Abstract: Dipyrrometheneboron difluoride dyes possessing a covalently attached basic amine moiety are described that have utility for staining acidic organelles. Samples comprising isolated acidic organelles, or a cell or cells containing acidic organelles, are stained by preparing an aqueous labeling solution of the dye and incubating the sample in the labeling solution for a time sufficient to produce fluorescent labeled acidic organelles.

Abstract: A compound of chemical formula (I) and its pharmaceutically acceptable salt: ##STR1## wherein X and Y are each hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, halosubstituted C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkylthio, C.sub.1 -C.sub.6 alkylsulfinyl, C.sub.1 -C.sub.6 alkylsulfonyl, or tri(C.sub.1 -C.sub.6 alkyl)silyl; Ar.sup.1 and Ar.sup.2 are each independently aryl or heteroaryl, optionally substituted by halogen; A is --CO-- or -(CH.sub.2)-; Z-A- is at the 2 or 3 position on the quinuclidine ring; and Z is --OH, C.sub.1 -C.sub.6 alkoxy, NR.sup.1 R.sup.2 or the like. Representative compounds are (3S,4R,5S,6S)-5-?3,5-bis(trifluoromethyl)-benzyloxy!-N,N-dimethyl-6-diphen ylmethyl-1-azabicyclo?2.2.2!octan-3-carboxamide, and -3-carboxylic acid.

Abstract: The present invention provides 8-substituted 1,3,7-trialkylxanthines useful as A.sub.2 -selective adenosine receptor antagonists and compositions comprising such compounds. Examples of the 8-substituted 1,3,7-trialkyl xanthines include: ##STR1## In compound (a), R.sub.1, R.sub.3, and R.sub.7 are methyl and X is one to three substituents, which may be the same or different and selected from the group consisting of amino, C.sub.1 -C.sub.4 alkylcarbonylamino, carboxy C.sub.2 -C.sub.4 alkylcarbonylamino, halo, C.sub.1 -C.sub.3 alkyloxy, amino C.sub.1 -C.sub.4 alkyloxy, C.sub.1 -C.sub.4 alkyloxy carbonylamino, amino C.sub.1 -C.sub.4 alkenyloxy, isothiocyanato, and diazonium tetrafluoroborate. In compound (b), R.sub.1, R.sub.3, and R.sub.7 are methyl, R.sub..beta. is hydrogen or methyl, and X is selected from the group consisting of R, C(.dbd.O)OR, and C(.dbd.O)NH--R, wherein R is a C.sub.1 -C.sub.6 alkyl.

Abstract: Disclosed are amino silicone derivatives having triazinyl groups or pyrimidinyl groups bound to amino groups of amino silicones, their production and use, said silicone derivatives being able to gel silicone oil or to increase the viscosity thereof stably and homogeneously, and therefore being useful as bases for cosmetics, pharmaceutical preparations and industrial materials.

Abstract: Substituted spiroalkylamino and -alkoxy heterocycles, processes for their preparation, and their use as pesticides and fungicidesThe invention relates to compounds of the formula ##STR1## in which Het is optionally substituted 4-pyridyl or 4-pyrimidinyl; X is NH, O or S(O).sub.0-2 ; E is a bond or alkanediyl; Y and Z are CH.sub.2, O and/or S(O).sub.0-2 ; W is (CH.sub.2).sub.0-4 ; R.sup.4 and R.sup.5 are halogen, (halo)alkyl, (halo)alkoxy or alkylthio; r and s are 0-2; U is a bond, O, S(O).sub.0-2 or optionally substituted imino; and V is a bond CO, SO.sub.2, --CQ--T-- or --CT'.dbd.N--; or U+V together are a double bond; and R.sup.6 is as defined in the description. The invention furthermore relates to processes for their preparation and to their use as pesticides and fungicides.

Abstract: Cyclohexylamino and cycloalkoxy nitrogen heterocycles, processes for their preparation, and their use as pesticides and fungicides.The invention relates to compounds of the formulaAr--X-E-Qin which Ar is substituted or unsubstituted 4-pyridyl or 4-pyrimidinyl; X is NH, O, S, SO or SO.sub.2 ; E is a bond or alkanediyl; and Q is a substituted cycloalkyl or 4-piperidyl.The invention also relates to processes and intermediates for their preparation, to compositions comprising them and to their use as pesticides and fungicide.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Disclosed are compounds having a straight or branched aliphatic hydrocarbon structure of formula I: ##STR1## In formula I, n is an integer from one to four and m is an integer from four to twenty. Independently, R.sub.1 and R.sub.2 are hydrogen, a straight or branched chain alkyl, alkenyl or alkynyl of up to twenty carbon atoms in length or --(CH.sub.2).sub.w R.sub.5. If R.sub.1 or R.sub.2 is --(CH.sub.2).sub.w R.sub.5, w may be an integer from one to twenty and R.sub.5 may be an hydroxyl, halo, C.sub.1-8 alkoxyl group or a substituted or unsubstituted carbocycle or heterocycle. Alternatively, R.sub.1 and R.sub.2 may jointly form a substituted or unsubstituted, saturated or unsaturated heterocycle having from four to eight carbon atoms, N being a hetero atom of the resulting heterocyle. R.sub.3 may be either hydrogen or C.sub.13. In the compounds, a total sum of carbon atoms comprising R.sub.1 or R.sub.2, (CH.sub.2).sub.n and (CH.sub.2).sub.m does not exceed forty. R.sub.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Compounds of the formula ##STR1## where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.

Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.

Abstract: Compounds of the general formula I: (SIL--X--).sub.m IN (I), in which SIL is a radical of the formula Si(R.sup.1)(R.sup.2)(R.sup.3), where R.sup.1 is an alkyl, haloalkyl or alkoxy radical of 1 to 8 carbon atoms, an alkenyl radical, an alkenyloxy or acyloxy radical of 2 to 8 carbon atoms, an aryl or aryloxy radical of 6 to 10 carbon atoms, or a dialkyl-, diaryl- or alkylaryl-methyleneaminooxy radical having C.sub.1 -C.sub.4 -alkyl or C.sub.6 -aryl groups; and R.sup.2 and R.sup.3 are identical or different radicals with the meaning of R.sup.1 or X--IN; X is a group C.sub.n H.sub.2n ; IN is the radical of a compound which is active as a photoinitiator or photosensitizer and which has at least one carbonyl group located on an aromatic nucleus; m is a number from 1 to 4; and n is a number from 2 to 12, or of the formula II: Si.sub.o O.sub.o-1 (--X--IN).sub.p R.sup.4.sub.2o+2-p (II), in which R.sup.4 is a radical with the meaning of R.sup.1, and two or more radicals R.sup.

Abstract: There are disclosed 18-thiomarcfortine derivatives of the natural products marcfortine A, B and C, C-18 thioparaherquamide and derivatives thereof, novel N-1 marcfortines A, B, and C and derivatives thereof, novel N-1 paraherquamide and derivatives thereof usefull in the treatment and prevention of helninth and arthropod infections of animals and plants.Any inquiry concerning this communication or earlier communications from the examiner should be directed to Examiner Robert T. Bond whose telephone number is (703)308-4711. The examiner can normally be reached on Monday through Friday from 8:00 AM to 4:30 PM.

Abstract: A compound of the Formula I or Formula II ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, hydroxy, chlorine, fluorine, bromine, or an organic substituent having 1 to 5 carbon atoms and selected from acyloxy having a hydrocarbon stem of 1 to 4 carbon atoms, alkoxy, alkylthio, amino, alkylamino and dialkylamino;R.sup.3 and R.sup.4 are independently hydrogen, or organic phosphonic ester substituents having 1 to 12 carbon atoms and selected from alkyl, alkenyl, aryl, and aralkyl; andB is a heterocyclic group selected from the group consisting of pyrimidine, purine, triazine, deazapurine, and triazole, attached through a ring nitrogen atom thereof optionally substituted with 1 to 3 substituents selected from the group consisting of hydroxy, mercapto, amino, hydrazino, fluoro, chloro, bromo, iodo, C.sub.1 to C.sub.3 alkyl, C2-C3 alkenyl, C2-C3 haloalkenyl, C1-C3 alkoxy, and C1-C3 alkylthio;and the pharmaceutically acceptable acid addition, metal, and amine salts thereof.

Abstract: The present invention relates to certain novel substituted derivatives which are 1-pyrimidinylacetamide derivatives of formula I, ##STR1## which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these substituted derivatives, processes for preparing the substituted derivatives, pharmaceutical compositions containing such substituted derivatives and methods for their use.

Abstract: A class of 2-arylpyrimidines which is useful in the control of weeds of the general formula: ##STR1## wherein R.sup.2 is an optionally substituted aromatic ring; R.sup.3 is a saturated or unsaturated alkyl group; R.sup.5 is selected from acyl, alkoxyalkyl, alkoxyimino, dialkoxyalkyl, formyl, hydroxyalkyl, alkoxyalkoxy, cyanoalkyl and hydroxyimino; R.sup.6 is selected from hydrogen, halo, alkyl, haloalkyl, aryl, and alkoxy; and X is oxygen or sulfur.

Abstract: Optically pure intermediates of formula (1) wherein the substituent B is either cis or trans to the C.sub.9a -C.sub.1 bond and is selected from the group consisting of --CH.sub.2 OH, --CHO, --CH.sub.2 OSO.sub.2 R, --CH.sub.2 CN, --CH(OH)CH.sub.2 NO.sub.2, --CH.dbd.CH--NO.sub.2, (2) and (3), C is selected from the group consisting of --H, (4), (5), and a nitrogen protecting group which is removable by hydrogenation or acid treatment; and wherein R is (C.sub.1 -C.sub.8) alkyl, phenyl or alkyl substituted phenyl; X is N or CH; Y is O or S and Z is H or Cl; for the synthesis of octahydro-1H-pyrido(1,2-a)pyrazinyl ethyl carboxamide anxiolytic agents.

Abstract: Heterocyclylamino- and heterocyclyloxy-cycloalkyl derivatives, their preparation, and their use as pesticides and fungicides ##STR1## in which Ar is optionally substituted 4-pyridyl or 4-pyrimidinyl; X is NH, O or S; E is a bond or alkanediyl; n is 2-7; R.sup.4 is H or alkyl, Y is O or a bond; and Ac is acyl, and salts thereof. The invention furthermore relates to processes for their preparation, to compositions comprising them, and to their use as pesticides and fungicides.

Abstract: A process for preparing polycyclic aromatic compounds by cross-coupling aromatic boron compounds with aromatic halogen compounds or perfluoroalkylsulfonates in the presence of metallic palladium as catalyst comprises adding to the reactiona) at least one water-soluble complexing ligand andb) sufficient water for the reaction mixture to form an aqueous phase.The reaction of the invention proceeds chemoselectively so that even electrophilic groups such as esters or nitriles do not have an adverse effect on the course of the reaction.The use according to the invention of a water-soluble complexing ligand in an aqueous phase enables polycyclic aromatic compounds to be prepared in very good yields and at the same time very high purity, in particular without contamination by the complexing ligands.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Abstract: Novel imidazoles of the formula ##STR1## wherein the substituents are as defined in the disclosure and their non-toxic, pharmaceutically acceptable addition salts with acids and bases having antiandrogenic activity.

Abstract: Novel N-substituted-(dihydroxyboryl)alkyl purine, indole and pyrimidine derivatives have been found to be useful as inhibitors of inflammatory cytokines. They can be used, inter alia, in the therapy of septic shock, cachexia, rheumatoid arthritis, inflammatory bowel disease, multiple sclerosis and AIDS. The compounds are typically prepared by reaction of an bromoalkyl boronic acid with the purine, indole or pyrimidine base.

Abstract: The present invention relates generally to .alpha.-aminoboronic acids and corresponding peptide analogs of the formula (I): ##STR1## in which the .alpha.-carbon is substituted with an optionally functionalized imidazole containing alkyl group. These compounds are useful as inhibitors of trypsin-like serine protease enzymes, especially thrombin, Factor X and Factor VII.

Abstract: Compounds with fungicidal and insecticidal properties having formula I ##STR1## wherein W is CH.sub.3 --O-A.dbd.C--CO(V)CH.sub.3 ; n is 0 or 1;A is N or CH;V is O or NH;whereinY is O, S, NR.sub.1, or R.sub.6, the ring bond containing R.sub.4 and R.sub.5 is a single or double bond and R.sub.4 and R.sub.5 are independently selected from hydrogen and substituted or unsubstituted alkyl and aryl groups.

Abstract: Disclosed us a compound of Formula 1.0: ##STR1## or a pharmaceutically acceptable salt or solvate thereof. Also disclosed are pharmaceutical compositions comprising a pharmaceutically acceptable carrier and an effective amount of a Compound of Formula 1.0.Further disclosed is a method of treating allergy (for example asthma), inflammation, hypertension, raised intraocular pressure (such as glaucoma)--i.e., a method of lowering intraocular pressure, sleeping disorders, states of hyper and hypo motility and acidic secretion of the gastrointestinal tract, hypo and hyperactivity of the central nervous system (for example, agitation and depression) and other CNS disorders (such as Alzheimers, Schizophrenia, and migraine) comprising administering an effective amount of a compound of Formula I to a patient in need of such treatment.

Abstract: Disclosed are certain 3-phenylpyridazines, compositions thereof which are herbicidal and methods of using such compositions for controlling undesired plants. Intermediates useful in preparing the 3-phenylpyridazines are disclosed.

Abstract: 5-Substituted-2,4-diaminopyrimidines, and agriculturally acceptable salts thereof, when present in insecticidally or acaricidally effective amounts, and with a suitable agricultural carrier, are useful as active ingredients in novel insecticidal and acaricidal compositions. These pyrimidines may be represented by the following formula: ##STR1## wherein Ar is ##STR2## and wherein U is an alkenylene or alkynylene moiety, and R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, V, W, X, Y, Z and n are as defined herein; also disclosed and claimed are novel intermediates thereof.

Abstract: Compounds of the formula ##STR1## the symbols have the meaning described in the specification have retinoid-like biological activity.

Abstract: The present invention is directed to a compound represented by the structural formula: ##STR1## wherein Z-- represents a negatively charged counterion.

Abstract: Compounds of the formula ##STR1## wherein the symbols have the meaning described in the specification have retinoid-like biological activity.

Abstract: A condensed heterocyclic derivative of the formula (I): ##STR1## (wherein R is a hydroxyl group, R.sup.3 or R.sup.4 is an alkoxy group, W is an oxygen atom, Yn is a hydrogen atom, Z is a methine group, and A is a 5- or 6-membered heterocyclic ring which may be substituted, and a herbicide, are presented. When used for paddy field treatment, upland soil treatment and foliage treatment, the condensed heterocyclic derivative of the present invention exhibits excellent herbicidal activities against gramineous and non-gramineous weeds without adversely affecting crop plants.

Abstract: Compounds of the formulae I and Ia and their racemates ##STR1## in which A is --CH.sub.2 -- or --CH.sub.2 CH.sub.2 --, R.sub.1 is hydrogen or a protective group, R.sub.2 is hydrogen or a protective group or a radical forming a phosphorus-containing nucleotide bridge group and B is a purine or pyrimidine radical or an analogue thereof, can be used as antiviral active ingredients or for the preparation of biologically active oligonucleotides.

Abstract: A butenoic or propenoic acid derivative having the following formula in which G is an aryl or a heterocyclic ring, R11 and R12 are hydroben or an alkyl, X is sulfur or oxygen, R2 and R3 are hydrogen, an substituent such as an alkyl and J is pyridyl or phenyl having substituents and a heterocyclic ring may be formed between R2, R3 and J is provided here and is useful in the pharmacological field.

Abstract: Substituted pyridines and pyrimidines, processes for their preparation and their use as pesticides and fungicides.The invention relates to compounds of the formula ##STR1## in which A is N or CH, R is H, halogen, alkyl or cycloalkyl, R.sup.2 and R.sup.3 are H, halogen or an aliphatic radical or together form a ring, X is O, NH Or S(O).sub.q where q=0, 1 or 2, R.sup.4.sub.q is 0-4 radicals selected from the series consisting of halogen, optionally substituted alkyl or alkoxy, cycloalkyl and optionally substituted phenyl, n=0-2, m=1-3 and Y is optionally substituted methylene or imino.The invention furthermore relates to a process for their preparation and for their use as pesticides, in particular as insecticides, acaricides and fungicides. The compounds are furthermore suitable for controlling nematodes, helminths and molluscs, and for controlling endoparasites and ectoparasites in the field of veterinary medicine.

Abstract: The present invention relates to a novel and economical process for the synthesis of HPMP-substituted nucleotide antiviral compounds. Also disclosed are novel intermediates produced in the process for the preparation of HPMPC.

Abstract: The present invention provides heterocyclylalkyl diarylboron ester and thioester compounds of formula I ##STR1## and their use for the prevention, control or amelioration of diseases caused by fungi. Further provided are compositions and methods comprising those compounds for the protection of plants from fungal infection and disease.

Abstract: The invention relates to compounds of the formula ##STR1## in which R.sup.1, R.sup.2, R.sup.3 and Q are as defined in the description, X is NH or oxygen and E is a bond or a 1- to 4-membered carbon chain, to a process for their preparation, to agents containing them, and to their use in the control of pests and as fungicides.

Abstract: This invention relates to compounds having the formula R.sub.1 -(CH.sub.2).sub.n -Het wherein R.sub.1 is a residue having the formula (B), (C), (D); Het represents a radical phenyl-4 tetrahydro-1,2,3,6 pyridyl-1 whose phenyl cycle is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical; a radical phenyl-4 piperazinyl-1 whose phenyl cycle is optionally substituted by a halogen atom or an alkyl, alkoxy or hydroxy radical; R.sub.3 is a hydrogen atom or a phenyl radical; R.sub.4 is a hydrogen or halogen atom or a residue Het; R.sub.5 is a carbonyl or sulfonyl radical; R.sub.6 is a radical Si(CH.sub.3).sub.2 or C(CH.sub.3).sub.2 ; n equals 1, 2, 3 or 4; excepting {[(phenyl-4 tetrahydro-1,2,3,6 pyridyl-1)-2 ethyl] amino}-3 benzisothiazol-1,2 dioxyde-1,1; their salts, their preparation and medicaments containing them.

Abstract: Disclosed are certain 3-phenoxypyridazines, compositions thereof which are herbicidal and methods of using such compositions for controlling undesired plants. Intermediate compounds useful in preparing the phenoxypyridazines are also disclosed.

Abstract: Aminoureidofullerene and aminothioureidofullerene derivatives and the process for the preparation thereof Aminoureido and aminothioureido compounds of the fullerenes C.sub.60 and/or C.sub.70 and processes for the preparation thereof and use thereof are described.

Abstract: Compounds of formula (I), and salts and prodrugs thereof, wherein Q is optionally substituted phenyl or benzhydryl; X and Y are each H or together form a group=O; Z is O, S or NR.sup.9, where R.sup.9 is H or C.sub.1-6 alkyl; R.sup.1 represents H or C.sub.1-6 alkyl; R.sup.2 represents C.sub.1-6 alkyl substituted by CONR.sup.7 (CH.sub.2).sub.p R.sup.8 (where R.sup.7 is H or C.sub.1-6 alkyl, R.sup.8 is optionally substituted heteroaryl and p is 0, 1, 2, 3, 4, 5 or 6); R.sup.3 represents H, C.sub.1-6 alkyl or C.sub.2-6 alkynyl; R.sup.4 represents H, C.sub.1-6 alkyl or optionally substitute phenyl; R.sup.5 represents optionally substituted phenyl; R.sup.6 is H or C.sub.1-6 alkyl; and q is 0, 1, 2 or 3; are tachykinin antagonists useful in therapy.

Abstract: This invention relates to substituted dihydropyridazinones, pyridazinones and related compounds, of the formula ##STR1## wherein A, Q, D and R.sup.1 are as defined within, compositions containing these compounds and methods of controlling agricultural and mammalian fungal diseases.

Abstract: The present invention relates to novel adducts of cyclic carbonyl monomers with substituted olefins, which also are useful as solution viscosifiers.

Abstract: The present invention relates to a method of preparing BCH-189 and various analogs of BCH-189 from inexpensive precursors with the option of introducing functionality as needed. This synthetic route allows the stereoselective preparation of the biologically active isomer of these compounds, .beta.-BCH-189 and related compounds. Furthermore, the steochemistry at the nucleoside 4' position can be controlled to produce enantiomerically-enriched .beta.-BCH-189 and its analogs.

Abstract: A 4-desoxy-4-epipodophyllotoxin derivative of the following formula ##STR1## wherein R and R.sub.1 are as defined in the specification or a pharmaceutically acceptable salt thereof as well as an antitumor composition comprising such derivative or salt as an active ingredient.

Abstract: The present invention provides an N-sulfonyl carboxylic amide derivative including an N-containing 6-membered aromatic ring represented by formula [I]: ##STR1## wherein R.sup.1 represents an alkyl group, an alkenyl group, or the like, R.sup.2 represents a hydrogen atom, an alkyl group, or the like, R.sup.3 and R.sup.4 represent independently an alkyl group, alkoxy group, or the like, and X and Y represent independently a methyne group or a nitrogen atom; or the salt of the same, a method for producing the same, and a biocide containing the same as an active ingredient. The N-sulfonyl carboxylic amide derivative including an N-containing 6-membered aromatic ring according to the present invention exhibits superior effects against blight caused by plant pathogenic fungi belonging to Oomycetes such as downy mildew, late blight, or the like in a low concentration as well as controls weeds occurring in paddy fields and plowed fields.

Abstract: There is provided an insecticidal composition comprising, in admixture with an agriculturally acceptable carrier, an insecticidally effective amount of a tetrahydroquinazoline compound of the formula ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 are as defined herein, and methods of using the same. Certain novel substituted-phenyl tetrahydroquinazoline compounds per se are also identified.

Abstract: A compound and method of making a compound for use as a diagnostic or therapeutic pharmaceutical comprises either a phosphorous or germanium core and at least two hydrazine groups forming a ligand for bonding to a metal extending from the phosphorous or germanium core.

Abstract: The present invention provides compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof.