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

Abstract: A process for the preparation of 1,3-oxathiolane nucleoside analogues in predominantly the cis-form, from mixture of cis-/trans-1,3-oxathiolane nucleosides or their protected derivatives thereof, comprising: (i) treatment of the cis-/trans-1,3-oxathiolane nucleosides (or protected derivatives thereof) with a pyrimidine base (or it derivatives thereof) and an acid, (ii) adding a suitable acid to the obtained cis-/trans-mixture of isomers, (iii) selective crystallization of the desired cis-isomer salt from a solvent or combination of solvents, and (iv) treatment of the predominantly cis-isomer salt with a suitable base to offer the free 1,3-oxathiolane nucleosides, and thereafter optionally repeating steps (i) to (iv) inclusive.

Abstract: The invention relates to novel substituted phenyluracils of the general formula (I) in which A represents alkanediyl or alkenediyl, each of which has 2 to 5 carbon atoms and each of which is optionally substituted by cyano, halogen or by in each case optionally halogen- or C1-C4-alkoxy-substituted C1-C4-alkyl, C1-C4-alk-oxy-carbonyl or C2-C4-alkenyl or interrupted by O (oxygen), or represents cyclohexane-1,2-diyl or 1,2-phenylene, Q1 represents O (oxygen) or S (sulphur), Q2 represents O (oxygen) or S (sulphur), R1 represents hydrogen, amino or optionally cyano-, halogen- or C1-C4-alkoxy-substituted alkyl having 1 to 4 carbon atoms, R2 represents optionally halogen-substituted alkyl having 1 to 4 carbon atoms, R3 represents hydrogen, halogen or optionally halogen-substituted alkyl having 1 to 4 carbon atoms, R4 represents hydrogen, cyano, carbamoyl, thiocarbamoyl or halogen, R5 represents cyano, carbamoyl, thiocarbamoyl or in each case optionally halogen-substituted alkyl or alkoxy ha

Abstract: The invention relates to novel substituted phenyluraciles of the general formula (I) in which m, n, Q and R1-7 are each as defined in the description, and to processes for their preparation and to their use as herbicides.

Abstract: The invention relates to a novel, heretofore unknown polymorphous modification of 5-fluoro-1-(tetrahydro-2-furyl)uracil (tegafur) having antineoplastic activity. This form is crystalline, and its characteristics it differs essentially from the modification known earlier. In particular, it has an enhanced specific activity. The new form is physically stable and may find application in medicine for treating oncological patients. New anticancer medicinal substances prepared in the form of stable molecular complexes on the basis of said new modification, in particular, crystalline complexes with 6-methyluracil, and amorphous complexes with the biologically active substances from licorice, are also described.

Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.

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 alkanedlyl, 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: 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 aryluracils of the formula (I): to processes for their preparation and to their use as crop protection agents.

Abstract: The invention relates to novel substituted p-trifluoromethylphenyluracils of the general formula (I) in which R1, R2, R3, R4 and R5 are each as defined in the description, to a process for their preparation and to their use as herbicides.

Abstract: The invention is directed towards gene expression characteristic for cancer, in particular brain cancers such as glioblastoma. Compositions, methods and kits encompassing such therein.

Abstract: The invention is directed to a process for the preparation of a substituted phenyluracil of the formula: The process broadly comprises reacting a carbonylphenyluracil of the formula: with an amino compound, an alcohol or a mercaptan. The resultant products are useful as herbicides.

Abstract: The invention relates to novel aminouracils of the general formula (I) in which, Q, R1, R2, R3, R4, R5, R6 and R7 are each as defined in the description, to their use as herbicides and to novel intermediates.

Abstract: A group of novel pyrimidone compounds are inhibitors of the enzyme LDL PLA2 and therefore of use in treating atherosclerosis.

Abstract: The present invention relates to a method for controlling weeds in corn field which comprises applying a herbicidal composition comprising 2-[2-chloro-4-fluoro-5-{3-methyl-2,6-dioxo-4-(trifluoromethyl)-1,2,3,6-tetrahydropyrimidin-1-yl}phenoxy]propionic acid ester as an active ingredient to corn fields after seeding corn. According to the present method, kinds of weeds in corn fields can be controlled widely and no problematic phytotoxicity to corn is caused.

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: The present invention provides compounds comprising propynyl uracils having the formula wherein R1 is hydrogen, chlorine, bromine, iodine, fluorine, —CN, substituted or unsubstituted linear or branched C1-C4 alkyl, —NO2, methoxy, ethoxy, n-propoxy, or iso-propoxy; R2 is iodine or bromine; and R3 is propynyl, 3-iodopropynyl, 3-bromopropynyl, substituted or unsubstituted 2-furanyl, substituted or unsubstituted 3-furanyl, substituted or unsubstituted 2-pyrrolidinyl, substituted or unsubstituted 3-pyrrolidinyl, D-ribose, or deoxyribose. Another embodiment of the invention encompasses propynyl uracils having the formula wherein R4 is hydrogen, chlorine, bromine, iodine, fluorine, —CN, substituted or unsubstituted linear or branched C1-C4 alkyl, —NO2, methoxy, ethoxy, n-propoxy, or iso-propoxy; R5 is hydrogen or propynyl; and R6 is iodine or bromine. Also, methods of preparing these propynyl uracils are provided.

Abstract: The novel compounds of formula I: (A, B, R1, R2, R3, X and m are defined in the specification) show selective herbicidal activity. The new compounds can be prepared according to known methods and can be used as herbicides in agriculture and related fields.

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: Uracil reductase inactivators, notably a 5-substituted uracil or 5,6-dihydro-5-substituted uracil, potentiate 5-fluorouracil and find use particularly in the treatment of cancer. The 5-substituent is selected from bromo, iodo, cyano, halo-substituted C1-4 alkyl, C2-6 alkenyl, 1-halo-C2-6 alkenyl and halo-substituted C2-6 aklynyl.

Abstract: The invention relates to novel uracil derivatives having excellent inhibiting effects on human derived thymidine phosphorylates and anti-tumor activity. The pharmaceutical compositions, anti-tumor potentiators and antitumor agents containing such novel compounds, and a process for their preparation and use are described.

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: Patients susceptible to or suffering from conditions and disorders, such as central nervous system disorders, are treated by administering to a patient in need thereof aryloxyalkylamines, including pyridyloxylalkylamines and phenoxyalkylamines.

Abstract: The present invention relates to a group of 5-substituted uracil derivatives which are inactivators of uracil reductase and which are particularly useful in cancer chemotherapy, especially in combination with antimetabolite antineoplastic agents such as 5-fluorouracil.

Abstract: A compound of the Formula (1) and salts thereof: wherein: Ar, Ar1, J, J1, X, X1 W, W1, L and m are as defined in the description. The compounds of Formula (1) are useful as additives in inks, especially ink jet printing inks, for reducing color bleed between adjacent printed regions. Also claimed are inks containing a compound of the Formula (1), a method of ink jet printing using the inks, a substrate printed with the ink and an ink jet printer cartridge containing the ink.

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

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: This invention is directed to benzamidine derivatives substituted by cyclic amino acid and cyclic hydroxy acid derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.

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 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: 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: 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: 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: The invention relates to novel uracil derivatives having excellent inhibiting effects of human derived thymidine phosphorylase and anti-tumor activity. The pharmaceutical compositions, anti-tumor potentiators, antitumor agents containing such novel compounds, and a process for their preparation and use is described.

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: The present invention relates to a process for producing a compound represented by the formula (II): ##STR1## wherein X is a halogen atom, each of A.sup.1, A.sup.2 and A.sup.3 are the same or different and are selected from a carbon atom or a nitrogen atom, provided that at least A.sup.1, A.sup.2, or A.sup.3 is a nitrogen atom. Each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are selected from a hydrogen atom, a lower alkyl group, a cyano group, a carboxyl group, a lower alkoxycarbonyl group, a halogen atom, and a nitro group. It is also provided that where R.sup.1 and R.sup.2 are adjacent to each other, R.sup.1 and R.sup.2 may be combined with each other to form a 5- or 6-membered ring which may carry on the ring thereof one substituent selected from the group consisting of a lower alkyl group, a nitrile group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a halogen atom, a nitro group, and an amino-(lower alkyl) group.

Abstract: The invention relates to new N-cyanoaryl-nitrogen hetero-cycles of the general formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and Z have the meanings given in the description,to a plurality of processes for their preparation, to their use as herbicides and to novel intermediates.

Abstract: Chloropyrimidine compounds, such as 4,6-dichloro-2-ethoxypyrimidine, were prepared in good yield and good purity from the corresponding hydroxypyrimidine compounds in the absence of organic solvents and with a reduced amount of phosphorus oxychloride by carrying out the reaction in the presence of a trialkylamine compound and phosphorus trichloride. The additions of hydroxypyrimidine compound and trialkylamine compound could be made in segments. The chloropyrimidine compounds produced were recovered in an improved manner by adding chlorine to convert the chlorophosphoric acid by-products and phosphorus trichloride to phosphorus oxychloride, diluting the mixture with additional chloropyrimidine compound and removing the phosphorus oxychloride by distillation, combining the residue with water and a base, distilling the trialkylamine compound from the resulting mixture, and removing the aqueous phase.

Abstract: 4-Ethoxy-pyrimidines useful as intermediates in preparing antiviral 1,3-oxathiolane nucleosides are described.

Abstract: The subject invention relates to pyrimidine-thioalkyl and alkylether compounds of Formula (I) and pyrimidine-thioalkyl and alkylethers of Formula (IA), namely the compounds of Formula (I) where R.sub.4 is selected from the group consisitng of --H or --NR.sub.15 R.sub.16 where R.sub.15 is --H and R.sub.16 is --H, C.sub.1 -C.sub.6 alkyl, NH.sub.2 or R.sub.15 and R.sub.16 taken together with the --N form 1-pyrrolidino, 1-morpholino or 1-piperidino; and R.sub.6 is selected from the group consisting of --H, or halo (preferably --Cl); with the overall proviso that R.sub.4 and R.sub.6 are not both --H. The compounds of Formula (IA) are useful in the treatment of individuals who are HIV positive being inhibitors of viral reverse transcriptase.

Abstract: Nucleoside derivatives represented by formula (I); ##STR1## wherein, R.sub.1 represents hydrogen, phosphate or phosphonate group, R.sub.2 represents substituted or unsubstituted pyrimidine or purine base, and Z represents S, SO, SO.sub.2, O or C; or pharmaceutically acceptable salts thereof. Compound (I) can be obtained by reacting a compound of the formula (II); ##STR2## wherein, R.sub.7 represents hydrogen or hydroxy-protecting group, L represents aromatic or nonaromatic acyl, halide or alkoxy, and Z represents S, SO, SO.sub.2, O or C, with a base.

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: Compounds of formula (I): ##STR1## wherein: R is halogen;Y is hydrogen, NH.sub.2, SH or OH;X is: ##STR2## wherein: either R.sub.1 or R.sub.2 is a bond, with the other being hydrogen;either R.sub.3 or R.sub.4 is hydrogen, with the other being hydrogen, OH, OAc or NHAc;R.sub.5 is OH or OAc;either R.sub.7 or R.sub.8 is hydrogen, with the other being OH or OAc;R.sub.9 is hydrogen, CH.sub.2 OH or CH.sub.2 OAc;with the proviso that when R.sub.4 is OH, OAc or NHAc then R.sub.8 is hydrogen;and enantiomers of such compounds, are disclosed. Pharmaceutical formulations comprising such compounds, their use in the treatment of various disease states, and methods of treatment employing the compounds are also provided.

Abstract: The invention is related to a novel phenylacetylene derivates of formula: ##STR1## wherein X represents hydrogen, halogen, optionally substituted C.sub.1-6 alkyl; Y represents hydrogen, halogen, cyano, nitro, optionally substituted C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.3-8 cycloalkoxy, optionally substituted C.sub.1-6 alkylthio, C.sub.3-8 cycloalkylthio, C.sub.1-6 alkylsulfinyl, optionally substituted C.sub.1-6 alkylsulfonyl, C.sub.3-8 cycloalkylsulfonyl, C.sub.1-6 alkylsulfonyloxy, optionally substituted sulfonamide, optionally substituted carboxamide, etc., or Y may form together with Z which is bonded to the vicinal carbon atom a 5- or 6-membered ring; n is 0 or 1; Z represents hydrogen or halogen; m is 1 or 2; R represents hydrogen, halogen, C.sub.1-6 alkyl, tri(C.sub.1-6 alkyl)silyl, COOR.sup.c or CONR.sup.d R.sup.e ; Q represents a heterocyclic group, and their use as herbicid.

Abstract: The present invention provides certain 6-hetarylalkyloxy pyrimidine derivatives of formula II ##STR1## wherein R is (i) a cyclic group having at least one 5- or 6-membered heterocyclic ring, optionally with a carbocyclic or heterocyclic ring fused thereto, the or each heterocyclic ring having at least one hetero atom chosen from O, N, or S, or a substituted derivative thereof; or (ii) phenyl or a substituted derivative thereof,R.sup.2 is selected from H, C.sub.1 -C.sub.5 alkyl, halogen or NH.sub.2,R.sup.4 and R.sup.5 which are the same or different are selected fromH, NH.sub.2 or NO.sub.n where n=1 or 2, or R.sup.4 and R.sup.5 together with the pyrimidine ring form a 5-or 6-membered ring structure containing one or more heterocyclic atoms, and pharmaceutically acceptable salts thereof, exhibit the ability to deplete O.sup.6 -alkylguanine-DNA alkyltransferase (ATase) activity.

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 process for the resolution of a racemic mixture of nucleoside enantiomers that includes the step of exposing the racemic mixture to an enzyme that referentially catalyzes a reaction in one of the enantiomers. The nucleoside enantiomer (-)-2-hydroxymethyl-5-(5-fluorocytosin-1-yl)-1,3-oxathiolane is an effective antiviral agent against HIV, HBV, and other viruses replicating in a similar manner.

Abstract: The invention relates to pyrimidinone derivatives and the pharmaceutically acceptable salts thereof having remarkable antagonistic action against angiotensin II receptor, and thus useful in treating cardiovascular diseases caused by angiotensin II.

Abstract: The disclosure concerns pyrimidine derivatives represented by the following general formulas [I] and [I′] and having antiviral activity, particularly antiretroviral activity such as anti-HIV activity: and pharmaceutical compositions having antiviral activity and comprising the above-described derivative(s) as an active ingredient.