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Bicyclo ring system having the seven-membered hetero ring as one of the cyclos

Subclass of:

514 - Drug, bio-affecting and body treating compositions

514001000 - DESIGNATED ORGANIC ACTIVE INGREDIENT CONTAINING (DOAI)

514183000 - Heterocyclic carbon compounds containing a hetero ring having chalcogen (i.e., O,S,Se or Te) or nitrogen as the only ring hetero atoms DOAI

514211010 - Hetero ring contains seven members including nitrogen, carbon and chalcogen

514211030 - Chalcogen double bonded directly to a ring carbon which is adjacent to the ring nitrogen

514211040 - Polycyclo ring system which contains the seven-membered hetero ring as one of the cyclos

Patent class list (only not empty are listed)

Deeper subclasses:

Class / Patent application numberDescriptionNumber of patent applications / Date published
514211050 Bicyclo ring system having the seven-membered hetero ring as one of the cyclos 84
20080200449TREPROSTINIL ADMINISTRATION USING A METERED DOSE INHALER - Treprostinil can be administered using a metered dose inhaler. Such administration provides a greater degree of autonomy to patients. Also disclosed are kits that include a metered dose inhaler containing a pharmaceutical formulation containing treprostinil.08-21-2008
20090036425SUBSTITUTED BICYCLOLACTAM COMPOUNDS - The invention provides compounds of formula (1),02-05-2009
20090069290Method for treating a demyelinating condition - Methods for treating a demyelinating condition in a subject in need of treatment are provided. In some aspects the methods encompass administering to the subject an amount of a Ca03-12-2009
20090082333REMEDY FOR XANTHOMA - A preventive/remedy for xanthoma which contains a compound having an inhibitory effect on squalene synthase, its prodrug or its salt.03-26-2009
20090088416DEUTERIUM-ENRICHED LAPAQUISTAT - The present application describes deuterium-enriched lapaquistat, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.04-02-2009
20090105214Heteroaryl Benzamide Derivatives for Use as Glk Activators in the Treatment of Diabetes - Compounds of formula (I), wherein R04-23-2009
20090118255Crp Lowering Agent - The present invention provides a novel drug which is useful as a preventive and/or therapeutic agent for various diseases involved in elevation of CRP level, in particular, inflammatory disease and cancer comprising a compound having inhibitory activity against squalene synthase or a salt thereof, or a prodrug thereof.05-07-2009
20090137551Substituted Bicyclolactam Compounds - The invention provides compounds of formula (1),05-28-2009
20090221548MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS - The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I09-03-2009
20090253680SELECTED CGRP-ANTAGONISTS, PROCESSES FOR PREPARING THEM AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS - The present invention relates to the CGRP-antagonists of general formula I10-08-2009
20090258856IMIDAZOPYRIDAZINONE AND IMIDAZOPYRIDONE DERIVATIVES, THE PREPARATION THEREOF AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS - The present invention relates to substituted imidazo-pyridinones and imidazo-pyridazinones of general formula10-15-2009
20090281077Cyclic sulfones useful as mitochondrial sodium-calcium exchangers - The invention relates to novel heterocyclic compounds of the formula11-12-2009
20100063027Amine Derivative Having NPY Y5 Receptor Antagonistic Activity - This invention provides a compound of the formula (I):03-11-2010
20100137281HETEROCYCLIC COMPOUND AND USE THEREOF - The present invention aims to provide a compound having superior pharmacological action, physicochemical properties and the like, which is useful for the prophylaxis or treatment s of circulatory diseases such as hypertension, cardiac diseases, arteriosclerosis, renal diseases, cerebral apoplexy and the like and/or metabolic diseases such as hyperlipidemia, obesity, diabetes and the like, central nervous disorders such as cerebral infarction and the like, mental diseases such as dementia, depression and the like, and the like.06-03-2010
20100273768Inhibitors of Bruton's Tyrosine Kinase - This application discloses 5-phenyl-1H-pyridin-2-one, 6-phenyl-2H-pyridazin-3-one, and 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-II:10-28-2010
20110288071SUBSTITUTED PYRIMIDINES FOR THE TREATMENT OF DISEASES SUCH AS CANCER - The present invention encompasses compounds of general formula (1) wherein A, B, X, R11-24-2011
20120065189HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF STRESS-RELATED CONDITIONS - The present invention provides a novel heterocyclic compound. A heterocyclic compound represented by general formula (1) wherein, R03-15-2012
20120122844METHOD OF TREATING CONTRAST-INDUCED NEPHROPATHY - The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I:05-17-2012
20120225857MST1 KINASE INHIBITORS AND METHODS OF THEIR USE - Compounds for the inhibition of mammalian Ste20-like kinase 1 (MST1) are disclosed, along with compositions comprising them and methods of their use in the treatment, management or prevention of an inflammatory or autoimmune diseases or disorders.09-06-2012
20130158006AMINOPYRIMIDINE DERIVATIVES AS LRRK2 MODULATORS - Compounds of the formula I:06-20-2013
20130184255FUSED HETEROCYCLIC COMPOUNDS AS ION CHANNEL MODULATORS - The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I:07-18-2013
20130281435THERAPEUTIC AGENT FOR IRRITABLE BOWEL SYNDROME10-24-2013
20130338142IMIDAZOPYRAZINE SYK INHIBITORS - Certain imidazopyrazines and pharmaceutical compositions thereof are provided herein. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of Syk activity, which comprises administering to such patients an amount of an imidazopyrazine compound effective to reduce signs or symptoms of the disease or disorder are provided.12-19-2013
20140031338INHIBITORS OF VIRAL REPLICATION, THEIR PROCESS OF PREPARATION AND THEIR THERAPEUTICAL USES - The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV.01-30-2014
20140051681MST1 KINASE INHIBITORS AND METHODS OF THEIR USE - Compounds for the inhibition of mammalian Ste20-like kinase 1 (MST1) are disclosed, along with compositions comprising them and methods of their use in the treatment, management or prevention of an inflammatory or autoimmune diseases or disorders.02-20-2014
20140080809Novel Compounds as Diacylglycerol Acyltransferase Inhibitors - This invention relates to novel compounds which are inhibitors of acyl coenzymeA: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, hypertriglyceridemia, hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, hepatitis C virus infection and acne or other skin disorders.03-20-2014
20140100216STIMULATORS OF INCRETIN HORMONES SECRETION, METHOD FOR PREPARATION AND USE THEREOF - The invention relates to the area of medicinal chemistry, pharmacology and medicine and includes description of pharmaceutical compositions and combined medicaments on the base of secretion stimulators and protectors of incretin hormones for treatment of metabolic diseases (among them, diabetes, obesity, metabolic syndrome and the like). The invention consists in that that pharmaceutical composition or combined medicament comprises a derivative of tetrahydrobenzo[f][1,4]oxazepine—either nonsteroidal agonist of bile aids receptor TGR5, or one of endogenous bile acids which stimulate incretin hormones secretion, and also one of the known inhibitors of DPP-IV proteinase. In this case administration of TGR5 agonists is carried out peroral, and administration of endogenous bile acids is exercised rectal in the form of suppository or gel. As proteinase DPP-IV inhibitors could be used Vildagliptin, Saxagliptin, Sitagliptin, Teneligliptin, Linagliptin, Dutogliptin, Alogliptin, Gemigliptin, Carmegliptin and the like. Besides, the invention includes description of novel tetrahydrobenzo[f][1,4]oxazepine derivatives—nonsteroidal agonist of bile aids receptors TGR5, and also methods for their preparation. The invention provides enhancement of therapy effectiveness owing to synergetic action of the components, thus making possible simultaneous treatment of diabetes, and obesity, other metabolic diseases and their cardiovascular and renal complications.04-10-2014
20140148437NOVEL COMPOUNDS AS DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS - This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, genetic (Type 1, Type 5 hyperlipidemia) and acquired forms of hypertriglyceridemia or hyperlipoproteinemia-related disorders, caused by but not limited to lipodystrophy, hypothyroidism, medications (beta blockers, thiazides, estrogen, glucocorticoids, transplant) and other factors (pregnancy, alcohol intake), hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, cardiovascular outcomes, angina, excess hair growth (including syndromes associated with hirsutism), nephrotic syndrome, fibrosis such as myocardial, renal and liver fibrosis, hepatitis C virus infection and acne or other skin disorders.05-29-2014
20140179676HETEROCYCLIC NUCLEAR HORMONE RECEPTOR MODULATORS - The invention provides a compound of Formula (I)06-26-2014
20140371205SUBSTITUTED PYRIMIDINES FOR THE TREATMENT OF DISEASES SUCH AS CANCER - The present invention encompasses compounds of general formula (1)12-18-2014
20140378433PYRIMIDOOXAZOCINE DERIVATIVES AS MTOR - INHIBITORS - The invention relates to bicydic heterocyclic derivatives of general formula (I) to a process for preparing them and to the therapeutic use thereof.12-25-2014
20140378434NOVEL COMPOUNDS AS DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS - This invention relates to novel compounds which are inhibitors of acyl coenzymeA: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, hypertriglyceridemia, hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, hepatitis C virus infection and acne or other skin disorders.12-25-2014
20150038487METHODS OF TREATING HYPERTROPHIC CARDIOMYOPATHY - The present disclosure relates to a compound of formula (I) or formula (II)02-05-2015
20150307499INHIBITOR OF APOPTOSIS PROTEIN (IAP) ANTAGONISTS - Provided herein are compounds that modulate the activity of inhibitor of apoptosis proteins (IAPs), compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.10-29-2015
20150322082NOVEL COMPOUNDS AS DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS - This invention relates to novel compounds which are inhibitors of acyl coenzyme A: diacylglycerol acyltransferase 1 (DGAT-1), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy, alone or in combination with weight management therapies or other triglyceride lowering therapy for the prevention or treatment of diseases related to DGAT-1 dysfunction or where modulation of DGAT-1 activity may have therapeutic benefit including but not limited to obesity, obesity related disorders, genetic (Type 1, Type 5 hyperlipidemia) and acquired forms of hypertriglyceridemia or hyperlipoproteinemia-related disorders, caused by but not limited to lipodystrophy, hypothyroidism, medications (beta blockers, thiazides, estrogen, glucocorticoids, transplant) and other factors (pregnancy, alcohol intake), hyperlipoproteinemia, chylomicronemia, dyslipidemia, non-alcoholic steatohepatitis, diabetes, insulin resistance, metabolic syndrome, cardiovascular outcomes, angina, excess hair growth (including syndromes associated with hirsutism), nephrotic syndrome, fibrosis such as myocardial, renal and liver fibrosis, hepatitis C virus infection and acne or other skin disorders.11-12-2015
20150335657Methods for Modulating Sirtuin Enzymes - This document relates to compounds useful for modulating sirtuin enzymes. For example, the compounds provided herein are useful as broad spectrum antiviral agents. In addition, the compounds provided herein may be used in the treatment of other disorders associated with sirtuin enzymes, such as diseases related to aging and stress, blood clotting disorders, cancer, cardiovascular diseases, diabetes, inflammation, neurodegenerative diseases, and obesity.11-26-2015
20150376141NEW COMPOUNDS - The present invention encompasses compounds of general formula (1)12-31-2015
20150376166INHIBITORS OF BRUTON'S TYROSINE KINASE - This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit BTK. The compounds disclosed herein are useful to modulate the activity of BTK and treat diseases associated with excessive BTK activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.12-31-2015
20160052935COMPOUNDS FOR USE IN SCREENING METHODS FOR SPINAL MUSCULAR ATROPHY - Disclosed herein are compositions and methods for treatment of spinal muscular atrophy (SMA). In certain embodiments, compounds are provided that increase full-length survival of motor neuron (SMN) protein production by an SMN2 gene.02-25-2016
20160200736NOVEL COMPOUNDS AS DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS07-14-2016
20180022737CRYSTALLINE FORMS OF (S)-5-BENZYL-N-(5-METHYL-4-OXO-2,3,4,5-TETRAHYDROBENZO[b][1,4]OXAZEPIN-3-- YL)-4H-1,2,4-TRIAZOLE-3-CARBOXAMIDE01-25-2018
514211060 Ring chalcogen and ring nitrogen are in the 1,5-positions of the seven-membered hetero ring 43
20080227770Benzoxazepine Compound - A compound represented by the formula [1]:09-18-2008
20080261949CYCLOHEXYL(ALKYL)PROPANOLAMINES, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME - The present invention relates to the compounds of formula (I):10-23-2008
20090042858LACTAM CONTAINING HCV INHIBITORS - The present invention discloses novel methods and compositions for viral inhibition, particularly inhibition of HCV and SARS. The invention also provides compositions including novel oxoazepanylacetamide derivatives useful for viral inhibition.02-12-2009
20090093457XANTHINE DERIVATIVES, THE PREPARATION THEREOF AND THEIR USE AS PHARMACEUTICAL COMPOSITIONS - Disclosed are substituted xanthines of general formula04-09-2009
200901565783-Heterocyclylacrylamide Compounds as Fab I Inhibitors and Antibacterial Agents - In part, the present invention is directed towards compounds with FabI inhibiting properties. Such compounds may also inhibit other enzymes, including those similar to FabI either structurally or functionally, for example, Fab K. Kits and compositions that include the disclosed compounds are also provided. Methods of treating a subject with a bacterial illness is also disclosed.06-18-2009
20090239839RECEPTOR ANTAGONIST - An agent for modulating the function of an RFRP receptor, characterized by containing either a compound represented by the formula (I)09-24-2009
20100130470ACRYLAMIDE DERIVATIVES AS FAB I INHIBITORS - In part, the present invention is directed to antibacterial compounds.05-27-2010
20100137282TRICYCLIC NITROGEN CONTAINING COMPOUNDS AS ANTIBACTERIAL AGENTS - Tricyclic nitrogen containing compounds and their use as antibacterials. Z06-03-2010
201100539102 -HETEROCYCLYLOXYBENZOYL AMINO HETEROCYCLYL COMPOUNDS AS MODULATORS OF GLUCOKINASE FOR THE TREATMENT OF TYPE 2 DIABETES - Compounds of formula (I)03-03-2011
20110086842Pyrimidines as PLK inhibitors - The present invention encompasses compounds of general formula (1),04-14-2011
20110112067Inhibitors of the Human Aldosterone Sythase CYP11B2 - The invention provides compounds of the general formula (I)05-12-2011
20110118232PYRIMIDINE COMPOUNDS AND USE THEREOF - The invention relates to novel pyrimidine compounds of general formula (I), in which: A represents a group C═W or CR05-19-2011
20130237523ACRYLAMIDE DERIVATIVES AS FAB I INHIBITORS - In part, the present invention is directed to antibacterial compounds.09-12-2013
20150038488SYK INHIBITORS - The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I02-05-2015
20150038489COMPOUND AND METHODS FOR TREATING LONG QT SYNDROME - Described herein is a method of treating long QT syndrome by administration of an effective amount of a potent and selective late sodium ion channel blocker02-05-2015
20150290213Composition For Prevention of Vasoactivity in the Treatment of Blood Loss and Anemia - The present invention relates to the prevention of cardiovascular and central nervous system side effects in mammals who receive transfusions of hemoglobin based oxygen carriers (HBOC) or stored blood products containing a concentration of hemoglobin sufficient to induce vasoconstriction, by adding a vasoactivity reducing effective amount of one or more phosphodiesterase inhibitors in combination with a calcium channel blocker and/or an alpha agonist, to the circulation, or alternatively to the HBOC or stored blood, thereby preventing the manifestation of vasoactivity attributable to the presence of free tetrameric hemoglobin (Hb).10-15-2015
20150353533HETEROCYCLIC AMIDES AS KINASE INHIBITORS - Disclosed are compounds having the formula:12-10-2015
514211070 Nitrogen attached directly or indirectly to the ring nitrogen of the seven-membered hetero ring by acyclic nonionic bonding (e.g., Diltiazem, etc.) 26
20090012057Cardiovascular Compounds Comprising Nitric Oxide Enhancing Groups, Compositions and Methods of Use - The invention describes compositions and kits comprising at least one cardiovascular compound comprising at least one nitric oxide enhancing group, or pharmaceutically acceptable salts thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; Q) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia. The cardiovascular compounds are angiotensin II antagonists, aldosterone antagonists, endothelin antagonists, hydralazine compounds, neutral endopeptidase inhibitors and renin inhibitors. The nitric oxide enhancing groups are nitroxides and/or heterocyclic nitric oxide donors.01-08-2009
20090075971DERIVATIVES OF 2-ALKOXY-3,4,5-TRIHYDROXY-ALKYL AMIDES, PREPARATION AND USE THEREOF, AND COMPOSITIONS CONTAINING THE SAME - The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide derivatives, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds, and to intermediate precursors to such compounds.03-19-2009
20090093458METHODS OF IDENTIFYING ANTI-CANCER AGENTS AND USES THEREOF - The present invention provides methods of identifying and/or detecting anti-cancer agents. The present invention provides methods of identifying and/or detecting compounds that can activate PARP and/or induce necrosis. The present invention also provides for methods of treating cancer in an individual. The present invention also provides kits for identifying and/or detecting anti-cancer agents.04-09-2009
200900934592-ALKOXY-3,4,5-TRIHYDROXYALKYLAMIDE-BENZOTHIAZEPINES PREPARATION THEREOF, COMPOSITIONS CONTAINING THEM AND USE THEREOF - The present invention relates to 2-alkoxy-3,4,5-trihydroxyalkylamide benzothiazepine compounds, to pharmaceutical compositions comprising such compounds, to methods of treatment comprising administering such compounds, to processes for the preparation of such compounds and to intermediate precursors to such compounds.04-09-2009
20090118256CHRONOTHERAPEUTIC DILTIAZEM FORMULATIONS AND THE ADMINISTRATION THEREOF - A method of treating or preventing myocardial ischemia in a patient in need thereof comprising administration of a controlled-release Galenical preparation of pharmaceutically acceptable Diltiazem including the pharmaceutically acceptable salts thereof, suitable for evening dosing every 24 hours containing from about 180 mg to about 420 mg of the form of Diltiazem associated with excipients to provide controlled (sustained) release of the form of Diltiazem for providing a Cmax of diltiazem in the blood at between about 10 hours and about 17 hours after administration, the preparation comprising the form of Diltiazem in oral sustained-release dosage form in which the Diltiazem is adapted to be released after administration over a prolonged period of time and exhibits when given to humans (i) a higher bioavailability when given at night compared to when given in the morning without food according to FDA guidelines or criteria and (ii) bioequivalence when given in the morning with and without food according to the same FDA guidelines or criteria.05-07-2009
20090221549ANTIHYPERTENSIVE THERAPY - A new use of darusentan is provided in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy with one or more drugs. The composition comprises darusentan in an amount providing a therapeutically effective daily dose; wherein (a) the composition is orally deliverable and/or (b) the daily dose of darusentan is effective to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures. Further provided is a new use of darusentan in preparation of a pharmaceutical composition for lowering blood pressure in a patient exhibiting resistance to a baseline antihypertensive therapy, wherein the composition is administered adjunctively with at least one diuretic and at least one antihypertensive drug selected from ACE inhibitors, angiotensin II receptor blockers, beta-adrenergic receptor blockers and calcium channel blockers.09-03-2009
20090275559Chronotherapeutic formulations of modified-release calcium channel blocker anti-hypertensive drugs in combination with other anti-hypertensive drugs for 24-hour optimal treatment of hypertension, nocturnal hypertension, and/or hypertension with angina - The present invention relates to formulations of anti-hypertensive drugs. The present invention includes a modified-release formulation of diltiazem hydrochloride that is suitable for once-daily use and which provides delivery of drug either in the early morning hours, or overnight, so as to blunt the natural rise in blood pressure (BP) and heart rate (HR) in the morning and to reduce the slope of the increase in BP in patients with elevated BP (hypertension).11-05-2009
20090318413BRONCHIAL SMOOTH MUSCLE REMODELING INVOLVES CALCIUM-DEPENDENT ENHANCED MITOCHONDRIAL BIOGENESIS IN ASTHMA - The present invention thus provides a method of inhibiting bronchial smooth muscle remodeling in asthma, comprising the step of administering to a subject having asthma an agent that inhibits calcium-dependent mitochondrial biogenesis.12-24-2009
20100130471Renin Inhibitors - Described are compounds which bind to aspartic proteases to inhibit their activity. They are useful in the treatment or amelioration of diseases associated with aspartic protease activity. Also described are methods of use of the compounds described herein in ameliorating or treating aspartic protease related disorders in a subject in need thereof.05-27-2010
20100152161COMPOSITIONS FOR WEIGHT MANAGEMENT - Methods and compositions for preventing or reducing weight gain associated with drug treatment, which utilize an H06-17-2010
20100204202DRUG FOR ALLEVIATING MOTOR COMPLICATIONS OR PSYCHIATRIC SYMPTOMS OF PARKINSON'S DISEASE - A drug containing a compound having the formula (I):08-12-2010
20100324019Use of Riboflavin in the Treatment of Hypertension - The invention provides the use of riboflavin in the manufacture of a medicament for the treatment or prophylaxis of elevated blood pressure in a subject homozygous or heterozygous for the MTHFR C677T polymorphism. The invention also provides a pharmaceutical product for the treatment or prophylaxis of elevated blood pressure in a subject homozygous or heterozygous for the MTHFR C677T polymorphism, comprising a pharmaceutically effective amount of an anti-hypertensive agent and riboflavin, and the invention further provides a method of treatment of such a subject comprising the administration of riboflavin.12-23-2010
20110098273Oligomer-Calcium Channel Blocker Conjugates - The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water soluble oligomer.04-28-2011
20110144087SHORT ACTING BENZOTHIAZEPINE CALCIUM CHANNEL BLOCKERS AND USES THEREOF - The present invention relates to short-acting calcium channel blocking compounds and their use to treat ischemic heart conditions, cardiac arrhythmias, hypertensive crisis in an emergency room setting, hypertension in general, hypertension been.) fore, during, or after surgery, no-reflow phenomenon following reperfusion, and diseases associated with decreased skeletal muscle blood flow. The invention also relates to pharmaceutical compositions formulated for use in such methods and to kits for such methods.06-16-2011
20110263568TOPICAL PHARMACEUTICAL COMPOSITION COMPRISING A CHOLINERGIC AGENT OR A CALCIUM CHANNEL BLOCKER - A method and composition are provided for the treatment of an anorectal disorder and for controlling the pain associated therewith. The method comprises administering to a subject in need of such treatment therapeutically effective amounts of a calcium channel blocker either alone or together with a nitric oxide donor. Amlodipine, anipamil, barnidipine, benidipine, bepridil, darodipine, diltiazem, efonidipine, felodipine, isradipine, lacidipine, lercanidipine, lidoflazine, manidipine, mepirodipine, nicardipine, nifedipine, niludipine, nilvadipine, nimodipine, nisoldipine, nitrendipine, perhexiline, tiapamil, verapamil and pharmaceutically acceptable salts thereof, are suitable calcium channel blockers.10-27-2011
20110319382COMPOSITIONS COMPRISING A CALCIUM CHANNEL BLOCKER OR A CALMODULIN BLOCKER FOR USE IN THE REMOVAL OF HYPERPLASTIC SKIN LESIONS - A composition, use of and a method of removing a hyperplastic skin lesion on a mammal comprising administering to the lesion or locus thereof a therapeutically effective amount of a composition comprising a blocker selected from the group consisting of a calcium channel blocker, a metabolite thereof, a calmodulin blocker and a metabolite thereof and a pharmaceutically acceptable diluent or carrier.12-29-2011
20120122845METHOD FOR THE PRODUCTION OF BIOADHESIVE COMPACT MATRICES - A method for the preparation of a bioadhesive compact matrix, which comprises the preparation of a uniform mixture of powders comprising one alkylcellulose or one hydroxy alkylcellulose and a non-water-soluble, water-swellable cross-linked polycarboxylic polymer; the preparation of compressed units starting from such powder mixture by direct compression and finally the heating of the compressed units thus obtained to a temperature in the range of 80-250° C. for a time of 1-60 minutes; the powder mixture can also comprise at least one active substance and the compressed units thus obtained are characterized by a prolonged release, and have a release kinetics of the active substance substantially of zero order in an aqueous solution at pH 4-8.05-17-2012
20120245145METHOD AND COMPOSITIONS FOR TREATMENT AND PREVENTION OF BROAD SPECTRUM VIRUS AILMENTS COMPRISING A CALCIUM CHANNEL BLOCKER OR A CALMODULIN BLOCKER - In the broadest aspect, the invention provides a composition for and a method of prophylactic and/or therapeutic treatment of a animal/mammal for any viral disease, mixed bacterial and viral infections, bacterial infections, bacterial endotoxins, bacterial exotoxins, autoimmune diseases, and cellular or humoral mediated allergic conditions that is caused by any virus that relies on the maintenance of specific calcium ion concentrations for the post ribosomal RNA synthesis processing of viral protein translation, transportation and processing of viral structural components by utilizing a therapeutic amount of a blocker selected from the group consisting of a calcium channel blocker, a metabolite thereof, a calmodulin blocker and a metabolite thereof, and a pharmaceutical acceptable diluent or carrier; and/or is caused by damage to the animal/mammal by a pathological immune response to antigens.09-27-2012
20130079332TOPICAL PHARMACEUTICAL COMPOSITION COMPRISING A CHOLINERGIC AGENT OR A CALCIUM CHANNEL BLOCKER - A method and composition are provided for the treatment of an anorectal disorder and for controlling the pain associated therewith. The method comprises administering to a subject in need of such treatment therapeutically effective amounts of a calcium channel blocker either alone or together with a nitric oxide donor. Amlodipine, anipamil, barnidipine, benidipine, bepridil, darodipine, diltiazem, efonidipine, felodipine, isradipine, lacidipine, lercanidipine, lidoflazine, manidipine, mepirodipine, nicardipine, nifedipine, niludipine, nilvadipine, nimodipine, nisoldipine, nitrendipine, perhexiline, tiapamil, verapamil and pharmaceutically acceptable salts thereof, are suitable calcium channel blockers.03-28-2013
20130178463ENHANCED TRANSBUCCAL DRUG DELIVERY SYSTEM AND COMPOSITIONS - A buccal delivery system is disclosed suitable for delivery of a therapeutic agent to the oral cavity of a patient. The delivery system comprises a matrix for containing and releasing the therapeutic agent into the oral cavity and an alkyl N,N-disubstituted amino acetate in said matrix. A particularly preferred delivery system comprises a matrix containing an effective amount of therapeutic agent together with an alkyl N,N-disubstituted amino acetate, such as dodecyl 2-(N,N-dimethylamino) propionate salt.07-11-2013
20130274245Composition For Prevention of Vasoactivity in the Treatment of Blood Loss and Anemia - The present invention relates to the prevention of cardiovascular and central nervous system side effects in mammals who receive transfusions of hemoglobin based oxygen carriers (HBOC) or stored blood products containing a concentration of hemoglobin sufficient to induce vasoconstriction, by adding a vasoactivity reducing effective amount of one or more phosphodiesterase inhibitors in combination with a calcium channel blocker and/or an alpha agonist, to the circulation, or alternatively to the HBOC or stored blood, thereby preventing the manifestation of vasoactivity attributable to the presence of free tetrameric hemoglobin (Hb).10-17-2013
20130338143Compositions for Transdermal Delivery of Active Agents - Disclosed herein are compositions that are useful in effecting the transdermal delivery of therapeutic agents. More particularly, the disclosed transdermal compositions may include a fatty alcohol (for example, octanol), a terpene (for example, limonene), and an active agent comprising an amine moiety.12-19-2013
20140148438NITRIC OXIDE RELEASING AMINO ACID ESTER FOR TREATMENT OF PULMONARY HYPERTENSION AND OTHER RESPIRATORY CONDITIONS - There is provided compositions and methods for the treatment of respiratory conditions such as pulmonary hypertension and sickle-cell disease in a patient in need thereof. The composition and method are for treating a patient in need thereof by inhalation of a composition containing amino acid ester compounds comprising at least one nitric oxide releasing group and pharmaceutical salts thereof.05-29-2014
20140378435Inhibition of Filovirus Entry Into Cells and Uses Thereof - The present invention discloses method to treat infections caused by filovirus. Such a method comprises blocking the PI3 kinase pathway or the calcium-associated pathway at the gene or protein level. Also disclosed herein are the compounds useful in the treatment of filoviral infection.12-25-2014
20150141404NON-IONIC VESICLE FORMULATIONS OF CALCIUM CHANNEL BLOCKERS - Disclosed are non-ionic surfactant vesicle formulations of calcium channel blockers, such as diltiazem, and methods of using the formulations for treating anal disorders.05-21-2015
20150361059SUBSTITUTED HETERO-AZEPINONES - There are provided compounds of the formula12-17-2015
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