Abstract: The invention describes the development of highly efficient, recyclable two component system, CuAl-hydrotalcite/rac 1,1?-Binaphthalene-2,2?-diol catalytic system for the N-alkylation of electron deficient aryl chlorides in presence of potassium carbonate as a base at room temperature in 3-6 h, wherein the process is provided for the preparation of various secondary amines via C—N coupling reaction of aliphatic amines(aliphatic open chain, acyclic, benzyl amines and heterocyclic amines) with various aryl chlorides.

Abstract: A compound represented by the following general formula (I): [wherein R1 represents hydrogen atom or a C1-6 alkyl group, A and B represent —(CH2)2—, —(CH2)3— or —(CH2)4—, X represents —N(R2)— (R2 represents hydrogen atom or a C1-6 alkyl group), —CO—, —C(?N—R3)— (R3 represents hydrogen atom or a C1-6 alkyl group), or —C(?C(R4)(R5))— (R4 and R5 independently represent hydrogen atom or a C1-6 alkyl group), and Ar represents an aryldiyl group or a heteroaryldiyl group], which has an action of controlling physiological activities of retinoids and useful as an active ingredient of a medicament.

Abstract: The present invention features a method for increasing hydrophilic properties of crystalline carbon using a surface modifier and a method for preparing a Pt/C catalyst using the same. In certain preferred embodiments, the present invention features a method for increasing hydrophilic properties of crystalline carbon having water repellency by forming ?-? interaction between the surface of the crystalline carbon and a surface modifier and a method for preparing a catalyst by supporting platinum (Pt) on the crystalline carbon having increased hydrophilic property. The Pt/C catalyst prepared by the methods of the present invention is useful for the preparation of electrode materials for fuel cells.

Abstract: The present invention relates to salts of Memantine and COX-INHIBITORs, their crystal form, the processes for preparation of the same and their uses for the treatment of various disorders, including pain.

Abstract: The invention provides novel compounds of formula (I), wherein: R1 is a radical derived from one of the known ring systems; R2 is a phenyl radical optionally substituted; Xn represents a birradical selected from the group consisting of: —(CH2)1-4—, (C2-C4)-alkenyl, (C2-C4)alkynyl, —S—(CH2)1-3—#, and —(CH2)1-3—O—#; wherein the symbol # indicates the position at which Xn is attached to R1; Yn is a birradical selected from the group consisting of: —(CH2)2-4—, —S—(CH2)1-3#, and —O—(CH2)1-3—#; wherein the symbol # indicates the position at which Yn is attached to R2; and R3 is a radical selected from the group consisting of: —OR4. The compounds of formula (I) are useful in the treatment of cancer.

Abstract: [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. [Means for Solving Problems] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic action, and as a result, they have found that various amide derivatives having a carboxylic group or an equivalent thereof exhibit an excellent EP4 receptor antagonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor antagonistic action, it is useful as an agent for preventing and/or treating chronic renal insufficiency or diabetic nephropathy.

Abstract: A process for the preparation of a compound of formula (I): which are useful as intermediates in the preparation of i.a. pharmaceutically active compounds.

Abstract: Covalent conjugates of an ?,?-disubstituted glycine ester and a modulator of the activity of a target intracellular enzyme or receptor, wherein the ester group of the conjugate is hydrolysable by one or more intracellular carboxylesterase enzymes to the corresponding acid and the ?,?-disubstituted glycine ester is conjugated to the modulator at a position remote from the binding interface between the inhibitor and the target enzyme or receptor pass into cells and the active acid hydrolysis product accumulates within the cells.

Abstract: The present invention provides novel compositions of allosteric hemoglobin modifiers which are substantially free of impurities, specifically polymeric impurities. In one embodiment, the novel compositions contain an allosteric hemoglobin modifier compound and less than 100 ppm of the polymeric impurities generated during the preparation of this compound. Included in the present invention are novel methods for preparing allosteric hemoglobin modifiers that are substantially free of polymeric impurities. Also included in the present invention are improved methods for the purification of the product formed by the method of this invention. The novel methods of purification comprise extracting the crude composition with a water immiscible or partially immiscible solvent such as methylisobutyl ketone (MIBK) to lower amounts of impurities, specifically polymeric impurities.

Abstract: A compound represented by the following general formula (I): [R1 to R5 represent hydrogen atom, an alkyl group, or a trialkylsilyl group, X represents —NH—CO—, —CO—NH—, —N(COR6)—CO—, —CO—N(COR7)— (R6 and R7 represent a lower alkoxy group, or a carboxy-substituted phenyl group) etc.; and Z represents —Y—CH(R12)—COOH, —CHO, —CH?CH—COOH, or —COOR13 (Y represents a single bond, —CH2—, —CH(OH)—, —CO—, —CO—NH—, or —CO—NH—CH2—CO—NH—, R12 represents hydrogen atom or a lower alkyl group, and R13 represents hydrogen atom, —CH(R14)—COOH(R14 represents hydrogen atom, a lower alkyl group, or hydroxy group), —[CH2CH2—O]n—CH2—CH2—OH, —CH2—O—[CH2CH2—O]m—CH2—OH, or —[CH(CH3)—CO—O]p—CH(CH3)—COOH (m, n and p represent an integer of 1 to 100))], a salt thereof or an ester thereof, which has a property of being converted into a retinoid after absorption in vivo.

Abstract: The invention relates to compounds of general formula (1): in which R1, R2, R3, R4, R5, A, B, D and E are as defined in Claim 1, and also to the preparation process therefor and the therapeutic use thereof. These compounds can be used in the treatment of pathologies associated with hyperglycaemia.

Abstract: The invention relates to (carboxylalkylenephenyl)phenyloxamides and their physiologically tolerated salts, and their use as a medicament.

Abstract: A method according to one embodiment includes growing an organic crystal from solution, the organic crystal exhibiting a signal response signature for neutrons from a radioactive source. A system according to one embodiment includes an organic crystal having physical characteristics of formation from solution, the organic crystal exhibiting a signal response signature for neutrons from a radioactive source; and a photodetector for detecting the signal response of the organic crystal. A method according to another embodiment includes growing an organic crystal from solution, the organic crystal being large enough to exhibit a detectable signal response signature for neutrons from a radioactive source.

Abstract: This invention relates to novel compounds that display retinoid like activities, including HB-EGF (Heparin Binding Epidermal Growth Factor) release from keratinocytes, cell proliferation, and epidermal thickening without the irritation potentials, such as release of interleukin 8 and inhibition of terminal differentiation of keratinocytes. This invention also relates to the use of such a compound for both external and non-external applications.

Abstract: Processes for the preparation of certain [3.1.0]hexane derivatives which are useful as mGluR agonists, and intermediates prepared during such processes.

Abstract: This invention relates to novel Spiro cyclopentane derivatives of formula (I) or a pharmaceutically acceptable salt thereof, for treating diseases and conditions of the central nervous system (CNS), in particular sleep disorders.

Abstract: An integrated process is provided for preparing complexes of 2,3,5,6-tetraminotoluene with an aromatic diacid starting with nitration of 2,6-dihalotoluene. The process design eliminates costly intermediate drying and recrystallization steps. Handling of solid materials with possible skin sensitizing properties and toxicity is avoided, thereby eliminating human and environmental exposure.

Abstract: Complexes of 2,3,5,6-tetraminotoluene with an aromatic diacid are prepared by reaction with a divalent salt of the aromatic diacid while maintaining the pH of the reaction solution between 3 and 10. The resulting complexes are suitable for making high molecular weight polybenzimidazole polymers for high-performance fibers.

Abstract: The present invention encompasses compounds of Formula (I): as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.

Abstract: The present invention provides a GPR receptor function regulator comprising the compound represented by the formula: [wherein ring A is an optionally substituted isocyclic or heterocyclic ring, P is a bond or spacer, ring D is an optionally substituted monocyclic aromatic ring which may be condensed with a 5- to 7-membered ring, V is a bond or the group represented by the formula —CR14?CR15— or —N?CR16— (wherein R14, R15 and R16 each represents a hydrogen atom or optionally substituted hydrocarbon group), Q is a bond or spacer, and W is a carboxyl or a group biologically equivalent to a carboxyl] or its salt or a prodrug thereof.

Abstract: The present invention relates to a dye compound represented by the following formula (I), or a salt thereof: wherein R1, R2, R3, R4, D1, D2, B, and n are defined the same as the specification, and also relates to a photoelectric component using the same. The dye compound of the present invention is suitable for Dye-Sensitized Solar Cell (DSSC). Hence, the photoelectric characteristics of the DSSC can be improved by using the dye compound of the present invention.

Abstract: A process for converting an arylamine into an arylamine derivative, includes (i) providing a first arylamine compound; (ii) formylating the first arylamine compound to form a formyl substituted arylamine compound, where the first arylamine compound is not a formyl substituted arylamine compound; and (iii) acidifying the formyl substituted arylamine compound, in the presence of a solvent and a solid organic catalyst, to convert formyl functional groups into acid functional groups to form an acidified compound.

Abstract: The present invention relates to new phenylacetic acid inhibitors of cyclooxygenase activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative.

Abstract: A polyimide obtained by reacting a tetracarboxylic acid component with a diamine component containing a diamine compound represented by the following general formula (1): wherein, A represents a biphenylene group which may be substituted with an alkyl group having up to 4 carbon atoms.

Abstract: The invention relates to tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents.

Abstract: The present patent application concerns new compounds of formula (I): displaying agonistic activity at sphingosine-1-phosphate (S1P) receptors, their process of preparation and their use as immunosuppressive agents.

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

Abstract: Compounds of formula (I) pharmaceutically acceptable salts thereof, and pharmaceutically acceptable esters thereof; which are useful for the treatment of COX-2 dependent disorders.

Abstract: The present invention relates to compounds having the general Formula (I) with the definitions of X, Y, R1, R2, R3, R4, R9, and R10 given below, and/or a salt or ester thereof. Furthermore the invention relates to the use of said compounds for the treatment of Alzheimer's disease and their use for the modulation of ?-secretase activity.

Abstract: The present invention relates to pharmaceutical and diagnostic compositions as well as to the use of the active substances contained therein for preparing a pharmaceutical or a diagnostic composition for the treatment or diagnosis of neurodegenerative disorders or amyloid diseases.

Abstract: The present application describes deuterium-enriched diclofenac, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: A method of decreasing neuropathic pain in a mammal, comprising administering to said mammal an effective amount of tranilast for a period of time sufficient to decrease pain.

Abstract: The present invention encompasses compounds of Formula (I): as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating atherosclerosis, dyslipidemias and the like. Pharmaceutical compositions and methods of use are also included.

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

Abstract: Pharmaceutical compositions comprising at least one compound of the formulas (Ia) or (Ib) and a pharmaceutically acceptable carrier which is useful in a medicine wherein the symbols, indices and substituents have the following meaning R1?H, CN, NO2, CF3, F, Cl, Br, I, CH3 R2?H, CN, NO2, CF3, F, Cl, Br, I, CH3, Et, n-Pr, i-Pr, n-Bu, t-Bu, phenyl, thienyl, furyl, thiazolyl and either R1 or R2 must be H R3?H, CN, NO2, CF3, F, Cl, Br, I, CH3, Et, n-Pr, i-Pr, n-Bu, t-Bu, phenyl, thienyl, furyl, thiazolyl then X is e.g. with R4 being H, CH3, CH2CH3 or and Y being or the pharmaceutically acceptable salts, esters or amides and prodrugs of the above identified compounds of formulas (Ia) or (Ib). The compounds are applied to modulate the in-vitro and in-vivo binding processes mediated by E-, P- or L-selectin binding.

Abstract: The present invention provides pharmaceutical compositions useful in treating hepatitis C infection. The present invention also provides methods of treating hepatitis C infection by administering to a mammal the pharmaceutical compositions of the present invention.

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 process for the preparation of 1-(2-ethyl-butyl)-cyclohexanecarboxylic acid which is useful as an intermediate in the preparation of pharmaceutical active compounds.

Abstract: 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 comprising hexafluoroleucine and congeners thereof have been characterized using comparative biophysical studies. In general, the fluorinated peptides show higher thermal stability and enhanced resistance to chemical denaturation. Further, mixed hydrocarbon-fluorocarbon cores self-sort into homogeneous bundles, suggesting new avenues for the design and manipulation of protein-protein interfaces.

Abstract: The present invention relates to a tetrafluorobenzyl derivative and a pharmaceutical composition for prevention and treatment of acute and chronic neurodegenerative disease in central nervous system and ophthalmic diseases containing the same. The tetrafluorobenzyl derivative of the present invention can effectively be used to prevent and treat chronic neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease and Huntington's disease, degenerative brain disease such as epilepsy and ischemic brain disease such as stroke.

Abstract: This invention relates to bicyclic amide, carbamate or urea derivatives and salts thereof which are useful as active ingredients of pharmaceutical preparations. The bicyclic amide, carbamate or urea derivative of the present invention has vanilloid receptor (VR1) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with VR1 activity, in particular for the treatment of urological diseases or disorders, such as detrusor overactivity (overactive bladder), urinary incontinence, neurogenic detrusor oeractivity (detrusor hyperflexia), idiopathic detrusor overactivity (detrusor instability), benign prostatic hyperplasia, and lower urinary tract symptoms; chronic pain, neuropathic pain, postoperative pain, rheumatoid arthritic pain, neuralgia, neuropathies, algesia, nerve injury, ischaemia, neurodegeneration, stroke, and inflammatory disorders such as asthma and chronic obstructive pulmonary (or airways) disease (COPD).

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: Compounds of formula (I) wherein R is hydrogen, lower alkyl, (C3–C6)cycloalkyl, hydroxy, halo, lower alkoxy, trifluoromethoxy, trifluoromethyl or cyano; and A is biaryl, optionally substituted ?-naphthyl, bicyclic heterocyclic aryl, (C3–C6)cycloalkyl-monocyclic carbocyclic aryl, or (C5 or C6)cycloalkane fused-monocyclic carbocyclic aryl; pharmaceutically acceptable salts thereof; and pharmaceutically acceptable esters thereof; which are useful for the treatment of COX-2 dependent disorders.

Abstract: Process for the separation of enantiomers comprising at least one free functional group, in which process a reagent based on an enantiopure amino acid is reacted in basic medium with a mixture comprising enantiomers.

Abstract: One aspect of the invention relates to hexafluoroleucine and congeners thereof, and methods of making the compounds. Another aspect of the nvention relates to the synthesis of protein cores comprising hexafluoroleucine and congeners thereof. Certain peptides comprising hexafluorleucine and congeners thereof have been characterized using comparative biophysical studies. In general, the fluorinated peptides show higher thermal stability and enhanced resistance to chemical denaturation. Further, mixed hydrocarbonfluorocarbon cores self-sort into homogeneous bundles, suggesting new avenues for the design and manipulation of protein-protein interfaces.

Abstract: Disclosed are the compounds of formula I wherein R is methyl or ethyl; R1 is chloro or fluoro; R2 is hydrogen or fluoro; R3 is hydrogen, fluoro, chloro, methyl, ethyl, methoxy, ethoxy or hydroxy; R4 is hydrogen or fluoro; and R5 is chloro, fluoro, trifluoromethyl or methyl; and pharmaceutically acceptable salts thereof, as selective COX-2 cyclooxygenase inhibitors; and pharmaceutically acceptable prodrug esters thereof.

Abstract: The present invention provides a process for preparing 3-amino-2-hydroxypropionic acid derivatives (1) which does not use dangerous reagents, is economically advantageous, and is suitable for an industrial production, which process comprises: treating N-protected-3-amino-2-hydroxypropionic acid derivatives (2) having a steric configuration at 2-position carbon reverse to that of derivatives (1) with a leaving group-introducing agent to convert into N-protected-3-aminopropionic acid derivatives (3), then treating the derivatives with a basic substance to convert into substituted-3-amino-2-hydroxypropionic acid derivatives (4) having an inverted steric configuration at 2-position carbon, and then converting the derivatives into 3-amino-2-hydroxypropionic acid derivatives (1).

Abstract: Prodrug compounds capable of permeating a desired biological compartment and releasing a biologically active molecule in active form to effect a therapeutic functional change in the compartment to which it is introduced.

Abstract: Diarylamines, such as 5-amide substituted diarylamines of formula (I) or formula (II) wherein A is hydroxy, C1-6 alkoxy, or NR6OR7; X is OR12, NR13R12, or NR14; inhibitors of MEK and are useful in the treatment of a variety of proliferative disease states, such as conditions related to the hyperactivity of MEK, as well as diseases modulated by the MEK cascade.