Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.

Abstract: A solution of hyaluronic acid and water-soluble salts thereof in a pharmaceutically acceptable media in which the hyaluronic acid concentration is at least about 0.4% by weight based on the weight of the solution and the solution having a viscosity at 25° C. of from about 500 to about 10,000 centipoises, serving as a carrier for medicaments to the peritoneal cavity.

Abstract: There are described new active compound combinations of a compound of the formula (I) 1

Abstract: A liquid pesticidal composition, which is substantially free of water, comprising a hydrophobic pesticide or mixture of pesticides dissolved in an organic solvent and comprising as surfactants (a) a castor oil ethoxylate having 30-50 mol ethoxylate, (b) a branched C8-C18 alcohol ethoxylate having 5-10 mol ethoxylate, and (c) a tristyrenephenol-ethoxylate having 8-30 mol ethoxylate, or its phosphate or salt thereof. The compositions also include gels having a viscosity of 500 to 20,000 mPas and comprising additionally a gelling agent.

Abstract: The present invention relates to insect repellant compositions containing, based upon the total weight of the composition, from about 6 to about 30 percent by weight of insect repellant active material having functionality selected from ester, amide, urethane or combinations thereof; from about 5 to about 30 percent by weight of alcohol, and from about 1 to about 10 percent by weight of nonionic surfactant. The compositions of the invention exhibit reduced rates of degradation of the active material in solution and are less drying and irritating to sensitive skin.

Abstract: Phenylacetic acid derivatives of the formula I where the substituents and the indexes have the meanings given in the specification, their salts, their preparation and their use.

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: Suspensions, emulsions or dispersions of therapeutically active agents which are water insoluble or water intolerant such as nutritional supplements, herbal products, drugs, bacteria, yeast, vitamins and minerals are prepared as suspensions in edible vegetable oils such as orange, lemon, soybean, cotton seed, peanut, canola corn oil, sunflower, safflower, palm kernel, palm and coconut. The active therapeutic agent may be in crystalline or amorphous form, it may be a liquid as for example an oil such as vitamin E or beta carotene, or a preparation of a comminuted plant structure such as flower, parts, leaf, stem, root or tree bark, or an extract of a dried plant structure, or a freeze dried preparation of a vital bacteria or yeast. The suspension is formed by active mixing of the active agent and oil.

Abstract: Oleamide is an endogenous fatty acid primary amide that possesses sleep-inducing properties in animals and has been shown to effect seratonergic systems and block gap junction communication in a structurally specific manner. Certain agents can serve both as an oleamide agonist and as an inhibitor of fatty acid amide hydrolase. Fatty acid amide hydrolase is responsible for the rapid inactivation of oleamide in vivo. The structural features of oleamide required for inhibition of gap junction-mediated chemical and electrical transmission in rat glial cells are defined. Effective inhibitors fall into two classes of fatty acid primary amides of which oleamide and arachidonamide are the prototypical members. Of these two, oleamide constitutes the most effective and its structural requirements for inhibition of the gap junction are well defined.

Abstract: A compound having formula (I): wherein R1 is a saturated or unsaturated chain of 1-5 carbons in length; and R2 is a saturated or unsaturated chain of 3-10 carbons in length; and A is selected from the group consisting of COOL and CONR′—R″, wherein L is a lipid moiety selected from the group consisting of glycerol, C3-20 fatty acid monoglycerides, C3-20 fatty acid diglycerides, hydroxy-C2-6-alkyl esters of C3-20 fatty acids, hydroxy-C2-6-alkyl esters of lysophosphatidic acids, lyso plasmalogens, lysophospholipids, lysophosphatidic acid amides, glycerophosphoric acids, sphingolipids, lysophosphatidylethanolamines, and N-mono and N,N-di-(C1-4)alkyl derivatives of the amines thereof; and R′ and R″ are each independently selected from the group consisting of hydrogen and a lower alkyl group comprising 1-5 carbon atoms; and pharmaceutically acceptable salts thereof. In addition, there is provided methods for using these compositions.

Abstract: This invention relates to pharmaceutical compositions and methods for effecting a neuronal activity using low molecular weight, small molecule carbamates and ureas having an affinity for FKBP-type immunophilins.

Abstract: A class of substituted b-amino acids are potent inhibitor of methionine aminopeptidase type 2 (MetAP2) and are thus useful in inhibiting angiogenesis and disease conditions which depend upon angiogenesis for their development such as diabetic retinopathy, tumor growth, and conditions of inflammation. Pharmaceutical compounds containing the compounds and methods of inhibiting methionine aminopeptidase-2, and angiogenesis are also disclosed.

Abstract: The invention provides adamantane derivatives, a process for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy.

Abstract: The present invention intends to provide a derivative of sphingosine analogue that is able to regulate the functions of sphigolipid, and its pharmaceutical compositions. The present invention is the derivatives of sphingosine analogues represented by the general formula (I) described below. In the formula, R1 and R2, which are the same or different each other, are hydrogen, alkyl groups having 1-4 carbon atoms, or acyl groups having 2-5 carbon atoms. R3 and R4, which are the same or different each other, are hydrogen or hydroxyl groups; or R3 and R4 make up a covalent bond. X1 is —(CH2)n—CO—NH—CH(R5)—R6 or —(CH2)m—O—CO—CH(R7)—R8.

Abstract: A method for increasing the effectiveness of a biocide is described. In the method, at least one biocide and at least one diethanolamide are applied to a substrate or aqueous system subject to the growth of microorganisms. The diethanolamide is applied in an amount effective to increase the biocidal activity of the biocide. Biocidal compositions are described where the biocide and the diethanolamide are present in a combined amount effective to control the growth of at least one microorganism. Methods for controlling the growth of microorganisms on various substrates and in various aqueous systems are also described. The combination of the biocide and the diethanolamide is particularly useful as a biocide in the leather industry, the lumber industry, the papermaking industry, the textile industry, the agricultural industry, and the coating industry, as well as in industrial process waters.

Abstract: There are described new active compound combinations of a compound of the formula (I) with known fungicidal active compounds, and their use for the control of phytopathogenic fungi.

Abstract: Use in medicaments for the treatment of chronic obstructive pulmonary disease of compounds of formula 1

Abstract: Non-peptide GnRH agents capable of inhibiting the effect of gonadotropin-releasing hormone are of the following general formula, where X1, X2, Y, and are defined variables: Such compounds and their pharmaceutically acceptable salts, multimers, prodrugs, and active metabolites are suitable for treating mammalian reproductive disorders and steroid hormone-dependent tumors as well as for regulating fertility, where suppression of gonadotropin release is indicated. Methods for synthesizing the compounds and intermediates useful in their preparation are also described.

Abstract: Yeast-derived fiber has been demonstrated, as described herein, to effectively improve the serum lipid profile in humans, when provided as a dietary supplement, without some of the disadvantages known to accompany dietary supplementation with oat fiber or psyllium fiber. Described herein are dietary supplements comprising yeast fiber, e.g., &bgr;-glucan or glucomannan, and further comprising folic acid or a salt thereof, vitamin B6, vitamin B12, and vitamin E. The dietary supplements of the invention can further comprise fats, carbohydrates and proteins, for example, and other ingredients added to formulate a food product. Such food products can be in the form, for example, of solid or semi-solid foods, such as food bars, pudding, or spreads. By including folate and vitamin B6, the dietary supplement provides a second benefit of suppressing the level of homocysteine in the blood.

Abstract: There are described new active compound combinations of a compound of the formula (I) with known fungicidal active compounds, and their use for combating phytopathogenic fungi.

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: The present invention relates to gel compositions comprising alkyl amides of tri-basic carboxylic acids and methods of making gel compositions.

Abstract: para-Aminomethylaryl carboxamides of Formula I are antagonists of VLA-4 and/or &agr;4&bgr;7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of asthma, allergies, inflammation, multiple sclerosis, and other inflammatory and autoimmune disorders.

Abstract: The present invention provides compounds that block calcium channels and have the Formula I: and pharmaceutically acceptable salts, esters, and pro-drugs thereof, wherein R1 and R2 are independently H, phenylcyclopentylcarbonyl, C1-C7 alkyl, cyclohexylmethyl, benzyl, C1-C5 alkylbenzyl, or C1-C5 alkoxybenzyl, A is —C(O)— or —CH2—; R3 is H or —CH3; R4 is C1-C4 alkyl or piperidin-1-ylethyl; R5 is phenyl-(CH2)n—, C1-C4 alkylphenyl-(CH2)n—, or halophenyl-(CH2)n—; and n is 1 or 2. The present invention also provides pharmaceutical compositions containing the compounds of Formula I and methods of using them to treat stroke, cerebral ischemia, head trauma, and epilepsy.

Abstract: A [6-(substituted-methyl)-3-cyclohexenyl]formamide derivative or a salt thereof expressed by the following Formula (I): wherein one of A and B is a hydrocarbon group of C10-30 expressed by R1 and the other is—(CH2)n-NR2R3; Z is —O—, —OCO—, —OCONR6— or —NR6—; R2 and R3 individually represent a hydrogen, lower alkyl, phenyl or benzyl group, or together represent a heterocycle having 3-7 members; —NR5—(CH2)n-NR2R3 or —NR6—(CH2)n-NR2R3 may be Group W, and —OCONR6—(CH2)n-NR2R3 may be —OCO—W, wherein W is a formula of: wherein ring E is a heterocycle of 6 or 7 members including two nitrogen atoms and R2 is a hydrogen, lower alkyl, phenyl or benzyl group; R4 is a halogen, lower alkyl, lower acyl, nitro, cyano, lower alkoxycarbonyl, carbamoyl, lower alkylcarbamoyl, lower alkylamino, lower acylamino, lower alkoxy or lower acyloxy group; each of R5 and R6 is a hydrogen, low

Abstract: The present invention provides the use of N-acetyl cysteine and its pharmaceutically acceptable salts and derivatives, for the preparation of a composition for treatment or prophylaxis of chronic ulcers. In particular, the treatment of venous ulcers, diabetic ulcers and decubitis ulcers.

Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.

Abstract: The subject of the invention is an agent for the permanent shaping of hair, characterized in that it contains as active keratin-reducing substance a compound in accordance with the general formula ##STR1## in which R.sub.1, R.sub.2 and R.sub.3 stand for H, carboxy or a straight- or branched-chain alkyl radical, monohydroxyalkyl radical or polyhydroxyalkyl radical with 1 to 6 carbon atoms respectively, on the condition thatnot all radicals R.sub.1 to R.sub.3 stand for H at the same time;if R.sub.1 and R.sub.2 stand for H, then R.sub.3 is carboxy or a branched alkyl, branched monohydroxyalkyl or branched polyhydroxyalkyl radical with 1 to 6 carbon atoms;if none of the radicals R.sub.1 to R.sub.2 stand for carboxy or have a branched alkyl, branched monohydroxyalkyl or branched polyhydroxyalkyl radical with 1 to 6 carbon atoms, then at least two of the radicals R.sub.1, R.sub.2 or R.sub.

Abstract: The present invention is directed to polymeric- prodrug transport forms of the formula: ##STR1## wherein: B is a leaving group, OH, a residue of a hydroxyl-containing moiety or ##STR2## wherein B.sub.1 is a leaving group, OH or a residue of a hydroxyl-containing moiety;Y.sub.1-2 are independently O or S;M is selected from either X or Q; wherein X is an electron withdrawing group and Q is a moiety containing a free electron pair positioned three to six atoms from C(.dbd.Y.sub.2); R.sub.2-5 are independently selected from the group consisting of hydrogen, C.sub.1-6 alkyls, C.sub.3-12 branched alkyls, C.sub.3-8 cycloalkyls, C.sub.1-6 substituted alkyls, C.sub.3-8 substituted cycloalkyls, aryls, substituted aryls, aralkyls, C.sub.1-6 heteroalkyls and substituted C.sub.1-6 heteroalkyls;(m) is zero or one;(n) is a positive integer;(p) is zero or a positive integer;Z is an electron withdrawing group; andR.sub.

Abstract: Anionic amino acid based surfactants are used to enhance antimicrobial effectiveness in topically administrable pharmaceutical compositions containing at least one active ingredient, a cationic preservative and an anionic polyelectrolyte, such as carboxyvinyl polymers, xanthan gum, polystyrene sulfonic acid polymers and cationic exchange resins.

Abstract: Compound of formula (I): ##STR1## wherein: T represents alkylene,A and B together form a naphthalene, dihydronaphthalene, or tetrahydronaphthalene group,R represents hydrogen, hydroxy, R' or OR', R' being as defined in the description,G.sub.1 represents halogen, a radical R.sub.1 or a group --O--CO--R.sub.1, R.sub.1 being as defined in the description,G.sub.2 represents a group selected from: ##STR2## X, R.sub.2 and R.sub.21 being as defined in the description, and medicinal products containing the same which are useful in the treatment of a condition related to the melatoninergic system.

Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.

Abstract: This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.

Abstract: The present invention provides novel compositions and methods relating to the treatment of Inflammatory Bowel Disease ("IBD"), most notably, Ulcerative Colitis, Crohn's Disease, Colitis and Diverticulitis. The invention relates to the discovery of a parasitic microsporidia infecting the epithelium cells lining the gastrointestinal tract of patients suffering from IBD. The discovery of this correlation between the disease and the microsporidia, described herein, led to the development of methods for the accurate diagnosis of patients suffering from IBD, and also of methods for treating such a patient in accordance with the invention. This discovery also provides for the development of animal models to further elucidate the mechanism of the disease and potential additional cures therefor.

Abstract: Inhibitors of oleamide hydrolase, responsible for the hydrolysis of an endogenous sleep-inducing lipid (1, cis-9-octadecenamide) were designed and synthesized. The most potent inhibitors possess an electrophilic carbonyl group capable of reversibly forming a (thio) hemiacetal or (thio) hemiketal to mimic the transition state of a serine or cysteine protease catalyzed reaction. In particular, the tight binding .alpha.-keto ethyl ester 8 (1.4 nM) and the trifluoromethyl ketone inhibitor 12 (1.2 nM) were found to have exceptional inhibitory activity. In addition to the inhibitory activity, some of the inhibitors displayed agonist activity which resulted in the induction of sleep in laboratory animals.

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 phenylenediamine derivative or a salt thereof in accordance with the present invention is expressed by the following formula 1: ##STR1## wherein A represents a group expressed by --CO--, --CH.sub.2 CO--, --CS--, or --SO.sub.2 --; Y represents a carbon atom or nitrogen atom; R.sub.1 represents a lower alkyl group; R.sub.2 represents a hydrogen, lower alkyl, alkenyl, benzyl, or benzoyl group; and each of R.sub.3 and R.sub.4 represents an alkyl group having 1-10 carbon atoms. The phenylenediamine derivative above mentioned, as a radical scavenger, has antioxidant effect and lipid peroxidation inhibitory activity so as to be available for inhibiting brain infarction or brain edema.

Abstract: Fish mycoses and single-cell ectoparasites on fish are controlled using an active compound suitable for inhibiting the mitochondrial respiratory chain at the stage of the b/c.sub.1 complex.

Abstract: There are described new active compound combinations of a compound of the formula (I) ##STR1## with known fungicidal active compounds, and their use for the control of phytopathogenic fungi.

Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided. The compound of formulae IIA, having the structure: ##STR1## wherein R.sub.1, R.sub.2 ;X.sub.4, X.sub.5 ; andAr and n are as described in the specification.

Abstract: Novel phytosphingosine-based analogs of ceramide I, methods for the preparation of these novel compounds, cosmetic and pharmaceutical compositions containing such compounds, and methods for the use thereof are described.

Abstract: Fluorinated butyric acid compounds and derivatives are described as well as acid methods for the preparation and pharmaceutical compositions of same, which are useful as inhibitors of matrix metalloproteinases, particularly gelatinase A (72 kD gelatinase) and stromelysin-1, and also collagenase, matrilysin, and MMP-13, and for the treatment of multiple sclerosis, atherosclerotic plaque rupture, aortic aneurism, heart failure, restenosis, periodontal disease, corneal ulceration, treatment of burns, decubital ulcers, wound healing, cancer, inflammation, pain, arthritis, or other autoimmune or inflammatory disorders dependent upon tissue invasion by leukocytes or other activated migrating cells, acute and chronic neurodegenerative disorders including stroke, head trauma, spinal cord injury, Alzheimer's disease, amyotrophic lateral sclerosis, cerebral amyloid angiopathy, AIDS, Parkinson's disease, Huntington's disease, prion diseases, myasthenia gravis, and Duchenne's muscular dystrophy.

Abstract: Compounds having kappa opioid agonist activity, compositions containing them and method of using them as analgesics and anti-pruritic agents are provided.The compounds of formula III having the structure: ##STR1## wherein Ar and X.sup.7 ;R.sub.1 and R.sub.2 ; andn are as described in the specification.

Abstract: A pharmaceutical or veterinary composition comprising a compound of formula I ##STR1## wherein X is a --CO.sub.2 H group and R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 are as defined in the specification, or a salt, hydrate or solvate thereof, and a pharmaceutically or veterinarily acceptable excipient or carrier. A method of treatment of diseases or conditions mediated by MMPs in mammals, such as rheumatoid arthritis, osteoarthritis, periodontitis, gingivitis, corneal ulceration or tumour invasion by secondary means, by administering to the mammal an effective amount of the composition.

Abstract: The present invention relates to methods of preventing or treating an infection or disease caused by an infectious agent. The present invention also relates to the augmentation of the efficacy of existing anti-infective agents by the co-administration of the compounds described herein.

Abstract: A naphthyloxyacetic acid derivative of the formula (I) ##STR1## wherein R.sup.1 is H, alkyl, alkylene-(--COOR.sup.10, --OH, --CONR.sup.4 R.sup.5, --CONR.sup.6 -alkylene-OH, --NR.sup.4 R.sup.5, -cyano or -tetrazolyl); A is single bond, alkylene, alkenylene, --S-alkylene, --O-alkylene; B is NR.sup.3 CO, CONR.sup.3 ; R.sup.2 is (1) alkyl (2) alkenyl, (3) alkyl or alkenyl substituted by 1-3 of phenyl, cycloalkyl, naphthyl and heterocyclic ring containing nitrogen atom (the said ring may be substituted by 1-3 of alkyl, alkoxy and halogen etc.), (4) NR.sup.7 R.sup.8 or (5) alkylene-NR.sup.7 R.sup.8 ; non-toxic salt thereof, non-toxic acid addition salt thereof and hydrate thereof can bind the PGE.sub.2 receptor and exhibits the activity to antagonize or agonize for PGE.sub.2., therefore, they are useful as PGE.sub.2 antagonist or PGE.sub.2 agonist.

Abstract: The present invention relates to novel fluorobutenyl aminocarboxylates of the formula (I)R--CO--O--CH.sub.2 --CH.sub.2 --CX.dbd.CF.sub.2 (I)in whichX represents hydrogen or halogen andR represents one of the groups ##STR1## (b) R.sup.3 --A--CO--NR.sup.4 --CR.sup.5 R.sup.6 -- or ##STR2## in which A, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each as defined in the description, to processes for their preparation and to their use for controlling animal pests.

Abstract: Plant disease caused by soil-borne fungus Gaeumannonyces graminis (Gg) is controlled by applying to the seed or the soil a fungicide which has the following general formula: ##STR1##

Abstract: An agent for contact lenses, comprising chloroacetamide. According to the present invention, chloroacetamide, which is the bacteriocidal component to be contained, is scarcely adsorbed not only to hard contact lenses and gas-permeable hard contact lenses, but also to soft contact lenses, and even if adsorbed, moreover, chloroacetamide is quickly released and is not accumulated on the contact lens to a greater extent. The inventive agent containing, in addition to chloroacetamide, sodium lauryl sulfate shows more superior bacteriocidal effect and cleaning effect. Therefore, the present invention provides an agent for contact lenses having superior bacteriocidal effect and cleaning effect, which can be used safely and with ease for various contact lenses inclusive of soft contact lenses.

Abstract: Compounds containing two aromatic systems covalently linked through a linker containing one or more atoms, or "linker" defined as including a covalent bond per se so as to space the aromatic systems at a distance 1.5-15 .ANG., are effective in treating conditions associated with bone deficits. The compounds can be administered to vertebrate subjects alone or in combination with additional agents that promote bone growth or that inhibit bone resorption. They can be screened for activity prior to administration by assessing their ability to effect the transcription of a reporter gene coupled to a promoter associated with a bone morphogenetic protein and/or their ability to stimulate calvarial growth in model animal systems.