Entries |
Document | Title | Date |
20080227826 | Inhibitors of Histone Deacetylase - The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions. One aspect of the invention provides compounds of formula (1): | 09-18-2008 |
20080255207 | 5-Thioxo-1,5-Dihydro-2H-Pyrrol-2-One Derivatives As Liver X Receptor Modulators - The present invention relates to certain novel compounds of the Formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) α(NR1H3) and/or β(NR1H2) and in treating clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them. | 10-16-2008 |
20080287506 | Insecticidal N,N-Di(Heteroarylalkyl) Amine Derivatives - Certain novel N,N-di(heteroarylalkyl)amine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula (I): wherein Ar Ar | 11-20-2008 |
20080287507 | Nicotine containing toiletry waters - A pharmaceutical liquid formulation for delivering nicotine in any form to a subject by transdermal uptake for treating tobacco dependence and similar conditions, said formulation being a toiletry-water. Toiletry-waters encompass aftershaves, eaux-de-parfum, eaux-de-toilette, eaux-de-cologne, toilet-waters and similar products, all in the form of a lotion, a balm or a gel. Embodiments for certain consideration are aftershave lotions, aftershave balms and aftershave gels. | 11-20-2008 |
20080293778 | Arylvinylazacycloalkane Compounds and Methods of Preparation and Use Thereof - Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain. | 11-27-2008 |
20080306122 | Novel Compounds - Compounds of formula (I) wherein the variables are defined herein, pharmaceutical compositions thereof and methods for treatment using the same. | 12-11-2008 |
20080319025 | Therapeutic and Diagnostic Methods Dependent on CYP2A Enzymes - A method of regulating the activity of human cytochrome P450 isozyme CYP2A6 to control nicotine metabolism or decrease to production of carcinogens from procarcinogens, such as those present in tobacco smoke, in an individual by selectively inhibiting CYP2A6. Various prophylactic (i.e., prevention and treatment) compositions and methods are also described, including an improved oral nicotine composition and method comprising the use of nicotine together with an inhibitor of the CYP2A6 enzyme. | 12-25-2008 |
20090005423 | SYSTEMS AND METHODS FOR EFFECTING CESSATION OF TOBACCO USE - The invention relates generally to a system and method for treating conditions responsive to nicotine therapy. More specifically, the invention relates to pulmonary administration of a nicotine containing formulation to effect smoking cessation. | 01-01-2009 |
20090042950 | TRANSDERMAL TOPICAL COMPOSITION AND ITS USES - At least one silicone is used to modify the release profile of the active compound(s) in a therapeutic composition for topical application the skin that also comprises at least one penetration enhancer and a fugitive solvent base. | 02-12-2009 |
20090048308 | VLA-4 Antagonists - 4-Thio, 4-sulfinyl and 4-sulfonyl proline derivatives of the present invention are antagonists of the VLA-4 integrin and are useful in the treatment, prevention and suppression of diseases mediated by VLA-4-binding and cell adhesion and activation. Moreover, the compounds of the present invention demonstrate significant receptor occupancy of VLA-4 bearing cells after oral administration and are suitable for once-, twice-, or thrice-a-day oral administration. This invention also relates to compositions containing such compounds and methods of treatment using such compounds. | 02-19-2009 |
20090137639 | METHODS FOR CONTROLLING FUNGI AND BACTERIA - The present invention includes compounds of pyridinium salts and methods of their use for agricultural purposes. The present invention also relates to methods of controlling fungi and/or bacteria. | 05-28-2009 |
20090143443 | CYCLIC AMINE COMPOUND AND PEST CONTROL AGENT - The present invention is directed to novel cyclic amine compounds represented by the formula [I]: | 06-04-2009 |
20090143444 | ACID SECRETION INHIBITOR - The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) | 06-04-2009 |
20090149509 | NOVEL PYRROLIDINE BICYCLIC COMPOUNDS AND ITS DERIVATIVES, COMPOSITIONS AND METHODS OF USE - N-[1-oxo-(optionally 2-aza)-2-alkyl-3-(carboxyl or thiol or hydroxyaminocarbonyl or N-hydroxyformamido)-propyl]-(aryl or heteroaryl)-azacyclo | 06-11-2009 |
20090156645 | Method for Increasing the Susceptibility of Peptide Deformylase Inhibitors by Using Efflux Pump Inhibitors - The present invention provides methods and compositions for increasing the susceptibility of PDF inhibitors against Gram-negative organisms by using efflux pump inhibitors. | 06-18-2009 |
20090163555 | SYNTHESIS AND USES OF PYROGLUTAMIC ACID DERIVATIVES - Novel pyroglutamic acid derivatives (I), wherein R | 06-25-2009 |
20090197921 | USE OF NICOTINE, ANALOGUES, THEREOF, PRECURSORS THEREOF OR DERIVATIVES THEROF IN THE TREATMENT OF VARIOUS PATHOLOGICAL PROCESSES CAPABLE OF IMPROVEMENT WITH a-MSH ADMINISTERED IN PROPHYLACTIC OR THERAPEUTIC FORM - This invention protects the use of nicotine, analogues thereof precursors thereof or its derivates for treatment of inflammatory, infectious, candidal or degenerative (of the joints and/or of the central nervous system, of kidneys, the lungs, liver), depression, obesity, bone disease and the like, which can be improved by means of intensification of the actions of α-MSH, given the fact that this hormone are extraordinary properties: e.g., it has an antipyretic potency 20,000 times as great as acetaminophen, its antimicrobian potency, is comparable to gentamycine, it is the best anticandidiasic known; it inhibits apoptosis of various stem cells, and significantly modulates the immune reactions, and therefore the use of agents that affect its release may have significant therapeutic potential. This patent protects the use of nicotine, analogues thereof, precursors thereof or its derivates for the purpose of increasing and/or reducing the bioavailability of α-MSH in blood and/or central or peripheral tissues to accentuate or diminish the effect of the α-MSH by means of changes in its concentration or its effect on the corresponding receptors of any cell, tissue or organ in the body, administrated for therapeutic and/or prophylactic purposes in the short medium and/or long term. | 08-06-2009 |
20090221648 | COMPOSITIONS FOR TREATMENT OF COGNITIVE DISORDERS - The present invention relates to compositions for treatment of cognitive deficits. Such compositions can have a nicotinic acetylcholine receptor ligand, of either α4β2 subtype or α7 nicotinic acetylcholine subtype, and a histamine-3 receptor ligand, a method of using the same, and a related article of manufacture. Combinations of such active agents with psychostimulants or monoamine reuptake inhibitors also is contemplated. | 09-03-2009 |
20090239911 | CYCLOHEXYL SUBSTITUTED PYRROLIDINONES AS INHIBITORS OF 11-BETA-HYDROXYSTEROID DEHYDROGENASE 1 - The present invention discloses novel compounds of Formula I: having 11β-HSD type 1 antagonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I, as well as methods of using the compounds and compositions to treat diabetes, hyperglycemia, obesity, hypertension, hyperlipidemia, metabolic syndrome, and other conditions associated with 11β-HSD type 1 activity. | 09-24-2009 |
20090253754 | Fast dissolving films and coatings for controlled release of flavors, active pharmaceutical ingredients, food substances, and nicotine - A fast-dissolving film for use as a platform for the delivery of material to the oral cavity, comprising a film forming agent; a plasticizing agent; and a fast-dissolving, water-soluble agent; and methods for producing same. | 10-08-2009 |
20090264475 | METHODS AND COMPOSITIONS FOR ALTERING DIETARY BEHAVIOR - The present invention concerns exploiting a characteristically negative behavior, such as habitual behavior or addiction, for example, for a beneficial purpose. In particular aspects, an individual desires eating healthy comestibles that comprises a positively-reinforcing compound, thereby consuming greater quantities of one or more healthy comestibles. In particular aspects, an obese or overweight individual loses weight and/or lowers BMI by consuming at least one healthy comestibles comprising the positively-reinforcing compound. In other aspects, an individual with a medical condition that could benefit from one or more particular comestibles consumes the one or more particular comestibles comprising a positively-reinforcing compound. | 10-22-2009 |
20090275618 | 1, 5-DIPHENYL-3-BENZYLAMINO-1, 5-DIHYDROPYRROLIDIN-2-ONE AS CB1 RECEPTOR MODULATORS - Compounds and pharmaceutical compositions of Formula (I) by blockade of the CB | 11-05-2009 |
20090286836 | Novel Compounds - The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is C | 11-19-2009 |
20100004294 | Stable Lozenge Compositions Providing Rapid Release of Nicotine - Compositions comprising nicotine, which compositions provide a rapid release of nicotine. Nicotine is present in the form of a nicotine-cellulose combination. The compositions are designed for administration to the oral cavity where the nicotine is rapidly released from the composition and available for absorption through the oral mucosa. The compositions are lozenges and have excellent storage stability. | 01-07-2010 |
20100016374 | Compounds Which Inhibit the Glycine Transporter and Uses Thereof - Compounds of formula (I) and salts and solvates are provided: | 01-21-2010 |
20100016375 | 1,5-DIPHENYL-3-PYRIDINYLAMINO-1,5-DIHYDROPYRROLIDIN-2-ONE AS CB1 RECEPTOR MODULATOR - Compound and pharmaceutical compositions of Formula by blockade of the CB | 01-21-2010 |
20100029723 | METHODS AND COMPOSITIONS FOR REDUCTION OF SIDE EFFECTS OF THERAPEUTIC TREATMENTS - The invention provides compositions and methods utilizing a nicotinic receptor modulator, e.g., to reduce or eliminate a side effect associated with dopaminergic agent treatment. In some embodiments, the invention provides compositions and methods utilizing a combination of a dopaminergic agent and a nicotinic receptor modulator that reduces or eliminates a side effect associated with dopaminergic agent treatment. | 02-04-2010 |
20100048642 | METHODS FOR TREATING COGNITIVE DISORDERS - Disclosed herein are methods of treating a patient suffering a cognitive disorder. | 02-25-2010 |
20100063110 | ORALLY ADMINISTRABLE FILMS - The invention relates to oral disintegrable films, which are mucoadhesive, which completely disintegrate in the mouth of a consumer within 1 to 10 minutes, and which include an alkaline substance and optionally a pharmaceutically active substance. | 03-11-2010 |
20100063111 | FORMULATION AND USE AND MANUFACTURE THEREOF - This invention relates to a liquid pharmaceutical formulation for delivering nicotine to a subject. This invention also relates to a method and a system for delivering nicotine as well as manufacturing and use of said liquid pharmaceutical formulation. | 03-11-2010 |
20100087493 | METHOD FOR IMPROVING THE PHARMACOKINETICS OF DRUGS METABOLIZED BY UGT2B10 - A method for modifying the pharmacokinetics of a pharmacologically active agent that undergoes direct N-glucuronidation by UDP-glucuronosyltransferase isoenzyme UGT2B10 in a human subject comprising administering an effective amount of an UGT2B10 modulator to said human subject. A method for identifying compounds which are directly metabolized by UGT2B10 or which act as UGT2B10 modulators is also disclosed. | 04-08-2010 |
20100125094 | PYRROLIDINYL MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS - The present invention relates to new pyrrolidinyl modulating nicotinic acetylcholine receptor compounds, pharmaceutical compositions thereof, and methods of use thereof. | 05-20-2010 |
20100130562 | Stabilized Nicotine Chewing Gum - A nicotine chewing gum composition with improved stability. | 05-27-2010 |
20100130563 | INHIBITORS OF PLASMA KALLIKREIN - The present invention provides compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating the formation of thrombin during or after a PK dependent disease or condition, for example, after fibrinolysis treatment. | 05-27-2010 |
20100197739 | Stable Suspension Concentrate Formulation for Water-Soluble Compounds - The present invention is directed to an insecticidal water based suspension concentrate formulation comprising a water-soluble insecticide selected from the group consisting of N-cyanomethyl-4-(trifluoromethyl)nicotinamide and (EZ)-1-(6-chloro-3-pyridylmethyl)-N-nitroimidazolidin-2-ylidineamine and at least one water-soluble salt selected from the group consisting of magnesium sulfate (hydrated and anhydrous forms) and sodium sulfate, wherein the water-soluble insecticide is present in an insecticidally effective amount and methods of use. | 08-05-2010 |
20100216847 | NORNICOTINE FOR THE TREATMENT OF PAIN - This invention relates to the use of R(+)-, S(−)- or racemic nornicotine for the treatment of pain. | 08-26-2010 |
20100227894 | BENZAMIDE FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS - The present invention provides novel benzamide derivatives of Formula (I): | 09-09-2010 |
20100234431 | PYRROLIDINE COMPOUNDS - A compound of the following formula: | 09-16-2010 |
20100261762 | SEROTONIN AND NOREPINEPHRINE REUPTAKE INHIBITOR - A serotonin and norepinephrine reuptake inhibitor of the formula: | 10-14-2010 |
20100267776 | ARYLVINYLAZACYCLOALKANE COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF - Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain. | 10-21-2010 |
20100331374 | PROLYL HYDROXYLASE INHIBITORS AND METHODS OF USE - The present disclosure relates to HIF-1α prolyl hydroxylase inhibitors, compositions which comprise the HIF-1α prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia. | 12-30-2010 |
20100331375 | BIPHENYL COMPOUNDS USEFUL AS MUSCARINIC RECEPTOR ANTAGONISTS - This invention provides compounds of formula I: | 12-30-2010 |
20110028520 | 1,5-DIPHENYL-PYRROLIDIN-2-ONE COMPOUNDS AS CB-1 LIGANDS - CB-1 receptor inverse agonist compounds of Formula and pharmaceutical compositions for the treatment of obesity or cognitive impairment associated with schizophrenia. | 02-03-2011 |
20110039896 | NOVEL 2-PYRROLIDINYL-3-AMIDO-6-AMINO-PYRIDINE DERIVATIVES USEFUL AS POTASSIUM CHANNEL ACTIVATORS - This invention relates to novel 2-pyrrolidinyl-3-amido-6-amino-pyridine derivatives having medical utility, to use of the 2-pyrrolidinyl-3-amido-6-amino-pyridine derivatives of the invention for the manufacture of a medicament, to pharmaceutical compositions comprising the 2-pyrrolidinyl-3-amido-6-amino-pyridine derivatives of the invention, and to methods of treating a disorder, disease or a condition of a subject, which disorder, disease or condition is responsive to activation of K | 02-17-2011 |
20110053987 | PYRIDINIUM AND THIAZOLIUM CONJUGATES INCLUDING POLYETHYLENE GLYCOLS AND METHODS OF USING THE SAME - Pegylated pyridinium and thiazolium compounds and methods of their use in medicine, research, industry, agriculture and recreational activities are disclosed. The present invention also provides methods of controlling microbial growth and infection. Additionally, the present invention provides methods of controlling microbial infestations relating to industrial and agricultural uses. The present invention can also be used to control insects. | 03-03-2011 |
20110053988 | Low-dose, non-irritating nicotine nasal composition to reduce the desire to smoke - A composition for administration to the nasal mucosa of a subject comprises a solution of nicotine or a pharmaceutically acceptable salt thereof in a pharmaceutically acceptable solvent. The composition has a nicotine concentration less than 1.0 mg/ml. The composition used alone assists in reduction of the desire of a subject to smoke tobacco. It also reduces the nasal symptoms associated with administration of higher concentrations of nicotine to the nasal mucosa. | 03-03-2011 |
20110060015 | 5-[5-[2-(3,5-BIS(Trifluoromethyl)Phenyl)-2-MethylpropanoMethylpropanoylmet- hylamino]-4-(4-Fluoro-2-Methylphenyl)]-2-Pyridinyl-2-Alkyl-Prolinamide As NK1 Receptor Antagonists - The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is C | 03-10-2011 |
20110065757 | METHODS FOR TREATMENT OF KALLIKREIN-RELATED DISORDERS - We have identified classes of kallikrein inhibitors as compounds that are useful in the reduction of vascular permeability (e.g., retinal vascular permeability and cerebral vascular permeability) and astrocyte activation. Diseases and conditions associated with increased vascular permeability include diabetic retinopathy, hemorrhagic stroke, and macular edema. Diseases and conditions associated with astrocyte activation include Alzheimer's disease, multiple sclerosis, Parkinson's disease, amyotrophic lateral sclerosis, Creutzfeldt-Jakob disease, stroke, epilepsy, and brain trauma. | 03-17-2011 |
20110077275 | ANTIOXIDANT COMPOSITIONS FOR SOFT ORAL TISSUE AND METHODS OF FORMULATION AND USE THEREOF - One embodiment of the invention is directed to an oral antioxidant composition including between 0.0001% and 5.0% w/w antioxidant, wherein the antioxidant includes cinnamic acid derivative, tetrahydrocurcuminoids, or phloretin and an orally pharmaceutically acceptable carrier. The composition may have a pH of at least 5.0. According to still further embodiments, the composition may also include between 0.0001% and 5.0% w/w of one or two more additional antioxidants that include cinnamic acid derivative, tetrahydrcurcuminoids, phloretin, or a stilbene derivative. In more particular embodiments, the cinnamic acid derivative may include trans-ferulic acid, the tetrahydrocurcuminoids may include tetrahydrcurcuminoids CG™, or the stilbene derivative may include resveratrol. Other embodiments may relate to methods of treating or preventing an oral disease by applying topically an antioxidant composition as described above. | 03-31-2011 |
20110077276 | Methods and Compositions for Reduction of Side Effects of Therapeutic Treatments - The invention provides compositions and methods utilizing a nicotinic receptor modulator, e.g., to reduce or eliminate a side effect associated with dopaminergic agent treatment. In some embodiments, the invention provides compositions and methods utilizing a combination of a dopaminergic agent and a nicotinic receptor modulator that reduces or eliminates a side effect associated with dopaminergic agent treatment. | 03-31-2011 |
20110082175 | INSECTICIDAL ARYL PYRROLIDINES - The present invention provides novel aryl pyrrolidines having an excellent insecticidal action as insecticides. Aryl pyrrolidines represented by the formula (I) and use thereof as insecticide. | 04-07-2011 |
20110105567 | Pyrrole Compounds Having Sphingosine-1-Phosphate Receptor Agonist Or Antagonist Biological Activity - Disclosed herein are compounds represented by: therapeutic methods, compositions, and medicaments related thereto are also disclosed. | 05-05-2011 |
20110105568 | NOVEL METHOD FOR THE PRODUCTION OF SULPHONYLPYRROLES AS HDAC INHIBITORS - Process for the preparation of a compound of formula (I) wherein R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification, comprising the step of reacting an acrylic acid chloride compound of formula (II′): wherein R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification, with aqueous hydroxylamine and optionally converting the resulting compound into an acid addition salt thereof. | 05-05-2011 |
20110118319 | Insecticidal Arylpyrroline Compounds - The present invention relates to novel arylpyrrolines having the formula (I) and their use as insecticides, as well as to processes for the preparation of the arylpyrrolines | 05-19-2011 |
20110118320 | SUBSTITUTED PYRROLES AND METHODS OF USE - The invention relates to substituted pyrrole compounds of Formula (I) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions. | 05-19-2011 |
20110124688 | NICOTINE RECEPTOR AGONISTS IN STEM CELL AND PROGENITOR CELL RECRUITMENT - The present invention features methods for recruitment of bone marrow-derived stem cells (e.g., endothelial cell precursors, hematopoietic stem cells) by administration of nicotine or other nicotine receptor agonist. The methods of the invention can be used in, for example, treatment of conditions amenable to treatment by recruitment of bone marrow-derived stem cells (e.g., neutropenia). | 05-26-2011 |
20110136875 | Pyrrole Inhibitors of S-Nitrosoglutathione Reductase - The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same. | 06-09-2011 |
20110201652 | 2,4-Disubstituted Pyrrolidine Orexin Receptor Antagonists - The present invention is directed to 2,4-disubstituted pyrrolidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. 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 orexin receptors are involved. | 08-18-2011 |
20110207781 | NOVEL MICROBIOCIDES - Compounds of Formula (I), in which the substituents are as defined in claim | 08-25-2011 |
20110207782 | NICOTINE-CONTAINING PRODUCT - A nicotine-containing product comprising a pharmaceutically acceptable polymeric substrate, which is able to bind cations, nicotine or a pharmaceutically acceptable nicotine derivative, and pharmaceutically acceptable inorganic cations. It further pertains to a method for the preparation of such a nicotine-containing product and to the use thereof for the preparation of a pharmaceutical product. | 08-25-2011 |
20110251243 | Method and Kit for Assessing a Patient's Genetic Information, Lifestyle and Environment Conditions, and Providing a Tailored Therapeutic Regime - A method of determining a personalised therapeutic regime, comprising: receiving genetic information relating to a patient; determining genetic criteria relevant to a personalised therapeutic regime for the patient using the genetic information; receiving personal information relating to the patient; determining personal criteria relevant to the personalised therapeutic regime using the personal information; and combining the genetic criteria and the personal criteria to determine the personalised therapeutic regime for the patient. | 10-13-2011 |
20110288132 | Nicotine and Cocoa Powder Compositions - The present invention relates to a nicotine-containing pharmaceutical composition and methods of using the composition in therapies, such as nicotine replacement therapy. | 11-24-2011 |
20110294859 | SUBSTITUTED PYRIDOXINE-LACTAM CARBOXYLATE SALTS - The present invention provides salt adducts comprising at least one positively charged moiety being a pyridoxine or a derivative thereof and at least one carboxylated 5- to 7-membered lactam ring, optionally additionally substituted, methods of their preparation, and pharmaceutical compositions and medicaments comprising them. Salt adducts of the invention and compositions comprising them may be used to in the treatment of diseases or disorders associated with or inflicted by alcohol consumption. | 12-01-2011 |
20120015983 | Synthesis and Novel Salt Forms of (R)-3-((E)-pyrrolidin-3-yl)vinyl)-5-tetrahydropyran-4-yloxy)pyridine - The present invention relates to (R)-3-((E)-2-(pyrrolidin-3-yl)vinyl)-5-(tetrahydropyran-4-yloxy)pyridine, its salt forms, and to processes for the commercial-scale production of these compounds in sufficient purity and quality for use in pharmaceutical compositions. | 01-19-2012 |
20120022114 | Low-dose, non-irritating nicotine nasal composition to reduce the desire to smoke - A composition for administration to the nasal mucosa of a subject comprises a solution of nicotine or a pharmaceutically acceptable salt thereof in a pharmaceutically acceptable solvent. The composition has a nicotine concentration less than 0.08 mg/ml. The composition used alone assists in reduction of the desire of a subject to smoke tobacco. It also reduces the nasal symptoms associated with administration of higher concentrations of nicotine to the nasal mucosa. | 01-26-2012 |
20120029031 | METADOXINE FOR USE AS INHIBITOR OF HEPATIC FIBROSIS - The use of metadoxine in the treatment of hepatic fibrosis is described. Metadoxine can be orally and/or parenterally administered at a dosage comprised between 50 and 1000 mg per dose, preferably between 300 and 600 mg per dose. In the in vitro study, metadoxine results effective at lower concentrations with respect to those that are obtained in the plasma after oral administration at the doses recommended for conventional pathology. | 02-02-2012 |
20120035223 | LIQUID PEST CONTROL FORMULATION - The present invention relates to a liquid pest control system that includes a synthetic pyrethroid as a pest control active ingredient and an agent selected from the group consisting of purified diethylene glycol monoethyl ether, tocopherol nicotinate and tocopherol succinate, and combinations thereof, to reduce or eliminate paresthesia of the synthetic pyrethroid. The system releases the synthetic pyrethroid efficiently and uniformly. The pest control system is less irritating to the animal's skin as compared to prior art systems, particularly to small breeds of dogs. The system is useful for making liquid spot-on treatments, sprays and the like. | 02-09-2012 |
20120065234 | SUBSTITUTED N-PHENYL-BIPYRROLIDINE CARBOXAMIDES AND THERAPEUTIC USE THEREOF - The present invention discloses and claims a series of substituted N-phenyl-bipyrrolidine carboxamides of formula (I). | 03-15-2012 |
20120077849 | INHALER FOR DELIVERING A METERED DOSE - An inhaler for delivering a metered dose of a medicament, the inhaler comprising a dispensing port ( | 03-29-2012 |
20120088797 | 1-HETEROCYCLYLSULFONYL, 3-AMINOMETHYL, 5- (HETERO-) ARYL SUBSTITUTED 1-H-PYRROLE DERIVATIVES AS ACID SECRETION INHIBITORS - The present invention provides a compound having a superior acid secretion inhibitory effect and showing an antiulcer activity and the like. The present invention provides a compound represented by the formula (I) wherein R | 04-12-2012 |
20120088798 | Intramolecular Hydrogen-Bonded Nitric Oxide Synthase Inhibitors - Compounds and related compositions and methods as can be used to selectively inhibit neuronal nitric oxide synthase and as can be employed in the treatment of various neurodegenerative diseases. | 04-12-2012 |
20120088799 | SEROTONIN REUPTAKE INHIBITORS - In one aspect, the invention relates to compounds of formula I: | 04-12-2012 |
20120245206 | MULTI-CYCLIC COMPOUNDS AND METHODS OF USE - The present invention relates to compounds of Formulas I and II, | 09-27-2012 |
20120270907 | THERAPEUTIC USES OF NICOTINE - The uses of nicotine, analogues, precursors or derivatives thereof for treatment of inflammatory, infectious, candidal or degenerative diseases of the joint, central nervous system, kidney, lung, and liver, depression, obesity, bone disease and the like are described. The various diseases, disorders or conditions can be improved by means of intensification of the actions of α-MSH, whose release is affected by the use of nicotine, analogues, precursors or derivatives thereof, which can increase and/or reduce the bioavailability of α-MSH in blood and/or central or peripheral tissues to accentuate or diminish the effect of the α-MSH for therapeutic and/or prophylactic purposes. | 10-25-2012 |
20120322832 | NICOTINIC ATTENUATION OF CNS INFLAMMATION AND AUTOIMMUNITY - The present invention relates to methods of treating and/or ameliorating the severity of inflammation and autoimmunity in the central nervous system (CNS). In one embodiment, the present invention provides a method of treating multiple sclerosis by administering a therapeutically effective dosage of nicotine, or a pharmaceutical equivalent, analog, derivative, or salt thereof. | 12-20-2012 |
20120322833 | Pesticidal Arylpyrrolidines - The present invention relates to novel pesticidal arylpyrrolidine compounds (arylpyrrolidines) having the general formula (I) | 12-20-2012 |
20130085165 | Buccal Drug Delivery - A lozenge is provided that has stable pH and stable levels of active ingredient over time. It comprises a combination of (i) at least one gum and (ii) at least one non-crystallising sugar or non-crystallising sugar alcohol in a matrix designed for controlled buccal delivery of a drug. The lozenge also contains water and optional components selected from flavourings, taste masking agents, colourings, buffer components, pH adjusting agents, excipients, stabilizers and sweeteners. Methods of preparing the lozenge are also provided. | 04-04-2013 |
20130109724 | N-AMINOPYRROLYLMETHYLTETRAHYDROPYRIDINES AS ANTI-CANCER AGENTS | 05-02-2013 |
20130143931 | 5-[5-[2-(3,5-BIS(TRIFLUOROMETHYL)PHENYL)-2-METHYLPROPANOMETHYLPROPANOYLMET- HYLAMINO]-4-(4-FLUORO-2-METHYLPHENYL)]-2-PYRIDINYL-2-ALKYL-PROLINAMIDE AS NK1 RECEPTOR ANTAGONISTS - The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is C | 06-06-2013 |
20130178501 | MANUFACTURE OF LOZENGE PRODUCT WITH RADIOFREQUENCY - The present invention features a process for making a lozenge product including the steps of forming a powder blend containing an amorphous carbohydrate polymer into the desired shape of the lozenge product and applying radiofrequency energy to the shape for a sufficient period of time to soften or melt said amorphous carbohydrate polymer to fuse the shape into said lozenge product. | 07-11-2013 |
20130178502 | Pyridine Compounds for Controlling Invertebrate Pests I - The present invention relates to novel pyridine compounds of the formulae I and II, to their salts, to their tautomers, to their N-oxides, and to the salts of these N-oxides or tautomers. The compounds are useful for combating or controlling invertebrate pests, in particular arthropod pests. The invention also relates to a method for controlling invertebrate pests by using these compounds. The invention further relates to plant propagation material and to agricultural compositions comprising said compounds. | 07-11-2013 |
20130184313 | NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS AND THE USES THEREOF - The invention relates to pyridinyl nicotinic acetylcholine receptor ligands, compositions comprising an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand and methods to treat or prevent a condition, such as depression and nicotine dependence, comprising administering to an animal in need thereof an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand. | 07-18-2013 |
20130231373 | HYDROXAMATE-BASED INHIBITORS OF DEACETYLASES - The present teachings relate to compounds of Formula (I): and pharmaceutically acceptable salts, hydrates, esters, and prodrugs thereof, wherein R | 09-05-2013 |
20130237570 | Formulation and Use and Manufacture Thereof - This invention relates to a liquid pharmaceutical formulation for delivering nicotine to a subject. This invention also relates to a method and a system for delivering nicotine as well as manufacturing and use of said liquid pharmaceutical formulation. | 09-12-2013 |
20130253013 | SEROTONIN REUPTAKE INHIBITORS - In one aspect, the invention relates to compounds of formula I: | 09-26-2013 |
20130274296 | REMELTED INGESTIBLE PRODUCTS - A method of preparing an orally ingestible hard boiled product, comprising: i) heating a sugar material to a first temperature sufficient to liquefy the sugar material; ii) cooling the liquefied sugar material to provide a cooled sugar material having a solid or semi-solid form; iii) heating the cooled sugar material to a second temperature, which is lower than the first temperature; iv) combining the sugar material with one or more temperature sensitive ingredients before, during, or after said heating step iii), but after said cooling step ii), such that an intimate mixture of the second liquefied sugar material and the one or more temperature sensitive ingredients is provided; and v) cooling the intimate mixture to form an orally ingestible product. Orally ingestible hard boiled products prepared according to this method are also provided. | 10-17-2013 |
20130289079 | Nicotine Lozenge Composition - The present invention relates to nicotine lozenge compositions comprising reduced levels of buffering agents from traditional nicotine lozenges and which provide optimal oral pH and prompt nicotine absorption in a smaller, more convenient dosage form. | 10-31-2013 |
20130338197 | PARASITE- AND HYGIENIC PEST-CONTROLLING AGENT - There is provided a novel agent for controlling harmful arthropods or nematodes that are parasites and hygienic pests for animals. An ecto- or endo-parasiticide for mammals or the like comprising as active ingredient, one or more selected from substituted benzamide compounds of formula (1) or salts thereof: | 12-19-2013 |
20140045902 | NEW TRIAZOLE COMPOUNDS AS POTENTIAL ANTI-INFLAMMATORY AGENTS - The present invention relates to a compound of formula 1 or 2 | 02-13-2014 |
20140088155 | d-Methadone for the Treatment of Psychiatric Symptoms - The present invention relates to a method of treating psychiatric symptoms in a subject having a NMDA receptor and a NE receptor which includes administering d-methadone, d-methadol, d-alpha-acetylmethadol, l-alpha-acetylmethadol, d-alpha-normethadol, l-alpha-normethadol, pharmaceutically acceptable salts thereof, or mixtures thereof, to the subject under conditions effective for the substance to bind to the NMDA receptor and NE receptor of the subject. | 03-27-2014 |
20140088156 | SORAFENIB DERIVATIVES AS SEH INHIBITORS - The present invention provides compounds for the inhibition of soluble epoxide hydrolase and associated disease conditions. | 03-27-2014 |
20140107163 | SYNTHESIS AND NOVEL SALT FORMS OF (R)-3-((E)-2-(PYRROLIDIN-3-YL)VINYL)-5-(TETRAHYDROPYRAN-4-YLOXY)PYRIDINE - The present invention relates to (R)-3-((E)-2-(pyrrolidin-3-yl)vinyl)-5-(tetrahydropyran-4-yloxy)pyridine, its salt forms, and to processes for the commercial-scale production of these compounds in sufficient purity and quality for use in pharmaceutical compositions. | 04-17-2014 |
20140107164 | ARYLVINYLAZACYCLOALKANE COMPOUNDS AND METHODS OF PREPARATION AND USE THEREOF - Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain. | 04-17-2014 |
20140113938 | Pyrrole Inhibitors of S-Nitrosoglutathione Reductase - The present invention is directed to inhibitors of S-nitrosoglutathione reductase (GSNOR), pharmaceutical compositions comprising such GSNOR inhibitors, and methods of making and using the same. | 04-24-2014 |
20140128436 | PRODRUGS OF INHIBITORS OF PLASMA KALLIKREIN - The present invention provides prodrugs of compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating plasma kallikrein dependent diseases or conditions, for example, diabetic macular edema, with the prodrugs having the formula: | 05-08-2014 |
20140249188 | 5-[5-[2-(3,5-BIS(TRIFLUOROMETHYL)PHENYL)-2-METHYLPROPANOMETHYLPROPANOYLMET- HYLAMINO]-4-(4-FLUORO-2-METHYLPHENYL)]-2-PYRIDINYL-2-ALKYL-PROLINAMIDE AS NK1 RECEPTOR ANTAGONISTS - The invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R is C | 09-04-2014 |
20140256773 | Novel nicotine derivatives - Described are novel nicotine derivatives represented by general formulas (I) and (III), and salts thereof, and herbicide & pharmaceutical compositions containing the same as the active ingredient. The compound and salts thereof can control annual or perennial weed growing on the land where various crops such as rice plant, wheat, cotton and corn grow for a wide period ranging from the pre-emergence to growth in a remarkably small dose. The compounds and salts thereof can be useful as an anti-microbial and anti-fungal agents and also for the treatment of blood pressure, skeletal muscle, attention deficit disorder, mental disorders, schizophrenia, Alzheimer disease, Parkinson's disease and depression. Also described is the preparation of the nicotine derivatives having formula (I) and (III). | 09-11-2014 |
20140275181 | Compounds and uses thereof for the modulation of hemoglobin - Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation. | 09-18-2014 |
20140275182 | BICYCLIC PYRROLE DERIVATIVES USEFUL AS AGONISTS OF GPR120 - The present invention is directed to bicyclic pyrrole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus. | 09-18-2014 |
20140303214 | TRANSMUCOSAL DRUG DELIVERY SYSTEM - Disclosed are preparations and formulations of high thermodynamic activity lipophilic associations (LA), in which there is pairing between an ionizable pharmaceutical agent and a lipophilic species having ionic characteristics opposite to that of the pharmaceutical agent. Such lipophilic associations manifest high thermodynamic activity, as evidenced by their being predominantly in a liquid phase at room temperature or solvated in a lower-than-water dielectric solvent. Further the pharmaceutical agent being solubilized means that dissolution is not rate limiting to transmucosal absorption. This LA or LA-solvate is formulated into a low dielectric dosage form, from whence, upon the dosage form's hydration, the pharmaceutical agent is driven through the mucosal tissue and into systemic circulation. The invention therefore provides an enhanced transmucosal drug delivery system for ionizable pharmaceutical agents at or near physiological pH. | 10-09-2014 |
20140364463 | NICOTINIC ATTENUATION OF CNS INFLAMMATION AND AUTOIMMUNITY - The present invention relates to methods of treating and/or ameliorating the severity of inflammation and autoimmunity in the central nervous system (CNS). In one embodiment, the present invention provides a method of treating multiple sclerosis by administering a therapeutically effective dosage of nicotine, or a pharmaceutical equivalent, analog, derivative, or salt thereof. | 12-11-2014 |
20140378512 | COMPOSITION FOR IMPROVING COGNITION AND MEMORY - The invention relates to a pharmacologically active combination, having utility in treating insomnia patients, which comprises: (a) at least one first active ingredient selected from melatonin, other melatonergic agents, melatonin agonists and melatonin antagonists; and (b) at least one second active ingredient selected from nicotine and nicotine receptor agonists; to use of a medicament containing component (a) with or without component (b) for alleviation of at least one adverse effect which occurs in a patient in the course of nicotine replacement therapy, or otherwise, selected from impairment of the quality of sleep, impairment of cognition and impairment of memory, as well as to a kit having utility in treating insomnia patients, which comprises components (a) and (b) in unit dosage form. | 12-25-2014 |
20150051253 | ( ) (2R,3S)-2-AMINO-3-HYDROXY-3-PYRIDIN-4-YL-1-PYRROLIDIN-1-YL-PROPAN-1-ON- E (L)-(+) TARTRATE SALT, ITS METHOD OF PRODUCTION AND USE - The present invention is directed to (−)-(2R,3S)-2-amino-3-hydroxy-3-pyridin-4-yl-1-pyrrolidin-1-yl-propan-1-one (L)-(+)tartrate salt, a pharmaceutical composition comprising said salt, a process for making said salt, and the use of said salt in the treatment of pain. | 02-19-2015 |
20150099787 | Non-Flushing Niacin Analogues, and Methods of Use Thereof - One aspect of the present invention relates to substituted pyridines and pharmaceutially acceptable salts thereof that are active against a range of mammalian maladies. Another aspect of the invention relates to a pharmaceutical composition, comprising a compound of the present invention or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable excipient. The present invention also relates to methods of treating a range of mammalian maladies or conditions, including but not limited to hyperlipidemia, hypercholesterolemia, atherosclerosis, coronary artery disease, congestive heart failure, cardiovascular disease, hypertension, coronary heart disease, angina, pellagra, Hartnup's syndrome, carcinoid syndrome, arterial occlusive disease, obesity, hypothyroidism, vasoconstriction, osteoarthritis, rheumatoid arthritis, diabetes, Alzheimer's disease, lipodystrophy, or dyslipidemia, raising serum high-density lipoprotein (HDL) levels, and lowering serum low-density lipoprotein (LDL) levels. | 04-09-2015 |
20150105431 | Nicotine Lozenge Composition - The present invention relates to nicotine lozenge compositions comprising reduced levels of buffering agents from traditional nicotine lozenges and which provide optimal oral pH and prompt nicotine absorption in a smaller, more convenient dosage form. | 04-16-2015 |
20150111928 | Disintegrable Oral Films - A water soluble film that is disintegrable in the oral cavity to deliver an active agent is provided. The disintegrable film includes at least one water soluble polymer and an active agent. Also provided are methods for preparing the disintegrable oral film and for using the disintegrable film to administer an effective dosage of an active agent into the oral cavity for absorption through the oral mucosa. According to certain embodiments, the disintegrable film includes at least one water soluble polymer and a nicotine active. | 04-23-2015 |
20150126561 | INHIBITION OF UNDESIRED SENSORY EFFECTS BY THE COMPOUND CAMPHOR - A smokeless tobacco product or medicinal nicotine product includes nicotine and camphor dissolved in a non-flavored oily carrier. Preferably, the camphor is present in a concentration ranging from about 600 ppm to about 1300 ppm. Also disclosed are methods of making such products. | 05-07-2015 |
20150322042 | SUBSTITUTED TRIAZOLE DERIVATIVES AS OXYTOCIN ANTAGONISTS - The present invention relates to substituted triazoles of formula (I), uses thereof, processes for the preparation thereof and compositions containing said compounds. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction. | 11-12-2015 |
20150328202 | EDIBLE PRODUCT FOR NICOTINE DELIVERY - An edible product for oral ingestion comprising one or more edible seeds infused with nicotine is disclosed. The edible product enables reduction in nicotine craving in nicotine addicted persons. A therapeutic package for use with one or more edible seeds is also disclosed, comprising a first predefined quantity of powdered nicotine; and a second predefined quantity of at least one control agent, wherein the powdered nicotine and the control agent are infused in the edible seeds for oral ingestion A method for administration of nicotine as a medical therapy to a person is also disclosed, comprising providing a dose of one or more edible seeds infused with nicotine to the person; and periodically repeating the dose over predefined time intervals to achieve a predefined level of nicotine in bloodstream of the person. | 11-19-2015 |
20150335629 | Methods Of Treating Fragile X Syndrome And Related Disorders - The present invention provides methods of alleviating a sign or a symptom of Fragile X Syndrome and related disorders such as autism spectrum disorders. | 11-26-2015 |
20150344456 | NICOTINE SALTS, CO-CRYSTALS, AND SALT CO-CRYSTAL COMPLEXES - The invention provides certain nicotine salts, co-crystals, and salt co-crystals and provides novel polymorphic forms of certain nicotine salts. In particular, nicotine salts with mucic acid, 3,5-dihydroxybenzoic acid, and 2,3-dihydroxybenzoic acid, and crystalline polymorphic forms of nicotine 4-acetamidobenzoate, nicotine gentisate, and nicotine 1-hydroxy-2-naphthoate are described. The invention further provides methods of preparation and characterization of such nicotine salts, co-crystals, and salt co-crystals and polymorphic forms thereof. In addition, tobacco products, including smoking articles, smokeless tobacco products, and electronic smoking articles comprising nicotine salts, co-crystals, and/or salt co-crystals are also provided. | 12-03-2015 |
20160008347 | THERAPEUTIC USES OF NICOTINE | 01-14-2016 |
20160090375 | SUBSTITUTED PHENYLAZOLE DERIVATIVE - Compounds are provided having an excellent hypoglycemic effect and β cell- or pancreas-protecting effects, or pharmaceutically acceptable salts thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause hyperglycemia due to abnormal glucose metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed. | 03-31-2016 |
20160137600 | Pyrrole Derivatives as Alpha 7 nAChR Modulators - Disclosed are compounds of the formula (I), wherein R | 05-19-2016 |
20160166564 | Nicotine Salt with Meta-Salicylic Acid | 06-16-2016 |
20160193199 | METHODS OF TREATING FRAGILE X SYNDROME AND RELATED DISORDERS | 07-07-2016 |
20160199362 | METHOD FOR THE TREATMENT, ALLEVIATION OF SYMPTOMS OF, RELIEVING, IMPROVING AND PREVENTING A COGNITIVE DISEASE, DISORDER OR CONDITION | 07-14-2016 |
20160374962 | MICROSIZED CURCUMIN COMPOSITIONS - Disclosed herein are formulations for the local delivery of therapeutically effective doses of curcumin that provide sufficient serum levels of curcumin to treat diseases such as head and neck disorders and upper aerodigestive disorders. | 12-29-2016 |
20180021328 | NICOTINE SALT WITH META-SALICYLIC ACID AND APPLICATIONS THEREIN | 01-25-2018 |