Abstract: A method of modulating the dopaminergic system of the central nervous system comprising administering to a subject a dopamine precursor and/or a dopamine agonist in an amount effective to induce a reward response in the subject is described, as are related compositions.

Abstract: The present invention is directed to a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use.

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: 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: The present invention relates to a tetracyclic fused heterocyclic compound represented by the following formula [I] wherein each symbol is as defined in the specification, or a pharmaceutically acceptable a salt thereof, and a hepatitis C virus (HCV) polymerase inhibitor and a therapeutic agent for hepatitis C containing this compound. The compound of the present invention shows an anti-HCV activity based on the HCV polymerase inhibitory activity, and useful as an agent for the prophylaxis or treatment of hepatitis C.

Abstract: The invention provides a compound of formula (I): or a salt or prodrug thereof, wherein Y, W, Z, Z1, Z2, Z3, Z4, and R1-R12 have any of the values described in the specification, as well as compositions comprising a compound of formula (I). The compounds are useful as antibacterial agents.

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 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 invention provides compositions comprising formula 1 steroids, e.g., 16?-bromo-3?-hydroxy-5?-androstan-17-one hemihydrate and one or more excipients, including compositions that comprise a liquid formulation comprising less than about 3% v/v water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16?-bromo-3?-hydroxy-5?-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using the compounds. The invention also provides methods to make and use these immunomodulatory compositions and formulations.

Abstract: Methods and compositions are described for the treatment of very severe acne vulgaris, including nodulocystic acne and conglobate acne. Compounds which inhibit either or both type 1 and type 2 isoforms of steroid 5?-reductase are administered daily in either oral or topical formulations to patients suffering from severe forms of acne vulgaris. Very high dosages of such compounds can effectively be administered oral just once a week and be successful.

Abstract: The invention relates to a dosage form that is thermoshaped without being extruded and that is safeguarded from abuse, comprising at least one synthetic or natural polymer having a breaking strength of at least 500 N in addition to one or more active substances that could be subject to abuse and optionally physiologically acceptable adjuvants. The invention also relates to a corresponding method for producing said dosage form.

Abstract: The present invention provides compounds of formula I: formula (I) wherein X1-X4 and R1-R12 have any of the values defined in the specification, as well as salts and prodrugs thereof, which inhibit major molecular mechanisms associated with bacterial cell division and proliferation so as to be useful for the treatment and/or prevention of bacterial infections. The invention also provides compositions comprising these compounds as well as methods for using these compounds to inhibit bacterial cell division and proliferation and to treat bacterial infections.

Abstract: The present invention is a method for identifying agents which modulate microRNA activity. The invention involves contacting a cell harboring a microRNA and a microRNA binding sequence, which is operably linked to a nucleic acid molecule encoding a reporter protein, with a test agent and determining whether the test agent increases or decreases the expression of the reporter protein thereby identifying a microRNA modulator. Antagonists identified by this screening assay are provided, as are methods for using the same to inhibit microRNA activity and prevent or treat disease.

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: The present technology relates to compounds of Formulas (V) and (VI) and methods of making and using such compounds. Methods of use include prevention and treatment of hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, hepatic steatosis, and metabolic syndrome. Compounds disclosed herein also lower total cholesterol, LDL-cholesterol, and triglycerides and increase hepatic LDL receptor expression, inhibit PCSK9 expression, and activate AMP-activated protein kinase.

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

Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.

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: 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: The invention relates to a population of tamsulosin-comprising pellets for oral administration of a combination dosage form containing physically separated a tamsulosin dose in the form of the population of the tamsulosin comprising pellets and at least one other dose of a pharmaceutically active substance, said pellets comprising tamsulosin hydrochloride uniformly dispersed in a carrier matrix, wherein (i) said pellets in the population have a size of less than about 1.4 mm and, advantageously, at least 90% of the pellets have a size of larger than 0.30 mm; and (ii) an average content of tamsulosin hydrochloride in the population of pellets is between about 0.15-3.00 weight percent, calculated on a dry pellet basis, to a process of making such population of pellets, and to their use.

Abstract: Pharmaceutical compositions are provided for treatment of Parkinson's disease comprising a pharmaceutically acceptable carrier and a fixed dose combination of two active agents selected from compounds having either neuroprotective or symptomatic effects, or both, in Parkinson's disease patients, wherein the molar ratio of the two compounds is in the range of 1:1 to 1:100.

Abstract: New aminoalkoxyimino derivatives at position 3 of substituted B-homoandrostanes and B-heteroandrostanes, processes for their preparation, and to pharmaceutical compositions containing them for the treatment of cardiovascular disorders, such as heart failure and hypertension. In particular compounds having the general formula (I) are described, where the radicals have the meanings described in detail in the application.

Abstract: Cytosine deaminase inhibitors and methods for identifying inhibitors of the anti-retroviral activity of APOBEC3G are described.

Abstract: The present invention relates to the topical and oral delivery of a composition comprising one or more active agents for treating a disease or symptoms in a subject. In some embodiments, the present invention comprises a composition comprising at least one active compound, e.g., finasteride or minoxidil, and one or more lipids. In some embodiments, the present invention relates to composition and method of preparation for treating androgenic alopecia (AGA), prevention of hair loss and female hirsutism. In some embodiment, the present invention comprises finasteride and at least one lipid component for the treatment of benign prostatic hyperplasia. In some embodiment, the present invention comprises tacrolimus or amphotericin B and at least one lipid component for the treatment of skin or eye related diseases.

Abstract: An azonafide-based compound of Formula I, a composition comprising the compound, and a method of using the compound to deliver a cytotoxic azonafide derivative to a cell, as well as related compounds and methods for the use thereof to pre-pare an azonafide-based compound of Formula I.

Abstract: The present invention relates to new piperidine modulators of dopamine receptors, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates to a novel technology for forming fine particles with a size of 0.02˜3 microns from a solid that can be dissolved in a liquid solvent and is not decomposed by heat. The particle preparation technology according to the present invention may be applicable to the fields of food, cosmetics, biopolymer, polymer compositions, and pharmaceuticals.

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: A method of treating hair comprising applying a hair building solid agent for use on or with one or more of hair, skin and hair building solids for altering and/or maintaining the electrostatic charge of the hair and/or skin such that it has a substantially negative polarity. The method further comprises applying hair building solids to hair before and/or during and/or after applying the hair building solid agent. The hair building solid agent is applied as a spray on to the hair and/or skin and/or hair building solid.

Abstract: Trans-hexahydrobenzoaphenanthridines of the formula (I) wherein X, Y, R1, R2, R3, R4, R5, R6, and R7 are as defined herein, are disclosed. Pharmaceutical formulations including such compounds, and methods of using such compounds for treating a patient suffering from dopamine-related dysfunction of the central or peripheral nervous system are also disclosed.

Abstract: The present invention provides zebrafish based methods for the identification of compounds potentially useful in the treatment of motor neuron degenerative diseases (MNDDs), compounds identified by these methods and compositions, methods and medicaments for treating MNDDs.

Abstract: The invention relates to indole-derived compounds and to the use of said compounds for the preparation of a medicament that can be used to treat diseases related to the process of splicing pre-messenger RNAs in the cell, such as Frasier syndrome, frontotemporal dementia linked to chromosome 17 (a form of Parkinson's disease), Leigh syndrome (a type of encephalopathy), atypical cystic fibrosis, certain neuropathologies including Alzheimer's disease linked to a mutation in the Tau protein, muscle atorphy which affects the SMN (Survival of Motor Neuron) gene, depression linked to a serotonin splicing impairment, and certain cancers in which the global splicing process is affected (e.g. breast cancer, colon cancer and certain lymphomas), as well as viral diseases such as AIDS.

Abstract: The present invention is directed to compounds of Formula (I): where variables A1, A2, B, J, K, m, n, R4, R5a, R5b, R5c and X are as defined herein useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

Abstract: The present invention is directed to liquid compositions containing chitosan, a chitosan derivative or a physiologically acceptable salt thereof, which form a film after application onto the scalp and/or the hair, which compositions are useful for delivery of actives onto the scalp surface and/or onto the hair.

Abstract: Liquid pharmaceutical compositions for administration to a mucosal surface, including a therapeutic agent and a pectin with a low degree of esterification are described. Such compositions gel, or can be adapted to gel, at the site of application in the absence of an extraneous source of divalent metal ions.

Abstract: The invention relates to compounds of formula I: along with pharmaceutical compositions containing the same and methods of use thereof for the treatment of autoimmune disease.

Abstract: The invention provides a method of sustained delivery of a tertiary amine-containing parent drug comprising administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile quaternary ammonium salts of tertiary amine-containing parent drugs (or tertiary imine-containing parent drugs) that are derivatized through aldehyde-linked prodrug moieties that reduce the solubility of the prodrug compound at a reference pH as compared to the parent drug. The physical, chemical and solubility properties of these derivatives can be further modulated by the choice of counterion X?. In one embodiment, the present invention provides a prodrug compound of Formula I: where R1-R5 are defined in the written description of the invention.

Abstract: A group of novel dibenzo[f,h]isoquinoline derivatives as shown in the specification. Also disclosed are methods of using the compounds for treating a disease associated with NO overproduction, cancer, or viral infection.

Abstract: In alternative embodiments, this invention provides compositions and methods for treating cancer or any condition caused by dysfunctional cells, side effects from treatments for cancer or any condition caused by dysfunctional cells, e.g., mucositis therapies (e.g., for oral mucositis; digestive mucositis; esophageal mucositis; intestinal mucositis). In alternative embodiments, the invention provides cytoprotection products that may be used either alone or in combination with other medical therapies such as cancer chemotherapies and radiation therapies.

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: The present invention provides methods and therapeutic agents for lowering or increasing serum serotonin levels in a patient in order to increase or decrease bone mass, respectively. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis and the agents are TPH1 inhibitors or serotonin receptor antagonists.

Abstract: The present invention relates generally to methods for transdermal delivery of a therapeutically effective amount of apomorphine using microneedles. The invention also provides methods for treatment of erectile dysfunction and Parkinson's disease using apomorphine hydrochloride or any pharmaceutically acceptable salt, and/or apomorphine prodrugs to the microneedle-treated site.

Abstract: A method of treating Alzheimer's disease, Parkinson's disease, sexual dysfunction or erectile dysfunction in a man by administration of a 5alpha reductase inhibitor together with a testosterone supplement is described. The method is also concerned with the use of the 5alpha reductase inhibiting compound and the testosterone supplement together with another agent useful for treating erectile dysfunction, including PDE V inhibitors; AGE (advanced glycation end-product) breakers; alpha 1 blockers; alpha 1A antagonists; alpha 2 antagonists; dopamine agonists; dopamine D4 agonists; melanocortin agonists; oxytocin agonists; prostaglandin; radical scavengers; rotamase inhibitors; aviptadil; nitroglycerine; and GPCR agonists for treating male sexual dysfunction or erectile dysfunction.

Abstract: The present invention relates to methods of treating a patient infected by Actinomycetes sp. by administering 6-aza-17-substituted-androst-4-en-3-one compounds to that patient. Another aspect of the invention relates to the screening for drug candidates to treat patients infected by Actinomycetes sp.

Abstract: The present invention is related to a use of a steroid sulfatase inhibitor in the manufacture of a medicament for preventing or inhibiting premature uterine contractions. Specifically, the present invention is related to steroid sulfatase inhibitors useful for the preparation of a pharmaceutical formulation for the modulation, notably the inhibition of pre-term labor.

Abstract: Methods and compositions are described for treating impaired neurological function, including altered state of consciousness disorders, in an individual who has sustained a brain injury comprising administering to the individual apomorphine. Methods and compositions are described for treating impaired neurological function, including altered state of consciousness disorders, in an individual who has sustained a brain injury comprising administering to the individual at least 1000 mg or more of L-dopa (levodopa) per day. The use of potent dopaminergic agents to stimulate emergence from an altered consciousness state, such as a coma, is disclosed.

Abstract: The invention features sublingual formulations of apomorphine and apomorphine prodrugs, and methods of treating Parkinson's disease, sexual dysfunction, and depressive disorders therewith.

Abstract: Methods and compositions are provided for preventing and treating neurological disorders, in particular Parkinson's disease.

Abstract: A method of treating male sexual dysfunction or erectile dysfunction by administration of a 5alpha reductase inhibitor together with a testosterone supplement is described. The method is also concerned with the use of the 5alpha reductase inhibiting compound and the testosterone supplement together with another agent useful for treating erectile dysfunction, including PDE V inhibitors; AGE (advanced glycation end-product) breakers; alpha 1 blockers; alpha 1A antagonists; alpha 2 antagonists; dopamine agonists; dopamine D4 agonists; melanocortin agonists; oxytocin agonists; prostaglandin; radical scavengers; rotamase inhibitors; aviptadil; nitroglycerine; and GPCR agonists for treating male sexual dysfunction or erectile dysfunction.

Abstract: The current invention is in the field of molecular biology/pharmacology and provides compounds which modulate the effects of GPR30 as well as the classical estrogen receptors alpha and beta (ER? and ER?). These compounds may function as agonists and/or antagonists of one or more of the disclosed estrogen receptors.