 is ...
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7462644 |
Therapeutic agents
The present invention provides the S enantiomer of a compound of formula I wherein R1 represents chloro, trifluoromethyl or trifluoromethoxy, R2 represents H or fluoro and R3 represents a C2-4alkyl...
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7459582 |
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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7456217 |
Inhibitors of alpha4 mediated cell adhesion
The present invention relates to a phenylalanine derivative of Formula (I) wherein X1 is a halogen atom, X2 is a halogen atom, Q is a CH2R— is a carboxyl group which may be esterified; or a p...
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7442830 |
Proteasome inhibitors
The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of...
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7439388 |
Process for converting primary amidoalcohols to amidocarboxylic acids in high yield using water as solvent
The invention relates to an improved process for oxidizing a primary amidoalcohol to the corresponding amidocarboxylic acid in high yield.
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7427688 |
Production method of optically active diphenylalanine compounds
The present invention provides a production method including reacting a diphenylmethylene halide compound represented by the following formula (1) with a malonic acid diester compound represented...
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7427600 |
Active agent delivery systems and methods for protecting and administering active agents
The present invention relates to active agent delivery systems and more specifically to compositions that comprise amino acids, as single amino acids or peptides, covalently attached to active...
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7425648 |
Process for the preparation of nateglinide, preferably in B-form
The present invention relates to a process for the preparation of nateglinide, preferably in B-form, substantially free from the H-form, comprising three steps starting from D-phenylalanine methyl...
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7419970 |
Cosmetic compositions comprising N-acylamino amides
The invention concerns novel compounds of the N-acylamino-amide family, compositions, in particular cosmetic or pharmaceutical, containing them, and their use for treating body or face skin ageing,...
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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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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 a...
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