Abstract: The present invention provides for methyl)-4-amino-2R-methyl butanoic acid ethyl ester sodium salt, a novel process for the preparation of crystalline Form B of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-2R-methyl butanoic acid ethyl ester sodium salt.

Abstract: The invention relates to crystalline tranilast salts. The crystalline tranilast salts, their preparation and their characterization are described and shown in the figures. The invention relates to pharmaceutical compositions containing a crystalline tranilast salt of the invention and a pharmaceutically acceptable carrier. The invention also relates to methods of treatment and the use of a therapeutically effective amount of a crystalline tranilast salt of the invention for treatment. The invention also relates to a method of preparing a liquid pharmaceutical composition comprising the step of dissolving a crystalline tranilast salt of the invention in a pharmaceutically acceptable solvent and to liquid pharmaceutical compositions prepared according to that method.

Abstract: The present invention provides for crystalline Form B1 of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenyl-methyl)-4-amino-2R-methyl butanoic acid ethyl ester sodium salt, crystalline Form B2 of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-2R-methyl butanoic acid ethyl ester sodium salt, a novel process for the preparation of crystalline Form B of N-(3-carboxyl-1-oxopropyl)-(4S)-(p-phenylphenylmethyl)-4-amino-2R-methyl butanoic acid ethyl ester sodium salt.

Abstract: Allosteric hemoglobin (Hb) modifiers of hemoglobin which contain nitric oxide (NO) moieties allowing for the release of NO in vivo. The compounds retain the oxygen delivery capability of the allosteric hemoglobin modifier to bind Hb and enhance Hb's ability to deliver oxygen to cells and tissues, and also release NO from the NO moiety. Methods of delivering oxygen and/or NO to cells and tissues are also provided.

Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).

Abstract: A method for the synthesis of daptomycin or a daptomycin analogue is carried out on a resin to form a linear precursor followed by a serine ligation macrocyclization in solution. Daptomycin analogues can differ from daptomycin by substitution of amino acids residues and/or deletion or addition of amino acid residues. Daptomycin analogues can include a different fatty acid in the side arm of the daptomycin analogue.

Abstract: Mew tranilast complexes and new tranilast cocrystals are disclosed. These include all tranilast nicotinamide complex, a 1:1 tranilast nicotinamide cocrystal, a 1:1 tranilast saccharin complex, a 1:1 tranilast saccharin cocrystal, a 1:1 tranilast gentisic acid complex, a 1:1 tranilast gentisic acid cocrystal, a 1:1 tranilast salicylic acid complex, a 1:1 tranilast salicylic acid cocrystal, a 1:1 tranilast urea complex, a 1:1 tranilast urea cocrystal, a 1:1 tranilast 4-amtnoben2oic acid complex, a 1:1 tranilast 4-am!nobers2oic acid cocrystal, a 1:1 tranilast 2,4-di?hydroxybenzoic acid complex and a 1:1 tranilast 2,4-dihydroxybenzoic acid cocrystal. Also disclosed are pharmaceutical compositions containing a tranilast complex or cocrystal of the invention and a pharmaceutically acceptable carrier. Methods of treatment using the tranilast complexes and cocrystais as well as the pharmaceutical compositions are disclosed.

Abstract: The invention provides a compound conforming to the structure of Formula (CX) The invention also provides a thermoplastic polymer composition comprising a polyolefin polymer and a compound conforming to the structure of Formula (CX) as a nucleating agent.

Abstract: The compounds of formula (1) in which R1, R4, A and X have the meanings as given in the description, are novel effective EP2 agonists.

Abstract: The present invention relates to a novel process for preparing cis-alkoxy-substituted spirocyclic phenylacetylamino acid esters and cis-alkoxy-substituted spirocyclic 1H-pyrrolidine-2,4-dione derivatives, and also to novel intermediates and starting materials which are produced and/or used in the process according to the invention.

Abstract: Substituted cinnamoyl anthranilate compounds exhibiting anti-fibrotic activity; or derivatives thereof, analogues thereof, pharmaceutically acceptable salts thereof, and metabolites thereof, with the proviso that the compound is no Tranilast.

Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).

Abstract: The present invention provides a compound of Formula (I): or a pharmaceutically acceptable salt thereof. Also, the present invention provides a pharmaceutical composition comprising a compound of Formula (I) or a pharmaceutically acceptable salt thereof and a pharmaceutically acceptable carrier. The present invention further provides methods for treating abdominal aortic aneurysm or atherosclerosis comprising administering a therapeutically effective amount of a compound of Formula (I) or a pharmaceutically acceptable salt thereof or a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of a compound of Formula (I) or pharmaceutically acceptable salt thereof.

Abstract: The invention provides 3-carboxypropyl-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, and R6 are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: The present application relates to novel 3-phenylpropionic acid derivatives which carry a branched or cyclic alkyl substituent in the 3-position, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular diseases.

Abstract: The present invention relates to substituted 6-methoxy-4-amino-N-phenyl-2-naphtamides derivatives, processes for preparing them, pharmaceutical compositions to containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.

Abstract: The invention relates to amide compounds of formula I and I? or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain.

Abstract: The present invention provides dihydroorotate dehydrogenase inhibitors, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of diseases or disorders wherein the inhibition of Dihydroorotate dehydrogenase is known to show beneficial effect.

Abstract: Disclosed herein are compounds that may be specific to PPAR and/or EGF receptors, and methods of making and using same.

Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

Abstract: The invention relates to compounds of the formula I in which R1, R2, X, A, B and Y1 to Y4 have the meanings indicated in the claims, and/or a pharmaceutically acceptable salt and/or a prodrug thereof. Because of their properties as inhibitors of chemokine receptors, especially as CXCR2 inhibitors, the compounds of the formula I and the pharmaceutically acceptable salts and prodrugs thereof are suitable for the prevention and treatment of chemokine mediated diseases.

Abstract: A compound of formula (I) or a pharmaceutically acceptable derivative thereof, wherein, R1, R2, R3, R4, R5, m, n and X are as defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.

Abstract: The present invention relates to a compound inhibiting HF-1 activity, a preparation method of the same, and a pharmaceutical composition comprising the same as an active ingredient. The compound of the present invention demonstrates anticancer activity not by non-selective cytotoxicity but by inhibiting the activity of HIF-1, the transcription factor playing an important role in cancer cell growth and metastasis. Accordingly, the compound or the pharmaceutically acceptable salt thereof according to the present invention inhibits HIF-1 activity, and therefore can be used as a therapeutic agent for solid tumors such as colon cancer, liver cancer, stomach cancer and breast cancer. In addition, the compound or the pharmaceutically acceptable salt thereof according to the present invention can be used as an active ingredient for a therapeutic agent for diabetic retinopathy or arthritis which may become worse when hypoxia-induced VEGF expression by HIF-1 increases.

Abstract: A mGlu2/3 receptor antagonist of the formula: its uses, and methods for its preparation are described.

Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.

Abstract: The invention relates to an N-acyl anthranilic acid derivative or it's salt having collagen production inhibitory action.

Abstract: Compounds of formula (I): in which R1, R2, R7, R8, R9, R10 and A have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.

Abstract: A compound of formula (I): wherein A1, A2, A3, A4, R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or salts or N-oxides thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.

Abstract: The present application relates to novel 3-phenylpropionic acid derivatives which carry a branched or cyclic alkyl substituent in the 3-position, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular diseases.

Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.

Abstract: The present invention relates to the field of therapeutic methods to screen for compounds on the basis of their ability to influence Wnt activity. The screening process is applied to both a physical library of a series of compounds and a virtual library of compounds that affect Wnt activity. In one aspect, the virtual screening process could be carried out where a permutational library of small peptides is substituted for the small organic molecules. The inventive methods may be used to empirically test for effects on Wnt activity and may also be applied to any pair of proteins involved in protein-protein interactions.

Abstract: The anthranilic acid derivative or the salt thereof represented by the general formula wherein R1 and R2 are hydrogen atom, or the like; R3 is a phenyl, cycloalkyl or bicyclic heterocyclic group which may be substituted, or the like; R4 is a phenyl, cycloalkyl or pyridyl group which may be substituted, or the like; X1 is an alkylene or alkenylene group which may be substituted or a bond; X2 is the general formula —X3—X4— or —X4—X3—, wherein X3 is a sulfur atom, an imino group or a bond, or the like; X4 means an alkylene or alkenylene group which may be substituted or a bond; is useful for a remedy such as rheumatoid arthritis, osteoarthritis and carcinoma, because it shows MMP—13 production inhibitory effect.

Abstract: A method of producing a compound represented by Formula (I), which comprises a step A of reacting an anthranilic acid compound with a carboxylic halide in the absence of a base, but does not comprise a step of isolating of an amide intermediate compound represented by Formula (II): wherein R1 represents a substituent; n1 is an integer of 0 to 4; R2 represents an n2-valent substituent or a linking group; and n2 is an integer of 1 to 4.

Abstract: The present invention relates to compounds of formula (I): wherein Q, G1, G2, and G3, are defined herein. Pharmaceutical compositions and methods for treating DGAT-1 related diseases or conditions are also disclosed.

Abstract: Compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract: The invention provides antimicrobial compounds and compositions, and methods of using them. The compounds and compositions include, for example, a compound of any one of Formulas I-X. The invention further provides methods of preparing the compounds, and useful intermediates for their preparation. The compounds can possess highly specific and selective activity, such as antibacterial activity and/or enzymatic inhibitory activity. Accordingly, the compounds and compositions can be used to treat bacterial infections, or to inhibit or kill bacteria, either in vitro or in vivo.

Abstract: A compound of the formula: where X is phenyl substituted at the 3, 4 and 5 positions with R1, R2 or R3 which are selected from hydrogen, chloro, lower alkyl of 1 to 5 carbons, phenoxy, phenyl, naphthyl, or phenyl (lower) alkyl where the lower alkyl group has 1-5 carbon atoms and m is 0 or 1; Y is —CONH— or —NHCONH— where the nitrogen atoms are unsubstituted or substituted with other phenoxyisobutyric acid derivatives, or the residue of a phenoxyisobutyric acid and n is 0 or 1; Z is unsubstituted phenyl when m is 1 and n is 1; when Y is 0, X is 0; Z is also substituted.

Abstract: Certain poly(oxyalkylene) colorants are disclosed along with method of preparation thereof. A method of using these colorants as fluorescent security taggants is also disclosed.

Abstract: The use of specific compounds of the Formula 1 (and also corresponding mixtures) in particular as cosmetic agents for the inhibition of the substance P-induced release of histamine from mast cells is described.

Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-amido-aryl compounds of the following formula (for convenience, collectively referred to herein as “AAA compounds”), which, inter alia, are (selective) retinoic acid receptor ? (RAR?) agonists. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to (selectively) activate RAR?, and in the treatment of diseases and conditions that are mediated by RAR?, that are ameliorated by the activation of RAR?, etc., including cognitive disorders, memory impairment, memory deficit, senile dementia, Alzheimer's disease, early stage Alzheimer's disease, intermediate stage Alzheimer's disease, late stage Alzheimer's disease, cognitive impairment, and mild cognitive impairment.

Abstract: Compounds of Formula (I): in which R1, R2, R7, R8, R9, R10 and A have the meanings given in the specification, are DP2 receptor modulators useful in the treatment of immunologic diseases.

Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).

Abstract: The present invention relates to halogenated compounds of formula (I) with the substituents as described within the specification. The compounds may be useful as anti-fibrotic agents. The present invention also relates to methods for their preparation.

Abstract: Disclosed herein are compounds that may be specific to PPAR and/or EGF receptors, and methods of making and using same.

Abstract: The present invention relates to renin inhibitor compounds having the structure and their use in treating cardiovascular events and renal insufficiency.

Abstract: The present invention relates to a salt selected from the group comprising the N-methyl-D-glucamine salt (NMG), the diethylamine salt (DEA) salt, the magnesium salt, the tromethamine salt, the choline salt, the L-arginine salt, the zinc salt, and the 4-(2-hydroxyethyl)morpholine (HEM) salt of compounds of the general formula (I) wherein X is selected from the group consisting of CH2, S, or O; D is O or S; R8 is hydrogen or alkyl; E is an optionally substituted phenylene group; Y is a monocyclic or bicyclic substituted or unsubstituted 6-9 membered ring system which may contain one or more heteroatoms selected from N or S and which contains at least one aromatic ring; n is 0 or 1; and q is 0 or 1; with the proviso that compounds wherein X?CH2, q=0, Y=unsubstituted phenyl and E=unsubstituted phenylene are excluded; or a hydrate thereof.

Abstract: The present invention relates to the treatment and prevention of immunological and inflammatory disorders with a compound of formula (I) in combination with methotrexate,

Abstract: This invention provides well defined 6-alkyl or hydroxyalkyl-1-naphthamide or quinoline compounds for treating glaucoma or ocular hypertension.

Abstract: The invention relates to substituted (2-aryloxyacetylamino)phenylpropionic acid derivatives, and to the physiologically acceptable salts thereof. The invention relates to compounds of the formula I in which R1, R2, R3, R4, R5, R6, R7, R8, R9 and A are each defined as specified, and the physiologically compatible salts thereof. The compounds are suitable, for example, for treatment of diabetes.

Abstract: The present invention relates to a compound which is characterized by the formula (I) or a pharmaceutically acceptable salt, solvate, hydrate thereof, wherein the ring systems A and B are independently selected from a monosaccharide, aryl (preferably phenyl), a heteroaryl or cycloalkyl (preferably cyclohexan), preferably with all substituents in equatorial configurations; R1 is independently selected from alkyl (preferably C1 to C6), a substituted or unsubstituted phenyl, preferably CH3; R2 is H, alkyl (preferably C1 to C6), a carbohydrate in a glycosidic ?-linkage, preferably H; R3, R4, R5, and R6 are independently selected from H, (OH) hydroxy, alkyl preferably C1 to C6, alkoxy (preferably C1 to C6), amino, alkylamino (preferably C1 to C6), halogen, benzylamino, or benzoylamino; X is O, NH, alkylamino (NR), CO, S; and Y is O, NH, alkylamino (NR), CO, S.