Abstract: The present invention provides pharmaceutically active compounds formula I wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2(C2-C6 alkyl); R2 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), —OSO2(C2-C6 alkyl), or halo; R3 is 1-piperidinyl, 1-pyrrolidinyl, methyl-1-pyrrolidinyl, dimethyl-1-pyrrolidino, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; and n is 2 or 3; and or a pharmaceutically acceptable salt thereof. Also provided are compounds of formula II wherein R1a is —H or —OR5 in which R5 is a hydroxy protecting group. R2a is —H, halo, or —OR6 in which R6 is a hydroxy protecting group; and R4 is —OH or —CHO; or a pharmaceutically acceptable salt thereof.

Abstract: In accordance with the present invention, there are provided normal modified forms of nonsteroidal anti-inflammatory drugs. Modified NSAIDs according to the invention provide a new class of anti-inflammatory agent which provide the therapeutic benefits of NSAIDs while causing a much lower incidence of side-effects then typically observed with such agents.

Abstract: The present invention is directed to compositions that inhibit the nonenzymatic glycation of albumin,, as well as methods of using compounds that inhibit albumin glycation for the treatment of glycation-related pathologies.

Abstract: The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and an intracellular transporting adjuvant, characterized by the presence of a covalent bond which is scission-sensitive to intracellular enzyme activity. The prodrug may be used in a technique for treating a condition or disease in a mammal related to supranormal intracellular enzyme activity, whereby on administering it to a human having such condition or disease, the bond is broken in response to such activity, and the pharmacologically active compound is activated selectively within cells having such supranormal intracellular enzyme activity.

Abstract: A class of novel phenyl acetamides is disclosed together with the use of such compounds for inhibiting sPLA2 mediated release of fatty acids for treatment of conditions such as septic shock.

Abstract: The invention relates to the use of trimebutine [2-dimethylamino-2-phenylbutyl-3,4,5-trimethoxy-benzoate hydrogen maleate] or its corresponding stereoisomers for the preparation of a medicament to prevent and/or treat arthritis, osteo-traumatic pain, and neuralgias.

Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) 1

Abstract: Haloacetoamido, benzoic acid derivatives having anti-tumorigenic activity. Examples of the haloacetoamido, benzoic acid derivatives include 3-chloroacetoamido, benzoylurea, 3-bromoacetoamido, benzoylurea, 3-iodoacetoamido, benzoylurea, ethyl-3-chloroacetoamido, benzoate, ethyl-3-bromoacetoamido, benzoate and ethyl-3-iodoacetoamido, benzoate. Intermediates for synthesizing the derivatives, along with method of making and using the derivatives, are also provided.

Abstract: Amphiphilic polyamide compounds and derivatives thereof having the property of promoting transfection of polynucleotides and polypeptides into cells, and formulations comprising said compounds.

Abstract: Methods of promoting allograft survival, by attenuating or preventing allograft rejection, and treating or ameliorating the post-transplantation syndrome complex associated with allograft rejection and immunosuppressive pharmacotherapy used to prevent allograft rejection, are described. These methods comprise administering to an human or animal in need of treatment an effective amount of an insulin-sensitizing compound or and pharmaceutically acceptable salts and solvates thereof, administered alone or in combination with other immunosuppressive drugs.

Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formula (XII) 1

Abstract: Methods for treating neurodegenerative diseases and disorders are disclosed. The methods utilize compositions containing certain compounds having an anti-inflammatory and anti-oxidant moiety covalently linked by an amide or ester bond.

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 relates to the method of using specially formulated neurotrophic pipecolic acid derivative compounds having an affinity for FKBP-type immunophilins as inhibitors of the enzyme activity associated with immunophilin proteins, and particularly inhibitors of peptidyl-prolyl isomerase or rotamase enzyme activity to stimulate or promote neuronal growth or regeneration.

Abstract: The present invention relates generally to mitochondria protecting agents for treating diseases in which mitochondrial dysfunction leads to tissue degeneration and, more specifically, to compounds, compositions and methods related to the same. The methods of this invention involve administration of a pharmaceutically effective amount of a mitochondria protecting agent to a warm-blooded animal in need thereof, and composition of this invention contain a mitochondria protecting agent in combination with a pharmaceutically acceptable carrier or diluent. Mitochondrial associated diseases which may be treated by the present invention include (but are not limited to) Alzheimer's Disease, diabetes mellitus, Parkinson's Disease, neuronal and cardiac ischemia, Huntington's disease and stroke.

Abstract: 1-phenyl-3-dimethylaminopropane compounds corresponding to the formula I 1

Abstract: Materials derived from Citrus plants can be administered orally to humans for the purpose of producing or maintaining weight loss as well as for improving the person's physical performance and increasing the person's lean muscle mass. The Citrus materials include those portions of the plant that are normally considered waste or inedible, such as the leaves, peel, and immature, unripe fruit. The materials contain at least one of the alkaloids from the group consisting of synephrine, hordenine, octopamine, tyramine and N-methyltyramine (1). Two species, Citrus aurantium and Citrus reticulata, are particularly useful. The materials can be administered in their natural form or as extracts, and can be administered in various ways including capsules and tablets. The Citrus materials may also be used as a tea. For weight loss and weight control, the materials can be administered concurrently with caloric restriction or in the absence of caloric restriction.

Abstract: Materials derived from Citrus plants can be administered orally to humans for the purpose of producing or maintaining weight loss as well as improving the person's physical performance and increasing the person's lean muscle mass. The Citrus materials include those portions of the plant that are normally considered waster or inedible, such as the leaves, peel and immature, unripe fruit. The materials contain as least one of the alkaloids from the group consisting of synephrine, hordenine, octopamine, tyramine and N-methylamine. Two species, Citrus aurantium and Citrus reticulata, are particularly useful. The materials can be administered in their natural form or as extracts, and can be administered in various ways including capsules and tablets. The Citrus materials may also be used as a tea. For weight loss and weight control, the materials can be administered concurrently with caloric restriction or in the absence of caloric restriction.

Abstract: The naphthyloxyacetic acid derivatives of the formula (I) wherein A is H, -(alkylene)COOR1, -(alkylene)CONR2R3, -(alkylene)OH, -(alkylene)tetrazole, -(alkylene)CN; E is single bond or alkylene; G is —S—, —SO—, —SO2—, —O— or —NR4—; L is alkylene, —(CH2)m—CH═CH—(CH2)n— or —(CH2)x—CH(OH)—(CH2)y—; M is phenyl, phenyl(thio, oxy, amino), diphenylmethyl, diphenylmethyl(thio, oxy, amino), and pharmaceutical composition comprising them as an active ingradient. The compounds of the formula (I) can combine PGE2 receptor and exhibit the activity to antagonize or agonize for PGE2 receptor. Therefore, they are useful as anti-hyperlipemia, for the prevention of abortion, for analgesics, as antidiarrheals, sleep inducer, diuretic, anti-diabetes, abortient, cathartics, antiulcer, anti-gastritis or antihypertensive etc.

Abstract: The subject invention provides compounds which are easily metabolized by the metabolic drug detoxification systems. Particularly, fluvoxamine analogs which have been designed to include esters within the structure of the compounds are taught. Also provided are methods of treating depression and affective disorders, such as obsessive compulsive disorder. Pharmaceutical compositions of the fluvoxamine analogs are also taught.

Abstract: Chemical structures have been identified which allosterically modify pyrvate kinase and inhibit enzymatic activity. These compounds can be used as pharmaceuticals in the treatment of a wide variety of diseases and disorders where influencing metabolic processes is beneficial, such as the glycolytic pathway, all pathways which use ATP as an energy source, and all pathways which involve 2,3-diphosphoglycerate related to the delivery of oxygen by modifying hemoglobin's oxygen affinity, treatments of tumor and cancer and Alzheimer's disease (AD).

Abstract: The present invention relates to compounds of formula (I) 1

Abstract: Snake repellents include a repellent composition, an inert carrier and an adjuvant. The snake repellents include an essential oil selected from a group of essentials oils or a reagent from one of the essential oils. Methods of repelling snakes include exposing snakes to the snake repellents by aerosol, vapor or fog.

Abstract: Materials derived from Citrus plants can be administered orally to humans for the purpose of producing or maintaining weight loss as well as for improving the person's physical performance and increasing the person's lean muscle mass. The Citrus materials include those portions of the plant that are normally considered waste or inedible, such as the leaves, peel, and immature, unripe fruit. The materials contain at least one of the alkaloids from the group consisting of synephrine, hordenine, octopamine, tyramine and N-methyltyramine (1). Two species, Citrus aurantium and Citrus reticulata, are particularly useful. The materials can be administered in their natural form or as extracts, and can be administered in various ways including capsules and tablets. The Citrus materials may also be used as a tea. For weight loss and weight control, the materials can be administered concurrently with caloric restriction or in the absence of caloric restriction.

Abstract: A dosage form, a therapeutic composition, and the use thereof is disclosed for administering a therapeutic agent accompanied by a pharmaceutically acceptable means administered for an indicated therapy.

Abstract: The present invention relates to compounds of the general formula (1) 1

Abstract: A method is provided for increasing the permeability of skin or mucosal tissue to transdermally administered oxybutynin. The method involves use of a specified amount of a hydroxide-releasing agent, the amount optimized to increase the flux of the drug through a body surface while minimizing the likelihood of skin damage, irritation or sensitization. Formulations, drug delivery systems and methods of treatment are provided as well.

Abstract: This invention relates to substituted bis-acridines and related compounds which are ligands, in particular, antagonists of the CCR5 receptor. In addition, this invention relates to the treatment and prevention of disease states mediated by CCR5, including, but not limited to, asthma and atopic disorders (for example, atopic dermatitis and allergies), rheumatoid arthritis, atherosclerosis, psoriasis, autoimmune disease such as multiple sclerosis, and inflammatory bowel disease, all in mammals, by the use of substituted bis-acridines and related compounds which are CCR5 receptor antagonists. Also, since CCR5 is a co-receptor for the entry of HIV into cells, selective receptor ligands may be useful in the treatment of HIV infection.

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: A class of cysteine protease inhibitors which inactivate a cysteine protease by covalently bonding to the protease and releasing a heterocyclic leaving group is presented. The cysteine protease inhibitors of the present invention comprise a first portion which targets a desired cysteine protease and positions the inhibitor near the thiolate anion portion of the active site of the protease, and a second portion which covalently bonds to the cysteine protease and irreversibly deactivates that protease by providing a carbonyl or carbonyl-equivalent which is attacked by the thiolate anion of the active site of the cysteine protease to sequentially cleave a heterocyclic leaving group. The heterocyclic leaving group of the protease inhibitor is of the formula: —O—Het, where Het is a heterocycle having 4-7 atoms in the ring, with at least one of the heterocycle atoms being N, O or S.

Abstract: Amidino and benzamidino compounds, including compounds of the formula: 1

Abstract: Dosage form unit is provided to deliver one or more beneficial agents into a fluid, such as liquid enteral nutritional product. The dosage form unit includes a core containing at least one beneficial agent, preferably a marker dye, which is dispersible in the fluid. The core also contains a compatible binding agent to bind the beneficial agent together. Additional components of the core may include a plasticizer, a standard flow agent, a lubricant, additional tableting aids and at least one hydrophilic agent. A latex coating encases the core. The latex coating includes a mixture containing a substantially hydrophobic base material, preferably formed from an emulsion of cellulose acetate microspheres, which is capable of defining a matrix-type membrane, and at least one hydrophilic component being dispersible in the fluid. A dispersible beneficial agent is preferred as one of the hydrophilic components of the latex coating to allow immediate release of the beneficial agent therefrom.

Abstract: Substantially optically pure S-oxybutynin, or a pharmaceutically acceptable salt thereof, is administered as a treatment for asthma. Such treatment is provided while reducing the adverse effects associated with the administration of racemic oxybutynin.

Abstract: The application discloses substituted norbornylamino derivatives, processes for their preparation, their use as medicaments or diagnostics and a medicament comprising them

Abstract: The present application relates to novel compounds belonging to the benzylaminodiacetamide family which have good anti-irritant and soothing properties. The invention also relates to their use in a composition comprising a physiologically acceptable medium, in particular in order to prevent and/or treat certain cutaneous disorders and more particularly in order to treat sensitive skins.

Abstract: 3-amino-3-arylpropan-1-ol compounds corresponding to the formula I in which R1 to R5, A and X have the meanings according to claim 1, and their preparation and use as medicaments.

Abstract: Pesticidally active cyclohexadienyl derivative compounds of the formula I that are esters, oximes or amides are claimed. These compounds may be used as fungicides, acaricides and insecticides in plant protection.

Abstract: The subject-matter of the present invention is novel compounds of the type of esters derived from alkylenediaminediacetic acid or alkylenediaminetriacetic acid and their-process of preparation. The invention also relates to the use of these compounds in cosmetic and pharmaceutical compositions, in particular for protecting the body against oxidative stress.

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: Alkoxy and/or acyloxy disubstituted and polysubstituted aralkyl and aralkenyl bis-quaternary ammonium derivatives of cyclic alkanol diesters have neuromuscular relaxant properties.

Abstract: Novel derivatives of 1-aminoindan and their salts are described. Optically active 1-aminoindan derivatives are prepared by reacting a N-benzyl analog of the desired compound with an enantiomer of mandelic acid.

Abstract: A composition and a dosage form are disclosed comprising oxybutynin alone/or accompanied by another drug indicated for therapy. A method is disclosed for administering oxybutynin alone/or accompanied by a different drug or for administering oxybutynin and a different drug according to a therapeutic program for the management of incontinence alone, and for other therapy.

Abstract: A composition and a dosage form are disclosed comprising oxybutynin alone/or accompanied by another drug indicated for therapy. A method is disclosed for administering oxybutynin alone/or accompanied by a different drug or for administering oxybutynin and a different drug according to a therapeutic program for the management of incontinence alone, and for other therapy.

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 provides a simple multi-tablet system for the treatment of urinary incontinence with oxybutynin. Particular embodiments of the invention provide a first tablet that releases oxybutynin over a short period of time, e.g. less than six hours, and a second tablet that releases oxybutynin over an extended period of time, e.g., eighteen to twenty-four hours, to maintain therapeutically effective levels oxybutynin in the mammal for a period of about twenty four hours. Unlike other systems, this system is easily adaptable to compensate for patient to patient variability in response to oxybutynin therapy. The invention also provides a method of treating urinary incontinence with the above system and a kit comprising various first and second tablets to rapidly develop a patient's preferred dosing regimen, i.e., the dosing regimen which provides the greatest therapeutic benefit and/or least amount or severity of side effects.

Abstract: 1-phenyl-3 -dimethylaminopropane compounds corresponding to the formula I a method of preparing them, and the use of these substances as analgesic active ingredients in pharmaceutical compositions.

Abstract: Novel compounds, their salts and compositions related thereto having activity against mammalian integrins are disclosed. The compounds are useful in vitro or in vivo for preventing or treating thrombotic or restenotic disorders.

Abstract: The invention relates to compounds of the formula in which: A is a divalent radical selected from: A1) —O—CO— A2) —CH2—O—CO— A3) —O—CH2—CO— A4) —O—CH2—CH2— A5) —N(R1)—CO— A6) —N(R1)—CO—CO— A7) —N(R1)—CH2—CH2— A8) —O—CH2— in which: R1 is a hydrogen or a (C1-C4)-alkyl; and Am is a nitrogen-containing heterocycle.

Abstract: Materials derived from Citrus plants can be administered orally to humans for the purpose of producing or maintaining weight loss as well as for improving the person's physical performance and increasing the person's lean muscle mass. The Citrus materials include those portions of the plant that are normally considered waste or inedible, such as the leaves, peel, and immature, unripe fruit. The materials contain at least one of the alkaloids from the group consisting of synephrine, hordenine, octopamine, tyramine and N-methyltyramine (1). Two species, Citrus aurantium and Citrus reticulata, are particularly useful. The materials can be administered in their natural form or as extracts, and can be administered in various ways including capsules and tablets. The Citrus materials may also be used as a tea. For weight loss and weight control, the materials can be administered concurrently with caloric restriction or in the absence of caloric restriction.

Abstract: An ascorbic acid-based composition and related method for the treatment of aging or photo-damaged skin is disclosed. The composition includes water and ascorbic acid, at least a portion of which has generally been pretreated by being dissolved under relatively high temperature and concentration conditions. The composition typically includes at least about 5.0% (w/v) ascorbic acid and may advantageously be formulated to have a pH above 3.5. Generally, the composition also includes non-toxic zinc salt, tyrosine compound, and/or pharmaceutically acceptable carrier. In addition, the composition may include an anti-inflammatory compound, such as aminosugar and/or sulfur-containing anti-inflammatory compound. The topical composition may be in the form of a serum, a hydrophilic lotion, an ointment, a cream, or a gel.