Abstract: Disclosed is use of nonsteroidal anti-estrogen compounds such as toremifene citrate as active ingredient for treating autoimmune diseases.

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: The compounds of this invention comprise 2-10 ligands covalently connected, each of the ligands being capable of binding to a ligand binding site in a Na+ channel, thereby modulating the biological activities thereof.

Abstract: The invention provides a method of treating a mammal having, or at risk of, an indication associated with a TGF-beta deficiency comprising administering one or more agents that is effective to elevate the level of TGF-beta. The invention also provides novel compounds that elevate TGF-beta levels, as well as pharmaceutical compositions comprising compounds that elevate TGF-beta levels, and methods for detecting diseases associated with endothelial cell activation.

Abstract: A method for treating or preventing cardiovascular pathologies by administering a compound of the formula (I): 1

Abstract: A pharmaceutical product comprising an SSRI and a non-sedating anxiolytic compound, which is a modulator of the benzodiazepine binding site of the human GABAA receptor, having a binding affinity for the &agr;3 subunit of the human GABAA receptor of 10 nM or less, which elicits at least a 40% potentiation of the GABA EC20 response in stably transfected recombinant cell lines expressing the &agr;3 subunit of &agr;3 and which elicits at most a 30% potentiation of the GABA EC20 response in stably transfected cell lines expressing the &agr;1 subunit of the human GABAA receptor is disclosed for simultaneous, separate or sequential administration.

Abstract: The present invention provides methods for the modulation of vascular tone in a patient having compromised vascular tissue, which methods comprise the administration of a chloride channel blocking agent or a pharmaceutically acceptable salt thereof.

Abstract: The present invention provides a compound of formula I wherein R1 is H, OH, halo, OCO(C1-C6 alkyl), OCO(aryl), OSO2(C4-C6 alkyl), OCOO(C1-C6 alkyl), OCOO(aryl), OCONH(C1-C6 alkyl), or OCON(C1-C6 alkyl)2; R2 is aryl, C1-C6 alkyl, C3-C6 cycloalkyl, or 4-cyclohexanol; R3 is O(CH2)2 or O(CH2)3; R4 and R5 are optionally CO(CH2)2CH3, CO(CH2)3CH3, C1-C6 alkyl, or R4 and R5 combine to form, with the nitrogen to which they are attached, piperidine, morpholine, pyrrolidine, 3-methylpyrrolidine, 3,3-dimethylpyrrolidine, 3,4-dimethylpyrrolidine, azepine, or pipecoline; and pharmaceutically acceptable salts thereof. The invention further provides pharmaceutical compositions containing compounds of formula I and methods of use for the compounds of formula I.

Abstract: Male menopause is characterized by significant decreases in serum levels of bioavailable androgens. The administration of antiestrogens to men experiencing male menopause can remedy the relative androgen deficiency in men by stimulating the body's production of testosterone.

Abstract: Disclosed is use of nonsteroidal anti-estrogen compounds such as toremifene citrate as active ingredient for treating autoimmune diseases.

Abstract: A method of treating an obsessive-compulsive spectrum disorder comprises the step of administering an effective amount of tramadol to an individual.

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, 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: Inhibitors of the cytosolic phospholypase A2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases.

Abstract: The present invention relates to methods and compositions comprising a very low dose of cyclobenzaprine or metabolite thereof for preventing and treating Generalized Anxiety Disorder. The present invention further relates to methods and compositions for treating and preventing symptoms associated with Generalized Anxiety Disorder using a very low dose of cyclobenzaprine.

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: The present invention relates to novel 3-alkoxybenzylamine derivatives of general formula (1): which are useful as medicinal products and in particular as antipsychotic agents.

Abstract: The present invention is concerned with the stereoisomeric forms of itraconazole (X=Cl) and saperconazole (X=F), which may be represented by the formula and the pharmaceutically acceptable acid addition salt forms thereof, processes for preparing said stereoisomeric forms, the complexes thereof with cyclodextrin derivatives, pharmaceutical compositions comprising said complexes and methods of preparing said complexes and pharmaceutical compositions.

Abstract: A composition comprising:

Abstract: Compositions for inhibiting nematocyst or polar capsule discharge are provided in the form of an effective amount of antihistamine, an effective amount of antihistamine and an effective amount of at least one cation, or an effective amount of at least one cation. The compositions can be in the form of ointments or can be added to the environment surrounding the nematocysts or polar capsules. Methods of inhibiting nematocyst or polar capsule discharge using the compositions of the invention are also provided.

Abstract: An aryloxyaniline derivative represented by the formula: wherein Ar1 and Ar2 are each a substituted or unsubstituted phenyl group, pyridyl group or naphthyl group, R1 is a hydrogen atom, an alkyl group, etc., X1 is a hydrogen atom, an alkyl group, etc., y1 is a branched or unbranched alkylene group having 1 to 6 carbon atoms or a single bond; or a pharmaceutically acceptable salt thereof can provide medicines having a high affinity for MDR, and therefore, exhibiting a therapeutic or preventive effect on anxiety, related diseases thereto, depression, etc.

Abstract: A method for the treatment of disorders relating to serotonergic system in humans, for example depression and anxiety, comprising orally administering deramciclane in a daily dosage of about 20 to about 60 mg.

Abstract: Identification of MYC target genes whose expression is either induced or repressed by c-myc induction in human fibroblasts is disclosed. Also disclosed are methods of inducing or repressing expression of MYC target genes.

Abstract: The present invention is a composition for preventing, minimizing, or reversing the development or growth of breast cancer. The composition contains a combination of a selective estrogen receptor modulator selected from at least one of raloxifene, droloxifene, toremifene, 4′-iodotamoxifen, and idoxifene and at least one isoflavone selected from genistein, daidzein, biochanin A, formononetin, and their respective naturally occurring glucosides and glucoside conjugates. The present invention also provides a method of preventing, minimizing, or reversing the development or growth of breast cancer in which a selective estrogen receptor modulator selected from at least one of raloxifene, droloxifene, toremifene, 4′-iodotamoxifen, and idoxifene is co-administered with at least one isoflavone selected from genistein, daidzein, biochanin A, formononetin, and their naturally occuring glucosides and glucoside conjugates to a woman having or predisposed to having breast cancer.

Abstract: The present invention relates to novel polymorphic Form A of fluoxetine hydrochloride.

Abstract: There is provided compounds of formula I, wherein R1 represents C3-5 alkyl; and R2 and R3 independently represent C1-3 alkyl; provided that when R2 and R3 both represent ethyl, then R1 does not represent n-butyl, i-butyl or n-pentyl; or a pharmaceutically acceptable salt thereof, which are useful as anaesthetics, in particular local anaesthetics and especially topically applied local anaesthetics.

Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule in an amount sufficient to control the aberrant growth state, e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. The present invention further makes available methods and reagents for ameliorating the consequences of hedgehog loss-of-function, ptc gain-of-function, or smoothened loss-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule, in an amount sufficient to ameliorate the In certain embodiments, the subject compounds, e.g., a cAMP analog, adenylate cyclase agonist, or cAMP phosphodiesterase inhibitor, regulate cAMP levels, which in turn modulates activity of the hedgehog pathway.

Abstract: The present invention is concerned with the identification of compounds which increase the therapeutic index of chemotherapy drugs and which stimulate the growth of cancers, their use in the treatment of cancer and with certain novel compounds useful in such treatment.

Abstract: The optically pure R(−) isomer of salmeterol, which is substantially free of the S(+) isomer, is a potent bronchodilator for relieving the symptoms associated with asthma in individuals. A method is disclosed utilizing the optically pure R(−) isomer of salmeterol for treating asthma while minimizing toxicity and other side effects associated with salmeterol.

Abstract: This invention provides the chemoprevention of prostate cancer and, more particularly, to a method of administering to a subject an effective dose of a chemopreventive agent, toremifene and analogs or metabolites thereof, to prevent recurrence of, suppress or inhibit prostate carcinogenesis. The present invention provides a safe and effective method for suppressing or inhibiting latent prostate cancer and is particularly useful for treating subjects having an elevated risk of developing prostate cancer, for example, those having benign prostatic hyperplasia, prostate intraepithelial neoplasia (PIN), or an abnormally high level of circulating prostate specific antibody (PSA), or who have a family history of prostate cancer.

Abstract: Treatments in which a progestational corticoid active compound is administered are improved by additionally administering a selective estrogen receptor modulator.

Abstract: The present invention relates to novel pharmaceutical formulations and methods of using Form A of fluoxetine hydrochloride.

Abstract: A method for treating or preventing cardiovascular pathologies by administering a compound of the formula (I): wherein Z is C═O or a covalent bond; Y is H or O(C1-C4)alkyl, R1 and R2 are individually (C1-C4)alkyl or together with N are a saturated heterocyclic group, R3 is ethyl or chloroethyl, R4 is H or together with R3 is —CH2—CH2— or —S—, R5 is I, O(C1-C4)alkyl or H and R6 is I, O(C1-C4)alkyl or H with the proviso that when R4, R5, and R6 are H, R3 is not ethyl; or a pharmaceutically acceptable salt thereof, effective to activate or stimulate production of TGF-beta to treat and/or prevent conditions such as atherosclerosis, thrombosis, myocardial infarction, and stroke is provided. Useful compounds include idoxifene and salts thereof. Further provided is a method for identifying a compound that is a TGF-beta activator or production stimulator is provided. Another embodiment of the invention is an assay or kit to determine TGF-beta in vitro.

Abstract: The present invention relates to a novel monophosphate salt of isopropyl-methyl-[2-(3-n-propoxyphenoxy)ethyl]amine. Moreover, the present invention also relates to a process for the preparation of the monophosphate salt of isopropyl-methyl-[2-(3-n-propoxyphenoxy)ethyl]amine as well as a pharmaceutical formulation containing it and its use in medicine.

Abstract: Compounds of formula (I) wherein R, R′, R″, R1, R2, R3, R4, R5, R6, X, Y, m, n, and p have the meanings reported in the description; and their pharmaceutically acceptable salts are described.

Abstract: Patients can be helped to break free of addictive or habit-forming narcotics and anti-depressants, by treatment using two drugs. One drug is dextromethorphan (DM), which has been used for decades as an anti-tussive (cough-suppressing) drug in cough syrups. The other drug is an oxidase inhibitor which suppresses activity of a liver enzyme called cytochrome P450-2D6 (also called debrisoquin hydroxylase, sparteine monooxygenase, cytochrome P450-DB, and CYP2D6). In most patients, this oxidase enzyme rapidly degrades DM and converts it into a metabolite called dextrorphan. An oxidase inhibitor (such as quinidine) which suppresses cytochrome P450-2D6 activity increases the half-life and concentration of DM in the circulating blood. When this combined treatment was administered orally to patients who had become dependent on morphine and anti-depressant drugs because of chronic intractable pain, it initially helped the patients reduce their dosages of morphine and other drugs, including anti-depressants.

Abstract: A new use of halogenated triphenylethylene derivatives for lowering levels of serum lipid peroxides and for the prevention or treatment of oxidative tissue damage induced by lipid peroxidation is disclosed. The new use includes the prevention or treatment of artherosclerosis, ischemic injury, psoriasis, inflammatory diseases, such as inflammatory bowel disease, or cardiovascular disorders, such as coronary heart disease, cardiac ischemic injury and post-ischemic cardiac arrhythmias, or the treatment of AIDS.

Abstract: A method for treating or preventing cardiovascular pathologies by administering a compound of the formula (I): wherein Z is C═O or a covalent bond; Y is H or O(C1-C4)alkyl, R1 and R2 are individually (C1-C4)alkyl or together with N are a saturated heterocyclic group, R3 is ethyl or chloroethyl, R4 is H, R5 is I, O(C1-C4)alkyl or H and R6 is I, O(C1-C4)alkyl or H with the proviso that when R4, R5, and R6 are H, R3 is not ethyl; or a pharmaceutically acceptable salt thereof, effective to elevate the level of TGF-beta to treat and/or prevent conditions such as atherosclerosis, thrombosis, myocardial infarction, and stroke is provided. Useful compounds include idoxifene, toremifene or salts thereof. Further provided is a method for identifying an agent that elevates the level of TGF-beta. Another embodiment of the invention is an assay or kit to determine TGF-beta in vitro.

Abstract: It has been found that the treatment of depression using known serotonin reuptake inhibitors (SRIs) and noradrenaline reuptake inhibitors (NRIs) may be improved by the administration therewith of folic acid or a precursor which produces folate in the patient. The daily dose of NRI or SRI is as prescribed for treatment of depression in the usual way. The daily dose of the folic acid or precursor should be such as to provide a folate dosage of 300-5000 micrograms/day.

Abstract: Disclosed is use of nonsteroidal anti-estrogen compounds such as toremifene citrate as active ingredient for treating autoimmune diseases.

Abstract: Norepinephrine reuptake inhibitors are used to treat conduct disorder.

Abstract: The power of citalopram, fluvoxamine and paroxetine to increase the availability of sarotonin, norepinephrine and dopamine, particularly serotonin, is augmented by administration in combination with a drug which is a serotonin 1A receptor antagonist.

Abstract: TGF-beta activators and TGF-beta production stimulators are employed to maintain or increase vessel lumen diameter in a diseased or injured vessel of a mammal. Conditions such as restenosis following angioplasty, vascular bypass grafts, transplanted organs, atherosclerosis or hypertension are characterized by a reduced vessel lumen diameter. In a preferred embodiment of the invention, TGF-beta activators and production stimulators inhibit abnormal proliferation of smooth muscle cells. TGF-beta activators or production stimulators that are not characterized by an undesirable systemic toxicity profile at a prophylactic dose are also amenable to chronic use for prophylactic purposes with respect to disease states involving proliferation and/or migration of vascular smooth muscle cells over time.

Abstract: The present invention provides novel assay methods for identifying compounds that may have both estrogen agonist and antagonist properties. In particular, the assay use cells comprising promoters having an AP1 site linked to a reporter gene. Compounds capable of inducing or blocking expression of the reporter gene can thus be identified. The compounds may be further tested for the ability to modulate the standard estrogen response, as well.

Abstract: The invention relates to a method of treating psychosis, acute mania, mild anxiety states or depression in combination with psychotic episodes by administering to a patient a combination of an atypical antipsychotic and a serotonin reuptake inhibitor.

Abstract: Compositions for inhibiting nematocyst or polar capsule discharge are provided in the form of an effective amount of antihistamine or an effective amount of antihistamine and an effective amount of at least one cation. The compositions can be in the form of ointments or can be added to the environment surrounding the nematocysts or polar capsules. Methods of inhibiting nematocyst or polar capsule discharge using the compositions of the invention are also provided.

Abstract: Found is a pharmaceutical preparation which provides Tamoxifen Citrate in a liquid dosage form, viz. as an oral solution. The finding is based on a solvent comprising the following components: (a) of from 10% to 20% by weight of ethanol, (b) of from 10% to 60% by weight of a glycol; and (c) water, optionally containing additives, in a volume percentage adding up to 100% by volume. A preferred additive is sorbitol.

Abstract: A method of treating atherosclerosis, independent of lipid lowering, in mammals, including humans, in need of treatment by inhibiting progression of an atherogenic lesion or by stabilizing plaque. Such lesion progression inhibition or plaque stabilization is preferably achieved by directly inhibiting chemokine expression leading to excessive inflammatory cell recruitment by administering certain estrogen agonist/antagonists.

Abstract: Method and composition for treating painful conditions of the anorectal region. The compositions include a combination of an .alpha.-adrenergic blocker and sucralfate, a combination of .alpha.-adrenergic blocker and lidocaine, and a combination of an .alpha.-adrenergic blocker, lidocaine, and sucralfate. Alternatively, the composition may contain only an .alpha.-adrenergic blocker. Additional active ingredients for reduction of anal pain may be added to the composition, particularly capsaicin. The compositions may be included in a petrolatum base along with a water soluble lubricant. These compositions have been found effective in treating painful conditions in the anal region, such as anal fissures, inflamed or recently thrombosed hemorrhoids, and chronic anal pain.

Abstract: The present invention provides novel compositions and methods relating to the treatment of Inflammatory Bowel Disease ("IBD"), most notably, Ulcerative Colitis, Crohn's Disease, Colitis and Diverticulitis. The invention relates to the discovery of a parasitic microsporidia infecting the epithelium cells lining the gastrointestinal tract of patients suffering from IBD. The discovery of this correlation between the disease and the microsporidia, described herein, led to the development of methods for the accurate diagnosis of patients suffering from IBD, and also of methods for treating such a patient in accordance with the invention. This discovery also provides for the development of animal models to further elucidate the mechanism of the disease and potential additional cures therefor.

Abstract: Proliferation of breast cancer is treated by a combined type I interferon/non-steroidal antiestrogen therapy. Preferably antiestrogen treatment is sequential to treatment with interferon.