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Hetero ring is six-membered and includes only one ring nitrogen

Subclass of:

514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

514075000 - Phosphorus containing other than solely as part of an inorganic ion in an addition salt DOAI

514079000 - Nitrogen containing hetero ring

Patent class list (only not empty are listed)

Deeper subclasses:

Class / Patent application numberDescriptionNumber of patent applications / Date published
514090000 Chalcogen in the six-membered hetero ring 21
Entries
DocumentTitleDate
20130045951Novel Nitroso Compounds as Nitroxyl Donors and Methods of Use Thereof - The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.02-21-2013
20100081634Novel Phosphorus-Containing Thyromimetics - The present invention relates to compounds of phosphonic acid-containing T3 mimetics and monoesters thereof, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndrome x and diabetes.04-01-2010
20100048511COMPLEX FORMULATION FOR PREVENTING OR TREATING OSTEOPOROSIS WHICH COMPRISES SOLID DISPERSION OF VITAMIN D OR ITS DERIVATIVE AND BISPHOSPHONATE - Provided is a solid dispersion comprising vitamin D or a derivative thereof and a cyclodextrin; a complex formulation for the prevention or treatment of osteophorosis, which includes the solid dispersion and a bisphosphonate; and a method for preparing said complex formulation. The complex formulation can maintain a constant therapeutic level of vitamin D or a derivative thereof through its improved drug stability, while enhancing the patient compliance by minimizing inconvenience and adverse effects when administered to patients.02-25-2010
20100113395LOW DOSAGE FORMS OF RISEDRONATE OR ITS SALTS - Oral dosage forms comprising risedronate or a salt thereof, a chelating agent, and means for effecting delayed release of the risedronate (or salt) immediate release of the oral dosage form to the small intestine of the mammal subject and pharmaceutically effective absorption of the bisphosphonate with or without food or beverages. The present invention substantially alleviates the interaction between the risedronate (or salt) and food or beverages, which interaction results in the active ingredient not being available for absorption. The resulting oral dosage form may thus be taken with or without food. Further, disclosed is delivery of risedronate and the chelating agent to the small intestine, substantially alleviating the upper GI irritation associated with bisphosphonate therapies. These benefits simplify previously complex treatment regimens and can lead to increased patient compliance with bisphosphonate therapies.05-06-2010
20100105637Drug-surfactant complexes for sustained release - The invention involves sustained-release pharmaceutical compositions containing a water-soluble ionic small molecule pharmaceutical agent complexed with an oppositely charged surfactant, particularly a natural bile surfactant. The complexes are sustained-release ionic complexes. The complexes release the ionic pharmaceutical agents into aqueous solution slowly and with zero-order kinetics. Thus, they can be formulated into sustained-release pharmaceutical compositions.04-29-2010
20100093669METHODS FOR PREPARING OXAZOLIDINONES AND COMPOSITIONS CONTAINING THEM - Methods of preparing a class of oxazolidinones useful to impede bacterial growth are disclosed.04-15-2010
20100069334Diagnostic method - A method for prognosing osteoporosis phenotypes or estimating osteoporosis quantitative traits comprising determining outcomes for selected SNP variables and clinical variables. Products and methods for genotyping multiple osteoporosis associated genetic variations.03-18-2010
20080293677Use of Alternating Amine and Non-Amine Bisphosphonate Combinations For Treating Osteoporosis - A method of treating osteoporosis in a human in need thereof by administering alternating amine and non-amine bisphosphonates in a defined dosing schedule. The invention demonstrates an effective response and sustained benefit in the treatment of osteoporosis. Particularly, the method involves administration of a time-dependent dose of more than one bisphosphonate, specifically, alternating administration of a first bisphosphonate with a second bisphosphonate, wherein at least one bisphosphonate is administered in a stepped-up dosage amount.11-27-2008
20080293676Insecticidal Agents Based on Selected Insecticides and Safeners - Insecticidal compositions characterized by an effective amount of an active ingredient combination comprising 11-27-2008
20080269171FUNGICIDAL MIXTURES BASED ON PROTHIOCONAZOLE AND AN INSECTICIDE - A fungicidal mixture, comprising 10-30-2008
20110281822AROMATIC COMPOUNDS HAVING SPHINGOSINE-1-PHOSPHONATE (S1P) RECEPTOR ACTIVITY - Novel aromatic compounds which are useful as sphingosine-1-phosphate modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.11-17-2011
20110281823Pharmaceutical preparation containing an angiotensin II Receptor antagonist, a calcium channel blocker and polyvinyl alcohol - A pharmaceutical preparation including a pharmacologically effective amount of a combination of active ingredients containing an angiotensin II receptor antagonist, a calcium channel blocker and polyvinyl alcohol, wherein the polyvinyl alcohol is in an amount of 5 to 85% by weight of the total weight of the pharmaceutical preparation. A method for the prophylaxis or treatment of hypertension by administering a pharmaceutically effective amount of the pharmaceutical preparation to a patient.11-17-2011
20100227838Combination Therapy for Treating Cancer and Diagnostic Assays for Use Therein - The present disclosure relates to a combination of therapeutic agents for use in treating a patient a subject suffering from cancer. In addition, the present disclosure also relates to diagnostic assays useful in classification of patients for treatment with one or more therapeutic agents.09-09-2010
20090239826COMPOSITIONS AND METHODS FOR THE REGULATION OF HOMOCYSTEINE LEVELS WITHIN THE BODY - Described herein is a method for reducing levels of the harmful metabolic waste product of S-adenosylmethionine (SAMe), homocysteine, and provide vitamin and other nutritional co-factors that reduce the production of homocysteine and either re-methylate homocysteine back to S-adenosylmethionine, or facilitate its conversion downstream to cystathione. The method of the invention may be achieved by administering 5-methyl tetrahydrofolate, methylcobalamin, and one or more compounds selected from the group consisting of betaine, pyridoxal-5-phosphate, N-acetyl-cysteine, and other cofactors.09-24-2009
20100113394LOW DOSAGE FORMS OF RISEDRONATE OR ITS SALTS - Oral dosage forms comprising risedronate or a salt thereof, a chelating agent, and means for effecting delayed release of the risedronate (or salt) immediate release of the oral dosage form to the small intestine of the mammal subject and pharmaceutically effective absorption of the bisphosphonate with or without food or beverages. The present invention substantially alleviates the interaction between the risedronate (or salt) and food or beverages, which interaction results in the active ingredient not being available for absorption. The resulting oral dosage form may thus be taken with or without food. Further, disclosed is delivery of risedronate and the chelating agent to the small intestine, substantially alleviating the upper GI irritation associated with bisphosphonate therapies. These benefits simplify previously complex treatment regimens and can lead to increased patient compliance with bisphosphonate therapies.05-06-2010
20090149427PHARMACEUTICALLY ACCEPTABLE SALTS AND HYDRATES OF RISEDRONIC ACID - The present invention is concerned with new hydrated forms of risedronate salts, processes of preparing the new hydrated forms, pharmaceutical compositions containing the same, therapeutic uses thereof and methods of treatment employing the same. In particular, the present invention provides tri-sodium risedronate dihydrate.06-11-2009
20100120720USE OF HMG-COA REDUCTASE AND FARNESYL-PYROPHOSPHATE SYNTHASE INHIBITORS FOR THE PREPARATION OF A MEDICINE - The invention relates to the use of a hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor and of a farnesyl-pyrophosphate synthase inhibitor, or of one of their associated physiologically acceptable salts, in the preparation of a composition, particularly a pharmaceutical composition, for use in the treatment of human or animal, pathological or nonpathological situations related to the accumulation and/or the persistence of prenylated proteins in cells, such as during progeria (Hutchinson-Gilford syndrome), restrictive dermopathy or physiological aging.05-13-2010
20080306026Capsule Formulation - An encapsulated composition of (a) a pesticide at least active via ingestion that is photolabile, and (b) at least one photoprotectant, wherein the encapsulating polymeric barrier is base triggerable is disclosed. A method for controlling damage of a material by a pest by the use of such encapsulated compositions is likewise disclosed. The composition as disclosed gives protection for beneficial arthropods and reduces workers exposure.12-11-2008
20100120721SUBSTITUTED PIPERIDINOPHENYL OXAZOLIDINONES - The present invention relates to oxazolidinones of Formula I and pharmaceutically acceptable salts, pharmaceutically acceptable solvates or polymorphs thereof. The invention also relates to processes for the preparation of the compound of Formula I and pharmaceutically acceptable salts, pharmaceutically acceptable solvates or polymorphs thereof, and to pharmaceutical compositions containing the compounds of Formula I and pharmaceutically acceptable salts, pharmaceutically acceptable solvates or polymorphs thereof and to methods for treating or preventing microbial infections using the compounds of Formula I and pharmaceutically acceptable salts, pharmaceutically acceptable solvates or polymorphs thereof.05-13-2010
20090203648Modified phosphocalcic compound, injectable composition containing same - A phosphocalcic compound modified by a gem-bisphosphonic acid or one of its salts, a method for preparing same, as well as its use for preparing an injectable composition. The modified phosphocalcic compound is obtained by adding a gem-bisphosphonic acid or one of its alkali metal or alkaline earth salts to a suspension of a precursor phosphocalcic compound in ultras-pure water, while stirring the reaction medium at room temperature, then in recovering by centrifuging the formed compound. The compound is useful for making an injectable composition, for use in the treatment of bone remodeling equilibrium.08-13-2009
20100249070Active Compound Combinations Having Insecticidal Properties - The invention relates to novel insecticidal active compound combinations comprising, firstly, anthranilamides (group 1) and, secondly, further insecticidal active compounds selected from the group of the (thio)phosphates (group 2) and/or the group of the carbamates (group 3), which combinations are highly suitable for controlling animal pests, such as insects.09-30-2010
20100249069S1P3 RECEPTOR INHIBITORS FOR TREATING PAIN - Disclosed herein are compositions and methods for treating pain using S1P3 receptor inhibitors.09-30-2010
20110172194COMPOSITION OF DIALYSIS LIQUID COMPRISING CRYSTALLISATION INHIBITOR SUBSTANCES - This invention relates to a composition that comprises inositol phosphates and/or bisphosphonates, and to the use thereof to prevent the loss of substances of biological interest in the body of patients subjected to dialysis and to maintain sufficient physiological levels of said substances to regulate physiological and/or pathological processes, these substances being inhibitors of pathological crystallisation.07-14-2011
20090286758SUBSTITUTED N-PHENYL-5-PHENYL-PYRAZOLIN-3-YL AMIDES AS CANNABINOID RECEPTOR ANTAGONISTS/INVERSE AGONISTS USEFUL FOR TREATING OBESITY - The present invention provides novel pyrazolines that are useful as cannabinoid receptor antagonists/inverse agonists and pharmaceutical compositions thereof and methods of using the same for treating obesity, diabetes, dyslipidemias, cardiovascular disorders, hepatic disorders, and a combination thereof.11-19-2009
20100298271COMPOUNDS FOR USE IN THE TREATMENT OF CANCER - Compound of Formula I or a salt thereof for treating cancer, wherein X represents CH or N; R11-25-2010
20080287399Substituted Aminopyridines and Uses Thereof11-20-2008
20080287400Low Dosage Forms Of Risedronate Or Its Salts - Oral dosage forms comprising risedronate or a salt thereof, a chelating agent, and means for effecting delayed release of the risedronate (or salt) immediate release of the oral dosage form to the small intestine of the mammal subject and pharmaceutically effective absorption of the bisphosphonate with or without food or beverages. The present invention substantially alleviates the interaction between the risedronate (or salt) and food or beverages, which interaction results in the active ingredient not being available for absorption. The resulting oral dosage form may thus be taken with or without food. Further, disclosed is delivery of risedronate and the chelating agent to the small intestine, substantially alleviating the upper GI irritation associated with bisphosphonate therapies. These benefits simplify previously complex treatment regimens and can lead to increased patient compliance with bisphosphonate therapies.11-20-2008
20120142637PRODRUGS OF 6-CYCLOHEXYL-1-HYDROXY-4-METHYLPYRIDIN-2-(1H)- ONE AND DERIVATIVES THEREOF - A prodrug can have a structure of Formula 10 or derivative thereof or stereoisomer thereof or pharmaceutically acceptable salt thereof. The prodrug can be included in a pharmaceutical composition for use in treatment of fungus, cancer, dermatitis, superficial mycoses; inflammation, tinea pedis, tinea cruris, and tinea corporis, 06-07-2012
20120196835ENZYME INHIBITING COMPOUNDS AND METHODS - The invention provides compounds, compositions, and methods for studying the Rohmer pathway and for treating bacterial infections or parasitic infections. The parasitic infection can be a protozoan infection, such as malaria. The compounds and compositions can also be used as antibiotics, for example, to kill bacteria or parasites, or to inhibit bacterial or parasite growth. The invention further provides inhibitors of isoprenoid biosynthesis enzymes, and methods of inhibiting the activity of isoprenoid biosynthesis enzymes. The compounds can be, for example, alkynes or allenes that bind to a unique Fe of an Fe4S4 cluster of an isoprenoid biosynthesis enzyme.08-02-2012
20100144678COMPOSITIONS AND METHODS FOR TREATING BONE CANCER - Small molecule bradykinin inhibitor bisphosphonate amide derivatives useful for inhibiting cancer growth and treating cancer residing in and around bone are disclosed. These compounds and pharmaceutical compositions containing these compounds are particularly useful for the treatment of prostate cancer bone metastases.06-10-2010
20080318907Nitroxide Free Radical Synergized Antineoplastic Agents - Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.12-25-2008
20090325905METHOD FOR TREATING DISEASES ASSOCIATED WITH ALTERATIONS IN CELLULAR INTEGRITY USING RHO KINASE INHIBITOR COMPOUNDS - This invention is directed to methods of preventing or treating diseases or conditions associated with alterations in cellular integrity including alterations in endothelial permeability, excessive cell proliferation or tissue remodeling. Particularly, this invention is directed to methods of treating diabetic nephropathy, malaria, or cancer. The method comprises identifying a subject in need of the treatment, and administering to the subject an effective amount of a novel rho kinase inhibitor compound to treat the disease.12-31-2009
20110230445Substituted Heteroaryls - The present invention provides Formula (1A) compounds09-22-2011
20090197835VINYL PHOSPHONATE LYSOPHOSPHATIDIC ACID RECEPTOR ANTAGONISTS - The present invention provides LPA analogs that are antagonists at the LPA receptors.08-06-2009
20100016258PHOSPHONATE DERIVATIVES AS AUTOTAXIN INHIBITORS - The present invention provides β-hydroxy phosphonate compounds that are autotaxin inhibitors.01-21-2010
20090281060HETEROCYCLIC DERIVATIVES AS GPCR RECEPTOR AGONISTS - Compounds of Formula (I), R11-12-2009
20110059922MITOCHONDRIA TARGETED CATIONIC ANTI-OXIDANT COMPOUNDS FOR PREVENTION, THERAPY OR TREATMENT OF HYPER-PROLIFERATIVE DISEASE, NEOPLASIAS AND CANCERS - The inventions disclosed include methods of treating cancers and related neoplasias, especially prostate cancer, with pharmaceutically acceptable salts comprising lipophilic cation moieties linked to nitroxide or linked to hydroxylamine anti-oxidant groups.03-10-2011
20100216747PREVENTIVE AGENT OR THERAPEUTIC AGENT FOR DISEASE CAUSED BY ABNORMAL BONE METABOLISM - An object of the present invention is to provide a preventive drug and a therapeutic drug for diseases caused by abnormal bone metabolism, especially osteoporosis, which is more effective than conventional drugs. Combined use of N-hydroxy-4-{5-[4-(5-isopropyl-2-methyl-1,3-thiazol-4-yl)phenoxy]pentoxy}-benzamidine, or a salt thereof; and at least one compound selected from the group consisting of etidronic acid, clodronic acid, pamidronic acid, tiludronic acid, risedronic acid, minodronic acid, ibandronic acid, zoledronic acid, and salts thereof can exert higher bone resorption inhibitory effect and provide a preventive effect and a therapeutic effect for diseases caused by abnormal bone metabolism, especially osteoporosis as compared with administration of the respective agents respectively.08-26-2010
20090075941TREATING NEOPLASMS - Methods of treating a subject with neoplasm (e.g., mesothelioma) or at risk of developing neoplasm by administering a mevalonate pathway inhibitor such as a nitrogen-containing bisphosphonate are disclosed. Examples of nitrogen-containing bisphosphonates include alendronate, ibandronate, minodronate, neridronate, olpadronate, pamidronate, risedronate, and zoledronate. The methods can further include the administration of a p38 inhibitor. Further disclosed are compositions and kits including a nitrogen-containing bisphosphonate and optionally a p38 inhibitor.03-19-2009
20090075940DEUTERIUM-ENRICHED RISEDRONATE - The present application describes deuterium-enriched risedronate, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.03-19-2009
20100197635TREATMENT OF TARDIVE DYSKINESIA WITH PYRIDOXAL 5'-PHOSPHATE - This invention relates to treatment of Tardive Dyskinesia through the administration of pyridoxal 5′-phosphate. The treatment may be an oral administration of 100-4000 mg/day, for example, 100-750 mg/day or about 250 mg/day. Also provided is the use of pyridoxal 5′-phosphate for the preparation of a medicament for the treatment of tardive dyskinesia, kits comprising pyridoxal 5′-phosphate for the treatment of tardive dyskinesia, and combination drugs for the treatment of tardive dyskinesia.08-05-2010
20100305069OXAZOLIDINONE CONTAINING DIMER COMPOUNDS, COMPOSITIONS AND METHODS TO MAKE AND USE - Dosage forms or pharmaceutical compositions comprise a compound having the structure of Formula IV:12-02-2010
20110112053PHARMACOLOGICAL TARGETING OF VASCULAR MALFORMATIONS - Disclosed herein are compositions and methods for decreasing vascular permeability in a blood vessel and treating or preventing conditions associated with defects or injuries of vascular endothelium. For example, the disclosed compositions and methods can be used to treat a vascular dysplasia such as cerebral cavernous malformation (CCM). These methods relate generally to the use of compositions that inhibit RhoA GTPase levels or activity, such as inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase.05-12-2011
20110034417SUBSTITUTED PIPERIDINE COMPOUNDS AND METHODS OF THEIR USE - Novel 3,4-disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.02-10-2011
201100344164-PYRIDINONE COMPOUNDS AND THEIR USE FOR CANCER - Disclosed are compounds of Formula (I):02-10-2011
20110039804 Composition of Risedronate and Vitamin D3 - The present invention is focused on compositions that contain risedronate and vitamin D as active ingredients. This dose combines the pharmaceutical properties of risedronate, which avoids bone degradation, and those from vitamin D, which fixates calcium to the bone, which are used for treating postmenopausal osteoporosis.02-17-2011
20110124600Use of Dopamine partial agonists for treament of the restless leg syndrome and corresponding pharmaceutical preparation - Disclosed is the oral use of dopamine partial agonists and the physiologically acceptable salts thereof in order to create a pharmaceutical preparation for treating the restless legs syndrome, which effectively controls the symptoms while having a significantly smaller undesired effect of a medicament than medicaments known in prior art.05-26-2011
20090253656BCRP/ABCG2 INHIBITOR - The present invention is directed to a breast cancer resistance protein (BCRP/ABCG2) inhibitor.10-08-2009
20090215727INHIBITION OF ATP-MEDIATED, P2X7 DEPENDENT PATHWAYS BY PYRIDOXAL-5-PHOSPHATE AND VITAMIN B6 RELATED COMPOUNDS - P5P can be used as effective treatments for the modulation of P2X7, IL-1β, and inflammation response, and for diseases in which prevention of P2X7-dependent pathways or prevention of release of IL-1β is desirable, such as epithelial cancer, leukemia, brain tumors, spinal cord injury, tuberculosis, Alzheimer's Disease, neurodegenerative diseases, autosomal recessive polycystic kidney disease, diabetes, including type I diabetes, prostate cancer, and osteoporosis, bone formation and resorption.08-27-2009
20110098251BISPHOSPHONATE COMPOUNDS - Novel bisphosphonate cyclic acetal compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating bone metabolism disorders, such as abnormal calcium and phosphate metabolism.04-28-2011
20090137529SUBSTITUTED ESTERS AS CANNABINOID-1 RECEPTOR MODULATORS - The compounds of the present invention are prodrugs of modulators of the Cannabinoid-1 (CB 1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the Cannabinoid-1 (CB 1) receptor. In particular, compounds of the present invention are 5 prodrugs of antagonists or inverse agonists of the CB 1 receptor. The invention is concerned with the use of these compounds to be converted to compounds that modulate the Cannabinoid-1 (CB 1) receptor. As such, the compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-10 Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia.05-28-2009
20100305068COMPOUNDS AND METHODS FOR MODULATING PROTEIN TRAFFICKING - Disclosed are compositions and methods for modulating protein trafficking and treating or preventing disorders characterized by impaired protein trafficking. Also disclosed are methods for producing a protein and identifying compounds that rescue protein trafficking defects.12-02-2010
20090281062NOVEL NITROSO COMPOUNDS AS NITROXYL DONORS AND METHODS OF USE THEREOF - The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.11-12-2009
20110212925NOVEL COMPOUNDS AS RECEPTOR MODULATORS WITH THERAPEUTIC UTILITY - The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.09-01-2011
20090118236Novel Phosphorus-Containing Thyromimetics - The present invention relates to compounds of phosphonic acid containing T3 mimetics, stereoisomers, pharmaceutically acceptable salts, co-crystals, and prodrugs thereof and pharmaceutically acceptable salts and co-crystals of the prodrugs, as well as their preparation and uses for preventing and/or treating metabolic diseases such as obesity, NASH, hypercholesterolemia and hyperlipidemia, as well as associated conditions such as atherosclerosis, coronary heart disease, impaired glucose tolerance, metabolic syndromex and diabetes.05-07-2009
20080214505Risedronate compositions and their methods of use - A method comprising orally administering to a human or other mammal a pharmaceutical composition comprising from about 65% to about 110% of the cumulative effective dose of risedronate or a pharmaceutically acceptable acid, salt, ester, solvate, or polymorph thereof according to a continuous dosing schedule of one, two, or three consecutive days per month is useful for treating or preventing osteoporosis and other bone metabolic disorders.09-04-2008
20080255070Bisphosphonate Compounds and Methods with Enhanced Potency for Multiple Targets including FPPS, GGPPS, AND DPPS - The disclosure provides, inter alia, novel bisphosphonate compounds and methods of making and using such compounds. In certain embodiments, compounds of the invention include bisphosphonates that are capable of selectively inhibiting one or more of farnesyl diphosphate synthase (FPPS), geranylgeranyl diphosphate synthase (GGPPS), and decaprenyl pyrophosphate synthase (DPPS). In preferred embodiments, compounds of the invention are capable of selectively inhibiting two or more of FPPS, GGPPS, and DPPS. In embodiments, compounds and methods of the invention demonstrate superior activity levels, such as in the anti-cancer context, immunostimulation context, and other contexts, which in several cases exceed the activity levels of previous generation bisphosphonate drugs by orders of magnitude. In embodiments, the invention provides compounds and methods in connection with research and therapeutic applications, e.g., for tumor or cancer cell growth inhibition, activation of gammadelta T cells, inhibition of certain enzymes related to the mevalonate metabolic pathway, bone resorption diseases, cancer, immune disorders, immunotherapy, and infectious diseases.10-16-2008
20110028436ORAL COMBINATION OF VITAMINS - This invention provides compositions for treating and preventing nausea and other disorders, the compositions comprising vitamins as active ingredients, including vitamin B6, vitamin K, and vitamin C, and a method for treating nausea or morning sickness with the oral compositions.02-03-2011
20100286095NOVEL USE OF A POLYAMINE-DEPLETED FOOD COMPOSITION FOR HUMAN OR VETERINARY USE, FOR PREPARING A THERAPEUTIC FOOD PRODUCT - A polyamine-depleted food compositions is provided for preparing foods, intended for humans or animals, for preventing or treating heart rate anomalies.11-11-2010
20110257130Compositions and Methods for Treatment of Renin-Angiotensin Aldosterone System (RAAS)- Related Disorders - Compounds are provided which can be useful in reducing the activity of an angiotensin-converting enzyme and thus be used to treat or prevent a renin-angiotensin aldosterone system-related disorder. These compounds include lipoic acid derivatives such as prolyl lipoic acid and pipecolinyl lipoic acid, and other compounds, and these compounds are useful in treating hypertension, stroke, or other renin-angiotensin aldosterone system-related disorders in human or animal patients. Pharmaceutical compositions prepared using these compounds and methods of treatment using these compounds are also provided.10-20-2011
20100298270Novel Compounds and Methods of Using Them - Described herein are novel HDAC modulators, formulations containing them and methods of using them. In some embodiments, the HDAC modulators possess specific stereo chemistry. In other embodiments, the compounds described herein are used in the treatment or prevention of histone deacetylase mediated disorders.11-25-2010
20100168067BIOMARKERS FOR BISPHOSPHONATE-RESPONSIVE BONE DISORDERS - This invention relates to the finding that the presence of polymorphisms in and around the farnesyl diphosphate synthase (FDPS) gene is predictive of the densitometric response of patients with bone disorders, such as osteoporosis, subsequent to commencing treatment with amino-bisphosphonates. Methods relating to the identification of individuals having bone disorders which are responsive to bisphosphonates and predicting the responsiveness of individuals with bone disorders to treatment with a bisphosphonate are provided.07-01-2010
20110190237Macrocyclic Prodrug Compounds Useful as Therapeutics - The present invention includes macrocyclic prodrug compounds, pharmaceutical compositions containing them. The present invention also includes use of these compounds in the treatment of various diseases including an autoimmune disease, an inflammatory disease, a neurological or neurodegenerative disease, cancer, a cardiovascular disease, allergy, asthma, a hormone-related disease, and tumors or symptoms resulting from neurofibromatosis.08-04-2011
20110218175ANTIVIRAL AGENTS - The present invention relates to antiviral compounds of formula (I),09-08-2011
20080214504Vitamin B6 Related Compounds and Methods for Recovery From Trauma - The present invention includes a method of promoting recovery from trauma in a patient in need thereof comprising administration of a therapeutically effective amount of a vitamin B6 related compound (excluding vitamin B6), preferable compounds include pyridoxal-5′-phosphate, 3-acylated analogues of pyridoxal, 3-acylated analogues of pyridoxy-4,5-animal, and pyridoxine phosphate analogues.09-04-2008
20090018106INTRAVENOUS FORMULATIONS OF PYRIDOXAL 5'- PHOSPHATE AND METHOD OF PREPARATION - The present invention provides a lyophilized formulation of pyridoxal 5′-phosphate and a method of making the same. The present invention also provides an injectable formulation of pyridoxal 5′-phosphate reconstituted from the lyophilized formulation. The present invention further provides uses of the lyophilized and injectable formulations.01-15-2009
20110028435CRYSTALLIZATION METHOD AND BIOAVAILABILITY - Preparation, in-vitro and in vivo characterization of novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl)phosphonic acid, suitable for pharmaceutical compositions in drug delivery systems for humans.02-03-2011
20100227839CRYSTALLINE FORM OF R)-3-(4-(2-(2-METHYLTETRAZOL-5-YL)PYRIDIN- 5-YL)-3-FLUOROPHENYL)-5-HYDROXYMETHYL OXAZOLIDIN-2-ONE DIHYDROGEN PHOSPHATE - A crystalline form of crystalline (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate, methods of making the crystalline form and pharmaceutical compositions comprising the crystalline form are useful antibiotics. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as 09-09-2010
20100087398DIHYDROPYRIDINE DERIVATIVE FOR TREATING CANCER OR A PRE-CANCEROUS CONDITION AND OTHER CONDITIONS - The use of dihydropyridine-5-phosphonic acid cyclic propylene ester derivatives of formula (I), a prodrug thereof, or a pharmaceutically acceptable salt of said compound or prodrug in the treatment of cancers, pre-cancerous conditions and other conditions is disclosed, wherein each of R04-08-2010
20100317625NOVEL SULFONAMIDOMETHYLPHOSPHONATE INHIBITORS OF BETA-LACTAMASE - This invention provides novel β-lactamase inhibitors of the aryl- and heteroaryl-sulfonamidomethylphosphonate monoester class. The compounds inhibit three classes of β-lactamases and synergize the antibacterial effects of β-lactam antibiotics (e.g., imipenem and ceftazimdime) against those micro-organisms normally resistant to the β-lactam antibiotics as a result of the presence of the β-lactamases.12-16-2010
200901565592-ethyl N,N-bis(2-chloroethyl)phosphorodiamidates - 2-{[2-(Substituted amino)ethyl]sulfonyl}ethyl N,N-bis(2-chloroethyl)phosphorodiamidates and their salts, their preparation and intermediates in their preparation, pharmaceutical compositions containing them, and methods of treatment using them. The compounds are useful for treating cancer and autoimmune diseases, alone and in combination with other therapies.06-18-2009
20090281061Impaired Alleles of Genes Involved in Metabolic Pathways and Methods for Detecting and Using the Same - The invention is directed to enzyme variants, responsiveness thereof to cofactors, and in vivo assays for testing the activity of enzyme variants as well as the responsiveness thereof to cofactors.11-12-2009
20130012478DOSAGE FORMS OF BISPHOSPHONATES - Provided is an oral dosage form comprising a bisphosphonate selected from the group consisting of a risedronate and salts thereof; an ethylenediaminetetraacetic acid (EDTA) or a pharmaceutically acceptable salt thereof; and a delayed release mechanism to deliver the risedronate and the EDTA in the lower gastrointestinal tract, wherein the oral dosage form is administered according to a scheduled dosing interval. The present invention substantially alleviates the interaction between bisphosphonates and food or beverages, which interaction results in the bisphosphonate active ingredient not being available for absorption. The resulting oral dosage form may thus be taken with or without food. Further, the present invention effects delivery of the bisphosphonate and the chelating agent to the lower GI tract, substantially alleviating the upper GI irritation associated with bisphosphonate therapies. These benefits simplify previously complex treatment regimens and can lead to increased patient compliance with bisphosphonate therapies.01-10-2013
20120065170Antimicrobial Cyclocarbonyl Heterocyclic Compounds For Treatment Of Bacterial Infections - The present invention provides indoline compounds of the following formula I:03-15-2012
20120071448S1P3 Receptor Inhibitors for Treating Conditions of the Eye - Disclosed herein are compositions and methods for treating conditions of the eye using S1P3 receptor inhibitors.03-22-2012
20110092461PYRIDYL INHIBITORS OF HEDGEHOG SIGNALLING - The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I:04-21-2011
20110082113PRODRUGS OF A PIPERIDINYL DERIVATIVE AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY - The present application describes prodrugs of the compound of formula (I):04-07-2011
20110105436HETEROARYL COMPOUNDS, COMPOSITIONS, AND METHODS OF USE IN CANCER TREATMENT - Provided herein are novel heteroaryl compounds, compositions comprising the compounds, and methods of treatment or prevention comprising administration of the compounds. The compounds are effective in the targeting of cells defective in the von Hippel-Lindau gene and in inducing autophagic cell death. The methods are directed to treating or preventing diseases such as cancer, and in particular cancers resulting from von Hippel-Lindau disease. The compounds of the invention may be administered in combination with another therapeutic agent.05-05-2011
20110105435THERAPY OPTION FOR RECOLORATION OF HAIR VIA BISPHOSPHONATES BY PHYSIOLOGICAL REPIGMENTATION WITH AGE-RELATED AND/OR PREMATURE "GRAYED" PATIENTS - The present invention relates to the use of a bisphosphonate derivative according to general Formula I05-05-2011
20120122820PRODRUGS AND THE USE THEREOF - The present application relates to prodrug derivatives of 2-amino-6-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}thio)-4-[4-(2-hydroxyethoxy)phenyl]pyridine-3,5-dicarbonitrile, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of cardiovascular disorders.05-17-2012
20120129813NOVEL COMPOUNDS AS RECEPTOR MODULATORS WITH THERAPEUTIC UTILITY - The present invention relates to novel derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.05-24-2012
20120129812NOVEL THYROID HORMONE BETA RECEPTOR AGONIST - Provided is a heterocyclic derivative showing a thyroid hormone β receptor agonist action, which is effective for the prophylaxis or treatment of the diseases relating to the action. A compound represented by the formula [I]:05-24-2012
20090005347DRUG FOR THE TREATMENT OF OSTEONECROSIS AND FOR THE MANAGEMENT OF PATIENTS AT RISK OF DEVELOPING OSTEONECROSIS - A bisphosphonate for the treatment of osteonecrosis and/or osteonecrosis dissecans. The drug may further be used to prevent the onset of osteonecrosis and/or osteonecrosis dissecans and any complications associated with both diseases.01-01-2009
20110124601AMINOPHOSPHINIC DERIVATIVES THAT CAN BE USED IN THE TREATMENT OF PAIN - The present invention relates to a compound of the following general formula (I): R05-26-2011
20120322767FORMULATIONS OF BISPHOSPHONATES AND VITAMIN D SUIUTABLE FOR INTERMITTENT INTRAMUSCULAR AND SUBCUTANEOUS ADMINISTRATION - Compositions for pharmaceutical use are described, comprising bisphosphonates and vitamin D in high concentration, destined to the intramuscular and subcutaneous intermittent administration for treatment of bone and skeletal system diseases, particularly osteoporosis, and sensitive cancers. These formulations are characterized by the use of a lipid and phospholipid emulsion at high concentration, having optimal carrier and solvent power for both the pharmacologically active components.12-20-2012
20100173871PHOSPHORYLATED DENDRIMERS AS ANTIINFLAMMATORY DRUGS - A method for treating inflammatory diseases through an anti-inflammatory type activation of monocytes, the method includes the administration to a patient in need thereof of an effective quantity of at least one dendrimer with mono- or biphosphonic terminations.07-08-2010
20100168066NOVEL INSECTICIDES - Compounds of formula (I) wherein the substituents are as defined in claim (07-01-2010
20120101066Pharmaceutical Compositions and Therapeutic Methods Employing a Combination of a Manganese Complex Compound and a Non-Manganese Complex Form of the Compound - A pharmaceutical composition for treatment of a pathological condition in a patient comprises, as a first component, a manganese complex of Formula I( ), and, as a second component, a non-manganese complex compound of Formula (I), optionally together with one or more physiologically acceptable carriers and/or excipients, wherein X, R, R, R, and R are as defined herein. Methods for treatment of a pathological condition in a patient, for example, a pathological condition caused by the presence of oxygen-derived free radicals, comprises administering to said patient the first component and the second component.04-26-2012
20120289482Method for modulating or controlling connexin 43(Cx43) level of a cell and reducing arrhythmic risk - A method of modulating or controlling connexin 43 (Cx43) level of a cell includes inducing mitochondrial reactive oxygen species (ROS) production in the cell.11-15-2012
20130018019AROMATIC COMPOUNDS HAVING SPHINGOSINE-1-PHOSPHONATE (S1P) RECEPTOR ACTIVITY - Novel aromatic compounds which are useful as sphingosine-1-phosphate modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.01-17-2013
20110160163INHIBITORS OF p38 - The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to inhibitors of ZAP70. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.06-30-2011
20130143843ARYL DIHYDROPYRIDINONE AND PIPERIDINONE MGAT2 INHIBITORS - The present invention provides compounds of Formula (I):06-06-2013
20130116214HETEROCYCLIC RING COMPOUND - The present invention provides a compound having a muscle cell or adipocyte differentiation regulating action, useful for the prophylaxis or treatment of diseases such as diabetes, obesity, dyslipidemia and the like, and the like, and having superior efficacy.05-09-2013
20130178444PRODRUGS OF A PIPERIDINYL DERIVATIVE AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY - The present application describes prodrugs of the compound of formula (I):07-11-2013
20110275599USE OF COLD-STABILIZED METHYLATED VEGETABLE OILS AS AN AGRICULTURAL CHEMICAL COFORMULANT - The invention describes the use of a methylated vegetable oil having less than 10 percent by weight of saturated fatty acid methyl esters and less than 10 percent by weight of fatty acid methyl esters of carbon chain length less than C11-10-2011
20110312916NOVEL PRODRUGS OF STEROIDAL CYP17 INHIBITORS/ANTIANDROGENS - Prodrugs of C-17-heterocyclic-steroidal drugs providing improved oral bioavailability and pharmacokinetics are described. The drugs are inhibitors of human CYP 17 enzyme, as well as potent antagonists of both wild type and mutant androgen receptors (AR), and are useful for the treatment of urogenital and/or androgen-related cancers, diseases and/or conditions, such as human prostate cancer, breast cancer, and prostate hyperplasia. The disclosure describes methods of synthesizing and using the prodrugs in cancer therapy.12-22-2011
20130157982NOVEL COMPOUNDS AS RECEPTOR MODULATORS WITH THERAPEUTIC UTILITY - The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.06-20-2013
20120028926Phosphate Management with Small Molecules - This invention relates to methods and small molecules having a phosphate group that can be used to inhibit phosphate transport and to treat or prevent diseases that are related to disorders in the maintenance of normal serum phosphate levels.02-02-2012
20130196952HETEROCYCLIC DERIVATIVES FOR THE TREATMENT OF DISEASES - The invention relates to compounds of Formula (1) and to processes for the preparation of intermediates used in the preparation of compositions containing and the uses of such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.08-01-2013
20130203704COMPOUNDS FOR THE TREATMENT OF ADDICTION - Disclosed are novel compounds having the structure of Formula (I):08-08-2013
20120094960DOSAGE FORMS OF RISEDRONATE - Oral dosage forms of a risedronate comprised of a safe and effective amount of a pharmaceutical composition comprising risedronate, a chelating agent, and, means for effecting delayed release of the risedronate and the chelating agent in the small intestine provide immediate release of the pharmaceutical composition to the small intestine of the mammal subject and pharmaceutically effective absorption of the bisphosphonate with or without food or beverages. The present invention substantially alleviates the interaction between risedronate and food or beverages, which interaction results in the bisphosphonate active ingredient not being available for absorption. The resulting oral dosage form may thus be taken with or without food. Further, the present invention effects delivery of risedronate and the chelating agent to the small intestine, substantially alleviating the upper GI irritation associated with bisphosphonate therapies. These benefits simplify previously complex treatment regimens and can lead to increased patient compliance with bisphosphonate therapies.04-19-2012
20120094959TREATMENT OF CYSTIC DISEASES - The invention described herein pertains to the treatment of cystic diseases. More particularly, the invention described herein relates to methods for treating cystic disease using one or more lysophosphatidic acid antagonists, TMEM16a inhibitors, and/or peroxisome proliferator-activated receptor modulators.04-19-2012

Patent applications in class Hetero ring is six-membered and includes only one ring nitrogen

Patent applications in all subclasses Hetero ring is six-membered and includes only one ring nitrogen