Abstract: A method and composition for the treatment of acne vulgaris, acne rosacea, and other inflammatory skin conditions comprises the oral administration of a composition comprising a dose of nicotinamide delivered at levels substantially in excess of normal dietary levels, the nicotinamide being delivered in combination with zinc. The composition may also include quantities of copper and folic acid. In a most preferred embodiment, the nicotinamide and copper each are present in immediate release formats, while the zinc is present in a sustained release format.

Abstract: 2-(S)-hydroxymutilin carbamate derivatives of formula (I), in which R1 is a 5- or 6-membered optionally substituted heteroaryl group; and R2 is vinyl or ethyl, are useful in the treatment of bacterial infections

Abstract: An amlodipine maleate pharmaceutical composition is provided with good stability when formulated with a pH within the range of 5.5 to 7, when measured as a 20 wt % aqueous slurry. The stability can also be aided by making the pharmaceutical composition from amlodipine maleate particles having an average particle size of greater than 20 microns, preferably greater than 100 microns.

Abstract: The present invention provides processes useful in the preparation of certain ?3-adrenergic receptor agonists of the structural formula the pharmaceutically acceptable salts thereof, and the hydrates of said pharmaceutically acceptable salts, wherein HET is as described herein. The invention further provides intermediates useful in the preparation of such agonists, and processes useful in the production of such intermediates.

Abstract: The invention relates to new piperazinyl-substituted pyridylalkane, alkene, and alkine acid amides substituted with saturated or one or several-fold unsaturated hydrocarbon residue in the carboxylic acid group according to the general formula (I) as well as methods for the production of these compounds, medicaments containing these and their production as well as their therapeutic use, especially as cytostatic agents and immunosuppressive agents, for example in the treatment or prevention of various types of tumors and control of immune reactions such as autoimmune diseases.

Abstract: The present invention relates to compositions without added iron and methods for prophylactic nutritional supplementation and therapeutic nutritional supplementation. Specifically, the method involves administering to an individual a composition comprising carotenoids, vitamin E, vitamin D, vitamin C, thiamine, riboflavin, niacin, folic acid, pyridoxine, biotin, pantothenic acid, cobalamin, magnesium, manganese, zinc, selenium, chromium, copper, alpha lipoic acid, and lutein, wherein the composition is free of added iron.

Abstract: The invention relates to compositions and methods for promoting production gains in animals, and of enhancing the efficacy of therapeutic agents. The gains are achieved through reduction in stress, including through the use of antistress agents. Compositions comprising therapeutic agents such as anthelmintics, and antistress agents are provided.

Abstract: The present invention is directed in part towards methods of modulating the function of calcium channels with pyridine- or 1,4-dihydropyridine-based compounds. In addition, the invention describes methods of preventing and treating protein kinase-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to pyridine- or 1,4-dihydropyridine-based compounds and pharmaceutical compositions comprising these compounds.

Abstract: The present invention is directed to an inhalable formulation for the treatment of pulmonary hypertension in a mammal (e.g., humans), wherein the formulation comprises at least one hypertension reducing agent, including but not limited to an angiotensin converting enzyme inhibitor, angiotensin receptor blocker, beta-blocker, calcium-channel blocker or vasodilator, or any combination thereof. The formulations of the present invention may be a solution or suspension, and preferably are suitable for administration via nebulization. The present invention is also directed to a method and kit for treating a mammal suffering from pulmonary hypertension.

Abstract: The invention relates to a process for preparing 2-halopyridinecarboxamides of primary aromatic monoamines I which have a substituent other than hydrogen in the ortho-position to the amino group by reaction of 2-halopyridinecarbonyl chloride II with the aromatic monoamine I, which comprises carrying out the reaction in a solvent mixture comprising water and at least one water-immiscible organic solvent in the presence of none or less than 10 mol %, based on the 2-halopyridinecarbonyl chloride II, of a base other than I or II.

Abstract: This invention pertains to therapeutic antibacterial/antifungal-wound healing compositions comprising a therapeutically effective amount of antibacterial agents and/or antifungal agents and/or wound healing composition alone. In one embodiment, the wound healing composition comprises (a) zinc oxide; (b) calcium channel blocker, and (c) fat-soluble vitamins admixed with antibacterial and antifungal agents. The therapeutic antibacterial/antifungal-wound healing compositions may be utilized in a wide variety of pharmaceutical products and administered orally or topically.

Abstract: The invention relates to a salt formed of at least one AT1-receptor antagonist having at least one acidic center and of at least one cardiovascular ingredient having at least one basic center that can be used for treating cardiovascular diseases and conditions, their prophylaxis or delay of progression.

Abstract: A topical composition which enhances sexual responsiveness of a mammal is disclosed. An effective dosage of a peripheral vasodilator, an absorption enhancer and, optionally, a vasoconstrictor and an alpha receptor blocker are combined with a pharmaceutically-acceptable topical vehicle to produce the composition. The compositions are applied topically to the penis or labia majora and minora pudenda to enhance erection or vasocongestion.

Abstract: Novel prodrugs of amino ceramide-like compounds are provided which inhibit glucosyl ceramide (GlcCer) formation by inhibiting the enzyme GlcCer synthase, thereby lowering the level of glycosphingolipids. The compounds of the present invention have improved GlcCer synthase inhibition activity and are therefore highly useful in therapeutic methods for treating various conditions and diseases associated with altered glycosphingolipid levels.

Abstract: Corticotropin-releasing factor (CRF) antagonists having the formulae wherein the dashed lines, A, B, Y, Z, G, R3, R4, R5, R6, R16 and R17 are as defined in the application, and processes for preparing them. These compounds and their pharmaceutically acceptable salts are useful in the treatment disorders including CNS and stress-related disorders.

Abstract: An easily absorbed and well tolerated proportional nutritional supplementation composition and method to be used in patients suffering from deficiency states due to bowel disease that may include malabsorption and inflammatory bowel disease. It is this unique proportional formulation of antacid, calcium, vitamins, minerals and simethicone in lactose free, sorbitol free, gluten free and hypo allergen solution that is the novel invention. This novel invention allows for nutrients to be readily absorbed with little or no side effects that may be experienced when taking conventional supplements. The supplementation contains amounts of vitamins and minerals that are commonly deficient in these states including magnesium, chromium, increased iron, increased folic acid, calcium and fat soluble vitamins.

Abstract: A method of enhancing the efficiency and increasing the duration of action of drugs (e.g. dihydropyridines and anti-bacterials) and particularly of nifedipine and penicillins wherein one or more hydrogen atoms are deuterated and wherein the deuterated drug has unexpectedly improved properties when used in much lower concentrations than unmodified drug. A method for determining the identity and bioequivalency of a new drug is also disclosed wherein the molecular and isotope structure of a new drug is determined by isotope ratio mass spectrometry and compared with the molecular and isotope structure of a known human drug.

Abstract: The invention is of a non-invasive, topical medicament and associated methodology for use thereof, through the use of which existing scars may be effectively, cost effectively, and painlessly treated. One or more calcium channel blocker agents serve as the primary active ingredient of the present compositions and transdermal penetration agents or carriers are included to facilitate topical delivery of the active ingredient(s) to the intended, sub-dermal treatment site.

Abstract: A method of treating HM74A and/or HM74 mediated disease in an individual which comprises administering to the individual a therapeutic amount of a modulator of HM74A and/or HM74 activity.

Abstract: The present invention relates to a method of treatment of a condition or disease selected from the group consisting of hypertension, left ventricular dysfunction and hypertrophic cardiomyopathy, diabetic cardiac myopathy, supraventricular and ventricular arrhythmias, atrial fibrillation, atrial flutter, detrimental vascular remodeling, myocardial infarction and its sequelae, atherosclerosis, angina (whether unstable or stable), renal insufficiency (diabetic and non-diabetic), heart failure, angina pectoris, diabetes, secondary aldosteronism, primary and secondary pulmonary hypertension, renal failure conditions, such as diabetic nephropathy, glomerulonephritis, scleroderma, glomerular sclerosis, proteinuria of primary renal disease, and also renal vascular hypertension, diabetic retinopathy, the management of other vascular disorders, such as migraine, peripheral vascular disease, Raynaud's disease, luminal hyperplasia, endothelial dysfunction, cognitive dysfunction (such as Alzheimer's), glaucoma and stroke,

Abstract: The present invention is directed to a method of promoting sleep by topically applying onto the skin a composition that comprises a non-hypnotic, vasoactive agent. The non-hypnotic, vasoactive agent is highly effective in providing for the improved quality of sleep through the use of topical application.

Abstract: The invention treats proteinase-related disorders by interfering with the binding of the metal needed by matrix metalloproteinases, such as PLA-2. The compounds used are known microbial-based chelators of known high solubility. For example, dipicolinic acid has a high affinity to calcium and is soluble in both water and glycerin, as might be expected due to its role in the formation of bacterial endospores. Thus, unlike most chelation agents, the compounds are intended to be permeable enough to cross a vertebrate's cell membrane, a prerequisite for meaningful inhibition of protein-regulated cellular functions such as the inflammatory cascade and accompanying formation of free fatty acids.

Abstract: Embodiments of the invention generally provide pharmaceutical drug compositions, methods of preparing oral drug compositions, such as extended release dosage compositions, and methods for treating infection. More particularly, the invention relates to formulations containing a drug and a carrier material. In one aspect, the invention provides a pharmaceutical formulation including a therapeutically active agent, from about 0.1% to about 4.9% by weight of a pharmaceutically acceptable polymer, and from about 0.1% to about 30% by weight of a pharmaceutically acceptable acid, wherein the pharmaceutical composition have a zero order release profile of the therapeutically active agent. In another aspect, the invention provides methods for preparing and administering a pharmaceutical antibiotic composition in oral dosage form, such as a tablet.

Abstract: This invention relates to pharmaceutical combinations of amlodipine or a pharmaceutically acceptable acid addition salt thereof and statins or pharmaceutically acceptable salts thereof, kits containing such combinations and methods of using such combinations to treat subjects suffering from angina pectoris, atherosclerosis, combined hypertension and hyperlipidemia and to treat subjects presenting with symptoms of cardiac risk, including humans. This invention also relates to additive and synergistic combinations of amlodipine or a pharmaceutically acceptable acid addition salt thereof and stains or pharmaceutically acceptable salts thereof whereby those additive and synergistic combinations are useful in treating subjects suffering from angina pectoris, atherosclerosis, combined hypertension and hyperlipidemia and those subjects presenting with symptoms of cardiac risk, including humans.

Abstract: The present invention relates generally to a composition for use in the prophylaxis and/or treatment of one or more symptoms caused or exacerbated by consumption fo alcolhol which composition comprises: (1) fructose and (2) fructose-containing oligosacchraride.

Abstract: The present invention provides compounds that possess inhibitory activity against PDE-3 and L-type calcium channels. The present invention further provides pharmaceutical compositions comprising such compounds and methods of using such compounds for treating cardiovascular disease, stroke, epilepsy, ophthalmic disorder or migraine.

Abstract: L-threo-&bgr;-benzyloxyaspartate derivatives having a substituent on the benzene ring, represented by the following formula (1): 1

Abstract: The present invention provides a method of administration of an agent which acts to remodel neuronal or vascular pathways for the long term management of sexual dysfunction in both males and females. In a preferred embodiment, the invention provides a method of ameliorating or reversing pathogenic vascular degradative modeling in the ilio-hypogastric-pudendal arterial bed and genitalia comprising administering to a human patient in need of such treatment a therapeutically effective amount of an anti-pressor agent. The anti-pressor agent comprises one or more compounds selected from the therapeutic classes of direct vasodilators such as hydralazine and NO donors, ACE inhibitors, angiotensin-II receptor antagonists, &agr;1-adrenergic receptor antagonists, &bgr;-adrenergic receptor antagonists, calcium channel blockers, and phosphodiesterase inhibitors.

Abstract: The present invention relates to a method for reducing symptoms related to stroke, this therapy comprising the administration of a therapeutically effective amount of at least two compounds selected from the group of an inhibitor of microglial activation, an antiglutaminergic agent and a voltage gated calcium channel blocker to a patient suffering from a neurodegenerative disease. The present invention also relates to a composition for reducing symptoms related to stroke, comprising a therapeutically effective amount of at least two compounds selected from the group of an inhibitor of microglial activation, an antiglutaminergic agent and a voltage gated calcium channel blocker in association with a pharmaceutically acceptable carrier.

Abstract: The present invention describes novel nitrosated and/or nitrosylated potassium channel activators, and novel compositions comprising at least one nitrosated and/or nitrosylated potassium channel activator, and, optionally, at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent. The present invention also provides novel compositions comprising at least one potassium channel activator, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one vasoactive agent.

Abstract: Methods and compositions are disclosed utilizing the optically pure (−) isomer of amlodipine. This compound is a potent drug for the treatment of hypertension while avoiding the concomitant liability of adverse effects associated with the racemic mixture of amlodipine. The (−) isomer of amlodipine is also useful for the treatment of angina and such other conditions as may be related to the activity of (−) amlodipine as a calcium channel antagonist such as cerebral ischemia, cerebral disorders, arrhythmias, cardiac hypertrophy, coronary vasospasm, myocardial infarction, renal impairment and acute renal failure, without the concomitant liability of adverse effects associated with the racemic mixture of amlodipine.

Abstract: The present invention relates to compositions comprising various vitamins and minerals and methods for using these compositions for nutritional supplementation in, for example, pregnant or lactating subjects.

Abstract: A class of substituted pyridines that are useful for inhibiting the activity of cholesteryl ester transfer protein, and have the structural formula (IA), wherein R2, R3, R4, R5, and R6 are defined in the claims.

Abstract: The invention describes novel lercanidipine crude Forms (A) and (B), novel lercanidipine hydrochloride crystalline Forms (I) and (II) obtained from said crude Forms, pharmaceutical, antihypertensive compositions containing as active agent at least one of the lercanidipine hydrochloride crystalline Forms (I) and (II) and methods of use thereof

Abstract: The invention relates to methods of using Cav2.2 subunit calcium channel modulators to treat painful and non-painfull lower urinary tract disorders and the related genitourinary tract disorders vulvodynia and vulvar vestibulitis in normal and spinal cord injured patients.

Abstract: The invention relates to the use of nicotinic acid and nicotinic acid esters, such as nicotinic acid alkyl esters, to increase the amount of leptin in a subject. As a result, one can treat conditions, such as conditions characterized by wounds, by administering sufficient amounts of nicotinic acid or nicotinic acid ester to increase leptin levels to alleviating amounts. Various conditions and modes of treatment are disclosed.

Abstract: In one aspect, the present invention provides a method for modulating an Edg-2 receptor mediated biological activity in a cell. A cell expressing the Edg-2 receptor is contacted with an modulator of the Edg-2 receptor, which modulates the Edg-2 receptor mediated biological activity. In another aspect, the present invention provides a method for modulating Edg-2 receptor mediated biological activity in a subject. A therapeutically effective amount of an modulator of the Edg-2 receptor is administered to the subject.

Abstract: Provided is a method of treating thrombosis in mammals by administering therapeutically effective amounts of a combination of (i) a Factor Xa inhibitor, and (ii) a compound selected from the group consisting of aspirin, TPA, a GPIIb/IIIa antagonist, low molecular weight heparin and heparin, wherein the dose administered for at least one of (i) and (ii) is a subtherapeutic dose. Preferably, the combination of (i) and (ii) provides a synergistic effect.

Abstract: The present invention is directed to substituted nicotinamides and analogs thereof, represented by Formula V: or a pharmaceutically acceptable salt or prodrug thereof, wherein: Ar′ and Ar are independently optionally substituted aryl or optionally substituted heteroaryl, provided that the ring structure of said optionally substituted heteroaryl comprises not more than two nitrogen atoms; and R11 is hydrogen; or alkyl, cycloalkyl, aryl or heteroaryl, each of which is optionally substituted. The present invention also relates to the discovery that compounds having Formula V are activators of caspases and inducers of apoptosis. Therefore, the compounds of this invention may be used to induce cell death in a variety of clinical conditions in which uncontrolled growth and spread of abnormal cells occurs.

Abstract: An insecticide of formula 1 1

Abstract: The invention concerns a dermatological composition comprising in combination at least nicotinic acid or a nicotinic acid amide such as nicotinamide (vitamin PP), and at least a sphingoid base selected among sphingosine, sphinganine, phytosph-ingosine, tetracetylphytosphingosine, N-acetylphytosphingosine, and phytosphingosine hydrochloride. The invention is useful for treating atopic dermatitis and acne.

Abstract: The use of calcium channel blockers administered intra-nasally to inhibit olfactory sensory perception to treat eating disorders, including obesity, is described. Also described is a method of reducing food intake in a subject by administering a pharmaceutical composition comprising an effective amount of a calcium channel blocker to the nasal mucosa, as well as screening methods for drugs to be used in treating obesity or associated disorders.

Abstract: In one aspect, the present invention provides a method of inhibiting an Edg-3 receptor mediated biological activity in a cell. A cell expressing the Edg-3 receptor is contacted with an amount of an Edg-3 receptor inhibitor sufficient to inhibit the Edg-3 receptor mediated biological activity. Preferably, the inhibitor is not a phospholipid.

Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.

Abstract: The invention provides a solid composition of nisoldipine and a mixture of two polyethylene oxides having specific viscosities. The invention also provides a process for manufacturing said composition.

Abstract: Mono-acylated o-phenylendiamines derivatives of formula A 1

Abstract: Fungicidal mixtures comprising as active components a) an amide compound of the formula I A—CO—NR1R2  I  in which A is an aryl group or an aromatic or non-aromatic, 5- or 6-membered heterocycle which has from 1 to 3 hetero atoms selected from O, N and S; where the aryl group or the heterocycle may or may not have 1, 2 or 3 substituents which are selected, independently of one another, from alkyl, halogen, CHF2, CF3, alkoxy, haloalkoxy, alkylthio, alkylsulfynyl and alkylsulfonyl; R1 is a hydrogen atom; R2 is a phenyl or cycloalkyl group which may or may not have 1, 2 or 3 substituents which are selected, independently of one another, from alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, cycloalkyl, cycloalkenyl, cycloalkyloxy, cyclo-alkenyloxy, phenyl and halogen, where the aliphatic and cycloaliphatic radicals may be partially or fully halogenated and/or the cycloaliphatic radicals may be substituted by from 1 to 3 alkyl groups and where the phenyl group may have from

Abstract: The present invention relates to (i) non-peptide aspartyl protease inhibitors; (ii) methods for modulating the processing of an amyloid precursor protein (APP); (iii) methods for modulating the processing of a tau protein (&tgr;-protein); and (iv) methods for treating neurodegenerative diseases.

Abstract: The present invention provides compositions and methods for lowering plasma Lp(a) levels in humans. The present invention provides compositions and methods for lowering the risk factors for cardiovascular diseases. Moreover, this invention provides therapeutic alternatives to current pharmaceutical interventions for the lowering of cholesterol, LDL-cholesterol, triglycerides and other metabolic risk factors.

Abstract: A method of inhibiting cell proliferation in a patient suffering from such disorder comprising administering to said patient an effective amount of a composition comprising, in admixture with a pharmaceutically acceptable carrier, a compound, or a pharmaceutically acceptable salt thereof, which is a substituted styrene compound which can also be a naphthalene, an indane or a benzoxazine; including nitrile and molononitrile compounds, and pharmaceutical compositions comprising, in admixture with a pharmaceutically acceptable carrier, a pharmaceutically-effective amount of such compound.