Abstract: The present invention relates to novel compounds, termed serpentemycins, of the formula (I) in which Y, R, R2, R3, R4, X, X2, X3, n, m and o are as defined in the specification, which are formed by the microorganism Actinomycetales sp. DSM 14865 during its fermentation, to chemical derivatives of the serpentemycins, to a process for preparing them, and to their use as pharmaceuticals, in particular for the treatment and prophylaxis of infectious bacterial diseases.

Abstract: Compounds of formula (I): wherein: Q represents an optionally substituted 5- or 6-membered aryl or heteroaryl ring; X represents O, S, NR5 or CR6 R7; Y represents CHOH, CHSH, NOR8, CNR8 or CNOR8; Z represents a bond, CR10R11, O, S, SO, SO2, NR10, OCR10R11, CR10R11 O or Z, R4 and Q together form an optionally substituted fused tricyclic group; R1, R1?, R3 and R3? each independently represents H, C1-6 alkyl or C1-4 alkylaryl; R2 represents CO2R8, CONR5OR9 or NR5COR9; R4 represents optionally substituted 5- or 6-membered aryl or heteroaryl; R5 represents H or C1-3 alkyl; R6 and R7 each independently represents H, C1-3 alkyl or halo; R8 represents H or C1-2 alkyl; R9 represents H or C1-3 alkyl; R10 and R11 each independently represents H, C1-6 alkyl or C1-4 alkylaryl; and physiologically functional derivatives thereof, processes for their preparation, pharmaceutical formulations containing them and their use as inhibitors of matrix metalloproteinase enzymes (MMPs) are described.

Abstract: 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 organic solvent to form a solution followed by precipitation of nateglinide from the solution, and isolating and drying the precipitated crystal form of nateglinide. The precipitation of nateglinide may be induced either by cooling the solution, or by addition of another solvent which is miscible with the first solvent but in which nateglinide is only poorly soluble, or by combination of the two. Depending on the solvent a specific crystal form of nateglinide may be obtained, e.g., the R?-type crystal form of nateglinide produced by the described method has a different melting point, infra red spectra and X-ray diffraction patterns from the previously known crystal forms of nateglinide.

Abstract: The present invention relates to substantially pure piperidine derivative compounds of the formulae: wherein R1 is hydrogen or hydroxy; R2 is hydrogen; or R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; R3 is —COOH or —COOR4; R4 has 1 to 6 carbon atoms; A, B, and D are the substituents of their respective rings each of which may be different or the same and are hydrogen, halogens, alkyl, hydroxy, alkoxy, or other substituents. A process of preparing such piperidine derivative compounds in substantially pure form is also disclosed.

Abstract: 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.

Abstract: Selective MMP-13 inhibitors are isophthalic acid derivatives of the formula wherein: R1, R2, and R3 independently are hydrogen, halo, hydroxy, C1–C6 alkyl, C1–C6 alkoxy, C2–C6 alkenyl, C2–C6 alkynyl, NO2, NR4R5, CN, or CF3; E is independently O or S; A and B independently are OR4 or NR4R5; each R4 and R5 independently are H, C1–C6 alkyl, C2–C6 alkenyl, C2–C6 alkynyl, (CH2)n aryl, (CH2)n cycloalkyl, (CH2)n heteroaryl, or R4 and R5 when taken together with the nitrogen to which they are attached complete a 3- to 8-membered ring, optionally containing a heteroatom selected from O, S, or NH, and optionally substituted or unsubstituted; n is 0 to 6; or a pharmaceutically acceptable salt thereof. The compounds are useful for treating diseases in a mammal that are mediated by MMP enzymes.

Abstract: 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.

Abstract: 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 with D-phenylalanine in a mixed solvent of ketone solvent and water in the presence of an alkali; and then adjusting the temperature of the mixture to 58° C. to 72° C. and the concentration of ketone solvent to more than 8 wt % and less than 22 wt % to conduct precipitation of nateglinide crystals. This producing method is the industrially beneficial methods for crystallization of nateglinide.

Abstract: Specified phenylpropionic acid derivatives and analogues thereof have an antagonistic activity to ? 4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning ? 4 integrin, such as inflammatory diseases in which ? 4 integrin-depending adhesion process participates in the pathology, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.

Abstract: 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 also improve HDL functionality by (a) increasing clearance of cholesteryl esters, (b) increasing HDL-particle affinity for hepatic cell surface receptors or (c) increasing the half life of apoAI-HDL.

Abstract: 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, ?, ?, ?, ?, ?, ?, ? and ?, processes for their preparation and processes for preparation of other crystalline forms of nateglinide. Also provided are their pharmaceutical formulations and methods of administration.

Abstract: N-Arylphenylacetamide derivatives represented by the following formula [I]: (wherein R1 is C1-6 alkoxy, etc.; R2 is hydrogen, —(CH2)m—N(R6)(R7) (m is an integer of from 1 to 4; R6 is hydrogen, C1-4 alkyl, etc., R7 is hydrogen, etc.), etc.; R3 is hydrogen, halogen, etc.; R4 is C6-10 alkyl, —Y—R8 (Y is a single bond, C1-6 alkylene, C2-6 alkenylene, C2-6 alkynylene, etc., R8 is aryl, C3-8 cycloalkyl, C6-15 polycycloalkyl, etc.), etc.; R5 is hydrogen, etc.; and X1 is hydrogen), or pharmaceutically acceptable salts thereof or hydrates or solvates of the same, and a pharmaceutical composition containing the same. These compounds are useful as preventives and/or remedies giving no pain at the early stage of administration, which are efficacious in oral administration and have potent analgesic and antiinflammatory effects.

Abstract: 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 pharmaceutical compositions for the treatment of inflammatory diseases

Abstract: The present invention relates to a novel compound having a molecular formula C13H15NO5 having molecular structure of Formula I and a process for the isolation of said compound. The present invention also relates to a method of inhibiting 13-lipoxygenase and having free radical scavenging activity.

Abstract: The invention provides novel substituted phenylpropionic acid derivatives that bind to the receptor as ligands of human peroxisome proliferator-activated receptor ? (PPAR?) to activate and exhibit potent lipid-decreasing action, and processes for preparing them.

Abstract: The invention relates to NEP inhibitors for treating cardiovascular disorders. Preferred NEP inhibitors are compounds of formula (I) wherein R1 is C1–C6alkyl, C1–C6alkoxyC1–C3alkyl or C1–C6alkoxyC1–C6alkoxyC1–C3alkyl; R2 is hydrogen or C1–C6alkyl; L is a three atom linkage selected from —CH2—X—CH2— and —CH2—CH2—X— where the right hand side of the linkage is attached to R3 and where X is oxygen, sulfur or methylene; R3 is phenyl or aromatic heterocyclyl, either of which may be independently substituted by one or more groups selected from: C1–C6alkyl, halo, haloC1–C6alkyl, C1–C6alkoxy, haloC1–C6alkoxy, C1–C6alkylthio, haloC1–C6alkylthio and nitrile; and R4 and R5 are either both hydrogen, or one of R4 and R5 is hydrogen and the other is a biolabile ester-forming group that in the body of a patient is replaced by hydrogen.

Abstract: 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 acid chloride with phenylalanine in a mixed solvent of an organic solvent and water, while keeping the solvent under the alkali condition by using potassium hydroxide.

Abstract: 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 pharmaceutically acceptable salt thereof.

Abstract: 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 carcinogenic diseases. Further, the invention refers to a pharmaceutical composition comprising the alkylating peptides of the invention.

Abstract: Pharmaceutically acceptable compounds for administering to a subject, comprising the general structure II: wherein R1 is an L-amino acid or salt or ester thereof, or an L-amino acid containing peptide or salt or ester thereof; and wherein the stereochemistry about the carbon-carbon double bond is trans. The invention further relates to pharmaceutical compositions comprising the aforementioned compounds.

Abstract: 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.

Abstract: 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 moieties; Y1 is selected from the group consisting of O, S, and NR5; M is NR3, O or S; Ar is a moiety which when included in Formula I forms a multi-substituted aromatic or heteroaromatic hydrocarbon or a multi-substituted heterocyclic group; (m) is zero or a positive integer; R1-3 and R5 are independently selected from the group consisting of hydrogen, C1-6 alkyls, C3-12 branched alkyls, C3-8 cycloalkyls, C1-6 substituted alkyls, C3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C1-6 heteroalkyls, substituted C1-6 heteroalkyls, C1-6 alkoxy, phenoxy and C1-6 heteroalkoxy; and R4 is a polymeric residue; as well as methods of making and using the same are disclosed.

Abstract: 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 diseases.

Abstract: This invention relates to a novel process to obtain highly pure 4-(cyclopropylcarbonyl)-?,?-dimethylphenylacetic acid of Formula I through crystallization from a mixture of para and meta regioisomers of Formula I and II in cyclohexane, whereby the amount of undesired meta isomer, 3-(cyclopropylcarbonyl)-?,?-dimethylphenylacetic acid of Formula II is decreased to below 0.5%. The compound of Formula I is a key intermediate for the preparation of high purity terfenadine carboxylate, which is a known antihistaminic.

Abstract: 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 also relates to dicarboxylic salicylamide delivery agent compounds for the delivery of active agents. Methods of administration are provided as well.

Abstract: The present invention provides novel compounds represented by formula I: or pharmaceutically acceptable salts thereof useful for treating Flaviviridae viral infection.

Abstract: 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 thionyl chloride in the presence of an effective amount of an organic amide. Also provided are processes for preparation of nateglinide by acylation of a suitable salt of D-phenylalanine with trans-4-isopropylcyclohexane acid chloride in both a single and a two phase system, and in water free of a co-solvent.

Abstract: The invention relates to compounds of formula (I) for treating for example sexual dysfunction, wherein R1 is optionally substituted C1-6alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, hydrogen, C1-6alkoxy, —NR2R3 or —NR4SO2R5; X is the linkage —(CH2)n— or —(CH2)q—O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C1-4alkoxy; hydroxy; hydroxy(C1-3alkyl); C3-7cycloalkyl; carbocyclyl; heterocyclyl; or by C1-4alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted; or two R8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused optionally substituted 5- or 6-membered carbocyclic or heterocyclyic ring.

Abstract: A compound of Formula I or a pharmaceutically acceptable salt thereof, or a tautomer thereof, wherein G1, G2, and B are as defined in the application, are selective inhibitors of MMP-13. The compounds are useful for treating diseases mediated by MMP-13, including cancer and arthritis.

Abstract: Disclosed are compounds and pharmaceutically acceptable salts of formula (I): 1

Abstract: These are described biphenylene compounds of formula (I) wherein R1 is a C1-C18alkyl, C2-C18alkenyl, C6-C10aryl or C6-C10aryl or C6-C10heteroaryl radical each unsubstituted or mono- or poly-substituted by hydroxy, halogen, C1-C18alkyl, C1-C18alkoxy, amino, C1-C5monoalkyamino or by di-C1-C5alkylamino; C5-C7cycloalkyl or C5-C7cycloalkenyl each unsubstituted or substituted by C1-C5alkyl; —OR′; or NR′R″; R2 is a C1-C18alkyl, C2-C18alkenyl, C6-C10aryl or C6-C10heteroaryl radical each unsubstituted or mono- poly-substituted by hydroxy, hadroxy, C1-C18alkoxy, amino, C1-C5monoalkylamino or by di-C1-C5alkylamino; —OR′; —NR′R″; or R1 and R2 together form a 5- to 7- membered monocyclic carbocyclic or heterocyclic ring; R3 is hydrogen; C1-C6alkyl or C1-C6alkoxy; R′ and R″ are each independently of the other hydrogen; unsubstituted or mono- or poly-hydroxy-, halo-, C1-C18alkyl-, C1-C18alkoxy-, amino- or quaternary ammonium groupsubstituted C1-C18alkyl, C5-C

Abstract: Compounds of formula (I): wherein when m is 0 to 4 R1 is selected from C1-6alkyl, C3-7cycloalkyl, C2-6alkenyl, —SO2NR4R5, —CONR4R5 and —COOR4; and when m is 2 to 4 R1 is additionally selected from C1-6alkoxy, hydroxy, NR4R5, —NR4SO2R5, —NR4SOR5, —NR4COR5, and —NR4CONR4R5; R2 is selected from hydrogen, C1-6alkyl and —(CH2)n-C3-7cycloalkyl; R3 is the group —CO—NH—(CH2)p-R6; U is selected from methyl and halogen; W is selected from methyl and chlorine; V and Y are each selected independently from hydrogen, methyl and halogen; m is selected from 0, 1, 2, 3 and 4 wherein each carbon atom of the resulting carbon chain may be optionally substituted with one or two groups selected independently from C1-6alkyl; n is selected from 0, 1, 2 and 3; p and r are independently selected from 0, 1 and 2; s is selected from 0, 1 and 2; or pharmaceutically acceptable salts or solvates thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors

Abstract: (R)-Enantiomers of quaternary ammonium salts of general formula (I) are described: 1

Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of formula (I): 1

Abstract: A novel class of dicarboxylic acid derivatives, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: This invention provides metabolites of a class of androgen receptor targeting agents (ARTA).

Abstract: The present invention relates to compounds and pharmaceutically acceptable salts of formula (I): 1

Abstract: N-Arylphenylacetamide derivatives represented by the following formula [I]: 1

Abstract: The present invention relates to a compound represented as formula (I): 1

Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S.

Abstract: L-threo-&bgr;-benzyloxyaspartate derivatives having a substituent on the benzene ring, represented by the following formula (1): 1

Abstract: Specified phenylpropionic acid derivatives and analogues thereof have an antagonistic activity to &agr; 4 integrin. They are used as therapeutic agents or preventive agents for various diseases concerning &agr; 4 integrin, such as inflammatory diseases in which &agr; 4 integrin-depending adhesion process participates in the pathology, rheumatoid arthritis, inflammatory bowel diseases, systemic lupus erythematosus, multiple sclerosis, Sjögren's syndrome, asthma, psoriasis, allergy, diabetes, cardiovascular diseases, arterial sclerosis, restenosis, tumor proliferation, tumor metastasis and transplantation rejection.

Abstract: A carboxylic acid derivative of formula (I) 1

Abstract: The present invention provides an anti-curl agent containing an amide compound of specific structure and molecular weight, an ink jet ink containing the amide compound, a method for ink jet recording to form images by ejecting the ink, and a method for reducing curl of recording media using the ink. The anti-curl agent of the present invention can reduce shape changes of a printed paper with a lapse of time, i.e., the curl phenomenon, tending to occur in particular with a plain paper printed over the entire surface, without deteriorating image quality.

Abstract: The present invention relates to certain novel benzylamine derivatives, to processes for their preparation, to pharmaceutical formulations containing them and to their use in medical therapy, particularly in the treatment of depression.

Abstract: The invention relates to compounds of formula (1) 1

Abstract: The present invention relates dipeptidyl peptidase IV inhibition and, more particularly, relates to glutaminyl derivatives, wherein the glutamin residue is bound in a peptide manner to a moiety which imitates the amino acid residue prolin, especially to a nitrogen containing moiety, pharmaceutical compositions containing said compounds, and the use of said compounds in inhibiting dipeptidyl peptidase IV and dipeptidyl peptidase IV-like enzyme activity.

Abstract: The present invention pertains to specific peptides obtainable from cocoa beans and giving rise to a particular and distinct savor when subjected to a Maillard reaction with reducing sugars. In particular, the present invention pertains to the use of one or more of these specific peptides for the preparation of a chocolate flavor, specifically a cocoa and a caramel flavor, a floral or specifically, a bonbon flavor, a bready flavor, a roasted flavor or a meat flavor.

Abstract: The present invention relates to a novel compound having a molecular formula C13H15NO5 having molecular structure of Formula I and a process for the isolation of said compound. The present invention also relates to a method of inhibiting 13-lipoxygenase and having free radical scavenging activity.

Abstract: Novel compounds of the formula (I) in which R1, R2, R3, R4, X and Z are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders and for the treatment of tumours.