Abstract: The invention relates to novel cyclic imines of the formula (I) in which Ar1 and Ar2 each represent substituted phenyl and n represents 1, 2 and 3, to a plurality of processes for their preparation and to their use as pesticides.

Abstract: The present invention provides a compound of formula I wherein R1 is H, OH, halo, OCO(C1-C6 alkyl), OCO(aryl), OSO2(C4-C6 alkyl), OCOO(C1-C6 alkyl), OCOO(aryl), OCONH(C1-C6 alkyl), or OCON(C1-C6 alkyl)2; R2 is aryl, C1-C6 alkyl, C3-C6 cycloalkyl, or 4-cyclohexanol; R3 is O(CH2)2 or O(CH2)3; R4 and R5 are optionally CO(CH2)2CH3, CO(CH2)3CH3, C1-C6 alkyl, or R4 and R5 combine to form, with the nitrogen to which they are attached, piperidine, morpholine, pyrrolidine, 3-methylpyrrolidine, 3,3-dimethylpyrrolidine, 3,4-dimethylpyrrolidine, azepine, or pipecoline; and pharmaceutically acceptable salts thereof. The invention further provides pharmaceutical compositions containing compounds of formula I and methods of use for the compounds of formula I.

Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 1-benzyl-naphthyls which are &agr;-substituted with ether, thioether amino, cyano or halo that are useful for the treatment of the various medical indications associated with post-menopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus and cervix. The present invention further relates to intermediate compounds and processes useful for preparing the pharmaceutically active compounds of the present invention, and pharmaceutical compositions.

Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.

Abstract: Aliphatic maleimides and methods using the same are disclosed. Polymerization of compositions which include the compounds of the invention may be activated by irradiating the composition with radiation.

Abstract: The present invention is directed to pyrrolidine compounds of the formula I: (wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.

Abstract: 1 The present invention ocncerns new amidinopyrroline derivatives of formula (I) with the meanings of the symbols as given in the description as well as a process for their production and their use in pharmaceutical preparations.

Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, hydroxy, or the like; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl or the like; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, pyridyl, and the like, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, C1-C4 alkyl, or the like; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, and the like or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.

Abstract: The present invention describes novel nitrosated and/or nitrosylated nonsteroidal antiinflammatory compounds, and novel compositions comprising at least one nitrosated and/or nitrosylated nonsteroidal antiinflammatory compound, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase. The present invention also provides methods for treating, preventing and/or reducing inflammation, pain, and fever; decreasing or reversing the gastrointestinal, renal and other toxicities resulting from the use of nonsteroidal antiinflammatory drugs; treating and/or preventing gastrointestinal disorders; treating inflammatory disease states and disorders; and treating and/or preventing ophthalmic diseases or disorders.

Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, hydroxy, or the like; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl or the like; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, pyridyl, and the like, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, C1-C4 alkyl, or the like; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, and the like or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.

Abstract: A compound of the following formula: and the salts thereof, wherein A is hydrogen, halo, hydroxy, or the like; the broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl or the like; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, pyridyl, and the like, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, C1-C4 alkyl, or the like; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, and the like or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine, piperidine or morpholine ring. These compounds are useful as kappa agonists.

Abstract: The invention relates to novel cyclic imines of the formula (I) in which Ar1 and Ar2 each represent substituted phenyl and n represents 1, to a process for their preparation and to their use as pesticides.

Abstract: The present invention provides compounds having the structure: and pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.

Abstract: A fluorination method of oxygen and halogen sites with diaryl-, dialkoxyalkyl-, alkylalkoxyalkyl-, arylalkoxyalkyl- and cyclic aminosulfur trifluorides fluorinating reagents is disclosed.

Abstract: Diaryl-, dialkoxyalkyl-, alkylalkoxyalkyl-, arylalkoxyalkyl- and cyclic aminosulfur trifluorides fluorinating agents are disclosed.

Abstract: A compound of the following formula: and the salts thereof wherein A is hydrogen, halo, or hydroxy, broken line represents an optional double bond with proviso that if the broken line is a double bond, then A is absent; Ar1 is optionally substituted phenyl; Ar2 is aryl or heteroaryl selected from phenyl, napththyl, or pyridyl, the aryl or heteroaryl being optionally substituted; R1 is hydrogen, hydroxy, or C1-C4 alkyl; and R2 and R3 are independently selected from optionally substituted C1-C7 alkyl, C3-C6 cycloalkyl, C2-C6 alkenyl, C2-C6 alkynyl, or R2 and R3, together with the nitrogen atom to which they are attached, form an optionally substituted pyrrolidine. These compounds are useful as kappa agonists.

Abstract: The invention relates to a process for preparing chiral 3,4-dehydroproline compounds of formula (I), in which R, R' and R" have the meanings given in the description. The invention is characterized by a pyrrolecarboxylic acid derivative compound of formula (II) reacted first with an alkali or alkaline earth metal in ammonia and then with an aqueous salt solution or a compound of formula (III) in which X is a leaving group to form the final chiral product compound.

Abstract: Disclosed are compositions containing compounds of the formula (I) below wherein A,B,C,G,Q and R are defined herein. The compounds are useful as phosphotyrosine mimics that, when incorporated into an appropriate molecular structure, inhibit the binding of tyrosine kinase-dependent regulatory proteins to their native phosphotyrosine-containing ligands or receptors. Also disclosed are methods for preparing the compounds of the formula (I).

Abstract: 3-Pyrroline-2-carboxylic acid derivatives of the formula I ##STR1## are prepared by eliminating the sulfonic acid residue, with the aid of a base, from a compound of the formula II ##STR2##

Abstract: A fluorination method of oxygen and halogen sites with diaryl-, dialkoxyalkyl-, alkylalkoxyalkyl-, arylalkoxyalkyl- and cyclic aminosulfur trifluorides fluorinating reagents is disclosed.

Abstract: A process for preparing .alpha.-hydroxy acids by heating ammonium salts of .alpha.-hydroxy acids of general formula (I), removing the formed ammonia and water, adding water to the residue, and heating the obtained mixture, wherein R is hydrogen, C.sub.1 -C.sub.6 alkyl, alkyl(C.sub.1 -C.sub.6)thioalkyl (C.sub.1 -C.sub.6), phenyl or the like. This process is freed from the problem of disposal of by-products such as ammonium bisulfate and makes it possible to prepare a free .alpha.-hydroxy acid from an ammonium salt thereof economically and in a high yield.

Abstract: The present application describes amidinophenyl-pyrrolidines, -pyrrolines, and -isoxazolidines and derivatives thereof of formula I: ##STR1## or pharmaceutically acceptable salt forms thereof, wherein one of D and D' may be C(.dbd.NH)NH.sub.2 and the other H, and J.sup.1 and J.sup.2 may be O or CH.sub.2, which are useful as inhibitors of factor Xa.

Abstract: This invention relates to the field of pharmaceutical and organic chemistry and provides benzothiophene compounds, intermediates, formulations, and methods.

Abstract: Activating groups for cyanine dyes used to label chain terminators in nucleotide sequencing, based on N-hydroxyphthalimide, are disclosed. From these activating groups, activated dyes of the present Invention are prepared which react with the derivitized nucleotide chain terminators to give a labeled chain terminator of the present Invention. The activating groups of the present Invention allow the dye-chain terminator reaction to occur at a much higher yield and with much greater selectivity for the mono-substituted product, compared with the prior art.

Abstract: Method of treating or reducing the risk of human disease or condition in which the synthesis or oversynthesis of nitric oxide forms a contributory part wherein a therapeutically effective amount of the compound of formula (I) as defined in the specification is administered to a person suffering from or susceptible to such disease or condition.

Abstract: The present invention relates to the discovery of novel, low molecular weight, non-peptide inhibitors of matrix metalloproteinases (e.g. gelatinases, stromelysins and collagenases) and TNF-.alpha. converting enzyme (TACE, tumor necrosis factor-.alpha.

Abstract: The present invention provides compounds having the structure: ##STR1## and pharmaceutically acceptable salts and stereoisomers thereof that are useful in the treatment of inflammatory diseases which are mediated by LTB.sub.4 production, such as psoriasis, ulcerative colitis, IBD, and asthma.

Abstract: Compound of formula (I) are disclosed ##STR1## as well as optically active isomers or pharmacologically acceptable salts thereof. The compounds are useful active ingredients in pharmaceutical compositions, and methods of treating osteoporosis, inflammation or diseases which are due to thromboembolic events. Compounds of formula (II) are also disclosed ##STR2## which are useful as starting compounds for preparing compounds of formula (I).

Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.

Abstract: The invention relates to substituted ethyl .alpha.,.alpha.-diarylmethyl ether derivatives and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the same, and methods of treating cocaine addiction and overdose, and diseases and conditions characterized by abnormal dopaminergic neurotransmission, using the same.

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 is selected from alkylthio, arylthio, aryloxy, halogen and cyano; R.sup.3, R.sup.4 are the same or different and selected from halogen, methyl, fluoroalkyl, cyano and Z--R.sup.5 wherein Z is selected from CH.sub.n, NH.sub.m, O, S, SO.sub.2 and CO wherein n=1 or 2; m=0 or 1 and R.sup.5 is selected from alkyl, aryl and fluoroalkyl; or R.sup.3 and R.sup.4 together form a saturated or unsaturated ring system Y--V--Z wherein Y and Z, independently of each other, are as defined for Z above and V is selected from C.sub.1 -C.sub.3 alkylene or alkenylene, --N.dbd., --N.dbd.N-- and ##STR2## wherein R.sub.

Abstract: Organosilicon polymers, including crosslinked polymers and crosslinkable prepolymers, of cyclic polysiloxane, organic dyes, and, optionally, polyenes. The dyes include those with delocalized Pi electron systems linking electron donor groups and electron acceptor groups, and with at least two carbon-carbon double bond-containing pendant groups attached to at least two different sites from among the indicated delocalized Pi electron systems, donor groups, and acceptor groups.

Abstract: A perfluoro-cyclic imine represented by the formula: ##STR1## is produced by a method which comprises placing in a reaction vessel a perfluoro compound represented by the formula: ##STR2## wherein X stands for one member selected from among CF.sub.2, CF(CF.sub.3), and oxygen atom, M for one member selected from among monovalent alkali metal ions and alkaline earth metal ions, and n for 0, 1, or 2 and heating the perfluoro compound to a temperature in the approximate range of 100.degree. C. to 500.degree. C.

Abstract: Disclosed are methods for synthesizing very large collections of diverse pyrrolidine compounds and derivatives thereof on solid supports and synthetic compound libraries comprising pyrrolidine groups and derivatives thereof prepared by such methods.

Abstract: Disclosed are methods for synthesizing very large collections of diverse pyrrolidine compounds on solid supports and synthetic compound libraries comprising pyrrolidine groups prepared by such methods.

Abstract: A powder-form composition of 2-acetyl-1-pyrroline incorporated with a support of maltodextrin and/or cyclodextrin. The composition is prepared by hydrolyzing a 2-(1-alkoxyethenyl)-1-pyrroline with an acid to obtain a reaction medium, adding an equimolar amount of a base to the reaction medium to obtain a neutralized reaction medium containing 2-acetyl-1-pyrroline, combining maltodextrin and/or cyclodextrin with the neutralized reaction medium to obtain a support solution and freeze-drying the support solution to obtain the composition.

Abstract: A herbicidal composition having acivicin, its derivatives or salts or combinations thereof as its active component.A process for controlling unwanted plants comprising applying a herbicidally effective amount of acivicin, its derivatives or salts or combinations thereof to the unwanted plant.

Abstract: A synthetic polyamide of formula I and its salts ##STR1## in which each R.sub.1 independently is selected from hydrogen, carboxyl, amino or a group of formula .alpha.-A.sub.1 -R.sub.10 (.alpha.)where A, is a bridging group and R.sub.10 is a sterically hindered amine group;each R.sub.2 independently is hydrogen or a group of formula .alpha.A is a bridging group of the formula ##STR2## is 0 or 1; R.sub.3 is hydrogen, C.sub.1-12 alkyl or is a significance of R.sub.10 ;R.sub.5 is hydrogen or C.sub.1-12 alkylR.sub.4 is a significance of R.sub.10 or a group of formula .alpha.; andp is an integer from 5 to 200;with the proviso that the compound of formula I contains 1-400 sterically hindered amine groups.

Abstract: A process for preparing five-membered nitrogen heterocycles of the general formula I ##STR1## where R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 are hydrogen,R.sup.1 is C.sub.1 -C.sub.10 -alkyl, C.sub.1 -C.sub.10 -hydroxyalkyl, C.sub.1 -C.sub.10 -aminoalkyl, aryl, C.sub.7 -C.sub.10 -aralkyl and C.sub.7 -C.sub.10 -alkylaryl,R.sup.5 and R.sup.6 are C.sub.1 -C.sub.8 -alkyl,R.sup.2 and R.sup.3 together are oxygen with the proviso that R.sup.8 is hydrogen,R.sup.3 and R.sup.4 and/or R.sup.7 and R.sup.8 or R.sup.4 and R.sup.7 together are a bond,comprises reacting vinyloxiranes of the general formula II ##STR2## where R.sup.5 and R.sup.6 have the abovementioned meanings, with ammonia or primary amines of the general formula IIIR.sup.1 --NH.sub.2 (III),where R.sup.1 has the abovementioned meanings, in the presence of a compound of an element of Group VIIIb or Ib of the Periodic Table, with or without the addition of a Lewis acid, at from 20.degree. to 200.degree. C.

Abstract: The phenylalkan(en)oic acids of the formula: ##STR1## as defined herein, possess an antagonistic activity on leukotriene B.sub.4.

Abstract: 2-acetyl-1-pyrroline is prepared by hydrolyzing a 2-(1-alkoxyethenyl)-1-pyrroline compound with an acid to obtain a reaction medium and then adding an equimolar amount of a base to the reaction medium to obtain a neutralized reaction medium containing 2-acetyl-1-pyrroline.

Abstract: This invention relates to compounds having the following formula ##STR1## or a pharmaceutically acceptable salt which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions--of such phenyl amidines derivatives.

Abstract: There are provided important pyrroline and glycine intermediates, methods for the preparation of said intermediates and the use thereof in the manufacture of arylpyrrole insecticidal agents.

Abstract: This application describes 3-arylalkyl esters of 4,5-dihydro-9,10-dioxo-2-anthracenecarboxylic acid and a process for making them. Also described is a method of using the compounds in the treatment of arthritis.

Abstract: 2-(1-alkoxyethenyl)-1-pyrroline compounds. The compounds may be employed for preparing food flavorant compositions, and 2-(1-ethoxyethenyl)-1-pyrroline, in particular, has characteristics suiting it as a flavoring agent for food products.

Abstract: The subject of the present invention is compounds which correspond to the following general formula: ##STR1## in which R.sub.1 and R.sub.3 independently of one another represent H, an alkyl, alkenyl, cycloalkyl, aryl, arylalkyl or an alkylaryl group, a heterocycle, or groups which are unsubstituted or substituted, in particular by one or more hydroxyl or alkoxy groups or halogen;n represents an integer from 1 to 5;i in each case takes values from 1 to n for the n successive ##STR2## links; R.sub.2, R.sub.4.sup.i and R.sub.5.sup.i independently of one another represent H, an alkyl, alkenyl, aryl, alkoxy, hydroxyalkyl, alkoxyalkyl, amido, acyl or carboxyalkyl group, or a salt, or an alkyl ester of the latter; or R.sub.4.sup.i and R.sub.5.sup.i together form an oxo group ##STR3## R.sub.6 and R.sub.7 represent H, or R.sub.6 and R.sub.7 together form an oxo group ##STR4## x represents a 5- or 6-membered heterocycle which contains at least one nitrogen atom, or, in the event that ##STR5## where R.sub.8 and R.sub.

Abstract: (-)-Swainsonine is prepared by the steps of first reacting a compound having the formula: ##STR1## wherein each R.sub.2 is lower alkyl, with (4-carbalkoxybutyl) triphenylphosphonium bromide in a strong base to obtain an alcohol having the formula: ##STR2## wherein R.sub.2 is as defined above and R is C.sub.1 -C.sub.8 alkyl; the alcohol is then reacted with methanesulfonyl chloride or p-toluenesulfonyl chloride or benzenesulfonyl chloride in the presence of a tertiary amine to obtain the corresponding sulfonate. Heating the sulfonate with an azide in an organic solvent yields an imine having the formula: ##STR3## wherein R.sub.2 and R are ad defined above. Treating the imine with an inorganic base, in aqueous alcohol provides upon acidification, the corresponding acid. Heating the acid at reflux temperature in organic solvent, yields an enamide having the formula: ##STR4## wherein R.sub.2 is as defined above.

Abstract: This invention relates to optical elements capable of second harmonic generation and novel compositions for use in such optical elements comprising polar molecules placed in noncentrosymmetric configuration wherein such optical element has an electron donor moiety linked through a conjugated bonding moiety to an electron acceptor moiety which consists of a selected fluorinated sulfone, fluorinated ketone, fluorinated vinyl sulfone or fluorinated alkyl vinyl sulfone.

Abstract: There are provided important pyrroline and glycine intermediates, methods for the preparation of these intermediates and their use in the manufacture of insecticidal, acaricidal and nematocidal arylpyrrole compounds. Illustrative of the pyrroline and glycine intermediates are compounds having the following structures: ##STR1## wherein A is hydrogen or C.sub.1 -C.sub.4 alkyl and W is CN, NO.sub.2 or CO.sub.2 R.sub.6.

Abstract: Lipid derivatives represented by the formula: ##STR1## wherein R.sup.1 stands for an optionally substituted higher alkyl group, R.sup.2 stands for an optionally substituted lower alkyl group or an optionally substituted nitrogen-containing heterocyclic group, R.sup.3 stands for a tertiary amino group or a quaternary ammonium group, J stands for oxygen atom or S(O)t (where t deontes 0, 1 or 2), m and n respectively denotes 1 or 2, p denotes 0, 1 or 2, q and r respectively denote an integer of 2 to 5.and salts thereof have antitumor activities including differentiation-inducing activity and are useful as antitumor agents.