Abstract: Compounds of formula (Ia) as potent, &bgr;1-specific beta blockers with a short duration of action in the systemic circulation, wherein R is 3′,4′-dimethoxyphenyl.

Abstract: The present invention relates to a new medical use of triphenylethylene antiestrogen toremifene or a phamaceutically acceptable thereof for lowering endothelin-1 levels in mammals, and for the prevention or treatment of endothelin mediated diseases.

Abstract: The invention encompasses methods of using racemic and enantiomerically pure norfluoxetine, as well as pharmaceutical compositions, pharmaceutical unit dosage forms, and kits comprising racemic and enantiomerically pure norfluoxetine. In particular, the invention encompasses a method of inhibiting or reducing the production of PGE2. The invention further encompasses a method of treating or preventing inflammation in a patient, as well as a method of treating or preventing a disease or disorder such as, but not limited to, autoimmune diseases, arthritis, neurologic diseases, inflammatory diseases, fibromyalgia, pain resulting from inflammation, neuropathic pain, and cancer.

Abstract: Methods of treating, preventing, and/or managing cardiovascular conditions such as hypertension, ischemic heart disease, atrial fibrillation, congestive heart failure, angina pectoris, and cardiac arrhythmias, with the (S) stereoisomer of bisoprolol are disclosed, as are compositions and formulations comprising (S)-bisoprolol.

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

Abstract: Compaction of mexiletine hydrochloride crystals is described, which provides a powder suitable for use in capsules without use of organic solvents.

Abstract: Mevinolin derivatives wherein the lactone ring is modified have interesting pharmaceutical properties, particularly in preventing or treating disorders or diseases mediated by LFA-1/ICAM-1 interactions.

Abstract: This application relates to the use of certain 3-aryloxy-3-phenylpropanamines in the treatment of chronic pain, including neuropathic pain.

Abstract: A method of chemosensitization which comprises administering at least one chemotherapeutic agent and at least one 3-aryloxy-3-phenylpropylamine to a subject in need thereof.

Abstract: The present invention relates to me methods for minimizing spasticity in blood vessels during transplantation and more particularly for minimizing spasticity in arterial transplants, for both ex-vivo and in-vivo procedures. The invention also relates to formulations, which can be used in these methods.

Abstract: This application relates to the use of certain 3-heterocyclo and 3-cycloalkyloxy-3-phenylpropanamines in the treatment of chronic pain, including neuropathic pain.

Abstract: Sympathetically maintained pain is treated topically by administering to the site where sympathetically maintained pain is present an &agr;-1-adrenergic antagonist, &agr;-2-adrenergic agonist, or other drug that depletes or blocks synthesis of sympathetic norepinephrine, known collectively as sympatholytic agents. Chemical formulas for several sympatholytic agents are given.

Abstract: A method of enhancing hair growth or treating alopecia in a subject uses topically administered estrogen receptor antagonists. Pharmaceutical formulations comprising estrogen receptor antagonists are described.

Abstract: Methods for increasing oligodendrocyte survival are disclosed. The methods of the invention are useful for the treatment of Multiple Sclerosis.

Abstract: Use of a compound of formula I 1

Abstract: Novel methods for reduction or elimination the incidence of hot flashes and menopausal symptoms, while decreasing the risk of acquiring breast or endometrial cancer and furthermore treating and/or inhibiting the development of osteoporosis, hypercholesterolemia, hyperlipidemia, atherosclerosis, hypertension, insulin resistance, diabetes, loss of muscle mass, obesity, irregular menstruation, Alzheimer's disease, or vaginal dryness in susceptible warm-blooded animals including humans involving administration of selective estrogen receptor modulator, particularly compounds having the general structure 1

Abstract: The present invention relates to pharmaceutical formulations comprising a betablocker and a cholesterol-lowering agent in admixture with a pharmaceutically acceptable adjuvant, diluent or carrier, as well as a kit of parts, a method for treatment and use of the formulations for the prophylactic or therapeutic treatment of atherosclerosis, hypercholesterolemia and hyperlipoproteinemia.

Abstract: A method for the treatment of diabetes mellitus, especially Type II diabetes and the cardiac conditions associated with diabetes mellitus in a mammal such as a human, which method comprises administering an effective non-toxic and pharmaceutically acceptable amount of an insulin sensitizer, such as Compound (I), and an agent used in the treatment of the cardiac conditions associated with diabetes mellitus.

Abstract: Disclosed is a novel enantiomeric synthesis cermamide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.

Abstract: Norepinephrine reuptake inhibitors are used to treat psoriasis.

Abstract: Disclosed is method for reducing myocardial cell damage during and/or after percutaneous coronary intervention in a subject's coronary artery. The method includes instilling a beta blocker directly into the subject's coronary artery prior to percutaneous coronary intervention. A kit for carrying out percutaneous coronary intervention is also disclosed. The kit includes a catheter and a beta blocker.

Abstract: Methods of treating stroke and conferring protection against cerebral injury in a subject following an ischemic event, wherein a tamoxifen compound is administered in an effective amount so as to confer protection on the population of cells. Treatable ischemic events include cerebrovascular disease or stroke, subarachnoid subhemorrhage, myocardial infarct, surgery and trauma.

Abstract: The present invention is directed to compounds effective for increasing the water solubility of poorly soluble drugs. Hydrotropic agents are identified, such as for increasing the solubility of paclitaxel. Polymerizable monomers of the hydrotropic agents are prepared and hydrotropic polymers formed from such monomers are generated. Both the monomers and resulting polymers increase the solubility of poorly soluble drugs. In some cases, the hydrotropic polymers are more effective at increasing solubility at low concentrations relative to a corresponding amount of the hydrotropic agent precursor. Additionally, the hydrotropic polymers (hytrops) can be crosslinked to yield hydrotropic hydrogels (hytrogels) capable of solubilizing a drug. The hytrogels can further be employed to generate micro- and nano-particle suspensions of a poorly soluble drug. The water solubility of paclitaxel can be increased by four orders of magnitude using compounds of the invention.

Abstract: Compositions comprising a pharmaceutically effective amount of a compound that impedes disruption of intact dense microspheres (DMS) by acting on DMS either to prevent disruption, or if disrupted, act on pre-disrupted DMS in such a way that, when the composition is administered to a test animal that has received an injection of DMS, it reduces the mean volume of tissue occupied by disrupted DMS, reduces the ratio of the number of inflammatory cells per DMS, or increases the ratio of the number of macrophages containing disrupted DMS per DMS, are useful for treating cerebral amyloidosis.

Abstract: This invention relates to substituted benzanilides which are ligands, agonists or 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, sarcoidosis and other fibrotic diseases, atherosclerosis, psoriasis, autoimmune diseases such as multiple sclerosis, and inflammatory bowel disease, all in mammals, by the use of substituted benzanilides which are CCR5 receptor antagonists. Furthermore, since CD8+ T cells have been implicated in COPD, CCR5 may play a role in their recruitment and therefore antagonists to CCR5 could provide potential therapeutic in the treatment of COPD. 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: The present invention relates to variant forms of human prolactin which act as antagonists at the prolactin receptor, and to the use of such variants in the treatment of human cancers and proliferative disorders, including both benign and malignant diseases of the breast and prostate.

Abstract: Provided herein is a method of method of treating an individual having a severe burn, comprising the step of administering to said individual a pharmacologically effective dose of a beta-adrenergic antagonist.

Abstract: The present invention relates to the delivery of analgesics through an inhalation route. Specifically, it relates to aerosols containing acetaminophen, orphenadrine or tramadol that are used in inhalation therapy. In a composition aspect of the present invention, the aerosol comprises particles comprising at least 5 percent by weight of acetaminophen, orphenadrine or tramadol. In a method aspect of the present invention, one of acetaminophen, orphenadrine or tramadol is delivered to a mammal through an inhalation route. The method comprises: a) heating a composition, wherein the composition comprises at least 5 percent by weight of acetaminophen, orphenadrine or tramadol, to form a vapor; and, b) allowing the vapor to cool, thereby forming a condensation aerosol comprising particles, which is inhaled by the mammal.

Abstract: The present invention relates to a method of treating asthma by raising the pH of the airways of an individual. The effect can be mediated directly by administering a pharmaceutically acceptable basic solution or alternatively, the effect can be mediated by enhancing the activity of glutaminase.

Abstract: A pharmaceutical composition, comprising: (a) a tiotropium salt (1); and (b) a salmeterol salt (2), optionally in the form of the enantiomers, mixtures of enantiomers, or in the form of the racemates thereof, optionally in the form of the solvates or hydrates and optionally together with a pharmaceutically acceptable excipient, and methods of treating respiratory diseases using such a pharmaceutical composition.

Abstract: A ligand adapted for use in a process for enantioselective reduction of unsaturated compounds carrying functional groups by a hydrogen transfer method including an optically active N-substituted chiral derivative of norephedrine and the associated process.

Abstract: The present invention provides a method for identifying a subject having a risk of developing obesity, coronary microvascular dysfunction, or hypertension, comprising detection of the presence of a single nucleotide polymorphism (SNP) in a nucleic acid encoding an element of at least one &bgr;-adrenergic receptor from the subject. The presence of the SNP is correlated with obesity, coronary microvascular dysfunction, or hypertension, and thereby identifies the subject as having a risk of developing obesity, coronary microvascular dysfunction, or hypertension. The subject invention also provides methods of identifying patients likely to benefit from the prescription of beta blocker hypertension medications. In various embodiments, the nucleic acids detected include those genes encoding ADRB1 (&bgr;1AR), ADRB2 (&bgr;2AR), ADRB3 (&bgr;3AR), GNB3 (G protein &bgr;3 subunit), or GNAS1 (GS protein alpha subunit). Methods of treating identified individuals are also provided.

Abstract: The invention discloses compositions and methods for increasing chemotherapeutic specificity to endocrine dependent cancers, and reducing systemic toxicity, through administration of endocrine hormones in conjunction with administration of phase specific chemotherapeutics. The invention also discloses why prior art phase specific chemotherapeutic regimens fail to achieve high cure rates for cancer. The failure relates to the Gompertzian acceleration, or reduction in cancer cell cycle time, induced by the chemotherapeutic reduction of tumor size, which in turn results in the cancer's lack of phase synchronicity to subsequent administrations of the phase specific chemotherapeutic(s).

Abstract: One aspect of the invention relates to anti-viral composition containing at least one zinc compound and at least one phenolic antioxidant (and optionally other ingredients such as at least one analgesic) at least one hydrocarbyl containing compound, and water. Another aspect of the invention relates to a method of treating lesionous symptoms of a viral infection involving applying an effective amount of the zinc containing anti-viral composition to the lesions.

Abstract: Estrogen receptor modulators, compositions comprising the compounds and methods relating to the use thereof are described. The compounds may be used in inhibiting the proliferation of and/or induces apoptosis in human breast cancer cells.

Abstract: The present invention describes novel nitrosated and/or nitrosylated &agr;-adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and/or nitrosylated &agr;-adrenergic receptor antagonist, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are a substrate for nitric oxide synthase, and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one &agr;-adrenergic receptor antagonist, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents.

Abstract: Methods for the simple, reliable application and local controlled release of selected anti-arrhythmia drugs from a hydrogel applied to or polymerized on the tissues of the heart or its vessels, especially in conjunction with cardiac bypass or other cardiac surgery, have been developed. The anti-arrhythmia drugs are incorporated into hydrogels that biodegrade and adhere to the tissues to which the anti-arrhythmic drugs are to be delivered. The hydrogels may be formed in vitro or in vivo. In a preferred embodiment, the drugs are effective to lengthen atrial effective refractory period. A particularly preferred drug is amiodarone.

Abstract: Pharmaceutical compositions which comprises R(−) fluoxetine and one or more other biologically active compounds are disclosed. Methods of treating or preventing a disease or disorder, especially a psychotic or psychiatric disease or disorder, using the above pharmaceutical composition or by administering a R(−) fluoxetine in combination with one or more other biologically active compounds are also disclosed. Methods of treating patients having or at risk of having AIDS or HIV infection, cancer, cardiac disorder, post-myocardial depression and posttraumatic stress disorder using optically pure R(−) fluoxetine in combination with one or more other biologically active compounds are further disclosed.

Abstract: Novel methods for the medical treatment and/or inhibition of the development of osteoporosis, breast cancer, hypercholesterolemia, hyperlipidemia or atherosclerosis in susceptible warm-blooded animals including humans involving administration of selective estrogen receptor modulator particularly compounds having the general structure: and an amount of a sex steroid precursor selected from the group consisting of dehydroepiandrosterone, dehydroepiandrosterone sulfate, androst-5-ene-3&bgr;,17&bgr;-diol and compounds converted in vivo to one of the foregoing presursor. Further administration of bisphosphonates in combination with selective estrogen receptor modulators and/or sex steroid precursor is disclosed for the medical treatment and/or inhibition of the development of osteoporosis. Pharmaceutical compositions for delivery of active ingredient(s) and kit(s) useful to the invention are also disclosed.

Abstract: Molecules demonstrating anti-proliferative effects against epithelial cancer cell lines, human estrogen-dependent cancer cells and endothelial cells are disclosed. The molecules are intended for use in therapeutic preparations for the treatment of various cancers. The compounds specified are 1,2-diphenyl-1-naphthyl ethene derivatives.

Abstract: The present invention relates to the use of deprenyl compounds to rescue damaged nerve cells in a patient and to kits containing deprenyl compounds useful for rescuing damaged nerve cells in a patient.

Abstract: A method of treating sexual disorders in a mammal by administering to the mammal an effective amount of 1,7,7-trimethylbicyclo[2.2.

Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 1-benzyl-naphthyls which are &agr;-substituted with ether, thioether, amino, hydrazino, cyano or halo that are useful for the treatment of the various medical indications associated with post-menopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus and cervix. The present invention further relates to intermediate compounds and processes useful for preparing the pharmaceutically active compounds of the present invention, and pharmaceutical compositions.

Abstract: The present invention is directed to a novel topical pharmaceutical water-in-oil composition in form of a cream or lotion, comprising

Abstract: A combination therapy comprising a therapeutically-effective amount of an epoxy-steroidal aldosterone receptor antagonist and a therapeutically-effective amount of a beta-adrenergic antagonist is described for treatment of circulatory disorders, including cardiovascular disorders such as hypertension, congestive heart failure, cirrhosis and ascites. Preferred beta-adrenergic antagonists are those compounds having high potency and bioavailability. Preferred epoxy-steroidal aldosterone receptor antagonists are 20-spiroxane steroidal compounds characterized by the presence of a 9&agr;,11&agr;-substituted epoxy moiety. A preferred combination therapy includes the beta-adrenergic antagonist metoprolol ((±)1-(isopropylamino)-3-[p-(2-methoxyethyl)phenoxyl]-2-propanolol succinate) and the aldosterone receptor antagonist epoxymexrenone.

Abstract: The present invention relates to a method of treating depression, obsessive compulsive disorder and psychosis in a mammal, including a human, by administering to the mammal an atypical antipsychotic in combination with an antidepressant agent with improvement in efficiency. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, an atypical antipsychotic, and an SRI.

Abstract: The present invention provides methods which increase the effectiveness of combination drug therapies for treating estrogen-sensitive diseases, such as breast cancer, as well as novel combinations useful to treat such diseases.

Abstract: The administration of antiestrogens to men suffering a relative androgen deficiency stimulates the body's production of testosterone leading to a correction of the deficiency. For example, male menopause, loss of cognitive function, insulin resistance, type 2 diabetes, obesity, excessive weight, Alzheimer's disease, and combinations thereof, can all be characterized by significant decreases in serum levels of bioavailable androgens. Administration of antiestrogens to men restores optimum serum levels of bioavailable androgens, and, thus, serves as a treatment for these disorders and relative androgen deficiency in general.

Abstract: The present patent application relates to new substituted 3-phenoxy- or 3-phenylalkyloxy-2-phenyl-propylamines of general formula 1, processes for preparing them and their use as pharmaceutical compositions.

Abstract: Methods are disclosed for increasing the effectiveness of dextromethorphan in treating chronic or intractable pain, for treating tinnitus and for treating sexual dysfunction comprising administering dextromethorphan in combination with a therapeutically effective dosage of a debrisoquin hydroxylase inhibitor. A preferred combination is dextromethorphan and the oxidative inhibitor quinidine.