Abstract: The present invention concerns prodrugs whose aromatic oxidation, particularly their enzymatic aromatic hydroxylation, results in their activation by the release of a drug moiety. It particularly concerns anti-tumor prodrugs and those which are specifically activated by the hydroxylation activity of the P-450 enzyme CYP1B1. Also provided are methods of detection of aromatic oxidation activity.

Abstract: The present invention provides novel aminoindenes having the structure: wherein n is 1 or 2, R1 is hydrogen, linear or branched chain C1-C8 alkyl or linear or branched chain C1-C8 alkoxy and R2 is hydrogen or a halogen. Such compounds may be used to treat neurodegenerative conditions such as Alzheimer's disease, head trauma, stroke, hypoxia, anoxia, epilepsy, convulsions, seizures.

Abstract: This invention relates to compositions and methods for achieving a therapeutic effect such as lowering blood pressure and treating congestive heart failure in a mammal. More specifically, this invention relates to synergistic compositions comprising amounts of at least two therapeutic agents selected from the group consisting of a renin inhibitor, an angiotensin I converting enzyme inhibitor and an angiotensin II antagonist, which inhibitors and antagonists are present in amounts sufficient to cause synergistic therapeutic effects such as lowering blood pressure and treating congestive heart failure in a mammal.

Abstract: This invention is a method for preventing or treating postoperative ileus comprising administering a vasopressin antagonist such as a compound of Formula (1), where R1, R2, and R3 include hydrogen, halo, alkyl, and alkoxy; R and R5 are hydrogen or alkyl; R4 is hydrogen, phenyl, or substituted phenyl, and pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to novel thiourca derivatives as a modulator for vanilloid receptor (VR) and the phar- maceutical compositions containing the same. As diseases associated with the activity of vanilloid receptor, pain acute pain, chronic pain, neuropathic pain, post-operative pain, migraine, arthralgia, neuropathies, nerve injury, diabetic neuropathy, neurodegeneration, neurotic skin disorder, stroke, urinary bladder hypersensitiveness, irritable bowel syndrome, a respiratory disorder such as asthma or chronic obstructive pulmonary disease, irritation of skin, eye or mucous membrane, fervescence, stomach-duodenal ulcer, inflam- matory bowel disease and inflammatory diseases can be enumerated. The present invention provides a pharmaceutical composition for prevention or treatment of these diseases.

Abstract: This invention is directed to compounds of the following formula: wherein when a is 0, b is 1 or 2; when a is 1, b is 1, m is from 0-3, X is O or S, Y is halogeno, R1 is hydrogen C1-4 alkyl, R2 is hydrogen, C1-4 alkyl, or optionally substituted propargyl and R3 and R4 are each independently hydrogen, C1-6 alkyl, C6-12 aryl, C6-12 aralkyl each optionally substituted. This invention is also directed to the use of these compounds for treating depression, Attention Deficit Disorder (ADD), Attention Deficit and Hyperactivity Disorder (ADHD), Tourette's Syndrome, Alzheimer's Disease and other dementia's such as senile dementia, dementia of the Parkinson's type, vascular dementia and Lewy body dementia. This invention is further directed to a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

Abstract: A pesticidal composition and anti-parasitic treatment using the same, wherein the composition includes, in a combined pesticidally effective amount (a) carbaryl and (b) a compound having the formula wherein: R1 is CN; R2 is S(O)nR3, 4,5-dicyanoimidazol-2-yl or haloalkyl; R3 is alkyl or haloalkyl; R4 is hydrogen, halogen, NR5R6, S(O)mR7, C(O)R7, C(O)O—R7, alkyl, haloalkyl, OR8 or —N═C(R9)(R10); R5 and R6 independently are hydrogen, alkyl, haloalkyl, C(O)alkyl, alkoxycarbonyl or S(O)rCF3; or R5 and R6 together form a divalent alkylene radical which is optionally interrupted by one or two divalent heteroatoms selected from the group consisting of oxygen and sulfur; R7 is alkyl or haloalkyl; R8 is alkyl, haloalkyl or hydrogen; R9 is alkyl or hydrogen; R10 is phenyl or heteroaryl optionally substituted by one or more halogen, OH, —O-alkyl, —S-alkyl, cyano or alkyl; R11 and R12 are, independently of each other, hydrogen, halogen, CN or NO2; R13 is halogen, haloalkyl, h

Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.

Abstract: This invention is directed to compounds of the following formula: 1

Abstract: The invention provides for astringent compositions comprising from about 0.1% to about 20% by weight of an astringent and between about 0.1% to 10% by weight of alcohol. The compositions have viscosity values of at least about 5,000 centipoise. The invention also provides for a method of using such compositions for delivering a topically active agent, such as salicylic acid, into skin.

Abstract: The invention provides novel non-&bgr;-lactam inhibitors of &bgr;-lactamases. In particular, the invention provides such inhibitors which are boronic acids of formula (1) which is set forth in the specification. These compounds may be used with &bgr;-lactam antibiotics to treat &bgr;-lactam-antibiotic-resistant bacterial infections. These compounds are also antibacterial by themselves. Finally, the invention provides a pharmaceutical composition comprising these compounds.

Abstract: The present invention relates to pesticide compositions. In particular, the present invention relates to pesticide compositions comprising a pesticide and a redispersible polymer and to a method for controlling agricultural pests by applying to the pest or the locus of the pest a pesticide composition comprising a pesticide and a redispersible polymer.

Abstract: A wood treatment material having a synergistic combination of fungicides including boron-containing compounds, organo-iodine compounds and amine-oxides is provided. This combination is shown to be especially effective in providing resistance to decay, mold and mildew when wood is treated with this combination. Also provided is wood treated by this combination, and a method of treatment for composite wood.

Abstract: The invention provides novel non-&bgr;-lactam inhibitors of &bgr;-lactamases. In particular, the invention provides such inhibitors which are boronic acids of formula (1) which is set forth in the specification. These compounds may be used with &bgr;-lactam antibiotics to treat 62 -lactam-antibiotic-resistant bacterial infections. These compounds are also antibacterial by themselves. Finally, the invention provides a pharmaceutical composition comprising these compounds.

Abstract: The present invention relates to urethanes and the thio and dithio analogues thereof of general formula wherein m, n, A, X, Y and R1 to R8 are defined as in claim 1, the enantiomers, diastereomers and the salts thereof, particularly the physiologically acceptable acid addition salts thereof which have valuable properties, particularly an inhibitory effect on cholesterol biosynthesis, pharmaceutical compositions containing these compounds, their use and processes for preparing them.

Abstract: The invention concerns the use of &bgr;2-adrenergic modulators for regulating cellular apoptosis.

Abstract: This invention is directed to compounds of the following formula wherein when a is O, b is 1 or 2; when a is 1, b is 1, m is from 0-3 X is O or S, Y is halogeno, R1 is hydrogen C1-4 alkyl, R2 is hydrogen, C1-4 alkyl, or optionally substituted propargyl and R3 and R4 are each independently hydrogen, C1-8 alkyl, C6-12 aryl, C6-12 aralkyl each optionally substituted. This invention is also directed to the use of these compounds for treating depression, Attention Deficit Disorder (ADC), Attention Deficit and Hyperactivity Disorder (ADHD), Tourette's Syndrome, Alzheimer's Disease and other dementia's such as senile dementia, dementia of the Parkinson's type, vascular dementia and Lewy body dementia. This invention is further directed to a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

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: Non-greasy topical solutions, emulsion gels or lotions comprising as the active agent a compound of formula I ##STR1## and a lower alkanol, and if desired together with a solubilizing agent or an oil phase such as isopropyl myristate are useful delivery systems.

Abstract: A topical mycological treatment composition for medical, veterinarian, or dental use contains as active ingredients clotrimazole, ketoconazole, micanazole, nystatin, tolnaftate, propionic acid, sodium propionate, undecelynic acid, and zinc undecelynate. These ingredients are contained in a natural cream base, and the base may also contain an anti-inflammatory agent and an antibacterial agent.

Abstract: An antifungal preparation for topical use is described containing tolnaftate and a quaternary ammonium compound. The formulation contains tolnaftate at a pharmaceutical effective concentration along with a quaternary ammonium compound such as benzalkonium chloride along with other ingredients. The resultant product is dramatically faster acting and significantly more potent than known tolnaftate formulations alone.

Abstract: The invention provides novel non-.beta.-lactam inhibitors of .beta.-lactamases. In particular, the invention provides such inhibitors which are boronic acids of formula (1) which is set forth in the specification. These compounds may be used with .beta.-lactam antibiotics to treat .beta.-lactam-antibiotic-resistant bacterial infections. These compounds are also antibacterial by themselves. Finally, the invention provides a pharmaceutical composition comprising these compounds.

Abstract: A water-free concentrate comprising, by weight,(a) 3-20% of amitraz insecticide, optionally with other agriculturally active chemicals, for example, a pyrethroid;(b) 30-80% of a nonionic surfactant having an HLB <7, and(c) 5-30% of a C.sub.1 -C.sub.8 alkyl pyrrolidone solvent.Clear, pour-on formulations of about 5-60% by weight of the concentrate and 40-95% of an oil are described.

Abstract: Non-greasy topical solutions, emulsion gels or lotions comprising as the active agent a compound of formula I ##STR1## and a lower alkanol, and if desired together with a solubilizing agent or an oil phase such as isopropyl myristate are useful delivery systems.

Abstract: Methods and compositions for decreasing the production of methane in ruminant animals, thereby increasing feed utilization efficiency, are disclosed. The methods employ HMG-CoA reductase inhibitors to selectively inhibit the growth of methane-producing bacteria without significantly inhibiting the growth of non-methanogens.

Abstract: This invention relates to the treatment of atherosclerosis via raising the level of HDL cholesterol by administration of a compound of the formula ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.0-6 Ph where Ph is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH;R.sub.4 and R.sub.5 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, or --(CH.sub.2).sub.0-6 Ar.sup.1 where Ar.sup.1 is phenyl, naphthyl, furanyl, pyridinyl or thenyl and Ar.sup.1 can be optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH; andAr is phenyl, naphthyl, furanyl, pyridinyl or thienyl or Ar is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.

Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.

Abstract: This invention relates to the treatment of atherosclerosis via raising the level of HDL cholesterol by administration of a compound of the formula ##STR1## wherein: R.sup.1, R.sup.2, and R.sup.3 are independently hydrogen, C.sub.1 -C.sub.6 alkyl or --(CH.sub.2).sub.0-6 Ph where Ph is phenyl optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH;R.sup.4 and R.sup.5 are independently hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.8 cycloalkyl, or --(CH.sub.2).sub.0-6 Ar.sup.1 where Ar.sup.1 is phenyl, naphthyl, furanyl, pyridinyl or thienyl and Ar.sup.1 can be optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, phenyl, C.sub.1 -C.sub.6 alkoxy, phenoxy, trifluoromethyl, C.sub.1 -C.sub.6 alkoxycarbonyl, --CO.sub.2 H or OH; andAr is phenyl, naphthyl, furanyl, pyridinyl or thienyl or Ar is optionally substituted by halogen, cyano, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.

Abstract: Use of compounds of formula (I), wherein R has various significances, in free base form or in pharmaceutically acceptable salt form, as agents against H. pylori infection and associated diseases.

Abstract: A compound of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent H or an optionally substituted hydrocarbon group; R.sup.3 represents an optionally substituted hydrocarbon group; R.sup.4 represents H or a hydrocarbon group; ring A represents a substituted benzene ring; X represents a C.sub.2-4 alkylene group etc.; and Y represents a bond or a lower alkylene group, or salts thereof is useful as prophylactic or therapeutic agents of diseases related with melatonin activity.

Abstract: In accordance with the present invention, there are provided methods for the in vivo reduction of free iron ion levels in a mammalian subject. The present invention employs a scavenging approach whereby free iron ions are bound in vivo to a suitable physiologically compatible scavenger. The resulting complex renders the free iron ions harmless, and is eventually excreted in the urine of the host. Further in accordance with the present invention, there are provided compositions and formulations useful for carrying out the above-described methods. An exemplary scavenger contemplated for use in the practice of the present invention is a dithiocarbamate-containing composition. This material binds to free iron ions, forming a stable, water-soluble dithiocarbamate-iron complex.

Abstract: A pharmaceutical composition of all fluoroquinolones, including but not limited to, ciprofloxacin, ofloxacin, enoxacin, cinoxacin, pefloxacin, lomefloxacin, norfloxacin, tosufloxacin, fleroxacin, temafloxacin, trovafloxacin, and difloxacin, mixed with benzoyl peroxide in a vehicle for the topical treatment of a variety of skin conditions. The topical antibiotic and peeling agent will be in the form of a cream, ointment, lotion, gel, suspension, emulsion, cleansing bar, pledget, salve, tincture, spray, transdermal device, or other appropriate non-toxic pharmaceutical carrier.

Abstract: Compounds of formula (I) and salts, esters and amides thereof, wherein R.sup.1 is a C.sub.1-6 straight or branched chain alkyl group, a C.sub.3-6 cycloalkyl group, a thiol group optionally substituted by a C.sub.1-6 alkyl group, or an amino group optionally substituted by one or two alkyl or alkenyl groups; R.sup.2 is H, C.sub.1-7 straight or branched chain alkyl, C.sub.3-6 cycloalkyl, C.sub.2-7 alkenyl or benzyl; A is a 5 or 6 membered aromatic carbocyclic or heterocyclic ring which may optionally be substituted by one or more suitable substituents such as C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, halo, nitro, cyano, trifluoro C.sub.1-6 alkyl, amino, C.sub.1-6 alkylamino or di C.sub.1-6 alkylamino; r is 0, 1 or 2; their use in medicine and in particular for conditions requiring inhibition of the NO Synthase enzyme, pharmaceutical formulations and processes for the preparation thereof are disclosed.

Abstract: A pesticidal composition to noxious organisms which comprises a diarylalkane and an active component effective for killing or repelling noxious organisms and the diarylalkane is at least one member selected from the group consisting of butyl diphenylmethane, butyl-1,1-diphenylethane and butyl-1,2-diphenylethane. The used diarylalkane has a high dissolving power to the effective component, a high boiling point and a high flash point with low unpleasant smell and does not deteriorate the effective component in the pesticidal composition.

Abstract: Non-greasy topical solutions, emulsion gels or lotions comprising as the active agent a compound of formula I ##STR1## and a lower alkanol, and if desired together with a solubilizing agent or an oil phase such as isopropyl myristate are useful delivery systems.

Abstract: The invention concerns tachykinin antagonists. The compounds are neopeptides which have utility in treating disorders mediated by tachykinins. Such disorders are respiratory, inflammatory, gastrointestinal, ophthalmic, allergies, pain, vascular, diseases of the central nervous system, and migraine. Methods of preparing compounds and novel intermediates are also included. The compounds are expected to be especially useful in asthma and rheumatoid arthritis.

Abstract: Tachykinin receptor antagonists are useful for the treatment of cystic fibrosis.

Abstract: The invention relates to a plaster for the treatment of nail mycoses, which s characterized by an antimycotically active substance, clotrimazole and bifonazole being excluded.

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: Non-greasy topical solutions, emulsion gels or lotions comprising as the active agent a compound of formula I ##STR1## and a lower alkanol, and if desired together with a solubilizing agent or an oil phase such as isopropyl myristate are useful delivery systems.

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 present invention provides a method of inhibiting gastric acid secretion in mammals by administering a 5-HT1A agonist compound or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides novel ring-substituted 2-amino-1,2,3,4-tetrahydronaphthalenes, 3-aminochromanes, and 3-aminothiochromanes, including their corresponding sulfoxides and sulfones, which ring-substituted compounds exhibit agonist activity at the serotonin 1A receptor.

Abstract: A method of inhibiting blood-platelet aggregation in warm-blooded animals comprising administering to warm-blooded animals a blood-platelet aggregation inhibiting effective amount of a compound selected from the group consisting of a compound of the formula ##STR1## wherein R is selected from the group consisting of --NH--CO--NH.sub.2, --NH--CO--CH.sub.3, --OH and their non-toxic, pharmaceutically acceptable acid addition salts.

Abstract: Novel 1-alkyl-, 1-alkenyl-, and 1-alkynylaryl-2-amino-1,3-propanediols, intermediates and processes for the preparation thereof, and methods of reducing inflammation and cell proliferation, and relieving memory dysfunction, and inhibiting bacterial and fungal growth are disclosed.

Abstract: The present invention provides novel HIV protease inhibitors, pharmaceutical formulations containing those compounds and methods of treating and/or preventing HIV infection and/or AIDS.

Abstract: The compounds of this invention which have the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1 -C.sub.8 alkyl, halogen, C.sub.1 -C.sub.8 alkoxy, or trifluoromethyl;R.sup.3 is --OH or --NHCO.sub.2 CH.sub.3 ;X is --CH.sub.2 -- or --OCH.sub.2 --;n is 1 or 2;or a pharmaceutically acceptable salt thereof,are useful in treating or inhibiting the long-term complications of diabetes such as diabetic retinopathy, nephropathy and neuropathy through the inhibition of the enzyme aldose reductase. Aldose reductase inhibitors have been shown to prevent the biochemical, functional and morphological changes induced by hyperglycemia.

Abstract: Carboxylic acid derivatives of the formula: ##STR1## are provided, which are useful for treatment of androgen dependent diseases.

Abstract: The present invention is directed to compounds of the following general Formula I, methods for using the compounds of Formula I, pharmaceutical compositions thereof, and processes for preparing the compounds. ##STR1## wherein X is oxygen or sulfur; wherein R is hydrogen, a straight or branched alkyl group having from 1 to 8 carbon atoms or benzyl;wherein each of R.sub.1 and R.sub.2 is phenyl, substituted phenyl, naphthyl, substituted naphthyl, an aralkyl group, a 5- or 6-membered monocyclic or fused bicyclic heterocyclic group, or a hydrocarbon chain having from 1 to 20 carbon atoms and from 1 to 3 double bonds.

Abstract: Alpha-Arylacrylic acid derivatives of the general formula I ##STR1## where X is ethylene or ethenylene; n is 0 or 1;m is 0, 1, 2, 3 or 4;R.sup.1 is cyano, cyanato, thiocyanato, nitro, hydroxyl, carboxyl, haloalkyl, haloalkoxy, unsubstituted or substituted cycloalkyl, cycloalkenyl, cycloalkadienyl, alkenyl, alkynyl or amino, alkylcarbonyl, alkoxycarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, unsubstituted or substituted benzyloxycarbonyl, benzoyl, phenylalkyl, phenylalkoxy or phenoxyalkyl,or R.sup.1 together with one of the radicals R.sup.2 forms an unsubstituted or substituted 1,3-butadiene-1,4-diyl group or an unsubstituted or substituted chain consisting of carbon members and an oxygen member, andR.sup.2 is halogen, unsubstituted or substituted alkyl, alkoxy, alkenyloxy, alkynyloxy, alkadienyloxy, benzyloxy or benzylthio, are used for controlling pests.