Abstract: The present invention is directed to novel tetracyclic heteroatom containing derivatives, pharmaceutical compositions containing them, their use in the treatment of disorders mediated by one or more sex steroid hormone receptors and processes for their preparation.

Abstract: The invention features derivatives of R(?)-11-hydroxyaporphines and methods of treating Parkinson's disease, sexual dysfunction, and depressive disorders therewith.

Abstract: This invention relates to novel compounds that are dihydroindoles derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel dihydroindoles derivatives that are derivatives of silodosin. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an ?-1A-adrenoreceptor antagonist, such as silodosin.

Abstract: The present invention relates to topical compositions comprising 5?-reductase inhibitors. The present invention also includes processes for preparation of such topical compositions and methods of using them.

Abstract: Methods for treating a patient having neurological, psychotic, and psychiatric disorders are described comprising the steps of administering to the patient an effective amount of a partial and/or full dopamine D1 receptor agonist, and administering to the patient an effective amount of a dopamine D2 receptor antagonist, Pharmaceutical compositions comprising a dopamine D1 receptor agonist and a dopamine D2 receptor antagonist are also described. The D1 dopamine receptor agonist and the D2 dopamine receptor antagonist can be administered to the patient in the same or in a different composition or compositions.

Abstract: The present invention is directed to compounds of Formula I: that are potassium channel modulators and pharmaceutical compositions thereof. The present invention is further directed to methods of treatment using the compounds and pharmaceutical compositions of the invention. The present invention is still further directed to synthetic processes for producing the compounds of the invention.

Abstract: The present invention relates to formulations suitable for transdermal administration characterized by containing SLNs which contain active principles with a very short half-life and/or drugs with high activity.

Abstract: A composition, device, and method for treating sexual dysfunction via inhalation is provided which comprises inhaling a dose of a powder composition, the powder composition comprising apomorphine or pharmaceutically acceptable salts thereof. Preferably, the powder composition further includes a carrier material, the carrier material has an average particle size of from about 40 to about 70 microns, and at least 90 percent of said apomorphine has a particle size of 5 microns or less.

Abstract: The present invention relates to Indenoisoquinolinone Analogs, compositions comprising an effective amount of an Indenoisoquinolinone Analog and methods for treating or preventing an inflammatory disease, a reperfusion injury, diabetes mellitus, a diabetic complication, reoxygenation injury resulting from organ transplantation, an ischemic condition, a neurodegenerative disease, renal failure, a vascular disease, a cardiovascular disease, cancer, a complication of prematurity, cardiomyopathy, retinopathy, nephropathy, neuropathy, erectile dysfunction or urinary incontinence, comprising administering to a subject in need thereof an effective amount of an Indenoisoquinolinone Analog.

Abstract: The present application provides methods for detecting, diagnosing, monitoring, predicting responsiveness to therapeutic agents and staging cancer. The present application provides methods and compositions useful for suppression of GRP78 expression or activity in cancer cells to overcome resistance of certain therapeutic agents. The present application also provides methods for predicting whether a subject with cancer is at risk for developing resistance to certain therapeutic agents.

Abstract: The invention features derivatives of R(—)-11-hydroxyaporphines and methods of treating Parkinson's disease, sexual dysfunction, and depressive disorders therewith.

Abstract: Disclosed are compositions and methods for modulating protein trafficking and treating or preventing disorders characterized by impaired protein trafficking. Also disclosed are methods for identification of compounds that rescue protein trafficking defects and methods of enhancing protein production.

Abstract: The present invention discloses novel pharmaceutically acceptable salts of aporphine compounds and carboxyl-group containing agents. Also, the present invention discloses methods for preparing the pharmaceutically acceptable salts. These pharmaceutically acceptable salts are suitable for use in treating and/or preventing hyperglycemic disease and/or several oxidative stress related diseases.

Abstract: The present invention discloses novel aporphine derivatives. Also, the present invention discloses that these novel aporphine derivatives can be used for treating oxidative stress induced diseases such as cardiovascular disease, diabetes, aging, Alzheimer's disease, kidney disease, cancer or brain ischemic disease etc.

Abstract: A method of treating Restless Legs Syndrome (RLS) comprises the joint administration of an agent selected from dopamine turnover increasing agent and dopaminergic receptor exciting agent, in particular pramipexole, and iron in a biologically usable form, in pharmacologically effective combined amounts. Also disclosed is a corresponding use; a pharmaceutical composition comprising an agent selected from dopamine turnover increasing agent and dopaminergic receptor exciting agent, in particular pramipexole, and iron in a biologically usable form, and a pharmaceutically acceptable carrier; a package comprising a pharmaceutical composition for per-oral administration comprising an agent selected from dopamine turnover increasing agent and dopaminergic receptor exciting agent and a pharmaceutically acceptable carrier and a pharmaceutical composition for per-oral administration comprising iron in a biologically usable form and a pharmaceutical acceptable carrier.

Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner.

Abstract: The use of phanquinone for the manufacture of a pharmaceutical composition for the prevention or the treatment of Alzheimer's disease is disclosed. Also methods of treatment or prevention of Alzheimer's disease are disclosed.

Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient. These compounds are therefore useful in the treatment of conditions caused by androgen deficiency or which can be ameliorated by androgen administration, including osteoporosis, osteopenia, glucocorticoid-induced osteoporosis, periodontal disease, bone fracture, bone damage following bone reconstructive surgery, sarcopenia, frailty, aging skin, male hypogonadism, postmenopausal symptoms in women, atherosclerosis, hypercholesterolemia, hyperlipidemia, obesity, aplastic anemia and other hematopoietic disorders, inflammatory arthritis and joint repair, HIV-wasting, prostate cancer, cancer cachexia, muscular dystrophies, premature ovarian failure, and autoimmune disease, alone or in combination with other active agents.

Abstract: Compounds of structural formula I are modulators of the androgen receptor (AR) in a tissue selective manner. They are useful as agonists of the androgen receptor in bone and/or muscle tissue while antagonizing the AR in the prostate of a male patient or in the uterus of a female patient.

Abstract: Disclosed herein are methods and compositions related to compound 1 or compound 2 or pharmaceutically acceptable salts, or prodrugs thereof, which are antagonists of a prostaglandin EP4 receptor, or are prostaglandin EP4 antagonists.

Abstract: A medicament effective for inhibiting onset of Alzheimer disease via intracellular aggregation mechanism is provided. A medicament for prophylaxis and treatment of Alzheimer disease comprising as an active ingredient apomorphine hydrochloride wherein cell death dependent upon intracellularly accumulated amyloid ? proteins and/or p53 is inhibited; and/or wherein a level of intracellularly accumulated amyloid ? proteins and/or phosphorylated tau proteins is lowered to improve energy production, protein metabolism and synaptic function of neurons so as to ameliorate the recognition capacity such as defects of memory.

Abstract: The present invention relates to cosmetic use, by topic application on the skin of at least one protoberberine, with exception of berberine, or a vegetable extract containing it, as an active substance reducing activity of the pilosebaceous unit, preferably inhibiting activity of the pilosebaceous unit. In particular, the invention relates to cosmetic use of at least one protoberberine, with exception of berberine, or a vegetable extract containing it, as an agent reducing, preferably inhibiting the growth of hairs of the face and/or the body, and/or seborrheic activity of the sebaceous glands. The invention also relates to a cosmetic composition comprising in a dermatologically acceptable carrier, at least one protoberberine, with exception of berberine, or a vegetable extract containing protoberberines, as an active substance, which reduces, preferably inhibits the skin's pilosebaceous unit activity.

Abstract: The present invention relates to stabilized aqueous solutions of an ergoline compound of formula I or their physiologically tolerable salt or derivative, in which R1 stands for an H atom or a halogen atom and R2 stands for an alkyl group or alkenyl group with 1 to 4 carbons and a single or double bond, also containing 0.05% to 90.00% of at least one oxygen-containing cosolvent. Likewise, the present invention relates to the use of the solutions stabilized according to the present invention to prepare an agent for parenteral treatment of neurodegenerative diseases or brain trauma.

Abstract: Methods and systems are described for prediction of a patient's response to a drug for treating androgenetic skin disorders such as alopecia, acne, and hirsutism. For a given drug such as anti-androgens and 5-alpha-reductase inhibitors, and a given dosage, the likely responsiveness of that drug and dosage may be determined, for example, by generating a set of patient scores based on a patient profile, including genetic sample information, and comparing that scores to a set of reference information.

Abstract: Methods and compositions for stimulating the growth of hair are disclosed wherein said compositions include a cyclopentane heptanoic acid, 2-cycloalkyl or arylalkyl compound represented by the formula I wherein the dashed bonds represent a single or double bond which can be in the cis or trans configuration, A, B, Z, X, R1 and R2 are as defined in the specification. Such compositions are used in treating the skin or scalp of a human or non-human animal. Bimatoprost is preferred for this treatment.

Abstract: The solid state chemistry of 17?-N-[2,5-bis(trifluoromethyl)phenyl]carbamoyl-4-aza-5-?-androst-1-en-3-one of which the international nonproprietary name is Dutasteride (the active ingredient in products marketed as Avodart, Avidart, Avolve, Duagen, Dutas, Dutagen, Duprost) and its process for preparing. The synthetic process comprises formation of the mixed anhydride, its subsequent reaction with 2,5-bis(trifluoromethyl)phenylamine in the presence of an appropriate Lewis catalyst and its isolation, purification and crystallization from acetonitrile/water.

Abstract: There is provided a compound having Formula I wherein G is a fluorocarbyl group, and wherein R1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group.

Abstract: A method of improving stool frequency in a subject having diarrhea-predominant IBS, comprising administering a composition comprising cilansetron or a pharmaceutically acceptable derivative thereof to a subject in need of treatment in an amount sufficient to decrease stool frequency within 2 days or less of administering.

Abstract: The present invention relates to new pharmaceutical uses of 4-azasteroid compounds, in particular of Finasteride/Dutasteride/Dutasteride and Dutasteride, particularly preferred of Finasteride/Dutasteride/Dutasteride, and its pharmaceutically acceptable derivatives, and combinations comprising said compounds. The invention also features generally the use of a modulator compound of neuroprotective conditions via beta subunits of shaker-type voltage-gated potassium channels and/or via members of solute carriers family 25, in particular Aralar (member 12) and adenine-nucleotide translocators 1 & 2 (member 4 & 5) and/or via a 4-nitrophenylphosphatase domain and non-neuronal SNAP25-like protein homolog 1 (NIPSNAP 1) as a neuroprotective medicament, particularly as a medicament for the prevention and/or treatment of neurological diseases such as dementia, Parkinson, Alzheimer, schizophrenia or epilepsy.

Abstract: The present invention is directed to rapid and efficient methods of identifying therapeutic compounds by allowing only the most favorable molecules initially selected based on their physical-chemical profile falling within a range predefined by the physical-chemical/biological relationship of a previously tested small subset of compounds of same core structure to be assayed; and to the therapeutic compositions identified by said methods.

Abstract: Pharmaceutical compositions and method using aminergic compounds and complement compounds. Compositions are provided comprising: (a) a subefficacious amount of a non-adrenergic aminergic compound or of an adrenergic antagonist; and (b) a safe and effective amount of a complement compound. Methods are also provided comprising the administration of: (a) a low dose of a non-adrenergic aminergic compound or of any adrenergic antagonist; and (b) a safe and effective amount of a complement compound. Non-adrenergic aminergic compounds can comprise a histaminergic, dopaminergic, muscarinergic, serotoninergic, octopaminergic, or trace aminergic compound. Complement compounds include ascorbates, opioids, polycarboxylic acid chelators, resveratrols, cysteines, substituted derivatives and analogs thereof, and mixtures thereof. Preferred complements include ascorbates, particularly ascorbic acid.

Abstract: The present invention relates to tetrahydroprotoberberines of the formula (I) and the physiologically acceptable salts thereof. The invention also relates to the use of the compounds of the formula (I) or pharmaceutically acceptable salts thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with dopamine receptor ligand, such as schizophrenia.

Abstract: The present invention relates to compositions and methods for the preventing, treating, and researching discoloration (e.g., hair graying, hair whitening, undesired change in hair color). In particular, the present invention provides compositions and methods for treating, preventing and researching hair discoloration through inhibition of mTOR function (e.g., mTOR activity, mTOR expression). In addition, the present invention provides methods and compositions that utilize mTOR inhibiting agents in the preventing, treating, and researching hair discoloration.

Abstract: Pseudobase benzo[c]phenanthridines and the pharmaceutically acceptable salts thereof of Formula I are provided herein. The variables R, R1, R2, R3, and R4 are defined herein. Certain pseudobase benzo[c]phenanthridines provided herein act as prodrugs, targeting the parent benzo[c]phenanthridinium alkaloid to hydrophilic or hydrophobic regions in the body. Pharmaceutical compositions comprising a pseudobase benzo[c]phenanthridine and a carrier, excipient, or diluent are provided herein. Methods of treating or preventing microbial, fungal and or viral infections and methods of treating diseases and disorders responsive to protein kinase C modulation, topoisomerase I, and/or topoisomerase II modulation are also provided.

Abstract: Particles are provided for use in restorative procedures to treat and/or retard alopecia The particles include poly[bis(trifluoroethoxy)phosphazene] and/or a derivatives thereof which may be present throughout the particles or within an outer coating of the particles. The particles may also include a core having a hydrogel formed from an acrylic-based polymer. Such particles may be provided to a user in various colors or with customized coloration to match desired scalp colors. Moreover, such particles may be loaded to provide localized treatment with an active component agent directed at restoration of normal function and hair production within the hair follicle.

Abstract: The present application describes deuterium-enriched finasteride, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: The present application describes deuterium-enriched dutasteride, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: Non-occlusive compositions for transdermal delivery of 5-alpha-reductase inhibitors, and more particularly finasteride or dutasteride or pharmaceutically acceptable salts or derivatives thereof, and methods of making same. The composition may, for example, be a gel suitable for transdermal or transmucosal applications. The compositions of the present invention typically include a mixture of water and alcohol, and a solvent system having a mono alkyl ether of diethylene glycol and a glycol present in specified ratios and in specific amounts, wherein the pH of the gel is usually between about pH 4.5 and about pH 8. The compositions may include further components, for example, the hydroalcoholic vehicle may further include additional penetration enhancer(s), buffering agent(s), antioxidant(s), stabilizer(s) and/or gelling agent(s). Also, a method for the sustained delivery of 5-alpha-reductase inhibitors to treat a variety of conditions and disorders.

Abstract: Provided are combinations of pharmaceutical agents capable of eliciting a therapeutic effect. A first therapeutic agent in the combination has 5HT2/5HT3 antagonist and alpha-2 antagonist activity. A second therapeutic agent possesses both serotonin reuptake inhibitory activity and norepinephrine reuptake inhibitory activity or is a reversible inhibitor of monoamine oxidase A (RIMA). In some embodiments, a combination of a first therapeutic agent and a second therapeutic agent results in reduction in one or deleterious side effects associated with the first therapeutic agent, the second therapeutic agent or both. Also provided are methods of treatment employing a first therapeutic agent and a second therapeutic agent. Also provided are kits containing a first therapeutic agent, a second therapeutic agent and instructions for administering the first therapeutic agent and the second therapeutic agent.

Abstract: The biphthalate salts of compound I are modulators of the androgen receptor (AR) in a tissue selective manner.

Abstract: Compositions comprising extracts or isolated or purified compounds from plants of the genus Corydalis provide prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Corydalis compounds and their derivatives of natural and synthetic origins lower total cholesterol, LDL-cholesterol, and triglycerides and increase hepatic LDL receptor expression and activate AMP-activated protein kinase. Specific stereoisomers of Corydalis compounds with lipid lowering activity include 14R-(+)-corypalmine, 14R,13S-(+)-corydaline, 14R-(+)-tetrahydropalmatin, (+)-corlumidin, d-(+)-bicuculline, and (+)-egenine.

Abstract: A patch pump device generally includes at least one fluid source, a fluid communicator, and an electrochemical actuator. The fluid communicator is in fluid communication with the fluid source. The electrochemical actuator is operative to cause fluid to be delivered from the fluid source into the fluid communicator.

Abstract: This invention provides novel caspase inhibitors of formula I: wherein R1 is hydrogen, CHN2, R, or —CH2Y; R is an aliphatic group, an aryl group, an aralkyl group, a heterocyclyl group, or a heterocyclylalkyl group; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; X2—X1 is N(R3)—C(R3), C(R3)2—C(R3), C(R3)2—N, N?C, C(R3)?C, C(?O)—N, or C(?O)—C(R3); each R3 is independently selected from hydrogen or C1-6 aliphatic; Ring C is a fused aryl ring; n is 0, 1 or 2; and each methylene carbon in Ring A is optionally and independently substituted by ?O, or one or more halogen, C1-4 alkyl, or C1-4 alkoxy. The compounds are useful for treating caspase-mediated diseases.

Abstract: Use of Fructus schisandrae in preparation of medicaments for preventing and reducing toxicity and side effects of antineoplastic agents. The toxicity and side effects of antineoplastic agents are cardiovascular toxicity, hepatotoxicity, nephrotoxicity, suppression of bone marrow, immunosuppression, or alopecia etc induced by antineoplastic agents. Fructus schisandrae and extracts thereof, especially ethanol extracts, schisandrin B, are effective in reducing antineoplastic agent's toxicity and side effects.

Abstract: The present invention provides a kit comprising, in separate compartments of a container, the following components (a) and (b): (a) a combination of apomorphine or a pharmaceutically acceptable acid addition salt thereof and a pharmaceutically acceptable excipient or carrier; and (b) a solution which comprises a diluent and a pH modifying agent; the components being presented such that they can be combined at the point of use into a formulation which is adjusted to a pH ranging from mildly acidic to alkaline and which is suitable for buccal administration. The formulation is useful in treating Parkinson's disease and in promoting sexual function.

Abstract: Disclosed are compositions for affecting weight loss comprising a first compound and a second compound, where the first compound is a psychotherapeutic agent and the second compound is a anticonvulsant. Also disclosed are methods of affecting weight loss, increasing energy expenditure, increasing satiety in an individual, or suppressing the appetite of an individual, comprising identifying an individual in need thereof and treating that individual with a psychotherapeutic agent and an anticonvulsant.

Abstract: This invention relates to novel compounds that are dihydroindoles derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel dihydroindoles derivatives that are derivatives of silodosin. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering an ?-1A-adrenoreceptor antagonist, such as silodosin.

Abstract: N-Substituted indenoisoquinoline compounds, and pharmaceutical formulations of N-substituted indenoisoquinoline compounds are described. Also described are processes for preparing N-substituted indenoisoquinoline compounds. Also described are methods for treating cancer in mammals using the described N-substituted indenoisoquinoline compounds or pharmaceutical formulations thereof.

Abstract: There is provided a compound having Formula (I) wherein G is H or a substituent, and wherein R1 is any one of a sulphamate group, a phosphonate group, a thiophosphonate group, a sulphonate group or a sulphonamide group, capable of inhibiting steroid sulphatase.

Abstract: The present invention provides compositions, methods, and kits for treatment of Parkinson's disease and other conditions for which treatment with a dopamine agonist is therapeutically beneficial. The invention provides a biocompatible nonerodible polymeric device which releases dopamine agonist continuously with generally linear release kinetics for extended periods of time. Dopamine agonist is released through pores that open to the surface of the polymeric matrix in which it is encapsulated. The device may be administered subcutaneously to an individual in need of continuous treatment with dopamine agonist.