Abstract: Compounds particularly for use in an autoimmune inflammatory disease and especially the treatment of inflammatory bowel disease have the absolute stereochemistry and formula: In some cases R1 is leucine and R is selected from: OH, OCH3, OCH2CH3, OCH2CH2CH3, NH2, NHCH2CH2OH, NHCH3, N(CH3)2, NH(4-OH-3-benzoic acid).

Abstract: A compound obtained by reaction of one or more amines of general formula NHR6R7 with a benzophenone derivative of the following general formula (IX) wherein M is a group comprising a number z of (meth)acrylate groups equal to at least one, L is a linker, G is linker comprising a number p? of unreacted hydroxyl groups, and R, R? and R?? are optional substituents as well as inks, coating compositions and adhesives comprising the same.

Abstract: The invention describes novel direct synthesis methods for converting a precursor into a PET-tracer with a 18F-fluoromethoxy-group. The invention is also directed to novel and stable precursors for the direct radiosynthesis of protected derivatives of O—([18F]Fluoromethyl)tyrosines.

Abstract: Methods of making polyglycerol based UV-filters, topical compositions comprising such polyglycerol based UV-filters and the use of such novel polyglycerol based UV-filters to enhance the solubility of butyl methoxydibenzoylmethane or bis-ethylhexyloxyphenol methoxyphenyl triazine in cosmetic oils are provided.

Abstract: The invention relates to a process for obtaining 3,3-diphenylpropylamines of general formula (I), particularly Fesoterodine, as well as their enantiomers, solvates and salts, comprising a chemoselective reduction of the acid group against the ester group in compounds of general formula (V), wherein R1 is C1-C8 alkyl; and R3 and R4, independently of one another, represent H or C1-C8 alkyl, or together form a ring of 3 to 7 members with the nitrogen to which they are bound. The invention also relates to the compounds of formula (V), as well as their enantiomers, solvates and salts.

Abstract: Compounds particularly for use in an autoimmune inflammatory disease and especially the treatment of inflammatory bowel disease have the formula: wherein R is selected from one or more of the same or different of hydrogen, hydroxyl, optionally substituted alkyl, optionally substituted aryl, alkoxy, aryloxy, thiol, and optionally substituted amino, and wherein R1 is selected from one or more of the same or different of hydrogen, acetyl, optionally substituted alkyl, optionally substituted aryl, and an amino acid selected from leucine, valine, isoleucine, and glycine.

Abstract: Disclosed are novel ultraviolet-absorbing compounds produced by two embodiments. By a first embodiment, the ultraviolet-absorbing compound is derived from at a first reactant being a UV absorber comprising a carbon-nitrogen triple bond and a second reactant having amine functionality. By a second embodiment, the ultraviolet-absorbing compound is derived from a first reactant being a UV absorber comprising amine functionality and a second reactant comprising a carbon-nitrogen triple bond. In both embodiments of the invention, the second reactant may be a small molecule, a monomer, a macromolecule, a biomolecule, or a polymer. The invention's ultraviolet-absorbing compounds are directed toward formulations and applications that serve to protect against UV radiation in any art.

Abstract: The present invention provides a compound useful as a synthetic intermediate for an anti-HIV agent having an integrase inhibitory activity, and a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate. Specifically, for example, a compound represented by the formula (2?): wherein R is a fluorine atom or a methoxy group, and R400 is a hydrogen atom or a C1-C4 alkyl group, or a salt thereof, and a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate.

Abstract: The invention relates to novel polyglycerol based UV-filters as well as to topical compositions comprising such novel polyglycerol based UV-filters. Furthermore, the invention relates to the use of such novel polyglycerol based UV-filters to enhance the solubility of butyl methoxydibenzoylmethane or bis-ethylhexyloxyphenol methoxyphenyl triazine in cosmetic oils.

Abstract: Disclosed are novel compounds and compositions for inhibition of androgen and estrogen receptor signaling, methods for inhibiting androgen signaling, methods for inhibiting estrogen signaling, methods for inhibiting the interaction between a co-regulatory protein and an androgen or estrogen receptor, and methods for treating cancer.

Abstract: A multifunctional Type II photoinitiator according to Formula (I): wherein X represents a structural moiety according to Formula (II): wherein: A represents a Norrish Type II initiating group; and L represents a divalent linking group positioning the Norrish Type II initiating group A and the CR2R3-group in a 1-5 to a 1-9 position wherein position 1 is defined as the first atom in the aromatic or alicyclic ring of A to which L is covalently bonded and the position 5 to 9 is defined as the carbon atom of the CR2R3-group to which L is covalently bonded, with the proviso that L does not contain an amine. Radiation curable compositions and inks include the multifunctional Type II photoinitiator.

Abstract: Disclosed are novel ultraviolet-absorbing compounds produced by two embodiments. By a first embodiment, the ultraviolet-absorbing compound is derived from at a first reactant being a UV absorber comprising a carbon-nitrogen triple bond and a second reactant having amine functionality. By a second embodiment, the ultraviolet-absorbing compound is derived from a first reactant being a UV absorber comprising amine functionality and a second reactant comprising a carbon-nitrogen triple bond. In both embodiments of the invention, the second reactant may be a small molecule, a monomer, a macromolecule, a biomolecule, or a polymer. The invention's ultraviolet-absorbing compounds are directed toward formulations and applications that serve to protect against UV radiation in any art.

Abstract: A benzophenone compound, and an ink composition that includes the benzophenone compound can absorb UV light, and thus improve lightfastness of images produced with the ink composition containing the compound. Due to the function of the benzophenone compound as a lightfast dispersant, the dispersibility and the lightfastness of an ink composition are improved with the benzophenone compound, without requiring an additional lightfastness enhancer.

Abstract: Biphenylcarboxamide compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.

Abstract: The invention relates to phenoxypropanolamines, to pharmaceutical compositions containing them, to processes for preparing them, and to the method of use thereof in the treatment of diseases that are improved by beta-3 agonist action.

Abstract: The invention relates to the use of novel anthracene based compounds for the inhibition or prevention of the growth or multiplication of cancer cells, and to therapeutic compositions containing such compounds. The invention relates more specifically to the use of hydroanthracene based compounds for the inhibition and/or prevention of cancer of the colon, pancreas, prostate, lung, larynx, ovary, breast, glioblastoma, oral cavity, endothelial cells and leukemias. The agents of the invention form a distinct class, distinct from the anthracene, anthrone or anthraquinone derivatives.

Abstract: Inhibitors of the cytosolic phospholypase A2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases. The inhibitors of the present invention have the general formula wherein X, Z, X1, R1, R2, Ra, Rb, R3, R4 and Y are as defined in the specification.

Abstract: Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-? and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.

Abstract: A lightfast additive and an ink composition including the same include a benzophenone moiety for lightfastness and a moiety for wettability and the ability to stabilize a colorant, wherein the two moieties are covalently bonded. The lightfast additive may exhibit effective ultraviolet (UV) light absorption capacity, effective wettability, and an ability to stabilize a colorant. The ink composition utilizing the light fast additive thus has an improved lightfastness and long-term storage stability.

Abstract: A benzophenone compound, and an ink composition that includes the benzophenone compound can absorb UV light, and thus improve lightfastness of images produced with the ink composition containing the compound. Due to the function of the benzophenone compound as a lightfast dispersant, the dispersibility and the lightfastness of an ink composition are improved with the benzophenone compound, without requiring an additional lightfastness enhancer.

Abstract: The invention relates to a method for producing derivatives of 3,3-diarylpropylamines of general formula (I) and sterically highly pure, stable intermediate products, and to their use for producing pharmaceutical compositions.

Abstract: The present invention relates to novel thyroid receptor ligands and, more particularly, relates to malonamic acids and derivatives thereof of Formula I, which are useful in the treatment of obesity, overweight condition, hyperlipidemia, glaucoma, cardiac arrhythmias, skin disorders, thyroid disease, hypothyroidism, thyroid cancer and related disorders and diseases such as diabetes mellitus, atherosclerosis, hypertension, coronary heart disease, congestive heart failure, hypercholesteremia, depression, osteoporosis and hair loss. The present invention also provides methods, pharmaceutical compositions and kits for treating such diseases and disorders.

Abstract: The present invention relates to an anthranilic acid derivative expressed by the following formula (1) or the following formula (2), or its pharmacologically permissible salt or solvate.

Abstract: Shock is a life threatening complication in situations associated with trauma including burns, surgery, ischemia, sepsis, and other critical care applications. Shock is induced by pancreatic proteases when they are released into the small intestine when the tissue is compromised due to trauma. Administration of protease inhibitors into the small intestine, either orally, intraveneously, or by direct lavage, was demonstrated to prevent shock in rats as determined by both survival time and molecular and histological analysis.

Abstract: Novel calcilytic compounds, pharmaceuticals compositions cotaining said compounds and their use as calcium receptor antagonists.

Abstract: A new method for producing unsymmetrically substituted fluorenyl compounds, one step of which is the preparation of 2,7-disubstituted fluoren-9-one derivatives via the nucleophilic substitution of a compound of the formula D wherein A′ is selected from the group consisting of —Br, —Cl, —F, —NO2, and —CN; A is selected from the group consisting of —NO2, —CN, —CO2R, —C(O)R, —SO2R, —SO2RF, —C(CN)═C(CN)2 and —CH═C(CN)2; RF is —CpF2p+1, p=from about 0 to about 10; R is an straight, branched or cyclic aliphatic alkyl group having about 1 to 10 carbon atoms, or an aromatic group such as phenyl or naphthyl; and is a carbonyl or a protected carbonyl such as a ketal or thio-ketal such as wherein R′ is —CrH2r+1; R″ is —(CH2)r—; and r is independently 2 or 3, with a nucleophilic reagent in the presence of an aprotic solvent

Abstract: A method of imparting a water repellent surface to a hydrophilic substrate which comprises contacting the substrate with a solution or dispersion of a suitable calixarene in a liquid medium.

Abstract: A method of selectively controlling undesirable vegetation in crops by using a postemergent application of an herbicidally effective amount of a metal chelate of a 2-(substituted benzoyl)-1,3-cyclohexanedione compound to the locus of such undesirable vegetation.

Abstract: The invention relates to 2-benzoylcyclohexane-1,3-diones of the formula I where R1, R2 are hydrogen, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, alkoxyalkyl, alkenyl, alkynyl, —OR5, —OCOR6, —OSO2R6, —SH, —S(O)nR7, —SO2OR5, —SO2NR5R8, —NR8SO2R6 or —NR8COR6; R3 is hydrogen, alkyl, haloalkyl, alkenyl or alkynyl; R4 is hydrogen, unsubstituted or substituted alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, —COR9, —CO2R9, —COSR9 or —CONR8R9; X is oxygen or sulfur; Z is oxygen or NR8; m is 0 or 1; n is 0, 1 or 2; R5 is hydrogen, alkyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl; R6 is alkyl or haloalkyl; R7 is alkyl, haloalkyl, alkoxyalkyl, alkenyl or alkynyl; R8 is hydrogen or alkyl; R9 is alkyl, alkenyl, alkynyl, phenyl or benzyl; R10 is alkyl, haloalkyl, alkenyl or alkynyl; Q is an unsubstituted or substituted cyclohexane-1,3-dione ring which is linked in the 2-position; where m is 1 if R3 is

Abstract: Described herein are compounds having the general formula: ##STR1## Ar.sub.1 and Ar.sub.2 are independently selected aryl groups, optionally substituted with substituents selected from the group consisting of alkyl, cycloalkyl, alkoxy, alkanoyl, aralkyl, aralkyloxy, halo, NO.sub.2, Ph, CF.sub.3, CN, OH, methylenedioxy, ethylenedioxy, SO.sub.2 NRR', NRR', CO.sub.2 R (where R and R' are independently selected from the group consisting of H and alkyl) and a second aryl group, which may be substituted as above;wherein any cycloalkyl or aryl substituent is linked to Ar.sub.1 or Ar.sub.2 by a bridging element which may be a single bond, a vinylene group, an ethynylene group, a Z group, a --Z--(CH.sub.2).sub.n -- group, a --(CH.sub.2).sub.n --Z-- group, or a --Z--(CH.sub.2).sub.n --Z-- group, where Z represents an O atom, a S atom, an NH group or an N-alkyl group, and n is an integer from 1 to 4;wherein Ar.sub.1 and Ar.sub.

Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.

Abstract: Cationic azo dyes of the formula I ##STR1## where the variables are as defined in the specification, amines as their intermediates, processes for preparing them, their use for dyeing and printing natural or synthtic substrates, and their mixtures are described.

Abstract: A method for preparing carbamoylmethylurea derivatives of the formula (I): ##STR1## characterized by reacting a compound of the formula (II): ##STR2## with a compound of the formula (III): ##STR3##

Abstract: A naphthyloxyacetic acid derivative of the formula (I) ##STR1## wherein R.sup.1 is H, alkyl, alkylene-(--COOR.sup.10, --OH, --CONR.sup.4 R.sup.5, --CONR.sup.6 -alkylene-OH, --NR.sup.4 R.sup.5, -cyano or -tetrazolyl); A is single bond, alkylene, alkenylene, --S-alkylene, --O-alkylene; B is NR.sup.3 CO, CONR.sup.3 ; R.sup.2 is (1) alkyl (2) alkenyl, (3) alkyl or alkenyl substituted by 1-3 of phenyl, cycloalkyl, naphthyl and heterocyclic ring containing nitrogen atom (the said ring may be substituted by 1-3 of alkyl, alkoxy and halogen etc.), (4) NR.sup.7 R.sup.8 or (5) alkylene-NR.sup.7 R.sup.8 ; non-toxic salt thereof, non-toxic acid addition salt thereof and hydrate thereof can bind the PGE.sub.2 receptor and exhibits the activity to antagonize or agonize for PGE.sub.2., therefore, they are useful as PGE.sub.2 antagonist or PGE.sub.2 agonist.

Abstract: A class of novel phenyl glyoxamides is disclosed together with the use of such compounds for inhibiting sPLA.sub.2 mediated release of fatty acids for treatment of conditions such as septic shock.

Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof wherein: R.sup.1 to R.sup.9 are as defined herein and m is the integer 0 or 1.These compounds are beta 3 adrenergic receptor agonists and are useful, therefore for example, in the treatment of diabetes, obesity, gastrointestinal diseases and achalasia.

Abstract: The present invention provides compounds of formula ##STR1## in which R represents an organic group, or a pharmaceutically acceptable metabolically labile ester or amide thereof, or a pharmaceutically acceptable salt thereof, which are useful as antagonists of one or more of the actions of L-glutamate at metabotropic excitatory amino acid receptors.

Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is R.sup.9 CR.sup.10 R.sup.11 or CH.sub.2 R.sup.9 CR.sup.10 R.sup.11 where R.sup.9 is H or OH and R.sup.10 and R.sup.11 are optionally substituted phenyl, optionally substituted benzyl, C.sub.5-7 cycoalkyl or (C.sub.5-7 cycloalkyl)methyl; R.sup.1 and R.sup.2 are H, optionally substituted C.sub.1-6 alkyl, optionally substituted phenyl(C.sub.1-4 alkyl), C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, COR.sup.a, COOR.sup.a, COC.sub.1-6 alkylhalo, COC.sub.1-6 alkylNR.sup.a R.sup.b, CONR.sup.12 C.sub.1-6 alkylCONR.sup.a R.sup.b, CONR.sup.a R.sup.b, or SO.sub.2 R.sup.a, or R.sup.1 and R.sup.2 together form a chain (CH.sub.2).sub.q optionally substituted by oxo where one methylene group may optionally be replaced by O or NR.sup.x ; R.sup.3 is H, C.sub.1-6 alkyl or C.sub.2-6 alkenyl; R.sup.4 is optionally substituted phenyl(C.sub.1-3 alkyl); X and Y are H, or X and Y together are .dbd.O; and Z is O, S, or NR.sup.7 ; are tachykinin antagonists.

Abstract: Compounds of the formula ##STR1## wherein the variables are defined in the specification. The compounds and their salts are soft anticholinergic/antisecretory agents especially useful as mydriatics and as antiperspirants.

Abstract: A pharmaceutical compound of the formula ##STR1## in which m is 0, 1 or 2, n and q are each 0 or 1 to 5, and p is 0 or 1, X is --CO.sub.2 H or tetrazolyl,Y is --CH.dbd.CH--, andZ is(i) phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted,(ii) --CHR.sup.1 R.sup.2 where R.sup.1 and R.sup.2 are each phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted,(iii) .dbd.CR.sup.1 R.sup.2 where R.sup.1 and R.sup.2 are each phenyl, naphthyl or thienyl, said phenyl, naphthyl and thienyl being optionally substituted, or(iv) ##STR2## where r is 0 or 1 to 3 and the phenyl rings are optionally substituted; provided that when Z is phenyl and m is 1, p is 1; and salts and esters thereof.

Abstract: Disclosed are compounds of Formula I: ##STR1## or a pharmaceutically acceptable salt or solvate thereof, wherein: R.sup.3 is alkyl, alkenyl, alkynyl, aryl, alkaryl, aralkyl, cycloalkyl, acyloxymethyl, alkoxy, alkoxymethyl, or alkyl substituted with cycloalkyl;R.sup.4 is H, alkyl, alkenyl, alkoxy, or --OH.Also disclosed are pharmaceutical compositions containing compounds of Formula I, methods for inhibiting tumor necrosis factor-.alpha. and methods for treating septic shock, inflammation, or allergic disease by administering a compound of Formula I.

Abstract: A fused benzeneoxyacetic acid derivative of the formula: ##STR1## wherein ##STR2## is (i) ##STR3## (ii) ##STR4## (iii) ##STR5## or (iv) ##STR6## A is (i) ##STR7## or (ii) ##STR8## R.sup.1 is hydrogen or C.sub.1-4 alkyl; R.sup.2 is hydrogen, C.sub.1-6 alkyl or phenyl;R.sup.3 is(i) C.sub.1-15 alkyl,(ii) C.sub.1-8 alkyl substituted by one or two of benzene, C.sub.4-7 cycloalkane or 4-7 ring-membered monocyclic ring which contains one nitrogen atom or(iii) C.sub.10-15 condensed tricyclic ring;e is 3-5;f is 1-3;p is 0-4;q is 0-2;s is 0-3With the proviso that, ring(s) in R.sup.3 may be substituted by one to three of C.sub.1-4 alkyl, .sub.1-4 alkoxy, halogen atom, nitro or trihalomethyl. And, when D--B is the formula (iii) or (iv), --(CH2)p- or .dbd.CH--(CH2)s- is attached at the position of a or b on the ring.

Abstract: Compounds containing at least one alkenyl group, at least one maleimide group and at least one rodlike mesogenic moiety are prepared by reacting one or more aminophenols containing one or more rodlike mesogenic moieties with a stoichiometric quantity of a maleic anhydride per amine group of said aminophenol and then alkenylating the resulting phenolic functional maleimide.

Abstract: Novel polycyanate compositions containing one or more mesogenic moieties as lateral substituents are disclosed which provide improved processability relative to polycyanates containing one or more mesogenic moieties in the main chain of the molecule. Molecular level ordering of the resulting thermosets is maintained much similar to that found thermosets of polycyanates which have one or more mesogenic moieties in the main chain.

Abstract: A diamine compound of the general formula ##STR1## wherein the arrows denote isomerism, R.sub.1 is a divalent aromatic group selected from the group consisting of ##STR2## R.sub.2 is a tetravalent aromatic group selected from the group consisting of ##STR3## and R.sub.4 is a monovalent aliphatic group selected from the group consisting of ethyl and isopropyl; and, a process for preparing same.

Abstract: Compounds having non-linear optical activity of the general formula ##STR1## wherein D and A are electron donor and acceptor groups, respectively, R.sup.1 and R.sup.2 are aromatic bridging groups, X and Y are preferably groups capable of partaking in polymerization reactions are suitable for use in polymer-based light modulator devices.

Abstract: The compounds are ethanolamine benzoate compounds useful for the treatment of syndrome X, and of hypertension in patients who are insulin resistant or have one or more metabolic anomalies.A compound disclosed is S-1-(m-trifluoromethylphenyl)-2-{.beta.-{4-[2-(N-(3,3-diphenylpropionyl)am ino)ethyl] benzoyloxy}ethylamino} propane.

Abstract: New ethanolamine benzoate compounds which can be used as medicaments and correspond to the formula: ##STR1## wherein R is as defined in the description, in the form of racemic compounds and enantiomers. These new compounds and their physiologically tolerable salts can be used therapeutically for treatment of insulin-resistance states.

Abstract: A method of preparing a compound of the formula ##STR1## in which R.sub.1 is CH.sub.3 or C.sub.2 H.sub.5,n is 0 to 4,m is 1 to 3,R.sub.2 is H, --COOR.sub.1, alkyl or aryl, andR.sub.3 and R.sub.4 each independently is H, alkyl or aryl,which comprises reacting an alkyl ester of a dicarboxylic acid of the formula R.sub.1 OOC--CR.sub.3 R.sub.4 --COOR.sub.1 with a nitrile of the formula N.tbd.C--(CH.sub.2).sub.m R.sub.2 and with hydrogen in the presence of a hydrogenation catalyst.

Abstract: The present invention relates to novel chromophore-containing compounds useful as sunscreen agents which have the ability to absorb both UVA and UVB wavelength radiation. These compounds comprise a specific type of UVA-absorbing chromophore covalently bonded to a specific type of UVB-absorbing chromophore. The chromophore moieties are covalently bonded together such that the electron systems of these moieties are directly coupled to thereby form a new chromophore.The present invention further relates to sunscreen compositions containing the hereinbefore described type of sunscreen agents. Furthermore, the present invention relates to methods for protecting the skin of humans or lower animals from the effects of UVA and UVB wavelength radiation. This method comprises topically applying to the skin an effective coating of a sunscreen composition of the present invention.