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| Number | Title | Issue Date |
| 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 preparing the same, and methods for facilitating the delivery of active a... | 09/27/2011 |
| 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 method of preparing (N-(5-chlorosalicyloyl)-8-aminocaprylic acid (5-C... | 09/06/2011 |
| 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 insulin, to a target. ... | 02/22/2011 |
| 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 for preparing such compounds. In another embodiment, the invention dis... | 10/19/2010 |
| 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 preparation of chirally pure nateglinide by treating a lower alkyl ester... | 08/03/2010 |
| 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. ... | 08/04/2009 |
| 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 solvent remains and making a crystal conversion thereof. According to t... | 06/09/2009 |
| 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 or... | 05/19/2009 |
| 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 preparation of other crystalline forms of nateglinide. Also provid... | 05/19/2009 |
| 7501538 | Aryl and heteroaryl compounds, compositions and methods of use This invention provides aryl and heteroaryl compounds of Formula (I) as described herein, and methods of their preparation. Also provided are pharmaceutical compositions made with the compounds of Formula (I) and methods for making such compositions. The compounds o... | 03/10/2009 |
| 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 humans and animals, in particular of cardiovascular disorders. ... | 03/03/2009 |
| 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 of administering and using the growth factor binding compounds or the ... | 01/27/2009 |
| 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 —(CH2)2— and Y is a lower alkyl group, or a pharmaceutically ... | 01/13/2009 |
| 7476759 | Matrix metalloproteinase inhibitors Compounds of Formula (I): wherein: R1 is optionally substituted —C4-12 alkyl, —C2-10alkylcycloalkyl, —C2-6alkylheterocycloalkyl, ... | 01/13/2009 |
| 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 hyperglycemia. Compounds of the inv... | 12/16/2008 |
| 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 selected from the group c... | 12/09/2008 |
| 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 being obtained by reacting trans-4-isopropylcyclohexylcarbonyl chloride ... | 12/02/2008 |
| 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 using the compositions in the treatment of various diseases. ... | 10/28/2008 |
| 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. ... | 10/21/2008 |
| 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 agents and methods for administering conjugated active agent compositions... | 09/23/2008 |
| 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 by the following formula (2) in an organic solvent selected from N-met... | 09/23/2008 |
| 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 ester or a salt thereof. ... | 09/16/2008 |
| 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, whether chronobiologic or light-induced, and in particular skin agei... | 09/02/2008 |
| 7420084 | Polymorphic forms of nateglinide Provides are crystalline forms of nateglinide, labeled Forms A, C, D, F, G, I, J, K, L, M, N, 0, P, Q, T, U, V, Y, α, β, γ, δ, ε, σ, θ and Ω, processes for their preparation and processes for preparation of other crystalline forms of nateglinide. Also provid... | 09/02/2008 |
| 7420085 | 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 insulin, to a target. ... | 09/02/2008 |
| 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 the treatment of hyperlipidemia... | 07/29/2008 |
| 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, the inventors have discovered that the disodium salts of these deliver... | 06/10/2008 |
| 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 an optical resolution by formation of diastereomer salts, and removi... | 06/10/2008 |
| 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 having a high degree of replication inhibitory activity against HCV,... | 05/27/2008 |
| 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 comprising hexafluoroleucine and congeners thereof. Certain peptides compri... | 05/13/2008 |
| 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 for preparation of other crystalline forms of nateglinide. Also provid... | 04/15/2008 |
| 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 R1 represents halo, a C1-4alkyl group which is optionally substituted by one or more fluoro, a C1-4alkoxy group which is optionally substituted by o... | 04/08/2008 |
| 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. ... | 04/01/2008 |
| 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; R1 represents halo, a C1-4alkyl group which is optionally substituted by one or more fluoro, a C1-4alkoxy group which is optionally substituted by one ... | 04/01/2008 |
| 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 duplexes of at least 20 base pairs that have significant binding activi... | 04/01/2008 |
| 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 volatile organic solvent under suitable reaction conditions to provide a sec... | 03/11/2008 |
| 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 stereoisomers thereof, which is useful in treating or preventing disorders mediat... | 01/22/2008 |
| 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. ... | 01/01/2008 |
| 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, R1, R2, R3 et R4 are indicated therein, which are cysteine protease inhibitors, including but not ... | 12/25/2007 |
| 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. ... | 12/11/2007 |