Abstract: Novel IL-8 receptor antagonists and methods of using them are provided.

Abstract: The present invention provides compounds of formula (I). The present invention also provides methods of treating or preventing inflammation or atherosclerosis, and a pharmaceutical composition that contains a compound of formula (I).

Abstract: Compounds having the formula:  wherein  R1-R5 are independently selected from hydrogen, alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 6 carbon atoms, alkynyl of 2 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 carbon members, aryl, heteroaryl, halogen, —CN, —NO2, —CO2R6, —COR6, —OR6, —SR6, —SOR6, —SO2R6, —CONR7R8, —NR6N(R7R8), —N(R7R8) or W—Y—(CH2)n—Z provided that at least one of R1-R5 is not hydrogen; or R2 and R3or R3 and R4, taken together form a 3 to 7 membered heterocycloalkyl or 3 to 7 membered heteroaryl;  R6 and R7 are independently hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, or aryl;  R8 is hydrogen, alkyl of 1 to 6 carbon atoms, perhaloalkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 10 carbon atoms, heterocycloalkyl of 3 to 10 members, aryl or heteroaryl, or  R7 an

Abstract: Compounds of the formula: are useful in the treatment of diseases associated with herpes viruses including human cytomegalovirus, herpes simplex viruses, Epstein-Barr virus, varicella-zoster virus, human herpesviruses-6 and -7, and Kaposi herpes virus.

Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved in cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.

Abstract: The present invention relates to polyaromatic compounds having useful antiviral activity against viruses of the herpes family, to a composition containing them, and to a method of using them for the treatment of herpes viruses infections.

Abstract: The invention relates to a compounds selected from these of formula (I): ##STR1## in which: R.sub.1, R.sub.2, R.sub.3 and A are as defined in the description, and a medicinal product containing the same useful for treating a melatoninergic disorder.

Abstract: A near-infrared absorbent is obtained by heating a dimerized thiourea derivative of Formula ?1! or ?2! and a copper compound: ##STR1## The near-infrared absorbent is used to obtain a near-infrared absorbent resin material having a wide absorption in the near-infrared region, and the absorbent does not substantially decompose at a molding temperature of the resin. Typical examples of the dimerized thiourea derivative are 4,4'-di(benzylthiocarbamoyl)-aminodiphenylmethane, 4,4'-di(benzylthiocarbamoyl)-aminodiphenylhexafluoropropane, and 1,4'-di(dibenzoylthiocarbamoylamino)-2,5-dimethylbenzene, and typical examples of the copper compound are copper stearate and copper .beta.-acryloyloxypropylhydrogenphthalate.

Abstract: The invention relates to a compound selected from these of formula (I): ##STR1## in which R.sub.7, R.sub.8, Y, n and A are as defined in the description, and medicinal product containing the same useful for treating a disorder of the melatoninergic system.

Abstract: A compound selected from those of formula (I): ##STR1## in which A, R, Y, R.sup.1, R.sup.2 and R.sup.3 are as defined in the description,and a medicinal product containing the same useful for treating a disorder of the melatoninergic system.

Abstract: The invention relates to a compound selected from those of formula (I): ##STR1## in which R, R.sub.1, R.sub.2 and R.sub.3 are as defined herein for use in the treatment of a disorder of the melatoninergic system.

Abstract: This invention relates to chelating agents useful for coupling metal ions to biologically active molecules. In particular, substantial thioureas for chelating metals such as technetium are provided that can be conjugated to a targeting molecule such as an antibody, a peptide or a protein.

Abstract: Dendritic derivatives of 3,5-bis(aminomethyl)benzene and aminomethyl benzene core groups are disclosed. In each derivative, termed an "amplifier" because the dendritic structure on each molecule terminates with multiple termini to each of which an "active group" can be attached, the desired effect of the active group per mole is amplified compared to conventional compounds having only one active group per molecule. Amplifier molecules can include a targeting group permitting the molecules to preferentially attach to a particular anatomical or physiological situs. Active groups are any of various pharmacologically or therapeutically active moieties, including moieties useful for magnetic-resonance contrast enhancement. The dendritic structures comprise linkers and branch groups covalently bonded to each other in any of various structural combinations. The amplifiers can be prepared as a solution or mixture with a physiologically compatible carrier for administration to a warm-blooded animal subject.

Abstract: A compound selected from those of formula (I): ##STR1## in which the meanings of R, R.sub.1, R.sub.2 and X are as defined in the specification, and medicinal products containing the same which are useful in treating or in preventing a disorder of the melatoninergic system.

Abstract: This invention relates to the preparation and use of novel open-chain or cyclic polypeptide constructs in which two or more polypeptide chains, in an open-chain construct, or one or more chains, in a cyclic construct, are chemically derivatized such that the resulting construct exhibits both metal-binding capability and tissue-, organ- or cell-targeting selectivity. In particular, the polypeptide constructs of the present invention comprise compounds of the formula (I): ##STR1## in which, "B" is a hydrocarbon backbone, "P" is a polypeptide capable of targeting particular cells, tissues or organs of the body, "A" may be the group --NR'--NR"-- or the group --NR'--NR"--L-- in which L may be an aliphatic or aromatic linker group, R, R' and R" may be the same or different and may be hydrogen or an aliphatic group, m is an integer .gtoreq.2, provided that the groups R, R', R', L and "P" of a given chain may be the same or different from the groups R, R', R", L and "P" of another chain, n is an integer .gtoreq.

Abstract: A compound selected from those of formula (I): ##STR1## in which the meanings of R, R.sub.1, R.sub.2 and X are as defined in the specification, andmedicinal products containing the same which are useful in treating or in preventing a disorder of the melatoninergic system.

Abstract: The compounds of the formula (I) ##STR1## in which R.sup.1 -R.sup.4, W, X, Y and Z are as defined in claim 1 are suitable for controlling harmful plants in crops.

Abstract: The present invention provides novel urea, thiourea and guanidine derivatives, pharmaceutical formulations thereof and a method of using same to prevent diabetic complications.

Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein m is 0 or 1;W is hydrogen, a C.sub.1-16 straight, branched, or cyclic alkyl group, or a C.sub.2-16 straight, branched, or cyclic alkenyl or alkynyl group, orPh(CH.sub.2).sub.n -- where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, orR.sup.1 NHCO-- where R.sup.1 is hydrogen or a C.sub.1-6 alkyl group, orR.sup.2 CONH-- where R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; ##STR2## Y is --(CH.sub.2).sub.q, where q is an integer of from 1 to 3, or --CH.dbd.CH-- (E or Z);Z is a C.sub.

Abstract: A compound selected from those of formula (I): ##STR1## in which the meanings of R, R.sub.1, R.sub.2 and X are as defined in the specification, andmedicinal products containing the same which are in treating or in preventing a disorder of the melatoninergic system.

Abstract: A compound selected from those of formula (I): ##STR1## in which the meanings of R, R.sub.1, R.sub.2 and X are defined in the specification, andmedicinal products containing the same which are useful in treating or in preventing a disorder of the melatoninergic system.

Abstract: The present invention relates to a composition comprising an antimicrobial effective amount of a biocide selected from the group consisting of aromatic 2-N-hydroxy-thiourea and N-hydroxy-quinazolinone, and derivatives and combinations thereof, and at least one component selected from the group consisting of soaps, shampoos, skin-care medicaments, cosmetics, plastics and paints. Also disclosed is a novel process for making the biocide.

Abstract: This invention relates to chelating agents useful for coupling metal ions to biologically active molecules. In particular, isothiocyanate derived thiocarbonyls for chelating metals such as technetium are provided that can be conjugated to a targeting molecule such as an antibody, a peptide or a protein.

Abstract: The present invention relates to a composition comprising an antimicrobial effective amount of a biocide selected from the group consisting of aromatic 2-N-hydroxy-thiourea and N-hydroxy-quinazolinone, and derivatives and combinations thereof, and at least one component selected from the group consisting of soaps, shampoos, skin-care medicaments, cosmetics, plastics and paints. Also disclosed is a novel process for making the biocide.

Abstract: The present invention is concerned with compounds of formula (I) ##STR1## wherein m is 0 or 1;W is hydrogen, a C.sub.1-16 straight, branched, or cyclic alkyl group, or a C.sub.2-16 straight, branched, or cyclic alkenyl or alkynyl group, or Ph(CH.sub.2).sub.n -- where Ph is phenyl and n is an integer of from 0 to 2, the phenyl group being optionally substituted by one or more atoms or groups independently selected from halogen, hydroxy, nitro, C.sub.1-4 alkoxy and C.sub.1-4 alkyl wherein one or more of the hydrogen atoms in said alkyl group is optionally replaced by halogen, or R.sup.1 NHCO-- where R.sup.1 is hydrogen or a C.sub.1-6 alkyl group, or R.sup.2 CONH-- where R.sup.2 is hydrogen or a C.sub.1-6 alkyl group; X is ##STR2## where A is halogen; Y is --(CH.sub.2).sub.q, where q is an integer of from 1 to 3, or --CH.dbd.CH-- (E or Z);Z is a C.sub.

Abstract: Compounds of the formula: ##STR1## wherein R.sub.1 is selected from (1) hydrogen; (2) --NR.sub.2 R.sub.3, --OR.sub.2 or --SR.sub.2 where R.sub.2 and R.sub.3 are independently selected from hydrogen, alkyl, aryl and alkylaryl; and (3) optionally substituted C1-C8 alkyl, C2-C8 alkenyl, arylalkyl or cycloalkyl;Y is selected from sulfur and oxygen;n is an integer selected from 0 and 1;M is hydrogen, a pharmaceutically acceptable cation, or a metabolically cleavable group; andZ is a residue of a non-steroidal antiinflammatory drug of general form Z--COOH;or a pharmaceutically acceptable salt, ester or prodrug thereof,as well as pharmaceutical compositions containing the above compounds and a method for their use as lipoxygenase inhibitors.

Abstract: Novel substituted phenyl-thioureas, -isothioureas and -carbodiimides of formula I ##STR1## in which R.sub.1 is C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 alkyl mono- or poly-substituted by halogen and/or by C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkyl mono- or poly-substituted by C.sub.1 -C.sub.3 alkyl, or is C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 C.sub.4 alkyl; each of R.sub.2 and R.sub.3 is C.sub.1 -C.sub.6 alkyl, C.sub.5 -C.sub.6 cycloalkyl or C.sub.5 -C.sub.6 cycloalkenyl; each of R.sub.4 and R.sub.5 is hydrogen or C.sub.1 -C.sub.4 alkyl; each R.sub.6 is halogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 C.sub.4 haloalkoxy or a --CH.dbd.CH, --CH.sub.2 or --CH.sub.2 bridge in the 2,3-or 3,4-position; n is 0, 1 or 2; Z is --NH--CS--NH--, --N.dbd.C(SR.sub.7) --NH--or --N.dbd.C.dbd.N--, and R.sub.7 is C.sub.1 -C.sub.10 alkyl or C.sub.3 -C.sub.

Abstract: Diurea Derivatives represented by the following general formula and salts thereof: ##STR1## The above compounds inhibit acyl-coenzyme A chloresterol acyl-transferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester to the smooth muscle of arterial wall in the blood vessel.

Abstract: Novel N-[substituted aryl]-N'-(substituted alkoxy)-urea and thiourea derivatives are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful in preventing the intestinal absorption of cholesterol and thus are useful in the treatment of hypercholesterolemia and atherosclerosis.

Abstract: Anxiolytic and antipsychotic treatment is provided to patients by administering therapeutically effective amounts of N-[2-(diethylamino)-ethyl]-2-methoxy-4-[(1-H-4,5-dihydro-2-imidazolyl)-ami no]-5-chlorobenzamide, or a pharmaceutically acceptable salt thereof.

Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxphenyl-N'-diarylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis with urea and thiourea compounds.

Abstract: Diurea derivatives are provided which are represented by the following general formula and salts thereof: ##STR1## The above compounds inhibit acyl-coenzyme A cholesterol acyl-transferase (ACAT enzyme), and thereby control the accumulation of cholesterol ester on the smooth muscle of arterial wall in the blood vessels.

Abstract: This invention relates to novel polymeric polyamines containing internal urea, biuret, thiourea, dithiobiuret, amide, and/or thioamide moieties, and to polymers prepared therefrom. This invention also relates to novel isocyanate-functional prepolymers containing urea, biuret, thiourea, dithiobiuret, amide, and/or thioamide moieties and to polymers prepared therefrom.

Abstract: This invention relates to a process for preparing useful thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)thioxomethyl]hydrazono]ethyl]-1.alpha. ,4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha.,7a.alpha.-4.alpha.,7.alpha.-meth ano-2H-inden-2-ones.

Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxyphenyl-N'-arylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis.

Abstract: Certain substituted urea, thiourea, carbamate, and thiocarbamate compounds are potent inhibitors of the enzyme acyl-CoA: cholesterol acyltransferase and are thus useful agents for inhibiting the intestinal absorption of cholesterol, and for lowering blood plasma cholesterol.

Abstract: Novel isoprenoidamine compounds (I) which show antiulcer activity are provided.

Abstract: Substituted phenoxy, phenylthio and anilino compounds, intermediates therefor, synthesis thereof, and their use for the control of pests.

Abstract: An amine-substituted thiourea dioxide is obtained by reacting thiourea dioxide and an aliphatic or aromatic primary amine in a neutral or acidic pH range.

Abstract: Novel substituted aryloxyphenyl-thioureas, -isothioureas and -carbodiimides of formula I ##STR1## in which R.sub.1 represents C.sub.1 -C.sub.12 alkyl, C.sub.1 -C.sub.12 alkyl mono- or poly-substituted by halogen and/or by C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkyl mono- or poly-substituted by C.sub.1 -C.sub.3 alkyl, or C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.4 alkyl;R.sub.2 represents hydroben or C.sub.1 -C.sub.5 alkyl;R.sub.3 represents a C.sub.1 -C.sub.5 alkyl or C.sub.5 -C.sub.6 cycloalkyl;R.sub.4 represents hydrogen or methyl;R.sub.5 represents a --CH.dbd.CH--.sub.2, --CH.sub.2 --.sub.3 or --CH.sub.2 --.sub.4 bridge in the 2,3- or 3,4-position;Z represents --NH--CS--NH--, --N.dbd.C(SR.sub.6)--NH-- or --N.dbd.C.dbd.N-- andR.sub.6 represents C.sub.1 -C.sub.

Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxyphenyl-N'-arylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis.

Abstract: Substituted benzylcycloalkenylurea derivatives of the formula (I) ##STR1## wherein X represents a halogen atom or a lower alkyl group, Y represents an oxygen atom or a sulfur atom,R.sup.1 represents a cycloalkenyl group andR.sup.2 represents a lower alkyl group, a cycloalkyl group, a benzyl group or a phenyl group optionally substituted by 1 to 5 substituents selected from the group consisting of a hydroxyl group or a lower alkoxy groupand their use as fungicides. They can be synthesized, for example, by reacting of a substituted benzyl-cycloalkenylamine with an isocyanate or by reacting of a carbamoyl halide with an amine. The starting material, the substituted benzyl-cycloalkenyl amines, are also new.

Abstract: An N,N-diaryl-N-alkylurea having the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are the same or different and are selected from the group consisting of hydrogen, halogen, cyano, trifluoromethyl, trifluoromethylthio, trifluoromethyl thionyl, trifluoromethane sulfonyl, sulfonamido, substituted phenoxy and substituted pyridyloxy groups wherein the substituent is any one of halogen, cyano, trifluoromethyl, trifluoromethylthio, trifluoromethyl thionyl, trifluoromethane sulfonyl, sulfonamido; andR.sub.5 is selected from the group consisting of alkyl, alkenyl, haloalkyl, haloalkenyl, hydroxyalkyl, hydroxylalkenyl, acetoxyalkyl, acetoxyalkenyl, mercaptoalkyl, and mercaptoalkenyl, wherein the alkyl or alkenyl group in each alkyl- or alkenyl-containing moiety has from 3 to 6 carbon atoms;X is oxygen or sulfur;and agriculturally acceptable salts thereof.Also disclosed is an herbicidal composition and method of treating weeds.

Abstract: New substituted benzamides have the general formula: ##STR1## A=alkyl, alkenyl, diethylaminoethyl or ##STR2## R.sub.1, R.sub.2 =H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl; R.sub.3, R.sub.4, R.sub.5, R.sub.6 =hydrogen or C.sub.1 -C.sub.6 alkyl;X=halogen;Y=H, halogen;Z=NH, oxygen or sulfur;their optical isomers and their physiologically acceptable salts. The compounds are used as activators of the central nervous system.

Abstract: N-(arylthioalkyl)-N'-(aminoalkyl)ureas and thioureas and oxidation derivatives having the formula ##STR1## wherein B is thio, sulfinyl or sulfonyl; R.sup.1 and R.sup.2 are hydrogen, loweralkyl, cycloalkyl, 2-furanyl, phenyl, substituted phenyl or phenyl-loweralkyl and R.sup.3 and R.sup.4 are hydrogen, loweralkyl, phenyl or phenyl-loweralkyl wherein phenyl is optionally substituted, or R.sup.3 and R.sup.4 taken with the adjacent nitrogen form a heterocyclic residue.

Abstract: 1-Aryloxy-3-(substituted aminoalkylamino)-2-propanols and pharmaceutically acceptable salts thereof have .beta.-adrenergic blocking activity with some cardioselectivity and hence are useful as antihypertensive, antianginal, antiarrhythmic and cardioprotective agents and in the treatment of elevated intraocular pressure such as glaucoma.

Abstract: Fungicidally active novel benzylurea derivatives of the formula ##STR1## in which R.sup.1 is a halogen atom or a lower alkyl group,X is an oxygen or sulfur atom, andR.sup.2 is an alkyl group, a cycloalkyl group having 5 to 8 carbon atoms, or a phenyl group which may be substituted by at least one member of the class consisting of halogen atoms, lower alkyl groups, lower alkoxy groups and hydroxyl groups.

Abstract: Dihalo and haloalkyl, haloalkoxy or haloalkylthio-substituted anilines and aniline derivatives, e.g. isocyanates that are useful in the preparation of acyl ureas having insecticidal activity.

Abstract: (Thio)-ureas of the formula ##STR1## in which R.sup.1 is an optionally alkyl-substituted cycloalkyl radical or a halogenoalkyl radical,R.sup.2 is an alkyl or cycloalkyl radical or an optionally substituted aryl radical,Ar is an optionally substituted aryl radical, at least one of the radicals R.sup.1, R.sup.2 and Ar carrying fluorine or a fluorine-containing substituent, andX is an oxygen or sulphur atom,which possess fungicidal activity. Novel intermediates are also disclosed.

Abstract: Tetrasubstituted urea and thiourea compounds useful as antiatherosclerotic agents, compositions thereof and processes for their preparation.