Abstract: This invention encompasses novel methods of preparing sibutramine and sibutramine derivatives, and stereomerically pure sibutramine derivatives in particular. Examples of sibutramine derivatives include, but are not limited to, sibutramine metabolites such as desmethylsibutramine and didesmethylsibutramine. The invention further encompasses novel compounds useful in the synthesis of sibutramine derivatives.

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: This invention provides a method of treating obesity, generalized anxiety disorder, post-traumatic stress disorder, late luteal phase dysphoric disorder (premenstrual syndrome), attention deficit disorder, with and without hyperactivity, Gilles de la Tourette syndrome, bulimia nervosa or Shy Drager Syndrome in a mammal by administering to the mammal an effective amount of a hydroxycycloalkanephenethyl amine of the following structural formula: in which A is a moiety of the formula where the dotted line represents optional unsaturation; R1 is hydrogen or alkyl; R2 is alkyl; R4 is hydrogen, alkyl, formyl, or alkanol; R5 and R6 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, cyano, nitro, alkylmercapto, amino, alkylamino, dialkylamino, alkanamido, halo, trifluoromethyl, or taken together, methylene dioxy; R7 is hydrogen or alkyl; and n is 0, 1, 2, 3, or 4; or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to derivatives of hydroxyphenyl, a method for preparing thereof and their pharmaceutical composition, more particularly the compounds of the present invention specifically inhibit the activation of T lymphocyte by src homology region 2(SH2) domain of T lymphocyte (lck), so that they can be used for the treatment, prevention and/or diagnosis of graft rejection, autoimmune diseases, inflammatory diseases, etc.

Abstract: Compound having Formula 1: 1

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 toward particles for delivery of epinephrine to the respiratory system and methods for treating a patient in need of epinephrine. The particles and respirable compositions comprising the particles of the present invention described herein comprise the bioactive agent epinephrine, or a salt thereof, as a therapeutic agent. The particles are preferably formed by spray drying. Preferably, the particles and the respirable compositions are substantially dry and are substantially free of propellents. In a preferred embodiment, the particles have aerodynamic characteristics that permit targeted delivery of epinephrine to the site(s) of action.

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-benzyl-N-phenyl aminoalcohols.

Abstract: This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.

Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1 )-Alkanol compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral N-benzyl-N-phenyl aminoalcohols.

Abstract: Methods of treating and managing cancer are disclosed, which comprise the administration of an antihistaminic agents or structurally/functionally related to compound, optionally in combination with one or more additional anti-cancer agents. Pharmaceutical compositions, including single unit dosage forms, and kits useful in the treatment and management of cancer are disclosed. Also disclosed is a method of determining effectiveness of a cancer treatment.

Abstract: This invention concerns the use of cyclopamine, a naturally occurring steroidal alkaloid known for over thirty years, for the treatment of psoriasis and achievement of rapid clearance of the psoriatic skin lesions together with the reversion of the histopathological signs of disease to normalcy with no detectable side effects. The cyclopamine-induced clearance of psoriatic lesions from the skin of patients is associated with the causation of cellular differentiation in lesional epidermis and with the rapid disappearance of CD4(+) lymphocytes and other inflammatory cells from lesional skin. Therapeutic compositions comprising of cyclopamine and a corticosteroid and/or the pre-treatment of lesions with a corticosteroid provide significantly further increased therapeutic effectiveness over the use of cyclopamine alone or a corticosteroid alone.

Abstract: Pharmaceutical tablets containing crystalline paroxetine hydrochloride anhydrate are prepared using a process comprising an initial wet granulation process in which an aqueous granulation liquid is added to a mixture of said anhydrate an excipients under high-shear conditions and the thus obtained wet granules are dried using a fluidized bed technique to obtain a water activity within a specified range, after which the dried granules after addition of further adjuvants are compressed into stable tablets each having an identical composition.

Abstract: The present invention is drawn to a pharmaceutical compound for the treatment of posterior retinal diseases through topical application of the compound. The compound includes an effective amount of a therapeutic compound, and at least one additional agent that helps to prolong the residence time of the therapeutic compound within the extraocular space, or increase the transport of the therapeutic compound across a tissue of an eye toward and into a posterior ocular region, or both. The invention is additionally drawn to a device and method for delivering the compound.

Abstract: Paroxetine salt compositions having improved stability are formed by controlling the pH to 6.5 or less. The compositions can be made with the aide of water without significant coloration problems. The paroxetine salts include paroxetine hydrochloride salts but preferably use paroxetine sulfonate salts such as paroxetine methane sulfonate.

Abstract: Methods are disclosed for the treatment and prevention of disorders and conditions such as, but are not limited to: eating disorders; weight gain; obesity; irritable bowel syndrome; obsessive-compulsive disorders; platelet adhesion; apnea; affective disorders such as attention deficit disorders, depression, and anxiety; male and female sexual function disorders; restless leg syndrome; osteoarthritis; substance abuse including nicotine and cocaine addiction; narcolepsy; pain such as neuropathic pain, diabetic neuropathy, and chronic pain; migraines; cerebral function disorders; chronic disorders such as premenstrual syndrome; and incontinence.

Abstract: The subject invention provides methods for the treatment of ASD and/or PTSD comprising the administration of a dose of an SSRI taken soon after a trauma (for example, less than 48 hours and before the onset of ASD.

Abstract: The invention relates to the use of compounds that enhance 5-hydroxytryptamine 1a receptor activity, or activation (e.g. a selective 5-hydroxytryptamine 1a receptor agonists) for preventing or reducing motor fluctuations associated with dopamine replacement therapy.

Abstract: Embodiments of the invention relate to C2-substituted indan-1-ols and to their physiologically acceptable salts and physiologically functional derivatives.

Abstract: This invention relates to a novel amorphous form of sertraline hydrochloride and a process for the preparation thereof.

Abstract: Methods of reversing local anesthesia are disclosed. The methods comprise administering a local anesthetic and alpha adrenergic receptor agonist to induce local anesthesia followed by reversing anesthesia with a low dose of an alpha adrenergic receptor antagonist. Also disclosed are kits comprising a local anesthetic, an alpha adrenergic receptor agonist and a low dose of an alpha adrenergic receptor antagonist.

Abstract: The invention relates to the use of 1-phenyl-1,2-diaminoethane derivatives of formula (I) 1

Abstract: The present invention relates to the use of compounds of the general Formula (I): 1

Abstract: A pharmaceutical composition comprises a once-a-day sustained release formulation of at least one amphetamine salt which provides mean plasma concentration profile aspects in human ADHD patients which are substantially the same as that provided by ADDERALL XR® type pulsatile formulations.

Abstract: Novel polyamines, their synthesis and use in pharmacological, cosmetic or agricultural applications are provided. The polyamines induce antizyme production which in turn down regulates both the production of polyamines by ornithine decarboxylase (ODC) and the transport of polyamines by its corresponding polyamine transporter. These compounds will preferably enter the cell independent of the polyamine transporter. As drugs, these compounds are used to treat any disease associated with cellular proliferation including but not limited to cancer.

Abstract: Neuroprotectant agents are provided which do not contain peptides and are protected from the degradation that limits the use of peptide-based drugs in systemic circulation. With great selectivity for NMDA receptors, the agents exert an open channel block on NMDA receptors, and protect neuronal cells containing such receptors from excitotoxic cell death.

Abstract: The present invention relates to novel compounds that are useful for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. This invention also relates to pharmaceutical formulations comprising these compounds and methods of using them for inhibition and prevention of cell adhesion and cell adhesion-mediated pathologies. The compounds and pharmaceutical compositions of this invention can be used as therapeutic or prophylactic agents. They are particularly well-suited for treatment of many inflammatory and autoimmune diseases.

Abstract: One aspect of the present invention relates to amines. A second aspect of the present invention relates to the use of the amines as inhibitors of a mammalian anandamide transporter. The compounds of the present invention will also find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to asthma, neuropathic pain, persistent pain, inflammatory pain, hyperactivity, hypertension, brain ischemia, Parkinson's disease, spasticity, Tourette's syndrome, schizophrenia, hemorrhagic shock, septic shock, cardiac shock, migrane, Horton's headache, multiple sclerosis, anorexia, AIDS wasting syndrome, organ rejection, autoimmune diseases, allergy, arthritis, Crohn's disease, malignant gliomas, neurodegenerative diseases, Huntington's chorea, glaucoma, nausea, anxiety, psychosis, attention deficit hyperactivity disorder, premature ejaculation, and stroke.

Abstract: The present invention provides a cytokine production inhibitor containing as an active ingredient an aniline derivative of the formula (I) or a salt thereof: 1

Abstract: A compound of the formula 1

Abstract: The invention relates to substituted 1 and 2 naphthol Mannich bases, a method for the production thereof, medicaments containing said compounds and the use of said compounds in the production of medicaments.

Abstract: There is provided a method and composition for treating urinary stress incontinence based upon the topical administration of an alpha-adrenoceptor agonist, such as phenylephrine. A daily dosage of 20 mg to 2000 mg is suitable, and the composition may conveniently be applied as a cream or gel to the vaginal or peri-urethral area.

Abstract: A pharmaceutical composition which reduces or eliminates the drug abuse potential of central nervous system stimulant comprising: (a) a drug selected from the group consisting of methylphenidate, amphetamine, methamphetamine, and combinations thereof; and (b) a gel forming polymer wherein the gel forming polymer is a polymer that forms a gel when contacted with moisture or placed in an aqueous solution. The present invention is based on the discovery that a central nervous system stimulant, such as methylphenidate in combination with a gel forming polymer reduces or eliminates drug abuse potential by swelling in the presence of moisture, and thus, preventing nasal absorption and injectability of the drug.

Abstract: The present invention encompasses methods of treating patients for tobacco addiction and nicotine addiction, for palliating the effects of nicotine withdrawal, for providing or facilitating the effects of smoking cessation therapies and as long-term smoking cessation maintenance therapy. The invention also includes related pharmaceutical compositions comprising nicotine receptor antagonists and either an anti-depressant or an anti-anxiety drug. Specific combinations of drugs (mecamylamine HCl and bupropion HCl) as well as mecamylamine in combination with certain drug classes (e.g., anti-anxiety drugs and anti-depressants) comprise the pharmaceutical compositions disclosed. These compositions are also contemplated for use in the treatment of cocaine addiction and the treatment of alcohol dependence.

Abstract: The present invention features compounds active at both the serotonin reuptake site and the N-methyl-D-aspartate (NMDA) receptor and the use of such compounds for treating different disorders. Compounds having activity at the serotonin reuptake site and the NMDA receptor (“multi-active compounds”) can be used to treat different types of disorders such as depression, obsessive-compulsive disorders (OCD), sleep, disorders, sexual dysfunction, and eating disorders. Preferably, the multi-active compounds are used to treat depression.

Abstract: The present invention is directed to gel compositions useful in the preparation of medicated gel products. Such medicated gel products are suitable for use in the treatment of anorectal disorders such as hemorrhoids. Also disclosed is a method for the treatment of such anorectal disorders using the claimed medicated gel products.

Abstract: Pharmaceutical formulations that include a combination of salmeterol and budesonide and the use of such formulations in medicine, particularly in the prophylaxis and treatment of respiratory diseases, are described.

Abstract: The present invention provides non-hygroscopic, crystalline salts of levodopa ethyl ester (LDEE), wherein the salt is the octanoate salt, the myristate salt, the succinate salt, the succinate dihydrate salt, the fumarate salt or the fumarate dihydrate salt of levodopa ethyl ester. The subject invention also encompasses compositions comprising a levodopa ethyl ester salt and a carrier and processes for making these compositions. In addition, the subject invention concerns pharmaceutical compositions comprising a levodopa ethyl ester salt and a pharmaceutically acceptable carrier, as well as processes for making these pharmaceutical compositions.

Abstract: The invention concerns novel cdc25 phosphatase inhibitors, and in particular cdc25-C, which correspond to the general formula (I) wherein: A represents a carbocyclic aryl radical optionally substituted 1 to 3 times by one or more radicals independently selected among a halogen atom and an alkyl, hydroxy, alkoxy, alkylthio or NR1R2 radical wherein R1 and R2 represent a hydrogen atom or an alkyl radical or R1 and R2 form together with the nitrogen atom a heterocycle of 4 to 7 members comprising 1 to 2 heteroatoms, the members required to complete the heterocycle being selected independently among the CR3R4—, —O—, —S and NR5-radicals, R3 and R4 representing independently each time they are involved a hydrogen atom or an alkyl, hydroxy, alkoxy, amino, alkylamino or dialkylamino radical, and R5 representing independently each time it is involved a hydrogen atom or an alkyl radical, or A represents a phenyl radical substituted by a phenyl radical optionally substituted 1 to 3 times by one or

Abstract: The invention relates to the use of 1-phenyl-3-dimethylaminopropane compounds for treating increased urinary urgency or urinary incontinence, as well as to the production of corresponding medicaments.

Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.

Abstract: The c-Myc oncoprotein, a helix-loop-helix-leucine zipper (HLH-ZIP) transcription factor, is frequently deregulated in human cancers. All known functions of c-Myc, including those pertaining to transformation, require that it heterodimerize with another HLH-ZIP protein, Max. Using a high throughput yeast-based assay, we identified seven low molecular weight substances that inhibit c-Myc-Max association. Each compound also prevented this interaction in vitro and inhibited the growth of c-Myc-expressing fibroblasts, although not of fibroblasts lacking c-Myc. Finally, short-term exposure of c-Myc over expressing fibroblasts to several of the compounds markedly reduced their in vivo tumorigenicity. These studies suggest that yeast-based assays can be used to identify inhibitors of protein-protein interactions and that these frequently function in mammalian cells. The signature specificities of each of the c-Myc-Max compounds identified here further suggest synergistic in vivo function.

Abstract: 2,2-Diphenylbutanamide derivatives represented by the following formula (1): 1

Abstract: A process for preparing methane diphenyl diamine (MDA) or a mixture of methane diphenyl diamine (MDA) and its higher homologues with a controlled isomer distribution using a silanised zeolite have “shape selectivity”. The mixture contains compounds having the following general formula (I): where R represents a hydrogen atom or a C1 to C8 (iso) alkyl group, a C4 to C10 cycloalkyl group or a C6 to C12 aromatic group and n is a whole number greater than or equal to one so as to give a functionally of 2 to 6.

Abstract: The present invention relates to a method of treating depression or anxiety in a mammal, including a human, by administering to the mammal a 5-HT3 receptor antagonist in combination with an SRI antidepressant agent with improvement in sexual function and/or reduction in gastrointestinal side effects. It also relates to pharmaceutical compositions containing a pharmaceutically acceptable carrier, a 5-HT3 receptor antagonist and an SRI antidepressant.

Abstract: This invention relates to the use of a CYP2D6 inhibitor in combination with a drug having CYP2D6 catalyzed metabolism, wherein the drug and the CYP2D6 inhibitor are not the same compound; and pharmaceutical compositions for said use.

Abstract: Disclosed is a method and composition for the treatment and prevention of a viral infection in a human or animal subject by administering bupropion or a physiologically acceptable salt, solvate or enantiomer thereof. Preferably, the virus is a virus of the Herpes family or condition caused thereby, particularly HSV1 or HSV2.

Abstract: The present invention is directed to a method of treating overweight and/or obesity and eating disorders such as binge-eating disorders, bulimia nervosa and anorexia nervosa. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of zonisamide (1,2-benzisoxazole-3-methanesulfonamide). The present method provides a sustained and significant weight loss in an overweight subject. The method can be used in conjunction with other therapeutic agents/methods commonly used to treat overweight and eating disorders thus enhancing the therapeutic effect of reducing weight and regulating eating disorders.

Abstract: The invention concerns novel bi-aromatic compounds having the formula: which are analogs of vitamin D, the process of preparing them, as well as their use in pharmaceutical compositions in human or veterinary medicine, particularly in dermatology, cancer treatment, treatment of auto-immune diseases, and in organ or tissue transplants. Cosmetic compositions and methods of use are also included.

Abstract: This invention relates to the use of a CYP2D6 inhibitor in combination with a drug having CYP2D6 catalyzed metabolism, wherein the drug and the CYP2D6 inhibitor are not the same compound; and pharmaceutical compositions for said use.