Abstract: An ultraviolet ray protection agent including a compound having an ultraviolet ray protection effect as an active ingredient. The compound is expressed by general formula I?: wherein X represents NH or O; Y? represents a vinyl group substituted by a methyl group or a phenyl group, or a phenyl group substituted by a methoxy group or a fluorine atom, or a naphthyl group; and Z represents a phenyl group substituted by a methyl group, a carboxyl group or a nitro group, or a naphthyl group. The compound represented by the general formula I? includes both novel compounds of the present invention and known compounds. The ultraviolet ray protection agent of the present invention offers outstanding ultraviolet ray protection effectiveness and is very safe.

Abstract: The present invention concerns 2,6-quinolinyl and 2,6-naphthyl derivatives of formula (I), processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals for the treatment of VLA-4 dependent inflammatory diseases such as for example asthma, allergic rhinitis, sinusitis, conjunctivitis, food allergy, psoriasis, urticaria, pruritus, eczema, rheumatoid arthritis, inflammatory bowel disease, multiple sclerosis and atherosclerosis. Formula (I): wherein X is N or CH.

Abstract: [PROBLEMS] To provide a method by which desired optically active carboxylic acids may be prepared from a carboxylic acid having a carbon-carbon double bond through asymmetric hydrogenation with a catalyst consisting of a transition metal complex containing a water-soluble ligand and which permits easy separation of the used catalyst from the product by liquid-liquid separation alone and enables the recovery of an expensive transition metal and the reuse of the catalyst. [MEANS FOR SOLVING PROBLEMS] Phosphines represented by the general formula (1): wherein X1 is oxygen or methylene; X2 is methylene, ethylene, trimethylene, 1,2-dimethylethylene, isopropylidene, or difluoromethylene; A is a Group IA alkali metal of the periodic table, hydrogen, or an ammonium ion; and a, b, c and d are each an integer of 0 or 1, with the proviso that the cases wherein the sum of a, b, c, and d is 0 are excepted.

Abstract: A compound of the formula [I] wherein R1 is optionally substituted aryl group or optionally substituted heteroaryl group; R2 is optionally substituted C1-6 alkyl group, C3-7 cycloalkyl group and the like; R3 is hydrogen atom, C1-6 alkyl group, hydroxyl group and the like; R4 is hydrogen atom, C1-6 alkyl group and the like; R5 and R6 are each C1-6 alkyl group and the like; R7 is optionally substituted aryl group or optionally substituted heteroaryl group; X1, X2 and X3 are each C1-6 alkylene group and the like; and X4 and X5 are each a single bond, methylene group and the like, a salt thereof, a solvate thereof or a prodrug thereof, and a pharmaceutical composition containing the compound, particularly a calcium receptor antagonist and a therapeutic agent for osteoporosis, are provided.

Abstract: A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I? wherein X, A1, A2, A3, A4, R, R?, R1 and R2 are as described in the specification.

Abstract: The present invention provides compounds of Formula (I): or a stereoisomer or pharmaceutically acceptable salt form thereof, wherein the variables A, R1, R2, R3, R4, Z, U, X, Y, Za, and n are defined are as defined herein, which are useful as inhibitors of matrix metalloproteinases (MMP) and/or TNF-? converting enzyme (TACE), or a combination thereof.

Abstract: The present invention concerns novel pharmaceutically active compounds, pharmaceutical compositions containing the same, the compounds for use as medicaments, and use of the compounds for the manufacture of specific medicaments. The present invention also concerns a method of treatment involving administration of the compounds. Specifically, the compounds are pharmaceutically acceptable salts of tolterodine or hydroxytolterodine, wherein the salt is of an acid selected from the group consisting of aliphatic mono- and dicarboxylic acids comprising from 7 to 24 carbon atoms, alkanedisulfonic acids comprising from 2 to 4 carbon atoms, naphthoic acid derivatives comprising from 11 to 27 carbon atoms, maleic acid and fumaric acid.

Abstract: Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.

Abstract: Methods and compositions for treating various disorders by administering a therapeutically effective amount of a retinoic acid receptor antagonist alone or in combination or in conjunction with other therapeutic agents to promote angiogenesis are provided. Also provided are methods for obtaining additional retinoic acid receptor antagonists for use as therapeutic agents to promote angiogenesis.

Abstract: Dimer-selective RXR modulator compounds having agonist, partial agonist and/or antagonist activity in the context of an RXR homodimer and/or RXR heterodimers are provided. Also provided are pharmaceutical compositions incorporating such dimer-selective RXR modulator compounds and methods for their therapeutic use.

Abstract: A compound of formula 1a 1

Abstract: A process for producing a high purity aromatic polycarboxylic acid by purifying a crude aromatic polycarboxylic acid in accordance with the steps of (I) forming an amine salt of an aromatic polycarboxylic acid from the crude polycarboxylic acid and an amine, (II) continuously decomposing the salt in a salt decomposition reactor in operations of (i) supplying an aqueous solution of the amine salt of an organic polycarboxylic acid formed in the step of forming a salt, (ii) removing the amine and water by distillation under heating and (iii) taking out a slurry containing crystallized aromatic polycarboxylic acid, and (III) separating and recovering crystals of the aromatic polycarboxylic acid from the slurry which is taken out in the step of decomposing the salt.

Abstract: The present invention concerns novel pharmaceutically active compounds, pharmaceutical compositions containing the same, the compounds for use as medicaments, and use of the compounds for the manufacture of specific medicaments. The present invention also concerns a method of treatment involving administration of the compounds.

Abstract: This invention relates to novel potent PPAR-alpha-activating compounds which are useful in the treatment of diseases such as coronary heart disease. The invention also relates to methods of preparation of PPAR-alpha-activating compounds.

Abstract: Process of treatment of mammals, including humans to treat diseases or conditions of the type which are normally treated with retinoid-like compounds is disclosed, with pharmaceutical compositions containing an active compound which is a selective agonist of the RXR retinoid receptor sites in preference to the RAR retinoid receptor sites. A compound is defined to be a selective agonist of the RXR receptor site if the compound is at least approximately ten times more effective as an agonist in the RXR receptor sites than in the RAR receptor sites.

Abstract: The invention relates to a method for carrying out CC-coupling reactions, in particular a Heck and Suzuki reaction, in the presence of supported palladium as the catalyst and a base in a monophase or multiphase solvent mixture. According to said method, palladium detaches itself from the support in a characteristic manner, is redeposited after the reaction and the quantity of palladium not deposited after the reaction is significantly lower than 5000 ppm, in relation to the palladium used.

Abstract: The present invention provides aromatic diamine/aromatic dicarboxylate having the following formula (I) NH2—Ar1—NH2.HOOC—Ar2—COOH  (I) wherein each symbol is as defined in the specification, which is in the form of particles having a median diameter of 5-100 &mgr;m and whiteness of not less than 75. This salt has high polymerizability and preferably has superior storage stability. Therefore, it can be preferably used for the production of polybenzazole that can be formed into a fiber and a film having high strength, high elastic modulus and high heat resistance.

Abstract: The present invention relates to new cinnamic acid salts of salmeterol, processes for the preparation thereof as well as the use thereof as pharmaceutical compositions.

Abstract: Compounds of the formula wherein R1 is a residue of the formula and R2-R10 have the significance given in the specification can be used as pharmaceuticals, particularly for the repair of photodamaged skin, other dermatological conditions, and oncological indications.

Abstract: Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, pyrrole, and polyenoic acid derivatives including carbocyclic polyenoic acids. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.

Abstract: The invention relates to novel bicyclic aromatic compounds which have the general formula (I): 1

Abstract: Fluoroquinolonecarboxylic acids can be prepared by hydrolysis of the corresponding C1-C4-alkyl esters with addition of water, acetic acid, and sulfuric acid using a drastically reduced amount of sulfuric acid if, relative to 1 mol of C1-C4-alkyl fluoroquinolonecarboxylate, less than 30 g of sulfuric acid are employed, the reaction mixture is heated to reflux for 0.5 to 8 hours, then a mixture of acetic acid, C1-C4-alkyl acetate, C1-C4-alkyl alcohol, and optionally water is distilled off, and finally the fluoroquinolonecarboxylic acid prepared is isolated.

Abstract: Phenylalkanoic acid derivatives of formula (1) are described: wherein Ar1 is an aromatic or heteroaromatic group; L1 is a covalent bond or a linker atom or group; A is an optionally substituted aliphatic, heteroaliphatic, cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; R is a carboxylic acid (—CO2H) or a derivative thereof; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of alpha 4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.

Abstract: A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I′ wherein X, A1, A2, A3, A4, R, R″, R1 and R2 are as described in the specification.

Abstract: The objective of this invention is to provide fluorescent compounds comprising a naphthalene skeleton, an electron donating group substituted at the 2- or 1-position of the naphthalene skeleton, and an electron attractive group substituted at the 6- or 4-position of the skeleton. The fluorescent compound of this invention is capable of emitting visible light having a desired color by choosing an appropriate combination of the electron donating group A, which has an electron-pushing function, and the electron attractive group B, which has an electron-pulling function.

Abstract: Disclosed is a process for disproportionation of potassium naphthoate to the dipotassium salt of 2,6-NDA which gives reproducible improved yields of up to 40% which comprises: a) reacting naphthoic acid in the presence of excess base to produce a disproportionation feed comprising a finely dispersed disordered salt mixture of excess base salts and naphthoic acid salts, wherein the feed is prepared by the steps of: (1) Reacting naphthoic acid in the presence of excess base selected from the group consisting of carbonates and bicarbonates to form a salt; (2) Drying said salt mixture by a method which forms a highly mixed disordered salt mixture characterized by a differential scanning calorimeter(DSC) signature characterized by low melting peaks not previously observed in the salt; and b) Disproportionating said solid salts in the presence of a disproportionation catalyst to form the dipotassium salts of 2,6-NDA.

Abstract: Compounds having Formula 8 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.

Abstract: The present invention provides a medicament exhibiting excellent retinoic acid receptor agonism. A Carboxylic acid derivative having a fused ring which is represented by the following formula or a pharmacologically acceptable salt thereof: {wherein the symbol represents a single bond or a double bond; X, Y, Z, P, Q, U, V and W are each a group represented by the formula: —O— or —S—, or a group represented by the formula: [wherein Rk (k: 1 to 8) is hydrogen, halogeno, optionally substituted lower alkyl or the like, with either of R7 and R8 being a group represented by the formula: (wherein A and B are each independently an optionally substituted aromatic hydrocarbon ring or an optionally substituted unsaturated heterocycle; and D is optionally protected carboxyl)]}.

Abstract: A propionic acid derivative having the following formula (II) and its salt: 1

Abstract: Disclosed is a process for preparing an optically active 1-aryl- or 2-aryl-alkylamines of formulas Ia, Ib and Ic with high optical purity and high yield. The process uses an optically active 1- or 2-naphthylglycolic acid of the general formula II as a resolving agent.

Abstract: Retinoid antagonist compounds have been found to be useful in the prevention and/or minimization of surgical adhesion formation. Also provided by the invention are certain novel substituted (5,6)-dihydronaphthalenyl compounds which are retinoid antagonists and possess the above-mentioned property in addition to their use as antiinflammatory agents for chronic skin inflammatory diseases, as agents for the treatment of rheumatic diseases and as agents for the treatment of various tumors as well as non-malignant proliferative skin conditions.

Abstract: Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, and pyrrole derivatives. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.

Abstract: Novel aromatic polycyclic retinoid-type derivatives of general formula (I), wherein groupings R3 and R4 attached to the double bond between carbons 11 and 12 are cis groupings, and pharmaceutical and cosmetic compositions containing same, are disclosed.

Abstract: Retinoid antagonist compounds have been found to be useful in the prevention and/or minimization of surgical adhesion formation.

Abstract: Compounds of formula I: as well as pharmaceutically acceptable salts, hydrates and esters thereof, are disclosed. The compounds are useful for treating or preventing prostaglandin mediated diseases. Pharmaceutical compositions containing such compounds and methods of treatment are also included.

Abstract: The invention concerns aromatic tetralcyclic compounds of the retinoid type of general formula (I). The invention also concerns the method for preparing them and the pharmaceutical compositions containing at least one of said compounds.

Abstract: Supported phase catalysts in which the support phase is highly polar, most preferably ethylene glycol or glycerol, are disclosed. An organometallic compound, preferably a metal complex of chiral sulfonated 2,2′-bis(diphenylphosphino)-1,1′-binaphthyl is dissolved in the support phase. Such supported phase catalysts are useful for asymmetric synthesis of optically active compounds, including the asymmetric hydrogenation of prochiral unsaturated carbon-hetero atom bonds, such as ketones, imines and beta-keto esters.

Abstract: A method is provided for preventing or reducing the risk of restenosis following angioplasty by administering a retinoid, such as an RXR-selective retinoid, e.g. the compound of the formula: and pharmaceutically acceptable salts and esters and amides thereof.

Abstract: The present invention relates to coding combinatorial chemical libraries synthesized on a plurality of solid supports by attaching “tags” that comprise fluorine containing compounds in combinations and/or ratios. The tags can be decoded while attached to the solid support by fluorine nuclear magnetic resonance spectroscopy to follow the reaction history of individual beads, and to determine the particular member of the library that is attached on the bead.

Abstract: The present invention provides particles of naphthalenedicarboxylic acid (NDA) exhibiting excellent slurry fluidity, which have an EG slurry property value of 2.7 or below, the above EG slurry property value being defined as a molar ratio of ethylene glycol (EG) to NDA (moles of EG/moles of NDA) of a slurry composed of a mixture of NDA and EG, the above slurry having a viscosity of 1000 cP as measured by Brookfield viscometer. The use of the above naphthalenedicarboxylic acid particles as a raw material for the production of polyethylene naphthalate is advantageous not only from the economic point of view but also in scarcely forming reaction products which deteriorate the quality of polyethylene naphthalate.

Abstract: A new family of inadone and tetralone tubulin-binding compounds (TBs) is disclosed. Unlike classical TBs, which inhibit mitosis among affected dividing cells, the TBs of the invention possess two unique properties: (1) they induce apoptosis among stationary phase (non-dividing) malignant cells, yet do not impair the viability of normal nonproliferating cells; and, (2) they affect cells which have acquired MDR more powerfully than they affect cells without MDR. Thus, the TBs of the invention provide means to target malignant cells for chemotherapy, even after previous therapies have failed, without affecting normal cells and tissues in the host.

Abstract: Process for the preparation of .alpha.-alkoxy-.alpha.-trifluoromethyl-arylacetic esters of the formula (I) ##STR1## wherein R is a component selected from the group consisting of C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.6 -C.sub.10 -aryl and C.sub.1 -C.sub.6 -halogenoalkyl, R' is selected from the group consisting of C.sub.1 -C.sub.4 -alkyl, X is selected from the group consisting of halogen, C.sub.1 -C.sub.4 -alkyl, C.sub.2 -C.sub.4 -alkenyl, C.sub.6 -C.sub.10 -aryl or C.sub.1 -C.sub.4 -alkoxy and nitro, and n is zero or an integer from 1 to 3.

Abstract: The present invention relates to a TEMPO-catalyzed oxidation of primary alcohols, RCH.sub.2 OH to corresponding carboxylic acids, RCOOH in the presence of catalytic in the presence of catalytic amount of NaClO and stoichiometric amount of NaClO.sub.2 as an oxidant.

Abstract: The present invention relates to specific adamantyl or adamantyl group derivative containing retinoid compounds induce apoptosis of cancer cells. These adamantyl retinoid derivatives are useful for the treatment of many cancers and solid tumors, especially androgen-independent prostate cancer, skin cancer, pancreatic carcinomas, colon cancer, melanoma, ovarian cancer, liver cancer, small cell lung carcinoma, non-small cell lung carcinoma, cervical carcinoma, brain cancer, bladder cancer, breast cancer, neuroblastoma/glioblastoma, and leukemia. Also, the invention relates to novel adamantyl or adamantyl group derivative compounds which are useful as active agents for the treatment or prevention of keratinization disorders and other dermatological conditions, and other diseases.

Abstract: Methods for reducing the fouling of process equipment used in the manufacture of aromatic compounds such as dimethyl-2,6-naphthalenedicarboxylate are disclosed. The methods require treating manufacturing process streams with a metal complexing agent. Novel compositions useful in the manufacture of aromatic materials such as dimethyl-2,6-naphthalenedicarboxylate also are disclosed.

Abstract: Dienoic retinoids having activity for retinoid X receptors or are panagonists on retinoic acid receptors and retinoid X receptors are provided. Also provided are pharmaceutical compositions incorporating such compounds and methods for their therapeutic use.

Abstract: The invention provides polymerizable dental, compounds, compositions, including the compounds and products for mixing the compositions and methods of using the compositions. Aryl acid compounds are provided in accordance with the invention. The compositions include at least one polymerizable aryl acid compound, an effective amount of a polymerization initiator, and at least 10 percent by weight of ceramic, metal and/or metal oxide filler particles having a particle size less than 500 microns. The dental products of the invention include a polymerizable composition in an enclosure having at least two chambers separated by a wall adapted to be ruptured prior to or during mixing of the composition. Compositions of the invention are preferred for use in these enclosures. Core build up material including a polymerizable acid containing compound is used to support dental crowns and adhere them to teeth in accordance with the invention.

Abstract: Certain novel substituted (5,6)-dihydroanthracenyl compounds of the general formula ##STR1## wherein A, n, p, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined in the specification exhibit retinoid-like properties and are particularly useful in the prevention of post-surgical adhesions.

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: Novel pharmaceutically/cosmetically-active aromatic polyenic compounds have the structural formula (I): and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.