| Entries |
| Document | Title | Date |
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| 20100029666 | Macrocyclic Quinoxaline Compounds as HCV NS3 Protease Inhibitors - The present invention relates to macrocyclic a compound of formula (I) and its use as inhibitors of the hepatitis C virus (HCV) NS3 protease, and in treating or preventing HCV infections. | 02-04-2010 |
| 20100029665 | Methods and Compositions for Treating Migraine Pain - The present invention provides novel methods and compositions for the treatment and prevention of headaches, vascular headaches, migraine headaches, cluster headaches, and migraine. One of the headaches, vascular headaches, migraine headaches, cluster headaches, and migraine treated by the methods and compositions of the invention is migraine. | 02-04-2010 |
| 20160008320 | STATINS IN THE TREATMENT OF MUSCULAR DYSTROPHIES AND MYOPATHIES | 01-14-2016 |
| 20130210830 | THERAPEUTIC COMPOSITIONS - The invention relates to a product containing the compound of formula (I) below (I) or a pharmaceutically acceptable salt of this compound, in combination with at least one compound having PDE5-inhibitory properties, or a pharmaceutically acceptable salt thereof, for therapeutic use, simultaneously, separately or over a period of time, in the treatment of a disease wherein vasoconstriction is involved. | 08-15-2013 |
| 20130197006 | Non-Starch Based Soft Chewables - The present invention generally relates to soft chewables, especially suitable for delivering active ingredients to animals and processes for the preparation thereof. In various embodiments, the soft chewable comprises a pharmaceutically effective amount of at least one active ingredient, a flavoring agent, a disintegrant a humectant, an antioxidant, a preservative, and water. In accordance with preferred embodiments, the soft chewable is essentially free of starch, oil glycols, waxes, and soy products. | 08-01-2013 |
| 20160083385 | PYRAZINOISOQUINOLINE COMPOUNDS - This invention in one embodiment is directed to a compound of Formula Ia; | 03-24-2016 |
| 20110015201 | HEDGEHOG PATHWAY ANTAGONISTS AND METHODS OF USE - The present disclosure provides for compounds, pharmaceutical preparations, kits and methods for the inhibition of the Hh pathway and the alleviation of cancer and developmental disorders associated with the Hh pathway. | 01-20-2011 |
| 20090312338 | Novel Tricyclic Compounds - The invention provides a compound of Formula (I) | 12-17-2009 |
| 20130203762 | VETERINARY ANTIPROLACTINIC COMPOSITION FOR RUMINANTS - This present invention relates to an antiprolactinic veterinary composition to be administered to ruminants. Said composition comprises at least one antiprolactinic compound which is an agonist of dopamine receptors, and is particularly useful for reducing udder engorgement and/or the reduction of pain after drying off and/or of increasing welfare, and/or of reducing milk leakage in ruminants as well as for preventing new mammary microbial infections, secondary infection, or co-infections in ruminants and mastitis. | 08-08-2013 |
| 20160130259 | SUBSTITUTED BENZOFURAN COMPOUNDS AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES - The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system. | 05-12-2016 |
| 20150065515 | LIVER X RECEPTOR MODULATORS - Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described. | 03-05-2015 |
| 20100130505 | COMPOSITIONS AND METHODS FOR INHIBITING G PROTEIN SIGNALING - Disclosed are compositions and methods for treating diseases associated with G protein βγ subunit activity. | 05-27-2010 |
| 20100075973 | POLO-LIKE KINASE INHIBITORS - The present invention provides PLK inhibitors of the formula | 03-25-2010 |
| 20090253707 | HETEROANNELATED ANTHRAQUINONE DERIVATIVES AND THE SYNTHESIS METHOD THEREOF - A heteroannelated anthraquinone derivative compound is provided. The heteroannelated anthraquinone derivative compound is represented by a formula (I): | 10-08-2009 |
| 20160030425 | METHODS AND COMPOSITIONS FOR SLEEP DISORDERS AND OTHER DISORDERS - Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals and pharmaceutical compositions comprising them for the treatment of one or more disorders involving the 5-HT2A, SERT and/or dopamine D2 pathways are disclosed. In addition, the compounds may be combined with other therapeutic agents for the treatment of one or more sleep disorders, depression, psychosis, dyskinesias, and/or Parkinson's disease or any combinations. | 02-04-2016 |
| 20110034471 | NOVEL COMBINATIONS COMPRISING A PHOSHODIESTERASE-5 INHIBITOR AND THEIR USE - The invention relates generally to novel pharmaceutical methods for the treatment of various conditions. Compositions comprising: at least one phosphodiesterase-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; a serotonin-norepinephrine reuptake inhibitor; a cholinesterase inhibitor; a dopamine agonist; or a medication suitable to increase the chemical concentrations of the neurotransmitters, selected from amino acids, monoamines, neuropeptides and other agents capable of primary neurotransmission in the synaptic clefts, and their use for treating a neurodegenerative disease in a subject. The invention also relates to: Compositions comprising: at least one phosphodiestersa-5-inhibitor in combination with one or more of the following medications: a selective serotonin reuptake inhibitor; or a cholinesterase inhibitor, and their use for treating damaged skin in a subject. | 02-10-2011 |
| 20110071155 | Tricyclic Nitrogen Containing Compounds And Their Use As Antibacterials - Compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides thereof: | 03-24-2011 |
| 20110082151 | SULFONYLUREA MODULATORS OF ENDOTHELIN RECEPTOR - The present invention relates to new sulfonylurea modulators of endothelin receptor activity, pharmaceutical compositions thereof, and methods of use thereof. | 04-07-2011 |
| 20110086859 | ALKYL SUBSTITUTED INDOLOQUINOXALINES - Novel substituted indoloquinoxalines of formula (I | 04-14-2011 |
| 20160030573 | STABLE PHARMACEUTICAL COMPOSITIONS OF 5,10-METHYLENETETRAHYDROFOLATE - This invention relates to stable pharmaceutical compositions of 5,10-methylene-(6R)-, -(6S)-, or -(6R,S)-tetrahydrofolate (MTHF), by adjusting a basic pH and the simultaneous use of citrate. Stabilisation is effected even in the absence of a reducing agent. The present invention is particularly suitable for producing lyophlisation solutions and lyophilisates or dry powders and dry mixtures, since the stable MTHF solutions can be used in high concentrations for filling corresponding vessels such as vials, ampoules, etc. The lyophilisates have a surprisingly long shelf life and are surprisingly stable. They can be reconstituted without problems by adding wateror aqueous solutions, and the final clear injection solutions again exhibit excellent stability properties. Moreover, the present invention even makes it possible to prepare difficulty soluble calcium 15 or acidic salts of MTHF in high concentrations and as physiologically compatible isotonic solutions. | 02-04-2016 |
| 20160031889 | ANTIVIRAL INDOLO[2,3-B]QUINOXALINE - A compound of formula (I) | 02-04-2016 |
| 20090247533 | Ecteinascidins - The present invention is directed to several newly discovered ecteinascidin (Et) species, designated herein as Et 731, Et 815, Et 808, and Et 594. The physical properties of these compounds, their preparation and therapeutic properties are also reported. | 10-01-2009 |
| 20140073647 | NOVEL FLUOROERGOLINE ANALOGS - Provided herein are novel fluoroergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT | 03-13-2014 |
| 20100267733 | Synergistic Modulation of Microglial Activation by Nicotine and THC - Treatment of microglial cells with nicotine and THC synergistically attenuate the microglial activation. Using microglial activation, the combination of THC and nicotine interact synergistically reduced LPS induced TNF-α release, showing that the combination of THC and nicotine clinically have greater efficacy in reducing neuroinflammation with less side effects than either drug given alone. CD40 signaling was found critically involved in pathological activation of microglial cells. This invention is also relevant to peripheral inflammation as well thru macrophages. In addition, other cannabinoids and other nicotinic-like medications currently in development are also covered under this discovery. | 10-21-2010 |
| 20110092511 | INHIBITORS OF AKT ACTIVITY - The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms, preferably Akt1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity especially Akt1 by administering the compound to a patient in need of treatment of cancer. | 04-21-2011 |
| 20100273803 | Oral Formulations for Tetrapyrrole Derivatives - Oral formulations and method of formulating photosensitive agents for oral administration during photodynamic therapy (PDT) and Antimicrobial photodynamic therapy (APDT) treatment are presented. The oral formulated photosensitizers show increased solubility and permeability, thus improving the bioavailability of photosensitizers at the treatment site. An orally administered photosensitizer is suitably formulated for mucosal adhesion and absorption via gastrointestinal mucosal membranes. Oral formulation provided herein use lipids and known proteins as carriers for photosensitizers by oral route. Carriers for encapsulating preselected photosensitizers include conventional liposomes, pegylated liposomes, nanoemulsions, nanocrystrals, nanoparticles, fatty emulsions, lipidic formulations, hydrosols, SMEDDS, Alpha-Feto protein (AFP), and Bovine-Serum-Albumin (BSA), fatty emulsions, hot-melt-extrudates and nanoparticles. The oral formulation, in case of a hydrophobic photosensitizer in the present invention, is stabilized using suitable surfactants/solubilizers thus preventing aggregation of the drug in the stomach and until it is absorbed in the duodenum and the small intestine. Oral formulations can be administered in the form of liquid, capsule, tablet, powder, paste or gel. Formulated drugs can be administered orally as one single dose or in multiple doses before administering PDT. In one embodiment Temoporfin (m-THPC) is used as a photosensitizer in the oral formulations. Temoporfin like many hydrophobic photosensitizers are especially suitable to be administered orally because there is no known enzyme system in the mammalian body which can metabolize Temoporfin or similar photosensitizers. Temoporfin can reach the blood system unchanged and fully active after absorption of the formulation in the gastrointestinal tract. | 10-28-2010 |
| 20110059977 | USE OF CANTHIN-6-ONE AND ITS ANALOGS IN THE TREATMENT OF MYCOBACTERIA-LINKED PATHOLOGIES ( amended - The present invention relates to the use, for the preparation of a medicament intended for the treatment or the prevention of pathologies linked to, or caused by mycobacteria, of at least one of the compounds of the following formula (I): in which B represents in particular a nitrogen atom, and R1, R2, R3, R4, R5, R6, R7 and R8 represent in particular a hydrogen atom. | 03-10-2011 |
| 20150133456 | FLUOROERGOLINE DERIVATIVES AND USES THEREOF - Provided herein are novel fluoroergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT | 05-14-2015 |
| 20110269764 | THERAPEUTIC APPROACHES FOR TREATING ALZHEIMER DISEASE AND RELATED DISORDERS THROUGH A MODULATION OF SYNAPSE FUNCTION - The present invention relates to compositions and methods for the treatment of Alzheimer's disease and related disorders. More particularly, the invention relates to combined therapies that modulate synapse function for treating said disease. | 11-03-2011 |
| 20110003824 | Caspase Inhibitors and Uses Thereof - This invention provides novel caspase inhibitors of formula I: | 01-06-2011 |
| 20140187560 | BROMOCRIPTINE FORMULATIONS - The present application describes pharmaceutical formulations of bromocriptine mesylate and methods of manufacturing and using such formulations. The formulations are useful for improving glycerine control in the treatment of type 2 diabetes. | 07-03-2014 |
| 20110105516 | POLYMERIZED MICELLES - Polymerised micelles comprising polymerised amphiphilic molecules obtained starting from amphiphilic molecules having one or two lipid chains each comprising one or two polymerisable moieties and linked to a polar head. | 05-05-2011 |
| 20110105515 | TARGETING THE ONCOPROTEIN NUCLEOPHOSMIN - (+)-Avrainvillamide, a naturally occurring alkaloid with antiproliferative activity, is shown to bind to the oncoprotein nucleophosmin. Nucleophosmin is known to regulate the tumor suppressor protein p53 and is overexpressed in many different human tumors. The invention provides methods of modulating nucleophosmin and p53 using (+)-avrainvillamide and analogues thereof. These compounds may provide leads for the development of novel anti-cancer therapies that target nucleophosmin. | 05-05-2011 |
| 20110112106 | TRICYCLIC INHIBITORS OF 5-LIPOXYGENASE - Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of 5-lipoxygenase (5-LO). Also described herein are methods of using such 5-LO inhibitors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other leukotriene-dependent or leukotriene mediated conditions, diseases, or disorders. | 05-12-2011 |
| 20110112105 | SUBSTITUTED HETEROCYCLE FUSED GAMMA-CARBOLINES SOLID - The present invention relates to toluenesulfonic acid addition salt crystals of specific substituted heterocycle fused gamma-carbolines, the method of making and using such crystals. | 05-12-2011 |
| 20110112104 | TRICYCLIC COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM. - Compounds of formula (I): | 05-12-2011 |
| 20160113930 | COMPOUNDS FOR USE IN TREATING RETT SYNDROME - Provided herein are compounds and pharmaceutically acceptable salts thereof that are useful therapeutics for Rett syndrome. | 04-28-2016 |
| 20150320746 | PHARMACEUTICAL FORMULATION COMPRISING 2,3-DIMETHYL-6-(N,N-DIMETHYLAMINOETHYL)-6H-INDOLO-(2,3-B)QUINOXALINE - A pharmaceutical composition for topical administration including 2,3-dimethyl-6-(N,N-dimethylaminoethyl)-6H-indolo-(2,3-b)quinoxaline (B-220) or a pharmaceutically acceptable salt thereof in a pharmaceutically acceptable carrier. The composition is useful for the treatment of herpes virus infections of the skin or mucous membranes in a mammal subject. | 11-12-2015 |
| 20090298842 | Novel therapeutic targets for the treatment of mycobacterial infections and compounds useful therefor - Described herein is the discovery that certain mycobacterial serine/threonine protein kinases, particularly protein kinase G (PknG), are effective therapeutic targets for the treatment of mycobacterial infections. Furthermore, the present application refers to the use of mycobacterial serine/threonine protein kinases for developing methods for detection and determination of these kinases for recognizing and monitoring diseases and for controlling therapy of diseases. Additionally disclosed are novel 4,5,6,7-tetrahydrobenzo[b]thiophene compounds, benzo(g)quinoxaline compounds, and pharmaceutically acceptable salts thereof, and methods of using such compounds and salts thereof for the prophylaxis and/or treatment of virally and/or bacterially induced infections, particularly mycobacteria-induced infections, including opportunistic infections, as well as pharmaceutical compositions containing at least one 4,5,6,7-tetrahydrobenzo[b]thiophene compound and/or benzo(g)quinoxaline compound and/or pharmaceutically acceptable salts thereof in a pharmaceutically acceptable carrier. | 12-03-2009 |
| 20100222357 | INDOL-3-Y-CARBONYL-PIPERIDIN AND PIPERAZIN-DERIVATIVES - The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: | 09-02-2010 |
| 20100249142 | IMIDAZOL[1,2-alpha]QUINOXALINES AND DERIVATIVES FOR THE TREATMENT OF CANCERS - Imidazo[1,2-a]quinoxaline compounds for the treatment of cancers as well as pharmaceutical compositions that include these compounds and their uses in therapy. | 09-30-2010 |
| 20090291958 | Substituted PDE5 inhibitors - Provided herein are substituted PDE5 inhibitors of Formula 1, and processes of preparation and pharmaceutical compositions thereof. Also provided are methods of their use for the treatment and/or management of hypertension, erectile dysfunction, and/or the inability to maintain improved erectile function. | 11-26-2009 |
| 20090318460 | AMORPHOUS VARENICLINE TARTRATE AND PROCESS FOR THE PREPARATION THEREOF - The present invention generally relates to an amorphous form of varenicline and its pharmaceutically acceptable salts thereof. More particularly the present invention relates to amorphous forms of varenicline and its L-tartrate salt; a process for their preparation and pharmaceutical compositions comprising the same. | 12-24-2009 |
| 20110130405 | SUBSTITUTED QUINAZOLINES AS BLOOD PLATELET LOWERING AGENTS - This invention relates to the discovery of 3-and 5-substituted analogues of the selective platelet lowering agent anagrelide with reduced potential for cardiovascular side-effects which should lead to improved patient compliance and safety in the treatment of myeloproliferative diseases. More specifically, the present invention relates to certain imidazoquinazoline derivatives which have the general formula (I) shown below wherein the meanings of the substituents are defined in claim 1 and which have utility as platelet lowering agents in humans. The compounds of the present invention function by inhibiting megakaryocytopoeisis and hence the formation of blood platelets. | 06-02-2011 |
| 20140031359 | Method Of Treating Metabolic Disorders And Depression With Dopamine Receptor Agonists - This invention relates to methods and formulations for treating metabolic disorders and depression. In some embodiments, the methods comprise administering a dopamine receptor agonist and an anti-depressant. | 01-30-2014 |
| 20120149709 | PYRAZINOISOQUINOLINE COMPOUNDS - This invention relates to novel compounds that are pyrazinoisoquinoline derivatives, and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel pyrazinoisoquinoline derivatives that are derivatives of praziquantel. 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 antihelminthic agent, such as praziquantel. | 06-14-2012 |
| 20100324055 | SOLID STATES FORMS OF VARENICLINE SALTS AND PROCESSES FOR PREPARATION THEREOF - Salts and crystalline forms of several salts of Varenicline, i.e., Varenicline sulfate, Varenicline mesylate, and Varenicline fumarate, methods of preparing the solid states of Varenicline sulfate, Varenicline mesylate, and Varenicline fumarate, and processes for preparing Varenicline base from those Varenicline salts are provided. | 12-23-2010 |
| 20120270881 | CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS - Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of formulae Ia and Ib are constituted by three distinct molecular parts: Template A, conformation Modulator B and Bridge C. These macrocycles Ia and Ib are readily manufactured by parallel synthesis or combinatorial chemistry in solution or on solid phase. They are designed to interact with a variety of specific biological target classes, examples being the agonistic or antagonistic activity on G-protein coupled receptors (GPCRs), ion channels and signal transduction pathways. In particular, these macrocycles act as antagonists of the motilin receptor, the FP receptor and the purinergic receptors P2Y | 10-25-2012 |
| 20110245261 | ANTIPROLACTINIC VETERINARY COMPOSITION FOR RUMINANTS - This present invention relates to an antiprolactinic veterinary composition to be administered to ruminants. Said composition comprises at least one antiprolactinic compound which is an agonist of dopamine receptors, and is particularly useful for promoting a substantial reduction of lactation, mammary involution, and for treating and/or intra-mammary diseases or infections of ruminants. | 10-06-2011 |
| 20130245032 | BICYCLIC AND TRICYCLIC INHIBITORS OF SUMOYLATION ENZYMES AND METHODS OF THEIR USE - According to the embodiments described herein, a tricyclic SUMOylation inhibitor compound is provided. In some embodiments, a method for inhibiting a SUMOylation enzyme in a cell is provided. Such a method may include administering a SUMOylation inhibitor compound to the cell. In some aspects, the SUMOylation enzyme is SUMO E1 or SUMO E2. In some aspects, the method may be used to inhibit a cancer cell in vitro (e.g., grown in culture) or in vivo (e.g., as part of a tumor in a subject). In other embodiments, a method for treating a cancer, degenerative diseases and viral infection is provided. Such a method may include administering an effective amount of a pharmaceutical composition to a subject having the cancer. The pharmaceutical composition may include a SUMOylation inhibitor compound. In some embodiments, the method for treating a disease may further comprise administering one or more DNA-damaging therapy in combination with administration of the pharmaceutical composition. | 09-19-2013 |
| 20140179704 | 8'-HYDROXY-DIHYDROERGOTAMINE COMPOUNDS AND COMPOSITIONS - 8′-Hydroxy-Dihydroergotamine (8′-OH DHE) medicinal compounds, compositions, and dosage forms containing such compositions are provided. Also provided herein are methods of treatment, prevention, or amelioration of migraine disorders using the compounds, compositions, dosage forms and administration techniques disclosed herein. | 06-26-2014 |
| 20100035886 | PARENTERAL FORMULATIONS OF DOPAMINE AGONISTS - This invention relates to stable pharmaceutical compositions for parenteral administration comprising dopamine agonists and peripheral acting agents useful for treatment of metabolic disorders or key elements thereof. The parenteral dosage forms exhibit long stable shelf life and distinct pharmacokinetics. | 02-11-2010 |
| 20110263607 | ALPHA HELIX MIMETICS IN THE TREATMENT OF CANCER - Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a compound relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed. | 10-27-2011 |
| 20110263606 | SOLID ORAL DOSAGE FORMS COMPRISING TADALAFIL - Improved pharmaceutical solid oral dosage forms for the buccal and/or sublingual delivery of Tadalafil. The improved delivery systems for solubilizing and stabilizing pharmaceutically active ingredients exhibit enhanced methods of preparation by the use improved solubilization systems which can maintain the Tadalafil in a buccal and/or sublingual oral dosage form or a polymeric film matrix that provides improved bioavailability and/or absorption of Tadalafil. | 10-27-2011 |
| 20150057287 | METHOD OF THERAPEUTIC ADMINISTRATION OF DHE TO ENABLE RAPID RELIEF OF MIGRAINE WHILE MINIMIZING SIDE EFFECT PROFILE - Pharmaceutical compositions containing dihydroergotamine (DHE) and methods in which DHE is administered to patients for treatment of migraine without side effects or adverse effects are disclosed. Methods for rapid treatment of migraine with DHE are disclosed comprising: dampening the peak plasma concentration (C | 02-26-2015 |
| 20100234388 | SUBSTITUTED PDE5 INHIBITORS - Provided herein are substituted PDE5 inhibitors of Formula (1), and processes of preparation and pharmaceutical compositions thereof. Also provided are methods of their use for the treatment and/or management of hypertension, erectile dysfunction, and/or the inability to maintain improved erectile function. The compounds are deuterated tadalafil derivatives. | 09-16-2010 |
| 20110082150 | Headache pre-emption by dihydroergotamine treatment during headache Precursor events - Disclosed are methods that address providing a subject experiencing, or who has experienced, a headache precursor event and administering dihydroergotamine, or a pharmaceutically acceptable salt or complex thereof, to the subject by oral inhalation, in an amount effective to pre-empt a subsequent headache in the subject. Also disclosed are compositions that are related to those methods. | 04-07-2011 |
| 20140309232 | BIOENGINEERING STRAIN FOR PRODUCTION OF NOVEL MICROORGANISM-ORIGINATED FUNGICIDES AND USES THEREOF - The present invention relates to a bioengineering strain for production of novel microorganism-originated fungicides and uses thereof. The bioengineering strain for production of microorganism-originated fungicides of the present invention is obtained by transforming a phzH gene recombination expression plasmid into a strain producing phenazine-1-carboxylic acid, wherein the bioengineering strain produces phenazine-1-carboxamide. The present invention utilizes an existing strain producing phenazine-1-carboxylic acid to carry the phzH gene recombination expression plasmid, thereby achieving efficient expression of the phzH gene and transforming phenazine-1-carboxylic acid into phenazine-1-carboxamide. The present invention further discloses uses of the bioengineering strain, including a microorganism-originated fungicide produced by the bioengineering strain through fermentation, and preparation and application of the microorganism-originated fungicide. The antifungal activity of phenazine-1-carboxamide is not influenced by the acidity under which it is used, so that it has a stabilized antifungal activity and can be more effective in prophylaxis and treatment of crop diseases. | 10-16-2014 |
| 20140194435 | NOVEL SUBSTITUTED INDOLO 4,3 FG QUINOLINES USEFUL FOR TREATING MIGRAINE - Provided herein are novel ergoline derivatives and pharmaceutical compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT | 07-10-2014 |
| 20140194434 | NOVEL SUBSTITUTED INDOLO 4,3 FG QUINOLINES USEFUL FOR TREATING MIGRAINE - Provided herein are novel ergoline derivatives and pharmaceutical compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT | 07-10-2014 |
| 20110136817 | Methods of identifying responders to dopamine agonist therapy - The present invention is directed to a method of identifying patients to be treated by dopamine agonist therapy comprising the step of analyzing a plasma or urine sample from said patient for concentrations of norepinephrine (NE), norepinephrine metabolites (NE metabolites), dopamine, dopamine metabolites, serotonin, serotonin metabolites, or fasting triglycerides, wherein one or more of: (a) NE metabolites, (b) NE/NE metabolites:dopamine/dopamine metabolites, (c) NE and serotonin, (d) NE/NE metabolites and serotonin, (e) NE and serotonin metabolites, (f) NE/NE metabolites and serotonin metabolites, or (g) NE is/are greater than about 30% over normal level; or dopamine/dopamine metabolites are less than about 30% below normal; or fasting triglycerides are greater than about 150 mg/dl and/or said patient has blood pressure of greater than about 135/85 mm Hg. The present invention is also directed to treating identified patients with dopamine agonist therapy. | 06-09-2011 |
| 20130310392 | PHARMACEUTICAL FORMULATION FOR TOPICAL ADMINISTRATION COMPRISING B220 - A pharmaceutical composition for topical administration including 2,3-dimethyl-6-(N,N-dimethylaminoethyl)-6H-indolo-(2,3-b)quinoxaline (B-220) or a pharmaceutically acceptable salt thereof in a pharmaceutically acceptable carrier. The composition is useful for the treatment of herpes virus infections of the skin or mucous membranes in a mammal subject. | 11-21-2013 |
| 20120040990 | INDOL-3-Y-CARBONYL-PIPERIDIN AND PIPERAZIN-DERIVATIVES - The present invention relates to indol-3-yl-carbonyl-piperidin and piperazin derivatives which act as V1a receptor antagonists and which are represented by Formula I: | 02-16-2012 |
| 20100179158 | INHIBITORS OF CYCLIC AMP PHOSPHODIESTERASES - Recombinant fission yeast cells and methods of using them are described, which provide for identification of chemical and biological inhibitors or activators of a target exogenous phosphodiesterase (PDE). The invention provides, in some aspects, compounds that inhibit cAMP PDE activity and compositions that include such compounds. The invention, in part, also includes methods of using cAMP PDE-inhibiting compounds in the treatment of cAMP PDE-associated diseases and/or disorders. | 07-15-2010 |
| 20140315911 | DIHYDROPTERIDINONES - Compounds of Formula I, as shown below and defined herein: pharmaceutically acceptable salts thereof, synthesis, intermediates, formulations, and methods of disease treatment therewith, including treatment of cancers, such as tumors driven or mediated at least in part by RSK. This Abstract is not limiting of the invention. | 10-23-2014 |
| 20110105517 | THERAPEUTIC AGENT FOR AMYOTROPHIC LATERAL SCLEROSIS - Disclosed is a safe and effective therapeutic agent that can alleviate the symptoms of the intractable disease ALS and slow the progress thereof. The therapeutic agent for amyotrophic lateral sclerosis contains bromocriptine or a pharmaceutically acceptable salt thereof as the active ingredient. | 05-05-2011 |
| 20100009999 | ALKYL SUBSTITUTED INDOLOQUINOXALINES - Novel substituted indoloquinoxalines of formula (I | 01-14-2010 |
| 20100137327 | NOVEL SEMICARBAZIDE AND CARBONYLHYDRAZIDE DERIVATIVES USEFUL AS POTASSIUM CHANNEL MODULATORS - This invention relates to novel semicarbazide and carbonylhydrazide derivatives that are found to be potent modulators of potassium channels and, as such, they are valuable candidates for the treatment of diseases or disorders as diverse as those which are responsive to modulation of potassium channels. | 06-03-2010 |
| 20130345230 | METHODS AND COMPOSITIONS FOR MODULATING CALCIUM CHANNELS - The present invention relates to methods and compositions for modulating calcium channels. In particular, the present invention provides methods and compositions for modulating (e.g., disrupting) Cav1.3a calcium channels for research and therapeutic methods (e.g., treating dopaminergic diseases and conditions). | 12-26-2013 |
| 20090325971 | Pentacyclic Alkaloid Compounds and Methods of Use Thereof - The present invention relates to Pentacyclic Alkaloid Compounds, compositions comprising an effective amount of a Pentacyclic Alkaloid Compound and methods for treating or preventing cancer, a bacterial infection, a fungal infection, or a yeast infection, comprising administering to a subject in need thereof an effective amount of a Pentacyclic Alkaloid Compound. The present invention also relates to compounds and methods that are useful for making Cribrostatin IV. | 12-31-2009 |
| 20100120781 | Novel Compounds for Treatment of Cancer and Disorders Associated with Angiogenesis Function - Novel compounds for treatment of cancer and disorders associated with angiogenesis function. Also disclosed are a method of preparing the compounds, pharmaceutical compositions and packaged products containing the compounds, a method of using these molecules to treat cancer (e.g., leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, renal cancer, and prostate cancer) and disorders associated with angiogenesis function (e.g., age-related macular degeneration, macular dystrophy, and diabetes), a method of monitoring the treatment, a method of profiling gene expression, and a method of modulating cell growth, cell cycle, apoptosis, or gene expression. | 05-13-2010 |
| 20100120782 | ENDOPARASITICIDAL GEL COMPOSITION - A homogenous, clear, veterinary gel composition which has a broad spectrum of efficacy against endoparasites over a prolonged period of time and which allows for higher concentrations of a mixture of parasiticidal agents in a single application. This composition is useful for treating and controlling endoparasiticidal infection and infestation in a homeothermic animal. | 05-13-2010 |
| 20100120780 | TREATMENTS FOR PREMATURE EJACULATION IN HUMANS - Provided are methods and compositions for the treatment of a sexual dysfunction such as premature ejaculation. In certain embodiments, a NMDA antagonist (e.g., dextromethorphan) is administered to a subject in combination with tramadol or a tramadol derivative to treat premature ejaculation. In certain embodiments, a capsaicinoid (e.g., capsaicin) and/or a phosphodiesterase type V inhibitor (e.g., sildenafil citrate) are further administered to the subject. Pharmaceutical preparations such as tablets and capsules are provided. | 05-13-2010 |
| 20100093744 | THIOGLUCOSE SPIROKETAL DERIVATIVE AND USE THEREOF AS THERAPEUTIC AGENT FOR DIABETES - The present invention provides a compound represented by Formula (II): | 04-15-2010 |
| 20140221380 | SUBSTITUTED SPIROPYRIDO[1,2-a]PYRAZINE DERIVATIVE AND PHARMACEUTICAL USE OF SAME AS HIV INTEGRASE INHIBITOR | 08-07-2014 |
| 20140323491 | SUBSTITUTED HETEROCYCLE FUSED GAMMA-CARBOLINES SOLID - The present invention relates to toluenesulfonic acid addition salt crystals of specific substituted heterocycle fused gamma-carbolines, the method of making and using such crystals. | 10-30-2014 |
| 20140357643 | Derivatives of Betulin - The present invention relates to compounds characterized by having a structure according to the following Formula I: | 12-04-2014 |
| 20110152280 | NOVEL ERGOLINE ANALOGS - Provided herein are novel ergoline derivatives and pharmaceutical compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT | 06-23-2011 |
| 20140275099 | METHODS FOR TREATING HCV - The present invention features interferon- and ribavirin-free therapies for the treatment of HCV. Preferably, the treatment is over a shorter duration of treatment, such as no more than 12 weeks. In one aspect, the treatment comprises administering at least two direct acting antiviral agents without interferon and ribavirin to a subject with HCV infection, wherein the treatment lasts for 12 weeks, and said at least two direct acting antiviral agents comprise (a) Compound 1 or a pharmaceutically acceptable salt thereof and (b) Compound 2 or a pharmaceutically acceptable salt thereof. | 09-18-2014 |
| 20140288085 | Methods for the Treatment of Cardiovascular Conditions - Provided herein are methods and systems for the treatment of cardiovascular conditions, including pulmonary hypertension (PH), in subjects that are being treated with a treatment regimen that includes a phosphodiesterase-5 (PDE-5) inhibitor. | 09-25-2014 |
| 20110160219 | Inhibitors of Phosphodiesterase Type 5A for Treating or Preventing Muscle Disease or the Symptoms Thereof in a Patient - Disclosed are pharmaceutical compositions and methods for treating or preventing muscle diseases or the symptoms thereof. The compositions typically include and the methods typically utilize phosphodiesterase type 5A inhibitors. | 06-30-2011 |
| 20110160218 | COMPOSITIONS COMPRISING MACROCYCLIC LACTONE COMPOUNDS AND SPIRODIOXEPINOINDOLES - The present invention provides formulations which may comprise macrocyclic lactones and at least one spirodioxepinoindole derivative or a spirooxepinoindole derivative for combating parasites in birds and mammals. The invention also provides for an improved method for eradicating, controlling and preventing parasite infestation in birds and mammals. | 06-30-2011 |
| 20110160217 | DEUTERIUM ENRICHED ANALOGUES OF TADALAFIL AS PDE5 INHIBITORS - The present invention relates to derivatives of tadalafil, substituted with fluorine on the methylene carbon atom situated between the oxygens of the benzodioxol ring, and optionally further substituted with deuterium atoms in place of normally abundant hydrogen, and | 06-30-2011 |
| 20100197695 | ANTITUMORAL DERIVATIVES OF ET-743 - Derivatives of Et-743 or Et-770 or Et-729 are provided. The derivatives are of the general formula Ia.: | 08-05-2010 |
| 20100035887 | THERAPEUTIC COMPOUNDS FOR BLOCKING DNA SYNTHESIS OF POX VIRUSES - This invention provides methods of inhibiting replication of a poxvirus by contacting a poxvirus with a compound having formula I, formula XXI, formula XXXII, or formula XLI which in turn reduce, inhibit, or abrogate poxvirus DNA polymerase activity and/or its interaction with its processivity factor. Formula I, formula XXI, formula XXXII, or formula XLI can be utilized to treat humans and animals suffering from a poxvirus infection. Pharmaceutical compositions for treating poxvirus infected subjects are also provided. | 02-11-2010 |
| 20120178760 | Heterocyclic-Fused Pyrazolo[4,3-c] Pyridin-3-One M1 Receptor Positive Allosteric Modulators - The present invention is directed to heterocyclic fused pyrazole[4,3-c]pyridine-3-one compounds of formula (I): which are M1 receptor positive allosteric modulators and that are useful in the treatment of diseases in which the M1 receptor is involved, such as Alzheimer's disease, schizophrenia, pain or sleep disorders. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatment of diseases mediated by the M1 receptor. | 07-12-2012 |
| 20120178759 | CONDENSED PYRIDINE DERIVATIVES USEFUL AS POTENT INHIBITORS OF THE PROTEIN KINASE CK2 - The invention relates to the use of specific compounds of formula (I) and their pharmaceutically-acceptable salts: (Formula 1) (I) as a new family of protein kinase CK2 inhibitors; the invention also relates to the use of compounds of formula (I) for the preparation of pharmaceutical compositions for the prevention and/or treatment of disorders and/or diseases chosen Camongst cancers; autoimmune and inflammatory diseases; infectious diseases; diabetes angiogenesis related disorders; retinopathies and cardiac hypertrophy. | 07-12-2012 |
| 20130172361 | ASSAYS AND METHODS FOR SELECTING A TREATMENT REGIMEN FOR A SUBJECT WITH DEPRESSION - Disclosed herein are novel assays, systems and kits for selecting a treatment regimen for a subject with depression by identifying at least one nucleic acid polymorphism, e.g., but not limited to, at the MTHFR, MTR, or MTRR locus, and/or determining expression levels of peripheral biomarkers (e.g., SAM, SAH, and 4-HNE) in a test sample from a human subject. These biomarkers can be used to determine the effectiveness of treating a depressed subject with a folate-containing compound (alone or as an adjunct to an antidepressant). Additionally, these biomarkers can be used to select an appropriate treatment regimen for subjects with treatment-resistant depression (e.g., resistant to at least one selective serotonin reuptake inhibitor). Methods and compositions for treating a subject with depression and/or determining or improving the effectiveness of an antidepressant drug taken by a subject are also provided herein. | 07-04-2013 |
| 20100168119 | COMPOSITIONS AND METHODS FOR MINIMIZING OR REDUCING AGONIST-INDUCED DESENSITIZATION - Methods and compositions are provided for preventing or reversing loss of the therapeutic effect of a drug, where the loss is associated with the repeated administration of the drug to a patient. The method includes administering to the patient a dopamine receptor agonist or partial agonist or a drug that increases the extracellular level of dopamine by enhancing release of dopamine, decreasing the removal of dopamine from the extracellular space, enhancing the synthesis of dopamine within the brain, or decreasing metabolic degradation of dopamine; and also administering to the patient an opioid receptor antagonist in an ultra-low dose amount, wherein the ultra-low dose amount is effective to prevent or reverse loss of therapeutic effects associated with the repeated administration of the drug to the patient. The methods are useful for various treatments, including treating Parkinson's Disease, Restless Leg Syndrome, depression, schizophrenia, psychostimulant drug abuse, or attention deficit disorder. | 07-01-2010 |
| 20140296244 | METHOD FOR TREATING A PULMONARY HYPERTENSION CONDITION - A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years. | 10-02-2014 |
| 20100249143 | METHOD FOR INHIBITING GROWTH OF CANCER CELLS AND CELL TELOMERE AND DISEASES OF CELL PROLIFERATION BY USING HETEROANNELATED ANTHRAQUINONE DERIVATIVE COMPOUNDS - A heteroannelated anthraquinone derivative compound is provided. The heteroannelated anthraquinone derivative compound is represented by a formula (I): | 09-30-2010 |
| 20140329823 | Dimeric IAP Inhibitors - Molecular mimics of Smac are capable of modulating apoptosis through their interaction with cellular IAPs (inhibitor of apoptosis proteins). The mimetics are based on a monomer or dimer of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac/DIABLO, Hid, Grim and Reaper, which interact with a specific surface groove of IAP. Also disclosed are methods of using these peptidomimetics for therapeutic purposes. In various embodiments of the invention the Smac mimetics of the invention are combined with chemotherapeutic agents, including, but not limited to topoisomerase inhibitors, kinase inhibitors, NSAIDs, taxanes and platinum containing compounds use broader language | 11-06-2014 |
| 20130289041 | QUINOXALINE COMPOUNDS AND USES THEREOF - Disclosed herein are compounds of formula (I) and methods of inhibiting IKKβ and the NF-κB signaling and mTOR pathways. | 10-31-2013 |
| 20100160334 | TRICYCLIC ANILIDE SPIROLACTAM CGRP RECEPTOR ANTAGONISTS - The present invention is directed to compounds of Formula I: I (where A | 06-24-2010 |
| 20100190799 | PHENAZINE COMPOUNDS AND USE THEREOF IN AUTOIMMUNE AND INFLAMMATORY DISEASES - The invention discloses compounds, compositions and methods useful for preventing and/or treating autoimmune diseases and inflammatory diseases. The methods and compositions utilize water-soluble phenazine compounds, or salts, or solvates thereof. These molecules can be delivered alone or in combination with agents which treat or prevent autoimmune diseases and inflammatory diseases such as those caused by arthritis and rheumatoid arthritis. | 07-29-2010 |
| 20150342889 | TABLETS WITH IMPROVED ACCEPTANCE AND GOOD STORAGE STABILITY - The present invention relates to tablets for animals, having improved acceptance and good storage stability. | 12-03-2015 |
| 20110034473 | NOVEL (PYRROLOQUINOXALINYL) PYRAZINECARBOHYDRAZIDE-OXALIC ACID CO-CRYSTAL FOR TREATMENT OF CANCER AND OTHER DISEASES - A novel co-crystal of N′-(7-fluoropyrrolo[1,2a]quinoxalin-4-yl)pyrazine-2-carbohydrazide with oxalic acid is disclosed. The disclosed oxalic acid co-crystal demonstrates cancer cell growth inhibition and is more bioavailable than the corresponding free base when administered as a suspension. | 02-10-2011 |
| 20110034472 | Novel Compounds for Treatment of Cancer and Disorders Associated With Angiogenesis Function - Novel compounds for treatment of cancer and disorders associated with angiogenesis function. Also disclosed are a method of preparing the compounds, pharmaceutical compositions and packaged products containing the compounds, a method of using these molecules to treat cancer (e.g., leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, renal cancer, and prostate cancer) and disorders associated with angiogenesis function (e.g., age-related macular degeneration, macular dystrophy, and diabetes), a method of monitoring the treatment, a method of profiling gene expression, and a method of modulating cell growth, cell cycle, apoptosis, or gene expression. | 02-10-2011 |
| 20120135998 | COMPOUNDS FOR TREATING RESPIRATORY SYNCYTIAL VIRUS INFECTIONS - The present invention relates to compounds of formula (I), racemates, isomers and/or salts thereof useful in the treatment of viral infections, in particular respiratory syncytial virus (RSV) infections. The present invention also relates to processes for preparing the compounds. | 05-31-2012 |
| 20130289042 | DIMERIC IAP INHIBITORS - Molecular mimics of Smac are capable of modulating apoptosis through their interaction with cellular IAPs (inhibitor of apoptosis proteins). The mimetics are based on a monomer or dimer of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac/DIABLO, Hid, Grim and Reaper, which interact with a specific surface groove of IAP. Also disclosed are methods of using these peptidomimetics for therapeutic purposes. In various embodiments of the invention the Smac mimetics of the invention are combined with chemotherapeutic agents, including, but not limited to topoisomerase inhibitors, kinase inhibitors, NSAIDs, taxanes and platinum containing compounds use broader language | 10-31-2013 |
| 20100137328 | TRICYCLIC ANILIDE HETEROCYCLIC CGRP RECEPTOR ANTAGONISTS - Compounds of formula I: wherein variables A | 06-03-2010 |
| 20140243348 | COMPOSITIONS AND METHODS FOR TREATING HERPES VIRUSES - Compositions and methods that are useful for the treatment of herpesvirus infection (including herpes simplex virii) are disclosed. Methods for identifying compounds useful for the treatment of herpesvirus infection are also disclosed. | 08-28-2014 |
| 20150094313 | PHARMACEUTICAL FORMULATIONS OF ECTEINASCIDIN COMPOUNDS - Ecteinascidin formulations, methods of preparing the same, articles of manufacture and kits with such formulations, and methods of treating proliferative diseases with the same formulations are provided. | 04-02-2015 |
| 20100099687 | TADALAFIL SOLID COMPOSITES - This invention relates to oral pharmaceutical compositions suitable for making pharmaceutical formulations for oral administration that provide for the rapid dissolution of the phosphodiesterase 5 inhibitor tadalafil. In particular, the pharmaceutical compositions comprise solid composites of tadalafil exhibiting high solubility and rate of dissolution. The invention further relates to methods of preparing these pharmaceutical formulations and the use of such pharmaceutical formulations for treating diseases associated with PDE5 inhibitors. | 04-22-2010 |
| 20150080406 | LIVER X RECEPTOR MODULATORS - Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described. | 03-19-2015 |
| 20100179159 | METHOD FOR THE PRODUCTION OF A MEDICAMENT CONTAINING TADALAFIL - The invention relates to a method for producing a medicament containing tadalafil. In said method, tadalafil is mixed with suitable adjuvants and is heated to a temperature of about 100° C. to about 200° C., preferably about 150° C. to about 200° C., especially about 200° C. | 07-15-2010 |
| 20140336197 | SUBSTITUTED IMIDAZO [1,5-a]QUINOXALINES AS A PDE9 INHIBITOR - The invention discloses quinoxaline derivatives or salts thereof having PDE9-inhibiting activity and being useful as treating agent of dysuria and the like, which are represented by the formula (I) | 11-13-2014 |
| 20140135339 | MACROCYCLIC DERIVATIVES FOR THE TREATMENT OF DISEASES - The invention relates to compounds of formula (Φ) | 05-15-2014 |
| 20150336963 | LIVER X RECEPTOR MODULATORS - Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described. | 11-26-2015 |
| 20150336884 | NOVEL SYNTHETIC ANTIOXIDANTS AND THEIR USES - The present invention relates to synthetic organic antioxidants of small molecules. The novel dithiol-containing compounds in this invention possess strongest possible capability as both scavenger for free radicals and antioxidant. This invention is directed to novel molecules as prodrugs of the novel dithiol-containing compounds, their rational design, their feasible preparation route by means of synthetic organic chemistry, and their potential uses in application to treatment and/or prevention of major diseases associated with oxidative stress, such as Alzheimer's disease, Parkinson's disease, cancer, diabetes, HIV, acne, cardiovascular disease, renal disease, hypertension, hypercholesterolemia, hyperlipidemia, rheumatoid arthritis, inflammation, pain, aging, stroke, cataract, glaucoma, age-related macular degeneration, etc. | 11-26-2015 |
| 20150335641 | Method Of Treating Metabolic Disorders And Depression With Dopamine Receptor Agonists - This invention relates to methods and formulations for treating metabolic disorders and depression. In some embodiments, the methods comprise administering a dopamine receptor agonist and an anti-depressant. | 11-26-2015 |
| 20140275098 | COMPOSITIONS AND METHODS OF TREATING PULMONARY HYPERTENSION - Provided are formulations comprising therapeutically effective amounts of ambrisentan or a pharmaceutically acceptable salt thereof and tadalafil or a pharmaceutically acceptable salt thereof and methods of treating and/or preventing pulmonary hypertension by administration of the formulations. | 09-18-2014 |
| 20120015953 | METHODS AND COMPOSITIONS FOR THE TREATMENT OF ALLERGY - The present invention relates to compositions comprising an antagonist of the histamine H1 receptor and a compatible antagonist of the histamine H4 receptor. The antagonist compounds are selected to prevent the H4 receptor antagonist from interfering with the H1 receptor antagonist's suppression of acute phase allergic responses in a patient. The present invention also relates to compositions comprising a mast cell stabilizer and a compatible antagonist of the histamine H4 receptor. | 01-19-2012 |
| 20120202821 | CONFORMATIONALLY CONSTRAINED, FULLY SYNTHETIC MACROCYCLIC COMPOUNDS - Conformationally restricted, spatially defined 12-30 membered macrocyclic ring systems of type (I) are constituted by three distinct building blocks: an aromatic template a, a conformation modulator b and a spacer moiety c as detailed in the description and the claims. Macrocycles of type (I) are readily manufactured by parallel synthesis or combinatorial chemistry. They are designed to interact with specific biological targets. In particular, they show agonistic or antagonistic activity on the motilin receptor (MR receptor), on the serotonin receptor of subtype 5-HT | 08-09-2012 |
| 20100267732 | Prognostic Molecular Markers for ET-743 Treatment - The present invention relates to the use of ecteinascidin 743 in human patients having certain molecular markers profile which has been associated with the outcome of ET-743 chemotherapy. In particular, the invention relates to the use of ecteinascidin 743 in patients having high expression levels of XPG mRNA or protein and/or having a “wild type” genotype for Asp1104His SNP of XPG gene. | 10-21-2010 |
| 20130252961 | MACROCYCLIC DERIVATIVES FOR THE TREATMENT OF DISEASES - The invention relates to compounds of formula (Φ) | 09-26-2013 |
| 20140005202 | Inhibitors of Phosphodiesterase Type 5A for Treating or Preventing Muscle Disease or the Symptoms Thereof in a Patient | 01-02-2014 |
| 20150018359 | POLYCYCLIC-CARBAMOYLPYRIDONE COMPOUNDS AND THEIR PHARMACEUTICAL USE - Compounds for use in the treatment of human immunodeficiency virus (HIV) infection are disclosed. The compounds have the following Formula (I): | 01-15-2015 |
| 20110053947 | Arylchalcogenoarylalkyl-substituted imidazolidine-2,4-diones, process for preparation thereof, medicaments comprising these compounds and use thereof - The invention relates to compounds of formula (I) wherein the groups R and R′, A, D, E, G, L, p and R1 to R10 have the stated meanings and to their physiologically compatible salts. Said compounds are suitable, for example, as anti-obesity drugs. | 03-03-2011 |
| 20130005734 | THERAPEUTIC COMPOSITIONS - The invention relates to a product containing the compound of formula (I) below (I) or a pharmaceutically acceptable salt of this compound, in combination with at least one compound having PDE5-inhibitory properties, or a pharmaceutically acceptable salt thereof, for therapeutic use, simultaneously, separately or over a period of time, in the treatment of a disease wherein vasoconstriction is involved. | 01-03-2013 |
| 20130252962 | SPIRO-OXINDOLE COMPOUNDS AND THEIR USE AS THERAPEUTIC AGENTS - This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain. | 09-26-2013 |
| 20130296330 | MACROCYCLIC INTEGRASE INHIBITORS FOR USE IN THE TREATMENT OF FELINE IMMUNODEFICIENCY VIRUS - This invention concerns to naphthyridin derivatives of formula (I) for use in the treatment or prevention of feline immunodeficiency virus (FIV). Furthermore the present invention relates to a method of treating or preventing infection of feline immunodeficiency virus in a feline animal wherein said method comprises the administration to said feline animal of a therapeutically effective amount of a naphthyridin derivative. | 11-07-2013 |
| 20090306089 | COMPOUNDS - Compounds of Formula (I) or pharmaceutically acceptable salts or N-oxides thereof: | 12-10-2009 |
| 20150051214 | LIVER X RECEPTOR MODULATORS - Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described. | 02-19-2015 |
| 20150011557 | Benzyl Piperidine Compounds as Lysophosphatidic Acid (LPA) Receptor Antagonist - The invention provides novel substituted benzyl piperidine compounds according to Formula (I) as lysophosphatidic acid (LPA) receptor antagonists, their manufacture and use for the treatment of proliferative or inflammatory diseases, such as cancer, fibrosis or arthritis. | 01-08-2015 |
| 20090318459 | Therapeutic Compositions Comprising a Specific Endothelin Receptor Antagonist and a PDE5 Inhibitor - The invention relates to a product containing the compound of formula (I) below | 12-24-2009 |
| 20090318458 | NOVEL COMPOUNDS AND USE THEREOF - A semiautomatic vehicle gearbox comprising, for said gearbox, a shift lever ( | 12-24-2009 |
| 20100075974 | HETEROCYCLIC GPR40 MODULATORS - The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula I: | 03-25-2010 |
| 20120115875 | POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE HAVING HIV INTEGRASE INHIBITORY ACTIVITY - The present invention is to provide a novel compound (I) shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. | 05-10-2012 |
| 20130225595 | METHOD FOR TREATING PULMONARY ARTERIAL HYPERTENSION IN A PATIENT NOT HAVING IDIOPATHIC PULMONARY FIBROSIS - There is provided a method of treating pulmonary hypertension in a patient in need thereof, said method comprising: administering a therapeutically effective amount of ambrisentan to the patient with pulmonary arterial hypertension, wherein the patient has been determined not to have idiopathic pulmonary fibrosis. | 08-29-2013 |
| 20130116262 | BICYCLIC PIPERAZINE COMPOUNDS - Bicyclic piperazine compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 05-09-2013 |
| 20100081664 | METHOD OF THERAPEUTIC ADMINISTRATION OF DHE TO ENABLE RAPID RELIEF OF MIGRAINE WHILE MINIMIZING SIDE EFFECT PROFILE - Pharmaceutical compositions containing dihydroergotamine (DHE) and methods in which DHE is administered to patients for treatment of migraine without side effects or adverse effects are disclosed. Methods for rapid treatment of migraine with DHE are disclosed comprising: dampening the peak plasma concentration (C | 04-01-2010 |
| 20100081663 | METHOD OF THERAPEUTIC ADMINISTRATION OF DHE TO ENABLE RAPID RELIEF OF MIGRAINE WHILE MINIMIZING SIDE EFFECT PROFILE - Pharmaceutical compositions containing dihydroergotamine (DHE) and methods in which DHE is administered to patients for treatment of migraine without side effects or adverse effects are disclosed. Methods for rapid treatment of migraine with DHE are disclosed comprising: dampening the peak plasma concentration (C | 04-01-2010 |
| 20130040957 | Deuterium-Enriched Pyrimidine Compounds and Derivatives - The present invention is concerned with deuterium-enriched pyrimidine compounds of formula I, their derivatives, enantiomers, diastereomers, solvates and pharmaceutical salts thereof, | 02-14-2013 |
| 20130197005 | Parenteral Formulations Of Dopamine Agonists - This invention relates to stable pharmaceutical compositions for parenteral administration comprising dopamine agonists and peripheral acting agents useful for treatment of metabolic disorders or key elements thereof. The parenteral dosage forms exhibit long stable shelf life and distinct pharmacokinetics. | 08-01-2013 |
| 20150031701 | COMPOSITIONS AND METHODS FOR PREVENTING AND TREATING MUCOSITIS AND WEIGHT LOSS - Pharmaceutical compositions comprising 5-[2-pyrazinyl]-4-methyl-1,2-3-thione or an analogue, derivative, metabolite, prodrug, solvate or a pharmaceutically acceptable salt thereof; and a pharmaceutical carrier, which promotes association with the outer wall of a subject's digestive tract are described as well as their uses in treating and preventing mucositis and cachexia. | 01-29-2015 |
| 20150018362 | COMPOSITIONS AND METHODS FOR TREATING MITOCHONDRIAL DISEASES - The invention described herein relates to methods for treating mitochondrial diseases. In particular, the invention relates to methods for treating mitochondrial diseases by administering therapeutically effective amounts of one or more tetracyclic pyrazinoindoles, and/or pharmaceutically acceptable salts thereof. | 01-15-2015 |
| 20150018361 | ANTI-TUMOR ACTIVITY OF REDUCED FOLATES LIKE METHYLENE-TETRAHYDROFOLATE - The present invention relates to methylene-tetrahydrofolate for use in the treatment of cancer, based on its intrinsic antitumor activity. The cancers that may be treated include breast cancer, gastric cancer, gastrointestinal cancer, gall bladder cancer, bile duct cancer, colon cancer, rectal cancer, liver cancer, pancreatic cancer, head and neck cancer, esophageal cancer, mesothelioma cancer, lung cancer including non-small-cell lung cancer, ovarian cancer, endometrial cancer, cervical cancer, peripheral cell lymphoma (PTCL), melanoma, brain tumors, adenocarcinoma, esophageal cancer, and osteosarcoma. | 01-15-2015 |
| 20150018360 | COMPOSITIONS AND METHODS FOR TREATING METABOLIC DISORDERS - The present invention provides, inter alia, compositions containing enantiomerically pure (R)(+)-amisulpride or enantiomerically pure (R)(+)-sulpiride, optionally with dopamine receptor modulators. The present invention also provides compositions containing racemic (RS)-amisulpride or (RS)-sulpiride in combination with dopamine receptor modulators. Methods for preventing, treating, or ameliorating the effects of a metabolic disorder or key element thereof, for modulating blood glucose levels, and for preventing, treating, or ameliorating the effects of diabetes in a subject are also provided. Additionally, the present invention provides methods for counter-acting the dopamine antagonist activity of (S)-amisulpride in racemic (RS)-amisulpride, or the dopamine antagonist activity of (S)-sulpiride in racemic (RS)-sulpiride, administered to a subject to prevent, treat, or ameliorate the effects of a metabolic disorder. | 01-15-2015 |
| 20130029997 | PYRAZINOISOQUINOLINE COMPOUNDS - This invention in one embodiment is directed to a compound of Formula Ia; | 01-31-2013 |
| 20150080404 | NOVEL COMPOSITIONS AND METHODS - The present invention relates to use of particular substituted heterocycle fused gamma-carbolines as described herein, in free, pharmaceutically acceptable salt or prodrug form, and pharmaceutical composition comprising the same optionally in combination with one or more agents, for the prophylaxis or treatment of one or more disorders associated with dementia, particularly behavioral or mood disturbances (e.g., agitation/aggression), psychosis, depression and sleep disturbances among others in patients suffering from dementia. | 03-19-2015 |
| 20150080405 | COMPOUNDS, COMPOSITIONS AND METHODS OF AGELASTATIN ALKALOIDS - The present invention, among other things, provides compounds, compositions and methods for treatment of cancer. In some embodiments, the present invention provides methods for treating blood cancer using agelastatin alkaloids. | 03-19-2015 |
| 20160137666 | SUBSTITUTED CYCLOPENTA[4,5]OXAZOLO[3,2-a]PYRIDO[1,2-d]PYRAZINES AS HIV INTEGRASE INHIBITORS - The present invention is to provide a novel compound (I) shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof. | 05-19-2016 |
| 20120071484 | Topical Parasiticide Composition - A topical parasiticide composition comprising: (i) a phenyl pyrazole insecticide; and/or a neonicotinoid; (ii) a macrocylic lactone and/or an aminoacetonitrile derivatives; (iii) an Insect Growth Regulator; and (iv) a 2-acyl-4-oxo-1,2,3,6,7,11b-4H-pyrazino[2,1a]isoquinoline derivative. | 03-22-2012 |
| 20130035341 | MACROCYCLIC INTEGRASE INHIBITORS - Compound having formula I | 02-07-2013 |
| 20120088773 | Circadian rhythm modulation - A method and composition is herein described to modulate the circadian rhythm to effect summer metabolism and the metabolic syndrome. The method entails the once daily, timed ingestion of a dopamine precursor or a dopamine agonist, receptor primed with caffeine, and vitamin D | 04-12-2012 |
| 20150290137 | NOVEL METHOD FOR IMPROVING THE BIOAVAILABILITY OF LOW AQUEOUS SOLUBILITY DRUGS - The present invention relates to the implementation of a new method for manufacturing solid dosage forms for oral administration comprising poorly water soluble active ingredients which overcomes the associated solubility problems and affords improved dissolution profile. | 10-15-2015 |
| 20130296331 | COMPOSITIONS AND METHODS FOR AMELIORATING RENAL DYSFUNCTION INDUCED BY RENAL HYPOPERFUSION OR ACUTE KIDNEY INJURY - The invention provides compositions and methods for ameliorating renal dysfunction induced by renal hypoperfusion or acute kidney injury, resulting for example from increased intra-abdominal pressure, using phosphodiesterase inhibitors, more particularly phosphodiesterase type inhibitors, or pharmaceutically acceptable salts or solvates thereof. | 11-07-2013 |
| 20130296329 | QUINOXALINE COMPOUND - The present inventors have investigated a compound which has a PDE9-inhibitory action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, and bladder/urethral diseases, and the like, and thus, have found that an imidazoquinoxaline compound or a triazoloquinoxaline compound has a PDE9-inhibitory action, thereby completing the present invention. | 11-07-2013 |
| 20130137698 | SOLID ORAL FILM DOSAGE FORMS AND METHODS FOR MAKING SAME - Improved pharmaceutical solid oral film dosage forms for the buccal and/or sublingual delivery of pharmaceutical, nutraceutical or cosmetic ingredients are endowed with instant hydration potential and complete dissolution potentially enabling the active ingredient to become immediately available for enhanced buccal and/or sublingual absorption and/or reduced absorption through the gastrointestinal route. The improved delivery systems for solubilizing and stabilizing pharmaceutically active ingredients exhibit enhanced stability by the use of a combination of crystallization inhibitors, which together can maintain the active ingredient in a desired plurality of particles in an effective size range within a polymeric film matrix. | 05-30-2013 |
| 20130137697 | COMPOSITIONS, METHODS OF USE, AND METHODS OF TREATMENT - Briefly described, embodiments of this disclosure, among others, include compositions, pharmaceutical compositions, methods of treating nicotine dependence, methods of treating a subject who smokes and has a risk for depression or other neuropsychiatric disorder, method of treating a subject who smokes and has a risk for depression or other neuropsychiatric disorders, and the like. | 05-30-2013 |
| 20110065715 | Nogo Receptor Binding Small Molecules to Promote Axonal Growth - The present invention provides a method for identifying compounds which modulate the interaction of Nogo and Nogo receptor (NgR). The present invention also provides compounds that modulate the interaction of Nogo and Nogo receptor (NgR), the use of such compounds and compositions in the treatment or amelioration of conditions diseases or disorders, such as spinal cord injury, traumatic brain injury, stroke, multiple sclerosis, ALS, Huntington's disease, Alzheimer's disease, Parkinson's disease, epilepsy, Schizophrenia or schizoaffective disorders. | 03-17-2011 |
| 20120046297 | CRYSTALIZATION OF PHARMACEUTICAL COMPOUNDS - Novel crystalline forms of tadalafil suitable for pharmaceutical compositions in drug delivery systems for humans. | 02-23-2012 |
| 20160101103 | METHOD FOR THE PRODUCTION OF A MEDICAMENT CONTAINING TADALAFIL - The invention relates to a method for producing a medicament containing tadalafil. In said method, tadalafil is mixed with suitable adjuvants and is heated to a temperature of about 100° C. to about 200° C., preferably about 150° C. to about 200° C., especially about 200° C. | 04-14-2016 |
| 20100099686 | COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 04-22-2010 |
| 20130317036 | FOLIC ACID - RAMIPRIL COMBINATION: CELLPROTECTIVE, NEUROPROTECTIVE AND RETINOPROTECTIVE OPHTALMOLOGIC COMPOSITIONS - The invention relates to a cellprotective, neuroprotective and retinoprotective composition. In an embodiment of the invention, said composition comprises (i) Ramipril or Ramiprilate and (ii) folic acid. The composition of the invention can be used, in particular, for the prevention of loss of vision, or even for improving visual acuity and visual field in normal subjects, as well as for treating ophthalmologic pathologies, in particular: glaucoma, diabetic retinopathy, age related macular degeneration, hereditary dystrophy of the retina, uveitis, ammetropia (myopia, presbyopia). This combination of active principles could also be used in general conditions for treating general pathologies (cancer . . . ). | 11-28-2013 |
| 20140235645 | Pyridine Compounds and Uses Thereof - The present invention is directed to pyridine compounds of Formula (I). Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds as therapeutic agents treating neurological and psychiatric disorders. | 08-21-2014 |
| 20140235644 | INDOLYL-SUBSTITUTED PYRAZINO-QUINOLINES AND THEIR USE FOR THE TREATMENT OF CANCER - The disclosure describes compounds of formula I, | 08-21-2014 |
| 20150141431 | PYRAZINOISOQUINOLINE COMPOUNDS - This invention in one embodiment is directed to a compound of Formula Ia; | 05-21-2015 |
| 20140113906 | COMPOUNDS FOR TREATING RESPIRATORY SYNCYTIAL VIRUS INFECTIONS - The present invention relates to compounds of formula (I) or salts, racemates, isomers and/or prodrugs thereof useful in the treatment of viral infections, in particular respiratory syncytial viral (RSV) infections. The present invention also relates to processes for preparing the compounds and intermediates used in their preparation. | 04-24-2014 |
| 20120004239 | Process for Preparing Quinoxaline Derivatives - The present invention provides an improved process for preparing a compound of formula (IIIA), an intermediate of the synthesis of varenicline. Also, the present invention provides an improved process for preparing varenicline, or a pharmaceutically acceptable salt or solvate thereof. Furthermore, the present invention provides a process for decolorizing varenicline, or a salt or solvate thereof. Still further, the present invention provides a process of preparing varenicline L-tartrate with improved yield. Still further, the present invention relates to the use of compound of formula (V), or a salt or solvate thereof, as a reference marker and reference standard for assessing the purity of varenicline, or a salt or solvate thereof. | 01-05-2012 |
| 20120004240 | INHIBITORS OF AKT ACTIVITY - The instant invention provides for substituted fused naphthyridine derivatives that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer. | 01-05-2012 |
| 20120122879 | COMPOUNDS USEFUL AS PROTEIN KINASE INHIBITORS - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 05-17-2012 |
| 20120122878 | COMBINATION PRODUCTS - The invention concerns the combinations of an mGluR modulator, e.g. an mGluR5 modulator and at least one of L-dopa, a dopamine modulator, e.g. a dopamine agonist, a dopa decarboxylase inhibitor or a catechol-O-methyl transferase inhibitor. | 05-17-2012 |
| 20160074396 | TADALAFIL FREE BASE-CONTAINING FILM DOSAGE FORM CONTAINING POLYETHYLENE GLYCOL-BASED POLYMER AND/OR VINYL PYRROLIDONE-BASED POLYMER AS DISPERSION STABILIZER - The present disclosure relates to a film formulation for oral administration, containing tadalafil free base and a method of preparing the same, and a film may be provided with maximized dispersion stability of tadalafil free base in the film by the addition of a dispersion stabilizing agent in small amounts without unique fragrance or favor that may appear when other dispersion stabilizing agents known in the art are used, and an extremely low likelihood that a reagglomeration phenomenon of tadalafil free base particles will occur, and an amount of bubbles generated may be significantly reduced during a production process. | 03-17-2016 |
| 20140107126 | NOVEL INHIBITOR COMPOUNDS OF PHOSPHODIESTERASE TYPE 10A - The present invention relates to compounds of the formula I, the N-oxides, tautomers, the prodrugs and the pharmaceutically acceptable salts thereof. | 04-17-2014 |
| 20120088774 | ACTIVE PHARMACEUTICAL INGREDIENT ADSORBED ON SOLID SUPPORT - The present invention belongs to the field of pharmaceutical industry and relates to dosage forms comprising active pharmaceutical ingredients (API) such as tadalafil, simvastatin, fenofibrate and lovastatin that are practically insoluble in water, adsorbed on a carrier. Furthermore it relates to an adsorbate comprising API being practically insoluble in water and to a process for the preparation of said adsorbate with non-polar solvent (s) such as chlorinated hydrocarbon, diisopropylethes and hexane. Furthermore the invention relates to a process for the preparation of the dosage form, as well as to the use of the adsorbate for the preparation of the dosage form. Moreover it relates to the dosage form for use in the treatment of erectile dysfunction, human immunodeficiency virus (HIV) infections and/or Acquired Immune Deficiency Syndrome (AIDS). | 04-12-2012 |
| 20140371229 | NEW THERAPEUTIC APPROACHES FOR TREATING PARKINSON'S DISEASE - The present invention relates to compositions and methods for the treatment of Parkinson's disease and related disorders. More specifically, the present invention relates to novel combinatorial therapies of Parkinson's disease and related disorders targeting the alpha-synuclein aggregation network. In particular, the invention relates to compounds which, alone or in combination(s), can effectively protect neuronal cells from alpha-synuclein aggregates. The invention also relates to methods of producing a drug or a drug combination for treating Parkinson's disease and to methods of treating Parkinson's disease or a related disorder. | 12-18-2014 |
| 20120172367 | MACROCYCLIC INTEGRASE INHIBITORS - Compound having formula (I), wherein —W is NH—, —N(CH | 07-05-2012 |
| 20140357642 | IP receptor agonist heterocyclic compounds - The present invention provides heterocyclic derivatives which activate the IP receptor. Activating the IP receptor signaling pathway is useful to treat many forms of PAH, pulmonary fibrosis and exert beneficial effects in fibrotic conditions of various organs in animal models and in patients. Pharmaceutical compositions comprising such derivatives are also encompassed. | 12-04-2014 |
| 20120157461 | Indolyl-Substituted Pyrazino-Quinolines and Their Use for the Treatment of Cancer - There is provided compounds of formula I, wherein the wedged bonds, R | 06-21-2012 |
| 20120157460 | TETRAHYDRO-AZACARBOLINE MCH-1 ANTAGONISTS, METHODS OF MAKING, AND USES THEREOF - The present invention relates to tetrahydro-azacarboline derivatives of formula (I): | 06-21-2012 |
| 20140371228 | NOVEL THERAPEUTIC AGENTS - The present invention includes a method of treating or preventing a disease or disorder such as a mycobacterial infection, a Gram-positive bacterium infection, a yeast infection, an inflammatory condition, an auto-immune disorder and/or a proliferative disorder in a subject in need thereof. The method comprises administering to the subject a therapeutically effective amount of at least one compound of the invention, which includes clofazimine derivatives. | 12-18-2014 |
| 20150099755 | NOVEL FLUOROERGOLINE ANALOGS - Provided herein are novel fluoroergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT | 04-09-2015 |
| 20150368262 | ALPHA HELIX MIMETICS AND METHODS RELATING THERETO - Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a chemical library relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed. | 12-24-2015 |
| 20120196869 | PYRROLOPYRAZINE-SPIROCYCLIC PIPERIDINE AMIDES AS MODULATORS OF ION CHANNELS - The invention relates to pyrrolopyrazine-spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 08-02-2012 |
| 20120208822 | PYRIMIDO-PYRROLO-QUINOXALINEDIONE INHIBITORS OF CYSTIC FIBROSIS TRANSMEMBRANE CONDUCTANCE REGULATOR PROTEIN AND USES THEREFOR - Provided herein are pyrimido-pyrrolo-quinoxalinedione (PPQ) compounds, and compositions comprising these compounds, that inhibit cystic fibrosis transmembrane conductance regulator (CFTR) mediated ion transport and that are useful for treating diseases and disorders associated with aberrantly increased CFTR chloride channel activity. The compounds, and compositions comprising the compounds, described herein are useful for treating diseases, disorders, and sequelae of diseases, disorders, and conditions that are associated with aberrantly increased CFTR activity, for example, polycystic kidney disease. The compounds may be used for inhibiting expansion or preventing formation of cysts in persons who have polycystic kidney disease. | 08-16-2012 |
| 20120232086 | FUSED TRICYCLIC COMPOUNDS WITH ADENOSINE A2a RECEPTOR ANTAGONIST ACTIVITY - The present invention relates to certain fused tricyclic heteroaryl rings compounds of the Formula (I) (also referred to herein as the “Fused Tricyclic Compounds”), wherein M, Q, U, W, X, Y, Z, R | 09-13-2012 |
| 20120232085 | 3,4-DIHYDRO-2H-PYRAZINO[1,2-A]INDOL-1-ONE DERIVATIVES ACTIVE AS KINASE INHIBITORS, PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS COMPRISING THEM - Compounds which are 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one derivatives or pharmaceutically acceptable salts thereof, their preparation process and pharmaceutical compositions comprising them are disclosed; these compounds are useful in the treatment of diseases caused by and/or associated with an altered protein kinase activity such as cancer, viral infection, prevention of AIDS development in HIV-infected individuals, cell proliferative disorders, autoimmune and neurodegenerative disorders; also disclosed is a process under Solid Phase Synthesis conditions for preparing the compounds of the invention and chemical libraries comprising a plurality of them. | 09-13-2012 |
| 20150307496 | NOVEL TRICYCLIC 3,4-DIHYDRO-2H-PYRIDO[1,2-a]PYRAZINE-1,6-DIONE DERIVATIVES AS GAMMA SECRETASE MODULATORS - The present invention is concerned with novel tricyclic 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-dione derivatives of Formula (I) | 10-29-2015 |
| 20150306096 | 8'-HYDROXY-DIHYDROERGOTAMINE COMPOUNDS AND COMPOSITIONS - 8′-Hydroxy-Dihydroergotamine (8′-OH DHE) medicinal compounds, compositions, and dosage forms containing such compositions are provided. Also provided herein are methods of treatment, prevention, or amelioration of diseases, conditions or disorders selected from amyotrophic lateral sclerosis (ALS), Parkinson's disease, stress/anxiety, nausea, emesis, aggression, pain, neuropathic pain, sleeplessness, insomnia, restless leg syndrome and depression using the compounds, compositions, dosage forms and administration techniques disclosed herein. | 10-29-2015 |
| 20120329806 | NOVEL FLUOROERGOLINE ANALOGS - Provided herein are novel fluoroergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT | 12-27-2012 |
| 20160000788 | USE OF ITK INHIBITORS FOR THE TREATMENT OF CANCER - This invention relates generally to the use of ITK (IL-2 inducible T-cell kinase) inhibitors for the treatment of patients who have melanoma or other solid tumors. Applicants demonstrate that ITK lentiviral small hairpin RNA knockdowns and a small molecule inhibitor can each decrease the proliferation and migration of melanoma cell lines and a small molecule inhibitor can be used to inhibit the growth of melanomas in vivo. | 01-07-2016 |
| 20140107127 | PYRAZINOISOQUINOLINE COMPOUNDS - This invention relates to novel compounds that are pyrazinoisoquinoline derivatives, and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel pyrazinoisoquinoline derivatives that are derivatives of praziquantel. 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 ad ministering an antihelminthic agent, such as praziquantel. | 04-17-2014 |
| 20140066449 | DIPYRIDINIUM DERIVATIVES - Compounds of Formula (I): α-x-β (I) and pharmaceutically acceptable salts and solvates thereof, wherein α, x, and β have the meanings as indicated in the specification, are useful for treating a disease or disorder characterised by pathologically proliferating cells, particularly cancer. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described. | 03-06-2014 |
| 20140066450 | NOVEL FLUOROERGOLINE ANALOGS - Provided herein are novel fluoroergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT | 03-06-2014 |
| 20140100233 | CRYSTALIZATION OF PHARMACEUTICAL COMPOUNDS - Novel crystalline forms of tadalafil suitable for pharmaceutical compositions in drug delivery systems for humans. | 04-10-2014 |
| 20160016962 | P2X7 MODULATORS - The present invention is directed to a compound of Formula (I) Formula (I) The invention also relates to pharmaceutical compositions comprising compounds of Formula (I) and methods comprising administering to a subject at least one compound selected from compounds of Formula (I) for treating diseases mediated by P2X7 receptor activity, such as rheumatoid arthritis, osteoarthritis, psoriasis, septic shock, allergic dermatitis, asthma, allergic asthma, mild to severe asthma, steroid resistant asthma, idiopathic pulmonary fibrosis, allergic rhinitis, chronic obstructive pulmonary disease; airway hyper-responsiveness, diseases of the nervous and neuro-immune system, acute and chronic pain states of neuropathic pain, inflammatory pain, spontaneous pain, opioid induced pain, diabetic neuropathy, postherpetic neuralgia, low back pain, chemotherapy-induced neuropathic pain, fibromyalgia, diseases involved with and without neuroinflammation of the central nervous system, mood disorders, major depression, major depressive disorder, treatment resistant depression, bipolar disorder, anxious depression, anxiety, cognition, sleep disorders, multiple sclerosis, epileptic seizures, Parkinson's disease, schizophrenia, Alzheimer's disease, Huntington's disease, autism, spinal cord injury and cerebral ischemia/traumatic brain injury, stress-related disorders, diseases of the cardiovascular, metabolic, gastrointestinal and urogenital systems such as diabetes, diabetes mellitus, thrombosis, irritable bowel syndrome, irritable bowel disease, Crohn's disease, ischemic heart disease, ischaemia, hypertension, cardiovascular disease, myocardial infarction, and lower urinary tract dysfunction such as incontinence, lower urinary tract syndrome, Polycystic Kidney Disease, Glomerulonephritis, skeletal disorders, osteoporosis, osteopetrosis, and glaucoma, interstitial cystitis, cough, ureteric obstruction, sepsis, Amyotrophic Lateral Sclerosis, Chaga's Disease, | 01-21-2016 |
| 20140179706 | FLUOROERGOLINE DERIVATIVES AND USES THEREOF - Provided herein are novel fluoroergoline derivatives and compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT | 06-26-2014 |
| 20140179707 | NOVEL ERGOLINE DERIVATIVES AND USES THEREOF - Provided herein are 8′-Hydroxy-2-CF3-dihydroergotamine (8′OH-2-CF3-DHE) compounds, compositions, and dosage forms containing such compositions. Also provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, migraine using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods of agonizing receptors such as, for example, the 5-HT | 06-26-2014 |
| 20140179705 | 8'-HYDROXY-DIHYDROERGOTAMINE COMPOUNDS AND COMPOSITIONS - 8′-Hydroxy-Dihydroergotamine (8′-OH DHE) medicinal compounds, compositions, and dosage forms containing such compositions are provided. Also provided herein are methods of treatment, prevention, or amelioration of diseases, conditions or disorders selected from amyotrophic lateral sclerosis (ALS), Parkinson's disease, stress/anxiety, nausea, emesis, aggression, pain, neuropathic pain, sleeplessness, insomnia, restless leg syndrome and depression using the compounds, compositions, dosage forms and administration techniques disclosed herein. | 06-26-2014 |
| 20140045856 | 4-Methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalenes - The invention relates to 4-methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalene derivatives of general formula (I) which are inhibitors of phosphodiesterase 2 and/or 10, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention. | 02-13-2014 |
| 20140038976 | PIPERAZINE DERIVATIVES AS CAV2.2 CALCIUM CHANNEL BLOCKERS - The invention relates to novel piperazine compounds; to processes for their preparation; to pharmaceutical compositions containing the compounds; and to the use of the compounds in therapy to treat diseases for which blocking the Ca | 02-06-2014 |
| 20140045857 | 4-Methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalenes - The invention relates to 4-methyl-2,3,5,9,9b-pentaaza-cyclopenta[a]naphthalene derivatives of general formula (I) which are inhibitors of phosphodiesterase 2 and/or 10, useful in treating central nervous system diseases and other diseases. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture the compounds according to the invention. | 02-13-2014 |
| 20160060263 | PYRAZINOISOQUINOLINE COMPOUNDS - This invention relates to novel compounds that are pyrazinoisoquinoline derivatives, and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel pyrazinoisoquinoline derivatives that are derivatives of praziquantel. 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 antihelminthic agent, such as praziquantel. | 03-03-2016 |
| 20120245179 | Method Of Therapeutic Administration of DHE To Enable Rapid Relief Of Migraine While Minimizing Side Effect Profile - Pharmaceutical compositions containing dihydroergotamine (DHE) and methods in which DHE is administered to patients for treatment of migraine without side effects or adverse effects are disclosed. Methods for rapid treatment of migraine with DHE are disclosed comprising: dampening the peak plasma concentration (C | 09-27-2012 |
| 20130237544 | CDK INHIBITORS - Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors. | 09-12-2013 |
| 20110224218 | METHOD FOR INHIBITING GROWTH OF CANCER CELLS AND CELL TELOMERE AND DISEASES OF CELL PROLIFERATION BY USING HETEROANNELATED ANTHRAQUINONE DERIVATIVE COMPOUNDS - A heteroannelated anthraquinone derivative compound is provided. The heteroannelated anthraquinone derivative compound is represented by a formula (IV): | 09-15-2011 |
| 20110245260 | ANALOGS OF DEHYDROPHENYLAHISTINS AND THEIR THERAPEUTIC USE - Compounds represented by the following structure (II) are disclosed: | 10-06-2011 |
| 20110237597 | METHOD OF TREATING PERIPHERAL NERVE SENSORY LOSS USING COMPOUNDS HAVING NICOTINIC ACETYLCHOLINE RECEPTOR ACTIVITY - Methods for treatment of peripheral nerve sensory loss are disclosed. The methods involve treating a patient with a compound having nicotinic acetylcholine receptor activity. | 09-29-2011 |
| 20110263608 | 16-KETO ASPERGILLIMIDES AND HARMFUL ORGANISM CONTROL AGENT COMPRISING THE SAME AS ACTIVE INGREDIENT - Disclosed is a composition for use in controlling ectoparasites, comprising as an active ingredient at least one of compounds represented by formula (I) or (III) or salts thereof. The present invention provides a composition for use in controlling ectoparasites that has excellent ectoparasite control effect and is highly safe. | 10-27-2011 |
| 20110195970 | Methods of identifying and treating responders to dopamine agonist therapy - The present invention is directed to a method of identifying patients to be treated by dopamine agonist therapy comprising the step of analyzing a plasma or urine sample from said patient for concentrations of norepinephrine (NE), norepinephrine metabolites (NE metabolites), dopamine, dopamine metabolites, serotonin, serotonin metabolites, or fasting triglycerides, wherein one or more of: (a) NE metabolites, (b) NE/NE metabolites: dopamine/dopamine metabolites, (c) NE and serotonin, (d) NE/NE metabolites and serotonin, (e) NE and serotonin metabolites, (f) NE/NE metabolites and serotonin metabolites, or (g) NE is/are greater than about 30% over normal level; or dopamine/dopamine metabolites are less than about 30% below normal; or fasting triglycerides are greater than about 150 mg/dl and/or said patient has hypertension. The present invention is also directed to treating identified patients with dopamine agonist therapy. | 08-11-2011 |
| 20110195971 | Methods of identifying responders to dopamine agonist therapy - The present invention is directed to a method of identifying patients to be treated by dopamine agonist therapy comprising the step of analyzing a plasma or urine sample from said patient for concentrations of norepinephrine (NE), norepinephrine metabolites (NE metabolites), dopamine, dopamine metabolites, serotonin, serotonin metabolites, or fasting triglycerides, wherein one or more of: (a) NE metabolites, (b) NE/NE metabolites: dopamine/dopamine metabolites, (c) NE and serotonin, (d) NE/NE metabolites and serotonin, (e) NE and serotonin metabolites, (f) NE/NE metabolites and serotonin metabolites, or (g) NE is/are greater than about 30% over normal level; or dopamine/dopamine metabolites are less than about 30% below normal; or said patient has hypertriglyceridemai and/or hypertension . The present invention is also directed to treating identified patients with dopamine agonist therapy. | 08-11-2011 |
| 20110275646 | Novel Compounds for Treatment of Cancer and Disorders Associated with Angiogenesis Function - Novel compounds for treatment of cancer and disorders associated with angiogenesis function. Also disclosed are a method of preparing the compounds, pharmaceutical compositions and packaged products containing the compounds, a method of using these molecules to treat cancer (e.g., leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, renal cancer, and prostate cancer) and disorders associated with angiogenesis function (e.g., age-related macular degeneration, macular dystrophy, and diabetes), a method of monitoring the treatment, a method of profiling gene expression, and a method of modulating gene expression. | 11-10-2011 |
| 20110275645 | Small Molecules for Inhibition of Protein Kinases - The invention provides compounds that inhibit protein kinases, prodrugs of the compounds, intermediates and methods of synthesizing the compounds and/or prodrugs, pharmaceutical compositions including the compounds and/or prodrugs and methods of using the compounds and/or prodrugs in a variety of contexts, including, for example, in the treatment and/or prevention of various diseases that are responsive to protein kinase inhibition and/or that are mediated, at least in part, by inappropriate kinase activity. | 11-10-2011 |
| 20090239874 | Pyrido[3,2-e]pyrazines, their use as inhibitors of phospohodiesterase 10, and processes for preparing them - The invention relates to pyrido[3,2-e]pyrazines, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10, as active compounds for treating diseases of mammals including a human which can be influenced by using the compounds according to the invention to inhibit phosphodiesterase 10 activity in the central nervous system. More particularly, the invention relates to the treatment of neurologic and psychiatric disorders, for example psychosis and disorders comprising cognitive deficits as symptoms. | 09-24-2009 |
| 20080287450 | Novel Substituted Tetracyclic Tetahydrofuran, Pyrrolidine And Tetrahydrothiophene Derivatives - This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT | 11-20-2008 |
| 20090099191 | INHIBITION OF NF-KB - The present invention is generally related to the modulation of cell growth or apoptosis. Compositions for modulating cell growth or apoptosis, methods of use thereof, and methods of identification thereof are described. | 04-16-2009 |
| 20080293729 | COMPOSITION AND METHOD OF DECREASING RENAL ISCHEMIC DAMAGE - A method of decreasing renal ischemic damage comprising a) identifying an organism having a kidney that is susceptible to renal ischemic damage from an ischemic event; and b) administering to the organism one or more than one effective dose of an agent prior to the ischemic event; where administering to the organism the one or more than one effective dose of the agent serves to at least partially protect the organism's kidney from damage during a subsequent ischemic event. A composition for decreasing renal ischemic damage comprising one or more than one phosphodiesterase inhibitor, and one or more than one HMG-CoA reductase inhibitor. | 11-27-2008 |
| 20090233936 | Fused Aminopiperidines as Dipeptidyl Peptidase-4 Inhibitors for the Treatment or Prevention of Diabetes - The present invention is directed to novel substituted fused aminopiperidines of structural formula (I) which are inhibitors of the dipeptidyl peptidase-4 enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-4 enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-4 enzyme is involved. | 09-17-2009 |
| 20080214551 | Treatment of Burns - The present invention provides methods of treatment of burns, which comprise the step of applying to the burns of a subject a therapeutically effective amount of a metal ion chelating agent. | 09-04-2008 |
| 20090036458 | ENDOPARASITICIDAL TOPICAL COMPOSITIONS - The present invention provides a composition which comprises: an effective amount of (a) praziquantel and (b) a second endoparasiticidal agent selected from the group consisting of a macrocyclic lactone, imidacloprid and a combination thereof; and (c) 4-allyl-2-methoxyphenol as carrier. | 02-05-2009 |
| 20090042894 | NOVEL SPECIES OF ACROCARPOSPORA, A METHOD OF PREPARING IODININ, AND THE USES OF IODININ - The present invention provides a novel species of | 02-12-2009 |
| 20090062292 | Tetrahydropteridines useful as inhibitors of protein kinases - The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. | 03-05-2009 |
| 20090163507 | SYNTHESIS OF NATURALLY OCCURING ECTEINASCIDINS AND RELATED COMPOUNDS - Ecteinascidin compounds with a quinone ring for ring E are active as anti-cancer agents. Related processes and compounds are provided. | 06-25-2009 |
| 20090143391 | Aryl and heteroaryl fused imidazo [1,5-a] pyrazines as inhibitors of phosphodiesterase 10 - The invention relates to imidazo[1,5-a]pyrazine derivatives, to processes for preparing them, to pharmaceutical preparations which comprise these compounds and to the pharmaceutical use of these compounds, which are inhibitors of phosphodiesterase 10 (PDE10), as active compounds for treating central nervous system diseases of mammals, including humans. | 06-04-2009 |
| 20090143392 | Methods of Treating Obesity and Metabolic Disorders - The invention relates to methods of treating or preventing obesity, type 2 diabetes, metabolic syndrome, or glucose intolerance using pyrido[3,2-e]pyrazines which are inhibitors of PDE10. The invention further relates to methods of reducing body fat or body weight. | 06-04-2009 |
| 20090143390 | Parenteral Formulations of Dopamine Agonists - This invention relates to stable pharmaceutical compositions for parenteral administration comprising dopamine agonists and peripheral acting agents_useful for treatment of metabolic disorders or key elements thereof. The parenteral dosage forms exhibit long stable shelf life and distinct pharmacokinetics. | 06-04-2009 |
| 20090209547 | C-8 HALOGENATED MACROLIDES - The present invention discloses compounds of formula (I) or pharmaceutically acceptable salts, esters, or prodrugs thereof: | 08-20-2009 |
| 20090215788 | Pyrrolopyrazine kinase inhibitors - The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, | 08-27-2009 |
| 20080287451 | Method of therapeutic administration of DHE to enable rapid relief of migraine while minimizing side effect profile - Pharmaceutical compositions containing dihydroergotamine (DHE) and methods in which DHE is administered to patients for treatment of migraine without side effects or adverse effects are disclosed. Methods for rapid treatment of migraine with DHE are disclosed comprising: dampening the peak plasma concentration (C | 11-20-2008 |
| 20090215786 | NOVEL CYSTEINE PROTEASE INHIBITORS AND THEIR THERAPEUTIC APPLICATIONS - The present invention concerns new compounds of formula (I), their process of preparation and their therapeutic use. | 08-27-2009 |
| 20080269230 | Inhibitors of proton-gated cation channels and their use in the treatment of ischaemic disorders - This invention relates to the use of compounds capable of inhibiting the activity of a proton-gated cation channel in the treatment of alleviation of diseases or disorders associated with, or mediated by a drop in extra cellular pH. | 10-30-2008 |
| 20080255132 | Combination Therapy Comprising the Use of Et-743 and Paclitaxel for Treating Cancer - Methods of treating a human body for cancer are provided. In one aspect, an effective therapeutic amount of paclitaxel is administered in combination with ET-743 in a dose range between 0.5 and 1 mg/m | 10-16-2008 |
| 20090042895 | Antidepressant Piperidine Derivatives of Heterocycle-Fused Benzodioxans - Compounds of the Formula: | 02-12-2009 |
| 20090215787 | Preparations of new polymorphic forms of varenicline tartrate - The present invention is directed to an amorphous form, three novel polymorph form of crystalline varenicline tartrate, namely Form D, Form E and Form F. The present invention also provides processes of their preparations and pharmaceutical composition comprising such material and their use in therapy. Form D is new anhydrous varenicline tartrate, and can be prepared from recrystallizing varenicline tartrate in a mixture of methanol and water or a mixture of N,N-dimethylformamide and water. Form E is a new varenicline tartrate monohydrate, and can be prepared recrystallizing varenicline tartrate in a mixture of isopropanol and water. Form F is another new varenicline tartrate monohydrate, and can be prepared recrystallizing varenicline tartrate in a mixture of acetone and water. The X-ray powder diffraction pattern (X-RPD), Fourier transform infrared (FT-IR), differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA) techniques are used to characterize amorphous form and crystalline polymorphic forms. | 08-27-2009 |
| 20090030006 | SPIROKETAL DERIVATIVES AND USE THEREOF AS DIABETIC MEDICINE - The present invention provides a compound of Formula (I): | 01-29-2009 |
| 20090111818 | Combinations of Eszopiclone and O-Desmethylvenlafaxine, and Methods of Treatment of Menopause and Mood, Anxiety, and Cognitive Disorders - One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., menopause, mood disorders, anxiety disorders, or cognitive disorders. The first component of the pharmaceutical composition is a sedative eszopiclone. The second component of the pharmaceutical composition is O-desmethylvenlafaxine. The present invention also relates to a method of treating menopause, perimenopause, mood disorders, anxiety disorders, and cognitive disorders. | 04-30-2009 |
| 20090176791 | Diaryl Ureas for Treating Pulmonary Hypertension - The present invention relates to pharmaceutical compositions for treating, preventing or managing pulmonary hypertension comprising at least a diaryl urea compound optionally combined with at least one additional therapeutic agent. Useful combinations include e.g. BAY 43-9006 as a diaryl urea compound. | 07-09-2009 |
| 20080300253 | TREATMENT OF INFLAMMATORY DISORDERS WITH PRAZIQUANTEL - Methods of treating and/or preventing disorders mediated by one or more of TNF-α, NF-κB, IKK-α, IKK-β, ATF-2 and p38 kinase by administration of praziquantel, or a pharmaceutically acceptable salt, prodrug, ester or amide thereof. These disorders include inflammatory disorders such as autoimmune diseases. | 12-04-2008 |
| 20090209546 | L-Malate Salts of 6-(5-Chloro-2-Pyridyl)-5-[(4-Methyl-1-Piperazinyl)Carbonyloxy]-7-Oxo-6,7-- Dihydro-5H-Pyrrolo[3,4-b]Pyrazine - A novel L-malate salt of (6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine) is provided. | 08-20-2009 |
| 20090170860 | Use of PARP-1 Inhibitors - A method for improving the cytotoxic effect of Ecteinascidin-743 (ET-743) or an analog thereof on a tumor cell population in a patient the method including administering to the patient, sequentially or simultaneously, a therapeutically effective combination of a composition including ET-743 and an amount of a composition including a PARP-1 inhibitor effective to increase the cytotoxic effect of ET-743 on the tumor cell population. Anti-tumor compositions containing a therapeutically effective amount of ET-743 and an amount of a PARP-1 inhibitor effective to increase the tumor cytotoxicity of the ET-743 are also presented. | 07-02-2009 |
| 20090137598 | METHOD OF TREATING METABOLIC DISORDERS AND DEPRESSION WITH DOPAMINE RECEPTOR AGONISTS - This invention relates to methods and formulations for treating metabolic disorders and depression. In some embodiments, the methods comprise administering a dopamine receptor agonist and an anti-depressant. | 05-28-2009 |
| 20080234279 | Ecteinascidins - The present invention is directed to several newly discovered ecteinascidin (Et) species, designated herein as Et 731, Et 815, Et 808, and Et 594. The physical properties of these compounds, their preparation and therapeutic properties are also reported. | 09-25-2008 |
| 20090137599 | Methods of identifying responders to dopamine agonist therapy - The present invention is directed to a method of identifying patients to be treated by dopamine agonist therapy comprising the step of analyzing a plasma or urine sample from said patient for concentrations of norepinephrine (NE), norepinephrine metabolites (NE metabolites), dopamine, dopamine metabolites, serotonin, serotonin metabolites, or fasting triglycerides, wherein one or more of: (a) NE metabolites, (b) NE/NE metabolites:dopamine/dopamine metabolites, (c) NE and serotonin, (d) NE/NE metabolites and serotonin, (e) NE and serotonin metabolites, (f) NE/NE metabolites and serotonin metabolites, or (g) NE is/are greater than about 30% over normal level; or dopamine/dopamine metabolites are less than about 30% below normal; or fasting triglycerides are greater than about 150 mg/dl and/or said patient has blood pressure of greater than about 135/85 mm Hg. The present invention is also directed to treating identified patients with dopamine agonist therapy. | 05-28-2009 |
| 20080269231 | Phenazine Compounds and Use Thereof in Autoimmune and Inflammatory Disease - The invention discloses compounds, compositions and methods useful for preventing and/or treating autoimmune diseases and inflammatory diseases. The methods and compositions utilize water-soluble phenazine compounds, or salts, or solvates thereof. These molecules can be delivered alone or in combination with agents which treat or prevent autoimmune diseases and inflammatory diseases such as those caused by arthritis and rheumatoid arthritis. | 10-30-2008 |
| 20090137597 | Novel quinoxalinone derivatives - A quinoxalinone derivative of the formula (I): | 05-28-2009 |
| 20090239873 | Phenyl-piperazine derivatives as modulators of muscarinic receptors - The present invention relates to modulators of muscarinic receptors. The present invention also provides compositions comprising such modulators, and methods therewith for treating muscarinic receptor mediated diseases. | 09-24-2009 |
| 20090023743 | INHIBITORS OF PROTEIN KINASES - Compounds that inhibit Aurora-kinases, compositions containing the compounds and methods of treating diseases using the compounds are disclosed. | 01-22-2009 |
| 20090076016 | FORMULATIONS COMPRISING JORUMYCIN-, RENIERAMYCIN-, SAFRACIN- OR SAFRAMYCIN-RELATED COMPOUNDS FOR TREATING PROLIFERATIVE DISEASES - Jorumycin, renieramycin, safracin and saframycin related compounds formulations, methods of preparing the same, articles of manufacture and kits with such formulations, and methods of treating proliferative diseases with the same formulations are provided. | 03-19-2009 |
| 20090093489 | NOVEL COMPOUNDS FOR TREATMENT OF CANCER AND DISORDERS ASSOCIATED WITH ANGIOGENESIS FUNCTION - Novel compounds for treatment of cancer and disorders associated with angiogenesis function. Also disclosed are a method of preparing the compounds, pharmaceutical compositions and packaged products containing the compounds, a method of using these molecules to treat cancer (e.g., leukemia, non-small cell lung cancer, colon cancer, CNS cancer, melanoma, ovarian cancer, breast cancer, renal cancer, and prostate cancer) and disorders associated with angiogenesis function (e.g., age-related macular degeneration, macular dystrophy, and diabetes), a method of monitoring the treatment, a method of profiling gene expression, and a method of modulating cell growth, cell cycle, apoptosis, or gene expression. | 04-09-2009 |
| 20090076017 | DEUTERIUM-ENRICHED TRABECTEDIN - The present application describes deuterium-enriched trabectedin, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-19-2009 |
| 20090076015 | Tricyclic Spiro Compound Comprising Acyl Group Bound to Nitrogen Atom in the Ring - It is intended to provide an anticoagulant that has an extremely excellent FXa inhibitory action and an extremely weak hERG channel inhibitory action and can be orally administered, which is a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof. | 03-19-2009 |
| 20080280914 | Intravenous Formulations of Pde Inhibitors - The invention relates to a novel pharmaceutical dosage form of PDE 5 inhibitors for intravenous administration and the use thereof for the treatment of diseases. | 11-13-2008 |
| 20080318966 | Sinomenine Derivatives and Preparation and Uses Thereof - The present invention relates to the preparation and pharmacological use of sinomenine derivatives of formula I. The approach disclosed herein is the modification of D ring by-substituting for R. Additional substitutions in the other rings are also provided herein. Several of the sinomenine derivatives have significantly greater anti-inflammation activity when compared with the parent compound. | 12-25-2008 |
