Abstract: The present invention relates to compounds of the general formula I. The compounds are useful in the treatment of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: The invention provides novel substituted phenylpropanoic acid derivatives that activate by binding to receptor as ligands of human peroxisome preliferant-activated receptor &agr; (PPAR&agr;), and exhibit potent decreasing action on lipids in blood (cholesterol and triglyceride). It relates to a substituted phenylpropanoic acid derivatives represented by a general formula (1), their pharmaceutically acceptable salts and their hydrates, and processes for preparing them.

Abstract: The present invention is concerned with a novel process for the preparation of 3,5-bis(trifluoromethyl)benzoic acid (CAS 725-89-3). This compound is useful as an intermediate in the synthesis of compounds which possess pharmacological activity, in particular, as substance P (neurokinin-1) receptor antagonists.

Abstract: The present invention provides methods for producing a highly pure aromatic bromocarboxylic acid derivative and an aromatic acylthiocarboxylic acid derivative in high yields. The methods of the present invention include reacting an aromatic amino acid in an aqueous solvent in the presence of sodium nitrite, hydrogen bromide and at least one member selected from the group consisting of an aliphatic carboxylic acid and an alcohol, to give an aromatic bromocarboxylic acid derivative, and reacting the aromatic bromocarboxylic acid derivative and an organic thio acid in the presence of an amine to give an aromatic acylthiocarboxylic acid derivative.

Abstract: New benzenedicarboxylic acid derivative compounds; pharmaceutical compositions, diagnostic methods, and diagnstic kits that include those compounds; and methods of using those compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, neutopathy, pain, compulsive disorders, prostate diseases, cancers, and glaucoma.

Abstract: Disclosed are substituted phenoxyacetic acids useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds, alone or in combination with other therapeutic agents, and methods of treatment employing the compounds and pharmaceutical compositions, as well as methods for their synthesis.

Abstract: The present invention provides a novel ammonium salt of an organic acid. When the salt is used as a base additive for a chemically amplified resist, the environmental stability of the resist can be enhanced, and the T-top phenomenon can be effectively prevented. In addition, the line width change caused by acid diffusion can be prevented, and the E0 value of the resist can be decreased.

Abstract: A method for preparing chloromethylphenylacetic acids represented by formula (II): wherein a methylphenylacetic acid represented by formula (I): is reacted with a chlorine gas, in an inert solvent, under the irradiation with light or in the presence of a radical initiator, is disclosed. According to the preparation method, high purity chloromethylphenylacetic acids can be prepared at a high yield, without using toxic sulfuryl chloride as a chlorinating agent, by chlorinating the methyl group of the methylphenylacetic acids at a high selectivity while suppressing by-production of a dichloro form or &agr;-chloro form.

Abstract: The present invention is a method of producing dry, alkali metal or ammonium carboxylic acid salt particles. In accordance with the invention, a molten carboxylic acid is mixed with a solution of an alkali metal-containing or ammonium-containing alkaline compound and the carboxylic acid and alkaline compound are reacted to form the carboxylic acid salt. Water is then removed from the carboxylic acid salt to produce dry, carboxylic acid salt particles. The feed ratio of the molten carboxylic acid and the alkaline compound is controlled to neutralize the carboxylic acid in the process.

Abstract: Bidentate phosphine ligands of the formula 1

Abstract: A process for preparing a hydroxybenzoic acid is herein disclosed which comprises reacting a phenol with an alkali metal compound by the use of an aprotic polar organic solvent as a reaction solvent to form an alkali metal salt of the phenol, and then reacting this alkali metal salt with carbon dioxide to obtain a hydroxybenzoic acid, said process comprising the step of carrying out the reaction under conditions that a molar ratio of the phenol to the total of the alkali metal compound and the aprotic polar organic solvent is larger than 1. Furthermore, the process may contain the steps of precipitating crystals from the reaction solution, separating the solid from the solution to obtain a wet alkali metal salt of the hydroxybenzoic acid, dissolving the wet alkali metal salt in water, and precipitating crystals from the solution by acidification to obtain the hydroxybenzoic acid.

Abstract: The invention relates to a process for the preparation of ortho-alkylated benzoic acid derivatives of the formula I characterized in that an aryl bromide of the formula II is reacted with a secondary or tertiary organolithium compound and CO2.

Abstract: A tetrahydrofluorene, which is represented by the following formula (I) wherein R1 to R6 each independently represent a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, or R1 and R2 are combined together to represent ═O, ═N or ═S, R7 and R8 each independently represent a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a halogen atom, a hydroxyl group or a carboxyl group, is subjected to a hydrogen transfer reaction in the presence of a hydrogen acceptor and a catalyst, whereby a fluorene and a hydride of the hydrogen acceptor are formed at the same time.

Abstract: Disclosed are “acid-amide” calixarenes of formula (I) wherein: L is [—CH2—] or [—O—CH2—O—] and may be the same or different between each aryl group R5 is H, halogen, or C1-C10 aliphatic hydrocarbyl group, C6-C20 aryl group, any of which may optionally be substituted by one or more halo or oxo groups or interrupted by one or more oxo groups, and R5 may be the same or different on each aryl group; R1 comprises an optionally protected carboxy group; two groups out of R2, R3, and R4, are H; the one group out of R2, R3, and R4 not being H comprises an amide group. The amide group may be linked to a second calixarene to form a dimer. Also disclosed are methods of use of such calixarenes for the purposes of metal sequestration, especially of lanthanides and actinides. Also disclosed are calixarene dimer derivatives of the calixarenes of the invention.

Abstract: A cis-olefin of the formula: R1—CH═CH—R2 is prepared by reducing an alkyne of the formula: R1—C≡C—R2 with formic acid in the presence of a palladium catalyst. R1 and R2 are independently selected from the group consisting of a hydrogen atom, ester group, substituted silyl group, carboxyl group, cyano group, aliphatic C1-C20 hydrocarbon group, and phenyl group. The cis-olefin which is a useful intermediate for the synthesis of fine chemicals is selectively produced in high yields.

Abstract: An oxidation free process for converting a hydroxy substituted aromatic to an aromatic diacid which comprises reacting a hydroxy substituted aromatic with excess basic salt in the presence of carbon dioxide at disproportionation/isomerization reaction conditions.

Abstract: Methods and compositions for the treatment of lung disease, such as emphysema and/or bronchopulmonary dysplasia, in a mammal. Also disclosed are methods promoting the formation of alveolar septa and increasing the gas-exchange surface area of a mammalian lung, and for the prevention and/or treatment of alveolar destruction.

Abstract: The present invention provides compounds represented by the general formula (I): and a salt thereof, and anti-inflammatory agents and antitumor agents containing the compounds as the active ingredients.

Abstract: A process for producing trifluoroethoxybenzoic acids or salts thereof by reaction of halobenzoic acids or salts thereof with 2,2,2-trifluoroethanol in the presence of a strong base and copper containing materials. The compounds obtained by the process of the present invention may be used as synthetic intermediates in the pharmaceutical industry.

Abstract: A process for the preparation of sulphonated distyryl-biphenyl compounds of formula (1), in which R1 and R2, independently, are hydrogen, C1-C5-alkyl, C1-C5-alkyl or halogen, and M represents Li, K, an alkaline earth metal or ammonium, characterized by, firstly, reacting a compound of formula (2) with a di- or trialkylamine containing 6-12 carbon atoms in each alkyl group, in a two-phase system consisting of strong aqueous mineral acid and a water immisicible organic solvent and, secondly, reacting the resulting lypophilic ammonium salt with LiOH, KOH, an alkaline earth metal hydroxide, ammonia, a mono-, di- or trialkylamine or a tetraalkylammonium hydroxide, all containing 1-4 carbon atoms in each alkyl group; mono-, di- or tri(C2-C4)alkanolamine, morpholine, piperdine or pyrrolidine.

Abstract: A tetrahydrofluorene, which is represented by the following formula (I) 1

Abstract: An acidic organics-containing waste water stream (12) derived from for example plant for the production of an aromatic carboxylic acid such as terephthalic acid is treated to allow recovery of alkali and water for recycle to the production process. The treatment comprises adjusting the pH of the waste water stream using an alakaline medium, oxidising (10) the organics content of the stream to convert the same to water, carbon dioxide and (bi)carbonate ions, and supplying the treated stream to a reverse osmosis membrane (28, 30) to produce a retentate containing (bi)carbonate ions and cations derived from the alkaline medium and a permeate which is substantially free of those components. The retentate (46) is recycled for use in adjustment of the pH of the waste water stream and, if desired, water-consuming facilities which can tolerate less pure water.

Abstract: A process for preparation of crosslinked cellulosic products containing at least 30 wt. % cellulosic fibers and the polyanhydride crosslinked cellulosic products resulting therefrom wherein a cellulosic material is treated with an aqueous solution of a polycarboxylic acid formed by hydrolysis of a polyanhydride of the structure which comprises the reaction product of trimellitic anhydride and a diol in the mole ratio of from about 2.0:0.9 to about 2.0:1.1, wherein R is selected from the group consisting of alkyl, alkylene and cycloalkylene moieties of up to 12 carbon atoms and ethylene oxide and propylene oxide moieties of molecular weight up to about 6000, wherein said cellulosic material is impregnated with an aqueous solution of said polyanhydride, dried, and heated to a temperature of from about 120° C. to about 200° C.

Abstract: The present invention provides novel compounds of Formula 1, compositions containing these compounds, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B, CD45, SHP-1, SHP-2, PTP&agr;, LAR and HePTP or the like, wherein A, R1, R2, R3, R4, R16 and R17 are as defined in the specification.

Abstract: para-Aminomethylaryl carboxamides of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.

Abstract: 6-tert-Butyl-1,1-dimethylindane derivatives which are unsaturated in the 4-position of formula: X represents: (i) either a radical of formula: and Y represents a radical of formula: (ii) or a radical of formula: and Y represents either a radical of formula (b) or a radical of formula: Z being —O—, —S— or R1 represents —CH3, —(CH2)p—OR4, —(CH2)p—COR5 or —S(O)t—R6, p being 0, 1, 2 or 3, t being 0, 1 or 2, R2 represents H or lower alkyl, R3 represents H, lower alkyl or —COR7, R4 represents H, lower alkyl, —COR7, aryl, aralkyl, mono- or polyhydroxyalkyl, or a polyether radical, R5 represents H, lower alkyl, —OR8 or —N(r′)(r″), R6 represents H or lower alkyl, R7 represents lower alkyl, R8 represents H, alkyl, alkenyl, alkynyl, aryl, aralkyl, mono- or polyhydroxyalkyl, a sugar residue or an amino ac

Abstract: Intermediates for the synthesis of camptothecin of the formula II wherein: R1 is —(CH2)2NR1R2, where R1 is an amino protecting group and R2 is C2-C5 alkyl, hydroxyethyl or acetoxyethyl group, and of the formula III wherein: n is 1 or 2; R3 is hydrogen or —OR4, where R4 is hydrogen, —COR5, —CONHR6 or CH2OR7, where R5 is methyl or —CH2OCH3, R6 is isopropyl, phenyl or —CH2CH2Cl, and R7 is methyl, ethyl or —CH2CH2OCH3; with the proviso that when n is 2, R3 is not hydrogen.

Abstract: The invention relates to a compound having the general Formula I: including its salts, where Z is either the group having the general Formula II: where R1 is alkyl having 1-4 C atoms, alkoxyalkyl having 2-5 C atoms or aryloxyalkyl whose alkyl group has 1-4 C atoms, R2 is alkyl having 1-4 C atoms or alkoxyalkyl having 2-5 C atoms, R3 is H, alkoxy having 1-4 C atoms, halogen, NO or NO2, Y is H2 or O and L is a luminophoric moiety in a position para or meta to the nitrogen, or is the group having the general Formula III: where n is 2 or 3, R4 is alkyl having 1-4 C atoms or alkoxyalkyl having 2-5 C atoms, R5 is H, alkoxy having 1-4 C atoms, halogen, NO or NO2 and L is a luminophoric moiety in a position para or meta to the nitrogen, or is the group having the general Formula IV: where R6 is alkyl having 1-3 C atoms or phenyl, R7 is H, alkoxy having 1-4 C atoms, halogen, NO or NO2 and L is a luminophoric moiety in a position para

Abstract: The present invention provides a 4-fluorosalicylic acid derivative represented by the following general formula (1): ##STR1## (wherein X.sup.1, X.sup.2 and X.sup.3 are each independently a hydrogen atom or a halogen atom with a proviso that there is no case in which all of X.sup.1, X.sup.2 and X.sup.3 are hydrogen atoms or fluorine atoms simultaneously); and a process for producing the above 4-fluoro-salicylic acid derivative.The 4-fluorosalicylic acid derivative of the present invention is a novel compound not described in any literature and is very suitable as a raw material for production of a 3-fluorophenol derivative (the 3-fluorophenol derivative is very useful as an intermediate for liquid crystal, recording material, medicine and agricultural chemical) because the 4-fluorosalicylic acid derivative can be easily converted to the 3-fluorophenol derivative.

Abstract: 1,7-Disubstituted perylene-3,4,9,10-tetracarboxylic dianhydrides I and perylene-3,4,9,10-tetracarboxylic acids Ia ##STR1## where R is substituted or unsubstituted aryloxy, arylthio, hetaryloxy or hetarylthio,their preparation and use as pigments, laser dyes and precursors for preparing fluorescent dyes, polymeric colorants, pigments and pigment additives, and 1,7-disubstituted perylene-3,4,9,10-tetracarboxylic diimides (VI) as intermediates thereof.

Abstract: Compounds which can chelate paramagnetic bi- and trivalent metal ions, their chelates with said metal ions and their use as contrast agents in magnetic resonance imaging (MRI), the compounds having formula (I) ##STR1## wherein R is a --(CH.sub.2).sub.m --O--R.sub.2 group or hydrogen,R.sub.2 is a (C.sub.6 -C.sub.10) aryl, or an alkyl(C.sub.1 -C.sub.5)-aryl(C.sub.6 -C.sub.10) group, substituted or not by a group L corresponding to a OH group or a OR.sub.3 group, wherein R.sub.3 is a linear or branched (C.sub.1 -C.sub.5) alkyl group; or L is NH.sub.2, halogen, COOH or CONR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 are independently hydrogen, or a linear or branched (C.sub.1 -C.sub.5) alkyl which can be substituted by 1-6 hydroxy groups and/or 1-6 alkoxy groups,R.sub.1 can have the same meanings as R, independently from it, except for hydrogen,Z is independently OH or OR.sub.6, or NR.sub.4 R.sub.5 wherein R.sub.4 and R.sub.5 are as previously defined, and R.sub.6 is a (C.sub.1 -C.sub.

Abstract: The present invention relates to phenethanolamine derivatives of formula (I) wherein R.sup.1 represents an aryl group optionally substituted by one or more substituents selected from halogen, hydroxy, C.sub.1-6 -alkoxy, C.sub.1-6 -alkyl, nitro, cyano, hydroxymethyl and trifluoromethyl; R.sup.2 represents hydrogen or C.sub.1-6 -alkyl; R.sup.3 represents a group (A) where the ring is substituted by one to four further substituents selected from C.sub.1-6 -alkyl, halogen, trifluoromethyl, and C.sub.1-6 -alkoxy; or R.sup.3 represents a group (B) where the aromatic ring is optionally substituted by up to three further substituents selected from C.sub.1-6 -alkyl, halogen, trifluoromethyl, and C.sub.1-6 -alkoxy; R.sup.4 represents hydrogen, or C.sub.1-6 -alkyl; R.sup.5 represents ZCH.sub.2 CO.sub.2 H wherein Z represents a bond, or O; Y represents (CH.sub.2).sub.

Abstract: A process is disclosed for producing an optical active alkoxybenzonitrile derivative in which process a benzonitrile derivative is subjected to condensation reaction with an optical active alcohol.A process is also disclosed for producing an optical active alkoxy benzoic acid derivative in which process a benzonitrile derivative is subjected to condensation reaction with an optical active alcohol and the reaction product thus derived is hydrolyzed.In these processes conversion of an optical active alcohol to tosylate or halide is not required and thus it is possible to produces producing an optical active alkoxybenzonitrile derivative and an optical active alkoxy benzoic acid derivative in a simple and inexpensive manner.

Abstract: Novel nonatetraenoic acid derivatives which selectively bind to retinoic acid X-receptors (RXR) and which have anti-acne acitvity and which potentiate the activity of retinoids having RAR.alpha. activity are disclosed.

Abstract: A process for preparation of crosslinked cellulosic products containing at least 30 wt. % cellulosic fibers and the polyanhydride crosslinked cellulosic products resulting therefrom wherein a cellulosic material is treated with an aqueous solution of a polycarboxylic acid formed by hydrolysis of a polyanhydride of the structure ##STR1## which comprises the reaction product of trimellitic anhydride and a diol in the mole ratio of from about 2.0:0.9 to about 2.0:1.1, wherein R is selected from the group consisting of alkyl, alkylene and cycloalkylene moieties of up to 12 carbon atoms and ethylene oxide and propylene oxide moieties of molecular weight up to about 6000, wherein said cellulosic material is impregnated with an aqueous solution of said polyanhydride, dried, and heated to a temperature of from about 120.degree. C. to about 200.degree. C.

Abstract: Methods, compositions, and compounds for modulating the activity of an endothelin peptide are provided. The methods use compositions that contain compounds of formula (I): ##STR1## where X and Y are selected from groups that include O, S, and NH; and Ar.sup.1, Ar.sup.2 and Ar.sup.3 are independently selected from substituted or unsubstituted groups that include 5 to 6 membered aryl groups and heteraryl groups that contain one or two heteroatom(s). The methods are effected by contacting endothelin receptors with one or more of the compounds or with compositions containing one or more of the compounds prior to, simultaneously with, or subsequent to contacting the receptors with an endothelin peptide.

Abstract: Matrix metalloprotease inhibiting compounds, pharmaceutical compositions thereof and a method of disease treatment using such compounds are presented. The compounds of the invention have the generalized formulas: ##STR1## where R.sup.15 is selected from the group comprising: HOCH.sub.2, (n--Pr).sub.2 NCH.sub.2, CH.sub.3 CO.sub.2 CH.sub.2, EtOCO.sub.2 CH.sub.2, HO(CH.sub.2).sub.2, CH.sub.3 CO.sub.2 (CH.sub.2).sub.2, HO.sub.2 C(CH.sub.2).sub.2, OHC(CH.sub.2).sub.3, HO(CH.sub.2).sub.4, 3--HO--Ph, and PhCH.sub.2 OCH.sub.2 ; and R.sup.

Abstract: The invention is novel analogs of 9-cis-retinoic acid which are useful for the treatment and prevention of coronary artery disease and to protect against premature atherosclerosis by increasing HDL levels. The invention includes processes for preparing the novel 9-cis-retinoic acid analogs.

Abstract: This invention relates to novel carboxylic acid indole compounds and compositions for use in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: Cyano and carboxy derivatives of substituted styrenes are inhibitors of tumor necrosis factor .alpha., nuclear factor .kappa.B, and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3,3-bis-(3,4-dimethoxyphenyl)acrylonitrile.

Abstract: Compounds of the formulaY.sub.3 (R.sub.4)--X--Y.sub.1 (R.sub.1 R.sub.2)--Z--Y.sub.2 (R.sub.2)--A--Bwhere the symbols have the meaning defined in the specification, have retinoid, retinoid antagonist or retinoid inverse agonist type biological activity.

Abstract: Nucleophilic substitution reactions on halobenzenes are carried out in the presence of catalysts. In particular the present invention provides a process leading to optionally substituted hydroxybenzoic and alkoxybenzoic acids and optionally substituted hydroxybenzonitriles and alkoxybenzonitriles from substituted 2,6-dihalobenzenes.

Abstract: Enantiomerically substantially pure compounds of the formula ##STR1## where R is H or lower alkyl of 1 to 6 carbons, or pharmaceutically acceptable salts thereof have retinoid-like biological activity. The enantimerically pure or substantially pure compound of the above formula where R is H, or a pharmaceutically acceptable salt thereof, is highly specific agonist of RXR retinoid receptors in preference over RAR receptors.

Abstract: The present invention relates to novel derivatives of 3-hydroxyanthranilic acid, 3-HANA, of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and selected from H and alkyl; X and Y are the same or different and selected from alkoxy, aryloxy, alkyl, alkylthio, arylthio, fluoroalkyl, halogen, cyano, OCF.sub.3 and SCF.sub.3 with the proviso that the compound of formula I wherein R.sub.1 and R.sup.2 =H, X=Br and Y=Me is excluded;or a pharmaceutically acceptable salt thereof, methods and intermediates for their preparation, novel pharmaceutical compositions and the use thereof for inhibiting the enzyme 3-hydroxyanthranilate oxygenase, 3-HAO, responsible for the production of the endogenous neurotoxin quinolinic acid, QUIN.

Abstract: This invention relates to canvanine analogs, their pharmaceutical compositions, and a method for treatment of cancer, particularly pancreatic cancer.

Abstract: Amino acid derivatives of formula (Ia) and (Ib) and pro-drugs thereof containing a group responsible for chelating the zinc atom of enkephalinase and angiotensin convertase enzymes are disclosed as inhibitors of these enzymes.

Abstract: Bridged bicyclic aromatic compounds are provided having the structure ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n are as defined herein. The novel compounds are useful for modulating gene expression of retinoic acid receptors, vitamin D receptors and thyroid receptors. Pharmaceutical compositions and methods for modulating gene expression are provided as well.

Abstract: Compounds of formula (I) wherein R.sup.1 -R.sup.7, R.sup.10, X and the dotted bond have the meaning given in the specification, bind selectively to retinoid RXR receptors and are useful as antiproliferative agents for dermatological and oncological indications.

Abstract: Process for the preparation of 3-phenylpropionic acid in which 3-phenylpropanal is subjected to an oxidation, at elevated temperature, in particular at a temperature of between 40.degree. and 80.degree. C., using a medium containing molecular oxygen. A high degree of conversion and a high selectivity are obtained. The starting material 3-phenylpropanal can be prepared in a suitable manner through the hydrogenation of cinnamaldehyde in the presence of a Pd-containing catalyst, after which the reaction mixture obtained can without intermediate further processing be used in the oxidation reaction. The combination of the two process steps constitutes a simple, commercially attractive process for the preparation of 3-phenylpropionic acid using cinnamaldehyde as a starting material. 3-phenylpropionic acid can be used in particular in the preparation of pharmaceuticals such as HIV protease inhibitors.

Abstract: The present invention provides a compound of the formula ##STR1## which inhibit squalene synthetase and cholesterol biosynthesis and are useful in the treatment of e.g., hyperlipidaemia, atherosclerosis, or fungal infections, processes for the preparation of the compounds of the invention, intermediates useful in these processes, and pharmaceutical compositions containing the compounds.