Abstract: Provided herein are bitter taste receptor ligands, related agents, combinations, compositions, methods and systems for modulating release of a metabolic hormone in vitro or in vivo from cells of the GI tract of an individual.

Abstract: Disclosed herein are ionic liquid compositions comprising active pharmaceutical, biological, and nutritional compounds, and methods of use. Further disclosed are compositions of matter including liquid ion pairs alone or in solution and their use; compositions of ionic liquids that are ‘solvated,’ for example, ‘hydrated’ and their uses.

Abstract: The present invention, which is applicable in the pharmaceutical industry, relates to the use of fibrates, in particular fenofibrate, especially in the form of a solid oral composition, for the manufacture of a drug for the treatment of sleep apnea, sleep apnea syndrome, in particular obstructive sleep apnea or obstructive sleep apnea syndrome.

Abstract: The invention relates to the use of the acetyl L-carnitine in association with the biotin for the treatment of patients with Type 2 insulin-resistant diabetes mellitus.

Abstract: The present invention provides cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compounds, which may be substituted in the 1-position with amino, amido, ether or ester groups, e.g., a 1-OH cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compound. The cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma. Moreover, the cyclopentane heptanoic, 2-(cycloalkyl or arylalkyl) compounds of this invention are smooth muscle relaxants with broad application in systemic hypertensive and pulmonary diseases; smooth muscle relaxants with application in gastrointestinal disease, reproduction, fertility, incontinence, shock, etc.

Abstract: The present invention relates to salts and compositions of tramadol and ibuprofen, their crystal form, processes for preparation of the same and their uses for the treatment of pain.

Abstract: The present invention relates to oral formulations comprising an active agent comprising at least one of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid, salts of 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid or buffered 2-[4-(4-chlorobenzoyl)phenoxy]-2-methyl-propanoic acid.

Abstract: A compound of the general formula (I) is provided for use in the topical treatment of infection, inflammation and/or pain: wherein R1 independently represents a methylene group, an ethylene group or a straight or branched chain C3 to C6 alkylene group; R2 independently represents a hydrogen atom, a methyl group, an ethyl group or a straight or branched chain C3 to C20 alkyl group; x represents 0 or an integer from 1 to 4 and y represents 0 or an integer from 1 to 4, wherein the sum of x and y is 4; and Z represents a hydrogen atom or (HOR1)yR2XN+; compositions including the compound; use of the compound in the manufacture of a medicament; and methods of medical treatment including the topical application of the compound.

Abstract: Therapeutic compounds are disclosed herein. Methods, compositions, and medicaments related thereto are also disclosed. The compounds described herein are used to treat ocular conditions, bowel disease and baldness.

Abstract: The present invention relates to pharmaceutical compositions, formulations and medicaments comprising a bupropion salt, in particular, modified-release tablets comprising an effective amount of bupropion hydrobromide, and the use of the bupropion salt to prepare a medicament to treat a condition.

Abstract: Novel ligand antagonists of the RAR receptors have the following structural formula (I): in which A is a CH2, CHOH, C?O or C?N—OH radical or a sulfur or selenium atom; B is a radical selected from among those of formulae (a) to (f): and Ar is a radical selected from among those of formulae (g) to (i):

Abstract: Drug substances comprising a pharmaceutically acceptable organic acid addition salt 6f amine containing pharmaceutically active compounds useful for the treatment of a therapeutic ailment administration and exhibiting prophylactic properties when employed in non-therapeutic administration.

Abstract: The present invention relates to methods of treating ADAMTS-5-associated diseases and particularly osteoarthritis comprising administering an agent capable of modulating ADMATS-5 activity to a subject afflicted with the disease. The agent is preferably a biaryl sulfonamide compound. The invention is based, in part, on the discovery that transgenic animals that do not express functional ADAMTS-5 show a reduction in the degree of osteoarthritis after the induction of osteoarthritis as compared to WT animals. Furthermore, the ADAMTS-5 transgenic animals have reduced aggrecanase activity in articular tissue as compared to WT animals. These animals are good models for ADAMTS-5-associated diseases, and for screening of drugs useful in the treatment and/or prevention of these diseases. There are no other animal models in which the deletion of the activity of a single gene is capable of abrogating the course of osteoarthritis.

Abstract: A method for making a polycarbonate article is described wherein the article is made by rotation molding a melt polycarbonate having a weight average molecular weight from 25,000 to about 36,000. The melt polycarbonate is produced by transesterifying a diaryl carbonate and a dihydroxy compound in the presence of a catalyst system to form an intermediate aromatic polycarbonate, wherein the catalyst system comprises a first catalyst selected from the group consisting of alkali metal salts and alkaline earth metal salts; and a second catalyst selected from the group consisting of quaternary ammonium compounds and quaternary phosphonium compounds; adding to said intermediate aromatic polycarbonate a catalyst quencher, and rotation molding the aromatic polycarbonate at a temperature from about 305° C. to about 360° C. Also disclosed are polycarbonate light diffusive articles produced by rotation molding.

Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, X, Y, R1, R2, R3, and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.

Abstract: ?2-agonists, such as clenbuterol and salbutamol can enhance the recovery of locomotive function and/or neuromuscular strength following spinal cord injuries or as a result of degenerative neural conditions such as Mnd. Pharmacological compositions for treating spinal cord injuries and degenerative neural conditions are also provided.

Abstract: The present invention provides an essentially nonaqueous, liquid pharmaceutical concentrate composition for oral administration containing sertraline or a pharmaceutically acceptable salt thereof and one or more pharmaceutically acceptable excipients. The present invention also provides a use of this concentrate composition to prepare an aqueous solution of sertraline. In addition, the present invention provides a method of using this concentrate composition to treat or prevent a variety of diseases or conditions. Finally, the present invention provides the compound, (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamine methanesulfonate.

Abstract: The present invention is directed to a formulation comprising a lipid-regulating agent dissolved in at least one structured lipid as the primary solvent medium for said agent. One or more emulsifiers may be added to the formulation.

Abstract: The present invention concerns novel pharmaceutically active compounds, pharmaceutical compositions containing the same, the compounds for use as medicaments, and use of the compounds for the manufacture of specific medicaments. The present invention also concerns a method of treatment involving administration of the compounds. Specifically, the compounds are pharmaceutically acceptable salts of tolterodine or hydroxytolterodine, wherein the salt is of an acid selected from the group consisting of aliphatic mono- and dicarboxylic acids comprising from 7 to 24 carbon atoms, alkanedisulfonic acids comprising from 2 to 4 carbon atoms, naphthoic acid derivatives comprising from 11 to 27 carbon atoms, maleic acid and fumaric acid.

Abstract: The present invention relates to methods of improving a treatment outcome comprising administering a heat shock protein (HSP) preparation or an ?-2-macroglobulin (?2M) preparation with a non-vaccine treatment modality. In particular, an HSP preparation or an ?2M preparation is administered in conjunction with a non-vaccine treatment modality for the treatment of cancer or infectious diseases. In the practice of the invention, a preparation comprising HSPs such as but not limited to, hsp70, hsp90 and gp96 alone or in combination with each other, noncovalently or covalently bound to antigenic molecules or ?2M, noncovalently or covalently bound to antigenic molecules is administered in conjunction with a non-vaccine treatment modality.

Abstract: This invention relates to biocidal compositions and methods of using same. Also provided is a process for the manufacturing of a biocidal composition in the form of a tablet and a method of using the biocidal compositions for the disinfection of water that may contain microorganisms and biofilms.

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: The present invention is directed to a formulation comprising a lipid-regulating agent dissolved in at least one monoglyceride as the primary solvent medium for said agent. One or more emulsifiers may be added to the formulation.

Abstract: This invention relates to methods and compositions for bringing about changes in skin pigmentation. More particularly, this invention relates to compounds which affect melanogenesis and can be used as depigmenting agents or as agents for darkening skin utilizing the PAR-2 pathway.

Abstract: The present invention provides a novel agent for prophylaxis or treatment of inflammatory bowel diseases for oral administration or intra-intestinal infusion, which comprises as an active ingredient a compound of the formula (I): or a pharmaceutically acceptable salt thereof; a use of said active ingredient in preparation of an agent for prophylaxis or treatment of inflammatory bowel diseases; and a method for prophylaxis or treatment of inflammatory bowel diseases.

Abstract: Treatment of pain syndromes utilizes a topical polypharmaceutical preparation of phenoxybenzamine, ketamine, gabapentin, nifedipine, carbamazepine, or combinations of them. Other suitable components are blockers of sympathetic alpha 1, 2 and other receptors, NMDA receptor blockers, GABA receptor blockers, AMPA receptor blockers, nitric oxide synthase receptor blockers, calcium channel blockers, ACDP receptor blockers, prostaglandin and leukotriene blockers, substance P blockers, bradykinin and neurotenin as well as other peptide blockers, and TNF alpha blockers. Recommended delivery is by locating a predetermined neurodermal point and locating a gel patch over the predetermined neurodermal point. Iontophoresis then delivers the pharmaceutical agent from the gel patch.

Abstract: The present invention concerns novel pharmaceutically active compounds, pharmaceutical compositions containing the same, the compounds for use as medicaments, and use of the compounds for the manufacture of specific medicaments. The present invention also concerns a method of treatment involving administration of the compounds.

Abstract: The present invention relates to new cinnamic acid salts of salmeterol, processes for the preparation thereof as well as the use thereof as pharmaceutical compositions.

Abstract: A compound selected from the group consisting of a compound of formula I a compound of formula II and when the compound of formula I and II comprises an amino group pharmaceutically acceptable ammonium salts thereof, wherein R1, R2, Cx, n, R3, R4, R5, Y are as defined in the specification.

Abstract: The present invention provides cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compounds, which may be substituted in the 1-position with amino, amido, ether or ester groups, e.g., a 1-OH cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compound. The cyclopentane heptanoic acid, 2-(cycloalkyl or arylalkyl) compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma. Moreover, the cyclopentane heptanoic, 2-(cycloalkyl or arylalkyl) compounds of this invention are smooth muscle relaxants with broad application in systemic hypertensive and pulmonary diseases; smooth muscle relaxants with application in gastrointestinal disease, reproduction, fertility, incontinence, shock, etc.

Abstract: This invention relates to molecules which inhibit metalloproteinases, including aggrecanase, and the production of tumor necrosis factor (TNF). In particular, the compounds are inhibitors of metalloproteinases involved in tissue degradation and inhibitors of the release of tumor necrosis factor. The present invention also relates to pharmaceutical compositions comprising such compounds and to methods of using these compounds for the treatment of inflammatory diseases.

Abstract: Denatonium benzoate (Bitrex™) dissolves in molten flexible polyvinyl chloride, imparting a bitter flavor to the plastic which discourages rats from gnawing on it. Denatonium benzoate can in all likelihood be added to polymers other than polyvinyl chloride (e.g., polyurethane or polyethylene) either directly or by first dissolving the denatonium benzoate in an organic solvent which is miscible with the chosen polymer and then mixing this solution of organic solvent and denatonium benzoate into a molten solution of the chosen polymer.

Abstract: A pharmaceutical composition comprising: (i) metformin, optionally in the form one of its pharmaceutically acceptable salts; (ii) a fibrate selected from fenofibrate and bezafibrate; and optionally one or more pharmaceutically acceptable excipients, is suitable for use in the treatment of non-insulin-dependent diabetes.

Abstract: The novel agricultural and horticultural fungicidal compositions containing as active ingredients a combination of A) 1,1′-iminiodi(octamethylene)diguanidine of the formula  (iminoctadine) or an acid addition salt thereof and B) 1,1′-iminiodi(octamethylene)diguanidine of the formula  (fenhexamid) are outstandingly active as fungicides.

Abstract: A method is disclosed of preventing retinopathy of prematurity in a prematurely born neonate susceptible to developing retinopathy of prematurity, which comprises the step of parenterally administering to said prematurely born neonate, a therapeutically effective amount of a water-soluble, pharmaceutically effective salt of ibuprofen as an active ingredient to promote retinal and choroidal blood flow autoregulation in said neonate.

Abstract: This invention pertains to novel salt forms of trophenylethylene compound, such as 3-[4(1,2-diphenyl-but-1-enyl)-phenyl]-acrylic acid, as selective estrogen receptor modulators. This invention also provides methods for the treatment and/or prevention of breast, uterine, ovarian, prostrate and colon cancer, osteoporosis, cardiovascular disease, and benign proliferative disorders, as well as pharmaceutical compositions of the compounds of the present invention.

Abstract: An insect control mat having a heatable substrate; an insect control active material; and an aversion material in an amount effective to cause a person to avoid retaining the mat in the person's mouth. A method of controlling insects by use of such a mat is also disclosed.

Abstract: A therapeutic process for treating disease in mammals caused by retroviruses in which the infected mammal is treated with a ribonucleotide reductase inhibitor such as a polyhydroxy benzoic, mandelic or phenylacetic acid derivative, such as N,3,4-trihydroxybenzamide, a hlydroxyurea, a thiosemicarbazone or other ribonucleotide reductase inhibitor. The polyhydroxybenzoic acid derivatives are also useful in the treatment of diseases in mammals caused by DNA viruses.

Abstract: The subject of the invention is the products of formula (I): in which R1, R2, R3, R4, R5 and G are as defined in the description, the dotted lines represent an optional second bond, as well as the addition salts with acids and bases and the esters, their preparation process and the intermediates of this process, their use as medicines and the pharmaceutical compositions containing them.

Abstract: This invention provides for pharmaceutical formulations of compounds which are useful as protective agents when administered to patients also receiving antineoplastic drugs. The invention also includes methods of reducing the toxicity of various antineoplastic agents by administering an effective amount of the protective agent to a patient receiving one or more antineoplastic agents. The compounds useful as protective agents have either a sulfhydryl moiety or are reducible disulfides.

Abstract: Inflammatory dermatoses are controlled and cleared by topical application to the affected areas of the skin of a composition containing both a corticosteroid and a retinoid. The combined therapy is more effective than either active ingredient alone and is particularly effective for chronic dermatoses which are or have become resistant to corticosteroid treatment alone. After clearing has been obtained with once or twice daily applications of the corticosteroid-retinoid composition, usually after several weeks, clearance can be maintained by less frequent application or lower concentrations of the composition or by application of only one of the corticosteroid or retinoid, less potent corticosteroids, or other non-steroidal therapies, depending upon the particular dermatosis being treated.

Abstract: A method for treating emphysema and other disease states in mammals caused by mammalian cells involved in the inflammatory response is disclosed. Mammalian cells participating in the inflammatory response are contacted with an inflammatory response mediator which reduces the undesired inflammatory response and is an antioxidant. The inflammatory response mediator may further provide a cellular energy source and be a building block in the cellular synthesis of other cellular components. Compositions for reducing and treating undesired inflammatory response are also disclosed.

Abstract: A method and pharmaceutical for protecting against mutational damage in mammalian cells, irrespective of the nature of the mutagenic event or source of radiational or chemical insult or the like.

Abstract: Periauricularly administered topical therapy with a carrier system containing local anesthetics is a new and effective treatment of disorders of the inner ear and labyrinth, which has a low incidence of side effects. The use of this type of therapy applies especially to a non-invasive topical treatment of tinnitus, vertigo, lack of balance, and nausea.

Abstract: The invention relates to compounds of the formula (I): ##STR1## wherein A, B and D are various ring systems such as phenyl, R.sup.1 includes carboxy, R.sup.3 is hydrogen or C.sub.1-4 alkyl and Z is a linking group such as --(CH(R.sup.5)).sub.m -- wherein m is 2, 3 or 4, and R.sub.5 includes hydrogen and methyl; and pharmaceutically acceptable salts and in vivo hydrolysable esters or amides thereof, processes for preparing these compounds, pharmaceutical compositions comprising them, and their use in the treatment of pain.

Abstract: A pesticide preparation of aqueous suspension type which comprises:(a) a 1,1'-iminiodi(octamethylene)diguanidinium tris(alkyl-benzenesulfonate) as an active pesticide ingredient;(b) at least one dispersion stabilizer selected from among alcohols having a degree of ethoxylation of 0 to 4 and carrying an alkyl group or an alkenyl group having 8 to 18 carbon atoms and phospholipids;(c) at least one surfactant selected from among surfactants carrying an alkyl group or an alkenyl group having 6 to 20 carbon atoms; and(d) water.

Abstract: The present invention provides novel isocarbacyclin derivatives useful for search and study of prostacyclin receptor and as a therapeutic drug for central nervous system diseases, which derivatives are expressed by the following formula ?I!: ##STR1## ?where, R.sup.1 represents a hydrogen atom, an alkyl group, or cation of an appropriate amount, and R.sup.2 an alkylene group.

Abstract: A compound of the following structure: ##STR1## wherein R.sub.8 =H: R.sub.1 =alkyl, cycloalkyl, arylalkyl, aryl;R.sub.2 =cycloalkyl, aryl, C.sub.3 -C.sub.10 alkyl;X,Y=O, S(O).sub.n, NH;Z=CO.sub.2 R.sub.3, C(O)CO.sub.2 R.sub.3, CH(OH)CO.sub.2 R.sub.3, CHFCO.sub.2 R.sub.3, CF.sub.2 CO.sub.2 R.sub.3, CONR.sub.3 R.sub.4, CONR.sub.3 OR.sub.4, CONR.sub.3 NR.sub.4 R.sub.5, 1-tetrazole, C(O)CONR.sub.3 R.sub.4, CH(OH)CONR.sub.3 R.sub.4, CF.sub.2 CONR.sub.3 R.sub.4R.sub.3, R.sub.4, R.sub.5 =hydrogen, alkyl, aryl, aryalkyl, cycloalkyl, or fluoroalkyl;halo=Cl, Br, or I;fluoroalkyl=CF.sub.3, CHF.sub.2, CH.sub.2 F, CH.sub.2 CF.sub.3, C.sub.2 F.sub.5 ;cycloalkyl=C.sub.3 -C.sub.6 cycloalkyl;arylalkyl=C.sub.1 -C.sub.4 alkyl aryl;aryl=phenyl, furanyl, thienyl, or pyridyl; andn=0-2;or pharmaceutically acceptable salts thereof, useful in the treatment of asthma, and allergic and inflammatory diseases, as well as methods of treatment and pharmaceutical compositions utilizing the same.

Abstract: The present invention provides novel methods for prevention or treatment of primary and recurring squamous cell carcinoma of the oral cavity or oropharynx comprising topical administration, to the oral cavity or oropharynx, of an effective amount of an NSAID, especially a composition administering from about 0.001% to about 0.2% ketorolac to the oral cavity, alone or as an adjunct to surgery and/or radiation therapy.

Abstract: The invention relates to a new vitamin D compound of the general formula ##STR1## wherein: R.sub.1 is a hydrogen atom or a hydroxy group;R.sub.2 is a (C.sub.1 -C.sub.3)alkyl group, a hydroxy(C.sub.1 -C.sub.3)alkyl group, a (C.sub.1 -C.sub.2)alkoxymethyl group or a (C.sub.2 -C.sub.3)alkenyl or alkynyl group;R.sub.3 is a branched or non-branched, saturated or unsaturated aliphatic 3- to 5 -membered hydrocarbon or oxahydrocarbon biradical, having at least 3 atoms in the main chain and being optionally substituted with one or more substituents selected from epoxy, fluoro and hydroxy;R.sub.4 is a sec. or tert. (C.sub.3 -C.sub.6)alkyl group or a (C.sub.3 -C.sub.6)cycloalkyl group; andA and B are each individually hydrogen atoms or methyl groups, orA and B form together a methylene group.The invention further relates to a method of preparing these compounds and to their use in pharmacotherapy and cosmetics.