Abstract: The present invention provides combinations of cardiovascular therapeutic compounds for the prophylaxis or treatment of cardiovascular disease including hypercholesterolemia, atherosclerosis, or hyperlipidemia. Combinations disclosed include a nicotinic acid derivative combined with a cholesteryl ester transfer protein (CETP) inhibitor.

Abstract: A polymer comprising recurring units represented by formula (I): wherein X is selected from the group consisting of C(O)OR1, C(O)SR1, C(O)NR1R2, and VZ, where R1 and R2 are each individually selected from the group consisting of hydrogen, C1 to C10 alkyl, and C6 to C10 aryl, where V is a labile linker group, and where Z is selected from the group consisting of poly(ethyleneimine), poly(propyleneimine), poly(lysine), PAMAM dendrimer, octaamine dendrimer, and hexadecaamine dendrimer; and wherein Y is selected from the group consisting of —(CH2)2—, —(CH2)2—O—(CH2)2—, —(CH2)2—O—(CH2)2—, and —(CH2)3—NHC(O)—(CH2)6—C(O)NH—(CH2)3— is useful in nucleic acid delivery applications. Polyacetals of the formula (I) are preferably made by reacting appropriate diols and divinyl ethers. In preferred embodiments, complexes formed between polyacetals of the formula (I) and polynucleotides are useful as transfection reagents.

Abstract: Disclosed are anti-viral compositions containing at least one zinc compound and at least one phenolic antioxidant (and optionally other ingredients), and a pharmaceutical carrier. Also disclosed are methods of treating lesionous symptoms of a viral infection involving applying an effective amount of the anti-viral composition to the lesions.

Abstract: Pulmonary surfactant is required in order to reduce surface tension in the lungs so that less effort is needed to reinflate the lungs after exhalation. A number of diseases and conditions exist that disrupt the normal flow of surfactant secretion, resulting in respiratory distress or failure. The present invention provides a method of treating a patient in respiratory distress syndrome wherein a surfactant deficiency has occurred, thereby restoring a normal respiratory function.

Abstract: Nanobacteria contribute to pathological calcification in the human and animal body, including diseases such as kidney stones, salivary gland stones, dental pulp stones and atherosclerosis. The present invention provides methods for sterilizing articles contaminated with nanobacteria. The present invention also provides methods of treating patients infected with nanobacteria. In particular, the present invention provides a method for preventing the recurrence of kidney stones in a patient that has suffered from kidney stones, comprising administration of an antibiotic, a bisphosphonate, or a calcium chelator, either alone or in combination, in an amount effective to inhibit or prevent the growth and development of nanobacteria.

Abstract: The invention relates to a pharmaceutical composition comprising at least one phenol derivative represented by formula (I) 1

Abstract: Pressurized aerosol composition for administration by inhalation comprising a liquefied hydrofluoroalkane, a powdered medicament dispersed therein, and a suspending agent comprising a polymer soluble in the liquefied hydrofluoroalkane which is selected from polymers including recurring amide containing structural units, copolymers of amide containing units and carboxylic acid ester units, polyvinylacetate and acrylic acid/methacrylic acid ester copolymers.

Abstract: Disclosed are methods and compositions for regulating the melanin content of mammalian melanocytes; regulating pigmentation in mammalian skin, hair, wool or fur; treating or preventing various skin and proliferative disorders; by administration of various compounds, including alcohols, diodls and/or triols and their analogues.

Abstract: Biphenyl substituted amides with activity as antagonists of the neurokinin 1 (NK-1, substance P) receptor.

Abstract: There are described a flowable composition for controlling harmful insects and representatives of the order Acarina, comprising at least one pesticidally active compound, one or more signal substances selected from the group consisting of pheromones, kairomones and attractants, a UV absorber or a UV absorber mixture and, if appropriate, one or more additives selected from the group consisting of viscosity-regulating thickeners, fillers, solvents and other formulation auxiliaries, which composition comprises 40 to 98% by weight of the UV absorber or the UV absorber mixture, 0.01 to 30% by weight of one or more signal substance(s) and 0.1 to 20% by weight of one or more pesticidally active compound(s) of the formulae (I) to (V) as specified, and a method of controlling harmful insects and representatives of the order Acarina using this composition.

Abstract: The present invention provides combinations of cardiovascular therapeutic compounds for the prophylaxis or treatment of cardiovascular disease including hypercholesterolemia, atherosclerosis, or hyperlipidemia. Combinations disclosed include a nicotinic acid derivative combined with a cholesteryl ester transfer protein (CETP) inhibitor.

Abstract: The invention is directed to pharmaceutical compositions useful in the treatment of migraine. The compositions contain metoclopramide and one or more NSAIDs in unit dosage form. By selecting NSAIDs that are non-acidic or segregating the metoclopramide and NSAID, the storage life of the compositions has been increased. Also disclosed are coordinated dosage forms for the sequential release of drugs. The invention encompasses methods of treating migraine using any of these dosage forms.

Abstract: The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents.

Abstract: A dry powder formulation for treatment of pulmonary conditions, via inhalation, includes an effective amount of formoterol or a salt or solvate thereof, in a dry powder form, an effective amount of fluticasone, in a dry powder form, and an excipient. A method for preparing a physically stable dry powder formulation for inhalation includes the steps of micronizing a first active polar drug, a second active non-polar drug, and a polar excipient. The second non-polar active drug is first blended with the excipient to form an intermediate mixture. The intermediate mixture is then blended with the first active polar drug. The increased separation of the polar drug and polar excipient stabilizes the formulation.

Abstract: The present invention includes methods for treatment and prophylaxis of eye disorders and injuries, particularly treatment and prophylaxis of ocular neovascularization and disorders, especially a vasculopathy that affects retinal or chorodial vessels. The methods of the invention in general comprise administration of a therapeutically effective amount of a compound that inhibits farnesyl-protein transferase to a subject suffering from or susceptible to ocular neovascularization or associated disorder.

Abstract: The present invention describes novel nitrosated and/or nitrosylated phosphodiesterase inhibitors, and novel compositions containing at least one nitrosated and/or nitrosylated phosphodiesterase inhibitor, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one phosphodiesterase inhibitor, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents.

Abstract: A method of inhibiting or preventing the growth of tumor cells is disclosed. In one embodiment, this method comprises the step of administering a compound selected from the group consisting of citracetal, citral dimethyl acetal, citral diethyl acetal, geranyl benzoate, geranyl tiglate, geranyl anthranilate, farnesyl benzoate, farnesyl anthranilate, farnesyl tiglate, farnesyl acetate and combinations thereof to a human tumor patient, wherein the amount is effective to reduce or inhibit tumor growth by at least 50%.

Abstract: Disclosed are methods and compositions for regulating the melanin content of mammalian melanocytes; regulating pigmentation in mammalian skin, hair, wool or fur; treating or preventing various skin and proliferative disorders; by administration of various compounds, including alcohols, diols and/or triols and their analogues.

Abstract: The present invention describes a process for the preparation of aqueous formulations containing azithromycin for ophthalmic use, as well any formulations obtained by this process and their topical use in the ocular bacterial infections, more preferably in the treatment of conjunctivitis, keratitis and blepharitis.

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: Composition and methods of alleviating impaired mental function and memory loss in mammals and reducing the recovery time from anaesthesia in age mammals, comprising treating the mammal with a non-toxic, enhancing effective amount of a cell membrane permeant calcium buffer. The buffer is preferably a calcium ion chelating agent having a KD selected from the range 1×10−4 to 1×10−8 Molar and being essentially calcium ion-selective over other metal ions. A most preferred buffer is BAPTA-AM.

Abstract: The present invention relates to a leave-on antimicrobial composition comprising from about 0.001% to about 5% of an antimicrobial active; from about 0.5% to about 10% of an anionic surfactant; from about 0.1% to about 10% of a proton donating agent, wherein the proton donating agent is such that the composition is essentially free of C4-C20 alkyl fatty acid; and from about 0% to about 98.85% of water; wherein the composition is adjusted to a pH of from about 3.0 to about 6.0; wherein the leave-on antimicrobial composition has a One-wash Immediate Germ Reduction Index of greater than about 50%; and wherein the leave-on antimicrobial composition has a Mildness Index of greater than 0.3. The invention also encompasses methods for moisturizing skin, reducing germs on the skin, and providing residual effectiveness versus Gram positive bacteria using these products.

Abstract: The present invention relates to the use of an NK-1 receptor antagonist and a selective serotonin reuptake inhibitor for the treatment or prevention of obesity.

Abstract: Method and composition for treating painful conditions of the body, particularly the anal region. The compositions include a combination of nitroglycerin and sucralfate or a combination of nitroglycerin, lidocaine and sucralfate. The compositions may be included in a petrolatum base along with a water soluble lubricant. These compositions have been found effective in treating painful conditions in the anal region, such as anal fissures, inflamed or recently thrombosed hemorrhoids, and other chronic anal pain.

Abstract: The present invention relates to a rinse-off antimicrobial cleansing composition comprising from about 0.1% to about 5.0%, by weight of the cleansing composition, of an antimicrobial active; from about 6% to about 16%, by weight of the cleansing composition, of an anionic surfactant, wherein at least about 67% of the anionic surfactant is selected from the group consisting of Class A surfactants, Class C surfactants, and mixtures thereof, wherein the ratio of Class A surfactant to Class C is from about 100:0 to about 1.5:1; from about 2% to about 4%, by weight of the cleansing composition, of a proton donating agent having a Biological Activity Index, Z, of greater than about 0.75, wherein the proton donating agent is such that the composition is essentially free of C.sub.4 -C.sub.20 alkyl fatty acid, and wherein from about 0.

Abstract: Compounds of formula (1) ##STR1## are described wherein Y represents a halogen atom or a group --OR.sup.1, where R.sup.1 is an optionally substituted alkyl group; R.sup.2 represents an optionally substituted cycloalkyl or cycloalkenyl group; R.sup.3 is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen or sulphur atoms or a group --N(R.sup.4)-- where R.sup.4 is a hydrogen atom or an alkyl group; X is --O--, --S--, or --N(R.sup.5)--, where R.sup.5 is a hydrogen or an alkyl group; with the proviso that when X is --O-- then R.sup.3 is not a 3-cyanamino-6-pyridazinyl or a 3-chloro-6-pyridazinyl group; and the salts, solvates, hydrates and N-oxides thereof.The compounds are selective and potent inhibitors of phosphodiesterase IV and are useful for the prophylaxis and treatment of inflammatory diseases and the alleviation of conditions associated with central nervous malfunction.

Abstract: The invention is directed to a novel pharmaceutical composition comprising one or more local anaesthetics in oil form, one or more surfactants, water and optionally a taste masking agent. The novel composition is advantageously used as a local anaesthetic for pain relief within the oral cavity.

Abstract: Fungicidal mixtures, comprisinga) a carbamate of the formula I ##STR1## where T is CH or N, n is 0, 1 or 2 and R is halogen, C.sub.1 -C.sub.4 -alkyl or C.sub.1 -C.sub.4 -haloalkyl, it being possible for the radicals R to be different when n is 2, and/orb) an oxime ether of the formula II, ##STR2## where the substituents have the following meanings: X is oxygen or amino;Y is CH or N;Z is oxygen, sulfur, amino or C.sub.1 -C.sub.4 -alkylaminoR' is C.sub.1 -C.sub.6 -alkyl, C.sub.1 -C.sub.6 -haloalkyl, C.sub.3 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -haloalkenyl, C.sub.3 -C.sub.6 -alkynyl, C.sub.3 -C.sub.6 -haloalkynyl, C.sub.3 -C.sub.6 -cycloalkyl-methyl, or is benzyl which can be partially or fully halogenated and/or can have attached to it one to three of the following radicals: cyano, C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy and C.sub.1 -C.sub.4 -alkylthio; andc) a carbamate of the formula III(CH.sub.3).sub.2 N--CH.sub.2 CH.sub.2 CH.sub.

Abstract: The present invention is based on the discovery of a metabolic pathway in which a specific kinase converts fructose-lysine into fructose-lysine-3-phosphate in an ATP dependent reaction. Fructose-lysine-3-phosphate (FL3P) is then broken down to form free lysine, inorganic phosphate and 3-deoxyglucosone (3DG), the latter being a reactive protein modifying agent. 3DG can be detoxified by reduction to 3-deoxyfructose (3DF), or it can react with endogenous proteins to form advanced glycation end-product modified proteins (AGE-proteins), which are believed to be a cause of diabetic complications. Disclosed is a class of compounds which inhibit the action of FL3P kinase in the above-mentioned pathway.

Abstract: The following description concerns a therapeutic method for the treatment of diseases connected with the modulation of the cannabinoid peripheral receptor, comprising administering amidic derivatives of mono and bicarboxylic acids with aminoalcohols or arninoethers selectively active on said receptor.

Abstract: Compounds of general formula (1) ##STR1## are described wherein Y is a halogen atom or a group --OR.sup.1, where R.sup.1 is an optionally substituted alkyl group; X is --O--, --S-- or --N(R.sup.7)--, where R.sup.7 is a hydrogen atom or an alkyl group; R.sup.2 is an optionally substituted cycloalkyl or cycloalkenyl group; R.sup.3 and R.sup.4, which may be the same or different, is each a hydrogen atom or an alkyl, --CO.sub.2 R.sup.8 (where R.sup.8 is a hydrogen atom or an alkyl, aryl, or aralkyl group), --CONR.sup.9 R.sup.10 (where R.sup.9 and R.sup.10 which may be the same or different is each a hydrogen atom or an alkyl, aryl or aralkyl group), --CSNR.sup.9 R.sup.10, --CN, --CH.sub.2 CN group; Z is --(CH.sub.2).sub.n -- (where n is zero or an integer 1, 2 or 3; R.sup.5 is an optionally substituted monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; R.sup.

Abstract: Disclosed are chemical agents for modulating certain cellular immune reactions that can lead to autoimmune disorders. By specific modulation, harmful immune reactions can be lessened in severity or even prevented without resorting to potentially dangerous general immune suppression. The described chemical agents inhibit IL-12 induction of the secretion of key immune modulators. The described chemical agents are specific inhibitors of IL-12 induced Th1 immune response.

Abstract: Methods for achieving human male contraception are described in which compounds that substantially inhibit the movement of mannose lectins on the surface of human male sperm cells are administered to human male patients, and the inhibition achieved provides a reversible infertility that can serve as a means of birth control. The use of calcium (Ca.sup.+2) ion channel blocking pharmaceutical compositions is described, particularly the drugs nifedipine, verapamil, and calcium ionophore A23187.

Abstract: Methods for inhibiting the secretion of .beta.-amyloid peptide (.beta.AP) from cells comprise administering to the cells certain compounds which inhibit the activity of an approximately 31 kD protease involved in .beta.AP secretion. The 31 kD protease has been designated Cathepsin Y. Screening methods for .beta.AP inhibitors rely on determining the activity of test compounds in the presence of Cathepsin Y and a suitable peptide substrate. This invention is also directed to a nucleic acid sequence that encodes Cathepsin Y and the expression and isolation of Cathepsin Y.

Abstract: Compounds are provided which are crossreactive with peptides such as those bound by G-protein-linked receptors, together with preparative and therapeutic methods therefor. The compounds have the general structure: ##STR1## wherein at least one of R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 or R.sub.6 comprises a chemical functional group which causes the compounds to be crossreactive with the peptide of interest.

Abstract: The present invention is directed to certain novel compounds represented by structural formula I: ##STR1## or a pharmaceutically acceptable salt thereof, wherein R.sup.3, R.sup.6, R.sup.7, R.sup.8, R.sup.11, R.sup.12, R.sup.13, A, Q, W, X, Y, Z and n are defined herein. The invention is also concerned with pharmaceutical formulations comprising these novel compounds as active ingredients and the use of the novel compounds and their formulations in the treatment of certain disorders. The compounds of this invention are tachykinin receptor antagonists and are useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis.

Abstract: Methods for promoting animal growth comprising administering one or more substances selected from o-nitrophenol, p-nitrophenol, 5-nitroguaiacol and salts thereof as active ingredients.

Abstract: A class of terphenyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and halo; or wherein R.sup.2 and R.sup.3 together form --OCH.sub.2 O--; wherein each of R.sup.6 through R.sup.8 is independently selected from hydrido, lower alkyl, halo, lower alkoxy, lower haloalkyl, and lower dialkylamino; or wherein R.sup.6 and R.sup.7 together form --OCH.sub.2 O; and wherein R.sup.12 is selected from lower alkylsulfonyl and aminosulfonyl; or a pharmaceutically-acceptable salt thereof.

Abstract: Guanidine derivatives are provided useful for promoting growth, repair and regeneration of a neuronal axon and for treating neuropathies and myopathies. The compounds have the formula: ##STR1## wherein R.sub.1 is an isopropyl radical, a benzyl radical which is optionally substituted by one or more (C.sub.1 -C.sub.6)alkoxy radicals or a radical: ##STR2## R.sub.2, R.sub.3 and R.sub.

Abstract: Disclosed are methods for rectifying or ameliorating abnormal responses of mammalian immune systems. Also disclosed are methods for modifying normal responses of the mammalian immune system. Further disclosed are methods for accomplishing the foregoing by administering to a mammal a prolactin reducer and/or enhancer at a pre-determined time or times during a 24-hour period that results in modification of the mammal's abnormal prolactin profile so that it approaches or conforms to the prolactin profile of a young, healthy mammal of the same species (or to a standard profile generated from such individuals). Additionally, methods of upregulating or augmenting an immune response in a mammal are disclosed.

Abstract: A new class of biologically-active copolymers is provided capable of affecting biological systems in many different ways. The biologically-active copolymers of the present invention also have a wide variety of effects on individual cells. The biologically-active copolymers are also effective against certain microorganisms. The biologically active copolymers of the present invention can be administered to animals to provide specific effects on certain microorganisms that reside in the gut of the animal. A preferred use is administering the biologically active copolymers of the present invention to poultry to reduce the number of Salmonella in the poultry gut. Another preferred use is treatment of surfaces to interfere with the adhesion of microorganisms to the surfaces.

Abstract: Novel compounds of the general structural formula I: ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, pulmonary hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, inflammatory diseases including Raynaud's disease and asthma.

Abstract: Disclosed are x-ray contrast compositions for oral or retrograde examination of the gastrointestinal tract comprising iodophenoxy alkylene ethers and pharmaceutically acceptable clays in a pharmaceutically acceptable carrier; and methods for their use in diagnostic radiology of the gastrointestinal tract.

Abstract: A new class of biologically-active copolymers is provided capable of effecting biological systems in many different ways. The biologically active copolymers of the present invention also have a wide variety of effects on individual cells. The biologically active copolymers are also effective against certain microorganisms. The biologically active copolymers of the present invention can be administered to animals to provide specific effects on certain microorganisms that reside in the gut of the animal. A preferred use is administering the biologically active copolymers of the present invention to poultry to reduce the number of Salmonella in the poultry gut.

Abstract: Disclosed are contrast agents of the formula ##STR1## wherein Z is H, halo, C.sub.1 -C.sub.20 alkyl, cycloalkyl, lower alkoxy, alkoxycarbonyl, cyano, where the alkyl and cycloalkyl groups can be substituted with halogen or halo-lower-alkyl groups;R is C.sub.1 -C.sub.25 alkyl, cycloalkyl, ##STR2## or halo-lower-alkyl; each of which may be optionally substituted with halo, fluoro-lower-alkyl, aryl, lower-alkoxy, hydroxy, carboxy, lower-alkoxy carbonyl or lower-alkoxy-carbonyloxy;(CR.sub.1 R.sub.2).sub.p --(CR.sub.3 .dbd.CR.sub.4).sub.m Q, or (CR.sub.1 R.sub.2).sub.p --C.tbd.C--Q;R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are independently H or lower-alkyl, optionally substituted with halo;x is 1-4;n is 1-4;m is 1-15;p is 1-20; andQ is H, lower-alkyl, lower-alkenyl, lower-alkynyl, lower-alkylene, aryl, or aryl-lower alkyl;in an aqueous, pharmaceutically acceptable carrier comprising a cellulose derivative.

Abstract: A method of treating a subject in cardiac arrest, comprises blocking the descending aorta of the subject and then perfusing the aortic arch of the subject with a protective solution. The protective solution is one capable of delivering oxygen to the heart of said subject, such-as a perfluorochemical blood substitute. Following perfusion, spontaneous circulation is restored.In an improved embodiment of the foregoing, a vasoconstrictor such as epinephrine is administered concurrently with the perfusing step in an amount effective to enhance coronary perfusion with said protective solution.

Abstract: The present invention relates to stilbene derivatives which possess utility as anti-cancer agents. The compounds can be used to treat cancers which are susceptible to treatment therewith, and can be utilized in a method of treating such cancers. Pharmaceutical compositions containing the compounds are disclosed. Three preferred compounds among those disclosed are (Z)-1-(4-methoxyphenyl)-2-(3,4,5-trimethoxyphenyl)ethene, (Z)-1-(4-methylphenyl)-2-(3,4,5-trimethoxyphenyl)ethene, and 4-methyl-3',4',5'-trimethoxybenzylaniline hydrochloride.

Abstract: This invention relates to structurally novel acyclic tocotrienol analogs, which are useful for cholesterol/lipid lowering in cases of hypercholesterolemia and hyperlipidemia, and for atherosclerosis. Also provided are pharmaceutical compositions and a method of use employing those compositions.

Abstract: A quinone derivative useful in the treatment of hepatic diseases defined by the general formula: ##STR1## where X and Y may be the same or different from each other and are each a hydroxyl group, a group represented by the formula --(--OCH.sub.2 --).sub.n --OR.sup.6, wherein n is 0 or 1 and R.sup.6 is a lower alkyl group, or an acyl group.

Abstract: There are provided new alkane and alkoxyalkane derivatives of the general formula I in which R1, R2, R3, R4 and A have the meanings given in the description, processes for their preparation and insecticidal and acaricidal compositions containing these compounds.