Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) 1

Abstract: The present invention relates to beta-amino acid nitrile derivatives and pharmaceutically acceptable salts and/or pharmaceutically acceptable esters thereof. The compounds are cysteine protease inhibitors useful for the treatment of diseases associated with cysteine proteases, such as osteoporosis, osteoarthritis, rheumatoid arthritis, tumor metastasis, glomerulonephritis, atherosclerosis, myocardial infarction, angina pectoris, instable angina pectoris, stroke, plaque rupture, transient ischemic attacks, amaurosis fugax, peripheral arterial occlusive disease, restenosis after angioplasty and stent placement, abdominal aortic aneurysm formation, inflammation, autoimmune disease, malaria, ocular fundus tissue cytopathy and respiratory disease.

Abstract: A soothing anti-viral lotion composition and a lotioned tissue product having a surface with the lotion composition applied thereto, and methods for making and using the same. The lotion composition includes an anti-viral organic acid and a topical delivery system. The topical delivery system includes one or more polyesters which allow incorporation of the organic acids into the lotion formulation, controls their delivery, and maintains them in the stratum corneum. The lotion composition may optionally contain a surfactant, an irritation inhibiting agent, and other additives.

Abstract: Controlled release compositions of matter are disclosed comprising complexes for treating a population of one or more aquatic organisms in a column of water. The complexes comprise at least one system wherein the system comprises at least one bioactive agent as a component selected for treating a population of aquatic organisms, at least one carrier component, and at least one coating component for regulating the controlled release rate and release profile of the bioactive agent in water or at least one bioactive agent and one joint-function component that can serve as both a carrier and coating to regulate the controlled release rate and release profile of the bioactive agent in water, with or without optional binder components and/or additional formulation materials. The components are selected to sink or float so that the complexes will permeate and/or remain in any planar or volumetric segment of a water column for a period of time that is sufficient to effectively treat a population of aquatic organisms.

Abstract: Compounds and methods useful for chemopreventative treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, inflammatory bowel diseases, and multiple sclerosis.

Abstract: This invention relates to a method for the prophylaxis of or reducing the severity of post-viral bacterial infection by administering a PDE 4-specific inhibitor prior to or during the course of a viral infection or thereafter during the course of the bacterial infection.

Abstract: Disclosed are novel succinate derivative compounds of the formula (I)/(Ia): 1

Abstract: A method of termite control consists of injecting a foam formulation above ground into the walls of a structure infested with termites or other undesirable pests. The inner spaces of affected walls are flooded at and above ground level to ensure that the foam formulation reaches all passages open to the soil under the structure and establishes an above-ground layer of pest-control chemicals. The foam penetrates all porous material exposed to the injection and impregnates it with active ingredients that remain embedded in the material long after the foam disappears, thereby retaining the insecticidal, repellant and preservative properties of the active agents for a long time without exposure to normal degrading forces. The pest-control formulation preferably comprises pesticide, repellant and preservative components, and a foaming agent in a liquid carrier.

Abstract: A preparation for the treatment and/or prevention of dementia disorders, especially disorders due to regressive cellular changes. A dose of at least one steroidal antagonist is included as the active agent. A mixture of such substances can also be applied.

Abstract: Compositions and methods for use in preventing conception or treating benign gynecological disorders, wherein an effective amount of an antiprogestational agent [e.g., progesterone (progestin, progestogen, gestagen) antagonist or progesterone synthesis inhibitor] administered over a first period of time is combined with an effective amount of a progestogen for a second period of time. The antiprogestational agent is selected from single agents or mixtures thereof. The progestogen is selected from single agents or mixtures of natural or synthetic progestogens. The formulations are effective as contraceptive agents and for treatment of benign gynecological disorders including uterine fibroids, premenstrual syndrome, dysfunctional uterine bleeding, polycystic ovarian syndrome and endometriosis.

Abstract: The present invention relates to methods for the use of specified inhibitors of multicatalytic protease (MCP) for use as inducers of programmed cell death (i.e., apoptosis) in tumor cells, and more particularly as anti-tumor agents. The present invention provides methods for inducing apoptosis in transformed cells, inhibiting proliferation of transformed cells, and inhibiting the growth of tumors using the MCP inhibitors.

Abstract: Novel derivatives of 1-aminoindan and their salts are described. Optically active 1-aminoindan derivatives are prepared by reacting a N-benzyl analog of the desired compound with an enantiomer of mandelic acid.

Abstract: Compositions for controlling harmful fungi, containing in a solid or liquid carrier a) at least one p-hydroxyaniline derivative of the formula I b) at least one amide compound of the formula II A—CO—NR8—R9  (II) where the substituents have the meanings indicated in the description; and methods of controlling harmful fungi using compositions of this type are described.

Abstract: Compounds of Formula (I) are disclosed which are useful as fungicides, wherein Q is: (Q−1) or (Q−2), Z is (Z−1); (Z−2); (Z−3) or (Z−4); X is —O—, —CH(R11)— or ═C(R11)—; R1 is H or C1-C2 alkyl; R2 is H; C1-C6 alkyl; C3-C6 cycloalkyl; or phenyl optionally substituted with halogen, cyano, C1-C2 alkyl or C1-C2 alkoxy; and R3-R11 are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula (I) and a method for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound of Formula (I).

Abstract: The present invention provides novel biopesticides which can replace commercial pesticides and biopesticides which have been banned, restricted, or are being phased out, including, but not limited to chloropicrin, dichlorvos and methyl bromide. Many of the biopesticides of the present invention are excellent fumigants, possessing quick action and volatility, while posing less risk than currently used pesticides to humans and the environment. The biopesticides of the present invention are natural and closely-related synthetic derivatives or analogs related to two classes of natural compounds, namely glucosinolates and monoterpenoids.

Abstract: The invention is related to the use of COMT inhibitors in the treatment of diabetic vasculat dyfunctions.

Abstract: The present invention relates to chromotropic nitrone spin trapping agents, methods of making these agents, compositions comprising same, and methods of their use. In particular, azulenyl nitrones of the present invention are effective agents for trapping free radical species and find use as efficient antioxidants in physicochemical and biological systems. Accordingly, the invention also relates to spin adducts formed from the combination of azulenyl nitrones with free radicals. The compounds of the present invention are readily prepared from available starting materials and find further use in assays and in a number of diagnostic, prophylactic and therapeutic applications, including but not limited to the alleviation, modulation and inhibition of the negative effects of carbon-centered or oxygen-centered radical species and other products of oxidation. Moreover, the combination adducts may be calorimetrically detected and, optionally, isolated and characterized to obtain valuable information (e.g.

Abstract: An adhesive composition includes compounds having the following formula: wherein R1 is alkyl, alkoxy alkyl, anhydride, ether, ester, or amide, and R2 and R3 are hydrogen, alkyl, alkoxy alkyl, hydroxy, alkenyl, ester, carboxylic acid or ether and wherein R1 is optionally omitted where R2 and R3 are not both hydrogen.

Abstract: Compounds of the formula ##STR1## in which R.sup.1 and R.sup.2 are as defined in the specification, and non-toxic metabolically labile ester and amides thereof are useful as modulators of metabotropic glutamate receptor function.

Abstract: A method for inhibiting mammalian cell growth is disclosed. The method uses compounds known as N-acetonylarylamides. The compounds have been shown to inhibit cell mitosis and to inhibit microtubule assembly. The method may be used to treat diseases associated with rapid cell growth, particularly cancer. The compounds used in the method of the present invention may be used in combination with other therapies and may be administered by known techniques for drug administration.

Abstract: The invention relates to new alkoximinoacetic acid amides, a process for their preparation and their use as agents for combating pests.

Abstract: 2-Cyano-3,5-dihydroxyhex-2-enecarboxamide derivatives ##STR1## are suitable for the production of pharmaceuticals for the prophylaxis and therapy of diseases or dissorders whose course involves increased connective tissue or cartilage degradation.

Abstract: Carboxamides of the formula I ##STR1## where the substituents have the following meanings: R.sup.1 is unsubstituted or substituted bicycloalkyl, tricycloalkyl or bicycloalkenyl;R.sup.2,R.sup.3 and R.sup.4 are each, independently of one another, hydrogen, or unsubstituted or substituted: alkyl, cycloalkyl, cycloalkenyl or heterocyclyl;Ar is unsubstituted or substituted aryl or hetaryl,but excluding 2-cyano-N-[1-(1-naphthyl)ethyl]-3-phenyl-bicyclo[2.2.1]hept-5-ene-2-carbox amide, a process for their preparation, compositions comprising compounds I and the use of compounds I for preparing the compositions, and further a process for controlling harmful fungi and the use of the compounds I for this purpose.

Abstract: Novel indane and indene derivatives are described which are endothelin receptor antagonists.

Abstract: The present invention relates to chromotropic nitrone spin trapping agents, methods of making these agents, compositions comprising same, and methods of their use. In particular, azulenyl nitrones of the present invention are effective agents for trapping free radical species and find use as efficient antioxidants in physicochemical and biological systems. Accordingly, the invention also relates to spin adducts formed from the combination of azulenyl nitrones with free radicals. The compounds of the present invention are readily prepared from available starting materials and find further use in assays and in a number of diagnostic, prophylactic and therapeutic applications, including but not limited to the alleviation, modulation and inhibition of the negative effects of carbon-centered or oxygen-centered radical species and other products of oxidation. Moreover, the combination adducts may be calorimetrically detected and, optionally, isolated and characterized to obtain valuable information (e.g.

Abstract: A method of inhibiting bacterial sialidase comprising administering to a subject an inhibiting effective amount of a compound of formula I: ##STR1## wherein A is CO.sub.2 H, PO.sub.2 H, or SO.sub.2 H; B is N; R.sub.1 and R.sub.2 are H; R.sub.3 and R.sub.4 are, independently, H, OH, NO.sub.2, guanidino, or alkyl or alkenyl of from 1 to 3 carbons where the alkyl or alkenyl is unsubstituted or is substituted, independently, with one or more of OH, NH2, or halide; R.sub.5 is H; and R.sub.6 is COCH.sub.3, or COCI.sub.3 ; or an analog, pharmaceutically acceptable salt, derivative, or mixture thereof. A method of preventing a bacterial or trypanosomal infection using the compounds of formula I. A method of treating a bacterial or trypanosomal infection using the compounds of formula I. A pharmaceutical composition comprising a pharmaceutically acceptable carrier admixed with an inhibiting effective amount of a compound of formula I.

Abstract: Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitrites thereof, and are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, as anti-viral and anti-fungal agents or pro-drugs of such agents.

Abstract: Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitriles thereof, and are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, as anti-viral and anti-fungal agents or pro-drugs of such agents.

Abstract: A method of using compounds of formula I ##STR1## in which the C.dbd.C double bond is present in E and/or Z configuration and the variables have the following meanings:R.sup.1 denotes COOR.sup.5, COR.sup.5, CONR.sup.5 R.sup.6, CN, O.dbd.S(--R.sup.5).dbd.O, O.dbd.S(--OR.sup.5).dbd.O, R.sup.7 O--P(--OR.sup.8).dbd.O;R.sup.2 denotes COOR.sup.6, COR.sup.6, CONR.sup.5 R.sup.6, CN, O.dbd.S(--R.sup.6).dbd.O, O.dbd.S(--OR.sup.6).dbd.O, R.sup.7 O--P(--OR.sup.8).dbd.O;R.sup.3 denotes hydrogen, an optionally substituted aliphatic, cycloaliphatic, araliphatic or aromatic radical having in each case up to 18 carbon atoms;R.sup.4 denotes an optionally substituted aromatic or heteroaromatic radical containing from 5 to 12 ring atoms;R.sup.5 toR.sup.8 independently denote hydrogen, an open-chain or branched-chain aliphatic, araliphatic, cycloaliphatic or optionally substituted aromatic radical containing in each case up to 18 carbon atoms,where the variables R.sup.3 to R.sup.

Abstract: Novel derivatives of fatty acid analogs that have from one to three heteroatoms in the fatty acid moiety which can be oxygen, sulfur or nitrogen, are disclosed in which the carboxy-terminus has been modified to form various amides, esters, ketones, alcohols, alcohol esters and nitriles thereof.These compounds are useful as substrates for N-myristoyltransferase (NMT) and/or its acyl coenzyme, and as anti-viral and anti-fungal agents or pro-drugs of such agents. Illustrative of the disclosed compounds are fatty acid amino acid analogs of the structure ##STR1## in which X is the ethyl or t-butyl ester of an amino acid such as Gly, L-Ala, L-Ile, L-Phe, L-Trp, L-Thr or an amide such as NHCH.sub.2 C.sub.6 H.sub.5 or NH(CH.sub.2).sub.2 C.sub.6 H.sub.5.

Abstract: An ester compound represented by the formula ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different and each represent a C.sub.1 -C.sub.6 alkyl group, or other specified groups, which may be optionally substituted with one or more halogen atoms; and R.sub.3 represents a pyrethroid acid residue (a group resulting from elimination of the carboxyl group from pyrethroid acid), and a pesticidal composition containing the ester compound as an active ingredient.

Abstract: A method for preventing settlement of aquatic fouling organisms on surface of an aquatic structure without environmental hazard is provided. The method is based upon absolutely novel concept to prevent the settlement by means of thick slime layer, i.e. bio-jelly, deposited on said surface. The present invention also provides a bio-jelly producing agent and a bio-jelly producing paint both useful for the present method. Further, the present invention provides a novel low toxic antifouling agent.

Abstract: The present invention is concerned with diaryl compounds of formula (l) and their use in medical therapy, particularly in the prophylaxis or treatment of a clinical condition for which an ACAT inhibitor is indicated, such as hyperlipidaema or atherosclerosis. The invention also relates to pharmaceutical compositions and processes for the preparation of compounds according to the invention.

Abstract: Substituted propane derivatives, a process for their preparation and the use of the compounds for treating diseasesPropane derivatives of the formula I ##STR1## in which the radicals have the meanings stated in the description, a process for the preparation of these compounds, their use as pharmaceuticals, and pharmaceutical products are described. Also described are novel intermediates for preparing the compounds of the formula I.

Abstract: The present invention relates to 2-cyano-3-mercaptocrotonamide derivatives, a process for their preparation, and their use the treatment of immune disorders, carcinomatous disorders, rejection reactions in transplantations and skin disorders or allergy.

Abstract: An insecticide composition is enhanced from the standpoint of its ability to be absorbed by insects, such as red fire ants, particularly dithiophosphate ester pesticides by the addition of a small amount of a water soluble non-aromatic polyorganic acid or salt form thereof such as polyaspartic acid, particularly preferred with a molecular weight in the range of about 3000 to 40,000.

Abstract: The invention relates to an insecticidal composition which comprises at least one pyrethroid, at least one UV absorbing agent and at least one antioxidant from the group consisting of tocopherol derivatives and citric acid esters. This insecticidal composition can in particular be used as an emulsion or on a powdery carrier for the control of flying and crawling insects such as flies and cockroaches.

Abstract: The invention relates to an insect repellent which contains at least one fatty acid alkyl ester having 1 to 4 carbon atoms in the alkyl group and at least one natural, nature-identical or synthetic fatty alcohol as the active substance and at least one natural or nature-identical vegetal or animal fatty oil as the carrier. The insect repellent serves for repelling flying, biting and sucking insects in man and beast and is applied onto the skin.

Abstract: Perfluoroalkyl-substituted benzoylguanidines, a process for their preparation, their use as a medicament or diagnostic agent, and a medicament containing themA description is given of perfluoroalkyl-substituted benzoylguanidines of the formula I ##STR1## where R(1) is (C.sub.1 -C.sub.6)-perfluoroalkyl-SO.sub.m ; R(2) and R(3) are H, halogen, alk(yl)(oxy), phenoxy; R(4) and R(5) are H, alkyl, Hal, CN, OR(7), NR(8)R(9), --(CH.sub.2).sub.n --(CF.sub.2).sub.o --CF.sub.3 and of the pharmacologically acceptable salts thereof; the compounds I are obtained by reacting a compound II ##STR2## with guanidine, L being a leaving group which is able readily to undergo nucleophilic substitution.

Abstract: A hydrazone compound of the general formula (I): ##STR1## wherein X is halogen; R.sup.1 is hydrogen, optionally substituted C.sub.1 -C.sub.4 alkyl or optionally substituted C.sub.1 -C.sub.4 alkoxy; R.sup.2 's are independently hydrogen or fluorine; R.sup.3 is a group of the general formula: CH.sub.2 R.sup.4 wherein R.sup.4 is cyano or C.sub.1 -C.sub.4 alkoxy; or R.sup.3 is a group of the general formula: SR.sup.5 wherein R.sup.5 is optionally substituted C.sub.1 -C.sub.16 alkyl; optionally substituted phenyl, or the like, has excellent insecticidal activity and rather low toxicity to mammals. The hydrazone compound is useful as an active ingredient of insecticides for controlling harmful insects.

Abstract: The cyclohexadiene derivatives are prepared by reaction of cyclohexanones with amines and subsequent dehydration. The compounds are suitable as active compounds in medicaments on account of their property of being selective modulators of calcium channel-dependent potassium channels.

Abstract: This invention provides a purified retro-retinoid compound characterized by a molecular mass of about 302 daltons. Also provided by this invention is a method of enhancing the growth of a cell in a vitamin A reduced environment which comprises contacting the cell with an effective growth enhancing amount of a compound having a structure: ##STR1## wherein the configuration of the C6, C8, C10 and C12 double bond independently is Z or E and the absolute configuration at C-14 is independently R or S; wherein R.sub.1 is alkyl, alkyl halide, alcohol, ester, ether, aldehyde, ketone, carboxylic acid, carboxylic ester, acid halide, amide, nitrile, or amine; and wherein R.sub.2 is hydroxyl, halide, alkoxy, ester, alkyl, alcohol, ether, aldehyde, ketone, carboxylic acid, carboxylic ester, nitrile, amine, azide, alkyl halide, acid halide, acid azide, or amide; or wherein R.sub.1 and R.sub.2 are replaced by a 14, 15-oxirane group; and wherein the retro structure is alpha or gamma.

Abstract: Substituted cyclohexane derivatives for the treatment of diseases Esters of cyclohexane derivatives of the formula I ##STR1## in which A--B, R.sup.3, R.sup.4, R.sup.5, Y and Z have the meanings indicated, for use as inhibitors of the glucose-6-phosphatase system of the liver in mammals are described. The compounds are suitable for the production of pharmaceutical preparations.

Abstract: 1-Ether and 1-thioether-naphthalene-2-carboxamides are described, methods of manufacture therefor and their use as agents which inhibit leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases, and their utility in inhibiting the activation of human immunodeficiency virus (HIV), latent in infected humans.

Abstract: Combating fungi with substituted amine acid derivatives of the formula ##STR1## in which R.sup.1 represents alkyl, alkenyl, alkinyl, halogenoalkyl, halogenoalkenyl, halogenoalkinyl, cycloalkyl or cycloalkenyl,R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are identical or different and represent hydrogen, cycloalkyl or alkyl, orR.sup.3 and R.sup.4, together with the carbon atom to which they are bonded, form a cycloalkyl ring, andR.sup.6 represents hydrogen, alkyl, alkenyl, alkinyl, cyanoalkyl, unsubstituted or substituted phenylalkyl, unsubstituted or substituted phenyl or unsubstituted or substituted cycloalkyl, or represents unsubstituted or substituted heterocyclyl or heterocyclylalkyl,orR.sup.5 and R.sup.6, together with the nitrogen atom to which they are bonded, represent a heterocyclyl radical, which can contain further hetero atoms.

Abstract: The invention concerns nitric acid esters of cyclohexanol of formula I ##STR1## in which A signifies a valency bond or a C.sub.1 -C.sub.6 -alkylene chain and B the group --NR.sup.1 --CO--Z, --NR.sup.1 --SO.sub.2 --Z or --CO--NR.sup.2 --Z, whereby R.sup.1 signifies hydrogen or a C.sub.1 -C.sub.6 -alkyl alkyl group R.sup.2 hydrogen, a hydroxyl, hydroxy-C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -alkoxy, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.2 -C.sub.6 -alkynyl group and Z signifies hydrogen a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.2 -C.sub.6 -alkynyl group which may optionally be substituted for the case that B is an --NR.sup.1 --CO--Z group, Z can also signify a C.sub.1 -C.sub.6 -alkoxy group.

Abstract: Modulators of neurotransmitter release including substituted guanidines, N"-aminoguanidines, and N,N'N",N"'-tetrasubstituted hydrazinedicarboximidamides, and pharmaceutical compositions thereof are disclosed. Also disclosed are methods involving the use of such neurotransmitter release modulators for the treatment or prevention of pathophysiologic conditions characterized by the release of excessive or inappropriate levels of neurotransmitters. Also disclosed are screening assays for compounds which selectively inhibit glutamate release. Also disclosed are methods of blocking voltage sensitive sodium and calcium channels in mammalian nerve cells.

Abstract: The present invention relates to novel benzoquinones which are useful as antihyperlipidemic agents. The present invention also provides a process for their preparation, pharmaceutical compositions, and a method for treating birds and mammals in need thereof which comprises administering to said host an effective amount of a benzoquinone of the present invention.

Abstract: Compounds of formula (II) ##STR1## wherein R.sub.1 and R.sub.2 are each separately selected from hydrogen, alkyl, alkenyl and alkynyl groups having up to a maximum of four carbon atoms and being unsubstituted, and alkyl, alkenyl and alkynyl groups having up to a maximum of three carbon atoms and being substituted by one, or in the case of fluoro by one or more, substituents but with the proviso that when R.sub.1 is hydrogen then R.sub.2 is hydrogen or methyl, or R.sub.1 and R.sub.2 together constitute an ethylene bridging group, and R.sub.3 is a group which under physiological conditions undergoes elimination with the formation of a 3,5-dioxopiperazinyl ring, with the further proviso that the compound is in the meso or erythro configuration when each of R.sub.1 and R.sub.2 is the same or different unsubstituted or substituted alkyl, alkenyl or alkynyl group, and salts thereof with a physiologically acceptable inorganic or organic acid, are of value as prodrugs, particularly for effecting cardioprotection.

Abstract: Novel pesticidal compositions, which are characterized by biodegradability and do not bioaccumulate to an unacceptable level in fats and tissues of animals, fowl and fish, containing active compounds and optionally a carrier suitable for administering said compounds to a pest by contact, ingestion or inhalation, are disclosed. Such compositions comprise in addition to the carrier compounds of the formula ##STR1## where R is H, Cl or other Hal, hydroxyl, lower alkoxyl, lower alkyl, cyano, CONR.sub.2 or NR.sub.2 where R.sub.