Abstract: This invention relates to the use of a composition for local percutaneous delivery of a drug such as a muscle relaxant, more particularly cyclobenzaprine in an organogel cream. The composition is applied by the patient directly to the skin over accessible muscles of mastication i.e., masseter and temporalis. The composition is rapidly absorbed through the skin to provide control of harmful habits such as bruxism and tooth clenching. The composition can also be applied to the skin overlying these muscles to control muscle hyperactivity (spasm) and/or trigger points, from other causes. The composition can be formulated to include another active agent such as a non-steroidal anti-inflammatory, for example ketoprofen.

Abstract: Compounds that inhibit 5-alpha-reductase are provided. The compounds are used to treat prostate cancer, breast cancer, obesity, skin disorders and baldness.

Abstract: Amide compounds of the formula: 1

Abstract: Novel intermediates of Formula IV wherein the substituents are as defined in the specification and a process for preparing the same.

Abstract: A combination of Vitamin C and a quinone used as a supplemental treatment for a cancer patient. The combination may be administered before, during and after the patient undergoes a conventional cancer treatment protocol. The combination may be administered orally, intravenously, or intraperitoneally. Oral administration may be in the form of capsules containing a predetermined ratio of Vitamin C to Vitamin K3. The supplemental treatment is effective to inhibit metastases of cancer cells and inhibit tumor growth. The ratio of Vitamin C to Vitamin K3 is in the range of about 50 to 1 to about 250 to 1. A method for evaluating the effectiveness of the supplemental treatment includes monitoring the patient's serum DNase activity throughout the course of treatment.

Abstract: The present invention provides compounds of general formula I or II: wherein R1, R2, R3, R4, R5, R6, and R7 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I or II, intermediates and processes useful for preparing compounds of formula I or II, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I or II.

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: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.

Abstract: The present invention is directed to a solid formulation comprising the lipid-regulating agent dispersed in a hydrophilic, amorphous polymer in which said lipid-regulating agent is present as a meta-stable, amorphous phase.

Abstract: Methods and compositions for treatment of, or protection from, neuropathy resulting from reperfusion injury upon reversal of an ischemic condition, comprising treatment or prophylactic treatment of the patient with an antagonist of the type 3 ryanodine receptor, such that a rise in cytosolic Ca2+ concentration is prevented. Therapeutic compositions containing dantrolene or aminodantrolene are administered to the patient to prevent a rise in cytosolic Ca2+ that would otherwise result in Ca2+-mediated neuronal damage. Treatment of ischemic optic neuropathy by this method is shown, and the methods and compositions presented are also applicable to other ischemic reperfusion neuropathies, such as stroke, reperfusion injury after TPA treatment/carotid endarterectomy, seizures, and excitotoxic retinal damage in glaucoma.

Abstract: The present invention is directed to aromatic derivatives of formula (I), wherein: R1 is (a), wherein R3 and R4 are selected from between H and OH, provided that R3 and R4 are not simultaneously H, and R2 is H; or R1 and R2 taken together, are (b), wherein R5 is selected from between CH3 and (CH2)5OH, to the iron complexes thereof, and to their use for the preparation of pharmaceutical compositions for the normalization of iron level.

Abstract: A product and method for reducing and preventing the ingestion of substrates by avians wherein the substrates are disposed within an avian house. The product is a bird repellent in combination with a substrate disposed within an avian house. As a result of the reduced ingestion of substrates such as litter, healthier avians are achieved.

Abstract: There is provided a method of contraception, comprising exposing a spermicidally sufficient quantity of an agent to spermatozoa. The agent is a quinone represented by the following formula: Each group A is H or an electron releasing moiety. The agent is capable of generating reactive oxygen species including free radicals, superoxide and hydrogen peroxide in the presence of spermatozoa.

Abstract: Indane compounds of general formulae (1) to (4) and their pharmaceutical use, particularly to achieve mast cell stabilising activity and/or anti-inflammatory activity are described.

Abstract: The present invention is directed to curcumin analogs exhibiting anti-tumor and anti-angiogenic properties, pharmaceutical formulations including such compounds and methods of using such compounds.

Abstract: The present invention provides illudin analogs of the general formula I: wherein R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising compounds of formula I, intermediates and processes useful for preparing compounds of formula I, and methods comprising inhibiting tumor growth or treating cancer by administering one or more compounds of formula I.

Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; composition comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.

Abstract: A compound having the formula wherein R5 is an [A]—CH3, —[A]—C(OH)ZZ′ or —[A]—C(O)Z″ grouping where —[A]— is an alkylene, alkenylene or alkynylene radical or a single bond, and Z, Z′ and Z″ are a hydrogen atom or an optionally substituted alkyl, alkenyl, alkynyl or aryl radical; and R1, R2, R3, R4, R6, R7 and R8 are as defined in the description; the use thereof as a drug, pharmaceutical compositions containing same, a preparation method therefor, and intermediates of said method, are disclosed.

Abstract: A method is described for controlling or exterminating moles through the use of a bait composition in the form of a gel, paste, or grease. The composition includes an attractant and an active ingredient capable of killing vertebrate pests. The composition is injected into a mole tunnel through a small diameter nozzle, tube or needle to avoid digging open the tunnel or causing it to collapse.

Abstract: The present invention pertains to a method for healing a wound in a mammal which comprises the steps of (A) providing a therapeutic wound healing composition comprising a therapeutically effective amount of an inhibitor of mono-adenosine diphosphate-ribosyl transferase to inhibit adenosine diphosphate-ribosylation of vascular endothelial growth factor; and (B) contacting the therapeutic wound healing composition with a wound in a mammal. This invention also pertains to wound healing compositions and to methods for preparing and using the wound healing compositions and the pharmaceutical products in which the therapeutic compositions may be used. This invention further pertains to therapeutic dermatological-wound healing compositions useful to minimize and treat diaper dermatitis and to methods for preparing and using the therapeutic dermatological-wound healing compositions.

Abstract: Conformationally rigid aryl prostaglandins are useful in the treatment of glaucoma and ocular hypertension. Also disclosed are ophthalmic pharmaceutical compositions comprising said prostaglandins.

Abstract: The present invention provides compounds of Formula (I). The present invention also provides a method of treating cancer and treating or preventing restenosis or atherosclerosis. Also provided by the present invention is a pharmaceutically acceptable composition containing a compound of Formula (I).

Abstract: The invention described here concerns the unique utility of fatty acids and their derivatives to eradicate existing fungal and bacterial infections in plants. Also, described herein are combination treatments whereby fatty acids are used to enhance or augment the activity of fungicides, bactericides, and biological control agents.

Abstract: A method of preventing and treating a viral condition caused by an enveloped virus is described, comprising using a therapeutically effective amount of a compound selected from the group consisting of a substituted hydroquinone and the corresponding benzoquinone, wherein said hydroquinone comprises a 2-R.sup.1, 3-R.sup.2 -1,4-hydroquinone where at least one of R.sup.1 and R.sup.2 include a carbon linkage to the benzene ring of the hydroquinone. Particularly useful compounds include 5,8-dihydro-5,8-methano-1,4-naphthalenediol, 1,4-naphthoquinone, 3', 6'-dihydroxybenzo-norbornane, tert-butylhydroquinone, other diols, e.g. 1,5-naphthalenediol, and alkylated diols, e.g. 4-methoxy-1-naphthol.

Abstract: The present invention provides new tetralone or benzopyranone derivatives and a method for producing the derivatives useful for a therapeutic agent for preventing and/or treating hormone dependent diseases. The present invention is a new tetralone or benzopyranone derivative represented by a particular general formula (I). ##STR1## wherein R.sub.1 and R.sub.2 represent hydrogen, a hydroxy group, an alkyloxy group or an aralkyloxy group, respectively, R.sub.3 -R.sub.7 represent hydrogen, a hydroxy group or a straight or branched alkyl, alkyloxy or aralkyloxy group having 1-6 carbon atoms, a halogen, an amino group or an alkylene dioxy group joined at R.sub.3 and R.sub.4, R.sub.4 and R.sub.5, R.sub.5 and R.sub.6, or R.sub.6 and R.sub.7, respectively, and A represents a methylene or oxygen.In the production, a particular tetralone or benzopyranone compound and a particular benzaldehyde compound are reacted.

Abstract: The present invention provides an composition for attracting noctuid and/or other lepidopteran species. Liquid and solid formulations are provided, along with methods for their use, for controlling or eliminating noctuid and/or other lepidopteran species, and/or protecting plants susceptible to noctuid and/or other lepidopteran species damage.

Abstract: The use of certain heterocyclic derivatives for treating parasitic protozoa infections in mammals, in particular bovine trichomoniasis and giardiasis, is disclosed.

Abstract: Nonsteroidal antiinflammatory drugs which have been substituted with a nitrogen monoxide group; compositions comprising (i) a nonsteroidal antiinflammatory drug, which can optionally be substituted with a nitrogen monoxide group and (ii) a compound that directly donates, transfers or releases a nitrogen monoxide group (preferably as a charged species, particularly nitrosonium); and methods of treatment of inflammation, pain, gastrointestinal lesions and/or fever using the compositions are disclosed. The compounds and compositions protect against the gastrointestinal, renal and other toxicities that are otherwise induced by nonsteroidal antiinflammatory drugs.

Abstract: A compound comprising a non-steroidal antiinflammatory agent to which is directly or indirectly linked an NO group, a pharmaceutical composition including the compounds and methods of treatment of pain and/or inflammation using the compounds and compositions are disclosed. Also disclosed is a composition comprising a non-steroidal antiinflammatory agent and a compound that donates, transfers or releases nitric oxide.

Abstract: Pesticidal as a pesticide against whitefly, Lepidoptera and certain fungi is provided of compound of general formula (I) ##STR1## or a salt thereof is provided, in which n represents an integer from 0 to 4; m represents an integer 0 or 1;each R independently represents a halogen atom or a nitro, cyano, hydroxyl, alkyl, alkenyl, haloalkyl, haloalkenyl, alkoxy, haloalkoxy, haloalkenoxy, amino, alkylamino, dialkylamino, alkoxycarbonyl, carboxyl, alkanoyl, alkylthio, alkylsulphinyl, alkylsulphonyl, carbamoyl, alkylamido, cycloalkyl, aryl or aralkyl group;R.sup.1 and R.sup.2 each independently represent an optionally substituted alkoxy group or together represent a group .dbd.O, .dbd.S or .dbd.N--OR.sup.9, where R.sup.9 represents a hydrogen atom or an optionally substituted alkyl group;R.sup.3 represents a hydroxyl group, or a group --OL where L is a leaving group, or a group which in vivo is transformed into a group --OL.sup.1 where L.sup.1 is a leaving group;R.sup.7 and R.sup.

Abstract: This invention provides peptidomimetics which bind to T4 or CD4 cell receptors and are useful in inhibiting viral infectivity by viruses which bind to T4 cell receptors. More specifically, peptidomimetics of this invention can alleviate symptoms of AIDS by inhibiting binding of HIV, the virus associated with AIDS, to receptor sites in human cells susceptible to HIV infection. These peptidomimetics, in particular, inhibit binding of HIV to cells of brain membrane and the immune system. They also display substantially longer half-lives in vivo than peptide T. The compounds of this invention which bind to T4 or CD4 receptors and thereby inhibit binding of HIV, alone or in combination with one another, can be used to alleviate AIDS symptoms and ameliorate symptoms of HIV infection, especially neuronal dementias and Kaposi's sarcoma. The compounds of this invention, alone or in combination, can further be used to prevent development of AIDS in persons who might become exposed to HIV.

Abstract: The invention relates to the use of .alpha.-hydroxyketoalkyl derivatives as light protection filters for cosmetic or pharmaceutical products, the .alpha.-hydroxyketoalkyl group being linked, if appropriate via a spacer, to a chromophoric group which has an absorption maximum in a wavelength range of between 280 and 400 nm and has a conjugated .pi.-electron system of at least 8 .pi.-electrons, and to new .alpha.-hydroxyalkyl derivatives, processes for their preparation and pharmaceutical and cosmetic formulations comprising these derivatives as light protection substances.

Abstract: Method of treating osteoporosis according to the present invention comprises the administration to a subject in need thereof a therapeutically effective amount of diosgenin, a therapeutically effective amount of vitamin K and a therapeutically effective amount of vitamin D.

Abstract: A sterile bicarbonate concentrate for use in the present invention relates to a sterile calcium-free bicarbonate concentrate for use in peritoneal dialysis, hemofiltration, cardiac bypass surgery and in electrolyte replacement therapy.

Abstract: The present invention provides illudin analogs of the general formula (I): ##STR1## where R.sub.1 is (CH.sub.2).sub.n --X--Y or H; n is 0 to 4; X is O or S or N or absent; and Y is an optionally substituted (C.sub.1 -C.sub.8)alkyl, (C.sub.6 -C.sub.10)aryl, (C.sub.6 -C.sub.10)aryl(C.sub.1 -C.sub.4)alkyl or cyclo(C.sub.3 -C.sub.6)alkyl optionally comprising one or more heteroatoms; a monosaccharide, an amino acid residue, or H when n is 2-4; R.sub.2 is absent; or R.sub.1 and R.sub.2 together comprise a 5-7 membered cyclic ring;R.sub.3 is (C.sub.1 -C.sub.4)alkyl or H; R.sub.4 is H, SCH.sub.2 CO.sub.2 (C.sub.1 -C.sub.4)alkyl, O--(C.sub.5 --C.sub.12)aryl or --S--(C.sub.5 -C.sub.12)aryl; R.sub.5 is H, OH or absent; R.sub.6 is (C.sub.1 -C.sub.4)alkyl or absent; R.sub.7 is OH or OSi((C.sub.1 -C.sub.4)alkyl).sub.3 ; orR.sub.6 and R.sub.7 together are ethylenedioxy;R.sub.8 is optionally substituted (C.sub.1 -C.sub.4)alkyl; andthe bonds represented by -- are individually present or absent.

Abstract: Strong 5.alpha.a-reductase inhibitors are extracted and fractionated from Thuja orientalis and other similar crude drugs or they may be purified as diterpenes in isolated form. The inhibitors are used either on their own or as active ingredients of therapeutics in the treatment of diseases caused by the overactivity of 5.alpha.a-reductase or the hypersecretion of androgens, such as male pattern baldness, androgenetic alopecia, hirsutism, acne, prostatomegaly and cancer of the prostate.

Abstract: An object of the present invention is to provide an infusion preparation set (a container filled with infusion liquids) useful for preparation of an infusion liquid containing sugars, amino acids, electrolytes, a fat emulsion and vitamins. The present invention is constituted by the use of a container having two compartments which are separated from each other by a separation means, which contains an infusion liquid comprising a fat emulsion, sugars, fat-soluble vitamins and specified water-soluble vitamins in the first compartment and an infusion liquid comprising amino acids, electrolytes and other specified water-soluble vitamins in the second compartment. An infusion preparation containing sugars, amino acids, electrolytes, a fat emulsion and vitamins can be obtained easily and aseptically upon use, by simply removing a separation means and mixing the infusion liquids included in the first and second compartments.

Abstract: A redox, hydrogen-acceptor compound, having utility in treating inflammation, is a 1,4-dioxonaphthalene or 1,4-dilminon aphthalene having either a 2,3-double bond, in which cast there are 2 and 3-substituents, or a 2,3-single bond. Examples of such compounds are menadione epoxide and water-soluble derivatives or menadione such as menadione bisulphite.

Abstract: A rodenticidal bait in the form of agglomerated granules comprising: a cereal base comprising a ground cereal; a rodenticide; and a water-soluble film-forming binder.

Abstract: An anti-osteopathic composition comprising as an active ingredient a compound represented by the following formula (I), (II) or (III): ##STR1## which is useful for therapeutic and prophylactic treatment of osteopathia such as osteoporosis and bone fracture.

Abstract: The present invention provides a method for providing nutrition to non-catabolic and moderately catabolic patients. Pursuant to the present invention, the enteral composition includes a peptide based protein source of hydrolyzed whey, a lipid source, and a carbohydrate source. Preferably, the protein source includes approximately 22% to about 27% of the total calories. The composition has a caloric density of approximately 1000 Kcal/L and a low osmolality of approximately 300 to 450 mOsm/Kg H.sub.2 O. Still further, the composition of the present invention also includes increased levels of certain vitamins and minerals.

Abstract: A nutritional composition, adapted for consumption by mammals, contains (1) an orally ingestible diluent or carrier, except an oily carrier or diluent which comprises C.sub.8-18 saturated fatty acids, oleic acid and derivatives of these acids, and (2) a composition of matter which consists of (a) from about 13.0 to about 27.5% by weight of at least one compound selected from linolenic acid and its salts, esters and amides, calculated as the free acid, and (b) about 87.0 to about 72.5% by weight of at least one compound selected from linoleic acid and its salts, esters and amides thereof, calculated as the free acid, the salts, esters and amides of linolenic and linoleic acid being both physiologically hydrolyzable and pharmacologically acceptable. The invention also relates to a method for treating a mammal for the purpose of inducing therein at least one physiological effect selected from memory enhancement and analgesia, by administration of an effective amount of the nutritional composition.

Abstract: Compounds of formula I, ##STR1## wherein the substituents R.sub.1 -R.sub.4 and a have the given meanings and show an activity against inflammatory conditions.

Abstract: New indene derivative, obtainable from etiolated seedlings of Adlay and shown by Formulas (1) and (2) given below, have antimicrobial effects and can serve as effective components of antimicrobial agents: ##STR1##

Abstract: A vitamin K mixture is used in a topical application for the treatment of blood vessel disorders of the skin which include, but are not limited to, actinic and iatrogenic purpura, lentigines and other vascular problems of the skin and subcutaneous tissue. The formulation of the mixture includes a number of the following substances: vitamin K, 95% ethyl alcohol SD40, isopropyl alcohol 99%, benzyl alcohol, lecithin granules, isopropyl palmitate NF, propyl paraben, methyl paraben, Pluronic F-127 NF, Dowicil 200 and preserved water. The concentrations of the substituent compounds vary in the different formulations of the vitamin K cream.

Abstract: Stable, cold water-dispersible, liquid or pulverous compositions of fat-soluble substances which contain fish gelatin as the protective colloid and a method of making same are described.

Abstract: Diaromatic compounds, characterized in that they correspond to the following general formula: ##STR1## in which: R.sub.1 is --CH.sub.3, --CH.sub.2 OH, --COR.sub.8 or --CH.sub.2 OCOR.sub.9, R.sub.8 is H, OH, --OR.sub.10, --N(rr') or alkyl, R.sub.10 is alkyl, alkenyl, aryl or aralkyl, r and r' being H, alkyl, aryl, aralkyl, etc., r and r' together form a heterocycle, R.sub.9 is alkyl, alkenyl or a sugar residue, R.sub.2 and R.sub.3 are --OR.sub.11 or --OCOR.sub.11, R.sub.11 is H, alkyl, fluoroalkyl, aryl or aralkyl, R.sub.3 in addition being H, R.sub.4 is H, OH, alkyl, alkoxy, F, Cl or --CF.sub.3, R.sub.5 and R.sub.7 are H, OH, alkoxy, .alpha.-substituted alkyl or .alpha.,.alpha.'-disubstituted alkyl, etc., R.sub.6 is H, OH, alkyl, alkoxy, cycloalkyl, etc., R.sub.5 and R.sub.7 cannot simultaneously be OH or alkoxy and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 cannot simultaneously be H, R.sub.5 and R.sub.6 or R.sub.6 and R.sub.

Abstract: Substituted hydrindanes and their use in controlling angiogenesis-dependent diseases in warm blooded animals are disclosed.

Abstract: Disclosed are compounds of formula ##STR1## wherein F represents: ##STR2## or a pharmaceutically acceptable salt. The compounds are useful in treating hyperproliferative skin disease, allergic reactions and inflamation.

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.