Abstract: Novel triazolinethilone-phosphoric acid derivatives of the formula 1

Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.

Abstract: Novel compounds with activity as chemical hybridizing agents and methods for synthesis of such compounds are disclosed. These compounds are useful in producing hybrid wheat (Triticum aesativum) and other crops.

Abstract: The invention relates to the preparation of enantiomerically pure bis-diphenylphosphine oxides in a particularly advantageous manner by (1) reacting an aromatic bromine compound with a diphenylphosphinic chloride in a mixture of tetrahydrofuran and an aromatic hydrocarbon to give a diphenylphosphine oxide, which is isolated from a solution in an aromatic hydrocarbon by adding a saturated aliphatic hydrocarbon; (2) metalating the resulting diphenylphosphine oxide in the 6-position and reacting the metalated diphenylphosphine oxide with iodine at temperatures not less than −25° C.

Abstract: Novel triazolinethione-phosphoric acid derivatives of the formula in which R1, R2, R3 and Q are each as defined in the description and their metal salt complexes, a process for preparing the novel substances and their use as microbicides in crop protection and in the protection of materials are described.

Abstract: The invention provides novel bifunctional phosphitylating reagents and their application in in situ preparation of 5′-protected nucleoside phosphoramidites and synthesis of oligonucleotides. Bifunctional phosphitylating reagents according to the invention react quickly with nucleosides under neutral or weakly basic conditions, without an additional activation step. In addition, the bifunctional phosphitylating reagents according to the invention generate chemoselectively the corresponding nucleoside phosphoramidites in situ, without need to purify the nucleoside phosphoramidites before using them in oligonucleotide synthesis. Finally, the bifunctional phosphitylating reagents according to the invention are relatively stable and easy to handle.

Abstract: Disclosed are novel substituted pyrroles having the formula These compounds and their pharmaceutically acceptable salts are suitable for administration to patients as continuous infusion solution and are useful in the treatment and/or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing the foregoing compounds and methods for the treatment and/or control of cancer.

Abstract: The present application describes nitrogen containing heteroaromatics with ortho-substituted P1's and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D is substituted ortho to G on E and may be CH2NH2, which are useful as inhibitors of factor Xa.

Abstract: Copolymers containing N-vinyllactam derivatives protected at 3-position are provided and represented by the following formula. The copolymers are used as a photoresist material suitable for deep uv process so that high sensitivity and resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in PED stability can be accomplished by use of the photoresist.

Abstract: Novel triazolinethione-phosphoric acid derivatives of the formula in which R1, R2, R3 and Q are each as defined in the description and their metal salt complexes, a process for preparing the novel substances and their use as microbicides in crop protection and in the protection of materials are described.

Abstract: A process for producing phosphinopyrrolidine compounds especially useful for preparing optically active compounds through asymmetric synthesis which is a simplified short process requiring neither a step necessitating a high-temperature and high-pressure reaction nor special equipment for production. A phosphino group is incorporated into a pyrrolidine compound in the presence of a boron compound, and the resultant pyrrolidine compound is further reacted while protecting the phosphorous atom, whereby a dicyclohexylphosphino group can be efficiently incorporated into the pyrrolidine nucleus in the 4-position. Thus, the target phosphinopyrrolidine compounds useful as ligands for asymmetric synthesis catalysts can be obtained through a significantly small number of steps without resort to troublesome steps such as the step of reducing a phenyl group at high temperature and high pressure.

Abstract: New halogenobezimidazoles of the formula ##STR1## in which A, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X have the meanings given in the description,and their acid addition salts and metal salt complexes,a process for their preparation and their use as microbicides in crop protection and in the protection of materials.New intermediates of the formulae ##STR2## which R.sup.12 -R.sup.7 and X have the meanings given in the description,and processes for the preparation of these substances.

Abstract: Diphosphines of a mixed heteroarylic-arylic type, wherein the phosphine group carrying backbone is constituted by the interconnection of a five-atom heteroaromatic ring and a carbocyclic aromatic ring, forming an atropoisomeric chiral system with a C.sub.1 symmetry. Said chiral diphosphines are advantageously used as ligands for the formation of chiral complexes with transition metals, in particular Ru, Rh, Pd, Ir, Ni. The so-obtained chiral complexes are used as chiral complexes are used as chiral catalysts for stereocontrolled reactions, in particular diastereo and enantioselective reduction reactions, hydroformylation reactions, hydrosilylation reactions, hydrocyanation reactions, double-bond isomerisation reactions, other reactions of carbon--carbon bond formation.

Abstract: Chiral diphosphines are constituted by an aromatic pentatomic biheterocyclic system, suitable to act as chiral ligands and complexes between the diphosphines and transition metals. They may be utilized as chiral catalysts in stereocontrolled reactions, such as diastereo- and enantioselective reduction reactions. Process is for the preparation of these chiral diphosphines; and process is for the preparation of these complexes and for their utilization as chiral catalysts in stereocontrolled reactions.

Abstract: A process of synthesizing a compound of the formula 1: ##STR1## is described. A compound of the formula 2: ##STR2## is reacted with diphenylphosphinic chloride to activate the carboxylic acid group, and then reacted with methanesulfonyl chloride to produce a compound of formula 4: ##STR3## Compound 4 is then reacted with a group II metal sulfide source in water to produce a compound of formula 1.

Abstract: A compound of formula (II): ##STR1## in which R is a hydrogen atom or a carboxy, alkoxycarbonyl, --CO--NR.sub.4 R.sub.5, --PO.sub.3 H.sub.2 or --CH.sub.2 OH radical, and R.sub.1 is an -alk-NH.sub.2, -alk-NH--CO--R.sub.3, -alk-COOR.sub.4, -alk-CO--NR.sub.5 R.sub.6 or --CO--NH--R.sub.7 radical. The compounds of formula (II) can be used to prepare compounds of formula (I): ##STR2## in which R and R.sub.1 have the same meanings as above. The compounds of formula (I) have valuable pharmacological properties and are antagonists of the .alpha.-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor, also known as the quisqualate receptor. The compounds of formula (I) are also non-competitive antagonists of the N-methyl-D-aspartate (NMDA) receptor and more specifically are ligands for NMDA receptor glycine modulator sites.

Abstract: Copolymers containing N-vinyllactam derivatives protected at 3-position are provided and represented by the following formula. The copolymers are used as a photoresist material suitable for deep uv process so that high sensitivity and resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in PED stability can be accomplished by use of the photoresist.

Abstract: The present invention concerns novel imidazol derivatives of the formula (I), ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and A have the meanings given in the description,and the acid addition salts and metal salt complexes, several processes for the production of the novel substances and their use for combating undesirable micro-organisms in plant and material protection.

Abstract: New halogenobenzimidazoles of the formula in whichA, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and X have the meanings given in the description,and their acid addition salts and metal salt complexes,a process for their preparation and their use as microbicides in crop protection and in the protection of materials.New intermediates of the formula ##STR1## in which R.sup.12 -R.sup.17 and X have the meanings given in the description,and processes for the preparation of these substances.

Abstract: A salt useful as an active species in an organic reaction and represented by the following chemical formula (1): ##STR1## wherein n stands for an integer of from 1 to 8, Z.sup.n- represents an n-valent anion of an active hydrogen compound, a, b, c and d each stands for a positive integer, and Rs represent the same or different hydrocarbon groups. In addition, a simple and efficient process is provided for producing a poly(alkylene oxide) by polymerizing an alkylene oxide compound in the presence of the salt represented by the chemical formula (1).

Abstract: Antigens capable of eliciting antibodies which can catalyze chemical reactions, in particular, the cleavage or formation of a peptide linkage, comprising a hapten or a hapten and a suitable carrier molecule are disclosed. Haptens include, among others, silicon and boron containing compounds. Antibodies which are catalytically active for chemical reactions, in particular, the cleavage or formation of a selected peptide linkage or an ester bond, and which are elicited by such antigens are disclosed as well as methods for producing the antibodies and methods for catalyzing the cleavage or formation of a peptide linkage or in ester bond in a molecule.

Abstract: Novel substituted benzimidazoles of the formula ##STR1## in which Q, R, X and Z have the meanings given in the description,a process for the preparation of the novel substances and their use for combating pests.

Abstract: The present invention relates particularly to novel preorganized hexadentate ligands that are suitable for completing with a radionuclide, and are useful as general imaging agents for diagnostic purposes.

Abstract: Compounds of formula (I), wherein R is a hydrogen atom or a carboxy, alkoxycarbonyl, --CO--NR.sub.4 R.sub.5, --PO.sub.3 H.sub.2 or --CH.sub.2 OH radical, and R.sub.1 is an -alk-NH.sub.2, -alk-NH--CO--R.sub.3, -alk-COOR.sub.4, -alk-CO--NR.sub.5 R.sub.6 or --CO--NH--R.sub.7 radical. The compounds of formula (I) have valuable pharmacological properties and are antagonists of the .alpha.-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor also known as the quisqualate receptor. Furthermore, the compounds of formula (I) are non-competitive antagonists of the N-methyl-D-aspartame (NMDA) receptor and more specifically are ligands for NMDA receptor glycine modulator sites.

Abstract: A compound having the formula (I), a physiologically tolerable salt of the compound having the formula (I) and/or a steroisomeric form of the compound having the formula (I), in which one residue R.sup.1 or R.sup.2 stands for the formula (II), are suitable for preparing medicaments for the therapy of inflammations, asthma, rheumatoid diseases and auto-immune diseases.

Abstract: Disclosed are quaternary nitrogen-containing, saturated or unsaturated monocyclic and bicyclic ring-containing bisphosphonate compounds, and pharmaceutically-acceptable salts and esters thereof. These compounds, which are useful for treating or preventing disorders of calcium and phosphate metabolism, have the following general structure: ##STR1## wherein (a) each X and Y are independently selected from nil, O, S, NR.sup.1 and N.sup.+ (R.sup.2).sub.2 ; if no R.sup.1 is N.sup.+ (R.sup.2).sub.2, then at least one of X or Y must be N.sup.+ (R.sup.2).sub.2 ;(b) m and n and m+n are integers from 0 to 5; p and q and p+q are integers from 0 to 3;(c) s is an integer from 0 to 2 and when m+n=0 and X is nil, s=2;(d) each R.sup.1 is independently selected from the group consisting of nil, N.sup.+ (R.sup.2).sub.2, R.sup.9 SR.sup.6, SR.sup.6, hydrogen, hydroxy; unsubstituted or substituted C.sub.1 -C.sub.8 alkyl, --OR.sup.3, --CO.sub.2 R.sup.3, --O.sub.2 CR.sup.3, NR.sup.3.sub.2, --N(R.sup.3)C(O)R.sup.3, --C(O)N(R.sup.3).

Abstract: New nitrones which are usable for the scavaging of free radicals, are selected from 5-diethoxyphosphoryl-5-methyl-1-pyrroline 1-oxide, 5-phosphono-5-methyl-1-pyrroline 1-oxide, and 5-diethoxyphosphoryl-5-methyl-(2,3,3-.sup.2 H.sub.3)-1-pyrroline 1-oxide, as well as its corresponding physiologically acceptable salts obtained by the action of an inorganic or organic base.

Abstract: N-vinyllactam derivatives protected at the 3-position are provided and represented by the following formula (I). These are polymerized into homo- and copolymers for use in microlithography of semiconductor manufacture. The polymers are used as a photoresist material suitable for a deep UV process so that pictures of high sensitivity and high resolution can be obtained. In addition, ultrafine circuits can be formed and an exceptional improvement in pattern formation can be accomplished through the use of the photoresist of the invention.

Abstract: Novel substituted benzimidazoles of the formula ##STR1## in which Q, R, X and Z have the meanings given in the description,a process for the preparation of the novel substances and their use for combating pests.

Abstract: This invention relates to 3-aryl-2-isoxazoline compounds which are selective inhibitors of phosphodiesterase type IV (PDE.sub.IV). The 3-aryl-2-isoxazolines are useful in the treatment of AIDS, asthma, arthritis, bronchitis, chronic obstructive pulmonary disease, psoriasis, allergic rhinitis, dermatitis, shock, atopic dermatitis, rheumatoid arthritis and osteoarthritis. This invention also relates to pharmaceutical compositions useful therefor.

Abstract: Sulphonylbenzyl-substituted imidazolylpropenoic acid derivatives can be prepared by reacting sulphonylbenzyl-substituted aldehydes with appropriate CH-acidic compounds and then dehydrating.The sulphonylbenzyl-substituted imidazolylpropenoic acid derivatives can be used in medicaments, in particular for the treatment of high blood pressure and atherosclerosis.

Abstract: This invention relates to a compound represented by the formula: ##STR1## wherein B represents a hydrogen atom or a lower alkyl group; ring A represents a benzene ring which may have one or more substituents; .multidot..multidot..multidot..multidot..multidot. represents a single or double bond; Q.sub.1 represents the group represented by the formula, ##STR2## or a hydrocarbon residue substituted with the group represented by the formula, ##STR3## wherein X represents a bond or a spacer having a chain length of 1 to 4 atoms as the linear moiety which may have one or more side chains; R.sup.1 and R.sup.2, whether identical or not, independently represent a hydrogen atom or a lower alkyl, or may bind together to form a ring; Q.sub.2 represents a hydrogen atom, a hydrocarbon residue which may be substituted or a heterocyclic ring residue which may be substituted; or a salt thereof.

Abstract: Novel inhibitors of protein farnesyltransferase enzyme are described, as well as methods for the preparation and pharmaceutical compositions of the same, which are useful in controlling tissue proliferative diseases, including cancer and restenosis.

Abstract: Compounds useful in the treatment of inflammation structurally represented as Formula I ##STR1## one of X or Y is H and the other is selected from the group consisting of: ##STR2## or X and Y are taken together to form a ring selected from the group consisting of: ##STR3## as herein defined. The compounds are useful as anti-inflammatory and anti-arthritic agents.

Abstract: 3-Phenylpyrrolidine compounds of the formula ##STR1## effectively inhibit phosphodiesterase (PDE) IV activities and can be used as medicaments for conditions such as asthma.

Abstract: Peptidyl derivatives of diesters of .alpha.-aminoalkylphosphonic acids, particularly those with proline or related structures, their use in inhibiting serine proteases with chymotrypsin-like, trypsin-like, elastase-like, and dipeptidyl peptidase IV specificity and their roles as anti-inflammatory agents, anticoagulants, and anti-tumor agents.

Abstract: Sulphonylbenzyl-substituted imidazolylpropenoic acid derivatives can be prepared by reacting sulphonylbenzyl-substituted aldehydes with appropriate CH-acidic compounds and then dehydrating.The sulphonylbenzyl-substituted imidazolylpropenoic acid derivatives can be used in medicaments, in particular for the treatment of high blood pressure and atherosclerosis.

Abstract: Compounds of the formula ##STR1## wherein X.sub.1 to X.sub.5 are as defined herein, the tautomers, the stereoisomers including the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases. The compounds are useful for inhibiting undesirable cell aggregation.

Abstract: Arenebisphosphine oxides of the general formula ##STR1## where R.sup.1 to R.sup.4 independently of one another are each hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.5 -C.sub.10 -aryl, C.sub.5 -C.sub.12 -aryloxy or C.sub.7-C.sub.14 -arylalkoxy, R.sup.5 and R.sup.6 independently of one another may each be C.sub.1 -C.sub.6 -alkyl, C.sub.5 -C.sub.10 -cycloalkyl or C.sub.5 -C.sub.12 -aryl, each of which may furthermore contain one or two nitrogen or sulfur atoms in the ring system or carry one or two halogen atoms or C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -alkoxy groups as substituent on the ring system, or C.sub.1 -C.sub.6 -alkoxy, C.sub.3 -C.sub.8 -alkoxyalkoxy, C.sub.5 -C.sub.12 -aryloxy or C.sub.7 -C.sub.14 -arylalkoxy, or R.sup.5 and R.sup.6 together form a bridge of 2 to 10 carbon atoms, in which some of the carbon atoms may furthermore be part of an aromatic ring.

Abstract: The invention relates to new phosphorylated aza compounds, to processes for their preparation and to their use as pesticides, in particular as soil-acting insecticides and nematicide.The new compounds have the general formula (I) ##STR1## in which R.sup.1 -R.sup.5, X and Y are defined as in the specification, with the exception of compound O-ethyl S-propyl 3-(6-chloro-3-pyridinylmethyl)-2-nitroimino-imidazolidine-1-thiophosphate.

Abstract: Insecticidal, acaricidal or nematocidal compositions which comprise a series of organophosphorus compounds represented by the compounds represented by the following structural formulae: ##STR1## show excellent effect for controlling harmful insects, mites and nematodes, do not give off a bad or irritating odor and exhibit very low toxicity to warm-blooded animals.

Abstract: Insecticidal, acaricidal or nematocidal compositions which comprise a series of organophosphorus compounds represented by the following representative structural formulae: ##STR1## show excellent effect for controlling harmful insects, mites and nematodes, do not give off a bad or irritating smell and exhibit very low toxicity to warm-blooded animals.

Abstract: A novel process for the preparation of a compound of the formula ##STR1##

Abstract: The invention relates to phosphonate-containing pseudopeptides of the hydroxyethylamine and norstatin type, to new oxirane- and thiirane-containing pseudopeptides as intermediates, to processes for their preparation and to their use as retroviral agents.

Abstract: 2-(1-Substituted-2-imidazolin-2-yl)benzoic and nicotinic acids, and derivatives thereof, which are effective in the control of undesirable plant species are described, Also described are a method for the herbicidal use of the compounds and a method for their preparation.

Abstract: The invention is directed to a pesticide composition comprising free flowing, essentially spherical, water-dispersible granules wherein said water-dispersible granules are from about 150 to about 850 microns in diameter; wherein said granules contain up to about 8.0% by weight moisture; wherein each individual water-dispersible granule is an aggregation of individual spherical microcapsules which contain at least one water-insoluble pesticide within a polymeric shell wall; and wherein said water-dispersible granule disintegrates upon contact with water to release said individual microcapsules.The invention also relates to dry flowable pesticidal formulations of the above water-dispersible granules, together with formulation adjuvants.The invention is further directed to a process for preparing a water-dispersible granule by spary drying an aqueous suspension comprising discrete microcapsules containing at least one water-insoluble pesticide within a polymeric shell wall suspended in an aqueous liquid.

Abstract: Sulphonylbenzyl-substituted imidazoles can be prepared by first reacting imidazolylaldehydes with sulphonylbenzyl compounds and then oxidising or reducing the aldehyde function in the customary manner.The sulphonylbenzyl-substituted imidazoles can be used as active compounds in medicaments.

Abstract: The present invention relates to novel 3-benzylidene-1-carbamoyl-2-pyrroridone analogues having advantage anti-inflammatory activities, which is represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 each is independently hydrogen, alkyl, alkoxy, or halogen; R.sup.3 is hydrogen or acyl; R.sup.4 is hydrogen, alkyl, hydroxy, alkoxy, cyano, or halogen; R.sup.5 and R.sup.6 each is independently hydrogen, alkyl, aryl, aralkyl, heterocyclic group, substituted or unsubstituted amino, or OR.sup.7 wherein R.sup.7 is hydrogen, alkyl, aryl, acyl, or aralkyl, or taken together with the adjacent nitrogen atom may form heterocyclic group which may contain N, O, and/or S, and X and Y each is independently O, S, substituted or unsubstituted imino, or substituted or unsubstituted methylene. In more detail, the present invention provides an anti-inflammatory agent which is useful for the treatment of chronic inflammation and has little side effect, e.g., stomach disease.

Abstract: Substituted phosphorothioate derivatives and pharmaceutical compositions thereof as potential antiradiation agents are disclosed.

Abstract: Insecticidal, acaricidal or nematocidal compositions which comprise organophosphorus compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 each represents a C.sub.1 to C.sub.4 alkyl group;X represents NH or N--R.sup.4 wherein R.sup.4 represents an alkyl; an alkenyl; an alkynyl; a phosphoric acid ester radical; a cyano group; a group of formula (II): ##STR2## (wherein R.sup.5 represents an alkyl or alkylamino group); or a group of the formula: --(R.sup.6).sub.n --CO--R.sup.7 (wherein n is 0 or 1; R.sup.6 represents a methylene or an ethylene group; and R.sup.7 represents an alkyl, an alkoxy, an alkylthio group, an alkylamino group or a hydrogen atom);Z represents N--R.sup.8 (wherein R.sup.8 represents a nitro group, a cyano group, an alkylsulfonyl group, a tosyl group or an alkylcarbonyl group) or a group represented by the formula: C(CN)R.sup.9 (wherein R.sup.9 represents a cyano group or an alkoxycarbonyl group); andA represents an ethylene group which may be substituted with C.sub.1 to C.sub.