Abstract: A novel process for the preparation of benzonitrile compounds useful for herbicides or their intermediates is provided. A process for the preparation of compounds of the formula (1), characterized in comprising reacting a compound of the formula (1a) with one or more cyanides selected from potassium cyanide, sodium cyanide and zinc cyanide in the presence of a metallic catalyst. In the scheme, X is hydrogen, fluorine or chlorine atom; Z is nitro, amino or C1-C4 alkylsulfonylamino group or the like; Y is fluorine, chlorine or bromine atom or the like; and Q is hydrogen atom, or nitro or amino group or the like.

Abstract: There are provided compositions and methods comprising compounds of formula I: wherein R1, A, B, X, Y and Z have the meaning given in claim 1, for the control of insect and acarid pests.

Abstract: The invention relates to novel substituted aminophenyluracils of the general formula (I) to a process for their preparation and to their use as herbicides and insecticides.

Abstract: The present invention provides compounds of Formula I methods for their preparation and their use as acaricidal and insecticidal agents.

Abstract: The invention relates to substituted phenyluracils of the general formula (I) in which the radicals R1 to R5, Q and n are each as defined in the description, and to processes for their preparation and to their use as herbicides.

Abstract: A process for the preparation of the compound of the formula (I) by reacting a compound of the formula (IV) with a compound of the formula (III).

Abstract: 1-Amino-3-benzyluracils I (X=oxygen, sulfur; R1=C1-C4-haloalkyl; R2=H, halogen; R3, R7=H, CN, SCN, halogen, C1-C4-haloalkyl, C1-C4-haloalkoxy, C1-C4-haloalkylthio; R4=H, CN, SCN, halogen, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, C1-C4-haloalkylthio, C1-C6-alkylaminocarbonyl; R5=H, CN, NO2, halogen, OH, C1-C4-alkoxy, NH2, C1-C6-alkyl-amino; R6=H, CN, NO2, halogen, OH, C1-C4-alkoxy, NH2, C1-C6-alkyl-amino, CHO) and their salts are used as herbicides and for the desiccation/defoliation of plants.

Abstract: The invention relates to novel substituted phenyluracils of the general formula (I) in which R1, R2, R3, R4, R5 and R6 are each as defined in the description, to processes for their preparation, to novel intermediates and to their use as herbicides.

Abstract: The invention relates to novel substituted phenyluracils of the general formula (I) 1

Abstract: The invention relates to novel substituted iminoalkoxy-phenyluracils of the general formula (I) in which R1 is hydrogen, amino or optionally substituted alkyl, R2 is carboxyl, cyano, carbamoyl, thiocarbamoyl or alkyl or alkoxycarbonyl, the latter two being optionally substituted, R3 is hydrogen, halogen or optionally substituted alkyl, R4 is hydrogen, cyano, thiocarbamoyl or halogen, R5 is cyano, thiocarbamoyl or halogen, R6 is hydrogen or optionally substituted alkyl, R7 is optionally substituted alkyl, and R8 is hydroxyl, amino or a radical of the series alkyl, alkoxy, alkylamino, dialkylamino, alkylcarbonylamino, alkoxycarbonylamino, alkylsulfonylamino, alkenyl, alkynyl, alkenyloxy, alkynyloxy, aryl, aryloxy, arylamino, arylcarbonylamino, arylsufonylamino, arylalkyl, arylalkylamino, arylalkylcarbonylamino or arylalkylsulfonylamino, each of which is optionally substituted. The invention further relates to methods for producing said compounds and their use as herbicides.

Abstract: New substituted phenyl uracils are described which have general formula (I), in which R1 is halogen, or optionally substituted alkyl, R2 is optionally substituted alkyl, R3 is an amino group or optionally substituted alkyl, alkenyl or alkynyl, R4 is a cyano group or halogen, R5 is a cyano group or thiocarbamoyl, R6 group (2) or group (3) in which Q1 and Q2 are oxygen or sulphur, R7 is hydrogen or optionally substituted alkyl, R8 is hydrogen or optionally substituted alkyl, alkoxy, alkylamino, dialkylamino, alkylcarbonylamino, alkylsulfonylamino, alkenyl, alkenyloxy, alkynyl, cycloalkyl, cycloalkyloxy, cycloalkylamino, cycloalkylcarbonylamino, cycloalkylsulfonylamino, aryl, aryloxy, arylamino, arylcarbonylamino, arylsulfonylamino, arylalkyl, arylalkoxy or arylalkylamino group, R9 and R10 are alkyl. A method for production of said compounds and their use as herbicides are described.

Abstract: A substituted 3-phenyluracil of the formula I where X1 and X2 are each oxygen; W is —C(R8)=X5, where X5 is oxygen, sulfur, or a radical —NR14; R14 is hydroxyl, alkoxy, alkenyloxy, alkynyloxy, cycloalkoxy, cycloalkenyloxy, haloalkoxy, haloalkenyloxy, hydroxyalkoxy, cyanoalkoxy, cycloalkylalkoxy, alkoxyalkoxy, alkoxyalkenyloxy, alkylcarbonyloxy, haloalkylcarbonyloxy, alkylcarbamoyloxy, haloalkylcarbamoyloxy, alkoxycarbonylalkoxy, alkylthioalkoxy, dialkylaminoalkoxy, R8 is hydrogen, cyano or alkyl; R1 is halogen or cyano; R2 is hydrogen or halogen; R3 is hydrogen or alkyl; R4 is cyano, alkyl or haloalkyl; R5 is hydrogen, halogen or alkyl; or a salt or enol ether of a compound I wherein R3 is hydrogen, or its tautomeric forms, for the desiccation and defoliation of plants or as an insecticide or herbicide.

Abstract: Novel pyrimidinedione compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.

Abstract: The invention relates to novel substituted aminophenyluracils of the general formula (I) to a process for their preparation and to their use as herbicides and insecticides.

Abstract: The invention relates to a process for preparing ar(alk)yluracils of the general formula (I) in which A represents a single bond or represents alkanediyl, Ar represents optionally substituted aryl, R1 represents optionally substituted alkyl and R2 represents hydrogen, halogen or alkyl, and to novel intermediates for this purpose and to processes for their preparation.

Abstract: Herbicidal composition, comprising A) at least, one compound from the group of the substituted phenylsulfonylureas of the formula I and agriculturally acceptable salts thereof and B) at least one herbicidally active compound selected from the group of the compounds consisting of Ba) herbicides which have selective activity against grasses in cereals,. Bb) herbicides which have selective activity against dicotyledons in cereals, Bc) herbicides which have selective activity against grasses and dicotyledons in cereals and Bd) herbicides which are active against weed grasses and broad-leaved weeds and which are nonselective in non-crop areas or perennial crops (plantations) and/or selective in transgenic crops.

Abstract: Imido and amido substituted alkanohydroxamic acids reduce the levels of TNF&agr; and inhibit phosphodiesterase in a mammal. A typical embodiment is 3-(3-cyclopentyloxy-4-methoxyphenyl)-N-hydroxy-3-phthalimidopropionamide.

Abstract: A compound of the general formula I: is disclosed as useful in treating disorders of the central nervous system. Pharmaceutical compositions, processes for preparing the compounds and methods of treatment are also disclosed.

Abstract: Pyrimidinone derivatives of the general formula: wherein R1 is hydrogen or alkyl; R2 is haloalkyl; R3 is nitrogen or CH; G is optionally substituted ethylene, trimethylene, or vinylene; and Q is selected from several optionally substituted or heterocyclic-condensed phenyl groups, are useful as the active ingredients of herbicides because of their excellent herbicidal activity.

Abstract: The invention is directed to novel 6-aromatic substituted uracil compounds of formula I therapeutic compositions comprising the compounds, and methods of treating Herpes simplex virus Type I and Type II recurrent infections and Herpes simplex virus Type I and Type II encephalitis in humans using the compounds and/or therapeutic compositions.

Abstract: Disclosed are processes for preparing compounds of the formula (I) and pharmaceutically acceptable salts or esters thereof: wherein R2 is a purine or pyrimidine base or an analogue or derivative thereof; and Z is S, S═O or SO2. The invention also relates to intermediates of use in the preparation of these compounds.

Abstract: A description is given of compounds of the general formula I where Y is oxygen or sulfur, and R1 and R2 independently of one another are C1-C18-alkyl, C3-C6-alkenyl, unsubstituted or C1-C4-alkoxy-, C5-C8-cycloalkyl-, —OH— and/or Cl-substituted C1-C18-alkyl, C5-C8-cycloalkyl, phenyl or C7-C9-phenylalkyl which is unsubstituted or substituted on the phenyl ring by C1-C4-alkyl, C1-C4-alkoxy, C5-C8-cycloalkyl, —OH and/or Cl, and R3 is unsubstituted C9-C18-alkyl or is C1-C18-alkyl substituted by —OH, C1-C12-alkoxy, phenoxy, C6-C8-alkylphenoxy, C7-C9-alkoxyphenyl, —C═O(OR4) and/or —O—COR4, or is C3-C6-alkenyl, C5-C8-cycloalkyl, or mono- to tri-OH—, —C1-C4-alkyl-, —C1-C4-alkoxy-, —C═O(OR4)— and/or —O—COR4-substituted phenyl or naphthyl, and where R4 is C1-C12-alkyl, which are suitable for stabilizing chlorine-containing polymers, especially PVC.

Abstract: This invention is directed to dihydropyrimidine compounds which are selective antagonists for human &agr;1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the &agr;1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Abstract: The invention relates to a novel process for preparing substituted cyanophenyluracils of the general formula (I) in which R1, R2, R3 and R4 are each as defined in the description, said compounds being known as herbicidally active compounds, to novel substituted N-(cyanophenyl)aminoalkenamides as intermediates therefor and to an inventive process for their preparation.

Abstract: Compounds of formula (I) ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.

Abstract: Novel compounds that are potent inhibitors of HIV reverse transcriptase (RT) are described in the invention. Thes novel compounds also inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (HIV-1). The novel compounds of the invention include analogs and derivatives of phenethylthiazolylthiourea (PETT), of dihydroalkoxybenzyloxopyrimidine (DABO), and of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT).The invention additionally provides a composite HIV reverse-transcriptase (RT) nonnucleoside inhibitor (NNI) binding pocket constructed from a composite of multiple NNI-RT complexes The composite RT-NNI binding pocket provides a unique and useful tool for designing and identifying novel, potent inhibitors of reverse transcriptase.

Abstract: A description is given of compounds of the general formula I ##STR1## n is 1 or 2, Y is oxygen or sulfur andR.sub.1, R.sub.2, R.sub.3 and R.sub.4 are as defined in claim 1which are suitable for stabilizing chlorine-containing polymers, especially PVC.

Abstract: A process for preparing (E)-methyl 2-[2-(6-(-cyanophenoxy)pyrimidin-4-yloxy)phenyl]-3-methoxypropenoate comprising contacting (E)-methyl 2-[2-(6-chloropyrimidin-4-yloxy)phenyl]-3-methoxypropenoate or methyl 2-[2-(6-chloropyrimidin-4-yloxy)phenyl]-3,3-dimethoxypropanoate with 2-cyanophenate anions, the process being conducted in the absence of copper or a copper salt and in the absence of N,N-dimethylformamide. The 2-cyanophenate anions are generated in situ by reacting 2-cyanophenol with an alkali metal carbonate.

Abstract: There are provided compositions and methods comprising compounds of formula I: ##STR1## wherein R.sup.1, A, B, X, Y and Z have the meaning given in claim 1, for the control of insect and acarid pests.

Abstract: By a novel process, trifluoroacetoacet-anilides of the formula ##STR1## in which R.sup.1 is as defined in the description, can be prepared by reacting trifluoroacetoacetyl chloride with anilines of the formula ##STR2## if appropriate in the presence of an acid binder and if appropriate in the presence of a diluent.The compounds of the formula (I) are suitable intermediates for preparing herbicidally active uracil derivatives.

Abstract: The invention relates to novel substituted p-trifluoromethylphenyluracils of the general formula (I) in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each as defined in the description, to a process for their preparation and to their use as herbicides.

Abstract: This invention relates to novel fused heterocycles which are useful as antagonists of the .alpha..sub.v .beta..sub.3 and related integrin receptors, to pharmaceutical compositions containing such compounds, processes for preparing such compounds, and to methods of using these compounds, alone or in combination with other therapeutic agents, for the inhibition of cell adhesion, the treatment of angiogenic disorders, inflammation, bone degradation, cancer metastasis, diabetic retinopathy, thrombosis, restenosis, macular degeneration, and other conditions mediated by cell adhesion and/or cell migration and/or angiogenesis.

Abstract: Novel compounds that are potent inhibitors of HIV reverse transcriptase (RT) are described in the invention. Thes novel compounds also inhibit replication of a retrovirus, such as human immunodeficiency virus-1 (HIV-1). The novel compounds of the invention include analogs and derivatives of phenethylthiazolylthiourea (PETT), of dihydroalkoxybenzyloxopyrimidine (DABO), and of 1-[(2-hydroxyethoxy)methyl]-6-(phenylthio)thymine (HEPT).The invention additionally provides a composite HIV reverse-transcriptase (RT) nonnucleoside inhibitor (NNI) binding pocket constructed from a composite of multiple NNI-RT complexes The composite RT-NNI binding pocket provides a unique and useful tool for designing and identifying novel, potent inhibitors of reverse transcriptase.

Abstract: N,N'-dialkylurea and an .alpha.,.beta.-unsaturated nitrile are reacted to form a cyclic N,N'-dialkylurea containing an imine group on a ring carbon. This compound is useful as an intermediate in the formation of N,N'-dialkylpropyleneureas by hydrogenation followed by hydrogenolysis to remove the imine group. Using N,N'-dimethylurea and acrylonitrile as the starting materials one can arrive at N,N'-dimethylpropyleneurea which is a compound useful as an organic solvent and known by its acronym, DMPU.

Abstract: Disclosed are herbicidal heterocyclic benzisoxazoles and benzisoxazolidinones of formula (I): ##STR1## wherein A is (a), (b) or (c); U is N or NR; X is CO or CR.sup.2 ; and R, R.sup.1, R.sup.2, R.sup.3, Y and Z are as disclosed in the disclosure.

Abstract: There are described N-ethylglycine derivatives of the formula I ##STR1## in which PG is a urethane-type or trityl-type amino protective group which is labile to weak acids, X is NH, O or S, Y is CH.sub.2, NH or O, and B' are bases customary in nucleotide chemistry, the exocyclic amino or hydroxyl groups of which being protected by suitable, known protective groups, or are base substitute compounds, and their salts with tert-organic bases, as well as a process for their preparation. The N-ethylglycine derivatives of the formula I are used in the preparation of PNA and PNA/DNA hybrids.

Abstract: The present invention relates to methods and compositions for preparing biologically important nucleoside analogues containing 1,3-dioxolane sugar rings. In particular, this invention relates to the stereoselective synthesis of the beta (cis) isomer by glycosylating the base with an intermediate of formula (II) below a temperature of about -10.degree. C. ##STR1## wherein R.sub.1 and L are as defined herein.

Abstract: Benzylhydroxylamines I ##STR1## (X=--N(R.sup.7)--O--; Y=O, S; R.sup.1 =halogen, CN, NO.sub.2, CF.sub.3 ; R.sup.2 =H, halogen; R.sup.3 =H, NH.sub.2, CH.sub.3 ;R.sup.4 =H, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.1 -C.sub.6 -alkylthio, C.sub.1 -C.sub.6 -alkylsulfinyl or C.sub.1 -C.sub.6 -alkylsulfonyl;R.sup.5 =H, halogen, C.sub.1 -C.sub.6 -alkyl;R.sup.6 =H, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.2 -C.sub.6 -alkenyl;R.sup.7 =H, C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.8 -cycloalkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, C.sub.1 -C.sub.6 -alkylcarbonyl, C.sub.3 -C.sub.6 -alkenylcarbonyl, C.sub.3 -C.sub.6 -alkynylcarbonyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, C.sub.2 -C.sub.8 -alkenyloxycarbonyl, C.sub.2 -C.sub.6 -alkynyloxycarbonyl, C.sub.1 -C.sub.6 -alkylthiocarbonyl, C.sub.1 -C.sub.6 -alkylsulfonyl, C.sub.1 -C.sub.

Abstract: The present invention comprises a method of synthesizing compounds of formula (I): wherein Z, R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.8 are as described herein; comprising the steps of.

Abstract: Substituted cinnamic oxime derivatives I and cinnamic hydroxamide derivatives II ##STR1## (R.sup.1= halogen, NO.sub.2, CN, CF.sub.3 ; R.sup.2 =H, halogen; R.sup.3= H, halogen, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, hydroxy-C.sub.1 -C.sub.6 -alkyl;R.sup.4= H, halogen, CN, C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl orR.sup.3 +R.sup.4 =chemical bond;Y=--O--, --S--, --O--CO--, --O--SO.sub.2 -- or chemical bond;Y'=--O-- or --S--;R.sup.5= unsubst. or subst. C.sub.1 -C.sub.6 -alkyl or C.sub.1 -C.sub.6 -haloalkyl; C.sub.3 -C.sub.6 -cycloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.3 -C.sub.6 -alkynyl, unsubst. or subst. phenyl or phenyl-C.sub.1 -C.sub.6 -alkyl, or, if Y is --O--, --S-- or a chemical bond, is (C.sub.1 -C.sub.6 -alkyl)carbonyl or (C.sub.1 -C.sub.6 -alkoxy)carbonyl; or, if Y is a chemical bond, is hydrogen or halogen;R.sup.5 '=R.sup.5, H or (C.sub.1 -C.sub.6 -haloalkyl)carbonyl;R.sup.6= H, C.sub.1 -C.

Abstract: The invention relates to novel substituted aminouracils of the general formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are each as defined in the claims,to the preparation thereof and to their use as herbicides.

Abstract: Compounds of structural Formula (I) ##STR1## and pharmacologically acceptable salts and esters thereof possess 5.alpha.-reductase inhibitory activity. These compounds inhibit 5.alpha.-reductase type 1 and type 2. The compounds of structural Formula I are useful in the systemic, including oral, and parenteral, including topical, treatment and prevention of hyperandrogenic conditions including prostatic carcinoma, benign prostatic hyperplasia, acne vulgaris, seborrhea, androgenic alopecia (also called androgenetic alopecia) which includes male- and female-pattern baldness, female hirsutism, and prostatitis. A class of compounds of the present invention are also potent antiandrogens. The present invention also relates to novel compositions containing such compounds, methods of their use and methods of their manufacture.

Abstract: The invention relates to new substituted diazacyclohexanedi(thi)ones of the general formula (I) ##STR1## in which Q.sup.1, Q.sup.2, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 have the meanings given in the description,a process for their preparation, new intermediate products and their use as herbicides.

Abstract: This invention relates to N-cyanoaryl compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Z have the meanings given in the description and their use as herbicides and insecticides.

Abstract: The present invention provides antineoplastic .alpha.-methylene-.gamma.-butyrolactones represented by the general formula ?I! wherein R.sub.1 is a phenyl group optionally substituted with one or two groups selected from the group consisting of halide, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4)alkoxy, phenyl, nitro and amino;.sub.2 R represents hydrogen, halide, (C.sub.1 -C.sub.4)alkyl or benzyl; X represents N; or wherein R.sub.1 is a phenyl group optionally substituted with one or two groups selected from the group consisting of halide, (C.sub.1 -C.sub.4)alkyl, (C.sub.1 -C.sub.4) alkoxy, nitro and amino; R.sub.2 represents Cl, F, or benzyl; X represents CH. These .alpha.-methylene-.gamma.-butyrolactones may be administered with an inert diluent or with a pharmaceutically acceptable carrier in controlling the growth of a neoplasm in a patient afflicted with a neoplasm disease.

Abstract: The present invention relates to heterocyclic compounds of the formula ##STR1## in which R.sup.1 -R.sup.7, B, a and X have the meanings recited in the specification. These compounds are usable in the treatment of diseases of the rheumatoid group and for the prevention of allergically induced diseases.

Abstract: 2-?(2-Alkoxy-6-trifluoromethylpyrimidin-4-yl)oxymethylene!-phenylacetic acid derivatives of the formula I ##STR1## where the index and the substituents have the following meanings: U is CH or N;V is O or NH;R is alkyl;R.sup.1 is cyano, halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or phenyl;n is 0 or an integer from 1 to 4,processes and intermediates for their preparation, and their use are described.

Abstract: Carboxylic acid derivatives ##STR1## where R-R.sup.6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.

Abstract: The present invention relates to methods and compositions for preparing biologically important nucleoside analogues containing 1,3-dioxolane sugar rings. In particular, this invention relates to the stereoselective synthesis of the beta (cis) isomer by glycosylating the base with an intermediate of formula (II) below a temperature of about -10.degree. C. ##STR1## wherein R.sub.1 and L are defined herein.

Abstract: It has now been found that certain novel (oxaalkyl)phenyl-substituted heterocycles are useful as pre-emergent and post-emergent herbicides. These compounds are represented by formula I: ##STR1## where Q is a heterocycle and X, Y, R, R.sup.1, R.sup.2, and R.sup.3 are substituents as described in the specification. Preferred are those compounds where Y and R are chloro; R.sup.1 and R.sup.2 are hydrogen or methyl; R.sup.3 is hydrogen or alkylaminocarbonyl; X is fluorine; and Q is a 1-substituted-6-trifluoromethyl-2,4(1H,3H)-pyrimidinedion-3-yl.