Abstract: A preparation method of zaleplon is provided and belongs to the technical field of pharmaceutical chemistry. The preparation method adopts simple and cheap m-nitrobenzaldehyde and triethylamine as raw materials, and constructs a core structure of zaleplon with high efficiency and high selectivity through a one-pot series reaction without transition metal catalysis, thereby avoiding the formation of isomers, reducing the generation of by-products, increasing the yield of target products and reducing the synthesis cost; and after simple nitro reduction modification, zaleplon is prepared. The method has the advantages of short preparation route, mild reaction conditions and simple operation, so the method is suitable for industrial production.

Abstract: The present invention provides compounds and compositions which are positive allosteric modulators of GABA-A receptors that selectively target the peripheral nervous system and organs of the body, and which do not pass through the blood-brain barrier. The compounds and compositions of the present invention are useful for treatment of diseases or disorders which are mediated by GABA-A neuronal activity, such as, for example, visceral pain, gut motility, irritable bowel syndrome, functional abdominal pain, functional idiopathic diarrhea, inflammatory bowel diseases, drug induced pain, bile salt malabsorption, lactase or other carbohydrate intolerance.

Abstract: A method for sealing a container having an opening by contacting the opening with a mixture including a phenethylamine and a first polymer, adding a fluid to be contained to the container, and then adding a second mixture, comprising a second polymer, whereupon an interaction between the first and second polymer mixtures result in a seal being formed over the opening, thereby containing the fluid. The first polymer is typically a water-swellable polymer and the second polymer is typically a hydrophilic polymer that will form an interpenetrating network with the swellable polymer.

Abstract: High density (density ?0.945 g/cm3) unimodal polyethylene compositions for use in hot-fill closures and processes.

Abstract: The present invention provides substituted pyrrolo-, furano-, and cyclopentylpyrimidine bicyclic compounds of Formula III, and Formula IV, and pharmaceutically acceptable salts, solvates, and hydrates thereof, having antimitotic activity, anti-multidrug resistance activity, such as for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds and pharmaceutical compositions for treating tumor cells and inhibiting mitosis of cancerous cells.

Abstract: High density (density ?0.950 g/cm3) polyethylene compositions for use in hot fill closures and processes.

Abstract: The invention relates to pharmaceutical combinations of potassium channel openers and sodium channel inhibitors, for treating pains which are accompanied by an increase in muscle tone.

Abstract: Chemical formulations and methods for reducing muscle and joint soreness are disclosed. A representative chemical formulation includes compounds such as a selenium-compound, chondroitin sulfate, glucosamine, and/or methylsulfonylmethane. A representative method for reducing muscle and joint soreness includes administering the chemical formulation to a host.

Abstract: A method for treating anorectal disorders, comprising a step of providing a suppository containing between 1000 and 500,000 IU of an antioxidant selected from the group of Vitamin A, Vitamin C, Vitamin E; and a step of placing the suppository within the rectal cavity for a period of time required for dissolution of the suppository.

Abstract: The bath product employs halite and a mixture of herbs and spices packed in water permeable bath bags to condition bath water and emit fragrances. The bath product includes five water permeable bags contained in an outer carrying bag. Four of the five water permeable bags contain the mixture and one contains halite. The mixture includes ground lemongrass, wrinkled skin lime, wrinkled skin lime leaves, holy basil, Zingiber cassumunar Roxb., and mint.

Abstract: Chemical formulations and methods for reducing muscle and joint soreness are disclosed. A representative chemical formulation includes compounds such as a selenium-compound, chondroitin sulfate, glucosamine, and/or methylsulfonylmethane. A representative method for reducing muscle and joint soreness includes administering the chemical formulation to a host.

Abstract: The invention discloses a process of extracting, fractionating and purifying bioactive molecules from an associated mangrove plant, methods of screening for pharmacological activities of crude extract, its fractions and purified compounds and use of the chloroform fraction of the crude extract as anti-spasmodic, anti-arrhythmic and anti-cholinergic agent.

Abstract: A method of inhibiting at least one symptomology of Restless Leg Syndrome (RLS) and its related disorders, including disorders such as periodic limb movements in sleep (PLMS) and periodic limb movement disorder (PLMD), is disclosed. The method optionally comprising identifying a host, afflicted with Restless Leg Syndrome (RLS) and its related disorders; and administering to the host a pharmaceutically effective amount of Valeriana. A novel method of inhibiting at least one symptomology of Restless Leg Syndrome (RLS) and its related disorders is disclosed.

Abstract: The present invention features methods and compositions for transdermal administration. In one embodiment, the invention features methods and compositions for transdermal administration of an amine containing compound having biphasic solubility and/or an agent which enhances the activity of the amine containing compound having biphasic solubility, e.g., a muscle relaxant, to relieve pain.

Abstract: There are provided a method to screen agonist or antagonist of the maxadilan receptor participating in vasodilating action, wherein a receptor of maxadilan is used, compounds which specifically bind to the receptor, and a tissue preparation having the receptor. The compounds are variants of maxadilan from the salivary glands of the sand fly.

Abstract: The invention relates to a device and method for the treatment of Alzheimer's dementia with desoxypeganine and/or a pharmaceutically acceptable acid addition salt of desoxypeganine.

Abstract: This invention provides the use of Botulinum toxin (BTX) to cause paralysis of a depressor anguli oris (DAO) musculature in a patient to alleviate downturn at corners of the patient's mouth.

Abstract: A novel method of inhibiting at least one symptomology of Restless Legs Syndrome (RLS) and its related disorders, including disorders such as periodic limb movements in sleep (PLMS) and periodic limb movement disorder (PLMD), is disclosed. Said method optionally comprising identifying a host, preferably a human, afflicted with Restless Legs Syndrome (RLS) and its related disorders; and comprising administering to said host a pharmaceutically effective amount of Valeriana, preferably an extract of Valeriana. A novel method of inhibiting at least one symptomology of Restless Legs Syndrome (RLS) and its related disorders is disclosed.

Abstract: The present invention refers to a method for producing vasodilation or analgesia in a mammal, comprising the use of vegetal material derived from the bark of a Trichilia species.

Abstract: The present invention discloses the use of nicorandil in treatment of male impotency and female sexual dysfunction. Nitric ester of N-(2-hydroxyethyl) nicotinamide or nicorandil, as it is better known is known as a drug for treatment of circulatory diseases. It is a pyridine derivative. Several clinical tests performed on male patients suffering from impotency including severe penile erectile dysfunction or female patients suffering from female sexual arousal dysfunction consistently showed excellent results. There was not a single instance of any of side effects or other symptoms of toxicity or deaths due to myocardial infarctions as was the case with other drugs including pyrazolopyrimidones compounds.

Abstract: Novel compounds of formula (1) together with their salts and solvates have a number of uses in medicine, in particular as central muscle relaxants.

Abstract: A polymeric composition capable of releasing nitric oxide including a polymer and a nitric oxide-releasing N.sub.2 O.sub.2.sup.- functional group bound to the polymer; pharmaceutical compositions including the polymeric composition; and methods for treating biological disorders in which dosage with nitric oxide is beneficial. The compositions can be used as and/or incorporated into implants, injectables, condoms, prosthesis coatings, patches, and the like for use in a wide variety of medical applications.

Abstract: Disclosed are methods for treating urinary incontinence using enantiomerically enriched (S)-trihexyphenidyl.

Abstract: An extract composition derived from the peel of a banana and the method for producing the extract composition. An aqueous solvent is combined with the peel of a banana. If the banana is unripe, a base is also added. The mixture is homogenized and allowed to react at least until a black supernatant appears. The entire slurry is filtered. The resulting extract is used alone or combined with a cream or ointment. Medicinal benefits of the extract include relief from pain, swelling, itching, bruising, wrinkles, and sunburn.

Abstract: Therapeutic bath salts for the relaxation of muscles, elimination or reduction of muscle spasms, and for the overall enhancement of a person's mood. The bath salts of the present invention are used as aromatherapy that has both the convenience of a bath and the internal mechanisms of ingested medication. The formula for the composition of the present invention includes a selected amount of magnesium sulfate trihydrate (a hydrated version of epsom salts), lithium chloride, copper gluconate, and essential oils. The oils include rosewood oil, ylang ylang oil, lavender oil and patchouli oil. The oils are provided as scents for use in the prescribed aromatherapy. The user mixes a preselected amount of the crystallized salt or liquid form of the present invention with the bath water. A period of time is allowed to elapse before the user departs the bath. By resting in the tub, the user accrues the combined benefits of external therapy and internal therapy.

Abstract: The present invention relates to a natural herbal composition of effective amounts of Aloe Vera, Capsicum, Golden Seal, Comfrey Root and water, to its method of use for external application to affected parts of the body for eliminating muscular pain and to its method of preparation.

Abstract: Novel compounds of formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each selected from hydrogen and fluoro and at least one and not more than two is fluoro;R.sup.5 is selected from hydrogen and C.sub.1 -C.sub.4 alkyl;R.sup.6 is selected from hydrogen, C.sub.1 -C.sub.4 ally and hydroxy; orR.sup.5 and R.sup.6 together with the ring carbon form a carbonyl group;R.sup.7 is selected from hydrogen and hydroxy,R.sup.8 and R.sup.9 are each selected from hydrogen, C.sub.1 -C.sub.4 alkyl and cyclo(C.sub.3 or C.sub.4) alkyl or together with the nitrogen form a morpholino group; andX is selected from a bond, methylene and --O-- and is always a bond or --O-- when any of R.sup.5, R.sup.6 and R.sup.7 is other than hydrogen and is always a bond when R.sup.5 and R.sup.6 together with the ring carbon form a carbonyl group;and their salts and solvates have a number of uses as central muscle relaxants. In particular, treatment of conditions associated with abnormally raised skeletal muscle tone.

Abstract: Medicated plasters composed of a flexible support and a pressure-sensitive adhesive layer laminated thereon, in which said pressure-sensitive adhesive layer has an exposed surface with pH of 7 or higher and contains one of the following three components:i) a basic physiologically active agent and an acidic substance,ii) a salt of a basic physiologically active agent and a basic substance, andiii) a basic physiologically active agent and a salt of a basic physiologically active agent.

Abstract: A composition for topical therapy for symptoms of back pain, muscle tension or myofascial pain or a combination thereof, which comprises a topical carrier system for intact skin of the back or outer synovial membranes or both, which comprises a therapeutic dose of a local anesthetic, and which applies the local anesthetic to a region of skin lying beneath the topical carrier system.

Abstract: The rate of absorption of drugs across skin and other body membranes such as mucous membranes and the blood brain barrier is enhanced by adding to the drug composition a compound which enhances the rate. This compound may be a macrocyclic ester, diester, amide, diamide, amidine, diamidine, thioester, dithioester, thioamide, ketone or lactone. The macrocyclic ketone contains at least 12 carbon atoms.

Abstract: A polymeric composition capable of releasing nitric oxide including a polymer and a nitric oxide-releasing N.sub.2 O.sub.2.sup.- functional group bound to the polymer; pharmaceutical compositions including the polymeric composition; and methods for treating biological disorders in which dosage with nitric oxide is beneficial. The compositions can be used as and/or incorporated into implants, injectables, condoms, prosthesis coatings, patches, and the like for use in a wide variety of medical applications.

Abstract: A method for the prevention or removal of undesired crystals of scopolamine from a non-aqueous matrix of a transdermal system in which the scopolamine is dispersed is disclosed wherein the method comprises dynamically heating the scopolamine containing layer during the process of or immediately prior to assembling two laminates which once assembled encase the scopolamine containing layer.

Abstract: Counter-irritants produce a slight irritation, as on an area of the skin, in order to relieve more serious inflammation elsewhere. Peppers, members of the Capsicum species, are a source of counter-irritants. The Scoville rating for a pepper provides a measure of the counter-irritant content of a given pepper. This invention provides for the solubilizing and recovery of the counter-irritants contained within peppers, having Scoville ratings of from 30,000 to 250,000, in the common capsaicin containing ethyl alcohol extract from the same specific peppers. The synergisitic pain relieving benefits of the counter-irritants in combination with the capsaicin provides superior pain relief for many hours after an application.

Abstract: Use of a medicament with a content of active substances from Rhizoma zingiberis and Ginkgo bilobae for the treatment of anxiety states.

Abstract: A common complication of vaginal delivery is the tearing of the muscles of the vagina and perineum. This tearing results in an irregular laceration which the surgeon must then repair. Current obstetrical practice is to prevent this irregular laceration by performing an episiotomy to create a regular laceration which is later sutured. However, both natural tearing of the vaginal and perineal muscles during delivery and surgical episiotomies are subject to further, more grave, complications. The use of medical therapy instead of surgical therapy will reduce the incidence of lacerations of the muscles of the vagina and perineum. The use of medical therapy for the relaxation of the muscles of the vagina and perineum is described.

Abstract: The treatment of erectile dysfunctions in mammals, including humans, comprises administering to a host in need thereof an effective dose of linsidomine or a pharmacologically compatible salt thereof, alone or in combination with adenosine, vitamins, prostaglandins, calcium antagonists, .alpha.-receptor blockers and/or smooth muscle relaxants. Also disclosed is a disposable medicament pack containing in a sterile package a disposable syringe containing a dose unit of an erection-promoting active substance or of a combination of active substances, sterile swabs provided with disinfectants, and instructions for use.

Abstract: Mixed ligand metal complexes of nitric oxide-nucleophile adducts, useful as cardiovascular agents of the formula KA, wherein A is[(M).sub.x.sup.x' (L).sub.y (R.sup.1 R.sup.2 N-N.sub.2 O.sub.2).sub.x ], andK is a pharmaceutically acceptable counterion present in the composition when the overall charge of A is not zero, counterion K being present only in an amount to neutralize A. Methods of treating mammals with such compounds are provided. Pharmaceutical compositions containing such compounds are also provided.

Abstract: A method for inhibiting oxytocin activity by administering an oxytocin inhibiting amount of a penicillide compound having the formula ##STR1## and compositions for such use are described.

Abstract: Peptide amide and amide dimer muscle relaxants represented by the formulae: ##STR1## wherein: R is lower alkyl; R.sub.1 and R.sub.2 independently selected from the group consisting of hydrogen, lower alkyl, allyl, propargyl, aryl lower alkyl and cyclo-lower alkyl lower alkyl, or R plus one or both of R.sub.1 and R.sub.2, together with the nitrogen to which they are attached, form a heterocyclic ring having 5 to 7 member atoms; AA are independently selected from certain amino acids moieties; n is 2 to 4; x is independently 0 or 1; y is independently 1 or 2; z is 2 to 12; and An.sup.- is a pharmaceutically acceptable anion.

Abstract: A method of preventing, treating and/or controlling diseases caused by dysregulation and/or dysfunction of various portions of the nervous system which comprises administering to a patient, an effective amount of a compound of the avermectin family, e.g. ivermectin, in single or multiple doses of up to 1.6 mg/kg at intervals of from 3 days to 4 months.

Abstract: The present invention relates to 1,4-disubstituted-piperidinyl compounds that have utility as analgesics and as muscle relaxants.

Abstract: Muscle activity can be reversibly arrested by administering a reagent, such as 2,3-butanedione monoxime (BDM), which selectively blocks the interaction of the contractile proteins actin and myosin. Muscle such as the heart is contacted with the reagent to arrest activity and, after surgery or transplantation, the reagent is removed from the muscle to restore muscle activity.

Abstract: Phenethanolamine derivatives are disclosed of formula ##STR1## wherein m is 2 to 8; n is 1 to 7 provided that m+n is 4 to 12;Ar is phenyl or phenyl substituted by one or two halogen atoms, alkyl or alkoxy groups or by an alkylenedioxy group;R.sup.1 and R.sup.2 are hydrogen or alkyl provided that the sum total of carbon atoms in R.sup.1 and R.sup.2 is not more than 4; and the physiologically acceptable salts and solvates thereof.The compounds have a selective stimulant action at .beta..sub.2 -adrenoreceptors and may be used inter alia in the treatment of diseases associated with reversible airways obstructions such as asthma and chronic bronchitis. The compounds may be formulated in conventional manner as pharmaceutical compositions with physiologically acceptable carriers or excipients.The compounds may be prepared, for example by alkylation of an amine: ##STR2## where R.sup.3, R.sup.5 and R.sup.6 is hydrogen or a protecting group, followed by removal of any protecting group.

Abstract: An external analgesic lotion containing active ingredients of camphor and menthol to relieve pain in muscles, joints, or viscera distal at the site of application by stimulating cutaneous sensory receptors and a method of making such lotion and being made from camphor and menthol crystals.

Abstract: A muscle relaxant and analgesic composition having at least five percent and preferably ten percent oil of Melaleuca spp. therein. The composition also contains other aromatic oils, such as camphor, menthol and methyl salicylate, a thickening agent, a preservative, and a carrier. The composition provides relief for sore muscles or joints when applied topically to the affected area. The Melaleuca oil preferably contains at least thirty percent terpinen-4-ol and less than fifteen percent 1,8-cineole.

Abstract: An analgesic composition useful in providing temporary relief from the symptoms of arthritis is disclosedng having the following components in approximately the stated weight-percentages ranges:______________________________________ Water (Deionized) 86.00-95.35% by weight; Carbopol 934 0.5-2.00% by weight; Methylparaben 0.1-0.40% by weight; Propylparaben 0.05-0.20% by weight; Hampene 100 0.05-0.20% by weight; Aloe Vera Gel 0.05-2.00% by weight; Benzyl Alcohol 0.30-1.20% by weight; Camphor (U.S.P.) 0.50-2.00% by weight; Menthol (U.S.P.) 1.00-4.00% by weight; Thymol 0.10-0.60% by weight; Eugenol 0.10-0.60% by weight; Witch Hazel 0.05-1.50% by weight; Isopropyl Alcohol 0.05-1.50% by weight; Eucalyptus Oil 0.50-2.00% by weight; Triethanolamine 0.50-2.00% by weight; and, Quaternium-15 0.10-0.40% by weight.

Abstract: A pharmaceutical preparation for the percutaneous administration comprises eperisone or tolperisone, including salts thereof, and a monoglyceride of an aliphatic acid having 8 to 12 carbon atoms or/and an ester of lactic acid with an aliphatic alcohol having 12 to 18 carbon atoms. It is improved in the percutaneous absorption.

Abstract: A pharmaceutical preparation for the percutaneous administration comprises eperisone or tolperisone, including salts thereof, and a monoglyceride of an aliphatic acid having 8 to 12 carbon atoms or/and an ester of lactic acid with an aliphatic alcohol having 12 to 18 carbon atoms. It is improved in the percutaneous absorption.

Abstract: Certain acylated benzilic acid derivatives are useful for influencing therapeutically the tone of the urinary bladder in humans and animals. These derivatives are N-alkyl-4-piperidyl .alpha.,.alpha.-diphenyl-.alpha.-acyloxyacetates having the formula ##STR1## wherein R is H, CH.sub.3, C.sub.2 H.sub.5 or C.sub.3 H.sub.7 ; R' is H, NH.sub.2, phenyl, carboxyphenyl, (C.sub.1 -C.sub.6)alkyl, hydroxy(C.sub.1 -C.sub.6)alkyl, methoxy, ethoxy, methoxymethyl, ethoxymethyl, amino(C.sub.1 -C.sub.6)alkyl which can be substituted in the alkyl radical by one or more of a --NH.sub.2, --COOH or --SCH.sub.3 group, N-acetylamino(C.sub.1 -C.sub.6)alkyl, or a group having the formula--CH.dbd.CH--COOR"or--(CH.sub.2).sub.n --COOR"where n is an integer from 0 to 8, and R" is H, CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, or a pharmacologically acceptable cation; or a salt thereof with a pharmaceutically acceptable acid.

Abstract: This invention provides the use of Botulinum toxin (BTX) to cause paralysis of a depressor anguli oris (DAO) musculature in a patient to alleviate downturn at corners of the patient's mouth.